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Metoprolol information from DrugsUpdate  

See Available Brands of Metoprolol in India

P - Contraindicated in pregnancy
FI - Food *

Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension. It is marketed under the brand name Lopressor by Novartis, and Toprol-XL (in the USA); Selokeen (in the Netherlands); as Minax by Alphapharm (in Australia), Metrol by Arrow Pharmaceuticals (in Australia), as Betaloc by AstraZeneca, as Neobloc by Unipharm (in Israel) and as Corvitol by Berlin-Chemie AG (in Germany). In India, this drug is available under the brand names of Metolar and Starpress. A number of generic products are available as well. The active substance metoprolol is employed either as metoprolol succinate or metoprolol tartrate (whereas 100 mg metoprolol tartrate corresponds to 95 mg metoprolol succinate), respectively as prolonged-release or conventional-release formulation.

Pharmacodynamics

Pharmacokinetics

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.

Duration
10-20 hours.

Absorption
Absorbed readily and completely for the GI tract (oral); peak plasma concentrations after 1.5-2 hours.

Distribution
Distributed widely, crosses the placenta and enters breast milk. Protein-binding: 12%.

Metabolism

Hepatic: By oxidative deamination, O-dealkylation followed by oxidation and aliphatic hydroxylation. Undergoes significant first-pass metabolism.

Excretion

Via urine (as metabolites and unchanged drug). Elimination half-life: 3-4 hours (fast hydroxylators), 7 hours (poor hydroxylators).

Metoprolol Indications / Metoprolol Uses

Information Not Available

Metoprolol Adverse Reactions / Metoprolol Side Effects

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.

Precautions

Information Not Available

Special 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.

Other 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.

Other Interactions

Food Interaction
Increased absorption with food. Bayberry, blue cohosh, cayenne, ephedra, ginger, American ginseng, gotu kola, licorice, yohimbe may exacerbate hypertension. Black cohosh, california poppy, coleus, garlic, golden seal, hawthorn, mistletoe, periwinkle, quinine, shepherd's purse have antihypertensive activity and may have an additive effect with metoprolol.

Dosage

Oral
Hypertension
Adult: Conventional preparation: Initially, 50-100 mg daily in single or 2 divided doses; may increase wkly to 400 mg daily depending on response. Maintenance: 100-200 mg daily; up to 400 mg daily. Extended-release preparation: 25-100 mg once daily.
Hepatic impairment: Reduce dose.

Oral
Angina pectoris
Adult: 50-100 mg bid-tid.
Hepatic impairment: Reduce dose.

Oral
Cardiac arrhythmias
Adult: 50 mg bid-tid; increased to 300 mg daily in divided doses if needed.
Hepatic impairment: Reduce dose.

Oral
Adjunct in hyperthyroidism
Adult: 50 mg 4 times daily.
Hepatic impairment: Reduce dose.

Oral
Prophylaxis of migraine
Adult: 100-200 mg daily in divided doses.
Hepatic impairment: Reduce dose.

Oral
Stable symptomatic heart failure
Adult: As a modified-release preparation of metoprolol succinate: Initially, 12.5-25 mg of equivalent metoprolol tartrate dose. Increase, as tolerated, at 2-weeks intervals to a max of 20 mg once daily.
Hepatic impairment: Reduce dose.

Intravenous
Emergency treatment of cardiac arrhythmias
Adult: Initially, up to 5 mg at a rate of 1-2 mg/min; may repeat at 5-minute intervals if needed up to a total dose of 10-15 mg. When acute arrhythmias are controlled, initiate maintenance therapy 4-6 hours after IV therapy using oral therapy not exceeding 50 mg tid.
Hepatic impairment: Reduce dose.

Intravenous
Prophylaxis or control of arrhythmias on induction of anaesthesia
Adult: 2-4 mg as slow injection; may repeat injections of 2 mg as necessary up to a max total dose of 10 mg.
Hepatic impairment: Reduce dose.

Intravenous
Adjunct in the early management of acute myocardial infarction
Adult: Admin within 12 hours of the onset of chest pain, 5 mg at 2-minute intervals to a total of 15 mg, if tolerated. After 15 minutes, for patients who have received full IV dose: Initiate oral therapy of 50 mg every 6 hours for 2 days; for patients who did not tolerate the full IV dose: Reduced oral dose should be given as and when their condition permits. Subsequent maintenance: 100 mg bid via oral route.
Hepatic impairment: Reduce dose.

Food(before/after)

May be taken with or without food

List of Contraindications

Metoprolol and Pregnancy

Contraindicated in pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

In 2nd & 3rd trimesters.
                   
Category D: There is positive evidence of human foetal risk, but the benefits from use in pregnant women may be acceptable despite the risk (e.g., if the drug is needed in a life-threatening situation or for a serious disease for which safer drugs cannot be used or are ineffective).

Metoprolol and Lactation

Information Not Available

Metoprolol and Children

Safety and efficacy not established (immediate-release); safety and efficacy not established in children younger than 6 years of age (ER).

Metoprolol and Geriatic

Information Not Available

Metoprolol and Other 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).

Storage

Intravenous
Do not store above 30°C (86°F). Protect from light.

Oral
Store at 15-30°C (59-86°F).

Lab interference

Intravenous
Do not store above 30°C (86°F). Protect from light.

Oral
Store at 15-30°C (59-86°F).

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