Timolol

In stock 1084 Items

Available since: 2019-09-19

Dosage form

eye drops

Brand & Manufacturer

Package Size

0.5% dropper bottle 5 ml

$20.56

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Clinical Pharmacology

Antiglaucoma β-blocker.

Non-selective p-adrenoreceptor blocker without sympathomimetic activity. When applied topically reduces intraocular pressure by reducing the formation of aqueous humor and a small increase in its outflow. Reducing intraocular pressure, does not affect the accommodation and pupil size, therefore, there is no deterioration in visual acuity; does not reduce the quality of night vision. The effect is manifested 20 minutes after instillation. The maximum effect is observed after 1-2 hours. The duration of action is 24 hours.

Indications

Open-angle glaucoma, secondary glaucoma (uveal, aphakic, post-traumatic), ocular hypertension, angle-closure glaucoma (in combination with myotics).

Composition

Timolol is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Timolol-mez			eye drops
Timolol-SOLOFARM	Grotex Ltd	Russia	eye drops
Occupress-E	Cadilla	India	eye drops
Timolol	Slavic pharmacy	Russia	eye drops
Ocumed	Sentiss Pharma	India	eye drops
Arutimol	Chauvin Ankerpharm	Germany	eye drops
Timolol renewal	PFK Obnovlenie	Russia	eye drops
Ocumed Sentiss Pharma	Sentiss Pharma	India	eye drops
			eye drops

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Dosage and Administration

At the beginning of treatment, 1-2 drops to the affected eye, 2 times a day.

If the intraocular pressure with normal use is normalized, the dose should be reduced to 1 drop once a day in the morning. Doses exceeding 1 drop of a 0.5% solution of thiolol 2 times a day do not lead to an additional decrease in intraocular pressure. If the application of timolol fails to achieve the required level of intraocular pressure, it is necessary to consider the use of additional antihypertensive drugs. The simultaneous use of two beta-blockers for local use is impossible. In patients with a significantly pigmented iris, there may be a less pronounced decrease in intraocular pressure. as well as a longer period to achieve compensation of intraocular pressure. After cessation of treatment, the hypotensive effect of timolol may persist in

for several days, and in the case of long-term prior treatment, the residual and potency effect can last from 2 to 4 weeks. During the treatment with thymolol only in relation to one eye, the hypotensive effect can be noted and in

against the contralateral eye.

Cantrol effectiveness of the drug is recommended approximately 3-4 weeks after the start of therapy (no earlier than 1-2 weeks). With long-term use of thymol tlol, the effect may be weakened.

Transition from another antihypertensive therapy:

When switching from therapy with one beta-blocker to another drug from the group of beta-blockers, it is recommended to complete a full day of therapy with the previously prescribed hypotensive agent, and start instillation of timolol 0.25% in each affected eye 1 drop 2 times a day .

In the absence of an adequate response to therapy, the dose can be increased to one drop of a 0.5% solution of timolol in each affected eye twice a day.

When switching to therapy with a hypotensive drug from another group, except for beta-blockers. continue instillation of a previously prescribed drug with the addition of instillations of one drop of a 0.25% solution of timolol in each affected eye twice a day. The next day, the previous treatment is canceled and timolol therapy is given.

Use in the pediatric population

According to limited data, timolol can be recommended for lowering intraocular pressure in infantile and juvenile congenital glaucoma in the preoperative period or in the case of ineffective surgical treatment. Before using the drug, it is necessary to carefully evaluate the risks and benefits of using timolol in the pediatric population by carefully collecting anamnesis for systemic disorders.

In case the benefit outweighs the risk, it is recommended to use timolol in the lowest available concentration of 1 drop 1 time a day. With insufficient control of intraocular pressure, it is necessary to switch to use 2 times a day.

1 drop with an interval of 12 hours between instillations. Control of eye and systemic side effects is necessary within 1-2 hours after the first instillation, especially in newborns and children under 3 years of age, due to the possibility of developing apnea and Cheyne-Stokes breathing. It is necessary to warn the parents of the child receiving treatment with timolol that the drug should be canceled if the child develops side effects on the side of the respiratory system, in particular, coughing and sneezing.

Treatment with Timolol is usually carried out for a long time. A break in treatment or a change in the dosage of the drug is carried out only as prescribed by the attending physician.

Adverse reactions

Undesirable reactions that occur after ingestion of timolol and other beta-blockers may be regarded as potential adverse reactions and for eyebrowth dosage form of timolol in the dosage form.

Undesirable reactions, information about which was obtained in the course of clinical trials and post-marketing observation of drugs of timothyl)

The frequency of side effects identified both in the course of the studies and in the case of the markup — observation was evaluated as follows: very often (> 1/10); often (> 1/100 to 1/1000 to 1 / 10,000 to

General reactions

With unknown frequency: headache, asthenia / fatigue, chest pain.

On the part of the organ of vision

Often: blurred vision, pain in the eyes, burning and itching in the eyes, discomfort in the eye, conjunctival injection.

Infrequently: blepharitis, spot keratitis, keratitis, conjunctivitis, iritis, diplopia, corneal erosion, corneal ulcer, tearing or reduction of tearing, photophobia, feeling of "sand" in the eyes, eyelid edema, conjunctival edema, ptosis.

Rarely: uveitis, double vision, corneal pigmentation, eyelid erythema.

Very rarely: the development of calcification of the cornea with significant damage due to the presence of phosphates in the composition of the droplets.

With an unknown frequency: decrease in the sensitivity of the cornea, detachment of the vascular window in the postoperative period of antiglaucomatous surgery.

Since the cardiovascular system Infrequently: bradycardia, hypotension.

Rarely: myocardial infarction, decrease or increase in blood pressure, intermittent claudication.

With unknown frequency: cardiac arrest, atrioventricular block, arrhythmia, rapid heartbeat, congestive heart failure, Raynaud's phenomenon.

On the part of the digestive system Infrequently: dysgeusia.

Rarely: dyspepsia, dryness of the oral mucosa, abdominal pain.

With unknown frequency: nausea, vomiting, diarrhea.

On the part of the immune system With an unknown frequency: systemic lupus erythematosus.

Mental disorders Rarely: depression.

With unknown frequency: insomnia, memory loss, nightmare dreams.

Of the nervous system Infrequent: headache.

Rarely: cerebral ischemia, dizziness, migraine.

With unknown frequency: impaired cerebral circulation, fainting, paresthesia, dizziness, aggravation of myasthenia gravis.

On the part of the rut and subcutaneous tissue Rschko: swelling of the face, erythema.

With an unknown frequency: psoriasis or worsening of the course of psoriasis, localized rash, and sweat.

On the part of the connective tissue With an unknown frequency: arthropathy. muscle pain.

Allergic reactions

With unknown frequency: systemic allergic reactions, including anaphylaxis, angioedema, urticaria, local or generalized rash. itchiness

On the part of the respiratory system and mediastinal organs. Infrequently: respiratory failure, shortness of breath, bronchitis.

Rarely: bronchospasm (mainly in patients with already existing bronchospastic conditions), cough, nasal congestion, infections of the upper respiratory tract.

From the endocrine system

With unknown frequency: subclinical course of hypoglycemia in patients with diabetes mellitus (see section "Special instructions").

From the genitourinary system

With unknown frequency: retroperitoneal fibrosis, sexual dysfunction (including impotence), decreased libido, Peyronie's disease.

On the part of ENT organs. With unknown frequency: ringing in the ears.

Adverse reactions that occur after taking timolol or other beta-a) re-blockers inside

Allergic reactions: erythematous rash, fever, accompanied by oolio in the throat, laryngiasia, accompanied by distress syndrome.

General reactions and reactions at the injection site: pain in the extremities, reduced exercise tolerance, weight loss.

Since the cardiovascular system: the worsening of arterial insufficiency, in the dilatation.

On the part of the digestive system: gastrointestinal ool. hepatomegaly. vomiting. thrombosis of mesenteric arteries, ischemic colitis.

From the side of blood and lymphatic system: net thrombocytopenic purpura, thrombocytopenic purpura, agranulocytosis.

On the part of the endocrine system: hyperglycemia, hypoglycemia.

On the part of the skin and subcutaneous tissues: itching, skin irritation, increased pigmentation, sweating.

On the part of the musculoskeletal system: arthralgia.

Nervous System / Mental Disorders: vertigo, reduced concentration of charging, reversible inhibition of mental functions, progressing to catatonia, acute reversible syndrome characterized by impaired orientation in time and space, emotional lability, some difficulty in perception and reduced ability to perform neuropsychiatric tests.

On the part of the respiratory system: wheezing, bronchial obstruction.

From the urinary system: difficulty urinating.

Contraindications

Bronchial asthma, sinus bradycardia, atrioventricular block II and III degrees without cardiac pacemaker, decompensated chronic heart failure, cardiogenic shock, severe chronic obstructive pulmonary disease, sick sinus syndrome. hypersensitivity to the drug.

Carefully:

Cerebrovascular insufficiency, arterial hypotension, diabetes mellitus, hypoglycemia, pulmonary insufficiency, thyrotoxicosis, myasthenia, sinoatrial blockade, impaired peripheral blood circulation (including Rtypo syndrome), pregnancy, simultaneous administration of other beta-adrenoblokagorov.

Drug interactions

The combined use of the drug with eye drops containing adrenaline, can cause dilated pupil.

The specific effect of the drug is a reduction in intraocular pressure, which may increase with simultaneous use of eye drops containing epinephrine and pilocarpine.

Two different adrenergic blocking runs should not be instilled into the same eye. Hypotension and bradycardia can increase with simultaneous use of the drug with antagonists of catcia, reserpine and systemic beta-blockers.

CYP2D6 inhibitors, such as quinidine and zimetidip, can increase the concentration of timolol in plasma.

Simultaneous use with insulin or oral antidiabetic agents can lead to hypoglycemia.

Timolol enhances the action of muscle relaxants, therefore, it is necessary to remove the drug 48 hours before the planned surgery under general anesthesia.

These data may also apply to drugs that were used shortly before.

Pregnancy and Lactation

During pregnancy, use with caution only when the expected therapeutic effect for the mother outweighs the potential risk to the fetus or child.

If you need to use the drug during lactation, breastfeeding should be stopped.

Special instructions

In the postoperative period of antiglaucomatous operations and with the use of drugs that reduce the secretion of intraocular fluid, the development of choroidal detachment is possible.

The use of timolol in patients with atopy or severe pathological reactions to various allergens in history can provoke more severe reactions in response to accidental, diagnostic or therapeutic management of allergens. Such patients may respond poorly to the administration of conventional doses of epinephrine to relieve anaphylactic reactions.

Beta-blockers are able to mask a number of clinical symptoms of hyperthyroidism (and particularly tachycardia). Care is required when using beta-arenoblockers in patients with the possibility of developing thyrotoxicosis.

In patients with a history of heart failure, prolonged myocardial depression in some cases can lead to the development of heart failure. At occurrence of the first signs of heart failure, timolol should be canceled.Care must be taken in the appointment of timolol in patients with atrioventricular block I degree, Prinzmetal angina pectoris and peripheral circulatory disorders (Raynaud's phenomenon).

The main pathogenetic aspect of the treatment of obstructed glaucoma is the need to open the anterior chamber angle, which is achieved by narrowing the pupil with miotics. In connection with the absence of the effect of timolol on the diameter of the pupil in the treatment of diarrhea glaucoma, the drug can be used only in combination with miotics. Because of the possible effect of beta-adrenoreceptor blockers on blood pressure and the number of heartbeats, these funds should be used with caution in patients with cerebrovascular insufficiency. If, after initiating therapy with timolol, signs or symptoms of decreased cerebral circulation develop, the need for therapy with local beta-blockers should be reconsidered.

The use of timolol may increase muscle weakness in myasthenia gravis (for example, it causes increased diplopia, ptosis and general weakness). In some patients with myasthenia gravis and other myasthenic diseases, an increase in muscle weakness was observed with timolol.

With simultaneous use with other drugs, it is necessary to observe the interval between instillations of at least 15 minutes.

When applied, it is necessary to control the function of the area, the state of the cornea, and to evaluate the size of the visual fields at least once every 6 months.

The drug contains preservative benzalkonium chloride, which can cause eye irritation, be absorbed by soft contact lenses, causing a change in their color and have an adverse effect on eye tissue. Contact lenses should be removed before use of the drug and, if necessary, wear them again no earlier than 15 minutes after instillation.

With prolonged use of the drug, the toxic effect of the preservative benzalkonium chloride on the corneal epithelium (the development of punctate keratopathy and / or toxic ulcerative keratopathy) is possible.

Cases of the development of bacterial keratitis in patients who used timolol in containers for multiple dosing of ophthalmic drugs have been noted. These containers were inadvertently contaminated with patients with concomitant corneal diseases.

When transferring patients to treatment with timolol, correction of refractive changes caused by previously used myotics may be necessary.

The drug, like other beta-blockers, can hide the possible symptoms of hypoglycemia in the blood of patients with diabetes mellitus.

In case of an upcoming surgery under general anesthesia, it is necessary to discontinue the drug 48 hours before the operation, since it enhances the action of muscle relaxants and general anesthetics.

Impact on the ability to drive trans. Wed and fur .:

During the period of treatment, care must be taken when driving and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions in connection with the profile of side effects (in particular, from the organ of vision and the nervous system).

Overdosage

Possible development of systemic effects characteristic of beta-blockers: dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea and vomiting, loss of consciousness, hypotension, shortness of breath, generalized convulsions, cardiogenic shock, heart failure and cardiac arrest.

In case of accidental ingestion of timolol, gastric lavage and the ingestion of activated carbon are necessary. It is shown that the drug can not be removed from the body by hemodialysis.

With the development of bradycardia and bradyarrhythmias (with atrioventricular blockade of grade II and III), intravenous administration of atropine sulfate in a dose of 0.25 to 2 mg is recommended; and the introduction of isoprenaline is shown in the partial relief of bradycardia. If hard-to-use bradycardia should be considered, the installation of a pacemaker should be considered. In case of hypotension, it is recommended to take sympathomics, such as dopamine, dobutamine, and neradrenaline. In the absence of effect - the introduction of glucagon.

With the development of acute heart failure, the use of digitalis and diuretics, as well as oxygen therapy, with the ineffectiveness of intravenous administration of aminophylline, is recommended.