Timolol-ACOS, eye drops 0.5% 5 ml

Timolol-ACOS is a non-selective beta-adrenoceptor blocker without sympathomimetic activity. When used topically it lowers intraocular pressure by reducing the formation of aqueous humor and slightly increasing its outflow. Decreasing intraocular pressure does not affect accommodation and pupil size, so there is no deterioration of visual acuity and quality of night vision. The action occurs 20 minutes after injection, the maximum effect – in 1-2 hours, the duration of action – 24 hours.

Pharmacokinetics

After instillation of eye drops in the moisture of the anterior chamber of the eye time to reach maximum concentration is 1-2 hours. The active substance enters the systemic bloodstream by absorption through the conjunctiva, nasal mucous membranes and the lacrimal tract. The drug is metabolized by the CYP2D6 enzyme system. Excretion of metabolites is by the kidneys. In infants the concentration of the active substance is significantly higher than its maximum concentration in adult plasma.

Indications

Elevated intraocular pressure, Glaucoma

• open angle glaucoma;
• secondary glaucoma (uveal, aphakic, posttraumatic);
• acute increase in ophthalmotonus;
• closed angle glaucoma (in combination with myotics).

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Active ingredient

Timolol

Composition

1 ml of eye drops contains:
Active ingredients: thymolol maleate (in terms of thymolol) – 5.0 mg.
Excipients: benzalkonium chloride, sodium phosphate dihydrate displaced, sodium phosphate displaced 12-water, water d/i.

How to take, the dosage

Adults and children over 1 year old:

• In the lower conjunctival sac of the affected eye (or eyes), 1 drop of 0.25% solution 2 times/day,
• In case of insufficient effectiveness, 1 drop of 0.
• After normalization of intraocular pressure – 1 drop of 0.25% solution 1 time/day

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Interaction

Epinephrine and pilocarpine enhance the hypotensive effect of timolol.

Concomitant use with reserpine may cause marked bradycardia or hypotension (if it is necessary to use this combination, close medical monitoring should be carried out).

Concomitant use with calcium channel blockers or cardiac glycosides may cause AV dysfunction, acute left ventricular failure, or arterial hypotension.

Timolol-ACOS potentiates the effects of muscle relaxants (therefore, the drug should be discontinued 48 h before the intended general anesthesia with peripheral muscle relaxants).

Special Instructions

During treatment at least once every 6 months, tear production, corneal integrity and visual fields should be monitored.

The effectiveness of the drug should be monitored 3-4 weeks after the start of therapy.

Contact lenses should be removed before injection and put on no earlier than 15 minutes after the procedure.

Two beta-adrenoblockers should not be injected into the eye simultaneously.

The effect may decrease with prolonged use.

The correction of refraction may be necessary when transferring patients to treatment with timolol maleate.

Impact on driving and operating ability

Cautious care should be taken with nighttime driving when using the drug.

Contraindications

• bronchial asthma;
• acute and chronic heart failure;
• cardiogenic shock;
• dystrophic corneal diseases;
• rhinitis;
• sinus bradycardia;
• AV-blockade of degree II and III;
• hypersensitivity to the drug components.

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Side effects

Local reactions: eyelid skin hyperemia, burning and itching in the eyes, conjunctival hyperemia, lacrimation or reduced lacrimation, transient visual acuity impairment, blepharitis, photophobia, corneal epithelial edema, conjunctivitis.

With long-term use of the drug it is possible to develop superficial pitting keratopathy (decreased corneal transparency), decreased corneal sensitivity, ptosis; rarely – diplopia.

Cardiovascular system disorders: decreased BP, bradycardia, bradyarrhythmia, AV blockade, heart failure, cardiac arrest.

Central nervous system disorders: paresthesias, dizziness, headache, somnolence, hallucinations, transient cerebral circulation disorder, depression.

Respiratory system: rhinitis, nasal congestion, shortness of breath, bronchospasm, pulmonary failure.

In the digestive system: nausea, vomiting, diarrhea.

Others: nasal bleeding, muscle weakness, impaired sexual function, decreased potency, collapse, allergic reactions (including urticaria).

Overdose

When administered topically, no symptoms of overdose have been described. In case of accidental ingestion there may be: nausea, vomiting, dizziness, headache, decreased blood pressure, bronchospasm, bradycardia.

Treatment: symptomatic therapy is carried out. If necessary, isoprenaline is administered intravenously to eliminate marked bradycardia or bronchospasm, dobutamine – in the development of arterial hypotension.

Pregnancy use

The use of the drug Timolol-ACOS during pregnancy is possible only when the expected benefits to the mother exceed the potential risk to the fetus.

Breast-feeding should be discontinued during the use of the drug.

Similarities

Arutimol, Okupres-E, Okumed, Timolol-Akos, Timolol Renewal, Timolol-SOLofarm