Class#10-Stimulants and cocaine

Question 1

Cocaine pharmacodynamics?

Answer 1

1. Blocks amine reuptake at synaptic cleft. Particular effect on dopamine reuptake. Block reuptake transporter that takes 2 K= in and 3 Na+ out and dopamine same time.
2. Blocks voltage gated sodium channels present on axons = local anesthetics

Question 2

Cocaine toxicity?

Answer 2

1.Convulsion, inhibition, block SA node

Question 3

Dopaminergic receptors? categories?

Answer 3

GCPR. D1-like and D-2like

Question 4

Metabolism, enz + metabolite

Answer 4

PO very high first pass.

Human Carboxylesterase 1 enzyme which cause esterification + some P450. Metabolite = Benzoylecgonine

Question 5

Distribution

Answer 5

Easily pass BBB.

Heart: Decrease blood supply but activete workload

Question 6

EtOH + cocaine

Answer 6

Cocaethylene

Question 7

Agitated delirium?

Answer 7

Not high dose and rapidly fatal, D2 receptor involved in temperature control resulting in fatal hyperthermia

Question 8

Chronic use? + effect on glutamate receptors.

Answer 8

1. Post synaptic become more sensitize to dopamine
2. First reduce AMPA to counteract effect of cocaine on dopaminergic system. Then increase AMPA with chronic use. And now lets in CA+ an NA+ instead of just NA+
3. Tremor and longer reaction time.
4. Tructural change in dentrites: expansion of nerve, increase number of receptors, nerve terminal may also shrink.

Question 9

Amphetamines action

Answer 9

1. Increase release of dopamine and noradrenaline
2. Blocks reuptake of amine
3. Block MAO

Question 10

Differential tolerance?

Answer 10

Tolerant to certain effect but not to others. In amphetamines can never overcome hyperactive effects

Question 11

MDMA

Answer 11

mostly block 5-HT reuptake

Question 12

Herbal extasy

Answer 12

Ephedrine

Question 13

Caffeine

Answer 13

Competititve antagonist of adenosine receptors. Adenosine inhibits release of NT. INhibiting the inhibitor.
INcrease cholinergic pathways