Lokren coated pills 20mg N28
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Active ingredients
Betaxolol
Release form
Pills
Composition
Active ingredient: Betaxolol (Betaxolol) Concentration of the active substance (mg): 20
Pharmacological effect
Selective beta1-blocker. Betaxolol is characterized by three pharmacological properties: cardio-selective beta1-adreno-blocking action; lack of partial agonistic activity (lack of internal sympathomimetic activity); a weak membrane stabilizing effect (like the action of quinidine or local anesthetics) in concentrations exceeding the therapeutic ones. It should be noted that the selective effect of betaxolol on β1-adrenergic receptors is not absolute, so when using it in high doses it is possible that betaxolol on β2-adrenoreceptors located mainly Thus, in the smooth muscles of the bronchi and blood vessels (however, the effect of Betaxolol on β2-adrenoreceptors is much weaker than that in non-selective beta-blockers). In the case of Betaxolol, its β1-adrenoreceptor blocking activity is manifested by the following pharmacodynamic effects: - Decrease in heart rate at rest and during physical exertion (due to the blockade of β-adrenoreceptors in the sinus node, which, combined with the absence of internal sympathomimetic activity in Betaxolol, slows the sinus node automaticity) - reduction of cardiac output at rest and during physical activity due to competitive antagonism with catecholamines in peripheral (especially cardiac) adrenergic nerves - reduction of systolic and diastolic blood pressure at rest and during exercise (the mechanism of antihypertensive action is described below); - reduction of the orthostatic tachycardia reflex. As a result of these effects, the load on the heart decreases at rest and during exercise. The mechanism of antihypertensive action of beta adrenergic blockers are not fully installed. Beta-adrenergic blockers suggest the following mechanisms of antihypertensive action: - reduction of cardiac output; - elimination of peripheral spasm x arteries (due to central action, which leads to a decrease of sympathetic impulses to the periphery, to the vessels, and by inhibiting the activity of renin) .Antigipertenzivnoe effect of betaxolol with its long reception is not reduced.When taking betaxolol (from 5 to 40 mg) once a day, the antihypertensive effect is the same after 3-4 hours (the time it takes Cmax 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 the antihypertensive effect when taking 20 mg of betaxolol. Thus, in the dose range of 5-20 mg, there is a dose-dependence of the antihypertensive effect mg to 20 mg increase in antihypertensive effect is negligible. 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 effect of betaxolol, the effect of reducing heart rate by increasing its dose (from 10 mg to 40 mg) does not increase. Moreover, betaxolol can slow down the AV node's conductivity.
Pharmacokinetics
AbsorptionAfter oral administration, betaxolol is rapidly and completely (100%) absorbed from the gastrointestinal tract. Cmax of betaxolol in blood plasma is achieved in 2-4 hours. Betaxolol has a slight effect of the first passage through the liver and high bioavailability - about 85%. 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 of Betaxolol is associated with plasma proteins by about 50%. It penetrates poorly through the BBB and the placental barrier, to a small extent excreted in breast milk. Vd - about 6 l / kg. Fat solubility is moderate. Metabolism Betaxolol is metabolized in the liver to form inactive metabolites. Excretion is excreted by the kidneys as metabolites (more than 80%), 10-15% - unchanged. T1 / 2 betaxolol - 15-20 hours. The pharmacokinetics in special clinical situations T1 / 2 in case of abnormal liver function is extended by 33%, but the clearance does not change; in case of impaired renal function, T1 / 2 doubles (dose reduction is necessary). It is not removed during hemodialysis.
Indications
Arterial hypertension (in monotherapy and combination therapy). Prevention of stress angina attacks (in monotherapy and combination therapy).
Contraindications
Hypersensitivity 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 decompensation stage, not compensated as a result of treatment with diuretics, inotropic drugs, ACE inhibitors, other vasodilators. blockade of II and III degree (without an installed artificial pacemaker). Prinzmetal stenocardia (monotexin is contraindicated rapia). Sinus node weakness syndrome (including sinoatrial blockade). Severe bradycardia (HR less than 45-50 beats / min) pressure <100 mmHg.). Anaphylactic reactions in history. Metabolic acidosis. When used simultaneously with floctafenin (see the section "Interaction with other drugs"). When applied simultaneously and sultopride (see. section "Interaction with other drugs"). While taking monoamine oxidase (MAO) inhibitors. Cardiomegaly (without signs of heart failure). Age up to 18 years (efficacy and safety not established). Lactase deficiency, lactose intolerance, glucose-galactose malabsorption ( due to the presence in the composition of the drug lactose)
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Pregnancy Experimental studies have not revealed the teratogenic effect of betaxolol. So far, no human teratogenic effects have been reported. As a rule, beta-adrenergic blockers reduce the blood flow in the placenta and can affect the development of the fetus. The blood flow in the placenta and uterus should be monitored, as well as the growth and development of the unborn child should be monitored, and in the event of adverse events with regard to pregnancy and / or the fetus, alternative therapeutic measures should be taken. The newborn should be carefully examined after delivery. In the first 3-5 days of life, symptoms of bradycardia hypoglycemia may occur, sincethe 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 the event of heart failure, hospitalization of the newborn in the intensive care unit is required. 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, careful observation of these newborns is required in a specialized unit (heart rate, blood glucose concentration). Therefore, the use of Lokren during pregnancy is not recommended and is only possible if the benefits for the mother outweighs the potential risk to the fetus or child. Lactation period Beta-blockers, including Betaxolol, are excreted in breast milk. The risk of hypoglycemia or bradycardia in infants has not been studied, so as a precautionary measure, breastfeeding during treatment should be discontinued.
Dosage and administration
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 tablet 20 mg). If target blood pressure values are not reached within 7-14 days of treatment, the dose doubles to 20 mg per day. Usually do not use doses of the drug Lokren greater than 20 mg (due to the fact that with increasing doses of more than 20 mg, there is no statistically significant increase in the antihypertensive effect of the drug). The maximum daily dose of the drug Lokren - 40 mg. Patients with renal insufficiency A 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 of 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 4-7 days of treatment). In case of severe renal failure (creatinine clearance less than 20 ml / min), the recommended initial dose of the drug is 5 mg / day (regardless of the frequency and days of the hemodialysis procedure in patients on hemodialysis)which, with insufficient efficiency, may increase by 2 times every 1-2 weeks. The maximum daily dose is 20 mg. Patients with liver failure In patients with liver failure, dose adjustment is usually not required. However, at the beginning of therapy, more careful clinical observation of the patient is recommended.
Side effects
Rarely: various skin reactions, including skin rash, itching, urticaria, psoriasis-like rashes or exacerbation of the course of psoriasis (see the “With Care” section). Nervous system disorders Often: dizziness, headache. Very rare: paresthesia. Violations of the organ of vision Rare: dry eyes. Very rare: visual impairment. Psychiatric disorders Often: asthenia, insomnia. Rarely: depression. Very rare: hallucinations, confusion, nightmares. Violations of the gastrointestinal tract Often: gastralgia, diarrhea, nausea, vomiting. Metabolism and nutrition disorders. Very seldom: hypoglycemia, hyperglycemia. Heart disorders Often: bradycardia, possibly severe. Rarely: development (or worsening) of symptoms of heart failure (swelling of ankles, feet, legs), marked reduction in blood pressure, slowing atrioventricular conductivity. Vascular disorders Often: a decrease in the skin temperature of the upper and lower extremities. Seldom: manifestations of an angiospasm: Raynaud's syndrome, strengthening of disturbances of peripheral blood circulation, including "the alternating lameness", increase in attacks of stenocardia. Disturbances from the respiratory system, organs of the chest and mediastinum Rarely: bronchospasm. Violations of the genital organs and breast cancer Often: impotence. Laboratory and instrumental data Rarely: the appearance of antinuclear antibodies, only in exceptional cases combined with the clinical manifestations of lupus-like syndrome, passing after discontinuation of treatment; reduction of intraocular pressure (due to the possibility of its reduction under the influence of beta-blockers). Effect on the fetus Fetal growth retardation, hypoglycemia, bradycardia.
Overdose
Symptoms: severe bradycardia, dizziness, AV blockade, marked reduction in blood pressure, arrhythmias,ventricular premature beats, fainting, heart failure, shortness of breath, bronchospasm, cyanosis of the nails of the fingers and palms, convulsions. Treatment: gastric lavage, prescription of absorbing agents; in the case of bradycardia, atropine 1-2 mg IV is recommended; then (if necessary) a slow infusion of 25 mcg of isoprenaline or an infusion of dobutamine 2.5-10 mcg / kg / min; sometimes it may require a temporary setting of an artificial pacemaker; in the case of an excessive decrease in blood pressure, it is recommended to / in the administration of plasma-substituting solutions and vasopressor preparations; with bronchospasm - the appointment of bronchodilators, incl. beta2-adrenomimetics and / or aminophylline; in case of heart failure (decompensation) in newborns whose mothers took beta-blockers during pregnancy, hospitalization to the intensive care unit, isoprenaline and dobutamine is recommended for a long time and usually in high doses, specialist supervision.
Interaction with other drugs
Contraindicated combinations With flactafenin In case of shock or arterial hypotension caused by floctafenn, the system has been used as a back-up. . With slow calcium channel blockers (bepridil, diltiazem and verapamil) H automatism disorders (severe bradycardia, sinus node arrest), AV conduction disturbances, heart failure (synergistic / mutually amplifying / effects). This combination can only be used under careful clinical and ECG observation, especially in elderly patients or at the beginning of treatment. glycosides of the Risk of development or worsening of bradycardia, AV blockade, cardiac arrest. Simultaneous use with MAO inhibitors is recommended with MAOH inhibitors due to a significant increase in antihypertensive vnogo action betaxolol treatment interruption between reception and betaxolol MAO inhibitors should be at least 14 dney.S iodinated contrast veschestvamiV case of shock or abrupt reduction in blood pressure when administered iodinated contrast agents, beta-blockers reduce the compensatory cardiovascular reactions.If possible, beta-adrenergic blocking treatment should be discontinued before radiographic studies using iodine-containing contrast agents. Combinations that should be used with caution With inhaled halogen-containing anesthetics Beta-adrenergic blockers have a cardiodepressant effect (inhibition of β-adrenoreceptors can be reduced with a β-ad-stimulator). As a rule, treatment with beta-blockers does not stop and in any case, abrupt withdrawal of beta-blockers should be avoided. Anesthetist must be made aware of the beta-adrenoblokatora.S drugs capable of causing ventricular arrhythmias of the heart, including ventricular tachycardia type pirouette: antiarrhythmics class IA (quinidine, gidrohinidin and disopyramide) and class III (amiodarone, dofetilide, ibutilide) , sotalol, some neuroleptics from the group of phenothiazine (chlorpromazine, cyamemazine, levomepromazine, thioridazine), benzamides (amisulpride, sulpiride, tiaprid), butyrophenones (droperidol, haloperidol), other neuroleptics (pimoz e) and other drugs (cisapride, diphemanil, administered intravenously erythromycin, halofantrine, mizolastine, moxifloxacin, pentamidine, administered intravenously in spiramycin and added in vinkamine. Increasing the risk of ventricular rhythm, in particular ventricular tachycardia, such as pirouette.). ECG control. With propafenone Disorders of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms). Clinical and ECG control are required. With baclofen Strengthening of the antihypertensive effect of betaxolol. Blood pressure control and dose adjustment of betaxolol are necessary if necessary. With insulin and hypoglycemic oral agents, sulfonylurea derivatives, all beta-adrenoblockers can mask certain symptoms of hypoglycemia, such as palpitations and tachycardia. The patient should be warned about the need to enhance regular monitoring of blood glucose concentrations, including active self-control by the patient, especially at the beginning of treatment. With cholinesterase inhibitors (ambenonium, donepezil, galantamine, neostigmine, pyridostigmine, rivastigmine, takrin) The risk of increased bradycardia (additive action).Regular clinical control is required. With antihypertensive drugs of central action (clonidine, apraclonidine, alpha-methyldopa, guanfacine, moxonidine, rilmenidine) Increased risk of developing bradycardia, AV-conduction disorders. A significant increase in blood pressure with a sharp cancellation of the centrally acting antihypertensive drug. It is necessary to avoid abrupt withdrawal of the hypotensive agent and to conduct clinical control. With lidocaine 10% solution (in / in as an antiarrhythmic agent) liver). Clinical and ECG observation and, possibly, control of plasma lidocaine concentration during treatment with beta-blockers and after its termination is recommended. If necessary, a dose adjustment of lidocaine. Combinations that should be taken into account with NSAIDs (drugs with systemic effects), including selective COX-2 inhibitors from the group of dihydropyridines Mutual enhancement of the antihypertensive effect of slow calcium channel blockers and betaxolol, the development of heart failure in patients with latent cardiac failure or uncontrolled heart failure. Treatment with beta-adrenergic blockers can minimize the reflex activation of the sympathetic nervous system in response to vasodilation averages ages anti-affections atop calcium channel blockers from the dihydropyridines group. With tricyclic antidepressants (such as imipramine), neuroleptics. additive action). With dipyridamole (in / in the introduction) Strengthening the antihypertensive effect of betaxolol. With alpha-adrenoblo cathores, including those used in urology (alfuzosin, doxazosin, prazosin, tamsulosin, terazosin) Strengthening the antihypertensive effect of betaxolol.Increased risk of orthostatic hypotension. With amifostine Enhancement of the 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. the probability of reducing blood pressure. With xanthinesBetaxolol decreases the clearance of xanthines (except for difillin) and increases their concentration in the blood plasma, 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 GCS and tetracosactids muscle relaxants Betaxolol prolongs the action of non-depolarizing muscle relaxants. With coumarins Strengthening the anticoagulant effect of coumarins. With alcohol (ethanol), sedatives and hypnotics by means of increased enhancement of CNS.C depressions with unhydrogenated ergot alkaloids. Unhydrogenated ergot alkaloids increase the risk of developing peripheral circulatory disorders when taking Betaxolol.
special instructions
Do not interrupt treatment with Lokren abruptly and change the recommended dose without first consulting a doctor, because This can lead to a temporary deterioration in the activity of the heart. Treatment should not be interrupted suddenly, especially in patients with coronary artery disease, because 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, you can simultaneously begin replacement therapy with another antianginal agent to avoid an increase in angina attacks. In patients taking Lokren, they should monitor their heart rate and blood pressure (at the beginning of treatment, daily once in 3-4 months), blood glucose concentration in patients with diabetes mellitus (1 time in 4-5 months), kidney function in elderly patients (1 time in 4-5 months). The patient should be trained in how to calculate the heart rate, and the patient should be proin truktirovan the need to see a doctor with a decrease in heart rate less than 50 beats. / min.Primerno 20% of patients with angina Beta-blockers are ineffective.The main reasons are severe coronary atherosclerosis with a low ischemic threshold (the heart rate at the time of an angina attack is less than 100 beats / min) and an increased end-diastolic pressure of the left ventricle that violates the subendocardial blood flow. If taken simultaneously, clonidine can be stopped only after several days after the abolition of the drug Lokren. Lokren should be abolished before the study of the concentration of catecholamines, normetanephrine and vanillin almond acid in the blood and urine; as well as titers of antinuclear antibodies in the blood. Bronchial asthma and chronic obstructive pulmonary disease Beta-blockers can be administered only to patients with a moderate degree of severity of the disease, with the choice of a selective beta-blocker in a low initial dose. Before starting treatment, it is recommended to evaluate the respiratory function. When developing attacks during treatment, bronchodilators (beta2-adrenomimetics) can be used. Heart failure In patients with heart failure that are controlled therapeutically, if necessary, betaxolol can be used under strict medical supervision in very low initial doses with gradual their increase, if necessary, and in the case of good tolerability (maintaining a compensated state of chronic cardiac n units) If heart rate at rest becomes below 50-55 beats / min, the dose of Lokren should be reduced. AV degree I blockade Considering the negative dromotropic effect of beta-adrenergic blockers, during blockade I degree, the drug should be used with caution. PrinzmetalBelet blockers can be used with I degree blockade. increase the frequency and duration of attacks in patients with Prinzmetal angina pectoris. The use of cardioselective beta1-adrenergic blockers is possible with mild severity of Prinzmetal stenocardia or mixed angina pectoris, provided that the treatment is carried out in combination with vasodilators. or chronic obliterating diseases of the arteries of the lower extremities) .Peochromocytoma If beta-adrenergic block is used In the treatment of arterial hypertension caused by pheochromocytoma, careful control of blood pressure is required.Administration of the drug Lokren is possible only with the use of alpha-blockers. Elderly patients Treatment of elderly patients should be started 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 CC. Patients with diabetes should warn the patient about the need to strengthen the control of glucose concentration in the blood, 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, feeling of heartbeat and sweating) may be masked by betaxolol. Psoriasis A careful assessment of the need to use the drug, since There are reports of a worsening of the course of psoriasis during treatment with beta-blockers. Allergic reactions Beta-blockers, including Lokren, may increase sensitivity to allergens and the severity of anaphylactic reactions due to the weakening of adrenergic compensatory regulation under the action of beta-blockers. Therapy of anaphylactic reactions with epinephrine (adrenaline) does not always give the expected therapeutic effect. In patients prone to severe anaphylactic reactions, especially those associated with the use of phloctaphenine or during desensitization, therapy with beta-adrenergic blockers may further enhance the reactions and reduce the effectiveness of treatment. Anesthesia When performing general anesthesia, the risk of blockade of β-adrenoreceptors (decrease in heart rate, decrease in cardiac output, decrease in systemic -crystal and diastolic blood pressure) .Beta-blockers mask reflex tachycardia and increase the risk of hypotension. Continuing therapy with beta-blockers reduces the risk of arrhythmias, myocardial ischemia and hypertensive crises. The anesthesiologist should be informed that the patient is receiving treatment with beta-blockers. If it is necessary to discontinue therapy with Lokren before surgery, this should be done gradually and completed 48 hours before general anesthesia, since it is consideredthat stopping therapy for 48 hours allows restoring receptor sensitivity to catecholamines. In some cases, therapy with beta-blockers may not be interrupted: - in patients with coronary insufficiency, it is desirable to continue treatment until surgery, given the risk associated with the sudden withdrawal of beta-blockers; - in case of emergency surgical interventions, or in cases where the discontinuation 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, general anesthesia requires the use of substances that inhibit myocardium to a lesser degree, and blood loss should be replenished. The risk of anaphylactic reactions should be taken into account. take into account that the drug contains an active substance that can give a positive reaction when conducting doping control tests Patients using contact lenses should be aware that treatment with beta-blockers may reduce the production of tear fluid. In smoking patients, the effectiveness of beta-blockers is lower. The effect on the ability to drive vehicles and engage in other potentially hazardous activitiesWhen driving vehicles or engaging in other potentially hazardous activities while taking Lokren, Match the caution (due to the risk of dizziness and weakness, which may reduce the attention and speed of psychomotor reactions necessary for these activities).