Diazepam spasticity

Muscle relaxant As an adjunct for the relief of skeletal muscle spasm because of reflex spasm caused by local pathology, spasticity caused by uppermotor neuron disorders, athetosis, stiff-man syndrome, used parenterally in the treatment of tetanus (diazepam). 

An adjunct for the relief of skeletal muscle spasm caused by reflex spasm to local pathology (such as inflammation of the muscles or joints, or secondary to trauma) spasticity caused by upper motor neuron disorders athetosis stiff-man syndrome. Injectable diazepam may also be used as an adjunct in tetanus. 

Benzodiazepines also possess muscle relaxant activity. Their pharmacology is discussed in Chapter 30. Diazepam Valium) has been used for control of flexor and extensor spasms, spinal spasticity, and multiple sclerosis. The muscle relaxant effect of the benzodiazepines may be mediated by an action on the primary afferents in the spinal cord, resulting in an increased level of presynaptic inhibition of muscle tone. Polysynaptic reflexes are inhibited. The most troublesome side effect is drowsiness, which is dose dependent. Tolerance to both the therapeutic effects and the side effects develops. 

Benzodiazepines have the capacity to depress polysynaptic reflexes and have been shown to decrease decerebrate rigidity in cats and spasticity in patients with cerebral palsy. What is not clear is whether they can, in humans, relax voluntary muscles in doses that do not cause considerable central nervous system depression. Nevertheless, benzodiazepines, such as diazepam, are often prescribed for patients who have muscle spasms and pain as a result of injury. In these circumstances, the sedative and anxiolytic properties of the drug also may promote relaxation and relieve tension associated with the condition. 

Meprobamate and the benzodiazepines have frequently been used as central muscle relaxants, though evidence for general efficacy without accompanying sedation is lacking. A possible exception is diazepam, which has useful relaxant effects in skeletal muscle spasticity of central origin (see Chapter 27). 

Baclofen is at least as effective as diazepam in reducing spasticity and causes less sedation. In addition, baclofen does not reduce overall muscle strength as much as dantrolene. It is rapidly and completely absorbed after oral administration and has a plasma half-life of 3-4 hours. Dosage is started at 15 mg twice daily, increasing as tolerated to 100 mg daily. Adverse effects of this drug include drowsiness however, patients become tolerant to the sedative effect with chronic administration. Increased seizure activity has been reported in epileptic patients. Therefore, withdrawal from baclofen must be done very slowly. 

Groves L, Shellenberger MK, Davis CS Tizanidine treatment of spasticity A meta-analysis of controlled, double-blind, comparative studies with baclofen and diazepam. Adv Ther 1998 15 241. [PMID 10186943]... 

The three agents traditionally used in the treatment of spasticity are baclofen, diazepam, and dantrolene sodium (see Table 13-3, Fig. 13-2). Two newer agents, gabapentin and tizanidine, are also available for treating spasticity in various conditions. All of these agents are addressed below. 

Diazepam (Valium] Adult 2-10 mg TID or QID. Children (older than 6 mo of age] 1.0-2.5 mg TID or QID (in both adults and children, begin at lower end of dosage range and increase gradually as tolerated and needed]. Produces sedation at dosages that decrease spasticity. 

Tizanidine [Zanaflex] Adult 8 mg every 6-8 hours as needed. Children The safety and effficacy of this drug in treating spasticity in children have not been established. May reduce a in spinal cord disorders while producing fewer side effects and less generalized muscle weakness than other agents (oral baclofen, diazepam]. 

As indicated earlier, diazepam is effective in reducing spasticity as well as muscle spasms because this drug increases the inhibitory effects of GABA in the CNS. 

Uses. Diazepam is used in patients with spasticity resulting from cord lesions and is sometimes effective in patients with cerebral palsy. 

Adverse effects. Use of diazepam as an antispasticity agent is limited by the sedative effects of this medication that is, patients with spasticity who do not want a decrease in mental alertness will not tolerate diazepam therapy very well. Extended use of the drug can cause tolerance and physical dependence, and use of diazepam for the long-term treatment of spasticity should be avoided whenever possible.102... 

Adverse Effects. The most common side effects associated with tizanidine include sedation, dizziness, and dry mouth.40 As indicated, however, tizanidine tends to have a more favorable side effect profile than other alpha-2 agonists, and this drug produces less generalized weakness than oral baclofen or diazepam. Tizanidine may therefore be a better alternative to these other agents in patients who need to reduce spasticity while maintaining adequate muscle strength for ambulation, transfers, and so forth. 

Most muscle relaxants are absorbed fairly easily from the gastrointestinal tract, and the oral route is the most frequent method of drug administration. In cases of severe spasms, certain drugs such as methocarbamol and orphenadrine can be injected intramuscularly or intravenously to permit a more rapid effect. Likewise, diazepam and dantrolene can be injected to treat spasticity if the situation warrants a faster onset. As discussed earlier, continuous intrathecal baclofen administration may be used in certain patients with severe spasticity, and local injection of botulinum toxin is a possible strategy for treating focal dystonias and spasticity. Metabolism of muscle relaxants is usually accomplished by hepatic microsomal enzymes and the metabolite or intact drug is excreted through the kidneys. 

Muscular disorders Diazepam is useful in the treatment of skeletal muscle spasms such as occur in muscle strain, and in treating spasticity from degenerative disorders, such as multiple sclerosis and cerebral palsy. 

Mathew A, Mathew MC. Bedtime diazepam enhances well being in children with spastic cerebral palsy. Pediatr Rehabil 2005 8(l) 63-6. 

Spasticity results from lesions at various sites within the central nervous system and spinal cord. Drugs used include the GABA agonist baclofen, diazepam and tizanidine (an Oj-adrenoceptor agonist). 

Baclofen facilitates GABA actions by acting as a direct agonist at GABAfi receptors in the spinal cord. The drug is as effective as diazepam in musde spasticity but causes much less sedation. 

Other drugs for different spasticities include baclofen (this chapter, earlier), which is useful in multiple sclerosis and spinal cord trauma but not rheumatoid conditions the centrally acting orphenadrine (Chapter 8, Fig. 8-4) for Parkinson-like symptoms and the BZDs, particularly diazepam (considered later). 

Muscle relaxation Relaxation of skeletal muscle occurs at high doses of most sedative-hypnotics. Diazepam is effective at sedative dose levels for specific spasticity states, including cerebral palsy. Meprobamate also has some selectivity as a muscle relaxant. 

Other uses Thiopental is commonly used for the induction of anesthesia, and certain benzodiazepines (eg, diazepam, midazolam) are used as components of anesthesia protocols. Special uses include the management of seizure disorders (eg, clonazepam, phenobarbital) and muscle spasticity (diazepam). Longer-acting dmgs (eg, chlordiazepoxide, diazepam) are used in the management of withdrawal states in persons physiologically dependent on ethanol and other sedative-hypnotics. 

Cyclobenzaprine is likely to diy oropharyngeal secretions and to decrease gut motility Dantrolene has little effect on calcium release in cardiac muscle Diazepam causes sedation at most doses required to reduce muscle spasms Intrathecal use of baclofen is effective in some refractory cases of muscle spasticity... 

Schmidt et al. Comparison of dantrolene sodium and diazepam in the treatment of spasticity. / Neurol Neurosurg Psychiatry 1976 39 350-356. 

Tizanidine is in general better tolerated by patients compared with baclofen and diazepam. In a comparative review of different muscle relaxants, Chou et aL [5] reviewed 101 trials and concluded that baclofen and tizanidine are equally effective in treating patients with spasticity, though tizanidine is more often associated with dry mouth, while baclofen causes increased weakness. 

Case series Severe vomiting was reported following domperidone administration in 10 paediatric patients witix severe acquired brain injury. These patients shared spastic tetraparesis, minimal consciousness and the inability to take solids or liquids orally. They were receiving treatment with baclofen, diazepam, valproate, omeprazole and antibiotics when needed. To facilitate gastric emptying, therapeutic doses of domperidone were administered 15-20 min... 

Several drugs including mephenesin, chlorphenesin, carisoprodol, chlorzoxazone, methocarbamol, metaxalone and diazepam, have been tried or are still used on a limited scale with varying success for the relief of spasticity. In the last few years diazepam and baclofen (and for the last 2 years dantrolene sodium) have gained wider clinical application in the treatment of spastic conditions. The side effects of diazepam are discussed together with those of the other tranquillizers in this chapter only baclofen and dantrolene will be considered. 

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