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Aliskiren


Generic Medicine Info
Indications and Dosage
Oral
Hypertension
Adult: As monotherapy or in combination with other antihypertensive agents: Initially, 150 mg once daily, may be increased to 300 mg once daily if necessary.
Child: ≥6 years weighing ≥50 kg: Same as adult dose. Dosage recommendations may vary among individual products or between countries (refer to specific product or local guidelines).
What are the brands available for Aliskiren in Hong Kong?
  • Rasilez
Renal Impairment
Severe (GFR <30 mL/min/1.73 m2): Not recommended.
Administration
Aliskiren May be taken with or without food. Do not take w/ high-fat meal to avoid decrease in absorption.
Contraindications
History of angioedema with aliskiren; hereditary or idiopathic angioedema. Concomitant use with ACE inhibitors or angiotensin II receptor blockers (ARBs) in patients with diabetes mellitus or renal impairment (GFR <60 mL/min/1.73 m2). Children <2 years. Pregnancy.
Special Precautions
Patient with marked volume or salt depletion, unilateral or bilateral renal artery stenosis, severe congestive heart failure, post-MI, diabetes; history of angioedema (of any aetiology) and airway surgery. Renal impairment. Children (≥6 years). Lactation.
Adverse Reactions
Significant: Hyperkalaemia, hypersensitivity reactions (e.g. anaphylaxis, angioedema); symptomatic hypotension; changes in renal function, including acute renal failure.
Cardiac disorders: Palpitations.
Gastrointestinal disorders: Diarrhoea, oral mucosal reactions.
General disorders and administration site conditions: Peripheral oedema.
Investigations: Increased creatine phosphokinase, serum creatinine and BUN.
Musculoskeletal and connective tissue disorders: Arthralgia.
Nervous system disorders: Dizziness.
Respiratory, thoracic and mediastinal disorders: Cough.
Skin and subcutaneous tissue disorders: Rash, pruritus, urticaria, severe cutaneous adverse reactions (e.g. Stevens-Johnson syndrome, toxic epidermal necrolysis).
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Correct volume or salt depletion prior to initiation of therapy. Monitor blood pressure, serum K levels, BUN, and serum creatinine periodically. Closely monitor for symptomatic hypotension and for signs of hypersensitivity reactions (including angioedema) at treatment initiation, during dose adjustments, and regularly during treatment.
Overdosage
Symptom: Hypotension. Management: Supportive treatment.
Drug Interactions
Increased risk of hypotension, hyperkalaemia, syncope, and decreased renal function (including acute renal failure) with ACE inhibitors or ARBs. Increased risk of hyperkalaemia with K-sparing diuretics, K supplements, K-containing salt substitutes, and heparin. Significantly increased serum concentration with potent P-gp inhibitors (e.g. ciclosporin, itraconazole); avoid concomitant use. May increase serum levels with moderate P-gp inhibitors (e.g. ketoconazole, verapamil). May reduce the antihypertensive effect and increase the risk of deteriorating renal function with NSAIDs. May decrease the serum concentration of furosemide and torasemide.
Food Interaction
Decreased absorption with high-fat meals. Significantly decreased serum concentration with orange, apple, and grapefruit juice.
Lab Interference
May result in false-positive or false-negative aldosterone/renin (ARR) ratio.
Action
Description:
Mechanism of Action: Aliskiren is an active, potent and selective non-peptide renin inhibitor. It directly reduces plasma renin activity, thereby inhibiting the conversion of angiotensinogen to angiotensin I, then subsequently blocking the production of angiotensin II and aldosterone.
Onset: Maximum hypertensive effect: Within 2 weeks.
Pharmacokinetics:
Absorption: Poorly absorbed from the gastrointestinal tract. Decreased absorption with high-fat meals. Bioavailability: Approx 3%. Time to peak plasma concentration: Approx 1-3 hours.
Distribution: Plasma protein binding: Approx 50%.
Metabolism: Minimally metabolised in the liver by CYP3A4 isoenzyme.
Excretion: Mainly via faeces (as unchanged drug via bile); urine (approx 25% as unchanged drug). Elimination half-life: Approx 24-40 hours.
Chemical Structure

Chemical Structure Image
Aliskiren

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5493444, Aliskiren. https://pubchem.ncbi.nlm.nih.gov/compound/Aliskiren. Accessed Oct. 25, 2024.

Storage
Store between 20-25°C. Protect from moisture.
MIMS Class
ACE Inhibitors/Direct Renin Inhibitors
ATC Classification
C09XA02 - aliskiren ; Belongs to the class of renin-inhibitors. Used in the treatment of cardiovascular disease.
References
Aliskiren. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 01/10/2024.

Anon. Aliskiren. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 01/10/2024.

Brayfield A, Cadart C (eds). Aliskiren Fumarate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2024.

Joint Formulary Committee. Aliskiren. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 01/10/2024.

Rasilez 150 mg Film-coated Tablets (Noden Pharma DAC). MHRA. https://products.mhra.gov.uk. Accessed 01/10/2024.

Tekturna Tablet, Film Coated (LXO US Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 01/10/2024.

Disclaimer: This information is independently developed by MIMS based on Aliskiren from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2025 MIMS. All rights reserved. Powered by MIMS.com
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