(a-zill-sar-tan) ,


(trade name)


Therapeutic: antihypertensives
Pharmacologic: angiotensin ii receptor antagonists
Pregnancy Category: D


Treatment of hypertension, alone or with other agents.


Blocks vasoconstrictor and aldosterone-producing effects of angiotensin II at receptor sites, including vascular smooth muscle and the adrenal glands.

Therapeutic effects

Lowering of BP.


Absorption: Azilsartan medoxomil, a prodrug, in hydrolyzed in the GI tract to azilsartan, the active component. 60% is absorbed from the GI tract.
Distribution: Approximately 16L.
Protein Binding: ≥99%.
Metabolism and Excretion: 50% metabolized by the liver, primarily by the CYP2C9 enzyme system. 55% eliminated in feces, 42% in urine (15% as unchanged drug).
Half-life: 11 hr.

Time/action profile (effect on BP)

POwithin 2 hr18 hr24 hr


Contraindicated in: Concurrent use with aliskiren in patients with diabetes or moderate-to-severe renal impairment (CCr <60 mL/min) Obstetric: Can cause injury or death of fetus – if pregnancy occurs, discontinue immediately. Lactation: Discontinue drug or use formula.
Use Cautiously in: genetic implication Black patients (may not be effective); HF (may result in potentially life-threatening renal failure); Renal impairment; may worsen renal function; Volume or salt depletion, including use of high-dose or potent diuretics may ↑ risk of serious hypotension; correct prior to use; Woman of childbearing potential; Geriatric: May have greater sensitivity, especially to adverse renal effects; Pediatric: Safety and effectiveness has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • dizziness
  • fatigue
  • weakness


  • hypotension (most frequent)

Fluid and Electrolyte

  • hyperkalemia


  • diarrhea (most frequent)
  • nausea


  • impaired renal function


  • muscle spasm


Drug-Drug interaction

Concurrent use of potassium-sparing diuretics, potassium-containing salt substitutes, or potassium supplements may ↑ risk of hyperkalemia.↑ risk of hyperkalemia, renal dysfunction, hypotension, and syncope with concurrent use of ACE inhibitors or aliskiren ; avoid concurrent use with aliskiren in patients with diabetes or CCr <60 mL/minNSAIDs and selective COX-2 inhibitors may blunt the antihypertensive effect and ↑ the risk of renal dysfunction.↑ antihypertensive effect with other antihypertensives or diuretics.


Oral (Adults) 80 mg once daily, initial dose may be ↓ to 40 mg once daily if high doses of diuretics are used concurrently.


Tablets: 40 mg, 80 mg
In combination with: chlorthalidone (Edarbyclor). See combination drugs.

Nursing implications

Nursing assessment

  • Assess BP (sitting, lying, standing) and pulse periodically during therapy.
  • Monitor frequency of prescription refills to determine adherence to therapy.
  • Lab Test Considerations: Monitor renal function. May cause small, reversible ↑ serum creatinine. May cause worsening renal function in patients with renal impairment. May rarely cause slight ↓ in RBC, hemoglobin and hematocrit.
    • May cause low and high markedly abnormal platelet and WBC.

Potential Nursing Diagnoses

Risk for injury (Adverse Reactions)
Noncompliance (Patient/Family Teaching)


  • Correct volume and salt depletion, if possible, before initiation of therapy, or start treatment at 40 mg.
  • Oral: Administer once daily without regard to food.

Patient/Family Teaching

  • Emphasize the importance of continuing to take as directed, even if feeling well. Take missed doses as soon as remembered if not almost before next dose; do not double doses. Medication controls but does not cure hypertension. Instruct patient to take medication at the same time each day. Warn patient not to discontinue therapy unless directed by health care professional.
  • Encourage patient to comply with additional interventions for hypertension (weight reduction, low-sodium diet, smoking cessation, moderation of alcohol consumption, regular exercise, and stress management). Medication controls but does not cure hypertension.
  • Instruct patient and family on proper technique for monitoring BP. Advise them to check BP at least weekly and to report significant changes.
  • Caution patient to avoid sudden position changes to decrease orthostatic hypotension. Use of alcohol, standing for long periods, exercising, and hot weather may ↑ orthostatic hypotension.
  • May cause dizziness. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications, especially NSAIDs and cough, cold, or allergy medications.
  • Instruct patient to notify health care professional of medication regimen before treatment or surgery.
  • Advise women of childbearing age to use contraception and notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Azilsartan should be discontinued as soon as possible when pregnancy is detected.
  • Emphasize the importance of follow-up exams to evaluate effectiveness of medication.

Evaluation/Desired Outcomes

  • ↓ in BP without excessive side effects.
Drug Guide, © 2015 Farlex and Partners
References in periodicals archive ?
She was prescribed azilsartan and carbamazepine after diagnosis of PRES and reversible cerebral vasoconstriction syndrome.
Several authors from both studies disclosed ties to the pharmaceutical industry; in the Nasrallah study, azilsartan and chlorthalidone (combined with azilsartan) were provided by Takeda Pharmaceuticals.
Nitrosamines have recently re-surfaced in the pharmaceutical world due to FDA and other international agencies finding traces of these compounds in the angiotensin II receptor blockers (ARBs), commonly known as the "sartans." The drugs involved are Valsartan, Losartan, Irbesartan, Azilsartan, Olmesartan, Eprosartan, Candesartan and Telmisartan.
In addition, the Group has completed 4 registration enabling clinical studies, namely Azilsartan Phase III clinical study, Azilsartan bioequivalence study, Natulan clinical study and Leuprorelin Pharmacokinetic/Pharmacodynamic ("PK/PD") study.
Azilsartan reduced TNF-[alpha] and IL-1[beta] levels, increased IL-10 levels and upregulated VEGF, FGF, KGF, and TGF-[alpha] in an oral mucositis model.
"Valsartan falls under a class of medication called angiotensin II receptor blocker (ARBs) and the other drugs in this class are losartan, candesartan, azilsartan, eprosartan, irbesartan, telmisartan and olmesartan.
(7) Amlodipine, chlorthalidone, and azilsartan medoxomil, all of which have long half-lives, are approximately 50% more potent than other antihypertensive agents.
Azilsartan medoxomil, a new [AT.sub.1] receptor antagonist, induces Akt phosphorylation and glucose uptake in Sprague-Dawley rats [104].
Common ARBs used to manage HTN include azilsartan (Edarbi[R]), candesartan (Atacand[R]), eprosartan (Teveten[R]), irbesartan (Avapro[R]), losartan (Cozaar[R]), olmesartan (Benicar[R]), telmisartan (Micardis[R]), and valsartan (Diovan[R]).
Imig, "Azilsartan improves glycemic status and reduces kidney damage in zucker diabetic fatty rats," The American Journal of Hypertension, vol.
A rise in the prevalence of hypertension, from a population of 181 million to 190 million, combined with the anticipated launches of azilsartan with amlodipine and AHU377 with valsartan, will also contribute."