Rifabutin
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Rifabutin 속성
- 녹는점
- 169-171°C
- 끓는 점
- 969.6±65.0 °C(Predicted)
- 밀도
- 1.33±0.1 g/cm3(Predicted)
- 저장 조건
- Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
- 용해도
- 에 용해됨 DMSO: >5mg/mL
- 물리적 상태
- 가루
- 산도 계수 (pKa)
- 3.31±0.70(Predicted)
- 색상
- 진한 빨간색에서 진한 보라색까지
- 수용성
- 0.19g/L(온도 미표시)
- BCS Class
- 2
- 안정성
- 흡습성 및 감광성
- InChIKey
- ATEBXHFBFRCZMA-VXTBVIBXSA-N
- CAS 데이터베이스
- 72559-06-9
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
WGK 독일 | 3 | ||
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RTECS 번호 | VJ6700000 | ||
HS 번호 | 2941906000 | ||
유해 물질 데이터 | 72559-06-9(Hazardous Substances Data) |
그림문자(GHS): | ||||||||||||||||||||||
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신호 어: | Warning | |||||||||||||||||||||
유해·위험 문구: |
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예방조치문구: |
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Rifabutin C화학적 특성, 용도, 생산
개요
Rifabutin, a rifamycin antibacterial derivative, is the first agent approved and introduced for the prevention of Mycobacterium avium complex (MAC) in AIDS patients. It is also indicated in combination chemotherapy for the prophylaxis and treatment of MAC infections in HIV positive patients and for newly diagnosed and chronic tuberculosis.화학적 성질
Red-Brown Powder용도
Rifamycins are antibiotics that inhibit DNA-dependent RNA polymerases and are usually bactericidal against Gram-positive bacteria but bacteriostatic against Gram-negative bacteria. Rifamycins are also effective against Mycobacterium species, including M. tuberculosis. Rifabutin is a broad-spectrum rifamycin antibiotic that has applications against tuberculosis, H. pylori, M. avium complex, Chlamydia, and other bacteria. It is also useful in co-infections with human immunodeficiency virus, including tuberculosis.Indications
Rifabutin (Mycobutin), an antibiotic related to rifampin, shares its mechanism of action, that is, inhibition of RNA polymerase. Rifabutin has significant activity in vitro and in vivo against M. avium-intracellular complex (MAC) isolates from both HIV-infected and non–HIV-infected individuals. It has better activity against MAC organisms than rifampin. Rifabutin is active against M. tuberculosis, including some rifampinresistant strains, such as M.leprae and M.fortuitum. It has a spectrum of activity against gram-positive and gramnegative organisms similar to that of rifampin. The molecular basis for resistance to rifabutin is shared by both rifampin and rifabutin; this explains the virtually complete cross-resistance that occurs between these drugs.Antimicrobial activity
The activity is similar to that of rifampicin, but it is more active against the Mycobacterium avium complex (MIC 0.01–2 mg/L) and several other atypical mycobacteria. It inhibits the replication of human immunodeficiency virus 1 (HIV-1) in concentrations (10 mg/L) that are not toxic to lymphoid cells, but no efficacy on HIV infections has been demonstrated.원료
The frequency of spontaneously resistant mutants in several bacterial species, including M. tuberculosis, M. leprae, Staphylococcus aureus and Chlamydia trachomatis, is somewhat lower than with rifampicin.Pharmaceutical Applications
Rifabutine; ansamycin. Molecular weight: 847.02.A semisynthetic spiropiperidyl derivative of rifamycin S, available for oral administration. It is slightly soluble in water and soluble in organic solvents.
Pharmacology
Rifabutin is well absorbed orally, and peak plasma concentrations are reached in 2 to 3 hours. Because of its lipophilicity, rifabutin achieves a 5- to 10-fold higher concentration in tissues than in plasma. The drug has a half-life range of 16 to 96 hours and is eliminated in urine and bile.Rifabutin appears as effective as rifampin in the treatment of drug-susceptible tuberculosis and is used in the treatment of latent tuberculosis infection either alone or in combination with pyrazinamide. Clinical use of rifabutin has increased in recent years, especially in the treatment of HIV infection. It is a less potent inducer of cytochrome 450 enzymes pathways than rifampin and results in less drug interaction with the protease inhibitors and nonnucleoside reverse transcriptase inhibitors. Rifabutin is therefore commonly substituted for rifampin in the treatment of tuberculosis in HIV-infected patients. Another important use of rifabutin in the HIV-infected population is prevention and treatment of disseminated MAC.
Pharmacokinetics
Oral absorption:12–20%Cmax 300 mg oral :0.38 mg/L after 3.3 h
Plasma half-life:16 h
Volume of distribution:9.3 L/kg
Plasma protein binding: 85%
absorption and distribution
Oral absorption is rapid but incomplete, with considerable interpatient variation. It is well distributed, concentrations in many organs being higher than that in plasma. The average concentration in lungs is 6.5 times the simultaneous plasma concentration.
Metabolism and excretion
Rifabutin is mainly metabolized to the active desacetyl derivative, although several other oxidation products have been detected in urine, where some 10% of the dose is eliminated. About 30–50% of the dose can be recovered from the feces. Elimination from plasma is biphasic, with a terminal half-life of 45 h. The drug is a weak inducer of hepatic enzymes. The rate of metabolism increases, and the plasma area under the concentration–time curve (AUC) declines as the treatment continues.
Clinical Use
Prevention of infections with M. avium complex in AIDS patientsTreatment of non-tuberculous mycobacterial disease (in combination with other agents)
Rifabutin in combination with other agents has been proposed as a rescue therapy after Helicobacter pylori treatment failures.Although some efficacy has been observed in the treatment of tuberculosis, its use for this condition is not recommended.
부작용
The adverse effects that most frequently result in discontinuation of rifabutin include GI intolerance, rash, and neutropenia. Rifabutin levels will be increased with concurrent administration of fluconazole and clarithromycin, resulting in anterior uveitis, polymyalgia syndrome, and a yellowish-tan discoloration of the skin (pseudojaundice). Other adverse reactions are similar to those of rifampin, such as hepatitis, red-orange discoloration of body fluids, and drug interactions due to effects on the hepatic P450 cytochrome enzyme system.Rifabutin 준비 용품 및 원자재
원자재
준비 용품
Rifabutin 공급 업체
글로벌( 316)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
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Hebei Mojin Biotechnology Co., Ltd | +8613288715578 |
sales@hbmojin.com | China | 12456 | 58 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21691 | 55 |
Nanjing ChemLin Chemical Industry Co., Ltd. | 025-83697070 |
product@chemlin.com.cn | CHINA | 3012 | 60 |
career henan chemical co | +86-0371-86658258 |
sales@coreychem.com | China | 29914 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 |
linda@hubeijusheng.com | CHINA | 28180 | 58 |
Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503282 |
alice@crovellbio.com | China | 8823 | 58 |
BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 |
sales@chemdad.com | China | 39916 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 49390 | 58 |
Shaanxi Dideu Medichem Co. Ltd | +86-29-87569265 +86-18612256290 |
1056@dideu.com | China | 3581 | 58 |
Rifabutin 관련 검색:
로듐
Rifapentine
Rifamycin Sodium
RIFAMYCIN SV
Rimsulfuron
Regorafenib
2-(4-BIPHENYL)ETHYLAMINE
5-ACETYL-2,3-DIHYDROBENZO(B)FURAN
3-Amino-4-imino-rifamycin S
2,3-Dihydrobenzo[b]furan-5-carbaldehyde
2,3-DIMETHYLANISALDEHYDE
3,3-Dimethoxybutan-2-one
PHENYLGLYOXAL MONOHYDRATE
2-Amino-4'-methoxyacetophenone
2,5-DIMETHYLPHENETHYLAMINE
RIFAMYCIN
1-(4-HYDROXY-2,5-DIMETHYL-PHENYL)-ETHANONE
25-O-Deacetyl Rifabutin,25-DESACETYL RIFABUTIN