Clinical use
Bisoprolol is a beta-adrenoceptor blocking drug (beta-blocker).
Many beta-blockers are now available and in general they are all equally effective. There are, however, differences between them which may affect choice in treating particular diseases or individual patients.
Beta-blockers with a relatively short duration of action have to be given two or three times daily. Many of these are, however, available in modified-release formulations so that administration once daily is adequate for hypertension. For angina twice-daily treatment may sometimes be needed even with a modified-release formulation. Some beta-blockers such as atenolol, bisoprolol, carvedilol, celiprolol, and nadolol have an intrinsically longer duration of action and need to be given only once daily.
Cautions
Beta-blockers can precipitate asthma and this effect can be dangerous. Beta-blockers should be avoided in patients with a history of asthma or bronchospasm; if there is no alternative, a cardioselective beta-blocker can be used with extreme caution under specialist supervision. Atenolol, bisoprolol, metoprolol, nebivolol, and (to a lesser extent) acebutolol, have less effect on the beta2 (bronchial) receptors and are, therefore, relatively cardioselective, but they are not cardiospecific. They have a lesser effect on airways resistance but are not free of this side-effect.
Side effects
Beta-blockers are also associated with fatigue, coldness of the extremities (may be less common with those with ISA, see above), and sleep disturbances with nightmares (may be less common with the water-soluble beta-blockers, see above).
Indications
Bisoprolol (Concor, Zebeta, Concore, Monocor can be used to treat cardiovascular diseases such as hypertension, coronary heart disease, arrhythmias, ischemic heart diseases and treatment of myocardial infarction after the acute event. Patients with compensated congestive heart failure may be treated with Bisoprolol as a comedication (usually together with an ACE inhibitor, a diuretic and a digitalis-glycosid, if indicated). In patients with congestive heart failure, it reduces the need for and the consumption of oxygen of the heart muscle. It is very important to start with low doses, as bisoprolol reduces also the muscular power of the heart, which is an undesired effect in congestive heart failure.
The drug is also used to treat other conditions, including dysautonomia, anxiety and hyperthyroidism (over active thyroid gland).
Bisoprolol will give a positive result in doping tests.
Beta-blockers are effective and safe, and thus a good and still recommended choice to control hypertension.
Beta-blockers are a cornerstone in the treatment of coronary artery disease and myocardial ischemia.
Beta-blockers are recommended to protect against perioperative cardiac events.
Beta-blockers now belong to the mainstay of chronic heart failure treatment.
Bisoprolol is used alone or in combination with other medications to treat high blood pressure. Bisoprolol is in a class of medications called beta blockers. It works by relaxing blood vessels and slowing heart rate to improve and decrease blood pressure.
Bisoprolol comes as a tablet to take by mouth. It is usually taken once a day. To help you remember to take bisoprolol, take it around the same time every day. Follow the directions on your prescription label carefully, and ask your doctor or pharmacist to explain any part you do not understand. Take bisoprolol exactly as directed. Do not take more or less of it or take it more often than prescribed by your doctor.
Your doctor will probably start you on a low dose of bisoprolol and gradually increase your dose.
Bisoprolol controls high blood pressure but does not cure it. It may take a few weeks before you feel the full benefit of bisoprolol. Continue to take bisoprolol even if you feel well. Do not stop taking bisoprolol without talking to your doctor. Suddenly stopping bisoprolol may cause angina (chest pain), heart attack, or irregular heartbeat. Your doctor will probably decrease your dose gradually.
Bisoprolol also is used sometimes to treat heart failure. Talk to your doctor about the possible risks of using this medication for your condition.
This medication may be prescribed for other uses; ask your doctor or pharmacist for more information.
Before taking bisoprolol,
• tell your doctor and pharmacist if you are allergic to bisoprolol or any other medications.
• tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking. Be sure to mention any of the following: calcium channel blockers such as diltiazem (Cardizem, Dilacor, Tiazac, others) and verapamil (Calan, Isoptin, Verelan); clonidine (Catapres); guanethidine (Ismelin); medications for irregular heartbeat such as disopyramide (Norpace); other beta blockers; reserpine (Serpalan, Serpasil, Serpatabs); and rifampin (Rifadin, Rimactane). Your doctor may need to change the doses of your medications or monitor you carefully for side effects.
• tell your doctor if you have or have ever had asthma or other lung disease; a slow heart rate; heart failure; heart, liver, or kidney disease; diabetes; severe allergies; circulation problems; or an overactive thyroid gland (hyperthyroidism).
• tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. If you become pregnant while taking bisoprolol, call your doctor.
• if you are having surgery, including dental surgery, tell the doctor or dentist that you are taking bisoprolol.
• you should know that bisoprolol may make you drowsy. Do not drive a car or operate machinery until you know how this medication affects you.
• remember that alcohol can add to the drowsiness caused by this medication.
• you should know that if you have allergic reactions to different substances, your reactions may be worse while you are using bisoprolol, and your allergic reactions may not respond to the usual doses of injectable epinephrine.
• unusual weight gain
• difficulty breathing or swallowing
• dizziness
• fainting
• shakiness
• sweating
• confusion
• blurred vision
• headache
• numbness or tingling of the mouth
• weakness
• extreme tiredness
• sudden hunger
• pale color
Bisoprolol belongs to a class of drugs called beta-adrenergic receptor blocking agents that also includes propranolol (Inderal), atenolol (Tenormin), and timolol (Blocadren). Bisoprolol is used for treating high blood pressure and heart pain (angina). Bisoprolol prevents the neurotransmitters (chemicals that nerves use to communicate with other nerves), norepinephrine and epinephrine (adrenaline), from binding to beta receptors on nerves. By blocking the effect of norepinephrine and epinephrine on the nerves reaching the heart and blood vessels, beta blockers reduce heart rate and the force with which the heart contracts and reduce blood pressure by dilating blood vessels but may constrict air passages by stimulating the muscles that surround the air passages. Angina occurs when the heart's need for oxygen exceeds the supply of oxygen-carrying blood. By slowing heart rate and decreasing the force with which the heart muscle contracts, bisoprolol reduces the work of the heart and the demand of the heart for oxygen. The FDA approved bisoprolol in July 1992.
PREPARATIONS: Tablets: 5 and 10 mg.
STORAGE: Bisoprolol should be stored at room temperature, 59-86 F (15-30 C) in an air-tight container.
PRESCRIBED FOR: Bisoprolol is used alone or with other drugs for treating patients with high blood pressure. It also is used for treating angina and congestive heart failure.
DOSING: The usual adult dose of bisoprolol is 2.5-20 mg once daily.
DRUG INTERACTIONS: Rifampin may increase the metabolism (destruction) of bisoprolol, possibly making bisoprolol less effective. Certain calcium channel blockers, especially verapamil (Calan, Isoptin) and diltiazem (Cardizem, Tiazac), may enhance the effect of bisoprolol on the heart. In some patients, this may cause excessive slowing of the heart rate or reduce the heart's ability to beat. The use of digoxin (Lanoxin) with bisoprolol also may cause an excessive reduction in heart rate.
Nonsteroidal antiinflammatory drugs (NSAIDs) such as ibuprofen (Motrin, Advil) and naproxen (Naprosyn, Anaprox, Aleve), can reduce the blood pressure lowering effects of beta- blockers.
PREGNANCY: There are no adequate studies in pregnant women.
NURSING MOTHERS: It is not known if bisoprolol is secreted in breast milk.
SIDE EFFECTS: Bisoprolol is generally well-tolerated, and side effects are mild and transient. Side effects include abdominal cramps, diarrhea, dizziness, fatigue, depression, headache, nausea, impotence, slow heart rate, low blood pressure, numbness, tingling, cold extremities, sore throat, and shortness of breath or wheezing.
Bisoprolol can aggravate breathing difficulties in patients with asthma, or chronic bronchitis and emphysema that have a component of bronchial spasm. In patients with existing slow heart rates (bradycardias) and heart blocks (defects in the electrical conduction within the heart), bisoprolol can cause dangerously slow heart rates and even shock. Bisoprolol reduces the force of contraction of heart muscle and can aggravate symptoms of heart failure. In patients with coronary artery disease, abruptly stopping bisoprolol can suddenly worsen angina and occasionally cause heart attacks. If it is necessary to discontinue bisoprolol, its dosage can be reduced gradually over one to two weeks. Bisoprolol can mask the early warning symptoms of low blood sugar (hypoglycemia), and should be used with caution in patients receiving treatment for diabetes.
Product | Therapeutic Category | Documentation / Specifications | CAS No. |
|---|---|---|---|
| Anti-viral drug | INN | [ 204255-11-8 ] | |
| Cough and Cold | BP / USP | [ 154-41-6 ] | |
| Cough and Cold | DMF, Cos | [ 20368-45-0 ] | |
| Etafedrine | Cough and Cold | DMF | [ 530-35-8 ] |
| Tramadol | Pain Management | TIP | [ 36282-47-0 ] |
| Methylphenidate | CNS | DMF | [ 113-45-1 ] |
| Morphine HCl | Analgesic | BP / EP | [52-26-6] |
| Morphine sulphate | Narcotic analgesic | BP / EP / USP | [64-31-3] |
| Ephedrine (EPH) | Cough and Cold | USP | [ 50-98-6 ] |
| Pseudoephedrine hydrochloride | Decongestant | INN | [ 90-82-4 ] |
| Codeine base | Analgesic,Antitussive | BP / EP / USP | [76-57-3] |
| Codeine phosphate hemihydrate | Analgesic,Antitussive | BP / EP / USP | [41444-62-6] |
| Zolpidem Tartrate | Hypnotic | BP / EP | [99294-93-6] |
| Product | Therapeutic Category | Specifications | CAS No. |
|---|---|---|---|
| Alcoholism Treatment | BP / EP | [77337-73-6] | |
| Antiosteoporosis | EP | [121268-17-5] | |
| Antidepressant | USP | [50-48-6] | |
| Antineoplastic | PN | [120511-73-1] | |
| Antidepressant | PN | [82248-59-7] | |
| Antiinflammatory | PN | [82101-18-6] | |
| NSAID | USP | [90357-06-5] | |
| Antiinflammatory Steroid | BP / EP | [51333-22-3] | |
| Antidepressant | BP / EP / USP | [31677-93-7] | |
| Antiosteoporosis | BP | [47931-85-1] | |
| Antineoplastic | PN | [154361-50-9] | |
| Antiepileptic | BP | [298-46-4] | |
| Anticancer | BP / EP / USP | [41575-94-4] | |
| Muscle Relaxant | USP | [78-44-4] | |
| Antihypertensive | BP / EP | [72956-09-3] | |
| 3rd Generation Cephalosporin | EP | [64544-07-6] | |
| Anticancer | EP / USP | [15663-27-1] | |
| Antidepressant | USP | [59729-32-7] | |
| Antidepressant | BP / EP | [17321-77-6] | |
| Antiepileptic | EP / USP | [1622-61-3] | |
| Antithrombotic | USP | [135046-48-9] | |
| Androgen Derivative | USP | [17230-88-5] | |
| Antihistaminic | PN | [100643-71-8] | |
| Vasopressin Analogue | EP | [62288-83-9] | |
| Antiepileptic | PN | [76584-70-8] | |
| Cardiovascular | EP / USP | [49745-95-1] | |
| Antialzheimer | PN | [120014-06-4] | |
| Antidepressant | BP / EP | [897-15-4] | |
| Antiparkinsons | PN | [130929-57-6] | |
| Antithrombotic | PN | [188627-80-7] | |
| Antidepressant | PN | [128196-01-0] | |
| Hypnotic | PN | [138729-47-2] | |
| Antialopecia Agent | PN | [98319-26-7] | |
| NSAID | BP / EP / JP | [5104-49-4] | |
| Antiallergic | BP / EP | [80474-14-2] | |
| Antidepressant | BP / EP | [61718-82-9] | |
| Antiepileptic | USP | [92134-98-0 | |
