| CANDESARTAN CILEXETIL
Classifications: angiotensin ii receptor antagonist, antihypertensive; Therapeutic: antihypertensive, angiotensin ii receptor antagonist
Pregnancy Category: C first trimester; D second and third trimester
4 mg, 8 mg, 16 mg, 32 mg tablets
Angiotensin II receptor (type AT1) antagonist. Angiotensin II is a potent vasoconstrictor and primary vasoactive hormone of the reninangiotensinaldosterone
system. Candesartan selectively blocks binding of angiotensin II to the AT1 receptors found in many tissues (e.g., vascular smooth muscle, adrenal glands).
Results in blocking the vasoconstricting and aldosterone-secreting effects of angiotensin II, resulting in an antihypertensive
effect. Effectively lowers BP from hypertensive to normotensive range.
Hypertension, heart failure in conjunction with ACE inhibitor.
Known sensitivity to candesartan or any other angiotensin II (AT1) receptor antagonist (e.g., losartan, valsartan); primary hyperaldosteronism; bilateral renal artery stenosis; pregnancy
(category C first trimester; category D second and third trimesters); lactation. Safety and effectiveness in children not
Concurrent administration with high-dose diuretics, potassium-sparing diuretics, or potassium salt substitutes; unilateral
renal artery stenosis; aortic or mitral valve stenosis; hypertrophic cardiomyopathy; CHF; diabetes; lactation; moderate
heptic or renal impairment, significant renal failure.
Route & Dosage
Adult: PO Start at 16 mg q.d. (range 832 mg divided once or twice daily)
Adult: PO Start at 4 mcg once daily, double the dose at 2 wk intervals as tolerated by the patient until a dose of 32 mg is reached
For patients with moderate hepatic impairment, initiate therapy at lower dose.
- Volume depletion should be corrected prior to initiation of therapy to prevent hypotension.
- Dose is individualized and may be given once or twice daily. The daily dose may be titrated up to 32 mg; larger doses are
not likely to provide additional benefit.
Adverse Effects (≥1%) Body as a Whole: Fatigue
, peripheral edema, back pain, arthralgia
Chest pain. GI:
Nausea, abdominal pain, diarrhea
, vomiting. CNS:
Headache, dizziness. Respiratory:
, upper respiratory infection
, pharyngitis, rhinitis. Urogenital:
Use with lithium
may increase risk of lithium toxicity
Rapidly from GI tract; activated by ester hydrolysis; 15% reaches systemic circulation. Peak: Serum
concentration, 34 h; therapeutic effect, 24 wk. Duration:
24 h. Distribution:
>99% protein bound; crosses placenta; distributed into breast milk. Metabolism:
Minimally in liver. Elimination:
Primarily unchanged in bile (67%) and urine (33%). Half-Life:
Assessment & Drug Effects
- Monitor BP as therapeutic effectiveness is indicated by decreases in systolic and diastolic BP within 2 wk with maximal
effect at 46 wk.
- Monitor for transient hypotension in volume/salt-depleted patients; if hypotension occurs, place in supine position and notify
- Monitor BP periodically; trough readings, just prior to the next scheduled dose, should be made when possible.
- Lab tests: Periodically monitor BUN and creatinine, serum potassium, liver enzymes, and CBC with differential.
Patient & Family Education
- Inform your physician immediately if you become pregnant.
- You may not notice maximum pressure-lowering effect for 6 wk.
- Report episodes of dizziness especially when making position changes.