Wk 26 - Cocaine Flashcards
What is cocaine?
- Psychoactive alkaloid of coca plant
- Addictive stimulant drug
- CNS effects similar to amphetamines
- Local anesthetic + vasoconstrictor
What are the 2 forms of illegal cocaine?
- Cocaine base (crack): difficult to dissolve for injection, smoked bc low MP
- Cocaine salt: readily injected or snorted, highly water sol
Give examples of inert fillers used as adulterants
- Dextrose
- Lactose
- Mannitol
- Starch
Give examples of active chemicals used as adulterants
- Benzocaine
- Lidocaine
- Procaine
- Ephedrine
- Amphetamine
- Caffeine
What are the contaminants found in street cocaine?
- Benzene
- Acetone
- Sodium carbonate
What is the common cocaine adulterant + what are the side effects?
Levamisole:
- Leucopenia
- Agranulocytosis
- Cutaneous vasculitis
What are the peak concentration of cocaine after smoking, injecting + intranasal?
- 5-10 mins: injection/smoking
- 60 mins: intranasal
Which is shorter acting, cocaine or amphetamines?
Cocaine
What are the major metabolites of cocaine?
- Benzoylecgonine
- Ecgonine methyl ester
What are the minor metabolites of cocaine?
- Norcocaine
- P-hydroxycocaine
- M-hydroxycocaine
How does cocaine produce anesthesia?
Inhibit excitation of nerve endings or blocking conduction in peripheral nerves
What are the mechanism of action of cocaine?
- Vasoconstriction
- Reversibly binds + inactivates sodium channels
- Affects cardiac myocytes by blocking sodium channels
What is the primary site of action of cocaine?
- Dopamine uptake transporter
- Block DAT, inc dopamine, mediates rewarding effect of cocaine
What other site of action does cocaine act on?
- Inhibits VTA GABA neurons -. disinhibits VTA DA neurons
- DA binds to post synaptic D1 receptor + regulates Glue transmission via NMDA + AMPA receptors
- Cocaine activates pre/postsynaptic D1 receptor -> inc Glu transmission
- Glu: triggers relapse
What are the short term effects of cocaine?
- Main: extreme happiness, alertness, hypersensitivity to sight + paranoia
- Other: constricted blood vessels, dilated pupils, nausea, raised temp + BP