Absorption and Excretion of 35s Dapsone in Dermatitis Herpetiformis

Alexander, J. O'd.; Young, E. Gordon; McFADYEN, T.; Fraser, Neil; Duguid, W. P.; Meredith, E. M.

doi:10.1111/j.1365-2133.1970.tb15756.x

Cited by 31 publications

(11 citation statements)

References 5 publications

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“…1.01 ± 0.11 1.09 ± 0.12 1.06 ± 0.12 range observed in the present study first order elimination kinetics were observed. Particularly in female volunteers highest DDS concentrations were measured very early compared to other studies, in which peak drug concentrations were reported to occur approximately 2 to 8 h after oral ingestion (Ahmad & Rogers, 1980a;Alexander et al, 1970;Lammintausta et al, 1979). In some studies the disease state of the patients might have caused a delay in absorption.…”

Section: Introduction Methodsmentioning

confidence: 73%

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The pharmacokinetics of dapsone after oral administration to healthy volunteers.

Pieters¹,

Zuidema²

1986

Brit J Clinical Pharma

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After oral administration of 100 mg dapsone (DDS) to 25 healthy volunteers peak serum DDS concentrations between 1.10 and 2.33 mg I-1 were reached within 0.5 to 4 h. AUCs varied from 20.3 to 75.4 mg I -1 h, while the elimination half-lives ranged from 11.5 to 29.2 h. The apparent volumes of distribution were 0.84 to 1.26 1 kg-l body weight, assuming complete bioavailability. Statistically significant differences in peak drug concentration, peak time and AUC existed between males and females. Absorption and elimination of DDS appeared to be faster than reported in other studies, suggesting differences in DDS kinetics between healthy volunteers and patients.

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Section: Introduction Methodsmentioning

confidence: 73%

“…Dapsone (diaminodiphenylsulphone, DDS) is slowly but probably well absorbed (Alexander et al, 1970). It has a relatively long elimination half-life (Ahmad & Rogers, 1980a;Gelber et al, 1971;Lammintausta et al, 1979;Peters et al, 1981;Swain et al, 1983).…”

Section: Introduction Methodsmentioning

confidence: 99%

The pharmacokinetics of dapsone after oral administration to healthy volunteers.

Pieters¹,

Zuidema²

1986

Brit J Clinical Pharma

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“…The amount in the polyethylene glycol precipitate is inversely proportional to the amount of competing, nonradiolabeled PG E2 in the test (supernatant) samples. The concentration of PG E2 in the supematants was calculated by using a standard curve with added pure PG E2 in the range of 1 (14). PMNL were pelleted at 12,000 x g for 3 min and the tubes were frozen at -70°C overnight.…”

Section: Methodsmentioning

confidence: 99%

Enhancement by clofazimine and inhibition by dapsone of production of prostaglandin E2 by human polymorphonuclear leukocytes in vitro

Anderson

1985

Antimicrob Agents Chemother

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The effects of the antileprosy agents clofazimine and dapsone (1 to 10 ,ig/mi) on the spontaneous and stimulated release of prostaglandin E2 (PG E2) by human polymorphonuclear leukocytes (PMNL) in vitro have been investigated. PMNL were obtained from normal adult volunteers and three patients with leprosy (two borderline lepromatous and one subpolar lepromatous leprosy). The synthetic chemotactic tripeptide N-formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP) at a concentration of 10-7 M was used as the stimulant of PG E2 synthesis. None of the test agents at the concentrations used inhibited the binding of radiolabeled FMLP to PMNL. However, dapsone at 5 and 10 ,ug/ml inhibited the spontaneous and FMLP-induced release of PG E2 by PMNL. Clofazimine, on the other hand, significantly Increased both the spontaneous and the FMLP-induced synthesis of PG E2 by PMNL. The enhancing effects of clofazimine on FMLP-mediated synthesis of PG E2 were particularly striking and were observed at concentrations of 1 to 10 jig of the drug per ml. Measurements of PMNL spontaneous and FMLP-induced synthesis of PG E2 in the presence of both clofazimine and dapsone (5 ,ug/ml) indicated that the two drugs are mutually antagonistic. PMNL from both normal control subjects and patients with leprosy were equally sensitive to these effects of clofazimine and dapsone. The immunostimulatory and immunosuppressive properties of dapsone and clofazimine, respectively, may be related to the opposite effects of these agents on PG E2 synthesis in human leukocytes.

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“…In man, the clearance rates of the two compounds do not differ No data are available on the occurrence or levels of other metabolites in the plasma of (23) * rats. In man receiving DDS, only DDS and MADDS have been found in the circulation by several laboratories (24)(25)(26). However, these compounds are minor urinary excretory products in both man and rats (7,22,27,28).…”

Section: Maddsmentioning

confidence: 97%

Disposition of Dapsone and Monoacetyldapsone in Rats

Peters

Ghoul

et al. 1975

Experimental Biology and Medicine

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From the time that the noncultivable Mycobacteriurn leprae was grown in mouse foot pads (1, 2), this rodent has been used widely for testing the activity of drugs against M . Zeprae and as the basis for laboratory studies of human leprosy (3). By the mouse foot pad test system, dapsone (4,4'-diaminodiphenyl sulfone, DDS), the most widely used drug for the treatment of human leprosy (4), was found to inhibit multiplication of M . Zeprae in mice exhibiting plasma levels of 1-10 ng DDS/ml ( 5 ) . The lower limit of this range was obtained by extrapolation and must be considered tentative.Previously, the disposition of DDS in mice (6) and human subjects (7) was examined to assess the value of the mouse as a model of man. Those studies showed that mice differed markedly from man in regard to the acetylation of DDS to monoacetyl DDS (MADDS), the deacetylation of MADDS to DDS, and the rate of clearance of DDS from the circulation. The only similarity between the two species was the extent of binding of DDS by plasma proteins. Thus, the mouse proved of little value as a model of man for studies on the disposition of DDS.A further disadvantage of the mouse test system is the limited multiplication of M . Zeprae in the foot pad. Other rodents have been tested (8, 9), but were not found to be superior to the mouse. More recently, Buffalo and Lewis rats that were neonatally thymec-

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Absorption and Excretion of 35s Dapsone in Dermatitis Herpetiformis

Cited by 31 publications

References 5 publications

The pharmacokinetics of dapsone after oral administration to healthy volunteers.

The pharmacokinetics of dapsone after oral administration to healthy volunteers.

Enhancement by clofazimine and inhibition by dapsone of production of prostaglandin E2 by human polymorphonuclear leukocytes in vitro

Disposition of Dapsone and Monoacetyldapsone in Rats

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