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Metoprolol therapeutic effect: Metoprolol: MedlinePlus Drug Information

Metoprolol – StatPearls – NCBI Bookshelf

Continuing Education Activity

Metoprolol is FDA-approved to treat angina, heart failure, myocardial infarction, atrial fibrillation/flutter, and hypertension. Off-label uses include supraventricular tachycardia and thyroid storm. Both oral and intravenous preparations are available. There are immediate and extended-release preparations available orally. There is controversy regarding the selection of beta-blockers in the management of the above conditions. There is also conflicting evidence regarding the optimal choice of a particular beta-blocker in treating each specific disease. This activity will highlight the mechanism of action, adverse event profile, pharmacology, monitoring, and relevant interactions of metoprolol, pertinent for members of the interprofessional team in the treatment of patients with conditions where it is of clinical value.

Objectives:

  • Identify the mechanism of action of metoprolol.

  • Describe the adverse effects of metoprolol.

  • Summarize the contraindications of metoprolol.

  • Employ interprofessional team strategies for enhancing care coordination and communication to advance the safe use of metoprolol and improve outcomes.

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Indications

Metoprolol is FDA-approved to treat angina, heart failure, myocardial infarction, atrial fibrillation/flutter, and hypertension. Off-label uses include supraventricular tachycardia and thyroid storm. Both oral and intravenous preparations are available. There are immediate and extended-release preparations available orally. There is controversy regarding the selection of beta-blockers in the management of the above conditions. There is also conflicting evidence regarding the optimal selection of a particular beta-blocker in treating each specific disease.[1] The role of beta-blockers as initial therapy for hypertension, particularly in the absence of compelling indications, has been questioned. [2][3] 

Several randomized trials in the 1980s showed a mortality benefit for beta-blockers in acute myocardial infarction.[4][5][6] The Metoprolol Atherosclerosis Prevention in Hypertensives (MAPHY) trial specifically showed a benefit of metoprolol over diuretics regarding sudden cardiac death as well as myocardial infarction.[7] A large randomized trial of over 50,000 patients in the 1990s showed metoprolol to reduce mortality and re-infarction when used chronically after myocardial infarction.[8] Beta-blockers have demonstrated prognostic benefit and reduce mortality in the treatment of chronic heart failure. The carvedilol or metoprolol European trial (COMET) enrolled patients with stable heart failure and compared each drug head-to-head. Carvedilol was associated with a statistically significantly lower risk of all-cause death.[9] However, recent trials have had conflicting evidence on whether selective beta-1 blockers such as metoprolol have any benefit over other beta-blockers like carvedilol. [1]

Mechanism of Action

Metoprolol is a cardioselective beta-1-adrenergic receptor inhibitor that competitively blocks beta1-receptors with minimal or no effects on beta-2 receptors at oral doses of less than 100 mg in adults. It decreases cardiac output by negative inotropic and chronotropic effects. Metoprolol does not exhibit membrane stabilizing or intrinsic sympathomimetic activity. Administration of metoprolol to normal subjects results in a reduction in heart rate and cardiac output; this appears to be related to the dose and concentration of the drug. Metoprolol is mainly lipophilic, and distribution is typical of a basic lipophilic drug. Based on animal studies, it appears to be almost completely absorbed from the gastrointestinal (GI) tract when taken orally.

There is significant hepatic first-pass elimination, which results in around 50% of the oral dose reaching the systemic circulation. It is 11% bound to serum albumin. The half-life of metoprolol is about 3 to 4 hours in most patients for non-extended release tabs. Metoprolol excretion principally occurs via the kidneys.[10] Metoprolol succinate produces more level drug concentrations as compared to metoprolol tartrate, which has more peak-to-trough variation. However, despite these differences in pharmacokinetics, studies have concluded that both agents produce similar clinical effects, both acute and chronic.[11]

Administration

Metoprolol may administration can be either oral or intravenous. The immediate-release oral formulation is to be administered with or immediately following food intake. The administration of the short-acting formulation of metoprolol tartrate is usually twice daily. It may be effective for hypertension when taken once per day; however, lower doses may not control blood pressure for 24 hours. Patients may take the extended-release metoprolol succinate formulation without regard to meals.[12]

Adverse Effects

The primary adverse effects of metoprolol include heart failure exacerbation, fatigue, depression, bradycardia or heart block, hypotension, bronchospasm, cold extremities, dizziness, decreased libido, diarrhea, tinnitus, decreased exercise tolerance, glucose intolerance, and may mask hypoglycemia. Abrupt cessation of the drug may lead to a withdrawal syndrome that could cause angina or myocardial infarction. Tachycardia and hypertension are both common in withdrawal syndrome.[13]

Contraindications

Metoprolol is contraindicated in patients with sick sinus syndrome, second or third-degree heart block (in the absence of pacemaker),  decompensated heart failure, hypotension, and documented hypersensitivity to the drug or components. Also, caution is necessary for patients with a history of noncompliance as the abrupt cessation of the drug can lead to withdrawal syndromes, including angina and myocardial infarction. Patients who have ingested cocaine or methamphetamine have traditionally had a contraindication to the use of selective beta-blocker such as metoprolol. This observation has its basis on case reports, and there is no strong evidence that they cause any deleterious effects. Regardless, agents such as labetalol, which have alpha and beta activity, or calcium channel blockers should be used in these cases. Metoprolol is a pregnancy risk factor Category C drug.[14]

Monitoring

The onset of action for oral immediate-release tablets is within 1 hour, with a duration of effect variable depending on the dose given. The extended-release preparation has a similar onset of action and a duration of up to 24 hours. Metabolism of metoprolol is hepatic with excretion in the urine. If there is renal impairment, there is no dosage adjustment necessary. If there is a history of hepatic impairment, slowly increasing titrated doses to effect should be used. With the use of intravenous (IV) administration, cardiac monitor, including ECG heart rate and blood pressure, should be constant. Oral administration heart rate rhythm and blood pressure require monitoring.[14]

Toxicity

Treatment will vary based on the amount of metoprolol amount taken, comorbidities, age, and other co-investments. On arrival, assess ABCs and monitor appropriate blood work, including coingestants, ECG, large-bore IVs, and pregnancy status if female. Consult poison control/toxicology early in the course. Treatment choices include volume resuscitation, activated charcoal, whole bowel irrigation, nasogastric lavage, atropine, glucagon, calcium gluconate/calcium chloride, high-dose insulin, vasopressors, Intralipid, transcutaneous, or transvenous pacemaker. Cardiac status and a current fluid balance will guide volume resuscitation. Activated charcoal is typically given 1 g/kg and usually only has efficacy if dosed within 1 to 2 hours of ingestion.[15] If the patient has any altered mentation, caution is necessary to the possibility of aspiration. Whole bowel irrigation should be a consideration for extended-release preparations or large quantity ingestion.

Nasogastric lavage is usually ineffective, except for large quantity ingestions. The clinician may consider atropine use, although it is typically ineffective in moderate-to-severe overdoses. Calcium administration to increase intracellular calcium at a dose of 60 mg/kg over 5 to 10 minutes of calcium gluconate. Calcium chloride at a dose of 10 to 20 mL of a 10% solution is an option if central access is obtained. Glucagon dosing is 50 mcg/kg as a bolus with titration of drip. High-dose insulin at a dose of 1 unit per kilogram bolus followed by 1 unit per kilogram per hour drip.[16]

Administration with dextrose with a drip titrating to euglycemia as well as potassium repletion as needed. Vasopressors with epinephrine or norepinephrine titrated rate and blood pressure. Intralipid IV lipid emulsion therapy can serve as a lipid sink that extracts the drug from the myocyte. It may also provide free fatty acids as a substrate. It should be noted that the use of this medication will affect some laboratory monitoring.[17] Consider a transcutaneous or transvenous pacemaker. Extracorporeal membrane oxygenation (ECMO) should be considered for refractory cases.[18] If the clinician is concerned about intentional overdose, they should order a mandatory psychiatric evaluation. There may also be a need for the possibility of co-ingestants and treatment of those as well. For non-extended or non-sustained-release preparations, 4 to 6 hours of observation without any derangement of mental status or vital signs is sufficient. Any extended-release or sustained-release preparation requires 12 to 24 hours of telemetry observation, depending on the preparation. Extra caution should be considered in the pediatric population as very low amounts, including one pill or even one-half pill, which can cause cardiovascular collapse and death.[19]

Enhancing Healthcare Team Outcomes

Metoprolol is an effective beta-blocker for many cardiac disorders. However, prescribers of this drug should be aware that specific indications for this drug are still lacking. While research has shown the drug to lower mortality in CHF patients, the same applies to several other beta-blockers. To ensure the safe use of the drug, all members of the interprofessional healthcare team, including clinicians (MDs, DOs, NPs, and PAs), specialists, nurses, and pharmacists, should be very familiar with the indications, administration, and potential adverse effects and drug interactions of metoprolol, as well as all members of the beta-blocker drug classification, including which agents are specific vs. beta-1 specific. This will result in improved patient outcomes with fewer adverse events. [Level 5]

Metoprolol can be administered orally or IV and works quickly. 

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References

1.

Fröhlich H, Zhao J, Täger T, Cebola R, Schellberg D, Katus HA, Grundtvig M, Hole T, Atar D, Agewall S, Frankenstein L. Carvedilol Compared With Metoprolol Succinate in the Treatment and Prognosis of Patients With Stable Chronic Heart Failure: Carvedilol or Metoprolol Evaluation Study. Circ Heart Fail. 2015 Sep;8(5):887-96. [PubMed: 26175538]

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Lindholm LH, Carlberg B, Samuelsson O. Should beta blockers remain first choice in the treatment of primary hypertension? A meta-analysis. 2005 Oct 29-Nov 4Lancet. 366(9496):1545-53. [PubMed: 16257341]

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Khan N, McAlister FA. Re-examining the efficacy of beta-blockers for the treatment of hypertension: a meta-analysis. CMAJ. 2006 Jun 06;174(12):1737-42. [PMC free article: PMC1471831] [PubMed: 16754904]

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Hjalmarson A, Herlitz J, Holmberg S, Rydén L, Swedberg K, Vedin A, Waagstein F, Waldenström A, Waldenström J, Wedel H, Wilhelmsen L, Wilhelmsson C. The Göteborg metoprolol trial. Effects on mortality and morbidity in acute myocardial infarction. Circulation. 1983 Jun;67(6 Pt 2):I26-32. [PubMed: 6342837]

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Intravenous beta-blockade during acute myocardial infarction. Lancet. 1986 Jul 12;2(8498):79-80. [PubMed: 2873383]

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Sleight P. Use of beta adrenoceptor blockade during and after acute myocardial infarction. Annu Rev Med. 1986;37:415-25. [PubMed: 2871805]

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Wikstrand J, Warnold I, Tuomilehto J, Olsson G, Barber HJ, Eliasson K, Elmfeldt D, Jastrup B, Karatzas NB, Leer J. Metoprolol versus thiazide diuretics in hypertension. Morbidity results from the MAPHY Study. Hypertension. 1991 Apr;17(4):579-88. [PubMed: 2013485]

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Freemantle N, Cleland J, Young P, Mason J, Harrison J. beta Blockade after myocardial infarction: systematic review and meta regression analysis. BMJ. 1999 Jun 26;318(7200):1730-7. [PMC free article: PMC31101] [PubMed: 10381708]

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Remme WJ, Cleland JG, Erhardt L, Spark P, Torp-Pedersen C, Metra M, Komajda M, Moullet C, Lukas MA, Poole-Wilson P, Di Lenarda A, Swedberg K. Effect of carvedilol and metoprolol on the mode of death in patients with heart failure. Eur J Heart Fail. 2007 Nov;9(11):1128-35. [PubMed: 17716943]

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Brogden RN, Heel RC, Speight TM, Avery GS. Metoprolol: a review of its pharmacological properties and therapeutic efficacy in hypertension and angina pectoris. Drugs. 1977 Nov;14(5):321-48. [PubMed: 201441]

11.

Kukin ML, Mannino MM, Freudenberger RS, Kalman J, Buchholz-Varley C, Ocampo O. Hemodynamic comparison of twice daily metoprolol tartrate with once daily metoprolol succinate in congestive heart failure. J Am Coll Cardiol. 2000 Jan;35(1):45-50. [PubMed: 10636257]

12.

Wikstrand J, Hjalmarson A, Waagstein F, Fagerberg B, Goldstein S, Kjekshus J, Wedel H., MERIT-HF Study Group. Dose of metoprolol CR/XL and clinical outcomes in patients with heart failure: analysis of the experience in metoprolol CR/XL randomized intervention trial in chronic heart failure (MERIT-HF). J Am Coll Cardiol. 2002 Aug 07;40(3):491-8. [PubMed: 12142116]

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Helfand M, Peterson K, Christensen V, Dana T, Thakurta S. Drug Class Review: Beta Adrenergic Blockers: Final Report Update 4 [Internet]. Oregon Health & Science University; Portland (OR): Jul, 2009. [PubMed: 21089245]

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Ripley TL, Saseen JJ. β-blockers: a review of their pharmacological and physiological diversity in hypertension. Ann Pharmacother. 2014 Jun;48(6):723-33. [PubMed: 24687542]

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Graudins A, Lee HM, Druda D. Calcium channel antagonist and beta-blocker overdose: antidotes and adjunct therapies. Br J Clin Pharmacol. 2016 Mar;81(3):453-61. [PMC free article: PMC4767195] [PubMed: 26344579]

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Stellpflug SJ, Harris CR, Engebretsen KM, Cole JB, Holger JS. Intentional overdose with cardiac arrest treated with intravenous fat emulsion and high-dose insulin. Clin Toxicol (Phila). 2010 Mar;48(3):227-9. [PubMed: 20141425]

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Walter E, McKinlay J, Corbett J, Kirk-Bayley J. Review of management in cardiotoxic overdose and efficacy of delayed intralipid use. J Intensive Care Soc. 2018 Feb;19(1):50-55. [PMC free article: PMC5810865] [PubMed: 29456602]

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Chenoweth JA, Colby DK, Sutter ME, Radke JB, Ford JB, Nilas Young J, Richards JR. Massive diltiazem and metoprolol overdose rescued with extracorporeal life support. Am J Emerg Med. 2017 Oct;35(10):1581.e3-1581.e5. [PubMed: 28705745]

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Euwema MS, Swanson TJ. StatPearls [Internet]. StatPearls Publishing; Treasure Island (FL): Aug 1, 2022. Deadly Single Dose Agents. [PubMed: 28722879]

Disclosure: Jason Morris declares no relevant financial relationships with ineligible companies.

Disclosure: Alexis Dunham declares no relevant financial relationships with ineligible companies.

Side effects, dosage, uses, and more

  1. Metoprolol oral tablet is available as generic drugs and as brand-name drugs. Brand names: Lopressor and Toprol XL.
  2. Metoprolol comes as immediate-release and extended-release tablets, and an extended-release capsule. It also comes in an injectable form that’s only given by a healthcare provider.
  3. Metoprolol is a drug called a beta-blocker. It’s used to treat conditions such as high blood pressure, heart failure, and angina (chest pain).

Metoprolol is a prescription drug. It comes as immediate-release and extended-release oral tablets, and extended-release oral capsules. It also comes in an injectable form that’s only given by a healthcare provider.

Metoprolol oral tablets are available as the brand-name drugs Lopressor and Toprol XL. They’re also available as generic drugs. Generic drugs usually cost less than the brand-name versions. In some cases, they may not be available in all strengths or forms as the brand-name drugs.

The two brand-name forms of metoprolol (as well as the different generic forms) are different versions of the medication. They’re both metoprolol, but they contain different salt forms. Lopressor is metoprolol tartrate, while Toprol-XL is metoprolol succinate. The different salt forms enable the drugs to be used to treat different conditions.

Metoprolol succinate is an extended-release version of metoprolol, so it remains in your bloodstream for a longer time. Metoprolol tartrate is an immediate-release version of metoprolol.

Why it’s used

Both forms of metoprolol — metoprolol tartrate (Lopressor) and metoprolol succinate (Toprol-XL) — are used to:

  • lower high blood pressure
  • reduce chest pain (angina)

However, metoprolol tartrate is also used to treat and prevent heart attacks, while metoprolol succinate is also used to treat heart failure.

Metoprolol may be used as part of a combination therapy. That means you may have to take it with hydrochlorothiazide or chlorthalidone.

How it works

Both versions of metoprolol belong to a class of drugs called beta-blockers. A class of drugs is a group of medications that work in a similar way. These drugs are often used to treat similar conditions.

Blood pressure is often raised because blood vessels are tightened. This puts a strain on the heart and increases the body’s oxygen demand.

Beta-blockers work by preventing norepinephrine (adrenalin) from acting on beta receptors in blood vessels and in the heart. This causes blood vessels to relax. By relaxing the blood vessels, beta-blockers help to lower the heart rate and decrease the heart’s demand for oxygen. This in turn helps decrease blood pressure and reduce chest pain.

Metoprolol oral tablet can cause certain side effects.

More common side effects

The more common side effects that can occur with metoprolol include:

  • tiredness
  • dizziness
  • diarrhea
  • constipation
  • breathing problems such as shortness of breath, cough, and wheezing
  • bradycardia (heart rate that’s slower than normal)
  • reduced interest in sex
  • rash

If these effects are mild, they may go away within a few days or a couple of weeks. If they’re more severe or don’t go away, talk to your doctor or pharmacist.

Serious side effects

Call your doctor right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects and their symptoms can include the following:

  • Low blood pressure (hypotension). Symptoms can include:
    • severe dizziness
    • lightheadedness
    • fainting
  • Cold hands and feet. Symptoms can include
    • hands and feet that are cold and may be painful
  • Very slow heart rate (severe bradycardia)
  • Extreme fatigue. Symptoms can include:
    • feeling more tired than usual
    • tiredness that gets progressively worse each day
  • Serious depression. Symptoms can include:
    • continuous feelings of sadness or anxiety
    • feelings of hopelessness or worthlessness
    • lack of interest in hobbies you once enjoyed
    • eating too much or too little
    • trouble concentrating

Metoprolol oral tablet can interact with other medications, vitamins, or herbs you may be taking. An interaction is when a substance changes the way a drug works. This can be harmful or prevent the drug from working well.

To help avoid interactions, your doctor should manage all of your medications carefully. Be sure to tell your doctor about all medications, vitamins, or herbs you’re taking. To find out how this drug might interact with something else you’re taking, talk to your doctor or pharmacist.

Examples of drugs that can cause interactions with metoprolol are listed below.

Mental health drugs

Taking metoprolol with reserpine and monoamine oxidase inhibitors (MAOIs) may increase or add to the effects of metoprolol. They may also increase lightheadedness or slow your heart rate more. MAOIs can continue to interact with metoprolol for up to 14 days after taking them. Examples of MAOIs include:

  • isocarboxazid
  • phenelzine
  • selegiline
  • tranylcypromine

Heart rhythm drugs

Taking heart rhythm drugs with metoprolol can slow down your heart rate too much. Examples of these drugs include:

  • digoxin
  • quinidine
  • propafenone

Calcium channel blockers

Like metoprolol, these drugs are used to treat high blood pressure and several other heart problems. Combined with metoprolol, calcium channel blockers may slow your heart rate even more. Doctors sometimes use this combination under close supervision.

Examples of calcium channel blockers include:

  • amlodipine
  • diltiazem
  • felodipine
  • isradipine
  • nicardipine
  • nifedipine
  • nimodipine
  • nisoldipine
  • verapamil

Drugs processed in the same way as metoprolol

Drugs used to treat depression and other mood disturbances are processed in your body by the same systems as metoprolol. Using these drugs with metoprolol could increase the levels of metoprolol in your body. Examples of these drugs include:

  • fluoxetine
  • fluvoxamine
  • paroxetine
  • sertraline
  • bupropion
  • clomipramine
  • desipramine
  • chlorpromazine
  • fluphenazine
  • haloperidol
  • thioridazine

Other drugs that are processed in the body the same way as metoprolol include:

  • the antiretroviral ritonavir
  • antihistamines, including diphenhydramine
  • antimalarial drugs, such as hydroxychoroquine and quinidine
  • antifungal drugs, such as terbinafine
  • the blood pressure drug hydralazine

These drugs can all increase the level of metoprolol in the body.

Alpha-blockers

Alpha-blockers also lower blood pressure. They may decrease blood pressure too much when combined with metoprolol. Examples of these drugs include:

  • reserpine
  • alpha-methyldopa
  • clonidine
  • prazosin

Clonidine must be carefully managed if it’s combined with metoprolol. Stopping the drug suddenly while also taking metoprolol can cause a big jump in blood pressure.

Ergot alkaloids

Ergot alkaloids, such as dihydroergotamine, narrow blood vessels to treat headaches. If you take them at the same time as metoprolol, they may cause dangerous narrowing of blood vessels.

Dipyridamole

Dipyridamole is used for heart testing. Because metoprolol affects your heart rate, you should stop taking it before you’re given dipyridamole to help ensure an accurate test result.

All possible dosages and forms may not be included here. Your dosage, form, and how often you take the drug will depend on:

  • your age
  • the condition being treated
  • how severe your condition is
  • other medical conditions you have
  • how you react to the first dose

Dosage for high blood pressure

Generic: Metoprolol

  • Form: immediate-release oral tablet (metoprolol tartrate)
  • Strength: 25 mg, 37. 5 mg, 50 mg, 75 mg, and 100 mg
  • Form: extended-release oral tablet (metoprolol succinate)
  • Strength: 25 mg, 50 mg, 100 mg, and 200 mg

Brand: Lopressor

  • Form: immediate-release oral tablet (metoprolol tartrate)
  • Strength: 50 mg and 100 mg

Brand: Toprol XL

  • Form: extended-release oral tablet (metoprolol succinate)
  • Strength: 25 mg, 50 mg, 100 mg, and 200 mg

Adult dosage (ages 18–64 years)

Immediate-release tablets

  • Typical starting dosage: 100 mg daily in a single or divided doses. This may be gradually increased if needed.
  • Typical maintenance dosage: 100–450 mg per day.
  • Maximum dosage: 450 mg per day.

Extended-release tablets

  • Typical starting dosage: 25–100 mg daily in a single dose. This may be gradually increased if needed.
  • Maximum dosage: 400 mg per day.

Child dosage (ages 6–17 years)

Extended-release tablets

  • Typical starting dosage: 1 mg/kg once daily (maximum initial dose should not exceed 50 mg once daily). This dosage may be gradually increased if needed.
  • Maximum dosage: 2 mg/kg (or 200 mg) once daily.

Immediate-release tablets

These tablets are not approved for use in this age group.

Child dosage (ages 0–5 years)

Dosage for people younger than 6 years hasn’t been established.

Senior dosage (ages 65 years and older)

Your body may process this drug more slowly. Your doctor may start you on a lowered dosage so that too much of this drug does not build up in your body. Too much of the drug in your body can be dangerous.

Dosage for angina (chest pain)

Generic: Metoprolol

  • Form: immediate-release oral tablet (metoprolol tartrate)
  • Strength: 25 mg, 37. 5 mg, 50 mg, 75 mg, and 100 mg
  • Form: extended-release oral tablet (metoprolol succinate)
  • Strength: 25 mg, 50 mg, 100 mg, and 200 mg

Brand: Lopressor

  • Form: immediate-release oral tablet (metoprolol tartrate)
  • Strength: 50 mg and 100 mg

Brand: Toprol XL

  • Form: extended-release oral tablet (metoprolol succinate)
  • Strength: 25 mg, 50 mg, 100 mg, and 200 mg

Adult dosage (ages 18–64 years)

Immediate-release tablets

  • Typical starting dosage: 50 mg, taken twice a day. This may be gradually increased as needed.
  • Typical maintenance dosage: 100–400 mg per day.
  • Maximum dosage: 400 mg per day.

Extended-release tablets

  • Typical starting dosage: 100 mg taken once a day. This may be gradually increased if needed.
  • Maximum dosage: 400 mg per day.

Child dosage (ages 0–17 years)

Dosage for people younger than 18 years hasn’t been established.

Senior dosage (ages 65 years and older)

Your body may process this drug more slowly. Your doctor may start you on a lowered dosage so that too much of this drug does not build up in your body. Too much of the drug in your body can be dangerous.

Dosage for after a heart attack

Generic: Metoprolol

  • Form: immediate-release oral tablet (metoprolol tartrate)
  • Strength: 25 mg, 37.5 mg, 50 mg, 75 mg, and 100 mg

Brand: Lopressor

  • Form: immediate-release oral tablet (metoprolol tartrate)
  • Strength: 50 mg and 100 mg

Adult dosage (ages 18–64 years)

Immediate-release tablets

Treatment with this drug is often started in the hospital with the intravenous formulation as soon as possible after a heart attack. Treatment with the oral medication as noted below is begun if your body tolerates the intravenous dosing.

  • Typical starting dosage: 50 mg every 6 hours starting 15 minutes after the last intravenous dose and continuing for 48 hours.
  • Typical maintenance dosage: 100 mg twice daily.

Child dosage (ages 0–17 years)

Dosage for people younger than 18 years hasn’t been established.

Senior dosage (ages 65 years and older)

Your body may process this drug more slowly. Your doctor may start you on a lowered dosage so that too much of this drug does not build up in your body. Too much of the drug in your body can be dangerous.

Dosage for heart failure

Generic: Metoprolol

  • Form: extended-release oral tablet (metoprolol succinate)
  • Strength: 25 mg, 50 mg, 100 mg, and 200 mg

Brand: Toprol XL

  • Form: extended-release oral tablet (metoprolol succinate)
  • Strength: 25 mg, 50 mg, 100 mg, and 200 mg

Adult dosage (ages 18–64 years)

Extended-release tablets

  • Typical starting dosage: For people with NYHA Class II heart failure, it’s 25 mg once daily for 2 weeks. For people with more severe heart failure, it’s 12.5 mg once daily.
  • Typical maintenance dosage: Your doctor can double the dosage every 2 weeks to the highest dosage level your body will tolerate, or up to 200 mg per day.

Child dosage (ages 0–17 years)

Dosage for people younger than 18 years hasn’t been established.

Senior dosage (ages 65 years and older)

Your body may process this drug more slowly. Your doctor may start you on a lowered dosage so that too much of this drug does not build up in your body. Too much of the drug in your body can be dangerous.

Special dosage considerations

For people with liver disease: Liver disease may affect your dosage. Your doctor can tell you more.

Disclaimer: Our goal is to provide you with the most relevant and current information. However, because drugs affect each person differently, we cannot guarantee that this list includes all possible dosages. This information is not a substitute for medical advice. Always speak with your doctor or pharmacist about dosages that are right for you.

FDA warning: Don’t stop taking metoprolol suddenly

  • This drug has a black box warning. This is the most serious warning from the Food and Drug Administration (FDA). A black box warning alerts doctors and patients about drug effects that may be dangerous.
  • Don’t stop taking metoprolol suddenly. If you do, you may experience worse chest pain, a jump in blood pressure, or even have a heart attack. Stopping metoprolol is not recommended. If you need to stop taking the drug, first talk to your doctor. Your dosage should be gradually decreased under a doctor’s supervision.

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Allergy warning

This drug can cause a severe allergic reaction. Symptoms can include:

  • trouble breathing
  • swelling of your throat or tongue

If you develop these symptoms, call 911 or go to the nearest emergency room.

Don’t take this drug again if you’ve ever had an allergic reaction to it. Taking it again could be fatal (cause death).

Warnings for people with certain health conditions

For people with asthma or COPD: Generally, people with asthma or chronic obstructive pulmonary disease (COPD) shouldn’t take metoprolol. A doctor may still prescribe it, but with careful monitoring. At higher doses, metoprolol can block different receptors on the breathing passages. This narrows the passages, which worsens asthma or COPD.

For people with diabetes: Metoprolol may eliminate tremors and reduce heart rate. Tremors and an increased heart rate are signs of low blood sugar. Without these signals, it becomes more difficult to recognize low blood sugar levels.

For people with poor circulation: If you have poor circulation in your feet and hands, it may become worse when taking metoprolol. Because metoprolol reduces blood pressure, you may get even less blood to these parts of your body.

Warnings for other groups

For pregnant women: Metoprolol is a category C pregnancy drug. That means two things:

  1. Research in animals has shown adverse effects to the fetus when the mother takes the drug.
  2. There haven’t been enough studies done in humans.

If you’re pregnant and have high blood pressure, speak with your healthcare provider about your treatment options during pregnancy.

For women who are breastfeeding: Metoprolol enters the breast milk and could be passed to your baby if you breastfeed while taking this drug. Talk to your healthcare provider before breastfeeding.

For seniors: Seniors may need a smaller dosage of metoprolol at first. The dosage may then increase gradually.

For children: The immediate-release form of the drug has not been established as safe or effective in children. The extended-release form of this drug can be used to treat high blood pressure in children 6 years of age or older.

Metoprolol oral tablet can be used either as a short-term drug or a long-term drug. It comes with serious risks if you don’t take it as prescribed.

If you stop taking the drug or don’t take it at all: You risk:

  • increasing your blood pressure
  • damaging your blood vessels or main organs, such as your lungs, heart, or liver
  • increasing your risk of a heart attack

Also, if you suddenly stop taking metoprolol for high blood pressure, chest pain, or after a heart attack, you raise your risk of heart attack.

If you miss doses or don’t take the drug on schedule: Not taking metoprolol every day, skipping days, or taking doses at different times of day also come with risks. Your blood pressure might fluctuate too often. That might increase your risk for a heart attack.

If you take too much: You could have dangerous levels of the drug in your body. Symptoms of an overdose of this drug can include:

  • severe low blood pressure
  • heart rhythm changes
  • nausea
  • vomiting

If you think you’ve taken too much of this drug, call your doctor or seek guidance from the American Association of Poison Control Centers at 800-222-1222 or through their online tool. But if your symptoms are severe, call 911 or go to the nearest emergency room right away.

What to do if you miss a dose: If you miss a dose, just take the next dose as planned. Don’t double your dose.

How to tell if the drug is working:

  • For high blood pressure or heart failure: You may not be able to tell if this drug is working. Your doctor can do tests to determine if the drug is helping to treat your condition.
  • For angina: Your chest pain should be reduced.

Keep these considerations in mind if your doctor prescribes metoprolol oral tablet for you.

General

  • Take metoprolol with food. This drug may cause nausea. Taking it with food will allow your stomach to digest it better. Take it either with a meal or right after a meal.
  • Don’t crush the extended-release tablet. However, you can cut the tablet along the score marks (the groove on the tablet) if your doctor recommends a smaller dose.
  • You can cut the immediate-release tablet.

Storage

  • Store at room temperature between 68°F and 77°F (20°C and 25°C). You may briefly store the drug at temperatures as low as 59°F (15°C) and as high as 86°F (30°C).
  • Keep this drug away from light.
  • Don’t store this medication in moist or damp areas, such as bathrooms.

Refills

A prescription for this medication is not refillable.You or your pharmacy will have to contact your doctor for a new prescription if you need this medication refilled.

There are other drugs available to treat your condition. Some may be better suited for you than others. Talk to your doctor about other drug options that may work for you.

Disclaimer: Medical News Today has made every effort to make certain that all information is factually correct, comprehensive, and up-to-date. However, this article should not be used as a substitute for the knowledge and expertise of a licensed healthcare professional. You should always consult your doctor or other healthcare professional before taking any medication. The drug information contained herein is subject to change and is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. The absence of warnings or other information for a given drug does not indicate that the drug or drug combination is safe, effective, or appropriate for all patients or all specific uses.

Arpimed

Metoprolol, 50 mg tablets

Release form Tablets

ATC category Cardiology. Angiology

ATC subcategory Adrenoblockers

Trade name Metoprolol

International name of the drug Metoprolol tartrate (Metoprolol tartrate)

Dosage form

Oral tablets

General characteristics

Basic physical and chemical properties

White, round, biconvex tablets scored on one side; without smell.

Composition

One tablet contains:

active substances: metoprolol tartrate – 50 mg

excipients: 9002 3 microcrystalline cellulose, lactose monohydrate, povidone, sodium starch glycolate, magnesium stearate, calcium hydrogen phosphate.

Pharmacological group and ATC code

Cardioselective beta 1 – adrenoblocker. C07AB02

Pharmacological action

Metoprolol selectively blocks beta1-adrenergic receptors located in the heart muscle. Reduces the formation of cAMP from ATP stimulated by catecholamines, inhibiting the activity of the renin-angiotensin system. It exhibits a membrane-stabilizing effect, has a negative chrono-, dromo-, batmo- and inotropic effect, removing excess impulses during arrhythmias, extrasystole, tachycardia. It slows down the sinus rhythm and suppresses the increased stimulation of the heart muscle in the atrioventricular node, thereby reducing conduction. As a result, the heart rate slows down, blood pressure decreases, and myocardial oxygen demand decreases. Possesses weakly expressed internal sympathomimetic activity.

Pharmacokinetics

Absorption: After oral administration, metoprolol is almost completely (approximately 95%) absorbed from the gastrointestinal tract. The maximum concentration in blood plasma is reached after 1.5-2 hours. Bioavailability increases with food intake.

Metabolism: Plasma protein binding – 12%. In the liver, metoprolol is intensively biotransformed, undergoing stereoselective metabolism with the formation of inactive metabolites. The half-life with active metabolism lasts 3-4 hours, and with passive metabolism 7-8 hours. Penetrates through the blood-brain and placental barrier. It is excreted in breast milk in small amounts.

Excretion: The plasma half-life is about 3.5 hours. Excreted mainly by the kidneys in the form of inactive metabolites (95%), about 3% – unchanged.

Indications

  • moderate to moderate arterial hypertension (as monotherapy or in combination with other antihypertensive drugs)
  • cardiac arrhythmia (sinus tachycardia, ventricular and supraventricular arrhythmia, extrasystole)
  • early use of metoprolol in acute myocardial infarction, reduces the size of the infarct zone and the frequency of ventricular fibrillation. Pain relief may reduce the need for opioid analgesics.
  • angina pectoris
  • secondary prevention of myocardial infarction
  • thyrotoxicosis (in complex therapy)
  • prophylaxis of migraine attacks

Dosage and administration

Inside, with a meal or immediately after a meal, the tablets can be divided in half, but not chewed and washed down with liquid.

The recommended maximum dose should not exceed 400 mg/day.

In arterial hypertension initial dose – 100 mg/day in 1-2 doses, if necessary – 200 mg/day. Combination therapy with diuretics and vasodilators may also be considered to further lower blood pressure.

For angina pectoris – 50 – 100 mg 2-3 times a day.

For tachyarrhythmia – 50 mg 2-3 times a day, if necessary – 200-300 mg / day.

Early prevention of myocardial infarction – 200 mg/day.

Orally, therapy should begin within 15 minutes of the last intravenous injection, 50 mg every 6 hours for 48 hours and preferably within 12 hours of onset of chest pain. Patients who cannot tolerate the full intravenous dose should receive half the recommended oral dose.

Maintenance dose

The usual maintenance dose is 200 mg divided into several doses. Treatment should continue for at least 3 months.

Thyrotoxicosis

50 mg 4 times a day. After normalization of thyroid function, the dose should be gradually reduced.

Migraine prophylaxis – 100-200 mg/day in 2-4 divided doses.

For relief of paroxysmal supraventricular tachycardia is administered parenterally, in a hospital, slowly, at a dose of 2-5 mg (1-2 mg/min). After stopping the attack of arrhythmia, patients are transferred to oral administration at a dose of 50 mg 4 times a day, with the first dose being taken 15 minutes after the cessation of intravenous administration.

Pediatric

Not recommended.

Patients with renal or hepatic insufficiency

Dose adjustment required. You need to follow the doctor’s advice.

Contraindications

  • if you are allergic (hypersensitive) to metoprolol or any of the other ingredients of this medicine
  • atrioventricular block 2-3 degree
  • uncontrolled heart failure
  • severe sinus bradycardia (< 45-50 bpm)
  • sick sinus syndrome (in case no pacemaker is installed)
  • Prinzmetal’s angina pectoris
  • myocardial infarction complicated by severe bradycardia, first-degree conduction block, systolic hypotension (less than 100 mmHg) and/or severe heart failure and cardiogenic shock – severe peripheral circulatory disorders
  • bronchial asthma or history of bronchospasm
  • pheochromocytoma
  • metabolic acidosis
  • concomitant intravenous use of calcium blockers such as verapamil or diltiazem or other antiarrhythmic drugs (such as disopyramide) is contraindicated (exception: use in the intensive care unit) – arterial hypotension
  • diabetes mellitus with frequent episodes of hypoglycemia
  • chronic obstructive pulmonary disease.

Adverse reactions

Adverse reactions identified in the course of clinical trials or as a result of established use according to the indication according to the following classification:

/ 10000 <1/1000) and very rarely (<1/10000)

Organ classification

Very often ( ≥1/10)

Common (≥1/100 to <1/10)

Uncommon (≥1/1000 to <1/100)

Rare (≥1/10000 to <1/1000)

Very rare (<1/10000)

Frequency unknown

Disorders from side of the hematopoietic and lymphatic system

Thrombocytopenia, agranulocytosis

Mental disorders

Depression, nightmares, nervousness, anxiety, impotence

Hallucinations, personality disorder, memory loss/impairment

Nervous system disorders

Dizziness, headache

Decreased alertness, drowsiness or insomnia, paresthesia

Visual impairment

Visual disturbances (e. g. blurred vision, dryness and/or irritation of the eyes

Hearing and vestibular disorders

Tinnitus and above recommended doses, “impaired hearing” (e.g. hearing loss or deafness)

Cardiac disorders

Bradycardia

Heart failure, arrhythmia, palpitations

Cardiac conduction disorders, pain in the region of the heart

Increase in existing intermittent claudication

Vascular disorders

Orthostatic hypotension (sometimes with syncope)

Edema, Raynaud’s phenomenon

Gangrene in patients with severe peripheral circulatory disorders.

Respiratory, thoracic and mediastinal disorders

Dyspnea on exertion

Bronchospasm (which may occur in patients without a history of obstructive pulmonary disease)

Rhinitis

Gastrointestinal disorders

Nausea and vomiting, abdominal pain

Diarrhea or constipation

Dry mouth

Retroperitoneal fibrosis *

Hepatobiliary disorders

Hepatitis

Diseases of the skin and subcutaneous tissue

Skin rash (in the form of urticaria, psoriasiform and dystrophic skin lesions)

Photosensitivity, hyperhidrosis, alopecia, exacerbation of psoriasis.

Occurrence of antinuclear antibodies (not associated with SLE)

Musculoskeletal and connective tissue disorders

Muscle cramps

Arthritis

Reproductive system and mammary gland disorders

Libido and potency disorders

Peyronie’s disease *

General disorders and changes at the injection site

Fatigue

Dysgeusia (taste disorder)

Laboratory instruments and and instruments data

Weight gain, liver dysfunction

* (relevance to the use of metoprolol has not been clearly established).

Beta-blockers may mask symptoms of thyrotoxicosis or hypoglycemia.

Reporting side effects

If you notice any side effects, tell your doctor, pharmacist or pharmacist, including any side effects not listed in this package insert. You can also report side effects to Arpimed LLC by going to the website www.arpimed.com and filling out the appropriate form “Report a side effect or ineffectiveness of a drug” and to the Scientific Center for Expertise of Drugs and Medical Technologies named after. Academician E.Gabrielyan by going to the website www.pharm.am in the section “Report a side effect of a drug” and fill out the form “Map of reports on a side effect of a drug”. Scientific center hotline: +37410200505; +37496220505 By reporting side effects, you help gather more information about the safety of this drug.

Overdose

Symptoms : severe arterial hypotension, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impaired consciousness, coma, nausea, vomiting, cyanosis, hypoglycemia, and occasionally hyperkalemia. The first manifestations usually appear within 20 minutes – two hours after taking the drug.

Treatment: symptomatic therapy, absorption of any drug still present in the gastrointestinal tract can be prevented by induction of vomiting, gastric lavage, administration of activated charcoal and laxative. Artificial respiration may be required. In case of bradycardia and myocardial conduction disturbances, intensive therapy is indicated: intravenous bolus (with a 25-minute interval) administration of atropine sulfate at a dose of 0.5-2 mg. With a decrease in myocardial contractility, intravenous administration of glucagon is indicated at an initial dose of 1-10 mg, then at a dose of 2-2.5 mg/h as a long-term drip infusion. If a convulsive syndrome occurs, a slow intravenous administration of diazepam is recommended. After taking a large dose or in case of hypersensitivity, the patient should be closely monitored and treated in an intensive care unit.

Hypotension and shock should be treated with plasma/plasma substitutes and, if necessary, catecholamines. The beta-blocking effect can be neutralized by slow intravenous administration of isoprenaline hydrochloride, starting at a dose of about 5 mcg / min, or dobutamine, starting at a dose of 2.5 mcg / min, until the desired effect is achieved.

In resistant cases, isoprenaline can be combined with dopamine. If the desired result is not achieved after this, the possibility of taking 8-10 mg of glucagon can be considered. If necessary, the injection can be repeated within 1 hour, after which, if necessary, make an intravenous infusion of glucagon at a rate of 1-3 mg/hour.

Calcium ions or a pacemaker may be considered.

In patients who have received an overdose of hydrophilic beta-blocking drugs, hemodialysis or hemoperfusion may be considered.

Special instructions

Abrupt discontinuation of therapy with beta-blockers should be avoided, especially in patients with ischemic heart disease. If possible, metoprolol should be discontinued gradually over 10 days, reducing the dose to 25 mg over the last 6 days. If necessary, you can start replacement therapy at the same time to prevent exacerbation of angina pectoris. In addition, hypertension and arrhythmia may develop.

In combination therapy with clonidine, the latter should be discontinued a few days after the withdrawal of metoprolol, in order to avoid a hypertensive crisis. At a dose above 200 mg / day, cardioselectivity decreases.

If a decision has been made to interrupt beta-blockade in preparation for surgery, therapy should be discontinued for at least 24 hours. Continued beta blockade reduces the risk of arrhythmia during induction and intubation, but the risk of hypertension may also increase. If treatment is continued, caution should be exercised when using certain anesthetics. The patient can be protected from vagal reactions by intravenous atropine. During its cancellation, the patient’s condition should be carefully monitored.

Although cardioselective beta-blockers may have less effect on lung function than nonselective beta-blockers, their use should be avoided in patients with reversible obstructive airway disease unless there are compelling clinical reasons for their use. Although metoprolol has been shown to be safe in a large number of asthma patients, caution is advised when treating patients with chronic obstructive pulmonary disease. Beta-2 stimulant therapy or adjustment of current therapy may be required. Thus, non-selective beta-blockers should not be used in such patients, and beta-1-selective blockers should only be used with extreme caution. It is recommended to stop therapy with the appearance of skin rashes and the development of depression caused by taking beta-blockers.

Discontinuation of the drug should be considered if any similar reaction cannot be explained by anything other than the drug. Cancellation of beta-blockers should be gradual.

Metoprolol should not be administered to patients with untreated congestive heart failure. The first step is to get congestive heart failure under control. If concomitant treatment with digoxin is carried out, it must be borne in mind that both drugs slow down AV conduction and, therefore, there is a risk of AV dissociation. In addition, mild cardiovascular complications may occur, manifesting as dizziness, bradycardia, and a tendency to collapse.

Serious, sometimes even life-threatening, deterioration in cardiac function may occur with the use of beta-blockers, especially in patients whose cardiac function depends on the supportive action of the sympathetic system. This is not so much due to an excessive beta-blocking effect, but to the fact that patients with limited heart function do not tolerate a decrease in sympathetic nervous system activity, even if this decrease is small. This leads to a weakening of contractility, a decrease in heart rate and a slowdown in AV conduction. This may result in pulmonary edema, atrioventricular block, and shock. Sometimes an existing AV conduction disorder may worsen, leading to AV block. Patients with pheochromocytoma should be given concomitant alpha-blockers.

If surgery is required, the anesthesiologist should be warned about the ongoing therapy (selection of a drug for general anesthesia with a minimal negative inotropic effect), drug withdrawal is not recommended.

Initial administration of high doses of metoprolol to patients undergoing extracardiac surgery should be avoided as it is associated with bradycardia, hypotension and stroke, including death in patients who have risk factors for the cardiovascular system.

Beta-blockers mask some of the clinical signs of thyrotoxicosis. Therefore, metoprolol should be used with caution in patients with or suspected of developing thyrotoxicosis, and thyroid and cardiac function should be closely monitored.

Concomitant use of epinephrine (epinephrine), norepinephrine (norepinephrine) and β-blockers may lead to increased blood pressure and bradycardia.

Metoprolol may cause or exacerbate bradycardia, peripheral arterial circulation symptoms and anaphylactic shock. If the pulse rate drops below 50-55 beats per minute at rest and the patient develops symptoms associated with bradycardia, the dose should be reduced.

Metoprolol can be used in controlled heart failure. In patients with a history of heart failure or low cardiac reserve, treatment with cardiac glycosides and/or diuretics should also be considered.

Metoprolol may reduce the effectiveness of diabetes treatment and mask the symptoms of hypoglycemia. The risk of impaired carbohydrate metabolism or masking symptoms of hypoglycemia is lower with extended release metoprolol tablets than with conventional beta-1 selective blocker tablets and significantly lower than with non-selective beta-blockers. In unstable and insulin-dependent diabetes mellitus, adjustment of hypoglycemic therapy may be required.

In the case of unstable or insulin-dependent diabetes mellitus, adjustment of hypoglycemic treatment may be required (because of the likelihood of severe hypoglycemic conditions).

In patients with significant hepatic impairment, dosage adjustment may be required because metoprolol is biotransformed in the liver. Patients with hepatic or renal insufficiency may require a lower dosage, metoprolol is contraindicated in patients with hepatic or renal disease / insufficiency. Older people should be given with caution, starting with a lower dose, although the elderly usually tolerate this drug well. In elderly patients and patients with hepatic or renal insufficiency, it may be necessary to use the drug at a lower dose, as well as the need to prescribe an alternative drug.

Patients with a history of psoriasis should only take beta-blockers after careful consideration as the drug may exacerbate psoriasis.

Beta-blockers can increase both sensitivity to allergens and the severity of anaphylactic reactions. Treatment with epinephrine (epinephrine) does not always provide the desired therapeutic effect in individuals receiving beta-blockers.

Beta-blockers may unmask myasthenia gravis.

In cirrhosis of the liver, the bioavailability of metoprolol may be increased and the dosage should be adjusted accordingly.

1 tablet of the drug contains 16 mg of lactose monohydrate, so if you have intolerance to some sugars, contact your doctor before taking this drug.

Patients using contact lenses should take into account that during treatment with beta-blockers, a decrease in the production of lacrimal fluid is possible. Dry eyes may occur, sometimes accompanied by skin rashes. In most cases, the symptoms disappeared after discontinuation of treatment with metoprolol. Patients should be closely monitored for adverse eye reactions. If such reactions occur, the possibility of discontinuing metoprolol should be considered.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and psychomotor speed.

Pregnancy and lactation

Pregnancy

Metoprolol is not recommended during pregnancy or lactation unless the expected benefit outweighs the possible risk to the fetus/infant.

Metoprolol, however, has been used for pregnancy-associated hypertension under close supervision after the 20th week of pregnancy. Although the drug crosses the placental barrier and is found in cord blood, there are no reported cases of fetal anomalies. Despite this, there is an increased risk of cardiac and pulmonary complications in the newborn in the postpartum period. Beta-blockers reduce placental perfusion and can cause fetal death and preterm birth.

Fetal growth retardation has been observed after long-term treatment in pregnant women with mild to moderate hypertension. Beta-blockers have been reported to cause fetal and neonatal bradycardia, and there have been reports of hypoglycemia and hypotension in neonates.

Interrupt treatment with metoprolol 48-72 hours before delivery. If this is not possible, close medical monitoring of the newborn is required 24 to 48 hours after birth for symptoms of beta-blockade (eg, cardiac and pulmonary complications). Careful medical supervision of newborns in the first 3-5 days of life is required. The drug passes into breast milk. If necessary, the use of the drug during lactation should stop breastfeeding.

Breast-feeding

Metoprolol is excreted in milk. Despite the fact that the concentration of metoprolol in milk is very low, it is necessary to stop breastfeeding during treatment with metoprolol.

If you are pregnant or breastfeeding, think you are pregnant or plan to become pregnant, ask your doctor or pharmacist for advice before using this medicine.

Drug interactions

  • drugs used to treat stomach ulcers such as cimetidine – drugs used to treat high blood pressure such as hydralazine, clonidine or prazosin
  • drugs used to treat irregular heart rhythms such as amiodarone and propafenone
  • medicines used to treat depression such as tricyclic antidepressants or SSRIs
  • drugs used to treat epilepsy, such as barbiturates
  • medicines for the treatment of mental illness, such as phenothiazines
  • anesthetics such as cyclopropane or trichloroethylene
  • medicines used to treat certain types of cancer, particularly kidney cancer, such as aldesleukin
  • medicines used to treat erectile dysfunction, such as alprostadil
  • anxiolytics or hypnotics (eg temazepam, nitrazepam, diazepam),
  • indomethacin or celecoxib (NSAID)
  • rifampicin (antibiotic) or terbinafine (antifungal)
  • estrogens, such as contraceptives or hormone replacement therapy
  • corticosteroids (eg hydrocortisone, prednisolone)
  • other beta-blockers, eg eye drops
  • epinephrine (epinephrine) or norepinephrine (norepinephrine), used in anaphylactic shock or other sympathomimetics, medicines used to treat diabetes mellitus
  • lidocaine (local anesthetic)
  • moxisilite (used for Raynaud’s syndrome)
  • drugs used in the treatment of malaria, such as mefloquine
  • medicines used to prevent nausea and vomiting, such as tropisetron – medicines used to treat bronchial asthma, such as xanthines, such as aminophylline or theophylline
  • drugs used to treat migraine, such as ergotamine
  • drugs used to treat heart problems, such as cardiac glycosides, such as digoxin
  • medicines used to treat rheumatoid arthritis, such as hydroxychloroquine
  • diphenhydramine (sedative, antihistamine).

Use with alcohol

Alcohol must be avoided while using this medicine. Alcohol can increase blood pressure, thereby weakening the effects of metoprolol.

Storage conditions

The drug should be stored out of the reach of children, protected from moisture and light at a temperature of 15-25 0 C.

Shelf life

Shelf life – 3 years. Do not use after the expiration date.

Dispensing conditions

Available by prescription.

Release form and packaging

3 blisters (1 blister containing 10 tablets) together with the leaflet are placed in a cardboard box.

What helps, analogues, how to take, dosage and side effects

Coronary heart disease (CHD) is the leading cause of disability and death in the population worldwide. The human “motor” experiences enormous loads and stresses throughout life.

In the 60s of the last century, new drugs were discovered that help the heart “rest”. They are called beta-blockers because of the interaction with the receptors of the same name in the heart and blood vessels. In 1988, a group of American scientists for the development and study of the mechanism of action of such drugs received the Nobel Prize.

We are talking about Bisoprolol, a commonly prescribed drug from this group.

All products Bisoprolol

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Bisoprolol: what

When taken internally, bisoprolol reduces blood pressure, regulates the heart rhythm, slows down the heart rate, improves blood supply to the heart muscle and reduces its need for oxygen.

Indications for use of the drug:

  • arterial hypertension (hypertension)
  • With hypertension, the therapeutic effect occurs after 2-5 days, and a stable effect after 1-2 months.
  • prevention of stable angina attacks in coronary heart disease (CHD)

To make it clear what bisoprolol helps in this case, we will tell you more about angina pectoris.

This syndrome occurs when there is an imbalance between the need for oxygen and its supply to the heart muscle. The popular name for angina pectoris is “angina pectoris”. It is manifested by stabbing, squeezing, pressing pain in the chest, which spreads to the left arm, neck, jaw, left shoulder blade and even to the stomach. An attack of angina pectoris can lead to damage or necrosis (death) of a part of the heart.

Due to its properties, bisoprolol protects the heart and helps to avoid such attacks.

Bisoprolol is taken once a day, in the morning, on an empty stomach. Dosage 5 mg or 10 mg, tablets are not chewed, washed down with a small amount of water.

Bisoprolol side effects

  • headache, dizziness
  • insomnia, drowsiness, fatigue
  • diarrhea, nausea, vomiting, dry mouth, constipation
  • nasal congestion, difficulty breathing
  • when administered at high doses in predisposed patients – laryngo- and bronchospasm

Bisoprolol has a “withdrawal” syndrome: upon discontinuation, patients experience an increase in angina attacks, an increase in pressure.

Bisoprolol and alcohol, when used together, increase the depression of the central nervous system.

Bisoprolol contraindications

Contraindications to taking Bisoprolol:

  • hypersensitivity to the active substance and components of the preparation
  • acute or chronic heart failure in the stage of decompensation (when the body itself cannot cope with the pathological situation)
  • cardiogenic shock
  • heart blocks of various origins
  • heart rate (HR) less than 60 beats per minute
  • low blood pressure
  • severe forms of bronchial asthma and obstructive pulmonary disease
  • severe disorders of peripheral circulation, Raynaud’s syndrome
  • breastfeeding period
  • concomitant use of several drugs (listed in the instructions)
  • under 18 years of age

Bisoprolol: analogues

The drug has over 300 analogues produced by Russian and international pharmaceutical companies. We list the most famous ones that can be taken instead of Bisoprolol (you can replace the drug after consulting a doctor)

  • direct (active ingredient identical): Bidop, Biol, Biprol, Concor, Cordinorm, Coronal, Niperten
  • group (similar in effect on the body): Atenolol, Betacard, Betalok, Lokren, Metoprolol, Nebivalol, Nebilet, Egilok

Compare with Bisoprolol, one analogue from each group.

Bisoprolol or Concor what is the difference

Concor is the original patented drug with the active ingredient bisoprolol. Produced by the German company Merck from Swiss-made substance.

Russian companies’ bisoprolol is produced mainly from an Indian substance. Numerous clinical studies have proven that Concor, unlike generics, provides patients with cardiovascular diseases with effective protection of blood vessels and the heart, control of heart rate and blood pressure, and guarantees high safety of use.

The difference between Concor and generic bisoprolol lies in the quality of the main molecule and excipients, as well as in the proven effectiveness.

What is the difference between bisoprolol and metoprolol

Both drugs from the same pharmacological group, but with different active ingredients.

The mechanism of action of both formulas is identical, but Bisoprolol in comparison with Metoprolol has a more pronounced cardioselectivity and a longer duration of action. It is used once a day at a dose of 2.5–20 mg. Metoprolol is prescribed 2 times a day for 50-100 mg.

Metoprolol has more indications for use: for example, doctors prescribe for arrhythmias and after a heart attack. Metoprolol has more side effects, so it is not suitable for long-term therapy.

All products Concor

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All products Metoprolol

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Let’s summarize the information about the drug.

Bisoprolol protects the heart and blood vessels, controls heart rate and blood pressure, guarantees efficacy and safety, which are proven by clinical studies.

Bisoprolol is a prescription drug.