Betaxolol film-coated pills 20mg N30
Condition: New product
999 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Betaxolol
Release form
Pills
Composition
Betaxolol hydrochloride 20 mg. Excipients: lactose monohydrate - 128.1 mg, microcrystalline cellulose - 85.8 mg, magnesium stearate - 2.5 mg, sodium carboxymethyl starch - 7.4 mg, aerosil - 1.2 mg. The composition of the film shell: opadry II white 85F18422, including polyvinyl alcohol - 2 mg, titanium dioxide - 1.25 mg, macrogol - 1.01 mg, talc - 0.74 mg.
Pharmacological effect
Cardioselective beta1-blocker without internal sympathomimetic activity. It has a weak membrane stabilizing activity. It has a hypotensive effect associated with a decrease in the minute volume of the heart and a decrease in sympathetic stimulation of peripheral vessels. When used in therapeutic doses, it does not have a cardiodepressive effect, does not affect glucose metabolism, does not reduce the bronchodilatory effect of beta-adrenomimetics, does not cause a delay of sodium ions in the body. Acts for a long time. When applied topically in the form of eye drops lowers increased intraocular pressure. Resorptive effect is expressed slightly.
Pharmacokinetics
After ingestion more than 95% of the dose of betaxolol is rapidly absorbed from the gastrointestinal tract. Cmax of the active substance in the blood plasma is achieved in 1-2 hours. It is subjected to the effect of "first passage" through the liver. Plasma protein binding is about 50%. Vd - about 6 l / kg. T1 / 2 betaxolol - 15-20 hours. It is excreted by the kidneys mainly as metabolites, 10-15% - unchanged.
Indications
For systemic use: as a monotherapy and as part of a combination therapy, arterial hypertension, prevention of strokes of exertional angina. For local use in ophthalmology: chronic open-angle glaucoma, increased intraocular pressure, the state after laser trabeculoplasty.
Contraindications
Cardiogenic shock; acute heart failure, chronic heart failure in the stage of decompensation, not compensated as a result of treatment with diuretics, inotropic agents, ACE inhibitors, other vasodilators; AV block II and III degree (without an installed artificial pacemaker); Prinzmetal angina pectoris (monotherapy is contraindicated); SSS,sinoatrial blockade; severe bradycardia (heart rate less than 45-50 beats / min); severe violations of the peripheral circulation, severe forms of bronchial asthma and COPD; severe forms of Raynaud's disease and peripheral arterial disease obliterans; pheochromocytoma without simultaneous administration of alpha-blockers; arterial hypotension (systolic blood pressure less than 100 mm Hg. Art.); history of anaphylactic reactions; metabolic acidosis; cardiomegaly (without signs of heart failure); simultaneous use with sultoprid and flaktafenin; simultaneous administration of MAO inhibitors; children and adolescents up to 18 years; hypersensitivity to betaxolol.
Use during pregnancy and lactation
During pregnancy and lactation (breastfeeding) use of betaxolol is possible only in cases where the intended benefits to the mother outweigh the possible risk to the fetus or child.
Dosage and administration
For systemic use by ingestion - 20 mg 1 time / day. For patients on permanent hemodialysis or peritoneal dialysis, the initial dose is 10 mg / day; Betaxolol administration time is set independently of the dialysis session mode. For local use in ophthalmology - 1 drop 2 times / day in the affected eye. During the first month, the therapy is carried out under the control of the level of intraocular pressure, then the frequency of measuring intraocular pressure is determined individually. In the case of the use of Betaxolol after the previous treatment with another similar drug, the dosing regimen is set individually.
Side effects
Since the cardiovascular system: at the beginning of treatment - AV-blockade, sinus bradycardia, arterial hypotension, heart failure, Raynaud's syndrome. On the part of the digestive system: rarely - abdominal pain, nausea, vomiting. From the side of the central nervous system and peripheral nervous system: at the beginning of treatment - asthenia, paresthesias of the extremities, sleep disorders, depression, drowsiness, dizziness. On the part of the respiratory system: rarely - bronchospasm. Allergic reactions: rarely - psoriasis-like skin manifestations. Local reactions: when applied in the form of eye drops immediately after instillation, short-term discomfort in the eyes is possible, sometimes lacrimation; rarely, a decrease in corneal sensitivity, erythema, pruritus, spotty staining of the cornea, keratitis, anisocoria, photophobia.
Interaction with other drugs
With simultaneous use with adrenomimetiki, xanthine derivatives decreases the effectiveness of betaxolol. With simultaneous use with antacids and antidiarrheal drugs, beta-blockers may be reduced. With simultaneous use with antihypertensive agents, the antihypertensive effect is enhanced. With the simultaneous use of halogen-containing agents for inhalation anesthesia may increase the negative inotropic effects. With simultaneous use of non-depolarizing muscle relaxants may increase their duration of action. With simultaneous use of NSAIDs, GCS decreases the antihypertensive effect of Betaxolol. With simultaneous use of cardiac glycosides may increase bradycardia. With the simultaneous use of tricyclic antidepressants (imipramine), blood pressure is reduced, there is a risk of orthostatic hypotension. With simultaneous use of amiodarone, verapamil, diltiazem, beta-blockers for topical use in glaucoma may increase the negative inotropic effects and conduction disorders. With simultaneous use of lidocaine increases the concentration of lidocaine in the blood plasma. With simultaneous use with drugs that deplete stocks of catecholamines (including with reserpine), it is possible to increase the hypotensive effect and bradycardia. With simultaneous use with sulfasalazine, the concentration of betaxolol in the blood plasma increases.
special instructions
It should be used with caution in bronchial asthma and moderately severe COPD (start treatment with small doses and preferably under the control of external respiratory function; due to beta1-selectivity of betaxolol in case of an asthma attack while taking it, it is possible to arrest the beta2-adrenomimetic attack); in 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 a gradual increase); with AV block I degree (requires careful observation, including ECG control); with obliterating diseases of peripheral arteries,Raynaud's syndrome (with the exception of the severe form) (possibly increased violations of the peripheral circulation); with Prinzmetal's angina pectoris (an increase in angina attacks is possible; the use of a selective beta-1 blocker is possible only with the simultaneous use of vasodilators); with 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 (if QC is more than 20 ml / min, careful observation of the patient during the first few days of treatment; if QC is less than 20 ml / min and / or hemodialysis, correction of the dosage regimen is required); in case of hepatic insufficiency (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; decrease in the severity of precursors of hypoglycemia, such as tachycardia, palpitations and increased sweating); in psoriasis (beta-blockers may worsen the course of psoriasis); during desensitization therapy. The abolition of betaxolol should be carried out gradually, especially in patients with coronary artery disease, angina. Betaxolol does not affect the size of the pupil, therefore, in case of angle-closure glaucoma, the drug should be used only in combination with myotics. When transferring the patient to betaxolol after treatment with several antiglaucoma drugs, the latter are gradually canceled, at least 1 week per drug. With the simultaneous use of betaxolol in the form of eye drops and beta-blockers inside, it is possible to develop additive effects from both intraocular pressure and manifestations of the systemic action of beta-blockers. Before performing a planned operation, beta-blockers, incl. betaxolol should be undone. With topical application of Betaxolol, contact lenses should not be worn. It is not recommended to use Betaxolol in children. Influence on the ability to drive motor vehicles and control mechanisms With caution used in patients whose activities require increased attention and quick psychomotor reactions.