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Medicines > classes: [[:Category:Antihypertensives|Antihypertensive]] & routes : Oral or Oral; sublingual IR is discouraged (uncontrolled BP drops

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classes: (Click arrow to add another value)
mechanism:
None (10) · '"`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-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:
'"`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-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`"' (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-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-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:
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) · 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) · 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) · 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)
routes: (Click arrow to add another value)
halflife:
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) · 3-7 hours (slow acetylators) vs 1-3 hours (rapid acetylators) via NAT2 polymorphism'"`UNIQ--ref-00000687-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) · ~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) · ~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:
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) · ~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) · ~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)
pregnancy:
None (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) · Limited data.<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; 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; 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)

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