Metoprolol Tartrate

Introduction

Metoprolol Tartrate is a selective beta-1 adrenergic blocker used primarily in the management of cardiovascular conditions. It is commonly prescribed to treat hypertension, angina pectoris, and heart failure. By selectively targeting beta-1 receptors in the heart, Metoprolol helps reduce heart rate, blood pressure, and cardiac workload.

Uses

Metoprolol Tartrate is used for:

• Managing hypertension (high blood pressure) to reduce the risk of stroke, heart attack, and kidney problems.
• Relieving angina pectoris (chest pain) by decreasing myocardial oxygen demand.
• Treating chronic heart failure to improve symptoms and reduce hospitalization rates.
• Preventing migraine headaches in some cases.

Brand Name	Metoprolol Tartrate
Type
Weight
Generic	Metoprolol Tartrate
Manufacturer
Available in	English বাংলা

Mechanism of Action

Metoprolol Tartrate works by selectively blocking beta-1 adrenergic receptors in the heart. This blockade reduces heart rate, myocardial contractility, and cardiac output, leading to a decrease in blood pressure and a reduction in cardiac workload. The medication also helps to improve heart function in heart failure.

How Long Does It Take to Work?

The onset of action for Metoprolol Tartrate is typically within 1 to 2 hours after oral administration. Peak effects are generally observed within 1 to 2 hours. The full therapeutic effects may take a few weeks to be fully realized, especially in chronic conditions such as heart failure.

Absorption

Metoprolol Tartrate is well absorbed from the gastrointestinal tract after oral administration. However, it undergoes significant first-pass metabolism in the liver, resulting in an oral bioavailability of approximately 50%. Peak plasma concentrations are usually reached within 1 to 2 hours after ingestion.

Route of Elimination

Metoprolol is primarily eliminated by the liver. After metabolism, it is excreted in the urine as metabolites, with a small amount of the drug being excreted unchanged. Renal clearance plays a role in the elimination process, especially in patients with impaired liver function.

Dosage

Film-coated tablet-

• Hypertension: Total daily dosage Metoprolol 100-400 mg to be given as a single or twice-daily dose. The starting dose is 100 mg (two Metoprolol-50 tablets) per day. This may be increased by 100 mg per day at weekly intervals. lf full control is not achieved using a single daily dose, a b.i.d. regimen should be initiated. Combination therapy with a diuretic or other antihypertensive agents may also be considered.
• Angina: Usually Metoprolol 50 mg (one Metoprolol-50 tablet) to 100 mg (two Metoprolol-50 tablets) twice or three times daily.
• Cardiac arrhythmias: Metoprolol 50 mg (one Metoprolol-50 tablet) b.i.d or t.i.d should usually control the condition. It is necessary the dose can be increased up to 300 mg per day in divided doses. Following the treatment of an acute arrhythmia with Metoprolol injection, continuation therapy with Metoprolol tablets should be initiated 4-6 hours later. The initial oral dose should not exceed 50 mg t.i.d.
• Hyperthyroidism: Metoprolol 50 mg (one Metoprolol-50 tablet) four times a day. The dose should be reduced as the euthyroid state is achieved.
• Myocardial infarction: Orally, therapy should commence 15 minutes after the last injection with 50 mg every 6 hours for 48 hours. Patients who fail to tolerate the full intravenous dose should be given half the suggested oral dose. Maintenance- The usual maintenance dose is 200 mg daily given in divided doses. Elderly’ There are no special dosage requirements in otherwise healthy elderly patients. Significant hepatic dysfunction: A reduction in dosage may be necessary.

Extended-release tablet-

• Hypertension: The usual initial dosage is 25 to 100 mg daily in a single dose, whether used alone or added to a diuretic.
• Angina Pectoris: The dosage of extended-release Metoprolol Succinate should be individualized. The usual initial dosage is 100 mg daily, in a single dose.
• Heart Failure: The recommended starting dose of sustained-release Metoprolol Succinate is 25 mg once daily for two weeks in patients with NYHA class II heart failure and 12.5 mg once daily in patients with more severe heart failure. The dosage may be increased at weekly (or longer) intervals until optimum blood pressure reduction is achieved. If treatment is to be discontinued, the dosage should be reduced gradually over a period of 1-2 weeks.

IV Injection-

• Arrhythmias: By intravenous injection, up to 5 mg at a rate of 1-2 mg/minute, repeated after 5 minutes if necessary, total dose 10-15 mg.
• In surgery: By slow intravenous injection 2-4 mg at induction or to control arrhythmias developing during anaesthesia; 2 mg doses may be repeated to a maximum of 10 mg.
• Myocardial Infarction: Early intervention within 12 hours of infarction, by intravenous injection 5 mg every 2 minutes to a maximum of 15 mg, followed after 15 minutes by 50 mg by mouth every 6 hours for 48 hours; maintenance 200 mg daily in divided doses.

The dosage of Metoprolol Tartrate varies depending on the condition being treated:

• Hypertension: Typically starts at 50 mg twice daily, with a usual range of 100 to 200 mg per day, depending on patient response.
• Angina Pectoris: Usual starting dose is 50 mg twice daily, with adjustments up to 200 mg per day based on efficacy and tolerance.
• Heart Failure: The dose may start at 25 mg twice daily and be gradually increased up to 200 mg per day, based on patient tolerance and clinical response.
• Migraine Prevention: Generally, 50 to 100 mg twice daily is used, depending on response and side effects.

Dosage adjustments may be necessary for patients with renal or hepatic impairment.

Administration

Metoprolol Tartrate should be administered orally, with or without food. It is typically taken in the form of tablets. The dosage should be taken at regular intervals to maintain consistent blood levels. It is important not to crush or chew the tablets.

Side Effects

Common side effects include:

• Dizziness or lightheadedness
• Fatigue
• Bradycardia (slow heart rate)
• Cold extremities
• Nausea

Serious side effects may include:

• Severe hypotension (low blood pressure)
• Heart block
• Severe allergic reactions (e.g., rash, itching, swelling)
• Worsening of heart failure symptoms

Toxicity

Symptoms of Metoprolol toxicity may include severe bradycardia, hypotension, and heart block. In cases of overdose, treatment may involve discontinuing the medication, administering activated charcoal if appropriate, and providing supportive care. In severe cases, intravenous fluids, atropine, or other interventions may be required.

Precautions

Precautions should be taken in patients with:

• Pre-existing heart conditions (e.g., heart failure, bradycardia)
• Chronic respiratory conditions such as asthma or COPD
• Diabetes mellitus, as Metoprolol may mask hypoglycemic symptoms
• Severe hepatic or renal impairment

Regular monitoring of heart rate, blood pressure, and renal function is recommended.

Interaction

Metoprolol Tartrate may interact with:

• Other antihypertensives: Additive effects may lead to excessive blood pressure reduction.
• Calcium channel blockers: Concurrent use may increase the risk of bradycardia and heart block.
• Antiarrhythmic agents: May enhance the effects of Metoprolol, requiring careful monitoring.

Disease Interaction

Use with caution in patients with:

• Asthma or other chronic respiratory conditions
• Diabetes mellitus
• Severe hepatic or renal impairment
• Peripheral vascular disease

Drug Interaction

Drug interactions with Metoprolol include:

• Medications affecting liver enzymes: Such as CYP2D6 inhibitors, which may increase Metoprolol levels.
• Other beta-blockers: Concurrent use may exacerbate side effects like bradycardia.
• Antidiabetic agents: Metoprolol may mask hypoglycemic symptoms, requiring careful blood glucose monitoring.

Food Interactions

There are no significant food interactions with Metoprolol. It can be taken with or without food. However, it is advisable to avoid excessive alcohol intake as it may enhance the hypotensive effects of the medication.

Pregnancy Use

Metoprolol is classified as pregnancy category C. It should be used during pregnancy only if the potential benefits outweigh the risks. It is important to carefully monitor both the mother and fetus if Metoprolol is used during pregnancy.

Lactation Use

Metoprolol is excreted in breast milk in small amounts. While it is generally considered safe for use during lactation, caution is advised. Monitor the nursing infant for potential adverse effects, and consult a healthcare provider if concerns arise.

Acute Overdose

Acute overdose symptoms may include severe bradycardia, hypotension, dizziness, and potential heart failure. Treatment involves discontinuing the medication, providing supportive care, and, if necessary, administering atropine or other interventions to manage bradycardia and hypotension.

Contraindication

Metoprolol Tartrate is contraindicated in patients with:

• Severe bradycardia
• Severe hypotension
• Heart block greater than first degree (unless a pacemaker is present)
• Severe hepatic impairment
• Known hypersensitivity to Metoprolol or any component of the formulation

Use Direction

Follow the healthcare provider's instructions for dosing and administration. Take Metoprolol Tartrate at the same time each day to maintain consistent blood levels. Adhere to any additional guidelines provided regarding food and fluid intake.

Storage Conditions

Store Metoprolol Tartrate at room temperature, between 20°C and 25°C (68°F and 77°F). Keep away from light and moisture. Store in the original container and out of reach of children.

Volume of Distribution

The volume of distribution for Metoprolol is approximately 4 to 5 liters/kg, indicating moderate distribution into tissues and fluids throughout the body.

Half Life

The elimination half-life of Metoprolol is approximately 3 to 7 hours. This relatively short half-life supports the need for twice-daily dosing to maintain therapeutic levels.

Clearance

Metoprolol is cleared primarily by the liver, with a clearance rate of approximately 10 to 20 L/h. Renal clearance also plays a role, particularly in patients with impaired hepatic function. Clearance rates may be affected by liver and renal function.

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