This study aimed to detect the concentrations of HCQ and its metabolites from peripheral blood of SLE patients and to investigate the relationship between those concentrations and SLE disease activity
Abstract
Hydroxychloroquine is metabolized in the liver and may alter metabolism of other medications
In vitro, hydroxychloroquine is metabolized mainly by CYP2C8, CYP3A4 and CYP2D6 as well as by FMO-1 and MAO-A
Metabolism of chloroquine into "2-hydroxychloroquine or hydroxychloroquine" and "4-amino chloroquine" is a phase I pathway
Scientific Reports - Simultaneous LC-MS/MS method for the quantitation of Azithromycin, Hydroxychloroquine and its metabolites in SARS-CoV-2(−/ +) populations using dried blood spots
Its structural formula is: Drug: Hydroxychloroquine
In vitro, hydroxychloroquine is metabolized mainly by CYP2C8, CYP3A4 and CYP2D6 as well as by FMO-1 and MAO-A
A cohort of 146 patients with SLE and RA treated with HCQ was The within- and between-day precision (relative standard deviation, % RSD) and accuracy were within the acceptable limits per FDA guidelines
0 µg/mL
In vitro, hydroxychloroquine is metabolized mainly by CYP2C8, CYP3A4 and These drugs undergo metabolism by several enzymes
After administration of single 155 mg and 310 mg intravenous doses, peak blood concentrations ranged from 1,161 ng/mL to 2,436 ng/mL (mean 1,918 ng/mL) following the 155 mg infusion and 6 months following the 310 mg infusion
5 mg/kg hydroxychloroquine sulfate once weekly on the Updating Hydroxychloroquine Physiologically-Based Pharmacokinetic Model
The mean fraction of the dose absorbed was 0
(2) We limited ourselves to the investigation of drug transporters most relevant for drug-drug interactions
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The inhibitory effects of HCQ and its metabolites on nine CYPs were also determined in HLMs, using an automated substrate cocktail method
Our metabolism data indicated that CYP3A4, CYP2D6, and CYP2C8 are the key enzymes involved in HCQ Chloroquine and hydroxychloroquine belong to the quinolone family
2 Due to its Background
Hydroxychloroquine (HCQ) was originally used as an antimalarial and immunomodulation drug
For CYP3A5 (rs776746), a greater risk of skin and mucous membrane ADRs was associated with the TT genotype than with the CT + CC genotypes (P = 0
Hydroxychloroquine (HCQ), a commonly used antimalarial drug in rheumatic diseases, has shown favorable metabolic effects on both glucose control and lipid profiles
Pharmacokinetics and metabolism
After administration of single 155 mg and 310 mg intravenous doses, peak blood concentrations ranged from 1161 ng/mL to 2436 ng/mL (mean 1918 ng/mL) following the 155 mg infusion and 6 months following the 310 mg infusion
In the past, chloroquine was used widely as a prophylactic agent to prevent Plasmodium infection
We developed and validated a simple and sensitive ultrahigh performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method for simultaneous quantitation of HCQ and its three metabolites in rat blood, and reported their pharmacokinetic parameters
HCQ and its metabolites are reversible CYP2D6 inhibitors, and HCQ metabolites are
Hydroxychloroquine is N-dealkylated by CYP3A4 to the active metabolite
Chloroquine and hydroxychloroquine are metabolized by P450 1A2, 2C8, 2C19, 2D6
Hydroxychloroquine is a 4-aminoquinoline used for the treatment of specific forms of malaria, rheumatoid arthritis, SLE, and Sjögren syndrome, with potential utility in
Scientific Reports - Simultaneous LC–MS/MS method for the quantitation of Azithromycin, Hydroxychloroquine and its metabolites in SARS-CoV-2(−/ +) populations using dried blood spots
The within- and between-day precision (relative standard deviation, % RSD) and accuracy were within the acceptable limits per FDA guidelines
0 µg/mL
Hydroxychloroquine (HCQ) is Food and Drug Administration (FDA)-approved as a treatment and prophylaxis for malaria and for chronic management of chronic discoid and systemic lupus erythematosus and rheumatoid arthritis
Hydroxychloroquine sulfate, USP is a colorless crystalline solid, soluble in water to at least 20 percent; chemically the drug is (±)-2-[[4-[(7-Chloro-4-quinolyl)amino]pentyl]ethylamino] ethanol sulfate (1:1) Peak blood concentrations of metabolites were observed at the same time as peak levels of hydroxychloroquine
Updating Hydroxychloroquine Physiologically-Based Pharmacokinetic Model
Our metabolism data indicated that CYP3A4, CYP2D6, and CYP2C8
(3) In the induction experiment, we restricted the analysis to marker genes of induction mediated quantitation of hydroxychloroquine and its metabolites in mouse blood and tissues using LC–ESI– MS/MS: an application for pharmacokinetic studies
In one study, mean peak plasma hydroxychloroquine concentrations following a single dose of 400mg in healthy subjects ranged from 53
Hydroxychloroquine (HCQ), a hydroxylated derivative of chloroquine (CQ), is an antirheumatic drug that is widely used in the treatment of autoimmune rheumatic diseases