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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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Inappropriate prescribing for older patients
From American Family Physician, 7/1/05 by Karl E. Miller

Less than 15 percent of the U.S. population is older than 65 years, yet this age group accounts for nearly one third of prescription drug use. Older patients also tend to have multiple chronic diseases, requiring them to take several drugs simultaneously. The risk of adverse events related to medication use increases among older patients because of age-related changes in metabolism and excretion of drugs. In 1991, criteria were published to determine the appropriateness of medications used by nursing home residents. These criteria were revised recently to include 28 medications or classes of medications considered inappropriate for use in older patients. Curtis and associates used these criteria to determine the extent of inappropriate outpatient prescribing for older patients.

The study design was a retrospective cohort analysis of outpatient prescription claims collected from the database of a large national pharmaceutical management company, which involved participants from all 50 states. Patients were included if they were 65 years or older at the start of the data collection period and had filed at least one prescription claim within the one-year study period. The authors limited their analysis to the 18 medications that the consensus panel recommended avoiding in older patients at any dosage or frequency. The main outcome measure was the number of patients taking one or more of the 18 medications. The secondary outcome measure was the number of patients taking two or more of the medications.

The data reviewed were from 1999 and identified 765,423 patients who met the inclusion criteria. Twenty-one percent (n = 162,370) filled a prescription for one or more of the medications. The most common prescription drugs that should be avoided in this age group include amitriptyline (Elavil) and doxepin (Sinequan; see the accompanying table). Of the patients who filled multiple prescriptions from this medication group, 16 percent received two prescriptions, and 4 percent received three or more. Psychotropic and neuromuscular drugs were the most commonly prescribed medication classes.

The authors concluded that, in 1999, more than one out of five older patients filled prescriptions for medications that should be avoided in this age group. Clinical and laboratory studies need to be performed to improve the quality of patient-specific alerts.

Curtis LH, et al. Inappropriate prescribing for elderly Americans in a large outpatient population. Arch Intern Med August 9/23, 2004;164:1621-5.

EDITOR'S NOTE: The issue of inappropriate prescription drug use by older patients has been identified for years in various publications, including two studies that were published 10 years ago. In a recent editorial, Steel (1) writes that although these and other studies concerning this issue have been published, "little or nothing" has been done to solve this problem. Various solutions include the development of computerized systems that could identify inappropriate prescriptions written for older patients. According to Steel, (1) if the outcome were this negative in any other setting, there would be a significant public reaction. The bottom line is that physicians and other health care professionals who see older patients and write prescriptions need to be aware of inappropriate medications and should avoid prescribing them to older patients.--K.E.M.

REFERENCE

(1.) Steel K. The time to act is now. Arch Intern Med 2004;164:1603-4.

COPYRIGHT 2005 American Academy of Family Physicians
COPYRIGHT 2005 Gale Group

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