Drilldown: Medicines

Bisoprolol (1) · Dexmethylphenidate (1) · Nebivolol (1) · Primidone (1) · Sildenafil (1)

Bystolic (1) · Focalin, Focalin XR (1) · Mysoline (1) · Viagra, Revatio (1) · Zebeta (1)

Beta Blocker (2) · Cardioselective (β1) (1) · Cardioselective (β1) + vasodilator (1) · CNS stimulant (1) · NDRI (1) · PDE5 Inhibitor (1) · Psychostimulant (1) · [[:Category:Anticonvulsants|Anticonvulsant]] (1) · [[:Category:Barbiturates|Barbiturate (parent compound)]] (1) · [[:Category:Tremor medicines|Tremor medicine]] (1)

Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol. (1) · Norepinephrine–dopamine reuptake inhibition (DAT, NET), d-threo enantiomer of methylphenidate (1) · Selective inhibitor of phosphodiesterase type 5 (PDE5), preventing cGMP breakdown in vascular smooth muscle. In the corpus cavernosum, potentiates the NO/cGMP cascade triggered by sexual stimulation. (1) · The d-enantiomer is a highly β1-selective antagonist; the l-enantiomer triggers endothelial nitric-oxide–mediated vasodilation. Unique among beta blockers for this NO mechanism. (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-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"' (1) · '"`UNIQ--vote-00000150-QINU`"', '"`UNIQ--vote-00000151-QINU`"' (1) · '"`UNIQ--vote-0000059D-QINU`"' (1) · '"`UNIQ--vote-00000636-QINU`"', '"`UNIQ--vote-00000637-QINU`"', '"`UNIQ--vote-00000638-QINU`"' (1) · '"`UNIQ--vote-00000705-QINU`"', '"`UNIQ--vote-00000706-QINU`"' (1)

None (1) · 2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration) (1) · 5 mg daily (1) · 50 mg ~1 h before sexual activity (ED); 20 mg TID (PAH) (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 (1) · 2.5, 5, 10, 20 mg tabs (1) · 25, 50, 100 mg tabs (Viagra); 20 mg tabs and 10 mg/mL oral suspension (Revatio) (1) · 5, 10 mg tabs (1) · Tablets 50, 250 mg (1)

None (1) · 100 mg/d (ED); 20 mg TID (PAH) (1) · 2 g/day (seizures); typically much lower for essential tremor (1) · 20 mg/d (1) · 40 mg/d (1)

IV (Revatio) (1) · Oral (5)

None · Hours · 30-60 minutes · 1-2 hours · ~30 min · LDL lowering at 2 weeks, max by 4 weeks · ~1 hour · 15-30 minutes · 15–30 min · 1–2 h · 30–60 min · Antidepressant effect emerges over 1-2 weeks · BP and symptomatic LUTS improvement within 1-2 weeks · BP effect within 1-2 weeks · Clinical improvement within 24-72 hours · Days · Motor improvement over days at therapeutic dose · Over weeks · Postprandial glucose effect within days; HbA1c by 12 weeks · Sleep effect from first dose; antidepressant effect over 1-4 weeks

Other values:

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24 h (2) · BID-TID dosing (1) · IR 4–6 h; XR 8–12 h (1) · ~4 h (1)

2.2 h (IR parent); ~3 h (XR parent) (1) · 9–12 h (1) · Primidone 5-15 hours; '''phenobarbital active metabolite 50-150 hours'''; PEMA (phenylethylmalonamide) active metabolite 16 hours'"`UNIQ--ref-00000017-QINU`"' (1) · ~10 h (CYP2D6 extensive metabolizers); up to 31 h (poor metabolizers) (1) · ~4 h (1)

~12% (extensive metabolizers); ~96% (poor metabolizers) (1) · ~22–25% (1) · ~40% (1) · ~90% (low first-pass) (1) · ~90% (oral)'"`UNIQ--ref-00000018-QINU`"' (1)

Category B (1) · Category C (3) · 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-only in US (3) · Schedule II (1) · [[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)