Drilldown: Medicines

None (1) · Finasteride (1) · Flibanserin (1) · Linagliptin (1) · Losartan (1) · Sitagliptin (1)

Addyi (1) · Cozaar (1) · Januvia; with metformin Janumet/Janumet XR (1) · Nuplazid (1) · Proscar (5 mg, BPH), Propecia (1 mg, alopecia) (1) · Tradjenta; with metformin Jentadueto (1)

Multimodal serotonergic; HSDD treatment (1) · Selective 5HT2A inverse agonist (with weaker 5HT2C inverse agonism) (1) · [[:Category:5-alpha-reductase_inhibitors|5α-reductase inhibitor]] (1) · [[:Category:Androgen_modulators|Androgen modulator]] (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (2) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:BPH_treatments|Benign prostatic hyperplasia treatment]] (1) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (2)

None (2) · 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-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)

Hallucinations and delusions associated with Parkinson's disease psychosis (PDP). Investigational for psychosis in other dementias and as augmentation for depression. (1) · '"`UNIQ--vote-000000B8-QINU`"', '"`UNIQ--vote-000000B9-QINU`"', '"`UNIQ--vote-000000BA-QINU`"', '"`UNIQ--vote-000000BB-QINU`"' (1) · '"`UNIQ--vote-000002C1-QINU`"' (1) · '"`UNIQ--vote-0000052E-QINU`"', '"`UNIQ--vote-0000052F-QINU`"', '"`UNIQ--vote-00000530-QINU`"' (1) · '"`UNIQ--vote-00000764-QINU`"' (1) · '"`UNIQ--vote-0000117B-QINU`"' (1)

100 mg at bedtime daily (1) · 100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (1) · 34 mg PO once daily (1) · 5 mg PO daily for BPH; 1 mg PO daily for androgenetic alopecia (1) · 5 mg PO once daily (no renal dose adjustment, unlike sitagliptin) (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1)

1 mg, 5 mg tablets (1) · 10 mg, 34 mg capsules/tablets (1) · 100 mg tabs (1) · 25 mg, 50 mg, 100 mg tablets (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 5 mg tablets; combination with metformin (1)

None · Indication-specific · 40 mg/d · 10 mg/d · 20 mg/d · 80 mg/d · 10 mg/d (adults) · 100 mg/d · 4 g/d · 400 mg/d · 40 mg/d typical; up to 240 mg/d for Zollinger-Ellison · 5 mg/d · 50 mg/d · 600 mg/d · No fixed ceiling; titrate to clinical effect and tolerability with CDC opioid prescribing guidance constraints on morphine-milligram-equivalent (MME) totals · No fixed maximum; titrated to TSH target · TID per eye · Titrated to glucose; no fixed ceiling · Titrated to glucose; no fixed maximum · '''20 mg/day in adults >60 years''' per FDA's 2011-2012 QT-prolongation warning; 40 mg/day in adults ≤60

Other values:

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Oral (6)

Benefit over weeks of dosing (1) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BPH symptom improvement at 3-6 months; prostate volume reduction over 6-12 months; hair regrowth at 6-12 months (1) · Effects accumulate over weeks; assess at 8 weeks (1) · Postprandial glucose effect within days; HbA1c by 12 weeks (2)

24 hours (4) · Continuous daily dosing (1) · Daily dosing (1)

2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · ~11 h (1) · ~12 hours (effective); terminal much longer'"`UNIQ--ref-0000117C-QINU`"' (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1) · ~5-6 hours in young men, ~8 hours in elderly'"`UNIQ--ref-00000531-QINU`"' (1) · ~57 hours (parent), ~200 h (active metabolite) (1)

Not characterized; oral dosing once daily (1) · ~30% (oral)'"`UNIQ--ref-0000117D-QINU`"' (1) · ~33% (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~63% (oral)'"`UNIQ--ref-00000532-QINU`"' (1) · ~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1)

'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · '''Pregnant individuals should not handle crushed/broken tablets''' (skin absorption risk); can cause hypospadias in male fetus. Not used in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; avoid (1) · Limited data; switch to insulin where feasible.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Not indicated; pregnancy effects unknown (1)

Rx-only in US (REMS program) (1) · Rx. FDA black-box warning for increased mortality in elderly patients with dementia-related psychosis (class warning shared with all antipsychotics) (1) · [[USLegal:Prescription only|Rx-only]] in US (4)