Metabolic Study and Controlled Clinical Trials of Rifampin

Sunahara, S; Nakagawa, Hideo

doi:10.1378/chest.61.6_supplement.526

Cited by 44 publications

(7 citation statements)

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“…Deacetylation to form deacetyl-RIM and hydrolysis to afford formyl-RIM occur during RIM metabolism (50), and urine deacetyl-RIM decreased after repeated administration of RIM (49). The possible occurrence of very small amounts of the Ndemethylderivative (51) and of RIMquinone (26,52) in human urine clearly needs further supportive evidence, as also the possible induction (50) of RIM-glucuronidation (53).…”

Section: Inducton Properties Of Rifampicin and Rifabutin In Animalsmentioning

confidence: 99%

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Benedetti¹,

Dostert²

1994

Environ Health Perspect

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Animal studies have demonstrated that the mouse and rabbit are far more responsive to the inductive properties of rifamycin derivatives than the rat and guinea pig. The rat hepatic cytochrome P450 system seems to be resistant to the action of rifampicin unless very high doses are used. Mouse hepatic microsomal mixed-function oxidase activity is markedly increased by repeated dosing with rifampicin, whereas administration of rifabutin may be ineffective. In humans, both rifampicin and rifabutin are extensively metabolized and induce their own metabolism. The induced metabolic pathways remain essentially unknown. Under autoinduction conditions, the elimination half-life of rifampicin decreases, whereas that of rifabutin is not altered. Although the effects of repeated administration of rifampicin and rifabutin on the various forms of cytochrome P450 in humans have not been extensively examined, there is convincing evidence that the P4503A subfamily is induced by either drug, whereas the P4501 A subfamily and P4502D6 do not appear to be affected by rifampicin. Limited reliable information is available concerning the induction of human glucuronyltransferase activities by rifampicin and rifabutin which, however, do not seem to influence zidovudine glucuronide formation in healthy subjects.

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Section: Inducton Properties Of Rifampicin and Rifabutin In Animalsmentioning

confidence: 99%

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Benedetti¹,

Dostert²

1994

Environ Health Perspect

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“…Importantly, for the first-line drugs isoniazid and rifampicin, several analytical methods using ultraviolet-visible (UV-VIS) spectrophotometry have been used in several studies. 65–67 In addition, for ethambutol, 68 moxifloxacin, 69 levofloxacin, 70 ofloxacin, 71 paraaminosalicylic acid, 72 amoxicillin/clavulanate, 73 and imipenem/cilastatin, 74 UV-VIS spectrophotometry methods were described in literature. Remarkably, 1 analytical method that determines isoniazid, rifampicin, and pyrazinamide simultaneously with a UV-VIS spectrophotometer was published.…”

Section: Discussionmentioning

confidence: 99%

Systematic Review of Salivary Versus Blood Concentrations of Antituberculosis Drugs and Their Potential for Salivary Therapeutic Drug Monitoring

Elsen

Oostenbrink

Heysell

et al. 2018

Therapeutic Drug Monitoring

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For gatifloxacin and linezolid, salivary therapeutic drug monitoring is likely possible due to a narrow range of saliva-plasma and saliva-serum ratios. For isoniazid, rifampicin, moxifloxacin, ofloxacin, and clarithromycin, salivary therapeutic drug monitoring might be possible; however, a large variability in saliva-plasma and saliva-serum ratios was observed. Unfortunately, salivary therapeutic drug monitoring is probably not possible for doripenem and amoxicillin/clavulanate, as a result of very low salivary drug concentrations.

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“…We followed the Sunahara method to extract total rifamycins from urine samples [ 16 ]. In brief, 50 μl of 100 mM phosphate buffer (pH 7) was added to 100 μl of urine sample followed by 100 μl of isoamylalcohol.…”

Section: Methodsmentioning

confidence: 99%

Urine colorimetry to detect Low rifampin exposure during tuberculosis therapy: a proof-of-concept study

et al. 2016

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BackgroundThe cost and complexity of current approaches to therapeutic drug monitoring during tuberculosis (TB) therapy limits widespread use in areas of greatest need. We sought to determine whether urine colorimetry could have a novel application as a form of therapeutic drug monitoring during anti-TB therapy.MethodsAmong healthy volunteers, we evaluated 3 dose sizes of rifampin (150 mg, 300 mg, and 600 mg), performed intensive pharmacokinetic sampling, and collected a timed urine void at 4 h post-dosing. The absorbance peak at 475 nm was measured after rifamycin extraction. The optimal cutoff was evaluated in a study of 39 HIV/TB patients undergoing TB treatment in Botswana.ResultsIn the derivation study, a urine colorimetric assay value of 4.0 × 10−2 Abs, using a timed void 4 h after dosing, demonstrated a sensitivity of 92 % and specificity of 60 % to detect a peak rifampin concentration (Cmax) under 8 mg/L, with an area under the ROC curve of 0.92. In the validation study, this cutoff was specific (100 %) but insensitive (28 %). We observed similar test characteristics for a target Cmax target of 6.6 mg/L, and a target area under the drug concentration-versus-time curve (AUC0–8) target of 24.1 mg•hour/L.ConclusionsThe urine colorimetric assay was specific but insensitive to detect low rifampin serum concentrations among HIV/TB patients. In future work we will attempt to optimize sampling times and assay performance, with the goal of delivering a method that can translate into a point-of-care assessment of rifampin exposure during anti-TB therapy.

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Metabolic Study and Controlled Clinical Trials of Rifampin

Cited by 44 publications

References 1 publication

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.

Systematic Review of Salivary Versus Blood Concentrations of Antituberculosis Drugs and Their Potential for Salivary Therapeutic Drug Monitoring

Urine colorimetry to detect Low rifampin exposure during tuberculosis therapy: a proof-of-concept study

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