betaxolol hydrochloride

INDICATIONS AND USAGE: Betaxolol tablets, USP is indicated in the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly thiazide-type diuretics.

DOSAGE AND ADMINISTRATION: The initial dose of betaxolol tablets, USP in hypertension is ordinarily 10 mg once daily either alone or added to diuretic therapy. The full antihypertensive effect is usually seen within 7 to 14 days. If the desired response is not achieved the dose can be doubled after 7 to 14 days. Increasing the dose beyond 20 mg has not been shown to produce a statistically significant additional antihypertensive effect; but the 40-mg dose has been studied and is well tolerated. An increased effect (reduction) on heart rate should be anticipated with increasing dosage. If monotherapy with betaxolol tablets, USP does not produce the desired response, the addition of a diuretic agent or other antihypertensive should be considered (see PRECAUTIONS, Drug Interactions ). Dosage Adjustments For Specific Patients: Patients with renal failure: In patients with renal impairment, clearance of betaxolol declines with decreasing renal function. In patients with severe renal impairment and those undergoing dialysis, the initial dose of betaxolol tablets, USP is 5 mg once daily. If the desired response is not achieved, dosage may be increased by 5 mg/day increments every 2 weeks to a maximum dose of 20 mg/day. Patients with hepatic disease: Patients with hepatic disease do not have significantly altered clearance. Dosage adjustments are not routinely needed. Elderly patients: Consideration should be given to reduction in the starting dose to 5 mg in elderly patients. These patients are especially prone to beta-blocker-induced bradycardia, which appears to be dose related and sometimes responds to reductions in dose. Cessation of therapy: If withdrawal of betaxolol tablets, USP therapy is planned, it should be achieved gradually over a period of about 2 weeks. Patients should be carefully observed and advised to limit physical activity to a minimum.

CONTRAINDICATIONS: Betaxolol tablets, USP is contraindicated in patients with known hypersensitivity to the drug. Betaxolol tablets, USP is contraindicated in patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, and overt cardiac failure (see Warnings ).

ADVERSE REACTIONS: Most adverse reactions have been mild and transient and are typical of beta-adrenergic blocking agents, e.g., bradycardia, fatigue, dyspnea, and lethargy. Withdrawal of therapy in U.S. and European controlled clinical trials has been necessary in about 3.5% of patients, principally because of bradycardia, fatigue, dizziness, headache, and impotence. Frequency estimates of adverse events were derived from controlled studies in which adverse reactions were volunteered and elicited in U.S. studies and volunteered and/or elicited in European studies. In the U.S., the placebo-controlled hypertension studies lasted for 4 weeks, while the active-controlled hypertension studies has a 22- to 24- week double-blind phase. The following doses were studied: Betaxolol tablets, USP-5, 10, 20, and 40 mg once daily; atenolol-25, 50, and 100 mg once daily; and propranolol-40, 80, and 160 mg b.i.d. Betaxolol tablets, USP, like other beta-blockers, has been associated with the development of antinuclear antibodies (ANA) (e.g. lupus erythematosus). In controlled clinical studies, conversion of ANA from negative to positive occurred in 5.3% of the patients treated with betaxolol tablets, USP, 6.3% of the patients treated with atenolol, 4.9% of the patients treated with propranolol, and 3.2% of the patients treated with placebo. Betaxolol adverse events reported with a 2% or greater frequency, and selected events with lower frequency, in U.S. controlled studies are: Of the above adverse reactions associated with the use of betaxolol, only bradycardia was clearly dose related, but there was a suggestion of dose relatedness for fatigue, lethargy, and dyspepsia. In Europe, the placebo-controlled study lasted for 4 weeks, while the comparative studies had a 4- to 52-week double-blind phase. The following doses were studied: Betaxolol 20 and 40 mg once daily and atenolol 100 mg once daily. From European controlled hypertension clinical trials, the following adverse events reported by 2% or more patients and selected events with lower frequency are presented: The only adverse event whose frequency clearly rose with increasing dose was bradycardia. Elderly patients were especially susceptible to bradycardia, which in some cases responded to dose-reduction (see Precautions ). The following selected (potentially important) adverse events have been reported at an incidence of less than 2% in U.S. controlled hypertension and open, long-term clinical studies, European controlled clinical trials, or in marketing experience. It is not known whether a causal relationship exists between betaxolol tablets, USP and these events; they are listed to alert the physician to a possible relationship: Autonomic: flushing, salivation, sweating. Body as a whole: allergy, fever, malaise, pain, rigors. Cardiovascular: angina pectoris, arrhythmia, atrioventricular block, heart failure, hypertension, hypotension, myocardial infarction, thrombosis, syncope. Central and peripheral nervous system: ataxia, neuralgia, neuropathy, numbness, speech disorder, stupor, tremor, twitching. Gastrointestinal: anorexia, constipation, dry mouth, increased appetite, mouth ulceration, rectal disorders, vomiting, dysphagia. Hearing and Vestibular: earache, labyrinth disorders, tinnitus, deafness. Hematologic: anemia, leucocytosis, lymphadenopathy, purpura, thrombocytopenia. Liver and biliary: increased AST, increased ALT. Metabolic and nutritional: acidosis, diabetes, hypercholesterolemia, hyperglycemia, hyperkalemia, hyperlipemia, hyperuricemia, hypokalemia, weight gain, weight loss, thirst, increased LDH. Musculoskeletal: arthropathy, neck pain, muscle cramps, tendonitis. Psychiatric: abnormal thinking, amnesia, impaired concentration, confusion, emotional lability, hallucinations, decreased libido. Reproductive disorders: Female: breast pain, breast fibroadenosis, menstrual disorder; Male: Peyronie’s disease, prostatitis. Respiratory: bronchitis, bronchospasm, cough, epistaxis …

DESCRIPTION: Betaxolol hydrochloride is a ß 1 -selective (cardioselective) adrenergic receptor blocking agent available as 10-mg and 20-mg tablets for oral administration. Betaxolol hydrochloride is chemically described as 2-propanol, 1- [4-[2-(cyclopropylmethoxy) ethyl] phenoxy]-3-[(1-methylethyl) amino]-, hydrochloride, (±)-. It has the following chemical structure: Each tablet for oral administration contains 10 mg or 20 mg of betaxolol hydrochloride equivalent to 8.94 mg or 17.88 mg of betaxolol respectively. In addition, each tablet contains the following inactive ingredients, hypromellose, anhydrous lactose, microcrystalline cellulose, polyethylene glycol, polysorbate 80, pregelatinized starch, sodium starch glycolate, stearic acid and titanium dioxide. Betaxolol hydrochloride is a water-soluble white crystalline powder with a molecular formula of C 18 H 29 NO 3 •HCl and a molecular weight of 343.9. It is freely soluble in water, ethanol, chloroform, and methanol, and has a pKa of 9.4. Chemical Structure

OVERDOSAGE: No specific information on emergency treatment of overdosage with betaxolol tablets, USP is available. The most common effects expected are bradycardia, congestive heart failure, hypotension, bronchospasm, and hypoglycemia. In one acute overdosage of betaxolol, a 16-year-old female recovered fully after ingesting 460 mg. Oral LD 50 s are 350 to 400 mg betaxolol/kg in mice and 860 to 980 mg/kg in rats. In the case of overdosage, treatment with betaxolol tablets, USP should be stopped and the patient carefully observed. Hemodialysis or peritoneal dialysis does not remove substantial amounts of the drug. In addition to gastric lavage, the following therapeutic measures are suggested if warranted: Hypotension: Use sympathomimetic pressor drug therapy, such as dopamine, dobutamine, or norepinephrine. In refractory cases of overdosage of other beta-blockers, the use of glucagon hydrochloride has been reported to be useful. Bradycardia: Atropine should be administered. If there is no response to vagal blockade, isoproterenol should be administered cautiously (see Warnings: Major surgery ). In refractory cases the use of a transvenous cardiac pacemaker may be considered. Acute cardiac failure: Conventional therapy including digitalis, diuretics, and oxygen should be instituted immediately. Bronchospasm: Use a ß 2 - agonist. Additional therapy with aminophylline may be considered. Heart block (2nd- or 3rd-degree): Use isoproterenol or a transvenous cardiac pacemaker.

HOW SUPPLIED: Betaxolol Tablets, USP are available as follows: Betaxolol Tablets, USP 10 mg: (Each tablet contains 10 mg betaxolol HCl equivalent to 8.94 mg betaxolol) are as white, round, film-coated biconvex tablets, debossed "k" above bisect "13" on one side and plain on the other. Bottles of 100, NDC 10702-013-01 Betaxolol Tablets, USP 20 mg: (Each tablet contains 20 mg betaxolol HCl equivalent to 17.88 mg betaxolol) are as white, round, film-coated biconvex tablets, debossed "K" above "14" on one side and plain on the other. Bottles of 100, NDC 10702-014-01 Store at 20° to 25°C (68° to 77°F) with excursions permitted between 15° to 30°C (59° to 86°F) [See USP Controlled Room Temperature]. Dispense in a tight container as defined in the USP, with a child-resistant closure (as required). Manufactured by: KVK-TECH, INC. 110 Terry Drive Newtown, PA 18940 ID # 006037/09 04/2020 Manufacturer’s Code: 10702 KvK logo