Betoftan eye drops 0.5%, 5 ml

• Ocular hypertension;

• chronic open-angle glaucoma;

• angle-closure glaucoma (in combination with miotics).

The drug is used topically. Instill 1-2 drops into the conjunctival sac 2 times / day. In some patients, intraocular pressure stabilization occurs within several weeks, therefore it is recommended to control intraocular pressure during the first month of treatment. If the required level of intraocular pressure is not achieved with Betoftan monotherapy, additional therapy should be prescribed.

Eye drops in the form of a clear solution, colorless or light yellow with a brown tint.

1 ml

betaxolol (in the form of hydrochloride) 5 mg

Excipients: sodium hydrogen phosphate dodecahydrate, sodium dihydrogen phosphate monohydrate, sodium chloride, disodium edetate dihydrate, benzalkonium chloride, purified water.

• Sinus bradycardia;

• AV block II and III degree;

• SSSU;

• children and adolescents under 18 years of age (due to the lack of data on efficacy and safety); hypersensitivity to the components of the drug.

  The drug is prescribed with caution in diabetes mellitus, thyrotoxicosis, simultaneous administration of oral beta-blockers, Raynaud's syndrome, pheochromocytoma, bronchial asthma, chronic obstructive bronchitis, AV blockade of the 1st degree, heart failure.

pharmachologic effect

Antiglaucoma drug. Betaxolol is a selective beta1-blocker without intrinsic sympathomimetic activity. Does not have a membrane stabilizing (local anesthetic) effect. When applied topically, betaxolol reduces both increased and normal intraocular pressure, due to a decrease in the production of intraocular fluid. The onset of the hypotensive effect is usually observed 30 minutes after application of the drug, and the maximum decrease in ophthalmotonus occurs after about 2 hours. After a single instillation, the effect on ophthalmotonus persists for 12 hours. Betaxolol does not cause miosis, accommodation spasm, hemeralopia (unlike miotics).

Pharmacokinetics

Suction

Betaxolol is highly lipophilic, as a result of which it penetrates well through the cornea into the anterior chamber of the eye, Cmax in the anterior chamber is determined 20 minutes after instillation. When applied topically, systemic absorption is low, the plasma concentration is below the detection threshold (2 ng / ml).

Distribution and excretion

Plasma protein binding - 50%. “1 / 2 - 14-22 hours. It is excreted by the kidneys (15% unchanged). Permeability through the BBB and the placental barrier is low, secretion in breast milk is insignificant.

Side effect

Local reactions: short-term discomfort in the eyes after instillation, lacrimation; in some cases - decreased sensitivity of the cornea, redness of the eye, keratitis, photophobia, anisocoria, blurred vision, itching, dry eyes, allergic reactions. Systemic side effects are rare. From the side of the central nervous system: dizziness, drowsiness, insomnia, headache, depression, increased symptoms of myasthenia gravis. From the side of the cardiovascular system: bradycardia, impaired cardiac conduction, heart failure. From the respiratory system: dyspnea, bronchospasm, bronchial asthma, respiratory failure. From the digestive system: nausea.

Application during pregnancy and lactation

The use of the drug during pregnancy and lactation (breastfeeding) is possible only if the intended benefit to the mother outweighs the potential risk to the fetus or child.

Application in children

Contraindicated in children and adolescents under 18 years of age.

special instructions

Betoftan contains a preservative, benzalkonium chloride, which can be adsorbed by soft contact lenses and have a damaging effect on eye tissue. Therefore, patients wearing soft contact lenses should remove them before applying drops and reinstall them no earlier than 20 minutes after instillation. To avoid contamination of the pipette, do not touch the eye while instilling. Beta-blockers should be used with caution in patients with a tendency to hypoglycemia, since these drugs can mask the symptoms of acute hypoglycemia. Beta-blockers can mask some of the symptoms of hyperthyroidism (eg, tachycardia). In patients with suspected thyrotoxicosis, beta-blockers should not be abruptly canceled, because this can cause increased symptoms. Beta-blockers can cause symptomssimilar to those in myasthenia gravis (for example, diplopia, ptosis, general weakness). Before the planned operation, beta-blockers should be gradually (not at once) canceled 48 hours before general anesthesia, because during general anesthesia, they can reduce the sensitivity of the myocardium to sympathetic stimulation necessary for the heart to work. Care should be taken when prescribing beta-blockers to patients with significantly reduced respiratory function. Despite the fact that clinical studies have shown the absence of the effect of betaxolol on respiratory function, the possibility of hypersensitivity to the drug should not be ruled out. Patients taking beta-blockers may have a history of atopy or anaphylactic reactions. In the event of repeated reactions, such patients may be insensitive to the usual doses of epinephrine,necessary for the relief of anaphylaxis. During instillation, the drug can enter the systemic circulation. Thus, the same side effects can be observed as with IV, and parenteral administration of beta-blockers. Betoftan has a minimal effect on blood pressure and heart rate. However, caution should be exercised when prescribing it to patients with grade I AV block or heart failure. Treatment should be discontinued when the first signs of cardiovascular decompensation appear.However, caution should be exercised when prescribing it to patients with grade I AV block or heart failure. Treatment should be discontinued when the first signs of cardiovascular decompensation appear.However, care should be taken when prescribing it to patients with grade I AV block or heart failure. Treatment should be discontinued when the first signs of cardiovascular decompensation appear.

Influence on the ability to drive vehicles and use mechanisms

Patients in whom, after instillation of the drug, the clarity of vision temporarily decreases, it is not recommended to engage in activities that require increased attention and response until it is restored.

Overdose

Currently, no cases of Betoftan overdose have been reported. In case of an overdose of beta1-blockers, the following symptoms may occur: arterial hypotension, bradycardia, acute heart failure. Treatment: symptomatic. In case of contact with the eyes of an excessive amount of the drug, rinse the eyes with warm water.

Drug interactions

With the simultaneous use of Betoftan and an adrenaline solution for ophthalmic use, in some cases, the development of mydriasis is possible. When using the drug Betoftan in combination with drugs that deplete the reserves of catecholamines (such as reserpine), there may be an increase in effects such as lowering blood pressure and bradycardia. With the simultaneous use of the drug Betoftan and beta-blockers for oral administration, the risk of side effects (both local and systemic) increases due to the additive effect. Care should be taken when using the drug Betoftan together with adrenergic psychotropic drugs due to the possible enhancement of their action. With the simultaneous appointment of muscle relaxants and hypoglycemic agents, an increase in their action may be observed.When used together with sympathomimetics, an increase in their vasoconstrictor effect is noted. If necessary, Betoftan can be used in combination with other topical ophthalmic drugs. In this case, the interval between their application should be at least 10 minutes.