Aliskiren fumarate


Concise Prescribing Info
Indications/Uses
HTN.
Dosage/Direction for Use
Adult : PO 150 mg once daily, increased to 300 mg once daily if needed.
Dosage Details
Oral
Essential hypertension
Adult: ≥18 yr 150 mg once daily, increased to 300 mg once daily if needed.
Elderly: No dosage adjustment needed.
Renal Impairment
Mild to moderate: No dosage adjustment needed. Severe: Contraindicated.
Hepatic Impairment
No dosage adjustment needed.
Administration
May be taken with or without food. Take consistently w/ or w/o meals. Avoid taking w/ high fat meals.
Contraindications
History of angioedema; severe renal impairment. Concomitant use w/ ACE inhibitors or angiotensin II receptor antagonists in patients w/ DM and renal impairment (GFR <60 mL/min). Concomitant use w/ ciclosporin, itraconazole and quinidine. Pregnancy.
Special Precautions
Serious CHF, sodium or volume depletion. Discontinue if diarrhoea is severe and persistent. Lactation.
Adverse Reactions
Diarrhoea, dyspepsia, GERD, abdominal pain, hypotension, headache, fatigue, dizziness, back pain, cough, rashes, hyperuricaemia, gout, renal calculi, hyperkalaemia, decreases in Hb levels (dose-related), angioedema and seizures.
Potentially Fatal: Anaphylactic reactions.
MonitoringParameters
Periodically monitor serum potassium concentration and renal function.
Overdosage
Symptoms: Hypotension. Management: Supportive treatment.
Drug Interactions
Increased risk of hypotension w/ other antihypertensives. Increased risk of acute renal failure w/ ACE inhibitors, angiotensin II receptor antagonists or NSAIDs. Antihypertensive effect may be reduced w/ NSAIDs. Increased serum levels w/ atorvastatin, itraconazole, ketoconazole, verapamil. Significant decrease in furosemide concentrations w/ aliskiren. Increased risk of hyperkalaemia w/ potassium-sparing diuretics, potassium supplements or any substances that may increase serum potassium levels.
Potentially Fatal: Increased risk of renal impairment, hypotension and hyperkalaemia w/ ACE inhibitors or angiotensin II receptor antagonists. Markedly increased plasma concentration w/ ciclosporin, itraconazole and quinidine.
Food Interaction
Avoid concomitant use w/ grapefruit juice. May decrease bioavailability w/ St John's wort.
Action
Description: Aliskiren is an orally active, potent, non-peptide and selective direct renin inhibitor used in the management of HTN. By inhibiting the enzyme renin, it prevents conversion of angiotensinogen into angiotensin I and therefore inhibits subsequent production of angiotensin II and aldosterone. Unlike ACE inhibitors and angiotensin II receptor antagonists which cause a compensatory rise in plasma renin activity, treatment w/ aliskiren decreases plasma renin activity and concentrations of angiotensin I, angiotensin II and aldosterone.
Pharmacokinetics:
Absorption: Poorly absorbed from GI tract. Absorption is reduced when taken w/ high fat diet. Bioavailability: Approx 2.5%. Time to peak plasma concentration: 1-3 hr.
Distribution: Distributes extensively into extravascular space. Plasma protein binding: Approx 50%.
Metabolism: Minimal metabolism via CYP3A4 isoenzyme.
Excretion: Mainly in the faeces (via the bile) and urine (approx 25% of absorbed dose) as unchanged drug. Elimination half-life: Approx 24-40 hr.
Storage
Store between 15-30°C.
Disclaimer: This information is independently developed by MIMS based on Aliskiren fumarate 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 © 2020 MIMS. All rights reserved. Powered by MIMS.com
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