Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Monoisotopic mass
199.168462309
InChI
InChI=1S/C10H21N3O/c1-4-12(5-2)10(14)13-8-6-11(3)7-9-13/h4-9H2,1-3H3
InChI Key
InChIKey=RCKMWOKWVGPNJF-UHFFFAOYSA-N
IUPAC Name
N,N-diethyl-4-methylpiperazine-1-carboxamide
Traditional IUPAC Name
diethylcarbamazine
SMILES
CCN(CC)C(=O)N1CCN(C)CC1
Độ hòa tan
63.7 mg/mL at 25 °C
pKa (Strongest Basic)
6.9
Refractivity
58.28 m3·mol-1
Dược Lực Học :
Diethylcarbamazine is an anthelmintic drug that does not resemble other antiparasitic compounds. It is a synthetic organic compound which is highly specific for several parasites and does not contain any toxic metallic elements. Diethylcarbamazine continues to be the mainstay for treatment of patients with lymphatic filariasis and loiasis.
Cơ Chế Tác Dụng :
An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa. [PubChem]
The mechanism of action of diethylcarbamazine is thought to involve sensitizing the microfilariae to phagocytosis. One study showed that diethylcarbamazine's activity against Brugia malayi microfilariae is dependent on inducible nitric-oxide synthase and the cyclooxygenase pathway. It confirmed the important role of the arachidonic acid metabolic pathway in diethylcarbamazine's mechanism of action in vivo and showes that in addition to its effects on the 5-lipoxygenase pathway, it targets the cyclooxygenase pathway and COX-1.
Dược Động Học :
▧ Absorption :
Readily absorbed following oral administration.
▧ Metabolism :
Partially metabolized to diethylcarbamazine N-oxide.
▧ Half Life :
Approximately 8 hours.
Độc Tính :
Oral LD50 in rat and mouse is 1400 mg/kg and 660 mg/kg, respectively.
Chỉ Định :
Used for the treatment of individual patients with certain filarial diseases including tropical pulmonary eosinophilia, loiasis, and lymphatic filariasis caused by infection with Wuchereria bancrofti, Brugia malayi, or Brugia timori.
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