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Cyclobenzaprine

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 American Family Physician, 3/1/05 by David Slawson

Clinical Question: What treatment modalities are most effective for fibromyalgia syndrome?

Setting: Various (meta-analysis)

Study Design: Meta-analysis (other)

Synopsis: The authors searched multiple sources, including MEDLINE, EMBASE, Science Citation Index, and the Cochrane Collaboration, for trials on the efficacy of fibromyalgia syndrome therapy. A total of 505 articles were reviewed and classified according to their level of evidence. It was unclear whether the articles were reviewed independently and the potential for publication bias. was not discussed. Evidence was ranked as strong (i.e., positive results from a meta-analysis or consistent results from more than one randomized controlled trial [RCT]), moderate (i.e., positive results from one RCT or mostly positive results from multiple RCTs or consistently positive results from non-RCT studies), or weak (i.e., 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 behavior therapy, and patient education. Moderate evidence for efficacy was found for tramadol, various selective serotonin reuptake inhibitors, acupuncture, hypnotherapy, and biofeedback. Weak evidence for efficacy was found for growth hormone therapy, S-adenosyl-methionine, chiropractic and massage therapy, electrotherapy, and ultrasonography. No evidence of any evaluation or effectiveness was found for steroids, nonsteroidal anti-inflammatory drugs, melatonin, benzodiazepine hypnotics, or trigger point injections.

Bottom Line: Treatments for fibromyalgia syndrome with the strongest evidence for efficacy include amitriptyline, cyclobenzaprine, exercise, cognitive behavior therapy, patient education, and multidisciplinary therapy. (Level of Evidence: 1a-)

Study Reference: Goldenberg DL, et al. Management of fibromyalgia syndrome. JAMA November 17, 2004;292:2388-95.

Used with permission from Slawson D. Useful treatments for fibromyalgia syndrome. Accessed online December 28, 2004, at: http://www.InfoPOEMs.com.

COPYRIGHT 2005 American Academy of Family Physicians
COPYRIGHT 2005 Gale Group

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