What Is Bisoprolol?

Bisoprolol (bisoprolol) is a kind of yellow oily chemical product, trade name: Concor, alias Kang Ke; Kang Xin; bisoprolol fumarate; Bosu and so on. Molecular formula: C18H31NO4, molecular weight: 325.44300. Bisoprolol is a beta-blocker, which can selectively act by blocking the connection of adrenalin to the beta 1 receptor without affecting the beta 2 receptor. It is a 1-blocker with high affinity and selectivity for cardiac 1-receptors. Its 1-selectivity is higher than that of cardiac selective -blockers such as atenolol and metoprolol. There is no cell membrane stabilization effect within the therapeutic dose range. It is clinically used to treat hypertension, and can be used alone or in combination with other antihypertensive drugs, and congestive heart failure. ^[1-3]

Drug Name: Bisolo
Alias: Concor
Foreign name: Bisoprolol
Main indications: Hypertension, coronary heart disease (angina pectoris)
Dosage: The details are as follows

Adverse reactions: Tiredness, dizziness, headache, etc.
Main medication contraindications: Allergic to this medicine, cardiogenic shock, etc.
Dosage form: Tablet: 5mg, 10mg.
Drug type: chemical
CAS: 66722-44-9

Basic information

Chinese name

English name: bisoprolol

English alias: 1- {4-[(2-Isopropoxyethoxy) methyl] phenoxy} -3- (isopropylamino) -2-propanol;

1- (propan-2-ylamino) -3- [4- (2-propan-2-yloxyethoxymethyl) phenoxy] propan-2-ol;

CAS number: 66722-44-9 ^[1]

Molecular formula: C18H31NO4

Molecular weight: 325.44300 ^[1]

Chemical structure of bisoprolol fumarate:

Exact mass: 325.22500 ^[1]

PSA: 59.95000

LogP: 2.75680 ^[1]

Physicochemical properties of bisoprolol

Appearance and properties: yellow oily

Density: 1.033 g / cm3

Boiling point: 176-178 ° C 16mm

Flash point: 176-178 ° C / 16mm

Refractive index: 1.5685

Storage conditions: storeroom ventilated, low temperature and dry ^[1]

Bisorol safety information

Customs Code: 2922509090

Danger category code: R36 / 37/38

Safety instructions: S26; S36

Dangerous goods mark: Xi ^[1]

Production method of bisoprolol

4-[(2-isopropoxyethoxy) methyl] phenol is reacted with epichlorohydrin, and the resulting epoxide is reacted with isopropylamine to obtain bisoprolol. ^[1]

Overview of Bisoprolol Drug Related Information

Bisoprolol drug name

Chinese name: Bisolol

English name: Bisoprolol

Alias: Kang Ke; Kang Xin; Bisoprolol fumarate; Bosu; Concor; Emcor; Euradal ^[2]

Bisoprolol classification

Circulatory Drugs> Antiarrhythmic Drugs> Beta Blockers ^[2]

Bisoprolol dosage form

Tablet: 5mg, 10mg. ^[2]

Bisoprolol pharmacological action

Bisoprolol is a selective 1 adrenergic receptor blocker, and within the therapeutic dose range, there is no obvious membrane stabilization effect or intrinsic sympathomimetic effect. However, its cardiac selectivity is not absolute, and it also inhibits 2 adrenergic receptors at high doses (20 mg), mainly in the bronchial and vascular smooth muscle; it is necessary to use the lowest effective dose to maintain selectivity. Selectivity to the 1 receptor is four times that of atenolol. Bisoprolol's 1 receptor blocking effect is its main effect in lowering blood pressure. ^[2]

Bisoprolol pharmacokinetics

The absolute bioavailability after oral bisoprolol 10mg is about 80%, and its absorption is not affected by food. Its first pass metabolism (first pass metabolism) is about 20%. The serum protein binding rate was approximately 30%. The peak plasma concentration of 5 20mg dose occurred in 2 4h. The elimination half-life is 9-12 hours. Once a day, steady state was reached in 5 days. Elimination by the renal and non-renal routes is equal, approximately 50% of the dose is excreted in the urine as it is, and the rest is excreted as inactive metabolites. ^[2]

Bisoprolol indication

Hypertension, can be used alone or in combination with other antihypertensive drugs, congestive heart failure. ^[2]

Bisoprolol contraindication

Patients with bisoprolol allergy, cardiogenic shock, hypotension, significant heart failure, or degree atrioventricular block, sick sinus syndrome, obvious sinus bradycardia and bronchial asthma are contraindicated. ^[2]

Bissolol notes

1. (1) chronic obstructive airway disease; (2) congestive heart failure; (3) bradycardia; (4) liver insufficiency; (5) renal insufficiency; (6) peripheral circulation disorders, if any Intermittent claudication or Raynaud's phenomenon; (7) Diabetes, especially those with large blood glucose fluctuations and acidosis; (8) Hyperthyroidism; (9) During anesthesia or surgery.

2. Regularly monitor heart function (heart rate, blood pressure, electrocardiogram, chest radiograph), liver and kidney function, and diabetic patients should check blood glucose regularly.

3. In the treatment of hypertension, the dosage must be individualized, and the dosage should be gradually increased until the best antihypertensive effect is achieved. However, it takes 1 to 2 weeks to achieve the best antihypertensive effect, so it should be observed for a period of time to determine the effect.

4. The dose should be decreased when the drug is stopped. Sudden withdrawal can cause worsening angina pectoris and even myocardial infarction, which can also cause hypertension to rebound. When discontinued, the dose should be gradually reduced, and physical activity should be limited as much as possible.

5. Atropine, isoproterenol, and cardiac pacing can be used when bradycardia or conduction blockage occurs due to overdose of the drug. Cardiac medicine, booster drugs, and fluid replacement can be given when heart failure or hypotension occurs. For treatment, beta 2 receptor agonists are given when bronchospasm occurs.

Bisoprolol medication for pregnant women

Bisoprolol may harm pregnant women and / or fetuses / newborns. In general, -adrenergic receptor antagonists can reduce placental perfusion, and placental perfusion is related to developmental delay, intrauterine death, absorption and premature delivery, and the fetus and newborn may have adverse reactions such as hypoglycemia and bradycardia If -adrenergic blockers must be used, selective 1-adrenergic blockers are ideal.
Unless it is clear that it must be used, pregnant women cannot use bisoprolol. If bisoprolol must be used for treatment, uterine placental blood flow and fetal growth should be monitored. Once it is found to have harmful effects on pregnant women and fetuses, other treatments should be selected. Neonates must be closely monitored. Hypoglycemia and bradycardia are most likely to occur in the first 3 days after birth. ^[3]

Bisoprolol breastfeeding women

Whether this product is excreted by human milk is not clear, therefore, bisoprolol is not recommended for breastfeeding women. ^[3]

Bisoprolol medication for children

There is no experience with bisoprolol in pediatric patients, so this product cannot be used in children.

Bisoprolol

No dose adjustment is required. ^[3]

Bisoprolol adverse reactions

1. Adverse reactions similar to other 1 receptor blockers, which are related to the dose of bisoprolol.

2. May have: tiredness, dizziness, headache, sweating, poor sleep. Occasional gastrointestinal reactions, bradycardia, marked drop in blood pressure, conduction block, rash, erythema, myalgia, and lower limb swelling ^[2]

Bisoprolol dosage

Usually the initial dose is 5mg each time, once a day, the initial dose for patients with bronchospasm can be 2.5mg. The dose can be increased to 10 mg and 20 mg if necessary. Patients with liver and kidney dysfunction (creatinine clearance of less than 40 ml per minute) should use the initial dose of 2.5 mg per day. Be careful when increasing the dose because bisoprolol cannot be replaced by dialysis. ^[2]

Interaction of bisoprolol with other drugs

1. It can aggravate the first dose response of 1 blockers. In addition to prazosin, other 1 blockers are rare, but they should still be used with bisoprolol.

2. Combined with amiodarone, obvious bradycardia and sinus arrest can occur.

3. Combination with dihydropyridine calcium channel blockers is effective in treating angina pectoris or hypertension, but it can also cause severe hypotension or decrease in heart reserve. Cardiac function should be carefully monitored in combination, especially for patients with impaired left ventricular function, arrhythmia, or aortic stenosis.

4. Diltiazem can enhance the pharmacological effects of -blockers and is beneficial to patients with normal cardiac function. However, there have been reports of hypotension, left ventricular failure, and atrioventricular block after combined use. If combined, the patient's cardiac function should be closely monitored, especially in the elderly, left ventricular failure, aortic stenosis, and the use of both drugs.

5. Verapamil and bisoprolol have direct negative muscle strength and negative conduction, which may cause hypotension, bradycardia, congestive heart failure, and conduction disorders. The risk increases with left ventricular dysfunction, aortic stenosis, or both doses. Cardiac function should be closely monitored when the two drugs are combined.

6. Combined with mibediril can cause hypotension, bradycardia or reduced heart reserve. Mbetidil should be discontinued for 7 to 14 days before starting beta blocker therapy. If combined, cardiac function should be monitored, especially in elderly patients with decreased left ventricular function, decreased cardiac conduction function, or aortic stenosis.

7. Used in combination with oloflex, it can cause hypotension or hypertension with bradycardia. If combined, the patient's blood pressure and heart rate should be monitored.

8. When fentanyl is anesthetized, the use of bisoprolol can cause severe hypotension.

9. Patients who have long-term use of -blockers before surgery are prone to bradycardia when given alfentanyl.

10. Angelica extract may inhibit the metabolism of bisoprolol by liver cytochrome P450 enzymes. If used in combination, attention should be paid to monitoring blood pressure.

11. Although there is no report on the interaction between benzprodil, flunarizine, lidofloxazine, golopamide, pecoxiline and bisoprolol, these drugs can all reduce myocardial contraction and slow Atrioventricular node conduction, which can lead to lower blood pressure, bradycardia, or decreased heart reserve. If combined, cardiac function should be monitored, especially in patients with decreased left ventricular function, decreased cardiac conduction function, or aortic stenosis.

12. Zileuton can cause a significant increase in propranolol concentration. Although there have been no reports of interactions with bisoprolol, caution should be exercised when combined.

13. Combination with digoxin can lead to prolonged atrioventricular conduction time, and can increase the blood concentration of digoxin. When combined, the ECG and the blood plasma concentration of digoxin should be carefully monitored and the dose adjusted accordingly.

14. In the combined treatment of bisoprolol and clonidine, sudden withdrawal of clonidine may exacerbate hypertension. Therefore, in order to withdraw cola, you should withdraw bisoprolol first, closely monitor blood pressure, and then gradually reduce clonidine after a few days. Caution should be taken when using Mosulidine in combination with sudden withdrawal of Mosulidine.

15. When combined with methacholine, beta-blockers can aggravate or prolong bronchoconstriction, so patients treated with bisoprolol should avoid inhaling methacholine.

16. In combination with methyldopa, very few patients can have abnormal reactions to endogenous or exogenous catecholamines, such as hypertension, tachycardia, or arrhythmia.

17. Combined with non-steroidal anti-inflammatory drugs, can cause blood pressure to rise. If combined, blood pressure should be monitored and the dose adjusted accordingly.

18. Abtamin has a beta receptor agonistic effect, which is reduced if bisoprolol is used in combination with it. Therefore, bisoprolol should be discontinued for at least 48 hours before the use of abutamine.

19. Beta-blockers can antagonize the effects of ritodrine, so the combination of bisoprolol and ritodrine should be avoided.

20. Ephedra contains ephedrine and pseudoephedrine, which can reduce the efficacy of antihypertensive drugs. Patients with hypertension treated with bisoprolol should avoid using ephedra-containing preparations.

21. Cardiac selective -receptor blockers are less likely to cause impaired glucose tolerance in patients with type 2 diabetes, but diabetic patients should still pay attention when combining bisoprolol with hypoglycemic agents.

22. The interaction of cimetidine, rifampicin and bisoprolol has no obvious clinical significance. ^[2]

Bisoprolol Expert Reviews

Beta adrenergic blockers are referred to as beta blockers. It is a kind of cardiovascular drug widely used in clinical practice. It has significant effects on a variety of cardiovascular diseases such as hypertension, myocardial ischemia, myocardial infarction, cardiomyopathy and arrhythmia. Recent clinical studies have shown that beta blockers Can reduce the overall mortality and sudden death rate of patients with CHF, and has become an indispensable treatment in addition to the standard triple therapy of heart failure (ACE I diuretic digoxin). After atenolol was applied topically, it took effect within 1 hour, peaked at 2 to 3 hours, lasted 7 hours, and had the greatest effect at 2 to 5 hours when taken orally. ^[2]