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Aliskiren
Systematic (IUPAC) name
(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2-methyl-
propyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)
phenyl]methyl}-8-methyl-2-propan-2-yl-nonanamide
Identifiers
CAS number 173334-57-1
ATC code C09XA02 C09XA52
PubChem 5493444
Chemical data
Formula C30H53N3O6 
Mol. mass 551. IUPAC Nomenclature is a system of naming Chemical compounds and of describing the science of Chemistry in general CAS registry numbers are unique numerical identifiers for Chemical compounds Polymers biological sequences mixtures and Alloys They are also referred to The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs It is controlled by the WHO Collaborating Centre for Drug A section of the Anatomical Therapeutic Chemical Classification System. A section of the Anatomical Therapeutic Chemical Classification System. PubChem is a Database of chemical Molecules The system is maintained by the National Center for Biotechnology Information (NCBI a component A chemical formula is a way of expressing information about the Atoms that constitute a particular Chemical compound, and how the relationship between those atoms changes Carbon (kɑɹbən is a Chemical element with the symbol C and its Atomic number is 6 Hydrogen (ˈhaɪdrədʒən is the Chemical element with Atomic number 1 Nitrogen (ˈnaɪtɹəʤɪn is a Chemical element that has the symbol N and Atomic number 7 and Atomic weight 14 Oxygen (from the Greek roots ὀξύς (oxys (acid literally "sharp" from the taste of acids and -γενής (-genēs (producer literally begetteris the The molecular mass (abbreviated m of a substance, more commonly referred to as molecular weight and abbreviated as MW, is the Mass of one 758 g/mol
Pharmacokinetic data
Bioavailability Low (approximately 2. In Pharmacology, bioavailability is used to describe the fraction of an administered Dose of unchanged drug that reaches the Systemic circulation, one of 5%)
Metabolism Hepatic, CYP3A4-mediated
Half life 24 hours
Excretion Renal
Therapeutic considerations
Licence data

EU, US
Pregnancy cat.

C in first trimester
D in second and third trimesters
Legal status

POM(UK) ℞-only(US)
Routes Oral

Aliskiren (INN) is the first in a class of drugs called a direct renin inhibitor, for lowering blood pressure. Drug metabolism is the Metabolism of drugs, their Biochemical modification or degradation usually through specialized enzymatic systems The liver is a vital organ in the human body and is present in Vertebrates and some other animals Cytochrome P450 3A4 (abbreviated CYP3A4) ( a member of the Cytochrome P450 mixed-function oxidase system is one of the most important enzymes involved in the metabolism The biological half-life of a substance is the time it takes for a substance (drug radioactive nuclide or other to lose half of its pharmacologic physiologic or radiologic activity Excretion is the process of eliminating waste products of Metabolism and other non-useful materials The kidneys are complicated organs that have numerous biological roles The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical if it is used as directed by the mother during The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained The United Kingdom of Great Britain and Northern Ireland, commonly known as the United Kingdom, the UK or Britain,is a Sovereign state located A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained The United States of America —commonly referred to as the In Pharmacology and Toxicology, a route An International Nonproprietary Name ( INN; also known as rINN, for recommended International Nonproprietary Name or pINN for proposed Renin (pronounced "Ree-nin" or "Rē-nin" (ˈriːnɨn also known as Angiotensinogenase, is a circulating Enzyme that participates in the body's Enzyme inhibitors are Molecules that bind to Enzymes and decrease their activity.

The renin-angiotensin-aldosterone system controls blood pressure. The renin-angiotensin system (RAS or the renin-angiotensin-aldosterone system (RAAS is a hormone system that regulates Blood pressure and water ( fluid Renin creates angiotensin. Angiotensin causes blood vessels to constrict and drives blood pressure up Angiotensin causes blood vessels to constrict, which drives blood pressure up. Angiotensin also creates aldosterone. Aldosterone is a hormone that causes the tubules of the kidneys to retain sodium and water Aldosterone causes the tubules of the kidneys to retain sodium and water, which also drives blood pressure up.

Many drugs control blood pressure by interfering with angiotensin or aldosterone. However, when these drugs are used for a long time, the body increases renin production, which drives blood pressure up again. Therefore, doctors have been looking for a drug to inhibit renin directly. Aliskiren is the first drug to do so. [1]

Aliskiren was co-developed by the Swiss pharmaceutical companies Novartis and Speedel. Novartis International AG is a multinational Pharmaceutical company based in Basel Switzerland that manufactures drugs such as Clozapine [2][3] It was approved by the U. S. Food and Drug Administration in 2007 for the treatment of hypertension. Hypertension, also referred to as high blood pressure, HTN or HPN, is a medical condition in which the Blood pressure is chronically elevated [4] The trade name for aliskiren is Tekturna in the USA, and Rasilez in the UK.

Contents

Adverse effects

A rare adverse event was allergic swelling of the face, lips or tongue and difficulty breathing, side effects that are common with other drugs for hypertension that act directly on the renin-angiotensin system. Angioedema ( BE: angiooedema) also known by its Eponym Quincke's edema, is the rapid swelling ( Edema) of the Dermis

Contraindications

As with ACE inhibitors, renin inhibitors should not be used in pregnancy, specifically the second and third trimesters, during which they will interfere with fetal kidney development and lead to oligohydramnios. ACE inhibitors, or inhibitors of '''A'''ngiotensin-'''C'''onverting '''E'''nzyme, are a group of Pharmaceuticals that are used primarily in treatment of Hypertension Oligohydramnios is a condition in Pregnancy characterised by a deficiency in Amniotic fluid.

Aliskiren has not yet been evaluated in patients with significantly impaired renal function.

Drug Interactions

Minor substrate of CYP3A4:

References

  1. ^ Ingelfinger JR, Aliskiren and dual therapy in type 2 diabetes mellitus, New England Journal of Medicine, 2008;358:2503
  2. ^ Gradman A, Schmieder R, Lins R, Nussberger J, Chiang Y, Bedigian M (2005). "Aliskiren, a novel orally effective renin inhibitor, provides dose-dependent antihypertensive efficacy and placebo-like tolerability in hypertensive patients". Circulation 111 (8): 1012–8. doi:10.1161/01.CIR.0000156466.02908.ED. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 15723979.  
  3. ^ Straessen JA, Li Y, and Richart T (2006). "Oral Renin Inhibitors". Lancet 368 (9545): 1449–56. doi:10.1016/S0140-6736(06)69442-7. A digital object identifier ( DOI) is a permanent identifier given to an Electronic document. PMID 17055947.  
  4. ^ "First Hypertension Drug to Inhibit Kidney Enzyme Approved", CBC, March 6, 2007. Retrieved on 2007-03-14. Year 2007 ( MMVII) was a Common year starting on Monday of the Gregorian calendar in the 21st century. Events 1489 - The Queen of Cyprus, Catherine Cornaro, sells her kingdom to Venice.  

External links

KEGG ( Kyoto Encyclopedia of Genes and Genomes) is a collection of Online databases dealing with Genomes Enzymatic pathways and biological chemicals Medical Subject Headings ( MeSH) is a huge Controlled vocabulary (or metadata system for the purpose of indexing journal articles and books
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