Wednesday, October 2, 2013

Dantrolene! A Direct Skeletal muscle Relaxant

Dantrolene is a drug that has a direct action on skeletalmuscle and is used for the relief of spasticity associated with a variety of conditions.Dantrolene sodium (Dantrium IV) is manufactured by Procter & Gamble Pharmaceuticals.



How it acts?
It acts on Rayanodene receptors calcium channels present on sarcoplasmic reticulum in skeletal muscles thus leads to inhibit the release of calcium (involves in contractility of muscles.Its action is more strong on twitched mucles as compared to normal spastic muscles.

What is Malignant hyperthemia?
Malignant hyperthermia is a clinical syndrome characterized by increased body metabolism, muscle rigidity and high fever. Death may result from cardiac arrest, brain damage, internal hemorrhaging or failure of other body systems. Mostly inhalation anaesthetics and succinylcholine are triggering cause in sensitive patient. MH had a mortality rate of about 80 percent at the time Dantrlene was identified in 1960. Treatment included at this was only of cooling the patient and treating the specific symptoms, but not the underlying cause. Since 1979, the drug dantrolene sodium was used for the treatment of MH and has contributed greatly to a dramatic decrease in mortality.
Dantrolene is Only for Non ambulatory patient Why?

Dantrolene causes a generalized weakness; thus, its use should be restricted to non-ambulatory patients with severe spasticity. Dantrolene IV may decrease the grip strength and increase weakness of leg  muscles, especially walking down stairs.

Can dantrolene contribute to methotrexate toxicity? 
Dantrolene was considered to have caused methotrexate toxicity in a patient given high-dose methotrexate.

What should be precaution for its use?
  • It is recommended that dantrolene sodium should not be given to patients with active liver disease. Liver-function tests should be performed in all patients be-fore and during treatment; if abnormal values are found, treatment should generally be stopped. The risk of liver injury may be increased in patients over 30 years of age, in females (especially those taking oestro-gens), in those with a history of liver disease, and with doses above 400 mg daily (see under Effects on the Liver, above).
  • Dantrolene sodium should be used with caution in patients with cardiac or pulmonary disorders. It should not be given to patients who use their spasticity to maintain posture or function or to patients with acute muscle spasm.
  • Dantrolene sodium may cause drowsiness; patients affected should not drive or operate machinery.
Some Instruction  About Dantrolene Injecctables!
  • Give by rapid IV injection. Use of a central line is preferable if possible because of the high pH.
  • Give by IV infusion over 60 minutes.
  • Dantrolene sodium is incompatible with NaCl 0.9%, Gluc 5% so it is usually directly injected.It is compatible with water for injection.
Some Important Point to be memorized!
  • Possible increased risk of ventricular arrhythmias when diltiazem given with intravenous. Dantrolene manufacturer of diltiazem advises avoid concomitant
  • Hypotension, myocardial depression, and hyperkalaemia when intravenous dantrolene given with verapamil.
  • Photosensitization may occur; therefore, caution patientstotake
  • protective measures against exposureto ultraviolet light or sunlight untiltolerance is determined.
  • Exercise caution at meals onthe day of administration because difficulty swallowing and choking has been reported.
  • If no observable benefit is derived from therapy after 45 days, discontinue use.
  • For Long-term use: Safety and efficacy have not been established
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