基本情報
- CAS
16354-46-4- 標準SMILES
CCN(CC)C(=O)N1CCN(C)CC1.O=C(O)CC(O)(CC(=O)O)C(=O)O- InChIKey
PGNKBEARDDELNB-UHFFFAOYSA-N- 分子式
- C10H21N3O.C6H8O7
- 平均分子量
- 391.42 g/mol
- 単同位体質量
- 391.19546489
概要
Diethylcarbamazine citrate is a crystalline solid, scored white tablets. Used against filariasis in man and animals. (EPA, 1998)
名称と識別子
- 優先名称
- Diethylcarbamazine Citrate
- IUPAC
- N,N-diethyl-4-methylpiperazine-1-carboxamide;2-hydroxypropane-1,2,3-tricarboxylic acid
名称と別名
DIETHYLCARBAMAZINE CITRATE1642-54-2LoxuranDicarocideCaritrolFilazineFranocideFranozanCarbam PalatabsDitrazin citrateEthodryl citrateDirocide
名称をさらに表示
DitrazineDitrazinumFilarabitsLongicidDitrazini citrasDiethylcarbamazane citrateDiethylcarbamazine acid citrateDiethylcarbamazini citras
データベース識別子
- CAS
16354-46-4、1642-54-2- PubChem CID
- 15432
- DTXSID
DTXSID4045555- ChEMBL
CHEMBL937- ChEBI
CHEBI:4528- UNII
- OS1Z389K8S
- EC Number
- 216-696-6
物性
構造計算による物性
- 極性表面積
- 159 Ų
- 水素結合供与体数
- 4
- 水素結合受容体数
- 9
- 回転可能結合数
- 7
- 重原子数
- 27
- 形式電荷
- 0
- 複雑度
- 411
実験および物理化学的性質
OdorOdorless or slight odor
TasteBitter acid taste
Color/FormWhite, crystalline powder
Solubility
> 75% in water @ 20 °C
Freely sol in hot alcohol
Sparingly sol in cold alcohol
Practically insoluble in acetone, benzene, chloroform and ether
Human Drugs
FDA approved drugs -> Active ingredient
FDA approved drugs -> Active ingredient
Animal DrugsFDA approved animal drugs -> Active ingredient
DecompositionWhen heated to decomposition it emits ... fumes of nitrogen oxides.
Melting Point
286 to 289 °F (EPA, 1998)
141-143 °C
Physical DescriptionDiethylcarbamazine citrate is a crystalline solid, scored white tablets. Used against filariasis in man and animals. (EPA, 1998)
Stability/Shelf LifeThe product /as tablets/ is stable even under conditions of high temp and humidity.
安全と法規制
安全情報は参考情報です。供給元の安全データシート（SDS）、適用法令、専門家による評価に代わるものではありません。
GHS分類
GHS Classification
Danger
H302 (100%): Harmful if swallowed [Warning Acute toxicity, oral]
P260, P264, P270, P271, P284, P301+P317, P304+P340, P316, P320, P330, P403+P233, P405, and P501 (click each P-code to see the statement)
Aggregated GHS information provided per 40 reports by companies from 1 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.
危険有害性情報
Regulatory Information
Chemical: 1-Piperazinecarboxamide, N,N-diethyl-4-methyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Diethylcarbamazine citrate: Does not have an individual approval but may be used under an appropriate group standard
Other Safety InformationIMAP assessments - 1-Piperazinecarboxamide, N,N-diethyl-4-methyl-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1): Environment tier I assessment
DOT LabelPoison
Fire HazardsWhen heated to decomposition, it emits toxic fumes of nitrogen oxides. Avoid decomposing heat. (EPA, 1998)
Health Hazards
(Non-Specific -- Drugs, n.o.s.) May be fatal if inhaled, swallowed or absorbed through skin. Contact may cause burns to skin and eyes. Fire may produce irritating or poisonous gases. Runoff from fire control or dilution water may cause pollution. The average adult man tolerates a single dose of 1.5 gm without ill effects. (EPA, 1998)
Reactive GroupAlcohols and Polyols
Air and Water ReactionsNo rapid reaction with air. No rapid reaction with water.
化学と産業
薬理情報
Mechanism of Action
The drug has two types of action on susceptible microfilariae. The first is to decrease the muscular activity and eventually immobilize the organisms; this may result from a hyerpolarizing effect of the piperazine moiety, and it causes dislocation of the parasites from their normal habitat in the host. The second action is to produce alterations in the microfilarial surface membranes, thereby rendering them more susceptible to destruction by host defense mechanisms. There is definite evidence that diethylcarbamazine kills adult worms of Loa loa and presumptive evidence that it kills adult Wuchereria bancrofti and Wuchereria malayi. However, it has little action against adult Onchocerca volvulus. The mechanism of the filaricidal action of diethylcarbamazine is unknown. /Diethylcarbamazine/
It is postulated that in naturally infected animals, diethylcarbamazine somehow promotes the combination of antigen and antibody on the surface of serotonin-rich platelets. Serotonin is released from damaged platelets, which dramatically increases vascular permeability and leads to shock. This generally but not always occurs in dogs with a high microfilaremia.
Diethylcarbamazine causes rapid disappearance of microfilariae of Wuchereriia bancrofti, Wuchereria malayi, and Loa loa from the blood of man. The drug causes microfilariae of Onchlcerca volvulus to disappear from the skin but does not kill microfilariae in nodules that contain the adult (female) worms. It does not affect the microfilariae of Wuchereria bancrofti in a hydrocele, despite penetration into the fluid.
Biological Half-Life... the plasma half-life /in man/ is about 8 hr after a 200 mg dose and 12 hr after an 800 mg dose.
Metabolism/MetabolitesOnly 10-25% of the drug is excreted unchanged; the remainder is excreted as one of four known metabolites, all of which contain the intact piperazine ring.
MeSH Pharmacological Classification
Pharmacological agents destructive to nematodes in the superfamily Filarioidea.
Compounds that bind to and inhibit that enzymatic activity of LIPOXYGENASES. Included under this category are inhibitors that are specific for lipoxygenase subtypes and act to reduce the production of LEUKOTRIENES.
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