diethylcarbamazine Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
873 90-89-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • diethylcarbamazine citrate
  • diethylcarbamazine
  • carbamazine
  • carbilazine
  • bitirazine
  • caricide
  • ethodryl
  • notezine
An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa.
  • Molecular weight: 199.30
  • Formula: C10H21N3O
  • CLOGP: 1.62
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 26.79
  • ALOGS: 0.07
  • ROTB: 2

  • Status: OFM

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.40 g O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 0 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 63.70 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 35 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 30.11 ┬ÁM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Approvals:

DateAgencyCompanyOrphan
Nov. 13, 1950 FDA LEDERLE

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Vomiting 70.55 53.20 18 23 71584 2286460

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Vomiting 61.76 46.74 16 26 38299 1708440

Pharmacologic Action:

SourceCodeDescription
ATC P02CB02 ANTIPARASITIC PRODUCTS, INSECTICIDES AND REPELLENTS
ANTHELMINTICS
ANTINEMATODAL AGENTS
Piperazine and derivatives
FDA EPC N0000175481 Anthelmintic
FDA EPC N0000175481 Antihelminthic
MeSH PA D000871 Anthelmintics
MeSH PA D000890 Anti-Infective Agents
MeSH PA D000969 Antinematodal Agents
MeSH PA D000977 Antiparasitic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D005369 Filaricides
MeSH PA D016859 Lipoxygenase Inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Infection by Onchocerca volvulus indication 38539003 DOID:11678
Infection by Loa loa indication 44250009 DOID:13523
Lymphatic filariasis indication 240820001 DOID:12211
Eosinophilic asthma indication 367542003 DOID:9498
Bancroft's Filariasis indication

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 8.53 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Arachidonate 5-lipoxygenase Enzyme WOMBAT-PK
Prostaglandin G/H synthase 1 Enzyme WOMBAT-PK
Nematode GABA-A receptor Ion channel POSITIVE MODULATOR CHEMBL CHEMBL

External reference:

IDSource
D004049 MESH_DESCRIPTOR_UI
C0700531 UMLSCUI
D00803 KEGG_DRUG
3384 RXNORM
387340001 SNOMEDCT_US
60731009 SNOMEDCT_US
004969 NDDF
3052 PUBCHEM_CID
CHEBI:4527 CHEBI
CHEMBL684 ChEMBL_ID
CHEMBL48977 ChEMBL_ID
CHEMBL937 ChEMBL_ID
DB00711 DRUGBANK_ID
OS1Z389K8S UNII
1642-54-2 SECONDARY_CAS_RN
1540 INN_ID

Pharmaceutical products:

None