Drilldown: Medicines

Flibanserin (1) · Linaclotide (1) · Losartan (1) · Sitagliptin (1)

Addyi (1) · Cozaar (1) · Januvia; with metformin Janumet/Janumet XR (1) · Linzess (1)

Multimodal serotonergic; HSDD treatment (1) · [[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (1) · [[:Category:Guanylate_cyclase_C_agonists|Guanylate cyclase-C agonist]] (1) · [[:Category:IBS_treatments|IBS-C treatment]] (1) · [[:Category:Incretin_modulators|Incretin pathway modulator]] (1)

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) · '"`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) · '"`UNIQ--vote-00001197-QINU`"' Extracellular cGMP separately activates submucosal sensory afferents in a way that reduces visceral pain perception, distinguishing linaclotide from purely osmotic laxatives in IBS-C. Diarrhea is the dose-limiting effect'"`UNIQ--ref-00001198-QINU`"'. (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-00001199-QINU`"', '"`UNIQ--vote-0000119A-QINU`"', '"`UNIQ--vote-0000119B-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) · 145 mcg PO once daily for chronic idiopathic constipation; 290 mcg daily for IBS-C; pediatric 72 mcg daily (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1)

100 mg tabs (1) · 25 mg, 50 mg, 100 mg tablets (1) · 25, 50, 100 mg tablets; combination tablets with metformin (1) · 72, 145, 290 mcg capsules (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 (4)

Bowel movement within 1 week; abdominal pain improvement over weeks (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)

24 hours (3) · Continuous daily dosing (1)

2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · Not meaningfully described (negligible systemic absorption — the drug acts locally and is degraded in the GI tract)'"`UNIQ--ref-0000119C-QINU`"' (1) · ~11 h (1) · ~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1)

Negligible systemic absorption'"`UNIQ--ref-0000119D-QINU`"' (1) · ~33% (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-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) · Limited data; minimal systemic absorption likely renders fetal risk low.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (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)

Rx-only in US (REMS program) (1) · [[USLegal:Prescription only|Rx-only]] in US (2) · [[USLegal:Prescription only|Rx-only]] in US. Carries a '''Boxed Warning''' contraindicating use in children <2 years (lethal dehydration in animal studies)'"`UNIQ--ref-0000119E-QINU`"' (1)