METOPROLOL
METOPROLOL TARTRATE
Manufacturer: Baxter Healthcare Corporation
Clinical information
Indications & Usage
1 INDICATIONS AND USAGE Metoprolol tartrate injection is indicated in the treatment of definite or suspected acute myocardial infarction in hemodynamically stable patients to reduce cardiovascular mortality when used in conjunction with oral metoprolol maintenance therapy. Metoprolol tartrate injection is a beta-adrenergic receptor inhibitor indicated for the treatment of definite or suspected acute myocardial infarction in hemodynamically stable patients to reduce cardiovascular mortality when used in conjunction with oral metoprolol maintenance therapy ( 1 ).
Dosage & Administration
2 DOSAGE AND ADMINISTRATION Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit. Initiate treatment 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 injection each; give the injections at approximately 2-minute intervals. During the intravenous administration of metoprolol tartrate injection, monitor blood pressure, heart rate, and electrocardiogram. Transition to Oral Metoprolol: Following administration of metoprolol tartrate injection, transition patients to an oral formulation of metoprolol. See prescribing information for oral metoprolol for dose selection. • Initiate therapy in a coronary care or similar unit immediately after the patients hemodynamic condition has stabilized ( 2 ). • Begin treatment with an intravenous administration of three bolus injections of 5 mg each, at approximately 2-minute intervals. Monitor blood pressure, heart rate and electrocardiogram ( 2 ). • Following administration of metoprolol tartrate injection, transition the patient to an oral formulation of metoprolol ( 2 ).
Contraindications
4 CONTRAINDICATIONS Hypersensitivity to metoprolol tartrate injection and related derivatives, or to any of the excipients; hypersensitivity to other beta blockers (cross sensitivity between beta blockers can occur). Metoprolol tartrate injection is contraindicated in patients with a heart rate <45 beats/min; second- and third-degree heart block (unless a functioning pacemaker is present); significant first-degree heart block (P-R interval ≥0.24 sec); systolic blood pressure <100 mmHg; or decompensated cardiac failure. • Known hypersensitivity to product components. ( 4 ) • Severe bradycardia, greater than first degree heart block, or sick sinus syndrome without a pacemaker. ( 4 ) • Cardiogenic shock or decompensated heart failure. ( 4 )
Safety
Adverse Reactions
6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in labeling: • Worsening angina or myocardial infarction [see Warnings and Precautions (5) ] • Worsening heart failure [see Warnings and Precautions (5) ] • Worsening AV block [see Contraindications (4) ] • Most common adverse reactions: tiredness, dizziness, shortness of breath, bradycardia, hypotension, pruritus. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Baxter Healthcare Corporation at 1-877-725-2747 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The adverse reaction information from clinical trials does, however, provide a basis for identifying the adverse events that appear to be related to drug use and for approximating rates. Myocardial Infarction These adverse reactions were reported from treatment regimens where intravenous metoprolol tartrate injection was administered, when tolerated. Central Nervous System: Tiredness has been reported in about 1 of 100 patients. Vertigo, sleep disturbances, hallucinations, headache, dizziness, visual disturbances, confusion, and reduced libido have also been reported, but a drug relationship is not clear. Cardiovascular: In a randomized comparison of metoprolol tartrate injection and placebo, the following adverse reactions were reported: Metoprolol Tartrate Injection Placebo Hypotension (systolic BP <90 mmHg) 27.4% 23.2% Bradycardia (heart rate <40 beats/min) 15.9% 6.7% Second- or third-degree heart block 4.7% 4.7% First-degree heart block (P-R ≥0.26 sec) 5.3% 1.9% Heart failure 27.5% 29.6% Respiratory: Dyspnea of pulmonary origin has been reported in fewer than 1 of 100 patients. Gastrointestinal: Nausea and abdominal pain have been reported in fewer than 1 of 100 patients. Miscellaneous: Unstable diabetes and claudication have been reported. 6.2 Post-Marketing Experience The following adverse reactions have been identified during post-approval use of metoprolol. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. Cardiovascular: Cold extremities, arterial insufficiency (usually of the Raynaud type), palpitations, peripheral edema, syncope, and hypotension. Respiratory: Wheezing (bronchospasm), dyspnea. Central Nervous System: Confusion, short-term memory loss, headache, nightmares, insomnia, nervousness, hallucinations. Gastrointestinal: Nausea, dry mouth, constipation, flatulence, heartburn, hepatitis, vomiting. Hypersensitive Reactions: Pruritus. Miscellaneous: Musculoskeletal pain, arthritis, blurred vision, decreased libido, tinnitus, reversible alopecia, agranulocytosis, dry eyes, worsening of psoriasis, Peyronie’s disease, photosensitivity.
Drug Interactions
7 DRUG INTERACTIONS • Catecholamine-depleting drugs may have an additive effect when given with beta-blocking agents. ( 7.1 ) • Patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction. ( 7.2 ) • CYP2D6 Inhibitors are likely to increase metoprolol concentration. ( 7.3 ) • Concomitant use of glycosides, clonidine, and diltiazem and verapamil with beta-blockers can increase the risk of bradycardia. ( 7.4 ) • Beta-blockers including metoprolol, may exacerbate the rebound hypertension that can follow the withdrawal of clonidine. ( 7.4 ) 7.1 Catecholamine Depleting Drugs and Monoamine Oxidate (MAO) Inhibitors Catecholamine depleting drugs (e.g., reserpine) and monoamine oxidase (MAO) inhibitors) may have an additive effect when given with beta-blocking agents. Observe patients treated with metoprolol plus a catecholamine depletor for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension. 7.2 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. 7.3 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. 7.4 Digitalis, Clonidine, and Calcium Channel Blockers and Other Drugs that Decrease Heart Rate Digitalis glycosides, clonidine, diltiazem and verapamil slow atrioventricular conduction and decrease heart rate. Concomitant administration of beta-blockers with these and other drugs known to decrease heart rate such as sphingosine-1-phosphate receptor modulators (e.g. fingolimod) may result in additive heart rate lowering effects. If clonidine and metoprolol are co-administered, withdraw the metoprolol 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 . 7.5 Drugs that Decrease Blood Pressure Concomitant administration of beta-blockers with other drugs known to decrease blood pressure may result in an enhanced hypotensive effect.
Additional information
Description
11 DESCRIPTION Metoprolol tartrate injection USP is a selective beta 1 -adrenoreceptor blocking agent, available in 5 mL vials for intravenous administration. Each vial contains a sterile solution of metoprolol tartrate USP, 5 mg, and sodium chloride USP, 45 mg, and water for injection USP. Metoprolol tartrate USP is (±)-1-(Isopropylamino)-3-[p-(2- methoxyethyl)phenoxy]-2-propanol L-(+)-tartrate (2:1) 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. structural-formula-metoprolol
How Supplied
16 HOW SUPPLIED/STORAGE AND HANDLING Metoprolol Tartrate Injection, USP is available as 5 mL vials, each containing 5 mg of metoprolol tartrate, USP. Carton of 10 vials AIN00234 36000-033-10 Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) [See USP Controlled Room Temperature]. Do not freeze. Protect from light and heat.
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Frequently Asked Questions
What is metoprolol used for?+
Metoprolol is used to treat high blood pressure, chest pain (angina), and certain heart-related conditions. It works by reducing the heart rate and the heart's workload, which helps to lower blood pressure and increase blood flow to the heart. Consult a doctor to determine the best course of treatment for your specific condition.
How long does it take for metoprolol to start working?+
Metoprolol starts working within a few hours of taking the first dose, but it may take several days or weeks to reach its full effect. It's essential to take the medication as directed by your doctor and not to stop taking it without consulting them first. Consult a doctor to discuss the expected timeline for metoprolol to start working for your specific condition.
What are the common side effects of metoprolol?+
Common side effects of metoprolol include dizziness, lightheadedness, fatigue, and shortness of breath. In some cases, metoprolol can also cause more severe side effects, such as slow heart rate or allergic reactions. Consult a doctor if you experience any side effects, as they can help you manage them and adjust your treatment plan if necessary.
Can I stop taking metoprolol if I feel better?+
No, you should not stop taking metoprolol without consulting your doctor first. Stopping the medication abruptly can lead to a worsening of your condition or even a heart attack. Consult a doctor to discuss the best way to adjust your treatment plan and ensure your safety.
Can I take metoprolol with other medications?+
Metoprolol can interact with other medications, such as certain antidepressants, antihistamines, and decongestants. It's essential to inform your doctor about all the medications you're taking, including over-the-counter medications and supplements, to avoid potential interactions. Consult a doctor to discuss the safety of taking metoprolol with other medications.
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