Adverse effect of metoprolol. Metoprolol Succinate: Comprehensive Guide to Uses, Side Effects, and Precautions

13.01.197013.06.2021 by alexxlab

What are the primary uses of metoprolol succinate. How does metoprolol succinate affect the cardiovascular system. What are the most common side effects of metoprolol succinate. When should patients avoid taking metoprolol succinate. How should metoprolol succinate be taken for optimal effectiveness.

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Understanding Metoprolol Succinate: A Beta-Blocker for Cardiovascular Health

Metoprolol succinate, commonly known by its brand name Toprol XL, is a beta-blocker medication widely prescribed for various cardiovascular conditions. This extended-release formulation offers prolonged therapeutic effects, making it a preferred choice for many healthcare providers.

What is Metoprolol Succinate?

Metoprolol succinate belongs to the class of drugs called beta-blockers. It works by blocking the effects of epinephrine (adrenaline) on the heart and blood vessels, thereby reducing heart rate, blood pressure, and strain on the heart.

Primary Uses of Metoprolol Succinate

Treatment of high blood pressure (hypertension)
Management of angina pectoris (chest pain)
Heart failure therapy
Prevention of heart attacks in high-risk patients
Treatment of certain types of arrhythmias

Dosage Forms and Strengths of Metoprolol Succinate

Metoprolol succinate is available in various strengths to accommodate different patient needs. The extended-release tablets come in the following dosages:

25 mg
50 mg
100 mg
200 mg

The appropriate dosage is determined by a healthcare professional based on the patient’s condition, response to treatment, and other factors.

How to Identify Metoprolol Succinate Tablets

Metoprolol succinate tablets come in different shapes, colors, and imprints depending on the manufacturer and strength. For example:

Toprol XL 25 mg: Oval, white, imprinted with “A B”
Toprol XL 50 mg: Round, white, imprinted with “AMO”
Toprol XL 100 mg: Round, white, imprinted with “AMS”
Toprol XL 200 mg: Elliptical, white, imprinted with “A MY”

Generic versions may have different appearances but should contain the same active ingredient.

Common Side Effects of Metoprolol Succinate

While metoprolol succinate is generally well-tolerated, some patients may experience side effects. It’s important to be aware of these potential adverse reactions:

Frequently Reported Side Effects

Drowsiness
Dizziness
Fatigue
Slow heartbeat (bradycardia)
Diarrhea
Cold hands and feet
Depression
Shortness of breath

Can metoprolol succinate affect sexual function? In rare cases, decreased sexual ability has been reported. Patients experiencing this side effect should consult their healthcare provider for guidance.

Managing Side Effects

To minimize the risk of dizziness and lightheadedness, patients should rise slowly from a sitting or lying position. If side effects persist or worsen, it’s crucial to inform a doctor or pharmacist promptly.

Precautions and Warnings for Metoprolol Succinate Use

Before starting metoprolol succinate, patients should be aware of certain precautions and potential risks associated with its use.

Medical Conditions Requiring Caution

Asthma or other respiratory disorders
Diabetes
Thyroid disorders
Liver disease
Peripheral artery disease
History of severe allergic reactions

Is it safe to use metoprolol succinate during pregnancy? Metoprolol succinate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Pregnant women should consult their healthcare provider before using this medication.

Drug Interactions

Metoprolol succinate may interact with various medications, including:

Other blood pressure medications
Certain antidepressants
Antiarrhythmic drugs
Diabetes medications

Patients should inform their healthcare provider about all medications, supplements, and herbal products they are taking to avoid potential interactions.

Proper Administration of Metoprolol Succinate

To ensure optimal effectiveness and minimize side effects, it’s crucial to take metoprolol succinate as prescribed by a healthcare professional.

Dosing Instructions

Take metoprolol succinate at the same time each day
Swallow the extended-release tablet whole; do not crush, chew, or break it
The medication can be taken with or without food
If a dose is missed, take it as soon as remembered, unless it’s close to the next scheduled dose

Why might an empty tablet shell appear in stool? With some brands of metoprolol succinate, an empty tablet shell may be visible in the stool. This is normal and does not indicate a lack of medication absorption.

Monitoring and Follow-up While Taking Metoprolol Succinate

Regular monitoring is essential for patients taking metoprolol succinate to ensure its effectiveness and detect any potential complications.

Routine Check-ups

Blood pressure measurements
Heart rate monitoring
Blood tests to check liver and kidney function
Evaluation of symptoms and side effects

How often should patients have follow-up appointments? The frequency of check-ups will be determined by the healthcare provider based on the patient’s individual needs and response to treatment.

Long-term Effects and Considerations of Metoprolol Succinate Use

While metoprolol succinate is generally safe for long-term use, patients should be aware of potential long-term effects and considerations.

Benefits of Long-term Use

Improved cardiovascular health
Reduced risk of heart attacks and strokes
Better management of chronic conditions like hypertension and heart failure

Potential Long-term Concerns

Can long-term use of metoprolol succinate lead to dependency? Unlike some medications, metoprolol succinate does not cause physical dependence. However, abrupt discontinuation can lead to withdrawal symptoms, so any changes in medication should be done under medical supervision.

Some patients may experience metabolic changes with long-term use, such as:

Slight increase in triglycerides
Potential impact on glucose metabolism in diabetic patients

Regular monitoring and lifestyle modifications can help mitigate these potential effects.

Alternatives to Metoprolol Succinate

While metoprolol succinate is effective for many patients, alternative treatments may be considered in certain situations.

Other Beta-Blockers

Atenolol
Propranolol
Carvedilol
Bisoprolol

Alternative Drug Classes

Depending on the condition being treated, alternative medications may include:

ACE inhibitors
Angiotensin II receptor blockers (ARBs)
Calcium channel blockers
Diuretics

How do healthcare providers determine the best alternative? The choice of alternative treatment depends on various factors, including the patient’s specific condition, comorbidities, and potential drug interactions. A thorough evaluation by a healthcare professional is necessary to determine the most appropriate alternative.

Patient Education and Support for Metoprolol Succinate Users

Proper education and support are crucial for patients taking metoprolol succinate to ensure safe and effective use of the medication.

Key Points for Patient Education

Importance of adherence to prescribed dosage
Recognition of potential side effects and when to seek medical attention
Lifestyle modifications to support treatment (e.g., diet, exercise)
Proper storage of medication
Importance of regular follow-up appointments

Support Resources

What resources are available for patients taking metoprolol succinate? Patients can benefit from various support resources, including:

Pharmacist consultations for medication-related questions
Patient support groups for individuals with cardiovascular conditions
Educational materials provided by healthcare providers or pharmaceutical companies
Digital health apps for medication reminders and tracking

By utilizing these resources and maintaining open communication with healthcare providers, patients can optimize their treatment experience and manage their cardiovascular health effectively.

In conclusion, metoprolol succinate is a valuable medication for managing various cardiovascular conditions. While it offers significant benefits, patients should be aware of potential side effects and necessary precautions. With proper use, monitoring, and support, metoprolol succinate can contribute to improved cardiovascular health and quality of life for many individuals.

Side Effects of Toprol XL (Metoprolol Succinate), Warnings, Uses

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Metoprolol Succinate Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Metoprolol Side Effects: What to Watch Out For

If you have any medical questions or concerns, please talk to your healthcare provider. The articles on Health Guide are underpinned by peer-reviewed research and information drawn from medical societies and governmental agencies. However, they are not a substitute for professional medical advice, diagnosis, or treatment.

Metoprolol (brand name Lopressor, Toprol, Toprol XL) is a type of medication known as a beta blocker. This class of medications decreases strain on the heart. Metoprolol is most commonly used to prevent, treat, or improve symptoms for the following conditions (Morris, 2020):

High blood pressure (hypertension)
Chest pain (angina)
Heart failure
Fast, irregular heartbeat like atrial fibrillation or atrial flutter
Heart attack (myocardial infarction)

Metoprolol is a beta blocker commonly used to treat high blood pressure, chest pain, and heart failure.
Common side effects of metoprolol include skin rash, gastrointestinal problems, dry mouth, shortness of breath, weight gain, and depression.
Serious side effects include low blood pressure, very low heart rate, masking of low blood sugar symptoms, and worsening of asthma or heart failure.
The U.S. Food and Drug Administration (FDA) has issued an important warning (called a black box warning) about metoprolol: Do not abruptly stop taking metoprolol without talking to your healthcare provider. Stopping metoprolol suddenly may cause chest pain or a heart attack. If you need to stop metoprolol, your healthcare provider will help you decrease the dose gradually.

Metoprolol works by stopping epinephrine (also known as adrenaline) from binding to beta receptors in your heart muscle. Blocking the beta receptors allows metoprolol to decrease the workload on the heart. Metoprolol causes your heart to beat slower and squeeze less forcefully, thereby lowering blood pressure and improving chest pain.

Metoprolol is an effective drug, but, like most medicines, it can have both mild and severe side effects.

Common side effects of metoprolol include (UpToDate, n.d.):

Skin rash
Itching
Gastrointestinal problems like nausea, vomiting, diarrhea, or stomach pain
Depression
Dizziness
Tiredness
Vertigo
Cold hands and feet
Dry mouth
Dry eyes and/or blurred vision
Breathing difficulties like shortness of breath, wheezing, and cough
Weight gain – 1.2 pounds of weight gain on average (Sharma, 2001)
Sexual dysfunction

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Black box warning from the FDA (the most serious warning they issue): Do not abruptly stop taking metoprolol without talking to your healthcare provider. Stopping metoprolol suddenly may cause chest pain or heart attack (myocardial infarction). If you need to stop metoprolol, your healthcare provider will help you decrease the dose gradually (FDA, 2006). Serious side effects of metoprolol include (UpToDate, n.d.):

Slow heartbeat (bradycardia): One of the ways that metoprolol works is by decreasing the heart rate to lighten the load on the heart—so a somewhat lower heart rate is expected. However, some people may experience a heart rate that is too low, causing fainting spells (syncope), dizziness, chest pains, fatigue, and confusion.
Low blood pressure (hypotension): Metoprolol is often given to help lower blood pressure in people with high blood pressure or other heart conditions. Sometimes, the blood pressure can drop too low. Symptoms include dizziness, fainting, blurred vision, fatigue, shallow breathing, rapid pulse, and confusion. Your blood pressure may drop only after standing up from a sitting or laying down position—this is called orthostatic hypotension. Severely low blood pressure is a life-threatening emergency.
Worsening asthma or chronic obstructive pulmonary disease (COPD): Metoprolol, a beta-blocker, has a small risk of triggering an asthma attack or worsening COPD by causing bronchospasm (tightening of the airways). This is because the beta receptors that line the lungs are similar to the ones that metoprolol targets in the heart and blood vessels. However, metoprolol is less likely to cause breathing issues than some of the other beta blocker drugs.
Masking of hypoglycemic symptoms: When your blood sugar drops too low, your body gives you signals to let you know so that you can replenish your glucose reserves—these signals typically include shakiness, anxiety, confusion, rapid heartbeat (palpitations), lightheadedness, etc. However, metoprolol may mask these signs, preventing you from realizing that your blood sugars are too low. Keeping your blood sugars too low for too long can lead to seizures, unconsciousness, and even death in rare cases.
Heart block: Metoprolol can interfere with the normal electrical system of the heart; this can lead to heart block, which causes an irregular heartbeat.
Worsening of heart failure: People with heart failure who are taking metoprolol may notice a worsening of their heart failure symptoms; this may be especially true for women (DailyMed, 2018). An American Heart Association journal reported that women who are taking beta blockers (like metoprolol) have a higher risk of heart failure during an acute coronary syndrome (ACS) than men (Bugiardini, 2020).

This list does not include all possible side effects and others may exist. Check with your pharmacist or healthcare provider for more information.

Before starting metoprolol, or any other new medication, seek medical advice about potential drug interactions. Medicines that may interact with metoprolol include (DailyMed, 2018):

Monoamine oxidase inhibitors (MAOIs): These drugs are often used to treat depression and may increase the effects of metoprolol and can potentially increase side effects. Examples include isocarboxazid, phenelzine, selegiline, and tranylcypromine.
Epinephrine: People who take metoprolol and use epinephrine for severe allergic reactions, may find that the usual dose of epinephrine does not work as well. If you have a history of severe allergic reactions, be sure to let your healthcare provider know that you are taking a beta blocker.
Inhibitors of the CYP2D6 system: Metoprolol is broken down by the CYP2D6 system in the liver. Drugs that interfere with the CYP2D6 system prevent metoprolol from being metabolized. As a result, you can have double the typical amounts of metoprolol circulating in your bloodstream; this increases your risk of side effects. Examples of these medications include quinidine, fluoxetine, paroxetine, and propafenone.
Medications that slow the heart rate: Since metoprolol lowers the heart rate, combining it with other drugs that also decrease the heart rate increases your risk of having a very slow heart rate (bradycardia). Examples include digoxin, clonidine, diltiazem, and verapamil.
Sildenafil (brand name Viagra) or other phosphodiesterase-5 (PDE5) inhibitors: Metoprolol may cause more of a drop in blood pressure if taken with PDE5 inhibitors.
Alcohol: Some types of metoprolol (namely metoprolol succinate) are available in an extended-release formulation. In the presence of alcohol, this extended-release action is sped up, and the metoprolol is released into your system faster.

This list does not include all possible drug interactions with metoprolol and others may exist. Check with your pharmacist or healthcare provider for more information.

Certain groups of people should avoid using metoprolol or use it with caution (DailyMed, 2018):

People with asthma: Metoprolol may trigger an asthma attack, and people with asthma or COPD should avoid using it. Make sure your healthcare provider is aware that you have asthma before starting metoprolol.
People with diabetes: Metoprolol can block the signs of low blood sugar, like increased heart rate, sweating, and tremors.
People with a slow heart rate (bradycardia) or low blood pressure (hypotension): Metoprolol lowers blood pressure and heart rate.
Pregnant women: The U.S. Food and Drug Administration (FDA) has deemed metoprolol as pregnancy category C; this means that there is not enough information to determine the risk to the pregnancy (FDA, 2006). Women and their healthcare providers should weigh the benefits of taking metoprolol against the risk to the fetus.
Nursing mothers: Metoprolol does get into the breastmilk, in small quantities, and no adverse effects have been reported. Women and their healthcare providers should weigh the risks and benefits of the medication (FDA, 2006).
People with liver disease: Since metoprolol is broken down by the liver, people with liver disease may have higher than expected levels of metoprolol in their system. They may need a lower dose of metoprolol (DailyMed, 2018).

This list does not include all possible at risk groups and others may exist. Check with your pharmacist or healthcare provider for more information.

There are two different types of metoprolol: metoprolol tartrate and metoprolol succinate. Metoprolol tartrate (brand name Lopressor) is used in immediate-release tablets and comes in 25 mg, 37.5 mg, 50 mg, 75 mg, and 100 mg pills. Metoprolol succinate (brand name Toprol XL) is used in the extended-release capsules and tablets and comes in 25 mg, 50 mg, 100 mg, and 200 mg pills. The specific dose recommended by your healthcare provider will vary depending on the condition being treated, as well as your other medical issues.

Both forms of metoprolol are available as generic medications. Metoprolol tartrate ranges from $4 to $9 for a 30-day supply, depending on the dose. Metoprolol succinate varies from $6 to $18 for a 30-day supply, again depending on the dose.

Bugiardini, R., Yoon, J., Kedev, S., Stankovic, G., Vasiljevic, Z., Miličić, D., Manfrini, O., van der Schaar, M., Gale, C. P., Badimon, L., & Cenko, E. (2020). Prior Beta-Blocker Therapy for Hypertension and Sex-Based Differences in Heart Failure Among Patients With Incident Coronary Heart Disease. Hypertension https://doi.org/10.1161/HYPERTENSIONAHA.120.15323
DailyMed from the U.S. National Library of Medicine and the National Institutes of Health(NIH):Metoprolol succinate capsule, extended-release (2018). Retrieved on 12 August 2020 from https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=90aa06a3-100f-4466-b950-506303707b01
Morris J, Dunham A. Metoprolol. StatPearls [Internet]. 2020 Retrieved on 12 August 2020 from: https://www.ncbi.nlm.nih.gov/books/NBK532923/
Sharma, A. M., Pischon, T., Hardt, S., Kunz, I., & Luft, F. C. (2001). Hypothesis:β-Adrenergic Receptor Blockers and Weight Gain. Hypertension, 37(2), 250–254. doi: 10.1161/01.hyp.37.2.250 https://www.ahajournals.org/doi/full/10.1161/01.hyp.37.2.250
UpToDate – Metoprolol: Drug Information (n.d.) Retrieved on 12 August 2020 from https://www.uptodate.com/contents/metoprolol-drug-information?search=metoprolol&source=panel_search_result&selectedTitle=1~148&usage_type=panel&kp_tab=drug_general&display_rank=1#F195759
U.S. Food and Drug Administration (FDA) – Metoprolol succinate, extended-release tablets (2006) Retrieved on 12 August 2020 from https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/019962s032lbl.pdf

What should I avoid while taking metoprolol?

One of the perks of modern medicine is that it allows people to be their own health advocates. When contemplating a procedure or treatment plan, we now have the opportunity to work with our healthcare providers to make informed decisions about medical conditions and our health journey.

This is particularly useful when it comes to starting a new medication and understanding how your daily habits, diet, and lifestyle might influence outcomes.

Metoprolol (brand names Lopressor and Toprol-XL) is a beta-blocker that slows the heart rate, lowers blood pressure, and improves blood flow.
Certain drugs may interfere with the way metoprolol works.
Avoid alcohol and limit driving when first starting metoprolol or increasing the dose because of the side effects of drowsiness and dizziness.
Depending on the version, metoprolol can cost between $4 and $44 per month.
FDA black box warning: Sudden discontinuation of metoprolol can lead to chest pain and heart attack. When stopping the medication, create a plan for tapering the dose to avoid serious adverse effects.

This article focuses on metoprolol (brand names Lopressor and Toprol-XL), a prescription medication used to treat high blood pressure and heart problems. Other brand names for metoprolol include Apo-Metoprolol, Betaloc, Novo-Metoprol, and Minimax.

Metoprolol belongs to a class of medications known as beta-blockers, or beta-adrenergic blocking agents, designed to lower blood pressure. Metoprolol slows down your heart rate making it easier for your heart to circulate blood throughout your body. While other beta-blockers may affect other parts of the body, metoprolol works mainly on the heart (UpToDate, n.d.).

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In addition to managing high blood pressure, metoprolol is used to prevent severe chest pain (angina), improve survival after a heart attack, and treat congestive heart failure.

The medication comes in three forms: an immediate-release tablet (metoprolol tartrate), an extended-release tablet (metoprolol succinate), and in an injectable form (metoprolol tartrate). The tablets are prescription only, and the injection is usually performed in a hospital setting.

Metoprolol succinate (brand name Toprol-XL) tablets are taken once per day, while metoprolol tartrate (brand name Lopressor) can be taken two to four times per day. The exact dosage will depend on the condition being treated, other medications, age, etc.

No need to avoid grapefruits or greens with metoprolol! There’s been limited research on foods to avoid while taking either form of the medication. The main thing to note is that because metoprolol is a beta-blocker, a type of drug known to increase potassium levels in the blood, you might want to be mindful of potassium-rich foods like meat, bananas, and sweet potatoes (Chang, 2016). However, metoprolol only increases your risk of elevated potassium by 13%, compared to 54% for ACE (angiotensin-converting enzyme) inhibitors (Chang, 2016). Generally speaking, focus on eating a healthy and balanced diet as advised for anyone living with a heart condition.

Drinking alcohol while taking metoprolol can increase your risk of drowsiness. During the first few days of taking metoprolol, or after an increased dose, consider avoiding alcohol until you see how the medicine affects you. Also, if you are taking the extended-release form of metoprolol (metoprolol succinate), alcohol speeds up the action of metoprolol, and the drug is released into your system faster than expected (DailyMed, 2018)

Similarly, avoid driving a car or riding a bike when starting the medication or increasing the dose. Metoprolol can cause some people to feel dizzy, which isn’t conducive to safety behind the wheel (NIH, 2017)

Metoprolol is a category C pregnancy drug, which means that there aren’t adequate studies in humans to determine whether it harms the fetus (DailyMed, 2018). Pregnant women are advised to discuss medication options with their healthcare provider before starting metoprolol. If the potential risks outweigh the benefits, they may receive alternative medications for high blood pressure in pregnancy.

Metoprolol is also present in small quantities in breast milk. Nursing mothers should seek medical advice regarding the risks and benefits of using metoprolol (DailyMed, 2018).

Certain drugs may interfere with the way metoprolol works. Before starting metoprolol, tell your healthcare provider about any prescription drugs, as well as any over-the-counter medicines, vitamins, and herbal supplements you are taking—you may need to change the dose or monitor for side effects (NIH, 2017).

Also important to note, both forms of metoprolol share similar drug interactions. This means that if you’re taking any of the medications listed below, there could be a chance that combining them with metoprolol increases your risk of an adverse reaction (DailyMed, 2018):

Heart and blood pressure medications: reserpine, other beta-blocking agents (like propranolol), propafenone, hydralazine, calcium-channel blockers (like diltiazem)
Mental health medications: bupropion, fluoxetine, paroxetine, clonidine, thioridazine
Other medications: antiretroviral drugs like ritonavir, antihistamine drugs like diphenhydramine (brand name Benadryl), antimalarial drugs like quinidine, antifungal drugs like terbinafine (brand name Lamisil)

This list does not include all potential drug interactions. Seek medical advice for additional drug information if you have any questions/concerns.

Metoprolol is a widely prescribed medication for heart conditions in the United States, but it does come with a list of side effects and drug interactions.

While most common side effects of metoprolol succinate (brand name Toprol-XL) and metoprolol tartrate (brand name Lopressor) are mild and transient, the FDA has issued a black box warning for metoprolol: sudden discontinuation of metoprolol can lead to chest pain and heart attack. When stopping the medication, create a plan for tapering the dose to avoid serious adverse effects (FDA, 2008).

Other side effects of metoprolol include depression, tiredness, diarrhea, wheezing, shortness of breath, dry mouth, stomach pain, nausea, weight gain, constipation, and hives. More serious, yet less common, side effects are low blood pressure (hypotension), heart block, worsening asthma or other lung conditions, slow heart rate (bradycardia), worsening of heart failure, and masking of the low blood sugar response (DailyMed, 2018).

Generally speaking, metoprolol is considered an inexpensive and respected drug for treating heart conditions.

Metoprolol tartrate (brand name Lopressor) will cost anywhere from $4 to $18 for a one-month supply, while Metoprolol succinate (brand name Toprol-XL) costs about twice as much at $14 to $44 for a one-month supply (Good RX, 2020). Both versions of the drug are also available as generics, which is usually a cost-effective alternative to the brand name drugs.

Before starting the metoprolol, review all health information with your healthcare provider. Let them know if you have a history of slow heart rate, heart failure, blood circulation problems, thyroid disease, or pheochromocytoma. You should also consult your provider if you’re considering metoprolol while pregnant, planning to become pregnant, or breastfeeding.

While taking the medication, your healthcare provider may ask you to regularly check your blood pressure and pulse to determine your response and any potential adverse effects to metoprolol.

If you skip a dose, take the missed dose as soon as possible. If this aligns with the next dose, skip the missed dose and continue with a regular dosing schedule. The main thing to remember is never double dose to make up for the missed one (NIH, 2017).

Finally, consult your healthcare provider before ending a medication, and metoprolol is no exception. Abruptly stopping metoprolol can cause severe side effects, such as chest pain and an increased risk of heart attacks, so discuss a plan for slowly decreasing the dose before stopping this medication.

If you experience signs of an allergic reaction—hives, difficulty breathing, or swelling—seek immediate medical attention from a healthcare professional.

Chang, A. R., Sang, Y., Leddy, J., Yahya, T., Kirchner, H. L., Inker, L. A., Matsushita, K., Ballew, S. H., Coresh, J., & Grams, M. E. (2016). Antihypertensive Medications and the Prevalence of Hyperkalemia in a Large Health System. Hypertension. doi: 10.1161/HYPERTENSIONAHA.116.07363. Retrieved on 10 August 2020 from https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4865437/
DailyMed from the U.S. National Library of Medicine and the National Institutes of Health (NIH):Metoprolol succinate capsule, extended-release (2018). Retrieved on 10 August 2020 from https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=90aa06a3-100f-4466-b950-506303707b01
Good RX. (2020). Metoprolol Generic Lopressor. Retreived on 10 August 2020 from https://www.goodrx.com/metoprolol?form=tablet&dosage=25mg&quantity=60&days_supply
UpToDate – Metoprolol: Drug Information (n.d.). Retrieved 10 August 2020 from https://www.uptodate.com/contents/metoprolol-drug-information
U.S. Food & Drug Administration (n.d.). LOPRESSOR (metoprolol tartrate) tablet. Retrieved on 10 August 2020 from https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/017963s062,018704s021lbl.pdf
U.S. Food & Drug Administration (n.d.). METOPROLOL SUCCINATE EXTENDED-RELEASE TABLETS. Retrieved on 10 August 2020 from https://www.accessdata.fda.gov/drugsatfda_docs/label/2006/019962s032lbl.pdf
U.S. Department of Health & Human Services (HHS). (2020). FDA Pregnancy Categories. Retrieved on 10 August 2020 from https://chemm.nlm.nih.gov/pregnancycategories.htm
U.S. National Library of Medicine (NIH) Medline Plus – Metoprolol (2017). Retrieved on 10 August 2020 from https://medlineplus.gov/druginfo/meds/a682864.html#side-effects

Metoprolol – StatPearls – NCBI Bookshelf

Continuing Education Activity

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.

Earn continuing education credits (CME/CE) on this topic.

Indications

Metoprolol is FDA-approved for the treatment of 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 also is conflicting evidence regarding the optimal selection of a particular beta-blocker in the treatment of 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 chronically.[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 the 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 with documented hypersensitivity to the drug or components. Also, caution is necessary for patients that have 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 a consideration 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, healthcare workers, including nurse practitioners, should familiarize themselves with one or two beta-blockers, rather than know all of them.

Metoprolol can be administered orally or IV and works quickly.

Continuing Education / Review Questions

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): Apr 13, 2020. Deadly Single Dose Agents. [PubMed: 28722879]

Metoprolol – an overview | ScienceDirect Topics

Beta Blockers

For metoprolol, one of the most often-prescribed beta blockers, the role of CYP2D6 genetic polymorphisms in its pharmacokinetics seems to be well established. CYP2D6 catalyzes O-demethylation and, even more specifically, α-hydroxylation of the drug (Lennard et al., 1982a). Not only metoprolol plasma concentrations but also effects on heart rate correlated significantly with the CYP2D6 metabolic phenotype (Lennard et al., 1982b). In a study with 281 individuals, heart rate response differed significantly by CYP2D6 phenotype with PM and IM showing greater reduction (Hamadeh et al., 2014). In UM carrying the CYP2D6 gene duplication, total clearance of metoprolol was about 100% higher compared with the EM as the reference group (367 vs 168 L/h) (Kirchheiner et al., 2004a). The reduction of exercise-induced heart rate by metoprolol in the UM group was only about half of that observed in the EM.

On the basis of the considerable impact of the CYP2D6 polymorphism on the disposition of CYP2D6 substrates, it has often been suggested that CYP2D6 PM are more susceptible to adverse effects than EM at standard doses of metoprolol (Rau et al., 2002; Wuttke et al., 2002; Zineh et al., 2004) which is the same as for antidepressive and antipsychotic drugs. For instance, the CYP2D6 PM genotype was overrepresented among 24 patients with severe metoprolol-associated adverse effects in a retrospective study (Wuttke et al., 2002). However, metoprolol is well tolerated in the majority of patients with cardiovascular diseases irrespective of CYP2D6 genotype (Hamadeh et al., 2014). The effect of beta blockers on the quality of life of hypertensive patients has not been extensively studied. The wide therapeutic range of metoprolol may explain why it is well tolerated in the majority of CYP2D6 PM and IM, despite several-fold higher plasma concentrations.

Another beta blocker, the racemate carvedilol, which has been approved as an adjunctive therapy in the treatment of heart failure, is known to be stereoselectively metabolized by cytochrome P450 enzymes (Neugebauer and Neubert, 1991). CYP2D6 polymorphism has been shown to alter the stereoselective disposition of carvedilol with PM demonstrating an impaired clearance of the R-enantiomer; thus, the PM were affected by a more pronounced α1-blockade, which might outweigh the beneficial β1-blocking effects (Zhou and Wood, 1995). Hence, CYP2D6 genotyping might predict therapeutic outcomes in cardiac insufficient patients treated with carvedilol. However, inhibition of CYP2D6 metabolism by administration of fluoxetine in EM led to significant changes in plasma pharmacokinetics in favor of the R-enantiomer, without any effect on blood pressure and heart rate, which casts doubt on the clinical significance of the CYP2D6 genotype for treatment with carvedilol in antihypertensive therapy (Graff et al., 2001).

In summary, CYP2D6 genotyping might be beneficial, if at all, for long-term treatment with metoprolol in indications such as heart failure or in post-myocardial infarction patients when no surrogate parameter such as blood pressure is available to predict long-term efficacy. However, pharmacogenetic diagnostics is not generally done in patients using beta blockers, and at present it does not seem likely to become a general tool for therapeutic improvement.

Lopressor, Toprol XL, Kapspargo Sprinkle (metoprolol) dosing, indications, interactions, adverse effects, and more

Black Box Warnings

Lopressor and Toprol XL only

Ischemic heart disease may be exacerbated after abrupt withdrawal

Hypersensitivity to catecholamines has been observed during withdrawal

Exacerbation of angina and, in some cases, myocardial infarction (MI) may occur after abrupt discontinuance

When long-term beta blocker therapy (particularly with ischemic heart disease) is discontinued, dosage should be gradually reduced over 1-2 weeks with careful monitoring

If angina worsens markedly or acute coronary insufficiency develops, beta-blocker administration should be promptly reinitiated, at least temporarily (in addition to other measures appropriate for unstable angina)

Patients should be warned against interruption or discontinuance of beta-blocker therapy without physician advice

Because coronary artery disease (CAD) is common and may be unrecognized, beta-blocker therapy must be discontinued slowly, even in patients treated only for hypertension

Contraindications

Hypersensitivity

Lopressor

Hypertension and angina: Sinus bradycardia, 2°/3° heart block, cardiogenic shock, sick sinus syndrome (unless permanent pacemaker in place), severe peripheral vascular disease, pheochromocytoma
Myocardial infarction: Severe sinus bradycardia, heart rate

Toprol XL

Second- and third-degree heart block, deompensated heart failure, sick sinus syndrome (except in patients with functioning artificial pacemaker), severe bradycardia, cardiogenic shock

Kapspargo Sprinkle

Severe bradycardia, second or third degree heart block, cardiogenic shock, decompensated heart failure, sick sinus syndrome (unless a permanent pacemaker is in place), and in patients who are hypersensitive to any component of this product

Cautions

Use with caution in cerebrovascular insufficiency, CHF, cardiomegaly, myasthenia gravis, hyperthyroidism or thyrotoxicosis (may mask signs or symptoms), liver disease, renal impairment, peripheral vascular disease, psoriasis (may cause exacerbation of psoriasis)

May exacerbate bronchospastic disease; monitor closely

Beta blockers can cause myocardial depression and may precipitate heart failure and cardiogenic shock

Sudden discontinuance can exacerbate angina and lead to MI and ventricular arrhythmias in patients with CAD

Worsening cardiac failure may occur during up-titration of metoprolol succinate; if such symptoms occur, increase diuretics and restore clinical stability before advancing the dose of metoprolol succinate; it may be necessary to lower the dose of metoprolol succinate or temporarily discontinue it

Bradycardia, including sinus pause, heart block, and cardiac arrest, has been reported; patients with 1° atrioventricular block, sinus node dysfunction, or conduction disorders may be at increased risk

Increased risk of stroke after surgery

May potentiate hypoglycemia in patients with diabetes mellitus and may mask signs and symptoms

Avoid starting high-dose regimen of extended-release metoprolol in patients undergoing noncardiac surgery; use in patients with cardiovascular risk factors is associated with bradycardia, hypotension, stroke, and death

Long-term beta blockers should not be routinely withdrawn before major surgery; however, impaired ability of the heart to respond to reflex adrenergic stimuli may augment risks of general anesthesia and surgical procedures

Metoprolol loses beta-receptor selectivity at high doses and in poor metabolizers

If drug is administered for tachycardia secondary to pheochromocytoma, it should be given in combination with an alpha blocker (which should be started before metoprolol is started)

While taking beta blockers, patients with history of severe anaphylactic reaction to variety of allergens may be more reactive to repeated challenge

Extended release tablet should not be withdrawn routinely prior to major surgery

Hydrochlorothiazide, can cause an idiosyncratic reaction, resulting in acute transient myopia and acute angle-closure glaucoma, which can lead to permanent vision loss if not treated; discontinue hydrochlorothiazide as rapidly as possible if symptoms occur; prompt medical or surgical treatments may need to be considered if intraocular pressure remains uncontrolled; risk factors for developing acute angle-closure glaucoma may include history of sulfonamide or penicillin allergy

Caution in patients with history of psychiatric illness; may cause or exacerbate CNS depression

Beta-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease

Drug interactions overview

Catecholamine depleting drugs (eg, reserpine, monoamine oxidase (MAO) inhibitors) may have an additive effect when given with beta-blocking agents; monitor when coadministration with catecholamine depleting drugs for evidence of hypotension or marked bradycardia, which may produce vertigo, syncope, or postural hypotension
While taking beta-blockers, patients with a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated challenge and may be unresponsive to the usual doses of epinephrine used to treat an allergic reaction
Drugs that are strong inhibitors of CYP2D6, such as quinidine, fluoxetine, paroxetine, and propafenone, were shown to double metoprolol concentrations; no information about moderate or weak inhibitors, but are likely to increase metoprolol concentration; closely monitor patients when the combination cannot be avoided
Digitalis glycosides, clonidine, diltiazem and verapamil slow atrioventricular conduction and decrease heart rate
Concomitant administration of hydralazine may inhibit presystemic metabolism of metoprolol leading to increased concentrations of metoprolol
Concomitant use with beta blockers can increase the risk of bradycardia; if clonidine and a beta blocker, such as metoprolol are coadministered, withdraw the beta-blocker several days before the gradual withdrawal of clonidine because beta-blockers may exacerbate the rebound hypertension that can follow the withdrawal of clonidine
If replacing clonidine by beta-blocker therapy, delay introduction of beta-blockers for several days after clonidine administration has stopped
Metoprolol succinate is released faster from Kapspargo Sprinkle in the presence of alcohol; may increase the risk for adverse events associated with Kapspargo Sprinkle
Avoid alcohol consumption

Metoprolol instructions for use: indications, contraindications, side effects – description of Metoprolol tab. 25 mg: 10, 20, 30, 40, 50 or 60 pcs. (27338)

When used simultaneously with antihypertensive drugs, diuretics, antiarrhythmic drugs, nitrates, there is a risk of severe arterial hypotension, bradycardia, AV blockade.

When used simultaneously with barbiturates, the metabolism of metoprolol is accelerated, which leads to a decrease in its effectiveness.

With simultaneous use with hypoglycemic agents, it is possible to enhance the effect of hypoglycemic agents.

With simultaneous use with NSAIDs, it is possible to reduce the hypotensive effect of metoprolol.

With simultaneous use with opioid analgesics, the cardiodepressant effect is mutually enhanced.

With simultaneous use with peripheral muscle relaxants, neuromuscular blockade may increase.

With simultaneous use with agents for inhalation anesthesia, the risk of inhibition of myocardial function and the development of arterial hypotension increases.

With simultaneous use with oral contraceptives, hydralazine, ranitidine, cimetidine, the concentration of metoprolol in blood plasma increases.

With simultaneous use with amiodarone, arterial hypotension, bradycardia, ventricular fibrillation, asystole are possible.

With simultaneous use with verapamil, C _max in blood plasma and AUC of metoprolol increase. The minute and stroke volume of the heart, pulse rate, arterial hypotension decrease.Perhaps the development of heart failure, dyspnea and sinus blockade.

With intravenous administration of verapamil while taking metoprolol, there is a threat of cardiac arrest.

With simultaneous use, it is possible to increase the bradycardia caused by digitalis glycosides.

When used simultaneously with dextropropoxyphene, the bioavailability of metoprolol increases.

With simultaneous use with diazepam, a decrease in clearance and an increase in AUC of diazepam is possible, which can lead to an increase in its effects and a decrease in the speed of psychomotor reactions.

With simultaneous use with diltiazem, the concentration of metoprolol in the blood plasma increases due to the inhibition of its metabolism under the influence of diltiazem. The effect on the activity of the heart is additively inhibited due to the slowing down of the impulse conduction through the AV node caused by diltiazem. There is a risk of developing severe bradycardia, a significant decrease in stroke and minute volume.

With simultaneous use with lidocaine, a violation of the excretion of lidocaine is possible.

With simultaneous use with mibefradil in patients with low activity of the isoenzyme CYP2D6, it is possible to increase the concentration of metoprolol in the blood plasma and increase the risk of toxic effects.

With simultaneous use with norepinephrine, epinephrine, other adreno- and sympathomimetics (including in the form of eye drops or as part of antitussives), a slight increase in blood pressure is possible.

With simultaneous use with propafenone, the concentration of metoprolol in the blood plasma increases and a toxic effect develops.It is believed that propafenone inhibits the metabolism of metoprolol in the liver, decreasing its clearance and increasing serum concentrations.

With simultaneous use with reserpine, guanfacine, methyldopa, clonidine, severe bradycardia may develop.

With simultaneous use with rifampicin, the concentration of metoprolol in blood plasma decreases.

Metoprolol may cause a slight decrease in theophylline clearance in smokers.

Fluoxetine inhibits the isoenzyme CYP2D6, this leads to inhibition of the metabolism of metoprolol and its cumulation, which can enhance the cardiodepressant effect and cause bradycardia.A case of lethargy development is described.

Fluoxetine and mainly its metabolites are characterized by a prolonged T _1/2, so the likelihood of drug interaction persists even several days after discontinuation of fluoxetine.

There are reports of a decrease in the clearance of metoprolol from the body when used simultaneously with ciprofloxacin.

Simultaneous use with ergotamine may increase peripheral circulatory disorders.

With simultaneous use with estrogens, the antihypertensive effect of metoprolol decreases.

With the simultaneous use of metoprolol increases the concentration of ethanol in the blood and lengthens its excretion.

Memorial Sloan Kettering Cancer Center

This document, provided by Lexicomp ^®, contains all the information you need to know about the drug, including the indications, route of administration, side effects, and when you should contact your healthcare provider.

Trade names: USA

Kapspargo Sprinkle; Lopressor; Toprol XL

Trade names: Canada

AG-Metoprolol-L; APO-Metoprolol; APO-Metoprolol SR; APO-Metoprolol Type L; DOM-Metoprolol; DOM-Metoprolol-L; JAMP-Metoprolol-L; Lopresor SR; Lopresor [DSC]; Metoprolol-100; Metoprolol-25; Metoprolol-50; Metoprolol-L; PMS-Metoprolol-B; PMS-Metoprolol-L; RIVA-Metoprolol-L; SANDOZ Metoprolol (Type L) [DSC]; Sandoz Metoprolol SR; TEVA-Metoprolol

Warning

Do not stop taking this drug suddenly.If you stop taking this drug abruptly, your chest pain may worsen and, in some cases, even a heart attack. The risk may be increased with certain types of heart disease. To avoid side effects, this drug should be stopped gradually as directed by your doctor. Call your doctor right away if you experience or worsen chest pain or other heart problems.

What is this drug used for?

Used to treat high blood pressure.
Used to treat chest pain and chest pressure.
Used to treat heart failure (weakened heart).
It is used to prevent the development of repeated myocardial infarction and to prolong life.
This medicinal product may be used for other indications. Consult your doctor.

What do I need to tell my doctor BEFORE taking this drug?

If you are allergic to this drug, any of its ingredients, other drugs, foods or substances.Tell your doctor about your allergy and how it manifested itself.
If you have any of the following health problems: certain types of heart rhythm disturbances called heart block or weak sinus syndrome, heart failure (weakened heart), low blood pressure, poor blood flow to the upper or lower extremities, shock caused by disturbances from the side of the heart, or bradycardia.
If you have any of the following health problems: asthma or other breathing problems such as COPD (chronic obstructive pulmonary disease).

This list of drugs and diseases that may be adversely associated with this drug is not exhaustive.

Tell your doctor and pharmacist about all the medicines you take (both prescription and over-the-counter, natural products and vitamins) and your health problems. You need to make sure that this drug is safe for your medical condition and in combination with other drugs you are already taking.Do not start or stop taking any drug or change the dosage without your doctor’s approval.

What do I need to know or do while taking this drug?

Tell all healthcare providers that you are taking this drug. These are doctors, nurses, pharmacists and dentists.
Avoid driving or other activities that require increased attention until you see how this drug affects you.
To reduce the risk of dizziness or loss of consciousness, get up slowly from a lying or sitting position. Use caution when going up and down stairs.
Measure blood pressure and heart rate as directed by your doctor.
Perform blood tests as directed by your healthcare practitioner. Please consult your doctor.
This drug may interfere with some laboratory tests.Tell all healthcare providers and lab staff that you are taking this drug.
This drug may mask signs of low blood sugar. Consult your doctor.
If you have high blood sugar (diabetes), your blood sugar should be checked regularly.
If you are taking this drug and have high blood pressure, talk to your doctor before taking any over-the-counter drugs that can raise blood pressure.These drugs include medicines for coughs and colds, diet pills, stimulants, nonsteroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen or naproxen, and some naturally occurring drugs.
You may need to refrain from consuming alcoholic beverages with certain medications. Ask your doctor or pharmacist to see if you should refrain from drinking alcoholic beverages with this drug.
This drug may increase the severity of these conditions if you have signs of an overactive thyroid gland, such as tachycardia. If you have an overactive thyroid and suddenly stop taking this drug, your condition may worsen and be life threatening. Please consult your doctor.
If you have had a very severe allergic reaction, consult your doctor. If you come into contact with the agent that caused the allergy, there is a risk of an even more severe reaction.Talk to your doctor if you are using epinephrine to treat very severe allergic reactions. Epinephrine may not work well while you are taking this drug.
Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding. The benefits and risks for you and your child will need to be discussed.

What side effects should I report to my doctor immediately?

WARNING. In rare cases, some people with this drug can have serious and sometimes deadly side effects. Call your doctor or doctor right away if you have any of the following signs or symptoms, which may be associated with serious side effects:

Signs of an allergic reaction such as rash, hives, itching, reddened and swollen skin with blistering or scaling, possibly associated with fever, wheezing or wheezing, tightness in the chest or throat, difficulty breathing, swallowing or speaking, unusual hoarseness, swelling in the mouth, face, lips, tongue, or throat.
Depression.
Severe dizziness or fainting.
When chest pain occurs or worsens.
The appearance or aggravation of cardiac arrhythmias.
Bradycardia.
Shortness of breath, sudden weight gain, or swelling of the arms or legs.

What are some other side effects of this drug?

Any medicine can have side effects. However, many people have little or no side effects.Call your doctor or get medical help if these or any other side effects bother you or do not go away:

Feeling dizzy, tired, or weak.
Diarrhea, indigestion or vomiting.

This list of potential side effects is not exhaustive. If you have any questions about side effects, please contact your doctor. Talk to your doctor about side effects.

You can report side effects to the National Health Office.

You can report side effects to the FDA at 1-800-332-1088. You can also report side effects at https://www.fda.gov/medwatch.

What is the best way to take this drug?

Use this drug as directed by your healthcare practitioner. Read all the information provided to you. Follow all instructions strictly.

Immediate-release tablets:

Take with or immediately after meals.
Swallow whole with a full glass of water.
Continue taking this drug as directed by your doctor or other healthcare professional, even if you feel well.

Extended release tablets:

Take with or immediately after meals.
Swallow whole. Do not chew or crush.
You can break a tablet in half. Do not chew or grind.
Continue taking this drug as directed by your doctor or other healthcare professional, even if you feel well.

Sustained-release capsules:

Take this medication with or without food.
Swallow whole. Do not chew or crush.
If you cannot swallow this drug whole, pour the contents into applesauce, pudding, yogurt, or other soft foods.Then swallow the mixture without chewing within 60 minutes of mixing. Do not store for future use.
Continue taking this drug as directed by your doctor or other healthcare professional, even if you feel well.
This medication may be used by patients with feeding tubes. Apply as directed. Flush the feeding tube after using this drug.

Injection:

For intravenous injection.

What should I do if a dose of a drug is missed?

All oral preparations:

Skip the forgotten dose and return to your normal schedule.
Do not take 2 doses at the same time or an additional dose.

Injection:

Call your doctor for further instructions.

How do I store and / or discard this drug?

All oral preparations:

Store at room temperature in a dry place.Do not store in the bathroom.
Protect from heat.

Injection:

If you need to store this drug at home, ask your doctor, nurse, or pharmacist for information about how it is stored.

All forms of issue:

Store all medicines in a safe place. Keep all medicines out of the reach of children and pets.
Dispose of unused or expired drugs.Do not empty into toilet or drain unless directed to do so. If you have any questions about the disposal of your medicinal products, consult your pharmacist. Your area may have drug recycling programs.

General information on medicinal products

If your health does not improve or even worsens, see your doctor.
You should not give your medicine to anyone and take other people’s medicines.
Some medicines may come with other patient information sheets. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
Some medicines may come with other patient information sheets. Check with your pharmacist. If you have questions about this drug, talk with your doctor, nurse, pharmacist, or other healthcare professional.
If you think an overdose has occurred, call a Poison Control Center immediately or seek medical attention. Be prepared to tell or show which drug you took, how much and when it happened.

Use of information by consumer and limitation of liability

This information should not be used to make decisions about taking this or any other drug. Only the attending physician has the necessary knowledge and experience to make decisions about which drugs are suitable for a particular patient.This information does not guarantee that the drug is safe, effective, or approved for the treatment of any disease or specific patient. Here are only brief general information about this drug. It does NOT contain all available information on the possible use of the drug with instructions for use, warnings, precautions, information about interactions, side effects and risks that may be associated with this drug. This information should not be construed as a treatment guide and does not replace information provided to you by your healthcare professional.Please consult your doctor for complete information on the possible risks and benefits of taking this drug.

Copyright

instructions for use, analogs, articles »Drug Handbook

From the nervous system: increased fatigue, weakness, headache, slowing down of the speed of mental and motor reactions. Rarely: paresthesias in the extremities (in patients with “intermittent” claudication and Raynaud’s syndrome), tremors, convulsions, depression, anxiety, decreased attention, drowsiness, insomnia, “nightmares”, confusion or short-term memory loss, hallucinations, asthenia, myasthenia gravis …From the senses: rarely – decreased vision, decreased secretion of lacrimal fluid, dryness and soreness of the eyes, conjunctivitis, tinnitus, hearing loss.
From the CVS: sinus bradycardia, decreased blood pressure, orthostatic hypotension (dizziness, sometimes loss of consciousness). Rarely – a decrease in myocardial contractility, the development (worsening) of CHF (edema, swelling of the feet and / or lower legs, shortness of breath), cardiac arrhythmias, manifestation of angiospasm (increased peripheral circulation disorders, cooling of the lower extremities, Raynaud’s syndrome), myocardial conduction disturbances, cardialgia.Very rarely – aggravation of pre-existing abnormalities of AV conduction.
From the digestive system: nausea, vomiting, abdominal pain, dry mouth, constipation or diarrhea, in some cases – impaired liver function (dark urine, yellowness of the sclera or skin, cholestasis), changes in taste.
On the part of the skin: skin rashes (exacerbation of psoriasis), psoriasis-like skin reactions, skin flushing, exanthema, photodermatosis, increased sweating, reversible alopecia. From the respiratory system: nasal congestion, bronchospasm when administered in high doses (loss of selectivity and / or in predisposed patients), shortness of breath.
From the endocrine system: hyperglycemia (in patients with non-insulin dependent diabetes mellitus), hypoglycemia (in patients receiving insulin), hypothyroidism. Allergic reactions: urticaria, pruritus, rash. Laboratory indicators: thrombocytopenia (unusual bleeding and hemorrhage), agranulocytosis, leukopenia, increased activity of “liver” enzymes, hyperbilirubinemia.
Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.
Other: back or joint pain, weight gain, decreased libido and / or potency, with abrupt cessation of treatment – “withdrawal” syndrome (increased angina attacks, increased blood pressure).
Overdose. Symptoms: severe severe sinus bradycardia, dizziness, AV block (up to the development of complete transverse blockade and cardiac arrest), decreased blood pressure, fainting, arrhythmia, ventricular premature beats, HF, cardiogenic shock, cardiac arrest, bronchospasm, loss of consciousness, coma, nausea , vomiting, cyanosis. The first signs of an overdose appear 20 minutes – 2 hours after taking the drug.
Treatment: gastric lavage and the appointment of adsorbent drugs; symptomatic therapy: with a pronounced decrease in blood pressure – the patient should be in the Trendelenburg position; in the case of an excessive decrease in blood pressure, bradycardia and heart failure – IV, with an interval of 2-5 minutes, beta-adrenostimulants – until the desired effect is achieved or IV 0.5-2 mg of atropine sulfate. In the absence of a positive effect, dopamine, dobutamine, or norepinephrine. As a follow-up, it is possible to prescribe 1-10 mg of glucagon, staging a transvenous intracardiac pacemaker. In case of bronchospasm, intravenous beta2-adrenergic receptor stimulants should be administered. With convulsions – slow intravenous administration of diazepam. Hemodialysis is ineffective.

Evaluation of the efficacy of slow-release metoprolol in patients with arterial hypertension with disturbed circadian rhythm of arterial pressure | Tikhonov

1.2003 European Society of Hypertension – European Society of Cardiology guidelines for the management of arterial hypertension. J Hypertens 2003; 21: 1011-53.

2. Mazur N.A. Prevention of cardiovascular complications in patients with arterial hypertension. Moscow “Med-practice-M” 2003.

3. Crawford MH. Current diagnosis and treatment in cardiology.McGraw-Hill 2003.

4. Gogin E.E. Hypertonic disease. Moscow 1997.

5. Recommendations for the treatment of hypertension by the WHO and the International Society of Arterial Hypertension. Wedge pharmacol ter 1999; 3: 18-22.

6. Recommendations for the prevention, diagnosis and treatment of arterial hypertension.Arter hypert 2001; 7 (app. 1): 1-16.

7. Kobalava Zh.D., Kotovskaya Yu.V. Blood pressure monitoring: methodological aspects and clinical implications. Moscow 1999.

8. O’Brien ET, Coats A, Owens P, et al. Use and interpretation of ambulatory blood pressure monitoring: recommendations of the British Hypertension Society. BMJ 2000; 320: 1128-34.

9. Uzu T, Kimura G. Diuretics and circadian rhythm of blood pressure. J Clin Hypertens 2000; 2 (4): 273-8.

10. Uzu T, Kimura G. Diuretics shift circadian rhythm of blood pressure from nondipper to dipper in essential hypertension. Circulation 1999; 100 (15): 1635-8.

11.Chazova I.E., Ratova L.G., Dmitriev V.V. et al. The effect of long-term therapy with a combination of losartan and hydrochlorothiazide on the daily blood pressure profile and left ventricular hypertrophy in patients with mild and moderate arterial hypertension. Cardiology 2003; 10: 60-4.

12. Frisina N, Pedulla M, Mento G, et al. Frequency domain of heart rate and blood pressure variability in essential hypertensive patients during sleep: differences between dippers and nondippers.Blood Press Monit 1996; 1 (5): 425-31.

13. Hojo Y, Noma S, Ohki T, et al. Autonomic nervous system activity in essential hypertension: a comparison between dippers and non-dippers. J Hum Hypertens 1997; 11: 665-71.

14. Narkiewicz K, Winnicki M, Schroeder K, et al. Relationship between muscle sympathetic nerve activity and diurnal blood pressure profile.Hypertension 2002; 39 (1): 168-72.

15. Tikhonov P.P., Sokolova L.A. Interrelation between disturbances in the circadian rhythm of blood pressure and heart rate variability in patients with arterial hypertension according to bifunctional monitoring data. Problems of health promotion and disease prevention. Materials of the scientific and practical conference. St. Petersburg 2004; 288-9.

16.1993 guidelines for the management of mild hypertension: memorandum from a WHO / ISH meeting. Bull World Health Organ 1993; 71 (5): 503-17.

17. Mathias CJ. Role of sympathetic efferent nerves in blood pressure regulation and in hypertension. Hypertension 1991; 18: 22-30.

18. Folkow B. Autonomic nervous system in hypertension. Oxford 1994.

19. Shimada K, Kario K. Altered circadian rhythm of blood pressure and cerebrovascular damage. Blood Press Monit 1997; 2 (6): 333-8.

20. Sander D, Winbeck K, Klingelhofer J, et al. Extent of cerebral white matter lesions is related to changes of circadian blood pressure rhythmicity. Arch Neurol 2000; 57 (9): 1302-7.

21.Kukla C, Sander D, Schwarze J, et al. Changes of circadian blood pressure patterns are associated with the occurrence of lacunar infarction. Arch Neurol 1998; 55 (5): 683-8.

22. Galindo C, Soler A, Sanchez-Amat M, et al. To be a non-dipper: a higher cardiovascular risk? AJH 2004; 17 (5 Pt 2): 205A.

23. Bauduceau B, Mayaudon H, Dupuy O, et al.The impact of dipper and non-dipper characteristics in the fluctuation of arterial blood pressure. A study of a population of 484 diabetic patients. Arch Mal Coeur Vaiss 2000; 93 (8): 969-73.

24. Alcantra P, Moreira C, Alcantra C, et al. Abnormal nocturnal blood pressure pattern and prevalence of stroke. AJH 2004; 17 (5 Pt 2): 35A.

25.Cymerys M, Miczke A, Bryl W, et al. Circadian rhythm and variability of blood pressure and target organ damage in essential hypertension. Pol Arch Med Wewn 2002; 108 (1): 625-31.

26. Meredith PA, Perloff D, Mancia G, et al. Blood pressure variability and its implications for antihypertensive therapy. Blood Press 1995; 4: 5-11.

27.Fratolla A, Parati G, Cuspidi C. Prognostic Value of 24-hour Blood Pressure Variability. J Hypertens 1993; 11: 1133-7.

Arpimed

Symptoms : severe hypotension, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, cardiac arrest, bronchospasm, impaired consciousness, coma, nausea, vomiting, cyanosis, sometimes hypoglycemia, sometimes hypoglycemia,The first manifestations usually appear 20 minutes to 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 disorders, 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, 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, you can consider taking 8-10 mg of glucagon. If necessary, the injection can be repeated within 1 hour, after which, if necessary, give an intravenous infusion of glucagon at a rate of 1-3 mg / hour.

Consider taking calcium ions or using a pacemaker.

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

Special instructions

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

When combined therapy with clonidine, the latter should be discontinued a few days after discontinuation of metoprolol, in order to avoid a hypertensive crisis. Above 200 mg / day, cardioselectivity decreases.

If it was decided to interrupt beta-blockade in preparation for surgery, therapy should be discontinued for at least 24 hours.Continued beta blockade reduces the risk of arrhythmias during induction and intubation, but the risk of hypertension may also increase. If treatment continues, caution should be exercised with certain anesthetics. The patient can be protected from vagal reactions by intravenous administration of atropine. During its cancellation, you should carefully monitor the patient’s condition.

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

Discontinuation of the drug should be considered if any similar reaction cannot be explained by anything other than taking 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, manifested in the form of dizziness, bradycardia, and a tendency to collapse.

Serious, sometimes even life-threatening, deterioration of cardiac function can occur with beta-blockers, especially in patients in whom cardiac function depends on the supportive action of the sympathetic system. This is not so much due to the excessive beta-blocking effect as to the fact that patients with limited cardiac function do not tolerate a decrease in sympathetic nervous system activity, even if the decrease is small.This leads to a weakening of contractility, a decrease in heart rate and a slowdown in AV conduction. This can result in pulmonary edema, atrioventricular block and shock. Occasionally, an existing abnormality in AV conduction can worsen, which can lead to AV block. Patients with pheochromocytoma should be given alpha-blockers at the same time.

If it is necessary to carry out a surgical intervention, it is necessary to warn the anesthesiologist about the therapy (the choice 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 clinical signs of thyrotoxicosis. Therefore, metoprolol should be prescribed with caution in patients with thyrotoxicosis or with suspected development, and the function of the thyroid gland and heart should be carefully monitored.

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

Metoprolol may cause or aggravate bradycardia, symptoms of peripheral arterial circulation disorder 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 prescribed for controlled heart failure.In patients with a history of heart failure or a low heart reserve, treatment with cardiac glycosides and / or diuretics should also be considered.

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

In the case of unstable or insulin-dependent diabetes mellitus, it may be necessary to adjust the hypoglycemic treatment (due to the likelihood of severe hypoglycemic conditions).

In patients with significant impairment of liver function, dosage adjustment may be required, since metoprolol undergoes biotransformation in the liver. Patients with hepatic or renal impairment may require a lower dosage, metoprolol is contraindicated in patients with hepatic or renal disease / impairment.Elderly people should be prescribed with caution, starting at a lower dose, although the elderly usually tolerate this drug well. In elderly patients and patients with hepatic or renal impairment, it may be necessary to use the drug at a lower dose, as well as the need for an alternative drug.

Patients with a history of psoriasis should take beta-blockers only after careful study of the situation, as the drug can exacerbate psoriasis.

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

Beta-blockers can unmask myasthenia gravis.

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

1 tablet contains 16 mg of lactose monohydrate, so if you have an 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, it is possible to reduce the production of tear fluid. Dry eyes may occur, sometimes accompanied by skin rashes. In most cases, symptoms disappeared after discontinuation of metoprolol treatment. Patients should be carefully monitored for adverse reactions from the eyes. 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 of attention and speed of psychomotor reactions.

Pregnancy and breastfeeding

It is not recommended to take metoprolol during pregnancy or lactation, unless the expected benefit outweighs the potential risk to the fetus / infant.

Metoprolol has, however, been used for hypertension associated with pregnancy under close supervision after 20 weeks of gestation.Despite the fact that the drug crosses the placental barrier and is found in cord blood, there are no reported cases of fetal abnormalities. Despite this, there is an increased risk of cardiac and pulmonary complications in the newborn during the postpartum period. Beta blockers reduce placental perfusion and can cause fetal death and premature birth.

There was intrauterine growth retardation after long-term treatment of pregnant women with mild to moderate hypertension. There have been cases of beta blockers causing bradycardia in the fetus and newborn, and there have been reports of hypoglycemia and hypotension in newborns.

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

Breastfeeding

Metoprolol is excreted in milk.Although the concentration of metoprolol in milk is very low, breastfeeding should be discontinued during treatment with metoprolol.

If you are pregnant or nursing, think you are pregnant, or plan to become pregnant, consult your doctor or pharmacist before using this medicine.

Drug interactions

Medicines used to treat stomach ulcers such as cimetidine – medicines 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
Medicines used to treat epilepsy, such as barbiturates
drugs for the treatment of mental illness, such as phenothiazines
Anesthetics such as cyclopropane or trichlorethylene
Medicines used to treat certain cancers, in particular kidney cancer, such as aldesleukin
drugs 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, e.g. eye drops
epinephrine (epinephrine) or norepinephrine (norepinephrine), used for anaphylactic shock, or other sympathomimetics – drugs used to treat diabetes
lidocaine (local anesthetic)
moxysilite (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 aminphylline or theophylline
medicines used to treat migraines, such as ergotamine
drugs used to treat heart problems, such as cardiac glycosides, e.g. digoxin
Medicines used to treat rheumatoid arthritis, such as hydroxychloroquine
diphenhydramine (sedative, antihistamine).

Drinking alcohol should be avoided while using this medication. 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.

Vacation conditions

Available by prescription.

Release form and packaging

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

Republic of Armenia, Kotayki Marz, Abovyan, 2nd microdistrict, building 19

Tel .: 374 (222) 21703, 21740 Fax: 374 (222) 21924

instructions for use, analogs, composition, indications

Symptoms: hypotension, sinus bradycardia, atrioventricular block, heart failure, cardiogenic shock, asystole, nausea, vomiting, bronchospasm, cyanosis, hypoglycemia, loss of consciousness, coma.

The symptoms listed above may worsen with the simultaneous intake of alcohol, antihypertensive drugs, quinidine and barbiturates. The first symptoms of an overdose appear 20 minutes – 2 hours after taking the drug.

Treatment: requires intensive care and monitoring of the patient’s vital functions (circulation and respiration, kidney, glycemia, serum electrolytes). If the drug was taken not too long ago, gastric lavage is mandatory, if lavage is not possible and the patient is conscious, vomiting can be induced (in the presence of medical personnel), followed by the introduction of activated carbon and an osmotic laxative.

Atropine (0.25–0.5 mg IV for adults, 10–20 mcg / kg for children) should be given before gastric lavage (due to the risk of vagus stimulation).

In severe hypotension, bradycardia and the threat of heart failure, beta1-agonists (dobutamine) should be injected intravenously at intervals of 2-5 minutes or by infusion until the desired effect is achieved. In the absence of selective beta1-agonists, intravenous administration of atropine or dopamine. In the absence of the desired effect, it is possible to use other adrenergic agonists (isoprenaline or norepinephrine).The administration of glucagon in doses of 1-10 mg is useful in achieving reversibility of the effects of beta-receptor blockade. With severe bradycardia that is resistant to pharmacotherapy, implantation of a pacemaker may be required. Bronchospasm can be relieved by IV administration of a beta2-agonist (eg, salbutamol or terbutaline). These antidotes can be used in excess of therapeutic doses. Hemodialysis is ineffective.

Use during pregnancy and lactation

Metoprolol should not be prescribed during pregnancy and during breastfeeding, unless the expected benefit to the mother outweighs the potential risk to the fetus and / or baby.

Pregnancy

Beta-adrenolytic drugs can impair placental perfusion and cause fetal death and premature birth. There was a delay in intrauterine development of the fetus after prolonged use of metoprolol for pregnant women with small, moderately high blood pressure. Beta-adrenolytic drugs can prolong the course of labor and cause bradycardia in the fetus and newborn. There are also reports of hypoglycemia, hypotension, increased bilirubinemia, as well as a difficult reaction to tissue hypoxemia in a newborn.Treatment with the drug should be interrupted 48–72 hours before the planned date of delivery. Where this is not possible, the newborn should be monitored for 48–72 hours after birth for subjective and objective symptoms of beta-adrenergic receptor blockage (eg, cardiac and pulmonary complications).

Breastfeeding

The concentration of metoprolol in milk is approximately three times higher than in blood plasma.Despite the fact that after using the drug in therapeutic doses, the risk of harmful effects on an infant is small (except for people with a slow metabolism), a breastfed infant should be monitored for signs of beta-adrenergic receptor blockage.

Precautions and features of use

In case of an increase in bradycardia, the dose of the drug must be reduced or discontinued, gradually decreasing the dose.

Beta-adrenolytic drugs should be used with caution in patients with bronchial asthma. If a patient with asthma takes a beta2-adrenergic agonist (in the form of tablets or inhalations), in this case, starting treatment with metoprolol, the dose of beta2-adrenergic agonist should be monitored and increased if necessary.

Metoprolol can interfere with glycemic control in the treatment of diabetes mellitus and mask the signs of hypoglycemia. In patients with non-insulin dependent diabetes mellitus, plasma glucose should be monitored.

Atrioventricular conduction disorders can sometimes worsen during treatment with metoprolol (the possibility of an atrioventricular node blockade).

Metoprolol can exacerbate peripheral arterial disease such as intermittent claudication.

For Prinzmetal angina, beta-blockers can increase the number and duration of attacks.

In patients with psoriasis while taking metoprolol, an exacerbation of the disease is possible.Beta-adrenolytic drugs can exacerbate or cause scaly lichen symptoms.

In the case when metoprolol is prescribed for patients with tumors originating from chromaffin tissue (pheochromocytoma), it is necessary to first apply an alpha-adrenolytic drug and continue its use simultaneously with metoprolol.

Treatment with metoprolol may mask signs of hyperthyroidism.

When conducting general anesthesia while taking beta-blockers, the risk of developing arterial hypotension increases.If a surgical intervention is necessary, the anesthesiologist should be warned about the therapy in order to choose an anesthesia drug with a minimal negative inotropic effect, however, drug withdrawal before surgery in patients with coronary artery disease is not recommended.

Before conducting a radiological study with iodine-containing contrast agents, treatment with metoprolol should be discontinued in advance. In cases where the use of metoprolol is absolutely necessary and cannot be canceled, appropriate treatment must be prescribed.

Avoid prescribing high doses of metoprolol immediately without preliminary titration to patients undergoing noncardiac surgery, since in patients with cardiovascular risk factors this has been associated with bradycardia, arterial hypotension and stroke, including death.

Just like other beta-adrenolytic drugs, metoprolol can increase both sensitivity to allergens and intensify anaphylactic reactions.Epinephrine does not always give the desired therapeutic result in patients treated with beta-adrenolytic drugs.

Patients with severe renal impairment, with severe acute conditions accompanied by metabolic acidosis, and patients receiving combined treatment with digitalis drugs, should be given special attention.

For the elderly, the drug is prescribed with caution in low doses and under constant medical supervision with regular monitoring of renal function indicators.

Patients using contact lenses should take into account that during treatment with beta-blockers, it is possible to reduce the production of tear fluid.

The drug Metoprolol contains lactose monohydrate. It should not be administered to patients with rare hereditary impairment of galactose tolerance, hereditary lactase deficiency, or glucose-galactose malabsorption syndrome.

Influence on the ability to drive vehicles or potentially dangerous machinery

Use with caution during work for drivers of vehicles and people whose profession is associated with increased concentration of attention.During treatment with metoprolol, dizziness and increased fatigue may appear, so patients should assess their reaction to the drug before driving a car or servicing mechanical devices in motion. The described symptoms can be aggravated in case of simultaneous use of alcohol or after changing medications.

Metoprolol, 50 mg, extended release film-coated tablets, 30 pcs.

Co-administration of Metoprolol with the following drugs should be avoided:

Derivatives of barbituric acid : barbiturates (the study was carried out with phenobarbital) slightly increase the metabolism of metoprolol, due to the induction of enzymes.

Propafenone: it is possible to increase the plasma concentration of metoprolol by 2-5 times and the development of side effects characteristic of metoprolol. Probably, the interaction is due to the inhibition by propafenone, like quinidine, of metoprolol metabolism through the cytochrome P4502D6 system. Taking into account the fact that propafenone has the properties of a β-blocker, the joint appointment of metoprolol and propafenone does not seem appropriate.

Verapamil: The combination of β-blockers (atenolol, propranolol and pindolol) and verapamil can cause bradycardia and lead to a decrease in blood pressure.Verapamil and
β-blockers have a complementary inhibitory effect on atrioventricular conduction and sinus node function.

The combination of Metoprolol with the following drugs may require dose adjustment:

Class I antiarrhythmics: Class I antiarrhythmics and
β-blockers can add up negative inotropic effects, which can lead to serious hemodynamic side effects in patients with impaired left ventricular function.You should also avoid this combination in patients with sick sinus syndrome and impaired atrioventricular conduction. Interaction is described using disopyramide as an example.

Amiodarone: The combined use of amiodarone and metoprolol can lead to severe sinus bradycardia. Taking into account the extremely long half-life of amiodarone (50 days), the possible interaction should be considered long after the withdrawal of amiodarone.

Diltiazem: Diltiazem and β-blockers mutually enhance the inhibitory effect on atrioventricular conduction and sinus node function. With the combination of metoprolol with diltiazem, there have been cases of severe bradycardia.

Non-steroidal anti-inflammatory drugs (NSAIDs): NSAIDs weaken the antihypertensive effect of β-blockers. This interaction is most documented for indomethacin and celecoxib. No described interaction was noted for sulindak.In studies with diclofenac, the described reaction was not observed.

Diphenhydramine: Diphenhydramine reduces the clearance of metoprolol to
α-hydroxymetoprolol by 2.5 times. At the same time, there is an increase in the action of metoprolol.

Epinephrine (adrenaline): development of severe arterial hypertension and bradycardia is possible in patients taking nonselective β-blockers (including pindolol and proprapolol) and receiving epinephrine (adrenaline). It is assumed that similar reactions can be observed when using epinephrine in conjunction with local anesthetics in case of accidental ingestion into the vascular bed.It is assumed that this risk is much lower with the use of cardioselective β-blockers.

Phenylpropanolamine: Phenylpropanolamine (norephedrine) in a single dose of 50 mg can cause an increase in diastolic blood pressure. Propranolol mainly prevents the increase in blood pressure caused by phenylpropanolamine. However, β-blockers can cause paradoxical hypertension reactions in patients receiving high doses of phenylpropanolamine. Perhaps the development of a hypertensive crisis while taking phenylpropanolamine.

Quinidine: Quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation (approximately 90% of the population in Sweden), mainly causing a significant increase in the plasma concentration of metoprolol and an increase in
β-blockade. It is believed that a similar interaction is characteristic of other
β-blockers in the metabolism of which cytochrome P4502D6 is involved.

Clonidine: Hypertensive reactions with abrupt withdrawal of clonidine can be intensified by the joint administration of β-blockers.When used together, in case of cancellation of clonidine, the discontinuation of β-blockers should be started several days before the cancellation of clonidine.

Rifampicin: Rifampicin can increase the metabolism of metoprolol, decreasing the plasma concentration of metoprolol.

Cimetidine, hydralazine, selective serotonin reuptake inhibitors (including paroxetine, fluoxetine, sertraline) increase the concentration of metoprolol in blood plasma.

Adverse effect of metoprolol. Metoprolol Succinate: Comprehensive Guide to Uses, Side Effects, and Precautions

Understanding Metoprolol Succinate: A Beta-Blocker for Cardiovascular Health

What is Metoprolol Succinate?

Primary Uses of Metoprolol Succinate

Dosage Forms and Strengths of Metoprolol Succinate

How to Identify Metoprolol Succinate Tablets

Common Side Effects of Metoprolol Succinate

Frequently Reported Side Effects

Managing Side Effects

Precautions and Warnings for Metoprolol Succinate Use

Medical Conditions Requiring Caution

Drug Interactions

Proper Administration of Metoprolol Succinate

Dosing Instructions

Monitoring and Follow-up While Taking Metoprolol Succinate

Routine Check-ups

Long-term Effects and Considerations of Metoprolol Succinate Use

Benefits of Long-term Use

Potential Long-term Concerns

Alternatives to Metoprolol Succinate

Other Beta-Blockers

Alternative Drug Classes

Patient Education and Support for Metoprolol Succinate Users

Key Points for Patient Education

Support Resources

Side Effects of Toprol XL (Metoprolol Succinate), Warnings, Uses

Metoprolol Succinate Oral: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing

Metoprolol Side Effects: What to Watch Out For

What should I avoid while taking metoprolol?

Metoprolol – StatPearls – NCBI Bookshelf

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References

Metoprolol – an overview | ScienceDirect Topics

Beta Blockers

Lopressor, Toprol XL, Kapspargo Sprinkle (metoprolol) dosing, indications, interactions, adverse effects, and more

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Toprol XL

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Metoprolol instructions for use: indications, contraindications, side effects – description of Metoprolol tab. 25 mg: 10, 20, 30, 40, 50 or 60 pcs. (27338)

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Evaluation of the efficacy of slow-release metoprolol in patients with arterial hypertension with disturbed circadian rhythm of arterial pressure | Tikhonov

Arpimed

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Metoprolol, 50 mg, extended release film-coated tablets, 30 pcs.

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