Bisoprolol: 7 things you should know
Medically reviewed by Carmen Fookes, BPharm. Last updated on Aug 29, 2022.
1. How it works
- Bisoprolol works on specific receptors located in the heart (called beta1 receptors) to slow the heart rate.
- The exact way bisoprolol works to lower blood pressure is not known but studies have shown it decreases cardiac output, inhibits renin release from the kidneys, and reduces the activity of the sympathetic nervous system.
- Bisoprolol belongs to the class of drugs known as beta-blockers. It is called a cardioselective beta-blocker because at low dosages it only works on beta1 receptors in the heart and is unlikely to affect beta2 receptors located in the airways.
- Bisoprolol causes a reduction in heart rate both at rest and during exercise.
- Bisoprolol also lowers blood pressure and is used for the treatment of high blood pressure (hypertension).
- Bisoprolol may be used alone or in addition to other antihypertensives.
- Bisoprolol is cardioselective (mainly works on receptors in the heart) at low dosages. May be preferred for people with co-existing chronic obstructive pulmonary disorder (COPD) because it is less likely than nonselective beta-blockers to cause bronchoconstriction (narrowing of the airways).
- Can be taken once daily.
- Less likely than nonselective beta-blockers to cause fatigue and cold extremities.
- Generic bisoprolol is available.
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- A headache, dizziness, diarrhea, dizziness, rhinitis, and fatigue are the most common side effects reported.
- May also cause a dry mouth, erectile dysfunction, vivid dreams, and insomnia. May increase serum triglycerides in some people.
- Cardioselectivity of bisoprolol is not absolute, and at dosages higher than 20mg/day bisoprolol also inhibits beta2 receptors, mostly located in the bronchial and vascular musculature. The lowest effective dose should be used to maintain cardioselectivity.
- Generally not recommended for people with bronchospastic disease; however, it may be used in certain circumstances because bisoprolol is less likely than nonselective beta-blockers to cause bronchospasm.
- Can mask symptoms of hypoglycemia or hyperthyroidism, so should be used with caution in people with diabetes or thyroid disease.
- May cause a number of unwanted heart-related effects and aggravate peripheral circulatory disorders (conditions that cause reduced blood flow to the hands or feet).
- The clearance of bisoprolol from the body may be delayed in renal or liver disease which means the dosage of bisoprolol should be reduced in people with these conditions.
- May not be suitable for some people including those with heart failure, a significantly slow heartbeat, or reduced peripheral circulation.
- May interact with some medications including other medications used for the treatment of arrhythmias or angina.
- Abrupt stopping may precipitate angina and other unwanted heart effects including myocardial infarction. On discontinuation, bisoprolol should be tapered off slowly over at least a week. Warn people taking bisoprolol not to stop it suddenly. Does not need to be stopped prior to surgery; however, the effects of bisoprolol may impair the heart's ability to respond while under general anesthetic.
- Only give during pregnancy if the benefits outweigh the risks. Formal studies in humans have not been conducted and animal studies at 77 times the maximum recommended human dose have not shown teratogenicity. Small amounts (less than 2%) have been detected in the milk of lactating rats - it is not known whether bisoprolol is excreted into human milk.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Bottom Line
- Bisoprolol works on heart-specific receptors to lower blood pressure and slow heart rate; however, cardioselectivity may be lost if dosages are greater than 20mg/day.
- May be taken with or without food.
- Bisoprolol is taken once a day. Try to take tablets at the same time each day.
- Sudden discontinuation has been associated with an exacerbation of angina, and sometimes myocardial infarction (heart attack) or ventricular arrhythmias. If you need to discontinue bisoprolol, your doctor will advise how to do this slowly over at least a week.
- If you have diabetes, bisoprolol may mask some of the symptoms of hypoglycemia (low blood sugar).
- Should always be used as part of a comprehensive cardiovascular risk reduction program that includes diabetes management, smoking cessation, exercise, and other drug therapies. May be used in addition to other blood pressure-lowering medicines.
- Seek medical advice immediately if shortness of breath develops.
- Seek medical advice if any new numbness, pain, a cold feeling, skin color changes or reduced sensitivity occurs in fingers or toes.
- Talk to your doctor if you are having any side effects that are interfering with your quality of life, including erectile dysfunction. Do not stop taking bisoprolol suddenly.
- Your doctor will need to regularly monitor your blood pressure and possibly other markers. Keep your appointments.
- Bisoprolol may impair your thinking or reaction time and affect your ability to drive. Drinking alcohol may enhance these effects. Do not drive if you think your driving ability is being compromised by bisoprolol.
- Tell your doctor if you are breastfeeding, pregnant, or intending to become pregnant because bisoprolol may not be suitable for you.
6. Response and effectiveness
- Peak concentrations reached between two and four hours after an oral dose. May take up to a week before the full effects on blood pressure and heart rate are seen, although some effect is evident within 24 hours.
- Effects of bisoprolol persist for 24 hours following a single dose. Blood pressure returns to baseline within two weeks of tapering a dose of bisoprolol.
- The absolute bioavailability after 10mg of oral bisoprolol fumarate is about 80%. Absorption is not affected by the presence of food. The first-pass metabolism of bisoprolol fumarate is about 20%. The half-life of bisoprolol is increased three-fold in people with kidney disease and a creatinine clearance of less than 40 mL/min.
Medicines that interact with bisoprolol may either decrease its effect, affect how long it works for, increase side effects, or have less of an effect when taken with bisoprolol. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Common medications that may interact with bisoprolol include:
- diabetes medications, such as insulin
- heart medications, such as atenolol, carvedilol, clonidine, digoxin, diltiazem, disopyramide, labetalol, metoprolol, nadolol, propranolol, sotalol, trandolapril, or verapamil
- respiratory medications, such as albuterol, bitolterol, metaproterenol, pirbuterol, or terbutaline
- other medications such as fingolimod, reserpine, rifampin, or isoniazid.
Note that this list is not all-inclusive and includes only common medications that may interact with bisoprolol. You should refer to the prescribing information for bisoprolol for a complete list of interactions.
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Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use bisoprolol only for the indication prescribed.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
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