디디아이
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디디아이 속성
- 녹는점
- 193-195 °C
- 알파
- D25 -26.3° (c = 10 in water)
- 끓는 점
- 193-195 C
- 밀도
- 1.2917 (rough estimate)
- 굴절률
- -28 ° (C=0.34, H2O)
- 저장 조건
- Inert atmosphere,Store in freezer, under -20°C
- 용해도
- DMSO 또는 메탄올에 용해됨
- 물리적 상태
- 가루
- 산도 계수 (pKa)
- 9.12(at 25℃)
- 색상
- 흰색에서 황백색까지
- 수용성
- 21&C에서 1~5g/100mL
- Merck
- 14,3098
- BRN
- 3619529
- BCS Class
- 3
- 안정성
- 안정적인. 타기 쉬운. 강한 산화제와 호환되지 않습니다.
- CAS 데이터베이스
- 69655-05-6(CAS DataBase Reference)
- IARC
- 3 (Vol. 76) 2000
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | C | ||
---|---|---|---|
위험 카페고리 넘버 | 34-36/37 | ||
안전지침서 | 26-27-36/37/39-45-24/25 | ||
WGK 독일 | 2 | ||
RTECS 번호 | NM7460700 | ||
HS 번호 | 29335990 | ||
유해 물질 데이터 | 69655-05-6(Hazardous Substances Data) |
디디아이 C화학적 특성, 용도, 생산
개요
Didanosine is an orally active purine dideoxynucleoside analog indicated for adult and pediatric patients with advanced HIV infection who are either intolerant or significantly deteriorated on zidovudine. It appears to increase CD4 cell counts and decrease p24 antigen levels.Major adverse effects are pancreatitis, peripheral neuropathy and diarrhea.Unlike zidovudine, didanosine exhibits insignificant bone marrow suppression.화학적 성질
White Powder용도
2?,3?-Dideoxyinosine is a potent anti-retroviral agent. It is most effective in combination therapy for the treatment of HIV and related lymphoma.Indications
Didanosine (ddI, Videx) is an adenosine analogue with activity against HIV-1, HIV-2, and HTLV-I. It is approved as part of a multidrug regimen for the therapy of HIV infection and is also used as postexposure HIV prophylaxis정의
ChEBI: A purine 2',3'-dideoxyribonucleoside that is inosine in which the hydroxy groups at both the 2' and the 3' positions on the sugar moiety have been replaced by hydrogen.Antimicrobial activity
Didanosine is active against HIV-1, HIV-2 and HTLV-1.원료
Codon changes at positions 65 or 74 in HIV reverse transcriptase are associated with reduced susceptibility.일반 설명
Didanosine (Videx, ddI) is 2',3'-dideoxyinosine (ddI), a synthetic purine nucleoside analog that is bioactivatedto 2',3'-dideoxy-ATP (ddATP) by host cellularenzymes.The metabolite, ddATP, accumulates intracellularly,where it inhibits RT and is incorporated intoviral DNA to cause chain termination in HIVinfectedcells. The potency of didanosine is 10-to 100-foldless than that of AZT with respect to antiviral activity andcytotoxicity, but the drug causes less myelosuppressionthan AZT causes.Didanosine is recommended for the treatment of patientswith advanced HIV infection who have received prolongedtreatment with AZT but have become intolerant to, or experiencedimmunosuppression from, the drug. AZT and ddIact synergistically to inhibit HIV replication in vitro, andddI is effective against some AZT-resistant strains of HIV.Painful peripheral neuropathy (tingling, numbness, and painin the hands and feet) and pancreatitis (nausea, abdominalpain, elevated amylase) are the major dose-limiting toxicitiesof didanosine. Didanosine is given orally in the form ofbuffered chewable tablets or as a solution prepared from thepowder. Both oral dosage forms are buffered to preventacidic decomposition of ddI to hypoxanthine in the stomach.
공기와 물의 반응
Water soluble.건강위험
SYMPTOMS: Symptoms of exposure to a related compound include cutaneous eruptions, fever, mouth sores, thrombocytopenia, neutropenia, reversible peripheral neuropathy, gastrointestinal distress, headache, nausea and vomiting.화재위험
Flash point data for Dideoxyinosine are not available; however, Dideoxyinosine is probably combustible.Pharmaceutical Applications
An analog of deoxyadenosine, formulated for oral administration.Mechanism of action
Didanosine (ddl) is a purine dideoxynucleoside, which is an analogue of inosine. Chemically, it is 2′,3′-dideoxyinosine, and it differs from inosine by having hydrogen atoms in place of the 2′- and 3′-hydroxyl groups on the ribose ring. Didanosine is a pro-drug that is bioactivated by metabolism to dideoxyadenosine triphosphate, which is a competitive inhibitor of viral RT and is incorporated into the developing viral DNA in place of deoxyladenosine triphosphate. As such, this agent causes chain termination because of the absence of a 3′-hydroxyl group. Didanosine inhibits HIV RT and exerts a virustatic effect on the retroviruses. Combined with ZDV, antiretroviral activity of ddI is increased.Pharmacokinetics
Oral absorption: c. 40%Cmax 400 mg once daily: 0.93 mg/L
Plasma half-life: c. 1.4 h
Volume of distribution: c. 1 L/kg
Plasma protein binding: <5%
Absorption
Bioavailability is reduced by about half when taken with food and the drug should be given at least 30 min before a meal. The peak plasma concentration achieved by enteric-coated tablets is less than half that of buffered tablets.
Distribution
Central nervous system (CNS) penetration is relatively poor. Median concentrations in semen (455 ng/mL; range < 50–2190 ng/mL) are greater than those in blood (<50 ng/mL; range <50–860 ng/mL). It is secreted in breast milk.
Metabolism
Based upon animal studies it is presumed that metabolism occurs by the pathways responsible for the elimination of endogenous purines by xanthine oxidase. Metabolism may be altered in patients with severe hepatic impairment; however, no specific dose adjustment is recommended.
Excretion
Renal clearance by glomerular filtration and active tubular secretion accounts for 50% of total body clearance. Urinary recovery accounts for about 20% of the oral dose in adults. The half-life increases three-fold in patients requiring dialysis. Patients with a creatinine clearance <60 mL/min may be at greater risk of toxicity.
Clinical Use
Treatment of HIV infection (in combination with other antiretroviral drugs)부작용
Most serious are pancreatitis (fatal and non-fatal), lactic acidosis and severe hepatomegaly with steatosis (fatal and nonfatal), retinopathy, optic neuritis and dose-related peripheral neuropathy. Patients with low body weight may require dose modification. A strong association with non-cirrhotic portal hypertension has been described.The combination with stavudine should be avoided in pregnant women as fatal cases of lactic acidosis have been reported. Caution should also be exercised in patients with known risk factors for liver disease. Therapy should be stopped in patients who develop clinical or laboratory evidence of lactic acidosis or hepatotoxicity. Monitoring lactate levels prospectively is not recommended as mild hyperlactatemia occurs in asymptomatic patients and has a poor positive predictive value for the development of lactic acidosis.
Caution should be exercised in co-administering other drugs with known neurotoxicity and in patients with a history of neuropathy. Treatment should stop if symptoms and signs of neuropathy are observed, but the condition is usually reversible and patients with resolved neuropathy may be retreated at a reduced dosage. Retinal depigmentation has been observed in children and twice-yearly dilated retinal examination is recommended.
신진 대사
Didanosine is less toxic than ZDV. The CSF fluid/plasma ratio of ddI is 0.2. Didanosine is ultimately converted to hypoxanthine, xanthine, and uric acid through the usual metabolic pathway for purines. The latter is a nontoxic metabolic product.Didanosine is given in advanced HIV infection, ZDV intolerance, or significant clinical/immunologic deterioration.
주의 사항
Buffering agents that are compounded with didanosineto counteract its degradation by gastric acid mayinterfere with the absorption of other drugs that requireacidity (e.g., indinavir, delavirdine, ketoconazole, fluoroquinolones,tetracyclines, dapsone). An enteric-coatedformulation (Videx EC) that dissolves in the basic pH ofthe small intestine is not susceptible to these interactions.Ganciclovir and valganciclovir can increase bloodlevels of didanosine.The use of zalcitabine with didanosineis not recommended because that combination carriesan additive risk of peripheral neuropathy.The combinationof didanosine with stavudine increases the riskof pancreatitis, hepatotoxicity, and peripheral neuropa-thy. Stavudine should not be given with didanosine topregnant women because of the increased risk of metabolicacidosis.디디아이 준비 용품 및 원자재
원자재
아조비스이소부티로니트릴
클로로포름
이황화탄소
트라이-엔-뷰틸주석 하이드라이드
테트라하이드로푸란
이노신
3-브로모프로피오니트릴
사염화실란
테트라뷰틸암모늄 플루오린화물
효모 추출물
PEPTONE
트리스(하이드록시메틸)아미노메탄 수화염화물
MEAT EXTRACT
펩톤
2',3'-디데옥시-2',3'-디데하이드로이노신
준비 용품
디디아이 공급 업체
글로벌( 342)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Hebei Mojin Biotechnology Co., Ltd | +86 13288715578 +8613288715578 |
sales@hbmojin.com | China | 12446 | 58 |
Shanghai Daken Advanced Materials Co.,Ltd | +86-371-66670886 |
info@dakenam.com | China | 18628 | 58 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29888 | 58 |
Hebei Guanlang Biotechnology Co., Ltd. | +86-19930503282 |
alice@crovellbio.com | China | 8820 | 58 |
Nanjing Baifuli Technology Co., Ltd. | +86-15335185688 |
sales@unisyn.cn | CHINA | 332 | 58 |
BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 |
sales@chemdad.com | China | 39916 | 58 |
Alchem Pharmtech,Inc. | 8485655694 |
sales@alchempharmtech.com | United States | 63711 | 58 |
Antai Fine Chemical Technology Co.,Limited | 18503026267 |
info@antaichem.com | CHINA | 9641 | 58 |
SHANGHAI T&W PHARMACEUTICAL CO., LTD. | +86-021-61551413 +8618813727289 |
contact@trustwe.com | China | 5738 | 58 |
디디아이 관련 검색:
이노신 N2-아이소부티릴-5'-O-(4,4'-디메톡시트리틸)-2'-데옥시구아노신 구아노신 5′-이노신산이나트륨
3'-GMP DISODIUM SALT
GUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SODIUM SALT
2'-Deoxyinosine
2',3',5'-TRI-O-ACETYLINOSINE
2'-Deoxyguanosine-5'-diphosphate trisodium salt
2',3'-O-Isopropylideneinosine
N2-Isobutyryl-2'-deoxyguanosine
3'-AMINO-2',3'-DIDEOXYINOSINE
2',3'-DIDEHYDRO-2',3'-DIDEOXYINOSINE
8-AMINOGUANOSINE
N2-ISOBUTYRYL-3'-O-BENZOYL-2'-DEOXYGUANOSINE
5'-O-(4,4'-DIMETHOXYTRITYL)-N2-ISOBUTYRYL-2'-DEOXYGUANOSINE-3'-(METHYL-N,N-DIISOPROPYL)PHOSPHORAMIDITE
INOSINE-3',5'-CYCLIC PHOSPHATE
N2,2'-O-DIBUTYRYLGUANOSINE 3':5'-CYCLIC MONOPHOSPHATE SODIUM SALT