Trazodone, a second generation antidepressant, is helpful in the treatment of lasting alcohol withdrawal symptoms, such as sleep disturbances and craving. We report a case suggesting that trazodone is also efficient for the treatment of the acute phase of alcohol withdrawal treatment. A 30-year-old male patient with severe alcohol withdrawal symptoms was successfully treated with an adjuvant administration of 600 mg trazodone per day, while he had remained symptomatic for several days under high doses of diazepam and clomethiazolum. Controlled trials with trazodone for this indication could be useful.
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A series of alkyl lysophospholipid (ALP) analogs of ET-18-OCH3 (1-O-octadecyl-2-O-methyl-rac-glycero-3-phosphocholine) containing modifications in the long C-1 chain has been synthesized and evaluated in human tumor cell line cytotoxicity assays. The compounds have also been evaluated in platelet activating factor (PAF) receptor agonism and hemolysis tests. Two modifications have been studied, introduction of a carbonyl group at different positions of the C-1 chain and branching of this chain, in some compounds with incorporation of a phenyl group. Several compounds showed a cytotoxic potency comparable to that of the reference compound ET-18-OCH3, associated with reduced proaggregating and hemolytic effects. The two enantiomers of 1-O-(7-oxooctadecyl)-2-O-methyl-rac-glycero-3-phosphocholine (2) showed the same level of cytotoxicity or antiproliferative activity, with the PAF-agonistic effect confined to R-2. The very low stereoselectivity found in the in vitro cytotoxicity confirms earlier results and indicates a lack of stereospecific interactions with a macromolecular target.
Four series of potential PAF‐antagonists in which the isoxazole nucleus is condensed with a polyhydrogenated five‐ or six‐carbon ring were prepared. The synthesis of the compounds 3‐aryl‐4,5,6,7‐tetrahydrobenz[c]isoxazoles 1, 3‐arylcyclopent[c]isoxazoles 2, 3‐aryl‐4,5,6,7‐tetrahydrobenz[d]isoxazoles 3, and 3‐arylcyclopent[d]isoxazoles 4, required an extensive optimization and comparison of the methods available in the literature.
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