Bisoprolol

What is Bisoprolol?

• Bisoprolol (Zebeta) is a synthetic, beta1-selective (cardioselective) adrenoceptor blocking agent used in the treatment of hypertension.

Bisoprolol

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Bisoprolol ball-and-stick

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Bisoprolol structure

What are the uses of this medicine?

• Bisoprolol (Zebeta) is indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents.
• 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. In addition to taking medication, making lifestyle changes will also help to control your blood pressure.

How does this medicine work?

• Bisoprolol (bis" oh proe' lol) is considered a “selective” beta-adrenergic receptor blocker in that it has potent activity against beta-1 adrenergic receptors which are found in cardiac muscle, but has little or no activity against beta-2 adrenergic receptors found on bronchial and vascular smooth muscle.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• cardiogenic shock
• overt cardiac failure
• second or third degree AV block
• marked sinus bradycardia

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Be sure to mention the following:

• calcium channel blockers such as diltiazem (Cardizem, Cartia XT, Dilacor XR, Tiazac, others) and verapamil (Calan, Covera-HS, Verelan, in Tarka)
• clonidine (Catapres, Kapvay, in Clorpres)
• medications for irregular heartbeat such as disopyramide (Norpace)
• other beta blockers reserpine; and rifampin (Rifadin, Rimactane, in Rifamate, in Rifater)

Is this medicine FDA approved?

• Bisoprolol was approved for use in the United States in 1992 and is currently widely used in the therapy of hypertension alone or in combination with other agents.
• At present, more than 4 million prescriptions for bisoprolol are filled yearly.

How should this medicine be used?

Recommended dosage:

• The usual starting dose is 5 mg once daily. In some patients, 2.5 mg may be an appropriate starting dose.
• If the antihypertensive effect of 5 mg is inadequate, the dose may be increased to 10 mg and then, if necessary, to 20 mg once daily.

Patients with Renal or Hepatic Impairment:

• In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance less than 40 mL/min), the initial daily dose should be 2.5 mg and caution should be used in dose-titration.

Geriatric Patients: It is not necessary to adjust the dose in the elderly, unless there is also significant renal or hepatic dysfunction.

Administration:

• Bisoprolol comes as a tablet to take by mouth.
• It is usually taken once a day.
• To help you remember to take bisoprolol, take it around the same time every day.
• Your doctor will probably start you on a low dose of bisoprolol and gradually increase your dose.
• Bisoprolol controls high blood pressure but does not cure it.
• It may take a few weeks before you feel the full benefit of bisoprolol.
• Continue to take bisoprolol even if you feel well.
• Do not stop taking bisoprolol without talking to your doctor.
• Suddenly stopping bisoprolol may cause angina, heart attack, or irregular heartbeat.
• Your doctor will probably decrease your dose gradually.

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

This medicine is available in fallowing doasage form:

• As 5 and 10 mg tablets for oral administration

This medicine is available in fallowing brand namesː

• Zebeta

What side effects can this medication cause?

The most common side effects of this medicine include:

• increased sweating
• arthralgia
• dizziness
• headache
• hypoesthesia
• dry mouth
• bradycardia
• vivid dreams
• insomnia
• depression
• diarrhea
• nausea
• vomiting
• bronchospasm
• cough
• dyspnea
• pharyngitis
• rhinitis
• sinusitis
• URI
• asthenia
• chest pain
• fatigue
• edema (peripheral)

What special precautions should I follow?

• Beta-blocking agents should be avoided in patients with overt congestive failure. However, in some patients with compensated cardiac failure it may be necessary to utilize them. In such a situation, they must be used cautiously.
• Exacerbation of angina pectoris, and, in some instances, myocardial infarction or ventricular arrhythmia, have been observed in patients with coronary artery disease following abrupt cessation of therapy with beta-blockers. If withdrawal symptoms occur, BISOPROLOL FUMARATE therapy should be reinstituted, at least temporarily.
• BISOPROLOL FUMARATE may be used with caution in patients with bronchospastic disease who do not respond to, or who cannot tolerate other antihypertensive treatment.
• Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery.
• Patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned that beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia, and bisoprolol fumarate should be used with caution.
• Beta-adrenergic blockade may mask clinical signs of hyperthyroidism, such as tachycardia. Abrupt withdrawal of beta-blockade may be followed by an exacerbation of the symptoms of hyperthyroidism or may precipitate thyroid storm.
• Patients should know how they react to this medicine before they operate automobiles and machinery or engage in other tasks requiring alertness.
• Remember that alcohol can add to the drowsiness caused by this medication.
• If you are having surgery, including dental surgery, tell the doctor or dentist that you are taking bisoprolol.
• Bisoprolol 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
• hypotension
• congestive heart failure
• bronchospasm
• hypoglycemia

Management of overdosage:

• In general, if overdose occurs, BISOPROLOL FUMARATE therapy should be stopped and supportive and symptomatic treatment should be provided.
• Limited data suggest that bisoprolol fumarate is not dialyzable.

The following general measures should be considered when clinically warranted: Bradycardia:

• Administer IV atropine.
• If the response is inadequate, isoproterenol or another agent with positive chronotropic properties may be given cautiously.
• Under some circumstances, transvenous pacemaker insertion may be necessary.

Hypotension:

• IV fluids and vasopressors should be administered.
• Intravenous glucagon may be useful.

Heart Block (second or third degree):

• Patients should be carefully monitored and treated with isoproterenol infusion or transvenous cardiac pacemaker insertion, as appropriate.

Congestive Heart Failure:

• Initiate conventional therapy (i.e., digitalis, diuretics, inotropic agents, vasodilating agents).

Bronchospasm:

• Administer bronchodilator therapy such as isoproterenol and/or aminophylline.

Hypoglycemia:

• Administer IV glucose.

Can this medicine be used in pregnancy?

• Pregnancy Category C.
• There are no adequate and well-controlled studies in pregnant women.
• BISOPROLOL FUMARATE 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:

• BISOPROLOL FUMARATE

Inactive ingredients:

• ANHYDROUS DIBASIC CALCIUM PHOSPHATE
• CELLULOSE, MICROCRYSTALLINE
• CROSPOVIDONE
• FERRIC OXIDE RED
• FERRIC OXIDE YELLOW
• HYPROMELLOSE
• MAGNESIUM STEARATE
• POLYETHYLENE GLYCOL
• POLYSORBATE 80
• SILICON DIOXIDE
• STARCH, CORN
• TITANIUM DIOXIDE

Who manufactures and distributes this medicine?

Manufactured by:

• UNICHEM LABORATORIES LTD.
• Pilerne Ind. Estate, Pilerne, Bardez,
• Goa , India.

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

• Store at 20° to 25°C (68° to 77°F).
• Protect from moisture.
• Dispense in tight, light-resistant containers.

Antihypertensive agents

• Dailymed label info on Bisoprolol
• FDA Bisoprolol

Bisoprolol Resources
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