Lokren coated pills 20mg N56
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Active ingredients
Betaxolol
Release form
Pills
Composition
Betaxolol hydrochloride 20 mg; excipients: lactose monohydrate - 100 mg, microcrystalline cellulose - 113 mg, sodium carboxymethyl starch (type a) - 4 mg, colloidal silicon dioxide - 1.6 mg, magnesium stearate - 1.4 mg, shell composition: hypromellose - 3.9 mg, macrogol 400 - 0.43 mg, titanium dioxide (e171) - 0.67 mg.
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 therapeutic.; It should be noted that the selective effect of betaxolol on β1-adrenergic receptors is not absolute, so when applying it in high doses, the effect of betaxolol on β2-adrenoreceptors located mainly 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) .; when betaxolol is used, its activity blocking β1-adrenoreceptors 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, in combination with the absence of internal sympathomimetic activity in betaxolol, slows the sinus node automatism) ; - reduction of cardiac output at rest and during exercise due to competitive antagonism with catecholamines in peripheral (especially cardiac) adrenergic nerve endings; - 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 physical exertion; The mechanism of the antihypertensive effect of beta-adrenergic blockers is not fully established. - elimination of peripheral arterial spasm (due to the central action leading to a decrease in sympathetic impulses to the periphery, to the vessels,and by inhibiting the activity of renin); the antihypertensive effect of betaxolol does not decrease with its prolonged administration. 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, and 10 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 with an increase in its dose (from 10 mg to 40 mg) does not increase.
Pharmacokinetics
Absorption; After 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 "first pass" through the liver and high bioavailability - about 85%. Differences in its plasma concentrations in different patients or in one patient with prolonged use have minor differences, which is associated with a high bioavailability of betaxolol.; Distribution; Betaxolol binds to 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; excreted by the kidneys as metabolites (more than 80%), 10-15% - unchanged. T1 / 2 betaxolol - 15-20 hours; Pharmacokinetics in special clinical cases; T1 / 2 in violation of liver function is extended by 33%, but the clearance does not change; in case of impaired renal function, T1 / 2 doubles (a dose reduction is necessary); it is not removed during hemodialysis.
Indications
- arterial hypertension (in monotherapy and combination therapy); - prevention of strokes of angina (in monotherapy and combination therapy).
Contraindications
- 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 agents, ACE inhibitors, other vasodilators; - cardiogenic shock; - AV blockade II and III degree (without an installed artificial pacemaker); - Prinzmetal's angina (monotherapy is contraindicated); - SSSU (including sinoatrial blockade); - severe 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 mmHg); - Anaphylactic reactions in history; - metabolic acidosis; - Cardiomegaly (without signs of heart failure); - simultaneous use with sultoprid and floktafenin; - simultaneous administration of MAO inhibitors; - children's and teenage age up to 18 years (efficiency and safety are not established); - Lactase deficiency, lactose intolerance, glucose-galactose malabsorption (due to the presence of lactose in the formulation); - hypersensitivity to betaxolol and excipients of the drug. With caution use the drug: - for bronchial asthma and chronic obstructive pulmonary disease of moderate flow (start treatment with small doses and preferably under the control of indicators of respiratory function; due to beta1-selectivity of betaxolol when an attack occurs bronchial asthma against the background of its reception, it is possible to stop an attack with beta2-adrenomimetics); - in case of chronic heart failure in the stage of compensation (treatment with betaxolol is possible only under strict medical supervision; treatment should be started with very small doses with their gradual increase); - with AV block I degree (careful monitoring is required, including ECG control); - in case of obliterating diseases of the peripheral arteries, Raynaud’s syndrome (with the exception of the severe form) (possible increase in disorders of the peripheral blood circulation); - with Prinzmetal's angina pectoris (there may be an increase in angina attacks; the use of selective beta-1 adrenoblocker is possible only withsimultaneous use of vasodilators); - in case of a treated pheochromocytoma (when Lokren is treated with arterial hypertension against the background of a treated pheochromocytoma, careful monitoring of blood pressure indicators is required); - in elderly patients (treatment should be started with small doses and under close medical supervision); - in case of renal insufficiency (with CC more than 20 ml / min - careful observation of the patient during the first 4 days of treatment; with CC less than 20 ml / min and / or hemodialysis, correction of the dosage regimen is required); - in case of liver failure (more careful clinical observation is required at the beginning of treatment); - in patients with diabetes mellitus (regular monitoring of glucose concentration in the blood, including active self-control by the patient, is necessary at the beginning of treatment; reduction in the severity of precursors of hypoglycemia, such as tachycardia, palpitations, and increased sweating, is possible); - in psoriasis (beta-blockers can make it harder for psoriasis); - during desensitization therapy.
Use during pregnancy and lactation
Pregnancy; In experimental studies, no teratogenic effects of betaxolol have been identified. Until now, no human teratogenic effects have been reported.; As a rule, beta-adrenergic blockers decrease 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, and 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, since the 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 such newborns is required in a specialized department (heart rate, blood glucose concentration) .; Therefore, the use of Lokren during pregnancy is not recommended and is possible only when benefit to the mother outweighs the potential risk to the fetus or child.; Lactation; 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. You should not chew a pill.; The initial dose of the drug Lokren for both indications for use of the drug is usually 10 mg (1/2 tab. 20 mg). If target blood pressure values are not achieved within 7-14 days of treatment, the dose doubles to 20 mg / day. Usually, Lokren doses of more than 20 mg are not used (due to the fact that with an increase in the dose of more than 20 mg, a significant increase in the antihypertensive effect of the drug) .; The maximum daily dose of Lokren is 40 mg. In patients with renal insufficiency, dose adjustment is recommended depending on the functional state of the patient’s kidneys. When QA 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 (CC 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, if not sufficiently effective, can increase by 2 times every 1 -2 weeks. The maximum daily dose is 20 mg. In patients with hepatic insufficiency, dose adjustment is usually not required. However, at the beginning of therapy, more careful clinical observation of the patient is recommended.
Side effects
Allergic reactions: skin rash, itching, urticaria; The side effects listed below are given in accordance with the following gradations of the frequency of their occurrence: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10,000, <1/1000); very rarely (<1/10 000) (including individual messages) .; Dermatological reactions: rarely - various skin reactions, including skin rash, itching, urticaria, psoriasis-like rashes or exacerbation of the course of psoriasis. From the nervous system: often - dizziness, headache, asthenia, insomnia; rarely, depression; very rarely - hallucinations, confusion, nightmares, paresthesia. On the part of the organ of vision: rarely - dry eyes, reduced intraocular pressure (due to the possibility of its reduction under the influence of beta-blockers); very rarely - visual impairment. On the part of the digestive system: often - gastralgia, diarrhea, nausea, vomiting.; On the part of metabolism: very rarely - hypoglycemia, hyperglycemia.; On the part of the cardiovascular system: often - bradycardia, possibly severe, decrease in skin temperature of the upper and lower extremities; rarely - development (or worsening) of symptoms of heart failure (edema of the ankles, feet, legs), pronounced decrease in blood pressure, slowing of AV conduction, manifestations of angiospasm: Raynaud's syndrome, increased violations of the peripheral blood circulation, including and intermittent claudication, increased frequency of angina attacks; On the part of the respiratory system: rarely - bronchospasm.; On the part of the genitals: often - impotence; On the part of laboratory indicators: rarely - the appearance of antinuclear antibodies, only in exceptional cases combined with clinical manifestations of lupus-like syndrome following cessation of treatment.; Effect on the fetus: intrauterine growth retardation, hypoglycemia, bradycardia.; Other: withdrawal syndrome (increased or increased frequency of strokes, increased blood pressure).
Overdose
Symptoms: severe bradycardia, dizziness, AV blockade, marked reduction in blood pressure, arrhythmias, ventricular extrasystoles, fainting, heart failure, difficulty breathing, bronchospasm, cyanosis of the toenails of the fingers and palms, convulsions; Treatment: gastric lavage, prescription of adsorbing agents; whendevelopment of bradycardia is recommended atropine 1-2 mg IV; 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
Contraindications: With flactafenin; In case of shock or arterial hypotension caused by floctafenin, beta-adrenergic blockers cause a decrease in compensatory cardiovascular reactions. Violations of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms) .; With blockers of slow calcium channels (bepridil, diltiazem and verapam or; Automatism disorders (severe bradycardia, sinus node arrest), AV conduction disorders, heart failure (synergistic / mutually reinforcing / effects); This combination can only be used under careful clinical and ECG observation, especially in elderly patients or early treatment.; With cardiac glycosides; Risk of development or worsening of bradycardia, AV-blockade, cardiac arrest.; With MAO inhibitors; It is not recommended to use it simultaneously with MAO inhibitors due to a significant increase in antigi ertenzivnogo action betaxolol treatment interruption between the intake of MAO and betaxolol inhibitors should be at least 14 days. On the iodine-containing contrast media, in the case of shock or abrupt reduction in blood pressure when administered iodinated contrast agents, beta-blockers reduce the compensatory cardiovascular reactions.If possible, treatment with beta-adrenergic blocking agents 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 when administered beta adrenostimulyatorov). 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 about taking a beta-blocker. With drugs that can cause ventricular arrhythmias, including ventricular tachycardia of the pirouette type: antiarrhythmic drugs of class IA (quinidine, hydroquinidine and disopyramide) and class III (amiodarone, dofetil) , ibutilid), sotalol, some antipsychotics from the group of phenothiazine (chlorpromazine, cyamemazine, levomepromazine, thioridazine), benzamides (amisulpride, sulpiride, tiapride), butyrophenones (droperidol, haloperidol), other neuroptics Zid) and other drugs (cisapride, diphemanil, administered in / in erythromycin, halofantrine, mizolastin, moxifloxacin, pentamidine, injected in / in spiramycin and injected / in vincamine; Increased risk of ventricular arrhythmias, in particular, ventricular tachycardia of the type "pirouette Requires clinical and ECG control. With propafenone; Violations of contractility, automatism and conduction (suppression of sympathetic compensatory mechanisms). Clinical and ECG control is required. With baclofen; Enhancement 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 a heartbeat and tachycardia. The patient should be warned about the need to enhance the regular monitoring of glucose concentrations in the blood, including active self-control by the patient, especially at the beginning of treatment. With cholinesterase inhibitors (ambenonium, donepezil, galantamine, neostigmine, pyridostigmine, rivastigmine, takrin); Risk of increased bradycardia (additive action ).Regular clinical monitoring 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 antihypertensive agent and conduct clinical monitoring. With a lidocaine 10% solution (IV as an antiarrhythmic agent); Increasing the concentration of lidocaine in the blood plasma with a possible increase in unwanted neurological symptoms and cardiovascular effects (reduced metabolism lidocaine in the 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, dose adjustment of lidocaine.; Combinations that should be taken into account; With NSAIDs (drugs with a systemic effect), including selective COX-2 inhibitors; Reduction of the antihypertensive effect of betaxolol (suppression of the synthesis of prostaglandins NSAIDs and the delay of water and sodium pyrazolone derivatives) ; With slow calcium channel blockers from the group of dihydropyridines; Mutual enhancement of the antihypertensive effect of slow calcium channel blockers and betaxolol, the development of heart failure in the patient Comrade latentnoprotekayuschey with heart failure or uncontrolled heart failure. Treatment with beta-adrenergic blockers can minimize the reflex activation of the sympathetic nervous system in response to vasodilation under the influence of slow calcium channel blockers from the dihydropyridines group; With tricyclic antidepressants (such as imipramine), antipsychotics; With mefloquine; the risk of bradycardia (additive effect); With dipyridamole (in / in the introduction); Strengthening the antihypertensive effect of betaxolol.; With alpha-adren blockers, including used in urology (alfuzosin, doxazosin, prazosin, tamsulosin, terazosin); Amplification antihypertensive effect of betaxolol.Increased risk of orthostatic hypotension. With amifostine; Enhanced 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 (/ introduction); Increased severity of cardiodepressive action and the likelihood of lowering blood pressure. With xanthines; Betaxolol reduces the clearance of xanthines (except diphillin) and increases their plasma concentration in the blood , especially in patients with initially increased 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; With diuretics; Possible excessive reduction in blood pressure.; With non-depolarizing muscle relaxants; Betaxolol prolongs the action of non-depolarizing muscle relaxants. With coumarins; Strengthening of the anticoagulant effect of coumarins.; With alcohol (ethanol), sedatives and hypnotic medications; Strengthening of the CNS depression; with unhydrogenated ergot alkaloids; Unhydrogenated ergot alkaloids increase the risk of developing disorders of the peripheral circulation 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 start replacement therapy with another antianginal agent to avoid an increase in angina attacks. In patients taking Lokren, the heart rate and blood pressure should be monitored (at the beginning of treatment, then 1 time 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 HR, and the patient should be proi struktirovan the need to see a doctor with a decrease in heart rate less than 50 beats / min.. Approximately 20% of patients with angina Beta-blockers are ineffective.The main reasons are severe coronary atherosclerosis with a low ischemic threshold (heart rate at the time of an angina attack less than 100 beats / min) and increased end-diastolic pressure of the left ventricle, which violates the subendocardial blood flow. days after discontinuation of the drug Lokren.; Lokren should be discontinued before the study of the concentration of catecholamines, normetanephrine and vanillindic 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. With the development of attacks during treatment, bronchodilators can be used - beta2-adrenomimetics.; Heart failure; In patients with therapy that is controlled therapeutically, if necessary, betaxolol can be used under strict medical supervision in very low initial doses with a gradual increase, if necessary, and in the case of good tolerance (maintaining a compensated state of chronic cardiac insufficiency); Bradycardia; If the heart rate at rest becomes below 50-55 beats / min, the dose of Lokren should be reduced.; AV degree I blockade; Given the negative dromotropic effect of beta-adrenergic blockers, with I degree blockade, the drug should be used with caution .; Prinzmetal angina; Beta-blockers may increase the frequency and duration of seizures in patients with Prinzmetal angina. The use of cardioselective beta1-adrenergic blockers is possible with mild severity of Prinzmetal stenocardia or mixed-type angina pectoris, provided that the treatment is carried out in combination with vasodilators.; Disturbed peripheral blood circulation; Raynaud, arteritis or chronic obliterating diseases of lower limb arteries); Phaeochromocytoma; In the case of beta-adrenergic block When treating arterial hypertension caused by pheochromocytoma, careful control of blood pressure is required.The appointment of the drug Lokren is possible only against the background of 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 mellitus; It is necessary to warn the patient about the need to strengthen the control of the concentration of glucose in the blood, including the 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; Requires careful assessment of the need to use the drug, because 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 provide the expected therapeutic effect.; In patients prone to severe anaphylactic reactions, especially those associated with the use of floctafenin or during desensitization, beta-adrenergic blocking therapy may further enhance the reactions and reduce the effectiveness of treatment. ; General anesthesia; When conducting general anesthesia, the risk of blockade of β-adrenoreceptors (decrease in heart rate, decrease in cardiac output, decrease in systemic Tolic and diastolic blood pressure); Beta-blockers mask reflex tachycardia and increase the risk of arterial 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, because it is consideredthat cessation of therapy for 48 hours makes it possible to restore 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 up to surgical intervention, taking into account the risk associated with the sudden withdrawal of beta-blockers; - in the case of emergency surgical interventions or in cases where the discontinuation of treatment is impossible, the patient should be protected from the effects of excitation of the vagus nerve by appropriate premedication with atropine, repeating if necessary. In such patients, for general anesthesia, it is necessary to use substances that are least depressant myocardium, and blood loss should be replenished.; The risk of anaphylactic reactions should be considered.; Thyrotoxicosis; Thyrotoxicosis symptoms may be masked during therapy b ta-blockers. Athletes; Athletes should take into account that the drug contains an active substance that can give a positive reaction during doping control tests.; Alcohol should be excluded during treatment.; Patients using contact lenses should take into account that during treatment 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 activities; When driving or taking other potentially hazardous activities while taking the drug Lokren, caution should be exercised (due to the risk of dizziness, weakness, which can reduce the attention and speed of psychomotor reactions required for these activities).