Timolol

Timolol - eye drops that quickly normalize intraocular pressure (due to a significant decrease in secretion secreted fluid), relieve spasms of the muscles of the eyes, and with the course of reception completely restore visual acuity.

The main active compound in the formulation is maleate and thymolol hemihydrate, thanks to which antiglaucoma, antihypertensive, antiarrhythmic and antianginal action of "Timolol" is carried out.

The drug begins to act in twenty minutes.

Clinical and pharmacological group

Antiglaucomial drug - beta-blocker.

Terms of sale from pharmacies

Can buyby prescription.

Price

How much is Timolol in pharmacies? The average price in 2018 is at the level of27 rubles.

Composition and form of release

The drug is released in the form of drops of the eye 0.25% or 0.5%. Transparent yellow or colorless liquid is poured into tubes-droppers or vials of polymer droppers at 1; 1.5; 2; 5 or 10 ml, packaged in cardboard packs of 1, 2, 10, 50 or 100 pieces.

The composition of 1 ml of the solution includes:

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active ingredient: in a solution of 0.25%: 3.4 mg timolol maleate (corresponding to 2.5 mg timolol), in a solution of 0.5%: timolol maleate - 6.84 mg (corresponding to 5 mg timolol);
auxiliary substances: sodium dihydrogen phosphate dihydrate, hydrochloric acid, sodium hydroxide, benzalkonium chloride, sodium hydrogen phosphate dodecahydrate, water for injection.

pharmachologic effect

Non-selective beta-blocker. The drug reduces both normal and increased intraocular pressure by reducing the formation of intraocular fluid and improving its outflow. Does not affect the accommodation and the size of the pupil.

Has antianginal, hypotensive and antiarrhythmic effect, manifested in systemic application. Reduces the automatism of the sinus node, reduces heart rate, slows AV-conduction, reduces contractility and the need for myocardium in oxygen.

Pharmacokinetics

Timolol penetrates through the cornea into the tissues of the eye at a high rate. After it enters the moisture of the anterior chamber of the eye, the maximum concentration of the substance in the blood plasma is recorded after 1-2 hours. In a small amount enters the systemic bloodstream, absorbed through the mucous membranes of the lachrymal tract and nose, and also through conjunctivitis.

The maximum level of timolol in the blood plasma is approximately 0.824 ng / ml and remains up to the detection threshold for 12 hours. In newborns and young children, its maximum concentration in blood plasma significantly exceeds that of adults. The half-life of timolol with local application is 4.8 hours. It is metabolized in two ways, forming either an ethanolamine side chain on the thiadiazole ring to form an ethanol a side chain attached to the nitrogen of morpholine, or a similar side chain with a carbonyl group attached to nitrogen. In the processes of metabolism, the isoenzyme CYP2D6 takes part. The substance and its metabolites are excreted mainly in the urine, with approximately 20% of timolol being excreted unchanged.

Indications for use

This drug is prescribed to patients in the following cases:

for the treatment of glaucoma of a closed-angle and open-angle type,
with intraocular hypertension,
for the complex treatment of congenital glaucoma,
with a sharp increase in the ophthalmotonus,
to reduce spasms of the muscles of the eyes.

With topical application, the active ingredient, which is part of timolol, is able to quickly penetrate the cornea, while absorbing the lacrimal tract. The therapeutic effect is manifested as early as 30-40 minutes after instillation, the drug continues for 20-22 hours.

Contraindications

Dystrophic diseases of the cornea;
Cardiogenic shock;
Rhinitis;
Sinus bradycardia;
Bronchial asthma;
AV (atrioventricular) -blockade II and III degree;
Heart failure (acute and chronic);
Hypersensitivity to the components of the drug.

Timolol should be used with caution at the same time as other beta-blockers, children of childhood (especially during the neonatal period, because the composition of the drug includes benzalkonium chloride), as well as in severe chronic obstructive pulmonary disease, arterial hypotension, sinoatrial blockade, chronic heart failure, cerebrovascular insufficiency, myasthenia gravis, diabetes mellitus, thyrotoxicosis and hypoglycemia.

Intended use for pregnancy and lactation

The use of timolol by pregnant women is possible only in cases where the perceived benefit to the mother's health is greater than the potential risk to the fetus.

If it is necessary to use the drug by women during lactation, it is necessary to solve the problem of interrupting breastfeeding.

Dosage and route of administration

As indicated in the instructions for use, Timolol Eye Drops are intended for topical application by instillation into the conjunctival sac of the eye.

Recommended dosing:

children under 10 years of age, including newborns: 0.25% solution - 1 drop 2 times a day;
patients over the age of 10 years: 0.25% solution - 1 drop 2 times a day. In the absence of sufficient clinical effect, 0.5% solution is used - 1 drop 2 times a day. After normalization of intraocular pressure, the patient is transferred to use 0.25% solution in a maintenance dose 1 drop 1 time per day.

Side effects

When taking the drug, the following side effects are possible:

Digestive system: diarrhea, attacks of nausea, vomiting.
Sexual system: decreased potency, violation of sexual functions.
Respiratory system: epistaxis, nasal congestion, rhinitis, bronchospasm, shortness of breath, pulmonary insufficiency.
Cardiovascular system: bradyarrhythmia, bradycardia, lowering of arterial pressure, decrease in myocardial contractility, atrio-ventricular blockade, cardiac arrest, heart failure, collapse, transient impairment of cerebral circulation, chest pain.
Central and peripheral nervous system: drowsiness, dizziness, headache, hallucinations, paresthesia, depression, slowing of the speed of psychomotor reactions.
Organs of vision: itching and burning in the eyes, hyperemia of the skin of the eyelids, conjunctival hyperemia, corneal epithelial edema, decreased tearing or lacrimation, visual acuity (short-term), conjunctivitis, blepharitis, photophobia; with prolonged use - surface punctate keratopathy, ptosis, decreased sensitivity of the cornea; in rare cases - diplopia.
Other: urticaria, muscle weakness, ringing in the ears.

Overdose

With topical application in therapeutic doses, overdose cases are almost not encountered.

At casual oral reception occurrence of such signs, as a bradycardia, depression of arterial pressure, a headache, a giddiness, a nausea, a vomiting, a bronchospasm are possible. In this case, symptomatic therapy is prescribed. To treat arterial hypotension use dobutamine, and to eliminate bronchospasm or severe bradycardia intravenously inject isoprenaline.

special instructions

Before you start using the drug, read the special instructions:

Do not bother with two beta-blockers at the same time.
With prolonged use of timolol, the effect of the drug may be weakened.
When transferring a patient to treatment with timolol, correction of refraction may be necessary.
48 hours before the forthcoming surgery with the use of general anesthesia, the drug should be discontinued.
Control of the effectiveness of the drug 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 field of vision should be monitored.
The preparation contains a preservative of benzalkonium chloride, which can be adsorbed on the surface of soft contact lenses. In this regard, during the period of treatment is not recommended to use soft contact lenses. Rigid contact lenses should be removed before instillation and wear not earlier than 15 minutes after the procedure.
Caution should be given Timolol concomitantly with antihypertensive drugs, GCS and psychoactive drugs.
It can not be used simultaneously with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers).

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 30 minutes after instillation of the drug in the eye).

Interaction with other drugs

When using the drug, it is necessary to take into account the interaction with other drugs:

Simultaneous use increases the effect of muscle relaxants (the drug should be discontinued 48 hours before the expected general anesthesia with peripheral muscle relaxants).
When using local anesthetics, one should consider the possibility of increasing the risk of their undesirable effects on the cardiovascular system.
When used simultaneously with epinephrine, pilocarpine, systemic beta-blockers increase its effect.
With simultaneous application with reserpine, it is possible to develop severe bradycardia or arterial hypotension (the combination requires careful medical supervision).
When used simultaneously with calcium channel blockers or cardiac glycosides, it is possible to develop disorders of AV-conduction, acute left ventricular failure or arterial hypotension.
During treatment, Timolol is not recommended to take ethanol in order to avoid a sharp decrease in blood pressure.

Reviews

We offer to read reviews of people who used the drug Timolol:

Irina. My father discovered glaucoma. Naturally, the intraocular pressure began to rise. The doctor prescribed a drop of timolol 0.25%. Began to drip, and a week later the doctor measured the pressure, and said that it fell, not yet up to the norm. I prescribed timolol 0.5%. After a week of use, the pressure became normal. Now we drip only these drops. The father's condition improved.
Hope. To me the doctor has recommended to instill drops of Timolol from intraocular pressure. At first I liked the price, and when I began to use the drops, I appreciated their action. During the instillation there was no burning and other painful sensations. After a few days of taking the pain, my eyes grew tired and tired, even the headache was gone. After the course of treatment, normal eye pressure was normalized. Now I feel much better.

Analogues

Analogues can be called drugs: Arutimol, Glaumol, Iotim, Kuzimolol, Niolol, Normatin, Okumed, Okuril, Ophthalm Timolol, Ophthalmol, Unitimolol.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

Keep out of reach of children and protected from light at a temperature of up to 25 ° C. Shelf life of the unopened vial is 2 years, the opened one is 1 month.