Cocaine

Question 1

What was the original use of cocaine that Freud recommended?

Answer 1

It was originally an anesthetic, and Freud recommended it to treat depression and addiction.

Question 2

Where did cocaine come from?

Answer 2

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

Question 3

Explain the production process:

Answer 3

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

Question 4

What is cocaine hydrochloride?

Answer 4

Refinement of the paste and can result in salt. It is polar and soluble in water. Makes transporting easier

Question 5

What is cocaine usually cut with to maximize profit?

Answer 5

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

Question 6

What are the consequences of cutting with Levamisole? What is levamisole?

Answer 6

Its an anti-parasitic drug usually given to cattle. It produces purpura which leads to necrosis of tissue due to vasculitis.

Question 7

How quick is the onset of insufflation and how long do the effects last for?

Answer 7

Onset of about 3-5 mins. and effects last for about 30-40 mins. It is absorbed through the mucous membrane

Question 8

How quick is the onset of IV injection and how long does it last for?

Answer 8

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

Question 9

What is freebase cocaine?

Answer 9

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

Question 10

What is crack cocaine?

Answer 10

It is dissolved in low purity cocaine in water, add baking soda, heat up, the freebase will precipitate and can be purified

Question 11

What is the quickest method of administration?

Answer 11

Smoking gets into the brain the fastest, with onset of 6-10 seconds. Its very intense and short duration

Question 12

Which enzyme metabolizes cocaine in the blood and liver?

Answer 12

Carboxylesterase

Question 13

Which metabolite of taking cocaine with alcohol is damaging to the heart muscle?

Answer 13

Cocaethylene

Question 14

Which two major metabolites are tested in urine for the presence of cocaine? And how long can those metabolites be tested in urine for?

Answer 14

Benzoylecgonine and methylecgonidine, and can be detected in urine for up to 4 days

Question 15

What is 1 half life of cocaine?

Answer 15

1 hour

Question 16

What are the psychological effects of cocaine?

Answer 16

Extreme euphoria, energy, hyperactivity and hyper sexuality, confidence. But can develop psychosis and can be dangerous

Question 17

What are some physiological effects of cocaine?

Answer 17

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

Question 18

How does cocaine cause an accumulation in the synapse?

Answer 18

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

Question 19

Which groups on the cocaine structure might mimic the same groups found on dopamine?

Answer 19

The aromatic ring and nitrogen might mimic dopamine

Question 20

Which receptor does cocaine inhibit on the presynaptic membrane?

Answer 20

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

Question 21

What does the excess dopamine in the synapses cause?

Answer 21

Causes increased levels of dopamine in the NA–> high reward

Question 22

Which other NT probably contribute to the effects of cocaine?

Answer 22

Build up of noradrenaline (increase in energy) and serotonin (elevation in mood)

Question 23

Why is hyperthermia dangerous when taking cocaine? What causes it?

Answer 23

Its caused by the hyperactivity when taking cocaine combined with vasoconstriction. This prevents you from loosing heat

Question 24

What can hyperthermia lead to in chronic users?

Answer 24

Rhabdomyolosis, the breakdown of tissues, which causes myoglobinuria, myoglobin in urine which can lead to kidney failure

Question 25

What happens to your heart when you take cocaine?

Answer 25

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)

Question 26

What percent of all heart attack patients between 18-45 years old is associated with cocaine use?

Answer 26

About 25%

Question 27

How severe are cocaine withdrawal symptoms? What are they?

Answer 27

Not as severe as alcohol or sedative withdrawal, and the most prominent characteristic and depression

Question 28

What is a good cocaine treatment? Give an example

Answer 28

Any treatment that increases GABAergic activity are efficacious, they reduce the release in reward pathways. An example is gamma-vinyl-gabs (vigabatrin), or topiramate