opioids Flashcards
opium derivatives
morphine 10%
Codeine <1%
Thebaine
Harrison Narcotic Tax Act of 1914
US law that regulated and taxed the production, importation, and distribution of opiates. eventually was extended into modern drug laws.
US Drug Schedule I
No Medical use
LSD, MDMA, heroin
US Drug Schedule II
High abuse potential
amphetamine, morphine
US Drug Schedule III
Moderate abuse potential
ketamine, codeine
US Drug Schedule IV
Mild Abuse Potential
benzodiazepines
US Drug Schedule V
Low abuse potential
buprenorpine
semisynthetic Opioids
- heroin (diacetylmorphine)
- hydromorphone (Dilaudid)
synthetic Opioids
- Methadone (Dolophine)
- Meperidine (Demerol)
- Propoxyphene (Darvon)
- fentanyl (innovar)
Endogenous opioids
enkephalins
endorphins
dynorphins
criteria for opioid agonist classification
Exerts effects similar to morphine
Acts at opioid receptors
Effects blocked by antagonist, Naloxone
Naloxene
Opioid antagonist
other name is narcan
- reverses effects of opioid agonists
- precipitates withdrawal in users
Naltrexone (Trexan)
long acting form of opioid antagonist
opioid administration
weak base
- oral
- parenteral
- inhalation
- intranasal
opioid administration
onset and duration of action
depends on preperation
route of administration
metabolism
opioid receptors
metabotropic, inhibitory
inhibits formation of cyclic amp
post synaptic inhibition - k+ Efflux
Presynaptic inhibition - transmitter release
Autoreceptor activation - less transmitter release`
presynaptic inhibition
kappa receptors - Ca++ channels close - Reduced transmitter release
Autoreceptor activation
Autoreceptors - Ca++ channels close - Reduced Transmitter release
endogenous opioids
endomorphin - Mu receptor
Enkephalin - Proenkephalin precursor - Mu, Delta receptor
Dynorphin - Prodynorphin precursor, Kappa receptor
Endorphin - POMC precursor - Mu, Delta receptor
opioid Acute effects
cortex
sedation
drowsiness
relaxation