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Most popular brand: Toprol
Active ingredient: Metoprolol
Available dosage forms: 25, 50, 100 mg

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What is Metoprolol?

Metoprolol is a beta-blocker. It works by relaxing the blood vessels and reducing the heart rate. The end result is improved blood flow and lower blood pressure.

Metoprolol is a classic beta blocker. It shields the heart and circulation from the effects of the stress hormone adrenaline. Metoprolol lowers blood pressure, the heart rate, the heartbeat volume and the conduction velocity. Since the active ingredient also protects the heart, it is not only prescribed for the treatment of high blood pressure. The beta blocker metoprolol is also used after a heart attack, to prevent heart attacks from happening again, to treat tachycardiac arrhythmias (palpitations), heart failure (heart failure) or coronary artery disease. In addition, metoprolol is also used to prevent migraine attacks.

Metoprolol, sold under the brand name Toprol-XL among others, is a medication used to treat high blood pressure, chest pain, heart problems, and a heart arrhythmia. In the US it is available only by prescription. It is taken by mouth, injection into a muscle, or under the skin. There is evidence it may be effective in treating sexual impotence.

Common side effects include feeling dizzy or light-headed, trouble sleeping, trouble urinating, and tiredness. More serious side effects include heart failure, low potassium, and blood problems. If overdose is taken then heart muscle damage and decreased brain function may occur. It may also decrease seizure control in people with epilepsy.

It was patented in 1974 and came into medical use in 1981. It is available as a generic medication. In the United States the wholesale cost is less than $2 per day. In 2016 it was the 43rd most prescribed medication in the United States, with more than nine million prescriptions.

In the United Kingdom, the use of metoprolol tartrate and other β-blockers for anxiety and sleep disturbances was approved on 16 June 2012 by the Medicines and Healthcare products Regulatory Agency. The decision was based on clinical evidence and safety. The only indication not approved was anxiety related to chronic pain in patients without underlying cardiovascular disease, who are not suitable for the more sedating β-blockers. It may be used by all practitioners in the UK, however the decision to prescribe is made by the individual practitioner and their prescribing guidance may vary.

In April 2018 it was reported that metoprolol tartrate in combination with naloxone may be a safer alternative for those experiencing opiate-induced insomnia as it has “few or no side effects”, which includes the potentially fatal rebound insomnia, due to its antagonistic action at the naloxone receptors of the adrenergic receptors as well as its partial agonist action at the opiate receptors.

In the United States, metoprolol tartrate is available only with a prescription, is a Schedule III controlled substance, and may not be prescribed in general medical practice in some states.

What is metoprolol used for?

Metoprolol is used, including in combination with other medications, to treat high blood pressure. It may also be prescribed to prevent angina. In both cases, it is not a medicine, but a treatment to help control the problem.
Metoprolol is also used to improve survival after a heart attack, to treat irregular heartbeat, movement problems associated with taking psychotropic drugs, and to prevent migraines.

Metoprolol is used for the treatment of several different diseases:

• Cardiovascular disease
• Angina pectoris
• Hypertension
• Arrhythmias (e.g. supraventricular tachycardia, atrial fibrillation, atrial flutter,
• paroxysmal supraventricular tachycardia)
• Supraventricular tachycardia (SVT), which is due to electrical disturbances and
• can be either narrow complex or wide complex (which is faster than the heart’s
• normal resting rhythm)
• Hypertrophic cardiomyopathy
• Heart failure

In addition to its anti-anginal effects, it has also been found to be effective in treating the symptoms of intermittent claudication (pain in the legs).

Sedation
In combination with midazolam (Versed) it is used to provide amnestic sedation in the medical, dental, veterinary, and surgical applications. The sedative properties are used to reduce anxiety in children undergoing painful procedures. However, the use of metoprolol in patients under 18 years old in England is currently not licensed.

Indications:

– Arterial hypertension (in monotherapy or in combination with other antihypertensive agents);

– Functional disorders of cardiac activity, accompanied by tachycardia;

– Coronary heart disease: myocardial infarction (secondary prevention – combination therapy), prevention of angina attacks;

– Heart rhythm disorders (supraventricular tachycardia; ventricular extrasystole);

– Hyperthyroidism (complex therapy);

– Prevention of migraine attacks.

Metoprolol for anxiety

Like many other beta blockers, metoprolol is sometimes used off-label to control anxiety, including occasional performance anxiety and various anxiety disorders.

Talk to your doctor before taking metoprolol or any other anti-anxiety medication. There may be another drug that is safer and better suited to managing your anxiety.

Metoprolol: forms

Metoprolol tartrate: white, practically odorless crystalline powder, readily soluble in water, methylene chloride, chloroform and alcohol, slightly soluble in acetone, insoluble in ether.

Metoprolol succinate: white crystalline powder, easily soluble in water, soluble in methanol, sparingly soluble in ethanol and slightly soluble in dichloromethane and 2 – propanol, practically insoluble in ethyl acetate, acetone, diethyl ether and heptane.

Metoprolol fumarate.

Contraindications

Hypersensitivity, AV block II and III degree sinoatrial block, acute or chronic (in the stage of decompensation), heart failure, sick sinus syndrome, severe sinus bradycardia (heart rate less than 60 beats./Min), cardiogenic shock, hypotension ( Sad less than 100 mm Hg. Art.) expressed by human peripheral blood circulation, pregnancy, breast-feeding.

Restrictions

Diabetes, hypoglycemia, allergic history, metabolic acidosis, bronchial asthma, emphysema, bronchitis, non-allergic, hyperthyroidism, psoriasis, pheochromocytoma, human liver and/or kidney disease, myasthenia gravis, depression, conduct of general anesthesia, the elderly and children’s age.

Pregnancy and breastfeeding

Perhaps if the expected effect of therapy outweighs the potential risk to the fetus. At the time of treatment should stop breastfeeding.

Side effects

From the nervous system and sensory organs:

at least 10% ; weakness; 1 – 9,9% ; dizziness and headache; 0,1 – 0,9% ; decreased concentration, drowsiness/insomnia, nightmares, depression, muscle cramps, paresthesia; 0,01 – 0,09% ; nervousness, anxiety, weakening of libido, impaired vision, xerophthalmia, conjunctivitis; less than 0,01% ; lethargy, fatigue, anxiety, confusion, amnesia/short-term memory loss, hallucinations, tinnitus, impaired sense of taste.

From the cardio-vascular system:

1 – 9,9% ; bradycardia, palpitations, hypotension, cold extremities; in 0,1 – 0,9% ; heart failure, AV block, edema syndrome, chest pain; in 0,01 – 0,09% ; reduction in myocardial contractility, arrhythmia, less than 0,01% ; gangrene (in patients with severe peripheral circulatory disorders); conduction disturbances infarction, syncope, thrombocytopenia, leukopenia, agranulocytosis.

From the digestive tract:

1 – 9,9% ; nausea, abdominal pain, diarrhea or constipation; 0,1 – 0,9% ; vomiting; 0,01 – 0,09% ; dry mouth, abnormal liver function; flatulence, dyspepsia, heartburn, hepatitis.

From the respiratory system:

shortness of breath (1 – 9,9%), bronchospasm (0,1 – 0,9%), vasomotor rhinitis (0,01 – 0,09%), dyspnea.

For the skin:

0,1 – 0,9% ; rash, degenerative changes in the skin; 0,01 – 0,09% ; reversible alopecia; less than 0,01% ; photosensitivity, exacerbation of psoriasis; pruritus, erythema, urticaria, rash.

Other:

a decrease in body weight (0,1 – 0,9%), arthralgia, arthritis, myalgia, muscle weakness, Peyronie’s disease.

Metoprolol – interactions

The blood pressure lowering effect of metoprolol can be massively increased by the simultaneous administration of other agents for lowering blood pressure such as ACE inhibitors, vasodilators (agents to dilate blood vessels) such as dihydralazine and hydralazine, dehydrating agents (diuretics) or calcium channel blockers of the nifedipine type.

This is also the case if sleeping pills (barbiturates), neuroleptics, antihistamines, anesthetics, tricyclic antidepressants, other beta blockers (e.g. cimetidine) are taken or alcohol is consumed at the same time. Such an (excessive) drop in blood pressure can lead to cardiac insufficiency.

Calcium channel blockers of the verapamil or diltiazem type and agents that make the heart beat more regularly (antiarrhythmics) lead to a reduction in cardiac output (cardiodepressive effect). Lower blood pressure, slow pulse rate, cardiac arrhythmias and even heart failure can result. With the exception of intensive care measures, intravenous administration of these active substances should be avoided during use. Verapamil must not be administered into the veins until 48 hours after metoprolol has been discontinued.

Special blood pressure drugs such as reserpine, alphamethyldopa, guanethidine, guanfacine, cardiac glycosides or clonidine lead to a more pronounced drop in the heart rate and a delay in the conduction of excitation in the heart. A sharp rise in blood pressure can occur, especially after discontinuing clonidine. Metoprolol should therefore only be used several days after clonidine has been discontinued.

Active substances that increase blood pressure such as noradrenaline, adrenaline or MAO inhibitors (except MAO-B inhibitors) lead to a weakening of the antihypertensive effect with an excessive increase in blood pressure.

Simultaneous administration of active substances that lower blood sugar, such as insulin or oral antidiabetic drugs, can lead to an increase in the low blood sugar level (hypoglycaemia). The symptoms of hypoglycaemia, especially the rapid pulse (tachycardia) and tremors (tremor) can be masked or alleviated. Regular blood sugar checks are therefore necessary in diabetics.

Furthermore, increasing circulatory disorders can occur when taking metoprolol and anti-migraine drugs (ergotamine derivatives).

Simultaneous administration of or combinations with floctafenine and sultopride can trigger severe cardiac arrhythmias and should therefore be avoided.

Alpha-sympathomimetics (including tacrine) can, if administered at the same time, increase the conduction time in the heart’s AV node and trigger cardiac arrhythmias.

If digoxin is used at the same time to strengthen the heart, the excretion of digoxin in the blood is delayed. Therefore medical control and monitoring of the amount of digoxin in the blood is necessary. It may be necessary to reduce the digoxin dose.

If mefloquine (an anti-malarial agent) is administered at the same time, there is an increased risk of slow heartbeat (bradycardia).

Rheumatic drugs and pain relievers such as indomethacin or ibuprofen weaken the antihypertensive effect of bisoprolol. Active substances used to treat tuberculosis (for example rifampicin) also reduce the effectiveness of metoprolol and should not be given at the same time.

Anti-acidic agents (antiazida) such as cimetidine or ranitidine also increase the antihypertensive effect.

Overdose

Metoprolol, as with other β-adrenergic receptor blocking agents, can cause significant adverse effects in overdose. Overdose may lead to bradycardia, hypotension, hypothermia, hypoglycemia, and hyperglycemia, as well as other cardiovascular side effects.

How is metoprolol taken? Dosage

Metoprolol is taken orally, in the form of tablets or sustained-release tablets, 1-2 tablets a day with or immediately after meals. Your doctor may prescribe a low starting dose and then gradually increase it.
Long-release tablets can be divided in half, but should never be chewed or crushed.

The method of use and dosage depend on the form of release and other factors. The optimal dosing regimen is determined by the physician. The dosage form used for a particular drug should be strictly observed in accordance with the indications for use and dosage.

When administered orally, the average dose is 100 mg/day in 1-2 doses. If necessary, the daily dose is gradually increased to 200 mg. When intravenously administered, a single dose is 2-5 mg; if there is no effect, reintroduction is possible after 5 minutes.

Maximal doses: when administered orally, daily dose is 400 mg; when administered intravenously, a single dose is 15-20 mg.