Arutimol

Arutimol (also known as timolol) is a medication commonly used to treat glaucoma and increased pressure in the eye. Glaucoma is a serious eye condition characterized by increased pressure in the eye, which can lead to damage to the optic nerve and vision loss.

Timolol belongs to a class of drugs known as beta blockers. It works by reducing the production of aqueous fluid inside the eye, which in turn lowers the pressure in the eye. This helps reduce the risk of damage to the optic nerve and preserve vision in patients with glaucoma.

Arutimol is usually available in the form of eye drops. It is usually applied 1-2 times a day, depending on the doctor's instructions and the patient's specific needs. As with any medication, it is important to consult with your doctor before using Arutimol to ensure that it is suitable for your specific conditions and will not cause unwanted side effects.

Indications Arutimola

• Open-angle glaucoma: This is the most common form of glaucoma, where the pressure inside the eye (intraocular pressure) is elevated due to improper drainage of aqueous humor. Arutimol helps lower this pressure, which can help prevent damage to the optic nerve and preserve vision.
• Narrow-angle glaucoma: This is a less common but more severe form of glaucoma, characterized by poor drainage of aqueous fluid from the eye due to a narrow angle between the iris and cornea. Timolol may be used to lower intraocular pressure before procedures are performed to widen the angle and improve drainage.
• Focal or diffuse corneal atrophy: Arutimol may sometimes be recommended to treat this condition, which is characterized by a reduction in the thickness of the cornea.
• Elevated intraocular pressure without glaucoma: In some cases, timolol may be used to lower intraocular pressure in patients with elevated intraocular pressure without signs of glaucoma to prevent the disease from developing.
• Open-angle glaucoma: This is the most common form of glaucoma and is characterized by increased pressure in the eye due to limited or obstructed drainage of aqueous humor from the eye. Timolol helps lower the pressure in the eye, which can help prevent further damage to the optic nerve and preserve vision.
• Certain forms of hypertensive eye disease: Timolol may sometimes be used to control intraocular pressure in patients with hypertensive eye disease.

Release form

Arutimol is usually available in the form of eye drops. Eye drops are usually packaged in special containers that ensure sterility and ease of use. Usually, the drops are supplied in vials or plastic bottles with a dosing device that facilitates accurate dosing of the drops.

Pharmacodynamics

The pharmacodynamics of timolol, the main active component in Arutimol, are related to its ability to block beta-adrenergic receptors. Timolol is a direct non-cardioselective beta-adrenergic receptor blocker.

In the eye, timolol reduces intraocular pressure by decreasing the production of aqueous humor. This process occurs by blocking beta-adrenergic receptors in structures of the eye such as the rhizome epithelium of the ciliary body, which results in decreased aqueous humor formation.

Beta-blockade can also reduce aqueous secretion in the eye by reducing aqueous humor formation during the active aqueous humor production process in the ciliary body. This results in a decrease in intraocular pressure, which is especially important for the treatment of glaucoma and the prevention of optic nerve damage.

Timolol is usually applied topically as eye drops and exerts its action directly in the eye, minimizing systemic side effects. However, in rare cases, some of the drug may still be absorbed through the eye and exert a systemic effect, affecting other organs and tissues associated with beta-adrenergic receptors, which may cause side effects.

Pharmacokinetics

• Absorption: Following topical application of timolol as eye drops to the eye, the drug can be absorbed through the conjunctiva and cornea of the eye. However, systemic absorption of timolol is low because it mainly remains in the eye and virtually does not penetrate the ocular barrier into the blood.
• Distribution: Timolol, which is absorbed into the bloodstream, usually has a high volume of distribution, meaning it can spread quickly throughout the body.
• Metabolism: Timolol is metabolized primarily in the liver to form inactive metabolites. The main metabolic pathway is oxidation via the CYP2D6 enzyme.
• Elimination: Timolol metabolites and some unchanged drug are excreted primarily in the urine. Timolol is eliminated from the body primarily as metabolites.

Dosing and administration

• Dosage: The usual recommended dose for adults is one drop of 0.25% or 0.5% timolol solution into the conjunctival sac of the eye, once or twice daily. However, the exact dosage may be adjusted by the physician depending on the severity of the disease and the individual characteristics of the patient.
• Directions for use: Before using the drops, wash your hands thoroughly to avoid eye contamination. Then tilt your head back or lie down, lift your eyes up and gently pull your lower eyelid down to create a pocket for the drops. Then gently inject one drop of the solution into the conjunctival sac of the eye, close your eyes a little after injecting the drop to prevent leakage.
• Consistency in use: For best results, the drops should be used daily at the recommended doses and times, even if there are no symptoms. This will help maintain stable intraocular pressure and prevent the disease from progressing.

Use Arutimola during pregnancy

The use of Arutimol during pregnancy should be carried out under the supervision of a physician and only in the case of clear medical indications, when the benefits of its use outweigh the potential risks to the mother and fetus.

To date, data on the safety of timolol during pregnancy are limited and its effects on the fetus have not been fully studied. There have not been sufficient controlled clinical studies in pregnant women to assess the risk to the fetus.

Timolol, like many other drugs, can penetrate the placental barrier and affect fetal development. Therefore, its use should be carried out with caution and only after careful discussion with a doctor.

Contraindications

• Hypersensitivity or allergic reaction: People with a known hypersensitivity or allergic reaction to timolol or other components of the drug should avoid using it.
• Bronchial asthma or chronic obstructive pulmonary disease (COPD): Timolol, as a beta-blocker, may cause bronchial constriction and deterioration of respiratory function in patients with asthma or COPD. Therefore, it is contraindicated in such patients without strict medical supervision.
• Cardiovascular disease: Timolol may worsen symptoms of heart failure, exacerbate cardiac arrhythmias, or cause hypotension in patients with cardiovascular disease. Therefore, it is generally not recommended for people with serious cardiovascular disease.
• Sinus bradycardia syndrome: Timolol may cause bradycardia (slow heart rate) in patients with sinus bradycardia syndrome.
• Hypersensitivity to CYP2D6 enzyme inhibitors: Since timolol is metabolized by CYP2D6, patients with hypersensitivity to inhibitors of this enzyme should avoid its use or use it with caution.
• Paediatric population: The use of timolol in children may be limited due to insufficient safety and efficacy data in this patient group.

Side effects Arutimola

• Application site reactions: This may include irritation, burning, redness or itching of the eyes.
• Changes in taste: Some patients may experience changes in taste perception after using timolol eye drops.
• Slow heart rate (bradycardia): Timolol may slow the heart rate, which may cause bradycardia in some patients.
• Low blood pressure: Timolol may cause low blood pressure in some people.
• Dry eyes: Some patients may experience a feeling of dryness, discomfort, or a gritty sensation in the eyes.
• Headache: Patients may experience headaches after using timolol.
• Drowsiness: Some people may feel drowsy or tired after using timolol.
• Digestive problems: This may include diarrhea or nausea.
• Rarely, serious side effects may occur, such as allergic reactions, bronchospasm (narrowing of the airways), worsening of asthma, angioedema (Stuard-Adams edema), arrhythmia, and other cardiovascular problems.

Overdose

• Increased side effects: Such as severe drowsiness, dizziness, blurred vision, severe bradycardia (slow heart rate), headache, nausea, vomiting, etc.
• Serious cardiovascular complications: Including cardiac arrhythmia, cardiac arrest, and low blood pressure.
• Respiratory complications: Deterioration of respiratory function, bronchospasm (narrowing of the bronchi), obstructive airway diseases.

Interactions with other drugs

• Blood pressure lowering drugs (antihypertensive drugs): Using timolol in combination with other antihypertensive drugs such as beta blockers, diuretics, or ACE inhibitors may result in additional lowering of blood pressure.
• Cardiovascular drugs: Timolol may increase the effects of antiarrhythmic drugs such as aminoxidin and lead to serious heart rhythm problems.
• Central depressants and hypnotics: Timolol may enhance the depressant effects of central depressants and hypnotics, which may lead to increased drowsiness and respiratory depression.
• Antidepressants and neuroleptics: When combined with timolol, antidepressants and neuroleptics may enhance its hypotensive effect and increase the risk of orthostatic hypotension.
• Sympathomimetics: The use of sympathomimetics in combination with timolol may lead to a decrease in its antihypertensive effect.
• Monoamine oxidase inhibitors (MAOIs): Use of timolol in combination with MAOIs may result in increased antihypertensive effects and an increased risk of serious side effects.