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Medicines > classes : Tryptamine or [[:Category:Antihypertensives|Antihypertensive]] or [[:Category:Anxiolytics|Anxiolytic]]

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generic:
brand:
None (26) · Altace (1) · Apresoline (historical); mostly generic; combination with isosorbide dinitrate marketed as BiDil for self-identified Black patients with HFrEF (1) · Ativan (oral, injectable), Loreev XR (1) · Avapro (1) · Benicar (1) · Buspar (US brand discontinued; generic widely available) (1) · Calan, Calan SR, Verelan, Verelan PM, Isoptin SR (1) · Cardizem, Tiazac, Cartia XT, Dilacor XR, Taztia XT, Matzim LA (1) · Cardura, Cardura XL (1) · Coreg, Coreg CR (1) · Cozaar (1) · Diovan; Entresto (in fixed-dose combination with sacubitril) (1) · Effexor XR, Effexor IR (discontinued in US, generic widely available) (1) · Hytrin (US brand discontinued); mostly generic (1) · Kapvay (ER, ADHD), Catapres (IR, antihypertensive), Catapres-TTS (transdermal patch), Duraclon (epidural injection) (1) · Klonopin (1) · Lexapro (1) · Lotensin (1) · Luvox (US brand discontinued; generic widely available), Luvox CR, Faverin (other markets) (1) · Micardis (1) · Microzide; mostly prescribed generically (1) · Norvasc, Katerzia (1) · Paxil (IR), Paxil CR (controlled-release), Brisdelle (low-dose for menopausal vasomotor symptoms), Pexeva (paroxetine mesylate) (1) · Procardia, Procardia XL, Adalat CC, Afeditab CR (1) · Prozac (1) · Tenormin (1) · Thalitone; mostly prescribed generically (1) · Timoptic (ophthalmic), Timoptic-XE (gel-forming once-daily), Istalol (once-daily 0.5%), Betimol; Blocadren (oral, discontinued in many markets); combination eye drops Combigan (with brimonidine), Cosopt (with dorzolamide) (1) · Trandate, Normodyne (discontinued in US) (1) · Valium (oral, IV/IM, rectal), Diastat (rectal gel for breakthrough seizures), Valtoco (nasal spray for breakthrough seizures), Libervant (buccal film) (1) · Vasotec, Vasotec IV, Epaned (1) · Vistaril (pamoate), Atarax (HCl, discontinued in US as brand) (1) · Zestril, Prinivil, Qbrelis (1)
classes: (Click arrow to add another value)
mechanism:
None (18) · 5-HT2A agonist (15) · 5-HT2A agonist; 5-HT3 antagonist (1) · 5-HT2A agonist; minor psilocybin mushroom alkaloid (1) · 5-HT2A agonist; primarily auditory effects (1) · 5-HT2A agonist; sigma-1 agonist (1) · Monoamine releasing agent; 5-HT2A agonist; MAO inhibitor (1) · Potent 5-HT2A agonist; sigma-1 agonist (1) · Prodrug of 4-HO-DET; 5-HT2A agonist (1) · Prodrug of 4-HO-DiPT; 5-HT2A agonist (1) · Prodrug of 4-HO-MET; 5-HT2A agonist (1) · Prodrug of 4-HO-MiPT; 5-HT2A agonist (1) · Prodrug of psilocin; 5-HT2A agonist (1) · TrkB/BDNF'"`UNIQ--ref-00000047-QINU`"' '"`UNIQ--vote-00000048-QINU`"' (1) · '"`UNIQ--vote-00000015-QINU`"' CYP2D6 metabolism produces stereoselective clearance; CYP2D6 poor metabolizers have higher plasma exposure and may need lower doses'"`UNIQ--ref-00000016-QINU`"'. (1) · '"`UNIQ--vote-00000015-QINU`"' The favorable pregnancy safety profile and the dual mechanism support its first-line role in pregnancy-associated hypertension and in hypertensive emergencies where rapid, controllable BP reduction is needed'"`UNIQ--ref-00000016-QINU`"'. (1) · '"`UNIQ--vote-0000001D-QINU`"' '''QT prolongation''' risk at high doses prompted the FDA's 2015 caution against use in patients with prolonged QT or with concurrent QT-prolonging medicines'"`UNIQ--ref-0000001E-QINU`"'. (1) · '"`UNIQ--vote-0000001D-QINU`"' CYP2C19 + CYP3A4 metabolism, with CPIC PGx guidance: poor CYP2C19 metabolizers have ~3-fold higher exposure and benefit from a lower starting dose; ultrarapid metabolizers may have inadequate response'"`UNIQ--ref-0000001E-QINU`"'. (1) · '"`UNIQ--vote-00000053-QINU`"' Also raises bradykinin, contributing to vasodilation and the characteristic dry cough. Renally cleared, unmetabolized; dose-adjust by eGFR'"`UNIQ--ref-00000054-QINU`"'. (1) · '"`UNIQ--vote-00000073-QINU`"' The long half-life gives smooth, once-daily BP control with low rebound. CYP3A4 substrate; pedal edema is the characteristic, dose-related, non-fluid-overload side effect'"`UNIQ--ref-00000074-QINU`"'. (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-00000138-QINU`"' Decreases urinary calcium (used in stone prevention); raises serum uric acid, glucose, and lipids modestly; non-anion-gap hypokalemic metabolic alkalosis is the characteristic electrolyte pattern'"`UNIQ--ref-00000139-QINU`"'. (1) · '"`UNIQ--vote-000004C8-QINU`"' Largely hepatically cleared (~80% biliary); no active metabolite. Sacubitril-valsartan (Entresto) combines an ARB with neprilysin inhibition for HFrEF and was a notable advance over the ARB-alone trial (PARADIGM-HF, 2014)'"`UNIQ--ref-000004C9-QINU`"'. (1) · '"`UNIQ--vote-0000063C-QINU`"' Avoid in HFrEF (negative inotropy). CYP3A4 substrate AND moderate inhibitor — interacts substantially with statins (especially simvastatin), tacrolimus, cyclosporine, and many other CYP3A4 substrates'"`UNIQ--ref-0000063D-QINU`"'. (1) · '"`UNIQ--vote-0000083E-QINU`"' CYP2C9 substrate; no clinically active metabolites. The IDNT trial established renoprotection in diabetic nephropathy independent of BP lowering, contributing to the ARB class indication in T2DM with proteinuria'"`UNIQ--ref-0000083F-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) · '"`UNIQ--vote-00000AEA-QINU`"' The 24-hour half-life supports once-daily dosing with consistent overnight BP control. Largely hepatically cleared (~98% biliary); no significant renal clearance dependence'"`UNIQ--ref-00000AEB-QINU`"'. (1) · '"`UNIQ--vote-0000111B-QINU`"' Intraoperative floppy iris syndrome is a recognized class effect. Recently emerging evidence (observational) suggests possible Parkinson's disease risk reduction via PGK1 binding — investigational and not a clinical indication'"`UNIQ--ref-0000111C-QINU`"'. (1)
uses:
None (26) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"' (2) · '"`UNIQ--vote-00000019-QINU`"', '"`UNIQ--vote-0000001A-QINU`"', '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1) · '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"' (2) · '"`UNIQ--vote-0000001F-QINU`"', '"`UNIQ--vote-00000020-QINU`"', '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"' (6) · '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-QINU`"', '"`UNIQ--vote-00000029-QINU`"', '"`UNIQ--vote-0000002A-QINU`"' (1) · '"`UNIQ--vote-00000049-QINU`"', '"`UNIQ--vote-0000004A-QINU`"', '"`UNIQ--vote-0000004B-QINU`"' (1) · '"`UNIQ--vote-00000055-QINU`"', '"`UNIQ--vote-00000056-QINU`"', '"`UNIQ--vote-00000057-QINU`"', '"`UNIQ--vote-00000058-QINU`"' (1) · '"`UNIQ--vote-00000075-QINU`"', '"`UNIQ--vote-00000076-QINU`"', '"`UNIQ--vote-00000077-QINU`"' (1) · '"`UNIQ--vote-000000B8-QINU`"', '"`UNIQ--vote-000000B9-QINU`"', '"`UNIQ--vote-000000BA-QINU`"', '"`UNIQ--vote-000000BB-QINU`"' (1) · '"`UNIQ--vote-0000013A-QINU`"', '"`UNIQ--vote-0000013B-QINU`"', '"`UNIQ--vote-0000013C-QINU`"', '"`UNIQ--vote-0000013D-QINU`"' (1) · '"`UNIQ--vote-000004CA-QINU`"', '"`UNIQ--vote-000004CB-QINU`"', '"`UNIQ--vote-000004CC-QINU`"' (1) · '"`UNIQ--vote-0000056B-QINU`"' (1) · '"`UNIQ--vote-0000063E-QINU`"', '"`UNIQ--vote-0000063F-QINU`"', '"`UNIQ--vote-00000640-QINU`"', '"`UNIQ--vote-00000641-QINU`"' (1) · '"`UNIQ--vote-00000683-QINU`"', '"`UNIQ--vote-00000684-QINU`"', '"`UNIQ--vote-00000685-QINU`"', '"`UNIQ--vote-00000686-QINU`"' (1) · '"`UNIQ--vote-00000747-QINU`"', '"`UNIQ--vote-00000748-QINU`"', '"`UNIQ--vote-00000749-QINU`"', '"`UNIQ--vote-0000074A-QINU`"', '"`UNIQ--vote-0000074B-QINU`"', '"`UNIQ--vote-0000074C-QINU`"' (1) · '"`UNIQ--vote-00000780-QINU`"', '"`UNIQ--vote-00000781-QINU`"', '"`UNIQ--vote-00000782-QINU`"' (1) · '"`UNIQ--vote-00000840-QINU`"', '"`UNIQ--vote-00000841-QINU`"' (1) · '"`UNIQ--vote-00000A1F-QINU`"', '"`UNIQ--vote-00000A20-QINU`"', '"`UNIQ--vote-00000A21-QINU`"' (1) · '"`UNIQ--vote-00000A66-QINU`"', '"`UNIQ--vote-00000A67-QINU`"', '"`UNIQ--vote-00000A68-QINU`"', '"`UNIQ--vote-00000A69-QINU`"', '"`UNIQ--vote-00000A6A-QINU`"' (1) · '"`UNIQ--vote-00000AAD-QINU`"', '"`UNIQ--vote-00000AAE-QINU`"', '"`UNIQ--vote-00000AAF-QINU`"' (1) · '"`UNIQ--vote-00000AEC-QINU`"', '"`UNIQ--vote-00000AED-QINU`"' (1) · '"`UNIQ--vote-00000B81-QINU`"', '"`UNIQ--vote-00000B82-QINU`"', '"`UNIQ--vote-00000B83-QINU`"' (1) · '"`UNIQ--vote-00000C2E-QINU`"', '"`UNIQ--vote-00000C2F-QINU`"', '"`UNIQ--vote-00000C30-QINU`"', '"`UNIQ--vote-00000C31-QINU`"' (1) · '"`UNIQ--vote-0000111D-QINU`"', '"`UNIQ--vote-0000111E-QINU`"' (1)
starting dose:
None (26) · 1 mg PO at bedtime to limit first-dose syncope; titrate weekly to 5-10 mg (1) · 10 mg (1) · 10 mg PO once daily (5 mg if on a diuretic); titrate to 40 mg (1) · 10 mg PO once daily; titrate to 20 mg/day after 1-2 weeks if needed (1) · 12.5-25 mg PO once daily (1) · 12.5-25 mg PO once daily; titrate to 50 mg (1) · 150 mg PO once daily; titrate to 300 mg if needed (1) · 2.5 mg PO once daily (1.25 mg in CHF or volume depletion); titrate to 5-10 mg/d (1) · 2.5-5 mg PO once daily; titrate to 10 mg/d (1) · 20 mg PO once daily; titrate to 40 mg/d after 2 weeks if needed (1) · 25-50 mg PO once daily; titrate to 100 mg/day (1) · 40 mg PO once daily; titrate to 80 mg (1) · 5 mg PO TID or 7.5 mg PO BID; titrate by 5 mg every 2-3 days to clinical effect, commonly 30-60 mg/day divided BID-TID (1) · 5-10 mg PO once daily (2.5 mg if on diuretic or in heart failure); titrate to 10-20 mg BID for HFrEF (1) · 5-10 mg PO once daily (2.5 mg in heart failure, hyponatremia, or volume depletion) (1) · 50 mg PO at bedtime; titrate by 50 mg every 4-7 days to clinical effect. Total daily doses >100 mg divided BID. Luvox CR: 100 mg PO once daily, may titrate to 300 mg/day (1) · 50 mg PO daily (25 mg in volume depletion or hepatic impairment) (1) · 80-160 mg PO once daily (40 mg BID in HFrEF, titrating up to 160 mg BID) (1) · ADHD (Kapvay ER): 0.1 mg PO at bedtime, titrate weekly to 0.4 mg/day divided BID. HTN (IR): 0.1 mg PO BID, titrate by 0.1 mg increments (1) · Anxiety: 0.25 mg PO BID, titrate by 0.125-0.25 mg every 3 days to target 1-4 mg/day divided. Seizures: 1.5 mg/day divided TID, titrate by 0.5-1 mg every 3 days (1) · Anxiety: 0.5-1 mg PO BID-TID. Insomnia: 1-2 mg PO at bedtime. Status epilepticus: 4 mg IV (adult), repeat after 5-10 minutes if needed. Acute agitation: 1-2 mg IM (1) · Anxiety: 2-10 mg PO 2-4 times daily. Alcohol withdrawal: 10-20 mg PO/IV every 4-6 hours, symptom-triggered. Status epilepticus: 5-10 mg IV. Breakthrough seizures: Diastat rectal 0.2-0.5 mg/kg or Valtoco intranasal 5-20 mg (1) · Anxiety: 25-50 mg PO QID. Pruritus: 25 mg PO TID-QID. Insomnia: 25-50 mg PO at bedtime. Pediatric: 50-100 mg/day divided (1) · ER 180-240 mg PO once daily; IR 30 mg PO QID; IV 0.25 mg/kg over 2 min for acute rate control, then 5-15 mg/h infusion (1) · ER 30-60 mg PO once daily; immediate-release 10 mg PO TID (now rarely used for hypertension due to reflex tachycardia) (1) · Heart failure: 3.125 mg PO BID, doubling every 2 weeks as tolerated to target 25 mg BID (50 mg BID if >85 kg). Hypertension: 6.25 mg PO BID, titrate to 25 mg BID (1) · IR 1 mg PO at bedtime, titrate weekly; XL 4-8 mg PO daily (1) · IR 80-120 mg PO TID; ER 180-240 mg PO daily; IV 2.5-5 mg over 2 min for SVT termination (under monitoring); cluster prophylaxis up to 480-960 mg/d in divided doses (1) · MDD/GAD: 20 mg PO once daily. Panic disorder: 10 mg titrating to 40 mg. OCD: 20 mg titrating to 40-60 mg. CR: 25 mg/day. Brisdelle: 7.5 mg at bedtime for hot flashes (1) · Ophthalmic: 1 drop 0.5% in affected eye(s) BID (or once daily for XE / Istalol). Oral hypertension: 10 mg PO BID, titrate to 60 mg/day. Migraine prophylaxis: 10 mg BID, titrate to 30 mg/day (1) · Oral: 100 mg PO BID, titrate to 400 mg BID. IV: 20 mg over 2 minutes, repeat 40-80 mg every 10 minutes as needed (maximum cumulative 300 mg); continuous infusion 2 mg/minute (1) · PO 10 mg QID; IV 5-10 mg every 20-30 minutes for hypertensive emergency (1) · XR 37.5 mg PO once daily for 4-7 days, then 75 mg/day; titrate by 75 mg every ≥4 days to clinical effect. IR 25-37.5 mg BID-TID (1)
preparations:
None (26) · 1, 2, 4, 8 mg IR tablets; 4, 8 mg XL tablets (1) · 1, 2, 5, 10 mg capsules and tablets (1) · 1.25, 2.5, 5, 10 mg capsules (1) · 10 mg, 20 mg, 40 mg caps (1) · 10, 20 mg IR capsules; 30, 60, 90 mg ER tablets (1) · 10, 25, 50, 100 mg tablets; 20 mg/mL IV (1) · 12.5 mg capsules; 12.5, 25, 50 mg tablets (1) · 15 mg, 25 mg, 50 mg tablets (1) · 2.5, 5, 10 mg tablets; 1 mg/mL oral suspension (1) · 2.5, 5, 10, 20 mg tablets; 1 mg/mL oral solution (Epaned); 1.25 mg/mL IV (enalaprilat) (1) · 2.5, 5, 10, 20, 30, 40 mg tablets; 1 mg/mL oral solution (1) · 20, 40, 80 mg tablets (1) · 25 mg, 50 mg, 100 mg tablets (1) · 40, 80, 160, 320 mg tablets; oral suspension (1) · 5, 10, 20, 40 mg tablets (1) · 5, 20, 40 mg tablets (1) · 75, 150, 300 mg tablets (1) · IR 30, 60, 90, 120 mg tablets; multiple ER capsules and tablets 60-420 mg; IV 5 mg/mL (1) · IR 40, 80, 120 mg tablets; SR/ER 100-360 mg; IV 2.5 mg/mL (1) · IR tablets 0.1, 0.2, 0.3 mg; ER tablets 0.1, 0.2 mg (Kapvay); transdermal patches 0.1, 0.2, 0.3 mg/24h (TTS-1/2/3, weekly); epidural injection (Duraclon) (1) · IR tablets 10, 20, 30, 40 mg; CR tablets 12.5, 25, 37.5 mg; oral suspension 10 mg/5 mL; Brisdelle capsules 7.5 mg (1) · IR tablets 25, 37.5, 50, 75, 100 mg; XR capsules 37.5, 75, 150, 225 mg (1) · IR tablets 25, 50, 100 mg; Luvox CR capsules 100, 150 mg (1) · IR tablets 3.125, 6.25, 12.5, 25 mg; Coreg CR capsules 10, 20, 40, 80 mg (once-daily) (1) · Tablets 0.5, 1, 2 mg; oral concentrate 2 mg/mL; injection 2 mg/mL and 4 mg/mL; Loreev XR capsules 1, 2, 3 mg (1) · Tablets 0.5, 1, 2 mg; orally disintegrating tablets 0.125, 0.25, 0.5, 1, 2 mg (1) · Tablets 10, 25, 50 mg (HCl); capsules 25, 50, 100 mg (pamoate); oral suspension 25 mg/5 mL; injection 25, 50 mg/mL (IM only, never IV) (1) · Tablets 100, 200, 300 mg; injection 5 mg/mL (1) · Tablets 2, 5, 10 mg; oral solution 1, 5 mg/mL; injection 5 mg/mL; Diastat rectal gel 2.5, 5, 10, 20 mg; Valtoco nasal spray 5, 7.5, 10 mg/dose; Libervant buccal film (1) · Tablets 25, 50, 100 mg (1) · Tablets 5, 10, 20 mg; ophthalmic solution 0.25%, 0.5%; ophthalmic gel-forming solution 0.25%, 0.5% (Timoptic-XE) (1) · Tablets 5, 10, 20 mg; oral solution 1 mg/mL (1) · Tablets 5, 7.5, 10, 15, 30 mg (the 15 and 30 mg tablets are scored for halving and quartering) (1)
onset:
None (27) · '''Anxiolytic effect emerges over 2-4 weeks'''; buspirone does NOT work for acute anxiety, which is the central teaching point and the most common cause of treatment failure (1) · 15-30 minutes (oral) (1) · 15-60 minutes (oral); 1-5 minutes (IV); 4-10 minutes (rectal or intranasal) (1) · 20-60 minutes (1) · 30-60 min (IR oral); 2-3 days to steady state (transdermal patch) (1) · 30-60 minutes (oral); 5 minutes (IV); 15-30 minutes (IM) (1) · Antidepressant effect emerges over 1-2 weeks (1) · Antidepressant effect emerges over 1-2 weeks; full clinical effect 4-6 weeks (1) · Antidepressant effect over 1-2 weeks; anxiolytic effect over 4-6 weeks (1) · Antihypertensive effect within 1 week; heart-failure mortality benefit accrues over months of titration (1) · BP and symptomatic LUTS improvement within 1-2 weeks (2) · BP effect 1 hour; max at 4-6 hours (1) · BP effect 1-2 hours; max at 6 hours (1) · BP effect 1-2 weeks; antihypertensive peak 3-6 weeks (1) · BP effect 1-2 weeks; max at 2-3 weeks (1) · BP effect 2 hours; max at 4-6 weeks (1) · BP effect within 1-2 weeks (2) · BP effect within 24 hours; full effect at 1-2 weeks (long half-life) (1) · BP effect within hours (oral); 5-10 minutes (IV) (1) · BP effect within hours (oral); IOP reduction within 30 minutes, full effect 1-2 weeks (ophthalmic) (1) · BP effect within hours; full effect over 1-2 weeks (1) · BP lowering within 1 hour; max at 6 hours (1) · BP lowering within 1 hour; max effect at 6 hours (1) · Diuresis at 2 hours; antihypertensive effect within days, max at 3-4 weeks (1) · Diuresis at 2-3 hours; BP effect over weeks (1) · IR 20 minutes; ER ~6 hours (1) · IV: 1-3 minutes (SVT termination); PO IR: 30-60 minutes; ER: hours (1) · IV: 3-7 minutes (rate control); PO IR: 30-60 minutes; ER: hours (1) · IV: 5-20 minutes; PO: 30-60 minutes (1) · OCD effect over 1-2 weeks initial, with full effect typically 6-12 weeks; among the slowest SSRIs for OCD response (1)
halflife:
None (26) · 1-3 days acute, 4-6 days chronic; 4-16 days for norfluoxetine'"`UNIQ--ref-0000004C-QINU`"' (1) · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' (1) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · 12-15 hours (intermediate); '''no active metabolites''' (key clinical feature)'"`UNIQ--ref-00000023-QINU`"' (1) · 12-16 hours'"`UNIQ--ref-00000026-QINU`"' (1) · 14-25 hours (longer in elderly and hepatic impairment)'"`UNIQ--ref-00000026-QINU`"' (1) · 2 hours (parent); 6-9 hours for active carboxylic acid metabolite EXP3174'"`UNIQ--ref-000000BC-QINU`"' (1) · 2-5 hours (IR); ER formulations extend functional duration via osmotic/matrix release'"`UNIQ--ref-0000074D-QINU`"' (1) · 27-32 hours'"`UNIQ--ref-00000026-QINU`"' (1) · 3-4.5 hours (IR); 5-7 hours (ER; effective duration 24 hours via formulation)'"`UNIQ--ref-00000642-QINU`"' (1) · 3-7 hours (IR); functional 24 hours (ER)'"`UNIQ--ref-00000A6B-QINU`"' (1) · 3-7 hours (slow acetylators) vs 1-3 hours (rapid acetylators) via NAT2 polymorphism'"`UNIQ--ref-00000687-QINU`"' (1) · 30-40 hours (long; accumulates with chronic dosing)'"`UNIQ--ref-00000026-QINU`"' (1) · 30-50 hours'"`UNIQ--ref-00000078-QINU`"' (1) · 40-60 hours (notable for the thiazide class)'"`UNIQ--ref-00000783-QINU`"' (1) · 6-15 hours'"`UNIQ--ref-0000013E-QINU`"' (1) · 6-9 hours (substantially longer in renal impairment due to renal elimination)'"`UNIQ--ref-00000020-QINU`"' (1) · 7-10 hours'"`UNIQ--ref-0000001B-QINU`"' (1) · Buspirone 2-3 hours; 1-PP active metabolite 4-6 hours'"`UNIQ--ref-0000001D-QINU`"' (1) · Diazepam 20-50 hours; '''N-desmethyldiazepam (nordazepam) 30-200 hours''' is the major active metabolite and accumulates substantially with chronic dosing'"`UNIQ--ref-00000026-QINU`"' (1) · Venlafaxine 5 hours; desvenlafaxine active metabolite 11 hours'"`UNIQ--ref-00000026-QINU`"' (1) · ~11 hours (enalaprilat, the active metabolite)'"`UNIQ--ref-00000B84-QINU`"' (1) · ~12 hours (effective); terminal half-life is biphasic'"`UNIQ--ref-00000059-QINU`"' (1) · ~12 hours'"`UNIQ--ref-0000111F-QINU`"' (1) · ~13 hours'"`UNIQ--ref-0000056C-QINU`"' (1) · ~13-17 hours (ramiprilat, the active metabolite)'"`UNIQ--ref-00000C32-QINU`"' (1) · ~15 hours (IR)'"`UNIQ--ref-00000023-QINU`"' (1) · ~21 hours (with nonlinear pharmacokinetics from CYP2D6 autoinhibition)'"`UNIQ--ref-0000002B-QINU`"' (1) · ~22 hours'"`UNIQ--ref-00000AB0-QINU`"' (1) · ~24 hours (longest of the ARB class; suits patients with morning BP surge)'"`UNIQ--ref-00000AEE-QINU`"' (1) · ~4 hours (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~6 hours'"`UNIQ--ref-000004CD-QINU`"' (1) · ~6-8 hours'"`UNIQ--ref-0000001A-QINU`"' (1)
bioavailability:
None (26) · 42-58% (oral; dose-dependent)'"`UNIQ--ref-00000AEF-QINU`"' (1) · 60-80% (oral; not significantly affected by food)'"`UNIQ--ref-00000843-QINU`"' (1) · 64-90% (oral; not affected by food)'"`UNIQ--ref-00000079-QINU`"' (1) · 65-75% (oral)'"`UNIQ--ref-0000013F-QINU`"' (1) · 70–90% (oral) (1) · >90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-QINU`"' (1) · Highly variable due to saturable first-pass metabolism'"`UNIQ--ref-0000002C-QINU`"' (1) · ~20-35% (oral; extensive first-pass via CYP3A4 with R/S enantiomer differences)'"`UNIQ--ref-00000A6C-QINU`"' (1) · ~25% (oral; extensive first-pass)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~25% (oral; food does not affect absorption)'"`UNIQ--ref-0000005A-QINU`"' (1) · ~25% (oral; food reduces absorption ~40%)'"`UNIQ--ref-000004CE-QINU`"' (1) · ~25-35% (extensive first-pass), increased by food which slows absorption and reduces orthostatic risk'"`UNIQ--ref-0000001C-QINU`"' (1) · ~25-50% (oral; substantial first-pass via NAT2 acetylation, phenotype-dependent)'"`UNIQ--ref-00000688-QINU`"' (1) · ~26% (oral; prodrug hydrolyzed by intestinal esterases to active olmesartan; not affected by food)'"`UNIQ--ref-0000056D-QINU`"' (1) · ~28% (oral; food slows but does not reduce absorption)'"`UNIQ--ref-00000C33-QINU`"' (1) · ~33% (extensive first-pass via CYP2C9 and CYP3A4)'"`UNIQ--ref-000000BD-QINU`"' (1) · ~37% (oral; food does not affect)'"`UNIQ--ref-00000A23-QINU`"' (1) · ~4% (extensive first-pass metabolism)'"`UNIQ--ref-0000001E-QINU`"' (1) · ~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-QINU`"' (1) · ~45%'"`UNIQ--ref-00000027-QINU`"' (1) · ~50% (oral); systemic absorption from ophthalmic application is clinically meaningful via nasolacrimal drainage'"`UNIQ--ref-0000001C-QINU`"' (1) · ~50% (oral)'"`UNIQ--ref-00000021-QINU`"' (1) · ~50% IR (extensive first-pass via CYP3A4); ER products release-rate-limited'"`UNIQ--ref-0000074E-QINU`"' (1) · ~53% (oral)'"`UNIQ--ref-00000024-QINU`"' (1) · ~60% (oral; food does not affect absorption)'"`UNIQ--ref-00000B85-QINU`"' (1) · ~65% (oral)'"`UNIQ--ref-00000784-QINU`"' (1) · ~65% (oral)'"`UNIQ--ref-00000AB1-QINU`"' (1) · ~75-85% (oral); ~60% (transdermal at steady state)'"`UNIQ--ref-00000027-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000027-QINU`"' (2) · ~90% (oral)'"`UNIQ--ref-00000024-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~93% (oral); ~90% (rectal)'"`UNIQ--ref-00000027-QINU`"' (1)
pregnancy:
None (28) · '''Among the least preferred SSRIs in pregnancy.''' Observational signal for cardiac malformations (atrial and ventricular septal defects) with first-trimester exposure, and the most severe neonatal adaptation syndrome of any SSRI with third-trimester exposure'"`UNIQ--ref-0000002D-QINU`"' (1) · '''Among the safest antihypertensives in pregnancy''', recommended for chronic hypertension during pregnancy and first-line for severe hypertension in preeclampsia and eclampsia'"`UNIQ--ref-0000001C-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000000BE-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-000004CF-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-0000056E-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000844-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, hypocalvaria, hypotension. Stop on detection'"`UNIQ--ref-00000AF0-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-0000005B-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000A24-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension. Stop on detection'"`UNIQ--ref-00000B86-QINU`"' (1) · '''Contraindicated in pregnancy''' (all trimesters); fetal renal injury, oligohydramnios, skull hypoplasia, hypotension'"`UNIQ--ref-00000C34-QINU`"' (1) · '''Documented fetal growth restriction with chronic exposure'''; avoid in pregnancy if alternative β-blockers are appropriate. The β-blocker most consistently associated with intrauterine growth concerns'"`UNIQ--ref-00000022-QINU`"' (1) · Avoided where possible; same class concerns as HCTZ.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Category C'"`UNIQ--ref-0000004D-QINU`"' (1) · Limited data.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; alternative antihypertensives generally preferred. Crosses placenta.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; case series and registries suggest no major teratogenicity but other antihypertensives (labetalol, nifedipine) are typically preferred.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; labetalol/nifedipine generally preferred. Crosses placenta.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited data; rarely indicated in pregnancy.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; older agent with substantial use experience and no clear teratogenic signal.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; older agent with substantial use experience; some signal for first-trimester exposure but not conclusive.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Limited human data; β-blocker class effects include fetal growth restriction and neonatal bradycardia/hypoglycemia.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (2) · Observational signal for neonatal adaptation syndrome with late-pregnancy exposure; weigh against the risks of untreated maternal depression.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Observational signal for neonatal adaptation syndrome with third-trimester exposure (SSRI class effect).<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Older agent with substantial use experience but limited controlled data; case reports of neonatal sedation and transient hypertension with maternal use near term.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · One of the historically preferred IV agents for severe hypertension in pregnancy alongside labetalol and nifedipine.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Oral nifedipine is one of the preferred agents for severe hypertension in pregnancy and for tocolysis in preterm labor.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Some signal for cleft lip/palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1) · Some signal for cleft palate with first-trimester exposure (debated); neonatal sedation and withdrawal with third-trimester exposure.<sup class="pcp-cn" title="This claim needs a citation.">&#91;[[Pharmacopedia:Citation needed|citation&nbsp;needed]]&#93;</sup> (1)
legal:
None (26) · [[USLegal:Prescription only|Rx-only]] in US (23) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000025-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-00000028-QINU`"' (2) · [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults'"`UNIQ--ref-0000002E-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, like guanfacine and unlike the psychostimulant alternatives for ADHD'"`UNIQ--ref-00000028-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, which is a meaningful clinical advantage over benzodiazepine alternatives for chronic anxiety'"`UNIQ--ref-0000001F-QINU`"' (1) · [[USLegal:Prescription only|Rx-only]] in US. Not a controlled substance, which is a meaningful clinical advantage over the benzodiazepine alternatives for short-term anxiety'"`UNIQ--ref-00000028-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000025-QINU`"' (1) · [[USLegal:Schedule IV|Schedule IV controlled substance]] in US. Carries the benzodiazepine class '''Boxed Warning''' for risk of fatal respiratory depression, coma, and death when combined with opioids'"`UNIQ--ref-00000028-QINU`"' (2)

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