Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance

被引:0
|
作者
Habiburrahman, Muhammad [1 ]
Soetikno, Vivian [2 ]
Sirait, Wani Riselia [1 ]
Savira, Missy [1 ]
机构
[1] Univ Indonesia, Fac Med, Med Educ Study Program, Jakarta 10430, Indonesia
[2] Univ Indonesia, Dept Pharmacol & Therapeut, Fac Med, Natl Referral Hosp Ciptomangunkusumo, Jakarta 10430, Indonesia
来源
INDONESIAN JOURNAL OF PHARMACY | 2020年 / 31卷 / 04期
关键词
antibiotic; CEM-101; gonorrhea; solithromycin; resistance; ACQUIRED BACTERIAL PNEUMONIA; ANTIMICROBIAL RESISTANCE; ORAL SOLITHROMYCIN; DOUBLE-BLIND; CEM-101; SAFETY; ANTIBACTERIAL; SPECTINOMYCIN; SURVEILLANCE; MOXIFLOXACIN;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Gonorrhea is one of the most often sexually transmitted infection in the world. In 2016, WHO stated the Southeast Asia region as the fourth-highest incidence rate and prevalence of gonorrhea. One of the current problems with gonorrhea is related to its emerging resistance to first-line drugs such as cephalosporins, macrolides, and fluoroquinolones. This resistance has an impact on the difficulty of finding effective antibiotics to eradicate the infection, thus risking financial loss and infertility in sexually active age patients. This literature review will discuss solithromycin, the first fluoroketolide in phase III clinical trial, and show its potential as a new antibiotic against infection with resistant Neisseria gonorrhoeae. Literatures are searched using Pubmed and Google Scholar search engines with keywords: antibiotics, CEM-101, clinical trial, Neisseria gonorrhoeae, new treatment, pharmacology, pharmacokinetics, resistance, safety, and solithromycin. This semisynthetic antibiotic is supported by a different chemical structure from previous macrolides; improving solithromycin becomes more stable and able to bind easier with bacterial ribosomes. Pharmacologically, solithromycin provides an advantage in its high bioavailability, easy oral administration route, wide distribution, metabolism mainly in the liver, but not required dosage adjustments due to hepatic impairment, and a single dosage preparation that can increase patient compliance in healing gonorrhea infections. Also, its lower MIC50 than previous antibiotics makes it well-tolerated, therefore making this antibiotic as a potential recommendation for the management of multi-drug resistant gonorrhea in the future. Solithromycin is not inferior to the standard therapy (ceftriaxone and azithromycin), with 80% vs. 84% gonorrhea eradication rates. Per the anatomic site, the eradication rate is 92% in genital, 94% in the pharynx, and 83% in the rectum. However, special attention needs to be paid to the side effects of the gastrointestinal tract of solithromycin, as observed in phase III clinical trials at a dose of 1000 mg in the form of diarrhea (24%) and nausea (21%).
引用
收藏
页码:335 / 353
页数:19
相关论文
共 50 条
  • [31] Surveillance of antibiotic resistance in Neisseria gonorrhoeae in the Netherlands, 1977-95
    van de Laar, MJW
    van Duynhoven, YTHP
    Dessens, M
    van Santen, M
    van Klingeren, B
    GENITOURINARY MEDICINE, 1997, 73 (06): : 510 - 517
  • [32] Neisseria gonorrhoeae: first nationwide study on the spread of antibiotic resistance in Germany
    Horn, N.
    Kresken, M.
    Koerber-Irrgang, B.
    Wichelhaus, T. A.
    INTERNATIONAL JOURNAL OF MEDICAL MICROBIOLOGY, 2012, 302 : 125 - 125
  • [33] TRANSFER OF ANTIBIOTIC-RESISTANCE IN MIXED CULTURES OF NEISSERIA-GONORRHOEAE
    SARUBBI, FA
    SPARLING, PF
    JOURNAL OF INFECTIOUS DISEASES, 1974, 130 (06): : 660 - 663
  • [34] The epidemiology of global antibiotic resistance among Neisseria gonorrhoeae and Haemophilus ducreyi
    Ison, CA
    Dillon, JR
    Tapsall, JW
    LANCET, 1998, 351 : 8 - 11
  • [35] The Human Microbiome as a Focus of Antibiotic Discovery: Neisseria mucosa Displays Activity Against Neisseria gonorrhoeae
    Aho, Ellen L.
    Ogle, Jenie M.
    Finck, Anna M.
    FRONTIERS IN MICROBIOLOGY, 2020, 11
  • [36] Resistance of Neisseria gonorrhoeae to neutrophils
    Johnson, M. Brittany
    Criss, Alison K.
    FRONTIERS IN MICROBIOLOGY, 2011, 2
  • [37] Antimicrobial resistance in Neisseria gonorrhoeae
    Lind, I
    CLINICAL INFECTIOUS DISEASES, 1997, 24 : S93 - S97
  • [38] Fluorcquinolone resistance in Neisseria gonorrhoeae
    Knapp, JS
    Fox, KK
    Trees, DL
    Whittington, WL
    EMERGING INFECTIOUS DISEASES, 1997, 3 (01) : 33 - 39
  • [39] Resistance to peroxynitrite in Neisseria gonorrhoeae
    Barth, Kenneth R.
    Isabella, Vincent M.
    Wright, Lori F.
    Clark, Virginia L.
    MICROBIOLOGY-SGM, 2009, 155 : 2532 - 2545
  • [40] Quinolone resistance in Neisseria gonorrhoeae
    Janine R. Tompkins
    Jonathan M. Zenilman
    Current Infectious Disease Reports, 2001, 3 (2) : 156 - 161