Lokren - instructions for use, reviews, analogs and formulations (20 mg tablets) of the drug for the treatment of angina pectoris and pressure reduction in adults, children and pregnancy. Composition and interaction with alcohol

In this article, you can read the instructions for using the drug Lokren. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Lokren in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Lokren in the presence of existing structural analogs. Use for the treatment of angina pectoris tension and pressure decrease in adults, children, as well as during pregnancy and lactation. Composition and interaction of the drug with alcohol.

 

Lokren selective beta-1 blocker. Betaxolol (active ingredient of the drug Lokren) is characterized by three pharmacological properties: cardioselective beta1-adrenergic blocking action; absence of partial agonistic activity (absence of internal sympathomimetic activity); weak membrane-stabilizing action (similar to the action of quinidine or local anesthetics) in concentrations exceeding therapeutic.

 

It should be noted that the selective effect of betaxolol on beta1-adrenergic receptors is not absolute, so when using it in high doses, the effect of betaxolol on beta2-adrenoreceptors, located mainly in the smooth muscles of the bronchi and vessels (however, the effect of betaxolol on beta2-adrenergic receptors is significantly weaker than that of nonselective beta-blockers).

 

When using betaxolol, its blocking beta 1-adrenoreceptors activity is manifested by the following pharmacodynamic effects:

• a decrease in heart rate at rest and under physical exertion (due to the blockade of beta-adrenergic receptors in the sinus node, which in combination with the absence of internal sympathomimetic activity in betaxolol leads to a slowdown in 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;
• decrease in systolic and diastolic blood pressure at rest and under physical exertion (the mechanism of antihypertensive action is described below);
• a decrease in the reflex of orthostatic tachycardia.

 

As a result of these effects, there is a decrease in the load on the heart at rest and under physical exertion.

 

The mechanism of antihypertensive action of beta-blockers is not fully established.

 

In beta-adrenoblockers the following mechanisms of antihypertensive action are assumed:

• decreased cardiac output;
• elimination of spasm of peripheral arteries (due to central action leading to a decrease in sympathetic impulses to the periphery, to vessels, and by inhibiting renin activity).

 

The antihypertensive effect of Lokren in his long-term use does not decrease. At a single dose of betaxolol (from 5 to 40 mg) during one day, the antihypertensive effect is the same after 3-4 hours 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 the antihypertensive effect with 20 mg of betaxolol.

 

Thus, in the dose range of 5-20 mg, the dose-response 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.

 

Unlike the antihypertensive action of Lokren, the effect of decreasing heart rate with increasing dose (from 10 mg to 40 mg) does not increase.

 

In addition, Lokren is able to slow the conductivity of the AV node.

 

Composition

 

Betaxolol hydrochloride + excipients.

 

Pharmacokinetics

 

After ingestion, Lokren quickly and completely (100%) is absorbed from the digestive tract. Betaxolol has a slight effect of "primary passage" through the liver and high bioavailability - about 85%. Differences in plasma concentrations in different patients or in one patient with long-term use have insignificant differences, which is associated with high bioavailability of betaxolol. Betaxolol binds to blood plasma proteins by about 50%.Poorly penetrates the blood-brain barrier (BBB) ​​and the placental barrier, to a small extent excreted in breast milk. The solubility in fats is moderate. Betaxolol is metabolized in the liver with the formation of inactive metabolites. It is excreted by the kidneys in the form of metabolites (more than 80%), 10-15% - unchanged. It is not removed during hemodialysis.

 

Indications

• arterial hypertension (in monotherapy and combination therapy);
• prevention of angina pectoris attacks (in monotherapy and combination therapy).

 

Forms of release

 

The tablets covered with a cover of 20 mg.

 

Instructions for use and dosage

 

The drug is taken orally and washed down with a sufficient amount of liquid. Do not chew the tablet.

 

The initial dose of Lokren for both indications for use is usually 10 mg (1/2 tablet 20 mg). If within 7-14 days of treatment the target values ​​of blood pressure are not attained, then the dose is doubled to 20 mg per day.

 

Usually, do not use doses of Lokren, exceeding 20 mg (due to the fact that with a dose increase of more than 20 mg there is no statistically significant increase in the antihypertensive effect of the drug).

 

The maximum daily dose of Lokren is 40 mg.

 

In patients with hepatic insufficiency, dose adjustment is usually not required. However, at the beginning of therapy, a more thorough clinical observation of the patient is recommended.

 

Side effect

• skin rash;
• itching;
• hives;
• psoriasis-like rashes or exacerbation of psoriasis;
• dizziness;
• headache;
• asthenia;
• insomnia;
• depression;
• hallucinations;
• confusion of consciousness;
• nightmares;
• paresthesia;
• dry eyes;
• decrease in intraocular pressure (because of the possibility of its decrease under the influence of beta-blockers);
• visual impairment;
• diarrhea;
• nausea, vomiting;
• bradycardia, possibly severe;
• decrease in skin temperature of upper and lower extremities;
• development (or worsening) of symptoms of heart failure (swelling of the ankles, feet, legs);
• marked decrease in blood pressure;
• manifestations of angiospasm: Raynaud's syndrome, increased peripheral circulatory disorders, incl. and "intermittent" lameness;
• bronchospasm;
• impotence;
• intrauterine growth retardation;
• withdrawal syndrome (increased or more frequent angina attacks, increased blood pressure).

 

Contraindications

• severe forms of bronchial asthma and chronic obstructive pulmonary disease;
• acute heart failure, chronic heart failure in the stage of decompensation, not compensated as a result of treatment with diuretics, inotropic drugs, ACE inhibitors, other vasodilators;
• cardiogenic shock;
• AV-blockade of 2 and 3 degrees (without the installed artificial pacemaker);
• angina prinzmetal (contraindicated monotherapy);
• syndrome of weakness of the sinus node - SSSU (including sinoatrial blockade);
• pronounced bradycardia (heart rate less than 45-50 beats / min);
• severe forms of Raynaud's disease and obliterating diseases of peripheral arteries;
• pheochromocytoma without simultaneous administration of alpha-blockers;
• arterial hypotension (systolic blood pressure <100 mm Hg);
• anaphylactic reactions in the anamnesis;
• metabolic acidosis;
• cardiomegaly (no signs of heart failure);
• simultaneous application with sultopride and floktaphenin;
• simultaneous administration of MAO inhibitors;
• children and adolescents under 18 years of age (efficacy and safety not established);
• deficiency of lactase, lactose intolerance, glucose-galactose malabsorption (due to the presence of lactose in the formulation);
• increased sensitivity to betaxolol and excipients of the drug.

 

Be wary of the drug:

• with bronchial asthma and chronic obstructive pulmonary disease of moderate course (start treatment with small doses and preferably under the control of the parameters of the function of external respiration, thanks to beta1-selectivity of betaxolol in the event of an attack of bronchial asthma on the background of its admission, it is possible to stop the attack with beta2-adrenomimetics);
• with chronic heart failure in the compensation stage (treatment with betaxolol is possible only under strict medical supervision, treatment should be started from very small doses with a gradual increase);
• with AV-blockade 1 degree (requires close monitoring, including ECG monitoring);
• with obliterating diseases of peripheral arteries, Reynaud's syndrome (with the exception of severe form) (peripheral circulatory disorders may be increased);
• with Prinzmetal angina pectoris (there may be an increase in angina attacks, the use of selective beta 1-blocker is possible only with the simultaneous use of vasodilators);
• with the treated pheochromocytoma (with Lokren's treatment of arterial hypertension on the background of the treated pheochromocytoma, careful monitoring of blood pressure indices is required);
• in elderly patients (treatment with small doses should be started and under careful medical supervision);
• with renal insufficiency (with QC more than 20 ml / min - careful monitoring of the patient during the first 4 days of treatment, with a CC less than 20 ml / min and / or hemodialysis requires a correction of the dosing regimen);
• with liver failure (requires more thorough clinical observation at the beginning of treatment);
• in patients with diabetes mellitus (regular monitoring of blood glucose concentration, including active self-control by the patient, at the beginning of treatment, it is possible to reduce the severity of precursors of hypoglycemia such as tachycardia, palpitations and increased sweating);
• at a psoriasis (beta-adrenoblockers can weight a current of a psoriasis);
• with desensitizing therapy.

 

Application in pregnancy and lactation

 

Pregnancy

 

In experimental studies, there was no teratogenic action of Lokren.To date, no teratogenic effects have been reported in humans.

 

As a rule, beta-adrenoblockers reduce blood flow in the placenta and can affect the development of the fetus. Blood flow in the placenta and uterus should be monitored, and the growth and development of the unborn child should be monitored, and alternative therapeutic measures taken if pregnancy and / or fetus are undesirable.

 

You should carefully examine the newborn after delivery. In the first 3-5 days of life, bradycardia symptoms of hypoglycemia may occur, since the action of beta-blockers in newborns whose mothers took them before childbirth persists for several days after birth. In the neonatal and postnatal period, newborns have an increased risk of cardiac and respiratory complications. In the case of heart failure, hospitalization of the newborn in the intensive care unit is required. Use of plasma substitutes (risk of developing acute pulmonary edema) should be avoided. Also reported on the development of bradycardia, respiratory failure and hypoglycemia.In this regard, during the first 3-5 days of life requires careful monitoring of such infants in a specialized compartment (heart rate, blood glucose concentration).

 

In this regard, use of the drug Lokren during pregnancy is not recommended and is possible only when the benefit to the mother outweighs the potential risk to the fetus or child.

 

Lactation period

 

Beta-blockers, including Lokren, are excreted in breast milk. The risk of hypoglycemia and bradycardia in infants has not been investigated, so as a precaution, breast-feeding during treatment should be discontinued.

 

Application in elderly patients

 

With caution apply the drug in the elderly (you should start treatment with small doses and under careful medical supervision).

 

Use in children

 

Contraindicated in children and adolescents under the age of 18 years (efficacy and safety not established).

 

special instructions

 

Do not interrupt Lokren's treatment abruptly and change the recommended dose without first consulting a physician, since this can lead to a temporary worsening of the heart.Treatment should not be interrupted suddenly, especially in patients with ischemic heart disease. sudden cancellation can lead to severe heart rhythm disturbances, myocardial infarction or cardiac arrest. The dose should be reduced gradually, that is, within 2 weeks, and, if necessary, it is possible to simultaneously start substitution therapy with another antianginal agent in order to avoid the increase in angina attacks.

 

In patients taking Lokren, heart and blood pressure should be monitored (at the beginning of treatment daily, then once every 3-4 months), the concentration of glucose in the blood in patients with diabetes mellitus (1 every 4-5 months), kidney function in elderly patients (1 time in 4-5 months).

 

The patient should be taught how to calculate heart rate, and the patient should be instructed to consult a doctor if the heart rate is less than 50 beats per minute.

 

Approximately in 20% of patients with angina pectoris beta-blockers are ineffective. The main causes are severe coronary atherosclerosis with a low threshold of ischemia (heart rate at the time of development of an anginal attack less than 100 beats / min) and increased end-diastolic pressure of the left ventricle, which disrupts subendocardial blood flow.

 

With the simultaneous administration of clonidine, his reception may be discontinued only a few days after the withdrawal of the drug Lokren.

 

Lokren should be discontinued before the study of the concentration of catecholamines, normetanephrine and vanillin-mandelic acid in blood and urine; as well as titers of antinuclear antibodies in the blood.

 

Bronchial asthma and chronic obstructive pulmonary disease

 

Beta-blockers may be prescribed only to patients with moderate disease severity, with the choice of a selective beta-blocker in a low initial dose. Before the start of treatment it is recommended to perform an evaluation of the function of breathing.

 

With the development of seizures during treatment, bronchodilators - beta2-adrenomimetics - can be used.

 

Heart failure

 

In patients with heart failure controlled therapeutically, if necessary, betaxolol can be used under strict medical supervision at very low initial doses with a gradual increase if necessary and in case of good tolerability (preservation of the compensated state of chronic heart failure).

 

Bradycardia

 

If the heart rate at rest becomes less than 50-55 bpm, the dose of Lokren should be reduced.

 

AV-blockade of 1 degree

 

Given the negative dromotropic effect of beta-blockers, with blockade of 1 degree the drug should be used with caution.

 

Angina pectoris

 

Beta-adrenoblockers can increase the frequency and duration of seizures in patients with Prinzmetal angina pectoris. The use of cardioselective beta1-adrenoblockers is possible with mild severity of Prinzmetal angina or mixed-type angina pectoris, provided that the treatment is performed in combination with vasodilators.

 

Violations of peripheral circulation

 

Beta-blockers can lead to worsening of patients with impaired peripheral circulation (Raynaud's disease or Raynaud's syndrome, arteritis or chronic obliterating diseases of lower limb arteries).

 

Pheochromocytoma

 

In the case of using beta-adrenoblockers in the treatment of arterial hypertension caused by pheochromocytoma, careful monitoring of blood pressure is required. The purpose of the drug Lokren is possible only against the background of the use of alpha-blockers.

 

Elderly patients

 

Treatment of elderly patients should start with a small dose and under strict supervision.

 

Patients with renal insufficiency

 

The dose should be adjusted depending on the concentration of creatinine in the blood or QC.

 

Patients with diabetes mellitus

 

It is necessary to warn the patient about the need to strengthen the control of blood glucose concentration, including active self-control by the patient, at the beginning of treatment. The patient should be aware that the initial symptoms of hypoglycemia (especially tachycardia, palpitation and sweating) can be masked with betaxolol.

 

Psoriasis

 

It requires a careful assessment of the need for the drug, since there are reports of a heavier psoriasis during treatment with beta-blockers.

 

Allergic reactions

 

Beta-adrenoblockers, including Lokren, can increase sensitivity to allergens and severity of anaphylactic reactions due to weakening of adrenergic compensatory regulation under the action of beta-adrenoblockers. Therapy of anaphylactic reactions with epinephrine (adrenaline) does not always produce the expected therapeutic effect.

 

In patients prone to severe anaphylactic reactions, especially those associated with the use of floktaphenin or during desensitization, beta-blocker therapy may lead to further intensification of reactions and a decrease in the effectiveness of treatment.

 

General anesthesia

 

In the conduct of general anesthesia, the risk of blockade of beta-adrenergic receptors (a decrease in heart rate, a reduction in cardiac output, a decrease in systolic and diastolic blood pressure) should be considered.

 

Beta-adrenoblockers mask reflex tachycardia and increase the risk of developing arterial hypotension. Continuation of beta-blocker therapy reduces the risk of arrhythmia, myocardial ischemia and hypertensive crises. An anesthesiologist should be informed that the patient is receiving treatment with beta-blockers.

 

If it is necessary to discontinue therapy with Lokren before surgery, it should be done gradually and completed 48 hours before the general anesthesia, because it is believed that stopping the therapy for 48 h allows you to restore the sensitivity of the receptors to catecholamines.

 

Therapy with beta-blockers in some cases may not be interrupted:

• in patients with coronary insufficiency, it is desirable to continue treatment up to surgical intervention, taking into account the risk associated with the sudden abolition of beta-blockers;
• in the case of emergency surgical interventions or in cases where cessation of treatment is not possible, the patient should be protected from the effects of excitation of the vagus nerve by appropriate premedication with atropine, with repetition if necessary.

 

In such patients, for general anesthesia, it is necessary to use substances that are least depressing myocardium, and blood loss should be replenished.

 

The risk of developing anaphylactic reactions should be considered.

 

Thyrotoxicosis

 

Symptoms of thyrotoxicosis can be masked by therapy with beta-blockers.

 

Athletes

 

Athletes should consider that the drug contains an active substance, which can give a positive reaction when performing doping tests.

 

For the duration of treatment should be excluded from drinking alcohol.

 

Patients who use contact lenses should take into account that against the background of treatment with beta-blockers may reduce the production of tear fluid.

 

In smoking patients, the effectiveness of beta-blockers is lower.

 

Impact on ability to drive vehicles and engage in other potentially hazardous activities

 

When driving vehicles or engaging in other potentially hazardous activities with Lokren, caution should be exercised (due to the risk of dizziness, weakness, which may reduce the attention and speed of the psychomotor reactions required for these activities).

 

Drug Interactions

 

Contraindicated combinations

 

With floktaphenin

 

In the case of shock or arterial hypotension caused by floktaphenin, beta-adrenoblockers cause a decrease in compensatory cardiovascular reactions.

 

With sultopride

 

Violations of the automatism of the heart (pronounced bradycardia) due to an additional reduction in heart rate.

 

Not recommended combinations

 

With amiodarone

 

Violations of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms).

 

With blockers of slow calcium channels (beprideal, diltiazem and verapamil)

 

Violations of automatism (pronounced bradycardia, stopping the sinus node), violations of AV-conduction, heart failure (synergistic (mutually amplifying) effects).

 

This combination can be used only under close clinical and ECG observation, especially in elderly patients or at the beginning of treatment.

 

With cardiac glycosides

 

The risk of developing or worsening bradycardia, AV blockade, cardiac arrest.

 

With MAO inhibitors

 

It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive action of betaxolol, a break in treatment between taking MAO inhibitors and betaxolol should be at least 14 days.

 

With iodine-containing contrast agents

 

In the case of shock or a sharp decrease in blood pressure when Iodine containing contrast agents, beta-adrenoblockers reduce compensatory cardiovascular reactions. If possible, before the X-ray examination using iodine-containing contrast agents, treatment with beta-blocker should be discontinued.

 

Combinations that should be used with caution

 

With inhaled halogenated anesthetics

 

Beta-adrenoblockers have cardiodepressant action (inhibition of beta-adrenergic receptors can be reduced by the introduction of beta-adrenostimulants). As a rule, treatment with beta-blockers does not stop and in any case, abrupt withdrawal of beta-blockers should be avoided. An anesthesiologist should be informed of the use of the beta-blocker.

 

With drugs that can cause ventricular arrhythmias, including ventricular pirouette tachycardia: antiarrhythmic drugs of class 1 A (quinidine, hydroquinidine and disopyramide) and class 3 (amiodarone, dofetilide, ibutilide), sotalol, some neuroleptics from the phenothiazine group (chlorpromazine , tsiammazin, levomepromazine, thioridazine), benzamides (amisulpride, sulpiride, tiaprid), butyrophenones (droperidol, haloperidol), other antipsychotics (pimozide) and other drugs (cisapride, difemanyl, intravenously administered erythromycin, halophant rin, misolastine, moxifloxacin, pentamidine, intravenous spiramycin, and intravenously administered vincamine

 

Increased risk of ventricular arrhythmias, in particular ventricular pirouette tachycardia. Clinical and ECG monitoring is required.

 

With propaphenone

 

Violations of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms). Clinical and ECG monitoring is required.

 

With baclofen

 

Strengthening the antihypertensive action of Lokren. It is necessary to monitor blood pressure and dose correction of betaxolol in case of need.

 

With insulin and hypoglycemic agents for oral administration, derivatives of sulfonylureas

 

All beta-blockers can mask certain symptoms of hypoglycemia, such as palpitations and tachycardia. The patient should be warned about the need to strengthen regular monitoring of blood glucose concentration, including active self-monitoring by the patient, especially at the beginning of treatment.

 

With cholinesterase inhibitors (ambenomium, donepezil, galantamine, neostigmine, pyridostigmine, rivastigmine, tacrine)

 

Risk of increased bradycardia (additive effect). Regular clinical control is required.

 

With antihypertensive agents of central action (clonidine, apraklonidine, alpha-methyldopa, guanfacin, moxonidine, rilmenidine)

 

Increased risk of bradycardia, violation of AV-conduction.A significant increase in BP with a sharp reversal of the antihypertensive agent of central action. It is necessary to avoid a sharp abolition of the antihypertensive agent and to carry out clinical control.

 

With Lidocaine 10% solution (intravenously as an antiarrhythmic agent)

 

An increase in the concentration of lidocaine in the blood plasma with a possible increase in unwanted neurological symptoms and effects on the part of the cardiovascular system (a decrease in the metabolism of lidocaine in the liver). Clinical and ECG observation is recommended and, probably, control of lidocaine concentration in blood plasma during treatment with beta-blockers and after its termination. If necessary, adjust the dose of lidocaine.

 

Combinations that should be taken into account

 

With non-steroidal anti-inflammatory drugs (NSAIDs) (drugs with systemic action), including selective inhibitors of COX-2

 

Reduction of antihypertensive effect of betaxolol (oppression of prostaglandin synthesis of NSAIDs and retention of water and sodium with pyrazolone derivatives).

 

With blockers of slow calcium channels from the dihydropyridine group

 

Mutual enhancement of the antihypertensive effect of slow calcium channel blockers and betaxolol, the development of heart failure in patients with latent congestive heart failure or uncontrolled heart failure. Treatment with beta-adrenoblockers can minimize reflex activation of the sympathetic nervous system in response to vasodilation due to slow calcium channel blockers from the dihydropyridine group.

 

With tricyclic antidepressants (such as imipramine), antipsychotics

 

Increased antihypertensive effect of betaxolol and the risk of orthostatic hypotension (additive effect).

 

With mefloquine

 

Risk of bradycardia (additive effect).

 

With Dipyridamole (intravenous administration)

 

Strengthening of the antihypertensive effect of Lokren.

 

With alpha-adrenoblockers, including those used in urology (alfuzosin, doxazosin, prazosin, tamsulosin, terazosin)

 

Increased antihypertensive effect of betaxolol. Increased risk of orthostatic hypotension.

 

With amifostine

 

Increased antihypertensive effect of betaxolol.

 

With allergens used for immunotherapy or allergen extracts for skin tests

 

Increased risk of severe systemic allergic reactions or anaphylaxis in patients receiving betaxolol.

 

With phenytoin (intravenous administration)

 

Increased severity of cardiodepressive action and the likelihood of lowering blood pressure.

 

With xanthines

 

Betaxolol reduces the clearance of xanthines (except diphylline) and increases their concentration in the blood plasma, especially in patients with initially elevated clearance of theophylline (for example, under the influence of smoking).

 

With estrogens

 

Weakening of the antihypertensive effect of betaxolol (sodium and water retention).

 

With glucocorticosteroids (GCS) and tetracosactide

 

Weakening of the antihypertensive effect of Lokren (sodium and water retention).

 

With diuretics

 

There may be an excessive decrease in blood pressure.

 

With nondepolarizing muscle relaxants

 

Betaxolol prolongs the action of nondepolarizing muscle relaxants.

 

With coumarins

 

Strengthening the anticoagulant effect of coumarins.

 

With alcohol (ethanol), sedatives and hypnotic drugs

 

Increased oppression of the central nervous system.

 

With unhydrogenated ergot alkaloids

 

Unhydrated ergot alkaloids increase the risk of peripheral circulatory disturbances when taking betaxolol.

 

Analogues of Lokren

 

Structural analogs for the active substance:

• Betak;
• Betaxolol;
• Betalmic;
• Betoptik;
• Betofan;
• Xoneuf;
• Optibetol.

 

Analogues for the pharmacological group (beta-blockers):

• Anaprilin;
• Aritel;
• Arutimol;
• Atenolol;
• Betalk;
• Biol;
• Bisocardium;
• Bisoprolol;
• Vasocardine;
• Darub;
• Concor;
• Corvitol;
• Korgard;
• Cordinorm;
• Coronale;
• Xoneuf;
• Metocard;
• Metoprolol;
• Nebivolol;
• Non-ticket;
• Niebelong;
• Niperten;
• Obsidan;
• Propranolol;
• SotaGexal;
• Sotaleks;
• Sotalol;
• Tenoric;
• Timolol;
• Timothy;
• Fotil;
• Fotil forte;
• Egilok;
• Egilok Retard;
• Amzok;
• Estecor.

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