Dosing & Uses
Dosing Form & Strengths
tablet
- 40mg
- 80mg
Hypertension
Indicated for hypertension, either alone or in combination with other antihypertensives
80 mg PO qDay
Coadministration with high-dose diuretics: 40 mg PO qDay
Renal Impairment
No dose adjustment is required with mild-to-severe renal impairment or end-stage renal disease
Patients with moderate-to-severe renal impairment are more likely to report high serum creatinine values
Hepatic Impairment
Dose adjustment not necessary with mild-to-moderate hepatic impairment; monitor in severe impairment (data not available)
Administration
May be administered with or without food
Safety and efficacy not established
No dose adjustment is necessary in elderly patients
Abnormally high serum creatinine values were more likely to be reported for patients aged 75 or older
Hypertension
80 mg PO qDay
Coadministration with high-dose diuretics: 40 mg PO qDay
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Adverse Effects
1-10%
Diarrhea (2%)
<1%
Nausea
Asthenia
Fatigue
Muscle spasm
Dizziness
Postural hypotension
Cough
Postmarketing Reports
Nausea
Muscle spasm
Rash, pruritus, angioedema
Warnings
Black Box Warnings
Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death
Contraindications
Hypersensitivity
Do not coadminister with aliskiren in patients with diabetes
Cautions
Correct volume or salt depletion before administration (risk for excessive hypotension)
Abnormally high serum creatinine values more likely reported in patients aged 75 or older
Caution with hyperkalemia
Increased risk for renal failure in patients with risk factors (eg, renal artery stenosis); monitor for worsening renal function in patients with renal impairment
Dual blockade of the renin angiotensin system with ARBs, ACE inhibitors, or aliskiren associated with increased risk for hypotension, hyperkalemia, and renal function changes (including acute renal failure) compared to monotherapy
NSAIDs may attenuate antihypertensive response
Coadministration with NSAIDs increase risk of renal impairment including acute renal failure
Pregnancy & Lactation
Pregnancy Category: C (1st trimester); D (2nd and 3rd trimesters)
Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death
Lactation: unknown whether distributed in breast milk, decide on alternate antihypertensive therapy or do not breastfeed
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Angiotensin II blocker; displaces angiotensin II from AT1 receptor and may lower blood pressure by antagonizing AT1-induced vasoconstriction, aldosterone release, catecholamine release, arginine vasopressin release, water absorption, and hypertrophic responses
May induce more complete inhibition of renin-angiotensin system compared with ACE inhibitors; does not affect response to bradykinin
Inhibits the pressor effects of an angiotensin II infusion in a dose-related manner
Pharmacokinetics
Bioavailability: 60%
Peak Plasma Time: 1.5-3 hr
Vd: 16 L
Protein Bound: >99% (mainly albumin)
Metabolites: Forms 2 primary metabolites; 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; M-I and MII do not contribute to the pharmacologic activity
Metabolism: Azilsartan medoxomil is hydrolyzed to azilsartan (active drug) in GI tract during absorption
Enzymatic metabolism: major enzyme responsible for azilsartan metabolism is CYP2C9
Half-Life: 11 hr
Clearance: 0.14 L/hr
Excretion: feces (55%), urine (42%)
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Patient Handout
Formulary
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