Labetalol instructions for use and description of the medicine.

Side effects

It is worth considering that no dangerous consequences for the body have been registered, but the following early negative reactions stand out:

• headaches, dizziness;
• digestive system disorders, dry tongue;
• mental disorders;
• rashes, itching;
• allergic reactions.

Any of these conditions becomes a signal to stop taking the drug and visit a doctor. He will prescribe restorative therapy, write a prescription and replace this drug with an available analogue, the mechanism of therapeutic action of which is similar to Labetalol (example: Zocardis, Carvedilol, Dilator).

Reviews about the drug are mostly positive. By following the doctor's recommendations and observing the instructions in the medication manual, it is possible to normalize blood pressure in a short time.

Analogues of Labetalol in tablet form

What kind of medicine is this?

Anti-pressure tablets tenorik reviews
The active ingredient of this medicine is labetalol. It is able to reduce blood pressure due to blocking adrenaline receptors, as well as due to its vasodilating effect. The substance labetalol has antihypertensive, anti-ischemic effects. It has virtually no effect on cardiac output and does not cause reflex tachycardia, which often develops in response to a decrease in pressure. Absorbed into the blood very quickly and excreted in the urine. The advantage of labetalol over other antihypertensive drugs is that it begins to act quickly, and its therapeutic effect lasts for a long time. For example, if the medicine is used intravenously, a decrease in blood pressure levels is observed within 2–5 minutes. With long-term use of this medicine, hypertrophy of the walls of the left ventricle of the heart decreases.

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Pharmacological group of the drug

The action of the drug components is aimed at dilating blood vessels.

The substance labetalol is included in the group of beta-blockers, namely in the subgroup of non-selective hybrid drugs. A group of beta blockers block beta receptors for adrenaline and norepinephrine, which are located in the vascular wall and in the heart. Because labetalol is a hybrid blocker, it primarily acts on beta receptors and also has adrenal alpha blocking properties. Alpha blockers act on alpha receptors for epinephrine and norepinephrine, which are also found in the walls of blood vessels. Due to their dual nature, hybrid blockers promote the expansion of the vascular lumen, reducing overall peripheral vascular resistance. They also have an antiarrhythmic effect and can reduce the heart's need for oxygen.

Indications for the use of Labetalol

There are not many indications for the use of this drug. This medicine is prescribed by a cardiologist in the following situations:

• mono- or complex therapy of arterial hypertension (hypertension);
• relief of hypertensive (hypertensive) crises.

Contraindications for use

There are a number of contraindications to the use of Labetalol, including:

• severe heart failure;
• disruption of the passage of impulses through the heart muscle (atrioventricular, sinoatrial blockade);
• bronchial asthma;
• Prinzmetal vasospastic angina;
• chronic renal failure;
• cardiogenic shock;
• bradycardia (slow heart rate) and bradyarrhythmia;
• acute myocardial infarction;
• individual sensitivity to labetalol or other components of the drug.

Analogues of the drug "Labetalol"

The effectiveness of blood pressure pills during pregnancy

Abetol, Albetol, Amipress, Ipolab, Labetol, Labrokol, Lamitol. Operkol, Presolol, Trandat, Trandol.

Labetalol, like all medicines, has its own analogues. These are drugs that differ in manufacturer and trade name, but are absolutely identical in composition. These drugs include “Lacardia”, “Presolol”, “Trandat”, “Labetol”, “Operkol”, “Ipolab”, “Abetol”, “Amipress”.

Imported drugs are usually more effective. The drug is selected by the doctor individually for each patient. It is not recommended to replace medications on your own. In this regard, it is necessary to consult with your attending cardiologist.

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special instructions

Modern means for lowering blood pressure

The use of Labetalol in most cases masks the symptoms of hypoglycemia (tremor, tachycardia or palpitations).

Patients with liver disease should take this drug with extreme caution; When treating with a drug, it is important to regularly carefully monitor the results of indicators of the functional state of the liver. Labetalol is often effective as monotherapy for dissecting aortic aneurysm. Since T1/2 of the drug is very large, it is not recommended to carry out prolonged infusion for patients

Since T1/2 of the drug is very large, it is not recommended to carry out prolonged infusion for patients

Labetalol is often effective as monotherapy for dissecting aortic aneurysm. Since T1/2 of the drug is very large, long-term infusion is not recommended for patients.

Pregnant women can, of course, take this drug, since no bad effects have been identified to date, but before starting therapy, it is very important to assess the potential benefits and possible harm to the child. It is not recommended to take this drug during lactation only because scientists have not yet identified detailed information about the possible penetration of constituent substances into breast milk

It is not recommended to take this drug during lactation only because scientists have not yet identified detailed information about the possible penetration of constituent substances into breast milk.

In cases where a drug is prescribed for a short period of time, but there are no results from its treatment, it is imperative to reconsider the therapy and, if necessary, replace this drug.

Description

The active substance and name are identical - labetalol is the active component of this medicinal product. This ingredient is able to lower blood pressure by blocking adrenergic receptors, and also due to its additional vasodilating effect.

The composition has two main effects - hypotensive and anti-ischemic. They do not affect the volume of cardiac output and do not provoke reflex tachycardia, which is a consequence of a decrease in blood pressure.

The medication is produced in a tablet form familiar to the patient. It is recommended to take pills 3/24 (three times a day) 0.1 g. In case of severe disease, increasing the dosage is possible. The maximum daily dose cannot be higher than 1000 mg, which is divided into 4 oral doses. An alternative to tablets is an injection solution, also sold under the name Labetalol. This solution can be used mainly in inpatient treatment. The fact is that when it is administered, the pressure can drop sharply; it is prohibited to give injections without medical supervision.

Pills can be purchased in two dosages - 100 mg and 200 mg. The number of pieces in a pack is 30 or 100. The solution is purchased packaged in 10 ampoules of 50 mg of the active ingredient in 5 ml each.

Instructions for use

To reduce high blood pressure, Labetalol in tablet form should be taken 0.1 g three times a day. Depending on the severity of the condition, the dosage may be increased at the discretion of the doctor. The maximum daily dose should not exceed 1 g, divided into 4 doses. To maintain antihypertensive therapy, the medicine is prescribed 1 tablet in the morning, lunch and evening. Injections should be carried out exclusively in a hospital setting, under the strict supervision of a qualified physician.

Contraindications and side effects

It is prohibited to use Labetalol for the treatment of high blood pressure in patients with individual intolerance to its components, as well as in the presence of such pathological conditions as:

• heart failure;
• atrioventricular block;
• bronchial asthma.

During therapy, nightmares may appear as a side effect.

In most cases, the antihypertensive medication is well tolerated, but occasionally it can cause the development of some negative reactions, including:

• severe dizziness;
• headache;
• depression;
• sinus bradycardia;
• drop in blood pressure;
• feeling tired;
• nightmares;
• increased fatigue;
• dyspnea;
• urine retention;
• decreased potassium levels in the blood;
• itching of the skin, rash, xeroderma.

Overdose

Exceeding the dose recommended by the doctor or the instructions, the concentration of labetalol in the blood increases. This is indicated by severe headache, orthostatic hypotension and severe dizziness. To normalize the condition, the victim should consult a doctor and undergo symptomatic therapy.

Compatibility

At the beginning of the course of treatment, you should inform your doctor about the pills you are already taking.

Before using Labetalol, you must inform your doctor about the medications you are already taking, since many of them are incompatible with the antihypertensive drug and may negatively affect the patient’s condition. Thus, it is possible to enhance the antihypertensive effect and increase the risk of developing signs of overdose when used simultaneously with other medications for high blood pressure.

It is not recommended to combine the pharmaceutical drug in question with various antidiabetic agents, and together with MAO inhibitors, it is important to be especially careful, as sinus bradycardia may develop. It is possible to develop an enhanced hypotensive effect and cardiac output with the tandem of Labetalol and Halothane. It is possible to increase the bioavailability of the drug for blood pressure when taken simultaneously with Cimetidine and reduce its hypotensive effect when combined with the oral use of various sympathomimetics

The combination of Labetalol and Mefloquine is considered the most dangerous, since the interaction of their active components increases the chances of developing ECG changes and cardiac arrest

It is possible to increase the bioavailability of the drug for blood pressure when taken simultaneously with Cimetidine and reduce its hypotensive effect when combined with the oral use of various sympathomimetics. The combination of Labetalol and Mefloquine is considered the most dangerous, since the interaction of their active components increases the chances of developing ECG changes and cardiac arrest.

Side effects of the drug Labetalol

dizziness, hypertension (arterial hypertension), syncope, orthostatic hypotension (mainly with intravenous administration), sinus bradycardia, AV block, increased symptoms of heart failure, headache, fatigue, depression, nightmares, paresthesia, nausea, vomiting, hepatotoxic effect, shortness of breath, sexual dysfunction (impotence, ejaculation disorders, decreased libido, priapism), urinary retention, hypoglycemia, itching, xerosis and hyperpigmentation of the skin, reversible alopecia, exfoliative dermatitis.

Pharmacological characteristics of the drug

The combination of the properties of a beta-blocker and an alpha1-blocker gives an excellent effect and leads to a mild decrease in blood pressure. Labetalol does not affect LV output and heart rate. For hypertension, the drug acts only on blood pressure, without changing the functioning of other vital systems.

The main advantage is the antihypertensive properties of Labetalol and its speed of action. The drug is taken orally, after oral administration it is detected in the blood within 20 minutes, and intravenously after 3-5, giving an almost instant effect.

It is eliminated from the body by the excretory organs 4-5 hours after administration. Labetalol is taken for persistently elevated blood pressure to correct hypertension.

In order for the drug to act only favorably, it is recommended to follow the doctor’s instructions, take into account the pharmacological characteristics of the drug and the risk of side effects. Synonyms for Labetalol are often found in medical practice, but this particular drug gives the fastest results.

Imported tablets Labetalol

Action of Labetalol, dosage and instructions for use of the drug

Hypertensive patients are often prescribed Labetalol, the instructions for use of which contain all the information regarding the specific use of the drug, its features, and the nuances of interaction with other medications. The drug affects blood pressure and is indispensable for people who suffer from hypertension.

Pharmacological characteristics of the drug

The combination of the properties of a beta-blocker and an alpha1-blocker gives an excellent effect and leads to a mild decrease in blood pressure. Labetalol does not affect LV output and heart rate. For hypertension, the drug acts only on blood pressure, without changing the functioning of other vital systems.

• The main advantage is the antihypertensive properties of Labetalol and its speed of action. The drug is taken orally, after oral administration it is detected in the blood within 20 minutes, and intravenously after 3-5, giving an almost instant effect.
• It is eliminated from the body by the excretory organs 4-5 hours after administration. Labetalol is taken for persistently elevated blood pressure to correct hypertension.
• In order for the drug to act only favorably, it is recommended to follow the doctor’s instructions, take into account the pharmacological characteristics of the drug and the risk of side effects. Synonyms for Labetalol are often found in medical practice, but this particular drug gives the fastest results.

Imported tablets Labetalol

Pharmacology and procedure for taking Labetalol

• The drug Labetalol (Latin name Labetalol) is available in tablet form, taken orally, washed down with water.
• Only a doctor prescribes the drug and prescribes the dosage, depending on the complexity of the disease and the form of hypertension. The maximum permissible dose is 1000 mg per day, divided into 4 doses.
• The course of treatment is completed with maintenance therapy, continuing to take the drug 1 tablet 2-3 times a day.
• This product is also available in the form of an injection solution, but it is used only under the supervision of a doctor. By injecting Labetalol yourself, you can harm your health. The effect occurs very quickly, which is dangerous for patients with unstable blood pressure.

In order for the drug to provide the required treatment result, it is worth remembering the simple features of its use:

• the dosage must be individual;
• The drug is taken only for high blood pressure;
• Labetalol should only be administered by injection under the supervision of a physician;
• The permissible dosage may vary depending on the form of the disease.

By following simple recommendations and using Labetalol in accordance with the instructions, you can get good and quick results.

Bottles with solution for preparing injection solution

Side effects

It is worth considering that no dangerous consequences for the body have been registered, but the following early negative reactions stand out:

• headaches, dizziness;
• digestive system disorders, dry tongue;
• mental disorders;
• rashes, itching;
• allergic reactions.

Any of these conditions becomes a signal to stop taking the drug and visit a doctor. He will prescribe restorative therapy, write a prescription and replace this drug with an available analogue, the mechanism of therapeutic action of which is similar to Labetalol (example: Zocardis, Carvedilol, Dilator).

Reviews about the drug are mostly positive. By following the doctor's recommendations and observing the instructions in the medication manual, it is possible to normalize blood pressure in a short time.

Analogues of Labetalol in tablet form

Contraindications

Labetalol has contraindications for use, which are associated with the individual characteristics or concomitant diseases of the patient. For chronic diseases, the drug is taken after studying the patient’s clinical picture. Labetalol is contraindicated for use in:

• diseases of the cardiovascular system that are associated with CHF;
• individual intolerance to the active components of the drug, which can cause serious consequences and complications of hypertension.

In case of liver diseases and prerequisites for their development, it is recommended to take the drug extremely carefully.

• During pregnancy, it is permissible to take Labetalol, but only after consulting a doctor, and if the treatment does not harm the baby. It is possible to become pregnant during a therapeutic course using the drug, but in the first trimester, using Labetalol is allowed only under the supervision of a doctor.
• The price of Labetalol differs depending on the country of production and pharmacological company. The drug is available in the form of tablets and injection solution, which allows you to choose a convenient way to use it.
• For those who, due to circumstances, cannot take pills that lower blood pressure, or do not want to expose the body to the risk of adverse reactions, we recommend that you watch the video, from which you can learn several useful recipes for hypertension from traditional medicine.

Source: https://lechiserdce.ru/preparatyi/17083-labetalola-instruktsiya-po-primeneniyu.html

Cost of the drug in Russia and Ukraine

The average cost of the drug Labetalol in Russia is 1,480 rubles, and in Ukraine, accordingly, no more than 450 hryvnia.

Good analogues of this drug, which have no less effective effect, are the following drugs:

• Egilok - the average cost of Labetalol in Russia is about 87 rubles.
• Tenoric - about 73 rubles.
• Corvitol - 104 rubles.
• Metoprolol - 11 rubles.
• Penbutolol - 134 rubles.
• Viskaldix - 76 rubles.
• Pindolol - 346 rubles.
• Ategexal compositum - 56 rubles.
• Propranolol - 88 rubles.
• Kalbeta - 245 rubles.
• Korzid - 564 rubles.
• Metipranolol - 447 rubles.
• Nadolol - about 38 rubles.

Reviews of the drug Labetalol can be read at the end of this article. Most of the reviews left about the use of the pharmacological agent in question are positive: patients note that within a couple of days after starting to take the medicine they felt much better, blood pressure was effectively reduced, and test data improved.

Consider one of the reviews on the Internet:

Zinaida P., 47 years old. “Recently, I have been worried about regularly rising blood pressure, which was accompanied by severe headaches and significant weakening of the body. However, I always took pills that increase my blood pressure and it became easier for me.

Over time, my attacks began to become more frequent and taking the pills was no longer so effective; they stopped helping me. One day my blood pressure rose greatly and I felt bad; the medications no longer helped.

They called an ambulance and took me to a medical facility. There they conducted a thorough examination and the doctor prescribed me the drug Labetalol as treatment. I already doubted that regular pills could help me, but I still followed the specialist’s instructions.

After taking the drug for a long time, I felt much lighter. My blood pressure no longer rose that much and I no longer had to worry about my health. I am very grateful to Labetalol and its manufacturers. Thank you very much for creating this wonderful drug!

Analogues of the drug

Labetalol is the active ingredient in the following medications:

• Albetol;
• Amipress;
• Ipolab;
• Prezolol;
• Trandol.

Most pharmacies now offer labetalol under the name Trandate. This is an Italian-made drug. Abroad, such medicine is produced in the USA, Canada, the Netherlands, China, Taiwan, Great Britain, Slovenia and Malta.

In modern cardiology, Labetalol gives way to its group analogue - the alpha and beta adrenergic blocker Carvedilol. The latter acts more actively on beta receptors, its ability to cause postural hypotension is much weaker. In addition, Carvedilol has additional properties that allow it to be used in the treatment of heart failure.

We recommend reading about the drug Cardiket. You will learn about the properties and indications for the use of tablets, as well as contraindications and possible side effects when taking a heart drug. And here is more information about drugs for the treatment of hypertension.

Labetalol is a drug that blocks both alpha and beta adrenergic receptors. It is used in the form of tablets or intravenous solution for hypertension. It is indicated for increased blood pressure caused by hypertension, pheochromocytoma, pregnancy pathology, as well as during a hypertensive crisis.

To quickly relieve high blood pressure, the drug Labetalol is suitable: application, features

Labetalol is a drug that is used to quickly lower blood pressure (BP) in hypertension. It belongs to the group of “hybrid” adrenergic blockers; its active substance binds to both beta and alpha1 adrenergic receptors. It is worth understanding the peculiarities of taking the drug in advance.

Mechanism of action of the drug

The therapeutic effect of labetalol is associated with its ability to block adrenergic receptors. These are nerve endings that are stimulated by norepinephrine. There are 2 main classes of adrenergic receptors - alpha and beta.

Labetalol blocks alpha1-adrenergic receptors, which are located primarily in the walls of small arteries (arterioles). As a result, they expand in all tissues of the body.

Beta adrenergic receptors are divided into 3 subclasses:

• Labetalol combines a selective blocking effect on alpha1-adrenergic receptors and a non-selective (non-selective) one on beta-adrenergic receptors. The ratio of this activity is 1:3 when taking tablets and 1:7 when administering an injection solution.
• Blockade of beta-adrenergic receptors causes a slight slowdown in heart rate and relaxation of blood vessels. This “double effect” leads to a rapid decrease in blood pressure in people with hypertension.
• Despite the non-selective action, the medicine does not lead to pronounced spasm of the bronchi, in the wall of which beta2-adrenergic receptors are located.

The peculiarity of labetalol is its ability to quickly reduce blood pressure levels.

We recommend reading about calcium channel blockers. You will learn about the mechanism of action of drugs, the use of antianginal or selective blockers, as well as the types of slow calcium channel blockers.

Indications for the use of labetalol

Labetalol can be used as monotherapy or in combination with other medications to reduce high blood pressure. High blood pressure increases stress on the arteries and heart. With prolonged hypertension, it can cause stroke, heart or kidney failure, and also cause an attack of angina or myocardial infarction.

Under the influence of Labetalol, blood vessels dilate and the heartbeat slows down somewhat. As a result, blood pressure decreases, and blood flow in the tissues of the heart and other organs is restored.

Labetalol can be prescribed either in tablet form or as a slow intravenous infusion (infusion)..

Tablets are used in adults and elderly patients for all forms, degrees and stages of hypertension.

Contraindications

Labetalol is a non-selective beta-blocker, so it acts not only on blood vessels and the heart, but also on the bronchi, carbohydrate and fat metabolism. Therefore, it should not be used for the following disorders:

Directions for use and doses

The medicine can only be used as prescribed by a doctor. It is usually prescribed as an injection during hospital treatment. After completion of the infusion, it is recommended to remain in bed for 3 hours.

Treatment of hypertension in adults:

• initial dose 100 mg x 2 times a day, with a possible gradual increase to 400 mg x 2 times a day, maximum dose 2400 mg per day in 2 - 4 divided doses;
• in the elderly, it is recommended to start therapy with 50 mg x 2 times a day, gradually increasing to 100 - 200 mg x 2 times a day.

Labetalol infusion is not compatible with the administration of 5% sodium bicarbonate or other alkaline solutions.

Is it possible to take pills during pregnancy?

Pregnancy is not a contraindication for taking labetalol. But more often this remedy is used in emergency cases, for example, severe gestosis, preeclampsia or eclampsia.

Side effects

The most common side effect of the drug is postural hypotension, that is, a sharp decrease in blood pressure, dizziness and resulting falls when moving from a lying position to an upright position, for example, when getting out of bed. When such a symptom appears, a reduction in the dosage of the medication is required.

A new medicine for the treatment of coronavirus. Molnupiravir is already registered in the UK. Go to article

Rare side effects:

• weakness, rapid muscle fatigue;
• muscle cramps;
• mild constipation;
• headache and tingling sensation in the scalp;
• ejaculation disorder.

Cost of tablets

Despite the fact that Labetalol is excluded from the State Register of Medicines of Russia, it can be purchased under the trade name Trandat at a price of about 1,400 rubles for a package of 30 tablets of 100 mg.

In Ukrainian pharmacies you can buy a similar drug at a price of 570 UAH.

Analogues of the drug

Labetalol is the active ingredient in the following medications:

• Albetol;
• Amipress;
• Ipolab;
• Prezolol;
• Trandol.

Most pharmacies now offer labetalol under the name Trandate. This is an Italian-made drug. Abroad, such medicine is produced in the USA, Canada, the Netherlands, China, Taiwan, Great Britain, Slovenia and Malta.

• In modern cardiology, Labetalol gives way to its group analogue - the alpha and beta adrenergic blocker Carvedilol . The latter acts more actively on beta receptors, its ability to cause postural hypotension is much weaker. In addition, Carvedilol has additional properties that allow it to be used in the treatment of heart failure.
• We recommend reading about the drug Cardiket. You will learn about the properties and indications for the use of tablets, as well as contraindications and possible side effects when taking a heart drug.
• And here is more information about drugs for the treatment of hypertension.
• Labetalol is a drug that blocks both alpha and beta adrenergic receptors. It is used in the form of tablets or intravenous solution for hypertension. It is indicated for increased blood pressure caused by hypertension, pheochromocytoma, pregnancy pathology, as well as during a hypertensive crisis.

Source: https://CardioBook.ru/labetalol-primenenie/

Drug interactions

Read further - cardiology centers in Moscow. List of the best clinics.

In the news (here) instructions for Pectrol.

When taking Labetalol together with various other antihypertensive drugs, an additive effect is most often observed. When prescribed with the drug Verapamil or Diltiazem, the risk of developing AV block increases.

Adverse reactions often occur when Labetalol is taken simultaneously with various antidiabetic drugs.

The use of Labetalol with an anesthetic usually potentiates and prolongs the hypotensive effect of the former. The combined use of Halothane with Labetalol often causes a hypotensive effect, and also significantly reduces central venous pressure, as well as cardiac output.

It is necessary to take Labetalol with extreme caution in patients taking MAO inhibitors, this is due to the possible development of a disease such as sinus bradycardia. The use of Cimetidine increases the bioavailability of Labetalol in case of simultaneous oral administration, this most likely occurs due to an increase in absorption or a significant decrease in the effect of systemic metabolism

The use of Cimetidine increases the bioavailability of Labetalol in case of simultaneous oral administration, this most likely occurs due to an increase in absorption or a significant decrease in the effect of systemic metabolism.

The simultaneous use of various sympathomimetics with Labetalol almost always reduces the hypotensive effect of the latter.

The pharmacological drug Labetalol is able to reduce nitroglycerin-induced reflex tachycardia, and also effectively provide an additive hypotensive effect. In the case of simultaneous use of Labetalol and any tricyclic antidepressant, tremor develops in most cases.

The combined use of Labetalol with Mefloquine increases the risk of developing possible changes in the ECG, as well as cardiac arrest.

The recommended storage temperature for the drug is up to 25 degrees Celsius.

After the expiration date, it is strictly prohibited to take the medicine, as this may lead to undesirable effects.

Drug interactions Labetalol

With simultaneous use of labetalol with other antihypertensive drugs, an additive effect is observed. When prescribed with verapamil or diltiazem, the risk of developing AV block increases. Undesirable pharmacodynamic interactions are possible when combined with the simultaneous use of labetalol and antidiabetic agents. Anesthetics can potentiate and prolong the hypotensive effect of labetalol. The combination of halothane and labetalol may produce a synergistic hypotensive effect, reducing cardiac output and lowering central venous pressure. Labetalol should be used with caution in patients taking MAO inhibitors due to the possibility of developing sinus bradycardia. Cimetidine increases the bioavailability of labetalol when administered concomitantly, probably by increasing absorption or decreasing first pass metabolism. Concomitant use of sympathomimetics may reduce the hypotensive effect of labetalol. Labetalol reduces nitroglycerin-induced reflex tachycardia and has additive hypotensive effects. With simultaneous use of labetalol with tricyclic antidepressants, tremor may develop. When used simultaneously with mefloquine, the risk of developing ECG changes and cardiac arrest increases.

List of pharmacies where you can buy Labetalol:

• Moscow
• Saint Petersburg

pharmachologic effect

Labetalol is a non-selective beta-adrenergic receptor blocker with a selective blocking effect on postsynaptic alpha-1 adrenergic receptors. Due to the presence of two optical centers in the molecule, there are four diastereoisomers of labetalol, which differ in the degree of pharmacological activity. The ratio of beta and alpha adrenergic blocking activity of racemic labetalol ranges from 3:1 when administered orally to 7:1 when administered intravenously.

As a result of interaction with alpha and beta adrenergic receptors, labetalol causes vasodilation and a decrease in peripheral vascular resistance, leading to a decrease in systemic blood pressure without a significant decrease in cardiac output and the development of reflex tachycardia. The adverse effect of labetalol on the lipid spectrum of blood plasma is minimal. With systematic use, labetalol reduces the severity of left ventricular myocardial hypertrophy in patients with hypertension. Labetalol has a quinidine-like membrane-stabilizing effect, which, however, only occurs when labetalol is administered in very high doses. Compared with other beta-adrenergic blockers (eg propranolol), labetalol does not reduce glomerular filtration and renal blood flow.

Publications in the media

(Labetalolum) INN

Synonyms. Trandat.

Composition and release form. Tablets of 0.1 and 0.2 g labetalol; 1% solution of labetalol for injection in ampoules of 5 ml.

Indications. Hypertension of varying degrees.

Pharmachologic effect. An antiadrenergic agent that blocks beta and alpha 1-adrenergic receptors, leading to vasodilation, a decrease in peripheral vascular resistance and virtually no postural hypotension. The drug does not significantly affect cardiac output and heart rate. The maximum effect of the drug is observed 1 hour - 4 hours after administration and lasts up to 8-12 hours or up to 24 hours when using high doses.

Pharmacokinetics. Labetalol is almost completely absorbed from the gastrointestinal tract into the blood, but undergoes active “presystemic metabolism”, and its bioavailability is 25%. The maximum concentration in the blood is achieved 2-4 hours after a single oral dose. The drug is 50% bound to blood proteins. T 1/2 is 6-8 hours. Labetalol is metabolized in the liver and excreted from the body through the gastrointestinal tract, 55-60% in the urine.

Side effects. Heart failure, bronchospasm, hypoglycemia, dizziness, headache, nausea, vomiting, diarrhea or constipation, feeling tired.

Contraindications. Severe heart failure, AV block.

Adverse reactions when interacting with other drugs. Hypotension may develop when used in combination with other antihypertensive drugs or diuretics. When labetalol is used concomitantly with halogenated general anesthetics, excessive hypotension, a significant decrease in cardiac output and an increase in central venous pressure may occur. Cimetidine increases plasma concentrations of labetalol when used together. Estrogens reduce the hypotensive effect of labetalol. Labetalol reduces reflex tachycardia caused by nitroglycerin and increases the hypotensive effect. When using phenothiazines with labetalol, the plasma concentration of these drugs increases. Propafenone increases the plasma concentration and half-life of labetalol.

Information for the patient. Labetalol is taken 0.1 g 2-3 times a day after meals, mixed with liquid (water, juices), non-solid food (applesauce, pudding). If necessary, the dose can be increased. For hypertensive crises, the drug is used intravenously. Caution should be exercised when using the drug for bronchial asthma. The drug is discontinued gradually. Take the missed dose as soon as possible and do not take it at all if the next dose is less than 4 hours away; do not take double doses.

Labetalol: instructions for use

Labetalol is a fast-acting drug that lowers blood pressure. The medication is often used as an ambulance for high blood pressure. However, the rapid action of the drug imposes a number of restrictions on its use, which must be taken into account before starting therapy.

Labetalol is available in tablets and solution in ampoules, intended for slow intravenous administration. The main active ingredient of the drug is labetalol.

Tablets are available in two dosages - 100 and 200 mg of active ingredient. The tablets are packaged in blisters and polymer jars; the drug is available in 30 or 100 tablets (capsules) in one cardboard package. Ampoules of the drug with a capacity of 5 ml contain 50 mg of the main active ingredient.

The drug has many analogues, but is not a first-line drug of choice due to its rather aggressive effect on the body.

There is no solution of the drug in pharmacies

Labetalol is a non-selective adrenergic blocker. The drug simultaneously affects alpha and beta adrenergic receptors, which explains its rapid antihypertensive effect.

• vasodilator effect;
• rapid decrease in blood pressure;
• decreased peripheral vascular resistance;
• reducing the severity of left ventricular hypertrophy of the heart.

The drug quickly reduces blood pressure, but has virtually no effect on cardiac output. Taking the drug over a long course does not lead to the development of reflex tachycardia. At the same time, long-term therapy with Labetolol normalizes myocardial function and reduces left ventricular hypertrophy.

Instructions for use of the drug Labetalol suggests taking the drug to treat the following conditions:

• arterial hypertension;
• aortic aneurysm;
• pheochromocytoma.

The therapy uses tablets and injection solution. The tablets are intended for home treatment; injections or infusions are carried out only in a hospital setting.

Since the drug quite sharply reduces blood pressure, relief of a hypertensive crisis with Labetalol is carried out in a hospital, under the supervision of medical personnel. To quickly normalize blood pressure, intravenous injections of the drug are given. Labetalol, whose indications for use are quite broad, should be used only as prescribed by a doctor.

Self-administration of medication during a hypertensive crisis is not recommended.

Labetalol

Labetalol is a synthetic antihypertensive drug belonging to the group of non-selective beta blockers for oral and parenteral use.

Pharmacological properties

Labetalol is a synthetic drug that belongs to the group of non-selective beta blockers. Labetalol also has the properties of an alpha-blocker with an effect on postsynaptic α 1 -adrenergic receptors.

• Its chemical structure is a racemate, which consists of four stereoisomers. The ratio of beta and alpha adrenergic blocking activity in labetalol ranges from 3:1 when administered orally to 7:1 when administered intravenously.
• As a result of interaction with α- and β-adrenergic receptors, labetalol has a vasodilatory effect and reduces total peripheral vascular resistance, which leads to a decrease in systemic blood pressure without a significant decrease in cardiac output and the development of reflex tachycardia.
• With systematic use, labetalol reduces the severity of left ventricular myocardial hypertrophy in patients with hypertension. Labetalol also has a quinidine-like membrane-stabilizing effect, which manifests itself when the drug is used in high doses.
• Labetalol has little effect on lipid metabolism. Labetalol causes a decrease in renin synthesis. Compared with other beta blockers, labetalol does not impair glomerular filtration rate or renal blood flow.

Pharmacological

When taken orally, labetalol is rapidly and well absorbed from the gastrointestinal tract, but bioavailability is only 25% due to the first-pass effect through the liver. When administered intravenously, it is quickly distributed in the body; bioavailability when administered intravenously is 100%.

• After administration, the maximum concentration is reached within 2 minutes, but after 8.5 minutes it decreases. When taken orally, the hypotensive effect begins within 20-120 minutes with maximum effect after 1-4 hours. Labetalol penetrates the blood-brain barrier in small amounts.
• The drug penetrates the placental barrier and is excreted into breast milk. Labetalol is metabolized in the liver. The drug is excreted from the body mainly by the kidneys, partly with bile and feces. The half-life is 2.5-8 hours, this time may increase if renal function is impaired.
• In case of renal failure, labetalol may accumulate in the body.

Indications for use

Labetalol is used for hypertensive crisis, pheochromocytoma, dissecting aortic aneurysm, hypertension, arterial hypotension during clonidine withdrawal.

Side effect

When using labetalol, the following side effects are possible: rash, skin itching, skin hyperpigmentation, dry eye mucosa, orthostatic arterial hypotension, dizziness, headache, loss of consciousness, sinus bradycardia, blockade, increased symptoms of heart failure, depression, paresthesia, sexual dysfunction. (impotence, impaired ejaculation, decreased libido, priapism), urinary retention, hypoglycemia, nightmares, alopecia, Lyell's syndrome, increased bronchial muscle tone, nausea, vomiting, liver dysfunction, diarrhea, feeling of fatigue, allergic reactions.

Contraindications

Labetalol is contraindicated in case of hypersensitivity to the drug, cardiogenic shock; GOST standards for myocardial infarction; uncontrolled initial heart failure or heart failure refractory to cardiac glycosides; Prinzmetal's angina; sinoatrial block; AV block II-III degree; for broncho-obstructive diseases or bronchial asthma; untreated pheochromocytoma; bradycardia, arterial hypotension; metabolic acidosis; severe peripheral circulatory disorders. Labetalol is not used in childhood and adolescence. Labetalol is contraindicated during pregnancy and breastfeeding. It is prescribed with caution for severe impairment of liver and kidney function, myasthenia gravis, diabetes mellitus, thyrotoxicosis, and psoriasis.

Pharmacological properties of the drug Labetalol

Non-selective blocker of β-adrenergic receptors with a selective blocking effect on postsynaptic α1-adrenergic receptors. Due to the presence of two optical centers in the molecule, there are four diastereoisomers of labetalol, which differ in the degree of pharmacological activity. The ratio of β- and α-adrenergic blocking activity of racemic labetalol is 3–7:1. As a result of interaction with α- and β-adrenergic receptors, labetalol causes vasodilation and a decrease in peripheral vascular resistance, leading to a decrease in systemic blood pressure without a significant decrease in cardiac output and the development of reflex tachycardia. The adverse effect of labetalol on the lipid spectrum of blood plasma is minimal. With systematic use, labetalol reduces the severity of left ventricular myocardial hypertrophy in patients with hypertension (arterial hypertension). Labetalol has a quinidine-like membrane-stabilizing effect, which, however, only occurs when labetalol is administered in very high doses. Compared with other beta-adrenergic blockers (eg propranolol), labetalol does not reduce glomerular filtration and renal blood flow. After oral administration, labetalol is rapidly and almost completely absorbed. Concomitant use with food slows down the absorption of labetalol in the intestine, but increases absolute bioavailability. It undergoes significant first-pass metabolism in the mucous membrane of the digestive tract and during the initial passage through the liver, due to which only about 25% of the administered dose of labetalol enters the systemic circulation unchanged. The hypotensive effect develops within 20 minutes - 2 hours after oral administration, the maximum effect occurs after 1-4 hours. The duration of the hypotensive effect is dose-dependent and ranges from 8 to 24 hours. The hypotensive effect after IV administration develops after 2-5 minutes and reaches its maximum expression in 5–15 minutes; its duration is 2–4 hours. The half-life in patients with normal renal function ranges from 2.5–8 hours. With severe renal failure, accumulation of labetalol is possible. Widely distributed in all tissues of the body, penetrates the placenta, and is excreted in breast milk. In small quantities it penetrates the BBB. Extensively metabolized in the liver by glucuronidation. About 30% is excreted in bile and excreted in feces, the rest is excreted in urine (55–60% as metabolites and 5% unchanged).

Use of the drug Labetalol

In case of hypertensive crisis, it is administered intravenously slowly (over 2 minutes) at a dose of 20 mg (2 ml of 1 % solution). If necessary, the administration is repeated at intervals of 10 minutes. It is preferable to administer labetalol as an infusion in an isotonic solution of sodium chloride or glucose (the concentration of the solution for infusion is 1 mg/ml) at a rate of 2 mg/min. Typically the effective dose is 50–200 mg. The total dose for adults when administered intravenously should not exceed 300 mg. Information on use in children is limited. It is recommended to administer orally at a rate of 4 mg/kg/day in 2 divided doses with constant monitoring of blood pressure levels. When administered intravenously, the bolus dose (administered slowly) is 0.2–1 mg/kg. The initial infusion rate is 0.4–1 mg/kg/h, the maximum is no more than 3 mg/kg/h.