Benzodiazepinereceptor partial agonists

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As described earlier, the disadvantages of the benzodiazepines include sedation, psychomotor and cognitive impairment, and withdrawal symptoms after long-term use. Increased understanding of benzodiazepine-receptor mechanisms suggested that compounds might be developed which are partial agonists and/or selective to some subtypes of receptor.(34) Such compounds would be less efficacious than full agonists but might have better adverse-effect profiles and less dependence potential, i.e. superior risk-benefit ratios.

One such compound, alpidem, was actually marketed in France but had to be withdrawn because of liver toxicity. Initial data suggested that it was somewhat less effective than a typical full benzodiazepine agonist but that it had a distinctly better side-effect profile. (36).

Abecarnil is a b-carboline which is anxiolytic in doses of 3 to 9 mg/day. However, efficacy has been difficult to demonstrate convincingly, although the side-effect profile does appear to resemble that of a comparator benzodiazepine.

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How To Win Your War Against Anxiety Disorders

How To Win Your War Against Anxiety Disorders

Tips And Tricks For Relieving Anxiety... Fast Everyone feels anxious sometimes. Whether work is getting to us or we're simply having hard time managing all that we have to do, we can feel overwhelmed and worried that we might not be able to manage it all. When these feelings hit, we don't have to suffer. By taking some simple steps, you can begin to create a calmer attitude, one that not only helps you feel better, but one that allows you the chance to make better decisions about what you need to do next.

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