Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0026838 (spasticity)
 6,471 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Dantrolene sodium or dantrolene1 is 1([5-(nitrophenyl)furfurylidend] amino) hydantoin sodium hydrate. It is indicated for use in chronic disorders characterised by skeletal muscle spasticity, such as spinal cord injury, stroke, cerebral palsy and multiple sclerosis. Dantrolene is believed to act directly on the contractile mechanism of skeletal muscle to decrease the force of contraction in the absence of any demonstrated effects on neural pathways, on the neuromuscular junction, or on the excitable properties of the muscle fibre membranes. Controlled trials have demonstrated that dantrolene is superior to placebo in adults or children with spasticity from various causes, as evidenced by clinical assessments of disability and daily activities, and by muscle and reflex responses to mechanical and electrical stimulation. It is somewhat less effective in patients with multiple sclerosis than in those with spasticity from other causes. There has been a general clinical impression in controlled trials that dantrolene caused less sedation than would have been expected from therapeutically comparable doses of diazepam. In 2 controlled trials, there was no significant difference between dantrolene and diazepam in terms of reductions in spasticity, clonus, and hyperreflexia, but side-effects such as drowsiness and inco-ordination occurred significantly more frequently on diazepam. Long-term studies have indicated continuing benefit for patients taking dantrolene, though the incidence of side-effects has often been high and there has been a suggestion of exacerbation of seizures in children with cerebral palsy. Dantrolene may be of value in the medical treatment of spasm of the external urethral sphincter due to neurological and non-neurological disease, and animal studies suggest a potential use in the management of malignant hyperpyrexia. Chemical evidence of liver dysfunction may occur in 0.7 to 1% of patients on long-term treatment with dantrolene, with symptomatic hepatitis in 0.35 to 0.5% and fatal hepatitis in 0.1 to 0.2%. The drug commonly causes transient drowsiness, dizziness, weakness, general malaise, fatigue and diarrhoea at the start of therapy. Muscle weakness may be the principal limiting side-effect in ambulant patients, particularly in those with multiple sclerosis, and therapy could be hazardous in patients with pre-existing bulbar or respiratory weakness. The dosage of dantrolene has been fixed in most controlled trials, though long-term studies have indicated the need for individualisation of dosage. The initial dose is usually 25mg once daily, increasing to 25mg two, three or four times daily, and then by increments of 25mg up to as high as 100mg two, three or four times daily. The lowest dose compatible with optimal response is recommended.
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PMID:Dantrolene sodium: a review of its pharmacological properties and therapeutic efficacy in spasticity. 31 89

In 19 patients with multiple sclerosis and 1 with subacute sclerosing panencephalitis the mean increase in muscle tonus was found to be 3.1 (range 1--4 according to Burke-Ashwort). In 10 controls with multiple sclerosis the mean spasticity was 2.4. Dantrium was given in doses up to 800 mg for 14--16 days and it caused a greater reduction of spasticity than placebo (p less than 0.05). In 12 patients (60%) varying degrees of muscle tonus reduction was observed. In 11 patients the efect of Dantrium was compared with that of other drugs (Clonazepam, Tetradiazepam, Carisoprodol and Lyoresal). In 6 cases Dantrium was a more effective drug than other muscle relaxants and in 5 cases no difference was observed or other drugs were superior to Dantrium.
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PMID:[Dantrium in the treatment of increased muscle tonus in patients with multiple sclerosis]. 32 Apr 94

Dantrolene sodium is a muscle relaxant used in the treatment of spasticity. It has been shown to interfere with calcium release from the sarcoplasmic reticulum and thus to inhibit excitation--contraction coupling. The effect of dantrolene sodium on the twitch tension of the tibialis anterior muscle of the rat was measured after 2 mg/kg i.v. or 25 mg/kg orally. Plasma concentrations were estimated at maximum twitch depression and during recovery from the block. In a separate series of experiments the half-life of labelled dantrolene sodium was measured in blood plasma, skeletal muscle and heart muscle of rats. Dantrolene sodium 2 mg/kg i.v. gave a maximal block of approximately 47%, the mean dantrolene sodium concentration was then 5.8 microgram/ml. A half-life for distribution of 1.1 min and an elimination half-life of 31 min after intravenous administration were observed, elimination rate constants in skeletal and heart muscle were comparable. Recovery from the block went much slower, the half-time of the process being approximately 80 min. Dantrolene sodium 25 mg/kg orally gave a maximal block of approximately 38% at a mean plasma concentration of 3.6 microgram/ml after 14 min. The recovery was again very slow. These experiments demonstrated that dantrolene sodium acts according to a two-compartment pharmacokinetic model. There was a discrepancy between duration of effect and plasma concentration of dantrolene sodium in the rat. This suggests that the receptor for dantrolene sodium is not located in the central compartment.
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PMID:The effect of dantrolene sodium on rat skeletal muscle in relation to the plasma concentration. 42 31

Dantrium and Valium were compared in 22 children manifesting various degrees of spasticity. Treatment brought definite improvement in spasticity and in activities of daily living in 20 of the 22 patients. The two-part double-blind study showed that Dantrium was most effective in nine and Valium in seven cases. In four cases the drugs appeared to be equally beneficial. The combination of Dantrium and Valium appeared to be more effective in eight patients than either medication along, the greatest effect being seen in the upper extremities and about the hip joints. Patients on placebo showed no significant change. Side effects of lethargy and drowsiness on the combination were not bothersome after a short period of acclimation. The results indicate that the spasticity of cerebral palsy can be relieved significantly, and that the combination of peripherally and centrally acting agents is more beneficial than either medication alone.
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PMID:Medical treatment for spasticity in children with cerebral palsy. 79 60

Forty patients, whose ages varied from 4 to 65 years, presenting skeletal muscle spascitiy as sequel of cerebral palsy, spinovertebral trauma and cerebral vascular diseases were treated with Dantrium (dantrolene sodium), a drug muscle relaxing. Laboratory data included: electromiography, chronaximetry, EEG and blood and urine tests. Clinical followup revealed subjective improvement in the patients and also objective decrease of spasticity in a satisfactory number. Patients who had improvement with this therapy also had no beneficial results with other drugs.
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PMID:[Sodium dantrolene (dantrium) in the treatment of neurogenic muscular spasm]. 101 26

Dantrolene sodium has been given to 45 patients suffering from dyskinetic syndromes: 33 were suffering from spastic syndromes, either secondary to cerebral lesions at birth, or to other cerebral lesions, or to cord lesions; 9 were affected by infantile dystonic syndromes; 1 by dystonia muscolorum deformans and the last 2 patients were suffering from parkinsonism. The best dosage schedule was individual and ranged from 50 mg to 300 mg a day. In this range, the majority of the spastic patients showed reduction of spasticity, unrelated with the site of pathology: a slight one in 12 patients, a moderate one in 9 and a marked one in 2. On the contrary, slight improvement has been noticed in only two of the patients suffering from dystonic syndromes. In no case side effects has been noticed. In all patients who underwent slight or moderate improvement only, we tried to obtain better results on spasticity by growing the dosage schedules; but we have always noticed side effects, that is weakness or drowsiness and, sometimes, urinary uncontinence. Moreover 2 patients showed evidence of transitory metabolic side effects. Therefore our experience shows that dantrolene sodium is an useful drug into the therapy of spasticity, even if often a slight of moderate improvement only is achieved. Slow increase in dosage schedule, repeated laboratory controls and alternate periods of treatment and suspended treatment should be observed.
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PMID:[Clinical study of dantrolene sodium in the treatment of spastic and dystonic syndromes]. 102 44

Dantrolene sodium (Dantrium) is a skeletal muscle relaxant, unique in that it acts on the muscle itself. It should be considered for use in patients with skeletal muscle spasticity who are in a stable neurological state. After careful adjustment of the dose, a substantial number of such patients will experience one or more of the following benefits: (1) a reduction in pain, (2) an increased ability to make use of residual motor function, (3) a reduction in the level of nursing care required, (4) an increased ability to utilize devices, and (5) an increased ability to participate in rehabilitation. The drug should not be used when reduced spasticity will decrease functional ability. The adverse effects generally are transient; some are the result of central nervous system depression.
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PMID:Evaluation of a muscle relaxant: dantrolene sodium (Dantrium). 108 67

The effect of a new peripherally acting muscle relaxant drug Dantrium, on spasticity tested on 11 hemiplegic patients. The effect was evaluated both with regular clinical examination and with electromyographic technique. The latter concerned a quantitative analysis of the patients' voluntary control of fine neuromuscular activity both with and without the drug. The results indicated that spasticity was initially markedly reduced in the majority of the patients without, however, meaningfully increasing the daily-living functions of the patients. After a few months, the medication could be discontinued without any immediate increase in the spasticity. No severe side-effects were noted. In some cases, the medication had to be discontinued due to marked tiredness. Electromyographically, it was found that the ability of the patients to control fine neuromuscular activity with the paretic muscles was increased significantly with Dantrium, indicating that the reduction of the spasticity increased the ability for fine control of the muscles.
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PMID:The effect of dantrium on spasticity of hemiplegic patients. 113 Jan 70

The effects of dantrolene sodium (Dantrium) were studied in 23 patients with hemiplegic spasticity, 13 of whom were younger than 50, and 10 older than 50. The dosage of dantrolene ranged from 100 mg per day initially to 600 mg per day maximally. The drug was most effective in reducing or abolishing clonus and somewhat less efficacious in decreasing the resistance to stretch and the tendon reflexes. Functionally, gait was improved and the patients found it easier to take care of their personal needs. In general, motor performance was improved. The observation that patients in the 50+ age group responded less well remains unexplained. Dantrolene sodium is a valuable tool in the management of spasticity due to hemiplegia.
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PMID:Effect of dantrolene sodium on spasticity associated with hemiplegia. 114 24

The effect of a new, peripherally acting muscle relaxant drug (Dantrium) on spasticity was tested on 6 patients with spinal cord injuries. The effect was evaluated both by regular clinical examination and with an electromyographic technique. The latter concerned a quantitative analysis of the patients' ability to voluntarily control fine neuromuscular activity both with and without the drug. The results indicated that the spasticity was initially markedly reduced in all patients; in one case so markedly that the stability of the trunk was lost. Electromyographically it was found that the ability of the patients to relax the muscles was increased with Dantrium.
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PMID:The effect of Dantrium on spasticity in spinal cord injuries. 116


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