Diminazene
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| Trade names | Azidin, Berenil, Ganasag, Pirocide |
| Other names | 4,4'-(1-Triazene-1,3-diyl)bis(benzenecarboximidamide) |
| Routes of administration | IM, SC |
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| ECHA InfoCard | 100.007.860 |
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| Formula | C14H15N7 |
| Molar mass | 281.323 g·mol−1 |
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Diminazene (INN; also known as diminazen) is an anti-infective medication for animals that is sold under a variety of brand names. It is effective against certain protozoa such as Babesia, Trypanosoma, and Cytauxzoon. The drug may also be effective against certain bacteria including Brucella and Streptococcus.[1][2] Chemically it is a di-amidine and it is formulated as its aceturate salt, diminazene aceturate.
The mechanism is not well understood; it probably inhibits DNA replication,[1] but also has affinity to RNA. The drug is known to change the structure of kinetoplast DNA in the Trypanosoma cruzi parasite, which causes Chagas' disease. In particular, kinetoplasts from parasites exposed to the drug have more densely linked minicircles, leading to the formation of fibers within the networks. [3]
Side effects
[edit]Acute side effects include vomiting, diarrhea, and hypotension (low blood pressure). Diminazen can harm the liver, kidneys and brain, which is potentially life-threatening; camels are especially susceptible to these effects.[1]
Resistance
[edit]Drug resistance, or at least evidence of treatment failure, has been reported in several countries in Africa.[4][5][6] For example, the Gibe River Valley in southwest Ethiopia showed universal resistance between July 1989 and February 1993.[7] This likely indicates a permanent loss of function in this area against the tested target, T. congolense isolated from Boran cattle.[7]
References
[edit]- 1 2 3 Peregrine AS, Mamman M (September 1993). "Pharmacology of diminazene: a review". Acta Tropica. 54 (3–4): 185–203. doi:10.1016/0001-706X(93)90092-P. PMID 7902657.
- ↑ Mungube EO, Vitouley HS, Allegye-Cudjoe E, Diall O, Boucoum Z, Diarra B, et al. (August 2012). "Detection of multiple drug-resistant Trypanosoma congolense populations in village cattle of south-east Mali". Parasites & Vectors. 5 155. doi:10.1186/1756-3305-5-155. PMC 3432589. PMID 22852796.
- ↑ Zuma AA, Cavalcanti DP, Zogovich M, Machado AC, Mendes IC, Thiry M, et al. (February 2015). "Unveiling the effects of berenil, a DNA-binding drug, on Trypanosoma cruzi: implications for kDNA ultrastructure and replication". Parasitology Research. 114 (2): 419–430. doi:10.1007/s00436-014-4199-8. hdl:2268/173546. PMID 25349143.
- ↑ FAO (2022). Expert consultation on the sustainable management of parasites in livestock challenged by the global emergence of resistance - Part 2: African animal trypanosomosis and drug resistance – a challenge to progressive, sustainable disease control, 9–10 November 2021. FAO Animal Production and Health Report No. 18. Rome: FAO. doi:10.4060/cc2988en. ISBN 978-92-5-137217-3.
- ↑ Geerts S, Holmes PH (1998). Drug management and parasite resistance in bovine trypanosomiasis in Africa. PAAT Technical and Scientific Series, No. 1. Rome: FAO.
- ↑ FAO, WOAH, AU-IBAR (2026). Accelerating access to new veterinary trypanocides for Africa. Rome: FAO. doi:10.4060/cd9735en.
- 1 2 Mulugeta W, Wilkes J, Mulatu W, Majiwa PA, Masake R, Peregrine AS (April 1997). "Long-term occurrence of Trypanosoma congolense resistant to diminazene, isometamidium and homidium in cattle at Ghibe, Ethiopia". Acta Tropica. 64 (3–4). Elsevier BV: 205–217. doi:10.1016/s0001-706x(96)00645-6. PMID 9107367. S2CID 23878484.