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Drug

D1379 | atorvastatin

Molecular Formula C33H35FN2O5
Molecular Weight 558.6
Structure
State solid
Clearance The registered total plasma clearance of atorvastatin is of 625 ml/min.[A19474]
Volume of distribution The reported volume of distribution of atorvastatin is of 380 L.[A177397]
Route of elimination Atorvastatin is mainly eliminated in the bile without enterohepatic recirculation.[A177397] The renal elimination of atorvastatin is very minimal and represents less than 1% of the eliminated dose.[A19474]
Protein binding Atorvastatin is highly bound to plasma proteins and over 98% of the administered dose is found in a bound form.[A177397]
Half life The half-life of atorvastatin is of about 14 hours while the half-life of its metabolites can reach up to 30 hours.[A177397]
Absorption Atorvastatin presents a dose-dependent and non-linear pharmacokinetic profile.[A177436] It is very rapidly absorbed after oral administration. After the administration of a dose of 40 mg, its peak plasma concentration of 28 ng/ml is reached 1-2 hours after initial administration with an AUC of about 200 ng.h/ml.[A177478] It does present a very large first-pass metabolism and hence, its bioavailability is of only 14%.[A177397] Administration of atorvastatin with food results in prolonged Tmax and a reduction in Cmax and AUC.[A177415]
Trade names Lipitor, Sortis
Description statin; inhibiting HMG-CoA reductase

C

C10BX15 Atorvastatin and perindopril


[C10BX] HMG CoA reductase inhibitors, other combinations


[C10B] LIPID MODIFYING AGENTS, COMBINATIONS


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

C10BX12 Atorvastatin, acetylsalicylic acid and perindopril


[C10BX] HMG CoA reductase inhibitors, other combinations


[C10B] LIPID MODIFYING AGENTS, COMBINATIONS


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

C10BX11 Atorvastatin, amlodipine and perindopril


[C10BX] HMG CoA reductase inhibitors, other combinations


[C10B] LIPID MODIFYING AGENTS, COMBINATIONS


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

C10BX08 Atorvastatin and acetylsalicylic acid


[C10BX] HMG CoA reductase inhibitors, other combinations


[C10B] LIPID MODIFYING AGENTS, COMBINATIONS


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

C10BX06 Atorvastatin, acetylsalicylic acid and ramipril


[C10BX] HMG CoA reductase inhibitors, other combinations


[C10B] LIPID MODIFYING AGENTS, COMBINATIONS


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

C10BX03 Atorvastatin and amlodipine


[C10BX] HMG CoA reductase inhibitors, other combinations


[C10B] LIPID MODIFYING AGENTS, COMBINATIONS


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

C10BA05 Atorvastatin and ezetimibe


[C10BA] HMG CoA reductase inhibitors in combination with other lipid modifying agents


[C10B] LIPID MODIFYING AGENTS, COMBINATIONS


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

C10AA05 Atorvastatin


[C10AA] HMG CoA reductase inhibitors


[C10A] LIPID MODIFYING AGENTS, PLAIN


[C10] LIPID MODIFYING AGENTS


[C] Cardiovascular system

Toxicity Dose Time Species Model Method Action Positive criterion Reference
OPENING OF PERMEABILITY TRANSITION PORE (PTP) 50 µM 1 hour Human HepG2 High-content screening assay Decrease MEC 306
MEMBRANE POTENTIAL 100 µM 1 hour Human HepG2 High-content screening assay Increase MEC 306
ELECTRON TRANSPORT CHAIN C2C12 myoblasts affect 180
ROS PRODUCTION 100 µM 1 hour Human HepG2 High-content screening assay Increase MEC 306

Target Dose Time Species Model Method Action Positive criterion Reference
Qo site (Qp site or ubiquinol oxidation site) C2C12 myoblasts inhibitor 180
Reactive oxygen species 100 µM 1 hour Human HepG2 High-content screening assay increase MEC 306

Pictogram Signal Statements Precautionary Statement Codes
Warning

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.


H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]


H319 (100%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]


H335 (100%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure


Respiratory tract irritation]


H361 (100%): Suspected of damaging fertility or the unborn child [Warning Reproductive toxicity]


H362 (100%): May cause harm to breast-fed children [Reproductive toxicity, effects on or via lactation]


 P201, P202, P260, P261, P263, P264, P270, P271, P280, P281, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)
Warning

Aggregated GHS information provided by 79 companies from 14 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.


Reported as not meeting GHS hazard criteria by 3 of 79 companies. For more detailed information, please visit ECHA C&L website


Of the 13 notification(s) provided by 76 of 79 companies with hazard statement code(s):


H373 (48.68%): Causes damage to organs through prolonged or repeated exposure [Warning Specific target organ toxicity, repeated exposure]


H402 (38.16%): Harmful to aquatic life [Hazardous to the aquatic environment, acute hazard]


H411 (46.05%): Toxic to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard]


H412 (40.79%): Harmful to aquatic life with long lasting effects [Hazardous to the aquatic environment, long-term hazard]


Information may vary between notifications depending on impurities, additives, and other factors. The percentage value in parenthesis indicates the notified classification ratio from companies that provide hazard codes. Only hazard codes with percentage values above 10% are shown.


 P260, P273, P314, P391, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)
Warning

The GHS information provided by 1 company from 1 notification to the ECHA C&L Inventory.


H315 (100%): Causes skin irritation [Warning Skin corrosion/irritation]


H319 (100%): Causes serious eye irritation [Warning Serious eye damage/eye irritation]


H335 (100%): May cause respiratory irritation [Warning Specific target organ toxicity, single exposure


Respiratory tract irritation]


 P261, P264, P271, P280, P302+P352, P304+P340, P305+P351+P338, P312, P321, P332+P313, P337+P313, P362, P403+P233, P405, and P501; (The corresponding statement to each P-code can be found at the GHS Classification page.)


  • (3R,5R)-7-(2-(4-Fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-3,5-dihydroxy (3R,5R)-7-(2-(4-Fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-3,5-dihydroxyheptanoic acid (3R,5R)-7-[2-(4-Fluorophenyl)-5-isopropyl-3-phenyl-4-phenylcarbamoylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid
    (3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid (3R,5R)-7-[2-(4-fluorophenyl)-3-phenyl-4-(phenylcarbamoyl)-5-propan-2-ylpyrrol-1-yl]-3,5-dihydroxyheptanoic acid (3R,5R)-7-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid
    (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-phenylcarbamoyl-pyrrol-1-yl]-3,5-dihydroxy-heptanoic acid (3R,5R)-7-[3-(anilinocarbonyl)-5-(4-fluorophenyl)-2-isopropyl-4-phenyl-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid
    (3R,5R)-7-[3-(anilinocarbonyl)-5-(4-fluorophenyl)-4-phenyl-2-(propan-2-yl)-1H-pyrrol-1-yl]-3,5-dihydroxyheptanoic acid (R-(R*,R*))-2-(4-Fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-1H-pyrrole-1-heptanoic acid (betaR,deltaR)-2-(p-Fluorophenyl)-beta,delta-dihydroxy-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)pyrrole-1-heptanoic acid
    110862-48-1 134523-00-5 134523-03-8
    1H-Pyrrole-1-heptanoic acid, 2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-, (R-(R*,R*))- 1H-Pyrrole-1-heptanoic acid, 2-(4-fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-((phenylamino)carbonyl)-, (betaR,deltaR)- 28052-EP2269989A1
    28052-EP2269990A1 28052-EP2270011A1 28052-EP2270505A1
    28052-EP2272825A2 28052-EP2272841A1 28052-EP2280001A1
    28052-EP2284158A1 28052-EP2287165A2 28052-EP2287166A2
    28052-EP2292600A1 28052-EP2292620A2 28052-EP2295406A1
    28052-EP2295409A1 28052-EP2295417A1 28052-EP2295422A2
    28052-EP2298731A1 28052-EP2298742A1 28052-EP2298745A1
    28052-EP2298769A1 28052-EP2298772A1 28052-EP2298776A1
    28052-EP2298779A1 28052-EP2301923A1 28052-EP2301931A1
    28052-EP2301936A1 28052-EP2308839A1 28052-EP2308878A2
    28052-EP2314588A1 523A005 7-[2-(4-FLUORO-PHENYL)-5-ISOPROPYL-3-PHENYL-4-PHENYLCARBAMOYL-PYRROL-1-YL]- 3,5-DIHYDROXY-HEPTANOIC ACID
    7-[2-(4-FLUORO-PHENYL)-5-ISOPROPYL-3-PHENYL-4-PHENYLCARBAMOYL-PYRROL-1-YL]-3,5-DIHYDROXY-HEPTANOIC ACID A0JWA85V8F AC-9386
    ACT03225 AKOS000281127 AS-35260
    ATORVASTATIN CALCIUM ATORVASTATIN;Atorvastatin calcium;Atorvastatin Calcium Atofast
    Ator Atorcor Atorin
    Atorlip Atorvastatin & Primycin Atorvastatin (INN)
    Atorvastatin (Relative Stereo) Atorvastatin [INN:BAN] Atorvastatin calcium salt
    BDBM22164 BIDD:GT0336 BR-58267
    BRD-K69726342-001-02-6 C06834 C33H35FN2O5
    CAS-134523-00-5 CCG-221172 CCRIS 7159
    CHEBI:39548 CHEMBL1487 CI 981
    CS-2798 CTK4B9231 Cardyl
    Cardyl D07474 DB01076
    DSSTox_CID_9868 DSSTox_GSID_29868 DSSTox_RID_78825
    DTXSID60274003 DTXSID8029868 GTPL2949
    H942 HMS3715L05 HSDB 7039
    HY-B0589 LS-136975 Lipilou
    Lipilou Lipinon Lipitor
    Lipitor (TN) Lipitor(TM) MCULE-2368532812
    MRF-0000761 NCGC00159458-02 NCGC00159458-03
    NCGC00159458-20 NCGC00255181-01 Q668093
    S-2492 SCHEMBL3831 SR-01000872702
    SR-01000872702-1 Sortis (TN) Sotis
    Torvast Torvast Tox21_302417
    Tozalip Tozalip UNII-36TN91XZ0V component XUKUURHRXDUEBC-KAYWLYCHSA-N
    UNII-A0JWA85V8F Xavator Y-8867
    ZINC3920719 atorvastatin atorvastatina
    atorvastatine atorvastatinum atrovastin
    rel-Atorvastatin s5715

    DrugBank DB01076
    CAS Number 110862-48-1, 134523-00-5, 134523-03-8
    PubChem Compound 60823