Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance

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...

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Main Authors: Muhammad Habiburrahman, Vivian  Soetikno, Wani Riselia Sirait, Missy Savira
Format: Article
Language:English
Published: Universitas Gadjah Mada 2020-12-01
Series:Indonesian Journal of Pharmacy
Subjects:
Online Access:https://jurnal.ugm.ac.id/v3/IJP/article/view/1123
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author Muhammad Habiburrahman
Vivian  Soetikno
Wani Riselia Sirait
Missy Savira
author_facet Muhammad Habiburrahman
Vivian  Soetikno
Wani Riselia Sirait
Missy Savira
author_sort Muhammad Habiburrahman
collection DOAJ
description 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%).
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spelling doaj.art-cbae30110717402d9df5f0d7e0a579cb2022-12-21T19:29:27ZengUniversitas Gadjah MadaIndonesian Journal of Pharmacy2338-94272338-94862020-12-01335–353335–35310.22146/ijp.11231123Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae ResistanceMuhammad Habiburrahman0Vivian  Soetikno1Wani Riselia Sirait2Missy Savira3Medical Education Study Program, Faculty of Medicine Universitas Indonesia, Jakarta Indonesia 10430Department of Pharmacology and Therapeutics , Faculty of Medicine Universitas Indonesia—National Referral Hospital Ciptomangunkusumo, Jakarta Indonesia 10430Medical Education Study Program, Faculty of Medicine Universitas Indonesia, Jakarta Indonesia 10430Medical Education Study Program, Faculty of Medicine Universitas Indonesia, Jakarta Indonesia 10430Gonorrhea 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%).https://jurnal.ugm.ac.id/v3/IJP/article/view/1123antibioticcem-101gonorrheasolithromycinresistance
spellingShingle Muhammad Habiburrahman
Vivian  Soetikno
Wani Riselia Sirait
Missy Savira
Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
Indonesian Journal of Pharmacy
antibiotic
cem-101
gonorrhea
solithromycin
resistance
title Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_full Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_fullStr Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_full_unstemmed Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_short Solithromycin as A Potential Novel Antibiotic Against Neisseria Gonorrhoeae Resistance
title_sort solithromycin as a potential novel antibiotic against neisseria gonorrhoeae resistance
topic antibiotic
cem-101
gonorrhea
solithromycin
resistance
url https://jurnal.ugm.ac.id/v3/IJP/article/view/1123
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AT waniriseliasirait solithromycinasapotentialnovelantibioticagainstneisseriagonorrhoeaeresistance
AT missysavira solithromycinasapotentialnovelantibioticagainstneisseriagonorrhoeaeresistance