What are the FDA-approved indications for metoprolol. How does metoprolol work in the body. What are the different formulations of metoprolol available. How should metoprolol be administered properly. What are the key considerations for using metoprolol in different conditions.

Understanding Metoprolol: A Versatile Beta-Blocker

Metoprolol is a widely used medication that belongs to the class of drugs known as beta-blockers. It plays a crucial role in treating various cardiovascular conditions and has been the subject of extensive research and clinical trials. This article delves into the intricacies of metoprolol, exploring its uses, mechanism of action, and proper administration.

FDA-Approved Indications for Metoprolol

Metoprolol has received FDA approval for treating several cardiovascular conditions. What are the primary indications for metoprolol use? The medication is approved for:

• Angina
• Heart failure
• Myocardial infarction (heart attack)
• Atrial fibrillation/flutter
• Hypertension (high blood pressure)

Additionally, metoprolol finds off-label use in managing supraventricular tachycardia and thyroid storm. The versatility of this medication makes it a valuable tool in the arsenal of cardiovascular treatments.

Mechanism of Action: How Metoprolol Works

To understand the effectiveness of metoprolol, it’s essential to explore its mechanism of action. How does metoprolol exert its effects on the cardiovascular system?

Metoprolol is a cardioselective beta-1-adrenergic receptor inhibitor. It competitively blocks beta-1 receptors with minimal or no effects on beta-2 receptors at oral doses less than 100 mg in adults. This selective action results in:

• Decreased cardiac output through negative inotropic and chronotropic effects
• Reduction in heart rate
• Lowered cardiac output

Importantly, metoprolol does not exhibit membrane stabilizing or intrinsic sympathomimetic activity. Its lipophilic nature allows for efficient distribution throughout the body, typical of basic lipophilic drugs.

Absorption and Metabolism

How is metoprolol processed by the body? When taken orally, metoprolol is almost completely absorbed from the gastrointestinal tract. However, it undergoes significant hepatic first-pass elimination, resulting in approximately 50% of the oral dose reaching the systemic circulation. The drug is 11% bound to serum albumin, with a half-life of about 3 to 4 hours for non-extended release tablets.

Formulations and Administration of Metoprolol

Metoprolol is available in various formulations to suit different clinical needs. What are the different forms of metoprolol available for administration?

• Oral tablets (immediate-release and extended-release)
• Intravenous preparations

The choice between immediate-release and extended-release formulations depends on the specific clinical scenario and patient needs. How do these formulations differ in their pharmacokinetics?

Metoprolol succinate (extended-release) produces more level drug concentrations compared to metoprolol tartrate (immediate-release), which has more peak-to-trough variation. Despite these pharmacokinetic differences, studies have shown that both agents produce similar clinical effects, both acute and chronic.

Proper Administration Guidelines

Ensuring correct administration is crucial for optimal therapeutic outcomes. How should metoprolol be administered?

• Immediate-release oral formulation: Take with or immediately following food intake
• Short-acting formulation (metoprolol tartrate): Usually administered twice daily
• Extended-release formulation (metoprolol succinate): Can be taken once daily

It’s worth noting that while the short-acting formulation may be effective for hypertension when taken once per day, lower doses may not control blood pressure for a full 24 hours. The extended-release formulation can be taken without regard to meals, offering greater flexibility for patients.

Clinical Efficacy and Comparative Studies

The effectiveness of metoprolol in various cardiovascular conditions has been extensively studied. What does the evidence say about its clinical efficacy?

Several landmark trials have demonstrated the benefits of metoprolol:

• 1980s randomized trials showed mortality benefit in acute myocardial infarction
• The Metoprolol Atherosclerosis Prevention in Hypertensives (MAPHY) trial revealed benefits over diuretics in preventing sudden cardiac death and myocardial infarction
• A large 1990s trial with over 50,000 patients demonstrated reduced mortality and re-infarction when used chronically after myocardial infarction

However, the role of beta-blockers, including metoprolol, as initial therapy for hypertension has been questioned, particularly in the absence of compelling indications.

Comparative Studies: Metoprolol vs. Other Beta-Blockers

How does metoprolol compare to other beta-blockers in clinical efficacy? The carvedilol or metoprolol European trial (COMET) compared metoprolol head-to-head with carvedilol in patients with stable heart failure. The results showed that carvedilol was associated with a statistically significantly lower risk of all-cause death.

However, recent trials have presented conflicting evidence on whether selective beta-1 blockers like metoprolol have any benefit over other beta-blockers such as carvedilol in certain conditions. This ongoing debate underscores the importance of individualized treatment approaches based on patient-specific factors and the particular condition being treated.

Safety Profile and Adverse Effects

Understanding the potential side effects of metoprolol is crucial for safe and effective use. What are the common adverse effects associated with metoprolol?

While generally well-tolerated, metoprolol can cause several side effects, including:

• Fatigue
• Dizziness
• Bradycardia (slow heart rate)
• Hypotension (low blood pressure)
• Gastrointestinal disturbances
• Cold extremities

In rare cases, more serious adverse effects may occur, such as heart block or worsening of heart failure symptoms. Healthcare providers should monitor patients closely, especially when initiating therapy or adjusting doses.

Contraindications and Precautions

Are there situations where metoprolol should not be used? Metoprolol is contraindicated in patients with:

• Severe bradycardia
• Heart block greater than first degree
• Cardiogenic shock
• Decompensated heart failure
• Known hypersensitivity to metoprolol or any component of the formulation

Caution is advised when using metoprolol in patients with bronchospastic diseases, diabetes, and peripheral vascular disease. Abrupt discontinuation should be avoided to prevent potential rebound hypertension or exacerbation of angina symptoms.

Metoprolol in Special Populations

The use of metoprolol requires special consideration in certain patient groups. How should metoprolol be used in pregnant women, elderly patients, or those with renal impairment?

Pregnancy and Lactation

Metoprolol is classified as FDA pregnancy category C. While it has not been shown to cause harm in animal studies, there are no adequate and well-controlled studies in pregnant women. The potential benefits must be weighed against the potential risks when used during pregnancy. Metoprolol does pass into breast milk, and caution is advised when used by nursing mothers.

Elderly Patients

Elderly patients may be more sensitive to the effects of metoprolol, particularly its blood pressure-lowering effects. Dosage adjustments and close monitoring may be necessary in this population.

Renal Impairment

While metoprolol is primarily excreted by the kidneys, no dosage adjustment is necessary in patients with mild to moderate renal impairment. However, patients with severe renal impairment may require dose adjustment and closer monitoring.

Drug Interactions and Considerations

Understanding potential drug interactions is crucial for safe and effective use of metoprolol. What are the significant drug interactions to be aware of when prescribing metoprolol?

• CYP2D6 inhibitors (e.g., quinidine, fluoxetine) can increase metoprolol blood levels
• Calcium channel blockers may have additive effects on heart rate and conduction
• Concurrent use with other beta-blockers or antihypertensives may enhance blood pressure-lowering effects
• Caution is advised when used with drugs that can cause bradycardia (e.g., digoxin)

Healthcare providers should perform a thorough medication review before initiating metoprolol therapy and monitor for potential interactions throughout treatment.

Pharmacogenomics and Metoprolol Response

Recent research has highlighted the role of genetic factors in metoprolol metabolism and response. How do genetic variations affect metoprolol therapy? Variations in the CYP2D6 gene can influence metoprolol metabolism, potentially affecting its efficacy and side effect profile. Patients who are poor metabolizers may experience higher drug levels and increased risk of adverse effects, while ultrarapid metabolizers may have reduced therapeutic efficacy.

While routine genetic testing is not currently recommended for all patients starting metoprolol, it may be considered in cases of unexpected drug responses or side effects.

Future Directions and Ongoing Research

The field of cardiovascular medicine is constantly evolving, and research on metoprolol continues to advance our understanding of its optimal use. What are some areas of ongoing research and potential future developments in metoprolol therapy?

• Personalized medicine approaches based on genetic profiling
• Novel formulations for improved pharmacokinetics and patient adherence
• Exploration of potential neuroprotective effects in certain conditions
• Comparative effectiveness studies with newer beta-blockers and other cardiovascular medications

As research progresses, it’s likely that our approach to using metoprolol and other beta-blockers will become increasingly nuanced and personalized, leading to improved patient outcomes and reduced adverse effects.

In conclusion, metoprolol remains a cornerstone in the management of various cardiovascular conditions. Its versatility, well-established efficacy, and generally favorable safety profile make it a valuable tool in the therapeutic arsenal. However, as with all medications, its use requires careful consideration of individual patient factors, potential interactions, and ongoing monitoring to ensure optimal outcomes. As research continues to refine our understanding of metoprolol’s place in therapy, healthcare providers must stay informed about the latest developments to provide the best possible care for their patients.

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.

Access free multiple choice questions on this topic.

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. 

Review Questions

• Access free multiple choice questions on this topic.

• Comment on this article.

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]

2.

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]

3.

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]

4.

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]

5.

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

6.

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

7.

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]

8.

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]

9.

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]

10.

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]

13.

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]

14.

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]

15.

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]

16.

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]

17.

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]

18.

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]

19.

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.

What is the Best Time of Day to Take Metoprolol?

Written by
Juhi Modi

Medically reviewed by
HaVy Ngo-Hamilton, Pharm.D.
| Dec 20, 2022

Metoprolol is a commonly prescribed drug that is used with or without other blood pressure medications to treat hypertension (high blood pressure). It is also used to treat angina (chest pain) and heart failure, along with other medications. People who have suffered a heart attack are sometimes prescribed metoprolol to improve survival rates. There may be other uses of metoprolol, such as preventing migraine and treating thyrotoxicosis (excessive thyroid hormone).

This article will give you some important information about metoprolol, including how to take this medicine, the best time of day to take it, dosage, side effects, drug interactions, and more.

What is metoprolol? How does it work?

Metoprolol belongs to a group of drugs called selective beta blockers. Their effects occur due to the blocking of beta-1 receptors in the heart tissues. Therefore, a selective beta blocker like metoprolol works by slowing the heart rate while reducing the force of each beat and relaxing the blood vessels. This results in improved blood flow and lowering of blood pressure. 

Metoprolol is available as the active drug metoprolol tartrate in the form of immediate-release tablets and capsules (brand name: Lopressor). It is also available as the active drug metoprolol succinate in extended-release tablets (brand name: Toprol XL).

How to take metoprolol?

You should take metoprolol exactly as prescribed by your healthcare professional. Do not take this medicine more or less frequently than prescribed.

You can take metoprolol with meals or immediately after meals. Swallow the metoprolol tablets whole. Do not break, crush or chew the extended-release tablet or capsule. If you have trouble swallowing pills, you can open an extended-release capsule and sprinkle the contents on a small amount of soft food like applesauce. Do not store the mixture for more than 60 minutes.

Remember that many people with high blood pressure do not have any symptoms. It is important that you continue taking metoprolol even if you feel well. Metoprolol will control your blood pressure and reduce the risks of stroke and heart attacks. Do not suddenly stop taking this medicine without talking to your doctor first. Stopping metoprolol suddenly can lead to rebound hypertension, chest pain, or a heart attack.  

What is the dose of metoprolol for high blood pressure and other conditions?

• The usual dose of metoprolol for high blood pressure is 100 mg per day given in divided doses (immediate-release form) or 25 mg to 100 mg once a day (extended-release form). The maximum dose is 400 mg per day. 
• For chest pain, your doctor may prescribe immediate-release metoprolol, 50 to 100 mg to be taken 2 to 3 times a day
• For acute heart attack or heart failure, the initial metoprolol dose in adults is 25 mg (extended-release capsule) once daily for 2 weeks; the dose can be gradually increased as needed with the maximum dose of 400 mg. 

Why is it better to take metoprolol at night?

It doesn’t matter when you take this medication, as long as you remember to take this blood pressure consistently. You can take it in the morning or at night, but because this medicine can cause dizziness, lightheadedness, and drowsiness, it may be better to take metoprolol at night. Your doctor may advise you to take the first dose of metoprolol before going to bed to see how you feel. If the medicine does not make you feel dizzy or lightheaded, you can start taking single-dose metoprolol in the morning. If you have been prescribed metoprolol more than once a day, try to space out the doses evenly over the course of the day to get a consistent amount of the medication. Avoid drinking alcohol while on metoprolol, as this can make side effects like dizziness worse.

Can metoprolol help you sleep?

Metoprolol may help you sleep. Beta-blockers like metoprolol tartrate (Lopressor) and metoprolol succinate (Toprol XL) work by slowing the heart. These drugs can therefore make you feel tired and drowsy. 

However, it is worth noting that some studies have shown metoprolol can lead to worsening sleep. On the other hand, other beta-blockers like nebivolol (Bystolic) are associated with improved sleep. 

If you have trouble sleeping, talk to your doctor about which beta blocker is the best choice for you.

What is the peak time for metoprolol?

Metoprolol starts working about 2 hours after you take a dose. However, it can take one week or longer to get the full benefits of this medicine. Call your doctor if you do not notice an improvement in your blood pressure numbers at home after 1-2 weeks of taking metoprolol. 

Keep in mind that you may not feel any different while on metoprolol tablets. Do not stop taking metoprolol without your doctor’s approval. This can lead to an increased risk of chest pain and heart attack. If you want to come off metoprolol, your doctor will give you instructions to decrease the dose slowly. 

What should I do in case of a missed dose of metoprolol?

If you miss a dose of metoprolol, take it as soon as you remember. However, if it is almost time for the next dose, skip the missed dose and take the next dose according to your regular dosing schedule. Do not double up on the dose to make up for a missed dose.

What are the side effects of metoprolol?

Common side effects of metoprolol include lightheadedness or dizziness, unusual tiredness, dry mouth, blurred vision, depression, heartburn, stomach pain, gas, bloating, vomiting, constipation, rash, a cold feeling in the hands and feet, and runny nose. 

Tell your doctor if these side effects are severe or do not improve over time. Call your doctor immediately or seek emergency medical attention if you develop an allergic reaction. Signs and symptoms of allergic reactions include skin rash, hives, itching, swelling, and trouble breathing.

What should I avoid while taking metoprolol?

You should avoid taking certain other drugs while on metoprolol because there’s a risk of drug interactions. Some of the other medicines that can interact with metoprolol include:

• Other blood pressure medications like clonidine (Catapres) and reserpine
• Antidepressants like bupropion (Wellbutrin, Zyban), fluoxetine (Prozac, Sarafem), and paroxetine (Paxil, Brisdelle)
• Medications used to treat an irregular heartbeat, such as propafenone (Rythmol) and quinidine
• Psychiatric medications like thioridazine
• h3  blockers like cimetidine
• Antihistamines like diphenhydramine (Benadryl)
• Antimalarials like hydroxychloroquine
• Antivirals like ritonavir (Norvir, in Kaletra)
• Antifungals like terbinafine (Lamisil)

Who should not take metoprolol?

Metoprolol may not be suitable for people with certain medical conditions. Give your doctor a complete medical history before starting metoprolol. Be sure to mention medical conditions like angina, ischemic heart disease (chest pain or previous heart attacks), hypotension (low blood pressure), circulation problems, severe bradycardia (very slow heartbeat), cardiogenic shock, heart block, sick sinus syndrome, decompensated heart failure, lung disease, pheochromocytoma, diabetes, hypoglycemia (low blood sugar), hyperthyroidism (overactive thyroid), liver disease, and Wolff-Parkinson-White syndrome (a rare heart condition associated with a very slow heartbeat). Also, tell your doctor if you have ever had an allergic reaction to any of the active or inactive ingredients in metoprolol tablets.
 

References:

1. https://medlineplus.gov/druginfo/meds/a682864.html
2. https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/019962s032lbl.pdf
3. https://pubmed.ncbi.nlm.nih.gov/18758699/

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Calendar of events:

• 27
  Jul

  School of Pediatric Surgeon: Diagnostic and Therapeutic Endoscopy of the Small Intestine

  end date: July 27, 2023

  Venue: Online

• 09
  Sep

  Conference “Actual Issues of Allergology and Respiratory Medicine”

  end date: 09September 2023

  Venue: Moscow, st. Smolenskaya, 8 (AZIMUT Smolenskaya Hotel) with a partial online broadcast on the educational medical portal Medtouch.

• 14
  Sep

  X Anniversary Congress of pediatricians of the CIS countries “CHILD AND SOCIETY: PROBLEMS OF HEALTH, DEVELOPMENT AND NUTRITION” and the II Congress of Pediatric Surgeons of Central Asia

  end date: 16 September 2023

  Venue: Issyk-Kul district, Kyrgyz Republic, Bosteri village

• 20
  Sep

  XXII Russian Congress “Innovative Technologies in Pediatrics and Pediatric Surgery”

  end date: 22 September 2023

  Venue: Moscow Prospekt Mira, 150, Hotel “Cosmos”

• 21
  Sep

  III All-Russian scientific and practical conference “Musculoskeletal pain in rheumatic diseases”

  end date: 23 September 2023

  Venue: Moscow, hotel «Holiday Inn» Sokolniki, st. Rusakovskaya, house 24

Selective beta-1 adrenergic blockers in the treatment of high blood pressure

Relevance

Selective beta-1 blockers are a subclass of beta-blockers commonly used to treat high blood pressure (BP). Drugs in this class include atenolol (Tenormin), metoprolol (Lopressor), nebivolol (Bystolic), and bisoprolol (Zebeta, Monocor). We have developed a comprehensive methodology to study the effectiveness of lowering blood pressure with various doses and drugs of this class of drugs.

Description of included studies

We identified and included in the review 56 clinical trials investigating the blood pressure lowering effect of eight beta-1 blockers in 7812 participants with high blood pressure. These participants were randomized to either a fixed dose beta-1 blocker or placebo for 3-12 weeks.

Main results

On average, beta-1 blockers lower blood pressure by 10 millimeters systolic and 8 millimeters diastolic pressure in people with mild to moderate high blood pressure. In general, higher doses of beta-1 blockers did not show a greater reduction in blood pressure than lower doses. The maximum reduction in blood pressure was recorded at a dose twice the recommended starting dose.

Higher doses of beta-1 blockers reduced heart rate more than lower doses, so they are more likely to cause the overall side effect of slowing heart rate. Beta-1 selective blockers reduce systolic and diastolic blood pressure to the same extent as other subclasses of beta-blockers, and thus have little or no effect on pulse pressure. This distinguishes them from other classes of antihypertensive agents such as thiazide diuretics, angiotensin-converting enzyme inhibitors, and angiotensin receptor blockers.

Quality of evidence

The quality of the evidence was considered to be low due to various types of bias that may exaggerate the effect. The low quality of the evidence means that further studies are likely to have a major impact on our confidence in the effect estimate and are likely to change this estimate.