Zebeta


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.

bisoprolol

(bis-oh-proe-lol) bisoprolol,

Zebeta

(trade name)

Classification

Therapeutic: antihypertensives
Pharmacologic: beta blockers
Pregnancy Category: C

Indications

Management of hypertension.

Action

Blocks stimulation of beta1(myocardial)-adrenergic receptors. Does not usually affect beta2(pulmonary, vascular, uterine)-receptor sites.

Therapeutic effects

Decreased BP and heart rate.

Pharmacokinetics

Absorption: Well absorbed after oral administration, but 20% undergoes first-pass hepatic metabolism.Distribution: Unknown.Metabolism and Excretion: 50% excreted unchanged by the kidneys; remainder renally excreted as metabolites; 2% excreted in feces.Half-life: 9–12 hr.

Time/action profile (antihypertensive effect)

ROUTEONSETPEAKDURATION
POunknown 1–4 hr24 hr

Contraindications/Precautions

Contraindicated in: Uncompensated HF;Pulmonary edema;Cardiogenic shock;Bradycardia or heart block.Use Cautiously in: Renal impairment (dosage ↓ recommended);Hepatic impairment (dosage ↓ recommended);Pulmonary disease (including asthma; beta1 selectivity may be lost at higher doses); avoid use if possible;Diabetes mellitus (may mask signs of hypoglycemia);Thyrotoxicosis (may mask symptoms);Patients with a history of severe allergic reactions (intensity of reactions may be ↑); Obstetric / Lactation / Pediatric: Safety not established; crosses the placenta and may cause fetal/neonatal bradycardia, hypotension, hypoglycemia, or respiratory depression; Geriatric: ↑ sensitivity to beta blockers; initial dosage ↓ recommended.

Adverse Reactions/Side Effects

Central nervous system

  • fatigue (most frequent)
  • weakness (most frequent)
  • anxiety
  • depression
  • dizziness
  • drowsiness
  • insomnia
  • memory loss
  • mental status changes
  • nervousness
  • nightmares

Ear, Eye, Nose, Throat

  • blurred vision
  • stuffy nose

Respiratory

  • bronchospasm
  • wheezing

Cardiovascular

  • bradycardia (life-threatening)
  • HF (life-threatening)
  • pulmonary edema (life-threatening)
  • hypotension
  • peripheral vasoconstriction

Gastrointestinal

  • constipation
  • diarrhea
  • ↑ liver function tests
  • nausea
  • vomiting

Genitourinary

  • erectile dysfunction (most frequent)
  • ↓ libido
  • urinary frequency

Dermatologic

  • rash

Endocrinologic

  • hyperglycemia
  • hypoglycemia

Musculoskeletal

  • arthralgia
  • back pain
  • joint pain

Miscellaneous

  • drug-induced lupus syndrome

Interactions

Drug-Drug interaction

General anesthetics, IV phenytoin, and verapamil may cause additive myocardial depression.Additive bradycardia may occur with digoxin, diltiazem, verapamil, or clonidine.Additive hypotension may occur with other antihypertensives, acute ingestion of alcohol, or nitrates.Concurrent use with amphetamine, cocaine, ephedrine, epinephrine, norepinephrine, phenylephrine, or pseudoephedrine may result in unopposed alpha-adrenergic stimulation (excessive hypertension, bradycardia).Concurrent thyroid preparation administration may ↓ effectiveness.May alter the effectiveness of insulins or oral hypoglycemic agents (dose adjustments may be necessary).May ↓ the effectiveness of theophylline.May ↓ the beta1-cardiovascular effects of dopamine or dobutamine.Use cautiously within 14 days of MAO inhibitor therapy (may result in hypertension).

Route/Dosage

Oral (Adults) 5 mg once daily, may be ↑ to 10 mg once daily (range 2.5–20 mg/day).

Renal Impairment

Hepatic Impairment

Oral (Adults) CCr <40 mL/min—Initiate therapy with 2.5 mg/day, titrate cautiously.

Availability (generic available)

Tablets: 5 mg, 10 mg In combination with: hydrochlorothiazide (Ziac). See combination drugs.

Nursing implications

Nursing assessment

  • Monitor BP, ECG, and pulse frequently during dosage adjustment period and periodically throughout therapy.
  • Monitor intake and output ratios and daily weights. Assess routinely for signs and symptoms of HF (dyspnea, rales/crackles, weight gain, peripheral edema, jugular venous distention).
  • Monitor frequency of prescription refills to determine adherence.
  • Lab Test Considerations: May cause increased BUN, serum lipoprotein, potassium, triglyceride, and uric acid levels.
    • May cause increased ANA titers.
    • May cause increase in blood glucose levels.

Potential Nursing Diagnoses

Decreased cardiac output (Side Effects)
Noncompliance (Patient/Family Teaching)

Implementation

  • Do not confuse Zebeta with Diabeta or Zetia.
  • Oral: Take apical pulse before administering. If <50 bpm or if arrhythmia occurs, withhold medication and notify physician or other health care professional.
    • May be administered without regard to meals.

Patient/Family Teaching

  • Instruct patient to take medication exactly as directed, at the same time each day, even if feeling well; do not skip or double up on missed doses. If a dose is missed, it should be taken as soon as possible up to 4 hr before next dose. Abrupt withdrawal may precipitate life-threatening arrhythmias, hypertension, or myocardial ischemia.
  • Teach patient and family how to check pulse and BP. Instruct them to check pulse daily and BP biweekly and to report significant changes to health care professional.
  • May cause drowsiness. Caution patients to avoid driving or other activities that require alertness until response to the drug is known.
  • Advise patients to change positions slowly to minimize orthostatic hypotension.
  • Caution patient that this medication may increase sensitivity to cold.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care professional before taking any Rx, OTC, or herbal products, especially cold preparations, concurrently with this medication. Patients on antihypertensive therapy should also avoid excessive amounts of coffee, tea, and cola.
  • Diabetics should closely monitor blood glucose, especially if weakness, malaise, irritability, or fatigue occurs. Medication does not block dizziness or sweating as signs of hypoglycemia.
  • Advise patient to notify health care professional if slow pulse, difficulty breathing, wheezing, cold hands and feet, dizziness, light-headedness, confusion, depression, rash, fever, sore throat, unusual bleeding, or bruising occurs.
  • Instruct patient to inform health care professional of medication regimen before treatment or surgery.
  • Advise patient to carry identification describing disease process and medication regimen at all times.
  • Hypertension: Reinforce the need to continue additional therapies for hypertension (weight loss, sodium restriction, stress reduction, regular exercise, moderation of alcohol consumption, and smoking cessation). Medication controls but does not cure hypertension.

Evaluation/Desired Outcomes

  • Decrease in BP.

Zebeta

(zə-bā′tə) A trademark for the drug bisoprolol fumarate.

bisoprolol

A selective beta-1-blocker used to manage hypertension and cardiac ischaemia, blocking the G protein and cAMP-signalling cascade, reducing cardiac contractility and heart rate.
Adverse effects
Fatigue, hypotension, hypoglycaemia, bronchospasm, bradycardia.