Lokren tabs 20mg #56

User manual for Lokren

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Lokren is a selective beta1-blocker.

Release form and composition

Dosage form - film-coated tablets: round, biconvex, white, engraved with "KE 20" on one side and a dividing line on the other (14 pcs. In blisters, 1 blister in a cardboard box).
Lokren's active substance is betaxolol hydrochloride, in 1 tablet - 20 mg.
Auxiliary components: microcrystalline cellulose, lactose monohydrate, sodium carboxymethyl starch (type A), magnesium stearate, colloidal silicon dioxide.
The composition of the film shell: macrogol 400, hypromellose, titanium dioxide (E171).

Pharmacodynamics

The active component of Lokren is betaxolol, a selective beta1-adrenergic blocker, which has three pharmacological properties: cardioselective beta1-adrenergic blocking effect, lack of partial agonistic (internal sympathomimetic) activity, weak membrane stabilizing effect (similar to the action of local anesthetics and quinidine) when taken in excess of local anesthetics and quinidine.
It should be borne in mind that the selective effect of Lokren on β1-adrenergic receptors is not absolute. When used in high doses, betaxolol can have an effect on β2-adrenergic receptors located mainly in the smooth muscles of blood vessels and bronchi, but this effect is much weaker than that of non-selective beta-blockers.
The β1-adrenergic receptor blocking activity of betaxolol is manifested by the following pharmacodynamic effects:
    decrease in systolic and diastolic blood pressure at rest and during exercise;
    a decrease in heart rate at rest and during exercise (due to the blockade of β-adrenergic receptors in the sinus node, which leads to a slowdown in the automatism of the sinus node due to the fact that betaxolol lacks internal sympathomimetic activity);
    decrease in the reflex of orthostatic tachycardia;
    decrease in cardiac output at rest and during exercise (due to competitive antagonism with catecholamines in peripheral adrenergic nerve endings).
Due to the described effects, Lokren reduces the stress on the heart at rest and during physical exertion.
The mechanism of the drug's antihypertensive action has not been fully established. It is assumed that this property is due to the ability to reduce cardiac output and eliminate spasm of peripheral arteries (due to the central action, which leads to a decrease in sympathetic impulses to the periphery, to the vessels, and also due to inhibition of renin activity).
With prolonged use of betaxolol, the severity of the antihypertensive effect does not decrease. When Lokren is taken 1 time per day in the dose range of 5–40 mg, the hypotensive effect appears the same after 3-4 hours and after 24 hours (before taking the next dose). When using Lokren in doses of 5 mg and 10 mg, the hypotensive effect is, respectively, 50% and 80% of the effect observed with a dose of 20 mg. Thus, when taking the drug in doses from 5 to 20 mg, a dose-dependent effect is observed, while in the case of an increase in the dose from 10 to 20 mg, the increase in the effect is insignificant, as well as when the dose is increased from 20 to 40 mg. The maximum antihypertensive effect appears after 1–2 weeks of treatment.
In contrast to the hypotensive effect, when the dose is increased from 10 to 40 mg, the effect of reducing the heart rate does not increase.
Lokren can also slow down the conduction of the atrioventricular (AV) node.

Pharmacokinetics

After oral administration, betaxolol is rapidly and completely (100%) absorbed from the gastrointestinal tract. The maximum plasma concentration reaches after 2-4 hours. Has a minimal effect of the first passage through the liver.
It is characterized by high bioavailability - about 85%, which explains the insignificant differences in its plasma concentrations in different patients or in one patient with prolonged treatment.
It binds to plasma proteins by about 50%. The volume of distribution is ~ 6 l / kg. Poorly penetrates the blood-brain and placental barriers. It is excreted in breast milk to an insignificant extent. It is characterized by moderate solubility in fats.
Betaxolol is metabolized in the liver with the formation of inactive metabolites. It is excreted mainly (> 80%) in the form of metabolites, unchanged - no more than 15%.
The half-life (T½) is 15–20 hours. In case of impaired hepatic function, clearance does not change, but T½ increases by 33%. In case of impaired renal function, T½ is lengthened by 2 times.
Betaxolol is not excreted from the body during hemodialysis.

Indications for use

    Monotherapy and combined treatment of arterial hypertension;
    Prevention of exertional angina attacks (with monotherapy or combined treatment).

Contraindications

    Cardiogenic shock;
    Acute heart failure;
    Cardiomegaly (in the absence of symptoms of heart failure);
    Chronic heart failure in the stage of decompensation (with ineffective therapy with inotropic drugs, diuretics, angiotensin-converting enzyme inhibitors and other vasodilators);
    Atrioventricular (AV) block II and III degree (without an artificial pacemaker);
    Sick sinus syndrome (SSS), including sinoatrial block;
    Arterial hypotension (systolic blood pressure (BP) less than 100 mm Hg);
    Severe bradycardia (heart rate (HR) less than 45-50 beats per minute);
    Monotherapy for Prinzmetal angina pectoris;
    Severe form of obliterating pathologies of peripheral arteries and Raynaud's disease;
    Severe form of chronic obstructive pulmonary disease and bronchial asthma;
    Metabolic acidosis;
    Pheochromocytoma in the absence of the simultaneous use of alpha-blockers;
    Simultaneous use with sultopride, floctaphenin, monoamine oxidase inhibitors;
    Lactose intolerance, lactase deficiency, glucose-galactose malabsorption;
    Age under 18;
    Breastfeeding period;
    History of anaphylactic reactions;
    Hypersensitivity to the components of the drug.
According to the instructions, Lokren is recommended with caution to be prescribed to patients with chronic heart failure in the stage of compensation, AV blockade of the 1st degree, mild forms of obliterating peripheral arterial disease and Raynaud's syndrome, Prinzmetal's angina (only in combination with vasodilators), bronchial asthma and chronic obstructive pulmonary disease with moderate severity of the disease, patients with treated pheochromocytoma, hepatic and / or renal failure, diabetes mellitus, psoriasis, during desensitizing treatment and in the treatment of elderly patients.
It is not recommended to prescribe Lokren during pregnancy, unless the expected benefit of therapy for the mother outweighs the potential threat to fetal health.

Instructions for use of Lokren: method and dosage

Lokren tablets are taken orally, without chewing, with a small amount of liquid.
Recommended daily dosage for each clinical indication: 10 mg or ½ tablet. If, after 7-14 days of using the initial dose, it is not possible to achieve the target blood pressure, then the dose of Lokren should be increased to 20 mg.
Prescribing a daily dose usually does not exceed 20 mg, the maximum is 40 mg per day.
Patients with renal insufficiency should be prescribed taking into account the functional state of the kidneys. With a creatinine clearance (CC) of more than 20 ml / min, Lokren is prescribed at the recommended dose, but at the beginning of therapy (the first 4-7 days), clinical observation should be carried out regularly until the level of betaxolol concentration in the blood reaches equilibrium.
When CC is less than 20 ml / min, the initial daily dose is 5 mg, including patients on hemodialysis. To achieve clinical efficacy, it is allowed to increase the dose every 1-2 weeks by 2 times, but not more than 20 mg per day.
In liver failure, Lokren is prescribed in the usual dose, but careful clinical observation of the patient is necessary.

Side effects

    Cardiovascular system: often - bradycardia (including in severe form), decreased skin temperature of the upper and lower extremities; rarely - the development or aggravation of signs of heart failure (swelling of the feet, ankles, legs), manifestations of angiospasm: increased peripheral circulatory disorders (intermittent claudication), Raynaud's syndrome, increased frequency of angina attacks, slowing of AV conduction, a strong decrease in blood pressure;
    Nervous system: often - insomnia, headache, dizziness, asthenia; rarely, depression; very rarely - nightmares, hallucinations, paresthesia, confusion;
    Digestive system: often - nausea, vomiting, gastralgia, diarrhea;
    Organ of vision: rarely - decreased intraocular pressure, dry eyes; very rarely - visual impairment;
    Metabolism: very rarely - hyperglycemia, hypoglycemia;
    Respiratory system: rarely - bronchospasm;
    Laboratory indicators: rarely - the appearance of antinuclear antibodies, in exceptional cases accompanied by transient clinical signs of lupus-like syndrome;
    Dermatological reactions: rarely - skin rash, itching, urticaria, exacerbation of psoriasis or psoriasis-like rash;
    Genitals: often - impotence;
    Effect on the fetus: hypoglycemia, fetal growth retardation, bradycardia;
    Allergic reactions: skin rash, itching, urticaria;
    Others: withdrawal syndrome (increased blood pressure, increased frequency or increased angina attacks).

Overdose

Possible overdose symptoms: dizziness, marked decrease in blood pressure, AV block, arrhythmias, severe bradycardia, ventricular premature beats, heart failure, fainting, cyanosis of fingernails and palms, difficulty breathing, bronchospasm, convulsions.
First aid measures: gastric lavage and intake of adsorbing agents. In case of bradycardia, intravenous administration of atropine at a dose of 1–2 mg is recommended, then, if necessary, a slow infusion of isoprenaline (at a dose of 0.025 mg) or dobutamine (0.0025–0.01 mg / kg / min) is performed. In some cases, temporary installation of an artificial pacemaker is required. With an excessive decrease in blood pressure, intravenous administration of vasopressor drugs and plasma-substituting solutions is indicated. If bronchospasm develops, bronchodilators are prescribed, including beta2-adrenomimetics and / or aminophylline.
Newborns whose mothers took Lokren during pregnancy are hospitalized in the intensive care unit in the event of heart failure (decompensation), isoprenaline and dobutamine are prescribed (usually in high doses, for a long time), and careful medical supervision is provided.

Special instructions

Cancellation or change in the dose of Lokren should be done only after consulting a doctor, doing it gradually, so as not to cause a temporary deterioration in the activity of the heart in the form of an increase in the frequency of angina attacks. A dose reduction is achieved within 2 weeks, with the simultaneous appointment of antianginal replacement therapy. Abrupt interruption of treatment in patients with coronary artery disease can cause severe cardiac arrhythmias, myocardial infarction, or cardiac arrest.
At the beginning of treatment, patients should be monitored daily blood pressure and heart rate, then - at least 1 time in 3-4 months. In addition, once every 4-5 months in patients with diabetes mellitus, it is necessary to check the level of glucose concentration in the blood, and in elderly patients - the function of the kidneys.
Patients should be trained in self-calculation of heart rate, and remember that in case of heart rate below 50 beats per minute, you should immediately consult a doctor.
The ineffectiveness of the use of beta-blockers is noted in 1/5 of patients with angina pectoris due to severe coronary atherosclerosis with a low threshold of ischemia (with a heart rate of less than 100 beats per minute at the beginning of the development of an anginal attack) and increased end-diastolic pressure of the left ventricle, which disrupts subendocardial blood flow.
Lokren's reception should be temporarily canceled during a routine study of antinuclear antibody titers in the blood or the level of concentration of normetanephrine, vanillin-mandelic acid and catecholamines in the blood and urine.
The use of clonidine can be discontinued only after the cancellation of Lokren, after a few days.
Prescribing the drug to patients with bronchial asthma and chronic obstructive pulmonary disease is possible with a moderate severity of the disease and after assessing the respiratory function. Treatment should be started with small doses, beta1-selectivity of betaxolol allows you to stop the emerging attacks of bronchial asthma by taking beta2-adrenergic agonists.
Treatment of therapeutically controlled heart failure should be carried out under the strict supervision of a physician, starting with low doses. While maintaining chronic heart failure in a compensated state, a gradual increase in the dose is possible.
With bradycardia with a resting heart rate below 50-55 beats per minute, it is necessary to reduce the dose of Lokren.
Careful observation is required, including control of the patient's electrocardiogram, with AV block of the 1st degree.
The use of Lokren for Prinzmetal's angina can cause an increase in angina attacks, so the drug is recommended to be prescribed only for the treatment of mild pathology or mixed angina in combination with vasodilators.
In case of impaired peripheral circulation, taking betaxolol may worsen the patient's condition.
The appointment of Lokren for arterial hypertension against the background of pheochromocytoma requires the simultaneous use of alpha-blockers and blood pressure control.
Treatment of elderly patients begins with the appointment of a low dose under the strict supervision of a physician.
Dosage adjustment for patients with renal insufficiency depends on the CC or the level of creatinine concentration in the blood plasma.
Lokren should be taken with caution in patients with diabetes mellitus, especially at the beginning of treatment, since it is possible to reduce the severity of symptoms of hypoglycemia. The patient needs to regularly monitor the concentration of glucose in the blood.
The action of beta-blockers exacerbates the course of psoriasis.
When treating patients prone to anaphylactic reactions, especially against the background of floktaphenin or desensitization, it is necessary to take into account the property of Lokren to increase the susceptibility to allergens and the severity of anaphylactic reactions. The use of epinephrine (adrenaline) for the treatment of anaphylactic reactions is not always clinically effective.
When performing a surgical operation using general anesthesia, it is necessary to inform the anesthesiologist about the patient taking beta-blockers. If it is necessary to cancel Lokren, it is recommended to do this gradually, completing the drug intake 48 hours before the onset of anesthesia.
In case of emergency surgery, the impossibility of canceling betaxolol or surgery in patients with coronary insufficiency, the patient is prescribed appropriate premedication with atropine, without interrupting betaxolol intake. General anesthesia in this category of patients should include substances with a mild degree of myocardial depression. During surgery, it is necessary to replenish blood loss and take into account the risk of anaphylactic reactions.
Beta-blockers can mask the symptoms of thyrotoxicosis.
During the period of treatment, the use of alcoholic beverages is contraindicated.
Patients with contact lenses should take into account the possible decrease in the production of tear fluid during the use of Lokren.
The clinical effect of beta-blockers in smoking patients is lower.
Betaxolol during doping control tests in athletes can give a positive reaction.
Influence on the ability to drive vehicles and complex mechanisms
Due to the risk of Lokren's side effects in the form of weakness and dizziness, care should be taken when driving vehicles and mechanisms.
Application during pregnancy and lactation
In the course of experimental studies, the teratogenic effect of betaxolol was not revealed. No cases of teratogenic effects in humans have been reported to date. However, it was found that beta-blockers, as a rule, reduce blood flow in the placenta, and therefore can affect the development of the fetus. In this regard, it is necessary to monitor the blood flow in the placenta and uterus, monitor intrauterine development and growth of the fetus. In the event of adverse events, alternative therapeutic measures are prescribed.
Newborns whose mothers took Lokren before delivery should be carefully examined. In the first 3-5 days of life, the child may experience symptoms of bradycardia and hypoglycemia, since the effect of the drug can persist for several days. In the neonatal and postnatal periods, the risk of respiratory and cardiac complications in newborns is increased. In case of development of heart failure, hospitalization of the child in the intensive care unit is indicated. Due to the risk of acute pulmonary edema, the use of plasma substitutes should be avoided. There are also known cases of the development of bradycardia, hypoglycemia and respiratory failure. For this reason, the first 3-5 days, the newborn baby should be under close medical supervision, including monitoring the heart rate and blood glucose concentration.
Considering the above, during pregnancy, Lokren should be used only in exceptional cases, if the expected benefit is definitely higher than the potential risks to the fetus.
Betaxolol is excreted in breast milk. The likelihood of developing bradycardia and hypoglycemia in infants has not been studied, therefore, for safety reasons, it is recommended to stop feeding for the period of therapy.

Childhood use

Due to the lack of data confirming the safety and efficacy of betaxolol in pediatrics, Lokren is not prescribed to patients under the age of 18 years.

With impaired renal function

Lokren should be used with caution for the treatment of patients with concomitant renal failure: with creatinine clearance> 20 ml / min - carefully observe in the first 4 days of taking the drug, with creatinine clearance <20 ml / min and / or hemodialysis - adjust the dose of betaxolol.

For violations of liver function

When treating patients with concomitant hepatic insufficiency, Lokren should be used with caution, careful observation should be ensured at the beginning of therapy.

Use in the elderly

Lokren should be used with caution in elderly patients: start treatment with a low dose and carry it out under close medical supervision.

Drug interactions

Lokren is contraindicated to use simultaneously with floktaphenin. In case of shock or arterial hypotension due to the action of floctaphenin, betaxolol can reduce compensatory cardiovascular reactions.
It is forbidden to use the drug in combination with sultopride, since due to an additional decrease in heart rate, the automatism of the heart is disturbed (severe bradycardia develops).
Lokren is not recommended for use in combination with the following drugs due to the risk of unwanted interactions:
    amiodarone: possible violation of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms);
    blockers of slow calcium channels (for example, verapamil, diltiazem, bepridil): AV conduction and automatism are disturbed (severe bradycardia develops, the sinus node stops), heart failure is possible (due to the synergistic effects of drugs). The use of this combination is allowed only under the condition of ensuring careful clinical observation (including monitoring of the electrocardiogram), especially at the beginning of treatment and in elderly patients;
    cardiac glycosides: the likelihood of developing or aggravating bradycardia and AV block increases, the risk of cardiac arrest;
    monoamine oxidase inhibitors: the hypotensive effect of betaxolol is significantly enhanced (the interval between their doses should be at least 14 days);
    iodine-containing contrast agents: in cases of a sharp decrease in blood pressure or the development of shock due to the administration of iodine-containing contrast agents, betaxolol reduces compensatory cardiovascular reactions (Lokren, if possible, is recommended to be canceled before x-ray examination).
With the simultaneous appointment of the following drugs, caution should be exercised due to the likelihood of developing interaction reactions:
    inhalation halogen-containing anesthetics: their cardiodepressant effect is enhanced (the drug should not be canceled, but it is imperative to warn the anesthesiologist about taking the drug);
    baclofen: the hypotensive effect of betaxolol is enhanced (with their simultaneous use, blood pressure should be monitored and, if necessary, the dose of Lokren should be adjusted);
    propafenone: contractility, automatism and conductivity are impaired (sympathetic compensatory mechanisms are suppressed; careful clinical observation and control of the electrocardiogram are required);
    centrally acting antihypertensive drugs (for example, apraclonidine, moxonidine, alpha-methyldopa, rilmenidine, guanfacine, clonidine): when the drugs are used together, the risk of bradycardia and AV conduction disturbances increases; the antihypertensive drug should be abruptly canceled, clinical monitoring is recommended);
    cholinesterase inhibitors (for example, neostigmine, ambenonium, rivastigmine, galantamine, tacrine, donepezil, pyridostigmine): the likelihood of increased bradycardia due to additive action increases (constant clinical monitoring must be ensured);
    insulin and oral hypoglycemic agents, sulfonylurea derivatives: betaxolol can mask some symptoms of hypoglycemia, such as tachycardia and palpitations (it is necessary to regularly monitor the concentration of glucose in the blood, especially at the beginning of the use of Lokren);
    lidocaine 10% when used intravenously as an antiarrhythmic agent: betaxolol increases the concentration of lidocaine in the blood, as a result of which an increase in unwanted neurological and cardiovascular symptoms is possible (careful monitoring is recommended, including electrocardiogram and the level of lidocaine in the blood plasma, during the use of Lokren and after its cancellation, if necessary - correction of the dose of lidocaine);
    drugs that can cause ventricular arrhythmias (including pirouette-type ventricular tachycardia), such as benzamides (sulpiride, amisulpride, tiapride), butyrophenones (haloperidol, droperidol), sotalol, class IA antiarrhythmics (disopyramide, hydroquinine , quinidine) and class III (dofetilide, amiodarone, ibutilide), some antipsychotics from the phenothiazine group (levomepromazine, cyamemazine, chlorpromazine, thioridazine), other antipsychotics (pimozide), as well as some other drugs, for example, halofantrine, pentamidine, cisapride, , mizolastine, difemanil, erythromycin, spiramycin or vincamine administered intravenously: the risk of ventricular arrhythmias increases, in particular the development of ventricular tachycardia of the "pirouette" type (electrocardiogram control and clinical monitoring of the patient's condition is necessary).
When using the drug in combination with the following drugs, the likelihood of interactions should be considered:
    non-steroidal anti-inflammatory drugs of systemic action, including selective inhibitors of COX-2: the antihypertensive effect of betaxolol decreases;
    mefloquine: risk of developing bradycardia due to additive action;
    alpha-blockers, including those used in urology (prazosin, alfuzosin, terazosin, doxazosin, tamsulosin), antipsychotics and tricyclic antidepressants like imipramine: the hypotensive effect of betaxolol increases, the risk of orthostatic hypotension increases;
    phenytoin (when administered intravenously): the severity of the cardiodepressant effect increases, a decrease in blood pressure is possible;
    xanthines: their clearance decreases (with the exception of diphylline) and plasma concentration increases, especially in patients with an initially increased clearance of theophylline (for example, due to smoking);
    estrogens, glucocorticosteroids, tetracosactide: the antihypertensive effect of betaxolol is weakened (due to sodium and water retention);
    non-depolarizing muscle relaxants: their effect is prolonged;
    coumarins: their anticoagulant effect is enhanced;
    non-hydrogenated ergot alkaloids: increased risk of peripheral circulatory disorders;
    diuretics: an excessive decrease in blood pressure is possible;
    dipyridamole (when administered intravenously), amifostine: the antihypertensive effect of betaxolol is enhanced;
    ethanol, hypnotics and sedatives: increased depression of the central nervous system;
    allergens used for immunotherapy and allergen extracts for skin tests: increases the likelihood of developing severe systemic allergic reactions or anaphylaxis;
    blockers of slow calcium channels from the group of dihydropyridines: the hypotensive effect mutually increases, heart failure may develop in patients with uncontrolled or latent heart failure; Betaxolol can minimize the reflex activation of the sympathetic nervous system in response to vasodilation caused by slow calcium channel blockers from the dihydropyridine group.

Terms and conditions of storage

Store at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 5 years.

Reviews

Reviews about Lokren are positive. Patients note the effectiveness of the drug, ease of administration (1 time per day) and good tolerance. However, there is an opinion that this remedy is more suitable for patients of young and middle age, since in this category of patients, arterial hypertension is rarely associated with heart failure.

Terms of sell

You don't need a prescription from a doctor to buy Lokren.