Pitavastatin
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| Non-proprietary name | Pitavastatin | |||||||||||||||||||||
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| Molecular formula | C 25 H 24 FNO 4 | |||||||||||||||||||||
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| Molar mass | 421.46 g · mol -1 | |||||||||||||||||||||
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| As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions . | ||||||||||||||||||||||
Pitavastatin is the international non-proprietary name (INN) for a drug from the group of statins that is used to lower increased total cholesterol and LDL cholesterol levels .
Pitavastatin was approved as a finished medicinal product in August 2009 in the USA and 2011 in Germany. It was developed by the Japanese company Kōwa Sōyaku (Kowa Pharmaceutical), in the EU countries the drug is to be marketed by the company Recordati .
Clinical information
Application areas (indications)
The use of pitavastatin is indicated for the lowering of elevated total cholesterol and LDL cholesterol levels in patients with primary hypercholesterolaemia or combined hypercholesterolaemia and hypertriglyceridaemia in patients at increased cardiovascular risk.
Contraindications (contraindications)
The use of pitavastatin is contraindicated in:
- Patients with a known hypersensitivity to the active substance. Hypersensitivity reactions - including rash , itching (pruritus) and hives (urticaria) - were observed in the clinical trials .
- Patients with active liver disease , which can be expressed, for example, by an unexplained and permanent increase in aspartate aminotransferase (liver transaminases).
- Simultaneous administration of drugs containing cyclosporine is also contraindicated.
Pharmacokinetic properties
The bioavailability of pitavastatin is 80%; The plasma protein binding of the active substance is 96%. Pitavastatin is mainly through the cytochrome P450 - isoenzyme CYP2C9 metabolised . The elimination from the blood has a terminal half-life # biological half-life of 11 hours.
Other Information
Chemical and pharmaceutical information
In the finished product is pitavastatin hemicalcium (pitavastatin · calcium (2: 1)), CAS number 147526-32-7 used with the following chemical-physical characteristics: The name according to IUPAC nomenclature are: calcium (3 R , 5 S , 6 E ) -7- [2-cyclopropyl-4- (4-fluorophenyl) -3-quinolyl] -3,5-dihydroxyhept-6-enoate, the empirical formula is C 50 H 46 CaF 2 N 2 O 8 with a molar mass of 880.98 g · mol -1 . Pitavastatin Hemicalcium is an odorless, white to pale yellow, light-sensitive and hygroscopic powder. It is easily soluble in pyridine , chloroform , dilute hydrochloric acid and tetrahydrofuran , soluble in ethylene glycol , poorly soluble in octanol , slightly soluble in methanol , very slightly soluble in water or ethanol , practically insoluble in acetonitrile or diethyl ether . The melting point is 190-192 ° C .
First decision on early benefit assessment
As part of the early benefit assessment of pharmaceuticals, the Federal Joint Committee (G-BA) ... made the first decision. Medicines with the new active ingredient "Pitavastatin" will be transferred to the fixed-price system, as a therapeutic improvement for these preparations is not considered proven.
Individual evidence
- ↑ There is not yet a harmonized classification for this substance . A labeling of {[(3 R , 5 S , 6 E ) -7- [2-cyclopropyl-4- (4-fluorophenyl) quinolin-3-yl] -3,5-dihydroxyhept is shown, which is derived from a self-classification by the distributor -6-enoyl] oxy} calcio (3 R , 5 S , 6 E ) -7- [2-cyclopropyl-4- (4-fluorophenyl) quinolin-3-yl] -3,5-dihydroxyhept-6-enoate im Classification and Labeling Inventory of the European Chemicals Agency (ECHA), accessed on July 6, 2020.
- ↑ FDA Approves New Cholesterol-Lowering Drug . August 3, 2009. Retrieved September 4, 2009.
- ↑ a b Kowa Pharmaceutical Europe Co., Ltd .: Livazo (R) (pitavastatin), a new effective statin with a positive effect on lipid fractions associated with heart disease, is launched in Spain ( Memento of April 14, 2014 in the Internet Archive )
- ↑ DAZ: New cholesterol-lowering drug pitavastatin . August 2, 2010. Retrieved August 19, 2011.
- ↑ a b c FDA label for LIVALO (pitavastatin) ( en , PDF, 241 kB) on the website of the Food and Drug Administration FDA . S. 15 August 3, 2009. Retrieved September 4, 2009.
- ↑ Kajinami K, Mabuchi H, Saito Y: NK-104: a novel synthetic HMG-CoA reductase inhibitor . In: Expert Opin Investig Drugs . 9, No. 11, 2000, pp. 2653-2661. doi : 10.1517 / 13543784.9.11.2653 . PMID 11060827 .
- ↑ G-BA: First decision on early benefit assessment - procedure stable . August 18, 2011. Retrieved February 26, 2014.
Finished medicinal products
Livazo ( D ), Livalo ( USA ), Alipza ( I )
