NEW BENZODIAZEPINES
1
r rand d INPHARMA 10th April, 1976 p6 NEW BENZODIAZEPINES Estazolam Estazolam is a new triazolobenzodiazepine derivative developed in Japan. Its hypnotic activity is 5 times that of diazepam and twice that of nitrazepam in monkeys. The optimal dose of estazolam for improving sleep is 2mg, but 3mg may be ne_eded in subjects with severe anxiety. During a COI:ttrolled double-bli.>ld study, the effects were compared of estazolam, nitrazepam and placebo on the pre-operative night sleep in I ,139 surgical patients. The ranking of efficacy in improving sleep was estazolam 4mg > estazolam 3mg = nitrazepam 1 Omg = estazolam 2mg > nitrazepam 5mg > estazolam lmg > placebo. In terms of the incidence of side-effects the order was estazolam 4mg = estazolam 3mg > nitrazepam lOmg > estazolam 2mg > nitrazepam Smg > estazolam lmg =placebo. The incidence of unsteadiness was particularly high for estazolam 4mg. The state of sleep on the pre-operative night was significantly improved in all active drug groups except for those receiving estazolam lmg, as compared to placebo. Momose, T. et al.: Current Therapeutic Research 19: 277 (Mar 1976) Camazepam Camazepam (SB-5833; Simes) has been shown to be an effective anxiolytic drug in psychoneurotic patients. It seems to be more useful than diazepam during endoscopy inspection. Seventy patients undergoing diagnostic gastroduodenoscopy received either oral diazepam 1 Omg or camazepam 20mg, 2 hours before examination and under double-blind conditions. In the 65 patients analysed, patient co- operation was significantly better (P < 0.01) after camazepam and visceral reflexes were significantly less (P < 0.05). There was a significantly higher incidence (P < 0.001) of drowsiness in the diazepam group, with over 50% of patients experiencing it. Camazepam caused little drowsiness and did not interfere with secretion or peristalsis. Galli, G.: Current Therapeutic Research 19: 316 (Mar 1976) • Diclonium bromide (Norwich) has potential application in the treatment of spastic-colon disease and peptic ulcers. It has negligible anticholinergic activity, but exerts potent gastric acid-antisecretory and anti-ulcerogenic effects in the rat stomach together with a prolonged inhibitory action on contractions in the lower bowel of the dog. Goldenberg, M.M.: Arzneimittel-Forschung 26: 341, 347 (Mar 1 0'7t::\ .l.JIVJ
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Transcript of NEW BENZODIAZEPINES
r
rand d
INPHARMA 10th April, 1976 p6
NEW BENZODIAZEPINES
Estazolam Estazolam is a new triazolobenzodiazepine derivative developed in Japan. Its hypnotic activity is 5 times that of diazepam and twice that of nitrazepam in monkeys. The optimal dose of estazolam for improving sleep is 2mg, but 3mg may be ne_eded in subjects with severe anxiety. During a COI:ttrolled double-bli.>ld study, the effects were compared of estazolam, nitrazepam and placebo on the pre-operative night sleep in I ,139 surgical patients. The ranking of efficacy in improving sleep was estazolam 4mg > estazolam 3mg = nitrazepam 1 Omg = estazolam 2mg > nitrazepam 5mg > estazolam lmg > placebo. In terms of the incidence of side-effects the order was estazolam 4mg = estazolam 3mg > nitrazepam lOmg > estazolam 2mg > nitrazepam Smg > estazolam lmg =placebo. The incidence of unsteadiness was particularly high for estazolam 4mg. The state of sleep on the pre-operative night was significantly improved in all active drug groups except for those receiving estazolam lmg, as compared to placebo.
Momose, T. et al.: Current Therapeutic Research 19: 277 (Mar
1976)
Camazepam Camazepam (SB-5833; Simes) has been shown to be an effective anxiolytic drug in psychoneurotic patients. It seems to be more useful than diazepam during endoscopy inspection.
Seventy patients undergoing diagnostic gastroduodenoscopy received either oral diazepam 1 Omg or camazepam 20mg, 2 hours before examination and under double-blind conditions. In the 65 patients analysed, patient cooperation was significantly better (P < 0.01) after camazepam and visceral reflexes were significantly less (P < 0.05). There was a significantly higher incidence (P < 0.001) of drowsiness in the diazepam group, with over 50% of patients experiencing it. Camazepam caused little drowsiness and did not interfere with secretion or peristalsis.
Galli, G.: Current Therapeutic Research 19: 316 (Mar 1976)
• Diclonium bromide (Norwich) has potential application in the treatment of spastic-colon disease and peptic ulcers. It has negligible anticholinergic activity, but exerts potent gastric acid-antisecretory and anti-ulcerogenic effects in the rat stomach together with a prolonged inhibitory action on contractions in the lower bowel of the dog. Goldenberg, M.M.: Arzneimittel-Forschung 26: 341, 347 (Mar 1 0'7t::\ .l.JIVJ
