Arzneimittel Forsch
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Arzneimittel Forsch · Oct 1986
On steroid-saving drug combinations in carrageenin paw edema and adjuvant arthritis.
Sequential potentiation of antiinflammatory activity of dexamethasone was obtained by co-administration of diclofenac-Na (and indomethacin), but not of phenylbutazone and, apparently, of acetylsalicylic acid (ASA) in the carrageenin rat paw edema. In the adjuvant arthritic rat, additive effects were only seen. ⋯ However, phenylbutazone failed in this respect, possibly due to its different mode of action. Admixture of ascorbic acid rather decreased than increased antiinflammatory activity of cyclooxygenase inhibitors and drug combinations except ASA, the effectivity of which was practically not changed.
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Arzneimittel Forsch · Jul 1986
Randomized Controlled Trial Clinical Trial Controlled Clinical TrialDouble-blind placebo-controlled study of the efficacy and tolerability of suprofen suppositories in patients with osteoarthritic pain.
In a placebo-controlled double-blind trial analgesic effectiveness and tolerability of alpha-methyl-4-(2-thienyl-carbonyl)phenylacetic acid (suprofen, Suprol) 300 mg suppositories were evaluated for 45 informed patients suffering from chronic pain due to osteoarthritis; the subjects were treated rectally, t.i.d., for 10 days. Suprofen proved to be statistically significantly superior to placebo in all the variables considered for evaluation of the analgesic effect, i.e., pain intensity and relief scores, sum of pain intensity differences (SPID), total pain relief (TOTPAR), global assessments by investigator and patient. ⋯ Similar frequencies of rectal side-effects were observed in both treatment groups, with slightly but not significantly higher incidence in the group treated with suprofen. Haematologic and clinical chemistry laboratory tests showed no statistically significant alterations due to the treatment.
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Arzneimittel Forsch · Jul 1986
Randomized Controlled Trial Comparative Study Clinical TrialClinically controlled comparative study of intravenous single doses of suprofen versus indoprofen.
The analgesic effects of single intravenous doses of alpha-methyl-4-(2-thienyl-carbonyl)phenylacetic acid (suprofen, Suprol) 200 mg/ml and alpha-4-(2-isoindolinyl-2-one)-phenylpropionic acid (indoprofen) 200 mg were compared within the scope of a randomized single-blind study. The test population consisted of 87 patients for whom analgesic treatment was indicated as soon as severe to major pain set in following meniscectomy or disease of a ligament. The treatment groups were homogeneous with respect to demographic data and intensity of pain prior to treatment. ⋯ Therapeutic results were seen in 95.5% of the subjects on suprofen and in 97.6% of those on indoprofen. The tolerability of suprofen was very good in 95.3% of the cases on suprofen and in 97.3% of those on indoprofen. Four patients in the suprofen group experienced adverse reactions that were, however, not drug related.
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Arzneimittel Forsch · Mar 1986
[Detection and quantitative determination of lectins and viscotoxins in mistletoe preparations].
Mistletoe lectins and viscotoxins, which up to now have been isolated only from plant material, were detected and quantitatively determined in the mistletoe preparation Iscador and in a fermented mistletoe extract. Lectins were isolated by affinity chromatography and analyzed by isoelectric focussing. ⋯ The lectin content of the preparation and the extract was determined by "single radial immunodiffusion" (SRID). For identification and quantitative determination of viscotoxins, a HPLC method was designed.
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Arzneimittel Forsch · Jan 1986
2-Acetylpyridine thiosemicarbazones. 12. Derivatives of 3-acetylisoquinoline as potential antimalarial agents.
A series of 3-acetylisoquinoline thiosemicarbazones and their related thiosemicarbazides was prepared for evaluation as potential antimalarial agents. The former were synthesized by the reaction of 3-acetylisoquinoline with methyl hydrazinecarbodithioate to give methyl 3-[1-(3-isoquinolinyl)ethylidene]hydrazinecarbodithioate, IV. Displacement of the S-methyl group of this intermediate by the requisite amines gave 3-acetylisoquinoline thiosemicarbazones, V. ⋯ Reaction of this dithioester with amines gave 1-[1-(3-isoquinolinyl)ethyl-3-thiosemicarbazides, VII. The antimalarial properties of series V and VII were evaluated in mice infected with Plasmodium berghei. Significant curative activity could be observed at doses as low as 40 mg/kg for 3 of 10 compounds in series V and at 160 mg/kg for 3 of 11 compounds in series VII.