Spasticity, treatment

Ronan S, Gold JT Nonoperative management of spasticity in children. Childs Nerv Syst 2007 23 943 [PMID 17646995] Verrotti A et al Pharmacotherapy of spasticity in children with cerebral palsy. Pediatr Neurol 2006 34 1. [PMID 16376270] Ward AB Spasticity treatment with botulinum toxins. J Neural Transm 2008 115 607. [PMID 18389166]... 

For hookworms, treatment is continued for three days. In roundworms, muscle tissue is stimulated continuously, resulting in spastic paralysis. The dmg was introduced in veterinary medicine in 1966 and then appHed to clinical medicine three years later. 

Esters of diphenylacetic acids with derivatives of ethanol-amine show mainly the antispasmodic component of the atropine complex of biologic activities. As such they find use in treatment of the resolution of various spastic conditions such as, for example, gastrointestinal spasms. The prototype in this series, adiphenine (47), is obtained by treatment of diphenyl acetyl chloride with diethylaminoethanol. A somewhat more complex basic side chain is accessible by an interesting rearrangement. Reductive amination of furfural (42) results in reduction of the heterocyclic ring as well and formation of the aminomethyltetrahydro-furan (43). Treatment of this ether with hydrogen bromide in acetic acid leads to the hydroxypiperidine (45), possibly by the intermediacy of a carbonium ion such as 44. Acylation of the alcohol with diphenylacetyl chloride gives piperidolate (46). ... 

Currently, baclofen is the only clinically used GAB Ab receptor agonist. It is used as a muscle relaxant for treatment of spasticity in spinal injury and multiple sclerosis. The cloning of GABAb receptors has renewed the interest in the search for more selective diugs and novel therapeutic indications. 

Peripheral vasodilating drugs are chiefly used in the treatment of peripheral vascular diseases, such as arteriosclerosis obliterans, Raynaud s phenomenon, and spastic peripheral vascular disorders. Short-term use is rarely beneficial or permanent. Improvement, if it occurs, takes place gradually during weeks of therapy. 

The enantiomerically pure 3-arylglutaric ester are precursors for the synthesis of (—)-paroxetine [10], a selective serotonin reuptake inhibitor used in the treatment of depression, obsessive compulsive disorder, and panic, and (i )-Baclofen [11], a GABAb receptor agonist, which is used cHnically in the treatment of spasticity (Chart 5.1). 

MS patients develop many symptoms that require treatment. The symptoms most unique to MS are fatigue and spasticity ... 

After 3 years of treatment, CN has had one additional relapse, but otherwise is doing fairly well. At her routine clinic appointment, she describes some difficulty walking due to leg spasticity and urinary incontinence episodes that occur about twice a week. 

What treatment options are available for spasticity, and which would you choose ... 

Zajicek J, Fox P, Sanders H, Wright D, Vickery J, Nunn A and Thompson A (2003). Cannabinoids for the treatment of spasticity and other symptoms related to multiple sclerosis (CAMS study) Multicentre randomised placebo-controlled trial. Lancet, 362, 1517-1526. 

Other phenol-containing products are used as chemical peels to remove skin lesions, and in the treatment of chronic pain or spasticity. These uses have occasionally been associated with adverse outcomes, like cardiac arrhythmias, that have been seen in both adults and children. 

Petro DJ, Ellenberger C Jr. (1981). Treatment of human spasticity with delta 9-tetrahydrocannabinol. J Clin Pharmacol. 21(8-9 suppi) 413S-16S. 

Tablets Used as an anticholinergic CNS depressant in the symptomatic treatment of postencephalitic parkinsonism and paralysis agitans in spastic states and locally as a substitute for atropine in ophthalmology.

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). 

The efficacy as a treatment for spasticity of cerebral origin is not established. Unlabeled uses ... 

Spasticity Cyclobenzaprine is not effective in the treatment of spasticity associated with cerebral or spinal cord disease, or in children with cerebral palsy. 

Oral Active hepatic disease, such as hepatitis and cirrhosis where spasticity is used to sustain upright posture and balance in locomotion or to obtain or maintain increased function treatment of skeletal muscle spasm resulting from rheumatic disorders. 

All smooth muscle activity which is physiologically under a strong parasympathetic influence is effectively inhibited by atropine, for example in the gastrointestinal, genitourinary and respiratory tract. Parasympatholytics are very useful drugs in the treatment of spastic conditions (colic) in these regions. 

Baclofen is a GABA agonist at GABA B receptors and it has a presynaptic inhibitory function by reducing calcium influx. Its indication is increased extensor tone and clonus. Intrathecal administration may control severe spasticity pain. It is used for the treatment of spastic movement, especially in instances of spinal cord injury, spastic diplegia, multiple sclerosis and amyotrophic lateral sclerosis. Its central nervous system effects include drowsiness, somnolence and seizure activity in epileptic patients. 

Pyrantel is a dmg of first choice for the treatment of a number of round-, thread- and hookworm infestations. However, it has no activity against whipworm. Its mechanism of action is based on triggering the release of acetylcholine in helminths causing a depolarizing neuromuscular blockade that leads to spastic paralysis. 

Botulinum toxin is used clinically in the treatment of blepharospasm, writer s cramp, spasticities of various origins, and rigidity due to extrapyramidal disorders. It is also used to treat gustatory sweating and cosmetically to decrease facial wrinkles. Botulinum toxin A Botox, Oculinum) injected intramuscularly produces functional denervation that lasts about 3 months. Clinical benefit is seen within 1 to 3 days. Adverse effects range from diplopia and irritation with blepharospasm to muscle weakness with dystonias. 

Muscle relaxants have some value for relief of spastic muscle disorders, that is, a state of increased muscle tone that results from an imbalance between central and spinal control of muscle tone. Spasticity is the result of a general release from supraspinal control and is characterized by heightened excitability of a- and y-motor systems and the appearance of primitive spinal cord reflexes. Treatment is difficult, since relief often can be achieved only at the price of increased muscle weakness. 

P. Jobin, et al. Efficacy, safety and tolerability of an orally administered cannabis extract in the treatment of spasticity in patients with multiple sclerosis a randomized, double-blind, placebo-controlled, crossover study. 

Luo, J., J. H. Yin, H. Z. Wu, and Q. Wei. Extract from Fructus cannabis activating calcineurin improved learning and memory in mice with chemical drug-induced dysmnesia. Acta Pharmacol Sin 2003 24(11) 1137-1142. Degenhardt, L., W. Hall, and M. Lynskey. Exploring the association between cannabis use and depression. Addiction 2003 98(11) 1493-1504. Zajicek, J., P. Pox, H. Sanders, et al. Cannabinoids for treatment of spasticity and other symptoms related to multiple sclerosis (CAMS study) multicentre randomised placebo-controlled trial. Lancet 2003 362(9395) 1517-1526. 

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