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Methocarbamol


General


Pronunciation

(meth oh KAR ba mole)


Brand Names: U.S.

  • Robaxin
  • Robaxin-750

Indications


Use: Labeled Indications

Adjunctive treatment of muscle spasm associated with acute painful musculoskeletal conditions (eg, tetanus)


Contraindications


Hypersensitivity to methocarbamol or any component of the formulation; renal impairment (injection formulation)


Dosing and Administration


Dosing: Adult

Muscle spasm:

Oral: 1.5 g 4 times/day for 2-3 days (up to 8 g/day may be given in severe conditions), then decrease to 4-4.5 g/day in 3-6 divided doses

IM, IV: Initial: 1 g; may repeat every 8 hours if oral administration not possible; maximum dose: 3 g/day for no more than 3 consecutive days. If condition persists, may repeat course of therapy after a drug-free interval of 48 hours.

Tetanus: IV: Initial dose: 1-2 g by direct IV injection, which may be followed by an additional 1-2 g by infusion (maximum initial dose: 3 g total); may repeat initial dose every 6 hours until NG tube or oral therapy possible; total oral daily dose of up to 24 g may be needed; injection should not be used for more than 3 consecutive days


Dosing: Pediatric

Tetanus (recommended only for use in tetanus): IV: 15 mg/kg/dose or 500 mg/m2/dose, may repeat every 6 hours if needed; maximum dose: 1.8 g/m2/day for 3 days only

Muscle spasm: Oral: Children ≥16 years: Refer to adult dosing.


Dosing: Renal Impairment

No dosage adjustment provided in manufacturer 's labeling. However, administration of the parenteral formulation is contraindicated in patients with renal dysfunction due to the presence of polyethylene glycol.


Dosing: Hepatic Impairment

No dosage adjustment provided in manufacturer 's labeling. However, elimination may be reduced in patients with cirrhosis.


Reconstitution

Solution for injection: May administer undiluted or diluted in D5W or NS (1 vial/ ≤250 mL diluent).


Administration

Solution for injection:

IM: A maximum of 5 mL can be administered into each gluteal region.

IV: Maximum rate: 3 mL/minute; may be administered undiluted or diluted. Monitor closely for extravasation. Administer IV while in recumbent position. Maintain position for at least 10-15 minutes following infusion.

Tablet: May be crushed and mixed with food or liquid if needed.


Storage

Solution for injection: Prior to dilution, store at controlled room temperature of 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F); excursions permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F).

Tablet: Store at controlled room temperature of 20 ‚ °C to 25 ‚ °C (68 ‚ °F to 77 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Injection:

Robaxin: 1000 mg/10 mL (10 mL) [contains polyethylene glycol 300]

Generic: 1000 mg/10 mL (10 mL)

Solution, Injection [preservative free]:

Generic: 1000 mg/10 mL (10 mL)

Tablet, Oral:

Robaxin: 500 mg [scored; contains fd&c yellow #6 (sunset yellow), saccharin sodium]

Robaxin-750: 750 mg [contains fd&c yellow #10 (quinoline yellow), fd&c yellow #6 (sunset yellow), saccharin sodium]

Generic: 500 mg, 750 mg


Drug Interactions

Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Monitor therapy

Azelastine (Nasal): CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal). Avoid combination

Blonanserin: CNS Depressants may enhance the CNS depressant effect of Blonanserin. Consider therapy modification

Brimonidine (Topical): May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Buprenorphine: CNS Depressants may enhance the CNS depressant effect of Buprenorphine. Management: Consider reduced doses of other CNS depressants, and avoiding such drugs in patients at high risk of buprenorphine overuse/self-injection. Initiate buprenorphine patches (Butrans brand) at 5 mcg/hr in adults when used with other CNS depressants. Consider therapy modification

Cannabis: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Monitor therapy

Dimethindene: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Doxylamine: May enhance the CNS depressant effect of CNS Depressants. Management: The manufacturer of Diclegis (doxylamine/pyridoxine), intended for use in pregnancy, specifically states that use with other CNS depressants is not recommended. Monitor therapy

Dronabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Droperidol: May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (e.g., opioids, barbiturates) with concomitant use. Consider therapy modification

Eperisone: May enhance the adverse/toxic effect of Methocarbamol. Monitor therapy

Flunitrazepam: CNS Depressants may enhance the CNS depressant effect of Flunitrazepam. Consider therapy modification

HYDROcodone: CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Consider starting with a 20% to 30% lower hydrocodone dose when using together with any other CNS depressant. Dose reductions in the other CNS depressant may also be warranted. Consider therapy modification

HydrOXYzine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Kava Kava: May enhance the adverse/toxic effect of CNS Depressants. Monitor therapy

Magnesium Sulfate: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Methotrimeprazine: CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established. Consider therapy modification

MetyroSINE: CNS Depressants may enhance the sedative effect of MetyroSINE. Monitor therapy

Minocycline: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Mirtazapine: CNS Depressants may enhance the CNS depressant effect of Mirtazapine. Monitor therapy

Nabilone: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Orphenadrine: CNS Depressants may enhance the CNS depressant effect of Orphenadrine. Avoid combination

OxyCODONE: CNS Depressants may enhance the CNS depressant effect of OxyCODONE. Management: When oxycodone is combined with another CNS depressant, a dose reduction of one or both agents should be considered. The extended release oxycodone starting dose should be reduced 50% to 67% when initiated in patients already receiving CNS depressants. Consider therapy modification

Paraldehyde: CNS Depressants may enhance the CNS depressant effect of Paraldehyde. Avoid combination

Perampanel: May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination. Consider therapy modification

Piribedil [INT]: CNS Depressants may enhance the CNS depressant effect of Piribedil [INT]. Monitor therapy

Pramipexole: CNS Depressants may enhance the sedative effect of Pramipexole. Monitor therapy

Pyridostigmine: Methocarbamol may diminish the therapeutic effect of Pyridostigmine. Monitor therapy

ROPINIRole: CNS Depressants may enhance the sedative effect of ROPINIRole. Monitor therapy

Rotigotine: CNS Depressants may enhance the sedative effect of Rotigotine. Monitor therapy

Rufinamide: May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced. Monitor therapy

Selective Serotonin Reuptake Inhibitors: CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced. Monitor therapy

Sodium Oxybate: May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated. Consider therapy modification

Suvorexant: CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended. Consider therapy modification

Tapentadol: May enhance the CNS depressant effect of CNS Depressants. Management: Start tapentadol at a dose of one-third to one-half of the normal dose if being initiated in a patient who is taking another drug with CNS depressant effects. Monitor closely for evidence of excessive CNS depression. Consider therapy modification

Tetrahydrocannabinol: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Thalidomide: CNS Depressants may enhance the CNS depressant effect of Thalidomide. Avoid combination

Trimeprazine: May enhance the CNS depressant effect of CNS Depressants. Monitor therapy

Zolpidem: CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol. Consider therapy modification


Monitoring Parameters

Monitor closely for extravasation (IV administration).


Lab Test Interferences


Test Interactions

May cause color interference in certain screening tests for 5-HIAA using nitrosonaphthol reagent and in screening tests for urinary VMA using the Gitlow method.


Adverse Reactions


Frequency not defined.

Cardiovascular: Bradycardia, flushing, hypotension, syncope, thrombophlebitis

Central nervous system: Amnesia, ataxia (mild), confusion, dizziness, drowsiness, headache, insomnia, metallic taste, sedation, seizure, vertigo

Dermatologic: Pruritus, skin rash, urticaria

Gastrointestinal: Dyspepsia, nausea, vomiting

Hematologic & oncologic: Leukopenia

Hepatic: Jaundice

Hypersensitivity: Angioedema, hypersensitivity reaction (including anaphylaxis)

Local: Pain at injection site

Ophthalmic: Blurred vision, conjunctivitis, diplopia, nystagmus

Respiratory: Nasal congestion

Miscellaneous: Fever


Warnings/Precautions


Special Populations: Renal Function Impairment

Cl is decreased approximately 40% in patients with severe renal impairment.


Special Populations: Hepatic Function Impairment

Cl is decreased approximately 70%; t1/2 is prolonged ~ 3-fold in cirrhosis patients.


Warnings/Precautions

Concerns related to adverse effects:

- CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

Disease-related concerns:

- Hepatic impairment: Plasma protein binding and clearance are decreased and the half-life is increased in patients with hepatic impairment.

- Renal impairment: Use of IV formulation is contraindicated.

- Seizure disorder: Use injection with caution in patients with a history of seizure disorder.

Concurrent drug therapy issues:

- Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.

Special populations:

- Pediatric: IV formulation: Recommended only for the treatment of tetanus in pediatric patients.

Dosage form specific issues:

- Injection: Contraindicated in renal impairment. Contains polyethylene glycol. Rate of injection should not exceed 3 mL/minute; solution is hypertonic; avoid extravasation. Vial stopper contains latex.


Pregnancy Risk Factor

C


Pregnancy Considerations

Animal reproduction studies have not been conducted. The manufacturer notes that fetal and congenital abnormalities have been rarely reported following in utero exposure. Use during pregnancy only if clearly needed.


Actions


Pharmacology

Causes skeletal muscle relaxation by general CNS depression


Metabolism

Hepatic via dealkylation and hydroxylation


Excretion

Urine (primarily as metabolites); Clearance: Adults: 0.2 to 0.8 L/hour/kg


Onset of Action

Muscle relaxation: Oral: ~30 minutes


Time to Peak

Serum: Oral: 1 to 2 hours


Half-Life Elimination

1 to 2 hours


Protein Binding

46% to 50%


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience nausea, vomiting, fatigue, headache, insomnia, rhinitis, metallic taste, or injection site pain or irritation. Have patient report immediately to prescriber severe loss of strength and energy, jaundice, seizures, severe dizziness, passing out, bradycardia, chills, pharyngitis, memory impairment, confusion, vision changes, or involuntary eye movements (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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