Betaxolol Solofarm eye drops 0.5% 5 ml N1
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Active ingredients
Betaxolol
Release form
Drops
Composition
The composition of the drug per 1 ml of the active substance: Timolol - 5.0 mg (as timolol maleate) - 6.84 mg excipients: Benzalkonium chloride - 0.10 mg Sodium dihydrogen phosphate dihydrate - 6.10 mg Sodium hydrophosphate dihydrate - 15.16 mg Water for injection - up to 1 ml
Pharmacological effect
Betaxolol is a selective β1-blocker without its own sympathomimetic activity. Practically does not have a membrane stabilizing (local anesthetic) effect. The selective effect of betaxolol on β1 -adrenoreceptors is not absolute, since when used in high doses, betaxolol may affect β2 –adrenoreceptors, located mainly in the smooth muscles of the bronchi and blood vessels. The blockade of beta-adrenoreceptors in the bronchi and bronchioles increases the resistance of the respiratory tract, due to the absence of antagonism to parasympathomimetic activity. Such an effect in patients with asthma or other bronchospastic conditions can be a potential hazard. The blockade of beta-adrenoreceptors reduces cardiac output in both healthy subjects and patients with heart disease. In patients with severely impaired myocardial function, blockade of beta-adrenergic receptors may weaken the stimulating effect of the sympathetic nervous system, which is necessary to maintain adequate heart function. Betaxolol has a less pronounced effect on the cardiovascular and respiratory systems in comparison with other beta-blockers. Application in the form of eye drops is accompanied by a decrease in intraocular pressure by reducing the production of intraocular fluid. The hypotensive effect of betaxolol is realized both in relation to elevated and normal intraocular pressure. Betaxolol improves eye circulation (perfusion). Betaxolol does not cause miosis, spasm of accommodation, hemeralopia, the effect of "veil" before the eyes (as opposed to miotics).
Pharmacokinetics
Betaxolol is characterized by a high degree of lipophilicity, as a result of which it is rapidly absorbed by the corneal epithelium, and its high concentration is created in the intraocular fluid.The onset of the effect (reduction of intraocular pressure) is 30 minutes, the maximum effect after 2 hours, the duration of action 24 hours. The half-life (T1 / 2) is 12-16 hours, the bond with plasma proteins is 50%. Excreted mainly by the kidneys, to a small extent with feces, in the form of two carboxylic acids and in unchanged form (about 16% of the applied dose). The permeability through the hematoencephalic barrier (BBB) and the placental barrier is low, the secretion with breast milk is insignificant.
Indications
Reducing elevated intraocular pressure in patients with ophthalmic hypertension and primary open-angle glaucoma as monotherapy or in combination with other drugs.
Contraindications
-hypersensitivity to betaxolol and other components of the drug; - bradycardia; -atrioventricular block II and III degree not controlled by an artificial pacemaker; - syndrome of weakness of the sinus node; -Sinoatrial blockade; cardiogenic shock; -compensated chronic heart failure; -reactive diseases of the respiratory tract, including severe bronchial asthma (including a history of); - Severe chronic obstructive pulmonary disease.
Precautionary measures
Patients using β-adrenergic blocking agents and betaxolol (eye drops) should be treated under regular medical supervision due to the risk of the total potential effect on intraocular pressure and the appearance of unwanted systemic effects. Despite the mild general effect of betaxolol (in the form of eye drops) on body, care should be taken when prescribing it to patients with thyrotoxicosis and diabetes mellitus (especially unstable), since the drug can mask pro detecting gipoglikemii.Pered surgery with general anesthesia should gradually stop the use of the drug since the drug can alter the patient's reaction to the use of general anesthetics.
Use during pregnancy and lactation
Fertility Data on the effect of betaxolol on fertility are not available. Pregnancy There is no sufficient experience on the use of the drug during pregnancy. The use of Betaxolol during pregnancy is possible only if the expected benefit to the mother outweighs the possible risk to the fetus. According to the results of epidemiological studies, malformative effects were not detected. It is known that oral administration of beta-blockers, there is a risk of intrauterine growth retardation.In addition, newborns may experience signs and symptoms of beta-blockade (such as bradycardia, hypotension, respiratory distress syndrome, and hypoglycemia) in cases where beta-adrenergic blockers were taken by the mother before delivery. When using the drug betaxolol during pregnancy, it is necessary to monitor the condition of the newborn during the first days of life. Breastfeeding Beta-blockers are excreted in breast milk and can cause serious adverse reactions in breastfed babies. It is unlikely that with topical application of therapeutic doses of betaxolol in breast milk there will be a sufficient amount of the drug in order to cause the development of clinical symptoms of beta-adrenergic blockade in newborns. Due to the fact that the risk of systemic effects cannot be excluded, a decision should be made to stop breastfeeding or cancel therapy with betaxolol, taking into account the need to continue breastfeeding for the child and the benefit of therapy for the mother.
Dosage and administration
Locally. 1-2 drops in the conjunctival sac 2 times a day. In some patients, stabilization of intraocular pressure occurs within a few weeks, therefore it is recommended to control intraocular pressure during the first month of treatment. The duration of the drug is determined by the attending physician, depending on the effectiveness of therapy. With insufficient clinical efficacy of monotherapy prescribed additional therapy. The use of two beta-blockers for local use is not recommended. To reduce the systemic absorption of the drug, nasolacrimal occlusion is recommended - pressing the inner edges of the eyelids for 2-3 minutes after instillation of the drug. Switching from another antihypertensive therapy When switching from one beta-blocker therapy to another drug from the group of beta-blockers, it is recommended to complete a full day of therapy with the previously used antihypertensive agent, and the next day to start instillation of Betaxolol 0.25% in each affected eye with 1 drop 2 times a day. In the absence of an adequate response to therapy, the dose may be increased to 1-2 drops of a 0.5% betaxolol solution in each affected eye twice a day.When switching from another group of therapies to the hypotensive drug, other than beta-blockers, the instillations of the previously prescribed drug are continued with the addition of instillations of one drop of a 0.25% betaxolol solution to each affected eye twice a day. The next day, the previous treatment is canceled and therapy with betaxolol continues. Use in the pediatric population According to limited data, betaxolol can be recommended for reducing intraocular pressure in true congenital glaucoma, infantile and juvenile congenital glaucoma in the preoperative period or in the case of ineffective surgical treatment. Before using the drug, it is necessary to carefully evaluate the risks and benefits of using betaxolol in the pediatric population by carefully collecting anamnesis for systemic disorders. In case the benefit exceeds the risk, it is recommended to use betaxolol in the minimum available concentration of 1 drop 1 time per day. With insufficient hypotensive effect, it is necessary to switch to use 2 times a day with an interval between instillations of 12 hours. Control of eye and systemic side effects is necessary within 1-2 hours after the first instillation.
Side effects
Like other drugs in the form of eye drops, betaxolol can enter the systemic circulation, leading to the development of systemic side effects. Undesirable reactions are presented in accordance with the following gradation of the frequency of their development: very often (> 10%); often (> 1, <10%); infrequently (> 0.1, <1%); rarely (> 0.01, <0.1%); very rarely (<0.01%); frequency is unknown (according to the available data it is not possible to determine the frequency of development). Disturbances from the organ of vision. Very often: discomfort in the eyes. Often: blurred vision, increased tearing. Infrequently: punctate keratitis, keratitis, conjunctivitis, blepharitis, visual impairment, photophobia, eye pain, dry eye syndrome, asthenopia, blepharospasm, itching in the eye, discharge from the eyes, formation of crusts at the edges of the eyelids, eye irritation, irregularity of the conjunctiva, conjunctival edema, eye hyperemia. Rarely: cataract, decreased sensitivity of the cornea, redness of the eyelids. Nervous system disorders Often: headache.Seldom: faint. Frequency unknown: dizziness. Disturbances from the heart Infrequently: bradycardia, tachycardia. Frequency unknown: arrhythmia. Vascular disorders Rarely: hypotension. Disturbances of the respiratory system, organs of the piles of cells and mediastinum Infrequently: bronchospasm, shortness of breath, rhinitis Rarely: cough, rhinorrhea. Disorders of the gastrointestinal tract Infrequently: nausea. Seldom: dysgeusia. Disturbances of the skin and subcutaneous tissues Rarely: dermatitis, rash, alopecia. Disorders of the reproductive system of the willow system and the mammary gland Rarely: decreased libido. Mental disorders Rarely: anxiety, insomnia, depression. General disorders and reactions at the injection site. Frequency unknown: asthenia. Immune system disorders C unknown frequency: hypersensitivity. There were other adverse reactions that may develop when using local beta-blockers (information about the frequency of development is absent): Immune system disorders: systemic allergic reactions, including angioedema, urticaria, local and generalized rash, itching, anaphylactic reactions. Metabolic and nutritional disorders: hypoglycemia. Mental disorders: nightmares, memory loss, hallucinations, psychosis, confusion. Nervous system disorders: cerebrovascular disorders, cerebral ischemia, exacerbation of signs and symptoms of myasthenia gravis, paresthesia. Violations on the part of the organ of vision: detachment of the choroid after fistulatory anti-glaucoma operations, corneal erosion, ptosis, diplopia. Cardiac abnormalities: chest pain, palpitations, edema, chronic heart failure, atrioventricular block, cardiac arrest, heart failure, delayed atrioventricular conduction, or worsening of the degree of blockade. Vascular disorders: Raynaud's phenomenon, cooling and cyanosis of the hands and feet, aggravation of intermittent claudication. Disorders of the respiratory system, organs of the chest and mediastinum: bronchospasm (mainly in patients with a history of bronchospastic diseases).Disorders of the gastrointestinal tract: dyspepsia, diarrhea, dry mouth, abdominal pain, vomiting. Disorders of the skin and subcutaneous tissues: psoriasis rash or exacerbation of psoriasis. Disorders of the musculoskeletal system: myalgia. Violations of the genital and breast organs: sexual dysfunction, impotence. General disorders and reactions at the injection site: fatigue.
Overdose
If the contents of the vial are accidentally swallowed, symptoms of beta blockade may develop, including bradycardia, hypotension, acute heart failure and bronchospasm. Treatment of symptoms of overdose should be symptomatic and supportive. In case of topical application of an excess amount of the drug, it is necessary to wash the eyes with warm water.
Interaction with other drugs
Special studies of the interaction of Betaxolol with other drugs has not been conducted. In patients receiving betaxolol and simultaneously taking other beta-blockers orally, the risk of undesirable reactions (both systemic and local) may be higher due to a possible additive effect. Such patients should be under close medical supervision. With the simultaneous appointment of beta-blockers for local ophthalmic use with oral forms of slow calcium channel blockers, beta-blockers, antiarrhythmic drugs (including amiodarone), cardiac glycosides, parasympathomimetics, guanethidine, and drugs that deplete catecholamines. there is an increase in such effects as lowering blood pressure and severe bradycardia. There were cases of the development of mydriasis with simultaneous use of beta-blockers and epinephrine. With the simultaneous appointment of betaxolol with muscle relaxants and hypoglycemic agents, an increase in the action of the latter may be observed. Beta-blockers can reduce the effect of adrenaline used to relieve anaphylactic reactions. It should be used with extreme caution in patients with atopy or anaphylaxis in history. When combined with sympathomimetics, their vasoconstrictive effect is enhanced.Caution must be exercised in the combined use of betaxolol and adrenergic psychotropic drugs due to a possible increase in their action. If necessary, it can be used in combination with other local ophthalmologic preparations, in this case, the interval between their use should be at least 10 minutes.
special instructions
Diabetes mellitus Beta-blockers should be used with caution in patients with a tendency to spontaneous hypoglycemia and patients with diabetes mellitus, as these drugs can mask the signs and symptoms of acute hypoglycemia. Thyrotoxicosis Beta-blockers may mask some of the symptoms of hyperthyroidism (eg, tachycardia). In patients with suspected thyrotoxicosis, beta-blockers should not be abruptly discontinued, as this may cause an increase in symptoms. Myasthenia Beta-blockers can cause symptoms and signs similar to those with myasthenia gravis (for example, diplopia, ptosis, and general weakness). Surgery The anesthetist must be informed that the patient is taking betaxolol. Before the planned operation, the beta-adrenergic blockers should be gradually (not simultaneously!) Canceled 48 hours before general anesthesia, since during general anesthesia, they can reduce the sensitivity of the myocardium to sympathetic stimulation necessary for the heart to work (for example, they can block the action of adrenaline). Pulmonology There are reports of respiratory reactions, including death due to bronchospasm, in patients with asthma when using some beta-blockers in ophthalmology. Betaxolol should be used with caution in patients with moderate to moderate bronchial asthma (including history), and in patients with chronic obstructive pulmonary disease of mild and moderate severity. Anaphylactic reactions When betaxolol is used by patients with atopy or severe anaphylactic reactions to various allergens, a more pronounced reaction to the repeated administration of these allergens and immunity to standard doses of epinephrine can be observed when arresting anaphylactic reactions.Betaxolol should be used with caution in patients with severe disorders of the peripheral circulation (ie, in patients with severe Raynaud's disease or Raynaud's syndrome, as well as with pheochromocytoma). With local administration, beta-blockers can enter the systemic circulation and cause undesirable reactions from the cardiovascular, pulmonary and other systems. Cases of severe respiratory and cardiovascular disorders, including death from bronchospasm in patients with bronchial asthma and death from heart failure, have been described with betaxolol. Cardiac disorders In patients with cardiovascular diseases (for example, coronary heart disease, Prinzmetal angina pectoris, heart failure) and arterial hypotension, therapy with beta-blockers should be critically evaluated with consideration of the possibility of treatment with drugs from other groups. Careful monitoring of the development of signs of exacerbation and adverse reactions in patients with cardiovascular diseases is needed. Corneal diseases Beta-blockers can cause dry eyes. In patients with corneal diseases, the drug should be used with caution. The main pathogenetic aspect of the treatment of angle-closure glaucoma is the need to open the anterior chamber angle, which is achieved by narrowing the pupil with the help of miotics. Betaxolol does not affect the diameter of the pupil, therefore, in case of angle-closure glaucoma, the drug should be used only in combination with myotics. Choroid detachment The choroidal detachment is described when using drugs that reduce the production of intraocular fluid (eg, timolol, acetazolamide) after fistulizing antiglaucomatous operations. The drug contains preservative benzalkonium chloride, which can cause eye irritation and discoloration of soft contact lenses. Direct contact of the drug with soft contact lenses should be avoided. Patients using contact lenses, before using the drug should be removed lenses and set them back no earlier than 15 minutes after instillation.