Arzneimittel Forsch
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Arzneimittel Forsch · Jan 1985
Comparative Study[General pharmacologic studies on the analgesic flupirtine].
In the present study the general pharmacological properties of ethyl-N-[2-amino-6-(4-fluor-phenylmethylamino)pyridin-3-yl]carbama te (flupirtine, D 9998), a structural new analgesic, are described. In several tests with mice flupirtine shows a centrally depressant component of action. However, regarding undesirable side effects as ataxia, inhibition of motor activity etc. this action is, with respect to the analgesic effective doses less pronounced than those of comparable analgesics, for instance phenacetin. ⋯ Like several other analgesics flupirtine shows in rats a reversible antidiuretic action including sodium and chloride retention which is of relatively short duration and is not observed in long-term studies in rats and dogs. In contrast to many stronger antiinflammatory compounds, flupirtine does not possess ulcerogenic activity in rats up to high doses. A minimal inhibition of intestinal motility (mouse) is observed only in doses higher than the analgesic effective doses.
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To answer the questions of mode and site of action partly supplementary, partly new investigations with flupirtine (Katadolon) were carried out which are described below. The investigation for opiate receptor affinity of flupirtine in rat brain homogenate did not show any reduction in 3He-etorphine binding up to the highest concentration of flupirtine of 10(-5) mol/1. This result suggests that flupirtine either has a very low opiate receptor affinity or lacks it fully. ⋯ As in the experiments by oral administration, naloxone did not show any effect on the analgesic activity of flupirtine, neither by intracerebroventricular nor by intrathecal application. On the other hand, the analgesic effects of pethidine and morphine were completely suppressed by naloxone. These results demonstrate that the analgesic activity of flupirtine is not caused by the opiate mechanism.(ABSTRACT TRUNCATED AT 250 WORDS)
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Arzneimittel Forsch · Jan 1985
Randomized Controlled Trial Comparative Study Clinical TrialClinically controlled comparative study of suprofen, pentazocine, and placebo. Experience with intramuscular single doses.
Analgesic effect and tolerability of alpha-methyl-4-(2-thienylcarbonyl)-phenylacetic acid (suprofen, Suprol) 200 mg were compared with pentazocine 30 mg and placebo in 88 patients in moderate to severe postoperative pain. The trial was designed as a randomized single-blind study; the test drugs were in single doses (1 ml ampuls) administered by deep intragluteal injection in the upper outer quadrant. The test population was homogeneous as to anamnestic data; the initial intensity of pain was comparable in all three groups. ⋯ Systemic tolerability was considered good to very good in 97% of the subjects in all three treatment groups, whereas local tolerability was considered poor in 2 patients (6.9%) in the group on suprofen. There were no significant differences between the medications. Two subjects each on suprofen and pentazocine and 1 patient on placebo experienced side effects.
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Arzneimittel Forsch · Jan 1985
Randomized Controlled Trial Comparative Study Clinical TrialComparison of the oral effectiveness of etilefrine pivalate and etilefrine in a long-term trial in man.
The influence of equimolar oral doses of etilefrine pivalate (K 30 052, Ep) and etilefrine on blood pressure of patients suffering from orthostatic dysregulation was compared. Both drugs augmented the systolic blood pressure in both, the upright and horizontal body posture. ⋯ Ep in equimolar doses was nearly twice as active as etilefrine. This result is in line with the hypothesis that acylation of etilefrine with pivalinic acid inhibits the first-pass inactivation nearly completely.
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Arzneimittel Forsch · Jan 1985
Randomized Controlled Trial Clinical TrialNefopam in postoperative pain.
A comparative study between nefopam (Acupan) and pentazocine was carried out in 90 patients for treatment of postoperative pain following gynaecological operations. The results show that nefopam has an analgesic activity comparable with that of pentazocine, but its duration of action seems to be longer-lasting, even if with a longer period of latency. At equieffective analgesic action, nefopam shows a lower interference with the respiratory function. As far as side-effects are concerned a significant increase in drowsiness was observed with both types of treatment; sweating was observed only in nefopam group.