Pharmacology: Metoprolol, like all other β-blockers, are competitive antagonists at β-adrenergic receptor sites and are used in the management of cardiovascular disorder eg, hypertension, angina pectoris, cardiac arrythmias and myocardial infarction. They are also given to control symptoms of sympathetic over activity in alcohol withdrawal, anxiety states, hyperthyroidism and tremor, and in the prophylaxis of migraine and of bleeding associated with portal hypertension.
Pharmacokinetics: Metoprolol is readily and completely absorbed from the gastrointestinal tract but is subject to considerable first-pass metabolism. Peak plasma concentrations vary widely and occur about 1.5-2 hrs after a single oral dose. It is moderately lipid-soluble.
Management of hypertension, angina pectoris, cardiac arrythmias, myocardial infarction, hyperthyroidism and migraine.
Hypertension: 100-mg Tablet: Initial Dose: 1 tablet daily, increased weekly according to the response of the patient to 4 tablets, can be taken as single daily dose or twice daily. Maintenance Dose: 1-2 tablets daily taken with or immediately following a meal.
Angina Pectoris: 50-mg Tablet: 1-2 tablets 2 or 3 times daily.
Cardiac Arrythmias: 50-mg Tablet: 1 tablet to be taken 2 or 3 times daily, increased if necessary to 6 tablets daily in divided doses.
Should not be given to patients with heart failure unless it is controlled. Metabolic acidosis, sinus bradycardia or partial heart block.
Should not be given to patients with bronchospasm or asthma, or to those with history of obstructive airways disease.
Serious adverse effects include heart failure, heart block and bronchospasm. Metoprolol, like other β-blockers, are associated with fatigue, coldness of the extremities and sleep disturbances.
Fatigue is a common side effect experienced with metoprolol. Other side effects are reported as paresthesia, peripheral neuropathy and myopathies. Adverse gastrointestinal effects include nausea and vomiting, diarrhea, constipation and abdominal cramping.
Intravenous calcium antagonist of verapamil and diltiazem type class I antiarrhythmics. Antihistamines, H2 blockers, antidepressants, antipsychotics. Sympathomimetic ganglion-blocking agent, other β-blockers, monoamine oxidase inhibitors (MAOIs), clonidine, inhalation anesthetic, rifampicin, alcohol, hydralazine, indomethacin and other prostaglandin synthetase inhibitor. Oral antidiabetics. Digital glycosides.
Store at temperatures not exceeding 30°C.
C07AB02 - metoprolol ; Belongs to the class of selective beta-blocking agents. Used in the treatment of cardiovascular diseases.