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Flexeril

Cyclobenzaprine is a skeletal muscle relaxant and a Central Nervous System (CNS) Depressant. It is marketed as Flexeril (5 and 10 mg tablets). The 10 milligram tablets are available generically. more...

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Mechanism of Action

The exact mechanism of action for cyclobenzaprine is unknown. Current research appears to indicate that cyclobenzaprine acts on the locus coeruleus where it results in increased norepinephrine release, potentially through the gamma fibers which innervate and inhibit the alpha motor neurons in the vetral horn of the spinal cord. Decreased firing of the alpha motor neuron results in decreased muscular tone.

Indications

Cyclobenzaprine is typically prescribed to relieve pain and muscle spasms. Typically, muscle spasms occur in an injury to stabilize the affected body part and prevent further damage. The spasm of the muscles can actually increase the pain level. It is believed that by decreasing muscular spasm, pain is diminished. A common application would be that of a whiplash injury in a car accident.

It is also prescribed off-label as a sleep-aid.

Side Effects

Common side effects include drowsiness, dizziness, and blurred vision. Other side effects are respiratory depression and decreased functionality in various muscles.

Legality

Cyclobenzaprine is regulated in the U.S. for prescription only. Cyclobenzaprine is unscheduled, however, and it is not illegal to have cyclobenzaprine in your possesion, even without a prescription.

Abuse

Cyclobenzaprine is not widely abused, despite having an arguably high potential for abuse. As a generality, habitual drug users tend to steer clear of anti-depressants, because of the possibility of contraindications with other psychoactive drugs. Cyclobenzaprine, on the other hand, can induce moderate to severe anticholinergic effects at higher doses, as well as benzodiazepine-like sedation and often pleasurable muscle-relaxation. At even higher doses, cyclobenzaprine may cause severe ataxia, and due to excessive muscle-relaxation, and possibly disorienting side-effects such as a floating sensation or other imagined movements (usually experienced when at rest.) Side-effects such as these are directly related to the favoritism of newer, more mild antidepressant medications over tricyclic antidepressants. Although purportedly unpleasant, cyclobenzaprine is relatively benign in case of overdose, depending on it's toxicity level in the user, and also on the susceptibility of the user to possibly harmful effects of overdose. Note that the susceptibility to these potentially damaging effects are greatly increased when cyclobenzaprine is used in conjunction with other drugs, particularly Central Nervous System Depressants and other antidepressants. Use of cyclobenzaprine with a MAOI (Mono Amine Oxidase Inhibitor) will very possibly result in fatality. Use of cyclobenzaprine with an SSRI (Selective Seratonin Reuptake Inhibitor) is not recommended and could lead to unpleasant and possibly damaging interactions. No deaths have been associated with cyclobenzaprine overdose, and permanent damage is almost always related to overactivity of relaxed muscles or contraindications with other drugs.

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Useful treatments for fibromyalgia syndrome
From Journal of Family Practice, 2/1/05

* CLINICAL QUESTION

What treatment modalities are most effective for fibromyalgia syndrome?

* BOTTOM LINE

Treatments for fibromyalgia syndrome with the strongest evidence for efficacy include amitriptyline (Elavil), cyclobenzaprine (Flexeril), exercise, cognitive behavioral therapy, patient education, and multidisciplinary therapy. (Level of evidence [LOE]=1a-)

* STUDY DESIGN

Meta-analysis (other)

* SETTING

Various (meta-analysis)

* SYNOPSIS

The optimal method for treating fibromyalgia syndrome is unclear. The investigators thoroughly searched multiple sources--including Medline, EMBASE, Science Citation Index, and the Cochrane Collaboration--for trials evaluating the effectiveness of treatment for fibromyalgia syndrome. A total of 505 articles were reviewed and classified according to their level of evidence. The authors don't state whether the articles were reviewed independently and do not discuss the potential for publication bias.

Evidence was ranked as strong (positive results from a meta-analysis or consistent results from more than 1 randomized controlled trial [RCT]), moderate (positive results from 1 RCT or mostly positive results from multiple RCTs or consistently positive results from non-RCT studies), or weak (positive results from descriptive and case studies, inconsistent results from RCTs, or both).

Strong evidence for efficacy was found for treatment with amitriptyline, cyclobenzaprine, exercise, cognitive behavioral therapy, and patient education. Modest evidence for efficacy was found for tramadol (Ultram), various selective serotonin reuptake inhibitors, acupuncture, hypnotherapy, and biofeedback. Weak evidence for efficacy was found for growth hormone therapy, SAM (S-adenosyl-methionine), chiropractic and massage therapy, electrotherapy, and ultrasound. No evidence of any evaluation or effectiveness was found for steroids, nonsteroidal anti-inflammatory drugs, melatonin, benzodiazepine hypnotics, or trigger-point injections.

Goldenberg DL, Burchhardt C, Crofford L. Management of fibromyalgia syndrome. JAMA 2004; 292:2388-2395.

COPYRIGHT 2005 Dowden Health Media, Inc.
COPYRIGHT 2005 Gale Group

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