bisoprolol fumarate


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Related to bisoprolol fumarate: Beta blockers

bisoprolol fumarate

Apo-Bisoprolol, Bisoprolol (CA), Cardicor (UK), Emcor (UK), Emcor LS (UK), Monocor (CA), Novo-Bisoprolol (CA), PMS-Bisoprolol (CA), Sandoz Bisoprolol (CA), Zebeta

Pharmacologic class: Beta1-adrenergic blocker

Therapeutic class: Antihypertensive

Pregnancy risk category C

Action

Blocks beta1-adrenergic receptors of sympathetic nervous system in heart and kidney, thereby decreasing myocardial excitability, myocardial oxygen consumption, cardiac output, and renin release from kidney. Also lowers blood pressure without affecting beta2-adrenergic (pulmonary, vascular, and uterine) receptor sites.

Availability

Tablets: 5 mg, 10 mg

Indications and dosages

Hypertension

Adults: Initially, 2.5 to 5 mg P.O. daily. Dosages up to 20 mg P.O. daily have been used.

Dosage adjustment

• Renal or hepatic impairment

Contraindications

• Hypersensitivity to drug

• Sinus bradycardia

• Second- or third-degree heart block

• Cardiogenic shock

• Heart failure

• Children (safety and efficacy not established)

Precautions

Use cautiously in:

• renal or hepatic impairment, pulmonary disease, asthma, diabetes mellitus, thyrotoxicosis, peripheral vascular disease

• patients undergoing anesthesia or major surgery

• elderly patients

• pregnant or breastfeeding patients.

Administration

• Give with or without food, but be consistent to minimize variations in absorption.

• Be aware that drug may be given alone or added to diuretic therapy.

Adverse reactions

CNS: dizziness, depression, paresthesia, sleep disturbances, hallucinations, memory loss, slurred speech

CV: bradycardia, peripheral vascular insufficiency, claudication, hypotension, sinoatrial or atrioventricular (AV) node block, second- or third-degree heart block, heart failure, pulmonary edema, cerebrovascular accident, arrhythmias

EENT: blurred vision, dry eyes, conjunctivitis, tinnitus, rhinitis, pharyngitis

GI: nausea, vomiting, diarrhea, constipation, gastric pain, gastritis, flatulence, anorexia, ischemic colitis, acute pancreatitis, renal and mesenteric arterial thrombosis

GU: dysuria, polyuria, nocturia, erectile dysfunction, Peyronie's disease, decreased libido

Hematologic: eosinophilia, agranulocytosis, thrombocytopenia

Hepatic: hepatomegaly

Metabolic: hyperglycemia, hypoglycemia

Musculoskeletal: arthralgia, muscle cramps

Respiratory: dyspnea, cough, bronchial obstruction, bronchospasm

Skin: rash, purpura, pruritus, dry skin, excessive sweating

Interactions

Drug-drug. Amphetamines, ephedrine, epinephrine, norepinephrine, phenylephrine, pseudoephedrine: unopposed alpha-adrenergic stimulation

Antihypertensives: increased hypotension

Digoxin: additive bradycardia

Dobutamine, dopamine: decrease in beneficial beta1-adrenergic cardiovascular effects

General anesthetics, I.V. phenytoin, verapamil: additive myocardial depression

MAO inhibitors: hypertension (when taken within 14 days of bisoprolol)

Nonsteroidal anti-inflammatory drugs: decreased antihypertensive effect

Thyroid preparations: decreased bisoprolol efficacy

Drug-diagnostic tests. Alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, blood urea nitrogen, glucose, low-density lipoproteins,

potassium, uric acid: increased levels

Antinuclear antibodies: increased titers

Insulin tolerance test: test interference

Drug-behaviors. Acute alcohol ingestion: additive hypotension

Cocaine use: unopposed alpha-adrenergic stimulation

Patient monitoring

• Closely monitor blood glucose levels in diabetic patients.

• Assess for signs and symptoms of heart failure, including weight gain.

• Stay alert for blood pressure variations. Low blood pressure may indicate overdose.

Patient teaching

• Tell patient to weigh himself daily at same time and to report gain of 3 to 4 lb/day.

• Instruct patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from blood pressure decrease.

• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.

• Advise patient to restrict salt intake to help avoid fluid retention.

• Caution patient not to discontinue drug abruptly unless prescriber approves.

• Tell patient to carry medical identification stating that he's taking a beta blocker.

• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and behaviors mentioned above.

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References in periodicals archive ?
Saruta, "Comparison of efficacy and safety between bisoprolol transdermal patch (TY-0201) and bisoprolol fumarate oral formulation in Japanese patients with grade I or II essential hypertension: randomized, double-blind, placebo-controlled study," The Journal of Clinical Hypertension, vol.
A standard solution containing 0.005 mg/mL bisoprolol fumarate was prepared in a mixture of water and acetonitrile at the ratio 80% : 20% (v/v) and test solution containing 1 mg/mL bisoprolol fumarate.
Binary mixtures of bisoprolol fumarate with various excipients were placed on a quartz Petri dish and directly exposed to 40[degrees]C/75% RH, for 2, 4, and 8 weeks.
A film-coated tablets binary mixture as a formulation mass ratio of bisoprolol fumarate and calcium hydrogen phosphate anhydrous was placed on an open quartz Petri dish and kept at 80[degrees]C for 5 hours, for 5 days.
A binary mixture as equal mass ratio of bisoprolol fumarate and calcium hydrogen phosphate anhydrous was placed in an open quartz Petri dish and kept at 80[degrees]C for 72 hours.
After 8 weeks, the obtained results showed that the only increase of the amount of RRT 0.95 was found in the binary mixture of bisoprolol fumarate and calcium hydrogen phosphate, up to 0.08% (Table 1).
Tukey's multiple comparison test suggested that there was a significant difference in steady flux, cumulative permeation rate and ER at different polysorbate 80 concentrations Thus Bisoprolol fumarate transdermal patch may give a better flux rate with 35% polysorbate 80 through model skin.
Bisoprolol fumarate, permeation enhancer, polysorbate 80, rabbit's skin, transdermal patch.
Bisoprolol fumarate (donated by Mass Pharma, Lahore, Pakistan), Eudragit RS100 (Merck, Germany), Hydroxypropyl methylcellulose E5 (Merck, Germany), Polyethylene glycol 400 (Merck, Germany), Polysorbate 80 (Daejung, Korea), Polyvinyl alcohol (Merck, Germany), Sodium chloride (Merck, Germany), Potassium chloride (Aldrich Chemical Co Ltd.), Potassium dihydrogen phosphate (Fluka, Germany), Disodium hydrogen phosphate (Fluka, Germany), Sodium hydroxide (Riedel-de Haen), Silica beads (Uni-chem), Calcium chloride (Uni-chem), Methanol (BDH, England), Hydrochloric acid (BDH, England).
Table II.-Weight variation, thickness, drug content, swelling index and percentage weight increased due to swelling results of matrix type transdermal patch of Bisoprolol fumarate.
Table III.-Moisture content, percentage moisture uptake at 84% RH, water vapor transmission rate and water vapor permeability results of matrix type transdermal patch of Bisoprolol fumarate.