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Statewide Pharmacy and Therapeutics Committee Medication Review: Skeletal Muscle Relaxants May 17, 2002
Commonly Used Muscle Relaxants: Generic Drug Name Brand Drug Name

Carisoprodol Soma Chlorphenesin Maloate Chlorzoxazone Paraflex/Parafon Forte DSC Cyclobenzaprine Flexeril Metaxalone Skelaxin Methocarbamol Robaxin Orphenadrine Norflex Associated Drugs used in the Treatment of Muscle Spasm and Spasticity Baclofen Lioresal Dantrolene Dantrium Diazepam Valium Tizanidine Zanaflex Purpose of Review: To review the necessity of the addition of a skeletal muscle relaxant to the State P&T Formulary. The agents currently on the Formulary include baclofen and dantrolene. These agents are not commonly used for the treatment of acute musculoskeletal pain and muscle spasm. The addition of a Formulary agent may aid in choice of prescribing of these agents as there is not an established superiority for one agent over another. Indications: Used as adjuncts to rest, physical therapy, and other measures for relief of discomfort related to acute, painful musculoskeletal conditions. Mechanism of Action/Clinical Pharmacology: The exact mechanism of action of the skeletal muscle relaxants is not known. The centrally acting skeletal muscle relaxants, unlike some of the associated agents, appear to preferentially depress polysynaptic reflexes and may influence monosynaptic reflexes at higher doses. In animal studies, these drugs seem to produce muscle relaxation through the inhibition of interneuronal activity and blocking postsynaptic neurons in the spinal cord and descending reticular formation in the brain. In man, however, the skeletal muscle relaxants do not appear to directly relax skeletal muscle. They may produce their effects through sedation, with resultant depression of neuronal activity. Efficacy and Clinical Trials: Numerous clinical trials have been conducted. Deficiencies in study design have made interpretations and comparisons across agents difficult. However, most studies have shown the skeletal muscle relaxants to be more effective than placebo in the treatment of acute painful musculoskeletal disorders and muscle spasm, while efficacy was less consistent when treating chronic disorders. When 1

0. frequent usages of these are not anticipated within our hospital system.54 4.98-2. Central nervous system adverse effects include drowsiness. Studies have indicated they may be more effective in combination with analgesics. anaphylaxis) have been reported with some agents. 2 . and can be an adjunct in the treatment of painful musculoskeletal conditions with associated muscle spasm. agitation. withdrawal symptoms may occur. Toxicity is possible upon overdose. edema. confusion. Dosage and Administration: Agents are primarily dosed orally when used for acute musculoskeletal conditions.56-2. No studies have documented superior efficacy of one skeletal muscle relaxant over another.20-0. and headache. pain relief was superior to either agent used alone.64 pricing not available Approx. dizziness.28 0. These agents are hepatically and/or renally excreted. pruritus. so caution must be used when treating patients with hepatic or renal function. Although some parenteral formulations are available. hallucinations. When the skeletal muscle relaxants were used in combination with analgesics.60 0. Drug Interactions: See table Cost: Medication Carisoprodol Chlorphenesin Chlorzoxazone Cyclobenzaprine Metaxalone Methocarbamol Orphenadrine Cost/Day of Treatment (Dollars) 1. Upon abrupt cessation with some agents. blurred vision. have tolerable side effects. the skeletal muscle relaxants were not consistently superior to simple analgesics in relieving pain. The skeletal muscle relaxants may potentiate the effects of other CNS depressants.19 0. Pharmacokinetics: See table Adverse Effects: The most commonly reported adverse effect is drowsiness.28 Conclusions: The centrally acting skeletal muscle relaxants have been shown to be efficacious in the treatment of painful musculoskeletal disorders. Gastrointestinal side effects have been reported. See table for dosing recommendations for individual agents. Patients are cautioned to avoid activities requiring mental alertness while taking these medications.2 used as monotherapy.27-0. Allergic reactions (skin rash. The skeletal muscle relaxants are generally not recommended for use in children or in pregnant or lactating women.62-6. Studies have suggested that these drugs are effective. Skeletal muscle relaxants should be used cautiously when combined with other CNS depressants and alcohol.

3 References: AHFS Drug Information. Arch Intern Med. 3 .July 9. 2001. Jackson. Robert MD. MD. Browning. MD. Journal of Pain and Symptom Management 1994. O'Malley. Waldman HJ. Volume 161(13). Centrally Acting Skeletal Muscle Relaxants and Associated Drugs. Patrick G. 9(7): 434-441. MPH. 2002.1613-1620 Drug Facts and Comparisons®. MPH. Jeffrey L. 2001.

Contraindicated in patients with acute intermittent porphyria Caution in hepatic impairment. heart block. rare hematologic adverse effects. anaphylactoid reactions and drug fever Chlorphenesin Chlorzoxazone Onset: 1 hour Duration: 34 hours Onset: 1 hour Duration: 12-24 hours 800 mg TID until desired effect. 5. very rare hypersensitivity. use only for short periods (<3 wk) 400 mg tablets 250 and 500 mg tablets May produce urine discoloration (orange or purple-red). prostatic hypertrophy.5 gram QID for first 48-72 hours.4 Medication Carisoprodol Onset/ Duration Onset: 30 min Duration: 4-6 hours Onset: 30 min Duration: not reported Adult Oral Dosage 350 mg TID or QID Available Forms 350 mg tablets Precautions/ Comments Congener of meprobamate. stenosing peptic ulcers. max 750 mg QID 10 mg TID. Anticholinergic action may exacerbate urinary retention or glaucoma. spasticity caused by upper motor neuron disorders Muscle relaxant actions occur in two proposed sites. or 750 mg Q4H. 750 mg tablets 100 mg tablets Contraindication in glaucoma. increased antichol effects may be seen when used with amantadine 4 . reported cases of hepatotoxicity Cyclobenzaprine 10 mg tablets Diazepam 2-10 mg TID or QID. hypersensitivity. 10 mg tablets Metaxalone 400 mg tablets Similar to tricyclic antidepressants Not effective for spasticity assoc with spinal cord disease or cerebral palsy Contraindicated with MAOIs or within 14 days of MAOI. contains tartrazine. Drug interactions: effect of phenothiazines may be decreased. then 1 gram QID. Caution in hepatic/renal impairment. Caution in cardiac disease. at spinal level resulting in GABA-mediated presynaptic inhibition and at supraspinal sites. Not effective for spasticity associated with cerebral palsy or spinal cord disease Adjunct for relief of skeletal muscle spasm due to reflex spasm. probably in brain stem reticular formation Use with caution in patients with hepatic or renal impairment Contraindicated in patients with known tendencies for hemolytic anemia Use injectible form cautiously in patients with seizure disorder Methocarbamol Orphenadrine citrate Duration of action: 4-6 to 12-24 hours 1. hyperthyroidism. decreased haloperidol levels may occur.5 gram TID 100 mg BID 500. pyloric/duodenal obstruction. conduction disturbances. Potential for dependence and withdrawal symptoms. may reduce to 400 mg QID or less Start at 250 mg TID or QID. some products may contain sulfite. or 1. recent MI or CHF. arrhythmias. do not exceed 60 mg QD. individualize dosage for maximum benefit Onset: 30 min.1 hour Duration: 46 hours Onset: 1 hour Duration: 45 hours 800 mg TID or QID 2.

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