Composition, form of production and packaging
Drops of eye 0.5% in the form of a clear solution from colorless to light yellow color.
1 ml
betaxolol (in the form of hydrochloride) 5 mg
Excipients: benzalkonium chloride, hypromellose, sodium chloride, sodium hydroxide, disodium edetate, water d / u.
5 ml - a vial of a dropper plastic (1) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2011.
PHARMACHOLOGIC EFFECT
Antiglaucoma preparation. Selective beta- 1- adrenoblocker without internal sympathomimetic activity. Does not have a membrane-stabilizing (local anesthetic) action.
With topical application, betaxolol reduces intraocular pressure by reducing the production of intraocular fluid.
The onset of hypotensive action is observed 30 minutes after instillation, the maximum effect develops after 2 hours. After a single instillation, the effect on the ophthalmotonus persists for 12 hours.
Betaxolol (in comparison with other beta-adrenoblockers) does not cause a decrease in blood flow in the optic nerve.
The use of eye drops XonefВ® does not lead to the formation of miosis, spasm of accommodation, hemeralopia (in contrast to myotics).
PHARMACOKINETICS
Betaxolol is highly lipophilic, as a result of which it penetrates well through the cornea into the anterior chamber of the eye. C max (1.17 mg / ml) in the anterior chamber is determined 20 minutes after instillation. Penetrates into the systemic circulation. T 1/2 from the intraocular fluid for about 1 hour T 1/2 from the blood plasma 16-22 h. Excretion mainly through the kidneys.
INDICATIONS
As a monotherapy:
- to reduce intraocular pressure.
In combination with other drugs with:
- open-angle glaucoma;
ocular hypertension.
DOSING MODE
The drug is instilled in the conjunctival sac 1-2 drops 2 times / day.
In some patients, intraocular pressure stabilization occurs within a few weeks, therefore it is recommended to monitor intraocular pressure during the first month of treatment.
With insufficient clinical efficacy of monotherapy, additional therapy is prescribed.
SIDE EFFECT
From the side of the organ of vision: often - short-term discomfort in the eyes after instillation, lacrimation; in some cases - a decrease in the sensitivity of the cornea, redness of the eyes, punctate keratitis, photophobia, anisocoria, photophobia, itching, a feeling of "dryness" of the eyes, allergic reactions.
Systemic side effects are rare:
From the side of the central nervous system: dizziness, nausea, drowsiness, insomnia, headache, depression, increased symptoms of myasthenia gravis.
From the cardiovascular system: bradycardia, cardiac conduction disorder and heart failure.
On the part of the respiratory system: dyspnea, bronchospasm, bronchial asthma, respiratory failure.
CONTRAINDICATIONS
- sinus bradycardia;
- AV blockade II and III degree;
- severe heart failure;
- cardiogenic shock;
- arterial hypotension;
- children's age till 18 years;
- Hypersensitivity to the components of the drug.
With caution should apply the drug with thyrotoxicosis, myasthenia gravis, diabetes mellitus, Raynaud's syndrome, pheochromocytoma, bronchial asthma, chronic obstructive bronchitis.
PREGNANCY AND LACTATION
Sufficient experience in the use of KsonefВ® during pregnancy and lactation is not available.
The use of the drug during pregnancy and lactation (breastfeeding) is possible only if the intended benefit to the mother exceeds the potential risk to the fetus or child.
SPECIAL INSTRUCTIONS
Caution is prescribed to patients with diabetes mellitus, since beta-blockers may mask the symptoms of acute hypoglycemia.
With caution appoint the drug to patients with thyrotoxicosis, tk. beta-blockers may mask the symptoms of thyrotoxicosis (eg, tachycardia). Patients with suspected thyrotoxicosis should not abstain from beta-blockers, this can cause an increase in symptoms.
It should be borne in mind that beta-blockers can cause symptoms similar to those in myasthenia gravis (diplopia, ptosis, general weakness).
Caution should be given to beta-blockers in patients with severe impairment of the function of the respiratory system. Despite the fact that in clinical studies the absence of betaxolol in the ophthalmic dosage form on the function of external respiration has been shown, it is impossible to exclude the possibility of hypersensitivity to the drug.
Before the planned surgery, you should gradually cancel the beta-blockers 48 hours before the general anesthesia, tk. during general anesthesia, they can reduce the sensitivity of the myocardium to sympathetic stimulation.
Patients who use beta-blockers may have a history of atopy or anaphylactic reactions. In the case of the development of repeated reactions of hypersensitivity, such patients may not be sensitive to the usual doses of epinephrine (adrenaline) necessary for arresting anaphylaxis.
The drug should be administered with caution to patients with Reynaud's syndrome or pheochromocytoma.
When instilled in the eye, beta-blockers can be absorbed into the systemic circulation. In this case, the same side effects can be noted, as in systemic application. Cases of severe respiratory and cardiovascular disorders, including bronchospasm with fatal outcome in patients with bronchial asthma and death from heart failure are described.
XonefВ® has minimal impact on blood pressure and heart rate. However, care should be taken when administering the drug to patients with grade I AV blockade and mild to moderate heart failure. Treatment with XonefВ® should be stopped immediately if the first symptoms of cardiovascular decompensation appear.
XonefВ® contains a preservative of benzalkonium chloride, which can be deposited on soft contact lenses and have a toxic effect on the eye tissue. Therefore, patients wearing contact lenses should be removed before using drops and installed back no earlier than 20 minutes after instillation.
Impact on the ability to drive vehicles and manage mechanisms
If, after the application of droplets, patients temporarily lose visual clarity, it is not recommended to drive vehicles and engage in activities requiring increased attention and reaction before recovery.
OVERDOSE
If eye contact occurs in excess of the drug, wash your eyes with warm water.
Symptoms: with an overdose of beta 1- adrenoblokatorov can be observed a decrease in blood pressure, bradycardia, acute heart failure.
Treatment: conduct symptomatic therapy.
DRUG INTERACTION
With the simultaneous use of XonefВ® and beta-adrenoblockers for oral administration, the risk of side effects (both local and systemic) is increased due to the additive effect (therefore patients receiving this combination of drugs should be under medical supervision).
When XonefВ® is used in combination with preparations depleting catecholamine stores (such as reserpine), a decrease in blood pressure and bradycardia can occur.
With the simultaneous appointment of muscle relaxants and hypoglycemic agents, there may be an increase in their effect.
When combined with sympathomimetics, they intensify their vasoconstrictive effect.
Caution should be exercised in the joint use of XonefВ® and psychotropic drugs as a result of the possible intensification of their action.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a place protected from light, inaccessible to children at a temperature of no higher than 30 В° C; Do not freeze. Shelf life - 2 years.
Shelf life after opening the bottle is 45 days.
