Metoprolol Tartrate 100 MG Oral Tablet
Generic Name: METOPROLOL TARTRATE
Brand Name: Metoprolol Tartrate
- Substance Name(s):
- METOPROLOL TARTRATE
WARNINGS
Heart Failure Beta blockers, like metoprolol tartrate, can cause depression of myocardial contractility and may precipitate heart failure and cardiogenic shock.
If signs or symptoms of heart failure develop, treat the patient according to recommended guidelines.
It may be necessary to lower the dose of metoprolol tartrate or to discontinue it.
Ischemic Heart Disease Do not abruptly discontinue metoprolol tartrate therapy in patients with coronary artery disease.
Severe exacerbation of angina, myocardial infarction and ventricular arrhythmias have been reported in patients with coronary artery disease following the abrupt discontinuation of therapy with beta-blockers.
When discontinuing chronically administered metoprolol tartrate, particularly in patients with coronary artery disease, the dosage should be gradually reduced over a period of 1-2 weeks and the patient should be carefully monitored.
If angina markedly worsens or acute coronary insufficiency develops, metoprolol tartrate administration should be reinstated promptly, at least temporarily, and other measures appropriate for the management of unstable angina should be taken.
Patients should be warned against interruption or discontinuation of therapy without the physician’s advice.
Because coronary artery disease is common and may be unrecognized, it may be prudent not to discontinue metoprolol tartrate therapy abruptly even in patients treated only for hypertension.
Use During Major Surgery Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery; however, the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and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.
Bradycardia Bradycardia, including sinus pause, heart block, and cardiac arrest have occurred with the use of metoprolol tartrate.
Patients with first-degree atrioventricular block, sinus node dysfunction, or conduction disorders may be at increased risk.
Monitor heart rate and rhythm in patients receiving metoprolol tartrate.
If severe bradycardia develops, reduce or stop metoprolol tartrate.
Exacerbation of Bronchospastic Disease Patients with bronchospastic disease,should, in general, not receive beta blockers, including metoprolol tartrate.
Because of its relative beta1 selectivity, however, metoprolol tartrate 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 metoprolol tartrate and consider administering metoprolol tartrate in smaller doses three times daily, instead of larger doses two times daily, to avoid the higher plasma levels associated with the longer dosing interval (see DOSAGE AND ADMINISTRATION).
Bronchodilators, including beta2 agonists, should be readily available or administered concomitantly.
Diabetes and Hypoglycemia Beta blockers may mask tachycardia occurring with hypoglycemia, but other manifestations such as dizziness and sweating may not be significantly affected.
Pheochromocytoma If metoprolol tartrate 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.
Thyrotoxicosis Metoprolol tartrate may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism.
Avoid abrupt withdrawal of beta blockade, which might precipitate a thyroid storm.
OVERDOSAGE
Acute Toxicity Several cases of overdosage have been reported, some leading to death.
Oral LD 50’s (mg/kg): mice, 1158-2460; rats, 3090-4670.
Signs and Symptoms Potential signs and symptoms associated with overdosage with metoprolol tartrate are bradycardia, hypotension, bronchospasm, myocardial infarction, cardiac failure and death.
Management There is no specific antidote.
In general, patients with acute or recent myocardial infarction may be more hemodynamically unstable than other patients and should be treated accordingly (see WARNINGS, Myocardial Infarction).
On the basis of the pharmacologic actions of metoprolol tartrate, the following general measures should be employed: Elimination of the Drug: Gastric lavage should be performed.
Other clinical manifestations of overdose should be managed symptomatically based on modern methods of intensive care.
Hypotension: Administer a vasopressor, e.g., levarterenol or dopamine.
Bronchospasm: Administer a beta2-stimulating agent and/or a theophylline derivative.
Cardiac Failure: Administer digitalis glycoside and diuretic.
In shock resulting from inadequate cardiac contractility, consider administration of dobutamine, isoproterenol or glucagon.
DESCRIPTION
Metoprolol tartrate, USP is a selective beta1-adrenoreceptor blocking agent, available as 25, 50 and 100 mg tablets for oral administration.
Metoprolol tartrate is (±)-1-(isopropylamino)-3-[p-(2-methoxyethyl)phenoxy]-2-propanol (2:1) dextro-tartrate salt, and its structural formula is Metoprolol tartrate, USP is a white, practically odorless, crystalline powder with a molecular weight of 684.81.
It is very soluble in water; freely soluble in methylene chloride, in chloroform, and in alcohol; slightly soluble in acetone; and insoluble in ether.
Each tablet for oral administration contains 25 mg, 50 mg or 100 mg of metoprolol tartrate USP and the following inactive ingredients: colloidal silicon dioxide, croscarmellose sodium, hypromellose, lactose anhydrous, magnesium stearate, microcrystalline cellulose, sodium starch glycolate, polyethylene glycol, pregelatinized starch, titanium dioxide.
In addition the 25 mg and 100 mg tablet contain propylene glycol and sodium lauryl sulfate; the 50 mg tablet contains D&C Red #30 and talc.
figure-01
HOW SUPPLIED
Metoprolol tartrate tablets, USP 25 mg are available as white to off-white, round, film-coated tablets, debossed with “RE” above the bisect and “79” below the bisect on one side and plain on the other side.
Bottles of 10 NDC 63304-579-03 Bottles of 100 NDC 63304-579-01 Bottles of 1000 NDC 63304-579-10 Metoprolol tartrate tablets, USP 50 mg are available as pink colored, round, film-coated tablets debossed with “RE” above the bisect and “75” below the bisect on one side and plain on the other side.
Bottles of 10 NDC 63304-580-03 Bottles of 100 NDC 63304-580-01 Bottles of 1000 NDC 63304-580-10 Metoprolol tartrate tablets, USP 100 mg are available as white to off-white, round, film-coated tablets, debossed with “RE” above the bisect and “76” below the bisect on one side and plain on the other side.
Bottles of 10 NDC 63304-581-03 Bottles of 100 NDC 63304-581-01 Bottles of 1000 NDC 63304-581-10 Store at 20 – 25°C (68 – 77°F) [See USP Controlled Room Temperature].
Protect from moisture and heat.
Dispense in a tight, light-resistant container as defined in the USP using a child-resistant closure.
You may report side effects to FDA at 1-800-FDA 1088.
INDICATIONS AND USAGE
Hypertension Metoprolol tartrate tablets are indicated for the treatment of hypertension.
They may be used alone or in combination with other antihypertensive agents.
Angina Pectoris Metoprolol tartrate is indicated in the long-term treatment of angina pectoris.
Myocardial Infarction Metoprolol tartrate tablets are indicated in the treatment of hemodynamically stable patients with definite or suspected acute myocardial infarction to reduce cardiovascular mortality when used alone or in conjunction with intravenous metoprolol tartrate.
Oral metoprolol tartrate therapy can be initiated after intravenous metoprolol tartrate therapy or, alternatively, oral treatment can begin within 3 to 10 days of the acute event (see DOSAGE AND ADMINISTRATION, CONTRAINDICATIONS, and WARNINGS).
DOSAGE AND ADMINISTRATION
Hypertension Individualize the dosage of metoprolol tartrate tablets.
Metoprolol tartrate tablets should be taken with or immediately following meals.
The usual initial dosage of metoprolol tartrate tablets is 100 mg daily in single or divided doses, whether used alone or added to a diuretic.
Increase the dosage at weekly (or longer) intervals until optimum blood pressure reduction is achieved.
In general, the maximum effect of any given dosage level will be apparent after 1 week of therapy.
The effective dosage range of metoprolol tartrate tablets is 100-450 mg per day.
Dosages above 450 mg per day have not been studied.
While once-daily dosing is effective and can maintain a reduction in blood pressure throughout the day, lower doses (especially 100 mg) may not maintain a full effect at the end of the 24-hour period, and larger or more frequent daily doses may be required.
This can be evaluated by measuring blood pressure near the end of the dosing interval to determine whether satisfactory control is being maintained throughout the day.
Beta1 selectivity diminishes as the dose of metoprolol tartrate is increased.
Angina Pectoris The dosage of metoprolol tartrate tablets should be individualized.
Metoprolol tartrate tablets should be taken with or immediately following meals.
The usual initial dosage of metoprolol tartrate tablets is 100 mg daily, given in two divided doses.
Gradually increase the dosage at weekly intervals until optimum clinical response has been obtained or there is pronounced slowing of the heart rate.
The effective dosage range of metoprolol tartrate tablets is 100-400 mg per day.
Dosages above 400 mg per day have not been studied.
If treatment is to be discontinued, gradually decrease the dosage over a period of 1-2 weeks (see WARNINGS).
Myocardial Infarction Early Treatment: During the early phase of definite or suspected acute myocardial infarction, initiate treatment with metoprolol tartrate as soon as possible after the patient’s arrival in the hospital.
Such treatment should be initiated in a coronary care or similar unit immediately after the patient’s hemodynamic condition has stabilized.
Begin treatment in this early phase with the intravenous administration of three bolus injections of 5 mg of metoprolol tartrate each; give the injections at approximately 2-minute intervals.
During the intravenous administration of metoprolol tartrate, monitor blood pressure, heart rate, and electrocardiogram.
In patients who tolerate the full intravenous dose (15 mg), initiate metoprolol tartrate tablets, 50 mg every 6 hours, 15 minutes after the last intravenous dose and continue for 48 hours.
Thereafter, the maintenance dosage is 100 mg twice daily (see Late Treatment below).
Start patients who appear not to tolerate the full intravenous dose on metoprolol tartrate tablets either 25 mg or 50 mg every 6 hours (depending on the degree of intolerance) 15 minutes after the last intravenous dose or as soon as their clinical condition allows.
In patients with severe intolerance, discontinue metoprolol tartrate (see WARNINGS).
Late Treatment: Start patients with contraindications to treatment during the early phase of suspected or definite myocardial infarction, patients who appear not to tolerate the full early treatment, and patients in whom the physician wishes to delay therapy for any other reason on metoprolol tartrate tablets, 100 mg twice daily, as soon as their clinical condition allows.
Continue therapy for at least 3 months.
Although the efficacy of metoprolol tartrate beyond 3 months has not been conclusively established, data from studies with other beta blockers suggest that treatment should be continued for 1-3 years.
Special populations Pediatric patients: No pediatric studies have been performed.
The safety and efficacy of metoprolol tartrate in pediatric patients have not been established.
Renal impairment: No dose adjustment of metoprolol tartrate is required in patients with renal impairment.
Hepatic impairment: Metoprolol tartrate blood levels are likely to increase substantially in patients with hepatic impairment.
Therefore, metoprolol tartrate should be initiated at low doses with cautious gradual dose titration according to clinical response.
Geriatric patients (>65 years): 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.
Method of administration: For oral treatment, the tablets should be swallowed un-chewed with a glass of water.
Metoprolol tartrate should always be taken in standardized relation with meals.
If the physician asks the patient to take metoprolol tartrate either before breakfast or with breakfast, then the patient should continue taking metoprolol tartrate with the same schedule during the course of therapy.