Effect of 1- (m-Chlorophenyl) -3-N, N-dimethylcarbamoy1-5-methoxypyrazole (PZ-177) on Pain Threshold of Healthy Volunteers:A Double-blind Crossover Study with Aminopyrine, Mefenamic acid and Placebo

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PZ-177 has been found to have potent analgesic and anti-inflammatory actions comparable to aminopyrine in animal experiments . The present study was performed to evaluate the analgesic effectiveness of PZ-177 in human beings. Pain threshold was measured by the method of Hardy which was improved by Nakahama (Pain Meter). The radiant heat was given to hand skin of volunteers for 3 sec, the energy was increased till volunteers feel pain and the threshold value was recorded as mcal/sec/cm<SUP>2</SUP>. Volunteers were 20-30 years old, weighing 40-70kg and train ed in order to perceive pain threshold. After pain threshold was measured every 30 min till 2hrs, drug was administered orally and pain threshold was measured for 5hrs.<BR>The low dose test was performed in 3 male and 2 female volunteers . PZ-177 of 200mg showed significantly higher pain threshold than the placebo value and showed almost the same effect as aminopyrine of 200mg. In high dose test, mean pain threshold of 5 women was increased by placebo and did not show significant difference between each drug and placebo. While in 5 male volunteers, PZ-177 of 500mg showed significantly higher pain threshold than the placebo value and was more potent than mefenamic acid of the same dose. PZ-177 was less active than aminopyrine in immediate effect after administration, but more longer than aminopyrine in maintenance of effect.
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