Products

Candepressin

Indication
Hypertension &CHF

Pharmaceutical Form
film-coated tablets

 Candesartan cilexetil 32mg

Pharmacotherapeutic group:

Angiotensin II antagonists (candesartan),

Angiotensin II is the primary vasoactive hormone of the renin-angiotensin-aldosterone system and plays a role in the pathophysiology of hypertension, heart Failure and other cardiovascular disorders. It also has a role in the pathogenesis of end organ hypertrophy and damage.      The major physiological effects of angiotensin II, such as vasoconstriction, aldosterone stimulation, regulation of salt and water homeostasis and stimulation of cell growth, are mediated via the type 1 (AT1) receptor.

Candesartan cilexetil is a prodrug suitable for oral use. It is rapidly converted to the active drug, candesartan, by ester hydrolysis during absorption from the gastrointestinal tract. Candesartan is an angiotensin II receptor antagonist, selective for AT, receptors, with tight binding to and slow dissociation from the receptor. Candesartan has no agonist activity. Candesartan does not inhibit ACE, which converts angiotensin I to angiotensin II and degrade bradykinin. Candesartan does not affect ACE and gives no potentiation of bradykinin or substance 

 

Absorption and distribution

Following oral administration, candesartan cilexetil is converted to the active drug candesartan. The absolute bioavailability of candesartan is approximately 40% after an oral solution of candesartan cilexetil. The relative bioavailability of the tablet formulation compared with the same oral solution is approximately 34% with very little variability. The absolute bioavailability of the tablet is therefore estimated at 14%. The mean peak serum concentration (Cmax) is obtained 3 - 4 hours after the tablet intake. The candesartan serum concentrations increase linearly with increasing doses in the therapeutic dose range. No gender related differences in the pharmacokinetics of candesartan have been observed. The area under the serum concentration versus ns curve (AUC) of candesartan is not significantly affected by food.

Candesartan is highly bound to plasma protein (more than 99%). The apparent volume of distribution of candesartan is 0.1I/kg.

Metabolism and elimination

Candesartan is mainly eliminated unchanged via urine and bile and only to a minor extent eliminated by hepatic metabolism. The terminal half-life of candesartan is approximately 9 hours. There is no accumulation following multiple doses. Total plasma clearance of candesartan is about 0.37 ml/min/kg, with a renal clearance of about 0.19 ml/min/kg. The renal elimination of candesartan is both by glomerular filtration and active tubular secretion. Following an oral dose of radioactively labelled candesartan cilexetil, approximately 26% of the dose is excreted in the urine as candesartan and 7% as an inactive metabolite while approximately 56% of the dose is recovered in the faeces as candesartan and 10% as the inactive metabolite. 

For Hypertension:

The dose 16 mg once daily. If blood pressure is not sufficiently controlled after 4 weeks of treatment with 16 mg once daily,
 the dose may be further increased to a maximum of 32 mg once daily 

For Heart Failure:

The usual recommended initial dose of Candepressin is 8 mg once daily, Up-titration to the target dose of

32 mg once daily or the highest tolerated dose is done by doubling the dose at intervals of at least 2 weeks