Betaxolol
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Clinical Pharmacology
Antiglaucoma remedy - beta-blocker
Indications
Reducing elevated intraocular pressure in patients with ophthalmic hypertension and primary open-angle glaucoma as monotherapy or in combination with other drugs.
Composition
1 ml of betaxolol hydrochloride 5.6 mg, which corresponds to the content of betaxolol 5 mg
Excipients: benzalkonium chloride - 0.1 mg, sodium chloride - 5.49 mg, disodium phosphate dihydrate - 3.579 mg, disodium edetate (Trilon B) - 0.5 mg, sodium dihydrogen phosphate dihydrate - 3.165 mg, water d / and - up to 1 ml.
Betaxolol is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Betaxolol-SOLOpharm | Grotex Ltd | Russia | eye drops |
Betaxolol | Moscow Endocrine Plant | Russia | pills |
Betaxolol | Moscow Endocrine Plant | Russia | eye drops |
Xonef | Sentiss Pharma | India | eye drops |
Betaftan | K.O.Romparm Company S.R.L | Romania | eye drops |
Lokren | Sanofi-aventis | France | pills |
Betoptic S | Alcon | USA | eye drops |
Betoptic | Alcon | USA | eye drops |
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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, so 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.
In case of insufficient clinical efficacy of monotherapy, additional therapy is prescribed.
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.
Transition from another antihypertensive therapy
When switching from therapy with one beta-blocker 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 start instillation of Betaxolol 0.25% in each affected eye 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 therapy with a hypotensive drug of another group, other than beta-blockers, the instillations of the previously prescribed drug are continued, with instillations of one drop of a 0.25% betaxolol solution in each affected eye twice a day. The next day, the previously applied treatment is canceled and therapy with betaxolol continues.
Use in the pediatric population
According to limited data, it can be recommended for reducing intraocular pressure in case of 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 in the minimum available concentration 1 drop once a day. With insufficient hypotensive effect, it is necessary to switch to use 2 times a day with an interval of 12 hours between instillations. Control of eye and systemic side effects is necessary within 1-2 hours after the first instillation.
Adverse reactions
Like other drugs in the form of eye drops, it 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 (
Violations by 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, itchy eyes, discharge from the eyes, the formation of crusts on the edges of the eyelids, eye irritation, disorders of the conjunctiva, conjunctival edema, eye hyperemia.
Rarely: cataract, decreased corneal sensitivity, eyelid redness.
Nervous system disorders
Often: headache.
Seldom: faint.
Frequency unknown: dizziness.
Heart disorders
Infrequently: bradycardia, tachycardia.
Frequency unknown: arrhythmia.
Vascular disorders
Rarely: hypotension.
Disorders of the respiratory system, organs of the piled cell and mediastinum
Infrequently: bronchospasm, shortness of breath, rhinitis.
Seldom: cough, rhinorrhea.
Disorders of the gastrointestinal tract
Infrequently: nausea.
Seldom: dysgeusia.
Violations of the skin and subcutaneous tissue
Rarely: dermatitis, rash, alopecia.
Disorders of the reproductive system and the breast
Seldom: decrease in a libido.
Mental disorders
Rarely: anxiety, insomnia, depression.
General disorders and reactions at the site of administration
Frequency unknown: asthenia.
Immune system disorders
With unknown frequency: hypersensitivity.
Other undesirable reactions were observed 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, slowing atrioventricular conduction, or worsening 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.
Violations 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.
Contraindications
- Hypersensitivity to betaxolol and other components of the drug;
- bradycardia;
- atrioventricular block II and III degree, uncontrolled by an artificial pacemaker;
- Sick sinus syndrome;
- sinoatrial block;
- cardiogenic shock;
- decompensated chronic heart failure;
- reactive diseases of the respiratory tract, including severe bronchial asthma (including in history);
- Severe chronic obstructive pulmonary disease.
Carefully:
Patients using β1-adrenergic blocking agents and (eye drops) should be treated under regular medical supervision due to the risk of a total potential effect on intraocular pressure and the appearance of undesirable systemic effects.
Despite the mild general effect of betaxolol (in the form of eye drops) on the body, care should be taken when prescribing it to patients with thyrotoxicosis and diabetes mellitus (especially unstable), since the drug can mask the manifestations of hypoglycemia.
Before surgery using general anesthesia, the drug should be gradually discontinued, since the drug can change the patient's response to the use of general anesthetics.
Drug interactions
Special studies of the interaction of betaxolol with other drugs has not been conducted.
In patients receiving and simultaneously taking orally other beta-blockers, the risk of unwanted reactions (both systemic and local) may be higher due to the 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), cardiac glycosides, parasympathomimetics, guanethidine, and catecholamine-depleting drugs, by using the same catecholamine cells, by using heart control glycosides, para-sympathomimetics, manganidine, and catecholamine-depleting catecholamines. effects such 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 - enhancing their vasoconstrictive affect.
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.
Pregnancy and Lactation
Pregnancy
Sufficient experience in the use of the drug during pregnancy is not. 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 with oral 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 during pregnancy, it is necessary to monitor the condition of the newborn during canine days of life.
Breast-feeding
Beta blockers are excreted in breast milk and can cause serious adverse reactions in breastfed babies. It is unlikely that with the 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 baby and the benefit of therapy for the mother.
Fertility
Data on the effect of betaxolol on fertility are not available.
Special instructions
Diabetes
Beta-blockers should be used with caution in patients with a tendency to spontaneous hypoglycemia and labile patients with diabetes mellitus, since these drugs can mask the signs and symptoms of acute hypoglycemia.
Thyrotoxicosis
Beta-blockers may mask some of the symptoms of hyperthyroidism (for example, tachycardia). In patients with suspected thyrotoxicosis, beta-blockers should not be abruptly discontinued, as this may cause an increase in symptoms.
Myasthenia
Beta-blockers may cause symptoms and signs similar to those with myasthenia gravis (for example, diplopia, ptosis, and general weakness).
Surgery
The anesthesiologist should be informed that the patient is taking. Before a planned operation, beta-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 bronchial asthma with the use of certain beta-blockers in ophthalmology.
It should be used with caution in patients with moderate to moderate asthma (including a history of), and in patients with chronic obstructive pulmonary disease of mild to moderate severity.
Anaphylactic reactions
When betaxolol is used by patients with atopy or severe anaphylactic reactions to various allergens, a more pronounced reaction to repeated administration of these allergens and immunity to standard doses of epinephrine may occur when arresting anaphylactic reactions.
Betaxolol should be used with caution in patients with severe peripheral circulatory disorders (ie, 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 are described, including death from bronchospasm in patients with bronchial asthma and death from heart failure with betaxolol.
Heart disorders
In patients with cardiovascular diseases (eg, 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 of other groups. Careful monitoring of the development of signs of exacerbation of the disease 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. does not affect the diameter of the pupil; therefore, with open-angle glaucoma, the drug should be used only in combination with mystics.
Choroid detachment
Cases of detachment of the choroid when using drugs that reduce the production of intraocular fluid (for example, timolol, acetazolamide) after fistulizing antiglaucomatous operations are described.
The product contains a preservative, 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.
Impact on the ability to drive trans. Wed and fur .:
During the period of treatment, care must be taken when driving and occupying other potentially dangerous activities that require high concentration of attention and speed of psychomotor reactions.
Overdosage
If the vial contents 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, wash the eyes with warm water.
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