Candesartan Cilexetil
Synonymous： | 1H-Benzimidazole-7-Carboxylic acid |
CAS： | 145040-37-5 |
Molecular Formula： | C33H34N6O6 |
Molecular Weight： | 610.660 |
Appearance | white to beige powder |
Storage | Below to -20°C |
Category | Drugs for treating hypertension |
Product introduction:
This product is white and sweet. It is rapidly decomposed into the active metabolite candesartan in vivo. Candesartan is an angiotensin Ⅱ at receptor antagonist. It antagonizes the contraction of angiotensin Ⅱ by binding to at receptor of vascular smooth muscle, so as to reduce peripheral vascular resistance. It is suitable for essential hypertension.
Candesartan axetil is a prodrug of candesartan. Its action intensity is 10 times that of losartan. It has good selectivity (its affinity for AT1 receptor is more than 10000 times higher than that of AT2) and long action time (once a day). Because it is a prodrug, it releases activity gently in vivo after oral administration, so it is an ideal drug for the treatment of hypertension.
Pharmacological action:
Candesartan axetil is the precursor of candesartan, which is rapidly and completely hydrolyzed to candesartan during gastrointestinal absorption. The absolute bioavailability J of candesartan is about 15%, and the peak time of plasma candesartan concentration is 3-4 hours. The binding rate of candesartan to plasma protein was more than 99%, and the apparent distribution volume B was 0.13l/kg. Rat experiments showed that candesartan rarely passed through the blood-brain barrier, but it could pass through the placental barrier and distribute to the fetus.
Candesartan is mainly excreted in urine and feces in its original form, and a small part of candesartan is formed into inactive metabolites by o-deethylation in the liver. The excretion half-life of candesartan is about 9 hours. The plasma clearance X of candesartan was 14.07 L / h and the final elimination half-life was 9-13 hours. The data showed that the total clearance rate of candesartan was 0.37 ml / min · kg and the renal clearance rate was 0.19 ml; After oral administration of 14C labeled candesartan axetil, 33% and 67% of radioactive substances were recovered from urine and feces respectively.
Purpose:
Pesticides and pharmaceutical intermediates; Antihypertensive pharmaceutical raw materials.
Taboos:
(1) Patients with a history of allergy to the ingredients of this preparation.
(2) Pregnant or likely pregnant women.
Candesartan axetil was rapidly decomposed into the active metabolite candesartan in vivo. Candesartan is an angiotensin Ⅱ at receptor antagonist. It antagonizes the contraction of angiotensin Ⅱ by binding to at receptor of vascular smooth muscle, so as to reduce peripheral vascular resistance. It is suitable for essential hypertension.
IUPAC
1-cyclohexyloxycarbonyloxyethyl 2-ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]benzimidazole-4-carboxylate
SMILES
CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5)C(=O)OC(C)OC(=O)OC6CCCCC6
Zhejiang, China
