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Bisoprolol
drug data and news
Bisoprolol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.
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| Generic name | Bisoprolol | ||
| 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 | ||
| Indication | For the management of hypertension and prophylaxis treatment of angina pectoris and heart failure | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Bisoprolol News (When available) |
Amiodarone Plus Beta-Blocker Prevents ICD Shocks Jan 11, 2006 Premature pills Nov 11, 2005 Warning on halted trials Nov 8, 2005 Best Treatments: Managing Heart Failure Sep 24, 2005 Benefits of starting CHF treatment with beta-blocker, bisoprolol Sep 5, 2005 Flexibility of Heart Failure Drugs Sep 6, 2005 ESC: For Heart Failure Initial Therapy, Beta-Blockers Match ACE ... Sep 5, 2005 Study Supports New Sequencing of Heart Failure Drugs Sep 4, 2005 Study backs early use of Merck KGaA heart drug Sep 4, 2005 Changing heart drug sequence Sep 5, 2005 Drug names can fool travelers abroad Aug 22, 2005 New Data on Mylan Bertek's Investigational Beta-Blocker Compound ... May 18, 2005 Missing a beat Mar 12, 2005 Management of Hypertension in Older Persons Feb 21, 2005 BCBSNC Launches New Prescription Drug Savings Initiative Feb 17, 2005 | ||
| Dosage Forms | TABLET | ||
| Drug_Category | Sympatholytics; Antihypertensive Agents; Adrenergic beta-Antagonists; | ||
| 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. | ||
| Toxicity | Can lead to congestive heart failure | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | 1-[4-[2-(1-methylethoxy)ethoxymethyl]phenoxy]-3-(1-methylethylamino)propan-2-ol | ||
| Chemical Formula | C18H31NO4 | ||
| Molecular Weight | 325.443 g/mol | ||
| Smiles String | CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O | ||
| Melting Point | 100 °C | ||
| Water Solubility | 2240 mg/L | ||
| State | Solid; white crystalline powder | ||
| LogP/Hphobicity | 3.185 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Primarily hepatic (CYP2D6) | ||
| Half Life | 9-12 hours | ||
| Protein Binding [%] | binding to serum proteins is approximately 30% | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Bisoprolol.html http://www.rxlist.com/cgi/generic3/bisoprolol.htm http://www.pharmgkb.org/views/index.jsp?objId= | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00257 | ||
| CAS Registry Number | 66722-44-9 | ||
| KEGG Compound ID | C06852 | ||
| PubChem ID | SID:187179 | ||
| PharmGKB ID | PA448641 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | 2267489 |
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