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14 Cards in this Set

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Morphine
Mechanism: mu opioid receptor opens K and less Ca -> adenylate cyclase inhibition -> reduced transmitter release
Dorsal horn has opioid receptors that gate nociceptive input (these receptors receive input from 5-HT and NE)

Clinical Use: analgesia without loss of consciousness, continuous dull pain better relieved than sharp intermittent, cough suppression

Side Effects: prominent physical dependence (less severe than ethanol, barbiturates, and some BDZs), cross tolerance
respiratory depression (even low dose), resulting BP fall, constriction of pupils (miosis) useful for abuse diagnosis, hypotension only in hypovolemic patients, nausea, constipation, epigastric pain, and micturition
Naloxone
Naltrexone
Repeated injections of small dose of this opiate receptor antagonist.
May precipitate withdrawal in those who are dependent.
Naloxone given i.v.
Naltrexone, longer T1/2, orally given
NSAIDs + opiates
analgesic effects are additive
in some situations NSAIDs may be more analgesic
Codeine
Mechanism: methylated morphine, demethylated into morphine

Clinical Use: analgesic, cough suppressant
Hydromorphone
Oxymorphone
identical to morphine but more potent
Oxycodone
Hydrocodone
Mechanism: equipotent and better absorbed than morphine

Clinical Use: anti-tussive, analgesic-antipyretic mixtures
Heroin
Mechanism: acetylated morphine, deacetylated to morphine, high lipid solubility so rapid penetration through BBB
Miperidine
Mechanism: shorter duration of action than morphone

Clinical Use: obstetrical analgesia; less spasmogenic, less constipation/micturition, and less respitory depression than morphine
Diphenoxylate
Mechanism: insoluble -> little abuse potential, no CNS effect at therapeutic dose

Clinical Use: diarrhea treatment in combo w/ atropine
Fentanyl
80x more potent than morphine
patch for cancer patients
Methadone
Mechanism: better bioavailability than morphine, longer T1/2, less withdrawal

Clinical Use: superior to morphine, moderate to sever pain, replacement therapy for opiate addiction
Propoxyphene
less effective than codeine
mild to moderate pain
less abuse liability than codeine
Pentazocin
Mechanism: partial my agonist, powerful kappa agonist, 1/2 to 1/5 as potent

Clinical Use: analgesic

Side Effects: less respiratory depression, higher dysmorphic effect (anxiety, nightmares, hallucination), increase BP and HR
Clonidine
reduce acute phase of opiate withdrawal symptioms
also reduce psychological craving