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Aliskiren

Antihypertensive

Antihypertensive
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
12 major
incl. contraindicated
PREGNANCY
X
FDA category + note
Top interactionssee all 12
  • AzilsartanContraindicatedTextbookG&G 14e · p603
  • Losartan + HydrochlorothiazideContraindicatedTextbookG&G 14e · p603
  • Olmesartan + AmlodipineContraindicatedTextbookG&G 14e · p603
  • Olmesartan + HydrochlorothiazideContraindicatedTextbookG&G 14e · p603

Mechanism

Aliskiren is a direct renin inhibitor that blocks the rate-limiting step in angiotensin II (AngII) production. It is licensed for the treatment of hypertension.

Indications

HypertensionCongestive heart failure (CHF)Renoprotection in hypertensionRenoprotection in diabetes mellitus

Dosing

Renal adjustment
Contraindicated in combination with an ACE inhibitor for patients with eGFR less than 60 mL/minute/1.73 m2

Pharmacokinetics

Peak effect
3 to 6 h
Duration
BP lowering effect persists for days after regular intake
Half-life
20 to 45 h
Bioavailability
low (~2.5%)
Protein binding
50%
Metabolism
Hepatic metabolism is minimal.
Excretion
Elimination is mostly as unchanged drug in feces; approximately 25% of the absorbed dose appears in the urine as the parent drug.

Contraindications

  • Concomitant use with an ACE inhibitor in patients with an eGFR less than 60 mL/minute/1.73 m2
  • Concomitant use with an ACE inhibitor in patients with diabetes mellitus
  • Concomitant use with an angiotensin-II receptor antagonist (due to increased risk of hyperkalaemia, hypotension, and renal impairment compared to single drug use)
  • Pregnancy
  • Combination with other RAS inhibitors

Side effects

Common
diarrheaabdominal paindyspepsiagastroesophageal refluxheadachedizzinessfatigueupper respiratory tract infectionback painangioedemacoughrashhypotensionelevated uric acidrenal stonesgoutDiarrhea (especially at higher doses)Loose motions
Serious
  • hyperkalemia in diabetics on combination therapy
  • Angioedema
  • Increased cardiovascular events (in combination with ARB/ACE inhibitor)
  • Renal worsening (in combination with ARB/ACE inhibitor)
  • Hypotension (in combination with ARB/ACE inhibitor)
  • Hyperkalemia (in combination with ARB/ACE inhibitor)
  • Acute hypotension (much less frequent than ACEIs)
  • Hyperkalaemia (much less frequent than ACEIs)
  • Cough (much less frequent than ACEIs)
  • Angioedema (much less frequent than ACEIs)
  • Rashes (much less frequent than ACEIs)

Pregnancy & lactation

Pregnancy

X

Drug interactions

Azilsartan
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Losartan + Hydrochlorothiazide
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Olmesartan + Amlodipine
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Olmesartan + Hydrochlorothiazide
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Sacubitril With Valsartan
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Telmisartan + Amlodipine
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Telmisartan + Amlodipine + Hydrochlorothiazide
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Telmisartan + Chlorthalidone
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Telmisartan + Hydrochlorothiazide
Contraindicated
Textbook

Increased risk of hypotension, hyperkalemia, and renal impairment.

Avoid concomitant use.

Source: G&G 14e · p603

Benazepril
Contraindicated
Database

Dual RAAS blockade

Avoid combination

Source: Kimi deep-research + Cla

Candesartan
Contraindicated
Database

Dual RAAS blockade → hyperkalaemia/AKI/hypotension

Do not combine in diabetes/eGFR <60

Source: Kimi deep-research + Cla · p603

Irbesartan
Contraindicated
Database

Dual RAAS blockade → hyperkalaemia/AKI/hypotension

Do not combine in diabetes or eGFR <60

Source: Kimi deep-research + Cla

Related guidelines

Other Antihypertensive drugs

Ask House about Aliskiren

Continue into a citation-backed clinical answer with the drug context already attached.

Sources: KD Tripathi 7e, Goodman & Gilman 14e, Katzung, BNF·Verified: 2026-05-10 · House clinical team