• Initial treatment of hypertension in patients unlikely to respond to a single agent.
• Treatment of hypertension in patients inadequately treated with a single drug (add-on).
• Replacement therapy in patients controlled with its individual components.

Contraindicated in:

• Severe renal impairment
• OB: Pregnancy (can cause fetal/neonatal morbidity and death).

Use Cautiously in:

• Severe hepatic impairment (titrate carefully)
• OB: Women with child-bearing potential.

Aliskiren

Resp: cough.

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

Amlodipine

CNS: headache, dizziness, fatigue.

CV: peripheral edema, angina, bradycardia, hypotension, palpitations.

GI: gingival hyperplasia, nausea.

Derm: flushing.

Drug-Drug:

• Aliskiren — .Blood levels are ↓ by irbesartan.
• Blood levels are ↑ by atorvastatin, ketoconazole, verapamil, and cyclosporine (concurrent use with cyclosporine not recommended).
• 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.
• Amlodipine — .Additive hypotension may occur when used concurrently with fentanyl, other antihypertensives, nitrates, acute ingestion of alcohol, or quinidine.
• Antihypertensive effects may be ↓ by concurrent use of nonsteroidal anti-inflammatory agents.
• May ↑ risk of neurotoxicity with lithium.

Drug-Food:

• Aliskiren — . High fat meals significantly ↓ absorption.
• Amlodipine — .Grapefruit juice↑ serum levels and effect.

• Tablets: aliskiren 150 mg/ amlodipine 5 mg; aliskiren 150 mg/ amlodipine 10 mg; aliskiren 300 mg/ amlodipine 5 mg; aliskiren 300 mg/ amlodipine 10mg;

• PO (Adults): Add-on or initial therapy — alikiren 150 mg/amlodipine, titrate up to aliskiren 300 mg/amlodipine 10 mg; replacement therapy — substitute for individual components.

Tekamlo

• Aliskiren — Inhibition of renin results in decreased formation of angiotensin II, a powerful vasoconstrictor.
• Aliskiren — Inhibits the transport of calcium into myocardial and vascular smooth muscle cells, resulting in inhibition of excitation-contraction coupling and subsequent contraction.

• Lowering of BP.

Therapeutic Classification: antihypertensives

Pharmacologic Classification: calcium channel blockers

Absorption: Absorption is significantly decreased by high fat meals; Aliskiren — Poorly absorbed (bioavailability 2.5%); Amlodipine — Well absorbed after oral administration (64–90%).

Distribution: Aliskiren — Unk; Amlodipine — Probably crosses the placenta.

Protein Binding: Amlodipine — 95–98%.

Metabolism/Excretion: Aliskiren — 2% excreted unchanged in urine, remainder is probably metabolized (CYP3A4 enzyme system); Amlodipine — Mostly metabolized by the liver.

Half-life: Aliskiren — 24 hr; Amlodipine — 30–50 hr (↑ in geriatric patients and patients with hepatic impairment).

(effect on BP)

• Instruct patient to take medication as directed at the same time each day, even if feeling better. Take missed doses as soon as remembered, but not if almost time for next dose. Do not double doses. Do not share medication with others, even with same condition; may be harmful. Advise patient to read the Patient Package Insert before starting therapy and with each Rx refill in case of changes.
• May cause lightheadedness and dizziness, especially during first days of therapy. If syncope occurs, caution patient to lie down and notify health care professional. Also, avoid driving and other activities requiring alertness until response to medication is known.
• Advise patient to report signs and symptoms of angioedema (swelling of face, extremities, eyes, lips, tongue, difficulty swallowing, or breathing) to health care professional immediately.
• 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. Advise patient not to use potassium supplements or salt substitutes containing potassium without consulting health care professional.
• Advise female patients to notify health care professional if pregnancy is planned or suspected or if breastfeeding. If pregnancy is detected, discontinue medication as soon as possible.
• Advise patient to notify health care professional of side effects that are persistent or bothersome.

a-LIS-ki-ren/am-LOE-di-peen