Bisoprolol is successfully developed by the German Merck in 1978, in the world ,it is already the drug of choice on clinicalcommonly used to treat hypertension, angina, arrhythmias and heart failure and other cardiovascular diseases, the product is highly selective β1-adrenergic receptor blocker,it has hydrophilic and lipophilic properties,it has no intrinsic sympathomimetic activity and membrane stability, and its negative inotropic effect is weaker.It has two β receptor binding sites with ultra-high affinity and high affinity ,its drug action is extremely powerful,it is 7 to 10 times stronger than atenolol and metoprolol . It has highly β1 receptor selectivity, selective research about model complex β1/β2 finds out that: propranolol is 1/3,atenolol is 20/1 , bisoprolol is 60/1. Another study compares the β1/β2 selectivity of metoprolol and bisoprolol, the results show that the former is 74/1,the latter is 119/1. Like other β-blockers, bisoprolol by blocking heartβ1 receptors, and inhibiting the renin-angiotensin system, plays a role in the treatment of hypertension, angina, arrhythmia. Recent studies indicate that substance P has effect on dilating the blood vessels to reduce the role of peripheral resistance, content of substance P in patients with hypertension decreases significantly,there is a significant rebound of substance P while there is a decrease in blood pressure after the treatment of bisoprolol, which may be one of the possible mechanisms of antihypertension . Another study shows that bisoprolol can not only decrease the blood pressure, but can also improve diastolic function; it has no adverse effects on blood sugar, blood lipids , conclusion in diabetics is also like this . It is mainly used to treat supraventricular tachycardia, atrial fibrillation, ventricular premature contraction, coronary heart disease, angina, mild to moderate hypertension, it is also used in heart failure caused by dilated cardiomyopathy and ischemic heart disease.
Oral F is up to 88%. Tmax is 1.5~3 h. PPB is 30%. Plasma clearance T1/2 is 10~12 h. The one dose effect can be maintained for 24 h. Because its hydrophilic character is equal to lipophilic character, its adverse reactions on central nervous system are lighter than metoprolol with lipophilic character,and its adverse reactions on renal function is smaller compared withatenolol with hydrophilic character . Bisoprolol have two equal clearance ways ,half of it is metabolized to the non-active substances in the liver , the other half is excreted in the form of the prototype by the kidneys. [Note and taboos]it is similar to atenolol.
The above information is edited by the chemicalbook of Tian Ye.
It is used for the treatment of cardiovascular and cerebrovascular diseases.
Intravenous-Mouse LD50: 164 mg/kg.
Flammability hazard characteristics
Combustible; combustion produces toxic nitrogen oxide gases.
Ventilated, low-temperature ,dry storeroom.
Water, dry powder, foam, sand.
A selective a-adrenergic blocker. Used as an antihypertensive
Cardensiel is an intermediate in the synthesis of 3,3''-(Isopropylazanediyl)bis(1-(4-((2-isopropoxyethoxy)methyl)phenoxy)propan-2-ol) (I824005), which is an impurtiy of Bisoprolol (B510500), a selective β-adrenergic blocker. Used as an antihypertensive.
ChEBI: Bisoprolol is a secondary alcohol and a secondary amine. It has a role as an antihypertensive agent, a beta-adrenergic antagonist, an anti-arrhythmia drug and a sympatholytic agent.
This oral cardiospecific β-blocker (FWfree-base = 325.45 g/mol; CAS 66722- 44-9; IUPAC: (RS)-1-{4-[(2-isopropoxyethoxy)methyl]phenoxy}-3- (isopropylamino)propan-2-ol), also named Zebeta? (oral tablets as fumarate salt), selectively targets β1-adrenergic receptors, blocking epinephrine stimulation of β1-adrenoreceptors that are concentrated in the heart muscle cells and heart conduction tissue as well as kidney juxtaglomerular cells. Bisoprolol is used to treat hypertension, coronary heart disease, arrhythmias, ischemic heart diseases, and myocardial infarction after the acute event. Given such versatility, bisoprolol is understandably included in the World Health Organization's List of Essential Medicines. Pharmacokinetics: Bioavailability > 90%; Hepatic metabolism (50%) by CYP2D6 and CYP3A4; Biological t1/2 = 10-12 hours.
