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FACP. Colegio de médicos de Tarragona Nº 4305520 / fgcapriles@gmail.com

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lunes, 4 de junio de 2018

Dantrolene

EMCrit
EMCrit - June 4, 2018 - By Sarah Shafer
"Dantrolene is one of the few, true “muscle relaxers”. It was discovered in 1967 and approved by the FDA in 1979. Unlike paralytic neuromuscular blockers, dantrolene works post-synaptically, at the sarcoplasmic reticulum in the myocyte. It binds to the ryanodine receptor in skeletal muscle (RYR1), preventing sarcoplasmic calcium-induced calcium release.
When RYR1 works normally, calcium gets released from the sarcoplasmic reticulum and binds to troponin, exposing actin. This allows myosin to bind with actin to produce muscle contraction. When there is too much calcium, it causes excess muscle contraction. Without enough calcium, myosin is blocked from binding to actin. When dantrolene is at steady-state in healthy human volunteers, it produces a 75% reduction in muscle twitch without full paralysis. It reduces grip strength in volunteer subjects by over 50%, taking 20 hours to return to normal. Residual weakness can persist for up to 48 hours. [Flewellen 1983 PMID: 6614536]..."