Pitavastatin

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Pitavastatin
Pitavastatin2DCSD.svg
Pitavastatin3Dan.gif
Systematic (IUPAC) name
(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid
Clinical data
Trade names Livalo
AHFS/Drugs.com monograph
MedlinePlus a610018
Licence data US FDA:link
Pregnancy cat. D (AU) X (US)
Legal status Prescription Only (S4) (AU) -only (CA) POM (UK) -only (US)
Routes Oral
Pharmacokinetic data
Bioavailability 60%
Protein binding 96%
Metabolism minimally CYP2C9
Half-life 11 hours
Excretion Faeces
Identifiers
CAS number 147511-69-1 N
ATC code C10AA08
PubChem CID 5282452
ChemSpider 4445604 YesY
UNII M5681Q5F9P YesY
ChEBI CHEBI:32020 N
ChEMBL CHEMBL1201753 N
Chemical data
Formula C25H24FNO4 
Mol. mass 421.461
 N (what is this?)  (verify)

Pitavastatin (usually as a calcium salt) is a member of the blood cholesterol lowering medication class of statins,[1] marketed in the United States under the trade name Livalo. Like other statins, it is an inhibitor of HMG-CoA reductase, the enzyme that catalyses the first step of cholesterol synthesis. It has been available in Japan since 2003, and is being marketed under licence in South Korea and in India.[2] It is likely that pitavastatin will be approved for use in hypercholesterolaemia (elevated levels of cholesterol in the blood) and for the prevention of cardiovascular disease outside South and Southeast Asia as well.[3] In the US, it received FDA approval in 2009.[4]

Uses[edit]

Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease. A 2009 study showed that pitavastatin increased HDL cholesterol (24.6%), especially in patients with HDL lower than 40 mg/dl, in addition to greatly reducing LDL cholesterol (–31.3%).[5] As a consequence, pitavastatin is most likely to be appropriate for patients with metabolic syndrome with high LDL, low HDL and diabetes mellitus.

Side effects[edit]

Common statin-related side effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins. However, pitavastatin seems to lead to fewer muscle side effects than certain statins that are lipid-soluble, as a result of the fact that pitavastatin is water-soluble (as is pravastatin, for example).[6] One study found that coenzyme Q10 was not reduced as much as with certain other statins (though this is unlikely given the inherent chemistry of the HMG-CoA reductase pathway that all statin drugs inhibit).[3][7]

Hyperuricemia or increased levels of serum uric acid have been reported with pitavastatin.[8]

Metabolism and interactions[edit]

Most statins are metabolised in part by one or more hepatic cytochrome P450 enzymes, leading to an increased potential for drug interactions and problems with certain foods (such as grapefruit juice). Pitavastatin appears to be a substrate of CYP2C9, and not CYP3A4 (which is a common source of interactions in other statins). As a result, pitavastatin is less likely to interact with drugs that are metabolized via CYP3A4, which might be important for elderly patients who need to take multiple medicines.[3]

History[edit]

Pitavastatin (previously known as itavastatin, itabavastin, nisvastatin, NK-104 or NKS-104) was discovered in Japan by Nissan Chemical Industries and developed further by Kowa Pharmaceuticals, Tokyo.[3] Pitavastatin was approved for use in the United States by the FDA on 08/03/2009 under the trade name Livalo. Pitavastatin has been also approved by the Medicines and Healthcare products Regulatory Agency (MHRA) in UK on 17 August 2010.

References[edit]

  1. ^ Kajinami, K; Takekoshi, N; Saito, Y (2003). "Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor". Cardiovascular drug reviews 21 (3): 199–215. PMID 12931254.  edit
  2. ^ Zydus Cadila launches pitavastatin in India
  3. ^ a b c d Mukhtar, R. Y. A.; Reid, J.; Reckless, J. P. D. (2005). "Pitavastatin". International Journal of Clinical Practice 59 (2): 239–252. doi:10.1111/j.1742-1241.2005.00461.x. PMID 15854203.  edit
  4. ^ The Seventh Statin; Pitavastatin
  5. ^ http://www.ncbi.nlm.nih.gov/pubmed/19907105
  6. ^ ScienceDaily (11 May 2013). "Alternative Cholesterol-Lowering Drug for Patients Who Can't Tolerate Statins". ScienceDaily. 
  7. ^ Clin Pharmacol Ther. 2008 May;83(5):731-9. Epub 2007 Oct 24. Comparison of effects of pitavastatin and atorvastatin on plasma coenzyme Q10 in heterozygous familial hypercholesterolemia: results from a crossover study. Kawashiri MA, Nohara A, Tada H, Mori M, Tsuchida M, Katsuda S, Inazu A, Kobayashi J, Koizumi J, Mabuchi H, Yamagishi M.
  8. ^ Ogata, N.; Fujimori, S.; Oka, Y.; Kaneko, K. (2010). "Effects of Three Strong Statins (Atorvastatin, Pitavastatin, and Rosuvastatin) on Serum Uric Acid Levels in Dyslipidemic Patients". Nucleosides, Nucleotides and Nucleic Acids 29 (4–6): 321. doi:10.1080/15257771003741323.  edit

External links[edit]