Bisoprolol

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Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Bisoprolol.jpg

[edit] MECHANISM OF ACTION

Bisoprolol is a β1 selective adrenergic antagonist; It competes with sympathomimetic neurotransmitters such as catecholamines for binding at β1 adrenergic receptors in the heart and vascular smooth muscle, inhibiting sympathetic stimulation. This results in a reduction in resting heart rate, cardiac output, and blood pressure.

Bisoprolol has a low lipid solubility and lacks intrinsic sympathomimetic properties or membrane stabilizing activity.

[edit] INDICATIONS

  • Management of hypertension, alone or in combination with other antihypertensive agents. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
  • Angina pectoris

[edit] DOSAGE

  • Hypertension: The dosage must be individualized to the needs of the patient. The usual starting dose is 5 mg once daily in the morning with or without food. 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.
  • Angina pectoris: The usual starting dose is 5 mg once daily. If necessary, the dosage may be increased to 10 mg daily

[edit] CONTRAINDICATIONS

  • Patients in cardiogenic shock or decompensated heart failure requiring the use of IV inotropic therapy.
  • Second- or third-degree AV block
  • Sick sinus syndrome
  • Sinus bradycardia (resting heart rate of 60 beats per minute or less)
  • Hypotension (systolic bloodpressure less than 100 mm Hg)
  • Severe bronchial asthma or related bronchospastic conditions
  • Severe forms of peripheral arterial occlusive disease or severe forms of Raynaud's syndrome.
  • Untreated pheochromocytoma
  • Metabolic acidosis
  • Hypersensitivity to bisoprolol

[edit] WARNINGS AND PRECAUTIONS

  • Cardiac Failure : beta blockade may result in further depression of myocardial contractility and precipitate more severe failure. In general, 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.
  • In Patients Without a History of Cardiac Failure Continued depression of the myocardium with beta-blockers can, in some patients, precipitate cardiac failure. At the first signs or symptoms of heart failure, discontinuation of Bisoprolol should be considered
  • Acute exacerbation of coronary artery disease upon cessation of therapy: Severe exacerbation of angina and the occurrence of myocardial infarction and ventricular arrhythmias have been reported in angina patients following the abrupt discontinuation of therapy with beta blockers. Do not abruptly discontinue.
  • Patients with bronchospastic disease (e.g., chronic bronchitis and emphysema): Avoid β-blockers. However, because of its relative beta1-selectivity, however, Bisoprolol may be used if deemed necessary (patients who do not respond to, or cannot tolerate, other antihypertensive treatment), use with caution and at lowest effective dose.
  • Anesthesia and Major Surgery: If Bisoprolol treatment is to be continued perioperatively, particular care should be taken when anesthetic agents which depress myocardial function, such as ether, cyclopropane, and trichloroethylene, are used.
  • Diabetes and Hypoglycemia: Beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia. Nonselective beta blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels. Because of its beta1-selectivity, this is less likely with bisoprolol. However, patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned about these possibilities and bisoprolol should be used with caution

[edit] INTERACTIONS

  • Concomitant Use of Verapamil or diltiazem type calcium channel blockers: Bradycardia and heart block can occur. Use with care.
  • Hypotensive agents (e.g., reserpine, MAO inhibitors, clonidine) may increase the risk of hypotension and/or severe bradycardia.
  • Disopyramide is a Type I antiarrhythmic drug with potent negative inotropic and chronotropic effects. Disopyramide has been associated with severe bradycardia, asystole and heart failure when administered with beta blockers.
  • Amiodarone is an antiarrhythmic agent with negative chronotropic properties that may be additive to those seen with beta blockers.
  • Both digitalis glycosides and beta blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.
  • Insulin and oral antidiabetic drugs: Intensification of blood sugar lowering effect. Blockade of beta-adrenoreceptors may mask symptoms of hypoglycaemia (for example tachycardia).

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). There are no adequate and well-controlled studies in pregnant women. Bisoprolol should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing Mothers: Small amounts of bisoprolol fumarate (< 2% of the dose) have been detected in the milk of lactating rats. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk caution should be exercised when bisoprolol is administered to nursing women.

[edit] SIDE EFFECTS

Possible adverse effects include: bradycardia, diarrhea, asthenia, fatigue, dizziness, feeling of coldness or numbness in hands or feet, hypotension, nausea and vomiting.

Uncommon adverse effects include bronchospasm in patients with bronchial asthma or a history of obstructive airways disease, muscle weakness, muscle cramps, depression and sleep disorders

[edit] RELATED LINKS

[edit] REFERENCES

Antihypertensives
ACE inhibitors Benazepril (Lotensin)   Captopril (Capoten)   Cilazapril   Delapril   Enalapril (Renitec, Vasotec)   Fosinopril (Monopril)  Lisinopril (Prinivil, Zestril)   Moexipril (Univasc)  Perindopril (Aceon)  Quinapril (Accupril)  Ramipril (Altace, Triatec)   Trandolapril (Mavik)  Zofenopril (Bifril, Zopranol)
Angiotensin II receptor antagonist Azilsartan (Edarbi)   Candesartan (Atacand)   Eprosartan (Teveten)   Irbesartan (Aprovel, Avapro, Karvea)   Losartan (Cozaar)   Olmesartan (Benicar, Olmetec)   Telmisartan (Micadis)   Valsartan (Diovan, Tareg)
Renin inhibitors Aliskiren (Rasilez, Tekturna)
Alpha-1 blockers Doxazosin (Cardura)   Prazosin (Minipress)   Terazosin (Hytrin)
Alpha-2 agonists (centrally acting) Clonidine (Oral route)   Clonidine (Transdermal) (Catapresan)   Guanfacine (Tenex)   Methyldopa (Aldomet)
Calcium channel blockers Dihydropyridines‎ Amlodipine (Norvasc)   Barnidipine (Vasexten)   Felodipine (Plendil)   Isradipine (Dynacirc)   Lacidipine (Lacipil, Motens)   Lercanidipine (Zanidip)   Manidipine   Nicardipine   Nifedipine (Adalat)   Nisoldipine   Nitrendipine
Benzothiazepine‎ Diltiazem (Cardizem, Taztia XT, Tiazac, Tildiem)
Phenylalkylamine‎ Gallopamil   Verapamil (Calan)
Beta blockers Beta1 selective (cardioselective) Acebutolol (Sectral)   Atenolol (Tenormin)   Betaxolol (Kerlon)   Bisoprolol (Concor)   Celiprolol (Cordiax)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Nebivolol (Bystolic, Lobivon, Nebilox)
Nonselective (Beta1 and Beta2 blockers) Oxprenolol (Trasitensin)   Propranolol (Inderal)   Timolol (Blocadren)
Nonselective (Beta1, Beta2 and Alpha1 blockers) Carvedilol (Dilatrend)   Labetalol (Trandate)
Beta blocker with intrinsic sympathomimetic activity (ISA) Acebutolol (Sectral)   Celiprolol (Cordiax)
Lipophilic Beta blockers Propranolol (Inderal)   Metoprolol (Betaloc, Lopressor, Toprol-XL)   Oxprenolol (Trasitensin)
Diuretics Carbonic anhydrase inhibitors Acetazolamide (Diamox)
Loop diuretics Bumetanide   Etacrynic acid   Furosemide (Lasix)   Piretanide   Torasemide (Demadex)
Thiazide diuretics Chlorothiazide (Diuril)   Hydrochlorothiazide (Esidrex)
Thiazide-like diuretics Chlortalidone (Hygroton)   Indapamide (Lozol, Lozide)   Metolazone
Potassium-sparing diuretics Epithelial sodium channel blockers: Amiloride (Midamor)   Triamterene (Dyrenium)
Aldosterone receptor antagonists: Potassium canrenoate   Eplerenone (Inspra)   Spironolactone (Aldactone)
Osmotic diuretics Mannitol
Combination therapy Amiloride/Hydrochlorothiazide (Moduretic)   Spironolactone/Hydrochlorothiazide (Aldactazide)