Drilldown: Medicines

None (1) · Bromazolam (1) · Flibanserin (1) · Losartan (1) · Mirabegron (1) · Sitagliptin (1)

(none, never marketed) (1) · Addyi (1) · Cozaar (1) · Januvia; with metformin Janumet/Janumet XR (1) · Myrbetriq (1) · Quviviq (1)

Designer benzodiazepine (1) · Dual orexin receptor antagonist (DORA) (1) · Multimodal serotonergic; HSDD treatment (1) · Research material (1) · Sedative-Hypnotic (1) · Triazolobenzodiazepine (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:Beta-3_agonists|β3 adrenergic agonist]] (1) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (1) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (1) · [[:Category:Overactive_bladder_medications|Overactive bladder medication]] (1)

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) · Positive allosteric modulator of the GABA_A receptor at the benzodiazepine binding site; increases frequency of Cl⁻ channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (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)

Insomnia (sleep onset and/or sleep maintenance) in adults (FDA-approved Jan 2022) (1) · No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (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-00000764-QINU`"' (1) · '"`UNIQ--vote-00000C4C-QINU`"', '"`UNIQ--vote-00000C4D-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) · 25 mg PO at bedtime (no titration); may increase to 50 mg if 25 mg inadequate (1) · 25 mg PO once daily; titrate to 50 mg after 4-8 weeks if needed (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1) · No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1)

100 mg tabs (1) · 25 mg, 50 mg tablets (1) · 25 mg, 50 mg, 100 mg tablets (1) · 25, 50 mg ER tablets; 8 mg/mL granules for oral suspension (Myrbetriq Granules, pediatric) (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · Illicit tablets ("bars"), powders, blotter, occasionally solutions. No pharmaceutical product exists. (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:

Search

intranasal; rectal and IV reported. (1) · Oral (6) · sublingual (1)

BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · Effects accumulate over weeks; assess at 8 weeks (1) · Postprandial glucose effect within days; HbA1c by 12 weeks (1) · Symptom improvement within weeks (1) · ~20–40 min PO; faster sublingual/intranasal. (1) · ~30 min (1)

24 hours (3) · 6–10 h subjective; full pharmacologic effect considerably longer. (1) · Continuous daily dosing (1) · ~7-8 hours (1)

2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · Estimated ~12–17 h (some sources cite up to ~21 h); active metabolites prolong effect. (1) · ~11 h (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1) · ~50 hours'"`UNIQ--ref-00000C4E-QINU`"' (1) · ~8 hours (shorter than suvorexant and lemborexant) (1)

25 mg: ~29%; 50 mg: ~35%; food reduces absorption'"`UNIQ--ref-00000C4F-QINU`"' (1) · Not formally characterized in humans. (1) · ~33% (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~62% (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) · Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) · Limited data.<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> (1) · Not indicated; pregnancy effects unknown (1)

None (1) · Rx, Schedule IV (US) (1) · Rx-only in US (REMS program) (1) · [[USLegal:Prescription only|Rx-only]] in US (3)