Pitavastatin

drugbox
IUPAC_name = (E)-7- [2-cyclopropyl-4-(4-fluorophenyl)
quinolin-3-yl] -3,5-dihydroxy-hept-6-enoic acid


width = 200
CAS_number = 147511-69-1
ATC_prefix = C10
ATC_suffix = AA08
PubChem = 6366718
DrugBank =
C=25 | H=24 | F=1 | N=1 | O=4
molecular_weight = 421.461
bioavailability = 60%
metabolism = hepatic
elimination_half-life = 11 hours
excretion = biliary
protein_bound = 96%
pregnancy_category = X
legal_status = prescription
routes_of_administration = oral tablets 1 & 2 mg

Pitavastatin (usually as a calcium salt) is a novel member of the medication class of statins.Kajinami K, Takekoshi N, Saito Y. Pitavastatin: efficacy and safety profiles of a novel synthetic HMG-CoA reductase inhibitor. "Cardiovasc Drug Rev" 2003;21:199-215. PMID 12931254.] Like the 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. [http://www.expresspharmapulse.com/20050303/inthenews01.shtml Zydus Cadila launches pitavastatin in India] ] 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.Mukhtar RY, Reid J, Reckless JP. Pitavastatin. "Int J Clin Pract" 2005;59:239-52. PMID 15854203.]

Uses

Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease.

ide-effects

Common statin-related side-effects (headaches, stomach upset, abnormal liver function tests and muscle cramps) were similar to other statins.

Metabolism and interactions

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).

History

Pitavastatin (previously known as itavastatin, itabavastin, nisvastatin, NK-104 or NKS-104) was discovered in Japan by Nissan Chemical Industries, Ltd. and developed further by Kowa Pharmaceuticals, Tokyo.

References

External links