Colchicine‐resistance and enhancement of P‐glycoprotein activity after co‐cultivation of drug‐sensitive cells with multidrug resistant variants.

Eliseenkova, Anna V.; Kakpakova, E. S.; Abdrjashitov, R I; Stavrovskaya, A. A.

doi:10.1006/cbir.1995.1051

Cited by 4 publications

(5 citation statements)

References 4 publications

(4 reference statements)

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“…In the study involving clarithromycin, colchicine (0.6 mg) was administered before and after a 7-day regimen of clarithromycin 250 mg (administered twice daily on days [22][23][24][25][26][27][28][29]. In the azithromycin pharmacokinetics study, azithromycin 500 mg (2 ϫ 250 mg) was administered on day 15, and 250 mg (once daily) was administered on days [16][17][18][19].…”

Section: Methodsmentioning

confidence: 99%

“…At each of the specified sampling times, a 6-ml blood sample was collected from each subject by direct venipuncture. Samples were collected immediately prior to the administration of each dose of colchicine, and at 0.5, 1, 1.5, 2, 2.5, 3,4,5,6,8,12,24,36,48,72, and 96 hours post-dose. Samples were centrifuged, and plasma was transferred to polypropylene tubes and stored at Ϫ20°C or colder until the time of sample analysis.…”

Section: Methodsmentioning

confidence: 99%

“…P-glycoprotein is associated with drug efflux from cells, and certain P-glycoprotein genetic variants are linked with instances of "drug resistance" in FMF (22,23). Thus, in theory, systemic concentrations of colchicine may be altered when it is coadministered with inhibitors of CYP3A4 and/or P-glycoprotein (24,25).…”

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confidence: 99%

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Novel evidence‐based colchicine dose‐reduction algorithm to predict and prevent colchicine toxicity in the presence of cytochrome P450 3A4/P‐glycoprotein inhibitors

Terkeltaub¹,

Fürst²,

DiGiacinto³

et al. 2011

Arthritis & Rheumatism

197

109

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Objective. Drug-drug interactions can limit the safety of colchicine for treating rheumatic diseases. Seven separate drug-drug interaction (DDI) studies were performed to elucidate the in vivo effects of concomitant treatment with colchicine and known inhibitors of cytochrome P450 3A4 (CYP3A4)/P-glycoprotein (cyclosporine, ketoconazole, ritonavir, clarithromycin, azithromycin, verapamil ER [extended release]), and diltiazem ER) on the pharmacokinetics of colchicine. The objective was to develop colchicine-dosing algorithms with improved safety. Methods.All studies were open-label, nonrandomized, single-center, one-sequence, two-period DDI experiments, using two 0.6-mg doses of colchicine, separated by a minimum 14-day washout period, followed by administration of the approved on-label regimen of known CYP3A4/P-glycoprotein inhibitors. Plasma concentrations of colchicine, but not the reference CYP3A4/P-glycoprotein inhibitors, were determined, and the pharmacokinetic parameters were calculated.Results. The ratios of the maximum concentration and area under the curve from time 0 to infinity for colchicine plus CYP3A4/P-glycoprotein inhibitors versus colchicine alone were >125% across all studies, with the exception of studies involving azithromycin. Significant DDIs were present when single doses of colchicine were coadministered with most of the selected CYP3A4/ P-glycoprotein inhibitors. Recommended colchicine dose reductions of 33-66% for the treatment of acute gout and 50-75% for prophylaxis were calculated for concomitant therapy with each agent, with the exception of no dose adjustment when colchicine is used in combination with azithromycin.Conclusion. These studies provide quantitative evidence regarding drug interactions and necessary adjustments in the dose of colchicine if colchicine treatment is continued during therapy with multiple CYP3A4/Pglycoprotein inhibitors. We demonstrated the need for specific reductions in the dose of colchicine when it is used in combination with 2 broadly prescribed calcium channel blockers (verapamil ER and diltiazem ER) and that the dose of colchicine does not need to be adjusted when it is used in combination with azithromycin.Despite the widespread use of colchicine for the treatment and prophylaxis of gout flares (1-5) and the ClinicalTrials

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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Novel evidence‐based colchicine dose‐reduction algorithm to predict and prevent colchicine toxicity in the presence of cytochrome P450 3A4/P‐glycoprotein inhibitors

Terkeltaub¹,

Fürst²,

DiGiacinto³

et al. 2011

Arthritis & Rheumatism

197

109

View full text Add to dashboard Cite

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“…15 It also inhibits fibroblast proliferation and total collagen synthesis; 16 (ii) colchicine also promotes expression of ABC proteins such as P-gp which shares great structural homology with CFTR. 7,8,17,18 Several recent data also suggest functional homology. CFTR overexpression leads to a multidrug-resistance phenotype similar to P-gp.…”

Section: Discussionmentioning

confidence: 91%

Interest of Colchicine for the Treatment of Cystic Fibrosis Patients. Preliminary Report

Sermet‐Gaudelus

Stoven

Annereau

et al. 1999

Mediators of Inflammation

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Cystic fibrosis (CF) lung disease is characterized by persistent inflammation. Antiinflammatory drugs, such as corticosteroids and ibuprofen, have proved to slow the decline of pulmonary function although their use is limited because of frequent adverse events. We hypothesized that colchicine could be an alternative treatment because of its antiinflammatory properties and upregulatory effect on cystic fibrosis transmembrane regulator (CFTR) closely related proteins. We herein present results obtained in an open study of eight CF children treated with colchicine for at least 6 months. Clinical status was better in all patients and respiratory function tests significantly improved in five. Median duration of antibiotherapy decreased significantly. These preliminary results support our hypothesis of a beneficial effect of colchicine in CF patients and stress the need for a controlled therapeutic trial.

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“…23,24 Therefore, it is expected that systemic concentrations of colchicine may be increased when the drug is coadministered with inhibitors of CYP3A4 and/or P-gp. [25][26][27] colchicine drug-drug interactions involving antibiotics Several antimicrobials are inhibitors of CYP3A4 and therefore have the potential to interact with colchicine. In particular, macrolide antibiotics and azole antifungals inhibit the isoenzyme CYP3A4 to varying degrees.…”

Section: Colchicine Pharmacokineticsmentioning

confidence: 99%

Colchicine-Antimicrobial Drug Interactions: What Pharmacists Need to Know in Treating Gout

Davis¹,

Wason²,

DiGiacinto³

2013

The Consultant Pharmacist

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obJecTive: Review the magnitude and clinical relevance of drug-drug interactions between a new formulation of colchicine, used to treat gout, and antibiotics. seTTinG and PracTice descriPTion: Relevant to community and institutional pharmacists servicing patients with gout.PracTice innovaTion: Pharmacists have clear roles for the identification of drug-drug interactions, providing recommendations for alternative therapy or dose adjustments/modifications, and monitoring for interactionrelated adverse events.abbreviaTions: AE = Adverse event, AUC = Area under the drug concentration-time curve, C max = Maximum plasma concentration, CYP = Cytochrome P450, NSAID = Nonsteroidal anti-inflammatory drug, P-gp = P-glycoprotein efflux transporter.

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Colchicine‐resistance and enhancement of P‐glycoprotein activity after co‐cultivation of drug‐sensitive cells with multidrug resistant variants.

Cited by 4 publications

References 4 publications

Novel evidence‐based colchicine dose‐reduction algorithm to predict and prevent colchicine toxicity in the presence of cytochrome P450 3A4/P‐glycoprotein inhibitors

Novel evidence‐based colchicine dose‐reduction algorithm to predict and prevent colchicine toxicity in the presence of cytochrome P450 3A4/P‐glycoprotein inhibitors

Interest of Colchicine for the Treatment of Cystic Fibrosis Patients. Preliminary Report

Colchicine-Antimicrobial Drug Interactions: What Pharmacists Need to Know in Treating Gout

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