Azithromycin

Azithromycin 속성

Azithromycin MSDS

Azithromycin

Azithromycin C화학적 특성, 용도, 생산

용도

항생제는 호흡기 감염과 같은 다양한 민감한 세균 감염에 사용됩니다. 피부 및 연조직 감염.

용도

아지트로마이신(azithromycin)은 수많은 병균 감염 치료에 사용되는 항생물질이다. 여기에는 중이염, 연쇄상 구균 인두염, 폐렴, 물갈이, 기타 특정 장염이 포함된다. 클라미디아, 임질 등 수많은 성병에 대해서도 사용할 수 있다.다른 약물들과 함께 사용하여 말라리아를 대상으로 사용할 수도 있다.

개요

Azithromycin was the first of the azalides and was designed to improve the stability and biological half-life of erythromycin A, as well as improve activity against Gram negative bacteria. Azithromycin is a long-acting macrolide antibiotic structurally related to erythromycin A (EA), having a methyl-substituted nitrogen at position 9a in the aglycone ring.

화학적 성질

White Crystalline Powder

정의

ChEBI: Azithromycin is a macrolide antibiotic useful for the treatment of bacterial infections. It is an azalide, derived from erythromycin, and a member of a subclass of macrolide antibiotics with bacteriocidal and bacteriostatic activities.

Indications

Azithromycin in a 500-mg dose three times a week has been shown to yield a 60% reduction in inflammatory papules in 83% of patients enrolled in a 12- week study. There is no associated pseudotumor cerebri and, therefore, it can be used for an acne flare during early Accutane therapy.

Antimicrobial activity

It is less potent than erythromycin A against Gram-positive isolates, but is more active against Gram-negative bacteria. It is four times more potent than erythromycin A against H. influenzae, N. gonorrhoeae and Campylobacter spp., and twice as active against Mor. catarrhalis. It also exhibits superior potency against Enterobacteriaceae, notably Esch. coli, Salmonella enterica serotypes, and Shigella spp. It is active against Mycobacteria, notably the M. avium complex and against intracellular micro-organisms such as Legionella and Chlamydia spp.
Chemical modification at the 9 position of the erythronolide A ring of erythromycin A blocks the internal ketalization and markedly improves acid stability. At pH 2, loss of 10% activity occurred in less than 4 s with erythromycin A, but took 20 min with azithromycin. The AUC at 0–24 h is 4.5 mg.h/L. The level is only slightly increased on repeated dosing.
Binding to plasma protein varies with the concentration, from around 50% at 0.05 mg/L to 7.1% at 1 mg/L. The apparent elimination half-life is dependent upon sampling interval: between 8 and 24 h it ranged from 11 to 14 h; between 24 and 72 h it was 35–40 h.
It rapidly penetrates the tissues, reaching levels that approach or, in some cases, exceed the simultaneous plasma levels and persist for 2–3 days. Only about 6% of the dose is found in urine in the first 24 h.

일반 설명

The spectrum of antimicrobial activity of azithromycin issimilar to that observed for erythromycin and clarithromycinbut with some interesting differences. In general,it is more active against Gram-negative bacteria and less activeagainst Gram-positive bacteria than its close relatives.The greater activity of azithromycin against H. influenzae,M. catarrhalis, and M. pneumoniae coupled with its extendedhalf-life permits a 5-day dosing schedule for thetreatment of respiratory tract infections caused by thesepathogens. The clinical efficacy of azithromycin in the treatmentof urogenital and other sexually transmitted infectionscaused by Chlamydia trachomatis, N. gonorrhoeae, H.ducreyi, and Ureaplasma urealyticum suggests that singledosetherapy with it for uncomplicated urethritis or cervicitismay have advantages over use of other antibiotics.

생물학적 활성

Azithromycin is a macrolide antibiotic. It is active against S. pneumoniae, S. aureus, N. gonorrhoeae, M. pneumoniae, H. pylori, C. trachomatis, and H. influenzae in vitro (MIC90s = <0.01-2 mg/L). Azithromycin increases survival in mouse models of intraperitoneal S. pyogenes, S. pneumoniae, E. faecalis, or H. influenzae infection (ED50s = 0.78, 8.7, 12.7, and 30.3 mg/kg, respectively). It inhibits replication of severe acute respiratory coronavirus 2 (SARS-CoV-2), but not Middle East respiratory syndrome CoV (MERS-CoV), when used at concentrations of 5 and 10 μM. Azithromycin also decreases plasma levels of IL-6, TNF-α, and IL-1β and increases survival in a mouse model of LPS-induced sepsis when administered at a dose of 100 mg/kg. Formulations containing azithromycin have been used in the treatment of a variety of bacterial infections.

Pharmacokinetics

Oral absorption：37%
Cmax 250 mg oral： 0.17 mg/L after 2.2 h
500 mg oral： 0.4 mg/L after2h
Plasma half-life (terminal)： 11–40 h
Volume of distribution： 31 L/kg
Plasma protein binding ：7–50%
Chemical modification at the 9 position of the erythronolide A ring of erythromycin A blocks the internal ketalization and markedly improves acid stability. At pH 2, loss of 10% activity occurred in less than 4 s with erythromycin A, but took 20 min with azithromycin. The AUC at 0–24 h is 4.5 mg.h/L. The level is only slightly increased on repeated dosing.
Binding to plasma protein varies with the concentration, from around 50% at 0.05 mg/L to 7.1% at 1 mg/L. The apparent elimination half-life is dependent upon sampling interval: between 8 and 24 h it ranged from 11 to 14 h： between 24 and 72 h it was 35–40 h.
It rapidly penetrates the tissues, reaching levels that approach or, in some cases, exceed the simultaneous plasma levels and persist for 2–3 days. Only about 6% of the dose is found in urine in the first 24 h.

Clinical Use

This product is suitable for the treatment of the following symptoms of infection caused by susceptible bacteria:
1. For acute pharyngitis and acute tonsillitis caused by Streptococcus pyogenes and for nasosinusitis, acute otitis media, acute bronchitis, and acute exacerbation of chronic bronchitis caused by sensitive bacteria.
2. For pneumonia caused by Mycoplasma pneumonia, Streptococcus pneumonia and Haemophilus influenza.
3. For urethritis, cervicitis and pelvic inflammatory disease caused by chlamydia and non-multiple drug resistance Neisseria gonorrhoeae, and for simple genital infection caused by non-multiple drug resistance Neisseria gonorrhoeae (exclude co-infection of Misu spirochetes).
4. For skin and soft tissue infections caused by sensitive bacteria.

부작용

Azithromycin is well tolerated with little gastrointestinal disturbance.

Mode of action

Azithromycin reversibly binds to the 50S ribosomal subunit of the 70S ribosome of sensitive microorganisms, thereby inhibiting the translocation step of protein synthesis, wherein a newly synthesized peptidyl tRNA molecule moves from the acceptor site on the ribosome to the peptidyl (donor) site, and consequently inhibiting RNA-dependent protein synthesis leading to cell growth inhibition and cell death.

Azithromycin 준비 용품 및 원자재

원자재

준비 용품

Azithromycin 공급 업체

공급자	전화	이메일	국가	제품 수	이점
Shaanxi TNJONE Pharmaceutical Co., Ltd	+8618740459177	sarah@tnjone.com	China	893	58
Qiuxian Baitai New Material Co., LTD	+8618330912755	sale2@hbyalin.com	China	1677	58
Sinoway Industrial co., ltd.	0592-5800732; +8613806035118	xie@china-sinoway.com	China	992	58
Hubei Harvest Chemical CO.,Ltd	+86-13129915771 +86-15623179893	wendy@hb-harvestchem.com	China	931	58
Hebei ZB Gamay Biological Technology Co.,Ltd	+86-031189171450 +86-15632359451	chem@zbvet.net	China	222	58
Anhui Yiao New Material Technology Co., Ltd	+86-199-55145978 +8619955145978	sales8@anhuiyiao.com	China	253	58
Henan Tengmao Chemical Technology Co. LTD	+8615238638457	salesvip2@hntmhg.com	China	415	58
Henan Bao Enluo International TradeCo.，LTD	+86-17331933971 +86-17331933971	deasea125996@gmail.com	China	2503	58
Zibo Wei Bin Import & Export Trade Co. Ltd.	+86-0533-2091136 +8613864437655	ziboweibinmaoyi@163.com	China	100	58
Wuhan Haorong Biotechnology Co.,ltd	+8618565342920	sales@chembj.net	China	269	58

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