Source: Web Search Revision Year: 2011
Kerlone 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 Kerlone 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 Kerlone does not produce the desired response, the addition of a diuretic agent or other antihypertensive should be considered (see, Drug interactions).
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 Kerlone 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 do not have significantly altered clearance. Dosage adjustments are not routinely needed.
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.
If withdrawal of Kerlone 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.
No specific information on emergency treatment of overdosage with Kerlone 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 LD50s are 350 to 400 mg betaxolol/kg in mice and 860 to 980 mg/kg in rats.
In the case of overdosage, treatment with Kerlone 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: Anesthesia and 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 β2-agonist. Additional therapy with aminophylline may be considered.
Heart block (2nd- or 3rd-degree): Use isoproterenol or a transvenous cardiac pacemaker.
Store at controlled room temperature 15°-25°C (59°-77°F).
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