Exam 2: Cocaine Flashcards
produce modest stimulatory effects in the CNS
nicotine, caffeine, not scheduled
low-efficacy stimulants
increase CNS activity by a significant amount
strong behavioral effects
addiction liability greater
abuse potential inc
high-efficacy stimulants
cocaine
psychoactive substance extracted from leaves of coca plant
- coca leaves have 0.6-1.8% cocaine
- coca paste extracted from soaked and mashed leaves has 60-80% cocaine
- discovered and processed in 1860s
cocaine created from coca paste
2nd most abused controlled substance
cocaine
what schedule drug is cocaine
schedule 2 drug
- high potential for abuse
- known established medical uses
- severe psychological or physical dependence liability
major current problem with cocaine
lack of purity!!
it is laced with ther substances only 50% is actually cocaine
- phentanol is a common laced substance - lethal = toxic
forms of cocaine
cocaine salt, cocaine HCl : mixture of coca paste with HCl, readily water soluble
basic cocaine:
- freebase: dissolve cocaine HCl and ammonia, extract cocaine and ether (organic solvent)
crack: dissolve cocaine HCl mix with baking soda, heat, dry
absorption of cocaine
route of administration:
- nasal (insufflation, snorting) - cocaine HCl
- IV injection, mainlined
- inhalation, smoking
- oral - rare since poor bioavailability
nasal absorption of cocaine HCl
- bioavailability, onset of action, peak levels in brain, duration of action
bioavailability: 70%
onset: 30s-5min - snorting cocaine constricts blood vessels, slowing the absorption
peak in brain: 10-20 min
duration of action: 60-90 min
injection absorption of cocaine HCl
bioavailability, onset of action, peak levels in brain, duration of action
bioavailability: 90%
onset: 10-60s
peak in brain: 3-5min
duration of action: 20-60 min
another absorption f cocaine HCl besides nasal and injection
topical
inhalation absorption - freebase/crack cocaine
bioavailability, onset of action, peak levels in brain, duration of action
bioavailability: 90%
onset: 1-2s
peak in brain: 10s-30min
duration of action: 5-15 min
distribution of cocaine
cocaine = lipophillic - easily penetrates BBB and placental barrier
brain concentrations FAR exceed blood plasma levels
- important for addiction - bc of the speed
metabolism of cocaine
rapidly broken down in about 2 hrs
by enzymes in BLOOD and liver into metabolites
cocaine metabolites
benzoylecognine - broken down in bloodstream, inactive metabolite
ecgnonine methyl ester - broken down in liver - inactive metabolite
norcocaine - active metabolite broken down in liver - cytochrome p450s
- acute intoxication
metabolism: alcohol and cocaine
alcohol slows cocaine metabolism
react together to form cocaethylene - greater effects than cocaine
cocaethylene
- only known example where body forms new psychoactive compound from 2 others
- longer half life, but lower LD50
- more euphoria, increased cardiac toxicity
- seizures, liver damage, compromised immune system
elimination of cocaine
-SLOWLY removed from brain but RAPIDLY removed from blood
1-5% excreted unchanged in urine
rapid fall of blood cocaine level: rush followed by a crash