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¸®Æ÷¹ÙÀÌÁ¤0.1mg LIPOBAY TAB[Cerivastatin sodium]
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| Related FDA Approved Drug |
±âÁØ ¼ººÐ: CERIVASTATIN SODIUMBAYCOL (CERIVASTATIN SODIUM)
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| Mechanism of Action |
Cerivastatin¿¡ ´ëÇÑ Mechanism_Of_Action Á¤º¸ Cerivastatin competitively inhibits hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase, the hepatic enzyme responsible for converting HMG-CoA to mevalonate. As mevalonate is a precursor of sterols such as cholesterol, this results in a decrease in cholesterol in hepatic cells, upregulation of LDL-receptors, and an increase in hepatic uptake of LDL-cholesterol from the circulation.
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| Pharmacology |
Cerivastatin¿¡ ´ëÇÑ Pharmacology Á¤º¸ Cerivastatin, a competitive HMG-CoA reductase inhibitor effective in lowering LDL cholesterol and triglycerides, is used to treat primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb).
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| Metabolism |
Cerivastatin¿¡ ´ëÇÑ Metabolism Á¤º¸ # Phase_1_Metabolizing_Enzyme:Cytochrome P450 2C8 (CYP2C8)
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| Protein Binding |
Cerivastatin¿¡ ´ëÇÑ ´Ü¹é°áÇÕ Á¤º¸ More than 99% of the circulating drug is bound to plasma proteins (80% to albumin).
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| Half-life |
Cerivastatin¿¡ ´ëÇÑ ¹Ý°¨±â Á¤º¸ 2-3 hours
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| Absorption |
Cerivastatin¿¡ ´ëÇÑ Absorption Á¤º¸ The mean absolute oral bioavailability 60% (range 39 - 101%).
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| Biotransformation |
Cerivastatin¿¡ ´ëÇÑ Biotransformation Á¤º¸ Hepatic. Biotransformation pathways for cerivastatin in humans include the following: demethylation of the benzylic methyl ether to form Ml and hydroxylation of the methyl group in the 6'-isopropyl moiety to form M23.
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| Toxicity |
Cerivastatin¿¡ ´ëÇÑ Toxicity Á¤º¸ Rhabdomyolysis, liver concerns
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| Drug Interactions |
Cerivastatin¿¡ ´ëÇÑ Drug_Interactions Á¤º¸ Bezafibrate Increased risk of myopathy/rhabdomyolysisBosentan Bosentan could decrease the statin effectClarithromycin The macrolide possibly increases the statin toxicityColchicine Increased risk of rhabdomyolysis with this combinationCyclosporine Possible myopathy and rhabdomyolysisDiltiazem Diltiazem increases the effect and toxicity of the statinErythromycin The macrolide possibly increases the statin toxicityFenofibrate Increased risk of myopathy/rhabdomyolysisGemfibrozil Increased risk of myopathy/rhabdomyolysisImatinib Imatinib increases the effect and toxicity of statinItraconazole Increased risk of myopathy/rhabdomyolysisJosamycin The macrolide possibly increases the statin toxicityKetoconazole Increased risk of myopathy/rhabdomyolysisNefazodone Nefazodone increases the effect and toxicity of the statin drugQuinupristin This combination presents an increased risk of toxicityRifabutin The rifamycin decreases the effect of statin drugRifampin The rifamycin decreases the effect of statin drug
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CYP450 Drug Interaction |
[CYP450 TableÁ÷Á¢Á¶È¸] Cerivastatin¿¡ ´ëÇÑ P450 table
SUBSTRATES
CYP 3A4/3A5/3A7
Macrolide antibiotics:
clarithromycin
erythromycin
NOT azithromycin
telithromycin
Anti-arrhythmics:
quinidine
Benzodiazepines:
alprazolam
diazepam
midazolam
triazolam
Immune Modulators:
cyclosporine
tacrolimus (FK506)
HIV Protease Inhibitors:
indinavir
ritonavir
saquinavir
Prokinetic:
cisapride
Antihistamines:
astemizole
chlorpheniramine
Calcium Channel Blockers:
amlodipine
diltiazem
felodipine
nifedipine
nisoldipine
nitrendipine
verapamil
HMG CoA Reductase Inhibitors:
atorvastatin
**cerivastatin**
lovastatin
NOT pravastatin
simvastatin
aripiprazole
buspirone
gleevec
haloperidol (in part)
methadone
pimozide
quinine
NOT rosuvastatin
sildenafil
tamoxifen
trazodone
vincristine
INHIBITORS
CYP 3A4/3A5/3A7
HIV Protease Inhibitors:
indinavir
nelfinavir
ritonavir
amiodarone
NOT azithromycin
cimetidine
clarithromycin
diltiazem
erythromycin
fluvoxamine
grapefruit juice
itraconazole
ketoconazole
mibefradil
nefazodone
troleandomycin
verapamil
INDUCERS
CYP 3A4/3A5/3A7
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
St. John's wort
troglitazone
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| Food Interaction |
Cerivastatin¿¡ ´ëÇÑ Food Interaction Á¤º¸ Take without regard to meals.Grapefruit and grapefruit juice should be avoided throughout treatment as grapefruit can significantly increase serum levels of this product.
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| Drug Target |
[Drug Target]
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| Description |
Cerivastatin¿¡ ´ëÇÑ Description Á¤º¸ On August 8, 2001 the U.S. Food and Drug Administration (FDA) announced that Bayer Pharmaceutical Division voluntarily withdrew Baycol from the U.S. market, due to reports of fatal Rhabdomyolysis, a severe adverse reaction from this cholesterol-lowering (lipid-lowering) product. It has also been withdrawn from the Canadian market.
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| Dosage Form |
Cerivastatin¿¡ ´ëÇÑ Dosage_Form Á¤º¸ Tablet Oral
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| Drug Category |
Cerivastatin¿¡ ´ëÇÑ Drug_Category Á¤º¸ Anticholesteremic AgentsAntilipemic AgentsHydroxymethylglutaryl-CoA Reductase Inhibitors
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| Smiles String Canonical |
Cerivastatin¿¡ ´ëÇÑ Smiles_String_canonical Á¤º¸ COCC1=C(C2=CC=C(F)C=C2)C(C=CC(O)CC(O)CC(O)=O)=C(N=C1C(C)C)C(C)C
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| Smiles String Isomeric |
Cerivastatin¿¡ ´ëÇÑ Smiles_String_isomeric Á¤º¸ COCC1=C(C2=CC=C(F)C=C2)C(\C=C\[C@@H](O)C[C@@H](O)CC(O)=O)=C(N=C1C(C)C)C(C)C
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| InChI Identifier |
Cerivastatin¿¡ ´ëÇÑ InChI_Identifier Á¤º¸ InChI=1/C26H34FNO5/c1-15(2)25-21(11-10-19(29)12-20(30)13-23(31)32)24(17-6-8-18(27)9-7-17)22(14-33-5)26(28-25)16(3)4/h6-11,15-16,19-20,29-30H,12-14H2,1-5H3,(H,31,32)/b11-10+/t19-,20-/m1/s1/f/h31H
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| Chemical IUPAC Name |
Cerivastatin¿¡ ´ëÇÑ Chemical_IUPAC_Name Á¤º¸ (E,3R,5S)-7-[4-(4-fluorophenyl)-5-(methoxymethyl)-2,6-di(propan-2-yl)pyridin-3-yl]-3,5-dihydroxyhept-6-enoic acid
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µå·°ÀÎÆ÷ ÀǾàÇмúÁ¤º¸´Â ½ÄǰÀǾàǰ¾ÈÀüóÀÇ Á¦Ç°Çã°¡»çÇ×, Çмú¹®Çå, Á¦¾àȸ»ç Á¦°øÁ¤º¸ µîÀ» ±Ù°Å·Î ÀÛ¼ºµÈ Âü°í Á¤º¸ÀÔ´Ï´Ù.
Á¤º¸ÀÇ Á¤È®¼ºÀ» À§ÇØ ³ë·ÂÇϰí ÀÖÀ¸³ª ÆíÁý»óÀÇ ¿À·ù, Çã°¡»çÇ× º¯°æ, Ãß°¡ÀûÀÎ Çмú¿¬±¸ ¶Ç´Â Àӻ󿬱¸ ¹ßÇ¥ µîÀ¸·Î ÀÎÇØ ¹ß»ýÇÏ´Â ¹®Á¦¿¡ ´ëÇØ µå·°ÀÎÆ÷´Â
Ã¥ÀÓÀ» ÁöÁö ¾Ê½À´Ï´Ù. ÀÚ¼¼ÇÑ ³»¿ëÀº ¡°Ã¥ÀÓÀÇ ÇÑ°è ¹× ¹ýÀû°íÁö¡±¸¦ ÂüÁ¶ÇØ ÁֽʽÿÀ.
¹Ýµå½Ã Á¦Á¶¡¤¼öÀÔ»ç, ÆÇ¸Å»ç, ÀÇ»ç, ¾à»ç¿¡°Ô ÃÖÁ¾ÀûÀ¸·Î È®ÀÎÇϽñ⠹ٶø´Ï´Ù.
ÀüÈ: 02-3486-1061 ¤Ó À̸ÞÀÏ: webmaster@druginfo.co.kr
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