BETAXOLOL HYDROCHLORIDE

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Overview

What is BETAXOLOL HYDROCHLORIDE?

Betaxolol hydrochloride is a ß-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, carnauba wax, 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 CHNO•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.

What does BETAXOLOL HYDROCHLORIDE look like?

What are the available doses of BETAXOLOL HYDROCHLORIDE?

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What should I talk to my health care provider before I take BETAXOLOL HYDROCHLORIDE?

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How should I use BETAXOLOL HYDROCHLORIDE?

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.

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 ).

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.

What interacts with BETAXOLOL HYDROCHLORIDE?

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What are the warnings of BETAXOLOL HYDROCHLORIDE?

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What are the precautions of BETAXOLOL HYDROCHLORIDE?

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What are the side effects of BETAXOLOL HYDROCHLORIDE?

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What should I look out for while using BETAXOLOL HYDROCHLORIDE?

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 ).

Cardiac Failure:

In Patients Without a History of Cardiac Failure:

Exacerbation of Angina Pectoris Upon Withdrawal:

Bronchospastic diseases: PATIENTS WITH BRONCHOSPASTIC DISEASE SHOULD NOT IN GENERAL RECEIVE BETA-BLOCKERS. Because of its relative ß selectivity (cardioselectivity), low doses of betaxolol tablets, USP may be used with caution in patients with bronchospastic disease who do not respond to or cannot tolerate alternative treatment. Since ß selectivity is not absolute and is inversely related to dose, the lowest possible dose of betaxolol tablets, USP should be used (5 to 10 mg once daily) and a bronchodilator should be made available. If dosage must be increased, divided dosage should be considered to avoid the higher peak blood levels associated with once-daily dosing.

What might happen if I take too much BETAXOLOL HYDROCHLORIDE?

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 LDs 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:

Bradycardia:

Acute cardiac failure:

Bronchospasm:

Heart block (2nd- or 3rd-degree):

How should I store and handle BETAXOLOL HYDROCHLORIDE?

Store at 20° to 25°C (68° to 77°F); see USP controlled room temperature. Protect from light. Do not freeze.Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702Betaxolol Tablets, USP are available as follows:Betaxolol Tablets, USP 10 mg: Bottles of 100, NDC 10702-013-01Betaxolol Tablets, USP 20 mg: Bottles of 100, NDC 10702-014-01StoreDispense Manufactured by:KVK-TECH, INC.110 Terry DriveNewtown, PA 18940ID # 006037/08 12/17Manufacturer’s Code: 10702

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Clinical Information

Chemical Structure

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Clinical Pharmacology

Betaxolol is a ß-selective (cardioselective) adrenergic receptor blocking agent that has weak membrane-stabilizing activity and no intrinsic sympathomimetic (partial agonist) activity. The preferential effect on ß receptors is not absolute, however, and some inhibitory effects on ß receptors (found chiefly in the bronchial and vascular musculature) can be expected at higher doses.

Pharmacokinetics and Metabolism:

Betaxolol is approximately 50% bound to plasma proteins. It is eliminated primarily by liver metabolism and secondarily by renal excretion. Following oral administration, greater than 80% of a dose is recovered in the urine as betaxolol and its metabolites. Approximately 15% of the dose administered is excreted as unchanged drug, the remainder being metabolites whose contribution to the clinical effect is negligible.

Steady state studies in normal volunteers and hypertensive patients found no important differences in kinetics. In patients with hepatic disease, elimination half-life was prolonged by about 33%, but clearance was unchanged, leading to little change in AUC. Dosage reductions have not routinely been necessary in these patients. In patients with chronic renal failure undergoing dialysis, mean elimination half-life was approximately doubled, as was AUC, indicating the need for a lower initial dosage (5 mg) in these patients. The clearance of betaxolol by hemodialysis was 0.015 L/h/kg and by peritoneal dialysis, 0.010 L/h/kg. In one study (n=8), patients with stable renal failure, not on dialysis, with mean creatinine clearance of 27 ml/min showed slight increases in elimination half-life and AUC, but no change in C. In a second study of 30 hypertensive patients with mild to severe renal impairment, there was a reduction in clearance of betaxolol with increasing degrees of renal insufficiency. Inulin clearance (mL/min/1.73 m) ranged from 70 to 107 in 7 patients with mild impairment, 41 to 69 in 14 patients with moderate impairment, and 8 to 37 in 9 patients with severe impairment. Clearance following oral dosing was reduced significantly in patients with moderate and severe renal impairment (26% and 35%, respectively) when compared with those with mildly impaired renal function. In the severely impaired group, the mean C and the mean elimination half-life tended to increase (28% and 24%, respectively) when compared with the mildly impaired group. A starting dose of 5 mg is recommended in patients with severe renal impairment. (See .)

Studies in elderly patients (n=10) gave inconsistent results but suggest some impairment of elimination, with one small study (n=4) finding a mean half-life of 30 hours. A starting dose of 5 mg is suggested in older patients.

Pharmacodynamics:

The ß-selectivity of betaxolol in man was shown in three ways: (1) In normal subjects, 10 and 40 mg oral doses of betaxolol tablets, USP, which reduced resting heart rate at least as much as 40 mg of propranolol, produced less inhibition of isoproterenol-induced increases in forearm blood flow and finger tremor than propranolol. In this study, 10 mg of betaxolol tablets, USP was at least comparable to 50 mg of atenolol. Both doses of betaxolol tablets, USP, and the one dose of atenolol, however, had more effect on the isoproterenol-induced changes than placebo (indicating some ß effect at clinical doses) and the higher dose of betaxolol tablets, USP was more inhibitory than the lower. (2) In normal subjects, single intravenous doses of betaxolol and propranolol, which produced equal effects on exercise-induced tachycardia, had differing effects on insulin-induced hypoglycemia, with propranolol, but not betaxolol, prolonging the hypoglycemia compared with placebo. Neither drug affected the maximum extent of the hypoglycemic response. (3) In a single-blind crossover study in asthmatics (n=10), intravenous infusion over 30 minutes of low doses of betaxolol (1.5 mg) and propranolol (2 mg) had similar effects on resting heart rate but had differing effects on FEV and forced vital capacity, with propranolol causing statistically significant (10% to 20%) reductions from baseline in mean values for both parameters while betaxolol had no effect on mean values. While blood levels were not measured, the dose of betaxolol used in this study would be expected to produce blood concentrations, at the time of the pulmonary function studies, considerably lower than those achieved during antihypertensive therapy with recommended doses of betaxolol. In a randomized double-blind, placebo-controlled crossover (4X4 Latin Square) study in 10 asthmatics, betaxolol (about 5 or 10 mg IV) had little effect on isoproterenol-induced increases in FEV; in contrast, propranolol (about 7 mg IV) inhibited the response.

Consistent with the negative chronotropic effect, due to beta-blockade of the SA node, and lack of intrinsic sympathomimetic activity, betaxolol increases sinus cycle length and sinus node recovery time. Conduction in the AV node is also prolonged.

Significant reductions in blood pressure and heart rate were observed 24 hours after dosing in double-blind, placebo-controlled trials with doses of 5 to 40 mg administered once daily. The antihypertensive response to betaxolol tablets, USP was similar at peak blood levels (3 to 4 hours) and at trough (24 hours). In a large randomized, parallel dose-response study of 5, 10, and 20 mg, the antihypertensive effects of the 5 mg dose were roughly half of the effects of the 20 mg dose (after adjustment for placebo effects) and the 10 mg dose gave more than 80% of the antihypertensive response to the 20 mg dose. The effect of increasing the dose from 10 mg to 20 mg was thus small. In this study, while the antihypertensive response to betaxolol tablets, USP showed a dose-response relationship, the heart rate response (reduction in HR) was not dose related. In other trials, there was little evidence of a greater antihypertensive response to 40 mg than to 20 mg. The maximum effect of each dose was achieved within 1 or 2 weeks. In comparative trials against propranolol, atenolol, and chlorthalidone, betaxolol tablets, USP appeared to be at least as effective as the comparative agent.

Betaxolol tablets, USP has been studied in combination with thiazide-type diuretics and the blood pressure effects of the combination appear additive. Betaxolol tablets, USP has also been used concurrently with methyldopa, hydralazine, and prazosin.

The mechanism of the antihypertensive effects of beta-adrenergic receptor blocking agents has not been established. Several possible mechanisms have been proposed, however, including: (1) competitive antagonism established. Several possible mechanisms have been proposed, however, including: (1) competitive antagonism of catecholamines at peripheral (especially cardiac) adrenergic-neuronal sites, leading to decreased cardiac output, (2) a central effect leading to reduced sympathetic outflow to the periphery, and (3) suppression of rennin activity.

The results from long-term studies have not shown any diminution of the antihypertensive effect of betaxolol tablets, USP with prolonged use.

Non-Clinical Toxicology

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 ).

Cardiac Failure:

In Patients Without a History of Cardiac Failure:

Exacerbation of Angina Pectoris Upon Withdrawal:

Bronchospastic diseases: PATIENTS WITH BRONCHOSPASTIC DISEASE SHOULD NOT IN GENERAL RECEIVE BETA-BLOCKERS. Because of its relative ß selectivity (cardioselectivity), low doses of betaxolol tablets, USP may be used with caution in patients with bronchospastic disease who do not respond to or cannot tolerate alternative treatment. Since ß selectivity is not absolute and is inversely related to dose, the lowest possible dose of betaxolol tablets, USP should be used (5 to 10 mg once daily) and a bronchodilator should be made available. If dosage must be increased, divided dosage should be considered to avoid the higher peak blood levels associated with once-daily dosing.

No studies of interactions between tranexamic acid injection and other drugs have been conducted.

General:

Beta-adrenoceptor blockade can cause reduction of intraocular pressure. Since betaxolol hydrochloride is marketed as an ophthalmic solution for treatment of glaucoma, patients should be told that betaxolol tablets, USP may interfere with the glaucoma-screening test. Withdrawal may lead to a return of increased intraocular pressure. Patients receiving beta-adrenergic blocking agent orally and beta-blocking ophthalmic solutions should be observed for potential additive effects either on the intraocular pressure or on the known systemic effects of beta-blockade.

The value of using beta-blockers in psoriatic patients should be carefully weighed since they have been reported to cause an aggravation in psoriasis.

Impaired Hepatic or Renal Function:

Betaxolol tablets, USP is primarily metabolized in the liver to metabolites that are inactive and then excreted by the kidneys; clearance is somewhat reduced in patients with renal failure but little changed in patients with hepatic disease. Dosage reductions have not routinely been necessary when hepatic insufficiency is present (see ) but patients should be observed. Patients with severe renal impairment and those on dialysis require a reduced dose. (See ).

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

).

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:

Body as a whole:

Cardiovascular:

Central and peripheral nervous system:

Gastrointestinal:

Hearing and Vestibular:

Hematologic:

Liver and biliary:

Metabolic and nutritional:

Musculoskeletal:

Psychiatric:

Reproductive disorders:

Respiratory:

Skin:

Special senses:

Urinary system:

Vascular:

Vision:

Potential Adverse Effects:

Central nervous system:

Allergic:

Hematologic:

Gastrointestinal:

Miscellaneous:

The oculomucocutaneous syndrome associated with the beta-blocker practolol has not been reported with betaxolol tablets, USP during investigational use and extensive foreign experience. However, dry eyes have been reported.

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72

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