Parafon Forte DSC

Pronunciation

Generic Name: Chlorzoxazone
Class: Centrally Acting Skeletal Muscle Relaxants
VA Class: MS200
CAS Number: 95-25-0

Introduction

Centrally acting skeletal muscle relaxant.b

Uses for Parafon Forte DSC

Muscular Conditions

Adjunct to rest, physical therapy, analgesics, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions.a i

If pharmacologic therapy is required for acute low back pain (usually a benign and self-limiting condition105 106 108 ), an analgesic (e.g., acetaminophen, NSAIA) generally is recommended.104 105 106 108 117 Skeletal muscle relaxants may be used alone or in combination with analgesics for short-term relief; however, consider high incidence of adverse effects (e.g., CNS effects).104 106 107 108 Use skeletal muscle relaxants with caution and weigh risks against benefits.104 106 107 108

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Various skeletal muscle relaxants appear to have comparable efficacy for low back pain relief.103 104 106 108

Chlorzoxazone is ineffective in the treatment of skeletal muscle hyperactivity secondary to chronic neurologic disorders (e.g., cerebral palsy) and other dyskinesias.b

Parafon Forte DSC Dosage and Administration

Administration

Oral Administration

Administer orally.a i

Dosage

Adults

Muscular Conditions
Oral

Initially, 500 mg 3–4 times daily; if response inadequate, increase dosage to 750 mg 3–4 times daily.a i

When desired response is obtained, reduce dosage to lowest effective level.a i

Usual adult dosage: 250 mg 3–4 times daily.i

Cautions for Parafon Forte DSC

Contraindications

  • Known intolerance to chlorzoxazone or any ingredient in the formulation.a i

Warnings/Precautions

Warnings

Hepatotoxicity

Serious, possibly fatal, hepatotoxicity reported rarely; may be associated with increased serum AST, ALT, alkaline phosphatase, and bilirubin concentrations and increased sulfobromophthalein sodium (BSP) retention.100 101 102 Mechanism unknown but appears idiosyncratic and unpredictable.100 101 102

Perform liver function tests periodically in patients receiving long-term therapy.101

If elevated liver function tests or bilirubin reported or if signs and symptoms of hepatic dysfunction (e.g., fever, rash, anorexia, nausea/vomiting, fatigue, right upper quadrant pain, dark urine, or jaundice) occur, discontinue chlorzoxazone immediately.100 102 a

CNS Effects

Performance of activities requiring mental alertness or physical coordination may be impaired.a i

Concurrent use of other CNS depressants may potentiate CNS depression.a i (See Specific Drugs under Interactions.)

Sensitivity Reactions

Sensitivity reactions (e.g., urticaria, redness, petechiae, pruritus) reported rarely; angioedema and anaphylactic reactions are extremely rare.a i Use with caution in patients with allergies or with a history of allergic drug reactions.a b i

Specific Populations

Pregnancy

Category C.i

Lactation

Not known whether chlorzoxazone is distributed into milk; use with caution.b

Pediatric Use

Safety and efficacy not established.a i

Common Adverse Effects

Drowsiness, dizziness.b

Interactions for Parafon Forte DSC

Specific Drugs

Drug

Interaction

Comments

CNS depressants (e.g., alcohol, barbiturates)

Potential additive CNS depressiona i

Use concomitantly with cautiona i

Parafon Forte DSC Pharmacokinetics

Absorption

Well absorbed following oral administration,b with peak plasma concentrations usually attained within 1–2 hours.a i

Onset

Usually within 1 hour.b

Duration

3–4 hours.b

Distribution

Extent

In dogs, found in plasma and fat; also present in liver, muscle, brain, and kidneys.b

Not known whether chlorzoxazone crosses the placenta or is distributed into milk.b

Elimination

Metabolism

Rapidly metabolized in the liver to 6-hydroxychlorzoxazone, an inactive metabolite.b

Elimination Route

Excreted principally in urine as a conjugated glucuronide; <1 % excreted as unchanged drug.a i

Half-life

66 minutes.b

Stability

Storage

Oral

Tablets

15–30°C.a i

Actions

  • CNS depressant with sedative and skeletal muscle relaxant effects.b

  • Inhibits multisynaptic reflex arcs at the level of the spinal cord and subcortical areas of the brain; results in reduction of skeletal muscle spasm with relief of pain and increased mobility of involved muscles.a i

Advice to Patients

  • Importance of informing clinician if any early signs or symptoms of possible liver dysfunction (e.g., fatigue, anorexia, nausea and/or vomiting, fever, rash, jaundice, dark urine, right upper quadrant pain) occur.100 102

  • Potential to impair mental alertness or physical coordination, especially with concomitant use of alcohol or other CNS depressants; use caution when driving or operating machinery.a i

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs and dietary or herbal supplements, as well as concomitant illnesses.a i

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.a i

  • Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Chlorzoxazone

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Tablets

250 mg*

Chlorzoxazone Tablets

500 mg*

Chlorzoxazone Tablets

Parafon Forte DSC Caplets (scored)

Ortho-McNeil

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Chlorzoxazone 500MG Tablets (WATSON LABS): 90/$17.99 or 180/$24.98

Parafon Forte DSC 500MG Tablets (MCNEIL): 30/$92.99 or 90/$244.97

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions November 19, 2012. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

100. McNeil Pharmaceutical. Parafon Forte DSC (chlorzoxazone) prescribing information (dated 1994 Dec 8). In: Physicians’ desk reference. 48th ed. Montvale, NJ: Medical Economics Company Inc; 1996:1581.

101. Powers BJ, Cattau EL Jr, Zimmerman HJ. Chlorzoxazone hepatotoxic reactions. Arch Intern Med. 1986; 146:1183-6. [IDIS 217157] [PubMed 3521519]

102. McNeil Pharmaceutical. Paraflex (chlorzoxazone) prescribing information (dated 1994 Dec 8). In: Physicians’ desk reference. 50th ed. Montvale, NJ: Medical Economics Company Inc; 1996:1580-1.

103. See S, Ginzburg R. Skeletal muscle relaxants. Pharmacotherapy. 2008; 28:207-13. [PubMed 18225966]

104. van Tulder MW, Touray T, Furlan AD et al. Muscle relaxants for non-specific low back pain. Cochrane Database Syst Rev. 2003; :CD004252. [PubMed 12804507]

105. Roelofs PD, Deyo RA, Koes BW et al. Non-steroidal anti-inflammatory drugs for low back pain. Cochrane Database Syst Rev. 2008; :CD000396. [PubMed 18253976]

106. Chou R, Qaseem A, Snow V et al. Diagnosis and treatment of low back pain: a joint clinical practice guideline from the American College of Physicians and the American Pain Society. Ann Intern Med. 2007; 147:478-91. [PubMed 17909209]

107. Institute for Clinical Systems Improvement. Health care guideline: adult acute and subacute low back pain. 15th ed. Bloomington, MN; 2012 Jan. From the ICSI website

108. Toth PP, Urtis J. Commonly used muscle relaxant therapies for acute low back pain: a review of carisoprodol, cyclobenzaprine hydrochloride, and metaxalone. Clin Ther. 2004; 26:1355-67. [PubMed 15530999]

117. Boothby LA, Doering PL, Hatton RC. Carisoprodol: a marginally effective skeletal muscle relaxant with serious abuse potential. Hosp Pharm. 2003; 38:337-45.

a. Ortho-McNeil. Parafon Forte DSC caplets prescribing information. Raritan, NJ; 2000 Aug.

b. AHFS drug information 2006. McEvoy GK, ed. Chloroxazone. Bethesda, MD: American Society of Health-System Pharmacists; 2006:[1385-6.].

i. Amide Pharmaceutical, Inc. Chlorzoxazone tablets prescribing information. Little Falls, NJ: 2002 Apr.

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