Half-Life of Rifampicin after Repeated Administration of Different Doses in Humans

Curci, G; Bergamini, N.; Veneri, Federica; A, Ninni; Nitti, V

doi:10.1159/000220873

Cited by 23 publications

(5 citation statements)

References 2 publications

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“…It readily diffuses into most organs, tissues, bones, and body fluids, including exudates into TB-infected lung cavities. 29 About 20% of serum concentration has been observed in the saliva and other high-concentration therapeutic concentrations appeared in the lachrymal glands, tears, and urine. 30 The lateral ventricles house the choroid plexus, which is responsible for producing the CSF found in the brain.…”

Section: Resultsmentioning

confidence: 99%

Visualization of Time-Dependent Distribution of Rifampicin in Rat Brain Using MALDI MSI and Quantitative LCMS/MS

Shobo

BratkowskaDominika

Baijnath

et al. 2015

ASSAY and Drug Development Technologies

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Rifampicin (RIF) is a major component for short-course chemotherapy against tuberculosis, since it is active against rapidly metabolizing as well as dormant bacteria. According to the Lipinski rules, RIF should not enter the blood-brain barrier. Visualization of tissue drug distribution is of major importance in pharmacological studies; thus, far imaging of RIF in the brain has been limited to positron emission tomography. We propose using matrix-assisted laser desorption/ionization mass spectrometry imaging techniques as a suitable alternative for the visualization and localization of drug tissue distribution. Using the liquid chromatography mass spectrometric (LCMS) technique, we were able to quantify the concentrations of RIF in the uninfected rat brain; we paired this with matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI MSI) to show the time-dependent manner in which RIF is able to enter the brain. Our results show that even at the minute concentrations measured with LCMS/MS we were able visualize the drug and show its exact distribution in the rat brain. Other available methods require nuclear labeling and the detection of gamma rays produced by labeled compounds to visualize the compound and its localization; MALDI MSI is a more recently developed technique, which can provide detailed information on drug distribution in tissues when compared to other imaging techniques. This study shows that without any requirement for complex preprocessing we are able to produce images with a relatively improved resolution and localization than those acquired using more complex imaging methods, showing MALDI MSI to be an invaluable tool in drug distribution studies.

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Section: Resultsmentioning

confidence: 99%

Visualization of Time-Dependent Distribution of Rifampicin in Rat Brain Using MALDI MSI and Quantitative LCMS/MS

Shobo

BratkowskaDominika

Baijnath

et al. 2015

ASSAY and Drug Development Technologies

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“…The other liver function tests were carried out according to the routine methods used in the Hepatology Division. Calculation on half-life times of rifampicin was carried out as already described [1,2].…”

Section: Methodsmentioning

confidence: 99%

“…Previous investigations by our group [1,2] showed that, in subjects with normal liver function, an increase in the administered dose from 8 to 16 mg/kg b.w. is accompanied by a more than proportional increase in blood serum levels together with significant differences in half-life time.…”

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confidence: 99%

Studies on Blood Serum Levels of Rifampicin in Patients with Normal and Impaired Liver Function

Curci¹,

Claar²,

Bergamini³

et al. 1973

Chemotherapy

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Patients with normal liver function present a dose-related change in the kinetics of rifampicin. The drug interferes with serum bilirubin levels. Interference with serum bilirubin levels practically disappears during repeated administration. This fact is paralleled by a change in the slope of the excretory part of rifampicin blood serum level curve. Patients with liver cirrhosis or with other type of severe liver impairment present higher blood serum levels of the antibiotic. The slope of the curve is flat and remains practically constant during repeated administration. The interference with blood serum bilirubin remains unchanged throughout the treatment period. In such patients, a dose of 6–8 mg/kg b.w. of rifampicin should not be exceeded.

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“…This dilemma highlights the necessity of carefully tailored dosage adjustments. RIF shows a dose-dependent elevation in serum concentration [ 73 , 74 , 75 , 76 , 77 ], underscoring the importance of meticulous dosage adjustments to enhance its efficacy. In the treatment of bacterial meningitis, it is crucial to rapidly eliminate bacteria from the CSF to ensure survival without neurological impairment [ 78 ].…”

Section: Resultsmentioning

confidence: 99%

Comprehensive Therapeutic Approaches to Tuberculous Meningitis: Pharmacokinetics, Combined Dosing, and Advanced Intrathecal Therapies

Madadi,

Sohn

2024

Pharmaceutics

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Tuberculous meningitis (TBM) presents a critical neurologic emergency characterized by high mortality and morbidity rates, necessitating immediate therapeutic intervention, often ahead of definitive microbiological and molecular diagnoses. The primary hurdle in effective TBM treatment is the blood–brain barrier (BBB), which significantly restricts the delivery of anti-tuberculous medications to the central nervous system (CNS), leading to subtherapeutic drug levels and poor treatment outcomes. The standard regimen for initial TBM treatment frequently falls short, followed by adverse side effects, vasculitis, and hydrocephalus, driving the condition toward a refractory state. To overcome this obstacle, intrathecal (IT) sustained release of anti-TB medication emerges as a promising approach. This method enables a steady, uninterrupted, and prolonged release of medication directly into the cerebrospinal fluid (CSF), thus preventing systemic side effects by limiting drug exposure to the rest of the body. Our review diligently investigates the existing literature and treatment methodologies, aiming to highlight their shortcomings. As part of our enhanced strategy for sustained IT anti-TB delivery, we particularly seek to explore the utilization of nanoparticle-infused hydrogels containing isoniazid (INH) and rifampicin (RIF), alongside osmotic pump usage, as innovative treatments for TBM. This comprehensive review delineates an optimized framework for the management of TBM, including an integrated approach that combines pharmacokinetic insights, concomitant drug administration strategies, and the latest advancements in IT and intraventricular (IVT) therapy for CNS infections. By proposing a multifaceted treatment strategy, this analysis aims to enhance the clinical outcomes for TBM patients, highlighting the critical role of targeted drug delivery in overcoming the formidable challenges presented by the blood–brain barrier and the complex pathophysiology of TBM.

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Half-Life of Rifampicin after Repeated Administration of Different Doses in Humans

Cited by 23 publications

References 2 publications

Visualization of Time-Dependent Distribution of Rifampicin in Rat Brain Using MALDI MSI and Quantitative LCMS/MS

Visualization of Time-Dependent Distribution of Rifampicin in Rat Brain Using MALDI MSI and Quantitative LCMS/MS

Studies on Blood Serum Levels of Rifampicin in Patients with Normal and Impaired Liver Function

Comprehensive Therapeutic Approaches to Tuberculous Meningitis: Pharmacokinetics, Combined Dosing, and Advanced Intrathecal Therapies

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