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Medicines > fda max : 100 mg/d or 34 mg/d or 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison

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mechanism:
5-HT1A agonist, 5-HT2A antagonist, with weaker activity at D4 and other receptors. Net effect involves enhanced prefrontal dopaminergic/noradrenergic tone with decreased serotonergic inhibition of sexual desire. (1) · Selective inverse agonist at 5HT2A receptors with weaker activity at 5HT2C. Has no significant dopamine D2 affinity, unique among approved antipsychotics. Inverse agonism (rather than antagonism) reduces constitutive 5HT2A receptor activity below baseline. (1) · '"`UNIQ--vote-000000B6-QINU`"' Active metabolite EXP3174 is ~10-40-fold more potent than the parent and accounts for most of the antihypertensive effect; CYP2C9 polymorphism affects conversion'"`UNIQ--ref-000000B7-QINU`"'. (1) · '"`UNIQ--vote-00000117-QINU`"' Compared with omeprazole, pantoprazole has a more linear pharmacokinetic profile and is metabolized predominantly via CYP2C19 with CYP3A4 contribution; less CYP2C19-driven drug interaction with clopidogrel than omeprazole'"`UNIQ--ref-00000118-QINU`"'. (1) · '"`UNIQ--vote-00000762-QINU`"' Largely renally cleared, hence the eGFR-tiered dosing. Rare but well-documented signals: acute pancreatitis (uncertain causal contribution), severe joint pain, and bullous pemphigoid (class effect, especially in older Asian patients)'"`UNIQ--ref-00000763-QINU`"'. (1) · '"`UNIQ--vote-000008E1-QINU`"' Like omeprazole, it is an acid-activated prodrug that covalently and irreversibly binds the H+/K+ ATPase. CYP2C19 PGx remains clinically relevant for both'"`UNIQ--ref-000008E2-QINU`"'. (1)
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