Trade Names:Atacand- Tablets 4 mg- Tablets 8 mg- Tablets 16 mg- Tablets 32 mg
Antagonizes the angiotensin ΙΙ effect (vasoconstriction and aldosterone secretion) by blocking the angiotensin ΙΙ receptor (AT 1 receptor) in vascular smooth muscle and the adrenal gland, producing decreased BP.
Bioavailability is about 15%. T max is 3 to 4 h.
Vd is 0.13 L/kg. More than 99% protein bound.
Candesartan cilexetil is bioactivated by ester hydrolysis during absorption from the GI tract to candesartan. Candesartan undergoes minor hepatic metabolism by O-deethylation to an inactive metabolite.
The t ½ is about 9 h. Plasma Cl is 0.37 mL/min/kg. Renal Cl is 0.19 mL/min/kg. About 26% is excreted unchanged in urine.
In hypertensive patients with Ccr less than 30 mL/min/1.73 m 2 , the AUC and C max are approximately doubled. In heart failure patients with renal function impairment, AUC is 36% and 65% higher and C max is 15% and 55% higher in patients with mild and moderate renal function impairment, respectively.Hepatic Function Impairment
The AUC and C max increased 30% and 56% in mild impairment and 145% and 73% in moderate impairment, respectively.Elderly
C max is about 50% higher; AUC is about 80% higher.
Treatment of hypertension; treatment of heart failure.
PO Initial dose: 16 mg/day; consider lower dose if volume-depleted. Total daily doses range from 8 to 32 mg in 1 or 2 doses.Heart FailureAdults
PO Initial dose: 4 mg/day. Double the dose at 2î“¸wk intervals to achieve target dose of 32 mg/day.Hepatic Function Impairment
Consider using a lower initial dose in patients with moderate hepatic function impairment.
Administer without regard to food. Administer with food if GI upset occurs.
Store at controlled room temperature (59° to 86°F) in a tightly closed container.
Plasma concentrations of lithium may be increased, resulting in an increase in pharmacologic and adverse reactions.Potassium-sparing diuretics (eg, amiloride, spironolactone, triamterene)
Coadministration may cause elevated serum potassium concentrations in certain high-risk patients.
None well documented.
Dizziness (4%); fatigue, headache (1%).
Pruritis, urticaria (postmarketing).
Pharyngitis, rhinitis (2%); sinusitis.
Abdominal pain, diarrhea, nausea, vomiting (1%).
Renal failure, renal function impairment (postmarketing).
Agranulocytosis, leukopenia, neutropenia (postmarketing).
Hepatic function impairment, hepatitis (postmarketing).
Hyperkalemia, hyponatremia (postmarketing).
Upper respiratory tract infection (6%); bronchitis (1%); cough.
Back pain (3%); arthralgia, chest pain, peripheral edema (1%); albuminuria; edema.
When used in pregnancy during the second and third trimesters, drugs that act directly on the renin-angiotensin system can cause injury and even death to the developing fetus. When pregnancy is detected, discontinue therapy as soon as possible.
Monitor BP, serum potassium, and serum creatinine during therapy and periodically thereafter.
Category D (second and third trimester); Category C (first trimester).
Safety and efficacy not established.
Use caution in treating patients whose renal function may depend on the activity of the renin-angiotensin-aldosterone system (eg, patients with severe CHF).
Use with caution when initiating therapy; hypotension may occur.
May occur, especially in heart failure patients.
Symptomatic hypotension may occur in patients who are intravascularly volume depleted (eg, those treated with diuretics). Correct these conditions prior to administration or use a lower starting dose.
Bradycardia, dizziness, hypotension, tachycardia.
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