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Timolol

Prescription

ब्रांड नाम: BETIMOL

खुराक रूप
Drops
मार्ग
OPHTHALMIC
निर्माता
Thea Pharma Inc.

About This Medication

DESCRIPTION Betimol ® (timolol ophthalmic solution), 0.25% and 0.5%, is a non-selective beta-adrenergic antagonist for ophthalmic use. The chemical name of the active ingredient is (S)-1-[(1, 1-dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol. Timolol hemihydrate is the levo isomer. Specific rotation is [α] 25 405nm =-16° (C=10% as the hemihydrate form in 1N HCl). The molecular formula of timolol is Formula C 13 H 24 N 4 O 3 S and its structural formula is: Timolol (as the hemihydrate) is a white, odorless, crystalline powder which is slightly soluble in water and freely soluble in ethanol. Timolol hemihydrate is stable at room temperature. Betimol ® is a clear, colorless, isotonic, sterile, microbiologically preserved phosphate buffered aqueous solution. It is supplied in two dosage strengths, 0.25% and 0.5%. Each mL of Betimol ® 0.25% contains 2.56 mg of timolol hemihydrate equivalent to 2.5 mg timolol. Each mL of Betimol ® 0.5% contains 5.12 mg of timolol hemihydrate equivalent to 5.0 mg timolol. Inactive ingredients: monosodium and disodium phosphate dihydrate to adjust pH (6.5 - 7.5) and water for injection, benzalkonium chloride 0.01 % added as preservative. The osmolality of Betimol ® is 260 to 320 mOsmol/kg. Chemical Structure

सक्रिय तत्व

घटक शक्ति
Timolol -

संकेत और उपयोग

INDICATIONS AND USAGE Betimol ® is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

खुराक और प्रशासन

DOSAGE AND ADMINISTRATION Betimol® Ophthalmic Solution is available in concentrations of 0.25% and 0.5%. The usual starting dose is one drop of 0.25% Betimol® in the affected eye(s) twice a day. If the clinical response is not adequate, the dosage may be changed to one drop of 0.5% solution in the affected eye(s) twice a day. If the intraocular pressure is maintained at satisfactory levels, the dosage schedule may be changed to one drop once a day in the affected eye(s). Because of diurnal variations in intraocular pressure, satisfactory response to the once-a-day dose is best determined by measuring the intraocular pressure at different times during the day. Since in some patients the pressure-lowering response to Betimol® may require a few weeks to stabilize, evaluation should include a determination of intraocular pressure after approximately 4 weeks of treatment with Betimol®. Dosages above one drop of 0.5% Betimol® twice a day generally have not been shown to produce further reduction in intraocular pressure. If the patient's intraocular pressure is still not at a satisfactory level on this regimen, concomitant therapy with pilocarpine and other miotics, and/or epinephrine, and/or systemically administered carbonic anhydrase inhibitors, such as acetazolamide, can be instituted.

Side Effects Overview

ADVERSE REACTIONS The most frequently reported ocular event in clinical trials was burning/stinging on instillation and was comparable between Betimol ® and timolol maleate (approximately one in eight patients). The following adverse events were associated with use of Betimol ® in frequencies of more than 5% in two controlled, double-masked clinical studies in which 184 patients received 0.25% or 0.5% Betimol ® : OCULAR: Dry eyes, itching, foreign body sensation, discomfort in the eye, eyelid erythema, conjunctival injection, and headache. BODY AS A WHOLE: Headache. The following side effects were reported in frequencies of 1 to 5%: OCULAR: Eye pain, epiphora, photophobia, blurred or abnormal vision, corneal fluorescein staining, keratitis, blepharitis and cataract. BODY AS A WHOLE: Allergic reaction, asthenia, common cold and pain in extremities. CARDIOVASCULAR: Hypertension. DIGESTIVE: Nausea. METABOLIC/NUTRITIONAL: Peripheral edema. NERVOUS SYSTEM/PSYCHIATRY: Dizziness and dry mouth. RESPIRATORY: Respiratory infection and sinusitis. In addition, the following adverse reactions have been reported with ophthalmic use of beta blockers: OCULAR: Conjunctivitis, blepharoptosis, decreased corneal sensitivity, visual disturbances including refractive changes, diplopia and retinal vascular disorder. BODY AS A WHOLE: Chest pain. CARDIOVASCULAR: Arrhythmia, palpitation, bradycardia, hypotension, syncope, heart block, cerebral vascular accident, cerebral ischemia, cardiac failure and cardiac arrest. DIGESTIVE: Diarrhea. ENDOCRINE: Masked symptoms of hypoglycemia in insulin dependent diabetics (See WARNINGS ). NERVOUS SYSTEM/PSYCHIATRY: Depression, impotence, increase in signs and symptoms of myasthenia gravis and paresthesia. RESPIRATORY: Dyspnea, bronchospasm, respiratory failure and nasal congestion. SKIN: Alopecia, hypersensitivity including localized and generalized rash, urticaria.

चेतावनियाँ और सावधानियाँ

प्रतिनिर्देश

फार्माकोकाइनेटिक्स

Pharmacokinetics When given orally, timolol is well absorbed and undergoes considerable first pass metabolism. Timolol and its metabolites are primarily excreted in the urine. The half-life of timolol in plasma is approximately 4 hours.

Frequently Asked Questions

INDICATIONS AND USAGE Betimol ® is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

DOSAGE AND ADMINISTRATION Betimol® Ophthalmic Solution is available in concentrations of 0.25% and 0.5%. The usual starting dose is one drop of 0.25% Betimol® in the affected eye(s) twice a day. If the clinical response is not adequate, the dosage may be changed to one drop of 0.5% solution in the affected eye(s) twice a day. If the intraocular pressure is maintained at satisfactory levels, the dosage schedule may be changed to one drop once a day in the affected …

WARNINGS As with other topically applied ophthalmic drugs, Betimol ® is absorbed systemically. The same adverse reactions found with systemic administration of beta-adrenergic blocking agents may occur with topical administration. For example, severe respiratory and cardiac reactions, including death due to bronchospasm in patients with asthma, and rarely, death in association with cardiac failure have been reported following systemic or topical administration of beta-adrenergic blocking agents. Cardiac Failure Sympathetic stimulation may be essential for support of the circulation in individuals …

CONTRAINDICATIONS Betimol ® is contraindicated in patients with overt heart failure, cardiogenic shock, sinus bradycardia, second- or third-degree atrioventricular block, bronchial asthma or history of bronchial asthma, or severe chronic obstructive pulmonary disease, or hypersensitivity to any component of this product.

Timolol is a prescription medication. You will need a valid prescription from a licensed healthcare provider.

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References & Data Sources

चिकित्सा अस्वीकरण

इस पृष्ठ पर दी गई जानकारी केवल शैक्षणिक उद्देश्यों के लिए है और इसे पेशेवर चिकित्सा सलाह, निदान या उपचार के विकल्प के रूप में उपयोग नहीं किया जाना चाहिए।

किसी चिकित्सा स्थिति या दवा के बारे में आपके किसी भी प्रश्न के लिए हमेशा अपने चिकित्सक या अन्य योग्य स्वास्थ्य सेवा प्रदाता की सलाह लें।

डेटा स्रोत: DailyMed (NLM), openFDA, MFDS

Medical Disclaimer

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.