Drilldown: Medicines

None (1) · Benazepril (1) · Dapagliflozin (1) · Primidone (1) · Rosuvastatin (1)

Crestor, Ezallor (1) · Dayvigo (1) · Farxiga (US), Forxiga (international) (1) · Lotensin (1) · Mysoline (1)

Dual orexin receptor antagonist (DORA) (1) · [[:Category:ACE_inhibitors|ACE inhibitor]] (1) · [[:Category:Anticonvulsants|Anticonvulsant]] (1) · [[:Category:Antihyperglycemic_agents|Antihyperglycemic agent]] (1) · [[:Category:Antihypertensives|Antihypertensive]] (1) · [[:Category:Barbiturates|Barbiturate (parent compound)]] (1) · [[:Category:Heart_failure_medications|Heart failure medication]] (1) · [[:Category:Lipid-lowering_agents|Lipid-lowering agent]] (1) · [[:Category:SGLT2_inhibitors|SGLT2 inhibitor]] (1) · [[:Category:Statins|Statin]] (1) · [[:Category:Tremor medicines|Tremor medicine]] (1)

None (1) · Competitive antagonist at OX1R and OX2R. Faster receptor association/dissociation kinetics than suvorexant (~16 sec dissociation vs ~57 sec) hypothesized to support sleep onset, with sufficient duration for maintenance. (1) · '"`UNIQ--vote-00000013-QINU`"' Strong CYP3A4 induction via the phenobarbital metabolite produces many interactions (reduces oral contraceptives, warfarin, many psychotropics). Essential-tremor efficacy is the unique pharmacological selling point'"`UNIQ--ref-00000014-QINU`"'. (1) · '"`UNIQ--vote-000000F7-QINU`"' Minimal CYP3A4 dependence (CYP2C9 minor) reduces drug-drug interactions; transport in and out of hepatocytes is largely via OATP1B1, making SLCO1B1 PGx genotype the most clinically actionable marker for statin-associated myopathy'"`UNIQ--ref-000000F8-QINU`"'. (1) · '"`UNIQ--vote-00000A1D-QINU`"' Like other ACE inhibitors, it raises bradykinin (driving the dry cough and rare angioedema). Renally cleared; dose-adjust in renal impairment'"`UNIQ--ref-00000A1E-QINU`"'. (1)

Insomnia (sleep onset and/or maintenance) in adults (FDA-approved Dec 2019) (1) · '"`UNIQ--vote-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"' (1) · '"`UNIQ--vote-000000F9-QINU`"', '"`UNIQ--vote-000000FA-QINU`"', '"`UNIQ--vote-000000FB-QINU`"' (1) · '"`UNIQ--vote-0000054E-QINU`"', '"`UNIQ--vote-0000054F-QINU`"', '"`UNIQ--vote-00000550-QINU`"', '"`UNIQ--vote-00000551-QINU`"' (1) · '"`UNIQ--vote-00000A1F-QINU`"', '"`UNIQ--vote-00000A20-QINU`"', '"`UNIQ--vote-00000A21-QINU`"' (1)

10 mg PO once daily (5 mg if on a diuretic); titrate to 40 mg (1) · 10 mg PO once daily in the morning; 5 mg starting in heart failure (1) · 10-20 mg PO once daily (5 mg in Asian ancestry, elderly, hypothyroidism, or strong CYP/SLCO1B1 interactions) (1) · 5 mg PO at bedtime; may increase to 10 mg if inadequate (1) · Seizures: 100-125 mg PO at bedtime x 3 days, then BID, then TID, escalating to 750-1500 mg/day. Essential tremor: 25-50 mg PO at bedtime, titrate slowly to 250-750 mg/day (1)

None · 10 mg, 20 mg, 40 mg, 80 mg tablets · 2.5, 5, 10, 20 mg tabs · 5 mg, 10 mg tablets · 5, 10 mg tablets · 5, 10, 20, 40 mg tablets · 0.005% ophthalmic solution (50 mcg/mL); typical 2.5 mL bottle · 0.01%, 0.03% ophthalmic solution · 0.025%, 0.035% ophthalmic solutions · 0.1% (Patanol), 0.2% (Pataday once-daily original), 0.7% (Pataday 24-hour) ophthalmic solutions; 0.6% nasal spray · 0.1%, 0.15% intranasal spray; 0.05% ophthalmic solution; combination Dymista (azelastine 0.137 mg + fluticasone 50 mcg/spray) · 0.1%, 0.15%, 0.2% ophthalmic solutions; 0.33% topical gel; combinations with timolol (Combigan) and brinzolamide (Simbrinza) · 0.225%, 0.45%, 0.9%, 3%, 5% IV solutions; 0.9% nasal spray; 3% and 7% nebulizer solutions; oral tablets (1 g) · 0.25 mg, 0.5 mg, 1 mg, 2 mg tablets (immediate-release and orally disintegrating); 0.5 mg, 1 mg, 2 mg, 3 mg extended-release tablets; 1 mg/mL oral concentrate · 0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg tablets · 0.25, 0.5 mcg oral capsules; 1 mcg/mL oral solution; 1 mcg/mL IV; 3 mcg/g topical ointment · 0.35 mg POP tablets; 5 mg tablets (Aygestin); component of COCs and combination HRT · 0.4 mg capsules · 0.4, 0.8, 1 mg OTC; 1 mg Rx; 5 mg/mL injection · 0.5 g, 1 g capsules

Other values:

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10 mg/d (2) · 2 g/day (seizures); typically much lower for essential tremor (1) · 40 mg/d (rarely needed; 40 mg restricted to patients not at goal on 20 mg) (1) · 80 mg/d (1)

Oral (5)

Anticonvulsant effect emerges with slow titration over weeks; tremor effect over weeks (1) · BP lowering within 1 hour; max at 6 hours (1) · Glycosuria within hours; HbA1c effect at 12 weeks; CV/renal benefits over months (1) · LDL lowering at 1 week, max by 4 weeks (1) · ~30 min (1)

24 hours (3) · BID-TID dosing (1) · ~7-8 hours (1)

10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' (1) · Primidone 5-15 hours; '''phenobarbital active metabolite 50-150 hours'''; PEMA (phenylethylmalonamide) active metabolite 16 hours'"`UNIQ--ref-00000017-QINU`"' (1) · ~12.9 hours'"`UNIQ--ref-00000552-QINU`"' (1) · ~17-19 hours (longer than daridorexant) (1) · ~19 hours'"`UNIQ--ref-000000FC-QINU`"' (1)

~20% (oral; hydrophilic, minimal CYP metabolism, mostly excreted unchanged in bile)'"`UNIQ--ref-000000FD-QINU`"' (1) · ~37% (oral; food does not affect)'"`UNIQ--ref-00000A23-QINU`"' (1) · ~44% (1) · ~78% (oral; high-fat meal modestly reduces but is not clinically significant)'"`UNIQ--ref-00000553-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000018-QINU`"' (1)

'''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000A24-QINU`"' (1) · Avoid in second and third trimesters; fetal SGLT2 inhibition disrupts kidney development.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; avoid (1) · Previously Category X; FDA removed the blanket statin contraindication in pregnancy in 2021. Use individualized.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Substantial teratogenic signal (barbiturate class effects including neonatal withdrawal and hemorrhagic disease of newborn).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)

Rx, Schedule IV (US) (1) · [[USLegal:Prescription only|Rx-only]] in US (3) · [[USLegal:Prescription only|Rx-only]] in US. '''Federally non-controlled despite being a barbiturate''', a paradoxical situation given that its primary active metabolite phenobarbital is Schedule IV'"`UNIQ--ref-00000019-QINU`"' (1)