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OPIOID ANALGESICS & ANTAGONIST SUBCLASS Strong opioid agonist Morphine Methadone Fentanyl MECHANISM OF ACTION Strong--receptor agonist

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

Analgesia Relief of anxiety Sedation Slowed GI transit

Like strong agonists Toxicity dependent on genetic variation of metabolism Long duration action 4-8h May precipitate abstinence syndrome Like buprophine

Nalbuphine Antitussives Dextromethorphan

K agonist anatagonist Poorly understood

Like strong agonists but can antagonize their effects Also reduce craving for alcohol Similar to buprenorphine Reduces cough reflex

Moderate pain Some maintenance rehabilitation programs Moderate pain

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

Minimal as taken directed

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

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