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ALISKIREN

 ALISKIREN


BRAND NAME:- RASILEZ 150mg tab; RASILEZ-HC : along with hydrochlorothiazide


ALISKIREN is a direct renin inhibitors (DRIs) are the latest class of RSA inhibitory drugs, of which only one member Aliskiren has become available for the treatment of cardiovascular and renal diseases in which ACE inhibitors and ARBs are currently used.



 MECHANISM OF ACTION:-

Aliskiren is a nonpeptide which binds selectively to the catalytic site of renin and competitively blocks the access of angiotensinogen to this site –> Ang I is not produced and the chain of RSA is interrupted. While the concentration of renin in plasma is increased by feed back, the plasma renin activity (PRA) is  decreased. Ang I and II levels fall.

Aliskiren causes fall in BP which is more marked in the Na+ depleted subjects with High basal PRA . Similar to ACE inhibitors, plasma Aldosterone levels are lowered accompanied by mild natriuresis and a tendency to K+ retention. The antihypertensive  efficacy of Aliskiren is equivalent to that of ACE inhibitors or ARBs. Combination of these drug with Aliskiren produces greater fall in BP ,at least in the short term. This may be due to blockade of rise in PRA caused by ACE inhibitors/ ARBs. The pattern of haemodynamic effects of Aliskiren resembles ACEC  inhibitors; postural hypotension is not a problem.



OTHER INFORMATION:-

Trails so far have shown that Aliskiren can reduce hypertensive left ventricular hypertrophy and benefit CHF patients, but its value compared to ACE inhibitors/ARBs as monotherapy and as additional drug remains to be determined. Aliskiren has renoprotective effects as well in hypertension and diabetic mellitus . Its long- trem benefits and comparative position in relation to ACE inhibitors/ARBs is being evaluated.

At present, Aliskiren is recommended as an alternative antihypertensive drug and in combination with others for greater BP lowering.



PHARMACOKINETICS:- Aliskiren is administered orally,but bioavailability is very low due to active extrusion of absorbed drug by P- glycoprotein. The drug is mainly eliminated in faeces ; small amount in urine. The plasma t½ is > 24 hours, and its BP lowering effects persists for day's after regular intake.


ADVERSE EFFECTS:- Aliskiren produces few and mild effects —mainly dyspepsia, abdominal pain,loose motion, headache, dizziness. 

Acute hypotension, hyperkalemia,cough, angioedema and rashes are much less frequent than with ACE inhibitors. Aliskiren is contraindicated during pregnancy.


DOSE:- 150-300mg OD 


USE:-

Treatment of cardiovascular and renal diseases.






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