Effectiveness, Ease of Use, and Satisfaction

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Gene Health Metoprolol Succer 25 md 2per day 2014-11-27
Web MD Reviews: I came to Web MD Reviews because I suspected that I was suffering from side effects due to taking, by prescription of my heart surgeon, Metoprolol Succer, 25 mg 2 per day after formerly taking 12,5 mg per day for about 2 years.
Several of these side effects have been bothering me for over a year or more without my realizing …

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Have not taken yet, doctor prescribed just yesterday.

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Condition: High Blood Pressure EffectivenessEase of UseSatisfaction

Please be aware of the cognitive side effects of this drug. Some doctors will tell you there are no known cognitive side effects, but that is NOT TRUE at all. It has been documented by numerous and well respected sources. My mother had no cognitive issues prior to being put on this drug, at the tail end of the first year of being on it, she started displaying signs of forgetfulness. That’s all it ever was and did not disrupt her daily life at all. A few years ago her doctor increased her dosage from 50mg to 100mg and three months later she had her first hallucination. Everyone wrote my mother off has having dementia, but it never made any sense until I did the research myself when nobody else gave it a second thought, including “medical professionals”. This drug has been linked to triggering psychosis and delirium & has been documented as a drug with potential side effects that mimic dementia. This drug is also a beta blocker that can have awful side effects in elderly patients, like what was happening to my mom. If someone you love is taking this drug, and they start showing dementia like symptoms after being put on it, look at this drug as being the potential culprit. You are your loved ones best advocate and need to be their voice when they can’t explain what they’re going through, or are unaware of the symptoms they’re experiencing. It’s sad to say this, but not all doctors have your loved ones best interest in mind. Persistence is key. I hope this “review” will be helpful & insightful to anyone out there currently going through a similar situation.

1 ShapeCreated with Sketch.thumb_up copy 5Created with Sketch.Report this postFill 3Created with Sketch. Condition: Chronic Heart Failure EffectivenessEase of UseSatisfaction

Have been on Metoprolol 50mg for 3 years for heart failure and my Heart Doctor just increased to 100mg. Have the cold toes, fingers, watering eyes, drowsiness, etc.

1 ShapeCreated with Sketch.thumb_up copy 5Created with Sketch.Report this postFill 3Created with Sketch. Condition: Paroxysmal Supraventricular Tachycardia EffectivenessEase of UseSatisfaction

Had 2 bouts of svt 2 years apart which lasted about 5 days each. Other than that, heart in great shape. Always been healthy and active. Took metoprolol after the 2nd bout and my life has never been the same. It’s been almost a year and a half since I took it. Can’t exercise, can’t handle any type of stress, ongoing palpitations, nightmares, blood pressure fluctuations, depression, hypersensitivity, chest pressure, short of breath. Poison. Don’t take.

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I had covid in March 2020; recovered in April. July was in the ER for heart palpitations. Long story short, diagnosed with myocarditis resulting in heart failure (47% EFR). Prescribed 25 mg to lower heart rate and blood pressure. By 3 months, experienced significant side effects: 1) cold fingers/toes, 2) pruney fingers (Raynaud’s symptoms), 3) unbearable dry cough, 4) hair loss, 5) decreased libido, 6) inability to lose weight (and very easy to gain weight), 7) anxiety/depression. I take this at night as it makes me incredibly sleepy. Definitely lowers heart rate (my sleeping HR is ~ 48 bpm). Blood pressure ~ 111/68, so that’s good, but I’m not sure if the side effects are worth the trade off, and will ask my dr. to reduce and/or stop taking, or switch to something else.

3 ShapeCreated with Sketch.thumb_up copy 5Created with Sketch.Report this postFill 3Created with Sketch. Condition: inappropriate sinus tachycardia EffectivenessEase of UseSatisfaction

This drug has been a life changer. For years had issues with sudden rapid heart beat and irregular heart beat. I also have high blood pressure and suffered from panic attacks. I was taking meds for both and had been given other drugs to help with the heartbeat but they didnt work or I had a reaction (constant coughing). I got put on the 50 mg Succulent ER 24-Hour when I had to go to the ER for chest pains in 2012. Within a month my blood pressure was within normal range and I no longer had to take Paxil for panic attacks (which I have not had one single attack since 2012 when I was put on this medication). Now I only take my Diovan and this drug and do not need the other two I had to take prior to starting this. The only drawback it you want to call it is you absolutely have to take this drug at the exact same time every day. If I miss my dose by even an hr I begin having heart palpations and my bp will go up to 180/110.

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Differences, similarities, and which is better

Drug overview & main differences | Conditions treated | Efficacy | Insurance coverage and cost comparison | Side effects | Drug interactions | Warnings | FAQ

If you have experienced a heart attack or currently live with high blood pressure, your doctor may prescribe you a drug like metoprolol tartrate (Lopressor) or metoprolol succinate (Toprol XL). Although both drugs contain identical active ingredients, they may be used in different ways.

Both metoprolol tartrate and metoprolol succinate belong to a class of drugs called beta blockers. They are sometimes also known as beta-1 selective adrenoceptor blockers and beta antagonists.

These drugs work by blocking the effects of hormones such as epinephrine and norepinephrine in the sympathetic nervous system. The sympathetic nervous system is responsible for the typical “fight-or-flight” response. Metoprolol can help reduce stress on the heart, relax blood vessels to decrease blood pressure, and alleviate chest pain.

What are the main differences between metoprolol tartrate and metoprolol succinate?

The main difference between metoprolol tartrate (What is metoprolol tartrate?)  and metoprolol succinate (What is metoprolol succinate?) is in their formulations. Metoprolol tartrate is the immediate-release version of metoprolol while metoprolol succinate is the extended-release version. This means that metoprolol succinate is released over time in the body leading to longer-acting effects.

Metoprolol tartrate may need to be taken multiple times per day. Metoprolol succinate can be taken once daily since it lasts longer than the tartrate form. Metoprolol succinate can also be used in children aged 6 years and older whereas metoprolol tartrate can only be used in adults.

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Conditions treated by metoprolol tartrate and metoprolol succinate

The tartrate and succinate forms of metoprolol are FDA-approved to treat high blood pressure (hypertension) and chest pain (angina pectoris).

Metoprolol tartrate is also FDA-approved as treatment right after a heart attack (acute myocardial infarction). Taking metoprolol tartrate after a heart attack may help reduce the risk of further cardiovascular events and death especially in those with coronary artery disease. Treatment should usually start within 3 to 10 days after the heart attack.

In addition to high blood pressure and chest pain, metoprolol succinate is also FDA-approved to treat congestive heart failure. More specifically, metoprolol succinate treats chronic heart failure that is New York Heart Association class II or III. Given as a daily dose, metoprolol succinate can improve outcomes and decrease the risk of mortality in heart failure patients.

Off-label uses for metoprolol include supraventricular tachycardia (abnormally fast heart rate) and thyroid storm (a dangerous condition that results from the overproduction of thyroid hormone). Other off-label uses may include treatment for abnormal heart rhythm (arrhythmia) and performance anxiety.

Is metoprolol tartrate or metoprolol succinate more effective?

Metoprolol tartrate and metoprolol succinate are both similar in effectiveness for treating high blood pressure and chronic chest pain. However, metoprolol tartrate may be more effective as a treatment for acute heart attacks while metoprolol succinate may be more effective as a treatment for chronic heart failure.

Clinical trials have shown that metoprolol tartrate is effective for high blood pressure and preventing adverse outcomes after a heart attack. On the contrary, studies including the Merit-HF trial have shown that metoprolol succinate is superior to metoprolol tartrate for chronic heart failure.

Metoprolol succinate can decrease recurring hospital visits and death from heart failure. However, carvedilol, another common beta blocker, might be even more effective than metoprolol succinate, according to a trial published in the Lancet.

Because metoprolol tartrate is taken multiple times throughout the day, drug levels in the body may not be as consistent. This could result in more side effects and less tolerability compared to the extended-release succinate form. One analysis found that side effects such as a slow heartbeat (bradycardia) may be more likely to occur with immediate-release metoprolol tartrate.

Coverage and cost comparison of metoprolol tartrate vs. metoprolol succinate

Metoprolol tartrate can be purchased as a generic prescription drug that is usually covered by Medicare and other insurance plans. Without insurance, the average cash price for generic metoprolol tartrate is around $5. SingleCare discount cards can be used at participating pharmacies to reduce the cost of this drug. You may find a price closer to $4 with a savings coupon.

Metoprolol succinate or extended-release metoprolol is available as generic medication that is covered by most Medicare and insurance plans. Generic metoprolol succinate is more likely to be covered than the brand name Toprol XL. The average retail price for generic Toprol XL is around $56. Check with your pharmacy to see if you can save more with a SingleCare savings card. If accepted, you can reduce the cost to $9.

Get the pharmacy discount card

Common side effects of metoprolol tartrate vs.

metoprolol succinate

Metoprolol tartrate and metoprolol succinate can cause similar side effects. The most common side effects of metoprolol include fatigue or tiredness, dizziness, depression, shortness of breath (dyspnea), and slow heartbeat (bradycardia). Other side effects include diarrhea, nausea, vomiting, and dry mouth.

Hypersensitivity reactions such as rash or itching may also occur when taking either form of metoprolol. Based on the FDA label, metoprolol tartrate may be more likely to cause certain side effects.

This may not be a complete list. Consult your doctor or pharmacist for possible side effects.

Source: DailyMed (metoprolol tartrate), DailyMed (metoprolol succinate)

Drug interactions of metoprolol tartrate vs. metoprolol succinate

Metoprolol tartrate and metoprolol succinate can interact with many of the same medications. Other drugs that have similar actions or affect the metabolism of beta blockers can interact with both forms of metoprolol.

Metoprolol should not be taken with catecholamine-depleting drugs. Taking these drugs together may increase the effects of beta blockers and cause adverse events such as low blood pressure (hypotension) and slow heartbeat (bradycardia). Other adverse effects may include dizziness and fainting.

Metoprolol is heavily processed by the CYP2D6 enzyme. Therefore, drugs that inhibit this enzyme can cause increased metoprolol levels in the body. Increased metoprolol levels can increase the risk of adverse effects.

Digoxin and drugs called calcium channel blockers may have additive effects when given with metoprolol. Taking any of these drugs with metoprolol can cause side effects in the heart.

This may not be a complete list of all possible drug interactions. Consult a doctor with all the medications you may be taking.

Warnings of metoprolol tartrate and metoprolol succinate

Both metoprolol tartrate and metoprolol succinate should not be discontinued abruptly.   If treatment with metoprolol is stopped abruptly, some people may experience a higher risk of heart attack, abnormal heart rhythm, and chest pain. The risk of these events is higher in those with underlying heart disease.

Beta blockers like metoprolol should not be used in anyone with the following conditions:

• Severe bradycardia
• Heart block greater than first degree
• Cardiogenic shock
• Decompensated heart failure
• Sick sinus syndrome without a pacemaker
• Hypersensitivity to any ingredients in these drugs

Consult a doctor to see if you may have any of these conditions before starting treatment.

Beta blockers can mask the signs and symptoms of hypoglycemia, or low blood sugar. Those with diabetes may need to monitor their blood sugar while taking beta blockers.

Frequently asked questions about metoprolol tartrate vs. metoprolol succinate

What is metoprolol tartrate?

Metoprolol tartrate is the generic name for Lopressor. It is a beta blocker used to treat high blood pressure and chronic chest pain. It is also approved for the treatment of an acute heart attack to lower the risk of mortality.

What is metoprolol succinate?

Metoprolol succinate is also known by the brand name Toprol XL. It is the extended-release form of metoprolol. Metoprolol succinate is approved to treat high blood pressure, chronic chest pain, and congestive heart failure.

Are metoprolol tartrate and metoprolol succinate the same?

No. Metoprolol tartrate is an immediate-release tablet while metoprolol succinate is an extended-release tablet. They may be used in different ways.

Is metoprolol tartrate or metoprolol succinate better?

Metoprolol tartrate and metoprolol succinate are both effective depending on the condition being treated. Metoprolol succinate is more effective for treating heart failure. Metoprolol succinate may also be less likely to cause some side effects.

Can I use metoprolol tartrate or metoprolol succinate while pregnant?

Metoprolol should only be used during pregnancy if the benefits clearly outweigh the risks. Not enough studies have been done to show that these medications are 100% safe during pregnancy. Consult a doctor if you are pregnant or breastfeeding.

Can I use metoprolol tartrate or metoprolol succinate with alcohol?

Drinking alcohol while taking metoprolol may increase the risk of drowsiness and dizziness. It is not generally recommended to use metoprolol with alcohol.

Can you switch from metoprolol tartrate to succinate?

In some cases, metoprolol tartrate may be switched to metoprolol succinate. Metoprolol succinate may be preferred for its once-daily dosing. Consult a doctor to determine your treatment options when switching medications.

When should you not take metoprolol?

Metoprolol should not be taken if you experience very low heart rates, low blood pressure, or severe heart failure. It is important to discuss your medical history with a doctor to determine if you should be on metoprolol.

What should I avoid while taking metoprolol?

Alcohol and certain medications should be avoided while taking metoprolol. Some medications including calcium channel blockers, certain antidepressants, and those processed in a similar way as metoprolol may increase the risk of adverse effects with metoprolol.

Is metoprolol a high-risk medication?

Yes. Metoprolol may be considered a high-risk medication. When used improperly, metoprolol can cause significant harm.

Metoprolol – a beta-blocker – Lopresor for high blood pressure

About metoprolol

Metoprolol belongs to the group of medicines known as beta-blockers. It is a medicine which is used to treat several different medical conditions. It works on the heart and blood vessels.

Metoprolol slows down the activity of your heart by stopping messages sent by some nerves to your heart. It does this by blocking tiny areas (called beta-adrenergic receptors) where the messages are received by your heart. As a result, your heart beats more slowly and with less force. This allows the pressure of blood within your blood vessels to be reduced if you have high blood pressure (hypertension), and helps to prevent abnormally fast heart rhythms (arrhythmias). Because your heart is using less energy, this helps to reduce chest pain if you have angina. Metoprolol can also help to protect the heart following a heart attack.

Metoprolol is also prescribed to help ease some of the symptoms of an overactive thyroid gland, such as a fast heartbeat and trembling. It relieves these symptoms quickly, which allows time for other antithyroid treatments to take effect. Metoprolol is also prescribed to help prevent migraines. It can be helpful for people who find other treatments for migraine unsuitable.

Before taking metoprolol

Some medicines are not suitable for people with certain conditions, and sometimes a medicine may only be used if extra care is taken. For these reasons, before you start taking metoprolol it is important that your doctor or pharmacist knows:

• If you are pregnant, trying for a baby or breastfeeding.
• If you have asthma or any other breathing disorder.
• If you have any problems with the way your liver works.
• If you have low blood pressure or poor circulation.
• If you have high blood sugar levels (diabetes mellitus).
• If you have a skin problem called psoriasis.
• If you have a condition causing muscle weakness, called myasthenia gravis.
• If you have been told you have a slow heartbeat or heart block (a slow and irregular heartbeat).
• If you have been told you have chest pain called Prinzmetal’s angina (caused by spasms of your heart’s blood vessels).
• If you are taking any other medicines. This includes any medicines you are taking which are available to buy without a prescription, as well as herbal and complementary medicines.
• If you have ever had an allergic reaction to a medicine, or if you have ever had any other serious allergic reaction.

How to take metoprolol

• Before you start the treatment, read the manufacturer’s printed information leaflet from inside the pack. It will give you more information about metoprolol and will provide you with a full list of the side-effects which you may experience from taking it.
• Your doctor will tell you what dose is right for you, and this information will be printed on the label of the pack of tablets to remind you. Take metoprolol exactly as your doctor tells you to. You may be prescribed one, two, three or four doses to take each day, depending upon your medical condition. Try to take your doses at the same times of day each day, as this will help you to remember to take the tablets regularly. It is recommended that you take your doses before meals.
• If you forget to take a dose, take it as soon as you remember unless your next dose is due. If your next dose is due then take the tablet which is due but leave out the forgotten one. Do not take two doses together to make up for missing one.

Getting the most from your treatment

• Try to keep your regular appointments with your doctor. This is so your doctor can check on your progress.
• Treatment with metoprolol can often be long-term. Continue to take the tablets unless your doctor tells you to stop. Stopping treatment suddenly can cause problems in some people, so your doctor may want you to reduce your dose gradually if this becomes necessary.
• If you are due to have an operation or dental treatment, it is important to tell the person carrying out the treatment that you are taking a beta-blocker. This is because some anaesthetics may increase the risk of unwanted effects.
• If you drink alcohol, ask your doctor for advice about taking metoprolol and alcohol. Alcohol will add to the blood pressure-lowering effect of metoprolol and so may not be recommended for you.
• If you buy any medicines, check with a pharmacist that they are suitable for you to take. Some medicines (including some cough, cold and flu remedies) may not be.
• Your doctor may give you dietary and lifestyle advice about eating a healthy diet, not smoking, and taking regular exercise. If so, it is important that you follow the advice you are given.
• If you have diabetes, metoprolol can block the symptoms of low blood sugar. Your doctor will advise you about this.

Can metoprolol cause problems?

Along with their useful effects, most medicines can cause unwanted side-effects although not everyone experiences them. The table below contains some of the most common ones associated with metoprolol. You will find a full list in the manufacturer’s information leaflet supplied with your medicine. The unwanted effects often improve as your body adjusts to the new medicine, but speak with your doctor or pharmacist if any of the following continue or become troublesome.

If you experience any other symptoms which you think may be due to the medicine, speak with your doctor or pharmacist for further advice.

How to store metoprolol

• Keep all medicines out of the reach and sight of children.
• Store in a cool, dry place, away from direct heat and light.

Important information about all medicines

Blockers | Texas Heart Institute

Beta-blockers are used to treat high blood pressure (hypertension), congestive heart failure (CHF),abnormal heart rhythms (arrhythmias), and chest pain (angina). Beta-blockers are sometimes used in heart attack patients to prevent future heart attacks.

How do beta-blockers work?

• Beta-blockers “block” the effects of adrenaline on your body’s beta receptors. This slows the nerve impulses that travel through the heart. As a result, your heart does not have to work as hard because it needs less blood and oxygen. Beta-blockers also block the impulses that can cause an arrhythmia.
• Your body has 2 main beta receptors: beta 1 and beta 2.
• Some beta-blockers are selective, which means that they block beta 1 receptors more than they block beta 2 receptors. Beta 1 receptors are responsible for heart rate and the strength of your heartbeat.
• Nonselective beta-blockers block both beta 1 and beta 2 receptors. Beta 2 receptors are responsible for the function of your smooth muscles (muscles that control body functions but that you do not have control over).

How much do I take?

There are many different kinds of beta-blockers. The amount of medicine that you need to take may vary. Talk to your doctor or pharmacist for more information about how and when to take this medicine.

What if I am taking other medicines?

Other medicines that you may be taking can increase or decrease the effect of beta-blockers. These effects are called an interaction. Be sure to tell your doctor about every medicine and vitamin or herbal supplement that you are taking, so he or she can make you aware of any interactions.

The following are categories of medicines that can increase or decrease the effects of beta-blockers. Because there are so many kinds of medicines within each category, not every type of medicine is listed by name. Tell your doctor about every medicine that you are taking, even if it is not listed below.

• Other medicines used to treat high blood pressure. These other medicines may increase the effect of beta-blockers.
• Certain anti-depressants.
• Allergy shots.
• Medicines to treat diabetes, including oral medicines (pills that you swallow) and insulin.
• Medicines to treat asthma, chronic bronchitis, emphysema, or COPD.

While on beta-blockers, you should also avoid eating or drinking products that have caffeine or taking over-the-counter cough and cold medicines, antihistamines, and antacids that contain aluminum. You should also avoid drinking alcohol, because it can decrease the effects of beta-blockers.

What else should I tell my doctor?

Talk to your doctor about your medical history before you start taking beta-blockers. The risks of taking the medicine need to be weighed against its benefits. Here are some things to consider if you and your doctor are deciding whether you should take a beta-blocker.

• You have allergies to foods or dyes. Beta-blockers may make your allergic reactions worse.
• You are thinking of becoming pregnant, you are pregnant, or you are breast-feeding your baby.
• You are over 60. Younger people tend to have fewer problems while taking beta-blockers.
• You have heart disease or poor circulation to your hands or feet.
• You have a slow heart rate (bradycardia) or heart block.
• You have asthma. Beta-blockers may make your condition worse.
• You have hay fever symptoms, chronic bronchitis, emphysema, or COPD.
• You have diabetes or hypoglycemia. Beta-blockers may hide the symptoms of low blood sugar.
• You have an overactive thyroid.
• You have kidney or liver disease.

What are the side effects?

Sometimes a medicine causes unwanted effects. These are called side effects. Not all of the side effects for beta-blockers are listed here. If you feel these or any other effects, you should check with your doctor.

Common side effects:

• Drowsiness or fatigue.
• Cold hands and feet.
• Weakness or dizziness.
• Dry mouth, eyes, and skin.

Less common side effects:

• Wheezing, trouble breathing, or shortness of breath.
• Slow heartbeat.
• Trouble sleeping or vivid dreams while asleep.
• Swelling of the hands and feet.

Rare side effects:

• Abdominal cramps.
• Throwing up.
• Diarrhea.
• Constipation.
• Back or joint pain.
• Skin rash.
• Sore throat.
• Depression.
• Memory loss, confusion, or hallucinations.
• Impotence.

Again, tell your doctor right away if you have any of these side effects. Do not stop taking your medicine unless your doctor tells you to. If you stop taking your medicine without checking with your doctor, it can make your condition worse.

Safemedication.com

Your Good Health: Metoprolol can lower heart rate excessively

Dear Dr. Roach: My husband has been on metoprolol for about eight years. He was prescribed that medication right after he had a stent put in due to a clogged heart vessel. He is doing very well. His recent stress test was normal. The metoprolol took his heart rate down to a pulse of between 55 and 60 shortly after he started it. He is an active 79-year-old and in good shape. But he was told years ago, when the metoprolol lowered his pulse, that he may eventually need a pacemaker.

If the metoprolol is giving him a lower heart rate, causing a future need for a pacemaker, I would think the cardiologist would just give him a different blood pressure prescription that doesn’t lower the heart rate. He does not want a pacemaker due to a medication side-effect. Do you think a replacement for the metoprolol would keep his pulse in the normal range and dismiss the thought of a future pacemaker?

N.F.

Metoprolol — commonly used in patients with coronary artery blockages — is a beta blocker, and it works mainly by slowing the heart rate down and by decreasing how hard it contracts. Beta blockers reduce the risk of further heart attacks and death in people with coronary artery disease, and they should be given to most people with coronary artery disease unless there is a good reason not to. They also may act to reduce rhythm disturbances by counteracting adrenaline in the blood.

A heart rate of 55-60 is not unusual in people taking metoprolol. However, if a person had a heart rate that slow without a beta blocker, a doctor would be concerned that they would eventually develop symptoms from that slow of a heart rate. Symptomatic slow heart rate (“bradycardia,” from the Greek roots) is a clear indication for a permanent pacemaker, and extreme bradycardia (below 40) gets most cardiologists concerned enough to start thinking about a pacemaker even without symptoms.

In your husband’s case, if his heart rate were to prove too slow, his cardiologist would likely reduce the dose of the metoprolol, or even switch it out for a different drug.

Dear Dr. Roach: I am an 86-year-old man in pretty good health. I ran my entire life, including 10K and 10-mile races until my left hip was replaced three times. Is there any documented health benefit from taking 250 steps per hour (that’s the minimum on my smartwatch) daily? I am no longer doing duration exercises such as walking.

D.M.

Any exercise is better than none. If you are taking 250 steps for every hour you’re awake, that’s 4,000 steps per day, which is a lot better than some other people get. You don’t need 10,000 steps a day to get benefit.

The running and other exercises you did have been part of the reason you have enjoyed mostly good health until age 86.

Dr. Roach regrets that he is unable to answer individual letters, but will incorporate them in the column whenever possible. Readers can email questions to [email protected]

© Copyright Times Colonist

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Arpimed

Symptoms : severe arterial 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 in 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 overdosed with 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 impaired peripheral arterial circulation 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 may 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 90 100
• medicines used to treat irregular heart rhythms such as amiodarone and propafenone 90 100
• drugs used to treat depression such as tricyclic antidepressants or SSRIs
• drugs used to treat epilepsy, such as barbiturates
• drugs for the treatment of mental illness, such as phenothiazines 90 100
• anesthetics such as cyclopropane or trichlorethylene 90 100
• drugs used to treat certain cancers, in particular kidney cancer, such as aldesleukin 90 100
• drugs used to treat erectile dysfunction, such as alprostadil
• anxiolytics or hypnotics (eg temazepam, nitrazepam, diazepam),
• indomethacin or celecoxib (NSAID) 90 100
• rifampicin (antibiotic) or terbinafine (antifungal) 90 100
• Estrogens, such as contraceptives or hormone replacement therapy 90 100
• corticosteroids (eg, hydrocortisone, prednisolone) 90 100
• other beta blockers, e. g. eye drops 90 100
• epinephrine (epinephrine) or norepinephrine (norepinephrine), used for anaphylactic shock or other sympathomimetics – drugs used to treat diabetes 90 100
• lidocaine (local anesthetic)
• moxysilite (used for Raynaud’s syndrome) 90 100
• medicines used in the treatment of malaria, such as mefloquine 90 100
• medicines used to prevent nausea and vomiting, such as tropisetron – medicines used to treat bronchial asthma, such as xanthines, such as aminphylline or theophylline 90 100
• medicines used to treat migraines, such as ergotamine 90 100
• drugs used to treat heart problems, such as cardiac glycosides, such as digoxin
• medicines used to treat rheumatoid arthritis, such as hydroxychloroquine 90 100
• 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 90 155 0 90 156 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.

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Composition

Per one tablet:

active substance: metoprolol tartrate – 25.0 mg,

excipients : lactose monohydrate (milk sugar) – 180.0 mg, microcrystalline cellulose – 62.0 mg, croscarmellose sodium – 16.0 mg, sodium carboxymethyl starch 12.0 mg, povidone (polyvinylpyrrolidone) – 16.0 mg, magnesium stearate – 8.0 mg, colloidal silicon dioxide – 6.0 mg.

Dosage form

Tablets.

Description

Tablets, white or white with a grayish shade, round, flat, with a notch on one side and bevel on both sides.

Action

beta1-adrenergic blocker selective

Pharmacodynamics

Cardioselective blocker-adrenergic receptors, has a slight membrane-stabilizing effect and has no intrinsic sympathomimetic activity.

Has antihypertensive, antianginal and antiarrhythmic effects.Blocking in low doses beta1-adrenergic receptors of the heart, reduces the formation of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP) stimulated by catecholamines, reduces the intracellular flow of calcium ions (Ca ²⁺ ), has a negative chrono-, dromo-, batmo- and inotropic effect (reduces the heart rate (HR), inhibits conduction and excitability, reduces myocardial contractility).

The total peripheral vascular resistance at the beginning of the use of beta-blockers (in the first 24 hours after oral administration) increases (as a result of a reciprocal increase in the activity of alpha-adrenergic receptors and elimination of beta stimulation ₂ -adrenergic receptors), which returns to initial, and with a long value – decreases.

The antihypertensive effect is due to a decrease in cardiac output and renin synthesis, inhibition of the activity of the renin-angiotensin-aldosterone system (RAAS) (is of great importance in patients with initial hypersecretion of renin) and the central nervous system, restoration of the arc of the baroreceportic sensitivity ( there is an increase in their activity in response to a decrease in blood pressure) and, as a result, a decrease in peripheral sympathetic influences.Reduces high blood pressure (BP) at rest, during physical exertion and stress.

Antianginal effect is determined by a decrease in myocardial oxygen demand as a result of a decrease in heart rate (lengthening of diastole and improvement of myocardial perfusion) and contractility, as well as a decrease in myocardial sensitivity to the effects of sympathetic innervation. Reduces the number and severity of angina attacks and increases exercise tolerance.

Blood pressure decreases after 15 minutes, maximum – after 2 hours and lasts for 6 hours, diastolic blood pressure changes more slowly: a stable decrease is observed after several weeks of regular intake.

The antiarrhythmic effect is due to the elimination of arrhythmogenic factors (tachycardia, increased activity of the sympathetic nervous system, increased cAMP content, arterial hypertension), a decrease in the rate of spontaneous excitation of sinus and ectopic pacemakers and a slowdown of atrioventricular degree, in retrograde directions through the AV node) and along additional paths.With supraventricular tachycardia, atrial fibrillation, sinus tachycardia in functional heart disease and hyperthyroidism, it slows down the heart rate, or even can lead to the restoration of sinus rhythm.

Prevents the development of migraine.

When used in moderate therapeutic doses, in contrast to non-selective beta-blockers, it has a less pronounced effect on organs containing beta ₂ – adrenergic receptors (pancreas, skeletal muscles, smooth muscles of peripheral arteries, bronchi and uterus) and on carbohydrate exchange.

When taken for many years, it reduces the concentration of cholesterol in the blood.

When used in high doses (more than 100 mg / day), it has a blocking effect on both subtypes of beta-adrenergic receptors.

Pharmacokinetics

Absorption

When taken orally, metoprolol is almost completely absorbed (about 95%) from the gastrointestinal tract. Food intake increases bioavailability by 20-40%. Undergoes intensive first-pass metabolism, so the systemic bioavailability is about 35%.The maximum concentration in blood plasma is reached 1.5-2 hours after ingestion.

Distribution

Bond with blood plasma proteins 12%. The volume of distribution is 5.6 l / kg. Penetrates the blood-brain and placental barrier. Excreted in breast milk in small amounts.

Metabolism

Metoprolol is almost completely metabolized in the liver, mainly with the participation of the isoenzyme CYP2D6.The half-life is from 3 to 4 hours, but in patients with a slow metabolism it can increase to 7-8 hours. The metabolites o-desmethylmetoprolol and a-hydroxymetoprolol have weak beta-adrenergic blocking activity.

Excretion

Excreted mainly by the kidneys (about 95%), about 10% is excreted unchanged. Not excreted during hemodialysis.

In patients with liver cirrhosis and portocaval anastomosis bioavailability increases and clearance decreases.In patients with portocaval anastomosis, the AUC (area under the concentration-time curve) may increase 6-fold, and the clearance may decrease to 0.3 ml / min.

Indications for use

– Arterial hypertension (in monotherapy or in combination with other antihypertensive drugs),

– functional cardiac disorders accompanied by tachycardia,

– ischemic heart disease: myocardial infarction (secondary prevention – complex therapy), prevention of angina attacks,

– heart rhythm disturbances (supraventricular tachycardia, ventricular extrasystole),

– hyperthyroidism (complex therapy),

– prevention of migraine attacks.

Contraindications

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, pronounced decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, cardiac arrest, in acute atrophy blockade (up to the development of complete transverse blockade and cardiac arrest), cardialgia, hypoglycemia, hyperkalemia, convulsions, respiratory arrest.

The first signs of an overdose appear 20 minutes to 2 hours after taking the drug.In case of an overdose or a threatening decrease in heart rate and / or blood pressure, treatment with Metoprolol should be discontinued immediately.

Treatment : gastric lavage and prescribing adsorbing agents, symptomatic therapy: with a pronounced decrease in blood pressure – the patient should be in the Trendelenburg position, in case of an excessive decrease in blood pressure, bradycardia and heart failure – IV, with an interval of 2-5 minutes, beta-adrenomimetics – until the desired effect is achieved or intravenous 0.5-2 mg of atropine.In the absence of a positive effect, dopamine, dobutamine, or norepinephrine (norepinephrine).

As a follow-up, possibly an artificial pacemaker. In case of bronchospasm, intravenous beta ₂ -adrenomimetics should be administered. Metoprolol is poorly excreted by hemodialysis.

Use during pregnancy and lactation

During pregnancy, Metoprolol is prescribed only according to strict indications if the intended benefit to the mother outweighs the potential risk to the fetus (due to the possible development of bradycardia, arterial hypotension, hypoglycemia in the fetus).Beta-blockers reduce the permeability of the placenta, which can lead to premature birth or intrauterine fetal death.

The risk of complications from the heart and lungs increases in the postpartum period in those newborns whose mothers received metoprolol. The drug should be discontinued 48-72 hours before delivery. In cases where this is not possible, it is necessary to ensure strict observation of newborns within 48-72 hours after birth.

Metoprolol is excreted in breast milk.Children who are breastfed should be under medical supervision in connection with the possible development of symptoms of beta-adrenergic receptor blockade.

If it is necessary to use the drug Metoprolol, breastfeeding is recommended to be canceled.

Side effects

The incidence of side effects is classified according to the recommendations of the World Health Organization: very often – not less than 10%, often – not less than 1%, but less than 10%, infrequently – not less than 0.1%, but less than 1% , rarely – not less than 0.01%, but less than 0.1%, very rarely – less than 0.01%.

From the hematopoietic system : very rarely – thrombocytopenia, leukopenia.

From the side of the cardiovascular system : often – sinus bradycardia, postural disorders (very rarely accompanied by fainting), cold extremities, palpitations, infrequently – a temporary increase in symptoms of heart failure, atrioventricular block of the I degree, cardiogenic shock with acute myocardial infarction, peripheral edema, pain in the heart, rarely – other myocardial conduction disorders, arrhythmia, very rarely – gangrene in patients with previous severe peripheral circulatory disorders.

From the nervous system : very often – increased fatigue, often – headache, dizziness, infrequently – paresthesia, convulsions, depression, decreased concentration, drowsiness or insomnia, nightmares, rarely – increased nervous irritability , anxiety, impotence / sexual dysfunction, Peyronie’s disease, very rarely – amnesia / memory impairment, depression, hallucinations.

From the senses : rarely – visual impairment, dryness and / or irritation of the eyes, conjunctivitis, hearing impairment and tinnitus.

From the digestive system : often – nausea, abdominal pain, diarrhea, constipation, infrequently – vomiting, rarely – dryness of the oral mucosa, very rarely – a violation of taste.

From the liver : rarely – liver dysfunction, increased activity of hepatic transaminases, very rarely – hepatitis.

From the side of the skin : infrequently – urticaria, increased sweating, rarely – alopecia, very rarely – photosensitivity, exacerbation of psoriasis.

From the respiratory system : often – shortness of breath with physical exertion, infrequently – bronchospasm, rarely – rhinitis.

From the endocrine system : rarely – hypo-, hyperglycemia in patients with type 1 diabetes mellitus, masking the symptoms of thyrotoxicosis.

From the side of the musculoskeletal system : very rarely – arthralgia.

From the side of metabolism : infrequently – an increase in body weight, rarely – an aggravation of the course of latent diabetes mellitus.

Laboratory indicators : very rarely – a decrease in the concentration of high-density cholesterol and an increase in triglycerides in the blood plasma.

Interaction

Simultaneous use with monoamine oxidase (MAO) inhibitors is not recommended due to a significant increase in the antihypertensive effect. The break in treatment between taking MAO inhibitors and metoprolol should be at least 14 days.

Beta-adrenostimulants, theophylline, cocaine, estrogens (sodium retention), indomethacin and other non-steroidal anti-inflammatory drugs (sodium retention and blocking of prostaglandin synthesis by the kidneys) weaken the antihypertensive effect of metoprolol.

With simultaneous use with hypoglycemic agents for oral administration, a decrease in their effect is possible, with insulin – an increase in the risk of hypoglycemia, an increase in its severity and duration, masking of some symptoms of hypoglycemia (tachycardia / increased sweating, increased blood pressure).

With simultaneous use with antihypertensive drugs, diuretics, angiotensin-converting enzyme inhibitors, nitroglycerin or slow calcium channel blockers, a sharp decrease in blood pressure may develop (special caution is needed when combined with prazosin), the risk of bradycardia in combination with mefloquine and bradycardia increases when combined with epinephrine, a pronounced decrease in heart rate and inhibition of atrioventricular conduction up to complete blockade – when using metoprolol with verapamil, diltiazem, reserpine, methyldopa, clonidine, guanfacine and cardiac glycosides, agents for general anesthesia and cardiodepression.

Simultaneous intravenous administration of verapamil can cause cardiac arrest.

Medicines that induce or inhibit the isoenzyme CYP2D6 may affect the concentration of metoprolol in blood plasma. The concentration of metoprolol in blood plasma may increase when taken simultaneously with other drugs that are a substrate for the CYP2D6 isoenzyme, for example, antiarrhythmic drugs, antihistamines, antagonists of H ₂ -receptors, antidepressants (selective inhibitors of the reuptake of paroxetonin, for example sertraline), antipsychotics and cyclooxygenase-2 inhibitors.

Class I antiarrhythmic drugs can lead to the summation of a negative inotropic effect with the development of pronounced hemodynamic side effects in patients with impaired left ventricular function (this combination should be avoided in patients with sick sinus syndrome and atrioventricular conduction disorder).

Quinidine inhibits the metabolism of metoprolol in patients with rapid metabolism, leading to a significant increase in the concentration of metoprolol in blood plasma and an increase in its beta-adrenergic blocking action.

The combination with amiodarone increases the risk of developing severe sinus bradycardia (including long after the withdrawal of amiodarone, due to its long half-life).

If metoprolol and clonidine are taken simultaneously, then when metoprolol is discontinued, clonidine is discontinued after a few days (due to the risk of a withdrawal syndrome).

Inductors of microsomal liver enzymes (rifampicin, barbiturates) lead to an increase in the metabolism of metoprolol, to a decrease in the concentration of metoprolol in blood plasma and a decrease in the effect.Inhibitors (cimetidine, oral contraceptives, phenothiazines) – increase the concentration of metoprolol in blood plasma.

Diphenhydramine reduces the clearance of metoprolol, increasing its effect.

Simultaneous use with high doses of phenylpropanolamine can lead to a paradoxical increase in blood pressure (up to a hypertensive crisis).

Allergens used for immunotherapy, or extracts of allergens for skin tests, when used together with metoprolol, increase the risk of systemic allergic reactions or anaphylaxis, iodine-containing radiopaque substances for intravenous administration increase the risk of developing anaphylactic reactions.

Reduces the clearance of xanthines (except diphylline), especially in patients with an initially increased clearance of theophylline under the influence of smoking.

Reduces the clearance of lidocaine, increases the concentration of lidocaine in the blood plasma.

Strengthens and prolongs the effect of antidepolarizing, muscle relaxants, lengthens the anticoagulant effect of coumarins.

When combined with anxiolytics and drugs with hypnotic activity, the antihypertensive effect increases, with ethanol the risk of a pronounced decrease in blood pressure increases and the inhibitory effect on the central nervous system increases.

There is an increase in the risk of peripheral circulatory disorders – with ergot alkaloids.

Dosage and administration

The drug Metoprolol should be taken orally, during or immediately after a meal, the tablets can be divided in half (but not chewed) and washed down with liquid.

Arterial hypertension:

The initial daily dose is 50-100 mg in 1-2 doses (morning and evening) (1/2 tablet of 100 mg – 1 tablet).If the therapeutic effect is insufficient, the daily dose can be increased to 100-200 mg, or other antihypertensive drugs are additionally used. The maximum daily dose is 200 mg.

For arrhythmia, for the prevention of angina and migraine attacks:

100-200 mg per day in two doses (morning and evening).

Secondary prevention of myocardial infarction:

200 mg per day in two divided doses (morning and evening).

Functional disorders of cardiac activity, accompanied by tachycardia:

100 mg per day in two divided doses (morning and evening).

With hyperthyroidism – 150-200 mg per day in 2 divided doses (morning and evening).

Elderly patients are recommended to start treatment with 50 mg (1/2 100 mg tablet) per day.

In case of impaired renal function dose adjustment is not required.

In hepatic impairment , dose adjustment may be required depending on the clinical condition of the patient.

If it becomes necessary to interrupt or discontinue treatment with Metoprolol after prolonged therapy, the dosage of the drug should be gradually reduced by 2 times for at least 2 weeks.

When withdrawal occurs, dose reduction should be slower. Abrupt discontinuation of the drug can cause myocardial ischemia and can lead to an exacerbation of angina pectoris or myocardial infarction, as well as increase arterial hypertension.

Overdose

Symptoms: severe sinus bradycardia, dizziness, nausea, vomiting, cyanosis, marked decrease in blood pressure, arrhythmia, ventricular extrasystole, bronchospasm, fainting, at acute overdose blockade (up to the development of complete transverse blockade and cardiac arrest), cardialgia, hypoglycemia, hyperkalemia, convulsions, respiratory arrest.

The first signs of an overdose appear 20 minutes to 2 hours after taking the drug. In case of an overdose or a threatening decrease in heart rate and / or blood pressure, treatment with Metoprolol should be discontinued immediately.

Treatment : gastric lavage and prescribing adsorbing agents, symptomatic therapy: with a pronounced decrease in blood pressure – the patient should be in the Trendelenburg position, in case of an excessive decrease in blood pressure, bradycardia and heart failure – IV, with an interval of 2-5 minutes, beta-adrenomimetics – until the desired effect is achieved or intravenous 0.5-2 mg of atropine.In the absence of a positive effect, dopamine, dobutamine, or norepinephrine (norepinephrine).

As a follow-up, possibly an artificial pacemaker. In case of bronchospasm, intravenous beta ₂ -adrenomimetics should be administered. Metoprolol is poorly excreted by hemodialysis.

Special instructions

Patients taking beta-blockers should not be given intravenous blockers of slow calcium channels such as verapamil.

Monitoring the condition of patients taking beta-blockers includes regular monitoring of the heart rate (HR) and blood pressure, blood glucose concentration in patients with diabetes mellitus.

If necessary, for patients with diabetes mellitus, the dose of insulin or hypoglycemic agents administered by mouth should be selected individually.

The patient should be taught how to calculate the heart rate and instruct on the need for medical advice if the heart rate is less than 50 beats / min.

When taking a dose above 200 mg per day, cardioselectivity decreases.

In heart failure treatment with Metoprolol is started only after reaching the stage of compensation.

Patients with Prinzmetal angina are not recommended to prescribe non-selective beta-blockers.

Possible increased severity of hypersensitivity reactions (against the background of a burdened allergic history) and the lack of effect from the introduction of conventional doses of epinephrine (adrenaline).

In patients taking beta-blockers, anaphylactic shock is more severe.

May exacerbate symptoms of impaired peripheral arterial circulation.

Cancellation of the drug is carried out gradually, reducing the dose within 14 days. With an abrupt termination of treatment, a withdrawal syndrome may occur (increased angina attacks, increased blood pressure). When discontinuing the drug, special attention should be paid to patients with angina pectoris.

With exertional angina, the selected dose of the drug should provide a heart rate at rest within 55-60 beats / min, with a load – no more than 110 beats / min.

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

Metoprolol can mask some of the clinical manifestations of hyperthyroidism (eg, tachycardia). Abrupt withdrawal in patients with thyrotoxicosis is contraindicated, since it can aggravate the symptoms.

In diabetes mellitus, it can mask tachycardia caused by hypoglycemia. Unlike non-selective beta-blockers, it practically does not increase insulin-induced hypoglycemia and does not delay the restoration of blood glucose concentration to normal levels.

If necessary, the appointment of patients with bronchial asthma as concomitant therapy should be prescribed beta therapy _2- adrenomimetic.It is necessary to prescribe the minimum effective dose of metoprolol, and an increase in the dose of beta ₂ -adrenomimetic may be required.

Patients with pheochromocytoma, in parallel with the drug Metoprolol, should be prescribed an alpha-blocker.

If it is necessary to carry out a surgical intervention, it is necessary to warn the anesthesiologist about the therapy (the choice of a means for general anesthesia with a minimal negative inotropic effect), drug withdrawal is not recommended.

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.

Drugs that reduce the supply of catecholamines (for example, reserpine) can increase the effect of beta-blockers, therefore, patients taking such combinations of drugs should be under constant medical supervision for detecting excessive lowering of blood pressure or bradycardia.

In elderly patients, it is recommended to regularly monitor liver function.

Correction of the dosage regimen is required only if elderly patients develop bradycardia (less than 50 beats / min), a pronounced decrease in blood pressure (systolic blood pressure below 100 mm Hg), atrioventricular blockade, bronchospasm, ventricular arrhythmias, severe disorders liver function. Sometimes it is necessary to stop treatment.

Monitoring is recommended for patients with severe renal impairment.

Special monitoring of the condition of patients with depressive disorders taking Metoprolol should be carried out, in case of the development of depression caused by taking beta-blockers, it is recommended to discontinue therapy.

Influence on the ability to drive vehicles and control mechanisms

During the period of therapy, 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.

Release form

Tablets, 25 mg.

Conditions for dispensing from pharmacies

By prescription

Storage conditions

In a dry, dark place, at a temperature not exceeding 25 C.

Keep out of reach of children.

Shelf life

3 years. Do not use after the expiration date.

Manufacturer and organization accepting consumer claims

OZON LLC

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, 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.

METOPROLOL MV (Belarus) | JLLC “Lekpharm”

Metoprolol is a CYP2D6 substrate, therefore, drugs that inhibit CYP2D6 (quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine) can affect the plasma concentration of metoprolol.

Combined use of Metoprolol MB with the following drugs should be avoided:

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

Propafenone: when propafenone was prescribed to four patients treated with metoprolol, the plasma concentration of metoprolol was increased by 2-5 times, while in two patients there were side effects characteristic of metoprolol.This interaction was confirmed in a study on 8 volunteers. Probably, the interaction is due to the inhibition of metoprolol metabolism by propafenone, like quinidine, 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 : a 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 the drug Metoprolol MV with the following drugs may require dose adjustment:

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.

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 AV conduction disturbance. Interaction is described using disopyramide as an example.

Non-steroidal anti-inflammatory drugs (NSAIDs) : NSAIDs weaken the antihypertensive effect of β-blockers.This interaction has been documented for indomethacin. Probably, the described interaction will not be observed when interacting with sulindak. Negative interactions have been noted in studies with diclofenac.

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.

Diltiazem : Diltiazem and β-blockers mutually enhance the inhibitory effect on AV conduction and sinus node function.When metoprolol is combined with diltiazem, cases of severe bradycardia have been reported.

Epinephrine : 10 cases of severe arterial hypertension and bradycardia have been reported in patients taking nonselective β-blockers (including pindolol and propranolol) and receiving epinephrine. Interaction was also noted in a group of healthy volunteers. 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 to pathological values ​​in healthy volunteers. 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.Several cases of hypertensive crisis have been reported while taking phenylpropanolamine.

Quinidine : Quinidine inhibits the metabolism of metoprolol in a special group of patients with rapid hydroxylation, mainly causing a significant increase in the plasma concentration of metoprolol and increased β-blockade. It is believed that a similar interaction is typical for other β-blockers, in the metabolism of which cytochrome P4502D6 is involved.

Clonidine : Hypertensive reactions with abrupt withdrawal of clonidine can be intensified with the combined use 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 may increase the metabolism of metoprolol by decreasing the plasma concentration of metoprolol.

Patients concurrently taking metoprolol and other β-blockers (eye drops) or monoamine oxidase inhibitors (MAO) should be closely monitored. While taking β-blockers, inhalation anesthetics increase the cardiodepressant effect.While taking β-blockers, patients receiving hypoglycemic agents for oral administration may need to adjust the dose of the latter.

Plasma concentration of metoprolol can be increased when taking cimetidine or hydralazine.

Cardiac glycosides, when used together with β-blockers, can increase the time of atrioventricular conduction and cause bradycardia.

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