Tìm theo
Pitavastatin
Các tên gọi khác (5 ) :
  • NK 104
  • NK-104
  • Pitavastatia
  • Pitavastatine
  • Pitavastatinum
hypolipidemic agents
Thuốc Gốc
Small Molecule
CAS: 147511-69-1
ATC: C10AA08
CTHH: C25H24FNO4
PTK: 421.4608
Pitavastatin a lipid-lowering agent that belongs to the statin class of medications for treatment of dyslipidemia. It is also used for primary and secondary prevention of cardiovascular disease. FDA approved in Aug 3, 2009.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C25H24FNO4
Phân tử khối
421.4608
Monoisotopic mass
421.168936466
InChI
InChI=1S/C25H24FNO4/c26-17-9-7-15(8-10-17)24-20-3-1-2-4-22(20)27-25(16-5-6-16)21(24)12-11-18(28)13-19(29)14-23(30)31/h1-4,7-12,16,18-19,28-29H,5-6,13-14H2,(H,30,31)/b12-11+/t18-,19-/m1/s1
InChI Key
InChIKey=VGYFMXBACGZSIL-MCBHFWOFSA-N
IUPAC Name
(3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoic acid
Traditional IUPAC Name
pitavastatin
SMILES
O[C@H](C[C@H](O)\C=C\C1=C(N=C2C=CC=CC2=C1C1=CC=C(F)C=C1)C1CC1)CC(O)=O
Độ hòa tan
Very slightly soluble
logP
2.92
logS
-5
pKa (strongest acidic)
4.13
pKa (Strongest Basic)
4.86
PSA
90.65 Å2
Refractivity
115.74 m3·mol-1
Polarizability
43.86 Å3
Rotatable Bond Count
8
H Bond Acceptor Count
5
H Bond Donor Count
3
Physiological Charge
-1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : The magnitude of LDL-C reduction by pitavastatin (2 mg and 4 mg) is comparable to atorvastatin (10 mg and 20 mg) and simvastatin (20 mg and 40 mg). It also does not prolong the QTc interval to a clinically significant degree.
Cơ Chế Tác Dụng : Pitavastatin a lipid-lowering agent that belongs to the statin class of medications for treatment of dyslipidemia. It is also used for primary and secondary prevention of cardiovascular disease. FDA approved in Aug 3, 2009. Pitavastatin is lipid-lowering agent that works to control the synthesis of cholesterol via competitive inhibition of the liver enzyme, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. As a result, a compensatory increase in LDL-receptor expression can be observed which facilitates an increase LDL catabolism.
Dược Động Học :
▧ Absorption :
Bioavailability = 51%; Time to peak, plasma = 1 hour; Pitavastatin was absorbed in the small intestine but very little in the colon. Cmax decreases by 43% if pitavastatin is taken with a fatty meal but there are no significant changes to AUC or baseline LDL levels compared to fasting state. The Cmax and AUC of pitavastatin did not differ following evening or morning drug administration.
▧ Volume of Distribution :
148 L
▧ Protein binding :
>99% protein bound in human plasma, mainly to albumin and alpha 1-acid glycoprotein.
▧ Metabolism :
Pitavastatin is mainly metabolized by liver. It undergoes glucuronidation by uridine 5-diphosphate glucuronosyl transferases (UGT1A3 and UGT2B7) to form the major circulating metabolite, pitavastatin lactone. The cytochrome P450 system has little involvement with the metabolism of pitavastatin. There is some metabolism by CYP2C9 and to a lesser extent, CYP2C8. Studies suggest that concomitant therapy with drugs that are involved with the cytochrome P450 system will not effect the pharmacokinetics of pitavastatin.
▧ Route of Elimination :
79% in feces and 15% excreted in urine.
▧ Half Life :
Plasma elimination half-lfie = 12 hours
▧ Clearance :
CL/F (apparent clearance), 4 mg, healthy male Korean subjects = 23.6 L/h
Độc Tính : The most frequent adverse reactions (rate ≥2.0% in at least one marketed dose) were myalgia, back pain, diarrhea, constipation and pain in extremity.
Chỉ Định : Pitavastatin is used to lower serum levels of total cholesterol, LDL-C, apolipoprotein B, and triglycerides, and raise levels of HDL-C for the treatment of dyslipidemia.
Tương Tác Thuốc :
  • Atazanavir Increases serum concentration of pitavastatin and the potential for adverse drug reactions. Avoid concomitant drug therapy.
  • Colchicine Increased incidence of myotoxicity including rhabdomyolysis during concomitant therapy. The mechanism of this interaction is unclear, it may arise from pharmacodynamic and/or pharmacokinetic interactions.
  • Cyclosporine Cyclosporine decreases metabolism of pitavastatin thus increasing serum concentration. Avoid concomitant drug therapy.
  • Erythromycin Erythromycin decreases metabolism of pitavastatin. Do not exceed 1 mg per day of pitavastatin or use alternative therapy.
  • Fenofibrate Increased incidence of adverse drug reactions (ie. rhabdomyolysis) of both fenofibrate and pitavastatin via pharmacodynamic synergism. Use alternative therapy.
  • Gemfibrozil Increased incidence of adverse drug reactions (ie. rhabdomyolysis) of both gemfibrozil and pitavastatin via pharmacodynamic synergism. Use alternative therapy.
  • Lopinavir Lopinavir decreases metabolism of pitavastatin thus increasing serum concentration. Avoid concomitant drug therapy.
  • Niacin Increased incidence of adverse drug reactions (ie. rhabdomyolysis) of both niacin and pitavastatin via pharmacodynamic synergism. Use alternative therapy.
  • Rifampicin Rifampin significantly increased pitavastatin exposure. In patients taking rifampin, a dose of LIVALO 2 mg once daily should not be exceeded.
  • Rifampicin Rifampin significantly increased pitavastatin exposure. In patients taking rifampin, a dose of LIVALO 2 mg once daily should not be exceeded.
Liều Lượng & Cách Dùng : Tablet - Oral - 1 mg, 2 mg, 4 mg
Dữ Kiện Thương Mại
Nhà Sản Xuất
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB08860
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C13334
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01862
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0002-4771-90
PharmGKB
http://www.pharmgkb.org/drug/PA142650384
Wikipedia
http://en.wikipedia.org/wiki/Pitavastatin
RxList
http://www.rxlist.com/livalo-drug.htm
Drugs.com
http://www.drugs.com/ppa/pitavastatin.html
... loading
... loading