Drug

D1298 | Biotin

Molecular Formula C10H16N2O3S
Molecular Weight 244.31
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]
Description Nutritive agent

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
MEMBRANE POTENTIAL 4.3 µM 30 mins mouse liver mitochondria Rh123 fluorescence (excitation 485 nm, emission 535 nm) are recorded using a fluorescence multi-well plate reader (mCICCP (20 µM) treatments was considered as the 100% baseline for ΔΨm loss) decrease EC20 36
RESPIRATION 44.5 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. decrease EC20 36
RESPIRATION ND 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. Negative EC20 36
SWELLING 5.6 µM 30 mins mouse liver mitochondria swelling assay: Absorbance at 545 nm using a fluorescence multi-well plate reader (CaCl2 (50 µM) was considered as the 100% baseline for the swelling ) increase EC20 36

Target Dose Time Species Model Method Action Positive criterion Reference
NADH:ubiquinone reductase 44.5 µM 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Rotenone (2µM) was used as 100% baseline for complex I inhibition. inhibit EC20 36
Succinate dehydrogenase ND 60 mins mouse liver mitochondria Oxygen consumption was monitored with 50nM MitoXpress ( an oxygen-sensitive phosphorescent dye) using a spectrofluorimeter (Tecan Infinite 200; λExcitation 380nm; λEmission 650nm). Oligomycin A (1µM) was used as 100% baseline for complex II inhibition. Negative EC20 36
Cytochrome c < 50 µM 30 mins mouse liver mitochondria Cytochrome c release was evaluated using ELISA kit ( 20 µg/ml Alamethicin was used as 100% baseline) release EC20 36


  • DrugBank DB01076
    CAS Number 10406-89-0, 21788-37-4, 22377-59-9, 22879-79-4, 415725-35-8, 4492-73-3, 56846-45-8, 58-85-5, 8059-24-3
    PubChem Compound 171548