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Variable affinity for K receptors EFFECTS CLINICAL APPLICATIONS PHARMACOKINETICS & TOXICITIES First-pass effects Duration 1-4h except methadone,4-6h Respiratory depression Severe constipation Addiction liability Convulsions DOSE
Severe pain Adjunct in anesthesia (fentanyl & morphine) Pulmonary edema (morphine) Maintenance rehabilitation programs (methadone) *Hydromorphone, oxymorphone: Like morphine in efficiency, but higher potency *Meperidine: Strong agonist with anticholinergic effects *Sufentanil, alfentanil, remifentanil: Like fentanyl but shorter duration of actions Partial agonists Codeine Less efficacious than Like strong agonist Mild-moderate pain Hydrocodeine morphine Weaker effects Cough (codeine) Can antagonist strong agonist Mixed opioid agonist-anatagonist Buprenorphine Partial agonist K antagonist
Like strong agonists Toxicity dependent on genetic variation of metabolism Long duration action 4-8h May precipitate abstinence syndrome Like buprophine
Like strong agonists but can antagonize their effects Also reduce craving for alcohol Similar to buprenorphine Reduces cough reflex
Acute debillating
30-60min duration
but strong and partial agonists are also effective Codein, levopropoxyphene : Similar to dextromethorphan Opioid antagonists Naloxone Antagonist for all Rapidly antagonizes receptors all opioid effects
cough
Opioid overdose
Duration 1-2 h (may have to be repeated when treating overdose ) May precipitate abstinence syndrome in dependent user
Naltrexone,nalmefene: Like nalaxone but longer duration of action (10+h); Naltrexone used in maintenance programs and can blocks heroine effects for up to 48h Alvimopan,methylnaltrexone bromide: Potent antagonist with poorly enter to CNS;can be used to treat severe opioid-induced constipation without precipitating an abstinence syndrome Other analgesics used in moderate pain Tramadol Mixed effects: weak Analgesia Moderate pain Durations 4-6h agonist, moderate Adjunct to opioids in SERT inhibitor, weak chronic pain Seizures NET inhibitor syndromes
Basic pharmacology of the opioid analgesics Source: Papaver somniferum & P album -> crude opium have many alkaloids-> morphine->codeine Full agonist, partial agonists, antagonist & mixed