테트라사이클린 C화학적 특성, 용도, 생산
물성
테트라사이클린은 세균의 단백질 합성을 저해하여 항균작용을 나타내는 항생제이다. 미노사이클린, 독시사이클린 등과 함께 테트라사이클린계 항생제로 분류된다. 테트라사이클린의 구조를 일부 변형하여 개발된 약물들을 테트라사이클린계 항생제라고 한다. 과거에는 널리 사용되었으나 최근에는 부작용과 항생제 내성 등으로 인해 자주 사용되지는 않는다. 여러 종류의 세균 외에 리케차†, 클라미디아‡, 미코플라스마§ 등 광범위한 미생물에도 항균작용을 나타내므로 이들 미생물에 의한 감염증 치료에도 사용된다.
개요
테트라사이클린은 세균에 의한 감염을 치료하는 항생제이다. 세균의 단백질 합성을 저해하여 세균뿐 아니라, 리케차, 클라미디아, 미코플라스마 등의 미생물 감염에도 항균작용을 나타낸다. 소아가 복용할 경우 영구적 치아변색이나 법랑질 형성 이상이 나타날 수 있으므로 12세 미만의 소아와 임부, 수유부는 복용하지 않는다. 음식물, 우유, 제산제 등과 함께 복용 시 흡수가 억제될 수 있으므로 시간 간격을 두고 복용한다.
용도
테트라사이클린은 황색포도구균, 연쇄구균, 폐렴연쇄구균, 임균, 매독균, 콜레라균, 인플루엔자균, 대장균 등의 세균뿐만 아니라 리케차, 클라미디아, 미코플라스마 등에도 항균효과를 나타낸다.
테트라사이클린은 여드름, 편도염, 인두염, 후두염, 기관지염, 폐렴, 골수염, 신우신염, 방광염, 콜레라, 임질, 매독, 리케차에 의한 양충병(쯔쯔가무시), 클라미디아에 의한 결막염, 미코플라스마 폐렴 등의 치료에 사용된다.
개요
Tetracycline is an antibiotic that has been utilized in
disease management situations in which SmR strains of
E. amylovora or P. syringae already exist. However, tetracycline
does not appear to be as effective as streptomycin in
reducing blossom populations of E. amylovora (17). Additionally,
strains of P. syringae with resistance to tetracycline
have been isolated from pear orchards in Oregon
and Washington (18), suggesting that resistance to this
antibiotic will probably develop in orchards where it is
applied.
화학적 성질
Tetracycline trihydrate is a white crystalline substance.
용도
Tetracycline is a linear, tetracyclic, broad spectrum antibiotic first prepared chemically by dechlorination of chlortetracycline and subsequently isolated from several Streptomyces species. Tetracycline has broad spectrum antibacterial and antiprotozoan activity, and acts by binding to the 30S and 50S ribosomal subunits blocking protein synthesis. Tetracycline is a pigment and, like many pigments, is degraded by light, oxygen, trace metal ions and pH variations. The purity of tetracycline is often variable, with significant levels of degradation products.
Indications
Tetracycline is often the first antibiotic prescribed. It is the least expensive,
has few side effects, and is well tolerated for longer periods of time. Tetracycline
is effective in low doses because high concentrations are achieved within
sebaceous follicles, especially when inflammation is present.
World Health Organization (WHO)
The first tetracycline antibiotic, chlortetracycline, was introduced
in 1948 and subsequently several semisynthetic derivatives have been used as
antibacterial, antiamoebic and antirickettsial agents. All tetracyclines accumulate in
the developing bones and teeth of the foetus and young children which can result
in retarded bone growth and dental staining. Preparations intended specifically for
children have been withdrawn in some countries, whereas in others warnings are
required on the label advising against administration of tetracyclines to young
children and pregnant women. Non-paediatric dosage forms of tetracycline remain
in the WHO Model List of Essential Drugs.
Antimicrobial activity
It is also active against V. cholerae, chlamydiae,
rickettsiae and spirochetes.
일반 설명
Chemical studies on chlortetracycline revealed that controlledcatalytic hydrogenolysis selectively removed the 7-chloro atom and so produced tetracycline (Achromycin,Cyclopar, Panmycin, Tetracyn). This process was patentedby Conover in 1955. Later, tetracycline was obtainedfrom fermentations of Streptomyces spp., but the commercialsupply still chiefly depends on hydrogenolysis of chlortetracycline.
Tetracycline is 4-dimethyl amino-1,4,4a,5,5a,6,11,12aoctahydro-3,6,10,12,12a-pentahydroxy-6-methyl-1,11-dioxo-2-naphthacenecarboxamide. It is a bright yellow, crystallinesalt that is stable in air but darkens on exposure tostrong sunlight. Tetracycline is stable in acid solutions witha pH above 2. It is somewhat more stable in alkaline solutionsthan chlortetracycline, but like those of the other tetracyclines,such solutions rapidly lose potency. One gram ofthe base requires 2,500 mL of water and 50 mL of alcohol todissolve it. The hydrochloride salt is used most commonly inmedicine, though the free base is absorbed from the GI tractabout equally well. One gram of the hydrochloride salt dissolvesin about 10 mL of water and in 100 mL of alcohol.Tetracycline has become the most popular antibiotic of itsgroup, largely because its plasma concentration appears to behigher and more enduring than that of either oxytetracyclineor chlortetracycline. Also, it is found in higher concentrationin the spinal fluid than the other two compounds.
Pharmaceutical Applications
A fermentation product of Streptomyces aureofaciens, also produced
from chlortetracycline. Available as the hydrochloride
for oral and topical use.
Clinical Use
Along with doxycycline
it is one of the most commonly used tetracyclines.
잠재적 노출
Tetracycline is an antibiotic medicine used as capsules, tablets, or intravenous injections against certain infections in humans and animals.
운송 방법
UN3249 Medicine, solid, toxic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials.
Purification Methods
Tetracycline crystallises from toluene or aqueous MeOH as the trihydrate. [Stephen et al. J Am Chem Soc 76 3568 1954, Beilstein 14 IV 2625.]
비 호환성
Although no dangerous incompatibilities are reported, the potency of this medicine is reduced by heat, sunlight, and solutions with pH <2; and destroyed by caustic hydroxide solutions.
폐기물 처리
It is inappropriate and possibly dangerous to the environment to dispose of expired or waste pharmaceuticals by flushing them down the toilet or discarding them to the trash. Household quantities of expired or waste pharmaceuticals may be mixed with wet cat litter or coffee grounds, double-bagged in plastic, discard in trash. Larger quantities shall carefully take into consideration applicable DEA, EPA, and FDA regulations. If possible return the pharmaceutical to the manufacturer for proper disposal being careful to properly label and securely package the material. Alternatively, the waste pharmaceutical shall be labeled, securely packaged and transported by a state licensed medical waste contractor to dispose by burial in a licensed hazardous or toxic waste landfill or incinerator.
테트라사이클린 준비 용품 및 원자재
원자재
준비 용품
