Bisoprolol: profile and news

Amiodarone Plus Beta-Blocker Prevents ICD Shocks Jan 11, 2006
...of ICD shocks in 412 patients who were randomized to receive amiodarone plus a beta-blocker (either metoprolol, carvedilol, or bisoprolol), sotalol alone, or a ... - Medscape (subscription)

Premature pills Nov 11, 2005
...side-effects. One example involves the drug Bisoprolol, which is used for heart patients having vascular surgery. Researchers announced ... - Times Online,

Warning on halted trials Nov 8, 2005
The paper gave the example of a trial of perioperative treatment with the beta blocker bisoprolol for high-risk patients having vascular surgery. ... - AustralianDoctor.com (subscription),

Best Treatments: Managing Heart Failure Sep 24, 2005
Research has shown that beta blockers like carvedilol, bisoprolol and sustained-release metoprolol lower mortality by 30 percent or more. ... - Newsweek

Benefits of starting CHF treatment with beta-blocker, bisoprolol Sep 5, 2005
Initiating treatment with the selective beta-blocker, bisoprolol, is as effective and well tolerated as beginning treatment with an ACE inhibitor. ... - News-Medical.net,

Flexibility of Heart Failure Drugs Sep 6, 2005
Investigators found the beta-blocker bisoprolol could be used as initial therapy with ACE inhibitors added later in patients at least 65 years old. ... - Ivanhoe

ESC: For Heart Failure Initial Therapy, Beta-Blockers Match ACE ... Sep 5, 2005
In the open-label Cardiac Insufficiency Bisoprolol Study (CIBIS) III study, 1,010 treatment naïve patients with mild to moderate (New York Heart Association ... - MedPage Today,

Study Supports New Sequencing of Heart Failure Drugs Sep 4, 2005
...involving over 1,000 patients found that the reverse order (starting patients with mild- to moderate heart failure on the beta blocker Bisoprolol, then adding ... - HealthCentral.com

Study backs early use of Merck KGaA heart drug Sep 4, 2005
STOCKHOLM, Sept 4 (Reuters) - Starting treatment for heart failure with the drug bisoprolol, sold by Germany's Merck KGaA (MRCG.DE: Quote, Profile, Research ... - Reuters

Changing heart drug sequence Sep 5, 2005
...involving over 1 000 patients found that the reverse order (starting patients with mild- to moderate heart failure on the beta blocker bisoprolol, then adding ... - Health24.com,

Drug names can fool travelers abroad Aug 22, 2005
...standards for drugs and other health products, lists hundreds of confusing sound-alikes, such as the generics bisacodyl, a laxative, and bisoprolol, a blood ... - Baltimore Sun,

New Data on Mylan Bertek's Investigational Beta-Blocker Compound ... May 18, 2005
The beta-1/beta-2 ratio for each beta blocker investigated was: 321 for nebivolol; 103 for bisoprolol; 93 for betaxolol; 69 for celiprolol; 74 for metoprolol ... - Yahoo News

Missing a beat Mar 12, 2005
...daily intake of 40mg furosemide (to reduce fluid retention), 2.5mg lisinopril (an ACE inhibitor which helps dilate the arteries), 5mg bisoprolol (beta-blockers ... - Guardian,

Management of Hypertension in Older Persons Feb 21, 2005
Atenolol (Tenormin), bisoprolol (Zebeta), and metoprolol (Lopressor, Toprol XL) are cardioselective beta blockers with low lipid solubility, and therefore have ... - RedNova.com,

BCBSNC Launches New Prescription Drug Savings Initiative Feb 17, 2005
COMBINATIONS (Drugs to Treat High Blood Pressure) atenolol/chlorthalidone (generic Tenoretic) benazepril/HCTZ (generic Lotensin HCT) bisoprolol/HCTZ (generic ... - PR Newswire (press release)

Other information

Indication
For the management of hypertension and prophylaxis treatment of angina pectoris and heart failure

Pharmacology
Bisoprolol is a competitive, beta(1)-selective (cardioselective) adrenergic antagonist. Bisoprolol is used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and is also used to reduce non-fatal cardiac events in patients with heart failure. Activation of beta(1)-receptors (located mainly in the heart) by epinephrine increases the heart rate and the blood pressure, and the heart consumes more oxygen. Drugs such as Bisoprolol that block these receptors therefore have the reverse effect: they lower the heart rate and blood pressure and hence are used in conditions when the heart itself is deprived of oxygen. They are routinely prescribed in patients with ischemic heart disease. In addition, beta(1)-selective blockers prevent the release of renin, which is a hormone produced by the kidneys which leads to constriction of blood vessels. Bisoprolol is lipophilic and exhibits no intrinsic sympathomimetic activity (ISA) or membrane stabilizing activity.

Mechanism Of Action
Bisoprolol selectively blocks catecholamine stimulation of beta(1)-adrenergic receptors in the heart and vascular smooth muscle. This results in a reduction of heart rate, cardiac output, systolic and diastolic blood pressure, and possibly reflex orthostatic hypotension. Bisoprolol can also competitively block beta(2)-adrenergic responses in the bronchial and vascular smooth muscles, causing bronchospasm.

Drug Category
Sympatholytics; Antihypertensive Agents; Adrenergic beta-Antagonists;

Brand Names/Synonyms
Bisoprolol; Bisoprolol Fumarate; Bisoprolol Fumerate; Bisoprolol Hemifumarate; Bisoprolol [Usan:Ban:Inn]; Bisoprolol, Hemifumarate; Bisoprolol/Hydrochlorothiazide; Bisoprololum [Latin]; CHEMBANK1848; Concor; Detensiel; EMD 33 512; Emconcor; Emcor; Euradal; Isoten; Monocor; Soprol; Zebeta; Ziac

Dosage Forms
TABLET

Absorption
80%, not affected by the presence of food

Interactions
Interactions for Bisoprolol:

ZEBETA should not be combined with other beta-blocking agents. Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be closely monitored, because the added beta-adrenergic blocking action of ZEBETA may produce excessive reduction of sympathetic activity. In patients receiving concurrent therapy with clonidine, if therapy is to be discontinued, it is suggested that ZEBETA be discontinued for several days before the withdrawal of clonidine.

ZEBETA should be used with care when myocardial depressants or inhibitors of AV conduction, such as certain calcium antagonists (particularly of the phenylalkylamine [verapamil] and benzothiazepine [diltiazem] classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.

Concurrent use of rifampin increases the metabolic clearance of ZEBETA, resulting in a shortened elimination half-life of ZEBETA. However, initial dose modification is generally not necessary. Pharmacokinetic studies document no clinically relevant interactions with other agents given concomitantly, including thiazide diuretics, digoxin, and cimetidine. There was no effect of ZEBETA on prothrombin time in patients on stable doses of warfarin.

Risk of Anaphylactic Reaction: While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reactions.

Chemical IUPAC Name
1-[4-[2-(1-methylethoxy)ethoxymethyl]phenoxy]-3-(1-methylethylamino)propan-2-ol

Chemical Formula
C18H31NO4

Half Life
9-12 hours

Drug Type
Approved Drug

# Accession No
APRD00257

CAS Registry Number
66722-44-9