Insecticidal activity and microsomal metabolism of biooxidizable lindane analogs

The insecticidal activity of lindane analogs, in which some chlorine atoms were replaced by other groups susceptible to microsomal oxidative metabolism, was determined against mosquitos, house flies, and German cockroaches. When tested with a synergist, piperonyl butoxide, one of the methylthio analogs was as active as lindane, whereas several others were also highly active. By examining the ratio of synergized and unsynergized LD₅₀ values (synergistic ratio value), the highly insecticidal methylthio, methoxy, and methyl analogs appear to undergo metabolic detoxication effectively in house flies. By means of in vitro metabolism experiments using microsomal fraction from house fly abdomen, the methoxy, ethoxy, and methylthio analogs were shown to be metabolized rapidly at similar rates. The synergized insecticidal activities of these compounds against various insect species relate linearly with each other, suggesting that the oxidative degradation is inhibited by the synergist to a similar extent and that the transport process to the site of action is not a limiting factor in determining the relative insecticidal activity.     

Hepatic morphology and effects of intravenous injection of sodium propionate on plasma propionate and glucose in fed and fasted dairy cattle

Sodium propionate (3 mmol/kg) was injected IV into 8 nonlactating dairy cows before and after 6 days (144 hours) of fasting. During fasting, long-chain fatty acids in plasma increased from 0.30 +/- 0.05 (SE) mM to 1.09 +/- 0.15 mM (P less than 0.05). Liver fat increased from 0.5 +/- 0.3% to 9.3 +/- 1.7% (P less than 0.05). Half-life of injected sodium propionate increased significantly (P less than 0.05) from 7.6 +/- 0.5 minutes to 10.1 +/- 1.0 minutes during fasting. Sulfobromophthalein half-life did not change significantly (3.8 +/- 0.79 minutes to 5.3 +/- 1.3 minutes). Increases in plasma glucose concentrations after propionate loading were significantly less during fasting than during feeding. Thus, the change in glucose concentration served as an indicator of hepatic conversion of propionate to glucose. Increases in glucose concentration of less than 2 mM at 30 minutes after propionate loading indicated that liver function was altered in nonlactating dairy cows.     

The clinical administration of the opioid antagonist naloxone in dogs

The short introduction gives a review on the complex of exogen and endogen opioids and their receptors as well as on their pharmacodynamics, pharmacokinetics and toxicity of naloxone. The clinical efficacy of naloxone as an opioid antagonist is described. Applications of naloxone for the dog are specified: antagonisation of etorphine, morphine, levomethadone and fentanyl, antagonisation of exogen and endogen opioids in puppies and treatment of lactomania in the bitch. The mean effective dose to antagonize morphines is 0.003 mg/kg bodyweight. If persisting analgesia is indicated the dose of naloxone in titrating steps in 0.001 mg/kg bw. To antagonize postpartal hypoxia in puppies 0.02 mg per animal naloxone have to be injected. For treatment of lactomania a dose of 0.01 mg/kg bodyweight twice a day for a couple of days is recommended. The clinical effectivity of naloxone is proved doubtlessly. Compatibility and safety are very high.