Bisoprolol

Bisoprolol (brand names Cardicor, Congescor, Zebeta) is a beta blocker medication which treats high blood pressure (hypertension) and heart failure.[1]

Bisoprolol
Clinical data
Trade namesZebeta, Monocor, others
AHFS/Drugs.comMonograph
MedlinePlusa693024
Pregnancy
category
  • AU: C
Routes of
administration
By mouth
ATC code
Pharmacokinetic data
Bioavailability>90%
Protein binding30%[2]
Metabolism50% liver, CYP2D6, CYP3A4[3]
Elimination half-life10–12 hours[4]
ExcretionKidney, fecal (<2%)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard100.108.941
Chemical and physical data
ChiralityRacemic mixture
  (verify)

This medicine can cause serious allergic reactions that require emergency treatment. Make sure the signs of these reactions are known: read allergic reaction symptoms of drugs. Bisoprolol is also used to prevent chest pain caused by angina. It's also used to treat atrial fibrillation and other conditions that cause an irregular heartbeat.[1]

It works by slowing down the heart rate and making it easier for the heart to pump blood around the body.[1]

Bisoprolol was patented in 1976 and approved for medical use in 1986.[5] It was approved for medical use in the United States in 1992.[6]

Pregnancy category: US:[7] C (Zebeta (bisoprolol fumarate) tablets), AU:[8], UK:[9] 'Bisoprolol can be taken during pregnancy'.

Taking bisoprolol

Most adults aged 18 and over can take bisoprolol. There are some people who cannot take bisoprolol, such as in certain diseases or conditions[1]. Some medicines may affect bisoprolol. For conflics with other conditions and medicines see section: who cannot take bisoprolol.

It is a prescription-only medicine.

People usually take bisoprolol once a day in the morning. It works after about 2 hours to reduce high blood pressure, but it can take 2 to 6 weeks to fully take effect. The very first dose may cause feelings of dizziness, so take it at bedtime. After that, if not feeling dizzy, it's best to take it in the morning.[1]

It's best to stop drinking alcohol when first starting to take bisoprolol, or when the dose increases, until it can be seen how the medicine affects the person taking it. The doctor or a doctor should be told about taking bisoprolol if the person is going to have an anaesthetic.[1] It may need to stopped 48 hours before surgery[1] if taking certain medications like this one.

Who cannot take bisoprolol

Bisoprolol is not suitable for everyone. To make sure it's safe before starting bisoprolol, it should be reported if:[1]

  • there has ever been an allergic reaction to bisoprolol or any other medicine
  • there is hypotension or a slow heart rate
  • there is heart failure that's getting worse, heart disease, or a recent heart attack
  • there is severe blood circulation problems in the limbs (such as Raynaud's), which may make fingers and toes tingle or turn paler than usual or blue (this may be less obvious on brown or black skin)
  • there is metabolic acidosis. This is when there is too much acid in the blood
  • there is a lung disease or severe asthma

As conditions or other problems which may affect the medicine or how it works.

There are some medicines that may affect the way bisoprolol works. Report taking:[1]

There's very little information about taking herbal remedies and supplements with bisoprolol. It's not possible to say whether they are safe to take together. They're not tested in the same way as pharmacy and prescription medicines.[1]

Side effects

Bisoprolol can cause allergic reactions.[1] These are are a serious medical emergency.

Like all medicines, it can cause side effects in some people, but many people have no side effects or only minor ones.[1] Side effects often improve as the body gets used to the medicine.[1]

Common side effects

These common side effects of bisoprolol happen in more than 1 in 100 people. They're usually mild and shortlived. There are some ways to help cope with side effects. They are:[1]

Serious side effects

It happens rarely, but some people have serious side effects when taking bisoprolol. Call a doctor or ambulance now if:[1]

There is shortness of breath with a cough that gets worse with exercise (like walking up stairs). Or if swollen ankles or legs develop, or an irregular heartbeat. These are signs of heart problems.

If the whites of the eyes turn yellow, or skin turns yellow (although this may be less obvious on brown or black skin). These can be signs of liver problems

Dosage, missed doses

The dose needed depends on the condition it is meant to treat.

If a dose of bisoprolol is missed, it should be taken as soon as it is remembered that day. If the dose is not remembered until the next day, skip the missed dose and take the next dose at the usual time.[1]

Setting an alarm to take bisoprolol at the same time every day can help if doses are often missed.

References

  1. "About bisoprolol". nhs.uk. 2022-01-06. Retrieved 2024-05-31.
  2. Bühring KU, Sailer H, Faro HP, Leopold G, Pabst J, Garbe A (1986). "Pharmacokinetics and metabolism of bisoprolol-14C in three animal species and in humans". Journal of Cardiovascular Pharmacology. 8 (Suppl 11): S21–S28. doi:10.1097/00005344-198511001-00004. PMID 2439794. S2CID 38147937.
  3. Horikiri Y, Suzuki T, Mizobe M (March 1998). "Pharmacokinetics and metabolism of bisoprolol enantiomers in humans". Journal of Pharmaceutical Sciences. 87 (3): 289–294. doi:10.1021/js970316d. PMID 9523980.
  4. Leopold G (1986). "Balanced pharmacokinetics and metabolism of bisoprolol". Journal of Cardiovascular Pharmacology. 8 (Suppl 11): S16–S20. doi:10.1097/00005344-198511001-00003. PMID 2439789. S2CID 25731558.
  5. Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495. Archived from the original on 2017-09-08.
  6. "Zebeta (bisoprolol fumarate) tablets label - accessdata.fda.gov" (PDF).
  7. "Bisoprolol (Zebeta) Use During Pregnancy". Drugs.com. Retrieved 2024-05-31.
  8. "Pregnancy, breastfeeding and fertility while taking bisoprolol". nhs.uk. 2022-01-06. Retrieved 2024-05-31.
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