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Lexicon
Lexicon

Bisoprolol (Concor)

The standard cardiology beta blocker - outstandingly documented, but the more noticeable brake on training.

3 min read 7 sources

To the sources
Long molecule chain of glossy blue, light blue and white spheres with a six-membered ring in the middle floats above a white podium in a bright lab, symbolic image for bisoprolol
Compound approved · since 1992

Summary

At a glance

Sources checked on 26 Oct 2026

All-cause mortality (CIBIS-II)
−34 %

2,647 people with severe heart failure, 11.8 versus 17.3 percent, stopped early1

Sudden death (CIBIS-II)
−44 %

3.6 versus 6.3 percent with placebo (hazard ratio 0.56)1

Minutes of ischaemia (TIBBS)
−68 %

stable angina, after 4 weeks, about 28 percent less on nifedipine4

Half-life
9 to 12 h

slightly longer in older people, about three times as long with weak kidneys5

  • Bisoprolol is a beta blocker that mainly occupies the beta-1 receptors at the heart. Pulse and blood pressure fall, the heart needs less oxygen.75
  • The preference for the heart is not absolute: at higher doses bisoprolol also blocks beta-2 receptors in the bronchi and vessels.5
  • In CIBIS-II 11.8 instead of 17.3 percent died with severe heart failure, the trial was stopped early. In stable angina minutes of ischaemia fell more than on nifedipine.14
  • The most common complaint against placebo is fatigue. Abrupt stopping can trigger angina and heart rhythm problems, warning signs of low blood sugar are damped.5
  • According to ChEMBL bisoprolol has been approved since 1992. Everything here is the state of research, not a recommendation.7
Profile

Updated July 2026

How long does it stay in the body?

Share left after one dose, calculated with a half-life of ~11 hours

Half-life ~11 hours
After 22 hours: 25 %
Hour 11 · 50 %Hour 22 · 25 %Hour 24, next dose · 22 %Hour 33 · 12.5 %Hour 55 · 3.1 %

Simplified model without an absorption phase, half-life from the TPD lexicon. The lexicon gives 10 to 12 hours, we calculate with the middle.

Class
Beta blocker

beta-1 selective

Use
Oral

once daily in the morning

Half-life
10 to 12 hours
Training effect
Noticeably caps maximum heart rate

cardio more than lifting

Status
Clinically approved

one of the best documented agents there is

Contents 12 sections
  1. At a glance
  2. What is bisoprolol?
  3. How it works
  4. Use and dosing
  5. What the research shows
  6. Research status
  7. Side effects
  8. Storage
  9. Related compounds
  10. FAQ
  11. Glossary
  12. Sources

What is bisoprolol?

Bisoprolol is a beta-1 selective beta blocker. It occupies the beta-1 receptors at the heart and damps the effect of adrenaline and noradrenaline there. Result: slower pulse, weaker contraction, lower oxygen demand of the heart muscle and with it lower blood pressure.

In cardiology it is one of the most thoroughly investigated agents that exists. For anyone training it is the more noticeable brake compared with nebivolol, because it lacks the NO effect that compensates part of the frequency brake there.

This information is for research and educational purposes only. No medical advice.

Comparison

Beta blockers and a different path

Three beta blockers and a calcium channel blocker side by side, as stated in the TPD lexicon. Tap a card to open its entry.

Beta-1 selective Bisoprolol (Concor) Beta-1
Beta-1 selective with NO Nebivolol (Bystolic) Beta-1NO Beta-1 selective, extended release Metoprolol succinate ER (Toprol-XL) Beta-1 Calcium channel blocker Amlodipine (Norvasc) Calcium channel

Simplified: according to the lexicon nebivolol also releases nitric oxide and brakes the pulse less noticeably during training. 7

How it works

Beta-1 selective means bisoprolol occupies the receptors at the heart considerably more than the beta-2 receptors in bronchi, vessels and skeletal muscle. That is why it is better tolerated than the old non-selective agents. However, the selectivity is dose-dependent and decreases as the dose rises.

The effect in heart failure runs through a different route than the blood pressure reduction. A permanently overstimulated heart wears itself out. Blocking the sympathetic drive interrupts that cycle. That is why dosing in heart failure is raised very slowly over weeks: the heart first has to adapt to the reduced stimulation, otherwise the situation worsens short-term.

Where it acts

Where bisoprolol acted in studies

Tap a point or a card. Colour = beta-1 receptor, grey = observed in studies.

  1. Heart

    Blocks beta-1 receptors, pulse and oxygen demand fall7

    Beta-1
  2. Blood pressure

    Blood pressure fell against placebo in the US trials5

    Observed in trials
  3. Bronchi

    At higher doses also beta-2 blockade, caution in asthma5

    Observed in trials
  4. Kidney

    With weak kidneys bisoprolol stays in the blood about three times as long5

    Observed in trials
  5. Blood sugar

    Damps warning signs of low blood sugar such as a racing heart5

    Observed in trials

Targets in the ChEMBL database7

Compound CHEMBL1472989: one recorded mechanism, Antagonist, direct binding.

Beta-1 adrenoceptor
Gene
ADRB1
UniProt
P08588
ChEMBL
CHEMBL213
Action
Antagonist, direct binding
Close-up of translucent, shimmering heart muscle fibres, blue and white molecule chains resting in glowing hollows on the surface
Bisoprolol occupies the beta-1 receptors on the heart muscle. Symbolic image.

Use and dosing

Dosing

Dosing, titration and syringe

Loading the dosing information …

  • Getting started and stepping up, drawn as a staircase
  • Units on the U-100 syringe for every step
  • How long one vial lasts
White folding box with the TPD logo next to a blister of ten round white tablets, two loose tablets in front on a bright lab bench
Tablets in a blister. Symbolic image.

What the research shows

CIBIS-II (Lancet 1999) is the trial everything builds on. Over 2,600 patients with heart failure, randomised to bisoprolol or placebo. The trial was stopped early because the advantage was so clear: 34 percent lower all-cause mortality. Stopping for superiority is rare and a strong signal.

CIBIS (Circulation 1994) was the predecessor. It showed the direction but was too small to prove a mortality effect. CIBIS-III (Circulation 2005) answered a practical question: is it better to start with the beta blocker or with the ACE inhibitor? Result: starting with bisoprolol was not inferior to starting with enalapril, so the order is not decisive.

TIBBS (JACC 1995) compared against nifedipine in stable angina and found considerably fewer ischaemic episodes under bisoprolol.

Study results

What the trials measured

Interactive: switch tabs, tap points, show or hide arms. Arms are named relative to each other, no dosing advice.

Deaths in severe heart failure1

2,647 people, mean 1.3 years, on top of standard therapy

All-cause mortality1
Placebo 17.3%
Bisoprolol 11.8%
Sudden death1
Placebo 6.3%
Bisoprolol 3.6%

The trial was stopped after the second interim analysis. The effect did not depend on the severity or cause of heart failure.

Predecessor trial with 641 people2

Share over a mean of 1.9 years, calculated from the counts in the abstract

Hospital for cardiac decompensation2
Placebo 28.0%
Bisoprolol 19.1%
Deaths2 difference not significant
Placebo 20.9%
Bisoprolol 16.6%

90 versus 61 hospital admissions and 67 versus 53 deaths. CIBIS was too small to prove an effect on mortality, CIBIS-II followed up on that.

Minutes of ischaemia per 48 hours4

330 people with stable angina, Holter ECG before and after 4 weeks

At baseline4
Bisoprolol 99.3 min
Nifedipine (comparator) 101.0 min
After 4 weeks4
Bisoprolol 31.9 min
Nifedipine (comparator) 72.6 min

The number of ischaemic episodes fell from 8.1 to 3.2 on bisoprolol and from 8.3 to 5.9 on nifedipine. Bisoprolol also damped the morning peak.

Death or hospital by starting order3

1,010 people with mild to moderate heart failure, 505 per group

Primary endpoint3
Enalapril first (comparator) 36.8%
Bisoprolol first 35.2%

Calculated from 186 and 178 events. Non-inferior in the intention-to-treat analysis, not proven in the per-protocol analysis.

Row of sealed test tubes with clear liquid, a bright heart symbol glowing in several of them
The large trials measured mortality and hospital admissions. Symbolic image.

Research status

Where the research stands

Bisoprolol has been approved since 1992. On ClinicalTrials.gov 141 trials list bisoprolol among their interventions. The CIBIS trials and TIBBS date from before mandatory registration and are not listed there. Shown is a selection of completed trials with bisoprolol. As of 26 Oct 2026. 6

  1. Preclinical Beta-1 selectivity shown in animal and human studies
  2. Phase 1 no registered trial
  3. Phase 2 no registered trial
  4. Phase 3 2 trials, 2 completed
  5. Approval since 1992
780 participants in phase 3 Approved: ChEMBL lists bisoprolol with phase 4 as the highest phase and first approval in 1992.7
Show all 5 phase 3 and 4 trials on a timelineHide timeline 5 completed 0 running 0 with results
Phase 3
Phase 4

Bar: start to primary endpoint (planned for running trials). Green = completed, blue = progress until 26 Oct 2026.

Side effects

  • Capped maximum heart rate: the mechanism, not a side effect. Cardio performance drops measurably.
  • Fatigue and low drive: the most common subjective report, mostly in the first weeks.
  • Bradycardia: resting heart rate below 50 means the dose comes down.
  • Cold hands and feet: typical for the class.
  • Masked hypoglycaemia: the warning signs are damped. Relevant for diabetics.
  • Rebound on stopping: blood pressure spikes and palpitations are documented. Always taper.

Tolerability

Side effects compared with placebo

Out of 100 participants per group, how many had the event over 4 to 12 weeks.

2 of 100 Placebo
8 of 100 Bisoprolol
Event PlaceboBisoprolol
Fatigue5 2%8%
Diarrhoea5 2%4%
Headache5 11%11%
Slow heart rate5 0%1%

All study doses combined. Fatigue, diarrhoea and slow heart rate rose with the dose. 3.3 percent stopped because of side effects, 6.8 percent on placebo.5

Storage

Store dry, at room temperature and protected from light. Keep out of reach of children.

Three white tablet bottles on a bright shelf next to a folded light blue towel
Dry, at room temperature and away from light. Symbolic image.
Level · Bisoprolol (Concor)

How the level builds up

One dose per day: each dose adds to what is left of the previous one.

Lexicon: Oral, once daily in the morning
Peak 1.28×Trough 0.28×
Day 1 · 2. dose
1.22× of the first dose
Plateau
from Day 1

95 % of the plateau after dose 2

Peak
1.28×

of the first dose

Trough
0.28×

before the next dose

Simplified model, values relative to the first dose, no dosing information. Dashed: the first dose alone, green: the plateau.

Related

Related compounds

Same targets or a different path: all in the TPD lexicon.

Bisoprolol (Concor)
Nebivolol (Bystolic) Beta blocker with additional vessel widening Metoprolol succinate ER (Toprol-XL) Beta blocker, broken down via CYP2D6 Amlodipine (Norvasc) Different path to lower blood pressure Ramipril (Altace) ACE inhibitor, different path to lower blood pressure Telmisartan Angiotensin receptor blocker, different path

FAQ

Common questions about Bisoprolol (Concor)

Short answers, each backed by the sources below.

What does beta-1 selective mean?

Bisoprolol mainly occupies the beta-1 receptors at the heart and hardly the beta-2 receptors in the bronchi and vessels. According to the label this is not absolute: at higher doses it also blocks beta-2 receptors. That is why the label advises using the lowest effective dose.57

Is bisoprolol approved?

Yes. ChEMBL lists bisoprolol as an approved compound with first approval in 1992. On ClinicalTrials.gov 141 trials list bisoprolol (as of 26 October 2026), the large CIBIS trials are not registered there. Everything here is the state of research, not a recommendation.76

What did CIBIS-II show?

2,647 people with severe heart failure received bisoprolol or placebo on top of standard therapy, the dose was raised slowly. After a mean of 1.3 years 11.8 instead of 17.3 percent had died, sudden deaths occurred in 3.6 instead of 6.3 percent. The trial was therefore stopped early.1

Beta blocker first or ACE inhibitor first?

CIBIS-III started 1,010 people on bisoprolol or enalapril alone for six months, after that everyone got both. Death or hospital occurred in 178 versus 186. By intention to treat starting with bisoprolol was non-inferior, in the per-protocol analysis this was not proven.3

Why not stop abruptly?

After stopping beta blockers suddenly, worsened angina and in some cases heart attack and rhythm disturbances were observed in coronary heart disease. The label advises tapering over about one week. In an overactive thyroid abrupt stopping can worsen the symptoms.5

Which side effects are typical?

In the placebo-controlled US trials fatigue was the clearest difference: 8.2 versus 1.5 percent. Diarrhoea and slow heart rate rose with the dose. Beta blockers can also mask the warning signs of low blood sugar, above all a racing heart.5

What did the angina comparison show?

In TIBBS 330 people with stable angina received bisoprolol or nifedipine. After four weeks minutes of ischaemia per 48 hours fell from 99.3 to 31.9 on bisoprolol and from 101 to 72.6 on nifedipine. The pulse at the start of an episode fell by 13.7 beats per minute from baseline on bisoprolol and stayed the same on nifedipine.4

Glossary

Terms explained briefly

Dotted words in the text open these explanations directly.

ACE inhibitor
Blood pressure drug that slows the formation of angiotensin II, for example enalapril or ramipril.
Beta blocker
A compound that blocks beta receptors and so damps the effect of adrenaline on heart and vessels.
Beta-1 receptor
Docking site for adrenaline mainly at the heart. When activated it raises pulse and force of contraction.
Beta-2 receptor
Docking site for adrenaline in bronchi, vessels and skeletal muscle. When activated it widens the bronchi.
Bradycardia
Too slow a pulse, at rest usually below 50 to 60 beats per minute.
Heart failure
The heart no longer pumps enough blood for the needs of the body.
Ischaemia
Too little blood flow to a tissue. At the heart it shows on the ECG and often as chest tightness.
Nebivolol
Another beta-1 selective beta blocker that also releases nitric oxide.
Nifedipine
Calcium channel blocker that widens the vessels and hardly lowers the pulse.
Noradrenaline
Messenger of the sympathetic nervous system that raises pulse and blood pressure.
Placebo
Dummy preparation without active substance. Comparing against it shows what is due to the substance itself.
Sympathetic nervous system
The part of the nervous system for effort and stress. It drives pulse and blood pressure up.

Evidence

Sources

Show all 7 sourcesHide sources 4 Studies1 Trial registry2 Database checked 26 Oct 2026

Studies

  1. CIBIS-II: bisoprolol and mortality in heart failure

    CIBIS-II Investigators and Committees, The Lancet, 1999

    DOI 10.1016/S0140-6736(98)11181-9 PMID 10023943
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  2. CIBIS: first randomised trial of bisoprolol in heart failure

    CIBIS Investigators and Committees, Circulation, 1994

    DOI 10.1161/01.cir.90.4.1765 PMID 7923660
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  3. CIBIS-III: starting with bisoprolol or with enalapril

    Willenheimer et al., Circulation, 2005

    DOI 10.1161/CIRCULATIONAHA.105.582320 PMID 16143696
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed
  4. TIBBS: bisoprolol versus nifedipine in stable angina

    von Arnim et al., Journal of the American College of Cardiology, 1995

    DOI 10.1016/0735-1097(94)00345-q PMID 7798508
    Checked 26 Oct 2026 via doi.org, Crossref, PubMed

Trial registry

  1. Trials on bisoprolol on ClinicalTrials.gov

    ClinicalTrials.gov, U.S. National Library of Medicine

    Checked 26 Oct 2026 via ClinicalTrials.gov API v2

Database

  1. US prescribing information for bisoprolol

    DailyMed, U.S. National Library of Medicine (Stand 26.06.2023)

    Checked 26 Oct 2026 via DailyMed, openFDA
  2. Mechanism and approval in ChEMBL

    ChEMBL, EMBL-EBI (CHEMBL645, Mechanismus am Fumarat CHEMBL1472989)

    Checked 26 Oct 2026 via ChEMBL