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Linezolid and serotonin syndrome.
J Int Med Res
February 2025
Department of Pharmacy Practice, College of Clinical Pharmacy, King Faisal University, Al-Ahsa, Saudi Arabia.
Linezolid, a synthetic oxazolidinone antibiotic, is used to treat gram-positive bacterial infections, including methicillin-resistant . Despite its efficacy, linezolid can cause serotonin syndrome, a potentially fatal condition associated with excessive serotonin activity in the brain. This narrative review examined the pharmacological mechanisms of this interaction, particularly linezolid's mild monoamine oxidase-inhibitory activity, which can trigger serotonin syndrome in combination with serotonergic drugs.
View Article and Find Full Text PDFOptimizing Linezolid: Transforming It into a Selective MAO-B Inhibitor via a Toxicity-to-Activity Optimization Approach.
ACS Med Chem Lett
January 2025
Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Maharashtra 425405, India.
Linezolid, a widely used oxazolidinone antibiotic, exhibits potent activity against resistant bacterial infections but is associated with serotonergic toxicity, primarily due to its inhibition of monoamine oxidase (MAO). MAOs, consisting of MAO-A and MAO-B isoforms, play crucial roles in neurotransmitter metabolism, with implications for neurodegenerative disorders like Parkinson's and Alzheimer's diseases. This study aims to optimize Linezolid's structure to transform it into a selective MAO-B inhibitor.
View Article and Find Full Text PDFStructural toxicity relationship (STR) of linezolid to mitigate myelosuppression and serotonergic toxicity.
Bioorg Med Chem
February 2025
Division of Computer Aided Drug Design, Department of Pharmaceutical Chemistry, R. C. Patel Institute of Pharmaceutical Education and Research, Shirpur, Dhule 425405, Maharashtra, India. Electronic address:
Article Synopsis
- * Linezolid is an effective drug in the BPaL regimen for treating these resistant TB strains, but its use can be limited due to side effects like myelosuppression and MAO inhibition.
- * Research is focusing on modifying Linezolid and its analogues to reduce toxic effects while maintaining their antibacterial effectiveness, leading to the development of safer alternatives for treating drug-resistant TB.
Novel biaryloxazolidinone derivatives with broad-spectrum antibacterial activity, favorable drug-like profiles and in vivo efficacy against linezolid-resistant Staphylococcusaureus.
Eur J Med Chem
July 2024
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe District, Shenyang 110016, China. Electronic address:
The emergence of multidrug-resistant bacteria along with a declining pipeline of clinically useful antibiotics has led to the urgent need for the development of more effective antibacterial agents to treat drug-resistant bacteria. We previously discovered compound OB-158 with potent antibacterial activity but exhibited poor oral bioavailability. Herein, a systematic structural optimization of OB-158 to improve pharmacokinetic profiles yielded 26 novel biaryloxazolidinone analogues, and their activities against Gram-positive S.
View Article and Find Full Text PDFAdvances in contezolid: novel oxazolidinone antibacterial in Gram-positive treatment.
Infection
June 2024
Center of Medicine Clinical Research, Department of Pharmacy, Medical Supplies Center, PLA General Hospital, 28 Fu Xing Road, Beijing, 100853, China.
Article Synopsis
- The project aimed to explore the chemical properties, pharmacological effects, and measurement techniques related to contezolid, an emerging antimicrobial agent.
- The review included various studies examining contezolid's effectiveness against infections, highlighting its improved efficacy and safety compared to linezolid, particularly in minimizing side effects.
- Contezolid is approved for treating complicated skin infections and offers a new treatment option against multi-drug resistant Gram-positive bacteria without the need for dose adjustments in patients with mild to moderate organ impairment.
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