Displaying publications 1 - 20 of 47 in total

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  1. Takasaka M, Morota S, Kasono T, Abe M, Honjo S
    Jikken Dobutsu, 1973 Jul;22(3):227-36.
    PMID: 4204642
    Matched MeSH terms: Rifampin/therapeutic use
  2. Jani J, Mustapha ZA, Jamal NB, Stanis CS, Ling CK, Avoi R, et al.
    Data Brief, 2019 Oct;26:104445.
    PMID: 31534995 DOI: 10.1016/j.dib.2019.104445
    A Mycobacterium tuberculosis strain SBH162 was isolated from a 49-year-old male with pulmonary tuberculosis. GeneXpert MDR/RIF identified the strain as rifampicin-resistant M. tuberculosis. The whole genome sequencing was performed using Illumina HiSeq 4000 system to further investigate and verify the mutation sites of the strain through genetic analyses namely variant calling using bioinformatics tools. The de novo assembly of genome generated 100 contigs with N50 of 156,381bp. The whole genome size was 4,343,911 bp with G + C content of 65.58% and consisted of 4,306 predicted genes. The mutation site, S450L, for rifampicin resistance was detected in the rpoB gene. Based on the phylogenetic analysis using the Maximum Likelihood method, the strain was identified as belonging to the Europe America Africa lineage (Lineage 4). The genome dataset has been deposited at DDBJ/ENA/GenBank under the accession number SMOE00000000.
    Matched MeSH terms: Rifampin
  3. Dhana A, Hamada Y, Kengne AP, Kerkhoff AD, Rangaka MX, Kredo T, et al.
    Lancet Infect Dis, 2022 Apr;22(4):507-518.
    PMID: 34800394 DOI: 10.1016/S1473-3099(21)00387-X
    BACKGROUND: The WHO-recommended tuberculosis screening and diagnostic algorithm in ambulatory people living with HIV is a four-symptom screen (known as the WHO-recommended four symptom screen [W4SS]) followed by a WHO-recommended molecular rapid diagnostic test (eg Xpert MTB/RIF [hereafter referred to as Xpert]) if W4SS is positive. To inform updated WHO guidelines, we aimed to assess the diagnostic accuracy of alternative screening tests and strategies for tuberculosis in this population.

    METHODS: In this systematic review and individual participant data meta-analysis, we updated a search of PubMed (MEDLINE), Embase, the Cochrane Library, and conference abstracts for publications from Jan 1, 2011, to March 12, 2018, done in a previous systematic review to include the period up to Aug 2, 2019. We screened the reference lists of identified pieces and contacted experts in the field. We included prospective cross-sectional, observational studies and randomised trials among adult and adolescent (age ≥10 years) ambulatory people living with HIV, irrespective of signs and symptoms of tuberculosis. We extracted study-level data using a standardised data extraction form, and we requested individual participant data from study authors. We aimed to compare the W4SS with alternative screening tests and strategies and the WHO-recommended algorithm (ie, W4SS followed by Xpert) with Xpert for all in terms of diagnostic accuracy (sensitivity and specificity), overall and in key subgroups (eg, by antiretroviral therapy [ART] status). The reference standard was culture. This study is registered with PROSPERO, CRD42020155895.

    FINDINGS: We identified 25 studies, and obtained data from 22 studies (including 15 666 participants; 4347 [27·7%] of 15 663 participants with data were on ART). W4SS sensitivity was 82% (95% CI 72-89) and specificity was 42% (29-57). C-reactive protein (≥10 mg/L) had similar sensitivity to (77% [61-88]), but higher specificity (74% [61-83]; n=3571) than, W4SS. Cough (lasting ≥2 weeks), haemoglobin (<10 g/dL), body-mass index (<18·5 kg/m2), and lymphadenopathy had high specificities (80-90%) but low sensitivities (29-43%). The WHO-recommended algorithm had a sensitivity of 58% (50-66) and a specificity of 99% (98-100); Xpert for all had a sensitivity of 68% (57-76) and a specificity of 99% (98-99). In the one study that assessed both, the sensitivity of sputum Xpert Ultra was higher than sputum Xpert (73% [62-81] vs 57% [47-67]) and specificities were similar (98% [96-98] vs 99% [98-100]). Among outpatients on ART (4309 [99·1%] of 4347 people on ART), W4SS sensitivity was 53% (35-71) and specificity was 71% (51-85). In this population, a parallel strategy (two tests done at the same time) of W4SS with any chest x-ray abnormality had higher sensitivity (89% [70-97]) and lower specificity (33% [17-54]; n=2670) than W4SS alone; at a tuberculosis prevalence of 5%, this strategy would require 379 more rapid diagnostic tests per 1000 people living with HIV than W4SS but detect 18 more tuberculosis cases. Among outpatients not on ART (11 160 [71·8%] of 15 541 outpatients), W4SS sensitivity was 85% (76-91) and specificity was 37% (25-51). C-reactive protein (≥10 mg/L) alone had a similar sensitivity to (83% [79-86]), but higher specificity (67% [60-73]; n=3187) than, W4SS and a sequential strategy (both test positive) of W4SS then C-reactive protein (≥5 mg/L) had a similar sensitivity to (84% [75-90]), but higher specificity than (64% [57-71]; n=3187), W4SS alone; at 10% tuberculosis prevalence, these strategies would require 272 and 244 fewer rapid diagnostic tests per 1000 people living with HIV than W4SS but miss two and one more tuberculosis cases, respectively.

    INTERPRETATION: C-reactive protein reduces the need for further rapid diagnostic tests without compromising sensitivity and has been included in the updated WHO tuberculosis screening guidelines. However, C-reactive protein data were scarce for outpatients on ART, necessitating future research regarding the utility of C-reactive protein in this group. Chest x-ray can be useful in outpatients on ART when combined with W4SS. The WHO-recommended algorithm has suboptimal sensitivity; Xpert for all offers slight sensitivity gains and would have major resource implications.

    FUNDING: World Health Organization.

    Matched MeSH terms: Rifampin
  4. Lai JML, Yang SL, Avoi R
    J Glob Infect Dis, 2019 3 1;11(1):2-6.
    PMID: 30814828 DOI: 10.4103/jgid.jgid_50_18
    Introduction: Conventionally, a combination of four separate drugs (ethambutol, isoniazid, rifampicin, and pyrazinamide [EHRZ]) is the first-line pharmacotherapy for pulmonary tuberculosis (TB). In recent years, fixed-dose combination (FDC) formulation, where a single tablet contains the active ingredients of four aforementioned drugs, is gaining popularity due to its ease of administration.

    Objective: To compare the real-world effectiveness of EHRZ and FDC treatment groups on a cohort registry by investigating the sputum conversion rate and treatment outcomes of both groups.

    Methods: A total of 11,489 patients' data were extracted from the Sabah TB registry between January 2012 and June 2016, including EHRZ (n = 4188) and FDC (n = 7301) patients. Then, 1:1 propensity score matching was adopted to reduce the baseline bias. Caliper matching was conducted with maximum tolerance score set at 0.001. Confounders included in the propensity score matching were gender, nationality, diabetes, HIV status, smoking status, and chest X-ray status. Successful matching provided 4188 matched pairs (n = 8376) for final analysis.

    Results: In this matched cohort of 4188 pairs, the 2-month sputum conversion rate of FDC group was significantly higher than the EHRZ group (96.3% vs. 94.3%; P < 0.001) whereas 6-month sputum conversion of both groups showed no significant difference. Treatment outcomes such as noncompliance rate, failure rate, and success rate have no significant difference (P > 0.05) in both the treatment groups. There was an incidental finding of reduced death rate among FDC group compared to the EHRZ group (0.2% vs. 0.5%; P = 0.034).

    Conclusion: The FDC formulation has better sputum conversion rate at 2 months compared to conventional EHRZ regime as separate-drug formulation. It was also observed that FDC has a slight protective effect against all-cause death among TB patients. This protective effect of FDC, however, still needs to be proven further.

    Matched MeSH terms: Rifampin
  5. Ding CH, Ismail Z, Sulong A, Wahab AA, Gan B, Mustakim S, et al.
    Malays J Pathol, 2020 Dec;42(3):401-407.
    PMID: 33361721
    INTRODUCTION: Rifampicin is a key first-line antimycobacterial agent employed for the treatment of pulmonary tuberculosis (PTB). This study sought to obtain prevalence data on rifampicin-resistant Mycobacterium tuberculosis among smear-positive PTB patients in the Klang District of Malaysia.

    MATERIALS AND METHODS: A total of 103 patients from the Chest Clinic of Hospital Tengku Ampuan Rahimah with sputum smears positive for acid-fast bacilli were included in this cross-sectional study. All sputa were tested using Xpert MTB/RIF to confirm the presence of M. tuberculosis complex and detect rifampicin resistance. Sputa were also sent to a respiratory medicine institute for mycobacterial culture. Positive cultures were then submitted to a reference laboratory, where isolates identified as M. tuberculosis complex underwent drug susceptibility testing (DST).

    RESULTS: A total of 58 (56.3%) patients were newly diagnosed and 45 (43.7%) patients were previously treated. Xpert MTB/RIF was able to detect rifampicin resistance with a sensitivity and specificity of 87.5% and 98.9%, respectively. Assuming that a single resistant result from Xpert MTB/RIF or any DST method was sufficient to denote resistance, a total of 8/103 patients had rifampicinresistant M. tuberculosis. All eight patients were previously treated for PTB (p<0.05). The overall prevalence of rifampicin resistance among smear-positive PTB patients was 7.8%, although it was 17.8% among the previously treated ones.

    CONCLUSION: The local prevalence of rifampicin-resistant M. tuberculosis was particularly high among previously treated patients. Xpert MTB/RIF can be employed in urban district health facilities not only to diagnose PTB in smear-positive patients, but also to detect rifampicin resistance with good sensitivity and specificity.

    Matched MeSH terms: Rifampin/therapeutic use
  6. Damanhuri NS, Kumolosasi E, Omar MS, Razak AFA, Mansor AH
    Daru, 2021 Jun;29(1):13-22.
    PMID: 33405191 DOI: 10.1007/s40199-020-00377-2
    BACKGROUND: P-glycoprotein (P-gp) is an Adenosine triphosphate (ATP) dependent drug-efflux pump which is located abundantly in the stomach and protects the gut mucosa from xenobiotic.

    OBJECTIVE: The purpose of this study was to investigate the influence of P-gp modulation on the efficacy of treatment regimen.

    METHOD: P-gp modulation in rats was performed by using P-gp inducer (150 mg/kg rifampicin) and P-gp inhibitor (10 mg/kg cyclosporine A) for 14 days prior to be infected with Helicobacter pylori (H. pylori). The rats were further divided into groups, which were normal control, vehicle control, antibiotics and omeprazole, antibiotics only and omeprazole only for another 2 weeks of treatment. The ulcer formation and P-gp expression were determined by using macroscopic evaluation and western blot analysis, respectively.

    RESULTS: The highest P-gp expression was shown in the induced P-gp rats (2.00 ± 0.68) while the lowest P-gp expression was shown in the inhibited P-gp rats (0.45 ± 0.36) compared to the normal P-gp rats. In all groups, the rats which were infected with H. pylori, had a significant increase (p 

    Matched MeSH terms: Rifampin/pharmacology
  7. Hou LJ, Raju SS, Abdulah MS, Nor NM, Ravichandran M
    Jpn J Infect Dis, 2004 Oct;57(5):198-202.
    PMID: 15507775
    Chloroquine (CQ)-resistant Plasmodium falciparum appears to decrease CQ accumulation in its food vacuole by enhancing its efflux via an active membrane pump, which has been reported to be a P-glycoprotein-like transporter. Rifampicin (RIF) is a P-glycoprotein inhibitor and also has some antimalarial activity. It is hoped that a combination of choloroquine-rifampicin (CQ + RIF) would be advantageous in the treatment of CQ-resistant malaria. Swiss albino mice were inoculated with CQ-resistant P. berghei intraperitoneally, and studied for the effect of CQ versus the combination of CQ + RIF at various doses on the clearance of parasitemia, the survival of the mice, and the recrudescence of malaria. Paradoxically, RIF decreased the survival rate and rate of clearance of parasitemia and increased the rate of recrudescence significantly when combined with various doses of CQ. Our results indicated that RIF worsened the course of the disease, and we concluded that RIF should not be combined with CQ in the treatment of malaria.
    Matched MeSH terms: Rifampin/administration & dosage; Rifampin/pharmacology*
  8. Lee SL, Lim WJ, Chai ST
    Med J Malaysia, 2020 09;75(5):591-593.
    PMID: 32918434
    A 67-year-old mental institute resident was treated for smear-positive pulmonary tuberculosis. His background history included chronic essential hypertension which was well-controlled with amlodipine 10mg daily. However, his blood pressure became suboptimal one week into antitubercular treatment, necessitating escalation of antihypertensive therapy up to six medications. Following completion of antitubercular treatment, his blood pressure improved markedly. The number of antihypertensives was able to be reduced to only two after a month. We postulate that rifampicin has attenuated the therapeutic effect of amlodipine via potent induction of hepatic CYP3A4 but the failure to control the blood pressure even with medications unrelated to cytochrome P450 pathways raises the spectre of an additional interaction.
    Matched MeSH terms: Rifampin/adverse effects*; Rifampin/pharmacology*
  9. Nielsen HL, Tarpgaard IH, Fuglsang-Damgaard D, Thomsen PK, Brisse S, Dalager-Pedersen M
    JMM Case Rep, 2018 Aug;5(8):e005163.
    PMID: 30323938 DOI: 10.1099/jmmcr.0.005163
    Introduction: Elizabethkingia anophelis is a Gram-negative, aerobic, non-motile rod belonging to the family Flavobacteriaceae. Over the last 5 years, it has emerged as an opportunistic human pathogen involved in neonatal meningitis and sepsis, as well as nosocomial outbreaks. It has been isolated from the midgut of the Anopheles gambiae mosquito, but there is no evidence for a role of the mosquito in human infections, and very little is known regarding the routes of transmission to humans. Recent studies, primarily from South-East Asia, suggest that E. anophelis, and not Elizabethkingia meningoseptica, is the predominant human pathogen of this genus. However, identification to the species level has been difficult due to the limitations of the current MALDI-TOF MS (matrix-associated laser desorption ionization-time of flight MS) systems for correct species identification.

    Case presentation: Here, we present a rare case of E. anophelis meningitis in a Danish male, who had a travel exposure to Malaysia 7 weeks before hospitalization. A multidrug-resistant Elizabethkingia species was isolated from blood and cerebrospinal fluid, and genomic sequencing was used to characterize the phylogenetic position of the isolate, which was determined as associated with previously described sublineage 11. The patient was successfully treated with intravenous moxifloxacin and rifampicin for 2 weeks with no major sequelae, but we did not find the source of transmission.

    Conclusion: All clinical microbiologists should be aware of the present limitations of the MALDI-TOF MS systems for correct species identification, and therefore we recommend the use of genome sequencing for the correct identification at the species and sublineage level.

    Matched MeSH terms: Rifampin
  10. Sing CK, Md. Zahirul Islam Khan, Hassan Hj. Mohd Daud, Abd. Rahman Aziz
    Sains Malaysiana, 2016;45:1597-1602.
    The present study was conducted to determine the prevalence and antibiotic resistance of Salmonella sp. isolated from
    African catfish (Clarias gariepinus). A total of 30 catfish were harvested from four different farms and four different
    wet markets. A total of 60 samples (30 catfish skins and 30 catfish intestines) were used for Salmonella sp. isolation
    (pellet-method), its biochemical and serological test. Confirmation of Salmonella sp. were determined by polyvalent
    O antisera and polymerase chain reaction (PCR) using genus specific primers for invA genes (DNA amplification
    showed one distinct band with molecular weight of 389 bp) and the species of isolated Salmonella sp. were identified
    by serotyping. The result showed 6/30 (20%) of fish or 6/60 (10%) of organ samples were positive for Salmonella sp.
    Among those positive for Salmonella sp., 4/6 were from intestine samples and 2/6 were from skin samples. No significant
    difference was found in the prevalence of Salmonella sp. isolates between fish harvested from farms and wet markets
    (p-value= 0.406). The Salmonella serovars identified were Salmonella corvallis (n=3), Salmonella mbandaka (n=2)
    and Salmonella typhmurium (n=1). Salmonella sp. isolates were resistance to Penicillin (P 10, 100%), Clindamycin
    (DA 2, 100%), Tetracycline (TE 30, 100%) and Rifampicin (RD 5, 100%) and all of the isolates were susceptible or
    intermediate resistance to Ceftazidime (CAZ 30) and Trimethopin (W 5). Multiple antibiotic resistance (MAR) index of
    all Salmonella sp. isolates in current study was 0.67 indicating that fish sampled in the present study was under high
    risk of been exposed to the tested antibiotics.
    Matched MeSH terms: Rifampin
  11. Weerekoon L
    Br J Ophthalmol, 1972 Feb;56(2):106-13.
    PMID: 5010311
    Matched MeSH terms: Rifampin/administration & dosage; Rifampin/therapeutic use
  12. Nur Hidayah Masod, Noraziah Mohamad Zin, Alfizah Hanafiah
    Sains Malaysiana, 2018;47:543-549.
    Tuberculosis (TB) is a major health problem in many developing countries including Malaysia. In Malaysia, the number of death due to tuberculosis has decreased, but there is rising concern on the increase of drug resistance (multi drug resistance tuberculosis) cases. In this study, patients’ demographic data were analyzed and the susceptibility of Mycobacterium tuberculosis against anti-tuberculosis agents (isoniazid, streptomycin, rifampicin and ethambutol) was determined using susceptibility MYCOTB plates. A total of 40 clinical M. tuberculosis isolates, isolated from patients in PPUKM were randomly selected. Among these, 62.5% were male (mean age: 36.9±17.9 years) and 37.5% were female (mean age: 42.6±16.6 years). Malay patients accounted for the highest percentage of TB cases which was 60%, followed by Indians 15%, 5% Chinese and 20% other ethnics. The isolation of M. tuberculosis from clinical samples were 60%, 17.5%, 7.5%, 7.5%, 5% and 2.5% from sputum, tracheal aspirate, pus, blood, BAL and tissue, respectively. This is correlated with the majority of the patients (67.5%) infected with M. tuberculosis having persistent cough symptoms. The results from MYCOTB and BACTEC MGIT 960 susceptibility testing were compared. The average time taken to do the anti-TB susceptibility test by using MYCOTB plate and BACTEC MGIT 960 was 2 and 40.5 min, respectively. Cost per sample for MYCOTB and BACTEC MGIT 960 was RM16.65 and RM42.80, respectively. To conclude, based on our demographic data, TB infection was the highest amongst male Malay patients and the main specimens that been received was sputum sample. MYCOTB plate was more preferable than BACTEC MGIT 960 for the susceptibility testing and all clinical samples were 100% susceptible to all tested anti-TB agents. Data gathered from this study can be used as guideline for the management of TB diagnosis and treatment in the future.
    Keywords: BACTEC MGIT 960; Mycobacterium tuberculosis; MYCOTB plate; tuberculosis
    Matched MeSH terms: Rifampin
  13. Zaw MT, Emran NA, Lin Z
    J Infect Public Health, 2018 04 26;11(5):605-610.
    PMID: 29706316 DOI: 10.1016/j.jiph.2018.04.005
    BACKGROUND: Rifampicin (RIF) plays a pivotal role in the treatment of tuberculosis due to its bactericidal effects. Because the action of RIF is on rpoB gene encoding RNA polymerase β subunit, 95% of RIF resistant mutations are present in rpoB gene. The majority of the mutations in rpoB gene are found within an 81bp RIF-resistance determining region (RRDR).

    METHODOLOGY: Literatures on RIF resistant mutations published between 2010 and 2016 were thoroughly reviewed.

    RESULTS: The most commonly mutated codons in RRDR of rpoB gene are 531, 526 and 516. The possibilities of absence of mutation in RRDR of rpoB gene in MDR-TB isolates in few studies was due to existence of other rare rpoB mutations outside RRDR or different mechanism of rifampicin resistance.

    CONCLUSION: Molecular methods which can identify extensive mutations associated with multiple anti-tuberculous drugs are in urgent need so that the research on drug resistant mutations should be extended.

    Matched MeSH terms: Rifampin
  14. Lim KT, Teh CS, Yusof MY, Thong KL
    Trans R Soc Trop Med Hyg, 2014 Feb;108(2):112-8.
    PMID: 24336696 DOI: 10.1093/trstmh/trt111
    The prevalence of resistance to rifampicin and fusidic acid among Malaysian strains of methicillin-resistant Staphylococcus aureus (MRSA) is increasing. This study aimed to determine the mechanisms of rifampicin and fusidic acid resistance and the genetic diversity of MRSA strains from a Malaysian tertiary hospital.
    Matched MeSH terms: Rifampin/pharmacology*
  15. Yuan X, Amarnath Praphakar R, Munusamy MA, Alarfaj AA, Suresh Kumar S, Rajan M
    Carbohydr Polym, 2019 Feb 15;206:1-10.
    PMID: 30553301 DOI: 10.1016/j.carbpol.2018.10.098
    Natural polymer guar gum has one of the highest viscosities in water solution and hence, these are significantly used in pharmaceutical applications. Guar gum inter-connected micelles as a new carrier has been developed for poor water soluble rifampicin drug. The hydrogel inter-connected micelle core was formulated as a hydrophilic inner and hydrophobic outer core by using guar gum/chitosan/polycaprolactone and the carrier interaction with rifampicin was confirmed by FT-IR. The morphological observations were carried out through TEM, SEM and AFM analysis. The encapsulation efficiency and in-vitro drug release behavior of prepared hydrogel based micelle system was analyzed by UV-vis spectrometry. The anti-bacterial activity against K. pneumoniae and S. aureus was studied by observing their ruptured surface by SEM. The cytotoxicity study reveals that the pure polymeric system has no toxic effect whereas drug loaded ones showed superior activity against THP-1 cells. From the cell apoptosis analyses, the apoptosis was carried out in a time dependent manner. The cell uptake behavior was also observed in THP-1 cells which indicate that the hydrogel based micelle system is an excellent material for the mucoadhesive on intracellular alveolar macrophage treatment.
    Matched MeSH terms: Rifampin/pharmacology*; Rifampin/chemistry
  16. Norazah A, Lim VKE, Koh YT, Rohani MY, Zuridah H, Spencer K, et al.
    J Med Microbiol, 2002 Dec;51(12):1113-1116.
    PMID: 12466411 DOI: 10.1099/0022-1317-51-12-1113
    The emergence and spread of multiresistant methicillin-resistant Staphylococcus aureus (MRSA) strains, especially those resistant to fusidic acid and rifampicin, in Malaysian hospitals is of concern. In this study DNA fingerprinting by PFGE was performed on fusidic acid- and rifampicin-resistant isolates from Malaysian hospitals to determine the genetic relatedness of these isolates and their relationship with the endemic MRSA strains. In all, 32 of 640 MRSA isolates from 9 Malaysian hospitals were resistant to fusidic acid and rifampicin. Seven PFGE types (A, ZC, ZI, ZJ, ZK, ZL and ZM) were observed. The commonest type was type ZC, seen in 72% of isolates followed by type A, seen in 13%. Each of the other types (ZI, ZJ, ZK, ZL and ZM) was observed in a single isolate. Each type, even the commonest, was found in only one hospital. This suggests that the resistant strains had arisen from individual MRSA strains in each hospital and not as a result of the transmission of a common clone.
    Matched MeSH terms: Rifampin/pharmacology*
  17. Ikryannikova LN, Afanas'ev MV, Akopian TA, Il'ina EN, Kuz'min AV, Larionova EE, et al.
    J Microbiol Methods, 2007 Sep;70(3):395-405.
    PMID: 17602768
    A MALDI TOF MS based minisequencing method has been developed and applied for the analysis of rifampin (RIF)- and isoniazid (INH)-resistant M. tuberculosis strains. Eight genetic markers of RIF resistance-nucleotide polymorphisms located in RRDR of rpoB gene, and three of INH resistance including codon 315 of katG gene and -8 and -15 positions of the promoter region of fabG1-inhA operon were worked out. Based on the analysis of 100 M. tuberculosis strains collected from the Moscow region in 1997-2005 we deduced that 91% of RIF-resistant and 94% of INH-resistant strains can be identified using the technique suggested. The approach is rapid, reliable and allows to reveal the drug resistance of M. tuberculosis strains within 12 h after sample isolation.
    Matched MeSH terms: Rifampin/pharmacology
  18. Jalalonmuhali M, Lee YY, Lee CK, Ismail R, Chandran PA
    Int J Dermatol, 2014 Feb;53(2):234-7.
    PMID: 22913324 DOI: 10.1111/j.1365-4632.2012.05463.x
    Matched MeSH terms: Rifampin/therapeutic use
  19. Parumasivam T, Ashhurst AS, Nagalingam G, Britton WJ, Chan HK
    Mol Pharm, 2017 01 03;14(1):328-335.
    PMID: 27977216 DOI: 10.1021/acs.molpharmaceut.6b00905
    Rifapentine is an anti-tuberculosis (anti-TB) drug with a prolonged half-life, but oral delivery results in low concentrations in the lungs because of its high binding (98%) to plasma proteins. We have shown that inhalation of crystalline rifapentine overcomes the limitations of oral delivery by significantly enhancing and prolonging the drug concentration in the lungs. The delivery of crystalline particles to the lungs may promote inflammation. This in vivo study characterizes the inflammatory response caused by pulmonary deposition of the rifapentine particles. The rifapentine powder was delivered to BALB/c mice by intratracheal insufflation at a dose of 20 mg/kg. The inflammatory response in the lungs and bronchoalveolar lavage (BAL) was examined at 12 h, 24 h, and 7 days post-treatment by flow cytometry and histopathology. At 12 and 24 h post-treatment, there was a significant influx of neutrophils into the lungs, and this returned to normal by day 7. A significant recruitment of macrophages occurred in the BAL at 24 h. Consistent with these findings, histopathological analysis demonstrated pulmonary vascular congestion and significant macrophage recruitment at 12 and 24 h post-treatment. In conclusion, the pulmonary delivery of crystalline rifapentine caused a transient neutrophil-associated inflammatory response in the lungs that resolved over 7 days. This observation may limit pulmonary delivery of rifapentine to once a week at a dose of 20 mg/kg or less. The effectiveness of weekly dosing with inhalable rifapentine will be assessed in murine Mycobacterium tuberculosis infection.
    Matched MeSH terms: Rifampin/administration & dosage; Rifampin/adverse effects; Rifampin/analogs & derivatives*
  20. Omar MS, Damanhuri NS, Kumolosasi E
    Turk J Gastroenterol, 2017 Jan;28(1):53-59.
    PMID: 27991853 DOI: 10.5152/tjg.2016.0409
    BACKGROUND/AIMS: Helicobacter pylori is a carcinogenic bacterium that could induce P-glycoprotein expression in the human gastrointestinal tract. Bacterial adherence to the gastrointestinal cell lines could be influenced by the level of P-glycoprotein. This study aimed to determine the influence of proton pump inhibitors that exhibit an inhibitory effect on P-glycoprotein in gastrointestinal carcinoma cell lines, namely Caco-2 and LS174T, in relation to H. pylori adherence.

    MATERIALS AND METHODS: Caco-2 and LS174T cells lines treated with omeprazole and esomeprazole were used in this study to assess the bacterial attachment of H. pylori within certain incubation periods.

    RESULTS: The presence of proton pump inhibitors increased the H. pylori adherence in a time-dependent manner in both Caco-2 and LS174T cell lines. The double inhibition of P-glycoprotein using proton pump inhibitor and P-glycoprotein inhibitor caused low P-glycoprotein expression in the cell lines, resulting in higher H. pylori adherence compared to the control cell lines.

    CONCLUSION: Proton pump inhibitors may alter P-glycoprotein expression in the gastrointestinal tract, and subsequently H. pylori adherence on the cell lines, and may contribute to resistance to drug therapy.

    Matched MeSH terms: Rifampin/pharmacology
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