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Azilsartan

ARB · Antihypertensive

Also known as Azilsartan medoxomil

ARBAntihypertensive
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
Contraindicated during the second and third trimesters of pregnancy due to risk of fetal hypotension, anuria, renal failure, malformations or death. Increased teratogenic risk in first trimester.
FDA category + note
Top interactionssee all 12
  • AliskirenContraindicatedTextbookG&G 14e · p603
  • Sacubitril ValsartanContraindicatedTextbookG&G 14e · p602
  • Angiotensin Converting Enzyme InhibitorsSevereTextbookHarrison 22e · p2396
  • BenazeprilSevereTextbookG&G 14e

Mechanism

Azilsartan is an angiotensin II type 1 (AT1) receptor blocker, inhibiting the effects of angiotensin II. Unlike ACE inhibitors, it does not inhibit the breakdown of bradykinin and other kinins, offering more selective and potentially more complete inhibition of angiotensin action.

Indications

HypertensionHeart failureDiabetic nephropathy

Dosing

Adult
after any change in dose or during intercurrent illness. Other drugs used for Hypertension Amiloride hydrochloride, p. 243 . Chlortalidone, p. 244 . Cotriamterzide, p. 245 . Metolazone, p. Torasemide, p. 242 . Triamterene with chlortalidone, p. Xipamide, p. 245 ANTIHYPERTENSIVES, CENTRALLY ACTING Clonidine hydrochloride ▶ ▶ BY MOUTH ▶ Adult: Initially 50 micrograms twice daily for 2 we...

Pharmacokinetics

Peak effect
plasma concentrations (Cmax) are achieved within 1.5 to 3 h
Half-life
elimination t1/2 is approximately 11 h
Bioavailability
approximately 60% and is not affected by food
Metabolism
prodrug is hydrolyzed in the GI tract into the active form, azilsartan...metabolized mostly by CYP2C9 into inactive metabolites
Excretion
Elimination of the drug is 55% in feces and 42% in urine. About 15% of the dose is eliminated unchanged in urine.

Contraindications

  • Second and third trimesters of pregnancy
  • First trimester of pregnancy (increased teratogenic risk)
  • Concomitant use with ACE inhibitors
  • Concomitant use with aliskiren
  • Do not use in combination with ACE inhibitor
  • Contraindicated in pregnancy

Side effects

Common
HyperkalemiaAltered sense of tasteAllergic skin rashesDrug feverCoughhypotensionHyperkalemia in CKDReduced GFRAcute kidney failure in severe bilateral renal artery stenosis
Serious
  • Acute renal failure
  • Angioedema
  • anaphylaxis
  • abnormal hepatic function
  • hepatitis
  • neutropenia
  • leukopenia
  • agranulocytosis
  • pruritus
  • urticaria
  • hyponatremia
  • alopecia
  • vasculitis

Pregnancy & lactation

Pregnancy

Contraindicated during the second and third trimesters of pregnancy due to risk of fetal hypotension, anuria, renal failure, malformations or death. Increased teratogenic risk in first trimester.

Drug interactions

Aliskiren
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Sacubitril Valsartan
Contraindicated
Textbook

Potentially excessive hypotension, increased risk of adverse effects.

Do not use in conjunction with other ARBs.

Source: G&G 14e · p602

Angiotensin Converting Enzyme Inhibitors
Severe
Textbook

Greater incidence of acute kidney injury (AKI) and adverse cardiac events.

The combination of these two classes should be avoided.

Source: Harrison 22e · p2396

Benazepril
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Captopril
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Enalapril
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Enalaprilat
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Fosinopril
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Imidapril
Severe
Textbook

Greater incidence of acute kidney injury (AKI) and adverse cardiac events.

The combination of these two classes should be avoided.

Source: Harrison 22e · p2396

Lisinopril
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Moexipril
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Perindopril
Severe
Textbook

Increased worsening of renal function, hypotension, syncope, and hyperkalemia without increased efficacy.

Not recommended for the treatment of hypertension. Previous studies indicate more harm than benefit.

Source: G&G 14e

Related guidelines

Other ARB drugs

Ask House about Azilsartan

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Sources: Goodman & Gilman 14e, Harrison 22e, BNF·Verified: 2026-05-13 · House clinical team