Timolol-MEZ - instructions for use, doses, side effects, contraindications

Non-selective blocker of p-adrenergic receptors 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 observed after 1-2 hours. Duration 24 hours.

Pharmacokinetics:

Timolol quickly penetrates the cornea into the tissues of the eye. After instillation in the moisture of the anterior chamber, the maximum concentration (Cmax) in the blood plasma is reached after 1-2 hours. It enters the systemic bloodstream in an insignificant amount by absorption through the conjunctiva, the mucous membranes of the nose and the lacrimal tract.

The amount of timolol in blood plasma is about 0.824 ng / ml and is kept up to the detection threshold in the flow. 12 hours. In newborns and small children, Timolol's stach significantly exceeds its Stach in adult blood plasma. The half-life (T1 / 2) of timolol is 4.8 hours after topical administration. Metabolism of timolol occurs in two ways: with the formation of an ethanolamine side chain on the thiadiazole ring with the formation of an ethanol side chain in morpholine nitrogen and a similar side chain with a carbonyl group attached to nitrogen. Metabolism of timolol is carried out by the isoenzyme CYP2D6. Timolol and the resulting metabolites are mainly excreted by the kidneys. About 20% of timolol is excreted unchanged, the rest is kidney.

Indications:

Indications for use

Open angle glaucoma, secondary glaucoma (uveal, aphakic, posttraumatic), ocular hypertension, angle-closure glaucoma (in combination with miotics).

Contraindications:

Dystrophic diseases of the cornea, rhinitis, bronchial asthma, sinus bradycardia, atrioventricular blockade of II and III degree, acute and chronic heart failure, cardiogenic shock, severe chronic obstructive pulmonary disease, hypersensitivity to the drug components, lactation period, children under 1 year.

If you have any of these diseases, consult a doctor before taking the drug.

Carefully:

Cerebrovascular insufficiency, arterial hypotension, diabetes mellitus, hypoglycemia, atrophic rhinitis, chronic obstructive pulmonary disease of the severe course, pulmonary insufficiency, thyrotoxicosis, myasthenia gravis, sinoatrial blockade, peripheral circulation disorders (including Raynaud's syndrome), pheochromocytoma, pregnancy, simultaneous appointment other beta-blockers.

If you have any of these diseases, consult a doctor before taking the drug.

Pregnancy and lactation:

In pregnancy, the drug is used if the expected benefit for the mother exceeds the potential risk to the fetus or child.

During the use of the drug, breastfeeding should be discontinued.

Dosing and Administration:

The duration of treatment depends on the indications, the individual sensitivity of the patient and the doctor's recommendations.

Adult children, older than 1 year instilled in a conjunctival sac 1 drop 2 times a day of a solution with a concentration of 0.25%, with insufficient efficiency - 1 drop of solution with a concentration of 0.5% 2 times a day. With the normalization of intraocular pressure, a maintenance dose of 1 drop of solution at a concentration of 0.25% 1 time per day.

Side effects:

Local reactions: hyperemia of the skin of the eyelids, burning and itching in the eyes, conjunctival hyperemia, lacrimation or a decrease in teardrop, photophobia, corneal epithelial edema, short-term visual acuity; blepharitis, conjunctivitis, 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, keratitis, ptosis, diplopia is possible.

Systemic reactions: paresthesia, rhinitis, nasal congestion, epistaxis, decreased arterial pressure, bradycardia, bradyarrhythmia, atrioventricular block, heart failure, cardiac arrest; decreased myocardial contractility, chest pain, dizziness, headache, drowsiness, hallucinations, muscle weakness, impaired sexual function, decreased potency, transient cerebral circulatory disorders, collapse, depression; shortness of breath, bronchospasm, pulmonary insufficiency; nausea, vomiting, diarrhea, allergic reactions (including urticaria).

If any of the side effects listed in the manual are aggravated, or if you notice any other side effects not listed in the instructions, tell your doctor.

Overdose:

When topical application in the recommended dose, the symptoms of an overdose were not noted. At casual intake it is possible development of following signs: a nausea, vomiting, a giddiness, a headache, depression of arterial pressure, a bronchospasm, a bradycardia. In case of symptoms of overdose, treatment is symptomatic.Isoprenaline can be administered intravenously to eliminate severe bradycardia and bronchospasm, dobutamine for the treatment of arterial hypotension.

Interaction:

With caution appoint simultaneously with antihypertensive drugs, other beta-adrenoblockers, insulin or oral hypoglycemic drugs, glucocorticosteroid, psychoactive drugs, a. also drugs, the effect of which is associated with increased excretion of epinephrine.

Epinephrine and pilocarpine increase the hypotensive effect of timolol. Simultaneous administration of eye drops containing epinephrine, can cause a dilated pupil (mydriasis). There is a possibility of intensifying the hypotensive effect and / or development of severe bradycardia with simultaneous use of timolol with calcium channel blockers for ingestion, guanethidine, beta adrenoblockers, antiarrhythmics, cardiac glycosides and parasympathomimetics. When used with reserpine - it is possible to develop severe bradycardia or lower blood pressure (this combination requires careful medical control); with blockers"slow" calcium channels or cardiac glycosides - there may be a violation of atrioventricular conduction, acute left ventricular failure or a decrease in blood pressure.

The development of hypertension after a sharp abolition of clonidine can be enhanced with simultaneous reception of beta-blockers.

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 (reduction in heart rate).

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 (possibly suppressing atrioventricular conduction, development of bradycardia and lowering blood pressure) should be avoided.

It should not be used simultaneously with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers).

In case of use with other local ophthalmic preparations, the interval between their use should be at least 5 minutes. It is not recommended simultaneous use with MAO inhibitors due to a significant increase in antihypertensive effect, a break in the treatment with mepovodu intake of MAO inhibitors and timolol should be at least 14 days.

During treatment it is not recommended to take ethanol (possibly a sharp drop in blood pressure).

Special instructions:

Control of effectiveness should be carried out "approximately 3-4 weeks after the start of therapy.

During the treatment period, at least once every 6 months, the function of lacrimation, the integrity of the cornea and the evaluation of the field of vision should be monitored. Use intraocular pressure at least once a month.

Use with caution in chronic obstructive pulmonary disease, heart failure, accuracy; retinal detachment, thyrotoxicosis, myasthenia gravis, sinoatrial blockade, impaired peripheral circulation (including Raynaud's syndrome), pheochromocytoma.

It is not recommended to use soft contact lenses during the treatment period.Rigid contact: the lens should be removed before instillation and wear not earlier than 15 minutes after it.

Do not bother with two p-adrenoblockers at the same time.

With prolonged use of timolol, the effect may be weakened.

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

beta-blockers (including with topical application) can increase the hypoglycemic effect of antidiabetics and mask the symptoms of hypoglycemia.

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 staining in the eye).

Form release / dosage:

Eye drops 0.25% and 0.5 %.

1.5 ml, 2 ml or 5 ml in a tube-droppers polymer; 5 ml or

10 ml into the bottle of a dropper polymeric.

1, 2, 4, 5, or 10 tubes with intravenous instructions for use

of the drug is packaged in a cardboard.

1 or 2 vials of a dropper with instructions for the use of the drug are placed in a pack of cardboard.

Packaging:

1.5 ml, 2 ml or 5 ml in a tube-droppers polymer; 5 ml or

10 ml into the bottle of a dropper polymeric.

1, 2, 4, 5, or 10 tubes with intravenous instructions for use

of the drug is packaged in a cardboard.

1 or 2 vials of a dropper with instructions for the use of the drug are placed in a pack of cardboard.

Storage conditions:

In the dark place at a temperaturenot more than 15 ° C for the drug in a tubeDroppers and a bottle of droppers, indark place at a temperaturenot higher than 25 ° C for the drug in a vialnach glass. Keep in places, nedosdull for children.

Shelf life:

3 years.

Shelf life after the opening - 1 month.

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

Terms of leave from pharmacies:On prescription

Registration number:LS-002359

Date of registration:11.04.2012

The owner of the registration certificate:MOSCOW ENDOCRINE FACTORY, FSUE MOSCOW ENDOCRINE FACTORY, FSUE Russia

Manufacturer: & nbsp

MOSCOW ENDOCRINE FACTORY, FSUE Russia

Representation: & nbspMOSCOW ENDOCRINE FACTORY FGUP MOSCOW ENDOCRINE FACTORY FGUP Russia

Information update date: & nbsp31.08.2015

Illustrated instructions

Instructions

Timolol-MEZ (Timolol-MEZ)