Diminazene Aceturate

Product Name: Diminazen Aceturate

Physical & Chemical Properties:

CAS No908-54-3.
Molecular Weight515.52
Molecular FormulaC22H29N9O6
Melting Point219-228°C
Boiling Point422.6°C(Decompose).

Description:
Diminazene aceturate has been shown to be an effective treatment for T. evansi in dogs, with a subcutaneous dose of 7 mg/kg on the first day and 3.5 mg/kg on the following day. The problem with the treatment is that the disease tends to recur and the treatment then has to be repeated or prolonged. In rats, for example, the drug has been administered for five consecutive days. Other drugs have been tested in dogs too, but the side-effects have been too serious.
In general, the disease can be contained by controlling the vector population. For prophylaxis, several kinds of insecticides can be used. Drugs in the isoxazoline group have been shown to be effective in killing triatomine vectors. Dogs should also be prevented from eating possible infected material. Vaccine trials have been made with dogs with promising results; however, to date, no commercial vaccine is available. Motivation to vaccinate dogs is usually based on their reservoir role in human trypanosomiasis.

Treatment:
Diminazene aceturate is administered parenterally, primarily to dogs, for treatment of babesiosis, African trypanosomiasis, and, most recently, infections with Rangelia vitalii, a novel protozoal pathogen of dogs from Brazil.30 Diminazene aceturate is not readily available in the United States. Resistance to diminazene has been described in Babesia gibsoni.31

Pharmacokinetics:
The pharmacokinetics of diminazene have not been studied in humans. In animals, the half-life is between 11 and 14 h for sheep, dogs and goats, and 63 h for cattle (Klatt and Hadju, 1976; Aliu and Odegaard, 1985; Anika and Onyeyili, 1989). In the sheep, plasma protein binding was estimated at 65–85% (Aliu and Odegaard, 1985). Diminazene is to some extent absorbed when given orally, but its usefulness by that route of administration has not been further studied since the first report by Bailey (1968).

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