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morphine, heroin, codeine, fentanyl Mu receptor agonists pentazoicine kappa agonists and mu partial agonists, can percipitate withdrawal effects in addicts; don't give c full agonist naloxone, naltrexone Mu, kappa, a& sigma receptor Antagonist codeine, meperidine, propoxyphene produce convulsions c OD Morphine prodrug for opioids; stimulates all opiate receptors; administered IV, IM, buccal; T1/2: 1.5-2 hrs; metabolized by CYP450, can be conjugated to c glucuronic acid Hydrocodone semisynthetic codeine derivative, must be metabolized to be active, antitussive, analgesic (when combined c others) Oxycodone semisynthetic codeine derivative, must be metabolized to be active, used to treat moderate pain and non-pain conditions like Restless leg and Tourette's Meperidine (demerol) analgesic for healthy pts or those that cannot tolerate other opioid agonists. Used for very brief duration; has antimuscarinic effect, dilates pupils, no antitussive; prevents reuptake of 5-HT; metabolites can cause seizures and degeneration of dopmaninergic neurons. Methadone slow onset, very long duration of action; used for chronic moderate to severe pain; used to maintenance of heroin addicts; mild withdrawal symptoms Fentanyl very potent, rapid onset opioid for induction & maintenance of general anesthesia. Can be given IV, oral, or transdermally, zero order kinetics Alfentanil very fast onset, with short duration of action, 1st order elimination, metabolized by CYP3A4 Heroin schedule 1 drug, not used medically in US Codeine very good antitussive effect, most commonly used analgesic, metabolized by CYP2D6 to its active form; inhibited by SSRIs Propoxyphen high dose needed for analgesic effect, produces lots of severe side effect: cardiac toxicity, psychosis, seizures Buprenorphine partial agonist at mu receptors, provides relief of moderate to severe pain, reduces drug cravings in heroin addicts Tramadol weak mu agonist, used for mild to moderate pain; inhibits reuptake of NE and 5-HT, minimal opioid side effects, not completely reversed by naloxone Dextromethorphan antitussive used in OTC preparation, C/I in MAOIs Naloxone pure opioid antagonist; DOC for opioid OD, may percipitate withdrawal, repeated doses may be required, lasts 2 hrs Naltrexone long lasting opioid antagonist, given orally; risk of hepatoxicity, pt must be detoxed before administration Nalmefene similar to naloxone, but longer duration of action (2-6hrs)