Pharmacokinetics of diminazene in sheep
Tóm tắt
The pharmacokinetic behavior of diminazene in plasma after administration of 2 mg/kg i.v. and 3.5 mg/kg i.m. was studied in four healthy Dala × Ryggja rams. Following i.v. injection, the data were satisfactorily described by a triexponential equation; the apparent volume of distribution at the steady-state was 0.56±0.04 L/Kg (X±sd; n=4); total body clearance averaged 1.1±0.09 ml/kg/min and elimination half-life was 9.30±1.40 hr. After intramuscular administration peak plasma levels of 6.30–7.57 μg/ml were reached in 20 to 45 min and the mean absorption time averaged 5.83±1.61 hr. Systemic availability relative to the intravenous dose was 95.10±23.21% and mean residence time averaged 14.16±1.55hr. The partition of diminazene between erythrocytes and plasma averaged 0.64±0.10; plasma protein binding was high (65–85%) and concentration-dependent. Based on the experimental data obtained, an initial i.m. dose of 2.5 mg/kg followed by 2 mg/kg 24 hr later should be safe and effective in cases of babesiosis and trypanosomiasis sensitive to diminazene. A preslaughter withdrawal period of 14–26 days was estimated.
Tài liệu tham khảo
W. Raether, P. Hajdu, H. Seidenath, and D. Damm. Pharmakokinetische und Chemoprophylaktische Untersuchungen mit Berenil an Wistar-Ratten (Trypanosoma rhodesiense).Zeit. Tropenmed. Parasit. 23:418–427 (1972).
P. Klatt and P. Hajdu. Pharmacokinetic investigations on diminazene and rolitetracycline in comparison to a combination of both.Vet. Rec. 99:372–374 (1976).
H. G. Fouda. Gas chromatography chemical ionization mass spectrometric analysis of diminazene in plasma.Biomed. Mass Spectrom. 5:72–75 (1978).
R. J. Gilbert and B. A. Newton. Pharmacokinetics and efficacy of the trypanocide diminazene aceturate (Berenil) in rabbits.Vet. Rec. 111:397 (1982).
Y. O. Aliu and S. Ødegaard. Paired-ion extraction and high-performance liquid Chromatographie determination of diminazene in plasma.J. Chromatogr. 276:218–223 (1983).
E. Pike and B. Skuterud. Methodological aspects on the determination of plasma binding of amitriptyline and nortriptyline.Nor. Phartn. Acta 45:33–42 (1983).
J. G. Wagner.Fundamentals of Clinical Pharmacokinetics. Drug Intelligence Publications, Hamilton Press, Inc., Hamilton Illinois, 1975, p. 461.
D. W. Marquardt. An Algorithm for least-squares estimation of nonlinear parameters.J. Soc. Ind. AppL Math. 11:431–441 (1963).
M. Gibaldi and D. Perrier. Pharmacokinetics.In J. Swarbrick (ed.),Drugs and the Pharmaceutical Sciences. Vol. 1. Marcel Dekker, New York, 1975, p. 329.
A. Rescigno and G. Segre.Drug and Tracer Kinetics. Blaisdell Publishing Co., Waltham, Massachusetts, 1966, pp. 54–62; 91–98.
S. Riegelman and P. Collier. The application of statistical moment theory to the evaluation ofin vivo dissolution time and absorption time.J. Pharmacokin. Biopharm. 8:509–534 (1980).
L. Z. Benet and R. L. Galeazzi. Noncompartmental determination of the steady-state volume of distribution.J. Phartn. Sci. 68:1071–1074 (1979).
D. Perrier and M. Mayersohn. Noncompartmental determination of the steady-state volume of distribution for any mode of administration.J. Pharm. Sci. 71:372–373 (1982).
A. G. Rico, J. C. Godfrain, G. Lorque, and V. Burgat-Sacave. Mesure des secteurs hydrigues chez différentes espèces animals a l'aide de radioelements. InIsotope Studies in the Physiology of Domestic Animals. Proceedings of a Symposium, Athens, March 20–24, 1972. Jointly organized by the IAEA and FAO. International Atomic Energy Agency, Vienna 1972,. pp. 63–72.
V. E. Hodgetts. The dynamic red cell storage function of the spleen in sheep. III. The relationship to determination of blood volume and plasma volume.Aust. J. Exp. Biol. Med. Sci. 39:187–196 (1961).
H. A. von Ketz. Wasser-und Mineraistoffhaushalt.In E. Kolb (ed.),Lehrbuch der Physiologie der Haustiere. Verlag, Jena, 1967, Ch. XIV, pp. 581–582.
H. A. von Ketz. Die Physiologie der Niere.In E. Kolb (ed.),Lehrbuch der Physiologie der Haustiere. Verlag, Jena, 1967, Ch. XII, pp. 540–543.
J. D. Baggot. Some aspects of clinical pharmacokinetics in veterinary medicine II.J. Vet. Pharmacol. Ther. 1:111–118 (1978).
G. E. Farwell, E. K. LeGrand, and C. C. Cobb. Clinical observations onBabesia gibsoni andBabesia canis infections in dogs.J. Am. Vet. Med. Assoc. 180:507–511 (1982).
B. Singh, D. P. Banerjee, and O. P. Gautam. Comparative efficacy of diminazene diaceturate and imidocarb dipropionate againstBabesia equi infection in donkeys.Vet. Parasitol. 7:173–179 (1980).
W. Küpper and M. Wolters. Observation on drug resistance ofTrypanasoma (Nannomonas< congolense andTrypanosoma (Buttonella) vivax in cattle at a feedlot in the northern Ivory Coast.Tropenmed. Parasitol. 34:203–205 (1983).
S. A. Bida and Y. O. Aliu. Trypanosomiasis.In J. L. Howard (ed.),Current Veterinary Therapy: Food Animal Practice. W. B. Saunders, Philadelphia, 1981, pp. 788–791.
K. L. Kuttler. Chemotherapy of babesiosis: A review.In M. Ristic and J. P. Kreier (eds.),Babesiosis. Academic Press, New York, 1981, pp. 65–85.
F. Hawking. Chemotherapy of trypanosomiasis.In F. Hawking and R. J. Schnitzer (eds.),Experimental Chemotherapy. Vol. I. Academic Press, New York, 1963, pp. 129–256.
F. Hawking. The action of Berenil on trypanosomes, including strains resistant to antrycide and stilbamidine.J. Comp. Pathol. Therap. 68:295–299 (1958).
T. K. Ruebush, R. H. Rubin, E. R. Wolpow, P. B. Cassaday, and M. G. Schultz. Neurological complications following the treatment of humanBabesia microti infection with diminazene aceturate.Am. J. Trop. Med. Hyg. 28:184–189 (1979).
R. Fairclough. Observations on the use of Berenil against trypanosomiasis of cattle in Kenya.Vet. Rec. 75:1107–1112 (1963).
G. J. Losos and E. Crockett. Toxicity of Berenil in the dog.Vet. Rec. 85:196 (1969).
E. N. W. Oppong. Toxicity of Berenil in the dog.Vet. Rec. 85:370 (1969).
A. M. Homeida, E. A. El-Amin, S. E. I. Adam, and M. M. Mahmoud. Toxicity of diminazene aceturate (Berenil) to camels.J. Comp. Pathol. 91:355–360 (1981).
J. G. Wagner. Do you need a pharmacokinetic model, if so, which one?J. Pharmacokin. Biopharm. 3:457–478 (1975).
J. F. M. Nouws and G. Ziv. Pre-slaughter withdrawal times for drugs in dairy cows.J. Vet. Pharmacol. Ther. 1:47–56 (1978).