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Showing posts with label A. Show all posts

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......