Notezine - General Information
An anthelmintic used primarily as the citrate in the treatment of filariasis, particularly infestations with Wucheria bancrofti or Loa loa. [PubChem]
Pharmacology of Notezine
Notezine is an anthelmintic drug that does not resemble other antiparasitic compounds. It is a synthetic organic compound which is highly specific for several parasites and does not contain any toxic metallic elements. Notezine continues to be the mainstay for treatment of patients with lymphatic filariasis and loiasis.
Additional information about Notezine
Notezine Indication: Used for the treatment of individual patients with certain filarial diseases including tropical pulmonary eosinophilia, loiasis, and lymphatic filariasis caused by infection with Wuchereria bancrofti, Brugia malayi, or Brugia timori.
Mechanism Of Action: The mechanism of action of diethylcarbamazine is thought to involve sensitizing the microfilariae to phagocytosis. One study showed that diethylcarbamazine's activity against Brugia malayi microfilariae is dependent on inducible nitric-oxide synthase and the cyclooxygenase pathway. It confirmed the important role of the arachidonic acid metabolic pathway in diethylcarbamazine's mechanism of action in vivo and showes that in addition to its effects on the 5-lipoxygenase pathway, it targets the cyclooxygenase pathway and COX-1.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Diethylcarbamazine
Synonyms: Diethyl carbamazine; Ethodryl; Ditrazine base; Carbamazine; Carbilazine
Drug Category: Anthelmintics; Filaricides; Lipoxygenase Inhibitors
Drug Type: Small Molecule; Approved
Absorption: Readily absorbed following oral administration.
Toxicity (Overdose): Oral LD50 in rat and mouse is 1400 mg/kg and 660 mg/kg, respectively.
Protein Binding: Not Available
Biotransformation: Partially metabolized to diethylcarbamazine N-oxide.
Half Life: Approximately 8 hours.
Dosage Forms of Notezine: Not Available
Chemical IUPAC Name: N,N-diethyl-4-methylpiperazine-1-carboxamide
Chemical Formula: C10H21N3O
Diethylcarbamazine on Wikipedia: https://en.wikipedia.org/wiki/Diethylcarbamazine
Organisms Affected: Humans and other mammals; Parasitic nematodes and other roundworms