Details
Stereochemistry | RACEMIC |
Molecular Formula | C17H8Cl3N4O2.Na |
Molecular Weight | 429.62 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[Na+].ClC1=CC=C(C=C1)C(C#N)C2=C(Cl)C=C(C=C2Cl)N3N=CC(=O)[N-]C3=O
InChI
InChIKey=HMGDHGGCYNUBOJ-UHFFFAOYSA-M
InChI=1S/C17H9Cl3N4O2.Na/c18-10-3-1-9(2-4-10)12(7-21)16-13(19)5-11(6-14(16)20)24-17(26)23-15(25)8-22-24;/h1-6,8,12H,(H,23,25,26);/q;+1/p-1
DescriptionCurator's Comment: description was created based on several sources, including, https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=875c461a-e0db-4478-9006-7bd1d006ed3a
Curator's Comment: description was created based on several sources, including, https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=875c461a-e0db-4478-9006-7bd1d006ed3a
Diclazuril is a main component of veterinary drugs used for the treatment of coccidiosis (chickens, turkeys, rabbits, etc) and equine protozoal myeloencephalitis (horses). When used for the treatment of coccidiosis, it acts by causing the degeneration of schizonts and gamonts. While in the animals affected by protozoal myeloencephalitis the drug is believed to inhibit merozoite production. In vivo experiments on horses have shown that the drug may cross the blood brain barrier.
CNS Activity
Sources: http://thomastobin.com/archive/240%20-%20Detection,%20Quantification%20and%20pharmacokinetics%20of%20Dic.pdf
Curator's Comment: The drug was shown to cross the BBB in horses.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: Differentiation during parasite development |
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Target ID: Merozoite production |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Preventing | CLINACOX Approved UseFor the prevention of coccidiosis in animals. Launch Date1999 |
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Curative | PROTAZIL Approved UseFor the treatment of equine protozoal myeloencephalitis (EPM) caused by Sarcocystis neurona. Launch Date2007 |
PubMed
Title | Date | PubMed |
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In vitro cultivation of Cryptosporidium parvum and screening for anticryptosporidial drugs. | 1990 Aug |
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Anti-cryptosporidial drug activity screened with an immunosuppressed rat model. | 1991 Nov-Dec |
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Assessment of candidate anticryptosporidial agents in an immunosuppressed rat model. | 1993 Mar |
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Activity of diclazuril against Toxoplasma gondii in cultured cells and mice. | 1994 Apr |
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Quantitative analysis of diclazuril in animal plasma by liquid chromatography/electrospray ionization mass spectrometry. | 2002 |
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Resistance to anticoccidial drugs of Dutch avian Eimeria spp. field isolates originating from 1996, 1999 and 2001. | 2003 Aug |
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Anticoccidial efficacy of drinking water soluble diclazuril on experimental and field coccidiosis in broiler chickens. | 2005 Aug |
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Incidence of residues of nine anticoccidials in eggs. | 2005 Nov |
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The efficacy and economic benefits of Supercox, a live anticoccidial vaccine in a commercial trial in broiler chickens in China. | 2006 Nov 30 |
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Higher incidence of Eimeria spp. field isolates sensitive for diclazuril and monensin associated with the use of live coccidiosis vaccination with paracox-5 in broiler farms. | 2006 Sep |
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Increased level of Eimeria sensitivity to diclazuril after using a live coccidial vaccine. | 2006 Sep |
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New therapeutic approaches for equine protozoal myeloencephalitis: pharmacokinetics of diclazuril sodium salts in horses. | 2006 Spring |
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Efficacy of various anticoccidials against experimental porcine neonatal isosporosis. | 2007 Jan |
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Efficacy of some anticoccidial drugs for treating coccidial enteritis of the common carp caused by Goussia carpelli (Apicomplexa: Eimeriidae). | 2007 Mar |
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Use of antigen mimics to produce specific antibodies to anti-coccidial drugs. | 2007 May 31 |
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The effect of a metaphylactic treatment with diclazuril (Vecoxan) on the oocyst excretion and growth performance of calves exposed to a natural Eimeria infection. | 2007 Nov 10 |
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Effect of subcutaneously administered diclazuril on the output of Eimeria species oocysts by experimentally infected rabbits. | 2008 Feb 2 |
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Assessing the effect of diclazuril on the intestinal absorptive capacity of broilers infected with experimental coccidiosis, using d-xylose absorption test. | 2008 Jun |
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Comparison of three adjuvants used to produce polyclonal antibodies to veterinary drugs. | 2008 Mar 15 |
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Efficacy of toltrazuril (Baycox 5% suspension) in natural infections with pathogenic Eimeria spp. in housed lambs. | 2009 Apr |
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Study of the comparative efficacy of toltrazuril and diclazuril against ovine coccidiosis in housed lambs. | 2009 Aug |
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Genotype comparison of sorbitol-negative Escherichia coli isolates from healthy broiler chickens from different commercial farms. | 2009 Jul |
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Dietary supplementation of mannan-oligosaccharide enhances neonatal immune responses in chickens during natural exposure to Eimeria spp. | 2009 Mar 19 |
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[Comparison of pretreatment methods for the simultaneous determination of diclazuril and toltrazuril residues in chicken tissues]. | 2009 May |
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Fast liquid chromatography/multiple-stage mass spectrometry of coccidiostats. | 2009 May |
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Multi-residue confirmatory method for the determination of twelve coccidiostats in chicken liver using liquid chromatography tandem mass spectrometry. | 2009 Nov 13 |
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Validation of a multi-residue liquid chromatography-tandem mass spectrometry confirmatory method for 10 anticoccidials in eggs according to Commission Decision 2002/657/EC. | 2009 Nov 13 |
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Sensitivity of isolates of Eimeria from turkey flocks to the anticoccidial drugs amprolium, clopidol, diclazuril, and monensin. | 2009 Sep |
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Actin-depolymerizing factor of second-generation merozoite in Eimeria tenella: clone, prokaryotic expression, and diclazuril-induced mRNA expression. | 2010 Feb |
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Eimeria tenella: effects of diclazuril treatment on microneme genes expression in second-generation merozoites and pathological changes of caeca in parasitized chickens. | 2010 Jul |
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Multi-residue method for detecting coccidiostats at carry-over level in feed by HPLC-MS/MS. | 2010 Jun |
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Histomorphometry and macroscopic intestinal lesions in broilers infected with Eimeria acervulina. | 2010 Mar 25 |
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Effects of diclazuril on apoptosis and mitochondrial transmembrane potential in second-generation merozoites of Eimeria tenella. | 2010 Mar 25 |
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Pharmacokinetic and tissue distribution of doxycycline in broiler chickens pretreated with either: diclazuril or halofuginone. | 2010 Nov |
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Livestock drugs and disease: the fatal combination behind breeding failure in endangered bearded vultures. | 2010 Nov 30 |
Sample Use Guides
In Vivo Use Guide
Curator's Comment: http://www.accessdata.fda.gov/scripts/animaldrugsatfda/details.cfm?dn=141-268
Coccidiosis: Mix 200 gram of Clinacox 0.5% premix per ton of complete feed. Equine protozoal myeloencephalitis: 1 milligram per kilogram of body weight in the daily grain ration for 28 days
Route of Administration:
Oral
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112209-99-1
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5K4327702E
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59915424
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PARENT (SALT/SOLVATE)
SUBSTANCE RECORD