IMPORTANT SAFETY INFORMATION
INDICATIONS AND USAGE
LOPRESSOR (metoprolol tartrate) tablets are beta blockers and indicated for the treatment of Hypertension, Angina pectoris and Myocardial Infarction in adult patients.
ADMINISTRATION
Administer LOPRESSOR (metoprolol tartrate) tablets orally once daily with food or after a meal.
CONTRAINDICATIONS
LOPRESSOR is contraindicated in severe bradycardia, second- or third-degree heart block, cardiogenic shock, systolic blood pressure <100, decompensated heart failure, sick sinus syndrome (unless a permanent pacemaker is in place), and in patients who are hypersensitive to any component of this product.
WARNINGS AND PRECAUTIONS
Abrupt Cessation of Therapy: Following abrupt cessation of therapy with certain beta-blocking agents, exacerbations of angina pectoris and, in some cases, myocardial infarction have occurred. When discontinuing chronically administered LOPRESSOR, particularly in patients with ischemic heart disease, gradually reduce the dosage over a period of 1 to 2 weeks and monitor the patient. If angina markedly worsens or acute coronary ischemia develops, promptly reinstate LOPRESSOR, and take measures appropriate for the management of unstable angina. Warn patients not to interrupt therapy without their physician’s advice. Because coronary artery disease is common and may be unrecognized, avoid abruptly discontinuing LOPRESSOR in patients treated only for hypertension.
Heart Failure: Worsening cardiac failure may occur during up-titration of LOPRESSOR. If such symptoms occur, increase diuretics and restore clinical stability before advancing the dose of LOPRESSOR [see Dosage and Administration (2)]. It may be necessary to lower the dose of LOPRESSOR or temporarily discontinue it. Such episodes do not preclude subsequent successful titration of LOPRESSOR.
Bronchospastic Disease: Patients with bronchospastic disease, should in general, not receive beta-blockers, including Lopressor. Because of its relative beta1 cardio-selectivity, however, LOPRESSOR may be used in patients with bronchospastic disease who do not respond to, or cannot tolerate, other antihypertensive treatment. Because beta1-selectivity is not absolute, use the lowest possible dose of LOPRESSOR. Bronchodilators, including beta2-agonists, should be readily available or administered concomitantly [see Dosage and Administration (2)].
Pheochromocytoma: If LOPRESSOR is used in the setting of pheochromocytoma, it should be given in combination with an alpha blocker, and only after the alpha blocker has been initiated. Administration of beta-blockers alone in the setting of pheochromocytoma has been associated with a paradoxical increase in blood pressure due to the attenuation of beta-mediated vasodilatation in skeletal muscle.
Major Surgery: Avoid initiation of a high-dose regimen of beta-blocker therapy in patients undergoing non-cardiac surgery, since such use in patients with cardiovascular risk factors has been associated with bradycardia, hypotension, stroke and death.
Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery, however, the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.
Hypoglycemia: Beta-blockers may prevent early warning signs of hypoglycemia, such as tachycardia, and increase the risk for severe or prolonged hypoglycemia at any time during treatment, especially in patients with diabetes mellitus or children and patients who are fasting (i.e., surgery, not eating regularly, or are vomiting). If severe hypoglycemia occurs, patients should be instructed to seek emergency treatment. Beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia.
Thyrotoxicosis: Beta-adrenergic blockade may mask certain clinical signs of hyperthyroidism, such as tachycardia. Abrupt withdrawal of beta-blockade may precipitate a thyroid storm.
Risk of Anaphylactic Reaction: While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction.
Peripheral Vascular Disease: Beta-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease.
See Full Prescribing Information for warnings and precautions of LOPRESSOR (metoprolol tartrate) tablets.
ADVERSE REACTIONS
The following serious adverse reactions are described elsewhere in the labeling:
- Worsening angina or myocardial infarction
- Worsening heart failure
- Worsening AV block
To report SUSPECTED ADVERSE REACTIONS, contact Validus Pharmaceuticals LLC at 1-866-982-5438 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
See Full Prescribing Information for additional adverse reactions associated with LOPRESSOR (metoprolol tartrate) tablets.
DRUG INTERACTIONS
Catecholamine Depleting Drugs: Catecholamine depleting drugs (e.g., reserpine, monoamine oxidase (MAO) inhibitors) may have an additive effect when given with beta-blocking agents. Observe patients treated with LOPRESSOR plus a catecholamine depletor for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension.
Epinephrine: While taking beta-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to the usual doses of epinephrine used to treat an allergic reaction. CYP2D6 Inhibitors: Drugs that are strong inhibitors of CYP2D6 such as quinidine, fluoxetine, paroxetine, and propafenone were shown to double metoprolol concentrations. While there is no information about moderate or weak inhibitors, these too are likely to increase metoprolol concentration. Increases in plasma concentration decrease the cardioselectivity of metoprolol [see Clinical Pharmacology (12.3)]. Monitor patients closely, when the combination cannot be avoided.
Negative Chronotropes: Digitalis glycosides, clonidine, diltiazem and verapamil slow atrioventricular conduction and decrease heart rate. Concomitant use with beta-blockers can increase the risk of bradycardia.
If clonidine and a beta-blocker, such as metoprolol are coadministered, withdraw the beta-blocker several days before the gradual withdrawal of clonidine because beta-blockers may exacerbate the rebound hypertension that can follow the withdrawal of clonidine. If replacing clonidine by beta-blocker therapy, delay the introduction of beta-blockers for several days after clonidine administration has stopped. See Full Prescribing Information for Potential Drug Interactions.
USE IN SPECIFIC POPULATIONS
Pregnancy: Available data from published observational studies have not demonstrated an association of adverse developmental outcomes with maternal use of metoprolol during pregnancy. Untreated hypertension and myocardial infarction during pregnancy can lead to adverse outcomes for the mother and the fetus. In animal reproduction studies, metoprolol has been shown to increase post-implantation loss and decrease neonatal survival in rats at oral dosages of 500 mg/kg/day, approximately 11 times the daily dose of 450 mg in a 60-kg patient on a mg/m2 basis.
All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.
Lactation: Limited available data from published literature report that metoprolol is present in human milk. The estimated daily infant dose of metoprolol received from breastmilk ranges from 0.05 mg to less than 1 mg. The estimated relative infant dosage was 0.5% to 2% of the mother’s weight-adjusted dosage. No adverse reactions of metoprolol on the breastfed infant have been identified. There is no information regarding the effects of metoprolol on milk production.
Females and Males of Reproductive Potential: Based on the published literature, beta-blockers (including metoprolol) may cause erectile dysfunction and inhibit sperm motility. In animal fertility studies, metoprolol has been associated with reversible adverse effects on spermatogenesis starting at oral dose level of 3.5 mg/kg in rats, which would correspond to a dose of 34 mg/day in humans in mg/m2 equivalent, although other studies have shown no effect of metoprolol on reproductive performance in male rats. No evidence of impaired fertility due to metoprolol was observed in rats.
Pediatric Use: Safety and effectiveness of LOPRESSOR have not been established in pediatric patients.
Geriatric Use: In general, use a low initial starting dose in elderly patients given their greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Renal Impairment: No reduction in dosage is needed in patients with chronic renal failure.
Hepatic Impairment: No studies have been performed with LOPRESSOR in patients with hepatic impairment.
DOSAGE FORMS AND STRENGTHS
50 mg tablet – capsule shaped, biconvex, pink, scored (imprinted GEIGY on one side and 51 twice on the scored side)
100 mg tablet – capsule shaped, biconvex, light blue, scored (imprinted with GEIGY on one side and 71 twice on the scored side)
OVERDOSAGE
Signs and Symptoms – Overdosage of LOPRESSOR may lead to severe bradycardia, hypotension, and cardiogenic shock. Clinical presentation can also include:atrioventricular block, heart failure, bronchospasm, hypoxia, impairment of consciousness/coma, nausea and vomiting.
Treatment – Consider treating the patient with intensive care. Patients with myocardial infarction or heart failure may be prone to significant hemodynamic instability. Beta-blocker overdose may result in significant resistance to resuscitation with adrenergic agents, including beta-agonists.
On the basis of the pharmacologic actions of metoprolol, employ the following measures.
Hemodialysis is unlikely to make a useful contribution to metoprolol elimination
Bradycardia: Evaluate the need for atropine, adrenergic-stimulating drugs or pacemaker to treat bradycardia and conduction disorders.
Hypotension: Treat underlying bradycardia. Consider intravenous vasopressor infusion, such as dopamine or norepinephrine.
Heart failure and shock: May be treated when appropriate with suitable volume expansion, injection of glucagon (if necessary, followed by an intravenous infusion of glucagon), intravenous administration of adrenergic drugs such as dobutamine, with α1 receptor agonistic drugs added in presence of vasodilation.
Bronchospasm: Can usually be reversed by bronchodilators
Please see Full Prescribing Information for https://lopressor.us.com/
LOP-403-25
