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Medicines > classes : Tryptamine or [[:Category:Anticonvulsants|Anticonvulsant]] or [[:Category:Antihypertensives|Antihypertensive]]

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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) · Avapro (1) · Benicar (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) · Hytrin (US brand discontinued); mostly generic (1) · Kapvay (ER, ADHD), Catapres (IR, antihypertensive), Catapres-TTS (transdermal patch), Duraclon (epidural injection) (1) · Keppra (IR), Keppra XR, Spritam (3D-printed orally disintegrating), Roweepra (1) · Klonopin (1) · Lamictal (IR), Lamictal XR, Lamictal ODT (1) · Lotensin (1) · Lyrica (IR), Lyrica CR (1) · Micardis (1) · Microzide; mostly prescribed generically (1) · Mysoline (1) · Neurontin (IR), Gralise (ER), Horizant (gabapentin enacarbil ER) (1) · Norvasc, Katerzia (1) · Procardia, Procardia XL, Adalat CC, Afeditab CR (1) · Tegretol (IR, XR, suspension), Carbatrol (ER), Equetro (ER for bipolar), Epitol (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) · Topamax (IR), Trokendi XR, Qudexy XR, Eprontia (oral solution); component of Qsymia (with phentermine) (1) · Trandate, Normodyne (discontinued in US) (1) · Trileptal (IR), Oxtellar XR (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) · Zestril, Prinivil, Qbrelis (1)
classes: (Click arrow to add another value)
mechanism:
None (20) · 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) · '"`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`"' 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-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-00000015-QINU`"', '"`UNIQ--vote-00000016-QINU`"' (1) · '"`UNIQ--vote-00000017-QINU`"', '"`UNIQ--vote-00000018-QINU`"', '"`UNIQ--vote-00000019-QINU`"' (2) · '"`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`"' (1) · '"`UNIQ--vote-0000001B-QINU`"', '"`UNIQ--vote-0000001C-QINU`"', '"`UNIQ--vote-0000001D-QINU`"', '"`UNIQ--vote-0000001E-QINU`"', '"`UNIQ--vote-0000001F-QINU`"' (1) · '"`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`"' (4) · '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"' (1) · '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"' (1) · '"`UNIQ--vote-00000021-QINU`"', '"`UNIQ--vote-00000022-QINU`"', '"`UNIQ--vote-00000023-QINU`"', '"`UNIQ--vote-00000024-QINU`"', '"`UNIQ--vote-00000025-QINU`"', '"`UNIQ--vote-00000026-QINU`"', '"`UNIQ--vote-00000027-QINU`"', '"`UNIQ--vote-00000028-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 (27) · 1 mg PO at bedtime to limit first-dose syncope; titrate weekly to 5-10 mg (1) · 10 mg PO once daily (5 mg if on a diuretic); titrate to 40 mg (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) · 300 mg PO at bedtime night 1, 300 mg BID day 2, 300 mg TID day 3; titrate to clinical effect, commonly 1800-3600 mg/day divided TID (1) · 40 mg PO once daily; titrate to 80 mg (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 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) · Adult monotherapy: 300 mg PO BID, titrate by 300 mg every 3 days. Pediatric: weight-based titration starting 8-10 mg/kg/day divided BID (1) · Adult: 500 mg PO BID, titrate by 1000 mg/day every 2 weeks. Pediatric: 10-20 mg/kg/day divided BID, weight-titrated (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: 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) · 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) · Migraine: 25 mg PO at bedtime, titrate by 25 mg weekly to target 100 mg/day divided BID. Seizures: 25-50 mg/day, titrate weekly to 200-400 mg/day divided BID (1) · Neuropathic pain: 75 mg PO BID, titrate to 150 mg BID after 1 week. Fibromyalgia: 75 mg PO BID, titrate to 150 mg BID. Anxiety (off-label): 75-150 mg/day divided BID-TID (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) · 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) · Seizures: 200 mg PO BID, titrate by 200 mg/week to 800-1200 mg/day. Trigeminal neuralgia: 100-200 mg BID, titrate to 200-400 mg TID. Bipolar: 200 mg BID, titrate to 1600 mg/day (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, 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) · Capsules 100, 300, 400 mg; tablets 600, 800 mg; oral solution 250 mg/5 mL; Gralise ER tablets 300, 600 mg (once-daily); Horizant ER tablets 300, 600 mg (gabapentin enacarbil, an inactive parent compound metabolized to gabapentin in vivo) (1) · Capsules 25, 50, 75, 100, 150, 200, 225, 300 mg; oral solution 20 mg/mL; Lyrica CR tablets 82.5, 165, 330 mg (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 150, 300, 600 mg; oral suspension 60 mg/mL; XR tablets 150, 300, 600 mg (Oxtellar) (1) · IR tablets 200 mg; chewable 100 mg; oral suspension 100 mg/5 mL; XR tablets 100, 200, 400 mg (Tegretol XR); ER capsules 100, 200, 300 mg (Carbatrol, Equetro) (1) · IR tablets 25, 100, 150, 200 mg; chewable dispersible tablets 2, 5, 25 mg; ODT 25, 50, 100, 200 mg; XR tablets 25, 50, 100, 200, 250, 300 mg (1) · IR tablets 25, 50, 100, 200 mg; sprinkle capsules 15, 25 mg; Trokendi XR capsules 25, 50, 100, 200 mg; Qudexy XR capsules; Eprontia oral solution 25 mg/mL (1) · IR tablets 250, 500, 750, 1000 mg; XR tablets 500, 750 mg; oral solution 100 mg/mL; injection 100 mg/mL; Spritam ODT 250, 500, 750, 1000 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; orally disintegrating tablets 0.125, 0.25, 0.5, 1, 2 mg (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 50, 250 mg (1)
fda max:
None (26) · 10 mg/d (1) · 100 mg/d (1) · 100 mg/d (rarely used) (1) · 100-200 mg/day depending on indication (1) · 120 mg/d (ER); IR not for chronic hypertension (1) · 1200 mg/day (adult seizures); 1600 mg/day (bipolar mania) (1) · 16 mg/d (IR); 8 mg/d (XL) (1) · 1600 mg/day (theoretical seizure dosing); practical use 400 mg/day for seizures, 100-200 mg/day for migraine prophylaxis (1) · 2 g/day (seizures); typically much lower for essential tremor (1) · 2.4 mg/day (HTN, IR); 0.4 mg/day (ADHD, Kapvay) (1) · 20 mg/d (1) · 20 mg/d (hypertension); 10 mg/d (other indications typical) (1) · 20 mg/day (seizures); commonly limited to 4 mg/day for anxiety in current practice (1) · 2400 mg/day (adult) (1) · 2400 mg/day (oral); 300 mg total per IV bolus dosing series (1) · 300 mg/d (1) · 300 mg/d typical practical limit (toxicity rises sharply above) (1) · 3000 mg/day (1) · 320 mg/d (hypertension); 320 mg/d (HF) (1) · 3600 mg/day; off-label doses higher are common but bioavailability saturates well below this (1) · 40 mg/d (2) · 40 mg/day (oral, anxiety) (1) · 400 mg/day (bipolar monotherapy); 700 mg/day (epilepsy with enzyme-inducing comedication) (1) · 50 mg BID in heart failure (or once-daily equivalent CR); 25 mg BID in hypertension (1) · 50 mg/d (hypertension); up to 200 mg/d (edema) (1) · 60 mg/day (oral, hypertension); 0.5% BID (ophthalmic) (1) · 600 mg/day (seizures); 450 mg/day (fibromyalgia and neuropathic pain) (1) · 80 mg/d (3) · ~480 mg/d (oral) for cardiovascular indications; higher off-label for cluster (1) · ~480 mg/d (oral); IV per protocol (1)
onset:
None (26) · 1-2 weeks for neuropathic pain and anxiolytic effect; anticonvulsant effect at therapeutic plasma level (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) · Anticonvulsant effect emerges with slow titration over weeks; tremor effect over weeks (1) · Anticonvulsant effect within days at therapeutic level; migraine prophylaxis effect emerges over 2-3 months (1) · Anticonvulsant effect within days at therapeutic plasma level (1) · Anticonvulsant effect within days at therapeutic plasma level; rapid titration possible (1) · Anticonvulsant effect within days; trigeminal neuralgia relief 24-72 hours; mood-stabilizing effect over weeks (1) · Antiepileptic effect within days at therapeutic level; mood-stabilizing effect emerges over 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) · Neuropathic pain and fibromyalgia effect emerges over 1-2 weeks (1)
halflife:
None (26) · '''Autoinduction''': 25-65 hours initially, falling to 12-17 hours after 2-3 weeks of dosing as carbamazepine induces its own CYP3A4 metabolism. Major clinical implication: doses require re-titration after the autoinduction period'"`UNIQ--ref-0000001D-QINU`"' (1) · 10-11 hours (benazeprilat, the active metabolite)'"`UNIQ--ref-00000A22-QINU`"' (1) · 11-15 hours'"`UNIQ--ref-00000842-QINU`"' (1) · 12-16 hours'"`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) · 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) · 5-7 hours'"`UNIQ--ref-00000029-QINU`"' (1) · 6-15 hours'"`UNIQ--ref-0000013E-QINU`"' (1) · 6-8 hours'"`UNIQ--ref-0000001F-QINU`"' (1) · 6-9 hours (substantially longer in renal impairment due to renal elimination)'"`UNIQ--ref-00000020-QINU`"' (1) · 6.3 hours'"`UNIQ--ref-00000026-QINU`"' (1) · 7-10 hours'"`UNIQ--ref-0000001B-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) · Oxcarbazepine 2 hours; '''10-monohydroxy active metabolite (MHD) ~9 hours''' (the agent that produces essentially all of the clinical effect)'"`UNIQ--ref-0000001A-QINU`"' (1) · Primidone 5-15 hours; '''phenobarbital active metabolite 50-150 hours'''; PEMA (phenylethylmalonamide) active metabolite 16 hours'"`UNIQ--ref-00000017-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) · ~21 hours'"`UNIQ--ref-00000028-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) · ~25-33 hours alone; ~15 hours with enzyme inducers; '''≥60 hours with valproate''' (UGT inhibition)'"`UNIQ--ref-00000025-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) · '''Saturable''' via the LAT-1 amino-acid transporter, producing nonlinear pharmacokinetics: ~60% at 300 mg single dose, falling to ~35% at 1200 mg single dose'"`UNIQ--ref-0000002A-QINU`"' (1) · 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) · >90% (oral; not significantly affected by food)'"`UNIQ--ref-00001120-QINU`"' (1) · ~100% (oral)'"`UNIQ--ref-0000001B-QINU`"' (1) · ~100% (oral)'"`UNIQ--ref-00000020-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) · ~40% (oral; extensive first-pass via CYP3A4)'"`UNIQ--ref-00000643-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) · ~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-0000001E-QINU`"' (1) · ~80% (oral)'"`UNIQ--ref-00000029-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000018-QINU`"' (1) · ~90% (oral)'"`UNIQ--ref-00000027-QINU`"' (1) · ~93% (oral); ~90% (rectal)'"`UNIQ--ref-00000027-QINU`"' (1) · ~98% (oral)'"`UNIQ--ref-00000026-QINU`"' (1) · ≥90% (linear pharmacokinetics, distinguishing it favorably from gabapentin's saturable LAT-1 absorption)'"`UNIQ--ref-00000027-QINU`"' (1)
pregnancy:
None (27) · '''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) · '''Among the safest mood stabilizers in pregnancy''' with reassuring monotherapy registry data, in sharp contrast to valproate. Estrogen-containing contraceptives accelerate lamotrigine metabolism, requiring dose adjustments at start and stop of contraception'"`UNIQ--ref-00000027-QINU`"' (1) · '''Considered one of the safest anticonvulsants in pregnancy''', with reassuring monotherapy registry data comparable to lamotrigine and in sharp contrast to valproate, topiramate, and carbamazepine'"`UNIQ--ref-00000021-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) · '''Substantial teratogenic risk''' including cleft lip/palate, hypospadias, and growth restriction (pregnancy registry data clear); effective contraception and pre-pregnancy counseling are required in reproductive-age patients'"`UNIQ--ref-0000002A-QINU`"' (1) · '''Substantial teratogenic risk''' including neural tube defects, craniofacial malformations, cardiac defects, and growth restriction; folic acid supplementation and effective contraception are required in reproductive-age patients'"`UNIQ--ref-0000001F-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) · 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; some signal for cardiac malformations and developmental delay but confounded by maternal disease and polytherapy.<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) · 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 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 major congenital malformations; limited human data.<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) · Teratogenic signal less than carbamazepine but present; folate supplementation and effective contraception are appropriate in reproductive-age patients'"`UNIQ--ref-0000001C-QINU`"' (1)

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