Timololum Bufus of 0,5%

General characteristics. Structure:

Active ingredient: 2,5 mg or 5 mg of Timololum of a maleate (in terms of Timololum).

Excipients: a benzalkoniya chloride, dihydrophosphate sodium a dihydrate (sodium phosphate monosubstituted 2-water), hydrophosphate sodium dodecahydrate (sodium phosphate disubstituted 12-water), water for injections.

Pharmacological properties:

Pharmacodynamics. A non-selective blocker of beta adrenoceptors without sympathomimetic activity. At topical administration lowers intraocular pressure due to reduction of formation of watery moisture and small increase in its outflow. Reducing intraocular pressure, does not influence accommodation and the size of a pupil therefore there is no deterioration in visual acuity; does not reduce quality of a scotopia.

Action is shown in 20 min. after an instillation, the maximum effect – in 1-2 h; action duration – 24 h.

Pharmacokinetics. After instillation of eye drops in moisture of an anterior chamber of an eye TCmax – 1-2 h. Active agent gets to a system blood stream by absorption through a conjunctiva, a mucous membrane of a nose and the lacrimal path. Drug is metabolized by the fermental CYP2D6 system. Removal of metabolites – kidneys. At newborn and malelky children concentration of active agent significantly exceeds its Cmax in plasma of adults.

Indications to use:

Eye hypertensia: open angle glaucoma, secondary glaucoma (uveal, afakichesky, posttraumatic); as auxiliary medicine: closed-angle glaucoma (in a combination from miotika), inborn glaucoma (at inefficiency of other therapeutic actions), acute increase in intraocular pressure.

Route of administration and doses:

The adult 2 times a day dig in in a conjunctival sac on 1 cap 0,25% of solution, at insufficient efficiency – on 1 cap of 0,5% of solution 2 times a day. At normalization of intraocular pressure a maintenance dose – 1 cap of 0,25% once a day. The difference of expressiveness of action of 2 concentration makes 10-15%.

Features of use:

Control of efficiency is recommended to be carried out approximately in 3-4 weeks after the beginning of therapy (not earlier than in 1-2 weeks). At prolonged use of Timololum easing of effect is possible. At use it is necessary to control lacrimation function, integrity of a cornea and to estimate the size of fields of vision at least 1 time in 6 months. At least 1 time a month to measure intraocular pressure.

The preservative which is contained in drug can be absorbed by soft contact lenses (causes change of their color). Can render irritant action approximately when carrying contact lenses therefore, any contact lenses should be removed before an instillation and to put on not earlier than in 15 min. after it.

At transfer of patients into treatment with Timololum correction of a refraction after effects of the miotik applied earlier can be necessary.

In case of the forthcoming operative measure using the general anesthesia, it is necessary to cancel drug for 48 h before operation since Timololum strengthens action of muscle relaxants and the general anesthetics.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention, speed of psychomotor reactions and good sight (during 0,5 h after an instillation in an eye).

Beta adrenoblockers (including at topical administration) can mask hypoglycemia symptoms at the patients with a diabetes mellitus accepting insulin or peroral hypoglycemic dosage forms; hyperthyroidism symptoms (including tachycardia).

Side effects:

Local reactions: irritation of a conjunctiva – a conjunctiva hyperemia, dacryagogue or reduction of a slezootdeleniye, a photophobia, cornea epithelium hypostasis, burning and an itch in eyes, a dermahemia a century, short-term disturbance of visual acuity; a blepharitis, conjunctivitis, a keratitis, at prolonged use development of a superficial dot keratopathy (reduction of transparency of a cornea) and decrease in sensitivity of a cornea is possible, the ptosis is possible, it is rare – a diplopia.

System reactions: paresthesias, rhinitis, nose congestion, nasal bleeding, lowering of arterial pressure, collapse, bradycardia, bradyarrhythmia, AV blockade, decrease in contractility of a myocardium, aggravation of displays of chronic heart failure; headache, dizziness, drowsiness, hallucinations, depression, myasthenia, decrease in a potentiality; asthma, bronchospasm, pulmonary insufficiency; nausea, vomiting, diarrhea, a stethalgia, a ring in ears. Delay of speed of psychomotor reaction. Allergic reactions (including small tortoiseshell).

Interaction with other medicines:

Epinephrinum, Pilocarpinum, system beta adrenoblockers strengthen action. The simultaneous instillation of two various beta adrenoblockers is not recommended.

The concomitant use with the eye drops containing Epinephrinum can lead to a mydriasis.

Strengthens action of muscle relaxants and the general anesthetics (for 48 h before carrying out the general anesthesia, including using peripheral muscle relaxants, it is necessary to stop administration of drug).

Against the background of treatment by drug it is necessary to avoid intravenous administration of verapamil, diltiazem (oppression of AV of conductivity, development of bradycardia and a lowering of arterial pressure is possible).

With care to appoint with hypotensive medicines, other beta adrenoblockers, insulin or peroral hypoglycemic medicines, glucocorticosteroids, psychoactive medicines, and also drugs which effect is connected with strengthening of allocation of Epinephrinum.

CYPIID6 inhibitors (including quinidine, Cimetidinum) can increase concentration of Timololum in plasma, increasing risk of development of system side effects of beta adrenoblockers (including decrease in heart rate, a depression).

Contraindications:

Hypersensitivity, dystrophic processes in a cornea, bronchial asthma (including in the anamnesis), a heavy chronic obstructive pulmonary disease, a sinus bradycardia, AV blockade of II-III, dekompensirovanny chronic heart failure, cardiogenic shock, the lactation period, children's age up to 18 years.

With care. SA blockade, arterial hypotension, atrophic rhinitis, pulmonary insufficiency, heavy cerebrovascular insufficiency, diabetes mellitus, hypoglycemia, thyrotoxicosis, myasthenia, disturbance of peripheric circulation (including Reynaud's syndrome), pheochromocytoma, pregnancy.

Overdose:

Symptoms: development of the all-resorptive effects characteristic of beta adrenoblockers (dizziness, a headache, arrhythmia, bradycardia, a bronchospasm, nausea, vomiting) is possible.

Treatment: to immediately wash out eyes water or 0,9% NaCl solution, symptomatic therapy.

Storage conditions:

List B. To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Drops eye 0,25% and 0,5%. On 5 ml, 10 ml in bottles from a tube glass. On 5 ml, 10 ml in bottles polymeric with a screw mouth and the screwed cover with the condensing element and a nozzle doser, or a nozzle doser with the condensing elements or in bottles polymeric, pressurized by droppers with the screwed covers.

On 1 ml, 1,5 ml, 2 ml, 5 ml, 10 ml in a tube dropper. Each bottle or 1, 2, 5, 10 tube droppers with the application instruction in a pack. On 50, 100 tube droppers with application instructions in a box (for hospitals). On 50, 150 bottles with the equal number of application instructions in group packaging.