Steady-State Pharmacokinetics of Hydroxychloroquine in Rheumatoid Arthritis Patients

Steady-state pharmacokinetics of hydroxychloroquine (HC) sulfate (Plaquenil) were studied in five volunteers with rheumatoid arthritis who had taken 6 mg/kg/d of the drug for at least six months. Blood samples were drawn at 0, 1, 2, 4, 6, 8, 12, and 24 hours following an oral dose. Both whole blood and plasma were assayed by an HPLC method for HC and its metabolites desethylhydroxychloroquine, desethylchloroquine, and didesethylchloroquine. A 24-hour urine collection was obtained and assayed for the same compounds. The pharmacokinetics of HC and its metabolites conformed to the model predicted by single-dose studies. During the 24-hour period the absorption phase and both early and late distribution phases were seen. Variation in mean maximum/minimum concentration was 40 percent. Renal clearance accounted for only 16 percent of unchanged HC (22 percent of total drug and metabolites) and did not correlate with creatinine clearance.

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as the subjects. In a 2 × 2 trial, for example, each subject is given a single dose of T and R and blood samples are taken at a series of time points subsequent to dosing. Each blood sample is then assayed to de-termine the concentration of drug in the blood plasma. Often the blood sampling is taken more frequently during what is expected to be the absorption phase of the drug and then less frequently during the elimi-nation phase. For each subject and period the concentrations of drug in the blood are plotted against the corresponding sampling times to give a concentration-time proﬁle for that subject and period. A typical proﬁle is given in Figure 7.1. Once the drug gets past the stomach and into the small intestine it begins to be absorbed into the blood, eventually reaching a peak con-centration. From then on the concentration diminishes as the drug is eliminated from the body. The area under the proﬁle is referred to as

Design and Analysis of Cross-Over Trials ◽

10.1201/9781420036091-4 ◽

2003 ◽

pp. 349-349

Keyword(s):

Small Intestine ◽

Single Dose ◽

Blood Plasma ◽

Time Profile ◽

The Body ◽

Blood Sampling ◽

Blood Samples ◽

Time Points ◽

Absorption Phase ◽

Sampling Times

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Effects of BMS-986256 at Steady State on the Single Dose Pharmacokinetics of Mycophenolate Mofetil

Case Medical Research ◽

10.31525/ct1-nct04039373 ◽

2019 ◽

Author(s):

Keyword(s):

Mycophenolate Mofetil ◽

Single Dose ◽

Steady State

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Faculty Opinions recommendation of D₂-receptor occupancy measurement of JNJ-37822681, a novel fast off-rate D₂-receptor antagonist, in healthy subjects using positron emission tomography: single dose versus steady state and dose selection.

Faculty Opinions – Post-Publication Peer Review of the Biomedical Literature ◽

10.3410/f.717953114.793458670 ◽

2012 ◽

Author(s):

John Davis

Keyword(s):

Positron Emission Tomography ◽

Single Dose ◽

Steady State ◽

Receptor Antagonist ◽

Healthy Subjects ◽

Receptor Occupancy ◽

Emission Tomography ◽

Dose Selection ◽

Positron Emission

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Single-Dose and Steady-State Pharmacokinetics of Diltiazem Administered in Two Different Tablet Formulations

Pharmacology & Toxicology ◽

10.1111/j.1600-0773.1992.tb00989.x ◽

1992 ◽

Vol 71 (4) ◽

pp. 305-307 ◽

Cited By ~ 3

Author(s):

Lona L. Christrup ◽

Jan Bonde ◽

Søren N. Rasmussen ◽

Jørn Møller Sonnergaard ◽

Bodil H. Jensen

Keyword(s):

Single Dose ◽

Steady State ◽

Tablet Formulations

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Efficacy and Safety of Mizoribine by One Single Dose Administration for Patients with Rheumatoid Arthritis

Internal Medicine ◽

10.2169/internalmedicine.49.3810 ◽

2010 ◽

Vol 49 (20) ◽

pp. 2211-2218 ◽

Cited By ~ 15

Author(s):

Kunihiro Ichinose ◽

Tomoki Origuchi ◽

Shin-ya Kawashiri ◽

Naoki Iwamoto ◽

Keita Fujikawa ◽

...

Keyword(s):

Rheumatoid Arthritis ◽

Single Dose ◽

Efficacy And Safety ◽

Dose Administration ◽

Single Dose Administration

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Tapering versus steady-state methotrexate in combination with tocilizumab for rheumatoid arthritis: a randomized, double-blind trial

Rheumatology ◽

10.1093/rheumatology/kex358 ◽

2017 ◽

Vol 57 (1) ◽

pp. 84-91 ◽

Cited By ~ 6

Author(s):

Christopher J Edwards ◽

Andrew J K Östör ◽

Barbara Naisbett-Groet ◽

Patrick Kiely

Keyword(s):

Rheumatoid Arthritis ◽

Steady State ◽

Double Blind Trial ◽

Double Blind ◽

Blind Trial

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Comparison of Fluconazole Pharmacokinetics in Serum, Aqueous Humor, Vitreous Humor, and Cerebrospinal Fluid Following a Single Dose and at Steady State

Journal of Ocular Pharmacology and Therapeutics ◽

10.1089/jop.1998.14.459 ◽

1998 ◽

Vol 14 (5) ◽

pp. 459-471 ◽

Cited By ~ 25

Author(s):

UMAR K. MIAN ◽

MARTIN MAYERS ◽

YOGENDER GARG ◽

QING-FENG LIU ◽

GIRARD NEWCOMER ◽

...

Keyword(s):

Cerebrospinal Fluid ◽

Single Dose ◽

Steady State ◽

Aqueous Humor ◽

Vitreous Humor

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Comparative Study for Carrot Juice and Selenium Supplement in Many Physiological and Biochemical Parameters in Patients with Rheumatoid Arthritis in Kirkuk City

Bionatura ◽

10.21931/rb/2021.06.04.15 ◽

2021 ◽

Vol 6 (4) ◽

pp. 2228-2232

Author(s):

Wedad Mahmood Lahmood Al-obaidi ◽

Mohanad Hasan Mahmood Al-Izzi ◽

Aya Saad yaseen

Keyword(s):

Rheumatoid Arthritis ◽

Rheumatoid Arthritis Group ◽

Carrot Juice ◽

Blood Samples ◽

Reactive Protein ◽

Tnf Α ◽

Group 3 ◽

Group 2 ◽

Physiological And Biochemical ◽

Β Carotene

Carrot juice is a critical source of vitamins, selenium, and β-carotene, which is suggested to protect from Rheumatoid Arthritis (RA). The present study aimed to show the effect of carrot juice supplementation compared to selenium tablet supplementation, so our study includes (44) blood samples belonging to young men with RA. All patients aged (20-45) years, 44 blood samples were obtained before treatment at week (0), twenty-four men with RA were supplied with fresh carrot juice. The other group of 20 patients was given an artificial selenium supplement for 21 days as well, and the results were analyzed.The samples were collected from Kirkuk hospital, and external specialized clinical from October/2019 to September /2020; experimental groups were divided into three groups: Group 1 : (44) men Rheumatoid arthritis (RA) before treatment, Group 2: (24) men with RA+ Carrot juice, Group 3: (20) men with RA +Selenium Tab, We reach to following results: the patients who have RA consumption Carrot juice and patients take up Se tab. show significant decrease respectively in RBCs, WBCs, ERS, and RF compared with the Rheumatoid arthritis group, so as the results show a significant decrease in Leptin, IL-6, C-Reactive Protein, and TNF-α concentrations in comparison with the Rheumatoid arthritis group. In contrast, we found a significant increase in GSH, Selenium concentrations, and VD3 in men with RA administration carrot juice and patients' consumption Se tab. Respectively compared with the RA group and, finally, our finding shows no difference in Ceruloplasmin in experimental groups.

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