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Journal of the South African Veterinary Association

versão On-line ISSN 2224-9435
versão impressa ISSN 1019-9128

J. S. Afr. Vet. Assoc. vol.80 no.4 Cape Town  2009

 

ARTICLE ARTIKEL

 

The intravenous pharmacokinetics of diminazene in healthy dogs

 

 

V Naidoo; M S G Mulders; G E Swan

Department of Paraclinical Sciences, Faculty of Veterinary Science, University of Pretoria, Private Bag X04, Onderstepoort, 0110 South Africa

 

 


ABSTRACT

Diminazene remains one of South Africa's most commonly used antiprotozoal agents for the management of babesiosis in dogs . Although the drug has been on the market for over 40 years, its intravenous pharmacokinetics are poorly known. To better understand the pharmacokinetics of the drug Berenil®, it was reconstituted in sterile water and administered intravenously to 6 adult German shepherd dogs. All 6 dogs demonstrated the previously described secondary peak in the plasma concentration versus time profile. The plasma pharmacokinetics for diminazene are described by both non-compartmental and compartmental models. From non-compartmental analysis, the area under curve to the last sample point (AUQast), clearance (CL) and volume of distribution (Vz) were 4.65 ± 1.95 ng/ml/h, 0.77 ± 0.18 l/kg/h and2.28 ± 0.60 l/kg respectively. For compartmental modelling, the plasma concentrations were fitted to both a 2-compartmental open model and a recirculatory enterohepatic model. From the recirculation model, the rate of release and re-entry into the central compartment varied markedly with the rate of release from the gall bladder (Ttom) being estimated at 27 ± 20.90 h. Once released, drug re-entry into the central compartment was variable at 9.70 ± 5.48 h. With normal biliary excretion time being about 2 h, this indicates that the redistribution cannot be occurring physiologically from the bile. Although it was not possible to identify the site from which sequestration and delayed release is occurring, it is believed that it is most likely from the liver. The study therefore showed that the secondary peak described for the pharmacokinetics of intramuscular administered diminazene in the dog is not related to biphasic absorption.

Keywords: Berenil®, dog, enterohepatic, intravenous, pharmacokinetics, PK40, recirculation


 

 

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REFERENCES

1. Anika S M, Onyeyili P A 1989 Effects of trypanosomal infection on the pharmacokinetics of diminazene aceturate in dogs. Tropical Medicine and Parasitology 40: 419-421        [ Links ]

2. Botha H 1964 Berenil: Effect against Babesia canis and comparison with phenamidine. Journal of the South African Veterinary Association 35: 23-24        [ Links ]

3. Carrington, C, du Plessis, A, Naidoo, V 2008 Antimicrobials. Index ofveterinary specialities (46th edn) MIMS, Johannesburg        [ Links ]

4. CoetzerJAW,Tustin R C 2004 Babesioses. In CoetzerJAW, Tustin R C (eds). Infectious diseases of livestock in southern Africa (2nd edn). Oxford University Press, Cape Town: 405        [ Links ]

5. Collett M G 2000 Survey of canine babesiosis in South Africa. Journal of the South African Veterinary Association 71: 180-186        [ Links ]

6. Gabrielsson, J, Werner, D 2006 Enterohepatic recirculation. Pharmacokinetic and pharmacodynamic data analysis (4th edn). Swedish Pharmaceutical Press, Sweden        [ Links ]

7. Gummow B, Swan G E, du Preez J L 1994 A bioequivalence and pharmacokinetic evaluation of 2 commercial diminazene aceturate formulations administered intra-muscularly to cattle. Onderstepoort Journal of Veterinary Research 61: 317-326        [ Links ]

8. Jacobson L S, Clark I A 1994 The patho-physiology of canine babesiosis: new approaches to an old puzzle. Journal of the South African Veterinary Association 65: 134-145        [ Links ]

9. Joubert K E, Kettner F, Lobetti R G, Miller D M 2003 The effects of diminazene aceturate on systemic blood pressure in clinically healthy adult dogs. Journal of the South African Veterinary Association 74: 69-71        [ Links ]

10. Mamman M, McKeever D J, Aliu Y O, Peregrine A S 1996 Pharmacokinetics of diminazene in plasma and lymph of goats. American Journal of Veterinary Research 57: 710-714        [ Links ]

11. Miller D M, Swan G E, Lobetti R G, Jacobson L S 2005 The pharmacokinetics of diminazene aceturate after intramuscular administration in healthy dogs. Journal of the South African Veterinary Association 76: 146-150        [ Links ]

12. Milner R J 1997 The effect of diminazene aceturate on cholinesterase activity in dogs with canine babesiosis. Journal of the South African Veterinary Association 68: 111-113        [ Links ]

13. Moore A S, Coldham N G, Sauer M J 1996 A cellular mechanism for imidocarb retention in edible bovine tissues. Toxicology Letters 87: 61-68        [ Links ]

14. Naidoo V, Sykes R 2005 Overview of suspected adverse reactions to veterinary medicinal products reported in South Africa (March 2003 - February 2004). Journal of the South African Veterinary Association 76: 49-52        [ Links ]

15. Naudé T W, Basson P A, Pienaar J G 1970 Experimental diamidine poisoning due to commonly used babecides. Onderstepoort Journal of Veterinary Research 37: 173-184        [ Links ]

16. Onyeyili P A, Anika S M 1991 Diminazene aceturate residues in the tissues of healthy, Trypanosoma congolense and Trypanosoma brucei brucei infected dogs. British Veterinary Journal 147: 155-162        [ Links ]

17. Uilenberg G 2006 Babesia-Ahistorical overview. Veterinary Parasitology 138: 3-10        [ Links ]

 

 

Received: June 2009
Accepted: September 2009

 

 

* Author for correspondence. E-mail: vinny.naidoo@up.ac.za

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