Metoprolol

Therapeutic Class
 Beta Blocker, Beta-1 Selective
Indications

Treatment of angina pectoris, hypertension, or hemodynamically-stable acute myocardial infarction; to reduce mortality/hospitalization in patients with heart failure (stable NYHA Class II or III) already receiving ACE inhibitors, diuretics, and/or digoxin; Treatment of ventricular arrhythmias, atrial ectopy; migraine prophylaxis, essential tremor, aggressive behavior (not recommended for dementia-associated aggression); prevention of reinfarction and sudden death after myocardial infarction; prevention and treatment of atrial fibrillation and atrial flutter; multifocal atrial tachycardia; symptomatic treatment of hypertrophic obstructive cardiomyopathy
Adult Doses

Angina: Oral:
Immediate release: Initial: 50 mg twice daily; usual dosage range: 50-200 mg twice daily; maximum: 400 mg/day; increase dose at weekly intervals to desired effect
Extended release: Initial: 100 mg/day (maximum: 400 mg/day)

Atrial fibrillation/flutter (ventricular rate control), supraventricular tachycardia (SVT) (acute treatment): I.V.: 2.5-5 mg every 2-5 minutes (maximum total dose: 15 mg over a 10-15 minute period). 
Maintenance: Oral (immediate release): 25-100 mg twice daily

Note: take precaution in patients with concomitant heart failure; avoid in patients with decompensated heart failure.

Heart failure: Oral: Extended release: Initial: 25 mg once daily; may double dosage every 2 weeks as tolerated (target dose: 200 mg/day)

Hypertension: Oral:Immediate release: Initial: 50 mg twice daily; effective dosage range: 100-450 mg/day in 2-3 divided doses; increase dose at weekly intervals to desired effect; maximum: 450 mg/day; usual dosage range : 50-100 mg/day
Extended release: Initial: 25-100 mg once daily; increase doses at weekly (or longer) intervals to desired effect; maximum: 400 mg/day; usual dosage range : 50-100 mg/day

Hypertension/ventricular rate control: I.V. (in patients having nonfunctioning GI tract): Initial: 1.25-5 mg every 6-12 hours; titrate initial dose to response. Initially, low doses may be appropriate to establish response; however, although not routine, up to 15 mg administered as frequently as every 3 hours has been employed in patients with refractory tachycardia.

Myocardial infarction:
Acute: I.V.: 5 mg every 2 minutes for 3 doses in early treatment of myocardial infarction; thereafter, give 50 mg orally every 6 hours beginning 15 minutes after last I.V. dose and continue for 48 hours; then administer a maintenance dose of 100 mg twice daily. 
Note: Do not initiate this regimen in those with signs of heart failure, a low output state, increased risk of cardiogenic shock, or other contraindications (eg, second- or third-degree heart block). Secondary prevention
Oral: Immediate release: 25-100 mg twice daily; optimize dose based on heart rate and blood pressure; continue indefinitely.
Pediatric Doses

Hypertension: Oral:
Immediate release tablet: Children: 1-17 years (National High Blood Pressure Education Program Working Group on High Blood Pressure in Children and Adolescents, 2004): Initial: 1-2 mg/kg/day; maximum 6 mg/kg/day (≤200 mg/day); administer in 2 divided doses
Extended release tablet: Children ≥6 years: Initial: 1 mg/kg once daily (maximum initial dose: 50 mg/day). Adjust dose based on patient response (maximum: 2 mg/kg/day or 200 mg/day)
Doses in Renal impairment

No adjustment required
Doses in Hepatic impairment

Reduced dose may be necessary
Contraindications

2nd or 3rd degree AV block; sick sinus syndrome; decompensated heart failure; clinically relevant sinus bradycardia. Severe peripheral arterial circulatory disorders. Cardiogenic shock. Asthma. Phaeochromocytoma (without α-blockade), systolic BP <100 mmHg. Metabolic acidosis. Pregnancy (2nd and 3rd trimesters).
Boxed Warning

Beta-blocker therapy should not be withdrawn abruptly (particularly in patients with CAD), but gradually tapered over 1-2 weeks to avoid acute tachycardia, hypertension, and/or ischemia
Warnings / Precautions

Compensated heart failure, bronchospastic disease, hepatic impairment, AV conduction disorders, bradycardia, peripheral arterial circulatory disorders. An α-blocker should be given concurrently in patients with phaeochromocytoma. May mask signs of acute hypoglycaemia. May mask symptoms of hyperthyroidism. Caution when used in patients with history of cardiac failure or those with minimal cardiac reserve. Avoid using anaesthetic agents that may depress the myocardium. May impair ability to drive or operate machinery. Myasthenia gravis; history of psychiatric disorder. Lactation. Avoid abrupt drug withdrawal.
Adverse Reactions

Bradycardia, hypotension, arterial insufficiency, chest pain, CHF, oedema, palpitation, syncope, gangrene; dizziness, fatigue, depression, confusion, headache, insomnia, short-term memory loss, nightmares, somnolence; pruritus, rash, increased psoriasis, reversible alopecia; sexual dysfunction/impotence, Peyronie's disease; diarrhoea, constipation, flatulence, GI pain, heartburn, nausea, xerostomia; agranulocytosis (rare); musculoskeletal pain; blurred vision, dry eyes, oculomucocutaneous syndrome; tinnitus; dyspnoea, bronchospasm, wheezing, rhinitis; cold extremities.
Potentially Fatal: Heart failure, heart block, bronchospasm.
Overdose Reactions

Symptoms: Hypotension, bradycardia, AV block, intraventricular conduction disturbances, cardiogenic shock, asystole, bronchospasm, hypoglycaemia, hyperkalaemia., convulsions, coma, respiratory arrest. Management: Supportive and symptomatic.
Drug Interactions

Additive effect with catecholamine-depleting drugs e.g. reserpine and MAOIs. May antagonise β1-adrenergic stimulating effects of sympathomimetics. Additive negative effects on SA or AV nodal conduction with cardiac glycosides, nondihydropyridine calcium-channel blockers. Increased oral bioavailability with aluminium/magnesium-containing antacids. Paradoxical response to epinephrine may occur. Increased plasma concentrations with CYP2D6 inhibitors (e.g. bupropion, cimetidine, diphenhydramine, fluoxetine, hydroxycholoquine, paroxetine, propafenone, quinidine, ritonavir, terbinafine, thioridazine). Increased risk of hypotension and heart failure with myocardial depressant general anaesthetics (e.g. diethyl ether). Risk of pulmonary hypertension with vasodilators e.g. hydralazine in uraemic patients. Reduced plasma levels with rifampicin. May increase negative inotropic and negative dromotropic effect of anti-arrhythmic drugs e.g. quinidine and amiodarone. Propafenone may increase serum levels of metoprolol. Concurrent use with indomethacin may reduce the antihypertensive efficacy of β-blocker. May reduce clearance of lidocaine. May increase effects of hypoglycaemics. Efficacy may be reduced by isoprenaline. Concurrent use with digoxin may lead to additive bradycardia.
Potentially Fatal: Additive or synergistic effects with verapamil; increased oral bioavailability with verapamil. Exacerbation of rebound hypertension during abrupt clonidine withdrawal.
See Below for More metoprolol Drug Interactions
Food Interactions

Food: Food increases absorption. Metoprolol serum levels may be increased if taken with food.

Herb/Nutraceutical: Avoid bayberry, blue cohosh, cayenne, ephedra, ginger, ginseng (American), gotu kola, licorice, (may worsen hypertension). Avoid black cohosh, California poppy, coleus, golden seal, hawthorn, mistletoe, periwinkle, quinine, shepherd's purse (may have increased antihypertensive effect)
Mechanism of Actions

Metoprolol selectively inhibits β-adrenergic receptors but has little or no effect on β2-receptors except in high doses. It has no membrane-stabilising nor intrinsic sympathomimetic activity.
Metabolism

Substrate of CYP2C19 (minor), 2D6 (major); Inhibits CYP2D6 (weak)
Pharmacodynamics

Onset of action: Peak effect: Oral: 1.5-4 hours; I.V.: 20 minutes (when infused over 10 minutes)

Duration: Oral: Immediate release: 10-20 hours, Extended release: ~24 hours; I.V.: 5-8 hours

Absorption: 95%, rapid and complete

Distribution: Vd: 5.5 L/kg

Protein binding: 12% to albumin

Metabolism: Extensively hepatic via CYP2D6; significant first-pass effect (~50%)

Bioavailability: Oral: ~50%

Half-life elimination: 3-8 hours (dependent on rate of CYP2D6 metabolism)

Excretion: Urine (<5% to 10% as unchanged drug)
Monitoring

Acute cardiac treatment: Monitor ECG and blood pressure with I.V. administration; heart rate and blood pressure with oral administration. I.V. use in a nonemergency situation: Necessary monitoring for surgical patients who are unable to take oral beta-blockers (because of prolonged ileus) has not been defined. Some institutions require monitoring of baseline and postinfusion heart rate and blood pressure when a patient's response to beta-blockade has not been characterized (ie, the patient's initial dose or following a change in dose). Consult individual institutional policies and procedures
Administration

May be taken with or without food.

Oral: Extended release tablets may be divided in half; do not crush or chew

I.V.: I.V. dose is much smaller than oral dose. When administered acutely for cardiac treatment, monitor ECG and blood pressure; may administer by rapid infusion (I.V. push) over 1 minute. May also be administered by slow infusion (ie, 5-10 mg of metoprolol in 50 mL of fluid) over ~30-60 minutes during less urgent situations (eg, substitution for oral metoprolol).
Pregnancy Category

C: Drug Pregnancy Category Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Lactation

Enters breast milk/use caution
Storage Conditions

Intravenous: Do not store above 30°C (86°F). Protect from light. Oral: Store at 15-30°C (59-86°F).
ATC Classification
 C07AB02 - metoprolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.
GenericPedia Classification
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    Storage

    Intravenous: Do not store above 30°C (86°F). Protect from light. Oral: Store at 15-30°C (59-86°F).
    Available As
  • Metoprolol 1 mg
  • Metoprolol 100 mg
  • Metoprolol 12.5 mg
  • Metoprolol 23.75 mg
  • Metoprolol 25 mg
  • Metoprolol 40 mg
  • Metoprolol 47.5 mg
  • Metoprolol 50 mg

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