Timolol

Timolol - eye drops, which fairly quickly normalize the intraocular pressure (due to a significant decrease in secretion of secreted fluid), relieve spasms of the eye muscles, and during exchange intake completely restore visual acuity.

The main active compound in the formulation is maleate and timolol hemihydrate, due to which anti-glaucoma, antihypertensive, antiarrhythmic and antianginal action of Timolol is performed.

The drug starts the action after twenty minutes.

Clinico-pharmacological group

Antiglaucoma drug - beta-blocker.

Terms of sale from pharmacies

You can buy by prescription.

Price

How much does timolol in pharmacies? The average price in 2018 is at the level of 27 rubles.

Composition and release form

The drug is released in the form of eye drops of 0.25% or 0.5%. A transparent yellow or colorless liquid is poured into dropper tubes or polymer dropper bottles of 1 each; 1.5; 2; 5 or 10 ml, packaged in cardboard packs of 1, 2, 10, 50 or 100 pcs.

The composition of 1 ml of solution includes:

  • active ingredient: in a solution of 0.25%: 3.4 mg of timolol maleate (corresponds to 2.5 mg of timolol), in a solution of 0.5%: timolol maleate - 6.84 mg (corresponds to 5 mg of timolol);
  • excipients: sodium dihydrophosphate 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 pupil size.

It has antianginal, hypotensive and antiarrhythmic effects, manifested in systemic use. Reduces the automatism of the sinus node, reduces heart rate, slows AV-conductivity, reduces contractility and myocardial oxygen demand.

Pharmacokinetics

Timolol penetrates through the cornea into the eye tissue at high speed. After it enters the moisture of the anterior chamber of the eye, the maximum concentration of a substance in the blood plasma is recorded after 1-2 hours. In a small amount enters the systemic circulation, being absorbed through the mucous membranes of the lacrimal tract and nose, as well as through the conjunctiva.

The maximum level of timolol in the blood plasma is approximately 0.824 ng / ml and is maintained up to the detection threshold for 12 hours. In newborns and small children, its maximum plasma concentration is substantially higher than that in adults. The elimination half-life of timolol, when applied topically, is 4.8 hours. It is metabolized in two ways, forming either an ethanolamine side chain on the thiadiazole ring to form an ethanol side chain linked to morpholine nitrogen, or a similar side chain with a carbonyl group linked to nitrogen. CYP2D6 isoenzyme is involved in metabolic processes. The substance and its metabolites are excreted mainly in the urine, with approximately 20% of timolol excreted unchanged.

Indications for use

This drug is prescribed to patients in the following cases:

  • for the treatment of glaucoma of the angle-closure and open-angle type,
  • with intraocular hypertension,
  • for complex treatment of congenital glaucoma,
  • with a sharp increase in intraocular pressure,
  • to reduce eye muscle spasms.

When applied topically, the active ingredient in timolol can quickly penetrate the cornea while absorbing the lacrimal tract. The therapeutic effect is manifested within 30-40 minutes after instillation, the effect of the drug lasts for 20-22 hours.

Contraindications

  • Cornea dystrophic diseases;
  • Cardiogenic shock;
  • Rhinitis;
  • Sinus bradycardia;
  • Bronchial asthma;
  • AV (atrioventricular) block II and III;
  • Heart failure (acute and chronic);
  • Hypersensitivity to the drug.

Timolol should be used with caution simultaneously with other beta-blockers, pediatric patients (especially in the neonatal period, because benzalkonium chloride is a part of the drug), as well as in severe course of chronic obstructive pulmonary disease, arterial hypotension, sinoatrial blockade, chronic heart failure, cerebrovascular insufficiency, myasthenia, diabetes mellitus, thyrotoxicosis and hypoglycemia.

Appointment during pregnancy and lactation

Use of Timolol in pregnant women is possible only in cases where the intended benefits for the mother are higher than the potential risk to the fetus.

If necessary, the use of the drug by women during lactation is necessary to resolve the issue of interrupting breastfeeding.

Dosage and method of use

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

Recommended Dosing:

  • children under 10 years old, 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 a sufficient clinical effect, apply a 0.5% solution - 1 drop 2 times a day. After normalization of the intraocular pressure, the patient is transferred to the use of a 0.25% solution in a maintenance dose of 1 drop 1 time per day.

Side effects

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

  1. Digestive system: diarrhea, nausea, vomiting.
  2. The reproductive system: reduced potency, violation of sexual functions.
  3. Respiratory system: nasal bleeding, nasal congestion, rhinitis, bronchospasm, shortness of breath, pulmonary insufficiency.
  4. Cardiovascular system: bradyarrhythmia, bradycardia, lowering blood pressure, reducing myocardial contractility, atrio-ventricular block, heart failure, heart failure, collapse, transient cerebral circulation, chest pain.
  5. Central and peripheral nervous system: drowsiness, dizziness, headache, hallucinations, paresthesias, depression, slowing down the speed of psychomotor reactions.
  6. Organs of vision: itching and burning in the eyes, eyelid skin flushing, conjunctival hyperemia, corneal epithelium edema, decreased tearing or tearing, visual acuity (short term), conjunctivitis, blepharitis, photophobia; with prolonged use - superficial point keratopathy, ptosis, decreased corneal sensitivity; in rare cases - diplopia.
  7. Other: urticaria, muscle weakness, ringing in the ears.

Overdose

When applied topically at therapeutic doses, cases of overdose are practically absent.

In case of accidental oral administration, symptoms such as bradycardia, low blood pressure, headache, dizziness, nausea, vomiting, bronchospasm may occur. In this case, symptomatic therapy is prescribed. Dobutamine is used to treat hypotension, and isoprenaline is injected intravenously to eliminate bronchospasm or severe bradycardia.

Special instructions

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

  1. Do not bury two beta-blockers in the eye at the same time.
  2. With prolonged use of timolol may weaken the effect of the drug.
  3. When transferring a patient to treatment with timolol, a correction of refraction may be necessary.
  4. 48 h before the upcoming surgery with general anesthesia, the drug should be discontinued.
  5. Monitoring the effectiveness of the drug should be carried out approximately 3-4 weeks after the start of therapy. During treatment at least 1 time in 6 months, the function of tearing, corneal integrity, visual field should be monitored.
  6. The preparation contains benzalkonium chloride preservative, 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. Hard contact lenses should be removed before instillation and wear no earlier than 15 minutes after the procedure.
  7. With caution should appoint Timolol simultaneously with antihypertensive drugs, corticosteroids and psychoactive drugs.
  8. You can not simultaneously apply with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers).

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration, psychomotor speed and good vision (within 30 minutes after dropping the drug into the eye).

Interaction with other drugs

When using the drug, you must consider the interaction with other drugs:

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

Reviews

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

  1. Irina. My father found glaucoma. Naturally, intraocular pressure began to rise. The doctor prescribed a drop of timolol 0.25%. They began to drip, and a week later the doctor measured the pressure, and said that it had fallen, was not yet up to normal. Appointed timolol 0.5%. After a week of application, the pressure became normal. Now we are dripping only these drops. Father’s well-being improved.
  2. Hope. The doctor recommended me to drop Timolol from intraocular pressure. At first I liked the price, and when I began to use drops, I also appreciated their effect. During the instillation there was no burning and other painful sensations. After a few days of reception, the eyes stopped aching and tired, even the headache was gone. After the course of treatment, eye pressure returned to normal. Now I feel much better.

Analogs

Analogs can be called drugs: Arutimol, Glaumol, Iotim, Kuzimolol, Niolol, Normatin, Okumed, Okuril, Oftan Timolol, Oftimimol, Unithimolol.

Before buying an analogue, consult your doctor.

Shelf life and storage conditions

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

Watch the video: Using Eye Drops to Treat Glaucoma (December 2019).

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