Pentamidine
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Pentamidine 속성
- 녹는점
- 186 °C (dec.)
- 끓는 점
- 476.22°C (rough estimate)
- 밀도
- 1.1805 (rough estimate)
- 굴절률
- 1.6620 (estimate)
- 저장 조건
- Sealed in dry,Store in freezer, under -20°C
- 용해도
- DMSO, 메탄올(소량이 용해된)
- 물리적 상태
- 고체
- 물리적 상태
- 단단한 모양
- 산도 계수 (pKa)
- pKa 11.4 (Uncertain)
- 색상
- 흰색에서 황백색까지
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
유엔번호(UN No.) | 3249 | ||
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위험 등급 | 6.1(b) | ||
포장분류 | III | ||
유해 물질 데이터 | 100-33-4(Hazardous Substances Data) |
Pentamidine C화학적 특성, 용도, 생산
개요
Pentamidine is an aromatic diamine that is effective against protozoal diseases, such as amoebic dysentery, malaria, trypanosomiasis, and leishmaniasis. In clinical studies, it has also been shown to be an effective prophylaxis against pneumocystis pneumonia.화학적 성질
Crystalline SolidIndications
Pentamidine (Pentam 300) binds to DNA and may inhibit kinetoplast DNA replication and function. It also may act by inhibiting dihydrofolate reductase and interfering with polyamine metabolism. An effect on organism respiration, especially at high doses, also may play a role.Antimicrobial activity
Pentamidine has broad activity in experimental models against P. falciparum, Toxoplasma gondii, Leishmania spp., Trypanosoma spp. and Babesia spp. It also has activity against Pn. jirovecii.원료
Relapse rates of 7–16% have been reported in the treatment of human African trypanosomiasis in West Africa. Patients usually respond to a subsequent course of treatment with melarsoprol. A membrane transporter is involved in crossresistance of arsenic-resistant T. brucei to diamidines, affecting diminazene and stilbamidine more than pentamidine.Pharmaceutical Applications
A synthetic diamidine, available as the isethionate (2-hydroxymethane sulfonate) salt for parenteral use. It is also administered by instillation of a nebulized solution directly into the lungs.Mechanism of action
Pentamidine is not well absorbed from the intestinal tract after oral administration and generally is given by intramuscular injection. The drug binds to tissues, particularly the kidney, and is slowly excreted, mostly as the unmodified drug. It does not enter the central nervous system (CNS). Its sequestration in tissues accounts for its prophylactic use in trypanosomiasis.Pharmacokinetics
Oral absorption: NegligibleCmax 4 mg/kg intramuscular: c. 0.5 mg/L after 1 h
Plasma half-life: c. 6.5 h
Volume of distribution: 3 L/kg
Plasma protein binding: c. 70%
Pentamidine is rapidly and extensively metabolized by rat liver, and high concentrations are retained in renal and hepatic tissue for up to 6 months after administration. In humans distribution is mainly in the liver, kidney, adrenal glands and spleen, with lower accumulation in the lung. This tissue retention is the basis for its prophylactic use. Although transport across the blood–brain barrier has been demonstrated in experimental models, it is probably unable to cross the blood–brain barrier in sufficient quantity to be trypanocidal: <1% of the plasma concentration has been measured in the CSF of sleeping sickness patients. About 15–20% of the dose is excreted in the urine but because of retention in tissues there is an extremely long terminal half-life (>12 days).
Clinical Use
Pentamidine is active against Pneumocystis carinii, trypanosomes, and leishmaniasis unresponsive to pentavalent antimonials. It is an alternative agent for the treatment of P. carinii pneumonia. Although it is more toxic than trimethoprim–sulfamethoxazole, it has been widely used in patients with acquired immunodeficiency syndrome (AIDS), in whom P. carinii infection is common.Pentamidine is an alternative drug for visceral leishmaniasis, especially when sodium stibogluconate has failed or is contraindicated. Pentamidine is also a reserve agent for the treatment of trypanosomiasis before the CNS is invaded. This characteristic largely restricts its use to Gambian trypanosomiasis.
부작용
Side effects range from local irritation and sterile abscess at the site of injection to transient effects (vomiting, abdominal discomfort) and serious systemic effects (hypotension, effects on the heart, hypoglycemia and hyperglycemia, leukopenia, thrombocytopenia). In a study of the treatment of South American cutaneous leishmaniasis, 17% of patients prematurely terminated treatment due to toxicity and another 30% reported side effects.Pentamidine 준비 용품 및 원자재
원자재
준비 용품
Pentamidine 공급 업체
글로벌( 112)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Capot Chemical Co.,Ltd. | 571-85586718 +8613336195806 |
sales@capotchem.com | China | 29798 | 60 |
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32836 | 60 |
career henan chemical co | +86-0371-86658258 +8613203830695 |
sales@coreychem.com | China | 29888 | 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 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 49392 | 58 |
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 |
marketing@targetmol.com | United States | 19892 | 58 |
Hebei Zhanyao Biotechnology Co. Ltd | 15369953316 +8615369953316 |
admin@zhanyaobio.com | China | 2136 | 58 |
ANHUI WITOP BIOTECH CO., LTD | +8615255079626 |
eric@witopchemical.com | China | 23556 | 58 |
Chemsigma International Co., Ltd. | +86-18136843612 +86-19951791336 |
info@chemsigma.com | China | 1229 | 58 |
Pentamidine 관련 검색:
아니졸 4-메톡시페닐초산 2-페녹시에탄올 아니스알데히드 과산화 벤조일 3-페녹시벤즈알데하이드 트리플르오르메톡시벤젠
4-Methoxybenzoic acid
m-Anisyl alcohol
BENZAMIDINE
pentamidine isetionate,PENTAMIDINE ISETHIONATE NMDA ANTAGONIST, NEUR,PENTAMIDINE ISETHIONATE SALT,PENTAMIDINE ISETHIONATE,PENTAMIDINE DIISETHIONATE
N-hydroxypentamidine
PENTAMIDINE DIISETIONATE
PENTAMIDINE DIMETHANESULFONATE,pentamidine mesylate
N,N'-dihydroxypentamidine
Pentamidine
cis-platinum pentamidine bromide
cis-platinum pentamidine seleniocyanate