Timolol-pos, eye drops 0.5% 10 ml

Pharmacotherapeutic group – Antiglaucoma drug – beta-adrenoblocker.
ATX: S01ED01

Pharmacodynamics

Neselective beta-adrenoceptor blocker without sympathomimetic activity. When used topically, it lowers intraocular pressure by reducing aqueous humor formation and slightly increasing its outflow. Action appeared 20 min after dosing, maximum effect 1-2 h later; time of action – 24 h.

Pharmacokinetics

Timolol maleate rapidly penetrates through the cornea into the eye tissue. A small amount enters the systemic bloodstream by absorption through the conjunctiva, nasal mucosa and lacrimal tract. Metabolites are excreted by the kidneys. In infants and small children the concentration of the active substance is significantly higher than its maximum concentration in adult plasma.

Indications

– Primary open-angle glaucoma;

-secondary glaucoma (uveal, aphakic, post-traumatic);

– Congenital glaucoma (in case other therapeutic measures fail);

– Acute increase in ophthalmotonus

– Primary closed angle glaucoma (in combination with miotics).

Active ingredient

Composition

TIMOLOL-POS 0.5%
Active ingredient:
timolol maleate 6.84 mg (in terms of timolol – 5.0 mg)
Ancillary ingredients:sodium dihydrophosphate dihydrate, sodium hydrophosphate dodecahydrate, water for injection.

How to take, the dosage

In newborns and children up to 10 years of age, 1 drop of 0.25% solution is injected twice a day. In adults and children over 10 years of age 1 drop of 0.25% solution is placed into the conjunctival sac 2 times a day, if the effect is insufficient – 1 drop of 0.5% solution 2 times a day. If necessary the dose can be reduced to 1-2 drops once a day.

The protective cap should be removed before each injection. Before using the product for the first time, turn the bottle upside down with the drip tip facing down and press the base (bottom) several times until the first drop appears at the tip of the drip tip. The bottle is then ready for continued use. Hold the bottle with the dropper facing down, quickly and firmly press the base (bottom) of the bottle when the medication is being dripped. This actuates the drip mechanism and only one drop of medication is removed. The unique design of the dropper valve system ensures that the droplet always comes out the same size and at the same rate, even when you are pressing very hard on the base of the vial.

Take your head slightly back, gently move your finger away from the lower eyelid and drip one drop into the conjunctival sac as described above. Slowly close your eyes.

Place the protective cap over the dropper immediately after completion of the procedure.

Please avoid contact of the tip of the dropper with the surface of the eye and the skin when injecting.

Interaction

Epinephrine, pilocarpine, systemic beta-adrenoblockers increase the effect. When used with reserpine – pronounced bradycardia or hypotension may develop (this combination requires close medical supervision); with calcium channel blockers or cardiac glycosides – atrioventricular conduction disorders, acute left ventricular failure or arterial hypotension may occur.

It potentiates the effects of muscle relaxants (timolol should be discontinued 48 hours before the intended general anesthesia with peripheral muscle relaxants). It should not be used simultaneously with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers). During treatment it is not recommended to take ethanol (sharp decrease of blood pressure is possible).

Cautiously prescribe simultaneously with hypotensive drugs, other beta-adrenoblockers, insulin or oral hypoglycemic drugs, glucocorticosteroids, psychoactive drugs.

Special Instructions

The efficacy should be monitored approximately 3-4 weeks after the start of therapy. During treatment at least once every 6 months, tear secretion function, corneal integrity and visual field should be monitored. During the period of treatment, caution should be exercised when driving motor transport and engaging in other potentially dangerous activities requiring increased concentration and rapid psychomotor reactions and good vision (within 0.5 hours after eye-drop).

Contact lenses should be removed before and at least 15 minutes after each injection.

The effect of long-term use of timolol may be diminished.

Ahead of an upcoming operation with general anesthesia, discontinue the drug 48 hours before.
The unique design of the dropper bottle which operates on airless pump principle prevents external air from penetrating the bottle and thus provides sterile eye drops in the absence of preservative.

The use of “Timolol-POS eye drops [without preservative] avoids unwanted effects of the preservative on the external tissues of the eye, conjunctiva and cornea, and also eliminates the risk of allergic reactions to the preservative.
After opening the bottle and the first injection of Timolol-POS eye drops [without preservative] the drug can be used for 12 weeks. To do this, mark on the vial and/or on the carton pack the date on which you first injected the product. There is a space on the label of the vial and on the carton pack for the patient to fill out: “Date of First Use.”

After using the contents of the vial, a new vial of product must be purchased; the used vial is not eligible for reuse and must be disposed of (throw the used vial in the trash).

Synopsis

Contraindications

Side effects

Local reactions:

.Eye irritation manifested as conjunctivitis, blepharitis, keratitis (eyelid skin hyperemia, burning and itching in the eyes, conjunctival hyperemia, lacrimation or reduced lacrimation, photophobia, corneal epithelial edema, transient visual acuity impairment, with long-term use, possible development of surface pitting keratopathy (decrease in corneal transparency) and corneal sensitivity reduction), ptosis, diplopia;

Systemic reactions:

Cardiovascular system: decreased blood pressure, bradycardia, bradyarrhythmia, atrioventricular block, heart failure, cardiac arrest, decreased myocardial contractility, chest pain, transient cerebral circulation disorder, collapse;

Respiratory system: Dyspnea, bronchospasm, pulmonary failure;

Central nervous system: dizziness, headache, drowsiness, hallucinations, slowed psychomotor reactions;

Other side effects: allergic reactions (includingUrticaria), rhinitis, nasal congestion, nasal bleeding, nausea, vomiting, diarrhea, paresthesias, muscle weakness, sexual dysfunction, depression.

Overdose

Pregnancy use

Similarities