Aliskiren

Indications

Aliskiren is used for: Hypertension

Adult Dose

Oral Essential hypertension Adult: >18 yr 150 mg once daily, increased to 300 mg once daily if needed. Elderly: No dosage adjustment needed. Hepatic impairment: No dosage adjustment needed.

Child Dose

Renal Dose

Renal Impairment Mild to moderate: No dosage adjustment needed. Severe: Contraindicated.

Administration

Administration May be taken with or without food. Take consistently w/ or w/o meals. Avoid taking w/ high fat meals.

Contra Indications

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.

Precautions

Serious CHF, sodium or volume depletion. Discontinue if diarrhoea is severe and persistent. Lactation. Monitoring Parameters Periodically monitor serum potassium concentration and renal function. Discontinue as soon as possible when pregnancy is detected; affects renin-angiotensin system causing oligohydramnios, which may result in fetal injury and/or death. Lactation: Excretion in milk unknown/not recommended.

Pregnancy-Lactation

C (1st trimester), D (2nd & 3rd trimesters)

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.

Adverse Effects

Side effects of Aliskiren : 1-10% Diarrhea (2.3%),Cough (1.1%),Rash (1%),Increase in serum creatinine (<7%),Hyperkalemia (<1%) <1% Angioedema,Headache,Gout,Renal stones,Seizure,Severe hypotension,Rhabomyolysis,Toxic epidermal necrolysis,Increase in uric acid,Angina Potentially Fatal: Anaphylactic reactions.

Mechanism of Action

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 .