Timolol, eye drops 0.5% 5 ml tube-cup

Timolol is a non-selective beta-adrenoceptor blocker without sympathomimetic activity. When used topically, it lowers intraocular pressure by reducing aqueous humor formation and slightly increasing its outflow.

Lowering intraocular pressure does not affect accommodation and pupil size, so there is no deterioration in 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.

The 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

Active ingredient

Composition

How to take, the dosage

Adults are injected into the conjunctival sac with 1 drop of 0.25 % solution 2 times a day, in case of insufficient effectiveness – with 1 drop of 0.5 % solution 2 times a day. With normalization of intraocular pressure the maintenance dose is 1 drop of 0.25 % solution 1 time a day. The difference in the effect of 2 concentrations is 10-15%.

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Interaction

Special Instructions

Long-term use increases triglyceride levels in blood plasma, therefore the drug is used with special caution in patients with liver and kidney function abnormalities, diabetes mellitus (especially of labile course).

When using the drug at least once every 6 months the tear emission function and the state of visual fields should be checked, and the cornea should be examined.

Impact on the ability to drive vehicles and operate machinery

At the time of treatment, one must refrain from potentially hazardous activities requiring increased attention and quick psychomotor reactions.

When used in ophthalmology immediately after instillation, visual acuity may decrease and psychomotor reactions may be slowed, so refrain for 30 minutes from engaging in potentially hazardous activities requiring increased attention.

Contraindications

With caution
SA blockade, arterial hypotension, atrophic rhinitis, pulmonary insufficiency, severe cerebrovascular insufficiency, diabetes, hypoglycemia, thyrotoxicosis, myasthenia, peripheral circulatory disorders (includingincluding Raynaud’s syndrome), pheochromocytoma, pregnancy.

Side effects

Visually: when used topically irritation and hyperemia of conjunctiva, eyelid skin, burning and itching in the eyes, lacrimation, photophobia, corneal epithelium edema, pitting superficial keratopathy, corneal hypoesthesia, diplopia, ptosis, dry eyes are possible. In case of fistulizing antiglaucoma operations retinal detachment may develop in the postoperative period.

When used systemically, heart failure, bradycardia, AV-blockade, arterial hypotension; headache, sleep disturbances, nightmares, asthenia, agitation, depression, paresthesias and coldness of extremities are possible; nausea, vomiting, diarrhea; shortness of breath, bronchospasm; muscle weakness; skin allergic reactions, exacerbation of psoriasis, dry conjunctivae.

Overdose

Symptoms: possible development of general resorptive effects typical for beta-adrenoblockers (dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea, vomiting).
Treatment: immediately flush eyes with water or 0.9% NaCl solution, symptomatic therapy.

Treatment: immediately flush eyes with water or 0.9% NaCl solution, symptomatic treatment.

Pregnancy use

The use of Timolol during pregnancy is possible only when the expected benefit to the mother outweighs the potential risk to the fetus.

If the drug was used immediately prior to delivery, newborns should be closely monitored for several days after birth.

The safety and effectiveness in children has not been studied.

Similarities