Timolol - instructions for use, dose, side effects, contraindications

A non-selective beta-adrenergic receptor blocker without sympathomimetic activity. With topical application lowers the intraocular pressure by reducing the formation of watery moisture and a small increase in its outflow. Reducing intraocular pressure, does not affect the accommodation and the size of the pupil, so there is no deterioration in visual acuity; does not reduce the quality of night vision.

The effect manifests itself 20 minutes after instillation, the maximum effect is 1-2 short-lived - 24 hours.

Pharmacokinetics:

After instillation of eye drops.in the moisture of the anterior chamber of the eye TSam - 1-2 hours. The active substance enters the systemic bloodstream by absorption through the conjunctiva, the mucous membrane of the nose and the lacrimal tract. The drug is metabolized by the enzyme system CYP2D6. Excretion of metabolites by the kidneys. In newborns and young children, the concentration of the active substance is significantly higher than its Cmax in adult plasma.

Indications:

Eye hypertension: open-angle glaucoma, secondary glaucoma (uveal, aphakic, post-traumatic); as an auxiliary drug: closed-angle glaucoma (in combination with myotics), congenital glaucoma (with ineffectiveness of other therapeutic measures), acute increase in intraocular pressure.

Contraindications:

Thyrosensitivity, dystrophic processes in the cornea, bronchial asthma, severe chronic obstructive pulmonary disease, sinus bradycardia, AV blockade of MI, decompensated chronic heart failure, cardiogenic shock, lactation period, children under 18 years of age .

Carefully:

SA blockade, arterial hypotension, atrophic rhinitis, pulmonary insufficiency,severe cerebrovascular insufficiency, diabetes mellitus, hypoglycemia, thyrotoxicosis, myasthenia gravis, peripheral circulation disorders (including Raynaud's syndrome), pheochromocytoma, pregnancy.

Dosing and Administration:

Adults instill in the conjunctival sac 1 drop 0.25% solution 2 times a day, with insufficient efficiency - 1 drop of 0.5% solution 2 times a day. With the normalization of intraocular pressure, the maintenance dose is 1 drop 0.25% once a day. The difference in the severity of the action of 2 concentrations is 10-15%.

Side effects:

Local reactions: conjunctival irritation - conjunctival hyperemia, lacrimation or tearing, photophobia, corneal epithelial edema, burning and itching in the eyes, hyperemia of the eyelid skin, short-term visual acuity; blepharitis, conjunctivitis, keratitis, with prolonged use, it is possible to develop a surface point keratopathy (decrease the transparency of the cornea) and decrease the sensitivity of the cornea, it is possible ptosis, rarely - diplopia.

Systemic reactions: paresthesia, rhinitis, nasal congestion, epistaxis, lowering of arterial pressure, collapse, bradycardia, bradyarrhythmia, AV blockade,reduction of myocardial contractility, worsening of manifestations of chronic heart failure; headache, dizziness, drowsiness; hallucinations, depression, myasthenia gravis, decreased potency; shortness of breath, bronchospasm, pulmonary insufficiency; nausea, vomiting, diarrhea, chest pain, ringing in the ears. Deceleration of the speed of the psychomotor reaction. Allergic reactions (including urticaria).

Overdose:

Symptoms: it is possible to develop general obesity effects characteristic of beta-adrenoblockers (dizziness, headache, arrhythmia, bradycardia, bronchospasm, irritation, vomiting).

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

Interaction:

Epinephrine, pilocarpine, systemic beta-blockers increase the effect.

It is not recommended simultaneous instillation of two different beta-blockers.

Simultaneous reception with eye drops containing epinephrine, can lead to mydriasis.

Strengthens the action of muscle relaxants and general anesthetics (48 hours before the general anesthesia, including with the use of peripheral muscle relaxants, it is necessary to stop taking the drug).

Against the background of drug treatment, intravenous administration of verapamil, diltiazem (possibly inhibition of AV conduction, development of bradycardia and lowering blood pressure) should be avoided.

With caution appoint with antihypertensive drugs, other beta-blockers, insulin or oral hypoglycemic drugs, glucocorticosteroids, psychoactive drugs, as well as drugs that are associated with increased epinephrine release.

Inhibitors of CYPIID6 (incl. quinidine, cimetidine) can increase the concentration of thymolol in the plasma, increasing the risk of systemic side effects of beta-blockers, (including a reduction in heart rate, depression).

Special instructions:

Control of efficacy is recommended to be carried out approximately 3-4 weeks after the start of therapy (not earlier than in 1-2 weeks). With prolonged use of thymolol, "weakening of the effect is possible. When applying, it is necessary to monitor the function of tearing, the integrity of the cornea and assess the magnitude of the visual fields at least once every 6 months. At least once a month, measure intraocular pressure.

The preservative contained in the preparation can be absorbed by soft contact lenses (causing a change in their Colors). May cause irritation to the eye when wearing contact lenses, therefore, any contact lenses should be removed before instillation and put on not earlier than 15 minutes after it.

When transferring patients to treatment with timolol, correction of refraction after the effects of previously used miotics may be necessary.

In the case of an upcoming surgical intervention with general anesthesia, it is necessary to cancel the drug 48 hours prior to surgery, because timolol strengthens the action of muscle relaxants and general anesthetics.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention, rapidity of psychomotor reactions and good vision (within 0.5 h after instillation into the eye). Beta-blockers (including topical application) can mask symptoms of hypoglycemia in patients with diabetes mellitus taking insulin or oral hypoglycemic dosage forms; symptoms of hyperthyroidism (including tachycardia).

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention, rapidity of psychomotor reactions and good vision (within 0.5 h after instillation into the eye).

Form release / dosage:

Eye drops 0.25% and 0.5%.

For 1 ml, 2 ml in a tube-kapelyshtsy polymer with a valve or 5 ml, 10 ml in a tube-dropper polymer with screw thread, ukuporennye screwed polymer caps.

On a tube-dropper paste labels, or text labels are applied directly on a tube-dropper method of jet print.

1 tube of a dropper of 5 ml, 10 ml or 5, 10 tube-droppers for 1 ml, 2 ml with instructions for use are a pack of cardboard.

Packaging:

For 1 ml, 2 ml in a tube-kapelyshtsy polymer with a valve or 5 ml, 10 ml in a tube-dropper polymer with screw thread, ukuporennye screwed polymer caps.

On a tube-dropper paste labels, or text labels are applied directly on a tube-dropper method of jet print.

1 tube of a dropper of 5 ml, 10 ml or 5, 10 tube-droppers for 1 ml, 2 ml with instructions for use are a pack of cardboard.

Storage conditions:

List B. In the dark place at a temperature of no higher than 25 ° C Keep out of reach of children.

After opening, use within 14 days.

Shelf life:

2 years..

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-007441/09

Date of registration:24.09.2009

The owner of the registration certificate:UPDATE OF PFC, CJSC UPDATE OF PFC, CJSC Russia

Manufacturer: & nbsp

UPDATE, PFC CJSC Russia

Representation: & nbspUPDATE OF PFC, CJSCUPDATE OF PFC, CJSC

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Timolol (Timolol)