Pitavastatin
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| 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. | X |
| Legal status | ℞ Prescription only |
| Routes | Oral |
| Pharmacokinetic data | |
| Bioavailability | 60% |
| Protein binding | 96% |
| Metabolism | minimally CYP4502C9 |
| Half-life | 11 hours |
| Excretion | Faeces |
| Identifiers | |
| CAS number | 147511-69-1  |
| ATC code | C10AA08 |
| PubChem | CID 5282452 |
| ChemSpider | 4445604  |
| UNII | M5681Q5F9P |
| ChEMBL | CHEMBL1201753 |
| Chemical data | |
| Formula | C25H24FNO4 |
| Mol. mass | 421.461 |
| SMILES | eMolecules & PubChem |
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Pitavastatin (usually as a calcium salt) is a member of the 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]
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[edit] Uses
Like the other statins, pitavastatin is indicated for hypercholesterolaemia (elevated cholesterol) and for the prevention of cardiovascular disease. There have been many studies[which?] confirming that pitavastatin can consistently increase HDL cholesterol (10–25%), especially in patients with HDL lower than 40 mg/dl, in addition to strong reducing LDL cholesterol (–40%). As a consequence, pitavastatin is most likely to be appropriate for patients with metabolic syndrome with high LDL, low HDL and diabetes mellitus. Another reason is that pitavastatin, unlike other potent statins, does not affect glycelate control of type 2 diabetes mellitus.[clarification needed]
[edit] Side-effects
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 less muscle side effects than other statins, since coenzyme Q10 is not significantly reduced.[3][clarification needed]
[edit] 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). 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]
[edit] History
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.
[edit] References
- ^ 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.
- ^ Zydus Cadila launches pitavastatin in India
- ^ 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] External links
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