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Pronunciation: AY-zil-SAR-tan me-DOX-oh-mil
Class: Angiotensin II receptor antagonist
- Tablets, oral 40 mg
- Tablets, oral 80 mg
Blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II by selectively blocking the binding of angiotensin II to the AT 1 receptor in many tissues, such as vascular smooth muscle and the adrenal gland.
T max is 1.5 to 3 h. Absolute bioavailability is approximately 60%.
Vd is approximately 16 L. More than 99% protein bound, mainly to serum albumin.
The major metabolite in plasma is formed by O-dealkylation, referred to as metabolite M-II, and the minor metabolite is formed by decarboxylation, referred to as metabolite M-I. Systemic exposures to the major and minor metabolites in humans were approximately 50% and less than 1% of azilsartan, respectively. M-I and M-II do not contribute to the pharmacologic activity of azilsartan. The major enzyme responsible for azilsartan metabolism is CYP2C9.
Following an oral dose of 14 C-labeled azilsartan, approximately 55% of radioactivity was recovered in the feces and approximately 42% in the urine, with 15% of the dose excreted in urine as azilsartan. The elimination half-life is approximately 11 h and renal Cl is 2.3 mL/min.
Special PopulationsRenal Function Impairment
Dose adjustment is not required in patients with mild to severe renal impairment or ESRD. Patients with moderate to severe renal impairment are more likely to report abnormally high serum creatinine values.Hepatic Function Impairment
No dose adjustment is necessary for subjects with mild or moderate hepatic impairment. Azilsartan has not been studied in patients with severe hepatic impairment.
Indications and Usage
Treatment of hypertension alone or in combination with other antihypertensives.
None well documented.
Dosage and AdministrationHypertension
PO 80 mg once daily. Consider a starting dose of 40 mg in those who are treated with high doses of diuretics.
- May be taken orally with or without food.
- If BP is not controlled with azilsartan alone, additional BP reduction can be achieved by taking azilsartan with other antihypertensive agents.
Store at 77°F; excursions are permitted between 59° and 86°F. Protect from moisture and light. Do not repackage; dispense and store in original container.
Drug InteractionsNSAIDs (eg, ibuprofen) including selective cyclooxygenase-2 inhibitors (eg, celecoxib)
In patients who are elderly or volume-depleted (including those on diuretic therapy), or who have compromised renal function, administration of NSAIDs with azilsartan may result in deterioration of renal function, including possible acute renal failure. These effects are usually reversible. Periodically monitor renal function in patients receiving azilsartan and NSAIDs concurrently. In addition, the antihypertensive effect of azilsartan may be decreased by NSAIDs.
Asthenia; dizziness; fatigue; postural dizziness.
Diarrhea (2%); nausea.
Increased serum creatinine; decreased Hbg, Hct, and RBC.
Cough; muscle spasm.
Avoid use in pregnancy. When pregnancy is detected, discontinue azilsartan as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury to and death of the developing fetus.
Monitor BP periodically during therapy.
Category D (second and third trimester); Category C (first trimester). May cause injury to or death of fetus if used during the second or third trimester.
Safety and efficacy not established.
Abnormally high serum creatinine values are more likely to be reported.
Patients with moderate to severe renal impairment are more likely to report abnormally high serum creatinine values.
Decreases in BP may occur after first dose, especially in patients with severe salt or volume depletion.
As a consequence of inhibiting the renin-angiotensin system, changes in renal function may be anticipated in susceptible individuals treated with azilsartan. In patients whose renal function may depend on the activity of the renin-angiotensin system (eg, patients with severe congestive heart failure, renal artery stenosis, or volume depletion), treatment with ACE inhibitors and angiotensin receptor blockers has been associated with oliguria or progressive azotemia and, rarely, with acute renal failure and death.
None well documented.
- Advise patients to take azilsartan with or without food.
- Advise women of childbearing age that use of drugs such as azilsartan that act on the renin-angiotensin system can cause serious problems in the fetus and infant, including low BP, poor development of skull bones, kidney failure, and death, if they are used during pregnancy. These consequences do not appear to have resulted from intrauterine drug exposure that has been limited to the first trimester. Discuss other treatment options with women planning to become pregnant. Advise women using azilsartan who become pregnant to notify their health care provider as soon as possible.
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