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Studies of Pharmacokinetics and Toxicologic Effects of Ribovirin After Oral Administration in Vivo and Vitro of Pigs

Author: YuHong
Tutor: LiuSiDang
School: Shandong Agricultural University
Course: Basic Veterinary
Keywords: Piglets Ribavirin Pharmacokinetics Toxicity Cytotoxicity
CLC: S858.28
Type: Master's thesis
Year: 2010
Downloads: 44
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Abstract


Ribavirin (also known as ribavirin, ribavirin) (Ribavirin, Tribavirin, Virazole) guanosine compounds, first synthesized in 1972, has a broad-spectrum antiviral activity against RNA viruses and DNA viruses. Although the state has expressly prohibits ribavirin used in veterinary medicine, but in our animal viruses blight widely popular background, farming households prevention and control of animal diseases, the phenomenon of illegal use of ribavirin is still widespread, about pigs orally Lee ribavirin cause serious poisoning cases have occurred, and reported cases of poisoning, mostly conventional dosage instructions compared to pigs and other animals are more sensitive to the drug. Reveal pigs susceptible ribavirin causes and incidence and pathogenesis, and to prohibit abuse of veterinary clinical of ribavirin prevention swine illegal phenomenon provides theoretical support, re-evaluate the toxicity of ribavirin, for implementation of animal welfare and human safety drug references. The test from the plasma pharmacokinetics, the piglets poisoning modeling derived from pigs in vitro cytotoxicity test experimental study. Determination of ribavirin in pig plasma concentration of high-performance liquid chromatography (ie HPLC) method, to explore a single oral dose of 90mg/kg body weight, ribavirin, multiple oral first established in pigs (n = 3) Pharmacokinetics law. The results show that: given a single dose of 90mg/kg body weight pharmacokinetic model conforms to a two compartment compartment model, the main pharmacokinetic parameters were elimination half-life (t1/2β) (23.50 ± 3.95) h overall clearance (CL (s)) (1.97 ± 0.55) L · kg-1 · h-1, the apparent volume of distribution (V / F (c)) (33.09 ± 6.77) L · kg-1; more dose pharmacokinetic model in line with the single-chamber model, the main pharmacokinetic parameters were elimination half-life (t1/2Ke) (21.74 ± 25.41), total clearance (CL (s)) (0.73 ± 0.74) L · kg-1 · h-1, the apparent volume of distribution (V / F (c)) (9.11 ± 3.24) L · kg-1. Second, we studied the toxic effects of oral administration of different doses of ribavirin piglets. The selection of 12 kg of body weight (15.2 ± 1.5) crossbred piglets were randomly divided into four groups, respectively, for the blank control group, per kilogram of body weight ribavirin 10 mg, 30 mg, 90 mg oral test group. 10 consecutive days of administration, clinical manifestations groups were observed in detail, the dynamic detection of blood cells, serum, urine, bone marrow and liver function of various physical and chemical indicators of changes in the last bled to death necropsy and taken for histological examination. The results show that the piglets Although certain clinical manifestations of oral ribavirin 10mg/kg body weight, but no obvious lesions of poisoning;, high-dose ribavirin (30,90 mg / kg body weight) oral toxicity of pig side effects, and even lead to acute death ribavirin performance of various tissues and organs Pan addicted to toxicity, blood, bone marrow, gastrointestinal tract, pancreas, heart, liver, kidney, brain showed significant histological lesions. Hemolytic anemia pigs the poisoning incidence of major mechanism gastrointestinal catarrh necrotizing inflammation and pancreatic lesions in pigs with acute anorexia, appetite waste must, where the main reason for the constipation. Description of the porcine oral ribavirin especially in high doses will produce significant side effects, and may even cause poisoning death. Finally vitro WST-1 cytotoxicity assay kit cytotoxicity of different doses of ribavirin passaged cells derived from pigs, using an inverted microscope, making the cells seeded observed by light microscopy. The study showed that ribavirin in high concentrations of porcine kidney cells have certain toxic effects, and clinical observation to pig ribavirin poisoning prone to kidney disease, as measured according to preliminary pharmacokinetic data, the drug will remain for a long time in the red blood cells, a slower excretion, the plasma concentration of long-term at a higher range, may be the direct cause of the poisoning pig kidney disease. In short, ribavirin easier in pigs accumulation of drug widely in pigs distribution range. Performance of pigs Pan addicted toxic to red blood cells, bone marrow hematopoietic cells, gastrointestinal epithelial cells, renal tubular epithelial cells and epithelial cells of the pancreas is most sensitive to the toxic dose of piglet test the toxic dose and clinical reports, but caused large differences speculated that the clinical use of drugs herd poisoning may also, in addition to the dose, and the health status of the pigs themselves, age and physiological state, feed and other drugs impact factors.

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CLC: > Agricultural Sciences > Livestock, animal medicine,hunting,silkworm,bee > Animal Medicine ( Veterinary Medicine) > Livestock, poultry, wildlife diseases > Livestock > Pig
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