Cocaine Flashcards
What was the original use of cocaine that Freud recommended?
It was originally an anesthetic, and Freud recommended it to treat depression and addiction.
Where did cocaine come from?
It is a natural product of the coca plant, that comes from South America. Locals chew the leaves with lime to increase extraction. It is a very complex molecule and hard to synthesize. Cocaine = benzooylmethylecgonine
Explain the production process:
Extract the leaves and they get put a giant bin, stomp on the leaves and add a solvent (kerosine or gasoline) to break up the structure. Then they dry it up so the solvent evaporates and left with about 75% cocaine paste
What is cocaine hydrochloride?
Refinement of the paste and can result in salt. It is polar and soluble in water. Makes transporting easier
What is cocaine usually cut with to maximize profit?
It can be cut with any white powdered substance: powdered milk, baby laxative or other number anesthetics like lidocaine or benzocaine (to produce the similar freezing effect as cocaine)- tricks them into thinking its pure cocaine
What are the consequences of cutting with Levamisole? What is levamisole?
Its an anti-parasitic drug usually given to cattle. It produces purpura which leads to necrosis of tissue due to vasculitis.
How quick is the onset of insufflation and how long do the effects last for?
Onset of about 3-5 mins. and effects last for about 30-40 mins. It is absorbed through the mucous membrane
How quick is the onset of IV injection and how long does it last for?
Onset of about 15-30 seconds but effects only last for about 10-20 mins, this administration delivers a rapid large peak. But severe vasoconstriction and necrosis and a danger if needle goes into artery
What is freebase cocaine?
Trying to smoke cocaine hydrochoride with a cigarette, it doesn’t work because it will burn the cocaine before it produces vapours, so you don’t really get any high from this way. You must dissolve the cocaine in water and then add a base (ammonia), extract with ether and then evaporate to dryness for the cocaine to vaporize before it burns
What is crack cocaine?
It is dissolved in low purity cocaine in water, add baking soda, heat up, the freebase will precipitate and can be purified
What is the quickest method of administration?
Smoking gets into the brain the fastest, with onset of 6-10 seconds. Its very intense and short duration
Which enzyme metabolizes cocaine in the blood and liver?
Carboxylesterase
Which metabolite of taking cocaine with alcohol is damaging to the heart muscle?
Cocaethylene
Which two major metabolites are tested in urine for the presence of cocaine? And how long can those metabolites be tested in urine for?
Benzoylecgonine and methylecgonidine, and can be detected in urine for up to 4 days
What is 1 half life of cocaine?
1 hour
What are the psychological effects of cocaine?
Extreme euphoria, energy, hyperactivity and hyper sexuality, confidence. But can develop psychosis and can be dangerous
What are some physiological effects of cocaine?
Local anesthetic by blocking sodium channels and prevents nerve conduction (no pain signals). The sympathetic nervous system is stimulated due to excess NT in synapses, increased heart rate and BP, anorexia and insomnia
How does cocaine cause an accumulation in the synapse?
It blocks the transporter proteins for the re uptake of NT of the presynaptic membrane, so there is prolonged and higher stimulation of the post synaptic receptors–> build up of NT and dopamine in the NA
Which groups on the cocaine structure might mimic the same groups found on dopamine?
The aromatic ring and nitrogen might mimic dopamine
Which receptor does cocaine inhibit on the presynaptic membrane?
The DAT transporter receptor. This receptor uptakes the remaining dopamine back into the pre synaptic membrane so recycle it. Once dopamine has activated the post membrane, it can’t be reused. So you can actually run out of dopamine–> lead to Parkinson’s
What does the excess dopamine in the synapses cause?
Causes increased levels of dopamine in the NA–> high reward
Which other NT probably contribute to the effects of cocaine?
Build up of noradrenaline (increase in energy) and serotonin (elevation in mood)
Why is hyperthermia dangerous when taking cocaine? What causes it?
Its caused by the hyperactivity when taking cocaine combined with vasoconstriction. This prevents you from loosing heat
What can hyperthermia lead to in chronic users?
Rhabdomyolosis, the breakdown of tissues, which causes myoglobinuria, myoglobin in urine which can lead to kidney failure
What happens to your heart when you take cocaine?
Due to the stimulation of the sympathetic system, your heart and body needs more oxygen but it can’t supply it due to the vasoconstriction, less blood flow causes ischemia and parts of tissue start to die off –> myocardial infarction (heart attack)
What percent of all heart attack patients between 18-45 years old is associated with cocaine use?
About 25%
How severe are cocaine withdrawal symptoms? What are they?
Not as severe as alcohol or sedative withdrawal, and the most prominent characteristic and depression
What is a good cocaine treatment? Give an example
Any treatment that increases GABAergic activity are efficacious, they reduce the release in reward pathways. An example is gamma-vinyl-gabs (vigabatrin), or topiramate
