Drug: Betimol

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 HCI). The molecular formula of timolol is Formula C13H24N4O3S 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 hemihy-drate is stable at room temperature. Betimol® (timolol ophthalmic solution) 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® (timolol ophthalmic solution) is 260 to 320 mOsmol/kg.

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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® (timolol ophthalmic solution) in frequencies of more than 5% in two controlled, double-masked clinical studies in which 184 patients received 0.25% or 0.5% Betimol® (timolol ophthalmic solution) : 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. Read the Betimol (timolol ophthalmic solution) Side Effects Center for a complete guide to possible side effectsLearn More »

Source: http://www.rxlist.com

Betimol® (timolol ophthalmic solution) Ophthalmic Solution is available in concentrations of 0.25 and 0.5 percent. The usual starting dose is one drop of 0.25 percent Betimol® (timolol ophthalmic solution) 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 percent 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® (timolol ophthalmic solution) may require a few weeks to stabilize, evaluation should include a determination of intraocular pressure after approximately 4 weeks of treatment with Betimol® (timolol ophthalmic solution) . Dosages above one drop of 0.5 percent Betimol® (timolol ophthalmic solution) 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 ep-inephrine, and/or systemically administered carbonic anhydrase inhibitors, such as acetazolamide can be instituted.

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Beta-adrenergic blocking agents Patients who are receiving a beta-adrenergic blocking agent orally and Betimol® (timolol ophthalmic solution) should be observed for a potential additive effect either on the intraocular pressure or on the known systemic effects of beta-blockade. Patients should not usually receive two topical ophthalmic beta-adrenergic blocking agents concurrently. Catecholamine-depleting drugs Close observation of the patient is recommended when a beta-blocker is administered to patients receiving cate-cholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or marked bradycardia, which may produce vertigo, syncope, or postural hypotension. Calcium antagonists Caution should be used in the co-administration of beta-adrenergic blocking agents and oral or intravenous calcium antagonists, because of possible atrioventricular conduction disturbances, left ventricular failure, and hypotension. In patients with impaired cardiac function, co-administration should be avoided. Digitalis and calcium antagonists The concomitant use of beta-adrenergic blocking agents with digitalis and calcium antagonists may have additive effects in prolonging atrioventricular conduction time. Injectable Epinephrine (See PRECAUTIONS, General, Anaphylaxis.) Read the Betimol Drug Interactions Center for a complete guide to possible interactions Learn More »

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Betimol® (timolol ophthalmic solution) is indicated in the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma.

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Betimol® (timolol ophthalmic solution) 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. Last reviewed on RxList: 3/26/2009
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

No information is available on overdosage with Betimol® (timolol ophthalmic solution) . Symptoms that might be expected with an overdose of a beta-adrenergic receptor blocking agent are bronchospasm, hypotension, bradycardia, and acute cardiac failure.

Source: http://www.rxlist.com

Betimol® (timolol ophthalmic solution) is a clear, colorless solution. Betimol® (timolol ophthalmic solution) 0.25% is supplied in a white, opaque, plastic, ophthalmic dispenser bottle with a controlled drop tip as follows: NDC 68669-522-05 5.0mL fill in 5 cc container NDC 68669-522-10 10mL fill in 11 cc container NDC 68669-522-15 15mL fill in 15 cc container Betimol® (timolol ophthalmic solution) 0.5% is supplied in a white, opaque, plastic, ophthalmic dispenser bottle with a controlled drop tip as follows: NDC 68669-525-05 5.0mL fill in 5 cc container NDC 68669-525-10 10mL fill in 11 cc container NDC 68669-525-15 15mL fill in 15 cc container Storage Store between 15-25°C (59-77°F). Do not freeze. Protect from light. Marketed by: VISTAKON® Pharmaceuticals, LLC Jacksonville, FL 32256 USA. Manufactured By: Santen Oy, P.O. Box 33, FIN-33721 Tampere, Finland. November 2006 Version. Last reviewed on RxList: 3/26/2009
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

General Because of the potential effects of beta-adrenergic blocking agents relative to blood pressure and pulse, these agents should be used with caution in patients with cerebrovascular insufficiency. If signs or symptoms suggesting reduced cerebral blood flow develop following initiation of therapy with Betimol® (timolol ophthalmic solution) , alternative therapy should be considered. There have been reports of bacterial keratitis associated with the use of multiple dose containers of topical ophthalmic products. These containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface. (See PRECAUTIONS: Information For Patients.) Muscle Weakness: Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g. diplopia, ptosis, and generalized weakness). Beta-adrenergic blocking agents have been reported rarely to increase muscle weakness in some patients with myasthenia gravis or myasthenic symptoms. In angle-closure glaucoma, the goal of the treatment is to reopen the angle. This requires constricting the pupil. Betimol® has no effect on the pupil. Therefore, if timolol is used in angle-closure glaucoma, it should always be combined with a miotic and not used alone. Anaphylaxis: While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reactions to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenge with such allergens. Such patients may be unresponsive to the usual doses of epinephrine used to treat anaphylactic reactions. The preservative benzalkonium chloride may be absorbed by soft contact lenses. Patients who wear soft contact lenses should wait 5 minutes after instilling Betimol® (timolol ophthalmic solution) before they insert their lenses. Carcinogenesis, Mutagenesis, Impairment of Fertility Carcinogenicity of timolol (as the maleate) has been studied in mice and rats. In a two-year study orally administrated timolol maleate (300mg/kg/day) (approximately 42,000 times the systemic exposure following the maximum recommended human ophthalmic dose) in male rats caused a significant increase in the incidence of adrenal pheochromocytomas; the lower doses, 25 mg or 100 mg/kg daily did not cause any changes. In a life span study in mice the overall incidence of neoplasms was significantly increased in female mice at 500 mg/kg/day (approximately 71,000 times the systemic exposure following the maximum recommended human ophthalmic dose). Furthermore, significant increases were observed in the incidences of benign and malignant pulmonary tumors, benign uterine polyps, as well as mammary adenocarcinomas. These changes were not seen at the daily dose level of 5 or 50 mg/kg (approximately 700 or 7,000, respectively, times the systemic exposure following the maximum recommended human ophthalmic dose). For comparison, the maximum recommended human oral dose of timolol maleate is 1 mg/kg/day. Mutagenic potential of timolol was evaluated in vivo in the micronucleus test and cytogenetic assay and in vitro in the neoplastic cell transformation assay and Ames test, In the bacterial mutagenicity test (Ames test) high concentrations of timolol maleate (5000 and 10,000 g/plate) statistically significantly increased the number of revertants in Salmonella typhimurium TA100, but not in the other three strains tested. However, no consistent dose-response was observed nor did the number of revertants reach the double of the control value, which is regarded as one of the criteria for a positive result in the Ames test. In vivo genotoxicity tests (the mouse micronucleus test and cytogenetic assay) and in vitro the neoplastic cell transformation assay were negative up to dose levels of 800 mg/kg and 100 g/mL, respectively. No adverse effects on male and female fertility were reported in rats at timolol oral doses of up to 150 mg/kg/day (21,000 times the systemic exposure following the maximum recommended human ophthalmic dose). Pregnancy Teratogenic effects Category C: Teratogenicity of timolol (as the maleate) after oral administration was studied in mice and rabbits. No fetal malformations were reported in mice or rabbits at a daily oral dose of 50 mg/kg (7,000 times the systemic exposure following the maximum recommended human ophthalmic dose). Although delayed fetal ossification was observed at this dose in rats, there were no adverse effects on postnatal development of offspring. Doses of 1000 mg/kg/day (142,000 times the systemic exposure following the maximum recommended human ophthalmic dose) were maternotoxic in mice and resulted in an increased number of fetal resorptions. Increased fetal resorptions were also seen in rabbits at doses of 14,000 times the systemic exposure following the maximum recommended human ophthalmic dose in this case without apparent maternotoxicity. There are no adequate and well-controlled studies in pregnant women. Betimol® (timolol ophthalmic solution) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Nursing mothers Because of the potential for serious adverse reactions in nursing infants from timolol, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother. Pediatric use Safety and efficacy in pediatric patients have not been established. Last reviewed on RxList: 3/26/2009
This monograph has been modified to include the generic and brand name in many instances.

Source: http://www.rxlist.com

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