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Butalbital has generalized depressant effect on central nervous system and, in very high doses, has peripheral effects. Acetaminophen has analgesic and antipyretic effects; its analgesic effects may be mediated through inhibition of prostaglandin synthetase enzyme complex. Caffeine is thought to produce constriction of cerebral blood vessels.

Butalbital has half-life of about 35 hours. Acetaminophen half-life is 1.25 to 3 hours, but may be increased by liver damage and following overdosage. Caffeine half-life is about 3 hours.