Description:
Candesartan cilexetil is a kind of prodrug being hydrolyzed to candesartan during absorption from the gastrointestinal tract. It appears as a white or off-white powder with a molecular weight of 610.67. It is soluble in methan/ol but insoluble in water. It is a kind of selective AT1 subtype angiotensin II receptor antagonist, mainly used for the treatment of hypertension and heart failure. Candesartan cilexetil takes effects through selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland, further blocking the vasoconstrictor and aldosterone-secreting effects of angiotensin II. Therefore, its mode of action is not through interfering with the pathways for angiotensin II synthesis. Candesartan cilexetil may lead to various kinds of adverse reactions including headache, back pain, dizziness, upper respiratory tract infection, pharyngitis, rhinitis, bronchitis, coughing, sinusitis, nausea, abdominal pain, diarrhea, vomiting, arthralgia and albuminuria. It should be warned that candesartan cilexetil might have remarkable fetal toxicity. Therefore, upon pregnancy, candesartan cilexetil should be discontinued. It could also cause hypotension for heart-failure patients.
Function: Candesartan cilexetil is a prodrug of the potent, long-acting, and selective angiotensin II type 1 receptor AT1 antagonist, candesartan. It is rapidly hydrolyzed to candesartan during gastrointestinal absorption. After hydrolysis of candesartan cilexetil to candesartan during gastrointestinal absorption, candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 AT1 in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. In addition, antagonism of AT1 in the adrenal gland inhibits angiotensin II-stimulated aldosterone synthesis and secretion by the adrenal cortex; sodium and water excretion increase, followed by a reduction in plasma volume and blood pressure. Candesartan cilexetil can be used as pesticide and pharmaceutical intermediates. It can be used as the raw material of antihypertensive drugs. Candesartan is an angiotensin-receptor blocker (ARB),Angiotensin receptor blockers effectively protect against the harmful effects of the activation of the renin-angiotensin-aldosterone system that occur with hypertension or diabetes.It may be used alone or with other agents to treat hypertension. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of dry cough. Candesartan may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction and coronary artery disease.
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