Diethylcarbamazine citrate salt

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Diethylcarbamazine citrate salt
Category Others
Catalog number BBF-03797
CAS 1642-54-2
Molecular Weight 391.42
Molecular Formula C16H29N3O8
Purity > 98 %

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Description

Diethylcarbamazine Citrate can be used as an anthelmintic. The LD50 in rats is 1.38 g/kg. Diethylcarbamazine citrate is a muscle relaxant, causing general central nervous system depression, relieving pain caused by strains, sprains, and other musculoskeletal conditions. It can be used for cerebrospinal filariasis in horses and sheep, heart filariasis in dogs, as well as lung filariasis in livestock.

Specification

Synonyms Dicarocide; Caritrol; Loxuran
Storage Store at -20 °C
IUPAC Name N,N-diethyl-4-methylpiperazine-1-carboxamide;2-hydroxypropane-1,2,3-tricarboxylic acid
Canonical SMILES CCN(CC)C(=O)N1CCN(CC1)C.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
InChI InChI=1S/C10H21N3O.C6H8O7/c1-4-12(5-2)10(14)13-8-6-11(3)7-9-13;7-3(8)1-6(13,5(11)12)2-4(9)10/h4-9H2,1-3H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
InChI Key PGNKBEARDDELNB-UHFFFAOYSA-N

Properties

Appearance White, Crystalline powder
Boiling Point 297.4 °C at 760 mmHg
Melting Point 140 °C
Solubility Soluble in DMSO
LogP -0.67710

Reference Reading

1.Modulation of the formation and release of bovine SRS-A in vitro by several anti-anaphylactic drugs.
Burka JF;Eyre P Int Arch Allergy Appl Immunol. 1975;49(6):774-81.
Slow-reacting substance of anaphylaxis (SRS-A) is released immunologically from bovine lung in vitro. Various drugs known to protect calves and other animals during anaphylaxis were tested to investigate their modulation of the formation and release of SRS-A. The anti-inflammatory drugs, meclofenamate and aspirin, potentiated SRS-A release. Chlorphenesin and diethylcarbamazine citrate at high concentrations both inhibited SRS-A release. Two new anti-anaphylactic drugs, PR-D-92-EA and M&B 22,948, were particularly effective in inhibiting SRS-A release at low concentrations. The possible modes of actions of these drugs are discussed.
2.Microencapsulation of soluble pharmaceuticals.
Baveja SK;Rao KV;Kumar Y J Microencapsul. 1986 Jan-Mar;3(1):33-7.
A method to microencapsulate water-soluble and liquid-paraffin insoluble drugs into spherical, discrete and free-flowing particles of approximately 175 microns size with excellent yield has been described taking diethylcarbamazine citrate as a model drug. In this method a gelatin-drug dispersion at 50 degrees C is sprayed, using a simple apparatus designed in our laboratory, into chilled, dry liquid paraffin present in a china dish previously coated with a layer of hard paraffin and maintained at 5 degrees C. After allowing the droplets to gel at 5 degrees C for an hour, water was removed by freeze drying. Later liquid paraffin adhering to freeze-dried microcapsules was removed by washing with chilled, dry acetone. Various factors affecting the yield, size, shape and size distribution of microcapsules were optimized.
3.Further observations on the relationship between ocular onchocerciasis and the head nodule, and on the possible benefit of nodulectomy.
Fuglsang H;Anderson J Br J Ophthalmol. 1978 Jul;62(7):445-9.
From the examination of 197 patients who presented with one or more head nodules in the Sudan savanna in Cameroon, and from previous examinations of patients with ocular onchoceriasis, it concluded that in this part of Africa the formation of a head nodule is often preceded by the development of ocular lesions. Head nodulectomy is therefore of limited prophylactic value. Head nodules were removed from 107 of these patients, of whom 17 also received diethyl-carbamazine citrate (DEC), and 20 received both DEC and suramin. Fifteen other patients received DEC as the only treatment, and 4 suramin alone, while 5 received both DEC and suramin. From the follow-up examinations at 9, 12, and 24 months after treatment it was concluded that removal of the head nodule was of some benefit to lesions of the anterior segment, but that the procedure should be combined with efficient micro- and macrofilaricidal therapy in patients at risk of developing ocular pathology, that is, those with 15 or more microfilariae per skin snip near the outer canthus. This index can be measured by paramedical personnel and is therefore of great public health importance in the early detection of "at risk" patients.

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