Grapefruit Juice and its Constituents Augment Colchicine Intestinal Absorption: Potential Hazardous Interaction and the Role of P-Glycoprotein

Dahan, Arik; Amidon, Gordon L.

doi:10.1007/s11095-008-9789-7

Cited by 82 publications

(53 citation statements)

References 47 publications

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“…Thus, explanations for the antigenotoxic effect of Nar may also be related with actions that modify the biotransformation of the antineoplastic, as well as the efficacy of its transportation or its effect on the cell cycle. Such explanations include the controversially described inhibitory effect on the CYP3A4 enzyme, [35][36][37] the modifying effect on other enzymes as CYP1A2, hepatic acylCoA:cholesterol acyltransferase, or esterase, 35,38,39) in addition to a pharmacokinetics intervention by altering the P-glycoprotein-mediated drug efflux, [40][41][42][43] or the induction of the G1 cell cycle arrest. 44) These proposals suggest that Nar may have more than one form of action, depending on the particular experimental conditions.…”

Section: Discussionmentioning

confidence: 99%

Effect of Naringin on the DNA Damage Induced by Daunorubicin in Mouse Hepatocytes and Cardiocytes

Cariño-Cortés

Álvarez-González²,

Roaro³

et al. 2010

Biological & Pharmaceutical Bulletin

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Naringin (Nar) is a flavonoid that has shown antigenotoxic effect against the chromosome damage induced by various compounds. The aims of the present investigation on Nar were threefold: a) to determine its DNA breaking potential in mouse hepatocytes and cardiocytes, b) to evaluate its capacity to inhibit the DNA damage induced by daunorubicin (Dau) in the same tissues, and c) to determine its capacity to trap free radicals in vitro using the 1,1-diphenyl-2-picryl-hydrazyl (DPPH) method. For the two first purposes we applied the comet assay to three groups of animals administered with Nar by the oral route (50, 250, 500 mg/kg), and made the observations before the chemical administration and at 3, 12, and 21 h postadministration. Other three groups of mice were given equal doses of Nar, and 1 h later they were intraperitoneally injected with 1 mg/kg of Dau. The results showed that Nar did not induce DNA breakage in both types of studied cells, in contrast with the significant damage induced by Dau in hepatocytes and cardiocytes. Moreover, the administration of Nar protected the DNA damage produced by Dau, showing a maximum reduction of 71.3% and 51.1% in hepatocytes and cardiocytes, respectively. With respect to the antioxidant potential, 20 mM of Nar produced a free radical scavenging activity as high as 95%. Our study established a high DNA breaking potential of Dau, and a protective effect by Nar, probably related with its capacity to trap free radicals.

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Section: Discussionmentioning

confidence: 99%

Effect of Naringin on the DNA Damage Induced by Daunorubicin in Mouse Hepatocytes and Cardiocytes

Cariño-Cortés

Álvarez-González²,

Roaro³

et al. 2010

Biological & Pharmaceutical Bulletin

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“…The experimental procedure followed previous reports (22,23). Briefly, anesthetized rats were placed on a heated (37°C) surface (Harvard Apparatus Inc., Holliston, MA), and a midline abdominal incision of 3-4 cm was made.…”

Section: Rat Intestinal Perfusionsmentioning

confidence: 99%

Regional-Dependent Intestinal Permeability and BCS Classification: Elucidation of pH-Related Complexity in Rats Using Pseudoephedrine

Fairstein

Swissa

Dahan

2013

AAPS J

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Abstract. Based on its lower Log P value relative to metoprolol, a marker for the low/high-permeability (P eff ) class boundary, pseudoephedrine was provisionally classified as BCS low-permeability compound. On the other hand, following oral administration, pseudoephedrine fraction dose absorbed (F abs ) and systemic bioavailability approaches 100%. This represents a challenge to the generally recognized P eff -F abs correlation. The purpose of this study was to elucidate the underlying mechanisms behind the confusion in pseudoephedrine's BCS classification. Pseudoephedrine's BCS solubility class was determined, and its physicochemical properties and intestinal permeability were thoroughly investigated, both in vitro and in vivo in rats, considering the complexity of the whole of the small intestine. Pseudoephedrine was found to be unequivocally a high-solubility compound. All of the permeability studies revealed similar phenomenon; at any given intestinal segment/pH, the permeability of metoprolol was higher than that of pseudoephedrine, however, as the intestinal region becomes progressively distal, and the pH gradually increases, pseudoephedrine's permeability rises above that of metoprolol in the former segment. This unique permeability pattern likely explains pseudoephedrine's complete absorption. In conclusion, pseudoephedrine is a BCS Class I compound; no discrepancy between P eff and F abs is involved in its absorption. Rather, it reflects the complexity behind P eff when considering the whole of the intestine. We propose to allow high-permeability classification to drugs with P eff that matches/exceeds the low/high class benchmark anywhere throughout the intestinal tract and not restricted necessarily to the jejunum.

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“…Physicians should monitor for muscle involvement by measuring creatine kinase levels and advising colchicine-treated patients to report symptoms, especially those patients with chronic kidney disease or diabetes. Second, grapefruit juice may dramatically augment colchicine oral bioavailability (4,5), and due to a narrow therapeutic index for colchicine and severely toxic side effects, awareness of this interaction is necessary (5).…”

Section: To the Editormentioning

confidence: 99%

Advances in the proper use of colchicine and adapting dosages in other countries: Comment on the article by Terkeltaub et al

Lioté

2010

Arthritis & Rheumatism

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Grapefruit Juice and its Constituents Augment Colchicine Intestinal Absorption: Potential Hazardous Interaction and the Role of P-Glycoprotein

Abstract: The data suggest that GFJ may augment colchicine oral bioavailability. Due to colchicine narrow therapeutic-index and severely toxic side-effects, awareness of this interaction is prudent.

Cited by 82 publications

References 47 publications

Effect of Naringin on the DNA Damage Induced by Daunorubicin in Mouse Hepatocytes and Cardiocytes

Effect of Naringin on the DNA Damage Induced by Daunorubicin in Mouse Hepatocytes and Cardiocytes

Regional-Dependent Intestinal Permeability and BCS Classification: Elucidation of pH-Related Complexity in Rats Using Pseudoephedrine

Advances in the proper use of colchicine and adapting dosages in other countries: Comment on the article by Terkeltaub et al

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