"Operation Blackjack" Dismantles Drug Pipeline from New York City to Central NY
12 Pounds of Cocaine, 4 Guns, $26k Cash, 1 Pound of Marijuana,
Drug Paraphernalia, Ammunition and 2 Cars Seized
New York Drug Enforcement Administration Special Agent-In-Charge John P. Gilbride and Attorney General Andrew M. Cuomo announced today the indictment of 15 individuals involved in an alleged narcotics distribution ring where cocaine was transported from the Bronx and sold throughout the Central New York region.
The case involved the seizure of 12 pounds of cocaine worth $500,000, two revolvers, two shotguns, $26,000 in cash, drug paraphernalia, ammunition, and two vehicles.
DEA Special Agent-In-Charge John P. Gilbride said, “DEA and our state and local law enforcement partners are committed to identifying and arresting those responsible for distributing illegal narcotics. The Lockhart duo led this cocaine and crack cocaine distributing organization which led to their arrests and the dismantling of those who worked for them. Syracuse and our surrounding counties in Central New York can be assured that due to these arrests there are less drugs and guns on the streets, making our community safer from the perils of drug abuse.”
Today’s indictment is the result of a multi-agency investigation led by the Attorney General’s Organized Crime Task Force (OCTF) known as “Operation Blackjack.” The allegations included two main players of the drug ring who bought cocaine from suppliers in the Bronx and transported the drugs via car to Central New York to sell to mid-level dealers for distribution in Onondaga, Oswego, Oneida, and Madison counties.
One of the key players in the alleged distribution network, Antwan Lockhart, of N. Jay Street, Rome, was arrested December 23, 2007 when his car was stopped on Route 81 in Tully as he was transporting cocaine from the Bronx. At the scene, 4.5 pounds of cocaine were seized. An additional 2 pounds were taken from Lockhart’s stash house on Midler Ave, Syracuse, and .67 ounces of cocaine were found in another vehicle registered in Lockhart’s name. Lockhart pleaded guilty to criminal possession of a controlled substance in the third degree, for which he received a nine year prison sentence, three year post-release supervision, and forfeited two cars.
The other alleged key leader in the drug distribution network is Edward N. Lockhart, 30, of Caughdenoy Road, Hastings (last known address). As part of the investigation, law enforcement seized 5 ounces of cocaine and a shotgun from Edward Lockhart. He was charged with 20 counts criminal possession and sale of a controlled substance, including six counts of criminal sale of a controlled substance in the second degree (class A-II felony), which carries a maximum penalty of 10 years in prison and lifetime probation for each sales count.
Of the 15 indicted, 14 were charged with conspiracy in the second degree, a class B felony that carries the maximum penalty of 25 years in prison. Additionally, Marton Davis and Kamisha Rashad were each charged with criminal sale of a controlled substance in the second degree, and face the maximum penalty of 10 years in prison. Luis Abreu was charged with criminal possession of a controlled substance in the third degree and Sirena Sharpe was charged with criminal sale of controlled substance in the third degree. Both face the maximum penalty of 9 years in prison. Osbie McClain and Titus Stewart were charged with varying levels of narcotics and weapons related offenses and both face maximum sentences of 12 years in prison.
Onondaga District Attorney William J. Fitzpatrick said, “These arrests send a clear message that those of us who live and work in Central New York will not tolerate drug dealers and narcotics trafficking in our community. We are very appreciative of Attorney General Cuomo’s commitment to helping us rid Syracuse and Onondaga County of those who infuse poison and violence into our community. His office has worked diligently and combined forces with my office and our local enforcement to deliver a crippling blow to the illegal drug market. That kind of cooperative effort and his Upstate Guns, Gangs and Drugs Initiative has made Attorney General Cuomo one of the most effective and respected leaders in our state. I believe the success of Operation ‘Blackjack’ is evident of that.”
Onondaga County Sheriff Kevin E. Walsh said, “Today’s multi-agency sweep has been a resounding success, thanks to a coordinated effort headed up by Attorney General Cuomo’s OCTF. The Sheriff’s office welcomes this collaborative effort, and it is initiatives like the Attorney General’s Upstate Guns, Gangs and Drugs Initiative that will go a long way toward making our County and region safer. The narcotics trade throughout New York has run rampant for too long, and it’s a welcome sign that Attorney General Cuomo continues to make curbing it a priority.”
City of Syracuse Mayor Matthew J. Driscoll said, “Thanks to the hard work of various law enforcement agencies under the leadership of Attorney General Cuomo’s Organized Crime Task Force, another network of deadly narcotics in Central New York has been cut off. The scourge of drug trafficking from the New York City region to upstate communities continues to pose a threat to our neighborhoods and our children. However, it is a threat that we are eliminating by working together and pooling our resources.”
New York State Police Superintendent Harry J. Corbitt said, “Drug trafficking operations originating in New York City have expanded into our upstate communities. However, New York law enforcement agencies on every level, led by Attorney General Cuomo’s Upstate Guns, Gangs and Drugs Initiative, have impacted these operations. Through an organized effort, we worked together to bring down these highly organized drug rings. The state police are committed to working with the Attorney General and other law enforcement colleagues to improve the quality of life in our communities.”
“The impact of illegal drugs and guns on our communities is extensive and widespread,” said Attorney General Cuomo. “It is the goal of my Upstate Guns, Gangs, and Drugs Initiative to intercept the flow of drugs before they infect our neighborhoods. The recent takedown of several drug rings throughout Central and Upstate New York in past months proves that our formula of partnering with federal, state, and local law enforcement agencies is a successful model.”
Those indicted and their alleged roles include:
Luis Abreu, 33, of E. Spruce Ct., Altoona, PA, bought cocaine from A. Lockhart to resell (.6 ounces of cocaine seized at his residence).
Ralston Avery, 29, of E. 40th Street, Brooklyn, supplied cocaine to A. Lockhart, Feaggins and others.
Katy Campbell, a/k/a “Kate,” 20, of Pleasant Street, Canastota, sold cocaine she received from E. Lockhart and drove with E. Lockhart to the Bronx.
Faniel Denis, 28, of State Street, Canastota, bought cocaine from A. Lockhart and Stewart to resell.
Harmon Feaggins, 22, of Hoe Avenue, Bronx, transported cocaine to from the Bronx to Syracuse for A. Lockhart and sold cocaine he received from Avery.
Ronnie Golden, 28, of James Street, Syracuse, sold cocaine and allowed others indicted to store and sell cocaine at his residence.
Marton Davis, 29, of Presidential Plaza, Syracuse, sold cocaine to E. Lockhart, Golden, Poole, and Rashad for resale.
Edward N. Lockhart, Jr., 30, sold cocaine he received from A. Lockhart, Wade, Davis and others to Poole, Sarakby and others; drove to the Bronx (cocaine and shotgun seized during investigation).
Osbie McClain, 24, of Lillian Avenue, Syracuse, bought cocaine from A. Lockhart to resell (3.2 ounces of cocaine and a shotgun seized at residence).
Taurean Poole, 23, of Cairns Trail, Clay, bought cocaine from E. Lockhart and Davis to resell.
Kamisha Rashad, 22, of Presidential Plaza, Syracuse, sold cocaine she received from Davis and accompanied A. Lockhart when he drove to the Bronx.
Adib Sarakby, 53, of Gaskin Road, Baldwinsville, bought cocaine from E. Lockhart to resell.
Sirena Sharpe, 17, of Avery Avenue, Syracuse, sold cocaine for E. Lockhart.
Titus Stewart, 36, of Kirkpatrick Street, Syracuse, sold cocaine to Denis and others (2.5 ounces of cocaine and a revolver seized at his residence).
Robert Wade, 20, of Hoe Avenue, Bronx, bought and sold cocaine to E. Lockhart, A. Lockhart and others for resale.
The charges against the defendants are merely accusations and the defendants are presumed innocent until and unless proven guilty. Read More......
Drug Paraphernalia, Ammunition and 2 Cars Seized
New York Drug Enforcement Administration Special Agent-In-Charge John P. Gilbride and Attorney General Andrew M. Cuomo announced today the indictment of 15 individuals involved in an alleged narcotics distribution ring where cocaine was transported from the Bronx and sold throughout the Central New York region.
The case involved the seizure of 12 pounds of cocaine worth $500,000, two revolvers, two shotguns, $26,000 in cash, drug paraphernalia, ammunition, and two vehicles.
DEA Special Agent-In-Charge John P. Gilbride said, “DEA and our state and local law enforcement partners are committed to identifying and arresting those responsible for distributing illegal narcotics. The Lockhart duo led this cocaine and crack cocaine distributing organization which led to their arrests and the dismantling of those who worked for them. Syracuse and our surrounding counties in Central New York can be assured that due to these arrests there are less drugs and guns on the streets, making our community safer from the perils of drug abuse.”
Today’s indictment is the result of a multi-agency investigation led by the Attorney General’s Organized Crime Task Force (OCTF) known as “Operation Blackjack.” The allegations included two main players of the drug ring who bought cocaine from suppliers in the Bronx and transported the drugs via car to Central New York to sell to mid-level dealers for distribution in Onondaga, Oswego, Oneida, and Madison counties.
One of the key players in the alleged distribution network, Antwan Lockhart, of N. Jay Street, Rome, was arrested December 23, 2007 when his car was stopped on Route 81 in Tully as he was transporting cocaine from the Bronx. At the scene, 4.5 pounds of cocaine were seized. An additional 2 pounds were taken from Lockhart’s stash house on Midler Ave, Syracuse, and .67 ounces of cocaine were found in another vehicle registered in Lockhart’s name. Lockhart pleaded guilty to criminal possession of a controlled substance in the third degree, for which he received a nine year prison sentence, three year post-release supervision, and forfeited two cars.
The other alleged key leader in the drug distribution network is Edward N. Lockhart, 30, of Caughdenoy Road, Hastings (last known address). As part of the investigation, law enforcement seized 5 ounces of cocaine and a shotgun from Edward Lockhart. He was charged with 20 counts criminal possession and sale of a controlled substance, including six counts of criminal sale of a controlled substance in the second degree (class A-II felony), which carries a maximum penalty of 10 years in prison and lifetime probation for each sales count.
Of the 15 indicted, 14 were charged with conspiracy in the second degree, a class B felony that carries the maximum penalty of 25 years in prison. Additionally, Marton Davis and Kamisha Rashad were each charged with criminal sale of a controlled substance in the second degree, and face the maximum penalty of 10 years in prison. Luis Abreu was charged with criminal possession of a controlled substance in the third degree and Sirena Sharpe was charged with criminal sale of controlled substance in the third degree. Both face the maximum penalty of 9 years in prison. Osbie McClain and Titus Stewart were charged with varying levels of narcotics and weapons related offenses and both face maximum sentences of 12 years in prison.
Onondaga District Attorney William J. Fitzpatrick said, “These arrests send a clear message that those of us who live and work in Central New York will not tolerate drug dealers and narcotics trafficking in our community. We are very appreciative of Attorney General Cuomo’s commitment to helping us rid Syracuse and Onondaga County of those who infuse poison and violence into our community. His office has worked diligently and combined forces with my office and our local enforcement to deliver a crippling blow to the illegal drug market. That kind of cooperative effort and his Upstate Guns, Gangs and Drugs Initiative has made Attorney General Cuomo one of the most effective and respected leaders in our state. I believe the success of Operation ‘Blackjack’ is evident of that.”
Onondaga County Sheriff Kevin E. Walsh said, “Today’s multi-agency sweep has been a resounding success, thanks to a coordinated effort headed up by Attorney General Cuomo’s OCTF. The Sheriff’s office welcomes this collaborative effort, and it is initiatives like the Attorney General’s Upstate Guns, Gangs and Drugs Initiative that will go a long way toward making our County and region safer. The narcotics trade throughout New York has run rampant for too long, and it’s a welcome sign that Attorney General Cuomo continues to make curbing it a priority.”
City of Syracuse Mayor Matthew J. Driscoll said, “Thanks to the hard work of various law enforcement agencies under the leadership of Attorney General Cuomo’s Organized Crime Task Force, another network of deadly narcotics in Central New York has been cut off. The scourge of drug trafficking from the New York City region to upstate communities continues to pose a threat to our neighborhoods and our children. However, it is a threat that we are eliminating by working together and pooling our resources.”
New York State Police Superintendent Harry J. Corbitt said, “Drug trafficking operations originating in New York City have expanded into our upstate communities. However, New York law enforcement agencies on every level, led by Attorney General Cuomo’s Upstate Guns, Gangs and Drugs Initiative, have impacted these operations. Through an organized effort, we worked together to bring down these highly organized drug rings. The state police are committed to working with the Attorney General and other law enforcement colleagues to improve the quality of life in our communities.”
“The impact of illegal drugs and guns on our communities is extensive and widespread,” said Attorney General Cuomo. “It is the goal of my Upstate Guns, Gangs, and Drugs Initiative to intercept the flow of drugs before they infect our neighborhoods. The recent takedown of several drug rings throughout Central and Upstate New York in past months proves that our formula of partnering with federal, state, and local law enforcement agencies is a successful model.”
Those indicted and their alleged roles include:
Luis Abreu, 33, of E. Spruce Ct., Altoona, PA, bought cocaine from A. Lockhart to resell (.6 ounces of cocaine seized at his residence).
Ralston Avery, 29, of E. 40th Street, Brooklyn, supplied cocaine to A. Lockhart, Feaggins and others.
Katy Campbell, a/k/a “Kate,” 20, of Pleasant Street, Canastota, sold cocaine she received from E. Lockhart and drove with E. Lockhart to the Bronx.
Faniel Denis, 28, of State Street, Canastota, bought cocaine from A. Lockhart and Stewart to resell.
Harmon Feaggins, 22, of Hoe Avenue, Bronx, transported cocaine to from the Bronx to Syracuse for A. Lockhart and sold cocaine he received from Avery.
Ronnie Golden, 28, of James Street, Syracuse, sold cocaine and allowed others indicted to store and sell cocaine at his residence.
Marton Davis, 29, of Presidential Plaza, Syracuse, sold cocaine to E. Lockhart, Golden, Poole, and Rashad for resale.
Edward N. Lockhart, Jr., 30, sold cocaine he received from A. Lockhart, Wade, Davis and others to Poole, Sarakby and others; drove to the Bronx (cocaine and shotgun seized during investigation).
Osbie McClain, 24, of Lillian Avenue, Syracuse, bought cocaine from A. Lockhart to resell (3.2 ounces of cocaine and a shotgun seized at residence).
Taurean Poole, 23, of Cairns Trail, Clay, bought cocaine from E. Lockhart and Davis to resell.
Kamisha Rashad, 22, of Presidential Plaza, Syracuse, sold cocaine she received from Davis and accompanied A. Lockhart when he drove to the Bronx.
Adib Sarakby, 53, of Gaskin Road, Baldwinsville, bought cocaine from E. Lockhart to resell.
Sirena Sharpe, 17, of Avery Avenue, Syracuse, sold cocaine for E. Lockhart.
Titus Stewart, 36, of Kirkpatrick Street, Syracuse, sold cocaine to Denis and others (2.5 ounces of cocaine and a revolver seized at his residence).
Robert Wade, 20, of Hoe Avenue, Bronx, bought and sold cocaine to E. Lockhart, A. Lockhart and others for resale.
The charges against the defendants are merely accusations and the defendants are presumed innocent until and unless proven guilty. Read More......
Modesto Football Coach Indicted for Cocaine Trafficking
Federal Grand Jury indicts Armando Perez and three others connected in the investigation
SACRAMENTO, Calif.—United States Attorney McGregor W. Scott and Drug Enforcement Administration (DEA) Special Agent in Charge Javier F. Peña, announced today that ARMANDO VASQUEZ PEREZ, 28, of Modesto, California, and three others, were indicted today of five counts of conspiracy to distribute cocaine and distribution of cocaine. The five counts allege that PEREZ, a youth sports coach, was the cocaine supplier for a conspiracy that began in July 2007 and ended with his arrest on June 13, 2008. This case is the product of an extensive investigation by the Drug Enforcement Administration.
According to Assistant United States Attorney Jason Hitt, who is prosecuting the case, PEREZ was indicted along with JAIME FLORES, 25, NARCISCO MARTINEZ, 27, and GUADALUPE GUTIERREZ, 33, all of Modesto. According to the court documents, MARTINEZ sold large quantities of powder cocaine to a DEA undercover agent in September 2007 and May 2008. During the investigation, agents discovered that MARTINEZ was in frequent telephone contact with PEREZ before and after the cocaine deals. Law enforcement suspected PEREZ was supplying cocaine to MARTINEZ through his cousin FLORES. Subsequent investigation confirmed that suspicion. Specifically, on May 9, 2008, during an undercover drug transaction with MARTINEZ, agents watched and videotaped MARTINEZ meet with PEREZ and FLORES, at Los Compadres Auto Sales. According to the criminal complaint filed in the case, this meeting was consistent with MARTINEZ returning to his drug supplier, PEREZ, and providing him with some of the proceeds from the drug sale.
The investigation culminated on June 12, 2008, when the undercover agent arranged to purchase 2½ kilograms of cocaine from MARTINEZ in Modesto. After a series of recorded calls, MARTINEZ arrived at a Rite Aid parking lot in Salida, at which time MARTINEZ was arrested. At the time of his arrest, law enforcement discovered that MARTINEZ was in possession of approximately two kilograms of cocaine. Agents seized approximately one pound of cocaine from MARTINEZ’s residence at 904 Countryside Lane, Modesto. After being placed under arrest, MARTINEZ admitted that his cocaine supplier in July 2007 was PEREZ and FLORES. Agents served a federal search warrant at 1010 Sylvan Meadows Drive, Modesto, a residence MARTINEZ had been earlier that day. From the location, law enforcement seized approximately one kilogram cocaine and arrested FLORES. Agents also discovered a “kilo press,” a device commonly used by drug traffickers to add adulterant to existing bricks of cocaine and then press the adulterated kilogram of cocaine back into the form of a kilogram brick. The street value of the seized cocaine is approximately $60,000.
The defendants are scheduled to be arraigned on the indictment by Judge Kimberly J. Mueller at 2:00 p.m., on June 27, 2008. The maximum statutory penalty for conspiracy to distribute and possession with intent to distribute at least 500 grams of cocaine is 40 years in prison. The maximum statutory penalty for distribution of cocaine is 20 years in prison. In this case, each defendant faces a mandatory minimum of five years in prison on Counts 1 and 5 of the indictment based upon the amount cocaine alleged in those counts. The actual sentence, however, will be determined at the discretion of the court after consideration of the Federal Sentencing Guidelines, which take into account a number of variables and any applicable statutory sentencing factors. The charges are only allegations and the defendants are presumed innocent until and unless proven guilty beyond a reasonable doubt. Read More......
SACRAMENTO, Calif.—United States Attorney McGregor W. Scott and Drug Enforcement Administration (DEA) Special Agent in Charge Javier F. Peña, announced today that ARMANDO VASQUEZ PEREZ, 28, of Modesto, California, and three others, were indicted today of five counts of conspiracy to distribute cocaine and distribution of cocaine. The five counts allege that PEREZ, a youth sports coach, was the cocaine supplier for a conspiracy that began in July 2007 and ended with his arrest on June 13, 2008. This case is the product of an extensive investigation by the Drug Enforcement Administration.
According to Assistant United States Attorney Jason Hitt, who is prosecuting the case, PEREZ was indicted along with JAIME FLORES, 25, NARCISCO MARTINEZ, 27, and GUADALUPE GUTIERREZ, 33, all of Modesto. According to the court documents, MARTINEZ sold large quantities of powder cocaine to a DEA undercover agent in September 2007 and May 2008. During the investigation, agents discovered that MARTINEZ was in frequent telephone contact with PEREZ before and after the cocaine deals. Law enforcement suspected PEREZ was supplying cocaine to MARTINEZ through his cousin FLORES. Subsequent investigation confirmed that suspicion. Specifically, on May 9, 2008, during an undercover drug transaction with MARTINEZ, agents watched and videotaped MARTINEZ meet with PEREZ and FLORES, at Los Compadres Auto Sales. According to the criminal complaint filed in the case, this meeting was consistent with MARTINEZ returning to his drug supplier, PEREZ, and providing him with some of the proceeds from the drug sale.
The investigation culminated on June 12, 2008, when the undercover agent arranged to purchase 2½ kilograms of cocaine from MARTINEZ in Modesto. After a series of recorded calls, MARTINEZ arrived at a Rite Aid parking lot in Salida, at which time MARTINEZ was arrested. At the time of his arrest, law enforcement discovered that MARTINEZ was in possession of approximately two kilograms of cocaine. Agents seized approximately one pound of cocaine from MARTINEZ’s residence at 904 Countryside Lane, Modesto. After being placed under arrest, MARTINEZ admitted that his cocaine supplier in July 2007 was PEREZ and FLORES. Agents served a federal search warrant at 1010 Sylvan Meadows Drive, Modesto, a residence MARTINEZ had been earlier that day. From the location, law enforcement seized approximately one kilogram cocaine and arrested FLORES. Agents also discovered a “kilo press,” a device commonly used by drug traffickers to add adulterant to existing bricks of cocaine and then press the adulterated kilogram of cocaine back into the form of a kilogram brick. The street value of the seized cocaine is approximately $60,000.
The defendants are scheduled to be arraigned on the indictment by Judge Kimberly J. Mueller at 2:00 p.m., on June 27, 2008. The maximum statutory penalty for conspiracy to distribute and possession with intent to distribute at least 500 grams of cocaine is 40 years in prison. The maximum statutory penalty for distribution of cocaine is 20 years in prison. In this case, each defendant faces a mandatory minimum of five years in prison on Counts 1 and 5 of the indictment based upon the amount cocaine alleged in those counts. The actual sentence, however, will be determined at the discretion of the court after consideration of the Federal Sentencing Guidelines, which take into account a number of variables and any applicable statutory sentencing factors. The charges are only allegations and the defendants are presumed innocent until and unless proven guilty beyond a reasonable doubt. Read More......
CRACK COCAINE A once-in-a-lifetime experience?
HOW TO QUIT COCAINE
The high from crack cocaine is intensely rewarding. But the experience is short-lived. Such immense well-being is unsustainable because its mechanisms don't subvert the systems of homeostatic feedback inhibition of the brain. So it's reckless to try crack cocaine at all - at least until one's death-bed - because its euphoric effect is so extraordinarily hard to forget. If one succumbs to curiosity, and finds out what one is missing, then the rest of one's life may pall in comparison. For there is nothing in life that's naturally so enjoyable as crack. Tragically, the user's family and loved ones may suffer the price of pleasure almost as severely as the addict.
So is a crackhead inescapably doomed to an early grave? Or are there ways (s)he can escape from the abyss?
Perhaps. Most of the GIs who got hooked on unmistakably physically addictive heroin in Vietnam kicked the habit when they returned to the USA. The veterans quit, often without undue difficulty, because most of the "conditioned cues and reinforcers" associated with narcotic drug-use in South-East Asia were missing back home.
Thus a complete change of environment, especially a holiday in the company of supportive family and (drug-free) friends, can help break a user's self-destructive cycle of coke-binges. The brain is given time to recover. Cue-elicited craving is a major cause of relapse in recovering coke-users. Indeed this cue-elicited craving may even increase during the first few months of withdrawal.
Good food, particularly an idealised stone-age diet [fruit, vegetables, nuts, seeds, wholemeal bread, pasta, rice etc] should help. Regular vigorous exercise is useful as well [and probably Faith In Jesus, though this isn't always a realistic goal]. Another option is joining Cocaine Anonymous.
More controversially, "cocaine vaccines" may soon be licensed. They are designed to induce drug-specific antibodies in the bloodstream. In theory, cocaine-specific antibodies which sequester the drug before its passage into the brain will prevent the relapsing user getting high. Perhaps children "at risk" will be vaccinated at an early age. The possible coercive use of "vaccines against pleasure" raises profound ethical problems.
Cocaine addicts motivated to quit might consider a course of the antiepileptic drug vigabatrin (Sabril), though it isn't licensed in the USA. Vigabatrin is an irreversible inhibitor of gamma-aminobutyric acid transaminase (GABA-T). GABA-T the enzyme responsible for the catabolism of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA). Feedback inhibition between the "feel good" dopaminergic and GABA-ergic neurotransmitter systems explains vigabatrin's therapeutic "antidopaminergic" action. Vigabatrin is a relatively safe drug. Even so, its use sometimes causes colour vision defects; the most common adverse side-effects reported are sleepiness and fatigue.
A future option for cocaine addicts who want to quit may be taking a dual dopamine/serotonin releaser. PAL-287 is a rationally-designed drug aimed at treating stimulant dependence while having minimal "abuse potential" of its own. Much more research will be needed before it ever gets a product license.
Another future option may be the benztropine analog JHW007. It serves as a functional antagonist to cocaine. JHW007 has a high affinity for the dopamine transporter with minimal cocaine-like subjective and behavioural effects.
Some drug-pundits recommend Total Abstinence from chemical assistance: "Just Say No." The ex-addict is encouraged to renounce "unnatural" chemical highs altogether. This course of action may indeed be prudent given our bug-ridden genome and current crop of misbegotten street drugs. Unfortunately, opting to embrace godliness, hard work and clean living isn't always the recipe for a happy life either.
For many cocaine-users have a pre-existing psychiatric disorder - even by the touchstone of today's impoverished conception of mental health. In effect, such users are self-medicating, even if they ostensibly take cocaine hedonistically "for kicks". Such users need more effective medicine to flourish. So in place of cocaine, the option of taking one or more clinically therapeutic mood-brighteners [e.g. desipramine (Norpramin), a noradrenaline reuptake inhibitor; venlafaxine (Effexor), milnacipran (Ixel) or duloxetine (Cymbalta), dual-action serotonin and noradrenaline reuptake inhibitors; perhaps a glutamate-enhancing agent such as modafinil (Provigil); or more daringly, amineptine (Survector), a dopamine reuptake inhibitor; and/or anti-anxiety agents e.g. benzodiazepines] may be considered instead.
Alternatively, if the user wishes to Say No To Drugs completely, then a "natural", gentle mood-brightener and anti-anxiety agent, hypericum (St John's wort), may be taken indefinitely. Unfortunately, this traditional herbal medicine is not a dependable remedy for deep melancholic depression - coke-induced or otherwise.
S-Adenosyl-L-methionine (SAMe) is another natural antidepressant. But its efficacy in treating cocaine-induced depression is untested in controlled clinical trials.
Inevitably, present-day mood-brighteners, whether herbal or clinical, won't stand comparison with tomorrow's revolutionary designer-drugs. Nor do they deliver the rapturous but addictive rush of a fast-acting euphoriant. Contemporary therapeutic mood-boosters yield desperately little joy compared to the lifetime of genetically pre-programmed superhealth on offer to our descendants. But our legacy DNA didn't design us to be happy. So for now, the dirty chemical stopgaps licensed for use in contemporary clinical medicine are often better than nothing at all. Read More......
A Spoonful of Sugar?
The coca leaf doesn't travel well. By the time leaves sent by early colonists in South America reached Europe, they had lost much of their potency. So for centuries the plant remained litte more than a curiosity of interest only to obscure European botanists. The active alkaloid of the coca plant, cocaine, was first isolated from coca leaves by the German chemist Friedrich Gaedcke (1828-1890) in 1855. Gaedcke published his discovery in Archives de Pharmacie; he called it "Erythroxyline".
An improved step-by-step purification process was described by Albert Niemann (1834-1861) of Gottingen University in 1859. Niemann called the compound "cocaine"; and the name stuck. He was awarded a PhD; his dissertation was published in March 1860 as a slim volume called On a New Organic Base in the Coca Leaves. Niemann writes of its "colourless transparent prisms...Its solutions have an alkaline reaction, a bitter taste, promote the flow of saliva and leave a peculiar numbness, followed by a a sense of cold when applied to the tongue." Niemann had discovered that cocaine acted as a local anaesthetic. He died a year or so later in mysterious circumstances. The exact molecular formula of cocaine (i.e. C17H21NO4 ) was elucidated in 1863 by Niemann's colleague Wilhelm Lossen (1838-1906). In 1894, German chemist Richard Willstaetter (1872-1942) was awarded his doctorate from the University of Munich for discovering the its structural formula.
The commercial production of purified cocaine gained momentum only in the mid-1880s. Its greatest medical value was in ophthalmology. Eye-surgery stood in desperate need of a good local anaesthetic. This was because in eye operations it is often essential for a conscious patient to move his eye as directed by the surgeon - without flinching. Viennese ophthalmologist Karl Koller (1857-1944) discovered that cocaine was ideal for the task. From 1884, news of his successful experiments travelled round the world. The military took an interest as well. In 1883, German physician Theodor Aschenbrandt administered cocaine to members of the Bavarian army. It was found that the drug enhanced their endurance on manoeurvres.
Aschenbrandt's study was published in a German medical journal. The report was read by a young Viennese neurologist, Sigmund Freud (1856-1939). Freud was to play a significant role in the development of the Western cocaine-industry. "I take very small doses of it regularly and against depression and against indigestion, and with the most brilliant success", he observed. Drug giants Merck and Parke Davies both paid Freud to endorse their rival brands. Freud wrote several enthusiastic papers on cocaine, notably Ьber Coca (1884). He talks of "the most gorgeous excitement" animals display after receieving injection of a cocaine "offering". And in humans, cocaine induces...
"...exhilaration and lasting euphoria, which in no way differs from the normal euphoria of the healthy person...You perceive an increase of self-control and possess more vitality and capacity for work....In other words, you are simply normal, and it is soon hard to believe you are under the influence of any drug....Long intensive physical work is performed without any fatigue...This result is enjoyed without any of the unpleasant after-effects that follow exhilaration brought about by alcohol....Absolutely no craving for the further use of cocaine appears after the first, or even after repeated taking of the drug..."
Freud concluded Ьber Coca by recommending seven conditions for which cocaine pharmacotherapy might prove valuable:
as a mental stimulant
as a possible treatment for digestive disorders
as an appetite stimulant in case of wasting diseases
as a treatment for morphine and alcohol addiction
as a treatment for asthma
as an aphrodisiac
as a local anaesthetic
It was Freud's fourth recommendation that caused the most controversy. Cocaine is no longer prescribed as an antidote to morphine addiction.
Taken in an oral solution as Freud had envisaged, cocaine was indeed less likely to be addictive than when administered by the intravenous route. The euphoria induced is delayed; and it may be less intense and even subtle. A lot of the cocaine is broken down in the liver before it reaches the brain. However, hypodermic needles were starting to become widely available in the 1880s. Morphine addicts soon discovered that subcutaneous injections of cocaine yielded a quick, potent and addictive high. Before long, many users became hooked on cocktails including both. Using cocaine to cure morphine addiction, Freud later ruefully admitted, was "like trying to cast out the Devil with Beelzebub." Read More......
Vintage Wine
According to the Sears, Roebuck and Co. Consumers' Guide (1900), their extraordinary Peruvian Wine of Coca...
"...sustains and refreshes both the body and brain....It may be taken at any time with perfect safety...it has been effectually proven that in the same space of time more than double the amount of work could be undergone when Peruvian Wine of Coca was used, and positively no fatigue experienced....."
Some 99% of contemporary Western users mix cocaine and ethyl alcohol. Cocaine and alcohol combine to form another hugely reinforcing compound, cocaethlyene. Coca-use only really took off in the West when it was blended with an alcoholic beverage.
The real soaraway success in Europe was Vin Mariani. Launched in 1863, it was an extremely palatable coca wine developed by the Corsican entrepreneur, Angelo Mariani (1838-1914). Mariani first tried his new tonic on a depressed actress. The results were spectacular. She soon told all her friends. Mariani himself wrote a book eulogising coca; and he gathered artefacts of, and material on, the coca-loving Incas. At home, he collected coke-taking paraphernalia. He also took up amateur horticulture and cultivated the coca plant in his garden.
Coca wine made Mariani famous. Vin Mariani rapidly became the world's most popular prescription. Writers loved it. Anatole France, Henrik Ibsen, Йmile Zola, Jules Verne, Alexander Dumas, Robert Louis Stephenson, Sir Arthur Conan Doyle, and other literary luminaries all indulged freely. Composers such as Massenet, Gounod and Faurй gratefully honoured the Corsican druggist in their music. Vin Mariani was celebrated by royalty as well: by Queen Victoria; King George 1 of Greece; King Alphonse XIII of Spain; the Shah of Persia; and by William McKinley, President of the United States.
A devotion to Vin Mariani transcended petty differences of religious dogma. The Grand Rabbi of France, Zadoc Kahn, was moved to exclaim: "My conversion is complete. Praise be to Mariani's wine!" Pope Pius X was an enthusiast, as was Pope Leo XIII. He gave coca wine an official seal of approval by awarding Angelo Mariani a special gold medal. In recent years, however, the Vatican has felt unable to reiterate its original endorsement.
John Pemberton (1832-1888), the Atlanta-born creator of Coca Cola, was a keen pharmacist and coca-lover. He sought to combine the ultimate medicine and perfect drink in one glorious cocktail. Pemberton based his original drink on Vin Mariani. It was said to be "a most wonderful invigorator of the sexual organs". "Pemberton's French wine coca" proved singularly popular with American consumers. Coke was soon touted as "an intellectual beverage"; though not on the basis of controlled clinical trials.
Atlanta introduced Prohibition in 1886. So Pemberton had to replace the wine in his recipe with sugar syrup. Thus 'Pemberton's French wine cola' became 'Coca-Cola: the temperance drink'.
Official approval of coca-based tonics began to wane towards the end of the century. Unfortunately, people who were prescribed cocaine to combat morphine dependence were becoming addicted to both.
In 1904, America's gathering moral panic about Drug Abuse led the manufacturers to remove the cocaine from Coca-Cola. It is now official Coca-Cola Company policy to deny the existence of cocaine in their orginal world-winning formula. The US Government later tried to compel the company to drop the name 'Coca-Cola' too. After protracted legal argument, the name was saved; but traditionalists claimed the drink itself never quite recaptured its original glory. Read More......
C17H21NO4
Cocaine is habit-forming. It is potentially dangerous when indulged in to excess.
If rats or monkeys are hooked up to an intravenous source of heroin, they will happily self-administer the drug indefinitely; but they still find time to sleep and eat.
If rats or monkeys can freely self-administer cocaine, however, they will do virtually nothing else. Captive animals continue to press their drug-delivery lever for as long as they are physically capable of doing so. Their fate is similar to an intracranially self-stimulating laboratory rodent. Within weeks, if not days, they will lose a substantial portion of their body weight - up to 40%. Within a month, they will be dead.
Urinary Detection Times
SUBSTANCE DETECTION PERIOD
in trace amounts DETECTION PERIOD
resulting in positive test
Cocaine
Benzoylecgonine 2-4 days 2-4 days
Chronic Use up to 3 weeks up to 3 weeks
Amphetamines
Amphetamine 2-5 days 1-3 days
Methamphetamine 2-5 days 1-3 days
Cannabis (THC)
Casual Use 2-7 days 1-5 days
Chronic Use up to one month up to six weeks
Phencyclidine (PCP)
Casual Use 2-7 days 2-7 days
Chronic Use up to 30 days up to 14 days
Opiates
Codeine 2-5 days 1-3 days
Morphine 2-4 days 1-2 days
The world's first drug-testing scandal occurred in 1876. Competitive long-distance walking had become a popular sport. American Edward Weston challenged the English champion to a 24 hour race. The contest was held at the Agricultural Hall in the North London Borough of Islington. The effete Englishman gave up after a mere 14 hours and 66 miles. The American carried on walking for the full 24 hours and 110 miles. It later transpired that Weston had being chewing coca leaves - "Peruvian marching powder" - throughout the race. There was an outcry; but Weston kept his title. Read More......
Coca In Bloom
There are around 250 species of erythroxylon plants. At least 20 produce cocaine. Only two of them, erythroxylon coca and erythroxylon novogranatense, typically yield enough cocaine to justify commercial cultivation.
Chewing leaves of coca normally induces a pleasant and subtle sense of well-being. Other routes of administration may exert a more dramatic impact on the user; and pose substantially greater risks to health.
Yet sensitivity to coca-extract varies. Paola Mantegazza (1831-1910), an Italian physician working in northern Argentina in the 1850s, seems to have been unusually receptive to its properties:
"...I sneered at the poor mortals condemned to live in this valley of tears while I, carried on the wings of two leaves of coca, went flying through the spaces of 77, 438 words, each more splendid than the one before...An hour later, I was sufficiently calm to write these words in a steady hand: God is unjust because he made man incapable of sustaining the effect of coca all life long. I would rather have a life span of ten years with coca than one of 10 000 000..(and here I has inserted a line of zeros) centuries without coca."
The capacity "of sustaining the effect of coca all life long" will indeed not come from God - nor from godliness. Nor will it come from wholesome living and clean thoughts. This is because we are born with a "hedonic-treadmill" of mood-regulating negative-feedback mechanisms in the CNS. The hedonic treadmill is vicious. It prevents us from subverting our gene-driven "set-point" of emotional well/ill-being by cosmetic lifestyle-adjustments.
Fortunately, the application of designer-drugs, nanotechnology and gene-therapy promises eventually to get rid of suffering and malaise altogether. If we choose to abolish them, then the metabolic pathways of unpleasantness can be edited out of existence.
Better still, our genetically-enriched successors will be able to enjoy life-long bliss far richer than anything a drug or plant-extract can induce at present. The well-being of our descendants will be deeper, more diverse, more intense and (perhaps) more empathetic than anything physiologically accessible to drug-naïve mortals today. In the new reproductive era ahead, genetic disorders such as ageing and a capacity for aversive experience are destined to disappear into the evolutionary past. For tomorrow's paradise-engineers will rewrite the human genome to serve our own interests rather than selfish DNA.
But large-scale genetic-rewrites take time. The use of biotechnology to abolish suffering throughout the living world - and a possible Post-Darwinian Transition to paradise-engineering - will take many centuries, perhaps even millennia. And on the whole, we want to be happy right now.
Unfortunately, recreational drugs like cocaine offer only a deadly short-cut to nirvana. Read More......
Flower Erythroxylon Coca
Coca leaves have been chewed by South American Indians for many thousands of years to induce a mild and long-lasting euphoria. Anthropologists have speculated that the word coca derives from the pre-Incan Tiwanaku word khoka - meaning "the plant". The Aymara word q'oka means "food for travellers and workers".
The Incas in particular venerated coca. They used coca in magical ceremonies and initiation rites; for divination and fertility rituals; and to heal their physical and psychic woes. Two of the Inca emperors named their wives after the leaf - the honoured consorts were given the plant's sacred title, Mama Coca. The only object ever carried by the Inca emperor himself was a coca pouch. He wore it around his neck close to his heart.
In the Inca period, the elite regarded the sacred leaf as far too good for ordinary Indians. The invading Spanish conquistadores were more practical - and cynical. Intially coca use and cultivation was denounced, especially by the Catholic Church, for its destructive influence on the native populations. Coca was banned as an agent of idolatry and sorcery, "strengthening the wicked in their delusions, and asserted by every competent judge to possess no true virtues; but, on the contrary, to cause the deaths of innumerable Indians, while it ruins the health of the few who survive."
But the invaders were impressed at coca's efficacy as a stimulant: "The herb is so nutritious and invigorating that the Indians labour whole days without anything else." The Spanish needed native labour in their silver-mines. Work in the mines was extremely arduous; and taking coca reduces appetite and increases physical stamina. Hence there was a great surge in coca-use and the number of coqueros (coca-chewers).
Pope Paul III (r. Oct. 13, 1534 - Nov. 10, 1549) stated in his encyclical entitled "Sublimus Die" that Indians were not to be robbed of their freedom. He wrote "Notwithstanding whatever may have been or may be said to the contrary, the said Indians [of the New World] and all other people who may later be discovered by Christians, are by no means to be deprived of their liberty or the possession of their property, even though they be outside the faith of Jesus Christ; and that they may and should, freely and legitimately, enjoy their liberty and the possession of their property; nor should they be in any way enslaved..." Read More......
Hard Rock
Millions of years of evolution by natural selection has endowed the brain with a cruel web of negative-feedback mechanisms to regulate our moods, emotions and degree of well-being. Taking refined 'recreational' euphoriants, notably cocaine or the amphetamines, sends a signal to the brain that indicates, falsely, the impending arrival of an immense evolutionary benefit.
After the drug-fuelled high comes the crash. Genetically-driven feedback-inhibition kicks in. Cocaine-withdrawal causes a protracted biochemical abstinence-syndrome marked by craving, melancholy and anhedonia. Neuronal release of dopamine declines. So does the number of mesolimbic dopamine transporters. The spontaneous firing of dopamine cells decreases. Chronic cocaine dependence may cause long-lasting functional deficits in the frontal cortex as well.
The hedonic treadmill punishes naive attempts to get high. Read More......
Crack Cocaine
Cocaine is a powerful constrictor of blood vessels and a local anaesthetic. It is also a potent psychostimulant. The physical effects of cocaine on the user include excitement, alertness, tachycardia, pupillary dilatation, raised body-temperature, hypertension, brochodilation, enhanced glucose availability, and increased motor activity - all part of the "fight or flight" syndrome.
Taking cocaine also also gets you high. Its half-life in the plasma, however, is only 50 minutes; and the euphoria soon fades. Freebase/crack users desire more of the drug far sooner than users of the hydrochloride salt.
The rewarding properties of cocaine derive mainly from its effects on the neurotransmitter dopamine. The dopamine system is involved in the control of mood, motivation, cognition, locomotion, sexuality and endocrine function. There are only some 30-40 thousand dopamine neurons in the brain, but both the axons and dentrites of the dopamine neurons are unusually well arborised - with as many as 100,000 synapses for each dopaminergic neuron. Their distinctive morphology reflects dopamine's role in the "encephalisation of emotion".
Cocaine induces elation primarily by blocking the dopamine transporter. The blockade increases the availability of free dopamine in the mesolimbic pleasure-centres of the brain. Degree of transporter occupancy is correlated with the intensity of euphoria. Higher doses and faster routes of administration create vivid memories and intense cravings. But the biological substrates of pure pleasure remain elusive. Investigation of the possible final common pathway of pleasure in the brain continues. Endorphins and enkephalins activating receptors in the ventral pallidum apparently play a role too, as does the orbitofrontal cortex.
Recent research highlights the role of the sigma1 receptors in cocaine-induced euphoria. Co-administering a sigma1 agonist makes taking cocaine even more enjoyable. Sigma1 agonists like igmesine are also under investigation as potential antidepressants. Conversely, taking a sigma1 receptor antagonist makes cocaine use unrewarding.
Whatever its mechanisms, and unlike most clinically-approved mood-brighteners, cocaine is a pro-sexual drug. Taken before sex, it can induce prolonged and intense orgasm. Cocaine-induced lovemaking, however, is not especially warm or empathetic. Read More......
2-beta-carbomethoxy-3-beta-benoxytropane
Cocaine can be manufactured by converting tropinone into
2-carbomethoxytropinone, reducing this to ecgonine,
and then converting the ecgonine to cocaine.
This isn't as easy as it sounds. Read More......
The Vials Of Crack
Who invented crack?
No one knows for sure. One story credits its discovery to a chemist of the Cali cartel. An early epidemic of crack use occurred in the Bahamas from 1980; Bahamian hospital psychiatry departments recorded a surge of admissions from severely disturbed and psychotic users. In 1983, crack use filtered across the Florida Straits. It took hold in Miami, followed by New York. The first newspaper report of the phenomenon appeared in the Los Angeles Times in 1984, Within a year, crack use had swept across inner city ghettoes throughout America. The first "crack babies" were born.
Crack is actually a less pure variety of free-base cocaine. Unlike old-fashioned free-base, however, its production doesn't involve any flammable solvents. Unlike the hydrochloride salt, free base cocaine vapories at a low temperature. This makes it suitable for smoking.
Crack is usually made by mixing two parts of cocaine hydrochyloride with one part baking soda (sodium bicarbonate: NaHC03) in about 20 ml of water. The solution is then heated gently until white precipitates form. Heating is halted when precipitation stops. The precipitate is filtered and retained. The precipitate may then be washed with water; this procedure is usually omitted in the street product. The product may then be dried for 24 hours under a heat-lamp. Crack is then cut or broken into small 'rocks' weighing a few tenths of a gram.
The traditional method of taking cocaine in the West involves snorting the hydrochloride salt. But absorption through the nasal mucosa is relatively modest. This is because their surface-area is small and cocaine is vasoconstrictive. Classic freebase, on the other hand, is smoked and inhaled directly into the lungs. Therefore much higher doses are possible. Inhalation is followed by an intense euphoric rush. The euphoria doesn't last long. The user becomes irritable and craves more of the drug.
Chronic cocaine-use causes a decrease in the production of enkephalin, one of the brain's natural opioids. This in turn causes a compensatory increase in the number of mu-receptors. The number of unoccupied mu-receptors may be associated with the craving and abstinence syndrome.
After chronic exposure to cocaine, the number of post-synaptic dopamine receptors in the CNS is reduced. The amount of dopamine transporter protein is increased. Tolerance to cocaine's effects does exist over prolonged use; but the extent of this physiological adaptation is relatively modest. The cocaine-user still gets high; but in the absence of cocaine, his pre-synaptic neurons sequester dopamine in the synaptic cleft with greater efficiency. This may induce depression, and sometimes profound despair.
No one ever feels contented after taking cocaine. They just want more. Read More......
Erythroxylum Cataractarum
In its native habitat, the coca plant is resistant to drought and disease. Coca is a small shrublike tree that doesn't need irrigation. Its leaves are green, oval and tough. Its flowers are small and greenish white. A red fruit is produced with a single seed.
The introduction of coca to England was pioneered early in the nineteenth century by the Royal Botanical Gardens at Kew. However, the coca plant has yet to find a place in orthodox Western horticulture.
The growth of Net-based ecommerce in the early Twenty First Century nonetheless spurred an upsurge in demand and supply among horticulturalists across the globe. Gardening enthusiasts who visit Cocomama (2003) are told: "If you're interested to grow coca plant for hobby, research or conservation purposes, feel free to order the seeds."
In the 1980s, millions of drug-naïve Americans were introduced to "decocainised" coca tea imported from South America. The legitimate cultivation of Peruvian coca, and also the production of all Peruvian cocaine licensed for pharmaceutical export, was controlled by the government's own National Enterprise Of Coca. In a bid to expand and diversify its product range, the National Enterprise Of Coca promoted the benefits of coca in the form of a wholesome traditional beverage. This state-sponsored export-drive was successful: overseas demand proved brisk. From 1983, 'Inca Health Tea' sold especially well in the North American market. Lemongrass and other flavours were added to cater to American palates. Soon matй de coca could be bought in tea-shops and grocery stores in US cities.
Matй de coca is indeed an agreeable and invigorating mood-brightener. Matй de coca is also extremely benign: patients at the San Francisco National Addiction Research Foundation, for instance, were encouraged in the 1980s to drink as much mate de coca as they desired to help wean themselves off cocaine. When consumed in generous quantities, coca tea is remarkably good at easing drug-cravings. However, this is because the average "decocainized" tea-bag contains 5 milligrams of cocaine. Read More......
Erythroxylon Coca Farmer
Coca can be harvested four times a year. Traditionally, chewing the sacred leaf promotes contact with the spirit world. Chewing or smoking coca leaves invigorates the user, allowing him to absorb the plant's magical powers and protect body and spirit alike. Ancient Peruvians used coca as a local anaesthetic before trepanning - the hazardous surgical technique of drilling a hole in the skull to relieve various physical and psychic woes.
In traditional Indian cultures, Mama Coca was accounted a benevolent deity. She was regarded as a sacred goddess who could bless humans with her power. Before the coca harvest, the harvester would sleep with a woman to ensure that Mama Coca would be in a favourable mood. Typically, a decoction of coca and saliva was rubbed onto the male organ to prolong erotic ecstasy.
Tales of the aphrodisiacal properties of cocaine eventually reached the Old World too. In his journal of 1794, Hipolito Unanue writes of "coqueros, 80 years of age and over, and yet capable of such prowess as young men in the prime of life would be proud of."
Later authorities made no less extravagant claims. In Der Kokainismus (1926), Swiss psychiatrist Hans Maier records: "After a night of sexual prowesses, compared to which the seven labours of Hercules were a mere nothing, I fell asleep, only to be immediately awakened by the renewed demands of my insatiable partner. I was able to verify on myself the degree to which cocaine renders women incapable of achieving sexual relation. Orgasm follows orgasm, each one further increasing the intensity of the desire. The most sexually potent man must eventually give up the hope of satisfying such a woman. There was nothing to do but flee in self-preservation."
Such purple prose may mislead the unwary. Cocaine is not an aphrodisiac if taken in large quantities over prolonged periods. Indeed chronic cocaine use may suppress erotic behaviour altogether. This is because taking pure cocaine is typically more pleasurable than having sex. Captive animals given the opportunity to enjoy unlimited quantities of both will initially be more sexual active. But they end up focusing entirely on the cocaine. This pattern of behaviour is also the common experience of humans who pass from casual recreational use of the drug to become cocaine addicts. Read More......
Processing
Cocaine is the world's most powerful stimulant of natural origin. South American Indians have used cocaine as it occurs in the leaves of Erythroxylon coca for at least 5000 years. Coca-chewing promotes clarity of mind and a positive mood. Traditionally, the leaves have been chewed for social, mystical, medicinal and religious purposes. Coca has even been used to provide a measure of time and distance. Native travellers sometimes described a journey in terms of the number of mouthfuls of coca typically chewed in making the trip. This was a "cocada" - the time or distance and man could walk before a coca pellet was exhausted.
Physical constraints ensure that even the most ardent coquero can get only a modest amount of cocaine into his bloodstream. Coca-induced heart-attacks and strokes are thus extremely rare among traditional users. In recent decades, however, there have been changes in cocaine's route of administration, patterns of usage, the technology of cocaine production, and typical dosages.
There are four basic routes to coca intoxication:
chewing the leaves. Coca consumption was originally the prerogative of the Inca elite. Today, most of the natives indulge as well. Coca is also consumed as the highly esteemed matй de coca. Drinking coca-tea tends to soothe the stomach; so it's good for digestive problems. Matй de coca is less likely to induce jitteriness than coffee. It is also rather more effective as a mood-brightener.
cocaine sulphate - pasta, basuco, basa, pitillo, paste. This is the low-grade stuff that reaches the urban slums of South America. The sulphate is the intermediate stage between the coca leaf and the finished cocaine hydrochloride crystal. Coca leaves are stripped from the plant. They are put into plastic pit with a solution of water and dilute sulphuric acid. A bare-footed man will climb into the pit; step on the mess; and shove it around with his hands. In South America, coca paste in commonly mixed with tocacco and smoked.
cocaine hydrochloride - an odourless, white crystalline powder. It has a bitter, numbing taste. Cocaine hydrochloride is a stable, hydrophilic salt. Thus it can be snorted and absorbed through the nasal mucosa. Absorption at around 20-30% is still relatively poor. It is limited by the drug's tendency to cause vasoconstriction. Making cocaine hydrochloride is quite complicated. The pasta is first washed in kerosene. It is then chilled. The kerosene is removed. Gas crystals of crude cocaine are left at the bottom of the tank. Typically, the crystals are dissolved in methyl alcohol. They are then recrystallised and dissolved once more in sulphuric acid. Further washing, oxidation and separation procedures involve potassium permanganate, benzole, and sodium carbonate.
freebase/crack cocaine. The idea of smoking cocaine isn't new. Drug company Parke, Davies introduced coca-cigars as long ago as 1886. But heat degrades rather than vaporises cocaine hydrochloride. So coca-cigar sales never took off. Smokeable cocaine in the form of the base rather than the salt didn't become widespread in the US for another hundred years. Freebase/crack is derived from cocaine hydrochloride which has been chemically treated with ammonia or baking-soda to free the potent base material from the salt. Free-base was originally produced by a dangerous four-or-five step process in which the hydrochloride salt was heated with water and a volatile liquid such as ether. Base cocaine in the form of 'crack' is safer to produce; but it is no less addictive. Crack/free-base itself is indissoluble in water, so it can't easily be injected or sniffed. Instead, it is usually smoked from pipes; burnt on a piece of tin foil; or mixed with tobacco and perhaps cannabis in a smokable joint. The euphoric rush comes within a few seconds - even faster than from intravenous cocaine hydrochloride. Initially, the user may experience a profound sense of power, mastery, cleverness and uninhibited desire. Orgasm is intensified. Extravagant hyper-sexuality and rampant promiscuity are common. The exhilaration usually starts to fade within a few minutes. Cocaine is rapidly metabolised in the blood and liver. Its typical half-life is 30-90 minutes. Soon, the crackhead desperately craves another hit. Profound depression may occur if it is denied. Descent into the abyss has begun.
During crack-cocaine binges, addicts may become utterly drug-obsessed. The obsession is so all-consuming that food, money, sleep, loved ones, morality, any sense of responsibility, and even survival-instincts may be eclipsed. Users may smoke crack at fifteen-minute intervals for some 72 hours without pause for sleeping or eating. A "crash" inevitably follows; and a profound melancholy.
Thus crack-cocaine is neither a wise nor effective choice of long-term mood-brightener. Read More......
1kg
Cocaine is an integral part of the world economy. Its street price reflects the competitive pressures of today's global marketplace. In the past few decades, cocaine has become a significant export-earner for many poor South American countries, notably Peru, Bolivia and Colombia. South America currently exports some 1000 tons of refined cocaine per year. Smugglers can be quite ingenious. In recent years, US federal narcotics officials have seized $450,000 worth of cocaine moulded into dog kennels; and detained a consignment of sickly boa constrictors stuffed with cocaine-filled condoms.
Cocaine is now a leading export earner for Jamaica. Phil Sinkinson, Britain's deputy high commissioner to the island, was asked (2nd Jan 2002) on BBC Radio 4 Today programme to comment on newspaper claims that one in every ten air passengers travelling from Jamaica to the UK was a cocaine carrier or "drug mule". He replied: "Probably an estimate on the low side."
In the twentieth century, coca was grown commercially in Sri Lanka, Taiwan, Indonesia, Nigeria, Malaysia and Japan. The first cocaine cartel was formed, not in Colombia, but in Amsterdam. Founded in 1910, the Cocaine Manufacturers Syndicate included pharmaceutical giants Merck, Sandoz and Hoffman-LaRoche. At present, however, most production occurs in clandestine laboratories in South America.
The cocaine trade continues to spawn eyebrow-raising alliances. Declassified documents now available at the CIA web site disclose that in the 1980s CIA operatives teamed up with cocaine dealers in the fight against Communism.
In 1979, the people of the small Central American country of Nicaragua overthrew the US-backed Samoza dictatorship. To the dismay of US policy-makers, the Nicaraguans then elected a left-wing government. Investigative journalist Gary Webb [Dark Alliance: the CIA, the Contras, and the Crack Cocaine Explosion; June 1998] first revealed how profits from cocaine sold in Los Angeles and Miami were used by the CIA to fund - and buy guns for - the anti-Communist Contra rebels. Suitcases stuffed with coke-tainted US dollars were dispatched to Nicaragua to foment insurrection and civil war.
According to Internic records (1998), contact details for the domain cocaine.com still belonged to the CIA, although the accuracy of the whois record has been challenged. Read More......
Coca Negra
Cobalt and ferric chloride are virtually undetectable masking-chemicals.
They are mixed with pure cocaine - perhaps 40% - and later separated out.
In South America, customs' officers often use sniffer dogs that have been turned
into canine junkies. This ensures the dogs will avidly sniff out contraband narcotics.
Not only customs' officers rely on animal assistance. Dogs have recently
been used as "mules" by cocaine traffickers. Read More......
The Tools Of The Trade
Cocaine-merchants rely on weighing equipment whose accuracy of calibration is open to variation.
A 1994 survey by the General Accounting Office suggested
that in the previous year around one million US citizens
had used cocaine at least once a week.
Current usage estimates are broadly similar. Read More......
The Health Effects of Cocaine
Cocaine can be snorted, injected and even smoked in some forms of the drug. In all cases cocaine is a strong central nervous system stimulant which affects the brain's processing of dopamine.
Short-Term Effects
When cocaine is used it interferes with the reabsorption of dopamine, a brain chemical associated with pleasure and movement, producing a euphoric effect. Shortly after cocaine is ingested the user may experience the following symptoms:
Constricted blood vessels.
Dilated pupils.
Increased body temperature.
Increased heart rate.
Higher blood pressure.
During the euphoric period after cocaine use, which can last up until 30 minutes, user will experience hyperstimulation, reduced fatigue, and mental alertness. However, some users also experience restlessness, irritability, and anxiety.
During a cocaine binge, when the drug is taken repeatedly, users may experience increasing restlessness, irritability and paranoia. For some users this can lead to a period of paranoid psychosis, with auditory hallucinations and a disconnection with reality.
Long-Term Effects
Repeated cocaine use can cause the following health consequences:
Irregular heart beat.
Heart attack.
Chest pain.
Respiratory failure.
Stroke.
Seizures and headaches.
Abdominal pain and nausea.
Chronic users of cocaine can become malnourished due to the drug's ability to decrease appetite. Each method of taking cocaine can produce specific health effects, including:
Snorting: Chronically runny nose, nosebleeds, loss of smell, hoarseness, and problems swallowing.
Ingesting: Severe bowel gangrene due to a reduction in the flow of blood to the intestines.
Injecting: Severe allergic reactions. Increased risk for contracting HIV, Hepatitis and other blood-borne diseases.
Overdose
Although cocaine overdose is not common, it can occur and can be fatal. Because cocaine affects the heart and respiratory system, an overdose can cause death, especially when the drug is injected or smoked.
An overdose of cocaine can lead to:
Irregular heart beat or heart failure.
High blood pressure resulting in a brain hemorrhage.
Repeated convulsions.
Respiratory failure.
Addiction
Cocaine is highly addictive and those who smoke cocaine appear to develop an addiction to the drug more rapidly that those who snort it. However, even those who snort cocaine can find themselves addicted.
Cocaine users report that they are never able to achieve the "high" they felt the first time that they used the drug. A tolerance to the drug is developed so that the euphoric feeling users get is not as intense nor does it last as long.
When cocaine is injected, the euphoric feeling can last from 15 to 30 minutes, but when it is smoked, in may last only five to 10 minutes, causing the user to use more cocaine more often to try to maintain that high.
Withdrawal
When cocaine users stop using cocaine, or when they end a cocaine binge, they immediately experience a "crash" which includes depression, fatigue, lack of pleasure, anxiety, irritability, sleepiness and a strong craving for more cocaine.
Some people experience agitation and extreme suspicion when they quit using cocaine, but cocaine withdrawal usually does not have visible physical symptoms like vomiting, chills and tremors that occur with the withdrawal of other drugs. Read More......
How Synthetic Cocaine Is Made
Manufacturing Synthetic Cocaine
Cocaine produces central nervous system arousal or stimulant effects which closely resemble those of the amphetamines, the methylenedioxyamphetamines in particular.
This is due to the inhibition by cocaine of re-uptake of the norepinepherine released by the adrenergic nerve terminals, leading to an enhanced adrenergic stimulation of norepinephrine receptors.
The increased sense of well being and intense, but short lived, euphoric state produced by cocaine requires frequent administration.
Cocaine does not penetrate the intact skin, but is readily absorbed from the mucus membranes, creating the need to snort it. This accounts for the ulceration of the nasal septum after cocaine has been snorted for long periods.
The basic formula for cocaine starts by purchasing or making tropinone, converting the tropinone into 2-carbomethoxytropinone (also known as methyl-tropan-3-one-2-carboxylate), reducing this to ecgonine, and changing that to cocaine.
Sounds easy? It really is not very simple, but with new drug policies, cracking down on all of the drug smuggling at the borders, this synthetic cocaine may be the source of the future.
This synthesis is certainly worth performing with the high prices that cocaine is now commanding. As usual, I will start with the precursors and intermediates leading up to the product.
Succindialdehyde. This can be purchased, too. 23.2 g of succinaldoxime powder in 410 ml of 1 N sulfuric acid and add dropwise with stirring at 0j a solution of 27.6 g of sodium nitrite in 250 ml of water over 3 hours.
After the addition, stir and let the mixture rise to room temp for about 2 hours, taking care not to let outside air into the reaction. Stir in 5 g of Ba carbonate and filter.
Extract the filtrate with ether and dry, evaporate in vacuo to get the succindialdehyde.
This was taken from JOC, 22, 1390 (1957).
To make succinaldoxime, see JOC, 21, 644 (1956).
Complete Synthesis of Succindialdehyde. JACS, 68, 1608 (1946).
In a 2 liter 3 necked flask equipped with a stirrer, reflux condenser, and an addition funnel, is mixed 1 liter of ethanol, 67 g of freshly distilled pyrrole, and 141 g of hydroxylamine hydrochloride.
Heat to reflux until dissolved, add 106 g of anhydrous sodium carbonate in small portions as fast as reaction will allow. Reflux for 24 hours and filter the mixture.
Evaporate the filtrate to dryness under vacuo. Take up the residue in the minimum amount of boiling water, decolorize with carbon, filter and allow to recrystallize in refrigerator.
Filter to get product and concentrate to get additional crop. Yield of succinaldoxime powder is a little over 40 g, mp is 171-172j.
5.8 g of the above powder is placed in a beaker of 250 ml capacity and 54 ml of 10% sulfuric acid is added.
Cool to 0j and add in small portions of 7 g of sodium nitrite (if you add the nitrite too fast, nitrogen dioxide fumes will evolve).
After the dioxime is completely dissolved, allow the solution to warm to 20j and effervescence to go to completion. Neutralize the yellow solution to litmus by adding small portions of barium carbonate.
Filter off the barium sulfate that precipitates. The filtrate is 90% pure succindialdehyde and is not purified further for the reaction to create tropinone. Do this procedure 3 more times to get the proper amount for the next step, or multiply the amounts given by four and proceed as described above.
Take the total amount of succinaldehyde (obtained from 4 of the above syntheses combined) and without further treatment or purification (this had better be 15.5 g of succindialdehyde) put into an Erlenmeyer flask of 4-5 liters capacity.
Add 21.6 g of methylamine hydrochloride, 46.7 g of acetonedicarboxylic acid, and enough water to make a total volume of 2 liters. Adjust the pH to 8-10 by slowly adding a saturated solution of disodium phosphate.
The condensate of this reaction (allow to set for about 6 days) is extracted with ether, the ethereal solution is dried over sodium sulphate and distilled, the product coming over at 113j at 25 mm of pressure is collected.
Upon cooling, 14 g of tropinone crystallizes in the pure state. Tropinone can also be obtained by oxidation of tropine with potassium dichromate, but I could not find the specifics for this operation.
2-Carbomethoxytropinone. A mixture of 1.35 g of sodium methoxide (this is sodium in a minimum amount of methanol), 3.5 g of tropinone, 4 ml of dimethylcarbonate and 10 ml of toluene is refluxed for 30 min. Coo] to 0j and add 15 ml of water that contains 2.5 g of ammonium chloride.
Extract the solution after shaking with four 50 ml portions of chloroform, dry, evaporate the chloroform in vacuo. Dissolve the oil residue in 100 ml of ether, wash twice with a mixture of 6 ml of saturated potassium carbonate and three ml of 3 N KOH.
Dry and evaporate in vacuo to recover the unreacted tropinone. Take up the oil in a solution of aqueous ammonium chloride and extract with chloroform, dry, and evaporate in vacuo to get an oil.
The oil is dissolved in hot acetone, cool, and scratch inside of flask with glass rod to precipitate 2- carbomethoxytropinone. Recrystallize 16 g of this product in 30 ml of hot methyl acetate and add 4 ml of cold water and 4 ml of acetone. Put in freezer for 2l/2 to 3 hours.
Filter and wash the precipitate with cold methyl acetate to get pure product.
Methylecgonine. 0.4 mole of tropinone is suspended in 80 ml of ethanol in a Parr hydrogenation flask (or something that can take 100 psi and not react with the reaction, like stainless steel or glass).
10 g of Raney Nickle is added with good agitation (stirring or shaking) followed by 2- 3 ml of 20% NaOH solution.
Seal vessel, introduce 50 psi of hydrogen atmosphere (after flushing vessel with hydrogen) and heat to 40-50j.
After no more uptake of hydrogen (pressure gauge will hold steady after dropping to its lowest point) bleed off pressure and filter the nickle off, rinse out bottle with chloroform and use this rinse to rinse off the nickle while still on the filter paper. Make the filtrate basic with KOH after cooling to 10j.
Extract with chloroform dry, and evaporate the chloroform in vacuo to get an oil. Mix the oil plus any precipitate with an equal volume of dry ether and filter.
Add more dry ether to the filtrate until no more precipitate forms, filter and add to the rest of the precipitate. Recrystallize from isopropanol to get pure methylecgonine. Test for activity.
If active, skip down to the step for cocaine. If not active, proceed as follows. Stir with activated carbon for 30 min, filter, evaporate in vacuo, dissolve the brown liquid in methanol, and neutralize with 10% HCI acid in dry ether.
Evaporate the ether until the two layers disappear, and allow to stand for 2 hours at 0j to precipitate the title product. There are many ways to reduce 2-carbomethoxytropinone to methylecgonine.
I chose to design a Raney Nickle reduction because it is cheap and not as suspicious as LAH and it is much easier than zinc or sodium amalgams.
Cocaine. 4.15 g of methylecgonine and 5.7 g of benzoic anhydride in 150 ml of dry benzene are gently refluxed for 4 hours taking precaution against H20 in the air (drying tube).
Cool in an ice bath, acidify carefully with hydrochloric acid, dry, and evaporate in a vacuum to get a red oil which is treated with a little portion of isopropanoi to precipitate cocaine.
As you can see, this is quite a chore. The coca leaves give ecgonine, which as you can see, is only a Jump away from cocaine.
If you can get egconine, then dissolve 8l/2 g of it in 100 ml of ethanol and pass (bubble) dry HC1 gas through this solution for 30 min. Let cool to room temp and let stand for another 11/2 hours. Gently reflux for 30 min and evaporate in vacuo.
Basify the residue oil with NaOH and filter to get 8.4 g of methylecgonine, which is converted to cocaine as in the cocaine step above.
Below is given a somewhat easier method of producing tropinone by the general methods of Willstatter, who was instrumental in the first synthetic production of cocaine and several other alkaloids. After reviewing this method, I found it to be simpler than the above in many respects.
Tropinone. 10 g of pyrrolidinediethyl diacetate are heated with 10 g of cymene and 2 g of sodium powder, the reaction taking place at about 160j. During the reaction (which is complete in about 10 min) the temp should not exceed 172j.
The resulting reaction product is dissolved in water, then saturated with potassium carbonate, and the oil, which separates, is boiled with dilute sulfuric acid. 2.9 g of tropinone picrate forms and is filtered.
Here are two more formulas devised by Willstatter that produce tropinone from tropine. Take note of the yield differences.
Tropinone. To a solution of 25 g tropine, dissolved in 10 times its weight of 20% sulfuric acid are added 25 g of a 4% solution of potassium permanganate in 2 or 3 g portions over 45 min while keeping the temp at 10-12j.
The addition of permanganate will cause heat (keep the temp 10-12j) and precipitation of manganese dioxide. The reaction mixture is complete in I hour.
A large excess of NaOH is added and the reaction is steam distilled until I liter of distillate has been collected.
The tropinone is isolated as the dibenzal compound by mixing the distillate with 40 g of benzaldehyde in 500 cc of alcohol and 40 g of 10% sodium hydroxide solution. Let stand several days to get dibenzaltropinone as yellow needles. Yield: 15.5 g, 28%. Recrystallize from ethanol to purify.
Tropinone. A solution of 12 g of chromic acid in the same amount of water (12 g) and 60 g of glacial acetic acid is added dropwise with stirring over a period of 4 hours to a solution of 25 g of tropine in 500 cc of glacial acetic acid that has been warmed to 60-70j and is maintained at this temp during the addition.
Heat the mixture for a short time on a steam bath until all the chromic acid has disappeared, cool and make strongly alkaline with NaOH. Extract with six 500 cc portions of ether and evaporate the ether in vacuo to get an oil that crystallizes readily.
Purify by converting to the picrate or fractionally distill, collecting the fraction at 224-225j at 714 mm vacuo.
The tropinones can be used in the above formula (or in a formula that you have found elsewhere) to be converted to cocaine. Remember to recrystallize the 2-carbomethoxytropinone before converting to methylecgonine. Read More......
Cocaine produces central nervous system arousal or stimulant effects which closely resemble those of the amphetamines, the methylenedioxyamphetamines in particular.
This is due to the inhibition by cocaine of re-uptake of the norepinepherine released by the adrenergic nerve terminals, leading to an enhanced adrenergic stimulation of norepinephrine receptors.
The increased sense of well being and intense, but short lived, euphoric state produced by cocaine requires frequent administration.
Cocaine does not penetrate the intact skin, but is readily absorbed from the mucus membranes, creating the need to snort it. This accounts for the ulceration of the nasal septum after cocaine has been snorted for long periods.
The basic formula for cocaine starts by purchasing or making tropinone, converting the tropinone into 2-carbomethoxytropinone (also known as methyl-tropan-3-one-2-carboxylate), reducing this to ecgonine, and changing that to cocaine.
Sounds easy? It really is not very simple, but with new drug policies, cracking down on all of the drug smuggling at the borders, this synthetic cocaine may be the source of the future.
This synthesis is certainly worth performing with the high prices that cocaine is now commanding. As usual, I will start with the precursors and intermediates leading up to the product.
Succindialdehyde. This can be purchased, too. 23.2 g of succinaldoxime powder in 410 ml of 1 N sulfuric acid and add dropwise with stirring at 0j a solution of 27.6 g of sodium nitrite in 250 ml of water over 3 hours.
After the addition, stir and let the mixture rise to room temp for about 2 hours, taking care not to let outside air into the reaction. Stir in 5 g of Ba carbonate and filter.
Extract the filtrate with ether and dry, evaporate in vacuo to get the succindialdehyde.
This was taken from JOC, 22, 1390 (1957).
To make succinaldoxime, see JOC, 21, 644 (1956).
Complete Synthesis of Succindialdehyde. JACS, 68, 1608 (1946).
In a 2 liter 3 necked flask equipped with a stirrer, reflux condenser, and an addition funnel, is mixed 1 liter of ethanol, 67 g of freshly distilled pyrrole, and 141 g of hydroxylamine hydrochloride.
Heat to reflux until dissolved, add 106 g of anhydrous sodium carbonate in small portions as fast as reaction will allow. Reflux for 24 hours and filter the mixture.
Evaporate the filtrate to dryness under vacuo. Take up the residue in the minimum amount of boiling water, decolorize with carbon, filter and allow to recrystallize in refrigerator.
Filter to get product and concentrate to get additional crop. Yield of succinaldoxime powder is a little over 40 g, mp is 171-172j.
5.8 g of the above powder is placed in a beaker of 250 ml capacity and 54 ml of 10% sulfuric acid is added.
Cool to 0j and add in small portions of 7 g of sodium nitrite (if you add the nitrite too fast, nitrogen dioxide fumes will evolve).
After the dioxime is completely dissolved, allow the solution to warm to 20j and effervescence to go to completion. Neutralize the yellow solution to litmus by adding small portions of barium carbonate.
Filter off the barium sulfate that precipitates. The filtrate is 90% pure succindialdehyde and is not purified further for the reaction to create tropinone. Do this procedure 3 more times to get the proper amount for the next step, or multiply the amounts given by four and proceed as described above.
Take the total amount of succinaldehyde (obtained from 4 of the above syntheses combined) and without further treatment or purification (this had better be 15.5 g of succindialdehyde) put into an Erlenmeyer flask of 4-5 liters capacity.
Add 21.6 g of methylamine hydrochloride, 46.7 g of acetonedicarboxylic acid, and enough water to make a total volume of 2 liters. Adjust the pH to 8-10 by slowly adding a saturated solution of disodium phosphate.
The condensate of this reaction (allow to set for about 6 days) is extracted with ether, the ethereal solution is dried over sodium sulphate and distilled, the product coming over at 113j at 25 mm of pressure is collected.
Upon cooling, 14 g of tropinone crystallizes in the pure state. Tropinone can also be obtained by oxidation of tropine with potassium dichromate, but I could not find the specifics for this operation.
2-Carbomethoxytropinone. A mixture of 1.35 g of sodium methoxide (this is sodium in a minimum amount of methanol), 3.5 g of tropinone, 4 ml of dimethylcarbonate and 10 ml of toluene is refluxed for 30 min. Coo] to 0j and add 15 ml of water that contains 2.5 g of ammonium chloride.
Extract the solution after shaking with four 50 ml portions of chloroform, dry, evaporate the chloroform in vacuo. Dissolve the oil residue in 100 ml of ether, wash twice with a mixture of 6 ml of saturated potassium carbonate and three ml of 3 N KOH.
Dry and evaporate in vacuo to recover the unreacted tropinone. Take up the oil in a solution of aqueous ammonium chloride and extract with chloroform, dry, and evaporate in vacuo to get an oil.
The oil is dissolved in hot acetone, cool, and scratch inside of flask with glass rod to precipitate 2- carbomethoxytropinone. Recrystallize 16 g of this product in 30 ml of hot methyl acetate and add 4 ml of cold water and 4 ml of acetone. Put in freezer for 2l/2 to 3 hours.
Filter and wash the precipitate with cold methyl acetate to get pure product.
Methylecgonine. 0.4 mole of tropinone is suspended in 80 ml of ethanol in a Parr hydrogenation flask (or something that can take 100 psi and not react with the reaction, like stainless steel or glass).
10 g of Raney Nickle is added with good agitation (stirring or shaking) followed by 2- 3 ml of 20% NaOH solution.
Seal vessel, introduce 50 psi of hydrogen atmosphere (after flushing vessel with hydrogen) and heat to 40-50j.
After no more uptake of hydrogen (pressure gauge will hold steady after dropping to its lowest point) bleed off pressure and filter the nickle off, rinse out bottle with chloroform and use this rinse to rinse off the nickle while still on the filter paper. Make the filtrate basic with KOH after cooling to 10j.
Extract with chloroform dry, and evaporate the chloroform in vacuo to get an oil. Mix the oil plus any precipitate with an equal volume of dry ether and filter.
Add more dry ether to the filtrate until no more precipitate forms, filter and add to the rest of the precipitate. Recrystallize from isopropanol to get pure methylecgonine. Test for activity.
If active, skip down to the step for cocaine. If not active, proceed as follows. Stir with activated carbon for 30 min, filter, evaporate in vacuo, dissolve the brown liquid in methanol, and neutralize with 10% HCI acid in dry ether.
Evaporate the ether until the two layers disappear, and allow to stand for 2 hours at 0j to precipitate the title product. There are many ways to reduce 2-carbomethoxytropinone to methylecgonine.
I chose to design a Raney Nickle reduction because it is cheap and not as suspicious as LAH and it is much easier than zinc or sodium amalgams.
Cocaine. 4.15 g of methylecgonine and 5.7 g of benzoic anhydride in 150 ml of dry benzene are gently refluxed for 4 hours taking precaution against H20 in the air (drying tube).
Cool in an ice bath, acidify carefully with hydrochloric acid, dry, and evaporate in a vacuum to get a red oil which is treated with a little portion of isopropanoi to precipitate cocaine.
As you can see, this is quite a chore. The coca leaves give ecgonine, which as you can see, is only a Jump away from cocaine.
If you can get egconine, then dissolve 8l/2 g of it in 100 ml of ethanol and pass (bubble) dry HC1 gas through this solution for 30 min. Let cool to room temp and let stand for another 11/2 hours. Gently reflux for 30 min and evaporate in vacuo.
Basify the residue oil with NaOH and filter to get 8.4 g of methylecgonine, which is converted to cocaine as in the cocaine step above.
Below is given a somewhat easier method of producing tropinone by the general methods of Willstatter, who was instrumental in the first synthetic production of cocaine and several other alkaloids. After reviewing this method, I found it to be simpler than the above in many respects.
Tropinone. 10 g of pyrrolidinediethyl diacetate are heated with 10 g of cymene and 2 g of sodium powder, the reaction taking place at about 160j. During the reaction (which is complete in about 10 min) the temp should not exceed 172j.
The resulting reaction product is dissolved in water, then saturated with potassium carbonate, and the oil, which separates, is boiled with dilute sulfuric acid. 2.9 g of tropinone picrate forms and is filtered.
Here are two more formulas devised by Willstatter that produce tropinone from tropine. Take note of the yield differences.
Tropinone. To a solution of 25 g tropine, dissolved in 10 times its weight of 20% sulfuric acid are added 25 g of a 4% solution of potassium permanganate in 2 or 3 g portions over 45 min while keeping the temp at 10-12j.
The addition of permanganate will cause heat (keep the temp 10-12j) and precipitation of manganese dioxide. The reaction mixture is complete in I hour.
A large excess of NaOH is added and the reaction is steam distilled until I liter of distillate has been collected.
The tropinone is isolated as the dibenzal compound by mixing the distillate with 40 g of benzaldehyde in 500 cc of alcohol and 40 g of 10% sodium hydroxide solution. Let stand several days to get dibenzaltropinone as yellow needles. Yield: 15.5 g, 28%. Recrystallize from ethanol to purify.
Tropinone. A solution of 12 g of chromic acid in the same amount of water (12 g) and 60 g of glacial acetic acid is added dropwise with stirring over a period of 4 hours to a solution of 25 g of tropine in 500 cc of glacial acetic acid that has been warmed to 60-70j and is maintained at this temp during the addition.
Heat the mixture for a short time on a steam bath until all the chromic acid has disappeared, cool and make strongly alkaline with NaOH. Extract with six 500 cc portions of ether and evaporate the ether in vacuo to get an oil that crystallizes readily.
Purify by converting to the picrate or fractionally distill, collecting the fraction at 224-225j at 714 mm vacuo.
The tropinones can be used in the above formula (or in a formula that you have found elsewhere) to be converted to cocaine. Remember to recrystallize the 2-carbomethoxytropinone before converting to methylecgonine. Read More......
How Cocaine Is Made
Manufacturing Cocaine
There are around 250 species of plants in the Erythroxylum (Erythroxylon) genus. At least 17 produce cocaine. Only a few of these 17 species are commonly used for the production of South American cocaine because they produce a larger yield than the others.
Coca can be harvested several (usually 4-6) times a year. Traditionally, chewing the sacred leaf promotes contact with the spirit world. Chewing or smoking coca leaves invigorates the user, allowing the user to absorb the plant's magical powers and protect body and spirit alike.
In its native habitat, the coca plant is resistant to drought and disease. It doesn't need irrigation. The introduction of coca to England was pioneered early in the nineteenth century by the Royal Botanical Gardens at Kew. But the plant has yet to find a place in orthodox western horticulture.
Cocaine could only be taken in leaf form until about 1860. The natural source gives a low dose of cocaine with effects similar to drinking strong coffee. People who chew coca leaves do not often have a serious addiction problem because there is so little cocaine in each leaf.
However, in 1858-1860 cocaine was isolated from the plant material by chemist Albert Niemann at the University of Gottingen in Germany. Shortly after this form of purification was discovered, people began to inhale it (snort) and to inject it.
Cocaine Synthesis
Coca leaves are stripped from the plant and crushed, chopped, and/or pounded and mixed with a solution of alcohol, gasoline, kerosene, or some other solvent that will separate the cocaine from the leaves.
The resulting liquid contains unpurified cocaine alkaloids and may additionally contain waxy material from the leaves. This waxy material can be removed by heating and then cooling the mixture, a process that solidifies the unwanted wax.
The next step is to isolate the cocaine alkaloids from the liquid. This is done with acid and basic mixtures. The alkaloids that are removed in this process are then treated with kerosene.
The kerosene is removed and gas crystals of crude cocaine are left at the bottom of the tank. Typically, the crystals are dissolved in methyl alcohol. They are then recrystallized and dissolved in sulfuric acid, which results in cocaine that is about 60% pure.
It should be noted that cocaine at this point is basically freebase cocaine, very similar to crack. In fact, when a person freebases cocaine, or makes crack, they are reversing what is done in the next process.
What is done next is converting freebase cocaine to a salt called cocaine hydrochloride (regular cocaine). The reasons for converting it to a salt are:
1) If the cocaine was left in this form for long it would lose its potency.
2) To make it water soluble (it does not dissolve well in water unless converted to cocaine hydrochloride). The drug (in hydrochloride form) can be used for injecting or snorting into the bloodstream.
Blood is about 50 percent water, any drug which is injected into the human body must be dissolvable in water. If it is not, it will float around in the body in a non dissolved clump. Such clumps are likely to cause strokes or cardiac arrest (heart attack).
Because of factors like these cocaine is further treated with oxidizing agents to produce a water-soluble form of the drug. This is usually done by further washing, oxidation and separation procedures that involve potassium permanganate, benzole, and sodium carbonate. The result is an odorless, white crystalline powder. It has a bitter, numbing taste.
Freebase and crack cocaine are derived from cocaine hydrochloride that has been chemically treated with ammonia and ether (freebase) or baking soda (crack) to free the potent base material from the salt.
Freebase was originally produced by a dangerous four or five step process in which the hydrochloride salt was heated with water and a volatile liquid such as ether.
Base cocaine in the form of crack is safer to produce than freebase made with ether. Crack and freebase cocaine are not soluble in water, so they can't be injected or sniffed.
Instead, crack and freebase cocaine are usually smoked from pipes, burnt on a piece of tin foil, or mixed with tobacco or marijuana and smoked like a cigarette or joint. Read More......
Information About Coca Leaves
Coca is a densely-leafed plant native to the eastern slopes of the Andes. Erythroxylum coca has been widely cultivated in Bolivia, Peru and Ecuador. It is also been widely cultivated in Columbia, the source of a large percentage of the world's cocaine.
Of the over 200 varieties of coca plant, only three were commonly used for the production of South American cocaine. Colombian coca was used in Colombia. Amazonian coca was used in the Amazon River basin. Huanuco coca was used in Bolivia and Peru.
Typically, coca thrives in warm, moist valleys between 1500 and 6000 meters above sea level. The plant grows to a height of up to eight feet. The leaves are rich in vitamins, protein, calcium, iron and fiber.
The cocaine content of the leaves ranges from 0.1% to 0.9%; like the user, it tends to get higher with altitude. Plants grown at higher altitudes take longer to mature but are more potent than those grown at lower heights.
Some species of the plant can live up to 20 years. Most are ready to produce viable coca leaves within 2 years of sprouting, however some longer living varieties take more time. As the plant ages, the quantity of leaves the plant generates declines.
The leaves must be dried or converted to cocaine soon after harvest, or they will be attacked by mold that will render them worthless as a source of cocaine.
The coca plant's cocaine alkaloid is also a pesticide. Thus evolutionary selection pressure has favored its natural synthesis. Cocaine powerfully inhibits the neuronal reuptake of dopamine; but it is an even more potent inhibitor of the insect-specific neurotransmitter octopamine. Insects that feed on coca overdose on their own octopamine.
Chewing coca counters the symptoms of 'mountain sickness' and oxygen-deprivation. The daily dose of the average coquero is around 200mg, that is a little less than 1/4 gram.
Chewing coca leaves with a dash of powdered lime is a nutritious and energizing way to induce healthy mood without causing an unsustainable high. Unfortunately, it is not very good for one's teeth.
Strictly speaking, the leaves aren't actually chewed. Typically, the dried coca leaf is moistened with saliva. The wad is placed between the gum and cheek and it is gently sucked.
The invigorating juices are swallowed. Lime-rich materials such as burnt seashells or a cereal are used to promote the separation of the leaf's active alkaloid.
Shamans from some traditional Indian tribes still smoke coca leaves for magical purposes. Inhaling the sacred vapors induces a trance-like state.
Coca enables a shaman to cross 'the bridge of smoke', enter the world of spirits, and activate his magical powers. Alas the leaves don't travel well; and this ancient usage is uncommon in the urban industrial West.
Because the US government has (or paid others to) sprayed coca fields in South America with various chemicals to kill coca plants, it is said various new strains have emerged.
Some claim a strain called Boliviana Negra was developed (through selective breeding or genetic lab modification?) to be resistant to the herbicide Roundup (glyphosate). Spraying Boliviana Negra with glyphosate helps it grow faster by eliminating the weeds surrounding it.
In 1996, a patented glyphosate-resistant soybean was marketed by Monsanto, suggesting that it would be possible to genetic modify coca in the same manner. It is not known if Boliviana Negra is a real super-strain of coca that was developed in this manner.
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I read in Licit and Illicit Drugs that the people living in the Andes who chewed coca leaves to deal with the thin air had no trouble stopping use once they moved to a more airy clime.
People interested in checking further into this might be interested in a couple of articles about coca leaf chewing:
By Andrew Bell
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Cocaine Pharmacokinetics in Humans.
The Journal of Ethnopharmacology, 3 (1981) 353-366.
Therefore, on the basis of this new information that has come as a result of technological development we can conclude with a practical observation.
The size of the quid of coca leaves that can be comfortably accommodated by a person is such that it is unlikely that coca chewing, as practiced for centuries in places like Macchu Piccu, presents the dangers that may result from the modern forms of recreational use.
Particularly interesting about this article is that the report came out of the Division of Research of the National Institute on Drug Abuse.
By A. Barnett, R. Hawks, and R. Resnick
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The Therapeutic Value of Coca in Contemporary Medicine.
The Journal of Ethnopharmacology, 3 (1981) 367-376.
I have lived among coca-using Indians of the Andes and the Amazon basin in Columbia and Peru and have not seen any signs of physical deterioration attributable to the leaf. I have never seen an instance of coca toxicity. Nor have I observed physiological or psychological dependence on coca.
Even life-long chewers seem able to get the effect they want from the same dose over time; there is no development of tolerance and certainly no withdrawal syndrome upon sudden discontinuance of use.
By A. Weil Read More......
Cocaine Use
From Chewing Coca Leaves To Crack
Chewing Coca Leaves. Coca consumption was originally the prerogative of the Inca elite. Today, most of the natives indulge as well. Coca is also consumed as the highly esteemed coca de mate.
Drinking coca tea tends to soothe the stomach, so it's good for digestive problems. Coca de mate is less likely to induce jitteriness than coffee. It is a rather more effective mood brightener too.
Cocaine Sulfate - pasta, basuco, basa, pitillo, paste. This is the low grade stuff that reaches the urban slums of South America. The sulfate is the intermediate stage between the coca leaf and the finished cocaine hydrochloride crystal.
Coca leaves are stripped from the plant. They are put in plastic pit with a solution of water and sulfuric acid. A bare footed man will climb in the pit, step on the mess and move it around with his hands.
Cocaine Hydrochloride - an odorless, white crystalline powder. It has a bitter, numbing taste. This is the type of cocaine available in most cities.
Making cocaine hydrochloride is quite complicated. The pasta is first washed in kerosene. It is then chilled. The kerosene is removed. Gas crystals of crude cocaine are left at the bottom of the tank.
Typically, the crystals are dissolved in methyl alcohol. They are then re-crystallized and dissolved once more in sulfuric acid. Further washing, oxidation and separation procedures involve potassium permanganate, benzole, and sodium carbonate.
Freebase And Crack Cocaine. Freebase and crack cocaine are derived from cocaine hydrochloride which has been chemically treated to free the potent base material from the salt.
Freebase was originally produced by a dangerous four or five step process in which the hydrochloride salt was heated with water and a volatile liquid such as ether.
Base cocaine in the form of crack is safer to produce but it is no less addictive. Crack and freebase are indissoluble in water, so they can't be injected or sniffed easily.
Instead, base is usually smoked from pipes, burnt on a piece of tin foil, or mixed with tobacco and marijuana in a smokable joint.
The euphoric rush comes within a few seconds (even faster than from injecting cocaine hydrochloride). Initially, the user may experience a profound sense of power, mastery, cleverness and uninhibited desire. But the exhilaration usually starts to fade within a few minutes.
Cocaine Use
Physical constraints ensure that even the most ardent coquero can get only a modest amount of cocaine into his bloodstream. Coca induced heart-attacks and strokes are thus extremely rare among traditional users.
In recent decades, however, there have been changes in cocaine's route of administration, patterns of use, the technology of cocaine production, and typical dosages.
Crack is actually a less pure sort of freebase cocaine. Unlike old fashioned freebase, however, its production doesn't involve any flammable solvents.
Crack is usually made by mixing two parts of cocaine hydrochloride with one part baking soda in some water. The solution is then heated gently until white precipitates form. Crack is then cut or broken into small rocks weighing a few tenths of a gram.
The traditional method of taking cocaine in the west involved snorting the hydrochloride salt. But absorption through the nasalmucousa is relatively modest.
This is because their surface-area is small and cocaine is vasoconstrictive. Freebase, on the other hand, is smoked and inhaled directly into the lungs. Therefore much higher doses are possible. Inhalation is followed by an intense euphoric rush.
Chronic cocaine use causes a decrease in the production of enkephalin, one of the brain's natural opioids. This in turn causes a compensatory increase in the number of mu-receptors. The number of unoccupied mu-receptors may be associated with the craving and abstinence syndrome.
After chronic exposure to cocaine, the number of post-synaptic dopamine receptors in the CNS is reduced. The amount of dopamine transporter protein is increased.
Tolerance to cocaine's effects does exist over prolonged use; but the extent of this physiological adaptation is relatively modest. The cocaine user still gets high; but in the absence of cocaine, his pre-synaptic neurons sequester dopamine in the synaptic cleft with greater efficiency.
This may induce depression, sometimes severe. Read More......
What Is Crack Cocaine?
Crack is a form of freebase cocaine that is best suited to smoking. Smoking street cocaine (cocaine hydrochloride) is possible but a lot of the cocaine gets destroyed when heated.
Cocaine hydrochloride requires a high temperature to ignite, freebase cocaine requires a much lower temperature to ignite.
Converting cocaine to freebase is fairly easy and the resulting product is ideal for smoking. Very little of the cocaine is destroyed in the heating process when smoking freebase cocaine.
The reason people smoke freebase cocaine is because it provides a feeling that is similar to the effect one gets from injecting cocaine. But smoking freebase cocaine does not require needles.
See how to make crack and freebase cocaine for further information on freebase cocaine. Read More......
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