• Meto Zerok indications
• Uses of Meto Zerok in details
• Meto Zerok description
• Meto Zerok dosage
• Meto Zerok interactions
• Meto Zerok side effects
• Meto Zerok contraindications

What is Meto Zerok?

Meto Zerok is used alone or together with other medicines to treat high blood pressure (hypertension). High blood pressure adds to the workload of the heart and arteries. If it continues for a long time, the heart and arteries may not function properly. This can damage the blood vessels of the brain, heart, and kidneys, resulting in a stroke, heart failure, or kidney failure. A lower blood pressure can reduce the risk of strokes and heart attacks.

Meto Zerok is also used to treat severe chest pain (angina) and lowers the risk of repeated heart attacks. It is given to people who have already had a heart attack. In addition, Meto Zerok is used to treat patients with heart failure.

Meto Zerok is a beta-blocker. It works by affecting the response to nerve impulses in certain parts of the body, like the heart. As a result, the heart beats slower and decreases the blood pressure. When the blood pressure is lowered, the amount of blood and oxygen is increased to the heart.

Meto Zerok is available only with your doctor's prescription.

Meto Zerok indications

Hypertension

Meto Zerok tartrate tablets, USP are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensive agents.

Angina Pectoris

Meto Zerok tartrate tablets, USP are indicated in the long-term treatment of angina pectoris.

Myocardial Infarction

Meto Zerok tartrate tablets, USP 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 Meto Zerok.

Oral Meto Zerok tartrate tablets, USP therapy can be initiated after intravenous Meto Zerok therapy or, alternatively, oral treatment can begin within 3 to 10 days of the acute event.

How should I use Meto Zerok?

Use Meto Zerok tartrate as directed by your doctor. Check the label on the medicine for exact dosing instructions.

• Meto Zerok tartrate is usually given as an injection at your doctor's office, hospital, or clinic. If you will be using Meto Zerok tartrate at home, a health care provider will teach you how to use it. Be sure you understand how to use Meto Zerok tartrate. Follow the procedures you are taught when you use a dose. Contact your health care provider if you have any questions.
• Do not use Meto Zerok tartrate if it contains particles, is cloudy or discolored, or if the vial is cracked or damaged.
• Keep this product, as well as syringes and needles, out of the reach of children and pets. Do not reuse needles, syringes, or other materials. Ask your health care provider how to dispose of these materials after use. Follow all local rules for disposal.
• If you miss a dose of Meto Zerok tartrate, use it as soon as possible. If it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not use 2 doses at once.

Ask your health care provider any questions you may have about how to use Meto Zerok tartrate.

Uses of Meto Zerok in details

Use: Labeled Indications

Angina: Long-term treatment of angina pectoris.

Heart failure with reduced ejection fraction (ER oral formulation): Treatment of stable, symptomatic (NYHA class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin to reduce the rate of mortality plus hospitalization in patients already receiving angiotensin-converting enzyme inhibitors, diuretics, and/or digoxin.

Hypertension: Management of hypertension. Note: Beta-blockers are not recommended as first-line therapy (ACC/AHA [Whelton 2017]).

Myocardial infarction: Treatment of hemodynamically stable acute myocardial infarction to reduce cardiovascular mortality (injection to be used in combination with Meto Zerok oral maintenance therapy).

Off Label Uses

Atrial fibrillation/flutter

Based on the 2014 American Heart Association/American College of Cardiology/Heart Rhythm Society (AHA/ACC/HRS) guideline for the management of patients with atrial fibrillation (AF), the use of beta-blockers, including Meto Zerok, for ventricular rate control in patients with paroxysmal, persistent, or permanent AF is effective and recommended.

Atrial fibrillation prevention after cardiac surgery

Based on the American College of Cardiology Foundation/American Heart Association (ACCF/AHA) guideline for coronary artery bypass graft surgery, beta-blockers are recommended to help prevent postoperative atrial fibrillation.

Hypertrophic cardiomyopathy

Based on the American College of Cardiology Foundation/American Heart Association (ACCF/AHA) guideline for the diagnosis and treatment of hypertrophic cardiomyopathy, a beta blocker (eg, Meto Zerok) is an effective and recommended agent for the treatment of symptoms (eg, angina, dyspnea) in patients with obstructive or nonobstructive hypertrophic cardiomyopathy.

Marfan syndrome with aortic aneurysm

Based on the American College of Cardiology Foundation/American Heart Association/American Association for Thoracic Surgery (ACCF/AHA/AATS) guideline for the diagnosis and management of patients with thoracic aortic disease, a beta blocker (eg, Meto Zerok) is an effective and recommended agent to reduce the rate of aortic dilatation in patients with Marfan syndrome and aortic aneurysm, unless a contraindication exists.

Migraine prophylaxis

Data from small, randomized, active-controlled trials support the use of Meto Zerok for prevention of migraines.

Based on evidence-based guidelines for pharmacologic treatment for episodic migraine prevention in adults from the American Academy of Neurology and the American Headache Society, Meto Zerok is effective for migraine prevention in adults.

Supraventricular tachycardia (eg, atrioventricular nodal reentrant tachycardia, atrioventricular reentrant tachycardia, focal atrial tachycardia)

Based on the American College of Cardiology/American Heart Association/Heart Rhythm Society (ACC/AHA/HRS) guidelines for the management of adult patients with supraventricular tachycardia, the use of an oral or intravenous beta-blocker, including Meto Zerok, is effective and recommended for a variety of symptomatic supraventricular tachycardias (atrioventricular nodal reentrant tachycardia [AVNRT], atrioventricular reentrant tachycardia [AVRT], focal atrial tachycardia [AT], and multifocal atrial tachycardia [MAT]). In patients without pre-excitation, intravenous Meto Zerok is recommended for acute treatment in hemodynamically stable patients and oral Meto Zerok is recommended for ongoing management of symptomatic supraventricular tachycardias in patients who are not candidates for, or prefer not to undergo, catheter ablation.

Intravenous or oral Meto Zerok may be useful for rate control in the acute treatment or ongoing management of hemodynamically stable patients with atrial flutter.

Thyrotoxicosis

Based on the American Thyroid Association guidelines for diagnosis and management of hyperthyroidism and other causes of thyrotoxicosis, beta-blockers, including Meto Zerok, are effective and recommended in the treatment of symptomatic thyrotoxicosis. Beta-blockers should also be considered in asymptomatic patients who are at increased risk of complications due to worsening hyperthyroidism.

Ventricular arrhythmias

Based on the American Heart Association/American College of Cardiology/Heart Rhythm Society (AHA/ACC/HRS) guideline for management of patients with ventricular arrhythmias and prevention of sudden cardiac death, beta-blockers are effective for control of ventricular arrhythmias and ventricular premature beats.

Meto Zerok description

Meto Zerok is a cardioselective β1-adrenergic blocking agent used for acute myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension. It may also be used for supraventricular and tachyarrhythmias and prophylaxis for migraine headaches. Meto Zerok is structurally similar to bisoprolol, acebutolol and atenolol in that it has two substituents in the para position of the benzene ring. The β1-selectivity of these agents is thought to be due in part to the large substituents in the para position. At low doses, Meto Zerok selectively blocks cardiac β1-adrenergic receptors with little activity against β2-adrenergic receptors of the lungs and vascular smooth muscle. Receptor selectivity decreases with higher doses. Unlike propranolol and pindolol, Meto Zerok does not exhibit membrane-stabilizing or intrinsic sympathomimetic activity. Membrane-stabilizing effects are only observed at doses much higher than those needed for β-adrenergic blocking activity. Meto Zerok possesses a single chiral centre and is administered as a racemic mixture.

Meto Zerok dosage

Meto Zerok Dosage

Generic name: Meto Zerok SUCCINATE 25mg

Dosage form: tablet, extended release

The information at Drugs.com is not a substitute for medical advice. Always consult your doctor or pharmacist.

Meto Zerok is an extended-release tablet intended for once daily administration. For treatment of hypertension and angina, when switching from immediate-release Meto Zerok to Meto Zerok, use the same total daily dose of Meto Zerok. Individualize the dosage of Meto Zerok. Titration may be needed in some patients.

Meto Zerok tablets are scored and can be divided; however, do not crush or chew the whole or half tablet.

Hypertension

Adults: The usual initial dosage is 25 to 100 mg daily in a single dose. The dosage may be increased 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. Dosages above 400 mg per day have not been studied.

Pediatric Hypertensive Patients ≥ 6 Years of age: A pediatric clinical hypertension study in patients 6 to 16 years of age did not meet its primary endpoint (dose response for reduction in SBP); however, some other endpoints demonstrated effectiveness. If selected for treatment, the recommended starting dose of Meto Zerok is 1 mg/kg once daily, but the maximum initial dose should not exceed 50 mg once daily. Dosage should be adjusted according to blood pressure response. Doses above 2 mg/kg (or in excess of 200 mg) once daily have not been studied in pediatric patients.

Meto Zerok is not recommended in pediatric patients < 6 years of age.

Angina Pectoris

Individualize the dosage of Meto Zerok. The usual initial dosage is 100 mg daily, given in a single dose. Gradually increase the dosage at weekly intervals until optimum clinical response has been obtained or there is a pronounced slowing of the heart rate. Dosages above 400 mg per day have not been studied. If treatment is to be discontinued, reduce the dosage gradually over a period of 1 - 2 weeks.

Heart Failure

Dosage must be individualized and closely monitored during up-titration. Prior to initiation of Meto Zerok, stabilize the dose of other heart failure drug therapy. The recommended starting dose of Meto Zerok 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. Double the dose every two weeks to the highest dosage level tolerated by the patient or up to 200 mg of Meto Zerok. Initial difficulty with titration should not preclude later attempts to introduce Meto Zerok. If patients experience symptomatic bradycardia, reduce the dose of Meto Zerok. If transient worsening of heart failure occurs, consider treating with increased doses of diuretics, lowering the dose of Meto Zerok or temporarily discontinuing it. The dose of Meto Zerok should not be increased until symptoms of worsening heart failure have been stabilized.

More about Meto Zerok (Meto Zerok)

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Consumer resources

• Toprol
• Meto Zerok extended-release tablets
• Meto Zerok
• Meto Zerok (Advanced Reading)

• Other brands: Meto Zerok Tartrate, Meto Zerok Succinate ER, Lopressor

Professional resources

• Meto Zerok (FDA)
• Meto Zerok Succinate (AHFS Monograph)

Related treatment guides

• Heart Failure
• Angina
• Angina Pectoris Prophylaxis
• High Blood Pressure
• Left Ventricular Dysfunction
• More (2) »

Meto Zerok interactions

See also:
What other drugs will affect Meto Zerok?

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 Meto Zerok plus a catecholamine depletor for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension.

CYP2D6 Inhibitors

Drugs that inhibit CYP2D6 such as quinidine, fluoxetine, paroxetine, and propafenone are likely to increase Meto Zerok concentration. In healthy subjects with CYP2D6 extensive metabolizer phenotype, coadministration of quinidine 100 mg and immediate-release Meto Zerok 200 mg tripled the concentration of S-Meto Zerok and doubled the Meto Zerok elimination half-life. In four patients with cardiovascular disease, coadministration of propafenone 150 mg t.i.d. with immediate-release Meto Zerok 50 mg t.i.d. resulted in two- to five-fold increases in the steady-state concentration of Meto Zerok. These increases in plasma concentration would decrease the cardioselectivity of Meto Zerok.

Digitalis, Clonidine, And Calcium Channel Blockers

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 Meto Zerok 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 betablocker therapy, delay the introduction of beta-blockers for several days after clonidine administration has stopped.

Meto Zerok side effects

See also:
What are the possible side effects of Meto Zerok?

The following adverse reactions are described elsewhere in labeling:

•

Worsening angina or myocardial infarction.

•

Worsening heart failure.

•

Worsening AV block.

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.

Hypertension and Angina: Most adverse reactions have been mild and transient. The most common (>2%) adverse reactions are tiredness, dizziness, depression, diarrhea, shortness of breath, bradycardia, and rash.

Heart Failure: In the MERIT-HF study comparing Meto Zerok succinate in daily doses up to 200 mg (mean dose 159 mg once-daily; n=1990) to placebo (n=2001), 10.3% of Meto Zerok succinate patients discontinued for adverse events vs. 12.2% of placebo patients.

The table below lists adverse reactions in the MERIT-HF study that occurred at an incidence of ≥ 1% in the Meto Zerok succinate group and greater than placebo by more than 0.5%, regardless of the assessment of causality.

Adverse Reactions Occurring in the MERIT-HF Study at an Incidence ≥ 1% in the Meto Zerok Succinate Group and Greater Than Placebo by More Than 0.5%

Post-operative Adverse Events: In a randomized, double-blind, placebo-controlled trial of 8351 patients with or at risk for atherosclerotic disease undergoing non-vascular surgery and who were not taking beta–blocker therapy, Meto Zerok succinate 100 mg was started 2 to 4 hours prior to surgery then continued for 30 days at 200 mg per day. Meto Zerok succinate use was associated with a higher incidence of bradycardia (6.6% vs. 2.4%; HR, 2.74; 95% CI 2.19, 3.43), hypotension (15% vs. 9.7%; HR 1.55; 95% CI 1.37, 1.74), stroke (1% vs. 0.5%; HR 2.17; 95% CI 1.26, 3.74) and death (3.1% vs. 2.3%; HR 1.33; 95% CI 1.03, 1.74) compared to placebo.

Post-Marketing Experience

The following adverse reactions have been identified during post-approval use of extended-release Meto Zerok or immediate-release Meto Zerok. 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, chest pain and hypotension.

Respiratory: Wheezing (bronchospasm), dyspnea.

Central Nervous System: Confusion, short-term memory loss, headache, somnolence, nightmares, insomnia, anxiety/nervousness, hallucinations, paresthesia.

Gastrointestinal: Nausea, dry mouth, constipation, flatulence, heartburn, hepatitis, vomiting.

Hypersensitive Reactions: Pruritus.

Miscellaneous: Musculoskeletal pain, arthralgia, blurred vision, decreased libido, male impotence, tinnitus, reversible alopecia, agranulocytosis, dry eyes, worsening of psoriasis, Peyronie’s disease, sweating, photosensitivity, taste disturbance.

Potential Adverse Reactions: In addition, there are adverse reactions not listed above that have been reported with other beta-adrenergic blocking agents and should be considered potential adverse reactions to Meto Zerok succinate.

Central Nervous System: Reversible mental depression progressing to catatonia; an acute reversible syndrome characterized by disorientation for time and place, short-term memory loss, emotional lability, clouded sensorium, and decreased performance on neuropsychometrics.

Hematologic: Agranulocytosis, nonthrombocytopenic purpura, thrombocytopenic purpura.

Hypersensitive Reactions: Laryngospasm, respiratory distress.

Meto Zerok contraindications

See also:
What is the most important information I should know about Meto Zerok?

You should not use this medication if you are allergic to Meto Zerok, or if you have a serious heart problem such as heart block, sick sinus syndrome, or slow heart rate.

Before taking Meto Zerok, tell your doctor if you have congestive heart failure, low blood pressure, circulation problems, pheochromocytoma, asthma or other breathing problems, diabetes, depression, liver or kidney disease, a thyroid disorder, or severe allergies.

Meto Zerok may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.

Drinking alcohol can increase certain side effects of Meto Zerok.

Do not stop taking Meto Zerok without first talking to your doctor. Stopping suddenly may make your condition worse.

If you need surgery, tell the surgeon ahead of time that you are using Meto Zerok.

Meto Zerok is only part of a complete program of treatment for hypertension that may also include diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely if you are being treated for hypertension.

If you are being treated for high blood pressure, keep using this medication even if you feel well. High blood pressure often has no symptoms. You may need to use blood pressure medication for the rest of your life.

Active ingredient matches for Meto Zerok:

Metoprolol in Switzerland.

References

1. DailyMed. "METOPROLOL FUMARATE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
2. PubChem. "metoprolol". https://pubchem.ncbi.nlm.nih.gov/com... (accessed September 17, 2018).
3. DrugBank. "metoprolol". http://www.drugbank.ca/drugs/DB00264 (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology