Drilldown: Medicines
Medicines > fda max 
:
100 mg/d or
4.5 mg/day (Parkinson disease); 0.5 mg/day (restless legs syndrome) or
TID per eye
:
100 mg/d or
4.5 mg/day (Parkinson disease); 0.5 mg/day (restless legs syndrome) or
TID per eye Use the filters below to narrow your results.
generic:
brand:
classes:
Multimodal serotonergic; HSDD treatment (1) ·
[[:Category:Alpha-2_agonists|Alpha-2 adrenergic agonist]] (1) ·
[[:Category:Angiotensin_receptor_blockers|Angiotensin receptor blocker (ARB)]] (1) ·
[[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) ·
[[:Category:Antihypertensives|Antihypertensive]] (1) ·
[[:Category:Antiparkinsonians|Antiparkinsonian]] (1) ·
[[:Category:Carbonic_anhydrase_inhibitors|Carbonic anhydrase inhibitor (topical)]] (1) ·
[[:Category:Dopamine agonists|Dopamine D2/D3 receptor agonist (non-ergot)]] (1) ·
[[:Category:DPP-4_inhibitors|DPP-4 inhibitor]] (1) ·
[[:Category:Glaucoma_medications|Glaucoma medication]] (2) ·
[[:Category:Incretin_modulators|Incretin pathway modulator]] (1) ·
[[:Category:Ocular_hypotensive_agents|Ocular hypotensive agent]] (2)
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-00000764-QINU`"' (1) ·
'"`UNIQ--vote-00000B08-QINU`"', '"`UNIQ--vote-00000B09-QINU`"' (1) ·
'"`UNIQ--vote-000010CE-QINU`"', '"`UNIQ--vote-000010CF-QINU`"', '"`UNIQ--vote-000010D0-QINU`"' (1)
starting dose:
1 drop in affected eye(s) TID (monotherapy); BID with timolol (Cosopt) (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) ·
50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1) ·
Ophthalmic 1 drop in affected eye(s) TID; topical Mirvaso 0.33% gel applied to face daily (1) ·
Parkinson disease: 0.125 mg PO TID, titrate weekly to maintenance ~1.5 mg TID. Restless legs syndrome: 0.125 mg PO 2-3 hours before bedtime, titrate to 0.5 mg/day if needed (1)
preparations:
0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) (1) ·
100 mg tabs (1) ·
2% ophthalmic solution (Trusopt); 2%/0.5% fixed combination with timolol (Cosopt, Cosopt PF) (1) ·
25 mg, 50 mg, 100 mg tablets (1) ·
25, 50, 100 mg tablets; combination tablets with metformin (1) ·
IR tablets 0.125, 0.25, 0.5, 0.75, 1, 1.5 mg; ER tablets 0.375, 0.75, 1.5, 2.25, 3, 3.75, 4.5 mg (1)
fda max: (Click arrow to add another value)
routes:
onset:
BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) ·
Effects accumulate over weeks; assess at 8 weeks (1) ·
IOP lowering at 1 hour; max at 2-3 hours (1) ·
IOP lowering at 2 hours; max at 4 hours (1) ·
Motor improvement over days at therapeutic dose (1) ·
Postprandial glucose effect within days; HbA1c by 12 weeks (1)
duration:
halflife:
2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) ·
8-12 hours (longer in elderly and renal impairment)'"`UNIQ--ref-0000001B-QINU`"' (1) ·
~11 h (1) ·
~12.4 hours'"`UNIQ--ref-00000765-QINU`"' (1) ·
~3 hours'"`UNIQ--ref-000010D1-QINU`"' (1) ·
~4 months in erythrocytes (carbonic anhydrase binding in red cells; not relevant to topical IOP duration)'"`UNIQ--ref-00000B0A-QINU`"' (1)
bioavailability:
>90% (oral)'"`UNIQ--ref-0000001C-QINU`"' (1) ·
Topical with measurable systemic absorption (small CA inhibition observed clinically with chronic use)'"`UNIQ--ref-00000B0B-QINU`"' (1) ·
Topical; clinically meaningful systemic absorption can produce systemic α2 effects (somnolence, hypotension), especially in children'"`UNIQ--ref-000010D2-QINU`"' (1) ·
~33% (1) ·
~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) ·
~87% (oral)'"`UNIQ--ref-00000766-QINU`"' (1)
pregnancy:
'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) ·
Limited data.<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> (1) ·
Limited data; weigh against alternatives.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Limited human data; rarely indicated in pregnancy given the typical patient population.<sup class="pcp-cn" title="This claim needs a citation.">[[[Pharmacopedia:Citation needed|citation needed]]]</sup> (1) ·
Not indicated; pregnancy effects unknown (1)
Showing below up to 6 results in range #1 to #6.