Офтан® Timogel

General characteristics. Structure:

Active ingredient: 1,37 mg of Timololum of a maleate that corresponds to 1 mg of Timololum.

Excipients: a benzalkoniya chloride - 0.05 mg, carbomer - 3 mg, a lysine monohydrate - 5.9 mg, polyvinyl alcohol - 10 mg, acetate sodium trihydrate - 0.2 mg, sorbitol - 45 mg, water for and - q.s. to 1 g.

Protivoglaukomny drug.

Pharmacological properties:

Pharmacodynamics. Protivoglaukomny drug, non-selective beta adrenoblocker. Reduces the increased intraocular pressure due to reduction of products of watery moisture. Like other beta adrenoblockers, Timololum has insignificant effect on system of outflow of intraocular liquid. Has weak anesthetic effect and does not influence the size of a pupil and accommodation.

The effect of decrease in intraocular pressure is reached on condition of drug Oftan® instillation Timogel on 1 drops/days. The maximum decrease in intraocular pressure develops in several hours after instillation and remains within a day.

Pharmacokinetics. Absorption. Timololum can be exposed to system absorption through vessels of a conjunctiva, mucous a nose and the lacrimal path and, thus, reach a system blood-groove. Very seldom serumal level is defined within 90 min. after instillation.

Removal. Nevertheless, Timololum is defined in the minimum concentration in urine longer time. It is allocated with breast milk.

Indications to use:

— increase in intraocular pressure (oftalmogipertenziya);

— open angle glaucoma;

— secondary glaucoma (uveal, afakichesky, posttraumatic).

Route of administration and doses:

To adults and children 12 years are more senior appoint on 1 drops/days in the affected eye.

Features of use:

Use at pregnancy and feeding by a breast. Now there are no data on the conducted clinical trials of use of drug for pregnant women. At pregnancy of Oftan® Timogel it is necessary to apply only under a condition if the expected advantage of therapy for mother exceeds risk of development of possible side effects.

Timololum is allocated with breast milk. As Timololum can cause serious side effects in babies, it is necessary to decide whether it is necessary to stop breastfeeding or to cancel drug.

Use for children. It is not recommended to apply at children 12 years are younger (experience of use is not available).

At development of dermatological reactions, perhaps connected using drug, treatment by the drug Oftan® Timogel should be stopped immediately.

The Benzalkony chloride which is a part of eye Oftan® gel Timogel can cause allergic reactions in sensitive patients.

Patients with heart failure need to be inspected before an initiation of treatment the drug Oftan® Timogel. Patients with other serious cardiovascular illness need inspection for the purpose of identification of possible symptoms of the latent heart failure and regular control of ChSS and the ABP.

For decrease in the increased intraocular pressure at closed-angle glaucoma of Oftan® Timogel it is necessary to appoint in a combination from miotika. As well as at use of other protivoglaukomny drugs, after prolonged treatment cases of lack of reaction to Timololum a maleate are noted.

At drug Oftan® use Timogel it is necessary to control function of a slezootdeleniye, a condition of a cornea and to estimate the size of fields of vision at least 1 time in 6 months.

Any eye drops should be applied before drug Oftan® instillation Timogel. For preservation of its activity an interval between instillations of other eye drops and the drug Oftan® Timogel has to make not less than 5 min. Regular control of intraocular pressure is necessary each 3-4 weeks.

Before use of eye gel it is necessary to remove contact lenses and not to use them within 15 min. after drug instillation.

Influence on ability to driving of motor transport and to control of mechanisms. Drug Oftan® influence Timogel on ability to manage motor transport and/or to work with mechanisms was not studied. Such side effects of the drug Oftan® Timogel as short-term decrease in visual acuity, the ptosis, vision disorders including changes of a refraction and a diplopia, dizziness and increased fatigue can negatively influence ability to control of motor transport and other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

At use of eye Oftan® gel Timogel (also as well as other local ophthalmologic means) intake of drug in a system blood stream is possible. At receipt of Timololum in a system blood stream the same undesirable phenomena can be observed, as well as at system use.

From an organ of sight (local reactions): a weak hyperemia of a conjunctiva, feeling of a foreign body in an eye, burning or pain right after instillation; 1-3% - passing decrease in sight lasting more than 3 min., dacryagogue, a photophobia, cornea epithelium hypostasis, a dermahemia a century, a blepharitis, conjunctivitis, a keratitis, a ptosis, decrease in sensitivity of a cornea, the vision disorders including the changes of a refraction (arising in some cases in connection with cancellation of miotik), a diplopia; at prolonged use development of a superficial dot keratopathy is possible. At use of beta adrenoblockers cases of development of a syndrome of a dry eye were noted.

From cardiovascular system: bradycardia, AV conductivity disturbance (AV blockade development for the first time or progressing of already existing AV blockade), arterial hypotension, heart failure, arrhythmias, a syncopal condition (syncope), disturbance of cerebral circulation, a heart consciousness, Reynaud's syndrome, a cold snap of hands and legs, passing lameness, a sudden cardiac standstill.

From respiratory system: a bronchospasm (in most cases at patients with obstructive bronchopulmonary diseases), respiratory insufficiency, an asthma and cough.

Dermatological reactions: hypersensitivity reactions, local or generalized erythema, small tortoiseshell, hair loss, psoriazoformny damages of skin or progressing of psoriasis. Frequency of development of these undesirable phenomena was low. In most cases dermatological reactions disappeared after the therapy termination by drug.

From TsNS and nervous system: dizziness, deterioration in a current of a myasthenia, paresthesia, headache, adynamy, general weakness, mental disturbances, depression, sleeplessness, nightmare (dreadful dreams), memory impairment.

From the alimentary system: nausea, diarrhea, dyspepsia, dryness in a mouth.

From immune system: system lupus erythematosus.

From urinogenital system: decrease libido, erectile dysfunction, Peyroni's disease.

Others: increased fatigue, adynamy, thorax pain.

Undesirable reactions at system use of Timololum (regardless of existence of relationship of cause and effect using drug): afakichesky cystous hypostasis of a makula, dryness in a mouth, a nose congestion, anorexia, confusion of consciousness, a hallucination, a hyperexcitability, alarm, a disorientation, drowsiness and other mental disturbances, arterial hypertension, retroperitoneal fibrosis.

Interaction with other medicines:

Though Timogel exerted Oftan® insignificant impact on the size of pupils, at use of drug together with sympathomimetics (such as Epinephrinum) the mydriasis was noted.

At drug Oftan® use Timogel together with system beta adrenoblockers perhaps more expressed decrease in intraocular pressure, and also strengthening of systemic action of beta adrenoblockers. The patients receiving Oftan® Timogel together with system beta adrenoblockers have to be under strict medical control.

The patients accepting sympatholytics (for example, Reserpinum) together with beta adrenoblockers, have to be under strict medical control. At drug Oftan® use Timogel together with the drugs releasing catecholamines development of such undesirable phenomena as arterial hypotension, the expressed bradycardia, dizziness, a syncopal state and orthostatic hypotension is possible.

At use of beta adrenoblockers along with blockers of calcium channels development of arterial hypotension, disturbances of AV conductivity or a left ventricular failure is possible.

It is necessary to apply with care beta adrenoblockers along with the blockers of calcium channels entered in / century.

Dihydropyridine derivatives, such as nifedipine, can cause arterial hypotension whereas verapamil and diltiazem have tendency to cause disturbances of AV conductivity or a left ventricular failure at a combination with beta adrenoblockers.

Simultaneous use of beta adrenoblockers and drugs of a foxglove can lead to AV conductivity disturbance strengthening.

At use of beta adrenoblockers together with a clonidine (anti-hypertensive drug of the central action) perhaps substantial increase of the ABP after sharp cancellation of therapy by a clonidine.

Purpose of beta adrenoblockers in a combination with antiarrhytmic drugs of a class I (quinidine, Disopyramidum) and a class III can lead (Amiodaronum) to the expressed delay of conductivity in auricles and to strengthening of a negative inotropic effect.

At combined use with insulin and peroral hypoglycemic means it is necessary to consider that beta adrenoblockers can mask hypoglycemia symptoms (heartbeat and tachycardia).

It is not necessary to accept beta adrenoblockers along with antipsychotic (neuroleptics) and anxiolytic (tranquilizers) drugs. As reception of ethanol during therapy by beta adrenoblockers can lead to sharp decrease in the ABP, during treatment drug recommends to abstain from ethanol reception.

In case of carrying out surgical interventions with use of the general anesthesia treatment by drug it is necessary to cancel and warn gradually the anesthesiologist about the previous therapy by the drug Oftan® Timogel. Timogel together with the general anesthetics can lead simultaneous use of the drug Oftan® to development of compensatory tachycardia and the expressed arterial hypotension.

At simultaneous use of Cimetidinum and Timololum increase in concentration of the last in a blood plasma is possible.

It is necessary to be careful at purpose of the drug Oftan® Timogel together with lidocaine (in/in introduction) and iodinated X-ray contrast agents.

Contraindications:

— dystrophic diseases of a cornea;

— acute and chronic heart failure;

— cardiac arrhythmia (including AV blockade of II and III degrees);

— bradycardia;

— cardiogenic shock;

— bronchial asthma;

— chronic obstructive bronchitis with the bronchospasm phenomena;

— hypersensitivity to Timololum to a maleate or other components of drug.

It is not recommended to apply at children 12 years are younger (since there is no experience of use for this category of patients).

With care it is necessary to use drug at patients with pulmonary insufficiency, heavy cerebrovascular insufficiency, chronic heart failure, at a diabetes mellitus, a hypoglycemia, a thyrotoxicosis, a myasthenia, along with other beta adrenoblockers.

Overdose:

At topical administration in the recommended dose the overdose is improbable.

Symptoms: at accidental overdose symptomatic bradycardia, arterial hypotension, a bronchospasm, an acute heart failure, AV blockade of II and III degrees are possible.

Treatment: performing symptomatic therapy. Treatment of overdose can include (but it is not limited) the listed below measures.

Gastric lavage (if drug was accepted inside). Removal of Timololum from an organism by means of a hemodialysis is ineffective.

At symptomatic bradycardia for receiving vagal blockade in/in enter atropine sulfate in a dose of 0.25-2.0 mg (0.25-1 ml of 0.1% of solution). If bradycardia remains, in/in slowly enter изопреналин. In case of a refrakternost installation of an artificial pacemaker can be required.

At arterial hypotension carry out treatment by the sympathomimetic means raising the ABP, for example a dopamine, Dobutaminum, or Norepinephrinum. In case of inefficiency it is necessary to apply a glucagon.

At a bronchospasm carry out treatment izoprenaliny, it is possible in combination with Aminophyllinum.

At an acute heart failure it is necessary to begin immediately therapy using drugs of a foxglove, diuretic and oxygen. In case of inefficiency it is recommended to apply in/in Aminophyllinum if it is necessary, with the subsequent use of a glucagon.

At AV blockade (II and III degrees) apply изопреналин or an artificial pacemaker.

Storage conditions:

List B. Drug should be stored in the place, unavailable to children, at a temperature not above 25 °C; not to freeze. A period of validity - 18 months. After the first opening to store a bottle, having turned it upside down, in a cardboard pack. A period of validity after opening of a bottle - 4 weeks.

Issue conditions:

According to the recipe

Packaging:

5 g - bottles polyethylene with a dropper with the screwing-up cover (1) - packs cardboard.