Clonidine is an alpha-2 agonist that inhibits excessive afferent sensory transmission below the level of injury, decreasing spasticity. 23 In the past it was commonly used to diminish spasticity in patients with SCIs as well as to treat high blood pressure. 23 However, nowadays it is rarely used as a single agent in the treatment of spasticity because of adverse effects such as hypotension, bradycardia, and drowsiness. 24 Furthermore, some studies have shown that taking clonidine results in variable outcomes. 25 Thus, it may not be the most reliable option when treating spasticity.
Full Answer
When are antispastic agents indicated in the treatment of spasticity?
Oral antispastic agents are indicated when spasticity interferes with patients’ activities of daily living or causes pain. However, as with any medication, high doses can produce unwanted side effects of the CNS without sufficient symptom control.
Which medications are used to treat spasticity in cerebral palsy?
Oral treatment options for the control of spasticity in children include baclofen, clonidine, diazepam, dantrolene, and tizanidine. Their dosages are summarized in TABLE 1. Baclofen (Lioresal) is first-line oral therapy for the treatment of spasticity in children with cerebral palsy.
Is gabapentin or diazepam better for spinal spasticity?
Because spinal spasticity has a propensity toward flexor reflexes, diazepam is better suited for spinal spasticity than for cerebral spasticity.8However, these drugs also produce tolerance and dependence, limiting their long-term use.9,19 Gabapentin
What are benzodiazepines used to treat?
The patient may also experience light-headedness and dizziness. The benzodiazepines are used in treatment of muscle spasticity and convulsions.] 10 The primary benzodiazepine for intravenous use in conscious sedation today is:
Which drugs are used to treat spasticity?
Oral medications used to treat spasticity include:Baclofen (Lioresal®)Tizanidine (Zanaflex®)Dantrolene sodium (Dantrium®)Diazepam (Valium®)Clonazepam (Klonopin®)Gabapentin (Neurontin®)
Which of the following drugs to treat spasticity is a benzodiazepine?
Diazepam. Diazepam (Valium*), a long-acting benzodiazepine, is the oldest medication still in widespread use for the management of spasticity.
What is the best treatment for spasticity?
Casting or bracing: prevents involuntary spasms and reduces tightening of the muscles. Oral Medications: oral medications are used in combination with other therapies or medications, such as physical or occupational therapy. Oral medications are only used if symptoms interfere with daily functioning or sleep.
Does diazepam treat spasticity?
The benzodiazepine diazepam (Valium) is one of the oldest treatments for spasticity due to cerebral palsy. Benzodiazepines increase the affinity of GABA for its receptor. Studies comparing baclofen and diazepam found both agents to be equally effective in treating spasticity.
What is the best muscle relaxer for spasticity?
From a pharmacologic standpoint, if we base treatment on an upper motor neuron concern – for example, spasticity from MS or post-stroke pain, the most commonly used medications are baclofen even tizanidine – baclofen is a Gaba-b agonist whereas tizanidine is an alpha agonist – they may work at the muscle level to ...
How does baclofen treat spasticity?
Baclofen is one of the medications most commonly used to treat spasticity. Baclofen acts in the spinal cord, and improves hyperactive reflexes and excessive muscle tone.
What is the difference between dantrolene and baclofen?
Lioresal (baclofen) is a first choice treatment for muscle spasticity caused by multiple sclerosis or spinal cord injuries, but it's not recommended for other types of muscle spasms. Dantrium (dantrolene) effectively treats malignant hyperthermia. Can be used for muscle spasticity if other medications haven't worked.
Why are muscle relaxants such as diazepam prescribed for patients with multiple sclerosis?
Muscle relaxants are used to relieve muscle spasms which may result from some conditions which affect the nervous system. Conditions which may cause muscle spasms include multiple sclerosis, motor neurone disease and cerebral palsy.
Which medication is classified as an antianxiety medication but is also used to treat muscle spasms?
Flexeril (cyclobenzaprine) and Xanax (alprazolam) are used as adjuncts to rest and physical therapy for relief of muscle spasm. Xanax is mainly used as an anti-anxiety medication prescribed to treat panic attacks and anxiety disorders.
Is diazepam better than baclofen?
Baclofen (25 to 60 mg per day) and diazepam (10 to 40 mg per day) were evaluated for spasticity reduction in a double-blind, crossover study in 13 patients over a period of 19 weeks. Both drugs produced overall improvement and there was no significant difference in preference for one or other treatment.
What type of drug is baclofen?
Baclofen is in a class of medications called skeletal muscle relaxants. Baclofen acts on the spinal cord nerves and decreases the number and severity of muscle spasms caused by multiple sclerosis or spinal cord conditions. It also relieves pain and improves muscle movement.
Are baclofen and diazepam the same?
Baclofen and Valium (diazepam) are used for treating muscle spasms. Baclofen is specifically used to treat muscle clonus, rigidity, and pain caused by multiple sclerosis. Baclofen is also injected into the spinal cord to treat severe spasticity, spinal cord injuries, and other spinal cord diseases.
What is dantrolene used for?
Dantrolene is used to help relax certain muscles in your body. It relieves the spasms, cramping, and tightness of muscles caused by certain medical problems such as multiple sclerosis (MS), cerebral palsy, stroke, or injury to the spine.
Is dantrolene better than baclofen?
Dantrium (dantrolene) is not a first-choice treatment for general muscle spasms because it can damage your liver. Relaxes your muscles. Lioresal (baclofen) is a first choice treatment for muscle spasticity caused by multiple sclerosis or spinal cord injuries, but it's not recommended for other types of muscle spasms.
What is baclofen made of?
Each tablet, for oral administration, contains 10 mg or 20 mg Baclofen. In addition, each tablet contains the following inactive ingredients: colloidal silicon dioxide, microcrystalline cellulose, magnesium stearate, potato starch, povidone.
How do you treat spasticity naturally?
Natural Spasticity Management for SCIRange of Motion. One of the most important things you can do post-injury to prevent spasms is to do your daily range of motion regimen. ... Adaptive Yoga. ... CBD/THC. ... Herbs. ... Cherry Juice. ... Warm Water. ... Acupuncture.
How to treat spasticity?
Phenol concentrations ranging from 3–7% or alcohol concentrations ranging from 50–100% are used to reduce spasticity by chemical neurolysis. These high concentrations are essentially injected perineurally to irreversibly destroy the nerve causing spasticity.4,5,17This procedure is not commonly used as a first-line treatment because it is nonselective and has a variable duration of effect ranging from days to years8because of partial nerve regeneration and sprouting following the treatment.4,5This procedure is used mainly to help with gait, posture, and hygiene.44However, this is an effective treatment for patients with spasticity refractory to all other therapies5,16and should be reserved for patients with a complete loss of sensation and/or no functional movement in their lower body.3Caution must be taken because there can be potential adverse effects concerning the bladder, bowel, and sexual function.5Other adverse effects include transient flushing4and neuropathic pain.9In current practice, this therapy is starting to be replaced by Botox injections.8
What is the best treatment for spasticity?
There are a variety of treatments available for controlling spasticity. Nonmedical treatments including physical therapies, occupational therapies, and complementary and alternative medicine are effective adjuncts to mainstream oral agents and interventional therapies. While each therapy has been shown to be efficacious in treating spasticity, the treatments themselves also come with their own adverse effects. In general, oral agents are more inexpensive in the short term and easier to use, but they have unwanted systemic effects, which can outweigh the potential benefits they may provide.12,13At the same time, these systemic drugs may be better for patients with generalized spasticity.5On the other hand, interventional therapies pose the problem of procedural errors, difficulty in finding a provider who is trained to perform the procedure, and further complications.4However, it may provide greater control of spasticity with fewer systemic side effects if patients are compliant and can tolerate the procedures. Because of the possible risks and benefits of each treatment, it is important to assess a patient's medical history to determine which treatment option is best.
What is spasticity in the nervous system?
Spasticity is a velocity-dependent increase in muscle tone and uncontrolled, repetitive, involuntary contractions of skeletal muscles. Spasticity presents as upper motor neuron symptoms in patients with central nervous system pathology such as stroke, spinal cord injury, brain injury, or multiple sclerosis. As a result, a patient can have significant pain and limited mobility, which can lead to decreased quality of life and difficulty maintaining personal care. In this article we discuss mechanisms, indications, efficacy, and side effects of the most accepted current treatments. Currently available treatment options include oral medications and interventional procedures. Oral medications comprise centrally acting agents, such as baclofen, clonidine, and tizanidine, as well as anticonvulsants such as benzodiazepines and gabapentin and peripherally acting dantrolene. Interventional procedures include focal injections of botulinum toxin, phenol or alcohol, and an intrathecal baclofen pump. Surgical treatments include selective dorsal rhizotomy and neurectomy. We found that there are several treatments available with data to support their use, but many still need further research to prove their efficacy and develop optimal utilization.
How does spasticity affect a patient?
Spasticity affects a patient's independence in activities of daily living such as hygiene, dressing, self-comfort, ambulation, and sleep.10Later it may lead to significant pain, contractures, joint subluxations or dislocations, peripheral neuropathy, and pressure ulcers.11Therefore, treatment of this condition is imperative to improve quality of life and minimize medical complication. Spasticity can, conversely, be beneficial to help patients transfer, stand, ambulate, and maintain muscle bulk.
What is botox used for?
Botulinum toxin, commonly referred to as Botox (one of its trade names), is produced by the bacteria Clostridium botulinumand was originally used to treat strabismus.40It is currently the most widely used treatment for focal spasticity5,17and avoids the generalized weakness and sedation accompanying oral medications.3Botulinum works by inhibiting the release of vesicular acetylcholine from presynaptic nerve terminals at the neuromuscular junction.41There are 2 different subtypes available, A and B, which differ in their level of purification and immunogenicity.4Unlike other neurolytic drugs, the effects of Botox are reversible as the toxin begins to degrade, and effects last for 3–4 months.9A thorough knowledge of muscle anatomy is required, and the use of electromyography to localize the targeted nerve is recommended.4Botox has been shown to have better tolerance and efficacy than oral treatments42and has been gaining widespread use, especially in patients with cerebral palsy.43A major side effect is possible dissemination to other areas of the body,42which can lead to dysphagia if it is being used in the upper limbs or neck muscles.4The development of immunoresistance to the toxin can also be a potential problem.42As with all injections, this procedure is to be used with caution in patients receiving anticoagulation therapy.
Does baclofen cross the brain barrier?
The oral form of baclofen is rapidly absorbed and crosses the blood-brain barrier.4However, penetration of the blood-brain barrier is not very efficient, which explains the limited efficacy of oral baclofen in low doses (the efficacy of oral baclofen increases with higher doses). Studies using oral baclofen have reported significant improvement in flexion of the quadriceps in patients with MS when compared to a placebo (using the Ashworth scale20) and subjective improvements in general function.21,22Furthermore, one study showed the protective effects of oral baclofen on the deterioration in body musculature and metabolic profile that normally accompany spastic individuals with SCI.11While there is a breadth of studies demonstrating the effectiveness of baclofen, most studies adhere to testing the drug in the setting of a specific condition, such as MS or SCI.
Does gabapentin help with spasticity?
Gabapentin is usually given as an adjunct for spasticity treatments.24It has a structure similar to that of GABA but does not bind to those receptors.8The exact mechanism of the drug is relatively unknown, but it is thought to act at the alpha-2δ1subunit of voltage-dependent calcium channels, thus inhibiting calcium currents. Gabapentin is often prescribed when patients describe symptoms that are consistent with neuropathic pain along with spasticity.16A study by Gruenthal et al.29showed that using gabapentin alone, compared to a placebo, demonstrated a reduction in the Ashworth scale and in the spasticity Likert scale scores. However, gabapentin is not a first-line treatment for spasticity and is rarely used as a monotherapy. Adverse effects include somnolence, tremor, and nystagmus.8
Which agonists work in the spinal cord to reduce spasticity?
The centrally acting alpha 2 -agonists clonidine (Catapres) and tizanidine (Zanaflex) work in the spinal cord to reduce spasticity by hyperpolarizing motor neurons and reducing excitatory amino acid release. 15.
What is the treatment for spasticity in cerebral palsy?
Baclofen (Lioresal) is first-line oral therapy for the treatment of spasticity in children with cerebral palsy. Baclofen is a structural analog of the inhibitory neurotransmitter gamma-amino butyric acid (GABA). It acts on the GABA receptors in the central nervous system (CNS), inhibiting the release of excitatory neurotransmitters ...
What is the best treatment for spasticity?
Diazepam. The benzodiazepine diazepam ( Valium) is one of the oldest treatments for spasticity due to cerebral palsy. 14 Benzodiazepines increase the affinity of GABA for its receptor. Studies comparing baclofen and diazepam found both agents to be equally effective in treating spasticity.
What causes cerebral palsy?
The precise cause of cerebral palsy is still unknown. It results from the interaction of multiple risk factors before, during, and after birth. 4 While prematurity and congenital malformations are considered risk factors, in many cases no specific cause of cerebral palsy is identified. 5. Spasticity is the most common movement disorder ...
What are the other aspects of spasticity?
Other aspects of spasticity are decreased motor planning, loss of selective motor control, weakness, and poor endurance. 6 Other movement disorders of cerebral palsy are less common and may have extrapyramidal features such as athetosis, chorea, dystonia, and ataxia. Treatment of Spasticity. Spasticity is debilitating.
What is botulinum toxin?
Botulinum toxin is used as adjunctive therapy in the treatment of spasticity. Botulinum toxin is produced by the anaerobic bacterium Clostridium botulinum. There are seven toxin subtypes (A, B, C, D, E, F, and G); only A and B are commercially available.
Can baclofen cause spasticity?
An abrupt discontinuation of baclofen may result in a rebound increase in spasticity, rhabdomyolysis, disorientation, hallucinations, and seizures. 10,14,15. Diazepam.
How do benzodiazepines exert their effects?
Benzodiazepines exert their effects by facilitating the activity of gamma-aminobutyric acid(GABA) at various sites . Specifically, benzodiazepines bind at an allosteric site at the interface between the alpha and gamma subunits on GABA-A receptor chloride ion channels. The allosteric binding of diazepam at the GABA-A receptor leads to an increase in the frequency at which the chloride channel opens, leading to an increased conductance of chloride ions. This shift in charge leads to a hyperpolarization of the neuronal membrane and reduced excitability of the neuron. [5]
How to treat benzodiazepine overdose?
Treatment of benzodiazepine overdose involves protecting the airway, fluid resuscitation, and the use of flumazenil if indicated. Flumazenil works via competitive antagonism at the benzodiazepine receptor and can rapidly reverse coma. However, in patients with benzodiazepine tolerance, the use of flumazenil can precipitate acute withdrawal symptoms, autonomic instability, and seizures. [3]
What is diazepam used for?
It is a fast-acting, long-lasting benzodiazepine commonly used to treat anxiety disorders and alcohol detoxification, acute recurrent seizures, severe muscle spasms, and spasticity associated with neurologic disorders . In the setting of acute alcohol withdrawal, diazepam is useful for symptomatic relief of agitation, tremor, alcoholic hallucinosis, and acute delirium tremens.[1] Benzodiazepines have largely replaced barbiturates in treating anxiety and sleep disorders because of their improved safety profile, fewer side effects, and flumazenil(antagonist) availability that can reverse oversedation in cases of benzodiazepine intoxication. [2][3]
How long does diazepam last?
Diazepam is long-lasting with a duration of action of more than 12 hours. Benzodiazepines have largely replaced barbiturates in the treatment of anxiety and sleep disorders because of their improved safety profile, fewer side effects, and the availability of the antagonist flumazenil to reverse oversedation and benzodiazepine intoxication. ...
What is the interprofessional approach to diazepam?
As illustrated above, managing patients on diazepam requires an interprofessional team approach consisting of clinicians(MDs, DOs, NPs, PAs), specialists, nurses, pharmacists, and other healthcare providers. Further, prescribing physicians should be responsible for checking state and federal controlled substance databases to detect benzodiazepines use disorder, diversion, and prevent improper drug use.[33] An interprofessional team approach would achieve maximum efficacy and minimize potential adverse drug reactions for the patients requiring diazepam, which can translate to better patient outcomes. [level 5]
What are the side effects of diazepam?
Like most benzodiazepines, the adverse reactions of diazepam include CNS and respiratory depression, dependence, and benzodiazepine withdrawal syndrome. [13]
What is the RID of diazepam?
Relative infant dose (RID) is the dose received via breast milk relative to the mother’s dose. A relative dose below 10% is within an acceptable range regarded as reasonably safe in the short term.
Drugs used to treat Muscle Spasm
The following list of medications are in some way related to, or used in the treatment of this condition.
Alternative treatments for Muscle Spasm
The following products are considered to be alternative treatments or natural remedies for Muscle Spasm. Their efficacy may not have been scientifically tested to the same degree as the drugs listed in the table above. However there may be historical, cultural or anecdotal evidence linking their use to the treatment of Muscle Spasm.
Further information
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
GABA AGONISTS
GABA receptor sites are widely present in the CNS, and GABA is the third most prevalent neurotransmitter in the CNS. GABA is present in an estimated 60% to 70% of all synapses in the brain and is inhibitory on a variety of neural pathways associated with spasticity (10,29,31).
BACLOFEN
Baclofen is structurally similar to GABA and binds to presynaptic GABA-B receptors within the brainstem, dorsal horn of the spinal cord, and other CNS sites (40–44). Baclofen is a small molecule with a formula weight of 213.67 and the chemical name 4-amino-3 (p-chlorophenyl) butyric acid (C 10H12 ClNO 2 —see the chemical structure).
OTHER GABA DERIVATIVES
Gabapentin is an analog of GABA. Its chemical name is 1- (aminomethyl)cyclohexaneacetic acid. The mechanism of action of gabapentin continues to be a subject of debate. It is known for certain that gabapentin is not converted metabolically into GABA or a GABA agonist, and it is not an inhibitor of GABA uptake or degradation (109).
TIAGABINE
Tiagabine is an anticonvulsant drug that was designed to prevent GABA reuptake into neurons (84). First utilized as an add-on therapy for partial epilepsy (127), more recently it has been utilized as both an adjunctive medication and a monotherapy for complex–partial seizures and generalized tonic–clonic seizures (125,128).
VIGABATRIN
Vigabatrin was another attempt to “tailor make” an irreversible inhibitor of GABA-transaminase predominately as an antiepileptic agent (114). By inhibiting the neurotransporters of GABA and increasing the extracellular GABA, it has been demonstrated that this suppresses seizures (114,137). Vigabatrin is broadly licensed in Europe and Latin America.
TOPIRAMATE
Topiramate is another antiepileptic drug (AED) for tonic–clonic seizures by blockage of voltage-dependent sodium channels (149), an augmentation of gamma-aminobutyrate acid activity at some subtypes of the GABA-A receptors (4,150,151), and antagonism of α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)/kainite subtype of the glutamate receptor affecting Ca channels (151)..
CENTRAL ALPHA-ADRENERGIC AGENTS
The monoamines are widely distributed within the CNS. In spastic hypertonia, they appear to modulate sensory, autonomic, and motor functions through facilitation of presynaptic inhibition of spinal afferent inputs (30). The monoamines have an important role as modulators of spinal neuron excitability (157).