Dantrelax Actions

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Actions of Dantrelax in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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In isolated nerve-muscle preparation, Dantrelax has been shown to produce relaxation by affecting the contractile response of the muscle at a site beyond the myoneural junction. In skeletal muscle, Dantrelax dissociates the excitation-contraction coupling, probably by interfering with the release of Ca++ from the sarcoplasmic reticulum.

In the anesthetic-induced malignant hyperthermia syndrome, evidence points to an intrinsic abnormality of skeletal muscle tissue. In affected 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.

The addition of Dantrelax to the “triggered” malignant hyperthermic muscle cell may reestablish a normal level of ionized calcium in the myoplasm. Inhibition of calcium release from the sarcoplasmic reticulum by Dantrelax reestablishes the myoplasmic calcium equilibrium, increasing the percentage of bound calcium. In this way, physiologic, metabolic, and biochemical changes associated with the malignant hyperthermia crisis may be reversed or attenuated.

How should I take Dantrelax?

Dantrelax may be taken with or without food or on a full or empty stomach. However, if your doctor tells you to take the medicine a certain way, take it exactly as directed.

Take Dantrelax only as directed by your doctor. Do not take more of it and do not take it more often than your doctor ordered.

Dosing

The dose of Dantrelax will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Dantrelax. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (capsules):
    • For prevention or treatment of malignant hyperthermia:
      • Adults—Dose is based on body weight and must be determined by your doctor. The usual dose is 4 to 8 milligrams (mg) per kilogram (kg) of body weight each day, and is divided in 3 or 4 doses. Your doctor will tell you exactly when and how often to take your medicine.
      • Children—Use and dose must be determined by your doctor.
    • To relieve muscle spasms:
      • Adults—At first, 25 milligrams (mg) once a day. Your doctor may adjust your dose as needed. However, the dose is usually not more than 100 mg four times a day.
      • Children—Dose is based on body weight and must be determined by your doctor. At first, 0.5 milligram (mg) per kilogram (kg) of body weight twice a day. Your doctor may adjust the dose as needed. However, the dose is usually not more than 3 mg per kg four times a day or 100 mg four times a day.

Missed Dose

If you miss a dose of Dantrelax, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Dantrelax administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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Take this medication exactly as prescribed by your doctor. Do not take it in larger amounts or for longer than recommended. Follow the directions on your prescription label.

Your doctor may occasionally change your dose to make sure you get the best results from this medication.

Take this medicine with a full glass of water. If you take Dantrelax within 4 hours before surgery, use only enough water needed to swallow the pill.

Dantrelax can cause muscle weakness, which can affect your ability to swallow. Use caution to prevent choking while you are eating meals. Talk with your doctor if you are unable to eat because of this side effect.

Store Dantrelax at room temperature away from moisture and heat.

Dantrelax pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Mechanism of Action

In isolated nerve-muscle preparation, Dantrelax has been shown to produce relaxation by affecting the contractile response of the muscle at a site beyond the myoneural junction. In skeletal muscle, Dantrelax dissociates the excitation-contraction coupling, probably by interfering with the release of Ca++ from the sarcoplasmic reticulum.

In the anesthetic-induced malignant hyperthermia syndrome, evidence points to an intrinsic abnormality of skeletal muscle tissue. In affected 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.

The addition of Dantrelax to the “triggered” malignant hyperthermic muscle cell may reestablish a normal level of ionized calcium in the myoplasm. Inhibition of calcium release from the sarcoplasmic reticulum by Dantrelax reestablishes the myoplasmic calcium equilibrium, increasing the percentage of bound calcium. In this way, physiologic, metabolic, and biochemical changes associated with the malignant hyperthermia crisis may be reversed or attenuated.

Pharmacodynamics

The administration of intravenous Dantrelax to human volunteers was associated with loss of grip strength and weakness in the legs, as well as subjective CNS complaints.

Pharmacokinetics

The pharmacokinetics of Dantrelax was investigated in healthy volunteers following single-dose administration as an intravenous push over 60 seconds (dose range of 1 to 2.5 mg/kg), via a peripheral catheter. There was a dose-proportional increase in plasma exposure of Dantrelax and its metabolite, 5-hydroxydantrolene. Table 2 presents pharmacokinetic parameters of Dantrelax after administration of single Dantrelax dose of 2.5 mg/kg. Time to peak Dantrelax concentration was observed at the first time point collected (i.e. median Tmax is 1 minute post-dose). The mean half-life (t1/2) for Dantrelax was independent of the Dantrelax dose administered and ranged from 8.5 hours to 11.4 hours over the 1 to 2.5 mg/kg dose range.

Table 2: Pharmacokinetic Parameters for Dantrelax in Healthy Volunteers (Mean ± Standard Deviation)

1 n=15; single dose

Dantrelax dose1 Cmax

(μg/mL)

AUC0-inf

(μg*h/mL)

Half-life (hrs) Clearance

(L/hr)

Volume of distribution (L)
2.5 mg/kg 9.0 ± 4.6 77.7 ± 23.2 10.8 ± 2.2 2.5 ± 1.0 36.4 ± 11.7

When prophylactic intravenous Dantrelax infusion was administered, whole blood Dantrelax concentrations remained at a near steady state level for 3 or more hours after the infusion was completed.

Distribution

Based on assays of whole blood and plasma, slightly greater amounts of Dantrelax are associated with red blood cells than with the plasma fraction of blood. Significant amounts of Dantrelax are bound to plasma proteins, mostly albumin, and this binding is readily reversible. Binding to plasma protein is not significantly altered by diazepam, diphenylhydantoin, or phenylbutazone. Binding to plasma proteins is reduced by warfarin and clofibrate and increased by tolbutamide.

Information concerning the passage of Dantrelax across the blood-brain barrier is not available.

Metabolism

Dantrelax is found in measurable amounts in blood and urine. Its major metabolites in body fluids are 5-hydroxy Dantrelax and an acetylamino metabolite of Dantrelax. Another metabolite with an unknown structure appears related to the latter. Dantrelax may also undergo hydrolysis and subsequent oxidation forming nitrophenylfuroic acid. Following Dantrelax 2.5 mg/kg dose administration in healthy volunteers, mean peak plasma concentration for the primary metabolite, 5-hydroxydantrolene, was 640 ng/mL, and was achieved by approximately 24 hours post-dose, with an average metabolite-to-parent exposure ratio of 0.27 (AUC0-inf = 21.2 μg*h/mL). Median t1/2 for 5-hydroxydantrolene was 10 hours, the clearance was estimated to be 8.9 L/hr and the terminal phase volume of distribution was 144 L.

Dantrelax is metabolized by the liver, and it is possible that its metabolism may be enhanced by drugs known to induce hepatic microsomal enzymes. However, neither phenobarbital nor diazepam appears to affect Dantrelax metabolism.


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References

  1. DailyMed. "DANTROLENE SODIUM: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
  2. NCIt. "Dantrolene: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).

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Information checked by Dr. Sachin Kumar, MD Pharmacology

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