Pharm 2: Opioids

opioid receptor agonist
MOA: inhibition of adynylyl cyclase (dec cAMP, increase K conductance)
SE: respiratory depression, inc. intracranial pressure, N/V
Vaso dilator, metabolite more potent so adds to anaglesia

opioid receptor agonist
MOA: inhibition of adynylyl cyclase (dec cAMP, increase K conductance)
SE: respiratory depression, inc. intracranial pressure, N/V
inc. oral potency, less resp. depression, DOC for OB

opioid receptor agonist
MOA: inhibition of adynylyl cyclase (dec cAMP, increase K conductance)
SE: respiratory depression, inc. intracranial pressure, N/V
very long 1/2, used in treatment of heroin addiction and opioid withdrawal

opioid receptor agonist
MOA: inhibition of adynylyl cyclase (dec cAMP, increase K conductance)
SE: respiratory depression, inc. intracranial pressure, N/V
80X more potent than morphine, muscular rigidity, TD patch

opioid receptor agonist
MOA: inhibition of adynylyl cyclase (dec cAMP, increase K conductance)
SE: respiratory depression, inc. intracranial pressure, N/V
analgesic effect via metabolism to morphine, w/ NSAIDs for cough

opioid receptor agonist
MOA: inhibition of adynylyl cyclase (dec cAMP, increase K conductance)
SE: respiratory depression, inc. intracranial pressure, N/V
=potent, inc. oral avail than morphine, combo w/ NSAIDs (oxycontin)

opioid receptor agonist
MOA: inhibition of adynylyl cyclase (dec cAMP, increase K conductance)
SE: respiratory depression, inc. intracranial pressure, N/V
1/2 potent as codeine, can have toxic build-up, cause irritation through IV

Mixed opioid agonist/antagonist
MOA: Mu R antagonist, kappa R agonist
SE: less resp. depression, increased HR, BP, catecholamines

Mixed opioid agonist/antagonist
MOA: Mu R antagonist, kappa R agonist
SE: less resp. depression, increased HR, BP, catecholamines

unique in this class as doesn't exhibit significant cardiac effects
less likely to produce dysphoric effects

Mixed opioid agonist/antagonist
MOA: Mu R antagonist, kappa R agonist
SE: less resp. depression, increased HR, BP, catecholamines
nasal spray

Mixed opioid agonist/antagonist
MOA: Mu R antagonist, kappa R agonist
SE: less resp. depression, increased HR, BP, catecholamines
slow onset, long duration

Opioid Antagonists
MOA: blocks opioid R's (Mu best)
Gold standard, Tx or eval of opioid OD
used for neonatal resp. depression and mother takes opioids

Opioid Antagonists
MOA: blocks opioid R's (Mu best)
higher oral efficacy than Naloxone
used as oral maintenance of opioid addicts, alcoholism

Codeine: depresses medulla cough center
Dextromethorphan: depresses medulla cough center
Diphenoxylate: depresses medulla cough center
Loperamide: no CNS effects