28 opioids drugs Flashcards
what is the edogenous ligand for the Mu receptor?
beta-endorphins
how do opiod receptors work when an endogneous binds to them?
they are Gi .
when the ligand binds to them they decrease the activity of adenylate cyclase.
this decrease the amount of cAMP
increase efflux of K
leads to decrease of influx of Ca.
there is alot less neurotransmitter released.
what is the edogenous ligand for Kappa?
dynorphins
what is teh endogenous ligand for delta?
enkephalins
what drugs are activated by metabolism?
codeine and heroin
what opioids are also cough suppresants?
Codeine, hydrocodone and dextromethorphan
what drugs go thorgh extensive first pass effects?
morphine and naloxone.
μ agonist
with a Low oral to parenteral potency ratio - about 3 or 4 to 1
morphine
More lipophilic than morphine.
?
heroin
what mu agonists are for mild to moderate pain?
and often used in combination with NSIAD or acetominophen?
codeine hydrocodone oxycodone
mu agonist
Equipotent with morphine; has good oral availability
Longer duration of action
methadone
mu agonist
Shorter duration of analgesia than morphine
Forms toxic metabolite, normeperidine, that can accumulate with frequent use
Interactions with MAO inhibitors
Meperidine
μ agonist
100 X as potent as morphine
Short-acting – 1 to 1.5 hours
fentanyl
2-3 X as potent as morphine
hydromorphone
μ antagonist and kappa agonist
Similar in efficacy and potency to morphine
Much lower abuse potential
nalbuphine
Partial μ agonist
Used to treat moderate to severe pain – now available as patch
Oral buprenorphine combined with naloxone (Suboxone®) is used to treat opioid dependence
buprenorphine
opioid antagonist
High affinity for μ receptors. Significantly less for kappa and delta
Much greater activity parenterally than orally
Short duration of action – 1 to 2 hours
Used to treat opioid overdoses
naloxone
opioid antagonist
Orally active with long half-life
Can be used in treatment of alcoholism and opiate addiction
naltrexone
Antitussive, but not analgesic. Also is an NMDA antagonist.
dextromethorphan
weak mμ agonist. Also blocks NE and 5-HT uptake
- Used for mild to moderate pain
available in oral form
tramadol
what drug can you use for opioid abuse?
suboxone
