Metoprolol
- Atc Codes:C07AB02
- CAS Codes:98418-47-4#37350-58-6#56392-17-7
- PHARMGKB ID:98418-47-4#37350-58-6#56392-17-7
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Metobloc, Metohexal Retard, Metoprolol, Metotens, Seloken; Belgium: Lopresor, Metoprolol, Seloken, Selozok; Bulgaria: Betaloc, Egilok, Metoprolol, Metostad, Vasocardin; Cyprus: Betaloczok, Cardoxoner; Czech Republic: Belenzok, Betaloc, Egilok, Emzok, Lidazoc, Metoprolol, Metozok, Vasocardin, Verlok; Denmark: Betaloc, Mepronet, Metocar, Metoprolol, Metoratio, Seloken, Selo-zok; Estonia: Betaloc, Emzok, Metoprolol, Metotifi, Metozok, Spesimax; Finland: Metohexal, Metoprolin, Metoprolol, Seloken, Selopral, Spesicor; France: Selozok; Germany: Agoloc, Beloc, Beloken, Corvitol, Jeprolol, Jutabloc, Lopresor, Meprolol, Metobeta, Metodoc, Metodura, Metohexal, Metoprogamma, Prelis, Seloken, Selozok; Greece: Lopresor; Hungary: Betaloc, Egilok, Mecorlong, Metoprolol; Ireland: Betaloc, Metocor, Metop; Italy: Lopresor, Metoprololo, Seloken; Latvia: Betaloc, Corvitol, Egilok, Emzok, Metoprogamma, Metoprolol; Lithuania: Betaloc, Corvitol, Emzok, Metoprolol, Metotifi, Metprolong; Luxembourg: Lopresor, Metohexal, Metoprolol, Selozok; Malta: Metoprolol; Netherlands: Metoprololtartraat, Selokeen; Poland: Betaloc, Beto, Emzok, Mecorlong, Metocard, Metohexal, Metoprolol, Metostad; Portugal: Lopresor; Romania: Betaloc, Betaprol, Bloxan, Corvitol, Egilok, Emzok, Metopro, Metoprolol, Metosuccinat, Vasocardin; Slovakia: Betaloc, Corvitol, Egilok, Mertolok, Metoprolol, Vasocardin; Slovenia: Bloxan; Spain: Belokén, Lopresor; Sweden: Metomylan, Metoprolol, Metoratio, Mozoc, Seloken; UK: Betaloc, Lopresor.
North America
Canada: Betaloc, Lopresor, Metoprolol, Novo-Metoprol, Nu-Metop; USA: Lopressor, Metoprolol, Toprol.
Latin America
Argentina: Belozok, Lopresor; Brazil: Lopressor, Metoprolol, Seloken, Selozok; Mexico: Bioprol, Eurolol, Futaline, Kenaprol, Metopresol, Metoprolol, Proken, Prolaken, Promiced, Prontol, Ritmolol, Selectadril, Seloken Zok, Sermetrol, Tiazidol.
Asia
Japan: Cerekunart, Kokonalin, Lopresor, Medepine, Melucomon, Metoplic, Seloken, Sipseron, Zegmular.
Drug combinations
Metoprolol and Chlorthalidone
Metoprolol and Felodipine
Metoprolol and Hydrochlorothiazide
Metoprolol and Nifedipine
Metoprolol, Hydralazine, and Hydrochlorothiazide
Chemistry
Metoprolol Succinate: (C~15~H~25~NO~3~)~2~ C~4~H~6~O~4~. Mw: 652.82. (1) 2-Propanol, 1-[4-(2-methoxyethyl)phenoxy]-3-[(1-methylethyl)amino]-, (±)-, butanedioate (2:1); (2)(±)-1-(Isopropylamino)-3-[p-(2-methoxyethyl)phenoxy]-2-propanol succinate (2:1). CAS-98418-47-4; CAS-37350-58-6 (metroprolol)(1991).
Metoprolol Tartrate: (C~15~H~25~NO~3~)~2~ C~4~H~6~O~6~. Mw: 684.81. 2-Propanol, 1-[4-(2-methoxyethyl)phenoxy]-3-[(1-methylethyl)amino]-, (±)-, [R-(R*,R*)]-2,3-dihydroxybutanedioate (2:1). CAS-56392-17-7(1978).
Pharmacologic Category
Cardiovascular Drugs; β-Adrenergic Blocking Agents. (ATC-Code: C07AB02).
Mechanism of action
Competitively blocks β~1~-receptors, with little or no effect on β~2~-receptors at doses <100 mg.
Therapeutic use
Treatment of angina pectoris, hypertension, or hemodynamically-stable acute myocardial infarction. Treatment of angina pectoris or hypertension. To reduce mortality/hospitalization in heart failure patients already receiving ACEIs, diuretics, and/or digoxin.
Pregnancy and lactiation implications
Teratogenic effects not observed in animal studies. Metoprolol crosses placenta. β-Blockers generally safe during pregnancy. Cases of neonatal hypoglycemia reported following maternal use of β-blockers at parturition. Enters breast milk (use caution).
Unlabeled use
Treatment of ventricular arrhythmias, atrial ectopy. Migraine prophylaxis, essential tremor, aggressive behavior (not recommended for dementia-associated aggression). Prevention of myocardial infarction, atrial fibrillation, and atrial flutter. Symptomatic treatment of hypertrophic obstructive cardiomyopathy.
Contraindications
Hypersensitivity to metoprolol, any component of the formulation, or other β-blockers. Sick sinus syndrome (except in patients with a functioning artificial pacemaker). Severe peripheral arterial disease. Pheochromocytoma (without α-blockade). Severe sinus bradycardia (heart rate <45 beats/minute). Significant first-degree heart block (P-R interval ≥0.24 s). Second- and third-degree heart block. Systolic blood pressure <100 mm Hg. Moderate-to-severe cardiac failure. Cardiogenic shock.
Warnings and precautions
Use caution with history of severe anaphylaxis to allergens. Metoprolol commonly produces mild first-degree heart block (P-R interval >0.2-0.24 s). Metoprolol may also produce severe first- (P-R interval ≥0.26 s), second-, or third-degree heart block. Symptomatic hypotension might occur. In general, bronchospastic disease patients should not receive β-blockers. Use with caution in diabetes mellitus (may potentiate hypoglycemia and/or mask signs and symptoms), in compensated heart failure, in hepatic impairment, in myasthenia gravis, and in peripheral vascular disease (including Raynaud’s). Adequate α-blockade required prior to use of any β-blocker in untreated pheochromocytoma. Use with caution in history of psychiatric illness (might cause or exacerbate CNS depression). β-Blockade might mask signs of hyperthyroidism (e.g. tachycardia). Abrupt discontinuation might exacerbate symptoms of hyperthyroidism and may also induce thyroid storm. Use with caution in patients receiving inhalation anesthetic agents which may decrease myocardial function, or in patients on concurrent verapamil or diltiazem (risk of bradycardia or heart block). Use care in compensated heart failure. β-Blocker therapy should not be withdrawn abruptly.