Search for drugs:

ALISKIREN HEMIFUMARATE


DIR Classification


Classification:Less-DIR concern
Severity Score:1

Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF

  • ADVERSE REACTIONS
  • Clinical Trials Experience
  • Clinical Laboratory Findings
  • In controlled clinical trials, clinically relevant changes in standard laboratory parameters were rarely associated with the administration of Tekturna in patients with hypertension not concomitantly treated with an ARB or ACEI. In multiple-dose studies in hypertensive patients, Tekturna had no clinically important effects on total cholesterol, HDL, fasting triglycerides, or fasting glucose.
  • Blood Urea Nitrogen, Creatinine: In patients with hypertension not concomitantly treated with an ARB or ACEI, minor increases in blood urea nitrogen (BUN) or serum creatinine were observed in less than 7% of patients treated with Tekturna alone versus 6% on placebo [see Warnings and Precautions (5.2)].
  • Hemoglobin and Hematocrit: Small decreases in hemoglobin and hematocrit (mean decreases of approximately 0.08 g/dL and 0.16 volume percent, respectively, for all aliskiren monotherapy) were observed. The decreases were dose-related and were 0.24 g/dL and 0.79 volume percent for 600 mg daily. This effect is also seen with other agents acting on the renin angiotensin system, such as angiotensin inhibitors and ARBs and may be mediated by reduction of angiotensin II which stimulates erythropoietin production via the AT1 receptor. These decreases led to slight increases in rates of anemia with aliskiren compared to placebo were observed (0.1% for any aliskiren use, 0.3% for aliskiren 600 mg daily, versus 0% for placebo). No patients discontinued therapy due to anemia.
  • Serum Potassium: In patients with hypertension not concomitantly treated with an ARB or ACEI, increases in serum potassium greater than 5.5 mEq/L were infrequent (0.9% compared to 0.6% with placebo) [see Contraindications (4) and Warnings and Precautions (5.6)].
  • Serum Uric Acid: Aliskiren monotherapy produced small median increases in serum uric acid levels (about 6 micromol/L) while HCTZ produced larger increases (about 30 micromol/L). The combination of aliskiren with HCTZ appears to be additive (about 40 micromol/L increase). The increases in uric acid appear to lead to slight increases in uric acid-related AEs: elevated uric acid (0.4% versus 0.1%), gout (0.2% versus. 0.1%), and renal stones (0.2% versus 0%).
  • Creatine Kinase: Increases in creatine kinase of greater than 300% were recorded in about 1% of aliskiren monotherapy patients versus 0.5% of placebo patients. Five cases of creatine kinase rises, 3 leading to discontinuation and 1 diagnosed as subclinical rhabdomyolysis, and another as myositis, were reported as adverse events with aliskiren use in the clinical trials. No cases were associated with renal dysfunction.

Postmarketing Surveillance

Contingency Table:

Current Drug
Other Drugs
Rhabdomyolysis
18
42894
Other ADRs
8255
14109024

Odds Ratio = 0.718

Drug Property Information



ATC Code(s):
  • C09DX02 - aliskiren hemifumarate
    • C09DX -
    • C09D - "ANGIOTENSIN II ANTAGONISTS, COMBINATIONS"
    • C09 - AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C - CARDIOVASCULAR SYSTEM
  • C09XA02 - aliskiren hemifumarate
    • C09XA - Renin-inhibitors
    • C09X - OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C09 - AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C - CARDIOVASCULAR SYSTEM
  • C09XA52 - aliskiren hemifumarate
    • C09XA - Renin-inhibitors
    • C09X - OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C09 - AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C - CARDIOVASCULAR SYSTEM
  • C09XA53 - aliskiren hemifumarate
    • C09XA - Renin-inhibitors
    • C09X - OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C09 - AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C - CARDIOVASCULAR SYSTEM
  • C09XA54 - aliskiren hemifumarate
    • C09XA - Renin-inhibitors
    • C09X - OTHER AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C09 - AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
    • C - CARDIOVASCULAR SYSTEM
Active Ingredient:aliskiren hemifumarate
Active Ingredient UNII:C8A0P8G029
Drugbank ID:DB09026
PubChem Compound:5493444
CAS Number:173334-57-1
Dosage Form(s):tablet, film coated
Route(s) Of Administrator:oral
Daily Dose:
  • 150.0 mg/day C09XA02
Chemical Structure:
SMILE Code:
CC(C)[C@@H](CC1=CC(=C(C=C1)OC)OCCCOC)C[C@@H]([C@H](C[C@@H](C(C)C)C(=O)NCC(C)(C)C(=O)N)O)N

Reference

COHORT STUDY:

N/A

OTHER REFERENCE(S):

N/A

Disclaimer:

The content of this database of rhabdomyolysis is intended for educational and scientific research purposes only. It is not intended as a substitute for professional medical advice, diagnosis or treatment.

The views presented in this website do not necessarily reflect current or future opinion or policy of the US Food and Drug Administration. Any mention of commercial products is for clarification and not intended as endorsement.