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It has been shown to cause anemia so it is contraindicated in patients with any type of anemia, as well as any patient with liver or kidney compromise.
It is metabolized via several hepatocellular cytochrome P450 (CYP450) enzyme families; however, it has not been shown to be an inducer or an inhibitor.
It is structurally related to TCAs, and it has a similar ADE profile, including sedation, constipation, urinary retention, and dry mouth. Concomitant use of cyclobenzaprine with mono-amine oxidase inhibitors (MAOIs) may increase the potential for serotonin syndrome—fever/hypertensive crisis, seizures, and death.
Therefore, this medication is contraindicated in patients receiving MAOIs and should not be used within 14 days following discontinuance of these drugs.
There were not sufficient data of good quality to determine whether metaxalone, methocarbamol, chlorzoxazone, baclofen, or dantrolene were better than placebo for this indication.
A Cochrane systematic review found that all agents were better than placebo for short-term relief of acute low back pain, and all were equally effective; however, they were associated with more adverse effects than placebo.
At this time, guidelines do not recommend chronic use of muscle relaxants for musculoskeletal pain.
Antispasmodic Agents Agents that fall into this category act at the spinal cord or supraspinal level.
It is contraindicated in patients with glaucoma, gastrointestinal obstruction, and cardiac spasm.
Carisoprodol’s pharmacologic activity is γ-aminobutyric acid (GABA)ergic, with activity at the GABAA receptor.
However, because it is metabolized to meprobamate, a sedative/hypnotic similar to barbiturates, there is concern about misuse and abuse.
The skeletal muscle relaxants are a diverse class of drugs that are used for treating painful muscle spasticity or spasms, which can substantially affect a patient’s ability to function (Table 1).
About 2 million people annually report using muscle relaxants, with about 15% being elderly.
Well-controlled clinical studies have not conclusively demonstrated whether relief of musculoskeletal pain by cyclobenzaprine, carisoprodol, chlorzoxazone, metaxalone, or methocarbamol results from skeletal muscle relaxant effects, sedative effects, or a placebo effect of the drug.