クエン酸ジエチルカルバマジン

関: diethylcarbamazine

WordNet

a salt or ester of citric acid
cause to form a salt or ester of citric acid

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/07/22 21:41:51」(JST)

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Diethylcarbamazine Citrate (DEC) (N, N-diethyl-4-methyl-1-piperazine carboxamide dihydrogen citrate) is a synthetic derivative of piperazine, used as an anthelmintic drug used in the treatment of filariasis in humans, dogs and cats. Discovery was attributed to Yellapragada Subbarow.

DEC is a synthetic organic compound which is highly specific for several parasites and does not contain any toxic metallic elements.

It is on the World Health Organization's List of Essential Medicines, a list of the most important medication needed in a basic health system.^[1]

Medical uses

DEC is indicated for treatment of individual patients with certain filarial diseases. These diseases include: lymphatic filariasis caused by infection with Wuchereria bancrofti, Brugia malayi, or Brugia timori; tropical pulmonary eosinophilia, and loiasis.

In cases of onchocerciasis, another common filarial parasite, the drug is not used. This is because of the intense and unbearable itching associated with the dead subcutaneous parasites.

DEC continues to be the mainstay for treatment of patients with lymphatic filariasis and loiasis. DEC is also used in the prevention of dog heartworm Dirofilaria immitis.

Now WHO prescribes DEC to patients who are susceptible to filariasis by preventive regimen in endemic areas.

Contraindications are Previous history of heart problems, Gastrointestinal problems, allergic patients

Mechanism

DEC is an inhibitor of arachidonic acid metabolism in filarial microfilaria. This makes the microfilaria more susceptible to immune attack. However, DEC is not directly toxic to the filarial microfilaria ^[2].

Trade names

Hetrazan
Carbilazine
Caricide
Cypip
Ethodryl
Notézine
Spatonin
Filaribits
Banocide Forte
Eofil

references

^ "WHO Model List of EssentialMedicines". World Health Organization. October 2013. Retrieved 22 April 2014.
^ El-Shahawi GA et al. Setaria equina: in vivo effect of diethylcarbamazine citrate on microfilariae in albino rats. Exp Parasitol. 2010 Dec;126(4):603-10 from http://www.ncbi.nlm.nih.gov/pubmed/20599991 accessed on 11Jul2014

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UpToDate Contents

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1. リンパ管フィラリア症の診断、治療、および予防 diagnosis treatment and prevention of lymphatic filariasis
2. 駆虫薬療法 anthelminthic therapies
3. マンソネラ感染症 mansonella infections
4. オンコセルカ症 onchocerciasis
5. ロア糸状虫症（ロア糸状虫感染） loiasis loa loa infection

English Journal

Efficacy, Safety, and Pharmacokinetics of Coadministered Diethylcarbamazine, Albendazole, and Ivermectin for Treatment of Bancroftian Filariasis.

Thomsen EK1, Sanuku N2, Baea M2, Satofan S2, Maki E2, Lombore B2, Schmidt MS3, Siba PM2, Weil GJ4, Kazura JW5, Fleckenstein LL3, King CL6.
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America.Clin Infect Dis.2016 Feb 1;62(3):334-41. doi: 10.1093/cid/civ882. Epub 2015 Oct 20.
BACKGROUND: Available treatments for lymphatic filariasis (LF) are limited in their longterm clearance of microfilaria from the blood. The safety and efficacy of a single-dose triple-drug therapy of the antifilarial drugs diethylcarbamazine (DEC), ivermectin (IVM), and albendazole (ALB) for LF are u
PMID 26486704

A simple extraction method for the simultaneous detection of tetramisole and diethylcarbamazine in milk, eggs, and porcine muscle using gradient liquid chromatography-tandem mass spectrometry.

Zhang D1, Park JA1, Kim DS1, Kim SK1, Shin SJ2, Shim JH3, Shin SC4, Kim JS1, Abd El-Aty AM5, Shin HC6.
Food chemistry.Food Chem.2016 Feb 1;192:299-305. doi: 10.1016/j.foodchem.2015.07.014. Epub 2015 Jul 6.
Analysis of residual quantities of contaminants in foods of animal origin is crucial for quality control of consumer products. This study was aimed to develop a simple and raid analytical method for detection of tetramisole and diethylcarbamazine using gradient liquid chromatography coupled with tan
PMID 26304351

Loa loa in the vitreous cavity of the eye.

Nayak B1, Sinha S2, Nayak L3.
BMJ case reports.BMJ Case Rep.2016 Jan 8;2016. pii: bcr2015213879. doi: 10.1136/bcr-2015-213879.
A 25-year-old man presented with painful diminution of vision (20/160), accompanied by redness, pain and floaters, over a period of 2 weeks, in his left eye. On examination, the anterior segment revealed moderate inflammation. Posterior segment examination showed a grade one vitreous haze with a f
PMID 26746839

Japanese Journal

Nematocidal Activity of Picrodendrins against a Species of Diplogastridae

Watanabe Ie,Koike Kazuo,Satou Tadaaki [他],NIKAIDO Tamotsu
Biological & pharmaceutical bulletin 22(12), 1310-1313, 1999-12-15
… M) and 6-fold more potent than that of diethylcarbamazine citrate (3.0×10^<-2> …
NAID 110003639601

Spectrophotometric and Thermodynamic Studies of the Charge-Transfer Interaction between Diethylcarbamazine Citrate and Chloranilic Acid

Adikwu M.U.,Ofokansi K.C.,Attama A.A.
Chemical & pharmaceutical bulletin 47(4), 463-466, 1999-04-15
… The charge-transfer complex formed by the interaction between the electron acceptor, p-chloranilic acid and an electron donor diethylcarbamazine was adopted for the assay of the drug in pure powder and in tablets. … In dioxane-chloroform medium, chloranilic acid was found to form a 1 : 1 molecular complex with diethylcarbamazine with maximum absorption band at 540 nm. …
NAID 110003617243

Spectrophotometric and Thermodynamic Studies of the Charge-Transfer Interaction between Diethylcarbamazine Citrate and Chloranilic Acid.

ADIKWU Michael U.,OFOKANSI Kenneth C.,ATTAMA Anthony A.
ＣＨＥＭＩＣＡＬ　＆　ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ　ＢＵＬＬＥＴＩＮ 47(4), 463-466, 1999
… The charge-transfer complex formed by the interaction between the electron acceptor, p-chloranilic acid and an electron donor diethylcarbamazine was adopted for the assay of the drug in pure powder and in tablets. … In dioxane-chloroform medium, chloranilic acid was found to form a 1 : 1 molecular complex with diethylcarbamazine with maximum absorption band at 540 nm. …
NAID 130003947817

「ジエチルカルバマジン」

Diethylcarbamazine
Systematic (IUPAC) name
	N,N-diethyl-4-methylpiperazine-1-carboxamide
Clinical data
AHFS/Drugs.com	Micromedex Detailed Consumer Information
Legal status	Legal
Pharmacokinetic data
Half-life	.
Identifiers
CAS number	90-89-1
ATC code	P02CB02 QP52AH02
PubChem	CID 3052
DrugBank	DB00711
ChemSpider	2944
UNII	V867Q8X3ZD
KEGG	D07825
ChEMBL	CHEMBL684
Chemical data
Formula	C10H21N3O
Mol. mass	199.293 g/mol
	SMILES O=C(N1CCN(C)CC1)N(CC)CC;
	InChI InChI=1S/C10H21N3O/c1-4-12(5-2)10(14)13-8-6-11(3)7-9-13/h4-9H2,1-3H3 ; Key:RCKMWOKWVGPNJF-UHFFFAOYSA-N ;
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　　[★]

英: diethylcarbamazine
同: クエン酸ジエチルカルバマジン diethylcarbamazine citrate
商: スパトニン
関: 糸状虫症、駆虫薬

「diethylcarbamazine」

　　[★] ジエチルカルバマジン

同: DEC

[1] "WHO Model List of EssentialMedicines". World Health Organization. October 2013. Retrieved 22 April 2014.

[2] El-Shahawi GA et al. Setaria equina: in vivo effect of diethylcarbamazine citrate on microfilariae in albino rats. Exp Parasitol. 2010 Dec;126(4):603-10 from http://www.ncbi.nlm.nih.gov/pubmed/20599991 accessed on 11Jul2014

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diethylcarbamazine citrate