Candesartan cilexetil is (+)-1-[(cyclohexyloxy) carbonyl] oxyethyl 2-ethoxy-1-[2'-(1H-tetrazol-5-yl) [1,1'-biphenyl]-4- yl] methyl-1H-benzimidazole-7-carboxylate.
Antihypertensive. Candesartan is a selective AT1 subtype angiotensin II receptor antagonist.
Pharmacology: Mechanism of Action: Angiotensin II is formed from angiotensin I in a reaction catalyzed by angiotensin-converting enzyme (ACE, kininase II). Angiotensin II is the principal pressor agent of the renin-angiotensin system with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation and renal reabsorption of sodium. Candesartan blocks the vasoconstrictor and aldosterone secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT1 receptor in many tissues eg, vascular smooth muscle and the adrenal gland. Its action is therefore independent of the pathways for angiotensin II synthesis. Candesartan has much greater affinity (>10,000-fold) for the AT1 receptor than for the AT2 receptor.
Pharmacokinetics: Candesartan cilexetil is rapidly and completely bioactivated by ester hydrolysis during absorption from the gastrointestinal tract to candesartan. Peak serum concentration (Cmax) is reached after 3-4 hrs. Food with high-fat content does not affect the bioavailability of candesartan. It is mainly excreted unchanged in the urine and feces (via bile). It undergoes minor hepatic metabolism by O-deethylation to an inactive metabolite. The elimination half-life of candesartan is approximately 9 hrs. Candesartan and its inactive metabolite do not accumulate in serum upon repeated once-daily dosing.
Treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.
Dosage must be individualized. Blood pressure response is dose related over the range of 2-32 mg.
Usual Recommended Starting Dose: 16 mg once daily when used as monotherapy in patients who are not volume depleted. Candesartan cilexetil can be administered once or twice daily with total daily doses ranging from 8-32 mg. Larger doses do not appear to have a greater effect. Most of the antihypertensive effect is present within 2 weeks and maximal blood pressure reduction is generally obtained within 4-6 weeks of candesartan cilexetil treatment.
The most likely manifestation of overdosage would be hypotension, dizziness and tachycardia; bradycardia could occur from parasympathetic (vagal) stimulation. In managing overdose, the possibilities of multiple drug overdoses, drug-drug interactions and altered pharmacokinetics should be considered in patients. If symptomatic hypotension occurs, supportive treatment should be instituted.
Patients with known hypersensitivity to any component of Candelong.
In patients with an activated renin-angiotensin system eg, volume- and/or salt-depleted patients (eg, those being treated with diuretics), symptomatic hypotension may occur. These conditions should be corrected prior to administration of candesartan cilexetil. If hypotension occurs, the patient should be placed in the supine position and if necessary, given an IV infusion of normal saline. A transient hypotensive response is not a contraindication to further treatment, which can usually be continued without difficulty once the blood pressure has stabilized.
Use in pregnancy & lactation: Strictly not to be used during pregnancy. Drugs that can act directly on the renin-angiotensin system can cause fetal and neonatal morbidity and death when administered to pregnant women. When pregnancy is detected, candesartan cilexetil should be discontinued as soon as possible.
Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue candesartan, taking into account the importance of candesartan to the mother.
Strictly not to be used during pregnancy. Drugs that can act directly on the renin-angiotensin system can cause fetal and neonatal morbidity and death when administered to pregnant women. When pregnancy is detected, candesartan cilexetil should be discontinued as soon as possible.
Because of the potential for adverse effects on the nursing infant, a decision should be made whether to discontinue nursing or discontinue candesartan, taking into account the importance of candesartan to the mother.
In general, treatment with candesartan was well tolerated. The adverse events reported with candesartan cilexetil were:
Body as a Whole: Asthenia, fever.
Central and Peripheral Nervous System: Paraesthesia, vertigo.
Gastrointestinal System: Dyspepsia, gastroenteritis.
Heart Rate and Rhythm Disorders: Tachycardia, palpitation.
Metabolic and Nutritional Disorders: Increased creatinine phosphokinase, hyperglycemia, hypertriglyceridemia, hyperuricemia.
Musculoskeletal System Disorders: Myalgia.
Platelet, Bleeding/Clotting Disorders: Epistaxis.
Psychiatric Disorders: Anxiety, depression, somnolence.
Respiratory System Disorders: Dyspnoea.
Skin and Appendages Disorders: Rash, increased sweating.
Urinary System Disorders: Hematuria.
Other reported events seen less frequently include angina pectoris, myocardial infarction and angioedema.
No significant drug interactions have been reported when given with other drugs eg, glyburide, nifedipine, digoxin, warfarin, hydrochlorothiazide and oral contraceptives in healthy volunteers. Because candesartan is not metabolized by the cytochrome P-450 system and has no effects on P450 enzymes, interactions with drugs that inhibit or are metabolized by those enzymes would not be expected.
Store in a cool, dry place.
C09CA06 - candesartan ; Belongs to the class of angiotensin II receptor blockers (ARBs). Used in the treatment of cardiovascular disease.
Tab (uncoated) 4 mg x 10 x 10's. 8 mg x 10 x 10's.
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