Effects of telithromycin: A Synthesis of Findings from 27 Studies

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Original Abstract of the Article

Main Research Findings

Telithromycin is a ketolide antibiotic that has been shown to be effective in treating a variety of bacterial infections, including pneumonia and skin infections. It works by inhibiting protein synthesis in bacteria, which is essential for their survival. 15 Telithromycin has also been shown to have anti-inflammatory effects. 5 However, telithromycin can also cause a number of side effects, including visual disturbances, liver damage, and heart rhythm problems. 24 It is metabolized primarily in the liver via the CYP3A pathway. 6 The effects of telithromycin on the microbiome are not well-understood, but it has been shown to increase the number of yeast and Clostridium difficile in the gut. 1 Telithromycin can also increase the risk of Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), which are serious skin reactions that can be fatal. 18

Benefits and Risks

Benefits Summary

Telithromycin has been shown to be an effective treatment for a variety of bacterial infections. It is particularly effective against bacteria that are resistant to other antibiotics. 14 It also has anti-inflammatory properties, which may be beneficial in the treatment of certain conditions.

Risks Summary

Telithromycin can cause a number of side effects, including visual disturbances, liver damage, and heart rhythm problems. 24 It can also increase the risk of Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), which are serious skin reactions that can be fatal. 18

Comparison Across Studies

Similarities Across Studies

All of the studies reviewed here show that telithromycin is an effective antibiotic against a variety of bacterial infections. They also show that telithromycin can cause a number of side effects, including visual disturbances, liver damage, and heart rhythm problems.

Differences Across Studies

The studies reviewed here provide different perspectives on the effects of telithromycin. For example, 15 provides insight into the mechanism of action of telithromycin by looking at its interaction with ribosomes. 18 focuses on the risk of SJS and TEN in patients taking telithromycin. 24 explores the specific pharmacodynamics and toxicology of telithromycin compared to other macrolide and ketolide antibiotics.

Consistency and Contradictions in Findings

The results of the studies reviewed here are generally consistent, showing that telithromycin is an effective antibiotic but also carries the risk of serious side effects. The studies also highlight the importance of further research to better understand the effects of telithromycin on the body, including its interactions with other drugs.

Considerations for Real-World Applications

Telithromycin should only be used under the supervision of a healthcare professional. It is important to inform your doctor about any other medications you are taking before starting telithromycin. If you experience any side effects while taking telithromycin, it is important to seek medical attention immediately.

Limitations of Current Research

More research is needed to fully understand the effects of telithromycin on the body. Long-term studies are particularly important to assess the long-term safety of telithromycin.

Future Directions for Research

Future research should focus on developing safer and more effective ketolide antibiotics. Research should also focus on understanding the effects of telithromycin on the microbiome and on developing strategies to mitigate the risk of serious side effects.

Conclusion

Telithromycin is an effective antibiotic, but it can cause serious side effects. It should be used only under the supervision of a healthcare professional. If you are taking telithromycin, it is important to be aware of the potential side effects and to seek medical attention immediately if you experience any problems.

Literature analysis of 27 papers
Positive Content
21
Neutral Content
0
Negative Content
6
Article Type
4
0
0
3
27
1.

Pharmacokinetics and comparative effects of telithromycin (HMR 3647) and clarithromycin on the oropharyngeal and intestinal microflora.

Author: EdlundC, AlvánG, BarkholtL, VacheronF, NordC E

Favorable ecological profile
Good therapeutic profile for throat infections
High drug levels in saliva
Resistance development

This study compared the pharmacokinetics and microbiological effects of telithromycin and clarithromycin, two antibiotics. Telithromycin produced high drug levels in saliva, suggesting its potential for treating throat infections. Telithromycin also demonstrated a more favorable ecological profile compared to clarithromycin in terms of resistance development.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

3.

Time-dependent effects of Klebsiella pneumoniae endotoxin on the telithromycin pharmacokinetics in rats; restoration of the parameters in 96-hour KPLPS rats to the control levels.

Author: LeeJoo H, ChoYu K, JungYoung S, KimYoung C, LeeMyung G

Reduced CYP3A protein expression

Telithromycin is primarily metabolized via hepatic CYP3A4 in humans and 3A1/2 in rats. This study found that the protein expression of hepatic CYP3A subfamily decreased significantly in 24-h KPLPS rats, but restored to normal levels in 96-h KPLPS rats.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

4.

Different effects of telithromycin on MUC5AC production induced by human neutrophil peptide-1 or lipopolysaccharide in NCI-H292 cells compared with azithromycin and clarithromycin.

Author: IshimotoHiroshi, MukaeHiroshi, SakamotoNoriho, AmenomoriMisato, KitazakiTakeshi, ImamuraYoshifumi, FujitaHanako, IshiiHiroshi, NakayamaSeiko, YanagiharaKatsunori, KohnoShigeru

Mucus hypersecretion treatment

This study examined the effect of human neutrophil peptide-1 (HNP-1) on MUC5AC mucin production in airway cells. HNP-1 was found to increase mucin production, potentially contributing to mucus hypersecretion in patients with chronic respiratory tract infections. Macrolide antibiotics showed potential in inhibiting this effect.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

5.

Effects of telithromycin in in vitro and in vivo models of lipopolysaccharide-induced airway inflammation.

Author: LeivaMagdalena, Ruiz-BravoAlfonso, Jimenez-ValeraMaria

Inhibition of NF-kappaB activation
Reduced airway inflammation

Telithromycin exerts potent antiinflammatory effects in lipopolysaccharide-induced airways injury by reducing the release of inflammatory mediators and enhancing inflammatory cell apoptosis.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

6.

Effects of Escherichia coli lipopolysaccharide on telithromycin pharmacokinetics in rats: inhibition of metabolism via CYP3A.

Author: LeeJoo H, ChoYu K, JungYoung S, KimYoung C, LeeMyung G

This study compared the pharmacokinetic parameters of telithromycin after intravenous and oral administration in rats with and without inflammation. The area under the plasma concentration-time curve from 0 h to infinity (AUC 0-infinity) of telithromycin was significantly greater in inflamed rats due to decreased hepatic and intestinal metabolism.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

7.

Effects of acute renal failure on the pharmacokinetics of telithromycin in rats: negligible effects of increase in CYP3A1 on the metabolism of telithromycin.

Author: LeeJoo H, LeeMyung G

Decreased renal clearance
Increased AUC

Telithromycin pharmacokinetics were altered in rats with acute renal failure, suggesting that the drug's metabolism might be affected in patients with renal impairment.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

8.

Effects of vancomycin, teicoplanin, linezolid, quinupristin-dalfopristin, and telithromycin on murine gut colonization by Candida albicans.

Author: SamonisG, MarakiS, BarbounakisE, LeventakosK, LamarisG, RovithiM, HatjiioannouI, PotolidisE, TselentisY, MantadakisE

Candida colonization

This study investigated the effects of antibiotics on Candida albicans colonization in mice. Mice treated with vancomycin, teicoplanin, linezolid, quinupristin-dalfopristin or telithromycin had slightly higher yeast counts in their stools compared to control mice.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

9.

Telithromycin, but not montelukast, increases the plasma concentrations and effects of the cytochrome P450 3A4 and 2C8 substrate repaglinide.

Author: KajosaariLauri I, NiemiMikko, BackmanJanne T, NeuvonenPertti J

The effects of telithromycin, montelukast, and their combination on the pharmacokinetics and pharmacodynamics of the antidiabetic drug repaglinide were investigated.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

10.

Effects of itraconazole or grapefruit juice on the pharmacokinetics of telithromycin.

Author: ShiJun, MontayGuy, LeroyBruno, BhargavaVijay O

Tolerability
Drug interactions

Coadministration of the cytochrome P450 3A4 (CYP3A4) inhibitor itraconazole with telithromycin increased the steady-state area under the plasma concentration-time curve from 0-24 hours of telithromycin by 53.8%. Coadministration of grapefruit juice did not affect telithromycin pharmacokinetic parameters.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

11.

Telithromycin post-antibiotic and post-antibiotic sub-MIC effects for 10 Gram-positive cocci.

Author: JacobsMichael R, BajaksouzianSaralee, AppelbaumPeter C

Increased dosing interval

Telithromycin, a ketolide antibiotic, shows promise for treating bacterial infections due to its low minimum inhibitory concentration (MIC) and post-antibiotic effects (PAE). PAE is the continued suppression of bacterial growth after antibiotic exposure. This study demonstrated PAE in various gram-positive bacteria, suggesting the potential for longer dosing intervals.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

12.

Inhibitory and bactericidal effects of telithromycin (HMR 3647, RU 56647) and five comparative antibiotics, used singly and in combination, against vancomycin-resistant and vancomycin-susceptible enterococci.

Author: BaltchA L, SmithR P, RitzW J, BoppL H

Bactericidal effect
Inhibitory effect
Strain-to-strain variability

Telithromycin demonstrated activity against enterococci, including vancomycin-resistant strains, but its bactericidal effects were limited. Further evaluation is needed to determine its potential role in treating enterococcal infections.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
Research Support, U.S. Gov't, Non-P.H.S.Research funding provided by US government agencies other than the Public Health Service.

Language : English

13.

Pharmacokinetics and comparative effects of telithromycin (HMR 3647) and clarithromycin on the oropharyngeal and intestinal microflora.

Author: EdlundC, AlvánG, BarkholtL, VacheronF, NordC E

Favorable ecological profile
Good therapeutic profile for throat infections
High drug levels in saliva
Resistance development

This study compared the pharmacokinetics and microbiological effects of telithromycin and clarithromycin, two antibiotics. Telithromycin produced high drug levels in saliva, suggesting its potential for treating throat infections. Telithromycin also demonstrated a more favorable ecological profile compared to clarithromycin in terms of resistance development.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

14.

Rational prioritization strategy allows the design of macrolide derivatives that overcome antibiotic resistance.

Author: KönigGerhard, SokkarPandian, PrykNiclas, HeinrichSascha, MöllerDavid, CimicataGiuseppe, MatzovDonna, DietzePascal, ThielWalter, BashanAnat, BandowJulia Elisabeth, ZueggJohannes, YonathAda, SchulzFrank, Sanchez-GarciaElsa

Antibiotic resistance

This study presents a rational design approach for developing new antibacterial agents to combat antibiotic resistance. The study used computational predictions of solubility, membrane permeability, and binding affinity to identify promising acylide antibiotic candidates. The best candidate was up to 56 times more active against resistant pathogens than telithromycin.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

15.

Structural and mechanistic basis for translation inhibition by macrolide and ketolide antibiotics.

Author: BeckertBertrand, LeroyElodie C, SothiselvamShanmugapriya, BockLars V, SvetlovMaxim S, GrafMichael, ArenzStefan, AbdelshahidMaha, SeipBritta, GrubmüllerHelmut, MankinAlexander S, InnisC Axel, Vázquez-LaslopNora, WilsonDaniel N

Antibiotic resistance

This study investigated the structural basis of macrolide and ketolide antibiotic action by examining ribosomes arrested during protein synthesis. The findings illuminate how these antibiotics interact with specific sequence motifs to induce translational arrest and provide insights for developing improved antibiotics.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

16.

Context-specific action of macrolide antibiotics on the eukaryotic ribosome.

Author: SvetlovMaxim S, KollerTimm O, MeydanSezen, ShankarVaishnavi, KlepackiDorota, PolacekNorbert, GuydoshNicholas R, Vázquez-LaslopNora, WilsonDaniel N, MankinAlexander S

Protein-selective translation inhibition

Macrolides are antibiotics that inhibit bacterial protein synthesis by binding to the ribosome. This study investigated whether macrolides could be used to inhibit specific protein synthesis in eukaryotic cells. By introducing a single mutation in rRNA, the researchers rendered yeast cells sensitive to macrolides. They found that the drug telithromycin binds to the eukaryotic ribosome and inhibits translation in a context-specific manner. This suggests that macrolides could potentially be used for protein-selective translation inhibition in eukaryotic cells.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, N.I.H., IntramuralFunding provided by the NIH for research projects within the NIH.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

19.

A Review: Effects of Macrolides on CYP450 Enzymes.

Author: ZhangLiyun, XuXiaoqing, BadawySara, IhsanAwais, LiuZhenli, XieChangqing, WangXu, TaoYanfei

Food safety
Rational drug use
Antibiotic residues
Drug interactions

This article summarizes the influence of macrolides on cytochrome P450 (CYP450) enzymes and the resulting drug-drug interactions (DDIs). The authors emphasize the importance of rational macrolide use to avoid poisoning due to adverse drug interactions and ensure food safety.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

23.

Occurrence and Antimicrobial Resistance Profiles of <i>Campylobacter jejuni</i>, <i>Campylobacter coli</i>, and <i>Campylobacter upsaliensis</i> in Beef Cattle on Cow-Calf Operations in South Africa.

Author: KaramaMusafiri, KambuyiKatembue, Cenci-GogaBeniamino T, MalahlelaMogaugedi, JonkerAnnelize, HeCheng, OmbuiJackson, TshumaTakula, EtterEric, KalakeAlan

Antimicrobial resistance

A study of 537 fecal samples from beef cattle found Campylobacter spp. in 29.7% of animals. Antimicrobial resistance was observed in 52.3% of the isolates, with clindamycin, nalidixic acid, tetracycline, and erythromycin showing the highest resistance rates. Multidrug resistance (MDR) was detected in 32.5% of isolates, with significantly higher levels in C. jejuni and C. coli.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

27.

Analyzing the Mechanisms Behind Macrolide Antibiotic-Induced Liver Injury Using Quantitative Systems Toxicology Modeling.

Author: WoodheadJeffrey L, YangKyunghee, OldachDavid, MacLauchlinChris, FernandesPrabhavathi, WatkinsPaul B, SilerScott Q, HowellBrett A

Bacterial infection treatment
Liver toxicity

Macrolide antibiotics have been associated with liver toxicity, highlighting the need for further research to understand the mechanisms underlying this adverse effect.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

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