PHARM - pharm of abused substances Flashcards
example of pharmacokinetic and pharmacodynamic effect of tolerance
PK: increased enzymes that break down drug (decreased bioavailability)
PD: down regulation of receptors
opioid receptors important for addiction
mu receptors
define opium, opiate, opioid
opium - liquid from poppy plant
opiate - substance derived from opium
opioid - synthetic or partially synthetic with morphine like actions
difference between morphine and codeine
extra methyl group on codeine
contrast morphine and codeine
intake: codein is only oral while morphine is numerous
F: codeine higher, at 90% orally
heroin potency in comparison to morphine
2x
what are the semi-synthetic opioids?
oxycodone (percocet)
hydrocodone (vicodin)
hydrocodone in comparison to oxycodone
- faster onset
- shorter half life
- shorter duration
- pain relief about half of oxycodone
- does not have an active metabolite while oxycodone does
fully synthetic opioids
methadone
suboxone is a combo of…
buprenorphine and naloxone
discuss how buprenorphine works
very strong affinity for mu receptor so it knocks off heroin and methadone, and it takes a long time to dissociate, but it is only a partial agonist, whereas methadone and heroin are full agonists, so buprenorphine can induce withdrawal if it is displacing a full agonist
early opiate withdrawal signs
Lacrimation Yawning Rhinorhea Sweating Sense of anxiety and doom (leads to desperate measures)
middle opiate withdrawal signs
Restless sleep Dilated pupils (mydriasis) Anorexia Gooseflesh Irritability Tremor
late opiate withdrawal signs
Increase in all previous signs and symptoms Increase in heart rate and BP Nausea, vomiting, diarrhea Abdominal cramps Depression Muscle cramps Weakness Bone pain
contrast the mechanisms of cocaine and amphetamine
they have equivalent effects
cocaine blocks presynaptic DA reuptake transporter
amphetamines enter DA neurons via reuptake and then interact intracellularly to cause DA reverse transport into synaptic cleft
