azilsartan

azilsartan

(a-zill-sar-tan) ,

Edarbi

(trade name)

Classification

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

Indications

Treatment of hypertension, alone or with other agents.

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.

Pharmacokinetics

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)

ROUTEONSETPEAKDURATION
POwithin 2 hr18 hr24 hr

Contraindications/Precautions

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

Cardiovascular

  • hypotension (most frequent)

Fluid and Electrolyte

  • hyperkalemia

Gastrointestinal

  • diarrhea (most frequent)
  • nausea

Genitourinary

  • impaired renal function

Musculoskeletal

  • muscle spasm

Interactions

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.

Route/Dosage

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

Availability

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)

Implementation

  • 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.
References in periodicals archive ?
The most commonly prescribed drugs in the CCB class are amlodipine and lercanidipine, while the leading ARBs are telmisartan, candesartan, olmesartan, irbesartan, losartan, valsartan, azilsartan medoxomil, and eprosartan.
Zacras is a tablet taken orally once daily and has two dosage strengths, ZacrasA Combination Tablets LD and ZacrasA Combination Tablets HD which contain 20mg azilsartan / 2.
This edition includes new drugs, including Azilsartan Medoxomil, Boceprevir, Clobazam, Ezogabine, Fidaxomicin, Linagliptin, Rilpivirine, Rivaroxaban, Telaprevir, Roflumilast, Ticagrelor, and Vilazodone; updated bisphosphonate, antipsychotic, carbapenem, and proton pump inhibitor group monographs; new combinations such as Emtricitabine/Rilpivirine/Tenofovir; and a revised ophthalmic/otic chapter with additions like glaucoma combinations, mast cell stabilizers, ophthalmic antihistamines, and otic corticosteroids.
Azilsartan (Edarbi; D) is an angiotensin II receptor blocker used for hypertension.
CONTENTS: Section 1: Executive Summary Section 2: The Current Market Leaders in T2 Diabetes Section 3: Future Competitive Threats Novel Therapeutics in Late-Stage Development Section 4: Long-Term Potential Competitive Threats Innovative Therapies in Mid-Stage Development Section 5: APPENDIX Products Mentioned: - Alogliptin (SYR-322) - Liraglutide - Saxagliptin - AGI-1067 - Exanatide LAR (exenatide) - Dapagliflozin - Balaglitazone - BI-1356 - rivoglitazone (CS-011) - AVE-0010 - R1583 - AVE-2268 - remogliflozin - PHX1149 - INT131 - albiglutide - Aleglitazar - PF-00734200 - R1579 - TAK-472 (SYR-472) - AMG-222 (ALS 2-0426) - INCB13739 - MB07803 - ISIS 113715 - AZD2207 - DIO-902 - EMD 387008 - indeglitazar - azilsartan - MBX-2044 - CJC-1134-PC - CRx-401 - K-111 - MP-513 - AKP-020 - AVE0847
EDARBYCLOR (azilsartan medoxomil and chlorthalidone) is a fixed-dose combination therapy for the treatment of hypertension that combines azilsartan medoxomil and chlorthalidone in a single tablet.
5, 2012 /PRNewswire/ -- Results of a 10-week, phase 3 study published online in the American Journal of Medicine found the clinic systolic blood pressure (SBP) reductions of a fixed-dose combination of azilsartan medoxomil and chlorthalidone were significantly greater at six and ten weeks than those of azilsartan medoxomil co-administered with hydrochlorothiazide.
June 19, 2012 /PRNewswire/ -- Results of a 12-week, head-to-head, phase 3 study published online in the American Heart Association journal Hypertension found systolic blood pressure (SBP) reductions of a fixed-dose combination of azilsartan medoxomil and chlorthalidone 40/25 mg were statistically superior to those of the fixed-dose combination of olmesartan medoxomil-hydrochlorothiazide 40/25 mg.
EDARBYCLOR is a fixed-dose combination of two medications: azilsartan medoxomil, an ARB, and chlorthalidone, a long-acting diuretic used in the treatment of hypertension.
Food and Drug Administration (FDA) for an investigational fixed-dose combination of azilsartan medoxomil plus chlorthalidone (CLD) for the treatment of hypertension, or high blood pressure.
The only innovative antihypertensive agent expected to launch by 2019 is Takeda's ARB; azilsartan medoxomil (TAK-491).