Dantrolene
Dantrolene is a ryanodine (RYR1) receptor antagonist, which prevents release of Ca2+ from the sarcoplasmic reticulum, uncoupling the process of excitation-contraction.
| Property | Dantrolene |
|---|---|
| Uses | MH, NMS, ecstasy intoxication, chronic muscle spasticity |
| Presentation | Vials of orange powder containing 20mg dantrolene and 3g mannitol, reconstituted with 60ml of H2O to form an alkaline solution. |
| Dosing | 2.5mg.kg-1 IV every 10-15 minutes, up to 10mg.kg-1. Once resolved, continue giving 1mg.kg-1 every 4-6 hours for 24 hours. |
| Absorption | IV only, may cause skin necrosis if extravasates. |
| Distribution | 85% protein bound |
| Metabolism | Hepatic metabolism to active 5-hydroxy-dantrolene |
| Elimination | Renal of metabolites, t1/2β of 12 hours |
| Resp | Respiratory failure due to skeletal muscle weakness |
| CVS | Volume overload due to large volume given with administration |
| MSK | Skeletal muscle relaxation |
| Renal | Diuresis |
| GIT | Hepatic failure |
References
- Peck TE, Hill SA. Pharmacology for Anaesthesia and Intensive Care. 4th Ed. Cambridge University Press. 2014.
- Petkov V. Essential Pharmacology For The ANZCA Primary Examination. Vesselin Petkov. 2012.
- ANZCA August/September 2011