What Is Metoprolol Tartrate?

Metoprolol tartrate tablets are indicated for the treatment of hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism, and cardiac neurosis. In recent years, it is still used for the treatment of heart failure. At this time, it should be used under the guidance of an experienced physician.

Metoprolol tartrate tablets are indicated for the treatment of hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism, and cardiac neurosis. In recent years, it is still used for the treatment of heart failure. At this time, it should be used under the guidance of an experienced physician.

Drug Name

Metoprolol tartrate

Drug type

Prescription medicines, essential medicines, medicines for medical workers' injuries

Special medicine

Doping

Use classification

beta receptor blocker

Metoprolol tartrate tablets ingredients

The main ingredient of this product is metoprolol tartrate; the chemical name is: 1-isopropylamino-3- [p- (2-methoxyethyl) -2-propanol L (+)-tartrate.
Chemical Structure:

Molecular formula: (C ₁₅ H ₂₅ NO ₃ ) ₂ .C ₄ H ₆ O ₆
Molecular formula: 684.82

Metoprolol Tartrate Tablet Properties

This product is a white tablet.

Metoprolol tartrate tablets indications

For the treatment of hypertension, angina pectoris, myocardial infarction, hypertrophic cardiomyopathy, aortic dissection, arrhythmia, hyperthyroidism, cardiac neurosis, etc. In recent years, it is still used for the treatment of heart failure. At this time, it should be used under the guidance of an experienced physician.

Metoprolol tartrate tablets specifications

(1) 25mg (2) 50mg (3) 100mg

Metoprolol tartrate tablets dosage

oral. The dose should be individualized to avoid bradycardia. Medication should be taken on an empty stomach, and metoprolol's bioavailability should be increased by 40% when taken at meals.
Treatment of hypertension: 100 ~ 200mg once, divided into 1 or 2 times.
Acute myocardial infarction: It is advisable to use it in the early hours, that is, within the first few hours, because immediate use can reduce the infarct size and reduce the short-term (15 days) mortality in patients who fail to thrombolytic appear). Re-infarction and re-ischemia rates can be reduced in patients who have been thrombolytic, and mortality can be reduced if administered within 2 hours. General usage: May be intravenously injected with metoprolol 2.5 ~ 5mg once (within 2 minutes), and once every 5 minutes, the total dose is 10 ~ 15mg. After 15 minutes, oral administration of 25 to 50 mg was started every 6 to 12 hours for a total of 24 to 48 hours, and then 50 to 100 mg was orally administered twice a day.
Unstable angina pectoris: Early use is also recommended. Usage and dosage can refer to acute myocardial infarction.
When atrial fibrillation occurs in acute myocardial infarction, metoprolol can be administered intravenously if there is no contraindication. The method is the same as above.
It should be used long-term without contraindications after myocardial infarction, as it has been shown to reduce cardiogenic mortality, including sudden death. Usually 50 to 100 mg once, twice a day.
In the treatment of hypertension, angina pectoris, arrhythmia, hypertrophic cardiomyopathy, hyperthyroidism and other symptoms are usually 25 to 50 mg once, 2 to 3 times a day, or 100 mg once a day, twice a day.
Heart failure: This medicine should be used on the basis of anti-heart failure treatment such as digitalis and / or diuretics. The initial dose is 6.25mg, 2 to 3 times a day, and it will increase by 6.25 to 12.5mg every few days to once a week, depending on the clinical situation. The maximum dose can be used once to 50 to 100mg, 2 times a day.
The maximum dose should not exceed 300 mg to 400 mg per day.

Adverse Reactions of Metoprolol Tartrate

The incidence of adverse reactions is about 10% and is usually dose-related.
Common (> 1/100)
General side effects: Fatigue, headache, dizziness, circulatory system: coldness of the extremities, bradycardia, palpitations, gastrointestinal system: abdominal pain, nausea, vomiting, diarrhea and constipation are rare. General side effects: chest pain, weight gain. Circulatory system: Heart failure temporarily worsens the nerves. System: Sleep disturbance, paresthesia Respiratory system: Shortness of breath, bronchial asthma or asthma symptoms Bronchial spasm is rare (<1/1000)
General side effects: sweating, hair loss, altered taste, reversible sexual dysfunction, blood system: thrombocytopenia, circulatory system: prolonged atrioventricular conduction time, arrhythmia, edema, syncope, nervous system: nightmare, depression, memory impairment, insanity, neuroticism , Anxiety, hallucinogenic skin: skin allergic reactions, exacerbation of psoriasis, photosensitivity liver: elevated transaminase eyes: visual impairment, dry eyes and / or eye irritation ears: tinnitus with occasional joint pain, hepatitis, muscle painful spasms, mouth Cases of dryness, conjunctivitis-like symptoms, rhinitis, and impairment of attention and gangrene in patients with vascular disease.

Metoprolol Tartrate Taboo

Cardiogenic shock. Sick sinus node syndrome. II, III degree AV block. Patients with unstable, decompensated heart failure (pulmonary edema, hypoperfusion, or hypotension) who are receiving continuous or intermittent beta-receptor agonist orthostatic therapy. Symptomatic bradycardia or hypotension. This product should not be given to patients with suspected acute myocardial infarction with a heart rate <45 beats / min, a PQ interval> 0.24 seconds, or a systolic blood pressure <100 mmHg. Patients with severe peripheral vascular disease at risk of gangrene. Those who are allergic to any of the ingredients in this product or other beta-blockers.

Precautions for metoprolol tartrate tablets

Renal function impairment Renal function has no significant effect on the clearance of this product, so patients with renal impairment do not need to adjust the dose.
Hepatic impairment In patients with cirrhosis, metoprolol is usually used in the same dose as those with normal liver function. Consider reducing the dose only if the liver function is very severely impaired, such as in patients undergoing bypass surgery.
Patients receiving beta-blockers should not be given intravenous verapamil.
Metoprolol may exacerbate symptoms of peripheral vascular disorders such as intermittent claudication. Care must be taken when severe renal impairment, severe emergencies with metabolic acidosis, and digitalis are combined.
This product should not be used in patients with underlying or symptomatic cardiac insufficiency without concomitant treatment. Patients with variant (Prinzmetal's) angina pectoris may experience increased frequency and severity of angina pectoris due to beta receptor-mediated coronary vasoconstriction. Therefore, non-selective beta-blockers cannot be used in such patients. Selective beta ₁ blockers must also be used with caution.
For patients with bronchial asthma or other chronic obstructive pulmonary disease, adequate bronchodilator therapy should be given at the same time, and the dose of ₂ receptor agonist may need to be increased.
The effect of metoprolol on glucose metabolism or the risk of masking hypoglycemia is lower than that of non-selective beta blockers.
In rare cases, the original moderate atrioventricular conduction abnormalities may worsen (which may lead to atrioventricular block).
Treatment with beta-blockers may impede the treatment of allergic reactions, and conventional doses of adrenaline do not always give the desired effect. Patients with pheochromocytoma should consider the combined use of alpha blockers if using this product.
This product should be gradually withdrawn as much as possible. The entire withdrawal process takes at least 2 weeks, and the dose is gradually reduced until it is finally reduced to 25 mg (50 mg tablets in half). During this period, especially patients with known ischemic heart disease should be closely monitored. During beta blocker withdrawal, the risk of coronary events, including sudden cardiac death, may increase.
The anesthesiologist should be informed that the patient is taking this product before surgery. For patients undergoing surgery, discontinuation of beta-blockers is not recommended.
The impact on driving cars and operating machinery may cause dizziness and fatigue during the treatment with this product, so it should be used with caution when you need to concentrate, such as driving and operating machinery.
Use with caution by athletes.

Metoprolol tartrate tablets for pregnant and lactating women

The use of beta-blockers during pregnancy can cause various problems in the fetus, including fetal growth retardation. Beta-blockers can have adverse effects on the fetus and newborn, especially bradycardia, and should not be used during pregnancy or childbirth.

Metoprolol tartrate tablets for children

Children have limited experience with this product.

Metoprolol tartrate tablets for elderly

There is no significant change in the pharmacokinetics of the elderly compared with young people, so the dosage of elderly patients does not need to be adjusted.

Metoprolol tartrate tablets drug interactions

Metoprolol is a substrate for CYP2D6. Drugs that inhibit CYP2D6 can affect plasma concentrations of metoprolol. Drugs that inhibit CYP2D6 such as quinidine, terbinafine, paroxetine, fluoxetine, sertraline, celecoxib, propafenone and diphenhydramine. For patients taking this product, the dose of this product should be reduced before starting the treatment of the above drugs.
This product should be avoided in combination with the following drugs:
Barbiturates: Barbiturates (researched on pentobarbital) can increase the metabolism of metoprolol through enzyme induction.
Propafenone: In 4 patients who have been treated with metoprolol, the plasma concentration of metoprolol increased 2 to 5 times after the administration of propafenone, of which 2 patients had side effects related to metoprolol. This interaction was confirmed in 8 healthy volunteers. A possible explanation for this interaction is that propafenone is similar to quinidine and inhibits metoprolol metabolism through the cytochrome P4502D6 pathway. Since propafenone also has a beta-blocking effect, its combined use with metoprolol is difficult to grasp.
Verapamil: When Verapamil is used in combination with beta-blockers (it has been reported in combination with atenolol, propranolol, and indololol), it may cause bradycardia and lower blood pressure. Verapamil and beta-blockers have additive inhibitory effects on atrioventricular conduction and sinus node function.
This product may require dose adjustment when used in combination with the following drugs:
Amiodarone: One case reported that the simultaneous use of amiodarone and metoprolol may cause significant sinus bradycardia. Amiodarone has a long half-life (approximately 50 days), which means that the use of metoprolol may still cause interactions between the two drugs for a long period of time after amiodarone treatment is stopped.
Class I antiarrhythmic drugs: Class I antiarrhythmic drugs and -blockers have a negative inotropic effect, so it may cause severe hemodynamics in patients with impaired left ventricular function. side effect. Patients with sick sinus node syndrome and pathological atrioventricular block should also avoid the simultaneous use of metoprolol and class I antiarrhythmic drugs. There is clear data on the interaction between propiamine and metoprolol.
Non-steroidal anti-inflammatory / anti-rheumatic drugs (NSAID): NSAID anti-inflammatory analgesics have been found to counteract the antihypertensive effects of beta blockers. In this regard, the drugs studied are mainly indomethacin. Beta blockers are likely not to interact with sulindac. In a study of diclofenac, no beta-blockers were found to interact with diclofenac.
Diphenhydramine: In a rapidly hydroxylated population, diphenhydramine reduces metorolol's clearance to a-hydroxymetoprolol by CYP2D6 conversion and metabolism by 2.5 times. The role of metoprolol is thus enhanced. Diphenhydramine may inhibit the metabolism of other CYP2D6 substrates.
Diltiazem: Calcium antagonists and beta-blockers have additive inhibitory effects on atrioventricular conduction and sinus node function. Significant bradycardia has been reported when beta-blockers are used in combination with diltiazem.
Adrenaline: Approximately 10 reports have shown that patients treated with non-selective beta-blockers (including indolol and propranolol) developed significant hypertension and tachycardia after adrenaline administration. slow. These clinical observations have been confirmed in studies on healthy volunteers. Adrenaline in local anesthetics may cause this response when administered intravascularly. It is speculated that the use of cardiac selective beta-blockers has a lower risk of this response.
Phenylpropanolamine: A single dose of 50mg of phenylpropanolamine can increase the diastolic blood pressure of healthy volunteers to pathological levels. Propranolol usually antagonizes this increase in blood pressure caused by phenylpropanolamine. But in patients receiving high-dose phenylpropanolamines, beta-blockers can abnormally trigger a hypertensive response. Hypertension reactions have also been reported during phenylpropanolamine treatment alone.
Quinidine: Quinidine can inhibit the metabolism of metoprolol in so-called "rapid hydroxylators" (more than 90% of this type in Sweden), resulting in a significant increase in the latter's plasma concentration and beta receptor blockade. Stagnation effect is enhanced. Other beta-blockers that metabolize via the same enzymatic pathway (cytochrome P450 2D6) may also interact with quinidine.
Clonidine: beta-blockers may aggravate the rebound hypertension that occurs when clonidine is suddenly stopped. To discontinue combination therapy with clonidine, beta-blockers should be discontinued a few days before clonidine is discontinued.
Rifampicin: Rifampicin can induce the metabolism of metoprolol, leading to a decrease in the plasma concentration of the latter.
Patients receiving other beta-blockers (such as eye drops) or monoamine oxidase (MAO) inhibitors should be closely monitored. In patients receiving beta-blockers, inhalation anesthesia increases cardiac suppression.
Patients receiving beta blockers should readjust their oral hypoglycemic dose. If combined with cimetidine or hydralazine, the plasma concentration of metoprolol will increase.

Metoprolol tartrate tablets overdose

Toxicity: Metoprolol 7.5g causes fatal poisoning in adults. A 5-year-old child took 100mg by mistake and had no symptoms after gastric lavage. A 12-year-old child was given 450 mg to cause moderate poisoning, an adult was given 1.4 g to cause moderate poisoning, 2.5 g to cause severe poisoning, and 7.5 g to cause extremely severe poisoning.
Symptoms: Symptoms of the cardiovascular system are most pronounced, but in some cases, especially children and young patients, central nervous system symptoms and respiratory depression may be the main manifestations. The main symptoms of poisoning were bradycardia, I-III degree atrioventricular block, cardiac arrest, blood pressure drop, poor peripheral circulation perfusion, cardiac insufficiency, cardiogenic shock, respiratory depression and asphyxia. Other symptoms include fatigue, confusion, loss of mind, frequent tremors, cramps, sweating, paresthesia, bronchospasm, nausea, vomiting, possible esophageal spasm, hypoglycemia (especially in children), or hyperglycemia, high potassium Bloodemia, effects on the kidneys, and transient weakness syndrome. Combining alcohol, antihypertensive drugs, quinidine, or barbiturates may worsen the patient's condition. The first symptoms of overdose can be seen from 20 minutes to 24 hours after taking the drug.
Treatment: Those with a clear diagnosis are given gastric lavage and activated carbon, and closely observe the changes in the condition. note! In order to reduce the risk of vagus nerve stimulation, atropine should be given intravenously before gastric lavage (0.25-0.5% for adults and 10-20g /% for children). When indicated. Perform endotracheal intubation and respiratory support. Appropriate volume replacement therapy, glucose infusion, and ECG monitoring. Atropine is 1.0-2.0% intravenously, and can be repeated if necessary (mainly controlling vagus nerve symptoms). For patients with myocardial function inhibition, dobutamine or dopamine, calcium glucuronate (9 / ml) 10 to 20 ml can be instilled. Another alternative method is glucagon 50 ~ 150 g / , intravenous injection within 1 minute, followed by intravenous drip, or amrinone. Epinephrine is effective in some patients. Patients with widened QRS waves and arrhythmias can be infused with sodium chloride or sodium bicarbonate. A pacemaker may need to be installed. For patients with cardiac arrest, sometimes several hours of resuscitation are needed. When treating bronchospasm, terbutaline (injection or inhalation) can be used. In addition, symptomatic treatment is performed.

Pharmacology and toxicology of metoprolol tartrate tablets

Metoprolol is a selective ₁ receptor blocker, which requires a lower dose of ₁ receptor on the heart than the dose of 2 receptor on the peripheral blood vessels and bronchus. With increasing dose, ₁ receptor selectivity may decrease.
Metoprolol has no beta receptor agonism and almost no membrane activation. Beta blockers have a negative inotropic and time-varying effect.
Metoprolol treatment can reduce the effects of catecholamines related to physiological and psychological load, reducing heart rate, cardiac output and blood pressure. Under stress, the adrenaline secreted by the adrenal glands increases, and metoprolol does not interfere with normal physiological vasodilation. At the therapeutic dose, metoprolol has a weaker contraction effect on bronchial smooth muscle than non-selective beta blockers. This feature makes it possible to use it in combination with beta ₂ agonists for the treatment of bronchial asthma or other obvious Patients with obstructive pulmonary disease. The effect of metoprolol on islet release and glucose metabolism is less than that of non-selective beta blockers, so it can be used in patients with diabetes. Compared with non-selective beta-blockers, metoprolol has a lesser effect on the cardiovascular response to hypoglycemia, such as tachycardia, and the blood glucose returns to normal levels faster.
For patients with hypertension, this product can significantly reduce blood pressure in the upright, supine, and exercise, and the effect lasts more than 24 hours. An increase in peripheral vascular resistance was observed at the beginning of metoprolol treatment; however, the decrease in blood pressure obtained with long-term treatment may be due to a decrease in peripheral vascular resistance and constant cardiac output. For men with moderate to severe hypertension, metoprolol reduces the risk of cardiovascular death. Metoprolol does not cause electrolyte disturbances.
For patients with tachyarrhythmias. This product can block the effect of increased sympathetic nerve activity and slow down the heart rate. This is mainly achieved by reducing the autonomy of pacing cells and extending the supraventricular conduction time.
This product shows rapid and effective relief of the symptoms of thyroid toxicity. High doses of metoprolol reduce elevated T3 values. T4 levels are not affected.
Metoprolol can reduce the risk of another myocardial infarction, and reduce the risk of cardiac death, especially sudden death after myocardial infarction.

Pharmacokinetics of metoprolol tartrate tablets

The bioavailability of this product is 40-50%, and the maximum -receptor block effect is achieved within 1-2 hours after taking the drug. After 100 mg orally once daily, the effect on heart rate was still significant after 12 hours. Metoprolol is mainly metabolized by CYP2D6 in the liver. Three major metabolites have been identified, all of which have no clinically significant -receptor blockade. The plasma half-life is 3-5 hours. About 5% of metoprolol is excreted by the kidneys as a prototype, and the rest are metabolized.

Storage of metoprolol tartrate tablets

Keep away from light and keep tightly closed.

Packaging of metoprolol tartrate tablets

Aluminum blister packaging;
25mg: 20 tablets / board / box, 20 tablets / board * 2 board / box; 50mg: 20 tablets / board / box, 20 tablets / board * 2 board / box; 0.1g: 10 tablets / board / box.

Expiration Date of Metoprolol Tartrate

36 months.

Metoprolol tartrate tablets

"Chinese Pharmacopoeia" 2010 edition two ^[1]