Pentamidine

Pentamidine 속성

Pentamidine MSDS

4,4'-[1,5-Pentanediylbis(oxy)]bis-benzenecarboximidamide

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 Solid

Indications

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: Negligible
C_max 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

공급자	전화	이메일	국가	제품 수	이점
Capot Chemical Co.,Ltd.	571-85586718 +8613336195806	sales@capotchem.com	China	29797	60
ATK CHEMICAL COMPANY LIMITED	+undefined-21-51877795	ivan@atkchemical.com	China	32480	60
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	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	49390	58
Shaanxi Dideu Medichem Co. Ltd	+86-29-87569266 15319487004	1015@dideu.com	China	2263	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

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