Cocaine Flashcards
Is cocaine a CNS depressant or stimulant?
CNS stimulant
What are the forms of cocaine? (2)
Crack
Cocaine HCl powder
What locations does cocaine act? (3)
- Local anesthetic, decreases axon signaling
- Acts on the reuptake mechanism on nerve endings, psychoactive drug use
- Affects reuptake of dopamine (addiction due to this), noradrenaline, serotonin
When was cocaine first used?
1844, natives chewed on the leaves of the coco plant
What was cocaine first used as a local anesthetic for?
The eye, dentists used it for teeth too
Where does cocaine come from now?
Mostly Columbia and South America
How is crack cocaine administered?
smoked
How is Cocaine HCl administered?
sniffed or injected
Pharmacodynamics of cocaine, what does it act on (2)?
- Blocks voltage-gated sodium channels – blocks axonal conduction (other sites, heart, conduction of electrical system, all excitable tissue)
- Blocks neurotransmitter reuptake
- Blocks neurotransmitter reuptake
a. Blocks reuptake of dopamine, noradrenaline, serotonin
b. Neurotransmitter/sodium symporter family (sympathetic nervous system is very active)
c. Effect in the reward pathway due to increase in dopamine, since reuptake is blocked
- Blocks voltage-gated sodium channels – blocks axonal conduction (other sites, heart, conduction of electrical system, all excitable tissue)
a. CNS: excitation (convulsions) then Inhibition (respiratory arrest)
b. Rapid administration may produce immediate death
c. Heart: Blocks the SA node or conduction causing cardiac arrest
Cocaine causes CNS excitation causing?
More blood flows to the heart and less to the intestines – fight or flight active
It is rarely used as a local anesthetic anymore
What are the main type of dopamine receptors affected by cocaine?
D2 receptors
administration (smoking or sniffing)?
- Goes to heart then brain very quickly
- No liver first pass
- Blood from the lung does not go through the liver so it gets to the brain very fast
Administration (oral)?
- First pass 75% metabolized, first used by natives of South America, the rise was very slow, not addictive
- Absorption rapid at all parenteral sites (injection)