Sparfloxacin

한글명:Sparfloxacin

카스 번호110871-86-8

상품명:Sparfloxacin

CBNumberCB7407291

분자식C19H22F2N4O3

포뮬러 무게392.4

MOL 파일110871-86-8.mol

화학적 성질

녹는점	265°C
끓는 점	640℃
밀도	1.436±0.06 g/cm3(Predicted)
인화점	>110°(230°F)
저장 조건	Keep in dark place,Inert atmosphere,2-8°C
용해도	DMF: 10 mg/ml; DMF:PBS(pH 7.2)(1:1): 0.50 mg/ml
산도 계수 (pKa)	pKa1 6.25, pKa2 9.30(at 25℃)
물리적 상태	가루
색상	흰색에서 밝은 노란색
수용성	9mg/ml에서 DMSO에 용해됩니다. 물에 거의 녹지 않음
BRN	9170271
CAS 데이터베이스	110871-86-8(CAS DataBase Reference)

위험 및 안전 성명

위험품 표기

위험 카페고리 넘버

36/37/38

안전지침서

26-36

WGK 독일

RTECS 번호

VB1986500

HS 번호

29339900

NFPA 704:

	0
2		0

그림문자(GHS)

Sparfloxacin 화학적 특성, 용도, 생산

개요
Sparfloxacin is the most potent fluoroquinolone antibiotic introduced for the treatment of community acquired infections. It has superior and broad in vitro activity against members of family Enterobacferiaceae and anaerobic bacteria, some of which are resistant toβ-lactam antibiotics or to aminoglycosides. In patients with surgical infections, sparfloxacin shows excellent activity against resistant pathogens. It is effective in treating patients with bladder irritability and is reported to have potential in the treatment of leprosy and Mycobacterium tuberculosis in mice. Favorable pharmacokinetic properties, good intracellular penetration and a lack of transferable resistance have been reported.
화학적 성질
Light yellow powder
World Health Organization (WHO)
Sparfloxacin is a quinolone antimicrobial agent. See also under quinolone and fluoroquinolone antimicrobial agents.
Pharmaceutical Applications
It is highly active against most aerobic Grampositive cocci and Gram-negative bacilli, including fastidious Gram-negative bacilli, Acinetobacter spp., Campylobacter spp. and Legionella spp. Ps. aeruginosa is weakly susceptible. Activity also extends to the genital mycoplasmas, M. tuberculosis and M. avium complex isolates. It is moderately active against some anaerobes (including the B. fragilis group); L. monocytogenes is resistant.
It is well absorbed, achieving a plasma concentration of 1–1.5 mg/L 4.5 h after a 400 mg oral dose. Absorption is decreased in the presence of antacids owing to the formation of chelates with metallic ions. Concentrations in many tissues, including lung, exceed those in plasma. The plasma half-life is 15–20 h. CSF penetration is limited. Around 5–10% of a dose is eliminated unchanged in the urine, with about 30% appearing as the glucuronide. Total clearance is 10–15 L/h. The plasma half-life increases only modestly in renal failure to 30–40 h. About 50–60% of the dose appears as unchanged drug in the feces, mainly as the glucuronide, accounting for 10–20% of the administered dose.
Adverse events are those common to fluoroquinolones, in particular gastrointestinal tract disturbances, CNS effects (mainly headache and insomnia) and rashes. Photosensitivity reactions have been observed in 2–11% of patients. It can prolong the QTc interval and cases of torsade de pointes have been reported. It does not potentiate the toxicity of theophylline.
It has been used for respiratory and other infections caused by susceptible bacteria, but use has been restricted in the USA and Europe because of phototoxicity and cardiotoxicity.
Clinical Use
Sparfloxacin, (cis)-5-amino-1-cyclopropyl-7-(3,5-dimethyl)-1-piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylicacid, is a newer fluoroquinolone.
This compound exhibits higher potency against Grampositivebacteria, especially staphylococci and streptococci,than the fluoroquinolones currently marketed. It is also moreactive against chlamydia and the anaerobe Bacteroides fragilis.The activity of sparfloxacin against Gram-negative bacteriais also very impressive, and it compares favorably withciprofloxacin and ofloxacin in potency against Mycoplasmaspp., Legionella spp., Mycobacteria spp., and Listeria monocytogenes.Sparfloxacin has a long elimination half-life of18 hours, which permits once-a-day dosing for most indications.The drug is widely distributed into most fluidsand tissues. Effective concentrations of sparfloxacin areachieved for the treatment of skin and soft tissue infections,lower respiratory infections (including bronchitis and bacterialpneumonias), and pelvic inflammatory disease causedby gonorrhea and chlamydia. Sparfloxacin has also beenrecommended for the treatment of bacterial gastroenteritisand cholecystitis. The oral bioavailability of sparfloxacinis claimed to be good, and sufficient unchanged drug isexcreted to be effective for the treatment of urinary tract infections.Nearly 20% of an orally administered dose is excretedas an inactive glucuronide.

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