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Drilldown: Medicines

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

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mechanism:
None (4) · 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 alpha-1 adrenergic receptor antagonist. Lowers peripheral vascular resistance via vasodilation; in the CNS, blunts noradrenergic hyperarousal thought to drive trauma-related nightmares. (1) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (1) · TrkB/BDNF'"`UNIQ--ref-00000040-QINU`"' '"`UNIQ--vote-00000041-QINU`"' (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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