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Butalbital is used for its sedative and relaxant effects to impart relief from tension headaches. People also use Butalbital for migraine and pain. The medication works in the human brain to produce sedative effects. These effects, in turn, help manage complex headaches caused to muscle contraction.

Butalbital exerts its effects by inhibiting GABA (gamma-aminobutyric acid) effects. They bind to a different site of the GABA receptors from benzodiazepines. The attachment leads to increased duration of GABA-mediated opening of the channels of chloride, enhancing the inhibitory effects of GABA. As a result, Butalbital's psychological effects include hypnosis, sedation, reduced anxiety, and respiratory depression.

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