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Timolol Brand And Generic Names

Pharmaceutical group


Antiglaucoma agents - beta-blocker

Dosage form


Eye gel, eye drops

Pharmacological action


Timolol is a nonselective beta-adrenergic blocker. When applied topically, the drug lowers intraocular pressure by reducing aqueous humor formation and a slight increase in the outflow. Reducing the intraocular pressure, it does not affect the accommodation and pupil size, so there is no deterioration of visual acuity or reduction of the quality of color and night vision. Timolol shows no sympathomimetic and membrane stabilizing activity. It inhibits central sympathetic impulses and renin secretion, weakens the sensitivity of peripheral tissues to catecholamines, inhibits sinoatrial node automaticity and reduces the occurrence of ectopic foci in atria, the ventricles (in lesser extent). Timolol lowers the rate of excitation, contractility, cardiac output and myocardial oxygen demand, suppresses the activity of baroreceptors of the aortic arch, their response to low blood pressure, and shows cardioprotective effects. It can reduce mortality after myocardial infarction and the risk of sudden death, prevents the occurrence of headache of vascular origin. When applied topically, the agent reduces the secretion of aqueous humor and intraocular pressure (both high and normal), allowing to control intraocular pressure during sleep. Effect appears in 20 minutes after administration, the maximum effect can be seen after 1-2 hours; duration - 24 hours. The drug is well absorbed through the retina of the eye and nasal mucosa (may develop systemic effects), being absorbed from the gastrointestinal tract by 90%. Timolol passes the placental barrier.

Indications


Orally: hypertension, hypertrophic cardiomyopathy, mitral valve prolapse, angina, prevention of re-infarction, migraine (prevention of attacks), essential tremor, anxiety.

Ocular hypertension: open-angle glaucoma, secondary glaucoma (uveal, posttraumatic); as an auxiliary drug: angle-closure glaucoma (in combination with miotics), congenital glaucoma (with the ineffectiveness of other therapeutic interventions), including buphthalmos, and sharp rise in intraocular pressure.

Contraindications


Hypersensitivity to the drug, degenerative processes in corneal.
Caution: severe course of COPD, asthma, sinus bradycardia (heart rate less than 55/min), SA block, decompensated chronic heart failure, hypotension, atrophic rhinitis, pulmonary failure, severe cerebrovascular disease, diabetes, hypoglycemia, hyperthyroidism, myasthenia gravis, severe allergic inflammation of the nasal mucosa, pulmonary emphysema, chronic bronchitis, non-allergic vasomotor rhinitis, Raynaud's disease, liver and/or kidney disease, acidosis, older age, co-administration of other beta-blockers, administration in children (efficacy and safety have not been established), especially during the neonatal period (for drug forms containing benzalkonium chloride as a preservative), pregnancy, lactation.

Timolol Side effects


Local reactions: irritation of the conjunctiva - conjunctival hyperemia, tearing or decreased lacrimation, photophobia, corneal epithelial edema, burning and itchy eyes, redness of the eyelid skin, short-term disturbance of visual acuity, blepharitis, conjunctivitis, keratitis, prolonged use may develop superficial punctate keratopathy (decrease in transparency of the cornea) and decreased corneal sensitivity, possible ptosis, rarely - diplopia.
Systemic reactions: paresthesia, rhinitis, nasal congestion, nasal bleeding, decreased blood pressure, collapse, bradycardia, bradyarrhythmia, AV block, decrease in myocardial contractility, worsening manifestations of CHF, headache, dizziness, drowsiness, hallucinations, depression, myasthenia gravis, decreased potency, dyspnoea, bronchospasm, pulmonary insufficiency, nausea, vomiting, diarrhea, chest pain, ringing in the ears, slowing of psychomotor reactions.
Allergic reactions: urticaria.
Other: angioedema, withdrawal syndrome, changes in body weight, lupus syndrome, weakening of libido, impotence, Peyronie's disease, hyperkalemia, hyperuricemia, hypertriglyceridemia.

Overdose


Symptoms: may develop typical effects for beta-blockers (dizziness, headache, arrhythmia, bradycardia, bronchospasm, nausea, vomiting).
Treatment: Immediately flush your eyes with water or 0.9% solution of NaCl. When the drug is taken orally, do gastric lavage, take activated charcoal. Symptomatic therapy: atropine, beta-adrenoceptor agonists (isoprenaline, izadrin), glucagon hydrochloride, norepinephrine, dobutamine, cardiac glycosides, diuretics, aminophylline (with heart failure), oxygen therapy. Hemodialysis is ineffective.
 

Timolol Dosage and administration


Adults and children over 10 years: instilled into the conjunctival sac of 1 drop of 0.25% solution of 2 times a day or 1 drop of 0.5% solution two times a day in case of the lack of effectiveness. With the normalization of intraocular pressure, the maintenance dose is 1 drop of 0.25% 1 time per day. Infants and children up to 10 years - 1 drop of 0.25% solution of 2 times per day.

Special instructions


Use caution when driving at night and avoid activities with increased demands on adaptation to low light. Monitoring of the treatment effectiveness is recommended approximately 3-4 weeks after initiation of therapy (not earlier than in 1-2 weeks). With prolonged use of Timolol possible effects may weaken. During the treatment, it is strongly advisable to monitor the function of tearing, corneal integrity and evaluate visual margins of at least 1 time in 6 months. Measure your intraocular pressure at least 1 time per month. Preservative contained in the product may penetrate your soft contact lenses, so during treatment you should not wear soft contact lenses. Hard contact lenses should be removed prior to instillation and put no earlier than 15 minutes after it. During the period of treatment patients must be careful when driving and doing some activities that require high concentration, psychomotor speed of reaction and good vision (for 0.5 h after instillation into the eye).

Interaction


Epinephrine, pilocarpine, systemic beta-blockers increase the effect of Timolol. The drug should not be simultaneously applied with antipsychotic drugs (neuroleptics) and anxiolytic drugs (tranquilizers). Timolol enhances the action of muscle relaxants and general anesthetics (you should stop taking the drug a few days prior to general anesthesia with ether or chloroform or using peripheral muscle relaxants). On the background of treatment should be avoided verapamil, diltiazem (may develop: depression of AV conduction, bradycardia and decreased blood pressure). During treatment, it is not recommended to take ethanol (possibly sharp decline in arterial tension). Before taking concurrently Timolol with antihypertensive drugs, beta-blockers, insulin or oral hypoglycemic drugs, corticosteroids, psychoactive drugs, always consult a doctor because the effect of which are associated with increased elimination of epinephrine. The simultaneous use of eye drops containing epinephrine or norepinephrine may cause mydriasis. Epinephrine eye drops potentiate intraocular pressure reduction. Timolol increases the probability of violations of automaticity and contractility of heart on the background of amiodarone, quinidine drugs. NSAIDs weaken the antihypertensive effect of Timolol. When applied topically, it is compatible with miotics and carbonic anhydrase inhibitors.
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