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

Active ingredient: timolol maleate (in terms of timolol 2.5 mg or 5.0 mg.) Auxiliary substances: alkyldimethylbenzylammonium chloride (benzalkonium chloride) 0.1 mg, sodium dihydrogen phosphate (sodium phosphate mono-substituted 2-hydrochloride) - 7 , 26 mg, sodium [hydrophosphate] dodecahydrate (sodium phosphate disubstituted 12-water, disodium phosphate dodecahydrate) - 28.6 mg, water for injection - up to 1 ml.

Description:Transparent colorless or slightly colored liquid

Pharmacotherapeutic group:Antiglaucoma means β-blocker.

ATX: & nbsp

S.01.E.D. Beta-blockers

S.01.E.D.01 Timolol

Pharmacodynamics:

pharmachologic effect

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 of visual acuity and the quality of night vision does not decrease.

The effect manifests itself 20 minutes after instillation, the maximum effect - after 1-2 hours; the duration of action is 24 hours.

Pharmacokinetics:

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

Indications:

Eye hypertension, open-angle glaucoma, secondary glaucoma (uveal, aphakic, post-traumatic);

As an auxiliary drug: zakratougolnaya glaucoma (in combination with miotikami), congenital glaucoma (with ineffectiveness of other therapeutic measures), acute increase in intraocular pressure.

Contraindications:

Hypersensitivity, dystrophic processes in the cornea, bronchial asthma (including in the anamnesis), severe chronic obstructive pulmonary disease, sinus bradycardia, atrioventricular blockade of H-S st., Decompensated chronic heart failure, cardiogenic shock, children under 18 years of age, lactation period.

Carefully:

Sinoatrial blockade, II-III stage, arterial hypotension, atrophic rhinitis, pulmonary insufficiency, severe cerebrovascular insufficiency, diabetes mellitus, hypoglycemia, thyrotoxicosis, myasthenia gravis, simultaneous administration of other beta-adrenoblockers, pheochromocytoma, peripheral circulatory disturbance (including syndrome Raynaud), pregnancy.

Pregnancy and lactation:

The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.

If the drug was used immediately before delivery, the newborns should be carefully monitored for several days after birth.

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 of 0.25% once a day. The difference in the severity of the action of 2 concentrations is 10-15%.

Side effects:

Local reactions: irritation of the conjunctiva - congestion hyperemia,lacrimation or a decrease in teardrop, photophobia, corneal epithelial edema, burning and itching in the eyes, hyperemia of the eyelid skin, short-term impairment of 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, atrioventricular blockade, decreased 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-resorptive effects characteristic of beta-blockers (dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea, vomiting).

Treatment: immediately rinse, eye with water or 0.9% solution of sodium chloride, symptomatic therapy.

Interaction:

Epinephrine and pilocarpine increase the hypotensive effect of timolol. Simultaneous administration of eye drops containing epinephrine, can cause a dilated pupil (mydriasis).

Concomitant use with substances inhibiting the enzyme system CYP2D6 (amiodarone, quinidine, haloperidol, paroxetine, fluoxetine, citalopram, sertraline, terbinafine, ketoconazole, ritonavir, cimetidine) can provoke the appearance of symptoms of thymolol overdose, incl. expressed bradycardia (up to the frequency of cardiac contractions less than 40 per minute), in some cases - and deep lethargy. Strengthens the effect of muscle relaxants and general anesthetics (a few days before the general anesthesia with chloroform or ether or the use of peripheral muscle relaxants should stop taking the drug).

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

With caution appoint simultaneously with antihypertensive drugs, other beta-adrenoblockers, insulin or oral hypoglycemic drugs, glucocorticosteroid, psychoactive drugs

as well as with drugs, the effect of which is associated with increased epinephrine release.

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 timolol, the effect may be weakened.

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 deposited on soft contact lenses (causing a change in their color). 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 case of the forthcoming surgical intervention with the use of general anesthesia, it is necessary to cancel the drug 48 hours before the surgery, because timolol enhances the action of myorelaxants 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).

Possible masking of beta-adrenoblokatorami symptoms of hypoglycemia in patients taking insulin or oral hypoglycemic agents, symptoms of hyperthyroidism (including tachycardia).

Form release / dosage:

Eye drops 0.25% and 0.5%.

To 5 or 10 ml in bottles-droppers polyethylene. Each vial-dropper with instructions for use is placed in a pack of cardboard.

Packaging:

Eye drops 0.25% and 0.5%.

To 5 or 10 ml in bottles-droppers polyethylene. Each vial-dropper with instructions for use is placed in a pack of cardboard.

Storage conditions:

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

Keep out of the reach of children.

Shelf life:

3 years.After opening the vial, use within 1 month. Do not use the drug after the expiry date on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N002671 / 01

Date of registration:26.05.2008

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Representation: & nbspSYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products SYNTHESIS JSC Joint-Stock Kurgan Society of Medical Preparations and Products Russia

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Timolol-Akos (Timolol-AKOS)