Absorption, Distribution and Excretion
Diethylcarbamazine is readily absorbed from the gastrointestinal tract. After a single oral dose of 200 to 400 mg, the concentration in plasma peaks in 1 to 2 hours ... Excretion is nearly all urinary, & more than 70% of the drug appears as metabolites. The compound is distributed almost completely throughout all body compartments with the exception of fat. Little accumulation occurs when repeated doses are given. /Diethylcarbamazine/

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Metabolism / Metabolites
Only 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.

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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.

Non-Human Toxicity Values
LD50 Rat oral 1.38 g/kg

Diethylcarbamazine citrate is a crystalline solid, scored white tablets. Used against filariasis in man and animals. (EPA, 1998)
Diethylcarbamazine citrate is a piperazinecarboxamide.
An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa.
See also: Diethylcarbamazine Citrate; Oxibendazole (component of).

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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.

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Therapeutic Uses
Filaricides; Lipoxygenase Inhibitors
Dietylcarbamazine citrate is usually admin by mouth as tablets. ... It has also been given by intramuscular injection.
For mass treatment /against microfilariae of Wucereria bancrofti and Wuchereria malayi/ with the objective of reducing microfilaremia to subinfective levels for mosquitoes, the dose is 2 mg/kg, three times daily after meals, for 7 days for treatment directed toward possible cure, this dosage regimen is carried out for 10 to 30 days. ... For practical purposes, an adequate amount seems to be a total dose of about 72 mg/kg of the citrate salt.
For /treatment against Loa loa microfilariae/ a dose of 2 mg/kg should be given 3 times daily after meals for 2 to 3 weeks. If repeated courses are required to produce cure, they should be separated by periods of 3 to 4 weeks.
For more Therapeutic Uses (Complete) data for DIETHYLCARBAMAZINE CITRATE (16 total), please visit the HSDB record page.

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Drug Warnings
There are no contraindications to the use of diethylcarbamazine, other than the fact that low doses should be used for initial therapy, especially in onchocerciasis and infection due to Loa loa (to minimize adverse reactions to destruction of the parasites).
Special care should be taken in using diethylcarbamazine in areas where both onchocerciasis and loaiasis occur. /Diethylcarbamazine/
In patients infected with Onchocerca volvulus or Wuchereria malayi, and to a lesser extent in those infected with Wuchereria bancrofti and Loa loa, the initial systemic reactions provoked by the massive destruction of microfilariae, or both during treatment may be severs. In such cases the dosage should be lowered or the drug stopped temporarily. Relief of these symptoms in heavily infected individuals may be afforded by pretreatment with corticosteroids, for example, dexamethasone (2 to 4 mg twice daily).
... use of diethylcarbamazine in microfilariae-positive dogs, is strictly contraindicated. ... The AVMA Council on Veterinary Services advises that all previously treated heartworm cases should be checked 3 months after the dog is started on diethylcarbamazine. If microfilariae are detected, the prophylactic program must be stopped until existing microfilariae are eliminated.
For more Drug Warnings (Complete) data for DIETHYLCARBAMAZINE CITRATE (6 total), please visit the HSDB record page.

C16H29N3O8

391.4168

391.195

1642-54-2

Diethylcarbamazine;90-89-1

15432

White, crystalline powder

297.4ºC at 760 mmHg

140 °C

116.6ºC

4

9

7

27

411

0

O=C(N(C([H])([H])C([H])([H])[H])C([H])([H])C([H])([H])[H])N1C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H].O([H])C(C(=O)O[H])(C([H])([H])C(=O)O[H])C([H])([H])C(=O)O[H]

PGNKBEARDDELNB-UHFFFAOYSA-N

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)

N,N-diethyl-4-methylpiperazine-1-carboxamide;2-hydroxypropane-1,2,3-tricarboxylic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

H2O : ~100 mg/mL (~255.48 mM)
DMSO : ≥ 39 mg/mL (~99.64 mM)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.5 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)