Timololum

General characteristics. Structure:

Active ingredient: 2,5 mg or 5 mg  of Timololum a maleate (in terms of the basis) in 1 ml of solution of eye drops.

Pharmacological properties:

Pharmacodynamics. Timololum is a highly active non-selective blocker of beta adrenoceptors. Has no internal sympathomimetic and membrane stabilizing activity. At topical administration in the form of eye drops reduces both the normal, and increased intraocular pressure due to reduction of secretion of intraocular liquid. Does not exert impact on the pupil size. Allows to control intraocular pressure during sleep. Effect of drug is shown in 10-30 minutes after an instillation in a conjunctival cavity. The maximum decrease in intraocular pressure occurs in 1-2 hours and remains within 12-24 hours.

Pharmacokinetics. At topical administration of Timololum the maleate quickly gets through a cornea. In insignificant quantity gets to a system blood stream by absorption through vessels of a conjunctiva, mucous a nose and the lacrimal path.

Linkng with proteins of plasma – less than 10%. Gets into breast milk, there passes the blood-brain barrier and a placental barrier. It Biotransformirutsya in a liver. It is excreted by kidneys and intestines in not changed look and in the form of metabolites. At newborns and children of younger age concentration of active agent (Cmax) in a blood plasma significantly exceeds its Cmax in a blood plasma of adults.

Indications to use:

Drug is used at a chronic open angle glaucoma, secondary glaucoma (uveal, afakichesky, posttraumatic); at acute increase in intraocular tension; as an additional tool for decrease in intraocular pressure at closed-angle glaucoma (in a combination from miotika).

Route of administration and doses:

Drug is used in the form of instillations in the lower conjunctival sac of the affected eye. Treatment is begun with 0,25% of solution (1 drop of 1-2 times/days), at insufficient efficiency apply 0,5% solution (1 drop of 1-2 times/days). If intraocular pressure at regular use is normalized, it is necessary to limit a dosage to 1st once a day on the 1st drop in the morning.

Treatment is carried out, as a rule, for an appreciable length of time. Duration of a course of treatment depends on the course of a disease and is defined by the doctor. Having rummaged in use of drug or change of a dosage are carried out only according to the instruction of the attending physician.

Features of use:

Use at pregnancy and a lactation: there is no sufficient experiment on use of drug during pregnancy, however is established that Timololum passes a placental barrier. Use of drug for treatment during pregnancy to destination of the attending physician is possible if the expected medical effect exceeds potential risk for a fruit. If drug was used just before childbirth, then newborns have to be under careful observation within several days after the birth.

At use of Timololum it is necessary to control function of a slezootdeleniye, integrity of a cornea and a field of vision; it is necessary to carry out control of intraocular pressure (in 3-4 weeks after the beginning of therapy). If the patient carries soft contact lenses, then he should not apply eye drops as preservative can be laid in soft contact lenses and make an adverse effect on eye tissues. It is necessary to remove rigid contact lenses before an instillation of drug and to dress them again only 15 minutes later.

At transfer of patients into Timololum from therapy by other beta adrenoblockers stop use of the previous medicine and next day appoint Timololum. In case of cancellation of other antiglaukomny drugs it is necessary to apply within 1 days both medicines (under control of intraocular pressure) and then to continue use of Timololum. At transfer of patients into treatment with Timololum correction of a refraction after the effects caused by the miotika applied earlier can be necessary. In case of prolonged use of Timololum easing of therapeutic effect is possible.

In case of the planned surgical intervention using the general anesthesia, it is necessary to cancel Timololum in 48 hours prior to its carrying out. For reduction of absorption after an instillation in eyes it is necessary to press for 1-2 min. a finger on the lacrimal canal at an internal corner of an eye. At closed-angle glaucoma use is possible only together with miotocs. It is recommended to Instillirovat other drugs not less than in 10 min. prior to use of Timololum.

Influence on ability to driving of motor transport and to control of mechanisms. With care apply in operating time to drivers of vehicles and people whose work is connected with the increased concentration of attention. Within 30 minutes after use of drug it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention.

Precautionary measures. Drug is used with extra care at patients with emphysema of lungs, not allergic chronic allergic bronchitis, vasculomotor rhinitis, болезью Reynaud, acidosis, heavy cerebrovascular insufficiency, a diabetes mellitus (especially labile current), a hypoglycemia, a hyperthyroidism, a myasthenia. With care apply at patients of advanced age and at children. At use of Timololum for these categories of patients careful medical control is necessary.

With care apply Timololum along with blockers of calcium channels, foxglove drugs, with Reserpinum, and also at co-administration of other drugs of group of beta adrenoblockers.

Timololum masks symptoms (tachycardia) of a hypoglycemia against the background of reception of peroral antidiabetic means and insulin, masks thyrotoxicosis symptoms (sudden cancellation can cause thyrocardiac crisis).

Strengthening of expressiveness of reactions of hypersensitivity and absence is possible.

Side effects:

As a rule, drug is well transferred. At use of drug burning and an itch in eyes, dacryagogue or a xerophthalmus are possible passing misting of sight (lasting from 30 seconds up to 5 minutes), feeling of a foreign body in an eye.

At long use of Timololum the following local reactions can be noted: conjunctivitis, a blepharitis, reduction of sensitivity of a cornea, a dot superficial keratopathy, cornea epithelium hypostasis, an inflammation of edges a century, changes of visual acuity and a refraction it is (very rare). Drug use in some cases can be followed by development of system reactions: bradycardia, bradyarrhythmia, lowering of arterial pressure, atrioventricular block, passing disturbances of cerebral circulation; nose congestion, asthma, bronchospasm, respiratory insufficiency; headache, dizziness, weakness, depression; skin rash, itch, small tortoiseshell.

Interaction with other medicines:

Timololum at topical administration is compatible to miotocs and inhibitors of a karboangidraza.

Simultaneous use of the eye drops containing Epinephrinum or Norepinephrinum can cause a mydriasis.

Specific effect of drug - decrease in intraocular pressure - amplifies at simultaneous use of the eye drops containing Epinephrinum and Pilocarpinum.

It is not recommended to dig in two drugs of group of beta adrenoblockers at the same time.

At simultaneous system and topical administration of beta adrenoblockers perhaps mutual strengthening of expressiveness of side effects.

Timololum increases (mutually) probability of disturbances of automatism, conductivity and contractility of heart against the background of Amiodaronum, sympatholytics, diltiazem, verapamil, hinidinovy drugs; the risk of hypotension and a decompensation of cordial activity – against the background of antagonists of calcium (dihydropyridine derivatives), cardiac glycosides, inhalation anesthetics, strengthens action of muscle relaxants.

At simultaneous use with Reserpinum development of the expressed bradycardia, hypotonias is possible. Simultaneous use with insulin or oral antidiabetic means can lead to a hypoglycemia.

Contraindications:

The increased individual sensitivity to Timololum to a maleate or any of auxiliary components of drug; dystrophic diseases of a cornea, heavy allergic inflammations of a mucous membrane of a nose, bronchial asthma (including in the anamnesis), chronic obstructive diseases of lungs, a sinus bradycardia (50 and less уд. / mines), AV blockade of II and III degrees, sinuatrial blockade, acute and chronic heart failure, cardiogenic shock, a syndrome of weakness of a sinus node, a lactation (for treatment it is necessary to stop breastfeeding), early children's age.

Overdose:

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

Treatment: immediate washing of eyes water or normal saline solution, with the expressed side effects - symptomatic therapy.

Issue conditions:

According to the recipe

Packaging:

Solution (drops eye) 2,5 mg/ml and 5 mg/ml in bottles of 5 ml in packaging No. 1; in a tube droppers of 1 ml in packaging No. 2.