Aliskiren

Revision as of 15:58, 1 July 2019 by Rossdonaldson1 (talk | contribs) (Administration)

Administration

  • Type: Antihypertensive
  • Dosage Forms: 150mg, 300mg
  • Routes of Administration: Oral
  • Common Trade Names: Tekturna, Rasilez

Adult Dosing

Hypertension

  • 150-300 mg PO qd

Pediatric Dosing

Safety/efficacy not established in pediatric patients

Special Populations

Renal Dosing

  • Adult:
    • CrCl > 30: No adjustment
    • CrCl < 30: Not Definied
    • HD/PD: No Supplement
  • Pediatric: Safety/efficacy not established in pediatric patients

Hepatic Dosing

  • Adult: No adjustment
  • Pediatric: Safety/efficacy not established in pediatric patients

Contraindications

  • Allergy to class/drug
  • Pregnancy

Adverse Reactions

Serious

Common

Pharmacology

  • Half-life: 24h
  • Metabolism: Liver partially; 3A4 substrate
  • Excretion: Urine (25% unchanged)

Mechanism of Action

  • Decreases plasma renin activity via direct inhibition
  • Interferes with conversion of angiotensinogen to angiotensin I

Comments

See Also

References

  • Funder JW, Carey RM, Mantero F, et al. The management of primary aldosteronism: case detection, diagnosis, and treatment: an Endocrine Society Clinical Practice Guideline. J Clin Endocrinol Metab. 2016;101(5):1889-1916. doi: 10.1210/jc.2015-4061. [PubMed 26934393]
  • Go AS, Bauman M, King SM, et al. An effective approach to high blood pressure control: a science advisory from the American Heart Association, the American College of Cardiology, and the Centers for Disease Control and Prevention [published online November 15, 2013]. Hypertension. [PubMed 24243703]
  • Khadzhynov D, Slowinski T, Lieker I, et al, "Pharmacokinetics of Aliskiren in Patients With End-Stage Renal Disease Undergoing Haemodialysis," Clin Pharmacokinet, 2012, 51(10):661-9. [PubMed 23018529]
  • Parving HH, Persson F, Lewis JB, et al, “Aliskiren Combined With Losartan in Type 2 Diabetes and Nephropathy,” N Engl J Med, 2008, 358(23):2433-46. [PubMed 18525041]
  • Rasilez (aliskiren) [product monograph]. Dorval, Quebec, Canada: Novartis Pharmaceuticals Canada Inc; January 2018.
  • Straessen JA, Li Y, and Richart T, “Oral Renin Inhibitors,” Lancet, 2006, 368(9545):1449-56. [PubMed 17055947]
  • Tekturna (aliskiren) [prescribing information]. Boston, MA: Noden Pharma USA Inc; November 2017.
  • Vaidyanathan S, Bigler H, Yeh C, et al, “Pharmacokinetics of the Oral Direct Renin Inhibitor Aliskiren Alone and in Combination with Irbesartan in Renal Impairment,” Clin Pharmacokinet, 2007, 46(8):661-75. [PubMed 17655373]
  • Vaidyanathan S, Warren V, Yeh C, et al, “Pharmacokinetics, Safety, and Tolerability of the Oral Renin Inhibitor Aliskiren in Patients With Hepatic Impairment,” J Clin Pharmacol, 2007, 47(2):192-200. [PubMed 17244770]
  • Weber MA, Schiffrin EL, White WB, et al. Clinical Practice Guidelines for the Management of Hypertension in the community: a statement by the American Society of Hypertension and the International Society of Hypertension. J Clin Hyperten (Greenwich). 2014;16(1):14-26. [PubMed 24341872]
  • Whelton PK, Carey RM, Aronow WS, et al. 2017 ACC/AHA/AAPA/ABC/ACPM/AGS/APhA/ASH/ASPC/NMA/PCNA guideline for the prevention, detection, evaluation, and management of high blood pressure in adults: a report of the American College of Cardiology/American Heart Association Task Force on Clinical Practice Guidelines [published online ahead of print on November 13, 2017.]. Hypertension. 2017. doi: 10.1161/HYP.0000000000000065. [PubMed 29133356]