Timolol (Timolol) eye drops. Price, instructions for use, analogues, reviews

Ophthalmic drug Timolol is an eye drop used to treat glaucoma. The drug is prescribed to patients of different age categories. The low price of the drug ensures its availability and popularity.

Release form and composition of the drug

Eye drops are produced as a colorless solution for conjunctival administration. The drug is odorless. Timolol is delivered to pharmacies in soft bottles made of purified medical polymer with a volume of 5 ml.

The content of the active substance is 0.25 or 0.5%, depending on the dosage. The vials are equipped with a built-in dispenser for precise drop delivery of the medication. The carton contains 1 tube of antiglaucoma medicine and an insert sheet and instructions for use.

The pharmacologically active component of the drug is timolol maleate. This chemical compound is a non-selective type of beta-blocker that acts directly on the pupil and optic nerves. It has hypotensive and antiarrhythmic effects.

Timolol - eye drops, the price of which is low against the background of significant therapeutic effects with local conjunctival application.

The following auxiliary components are used in the preparation:

Chemical compound	Properties
Sodium dihydrogen phosphate	Inorganic compound with laxative effect, water retention and buffering properties.
Disodium salt of ethylenediaminetetraacetic acid	Forms a stable chemical bond with calcium ions. It is used to treat a wide range of diseases.
Disodium dihydrogen phosphate	Humectant, regulating acid balance and blocking heavy metal salts.
Benzalkonium chloride	Antiseptic with high antimicrobial activity, virus inactivator.
Sodium chloride	The most important inorganic element of extracellular fluids. Corrects osmotic pressure, relieves puffiness.
Sodium hydroxide	Compound with sedative properties.

Thanks to the balanced chemical formula, Timolol has a complex therapeutic effect on the ocular apparatus.

Pharmacological properties

The drug belongs to the category of non-selective beta-blockers. Its pharmacological action is aimed at restoring normal ocular pressure.

This clinical effect is achieved due to the ability of the active component and excipients included into the composition of Timolol, reduce the volume of pathological liquid secretion and partially evacuate it from the visual organ.

The drug does not dilate the pupils, and its active components easily overcome the corneal barrier, being rapidly absorbed into the systemic circulation and the lacrimal tract. The pharmacological properties of the ophthalmic medication are based on its antiglaucoma and myotic effects.

Timolol maleatate is an effective inhibitor of b1 and b2 adrenergic receptors. With conjunctival installation, it instantly reduces the pressure in the orbit by reducing the synthesis of liquid secretions.

The rapidity of the clinical effect is associated with the ability of timolol maleate to block biological activity. adenylate cyclase mechanism of ciliary fibers, which perform the function of transporting sodium ions from blood plasma to intraocular secret.

This reduces the intensity of moisture formation without affecting accommodation, refraction and changes in the size of the pupillary element. The drug does not affect visual acuity. Ophthalmic medication reduces intraocular pressure (IOP) without reference to the initial indicator.

Pharmacodynamics and pharmacokinetics

Timolol - eye drops, the price of which is due to the limited spectrum of therapeutic action. The drug is used exclusively for the treatment of glaucoma, including age-related. The medicine additionally has an antianginal effect.

Timolol does not possess sympathomimetic and membrane stabilizing properties. It slightly suspends central impulses and reduces the synthesis of renin in the ocular organ.

Timolol maleatate weakens the sensitivity of peripheral nerve fibers to the effects of catecholamines - physiologically active mediators of intercellular interaction. The drug inhibits the reflexes of the sinotrial node, minimizes the formation of ectopic foci.

The pharmacological activity of the drug is manifested within 20 minutes. after conjunctival application. The limiting concentration of the active substance of the eye drops is fixed for 1-2 hours. after instillation. The therapeutic effect lasts up to a day.

Saturation of blood plasma with the active substance after topical application in the recommended dosage is practically not detected. The bioavailability of the drug is 92%.

Timolol maleate metabolites have negligible pharmacological activity. They are 70% excreted by the renal organ and eliminated from the body through the urinary ducts.

Indications for use

Timolol is a narrowly targeted ophthalmic medication. The main indications for its appointment are open and closed angle glaucoma. The drug is effective for ocular hypertension.

In angle-closure glaucoma, Timolol is often used as part of a combination therapy in conjunction with the intake of miotic drugs.

The drug is prescribed for the treatment of the following diseases of the cardiovascular apparatus:

• arterial hypertension - due to its ability to be absorbed into the systemic circulation;
• hypertrophic cardiomyopathy - an autosomal dominant pathology, which is characterized by a thickening of the heart ventricles;
• mitral valve prolapse;
• angina pectoris;

In modern cardiological practice, drugs based on timolol maleate are used internally to prevent recurrent myocardial muscle infarction. Prescribe a medication to prevent migraine attacks, with essential tremor, to eliminate the state of increased anxiety in elderly patients.

Eye drops are used exclusively topically. They are effective in primary and secondary glaucoma, aphakia - surgical removal of the eye lens. The medication is prescribed for a sharp and sudden increase in IOP.

Contraindications

Timolol is a potent drug. There are contraindications for use.

The drug is not prescribed for:

• active phase of bronchial asthma;
• increased biological sensitivity to drug components;
• inflammation of the mucous membrane of the respiratory tract;
• ophthalmic pathologies associated with clouding of the eye lens;
• corneal dystrophy;
• 2nd and 3rd degree atrioventricular block;
• sinus bradycardia - a decrease in the number of contractions of the heart muscle;
• kidney failure;
• a state of cardiogenic shock;

Timolol - eye drops that should be used with extreme caution if the patient has severe endocrine disorders, in particular type 2 diabetes mellitus. The medicine has a low price, but an impressive list of absolute contraindications and time limits.

The conjunctival drug is not prescribed for:

• severe obstructive pulmonary disease;
• myasthenia gravis - an autoimmune neuromuscular disorder characterized by pathologically rapid fatigue of striated fibers;
• chronic liver disease;

Restrictions on Timolol treatment include the period of childbearing and breastfeeding.

At what age can the drug be used?

Ophthalmic medicine is prescribed for children from 5 years old. For patients in this category, a lower dosage is used. Treatment is carried out exclusively under the supervision of a physician. Given the ability of the active substance of the drug to lower IOP, regardless of the initial value, the drug is rarely prescribed to children.

Instructions for use, dosage

The drug for conjunctival use is used for therapeutic and prophylactic purposes. It is intended for monotherapy of glaucoma and is included in the complex drug treatment of hypertension of the optic organ.

The medicinal solution is supplied locally, instilled with a complete dispenser into the cavity of the conjunctival sac. The doctor calculates the therapy regimen and the maximum daily dosage individually based on the clinical characteristics of the pathology to be eliminated, the anamnesis and the patient's age.

At the beginning of the treatment course, a solution with a concentration of the active component of 0.25% is often used. A similar content of the active substance is used for prophylactic purposes. The standard therapeutic dosage is 1 drop in the conjunctival sac of each eye 2-3 times a day.

For children from 12 years old and adults, the norm is identical. If after 3 days of the course there is no improvement in the clinical picture, the patient is transferred to a more concentrated solution with an active substance content of 0.5%. The frequency of conjunctival installations is reduced when the desired therapeutic result is achieved.

The instillation session is carried out in the morning. The duration of the course of treatment is determined by the clinical efficacy of the drug and can reach 2-3 months of daily use. The expected result of therapy is a decrease in intraocular pressure to a normal value.

Side effects

Timolol is a biochemically aggressive drug. Its use is associated with numerous side effects. There is an increased photosensitivity of the eye organ for some time after instillation.

This effect is individual and largely affects older patients. Pain, itching and redness of the eyes are possible.

The most commonly reported side effects with conjunctival drug administration:

• nausea;
• vomiting;
• difficulty breathing;
• slight spasm of the bronchial cavity;
• arterial hypotension;
• decreased muscle tone;
• disorder of nervous reactions;

On the part of the cardiovascular apparatus, negative actions associated with the course of taking eye drops are manifested symptomatic bradycardia and Raynaud's syndrome - changes in the color and temperature of the extremities, tingling sensation in the fingers arms and legs.

Among the recorded side effects are nasal congestion, chest pain, angioedema.

The nervous system and cerebral organ can react to taking Timolol:

• auditory and visual hallucinations;
• headaches;
• asthenia;
• short-term impairment of coordination of movements and orientation in space;
• diplopia - double vision;

Due to the use of the drug, a weakening of libido, a sharp weight loss, and hyperkalemia were recorded. On the part of the hemostatic system, a decrease in the level of hemoglobin in the blood and a drop in the hematocrit number are possible.

Overdose

When the recommended daily intake of the drug is exceeded, typical signs of drug intoxication and symptoms characteristic of all adrenergic blockers:

• dizziness;
• general weakness;
• lowering body temperature;
• insomnia;
• feeling tired, others.

If such phenomena are detected, symptomatic therapy is carried out and an absorbent drug is taken. In severe cases, the patient is placed in a hospital under round-the-clock medical supervision with constant monitoring of the basic physiological parameters of the body.

special instructions

Timolol - eye drops (the price of the medicine is available to a wide range of patients) that do not affect mydriasis and visual acuity. However, when using this drug, IOP and the condition of the cornea, which may undergo dystrophic changes, should be monitored.

When Timolol is added to the complex therapy or when a patient is transferred to it from another drug, correction of the refraction of the optic organ is required. For 48 hours before surgery, the drug is stopped.

Carefully complete the course of treatment if there is a history of endocrine disorders. The entire period of taking Timolol should be monitored for blood glucose, especially in patients with type 2 diabetes mellitus.

Beta-blockers have the ability to absorb systemically, which leads to the accumulation of the active substance of the drug in the body and the occurrence of pronounced side effects.

Bronchospasm triggered by medication can cause cardiac arrest and death even with conjunctival drip. In patients with myasthenia gravis, Timolol is able to dramatically reduce muscle tone.

When treating with this drug, it is worth refusing to use contact lenses based on a chloride preservative. benzalkonium due to the risk of unwanted chemical reactions that lead to severe eye irritation apples.

Such accessories are removed before the instillation procedure and put on at least 15 minutes later. after her. There is a risk of systemic allergic manifestations in patients prone to anaphylactic reactions. When prescribing the drug, you should make sure that the body is normally susceptible to its constituents.

Drug interactions

Timolol - eye drops (the price of the medication is low, which makes it one of the most frequently used by ophthalmologists), the clinical effect of which is enhanced by other beta-blockers. This effect is exerted by Epinephrine and Pilocarpine.

You cannot combine Timolol with Reserpine. As a result, arterial hypotension develops rapidly. Parallel reception can lead to bradycardia. Do not combine eye drops with local anesthetic drugs.

It is forbidden to combine Timolol with drugs of the category of cardiac glycosides. Do not combine eye drops with calcium antagonists.

Mutually increase the risk of impaired natural reflexes, nerve conduction and heart rate:

• Amiodarone;
• antispasmodics,
• Dialtizem;
• Veralamil;
• preparations based on quinidine compounds.

Mixing timolol maleate with dihydropyridine calcium antagonists significantly increases the likelihood of a drop in blood pressure and cardiac decompensation.

Non-steroidal anti-inflammatory drugs significantly weaken the hypotensive effect of Timolol. Eye drops are fully compatible with any miotic drugs and inhibitors of the CA4 gene enzyme.

It is forbidden to simultaneously use Timolol with oral antidiabetic drugs. This contributes to the development of hypoglycemia. Eye drops enhance the neuroblockade effect of Tubocurarine.

Analogs

An extensive group of medications has a similar mechanism of pharmacological action with Timolol.

Rating of the most demanded:

• Arutimol. Eye drops for the elimination of hypertension and the treatment of various ophthalmic pathologies.
• Dorzolamide. Antiglaucoma drug, non-selective carbonic anhydrase inhibitor. Reduces the secretion of intraocular fluid.
• Brinzolamide. A medication used to eliminate intraocular hypertension in patients with angle-closure glaucoma.
• Okumed. Eye drops based on timolol maleate.
• Betaxolol. Cardioselective beta-blocker of antianginal, hypotensive, antiarrhythmic action.

These drugs are prescribed when there are contraindications to taking Timolol or it does not give the desired therapeutic effect.

Terms, conditions of sale and storage

The drug is suitable for use within 24 months from the date of manufacture. Timolol is sold in pharmacies only with a prescription. The optimal storage temperature is up to + 25 ° С. The opened bottle must be used as directed within 30 days.

Price

Ophthalmic drug Timolol - available eye drops. The approximate price in Russian pharmacies of domestic medicine is 50-70 rubles. for a 5 ml bottle with an active ingredient concentration of 0.5%. The cost of similar foreign-made products reaches 300 rubles.

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