Stereospecific Radioimmunoassays for l-Ephedrine and d-Ephedrine in Human Plasma

Midhax, K.K.; Hubbard, John W.; Cooper, J.K.; Mackonka, C.

doi:10.1002/jps.2600720705

Cited by 13 publications

(2 citation statements)

References 20 publications

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“…The clinical effects of Mao may be attributed more to ephedrine than pseudoephedrine because the present study found that the concentration profiles of ephedrine were almost 3-fold higher. The reported elimination half life of ephedrine administered as 50 mg of oral racemic ephedrine hydrochloride is 4.8 h with Cmax ／ values of 100 ng／mL 22) ；those of d-and l-ephedrine are about 8 and 10 h with Cmax values of 100 and 70 ／ ng／mL under the same administration conditions 23) . These results confirmed the linear kinetic profile of ephedrine at a dose of 50 mg of racemic ephedrine hydrochloride.…”

Section: Discussionmentioning

confidence: 97%

“…Kampo preparations should be clinically evaluated to ensure their efficacy and safety, particularly in relation to the pharmacokinetics of their ingredients. Several studies have shown higher rate constants during the elimination phase compared with values during the absorption phase after the oral administration of ephedrine and pseudoephedrine ORIGINAL 81 alone [20][21][22][23] . The present study showed that the absorption and elimination rate constants were almost identical in 2 volunteers at both doses possibly because of relatively low absorption rate constants in these volunteers.…”

Section: Discussionmentioning

confidence: 99%

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Pharmacokinetics of Ephedrine and Pseudoephedrine after Oral Administration of Kakkonto to Healthy Male Volunteers

Inotsume

Fukushima

Hayakawa

et al. 2009

Jpn. J. Clin. Pharmacol. Ther.

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The pharmacokinetics of serum ephedrine and pseudoephedrine as the indexed reference ingredients of Kampo Kakkonto（ge-gen-tang in Chinese）were compared after the oral administration of 2.5 g and 3.75 g of Kakkonto extract. The mean maximal serum concentrations of ephedrine and pseudoephedrine obtained after the administration at 3.75 g were 1.50-and 1.58-fold higher（p＜0.05), respectively, than those obtained after the administration of 2.5 g, whereas the time required to reach the maximal concentration did not significantly differ between the two doses. The mean areas under the concentration-time curves of ephedrine and pseudoephedrine obtained after the 3.75 g of Kakkonto were 1.31-and 1.48-fold higher（p＜0.05), respectively, than those obtained after the 2.5 g dose, while no significant differences were observed in the mean residence time and elimination rate constant of the terminal phase between the doses. Disposition profiles showed that the kinetic behavior of ephedrine and pseudoephedrine were largely linear at the doses examined.

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Section: Discussionmentioning

confidence: 97%

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of Ephedrine and Pseudoephedrine after Oral Administration of Kakkonto to Healthy Male Volunteers

Inotsume

Fukushima

Hayakawa

et al. 2009

Jpn. J. Clin. Pharmacol. Ther.

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Studies on drug metabolism by use of isotopes XXIX—studies of the differences in biological fates of ephedrine isomers by use of a pseudo-racemic mixture

Baba¹,

Kuroda²,

Horie³

1986

Biol. Mass Spectrom.

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The differences in metabolic fates of the optical isomers of ephedrine were investigated by use of a pseudo-racemic mixture technique. In rats, the (-)-isomer was more easily p-hydroxylated than the (+)-isomer. A stereoselective reaction in the formation of the glucuronides of ephedrine, norephedrine and p-hydroxyephedrine was observed. The (-)-isomers were more easily subjected to glucuronide formation than the (+)-isomers. In human subjects, N-demethylation proved to be a stereoselective reaction. It is also suspected that oxidative dealkylation of norephedrine is a stereoselective reaction.

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Consideration of other techniques

Lough¹,

Matlin²

1989

Chiral Liquid Chromatography

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Stereospecific Radioimmunoassays for l-Ephedrine and d-Ephedrine in Human Plasma

Cited by 13 publications

References 20 publications

Pharmacokinetics of Ephedrine and Pseudoephedrine after Oral Administration of Kakkonto to Healthy Male Volunteers

Pharmacokinetics of Ephedrine and Pseudoephedrine after Oral Administration of Kakkonto to Healthy Male Volunteers

Studies on drug metabolism by use of isotopes XXIX—studies of the differences in biological fates of ephedrine isomers by use of a pseudo-racemic mixture

Consideration of other techniques

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