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.
Untoward direct reactions to diethylcarbamazine ... are not severe and usually disappear within a few days despite continuation of therapy. These include headache, general malaise, weakness, joint pains, anorexia, nausea, & vomiting. Other adverse effects result directly or indirectly from destruction of the parasites. These are especially severe in patients heavily infected with Onchocerce volvulus. In Wuchereria bancrofti or Loa loa infections, reactions are usually milder, although the drug may induce severe encephalitis in Loa loa. /Diethylcarbamazine/
In patients with onchocerciasis, there is usually a typical reaction within 16 hours after the first oral dose. This consists in intense itching & skin rashes, enlargement & tenderness of the inguinal lymph nodes, sometimes a fine papular rash, hyperpyrexia, tachycardia, and headache. These symtoms persist for 3 to 7 days and then subside, after which quite high doses can be tolerated. Ocular complications include limbitis, punctate keratitis, uveitis, and atrophy of the retinal pigment epithelium. Nodular swellings may occur along the course of the lymphatics, & there is often an accompanying lymphadenitis. This reaction also subsides within a few days. Almost all patients receiving therapy exhibit a leukocytosis, first evident on the second day, reaching its peak on the fourth or fifth day, & gradually subsiding over a period of a few weeks. Reversible proteinuria may occur, and the eosinophilia frequently observed in patients with filariasis can be intensified by drug therapy. /Diethylcarbamazine/
来源:Hazardous Substances Data Bank (HSDB)
毒理性
人类毒性摘录
在20例接受二乙基碳酰胺柠檬酸盐治疗的病人中，报告了4例持续性蛋白尿和3例暂时性蛋白尿。
Four cases of persistent proteinuria and 3 cases of transient proteinuria are reported among 20 patients treated with diethylcarbamazine citrate, 2% topically or 50 mg orally.
Diethylcarbamazine apparently has no adverse effect on fertility of male dogs. A number of studies in the USA to evaluate continued daily use in males have concluded that the drug causes no significant deterioration in quantity, morphology, motility, or viability of sperm. /Diethylcarbamazine/
Rapid metabolism and excretion of diethylcarbamazine probably accounts for its low toxicity. It is relatively nontoxic and side effects usually do not occur at the low dose (6.6 mg/kg) used for heartworm prevention. The greatest disadvantage of the drug is irritation to the gastric mucosa, which occurs especially when high doses (55-110 mg/kg) are used against ascarid infections of dogs and cats. /Diethylcarbamazine/
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/
ANTHELMINTIC COMPOUNDS AND COMPOSITIONS AND METHOD OF USING THEREOF
申请人：Meng Charles Q.
公开号：US20140142114A1
公开（公告）日：2014-05-22
The present invention relates to novel anthelmintic compounds of formula (I) below:
wherein
Y and Z are independently a bicyclic carbocyclic or a bicyclic heterocyclic group, or one of Y or Z is a bicyclic carbocyclic or a bicyclic heterocyclic group and the other of Y or Z is alkyl, alkenyl, alkynyl, cycloalkyl, phenyl, heterocyclyl or heteroaryl, and variables X
1
, X
2
, X
3
, X
4
, X
5
, X
6
, X
7
and X
8
are as defined herein. The invention also provides for veterinary compositions comprising the anthelmintic compounds of the invention, and their uses for the treatment and prevention of parasitic infections in animals.
The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy1, Cy2, R1, R2, R3, R4, Ra and Rb is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.
BENZAZEPINE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND USE
申请人：Takeda Chemical Industries, Ltd.
公开号：EP1422228A1
公开（公告）日：2004-05-26
The present invention provides a novel benzazepine derivative represented by formula :
wherein, R1 is a 5- or 6-membered aromatic ring, R2 is lower alkyl group, etc., Y is an optionally substituted imino group, ring A and ring B are independently an optionally substituted aromatic ring, W is formula -W1-X2-W2- (W1 and W2 are independently S(O)m1 (m1 is 0, 1 or 2), etc., and X2 is an optionally substituted alkylene groupetc. ), a preparation method and use thereof.
[EN] HETEROCYCLIC COMPOUNDS AND THEIR USE AS RETINOID-RELATED ORPHAN RECEPTOR (ROR) GAMMA-T INHIBITORS<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES ET LEUR UTILISATION EN TANT QU'INHIBITEURS GAMMA-T DU RÉCEPTEUR ORPHELIN APPARENTÉ AUX RÉCEPTEURS DES RÉTINOÏDES (ROR) )
申请人：TAKEDA PHARMACEUTICAL
公开号：WO2016002968A1
公开（公告）日：2016-01-07
Provided are heterocyclic compounds having a RORγt inhibitory action represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
[EN] ANTI PARASITIC DIHYDROAZOLE COMPOUNDS AND COMPOSITIONS COMPRISING SAME<br/>[FR] DIHYDROAZOLES ANTIPARASITAIRES ET COMPOSITIONS LES INCLUANT
申请人：MERIAL LTD
公开号：WO2011075591A1
公开（公告）日：2011-06-23
The present invention relates to novel dihydroazole of formula (I) and salts thereof: Wherein R1, A1, A2, G, X and Y are as defined in the description, compositions thereof, processes for their preparation and their uses to prevent or treat parasitic infections or infestations in animals and as pesticides.
