Lokren pills 20mg №56

Composition

One pill contains:

active substance:

betaxolol hydrochloride -20.00 mg;

Excipients:

lactose monohydrate - 100.00 mg, microcrystalline cellulose - 113.00 mg, sodium carboxymethyl starch (type A) - 4.00 mg, colloidal silicon dioxide - 1.60 mg, Magnesium stearate - 1.40 mg; Shell: hypromellose-3.90 mg, titanium dioxide (E171) - 0.67 mg, macrogol-400 -0.43 mg.

Round biconvex tablets, film-coated white, with a risk on one side and engraved KE 20 on the other side.

Pharmacotherapeutic group: beta1-blocker selective.

Pharmacology

Pharmacodynamics

Betaxolol is characterized by the following three pharmacological properties:

cardio selective beta1

-adrenoblokiruyuschee action;

- lack of partial agonistic activity (lack of internal sympathomimetic activity);

- weak membrane stabilizing action (similar to quinidine or

local anesthetics) in concentrations exceeding therapeutic.

It should be noted that the selective effects of betaxolol on beta1-adrenergic

the receptors are not absolute, so when used in high doses it is possible

the effects of betaxolol on beta2-adrenergic receptors located mainly

way, in the smooth muscles of the bronchi and blood vessels (however, the effect of betaxolol on

beta2-adrenoreceptors are significantly weaker than those of non-selective beta-blockers).

When using betaxolol, its blocking beta1-adrenergic receptors

activity is manifested by the following pharmacodynamic effects:

-reduction of heart rate (HR) at rest and during exercise (due to beta blockade

-adrenoreceptors in the sinus node, which, in combination with the absence of internal betaxolol

sympathomimetic activity leads to a slowdown of the automatism of the sinus node);

-reduction of cardiac output at rest and during exercise due to competitive antagonism with catecholamines in peripheral (especially cardiac) adrenergic nerve endings;

-reduction of systolic and diastolic blood pressure at rest and with

physical activity (mechanism of antihypertensive action is described below);

-reduction of the reflex orthostatic tachycardia.

As a result of these effects, there is a decrease in the load on the heart at rest and with

physical exertion.

The mechanism of antihypertensive action of beta-blockers is not fully installed.In beta-blockers, the following mechanisms of antihypertensive action are suggested:

- decrease in cordial emission;

- elimination of peripheral arterial spasm (due to central action,

leading to a decrease in sympathetic impulses to the periphery, to the vessels, and due to inhibition of renin activity).

The antihypertensive effect of betaxolol with its prolonged use is not reduced.

When taking betaxolol (from 5 to 40 mg) once a day, antihypertensive

the effect is the same after 3-4 hours (the time to reach the maximum concentration of Betaxolol in the blood) and after 24 hours (before taking the next dose). When taking 5 mg and 10 mg of betaxolol, its antihypertensive effect is, respectively, 50% and 80% of

anti-hypertensive effect when taking 20 mg of betaxolol.

Thus, in the dose range of 5–20 mg, a dose-dependence of the antihypertensive effect is observed, and with an increase in the dose from 10 mg to 20 mg, the increase in the antihypertensive effect is insignificant.

Increasing the dose from 20 mg to 40 mg slightly changes the antihypertensive effect of betaxolol.

The maximum antihypertensive effect of each dose of betaxolol is achieved in 1-2 weeks. In an exception to the antihypertensive effect of betaxolol, the effect of reducing heart rate does not increase with an increase in its dose (from 10 mg to 40 mg).

In addition, betaxolol is able to slow down the conductivity of the atrioventricular node.

Pharmacokinetics

Suction

Betaxolol is rapidly and completely (100%) absorbed from the gastrointestinal

- intestinal tract.

Betaxolol has a slight effect of "primary passage" through the liver and high bioavailability - about 85%. Maximum plasma concentrations of Betaxolol

blood is reached in 2-4 hours. Differences in its plasma concentrations in different patients or in one patient with long-term use have minor differences, which is associated with a high bioavailability of betaxolol.

Distribution

Betaxolol binds to plasma proteins by about 50%.

The permeability through the blood-brain and placental barrier is low. Breast milk secretion is negligible. The volume of distribution is about 6 l / kg.

Metabolism

In the body, betaxolol is mainly converted into inactive metabolites.

Fat solubility is moderate.

Removal

Excreted by the kidneys as metabolites (more than 80%), 10-15% unchanged.

The half-life (T1 / 2) of Betaxolol is 15-20 hours. T1 / 2 in violation

liver function is prolonged by 33%, but the clear ns does not change; in violation of function

kidney T1 / 2 doubles (need to reduce doses).

Not removed during hemodialysis.

Indications and usage

- Arterial hypertension (in monotherapy and combination therapy).

-Prevention of strokes of angina (in monotherapy and combination therapy).

Contraindications

- Increased sensitivity to betaxolol and excipients of the drug.

- Severe forms of bronchial asthma and chronic obstructive pulmonary disease.

- Acute heart failure, chronic heart failure in the stage

decompensation, not compensated as a result of treatment with diuretics, inotropic

ACE inhibitors, other vasodilators.

- Cardiogenic shock.

-Atricoventricular block II and III degree (without an installed artificial pacemaker).

-Sinocardia Prinzmetala (monotherapy is contraindicated).

- Syndrome of weakness of the sinus node (including sinoatrial blockade).

- Pronounced bradycardia (heart rate less than 45-50 beats / min.).

- Severe forms of Raynaud's disease and peripheral arterial disease obliterans.

- Feochromocytoma without simultaneous administration of alpha-blockers.

-Arterial hypotension (systolic blood pressure <100 mmHg. Art.).

-Anaphylactic reactions in anam nez.

- Metabolic acidosis.

- At simultaneous use with flaktafenin (see the section "Interaction with Other Medicines"),

- At simultaneous use with a sultoprid (see the section "Interaction with Other Medicines"),

-When taking monoamine oxidase (MAO) inhibitors simultaneously.

- Cardiomegaly (without signs of heart failure).

- Age up to 18 years (efficacy and safety have not been established).

-Lactase deficiency, lactose intolerance, glucose-galactose malabsorption (due to the presence of lactose in the formulation).

Pregnancy and Breastfeeding

Pregnancy

In animal experiments, betaxolol was not detected teratogenic effects. To date, no teratogenic effects have been reported in humans. Usually beta

-blockers reduce blood flow in the placenta and may affect the development of the fetus. Should

monitor the blood flow in the placenta and uterus, as well as monitor the growth and development of the unborn child, and in the event of adverse events in relation to pregnancy and / or

of the fetus, to take alternative therapeutic measures.

You should carefully examine the newborn after childbirth. In the first 3-5 days of life, symptoms of bradycardia of hypoglycemia may occur, since the action of beta-blockers

in newborns whose mothers took them before birth, persists for several days after birth.

In the neonatal and postnatal period, newborns have an increased risk of cardiac and respiratory complications. In case of heart failure, the newborn is hospitalized in the intensive care unit.

(See the “Overdose” section).

The use of plasma substitutes should be avoided (risk of developing acute pulmonary edema). The development of bradycardia, respiratory failure and hypoglycemia has also been reported. In this regard, during the first 3-5 days of life requires careful monitoring of these newborns in a specialized department (heart rate, blood glucose concentration).In this regard, the use of the drug Lokren® during pregnancy is not recommended and

possible only when the benefit to the mother outweighs the potential risk to the fetus or child.

Lactation period

Beta-blockers, including betaxolol, are excreted in breast milk (see section

"Pharmacokinetics"). The risk of hypoglycemia or bradycardia in infants has not been studied,

therefore, as a precautionary measure, breastfeeding during treatment should be discontinued.

The drug is taken orally and washed down with a sufficient amount of liquid. Do not chew the pill. The initial dose of Lokren® for both indications for use of the drug is usually 10 mg (1/2 pill 20 mg). If within

7-14 days of treatment, target blood pressure values ​​are not achieved, then the dose doubles to 20 mg per day. Usually, do not use doses of Lokren® exceeding 20 mg (due to the fact that with increasing doses of more than 20 mg is not observed

a statistically significant increase in the antihypertensive effect of the drug).

The maximum daily dose of the drug Lokren® -40 mg.

Patients with renal failure

Dose adjustment is recommended depending on the functional state of the patient's kidneys.

When creatinine clearance of more than 20 ml / min dose adjustment is not required. However, at the beginning

treatment, it is recommended to conduct clinical observation until the equilibrium concentration of the drug in the blood is reached, which is achieved on average by the 4th – 7th day of treatment).

With severe renal failure (creatinine clearance less than 20 ml / min), the recommended initial dose of the drug is 5 mg / day (regardless of

frequency and days of the hemodialysis procedure in patients on hemodialysis), which, if not sufficiently effective, can increase by 2 times every 1-2 weeks. The maximum daily dose is 20 mg.

Patients with liver failure

In patients with hepatic insufficiency, dose adjustment is usually not required.

However, at the beginning of therapy, more careful clinical observation of the patient is recommended.

Store at a temperature not higher than 25 ° С. Keep out of the reach of children.