high efficacy stimulants - cocaine Flashcards
(60 cards)
what is a stimulant?
a drug that increases central nervous system activity and sympathetic nervous system activity (aka known as uppers)
what are low efficacy stimulants? give an example. what would the dose response curve look like?
produces a WEAK response
ex. nicotine and caffeine
dose response: would have a high x axis and low y axis
what are high efficacy stimulants? give an example. what would the dose response curve look like?
produces a STRONG response
ex. amphetamine and cocaine
dose response: would have a low x axis and high y axis
what occurs when stimulants activate the sympathetic nervous system?
it activates your flight or fight
examples:
- dilates pupils
- inhibits salivation
- increases heartbeat
- relaxes airways
-stimulates sweat glands
- relaxes bladder
where does cocaine come from?
it is extracted from the leaves of the coca plant
what are the street names for cocaine?
- crack
- rock
- blow
what schedule drug is cocaine? explain what that schedule indicates.
schedule II - high abuse likelihood but there is accepted medical use
what is the major problem associated with cocaine?
lack of purity
a lot of coke is now contaminated with fentanyl and there is more likelihood to die from it compared to the 80s
what are INSTRUMENTAL uses of cocaine?
topically
when is cocaine used topically?
ENTs use cocaine as a topical anesthetic during eye surgery to numb as well as preventing bleeding.
It can be topically places in nasal passage to treat certain bleeding disorders.
what are other forms of cocaine that is used as a topical anesthetic rather than cocaine itself?
novocain and lidocaine
what is the mechanism of action of cocaine in the body?
cocaine inhibits voltage-gated Na+ channels in axons, blocking nerve conduction soo… when applied locally - transmission of signals along sensory nerves does not occur hence the numbness
what are the forms of cocaine?
- cocaine hydrochloride
- base cocaine (no hydrochloride)
what are characteristics of cocaine hydrochloride?
- white powder
- water soluble
- cocaine alkaloid is extracted from coca leaves & converted into a hydrochloride salt (HCl) & crystalized
what are the 2 types of base cocaine and what are their characteristics?
- freebase
a. dissolve cocaine HCL in water +
ammonia, extract cocaine + organic
solvent (ether) - crack
a. dissolve cocaine HCl in water, mix with
baking soda, heat, dry
know the pharmacokinetic differences between forms of cocaine table on slide 11 - picture is camera roll
what are routes of administration for cocaine?
- nasal (snort)
- IV (mainline)
- inhaled (typically freebased or crack)
- oral
how does route of administration of cocaine affect its bioavailability?
- snorting (intranasal)
absorption: slowly because blood vessels
are constricted
bioavailability: 70% - iv injection
absorption: rapid because it bypasses all
barriers to absorption
bioavailability: 100% - oral
absorption: real slow
NOT COMMON - freebase/crack inhalation
bioavailability: 90%
can cocaine be smoked?
no, it decomposed before it volatizes when heated
what term describes cocaine distribution?
lipophilic – it easily penetrates the BBB and placental barriers
cocaine is a teratogen
what is true regarding cocaine’s movement in blood?
it moves about of blood very rapidly and into brain much quicker due to the fat in the brain. therefore, your concentration in the brain is much higher than the blood. this is why addiction exists because the biological action reaches the brain very quick
is cocaine metabolized only in liver?
no, it is broken down in all different parts of the body
what enzymes break down cocaine in the blood plasma, tissues, and live?
blood plasma: butrylcholinesterase (BChE)
tissue: esterases
liver: CYP3A4 enzyme
when CYP3A4 enzyme in the liver breaks down cocaine, what metabolites are formed?
inactive:
- benzoylecgonine
- ecgonine methyl ester
active:
- norcocaine (acute intoxication)
