Aliren is a direct renin inhibitor, resulting in blockade of the conversion of angiotensinogen to angiotensin I. Angiotensin I suppression decreases the formation of angiotensin II (Ang II), a potent blood pressure-elevating peptide (via direct vasoconstriction, aldosterone release, and sodium retention). Ang II also functions within the Renin-Angiotensin-Aldosterone System (RAAS) as a negative inhibitory feedback mediator within the renal parenchyma to suppress the further release of renin. Thus, reductions in Ang II levels suppress this feedback loop, leading to further increased plasma renin concentrations (PRC) and subsequent activity (PRA). This disinhibition effect can be potentially problematic for ACE inhibitor and ARB therapy, as increased PRA could partially overcome the pharmacologic inhibition of the RAAS. As aliskiren is a direct inhibitor of renin activity, blunting of PRA despite the increased PRC (from loss of the negative feedback) may be clinically advantageous. The effect of aliskiren on bradykinin levels is unknown.
Treating high blood pressure. It may be used alone or with other medicines. Aliren is a direct renin inhibitor. It works by relaxing blood vessels, which lowers blood pressure and helps the heart to pump blood more easily.
Aliren is also used to associated treatment for these conditions: High Blood Pressure (Hypertension)
|Other Names||Aliskiren, Aliskireno|
The plasma protein binding of aliskiren ranges from 47-51%.
|Therapeutic Class||Direct Renin Inhibitors|
|Manufacturer||Opsonin Pharma Ltd|
|Last Updated:||June 23, 2021 at 11:16 am|
Table Of contents
Initial adult dose: 150 mg orally once a day.
Maintenance adult dose: The dosage may be increased to 300 mg daily if blood pressure is not adequately controlled. No dosage adjustment is recommended based on gender, age, body weight or race.
Safety and efficacy have not been established in patients younger than 18 years. AUC is increased in elderly patients 65 years of age and older.
Skin rash (1%), Diarrhea (2%), Increased creatine phosphokinase, Increased blood urea nitrogen (≤7%), increased serum creatinine (≤7%), RespirCough (1%)
Limited to important or life-threatening: Anaphylaxis, decreased hematocrit, decreased hemoglobin, gastroesophageal reflux disease, hepatic insufficiency, hyperkalemia, increased uric acid, nausea, rhabdomyolysis, seizure, severe hypotension, Stevens-Johnson syndrome, tonic-clonic seizures, vomiting
Major: Highly clinically significant. Avoid combinations; the risk of the interaction outweighs the benefit.
Moderate: Moderately clinically significant. Usually avoid combinations; use it only under special circumstances.
Minor: Minimally clinically significant. Minimize risk; assess risk and consider an alternative drug, take steps to circumvent the interaction risk and/or institute a monitoring plan.
- Do not take with or immediately after a high-fat meal. The absorption of aliskiren is substantially reduced by taking it with high-fat meals.
- Take with or without food. Take consistently at the same time in regard to meals.
Volume of Distribution
Unchanged aliskiren accounts for about 80% of the drug found in the plasma.
Plasma half-life for aliskiren can range from 30 to 40 hours with an accumulation half-life of about 24 hours.
Aliren is partially cleared in the kidneys, and safety data have not been established for patients with a creatinine clearance of less than 30 mL/min. One pharmacokinetic study revealed an average renal clearance of 1280 +/- 500 mL/hour in healthy volunteers.
Pregnancy & Breastfeeding use
If pregnancy is detected, discontinue aliskiren as soon as possible. Drugs that act directly on the renin-angiotensin system can cause injury and death to the developing fetus.
Hypersensitivity to aliskiren or any component of the formulation; concomitant use with an ACE inhibitor or ARB in patients with diabetes mellitus History of angioedema with aliskiren, ACE inhibitors, or ARBs; hereditary or idiopathic angioedema; pregnancy, breast-feeding; concomitant use with ACE inhibitors or ARBs in patients with GFR <60 mL/minute/1.73 m2; patients <2 years of age.
Renal Dose Adjustments:
- Mild to moderate renal dysfunction (CrCl 30 mL/min or greater): No adjustment recommended.
- Severe renal dysfunction (CrCl 30 mL/min or less): Not recommended
Liver Dose Adjustments
: No adjustment recommended
Store aliskiren at room temperature, between 15° to 30° C. Store in the original bottle, away from heat, moisture, and light. Keep aliskiren out of the reach of children and away from pets.