Lokren, 20mg pills, 28pcs

Composition

1 coated tablet contains:

Betaxolol hydrochloride 20 mg,

Auxiliary substances:

lactose monohydrate,

sodium amylopectin glycolate,

microcrystalline cellulose,

colloidal anhydrous silicon dioxide,

magnesium stearate,

hypromellose,

macrogol 400,

titanium dioxide (E 171).

Pharmacological action

Locren is a selective beta-1-adrenoblocker with no intrinsic sympathomimetic activity.

In high doses (at concentrations exceeding therapeutic ones), it has a weakly expressed membrane-stabilizing effect.

Indications

-Arterial hypertension. – Prevention of angina attacks of tension.

Use during pregnancy and lactation

No teratogenic effects of Locren were detected in experimental animal studies. To date, no teratogenic effects have been observed in humans, and no congenital malformations have been observed in controlled prospective studies.

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.

Betaxolol is slightly excreted in breast milk. The child’s risk of hypoglycemia or bradycardia has not been studied. If it is necessary to use Locren during lactation, the question of stopping breastfeeding should be decided.

It was found that betaxolol has an effect on the fetus (intrauterine growth retardation, hypoglycemia, bradycardia). With the development of heart failure (decompensation) in newborns whose mothers took beta-blockers during pregnancy, they are hospitalized in the ICU; glucagon is prescribed at the rate of 0.3 mg / kg; isoprenaline and dobutamine are usually in sufficiently high doses and for a long time, which requires careful monitoring.

It should be borne in mind that in newborns whose mothers received beta-blockers, the effect of the latter persists for several days after birth. Although this residual effect may not have clinical consequences, it is nevertheless possible to develop a heart defect that requires intensive care of the newborn. In this situation, the use of solutions that increase BCC (risk of acute pulmonary edema) should be avoided. Bradycardia, respiratory distress syndrome, and hypoglycemia have also been reported. Therefore, careful monitoring of newborns in specialized settings (monitoring of heart rate and blood glucose levels during the first 3-5 days of life) is recommended.

Contraindications

-Chronic heart failure of II B-III stages. – Cardiogenic shock. – AV block of II and III degrees (without connecting an artificial pacemaker). – Prinzmetal’s angina pectoris. – SSS (including sinoatrial blockade). – Severe bradycardia. – Arterial hypotension. – Cardiomegaly (without signs of heart failure). – Simultaneous use with sultoprid and floctafenin. – Simultaneous use of MAO inhibitors. – Age up to 18 years (efficacy and safety have not been established). – Hypersensitivity to betaxolol. – The drug is contraindicated in cases of congenital galactosemia, glucose/galactose malabsorption or lactase deficiency (since it contains lactose).

The drug is used with caution in patients with a history of allergic reactions, pheochromocytoma, metabolic acidosis, obliterating peripheral vascular diseases (intermittent claudication, Raynaud’s syndrome), liver failure, chronic renal failure, hemodialysis, myasthenia gravis, depression (including in the anamnesis), in the elderly, with grade I AV block, with chronic obstructive pulmonary disease (bronchial obstruction). asthma, emphysema), in patients with psoriasis, chronic heart failure, thyrotoxicosis, diabetes mellitus.

Side effects

From the central nervous system and peripheral nervous system: increased fatigue, weakness, dizziness, headache, drowsiness, insomnia, nightmares, depression, anxiety, confusion or short-term memory loss, hallucinations, asthenic syndrome, muscle weakness, paresthesia in the extremities (with intermittent claudication, Raynaud’s syndrome), tremor.

From the cardiovascular system: sinus bradycardia, palpitations, orthostatic hypotension, impaired myocardial conduction, AV block (up to cardiac arrest), arrhythmias, weakening of myocardial contractility, development (or aggravation) of symptoms of heart failure (swelling of the ankles, feet, shins), marked decrease in blood pressure, manifestation of angiospasm (decreased peripheral circulation, cold of the lower extremities, Raynaud’s syndrome), back pain breasts.

From the digestive system: dryness of the oral mucosa, nausea, vomiting, abdominal pain, constipation or diarrhea, liver function disorders (dark urine, jaundice of the sclera or skin, cholestasis), taste changes.

From the respiratory system: nasal congestion, difficulty breathing when prescribed in high doses (loss of selectivity); laryngo-and bronchospasm (in predisposed patients).

From the sensory organs: visual disturbances, decreased secretion of the lacrimal gland, dry and painful eyes, conjunctivitis.

From the endocrine system: hyperglycemia in patients with non-insulin-dependent diabetes mellitus, hypoglycemia in patients receiving insulin, hypothyroidism.

Dermatological reactions: increased sweating, hyperemia of the skin, exanthema, psoriasis-like skin reactions, exacerbation of the course of psoriasis.

Allergic reactions: skin rash, pruritus, urticaria.

Others: back pain, arthralgia, decreased libido, decreased potency, withdrawal syndrome (increased angina attacks, increased blood pressure); rarely-the appearance of antinuclear antibodies (only in exceptional cases accompanied by clinical manifestations such as SLE, which pass when treatment is discontinued).

Interaction

Many medications can cause bradycardia. This group includes beta-blockers, Class IA antiarrhythmic drugs (quinidine, disopyramide), amiodarone and sotalol from Class III antiarrhythmic drugs, diltiazem and verapamil from Class IV, as well as digitalis glycosides, clonidine, guanfacine, mefloquine and cholinesterase inhibitors indicated for the treatment of Alzheimer’s disease.

Contraindicated combinations When used concomitantly with floctafenin (in case of shock or arterial hypotension caused by floctafenin), beta-blockers may lead to a decrease in compensatory reactions from the cardiovascular system. When used concomitantly with sultoprid, severe bradycardia develops (additive effect).

Combinations that should be avoided When used concomitantly with calcium channel blockers (bepridil, diltiazem and verapamil), there are violations of automatism (severe bradycardia, sinus node arrest), AV conduction disorders, heart failure (synergism). This combination can only be used under close clinical supervision and ECG monitoring (especially in the elderly or at the beginning of therapy). When used concomitantly with amiodarone, it is possible to develop disorders of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms).

Combinations that should be used with caution When using halogen-containing inhaled agents for general anesthesia, it should be taken into account that during surgery, the effect of blockade ?- adrenergic receptors can be eliminated by beta-adrenostimulants. As a rule, beta-blocker therapy should not be discontinued, and abrupt discontinuation of the drug should be avoided in any case. The anesthesiologist should be informed about the treatment being performed. When used concomitantly with Locren, antiarrhythmic drugs of class IA (quinidine, hydroquinidine and disopyramide) and class III (amiodarone, dofetilide, ibutilide, sotalol), some neuroleptics from the phenothiazine group (chlorpromazine, cyamemazine, levomepromazine, thioridazine), benzamides (amisulpride, sulpiride, tiapride), butyrophenones (droperidol, haloperidol), other neuroleptics (pimozide), as well as cisapride, difemanil, erythromycin (for intravenous use), halofantrin, mizolastine, moxifloxacin, pentamidine, spiramycin (for intravenous use) and vincamine (for intravenous use) may increase the risk of ventricular arrhythmia, especially the “pirouette” type (if necessary, combination therapy requires monitoring clinical condition and ECG). When used concomitantly with propafenone, it is possible to develop contractility, automatism and conduction disorders (due to the suppression of sympathetic compensatory mechanisms), which requires monitoring of the clinical condition and ECG. When combined with baclofen, it is possible to increase the antihypertensive effect (blood pressure monitoring and dose adjustment are necessary if necessary). When combined with insulin and oral hypoglycemic agents-sulfonylureas, it should be borne in mind that all beta-blockers can mask the symptoms of hypoglycemia (palpitation and tachycardia). The patient should be warned about the need to increase blood glucose control, especially at the beginning of treatment. Concomitant use with cholinesterase inhibitors (donepezil, galantamine, ambenonium chloride, neostigmine, pyridostigmine, rivastigmine, tacrine) may increase the risk of developing bradycardia (additive effect), which requires monitoring of the clinical condition.When combined with antihypertensive agents of central action (clonidine, apraclonidine, alpha-methyldopa, guanfacine, moxonidine, rilmenidine), a significant increase in blood pressure may occur with abrupt withdrawal of a centrally acting antihypertensive drug (it is necessary to avoid abrupt withdrawal of an antihypertensive agent and monitor the clinical condition). Intravenous lidocaine use may increase the plasma lidocaine concentration with a possible increase in undesirable neurological symptoms and effects from the cardiovascular system (decreased liver lidocaine metabolism), which requires monitoring of the clinical condition and ECG and, possibly, monitoring the plasma lidocaine concentration during treatment with beta-blockers and after its termination. If necessary, adjust the dose of lidocaine.

Combinations that should be taken into account When used concomitantly with NSAIDs for systemic use (including selective COX-2 inhibitors), it is possible to reduce the hypotensive effect (inhibition of prostaglandin synthesis and water and sodium retention). When used concomitantly with calcium channel blockers, arterial hypotension and circulatory insufficiency may develop in patients with latent or uncontrolled heart failure. Treatment with beta-blockers may minimize reflex sympathetic mechanisms. When combined with tricyclic antidepressants (such as imipramine), neuroleptics may increase the hypotensive effect and increase the risk of orthostatic hypotension (additive effect). When used concomitantly with mefloquine, the risk of developing bradycardia increases (additive effect). When combined with dipyridamole (for intravenous use), it is possible to increase the antihypertensive effect. When co-administered with alpha-blockers used in urology (alfuzosin, doxazosin, prazosin, tamsulosin, terazosin), the antihypertensive effect increases and the risk of orthostatic hypotension increases. When combined with amifostin, the antihypertensive effect may be enhanced. Allergens used for immunotherapy, or allergen extracts for skin tests, increase the risk of severe systemic allergic reactions or anaphylaxis in patients receiving betaxolol. Phenytoin when administered intravenously increases the severity of cardiodepressive effects and the likelihood of lowering blood pressure in patients taking betaxolol. When used together, betaxolol reduces the clearance of xanthines (except diphylline) and increases their concentration in blood plasma, especially in patients with an initially increased clearance of theophylline (for example, under the influence of smoking). The hypotensive effect of betaxolol is weakened by estrogens (sodium retention). When combined with betaxolol, cardiac glycosides, methyldopa, reserpine, and guanfacine increase the risk of developing or worsening bradycardia, AV block, and cardiac arrest. When combined with betaxolol, nifedipine, diuretics, clonidine, sympatholytics, hydralazine and other antihypertensive drugs can lead to a significant decrease in blood pressure. When used together, betaxolol prolongs the duration of action of non-depolarizing muscle relaxants and enhances the anticoagulant effect of coumarins. When combined with betaxolol, ethanol, sedatives and hypnotic drugs increase the suppression of the central nervous system. Concomitant use with MAO inhibitors is not recommended due to a significant increase in the antihypertensive effect, a break in treatment between taking MAO inhibitors and betaxolol should be at least 14 days. When combined with betaxolol, non-hydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders.

How to take, course of use and dosage

The average therapeutic dose is 20 mg (1 tab. ) 1 time/day.

When stopping treatment, it is recommended to gradually reduce the dose for 1-2 weeks, especially in patients with CHD, in order to prevent the development of withdrawal syndrome (due to secondary activation of the sympathetic nervous system).

Tablets are taken orally without chewing and washed down with a sufficient amount of liquid.

In patients with impaired renal function and creatinine clearance (creatinine clearance) of 20 ml/min or more, as well as in patients with hepatic insufficiency, no adjustment of the daily dose of Locren is required. However, at the beginning of treatment, it is recommended to conduct clinical monitoring until the equilibrium concentrations of the drug in blood plasma are reached (on average,4 days).

For patients with severe renal insufficiency (creatinine clearance less than 20 ml/min) and undergoing hemodialysis, the recommended initial dose of Locren is 5 mg / day, regardless of the frequency and time of hemodialysis sessions.

Overdose

Symptoms: Severe bradycardia, Dizziness, Marked decrease in blood pressure, Arrhythmias, ventricular extrasystole, AV block, Syncope, Heart failure, Difficulty breathing, bronchospasm, Cyanosis of the fingernails and palms, Convulsions.

Special instructions

Use with caution in patients with hepatic insufficiency.

Use with caution in patients with chronic renal failure, during hemodialysis. In patients with renal insufficiency, the dose should be adjusted depending on the concentration of creatinine in the blood or creatinine clearance ( CC ).

Treatment of patients with angina should never be abruptly interrupted, as sudden withdrawal can lead to severe cardiac arrhythmias, myocardial infarction, or sudden death.

Patients taking Locren need monitoring, which should include monitoring of heart rate and blood pressure (at the beginning of treatment daily, then 1 time in 3-4 months), glucose content in patients with diabetes mellitus (1 time in 4-5 months), monitoring of renal function in elderly patients (1 time in 4-5 months). The patient should be trained in the method of calculating heart rate and instructed about the need for medical consultation if the heart rate is less than 50 beats/min.

In patients with CHD, the dose should be reduced gradually (over 1-2 weeks) and, if necessary, replacement therapy should be initiated simultaneously to avoid angina progression. Beta-blockers are ineffective in approximately 20% of patients with angina pectoris (the main causes are severe coronary atherosclerosis with a low threshold of ischemia and heart rate at the time of anginal attack development less than 100 beats / min and increased end-diastolic pressure of the left ventricle, which disrupts subendocardial blood flow).

With simultaneous therapy with clonidine, its use can be stopped only a few days after the withdrawal of Locren.

Locren should be discontinued before testing the content of blood and urine catecholamines ( catecholamines in the blood, catecholamines in the urine ), normetanephrine (normetanephrine free in the urine) and vanillinmindalic acid; titers of antinuclear antibodies.

In bronchial asthma and chronic obstructive pulmonary disease, beta-blockers can be prescribed only for moderate-severity diseases, with the choice of a selective beta-blocker at a low initial dose. Before starting treatment, it is recommended to evaluate the respiratory function. If seizures develop during treatment, you can use bronchodilators (? 2-adrenomimetics).

In patients with therapeutically controlled heart failure, if necessary, betaxolol can be used in very low, gradually increasing doses under strict medical supervision.

The dose of the drug should be reduced if the resting heart rate is below 50-55 beats / min and the patient has clinical manifestations of bradycardia.

Given the negative dromotropic effect of beta-blockers, the drug should be used with caution in patients with grade I AV blockade.

Beta-blockers may increase the number and duration of attacks in Prinzmetal angina. Use of cardioselective drugs ? 1-adrenoblockers are possible in less severe and mixed forms, provided that the treatment is carried out in combination with vasodilators.

Beta-blockers may worsen the condition of patients with peripheral circulatory disorders (Raynaud’s disease or syndrome, arteritis, or chronic obliterating diseases of the lower extremities).

When using beta-blockers for the treatment of arterial hypertension caused by pheochromocytoma, careful monitoring of blood pressure is required.

Patients with diabetes should be warned about the need to strengthen self-monitoring of blood glucose levels at the beginning of treatment. The initial symptoms of hypoglycemia can be masked, especially tachycardia, palpitations, and sweating.

In psoriasis, careful evaluation of the need for prescribing the drug is required, since there are reports of worsening of the disease during treatment with beta-blockers.

In patients with a predisposition to severe anaphylactic reactions (especially those associated with the use of floctafenin or during desensitization), beta-blocker therapy may lead to a further increase in reactions and reduce the effectiveness of treatment. When using the drug, the risk of anaphylactic reactions should be taken into account.

When performing general anesthesia, it should be taken into account that beta-blockers mask reflex tachycardia and increase the risk of hypotension. Continued beta-blocker therapy reduces the risk of arrhythmia, myocardial ischemia, and hypertensive crises. The anaesthetist should be informed that the patient has been treated with beta-blockers.

In case of elective surgery and the need to stop therapy with the drug, it should be taken into account that discontinuation of the drug for 48 hours allows you to restore sensitivity to catecholamines.Beta-blocker therapy should not be interrupted in patients with coronary insufficiency, it is recommended to continue treatment until surgery, given the risk associated with sudden withdrawal of beta-blockers. In case of emergency operations or in cases where discontinuation of treatment is impossible, the patient should be protected from the effects of vagus nerve excitation by appropriate premedication with atropine (repeated if necessary). For general anesthesia, it is necessary to use drugs with minimal negative inotropic effect.

Symptoms of thyrotoxicosis may be masked by beta-blocker therapy.

Athletes should take into account that the drug may give a positive reaction during doping control tests.

When using the drug, the use of alcohol should be excluded.

Patients who use contact lenses should take into account that during treatment, a decrease in tear fluid is possible.

In smokers, the effectiveness of beta-blockers is lower.

Treatment of elderly patients should be started with a low dose and under strict supervision.

The drug should not be used in children, because there are no clinical data on the effectiveness and safety of its use in this category of patients.

Form of production

Coated tablets.

Storage conditions

Store at temperatures below 25 °C out of the reach of children.

Shelf

life is 5 years.

Active ingredient

Betaxolol

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Hypertension, Angina