Aliskiren

INTRODUCTION

Indications

Treatment of hypertension (alone or with other agents).

Action

Inhibition of renin results in decreased formation of angiotensin II, a powerful vasoconstrictor. Therapeutic Effects: Decreased blood pressure.

Adverse Reactions/Side Effects

Resp: cough. GI: abdominal pain, diarrhea ↑ (in females and elderly), dyspepsia, reflux. Misc: ANGIOEDEMA.

PHYSICAL THERAPY IMPLICATIONS

Examination and Evaluation

• Monitor signs of angioedema including rashes, raised patches of red or white skin (welts), burning/itching skin, swelling in the face, and difficulty breathing. Notify physician of these signs immediately.

• Assess blood pressure periodically, and compare to normal values (see Appendix F) to help document antihypertensive effects.

Interventions

• Avoid physical therapy interventions that cause systemic vasodilation (large whirlpool, Hubbard tank). Additive effects of this drug and the intervention may cause a dangerous fall in blood pressure.

Patient/Client-Related Instruction

• Remind patients to take medication as directed to control hypertension even if they are asymptomatic.

• Counsel patients about additional interventions to help control blood pressure, including regular exercise, weight loss, sodium restriction, stress reduction, moderation of alcohol consumption, and smoking cessation.

• Instruct patient to notify physician of a prolonged dry cough; drug therapy may need to be altered to resolve this side effect.

• Instruct patient or family/caregivers to report severe or prolonged GI problems such as diarrhea, indigestion, heartburn, and abdominal pain.

Pharmacokinetics

Absorption: Poorly absorbed (bioavailability 2.5%).

Distribution: Unknown.

Metabolism and Excretion: 2% excreted unchanged in urine, remainder is probably metabolized (CYP3A4 enzyme system).

Half-life: 24 hr.

Contraindications/Precautions

Contraindicated in: Hypersensitivity; OB: May cause fetal injury or death; Concurrent use with cyclosporine.

Use Cautiously in: Salt or volume depletion (correct before use); Severe renal impairment; Pedi: Safety not established.

Interactions

Drug-Drug: Blood levels are ↓ by irbesartan. Blood levels are ↑ by atorvastatin, ketoconazole, and cyclosporine (concurrent use with cyclosporine not recommended). ↓ blood levels and may ↓ effects of furosemide. Antihypertensive effects may be ↑ by other antihypertensives, diuretics, and nitrates. ↑ risk of hyperkalemia with concurrent use of ACE inhibitors, angiotensin II receptor antagonists, potassium supplements, potassium-sparing diuretics, or potassium-containing salt substitutes.

Drug-Food: High-fat meals significantly ↓ absorption.

Route/Dosage

PO (Adults): 150 mg/day initially; may be increased to 300 ...