azilsartan

Absorption: Azilsartan medoxomil, a prodrug, is hydrolyzed in the GI tract to azilsartan, the active component. 60% is absorbed from the GI tract.

Distribution: Approximately 16 L.

Protein Binding: ≥99%.

Metabolism/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)

ROUTE	ONSET	PEAK	DURATION
PO	within 2 hr	18 hr	24 hr

Contraind./Precautions ⬆ ⬇

Contraindicated in:

Concurrent use with aliskiren-containing products in patients with diabetes or moderate-to-severe renal impairment (CCr <60 mL/min)
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

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;
Rep: Woman of reproductive potential;
Pedi: Safety and effectiveness not established in children;
Geri: Older adults may have greater sensitivity, especially to adverse renal effects.

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypotension

F and E: hyperkalemia

GI: diarrhea, nausea

GU: renal impairment

MS: muscle spasm

Neuro: dizziness, fatigue, weakness

Interactions ⬆ ⬇

Drug-drug:

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/min
NSAIDs and selective COX-2 inhibitors may blunt the antihypertensive effect and ↑ the risk of renal dysfunction.
↑antihypertensive effect with other antihypertensives or diuretics.
May ↑ levels and may ↑ the risk of lithium toxicity.

Route/Dosage ⬆ ⬇

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

Availability ⬆ ⬇

(Generic available)

Tablets: 40 mg; 80 mg
In combination with: chlorthalidone (Edarbyclor). See Appendix [not included in this PDA edition].

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.

Implementation ⬆ ⬇

Correct volume and salt depletion, if possible, before initiation of therapy, or start treatment at 40 mg.
PO: 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. Advise patient to read Patient Information before starting and with each Rx refill in case of changes.
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.
Rep: May cause fetal harm. Advise females of reproductive potential to use effective contraception and notify health care professional immediately if pregnancy is planned or suspected, and to avoid breastfeeding. Azilsartan should be discontinued as soon as possible when pregnancy is detected. Conduct serial ultrasound exams in pregnant patients exposed to azilsartan; may cause oligohydramnios. Monitor infants exposed to azilsartan in utero for hypotension, oliguria, and hyperkalemia. If oliguria or hypotension occurs, support blood pressure and renal perfusion. Exchange transfusions or dialysis may be required as a means of reversing hypotension and/or substituting for disordered renal function.
Emphasize the importance of follow-up exams to evaluate effectiveness of medication.

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇