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Description: Chemically, dantrolene is a hydantoin derivative, but does not exhibit antiepileptic activity like other hydantoin derivates such as phenytoin.
Drug Type: Small Molecule; Approved
Pharmacology: Dantrolene is classified as a direct-acting skeletal muscle relaxant. It is currently the only specific and effective treatment for malignant hyperthermia. In isolated nerve-muscle preparation, Dantrium has been shown to produce relaxation by affecting the contractile response of the muscle at a site beyond the myoneural junction. In skeletal muscle, Dantrium dissociates excitation-contraction coupling, probably by interfering with the release of Ca2+ from the sarcoplasmic reticulum. In the anesthetic-induced malignant hyperthermia syndrome, evidence points to an intrinsic abnormality of skeletal muscle tissue. In selected humans, it has been postulated that “triggering agents” (e.g.,general anesthetics and depolarizing neuromuscular blocking agents) produce a change within the cell which results in an elevated myoplasmic calcium. This elevated myoplasmic calcium activates acute cellular catabolic processes that cascade to the malignant hyperthermia crisis. It is hypothesized that addition of Dantrium to the “triggered” malignant hyperthermic muscle cell reestablishes a normal level of ionized calcium in the myoplasm.
Mechanism of Action: Dantrolene depresses excitation-contraction coupling in skeletal muscle by binding to the ryanodine receptor 1, and decreasing intracellular calcium concentration. Ryanodine receptors mediate the release of calcium from the sarcoplasmic reticulum, an essential step in muscle contraction.
Indication: For use, along with appropriate supportive measures, for the management of the fulminant hypermetabolism of skeletal muscle characteristic of malignant hyperthermia crises in patients of all ages. Also used preoperatively, and sometimes postoperatively, to prevent or attenuate the development of clinical and laboratory signs of malignant hyperthermia in individuals judged to be malignant hyperthermia susceptible.
Half Life: The mean biologic half-life after intravenous administration is variable, between 4 to 8 hours under most experimental conditions, while oral is 8.7 hours for a 100mg dose.
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Data Correlations | 2 studies

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Genes category icon Genes
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RYR1 100 100
PBX1 94 94
CTSZ 89 89
RIT1 88 88
KIAA0125 86 86
ZNF506 85 85
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Biogroups category icon Biogroups
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I8 - chymotrypsin/elastase inhibit… 100 100
Transposase, L1 97 97
Fork head transcription factor 95 95
Globoside Metabolism 94 94
I27 - Inhibitor family I27 (calpas… 94 94
Thiamine Metabolism 93 93
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Individual Studies

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    Homo sapiens Homo sapiens | Therapeutic   Therapeutic

    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…

  • Broad Connectivity Map (CMAP 2.0) compound database

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    A reference collection of genome-wide transcriptional expression data from cultured human cells treated with bioactive small molecules that enable the discovery of functional connections between drugs, genes and diseases through the transitory feature of common gene-expression changes.

    Authors: Lamb J

    Organization: Broad Institute Seven Cambridge Center C…
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Associated Researchers

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Thought leaders and organizations working on research involving dantrolene.

View All Author iconAuthors
  • Takaaki Ikemoto
  • Toshiyuki Hiramatsu
  • Takamitsu Hosoya
  • Hiroshi Aoyama
  • Masaaki Suzuki
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • GlaxoSmithKline
  • Stanford University
  • Reata Pharmaceuticals, Inc.
  • Medical University of Vienna
  • University of Massachusetts
View All Affiliations icon Organizations
  • Atatürk University
  • Medical Research Centre
  • Okayama University Graduate School of Medicine and Dentistry
  • University of Massachusetts Medical School
  • Yamaguchi University Graduate School of Medicine

Clinical Trials | 17 trials

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