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Labetalol

Non-selective beta-blocker with additional alpha-1 blocking activity · Antihypertensive

Also known as Labetalol hydrochloride

START
Check HR, BP (supine and standing). Baseline LFTs. Assess asthma/COPD history. Counsel on orthostatic hypotension—rise slowly from sitting/lying.
TYPICAL MAX
2400mg/day oral. Hepatotoxicity risk increases at higher doses—monitor LFTs. IV cumulative max 300mg for hypertensive emergency.
STOP IF
Severe hypotension, HR <50 bpm, acute hepatic injury (jaundice, LFTs >3x ULN), bronchospasm, heart block.
WATCH
Orthostatic BP at each visit (alpha-1 effect). Hepatotoxicity—immune-mediated hepatitis has been reported (rare but fatal); monitor LFTs. Tingling scalp is benign and transient with IV use. Do not stop abruptly—rebound hypertension risk.
CDSCO approvedATC C07AG01
Dose laddermg/d
100Start BID200Step-up BID400titrate1.2kHigh dose BID2.4kMax daily
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo adjustment (hepatically cleared)15FULLNo adjustment90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
30minONSET1.5hPEAK6.5h10hDURATION
ONSET
30min · Onset ~30 min
PEAK
1.5h · Tmax 1-2 hours
6.5h · t½ ~5-8 hours
DURATION
10h · 8-12 hours (oral)
EXCRETION
Fecal as metabolites (~55-60%)
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Preferred antihypertensive in pregnancy (with methyldopa and nifedipine). Extensive safety data in preeclampsia. May cause neonatal bradycardia and hypoglycemia if used near delivery—monitor newborn for 48-72h.
FDA category + note
Top interactionssee all 12
  • AdrenalineSevereTextbookKDT 7e · p133
  • AmilorideSevereTextbookKDT 7e
  • SofosbuvirSevereTextbookHarrison 22e · unknown
  • AminophyllineSevereDatabaseDDInter
Available in India

83 branded formulations. Look up specific brands in the Drugs workspace.

Mechanism

Competitive blockade of beta-1, beta-2, and alpha-1 adrenergic receptors. The alpha-1 blockade causes peripheral vasodilation (reduces afterload), while beta-blockade reduces heart rate and myocardial contractility. Ratio of alpha:beta blockade is 1:3 (oral) and 1:7 (IV).

Indications

Severe hypertension / hypertensive emergencies (IV)Chronic hypertension (oral)Hypertension in pregnancy (including preeclampsia/eclampsia—first-line)Hypertensive crisisClonidine withdrawal rebound hypertension

Dosing

Adult
Hypertension (oral): 100mg PO BID initially, increase by 100mg BID every 2-3 days to 200-400mg BID; max 2400mg/day. Hypertensive emergency (IV): 20mg IV over 2 min, then 20-80mg q10min to total 300mg; OR 1-2mg/min infusion. Preeclampsia: 200-400mg PO, then 200mg q8-12h; OR 20mg IV, then 40mg, then 80mg q10min.
Pediatric
Not established in children.
Renal adjustment
No adjustment needed (hepatically metabolized).
Hepatic adjustment
Reduce dose 50% in severe hepatic impairment.
Geriatric
Start 100mg daily; increased orthostatic hypotension risk.
Max dose
2400mg/day (oral); 300mg cumulative IV (hypertensive emergency)

Pharmacokinetics

Onset
Oral: 1-2 hours; IV: 2-5 minutes
Peak effect
Oral: Tmax 1-2 hours; IV: 5-15 minutes; antihypertensive peak at 2-4 weeks
Duration
Oral: 8-12 hours; IV: 2-6 hours (dose-dependent)
Half-life
~5-8 hours (oral); ~5.5 hours (IV)
Bioavailability
~25% (extensive first-pass metabolism)
Protein binding
~50%
Metabolism
Extensive hepatic via glucuronidation (major) and CYP2C19/CYP2D6; active and inactive metabolites
Excretion
~55-60% fecal (metabolites); 5-15% renal (unchanged + metabolites)

Contraindications

  • Severe bradycardia
  • Second or third-degree AV block
  • Sick sinus syndrome
  • Cardiogenic shock
  • Severe asthma or COPD
  • Hypersensitivity to labetalol

Side effects

Common
Orthostatic hypotension (alpha-1 blockade)DizzinessFatigueNauseaNasal congestionEjaculatory failureTingling scalp (transient with IV)Bradycardia
Serious
  • Severe hypotension / syncope
  • Severe bradycardia / heart block
  • Bronchospasm / asthma exacerbation
  • Hepatotoxicity (rare but potentially fatal—immune-mediated hepatitis)
  • Heart failure decompensation
  • Jaundice

Pregnancy & lactation

Pregnancy

Preferred antihypertensive in pregnancy (with methyldopa and nifedipine). Extensive safety data in preeclampsia. May cause neonatal bradycardia and hypoglycemia if used near delivery—monitor newborn for 48-72h.

Lactation

Excreted in breast milk in low concentrations (~milk:plasma ratio 0.3-0.7); infant receives <1% of maternal dose. Compatible with breastfeeding. Monitor infant for bradycardia.

Drug interactions

Adrenaline
Severe
Textbook

Marked rise in BP.

Adrenaline should not be given to patients receiving β blockers.

Source: KDT 7e · p133

Amiloride
Severe
Textbook

Hyperkalaemia more likely.

Source: KDT 7e

Sofosbuvir
Severe
Textbook

Severe bradycardia.

Extreme caution advised if amiodarone is co-administered with sofosbuvir and a beta blocker.

Source: Harrison 22e · unknown

Aminophylline
Severe
Database

Drug interaction classified as: antagonism

Source: DDInter

Arformoterol
Severe
Database

Drug interaction classified as: antagonism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clonidine
Severe
Database

Rebound hypertension risk with abrupt withdrawal of either drug.

Withdraw labetalol first over 1-2 weeks, then taper clonidine.

Source: Kimi deep-research + Cla

Diltiazem
Severe
Database

Increased propensity for AV block, severe bradycardia, and decreased left ventricular function.

Avoid concurrent administration. The concurrent administration of diltiazem with a beta blocker is contraindicated.

Source: DDInter

Disopyramide
Severe
Database

Clinical effect not specified

Source: DDInter

Dolasetron
Severe
Database

Clinical effect not specified

Source: DDInter

Dyphylline
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Ask House about Labetalol

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-19 · House clinical team·Cockpit curated: 2026-05-19