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Classification of Skeletal Muscle Relaxants01:28

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Skeletal muscle relaxants are a group of drugs that can reduce muscle stiffness and induce temporary paralysis to relieve pain. These agents can act centrally to reduce muscle tone or spasms in painful conditions such as multiple sclerosis (MS), amyotrophic lateral sclerosis (ALS), or spinal injuries; they are called antispasmodics or spasmolytics.
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Spasmolytic agents are drugs used to alleviate muscle spasms and spasticity. They can be categorized into different chemical groups based on their mechanisms of action. Centrally acting spasmolytics primarily affect the spinal cord, while others directly target skeletal muscle cells.
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Skeletal muscle relaxants can target the central nervous system [CNS] to reduce muscle tension or act directly at the neuromuscular junction to induce temporary paralysis. These two classes of muscle relaxants are called centrally acting muscle relaxants and peripherally acting muscle relaxants. They differ in their action, mechanism, administration route, and clinical uses.
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Centrally acting muscle relaxants reduce muscle tone and tension by interfering with the postsynaptic reflexes in the central nervous system.
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CNS stimulants, such as cocaine, amphetamines, and cannabinoids, have varying structures and mechanisms of action that lead to different therapeutic effects and side effects. Cocaine, with its molecular formula C17H21NO4, is a tropane alkaloid and a tertiary amino compound. It has two chemical forms: the hydrochloride salt and the "freebase." The former is in powder form, while the latter involves removing the hydrochloride salt to create a form that can be smoked. Cocaine exerts its...
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Cannabinoids control spasticity and tremor in a multiple sclerosis model.

D Baker1, G Pryce, J L Croxford

  • 1Department of Neurochemistry, Institute of Neurology, University College London, UK. D.Baker@ion.ucl.ac.uk

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Cannabinoid receptor agonism effectively reduced spasticity and tremor in a multiple sclerosis mouse model. This suggests the endogenous cannabinoid system plays a role in controlling these debilitating symptoms.

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Area of Science:

  • Neuroscience
  • Immunology
  • Pharmacology

Background:

  • Chronic relapsing experimental allergic encephalomyelitis (CREAE) is a model for multiple sclerosis (MS).
  • MS patients report benefits from cannabis for tremor and spasticity, but evidence is largely anecdotal.
  • Tremor and spasticity are challenging symptoms in both CREAE and MS.

Purpose of the Study:

  • To investigate the therapeutic potential of cannabinoid receptor agonism for tremor and spasticity in CREAE mice.
  • To explore the role of the endogenous cannabinoid system in controlling these symptoms.

Main Methods:

  • Administered cannabinoid receptor agonists (R(+)-WIN 55,212, delta9-tetrahydrocannabinol, methanandamide, JWH-133) to CREAE mice.
  • Utilized cannabinoid receptor antagonists (SR141716A, SR144528) to block CB1 and CB2 receptors.
  • Quantitatively assessed the amelioration of tremor and spasticity.

Main Results:

  • Cannabinoid receptor agonism significantly reduced tremor and spasticity in diseased mice.
  • Antagonism of CB1 and CB2 receptors, particularly CB1, exacerbated these symptoms.
  • These findings indicate tonic activity of the endogenous cannabinoid system in controlling tremor and spasticity.

Conclusions:

  • Cannabinoid receptor activation offers a potential therapeutic strategy for managing tremor and spasticity in MS.
  • The endogenous cannabinoid system is actively involved in regulating these neurological symptoms.
  • This study provides a basis for evaluating selective cannabinoids for MS symptom management.