Products
Pitavastatin is commercially available in the form of film-coated tablets (Livazo). It was first approved in many countries in July 2012. In Japan, it has been on the market since 2003, and it is also available in other countries such as the United States and Germany.
Structure and properties
Pitavastatin (C25H24FNO4, Mr = 421.5 g/mol) is present in drugs as pitavastatin hemicalcium, an odorless, white to slightly yellowish powder that is very slightly soluble in water. It is a quinoline derivative, carries a cyclopropyl group, and unlike other statins, is not a prodrug. Pitavastatin has structural similarities to other statins such as atorvastatin (Sortis, generics).
Effects
Pitavastatin (ATC C10AA08) has lipid-lowering, anti-inflammatory, antioxidant, and has other, pleiotropic properties. The effects are due to competitive inhibition of HMG-CoA reductase and thus the synthesis of cholesterol. Pitavastatin binds with high affinity to the enzyme, lowering LDL-C, total cholesterol, and triglycerides and increasing HDL-C.
Indications
To lower elevated total cholesterol and LDL-C levels in disorders of lipid metabolism (hypercholesterolemia, combined dyslipidemia).
Dosage
According to the SmPC. Film-coated tablets are taken once daily, independent of meals.
Contraindications
- Hypersensitivity
- Severe hepatic insufficiency
- Active liver disease
- Unexplained persistent increases in serum transaminases
- Muscle disorders
- Pregnancy and lactation
- Pitavastatin must not be combined with ciclosporin.
For complete precautions, see the drug label.
Interactions
Pitavastatin is a substrate of OATP transporters on liver cells, from which interactions may result. Drug interactions are possible with ciclosporin, erythromycin and other macrolides, fibrates, niacin, fusidic acid, rifampicin, HIV protease inhibitors, and warfarin. Pitavastatin, in contrast to other statins, interacts little with CYP450 and is excreted predominantly unchanged. It therefore has a lower interaction potential than, for example, simvastatin or atorvastatin.
Adverse effects
The most common potential adverse effects include muscle and joint pain, headache, constipation, diarrhea, dyspepsia, and nausea. Statins can rarely cause muscle disease, life-threatening skeletal muscle breakdown, and liver damage.
