Betaxolol

What is Betaxolol?

• Betaxolol (Kerlone) is a β1-selective (cardioselective) adrenergic receptor blocking agent used in the treatment of hypertension.
• Ophthalmic betaxolol (Betoptic; Betoptic S) is used to treat glaucoma.

Betaxolol structure

Betaxolol ball-and-stick

What are the uses of this medicine?

• Betaxolol (Kerlone) is used in the management of hypertension. It may be used alone or concomitantly with other antihypertensive agents, particularly thiazide-type diuretics.
• High blood pressure is a common condition and when not treated, can cause damage to the brain, heart, blood vessels, kidneys and other parts of the body.
• Damage to these organs may cause heart disease, a heart attack, heart failure, stroke, kidney failure, loss of vision, and other problems.

How does this medicine work?

• Betaxolol is a β1-selective (cardioselective) adrenergic receptor blocking agent that has weak membrane-stabilizing activity and no intrinsic sympathomimetic (partial agonist) activity.
• The preferential effect on β1 receptors is not absolute, however, and some inhibitory effects on β2 receptors (found chiefly in the bronchial and vascular musculature) can be expected at higher doses.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• known hypersensitivity to the drug.
• sinus bradycardia
• heart block greater than first degree
• cardiogenic shock
• overt cardiac failure

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• amiodarone (Cordarone, Pacerone)
• beta blocker eye drops such as betaxolol (Betoptic), carteolol (Ocupress), levobunolol (Akbeta, Betagan), metipranolol (Optipranolol), and timolol (Betimol, Timoptic, in Cosopt)
• calcium channel blockers such as diltiazem (Cardizem, Dilacor, Tiazac, others), nifedipine (Adalat, Procardia), and verapamil (Calan, Verelan, Tarka, others)
• clonidine (Catapres, Kapvay, in Clorpres)
• digoxin ( Lanoxin)
• disopyramide (Norpace)
• epinephrine (Epipen)
• reserpine

Is this medicine FDA approved?

• Betaxolol was approved for use in the United States in 1985 and is currently used mostly in the therapy of hypertension in combination with other agents.

How should this medicine be used?

Recommended dosage:

• The initial dose of betaxolol 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.

Patients with renal failure:

• In patients with severe renal impairment and those undergoing dialysis the initial dose of betaxolol 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.

Administration:

• Betaxolol comes as a tablet to take by mouth.
• It is usually taken once a day.
• Take betaxolol at around the same time every day.
• Your doctor will probably start you on an average dose of betaxolol and may increase your dose after 7-14 days if your blood pressure is not controlled.
• Betaxolol controls high blood pressure but does not cure it.
• It may take 1-2 weeks or longer before the full benefit of betaxolol is noted.
• Continue to take betaxolol even if you feel well.
• Do not stop taking betaxolol without talking to your doctor.
• If you suddenly stop taking betaxolol, your blood pressure may increases and you may develop new or worsening chest pain.
• Your doctor will probably decrease your dose gradually over about 2 weeks and will monitor you carefully during this time.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As 10-mg and 20-mg tablets for oral administration.

This medicine is available in fallowing brand namesː

• Kerlone

What side effects can this medication cause?

The most common side effects of this medicine include:

• Bradycardia
• Symptomatic bradycardia
• Edema
• Headache
• Dizziness
• Fatigue
• Lethargy
• Insomnia
• Nervousness
• Bizarre dreams
• Depression
• Impotence
• Dyspepsia
• Nausea
• Diarrhea
• Chest pain
• Arthralgia
• Skin
• Rash

What special precautions should I follow?

• Patients, especially those with evidence of coronary artery insufficiency, should be warned against interruption or discontinuation of betaxolol therapy without the physician's advice.
• Patients should know how they react to this medicine before they operate automobiles and machinery or engage in other tasks requiring alertness. Do not drive a car or operate machinery until you know how this medication affects you.
• Patients should contact their physician if any difficulty in breathing occurs, and before surgery of any type. This is especially important if you are having surgery, including dental surgery.
• Patients should inform their physicians, ophthalmologists, or dentists that they are taking betaxolol.
• Patients with diabetes should be warned that beta-blockers may mask tachycardia occurring with hypoglycemia.
• Beta-adrenoceptor blockade can cause reduction of intraocular pressure. Withdrawal may lead to a return of increased intraocular pressure. Patients receiving beta-adrenergic blocking agents 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.
• In hypertensive patients who have congestive heart failure controlled by digitalis and diuretics, beta-blockers should be administered cautiously. Both digitalis and beta-adrenergic receptor blocking agents slow AV conduction.
• Continued depression of the myocardium with beta-blocking agents over a period of time can, in some cases, lead to cardiac failure. Therefore at the first sign or symptom of cardiac failure, discontinuation of betaxolol should be considered.
• Abrupt cessation of therapy with certain beta-blocking agents in patients with coronary artery disease has been followed by exacerbations of angina pectoris and, in some cases, myocardial infarction has been reported. Even in the absence of overt angina pectoris, when discontinuation of betaxolol is planned, the patient should be carefully observed and therapy should be reinstituted, at least temporarily, if withdrawal symptoms occur.
• Beta-blockers should be used with caution in diabetic patients. Beta-blockers may mask tachycardia occurring with hypoglycemia.
• Beta-adrenergic blockade may mask certain clinical signs of hyperthyroidism (eg, tachycardia). Abrupt withdrawal of beta-blockade might precipitate a thyroid storm; therefore, patients known or suspected of being thyrotoxic from whom betaxolol is to be withdrawn should be monitored closely.
• Betaxolol should not be given to patients with untreated pheochromocytoma.
• Betaxolol has not been linked to instances of clinically apparent drug induced liver injury.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• bradycardia
• congestive heart failure
• hypotension
• bronchospasm
• hypoglycemia

Management of overdosage:

• In the case of overdosage, treatment with betaxolol should be stopped and the patient carefully observed.
• Hemodialysis or peritoneal dialysis does not remove substantial amounts of the drug.

For 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.

For Bradycardia:

• Atropine should be administered.
• If there is no response to vagal blockade, isoproterenol should be administered cautiously.

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.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• There are no adequate and well-controlled studies in pregnant women.
• Betaxolol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• BETAXOLOL HYDROCHLORIDE

Inactive ingredients (intravenous):

• ANHYDROUS LACTOSE
• CARNAUBA WAX
• MICROCRYSTALLINE CELLULOSE
• POLYETHYLENE GLYCOL, UNSPECIFIED
• POLYSORBATE 80
• STARCH, CORN
• SODIUM STARCH GLYCOLATE TYPE A POTATO
• STEARIC ACID
• TITANIUM DIOXIDE
• HYPROMELLOSE

Who manufactures and distributes this medicine?

Distributed by:

• PuraCap Laboratories, LLC
• DBA Blu Pharmaceuticals
• Franklin, KY USA

What should I know about storage and disposal of this medication?

• Store at 20°–25°C (68°–77°F).

Antihypertensive agents

• Dailymed label info on Betaxolol
• FDA Betaxolol

Betaxolol Resources
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