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Metoprolol

Beta Blocker · Antihypertensive

Also known as Metoprolol tartrate, Metoprolol succinate, Lopressor, Toprol XL, Betaloc, Metocard

START
25 mg PO BID (tartrate) or 25-50 mg once daily (succinate XR)
TYPICAL MAX
400 mg/day
STOP IF
Severe bradycardia (HR <50) · 2nd-3rd degree AV block · decompensated HF · cardiogenic shock
WATCH
HR · BP · symptom control · CYP2D6 poor metabolizer status
CDSCO approvedSchedule HJan AushadhiATC C07AB02
Dose laddermg/d
25start50standard100moderate200titrate400max daily
Renal dose adjustmenteGFR mL/min/1.73m²
FULLNo renal adjustment (CYP2D6 hepatic clearance)90

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours
1hONSET1.5hPEAK4h12hDURATION
ONSET
1h · β-blockade onset
PEAK
1.5h · Cmax tartrate (XR: 7h)
4h · plasma t½ (tartrate); XR formulation extends
DURATION
12h · BID dosing window (XR: 24h)
EXCRETION
CYP2D6 hepatic · 5% renal unchanged
route + CYP
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
Category C — relatively safe; growth restriction with chronic use
FDA category + note
Top interactionssee all 12
  • LidocaineSevereTextbook-citedKDT 7e · p950
  • AdrenalineSevereTextbookKDT 7e · p133
  • AmilorideSevereTextbookKDT 7e
  • PridopidineSevereTextbookG&G 14e · p1591
Available in India

709 branded formulations and 613 fixed-dose combinations. Look up specific brands in the Drugs workspace.

Jan Aushadhi — generic available at GoI pharmacies

Mechanism

Metoprolol is a cardioselective beta-1 adrenergic blocker that competitively blocks beta-1 receptors primarily located in the heart, reducing heart rate, myocardial contractility, and cardiac output. It also reduces renin release from the kidneys, contributing to its antihypertensive effect. At higher doses, it may also block beta-2 receptors.

Indications

HypertensionAngina PectorisMyocardial Infarction (early and long-term management)Heart Failure (stable chronic heart failure, metoprolol succinate extended-release only)Supraventricular TachycardiaMigraine Prophylaxis (off-label)Essential Tremor (off-label)Anxiety (off-label)essential hypertensiontachycardiaheart failurevasovagal syncopesecondary prevention after myocardial infarctionadjunct in treatment of hyperthyroidismmigraine prophylaxisanginaprevention of arrhythmiasrate control in atrial fibrillationmigraineHypertension (extended-release succinate salt preferred for chronic HTN)CHFMyocardial infarction (i.v. in early treatment)mild to moderate (NYHA class II, III) dilated cardiomyopathy with systolic dysfunction (as add-on to ACE inhibitor ± diuretic, digitalis)Mitigating ischemic pain of STEMIReducing risks of reinfarction and ventricular fibrillationLong-term secondary prevention after STEMI

Dosing

Adult
Hypertension: Initial 25-100 mg once daily (succinate ER) or 50-100 mg daily in 1-2 divided doses (tartrate IR). Titrate every 1-2 weeks to desired effect, typically 100-200 mg/day. Angina: Initial 50 mg twice daily (tartrate IR) or 100 mg once daily (succinate ER). Titrate to response, typically 100-200 mg/day.…
Pediatric
Hypertension (≥6 years): Initial 0.5-1 mg/kg once daily (succinate ER), max 50 mg/day. Titrate up to 2 mg/kg/day (max 200 mg/day).
Renal adjustment
No dose adjustment typically required for renal impairment (including hemodialysis).
Hepatic adjustment
Dose reduction may be necessary in severe hepatic impairment (e.g., cirrhosis). Start with lower doses and titrate carefully.
Geriatric
Start with lower doses (e.g., 25 mg once daily) and titrate slowly due to increased sensitivity and potential for adverse effects (bradycardia, hypotension).
Max dose
400 mg/day (for metoprolol tartrate); 200 mg/day (for metoprolol succinate ER)

Pharmacokinetics

Onset
Oral (tartrate): ~15 minutes; Oral (succinate ER): ~1 hour; IV: Immediate
Peak effect
Oral (tartrate): 1.5-2 hours; Oral (succinate ER): 6-12 hours; IV: 20 minutes
Duration
Oral (tartrate): 6-12 hours; Oral (succinate ER): 24 hours
Half-life
3-7 hours
Bioavailability
~50% (oral, due to extensive first-pass metabolism)
Protein binding
~10-12%
Metabolism
Primarily hepatic, via CYP2D6 (extensive first-pass metabolism)
Excretion
Primarily renal (95% as metabolites, 5% as unchanged drug)

Contraindications

  • Sinus bradycardia (<45-50 bpm)
  • Second or third-degree atrioventricular (AV) block
  • Sick sinus syndrome (unless permanent pacemaker in place)
  • Cardiogenic shock
  • Decompensated heart failure
  • Severe peripheral arterial disease
  • Untreated pheochromocytoma
  • Severe bronchial asthma or severe COPD
  • Hypersensitivity to metoprolol or other beta-blockers
  • acute myocardial infarction (contraindicated if heart rate <45 bpm, heart block >first-degree, SBP <100 mmHg, or moderate-to-severe heart failure)
  • abrupt discontinuation (withdrawal syndrome)
  • Asthma
  • Peripheral vascular disease
  • Hypoglycemia
  • AV block (grade 2-3)
  • acute heart failure episode (should be stopped)
  • worsening of heart failure upon introduction
  • asymptomatic left ventricular dysfunction
  • Signs of acute heart failure
  • Evidence of a low-output state
  • Increased risk for cardiogenic shock
  • Bradycardia (>60 beats/min for IV use, otherwise a contraindication)
  • PR interval >0.24 s
  • Second- or third-degree heart block
  • Active asthma
  • Reactive airway disease
  • Severe HF or severely compromised LV function
  • Contraindicated in high-grade heart block

Side effects

Common
BradycardiaDizzinessFatigueHypotensionNauseaDiarrheaShortness of breath (especially in susceptible patients)Cold extremitiesHeadacheInsomnia/sleep disturbancesfluid retentionBronchospasmPeripheral vasoconstrictionWorsening of acute heart failureDepressionWorsening of psoriasisIncreased triglyceridesDecreased HDL cholesterolMilder side effects than propranololLess propensity to cause bronchoconstriction (though still avoided in asthmatics)Less interference with carbohydrate metabolismLower incidence of cold hands and feetNo/less deleterious effect on blood lipid profileAsthmaExercise intoleranceImpaired concentration
Serious
  • Severe bradycardia or heart block
  • Exacerbation of heart failure
  • Bronchospasm (in asthmatics/COPD patients)
  • Masking of hypoglycemia symptoms in diabetics
  • Raynaud's phenomenon exacerbation
  • Psoriasiform rash
  • Severe allergic reactions
  • Sudden withdrawal syndrome (rebound hypertension, angina, MI)
  • life-threatening bradyarrhythmias (with AV conduction defects or other drugs)
  • exacerbation of angina (abrupt discontinuation)
  • increased risk of sudden death (abrupt discontinuation)
  • blunted recognition/delayed recovery from hypoglycemia
  • AV block
  • bronchospasm
  • worsening of acute heart failure
  • depression
  • worsening of psoriasis
  • Withdrawal syndrome (rebound hypertension, exacerbation of CAD symptoms)
  • Severe hypertension and bradycardia (if used with epinephrine in nonselective beta blockers)

Pregnancy & lactation

Pregnancy

Category C — relatively safe; growth restriction with chronic use

Lactation

Excreted into breast milk in small amounts; generally considered compatible with breastfeeding, but monitor infant for signs of beta-blockade (e.g., bradycardia, hypoglycemia).

Drug interactions

Lidocaine
Severe
Textbook-cited

Enhanced bradycardia and hypotension.

Avoid concurrent use

Source: KDT 7e · p950

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

Pridopidine
Severe
Textbook

metoprolol AUC increased 5.1-fold.

coadministration generally contraindicate[d] or at least require[s] dosage adjustment.

Source: G&G 14e · p1591

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

Atazanavir
Severe
Database

Drug interaction classified as: synergy.

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Clonidine
Severe
Database

Severe rebound hypertension on clonidine withdrawal.

Taper clonidine slowly. Stop BB 2-3 days before stopping clonidine.

Source: DDInter

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

.

Source: DDInter

Related guidelines

Other Beta Blocker drugs

Ask House about Metoprolol

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

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Katzung·Verified: 2026-05-17 · House clinical team·Cockpit curated: 2026-05-16