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Monday, March 10, 2008 E-Mail this article to a friend Printer Friendly Version

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New data on anti-anxiety pill tolerance from KU

Daily Times Monitor

KARACHI: Researchers at the University of Karachi have found fresh data on tolerance to anti-anxiety medication and its links to responsiveness of serotonin receptors, Drug Week reported March 7.

The data on life sciences are presented in the report ‘Tolerance in the anxiolytic profile following repeated administration of diazepam but not buspirone is associated with a decrease in the responsiveness of postsynaptic 5-HT-1A receptors.’ The research was published in the journal Acta Biologica Hungarica. It aimed to understand the role of serotonin receptors in the treatment of anxiety and the development of tolerance to benzodiazepines. The study was designed to monitor the responsiveness of postsynaptic 5-HT-1A receptors following repeated administration of diazepam and buspirone.

Diazepam was first marketed as Valium by Hoffmann-La Roche. It is a benzodiazepine derivative drug. It possesses anxiolytic, anticonvulsant, sedative, skeletal muscle relaxant and amnestic properties. It is commonly used for treating anxiety, insomnia, seizures, alcohol withdrawal, and muscle spasms.

Buspirone (brand-names Ansial, Ansiced, Anxiron, Axoren, Bespar, BuSpar, Buspimen, Buspinol, Buspisal, Narol, Spitomin, Sorbon) is an anxiolytic agent and a serotonin receptor agonist belonging to the azaspirodecanedione class of compounds. Its structure is unrelated to those of the benzodiazepines, but it has an efficacy comparable to diazepam in treating generalized anxiety disorder.

The results showed that tolerance in the anxiolytic or anti-anxiety profile was produced following repeated administration (2 weeks) of diazepam (2 mg/kg) but not buspirone (0.5 mg/kg).

“The behavioral effects of 8-OH-DPAT at a dose of 0.25 mg/kg were monitored 3 days after repeated administration of saline or buspirone or diazepam. The results show that 8-OH-DPAT elicited forepaw treading was smaller in repeated diazepam but not repeated buspirone injected rats, while hyperlocomotive effects of 8-OH-DPAT were smaller in both repeated buspirone and repeated diazepam injected rats. The results suggest that postsynaptic 5-HT-1A receptor-dependent responses were attenuated following long-term administration of diazepam but not buspirone,” wrote A. Khan and colleagues.

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