Lokren

Lokren – the selection _{beta1-adrenoblocker}.

Form of release and structure

Dosage form – tablets, film coated: a round biconvex form, white color, with an engraving of "KE 20" on one party and dividing risky – on another (on 14 pieces in blisters, in a cardboard pack 1 blister).

Active agent of Lokren – a betaksolol a hydrochloride, in 1 tablet – 20 mg.

Auxiliary components: cellulose microcrystallic, lactoses monohydrate, sodium carboxymethylstarch (type A), magnesium stearate, silicon dioxide colloid.

Structure of a film cover: macrogoal 400, gipromelloza, titanium dioxide (E171).

Indications to use

• Monotherapy and the combined treatment of arterial hypertension;
• Prevention of attacks of an angina of exertion (at monotherapy or the combined treatment).

Contraindications

• Cardiogenic shock;
• Acute heart failure;
• Cardiomegaly (in the absence of symptoms of heart failure);
• Chronic heart failure in a decompensation stage (at inefficient therapy by inotropic means, diuretics, inhibitors of an angiotensin-converting enzyme and other vazodilatator);
• Atrioventricular (AV) blockade of II and III degrees (without artificial pacemaker);
• The Sick Sinus Syndrome (SSS), including sinuatrial blockade;
• Arterial hypotension (the systolic arterial pressure (AP) is less than 100 mm of a mercury column);
• Severe form of bradycardia (the heart rate (HR) is less than 45-50 beats per minute);
• Monotherapy of stenocardia of Printsmetal;
• Severe form of obliterating pathologies of peripheral arteries and Raynaud's disease;
• Severe form of a chronic obstructive pulmonary disease and bronchial asthma;
• Metabolic acidosis;
• Pheochromocytoma in the absence of simultaneous use of alpha adrenoblockers;
• Simultaneous use with sultopridy, floktafeniny, monoamine oxidase inhibitors;
• Lactose intolerance, deficit of lactase, glyukozo-galaktozny malabsorption;
• Age up to 18 years;
• Breastfeeding period;
• Anaphylactic reactions in the anamnesis;
• Hypersensitivity to drug components.

With care Lokren to patients with chronic heart failure in compensation stage, AV blockade of the I degree, not severe forms of obliterating diseases of peripheral arteries and Reynaud's syndrome, Printsmetal's stenocardia (only in combination with vazodilatator), bronchial asthma and a chronic obstructive pulmonary disease at moderately severe is recommended to appoint diseases, the patient with a treated pheochromocytoma, a liver and/or renal failure, a diabetes mellitus, psoriasis, when performing the desensibilizing treatment and at therapy of patients of advanced age.

Lokren during pregnancy and feeding is not recommended to appoint a breast, except cases when the estimated advantage of therapy for mother exceeds potential threat for health of a fruit or the child.

Route of administration and dosage

Pill is taken inside, without chewing, washing down with a small amount of liquid.

The recommended daily dosing for each clinical indication: 10 mg or ½ tablets. If after 7-14 days of use of an initial dose it is not possible to reach the ABP target value, then the dose should be brought to 20 mg.

Appointing a daily dose usually do not exceed 20 mg, maximum makes 40 mg a day.

Patients with a renal failure should make appointment taking into account a functional condition of kidneys. At the clearance of creatinine (CC) more than 20 ml/min. Lokren are appointed in the recommended dose, but at the beginning of therapy (the first 4-7 days) it is regularly necessary to make clinical observation until the level of concentration of a betaksolol in blood reaches balance.

At KK less than 20 ml/min. the initial daily dose makes 5 mg, including patients on a hemodialysis. For achievement of clinical performance increase in a dose each 1-2 weeks twice, but no more than 20 mg a day is allowed.

At a liver failure drug is appointed in a usual dose, but careful clinical observation of the patient is necessary.

Side effects

• Cardiovascular system: often – bradycardia (including in a severe form), decrease in temperature of skin of upper and lower extremities; seldom – development or aggravation of symptoms of heart failure (puffiness of feet, anklebones, shins), manifestations of a vasomotor spasm: strengthening of disturbances of peripheric circulation (the alternating lameness), Reynaud's syndrome, increase of attacks of stenocardia, AV conductivity delay, strong decrease in the ABP;
• Nervous system: often – sleeplessness, a headache, dizziness, an adynamy; seldom – a depression; very seldom – nightmares, hallucinations, paresthesia, confusion of consciousness;
• Alimentary system: often – nausea, vomiting, a gastralgia, diarrhea;
• Organ of sight: seldom – decrease in intraocular pressure, a xerophthalmus; very seldom – vision disorders;
• Metabolism: very seldom – a hyperglycemia, a hypoglycemia;
• Respiratory system: seldom – a bronchospasm;
• Laboratory indicators: seldom – the emergence of antinuclear antibodies which in exceptional cases is followed by passing clinical signs of a volchanochnopodobny syndrome;
• Dermatological reactions: seldom – skin rash, an itch, a small tortoiseshell, an exacerbation of psoriasis or psoriazopodobny rashes;
• Generative organs: often – impotence;
• Influence on a fruit: hypoglycemia, fruit growth inhibition, bradycardia;
• Allergic reactions: skin rash, itch, small tortoiseshell;
• Others: withdrawal (increase in the ABP, increase or strengthening of attacks of stenocardia).

Special instructions

Cancellation or change of a dose of Lokren should be made only after consultation of the doctor, doing it gradually not to cause temporary deterioration in action of the heart in the form of increase in frequency of attacks of stenocardia. The dose decline is reached within 2 weeks, with co-administration of replacement anti-anginal therapy. Sharp interruption of treatment with coronary heart disease can cause heavy disturbances of a cordial rhythm, a myocardial infarction or a cardiac standstill in patients.

In an initiation of treatment patients daily should control the ABP and ChSS, then – at least 1 time in 3-4 months. Besides, 1 time in 4-5 months at patients with a diabetes mellitus it is necessary to check the level of concentration of glucose in blood, and at patients of advanced age – function of kidneys.

Patients have to be trained in independent calculation of ChSS and remember that in case of ChSS lower than 50 beats per minute it is necessary to see a doctor immediately.

Inefficiency of use of beta adrenoblockers is noted at 1/5 patients with stenocardia because of heavy coronary atherosclerosis with a low threshold of ischemia (with ChSS less than 100 beats per minute at the beginning of development of an anginal attack) and the increased final diastolic pressure of the left ventricle breaking a subendocardial blood stream.

Administration of drug should be cancelled temporarily at a planned research of credits of antinuclear antibodies in blood or the level of concentration of a normetanefrin, vanilinmindalny acid and catecholamines in blood and urine.

Use of a clonidine can be stopped only after Lokren's cancellation, several days later.

Purpose of drug the patient with bronchial asthma and a chronic obstructive pulmonary disease is possible at moderate severity of a disease and after evaluating function of breath. Treatment should be begun with small doses, _{beta1-selectivity} of a betaksolol allows to stop the arising attacks of bronchial asthma reception _{of beta2-adrenomimetik}.

Therapeutic controlled heart failure needs to carry out treatment under strict observation of the doctor since low doses. At preservation of chronic heart failure in the compensated state perhaps gradual increase in a dose.

At bradycardia with ChSS at rest lower than 50-55 beats per minute it is necessary to lower a drug dose.

The careful observation including control of the electrocardiogram of the patient at AV blockade of the I degree is required.

Lokren's use at Printsmetal's stenocardia can cause increase of attacks of stenocardia therefore it is recommended to appoint drug only at treatment of easy degree of pathology or stenocardia of the mixed type in combination with vazodilatator.

At disturbance of peripheric circulation reception of a betaksolol can cause an aggravation of symptoms of the patient.

Purpose of drug at arterial hypertension against the background of a pheochromocytoma demands simultaneous use of alpha adrenoblockers and control of the ABP.

Treatment of patients of advanced age is begun with purpose of a low dose under strict control of the doctor.

Correction of dosing for patients with a renal failure depends on KK or the level of concentration of creatinine in a blood plasma.

With caution it is necessary to take drug a sick diabetes mellitus, especially in an initiation of treatment as decrease in expressiveness of symptoms of a hypoglycemia is possible. The patient needs to control regularly concentration of glucose in blood.

Effect of beta adrenoblockers aggravates the course of psoriasis.

At treatment of patients inclined to anaphylactic reactions, especially against the background of a floktafenin or performing desensitization, it is necessary to consider Lokren's property to raise a susceptibility to allergens and weight of anaphylactic reactions. Use of Epinephrinum (adrenaline) for treatment of anaphylactic reactions not always is clinically effective.

When carrying out surgery using the general anesthesia it is necessary to report to the anesthesiologist about reception by the patient of beta adrenoblockers. In need of drug withdrawal, it is recommended to do it gradually, having completed reception of medicine in 48 hours prior to the beginning of anesthesia.

In case of the emergency operative measure, impossibility of cancellation of a betaksolol or operation at patients with coronary insufficiency to the patient appoint the corresponding premedication atropine, without interrupting reception of a betaksolol. The general anesthesia at this category of patients has to include substances with easy extent of oppression of a myocardium. During operation it is necessary to fill blood losses and to consider risk of anaphylactic reactions.

Beta adrenoblockers can mask thyrotoxicosis symptoms.

During treatment the use of alcoholic beverages is contraindicated.

Patients with contact lenses have to consider possible decrease in production of the lacrimal liquid against the background of therapy.

The clinical effect of beta adrenoblockers at the smoking patients is lower.

Betaksolol when carrying out tests of doping control at athletes can give positive reaction.

Due to the risk of development of side effects of drug in the form of weakness and dizziness, it is necessary to be careful at control of vehicles and mechanisms.

Medicinal interaction

With other medicines only the attending physician on the basis of clinical testimonies and the accompanying pathologies of the patient can define a possibility of simultaneous use of Lokren.

Terms and storage conditions

To store at a temperature up to 25 °C. To protect from children.

Period of validity – 5 years.