azilsartan

Contraindicated in:

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

Potassium-sparing diuretics, potassium-containing salt substitutes, or potassium supplements may ↑ risk of hyperkalemia.
↑risk of hyperkalemia, renal dysfunction, hypotension, and syncope with 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 impairment.
↑antihypertensive effect with other antihypertensives or diuretics.
May ↑ levels and risk of lithium toxicity.

Availability ⬆ ⬇

(Generic available)

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

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.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

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.

Classifications ⬆ ⬇

Therapeutic Classification: antihypertensives

Pharmacologic Classification: angiotensin II receptor antagonists

Pharmacokinetics ⬆ ⬇

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

Distribution: Well distributed to tissues.

Protein Binding: ≥99%.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP2C9 isoenzyme. 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

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 provider. 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 ↓, low-sodium diet, smoking cessation, moderation of alcohol consumption, regular exercise, 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 ↓ 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 provider of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care provider before taking any new medications, especially NSAIDs and cough, cold, or allergy medications.
Instruct patient to notify health care provider of medication regimen before treatment or surgery.
May cause fetal harm. Advise women of reproductive potential to use effective contraception, notify health care provider immediately if pregnancy is planned or suspected, and 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 BP 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.

section name header

Indications ⬇

Contraind./Precautions ⬆ ⬇