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Candesartan ester is the precursor of candesartan, which is rapidly and completely hydrolysed to candesartan during gastrointestinal absorption.The absolute bioavailability of candesartan is about 15%, and the peak time of plasma candesartan concentration is 3-4 hours.
The binding rate of candesartan to plasma proteins is greater than 99%, and the apparent volume of distribution is 0.13 L/kg. Rat tests have demonstrated that candesartan rarely crosses the blood-brain barrier, but can cross the placental barrier and be distributed to the foetus.
Candesartan is excreted mainly in its original form in the urine and faeces, with a very small portion in the liver via O-deethylation to form inactive metabolites. The excretion half-life of candesartan is approximately 9 hours.
In hypertensive patients receiving 2-16 mg/day of the product orally for 4 weeks, the plasma clearance of candesartan was 14.07 L/h and the terminal elimination half-life was 9-13 hours.
It has been shown that the total clearance of candesartan is 0.37 ml/min-kg, renal clearance is 0.19 mL, and after oral administration of 14C-labelled candesartan ester, 33% and 67% of the radioactivity is recovered in urine and faeces, respectively.
Uses and functions of Candesartan Cilexetil (C11) .
Candesartan is a antihypertensive agent. It is a selective angiotensin I receptor (ATI) antagonist. By binding to ATI receptor of vascular smooth muscle, Candesartan inhibits vasoconstriction of angiotensin II, thereby reducing peripheral vascular resistance. It is mainly used to treat essential hypertension and can be used alone or in combination with other antihypertensive drugs.
Pharmacological Effects of Candesartan Cilexetil (C11) .
Candesartan ester is rapidly hydrolysed in vivo to the active metabolite candesartan, which is a selective angiotensin II receptor (AT1) antagonist, antagonising the vasoconstrictor effect of angiotensin II by binding to the AT1 receptor in vascular smooth muscle, thereby reducing peripheral vascular resistance.
It is also believed that Candesartan may exert some antihypertensive effects by inhibiting the secretion of aldosterone from the adrenal glands. Candesartan does not inhibit kininase II and does not affect bradykinin degradation.
Experiments conducted in hypertensive patients have shown that repeated administration of this product to patients can lead to an increase in plasma renin activity, angiotensin 1 concentration and angiotensin II concentration;
The continuous administration of 2-8mg of this product once a day can lead to a decrease in systolic and diastolic blood pressure, a decrease in left ventricular myocardial weight and peripheral vascular resistance, while there is no significant effect on cardiac output, ejection fraction, renal vascular resistance, renal blood flow and glomerular filtration rate; there is no effect on cerebral blood flow in patients with proto-genital hypertension who have cerebral vascular disorders.
Production method of Candesartan Cilexetil (C11) Raw Powder.
Oral, usually 4 to 8mg candesartan cilostatin once a day for adults, increase the dose to 12mg if necessary.
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