Bisoprolol Brand Name– Zebeta
What is Bisoprolol
Bisoprolol is an oral beta-adrenergic antagonist. Bisoprolol is cardioselective (beta-1-receptor-specific), has low lipid solubility, and is excreted by renal and non-renal pathways.
Bisoprolol is devoid of partial agonist or membrane stabilizing activity. The pharmacodynamic and pharmacokinetic properties of bisoprolol are similar to those of betaxolol, although betaxolol has a longer elimination half-life.
Bisoprolol has been shown to reduce non-fatal cardiac events in patients with chronic systolic heart failure (CIBIS).
Compared with the placebo group, patients treated with bisoprolol required fewer hospitalizations for cardiac decompensation and had more significant improvements in NYHA functional class.
Patients with nonischemic cardiomyopathy appeared to derive the greatest benefit. In a long-term follow-up study of stable heart failure patients (CIBIS-II), bisoprolol has prolonged survival and reduced the incidence of hospitalization; however, this study did not include Class IV heart failure patients.
Bisoprolol has also been shown to be effective in the management of chronic stable angina.
The 2007 AHA guidelines for the management of hypertension state beta-blockers should not be used as first-line therapy for the treatment of hypertension, as several comparative clinical trials have shown beta blockers to be inferior to ACE inhibitors, angiotensin-receptor blockers, or calcium channel blockers for preventing both stroke and coronary artery disease complications.
These guidelines do, however, recommend the use of beta-blockers for the treatment of hypertension in patients with angina, prior myocardial infarction, or heart failure.
Bisoprolol was originally approved by the FDA in July 1992 for the treatment of hypertension.
A combination product with HCTZ (e.g., ‘Ziac’) was also approved for hypertension March 1993.
Indications
- angina
- atrial fibrillation
- atrial flutter
- heart failure
- hypertension
Side Effects
- acne vulgaris
- alopecia
- angina
- angioedema
- arthralgia
- asthenia
- AV block
- back pain
- bradycardia
- bronchospasm
- chest pain (unspecified)
- cough
- depression
- diabetes mellitus
- diaphoresis
- diarrhea
- dizziness
- dyspnea
- elevated hepatic enzymes
- exfoliative dermatitis
- fatigue
- flushing
- hallucinations
- headache
- heart failure
- hyperglycemia
- hypertension
- hypertriglyceridemia
- hypoesthesia
- hypoglycemia
- impotence (erectile dysfunction)
- insomnia
- libido decrease
- muscle cramps
- musculoskeletal pain
- myalgia
- nausea
- nightmares
- orthostatic hypotension
- palpitations
- peripheral edema
- peripheral vasoconstriction
- pharyngitis
- pruritus
- rash
- rhinitis
- sinus tachycardia
- sinusitis
- skin irritation
- syncope
- tremor
- vasculitis
- vomiting
- wheezing
- withdrawal
- xerostomia
Monitoring Parameters
- blood pressure
- heart rate
- serum creatinine/BUN
Contraindications
- abrupt discontinuation
- acute bronchospasm
- acute heart failure
- asthma
- AV block
- beta-blocker hypersensitivity
- bradycardia
- breast-feeding
- bronchitis
- cardiogenic shock
- cerebrovascular disease
- children
- chronic obstructive pulmonary disease (COPD)
- depression
- diabetes mellitus
- driving or operating machinery
- emphysema
- geriatric
- hepatic disease
- hyperthyroidism
- hypotension
- myasthenia gravis
- peripheral vascular disease
- pheochromocytoma
- pregnancy
- psoriasis
- pulmonary disease
- pulmonary edema
- Raynaud’s phenomenon
- renal disease
- renal failure
- renal impairment
- sick sinus syndrome
- surgery
- thyroid disease
- thyrotoxicosis
- vasospastic angina
- ventricular dysfunction
Interactions
- Acetaminophen; Aspirin, ASA; Caffeine
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