A new approach to the use of histamine skin tests in the study of antihistamine drugs

Joubert, L; Gaut, Zane N.; Abrams, William B.

doi:10.1002/cpt1969102250

Cited by 12 publications

(1 citation statement)

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“…In the initial work (Bain et al, 1948) the wheal areas were measured either by transcribing the wheals onto tracing paper and computing them directly, or by calculating the areas using the mean radius of each wheal; the radius has been obtained from the average of the two diameters measured at right angles to each other for each wheal (Joubert et al, 1969). In a more recent study (Sullivan, 1982) cross diameters of each wheal were measured and from their averages the wheal area calculated.…”

Section: Introductionmentioning

confidence: 99%

The basis of the histamine assay in skin.

Byrom

Clark

White

et al. 1991

Brit J Clinical Pharma

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1 The assay of wheal response to histamine injected sub-epidermally has been reviewed.Several discrepant claims were found in earlier work. 2 The saline control injection may evoke a wheal, which if present should be allowed for in the assay procedure. 3 There was no evidence for a limb dominance effect.4 Using a 3.26 mm (1 mg ml-1) standard solution of histamine acid phosphate (1.18 mm as free base) and 0.1 ml injections, the straight central portion of the assay curve was found to be between 0.3 and 2.3 x 10-3 mM, as free base, with an ED50 of about 0.018 mm histamine base.

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Section: Introductionmentioning

confidence: 99%

The basis of the histamine assay in skin.

Byrom

Clark

White

et al. 1991

Brit J Clinical Pharma

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Design of a suitable formulation of FK613, a novel antiallergic agent, based on its pharmacokinetic and pharmacodynamic properties in healthy subjects

Nagashima

Inaba

Kajiho

et al. 1996

Eur J Clin Pharmacol

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The pharmacokinetic and pharmacodynamic properties of FK613, a novel indolyl piperidine derivative, were investigated after oral administrations of 5, 10 and 20 mg in hard gelatin capsules to healthy male volunteers. FK613 was rapidly and almost completely absorbed, and >89% was recovered in the urine as the unchanged form. The urinary excretion of FK613 was linearly correlated with plasma concentration and its low water solubility was the main concern regarding the safety. In another experiment using a double-blind crossover design, in which 0 (placebo), 5 and 20 mg FK613 were administered to determine the plasma concentration-effect relationship, suppression of the intradermal histamine-induced skin reaction by FK613 was observed. Thus, the maintenance of a plasma concentration of FK613 in the range of 80-250 ng center dot ml-1 was recommended to ensure the suppression of histamine-induced wheal by >50% and not to exceed the solubility in urine. To achieve this, a new hydrogel-type formulation of FK613 was developed, with the aim both of delaying its absorption, so as to suppress the sharp rise in plasma concentration, and of maintaining the effective concentration for a longer period of time. This formulation was administered after meals at the doses of 20, 30, 40, 50 and 60 mg, and at repeated doses of 40 mg twice daily for 6.5 days to evaluate the pharmacokinetics and safety in healthy subjects. The area under the plasma concentration curve increased linearly with dose, whereas maximum plasma concentration (Cmax) tended to peak as dose increased, indicating the desirable properties of this formulation. Although Cmax exceeded 250 ng/ml at doses of 30 mg or more, no urinary crystal formation was observed on careful inspection of urine.

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