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Medicines > classes : Dissociative or Opioid or [[:Category:Antihypertensives|Antihypertensive]]

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generic:
Codeine (2)
brand:
None (29)
classes: (Click arrow to add another value)
mechanism:
None (12) · Potent mu-opioid receptor agonist (6) · Mu-opioid receptor agonist (4) · NMDA antagonist (3) · NMDA antagonist; sigma receptor agonist (2)
uses:
None (50) · Mild to moderate pain; cough suppression (low-dose). (1) · Treatment-resistant depression (TRD) in adults, as adjunct to oral antidepressant (FDA-approved March 2019). Depressive symptoms in adults with MDD with acute suicidal ideation or behavior (FDA-approved Aug 2020). (1) · '"`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-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 (50) · 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) · Adult: 15–60 mg every 4 hours as needed. (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) · Induction (TRD): 56 mg intranasal twice weekly × 4 weeks. Maintenance: 56-84 mg once weekly × 4 weeks, then 56-84 mg every 1-2 weeks. For acute suicidality: 84 mg twice weekly × 4 weeks. Administered under medical supervision in REMS-certified site. (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) · 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)
preparations:
None (50) · 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) · 28 mg/device (each dose uses 2 devices) (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 3.125, 6.25, 12.5, 25 mg; Coreg CR capsules 10, 20, 40, 80 mg (once-daily) (1) · Tablet (15, 30, 60 mg); oral solution; combination products (with [[Acetaminophen|acetaminophen]] or ibuprofen). (1) · Tablets 100, 200, 300 mg; injection 5 mg/mL (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)
halflife:
None (50) · 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) · 2.5–3 hours (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) · 30-50 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) · ~7-12 hours (1)
bioavailability:
None (50) · 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) · ~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) · ~48% intranasal (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% (variable, CYP2D6-dependent for analgesic effect). (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 (51) · '''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) · Avoid; may cause fetal harm (1) · Avoid; risk of neonatal opioid withdrawal with chronic use; UM-mother breastfeeding contraindicated. (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; 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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