Drilldown: Medicines
Use the filters below to narrow your results.
generic:
brand:
classes:
Multimodal serotonergic; HSDD treatment (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:Decongestants|Decongestant]] (1) ·
[[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (2) ·
[[:Category:Incretin_modulators|Incretin pathway modulator]] (2) ·
[[:Category:Sympathomimetics|Sympathomimetic (indirect-acting)]] (1)
mechanism:
None (3) ·
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)
uses:
'"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-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-0000052E-QINU`"', '"`UNIQ--vote-0000052F-QINU`"', '"`UNIQ--vote-00000530-QINU`"' (1) ·
'"`UNIQ--vote-00000764-QINU`"' (1) ·
'"`UNIQ--vote-0000117B-QINU`"' (1)
starting dose:
100 mg at bedtime daily (1) ·
100 mg PO once daily (50 mg if CrCl 30-44; 25 mg if <30 or dialysis) (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) ·
IR: 60 mg PO every 4-6 hours. 12-hour ER: 120 mg PO every 12 hours. 24-hour ER: 240 mg PO once daily. Pediatric: weight-based (1)
preparations:
1 mg, 5 mg 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) ·
IR tablets 30, 60 mg; 12-hour ER tablets 120 mg; 24-hour ER tablets 240 mg; oral liquid; multiple combination products with antihistamines, NSAIDs, or expectorants (1)
fda max: (Click arrow to add another value)
routes:
onset:
30-60 minutes (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)
halflife:
2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) ·
9-16 hours (pH-dependent: acidic urine shortens, alkaline urine substantially extends)'"`UNIQ--ref-0000001B-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)
bioavailability:
~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) ·
~90% (oral, low first-pass)'"`UNIQ--ref-0000001C-QINU`"' (1)
pregnancy:
'''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.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited data; switch to insulin where feasible.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (2) ·
Not indicated; pregnancy effects unknown (1) ·
Some controversial signal for first-trimester gastroschisis association in observational studies; limited use is generally considered acceptable after the first trimester.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1)
legal:
'''[[USLegal:Behind-the-counter|Behind-the-counter]] in US''' under the Combat Methamphetamine Epidemic Act 2005: purchase restricted to ≤3.6 g/day and ≤9 g/30 days, with photo ID, logbook signature, and quantity logging required. Several states schedule higher than federal (1) ·
Rx-only in US (REMS program) (1) ·
[[USLegal:Prescription only|Rx-only]] in US (4)
Showing below up to 6 results in range #1 to #6.