Moderate and other opioid agonists Flashcards
Moderate opioid agonists - 3 drugs
Codeine
Hydrocodone
(Propoxyphene - removed)
Moderate opioid agonists - adm
Oral with nonopioid analgesic. High dose cause intolerable side effects.
Moderate opioid agonists - indications
Mild to moderate pain
Alleviate or prevent coughing.
Codeine - MOA
Most of the therapeutic effect is caused by metabolism to morphine.
Explain the different effect of codeine and hydrocodone in different patients.
Most of therapeutic effect caused by metabolism to morphine. Pts deficient in CYP2D6 have little pain relief. Pts who are ultra-rapid metabolizers may have a higher peak, and cause intoxication of fetus/infant if pregnant/nursing.
Other opioid agonists
Tramadol Tapentadol Dextromethorphan Diphenoxylate Loperamide
Tramadol - MOA
Dual-action analgesic: agonist at μ receptors and inhibits neuronal reuptake of serotonin and norepinephrine.
Analgesic effect is only partially inhibited by opioid antagonists.
Tramadol - indications
Moderate pain.
Chronic pain syndromes
Tramadol - side effects
Lowers seizure threshold
Increased risk of suicidal thoughts and behaviors.
Tapentadol - MOA
Acts on μ receptors and inhibit NE reuptake.
Dextromethorphan - indications
Antitussive (little analgesic effect).
Used with quinidine for psuedobulbar affect in neurodegenerative disease.
Opioids used for diarrhea
Diphenoxylate and loperamide.