Methocarbamol (injection): Difference between revisions
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|genericName=methocarbamol | |genericName=methocarbamol | ||
|aOrAn=a | |aOrAn=a | ||
|drugClass=[[central nervous system]] (CNS) [[depressant]] with [[sedative]] and [[musculoskeletal relaxant]] properties | |drugClass=[[central nervous system]] (CNS) [[[[depressant]]]] with [[[[sedative]]]] and [[musculoskeletal relaxant]] properties | ||
|indicationType=treatment | |indicationType=treatment | ||
|indication=rest, physical therapy, and can be used as an adjunct to other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions | |indication=rest, physical therapy, and can be used as an adjunct to other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions | ||
|adverseReactions=[[dizziness]], [[headache]], [[lightheadedness]], [[somnolence]] | |adverseReactions=[[[[dizziness]]]], [[[[headache]]]], [[lightheadedness]], [[[[somnolence]]]] | ||
|blackBoxWarningTitle=<span style="color:#FF0000;">ConditionName: </span> | |blackBoxWarningTitle=<span style="color:#FF0000;">ConditionName: </span> | ||
|blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i> | |blackBoxWarningBody=<i><span style="color:#FF0000;">ConditionName: </span></i> | ||
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|fdaLIADAdult=====Indications==== | |fdaLIADAdult=====Indications==== | ||
The injectable form of methocarbamol is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. The mode of action of this drug has not been clearly identified, but may be related to its sedative properties. Methocarbamol does not directly relax tense skeletal muscles in man. | The injectable form of methocarbamol is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. The mode of action of this drug has not been clearly identified, but may be related to its [[sedative]] properties. Methocarbamol does not directly relax tense skeletal muscles in man. | ||
====Dosage==== | ====Dosage==== | ||
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|fdaLIADPed=====Indications==== | |fdaLIADPed=====Indications==== | ||
* Tetanus | * [[Tetanus]] | ||
====Dosage==== | ====Dosage==== | ||
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ROBAXIN Injectable is contraindicated in patients hypersensitive to methocarbamol or to any of the injection components. | ROBAXIN Injectable is contraindicated in patients hypersensitive to methocarbamol or to any of the injection components. | ||
|warnings=Since methocarbamol may possess a general CNS depressant effect, patients receiving ROBAXIN Injectable should be cautioned about combined effects with alcohol and other CNS | |warnings=Since methocarbamol may possess a general CNS [[depressant]] effect, patients receiving ROBAXIN Injectable should be cautioned about combined effects with alcohol and other CNS [[depressant]]s. | ||
Safe use of ROBAXIN Injectable has not been established with regard to possible adverse effects upon fetal development. There have been very rare reports of fetal and congenital abnormalities following in utero exposure to methocarbamol. Therefore, ROBAXIN Injectable should not be used in women who are or may become pregnant and particularly during early pregnancy unless in the judgment of the physician the potential benefits outweigh the possible hazards. | Safe use of ROBAXIN Injectable has not been established with regard to possible adverse effects upon fetal development. There have been very rare reports of fetal and congenital abnormalities following in utero exposure to methocarbamol. Therefore, ROBAXIN Injectable should not be used in women who are or may become pregnant and particularly during early pregnancy unless in the judgment of the physician the potential benefits outweigh the possible hazards. | ||
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''Body as a Whole'' | ''Body as a Whole'' | ||
Anaphylactic reaction, angioneurotic edema, fever, headache | [[Anaphylactic reaction]], angioneurotic [[edema]], [[fever]], [[headache]] | ||
''Cardiovascular System'' | ''Cardiovascular System'' | ||
Bradycardia, flushing, hypotension, syncope, thrombophlebitis | [[Bradycardia]], [[flushing]], [[hypotension]], [[syncope]], [[thrombophlebitis]] | ||
In most cases of syncope there was spontaneous recovery. In others, epinephrine, injectable steroids, and/or injectable antihistamines were employed to hasten recovery. | In most cases of syncope there was spontaneous recovery. In others, [[epinephrine]], injectable steroids, and/or injectable [[antihistamines]] were employed to hasten recovery. | ||
''Digestive System'' | ''Digestive System'' | ||
Dyspepsia, jaundice (including cholestatic jaundice), nausea and vomiting | [[Dyspepsia]], [[jaundice]] (including [[cholestatic jaundice]]), [[nausea]] and [[vomiting]] | ||
''Hemic and Lymphatic System'' | ''Hemic and Lymphatic System'' | ||
Leukopenia | [[Leukopenia]] | ||
''Immune System'' | ''Immune System'' | ||
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''Nervous System'' | ''Nervous System'' | ||
Amnesia, confusion, diplopia, dizziness or | [[Amnesia]], [[confusion]], [[diplopia]], [[dizziness]] or [[lightheadedness]], [[drowsiness]], [[insomnia]], mild muscular incoordination, [[nystagmus]], [[sedation]], [[seizures]] (including grand mal), [[vertigo]] | ||
The onset of convulsive seizures during intravenous administration of methocarbamol has been reported in patients with seizure disorders. The psychic trauma of the procedure may have been a contributing factor. Although several observers have reported success in terminating epileptiform seizures with ROBAXIN Injectable, its administration to patients with epilepsy is not recommended. | The onset of convulsive seizures during intravenous administration of methocarbamol has been reported in patients with seizure disorders. The psychic trauma of the procedure may have been a contributing factor. Although several observers have reported success in terminating epileptiform seizures with ROBAXIN Injectable, its administration to patients with epilepsy is not recommended. | ||
''Skin and Special Senses'' | ''Skin and Special Senses'' | ||
Blurred vision, conjunctivitis, nasal congestion, metallic taste, pruritus, rash, urticaria | [[Blurred vision]], [[conjunctivitis]], [[nasal congestion]], [[metallic taste]], [[pruritus]], [[rash]], [[urticaria]] | ||
''Other'' | ''Other'' | ||
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|drugInteractions=Methocarbamol may inhibit the effect of pyridostigmine bromide. Therefore, methocarbamol should be used with caution in patients with myasthenia gravis receiving anticholinesterase agents. | |drugInteractions=Methocarbamol may inhibit the effect of pyridostigmine bromide. Therefore, methocarbamol should be used with caution in patients with myasthenia gravis receiving anticholinesterase agents. | ||
Because methocarbamol may possess a general CNS-depressant effect, patients should be cautioned about combined effects with alcohol and other CNS | Because methocarbamol may possess a general CNS-[[depressant]] effect, patients should be cautioned about combined effects with alcohol and other CNS [[depressant]]s. | ||
|FDAPregCat=C | |FDAPregCat=C | ||
|useInPregnancyFDA=Animal reproduction studies have not been conducted with methocarbamol. It is also not known whether methocarbamol can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. ROBAXIN Injectable should be given to a pregnant woman only if clearly needed. | |useInPregnancyFDA=Animal reproduction studies have not been conducted with methocarbamol. It is also not known whether methocarbamol can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. ROBAXIN Injectable should be given to a pregnant woman only if clearly needed. | ||
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|monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label. | |monitoring=There is limited information regarding <i>Monitoring</i> of {{PAGENAME}} in the drug label. | ||
|IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label. | |IVCompat=There is limited information regarding <i>IV Compatibility</i> of {{PAGENAME}} in the drug label. | ||
|overdose=Limited information is available on the acute toxicity of methocarbamol. Overdose of methocarbamol is frequently in conjunction with alcohol or other CNS | |overdose=Limited information is available on the acute toxicity of methocarbamol. Overdose of methocarbamol is frequently in conjunction with alcohol or other CNS [[depressant]]s and includes the following symptoms: nausea, drowsiness, blurred vision, hypotension, seizures, and coma. In post-marketing experience deaths have been reported with an overdose of methocarbamol alone or in the presence of other CNS [[depressant]]s, alcohol or psychotropic drugs. | ||
====Treatment==== | ====Treatment==== | ||
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<!--Mechanism of Action--> | <!--Mechanism of Action--> | ||
|mechAction=The mechanism of action of methocarbamol in humans has not been established, but may be due to general CNS depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber. | |mechAction=The mechanism of action of methocarbamol in humans has not been established, but may be due to general CNS depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber. | ||
|structure=ROBAXIN (methocarbamol injection, USP) Injectable, a carbamate derivative of guaifenesin, is a central nervous system (CNS) depressant with sedative and musculoskeletal relaxant properties. It is a sterile, pyrogen-free solution intended for intramuscular or intravenous administration. | |structure=ROBAXIN (methocarbamol injection, USP) Injectable, a carbamate derivative of guaifenesin, is a central nervous system (CNS) [[depressant]] with [[sedative]] and musculoskeletal relaxant properties. It is a sterile, pyrogen-free solution intended for intramuscular or intravenous administration. | ||
Each mL contains: methocarbamol, USP 100 mg, polyethylene glycol 300, NF 0.5 mL, Water for Injection, USP q.s. The pH is adjusted, when necessary, with hydrochloric acid and/or sodium hydroxide. The chemical name of methocarbamol is 3‑(2‑methoxyphenoxy)‑1,2-propanediol 1‑carbamate and has the empirical formula of C11H15NO5. Its molecular weight is 241.24. The structural formula is shown below: | Each mL contains: methocarbamol, USP 100 mg, polyethylene glycol 300, NF 0.5 mL, Water for Injection, USP q.s. The pH is adjusted, when necessary, with hydrochloric acid and/or sodium hydroxide. The chemical name of methocarbamol is 3‑(2‑methoxyphenoxy)‑1,2-propanediol 1‑carbamate and has the empirical formula of C11H15NO5. Its molecular weight is 241.24. The structural formula is shown below: | ||
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ROBAXIN Injectable has a pH between 3.5 and 6.0. | ROBAXIN Injectable has a pH between 3.5 and 6.0. | ||
|PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label. | |PD=There is limited information regarding <i>Pharmacodynamics</i> of {{PAGENAME}} in the drug label. | ||
|PK=In healthy volunteers, the plasma clearance of methocarbamol ranges between 0.20 and 0.80 L/h/kg, the mean plasma elimination half-life ranges between 1 and 2 hours, and the plasma protein binding ranges between 46% and 50%. | |PK=In healthy volunteers, the plasma clearance of methocarbamol ranges between 0.20 and 0.80 L/h/kg, the mean plasma elimination half-life ranges between 1 and 2 hours, and the plasma protein binding ranges between 46% and 50%. | ||
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Long-term studies to evaluate the carcinogenic potential of methocarbamol have not been performed. No studies have been conducted to assess the effect of methocarbamol on mutagenesis or its potential to impair fertility. | Long-term studies to evaluate the carcinogenic potential of methocarbamol have not been performed. No studies have been conducted to assess the effect of methocarbamol on mutagenesis or its potential to impair fertility. | ||
|clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label. | |clinicalStudies=There is limited information regarding <i>Clinical Studies</i> of {{PAGENAME}} in the drug label. | ||
|howSupplied=ROBAXIN Injectable (100 mg/mL) supplied in – 10 mL single dose vials in packages of 25 (NDC 60977-150-01). | |howSupplied=ROBAXIN Injectable (100 mg/mL) supplied in – 10 mL single dose vials in packages of 25 (NDC 60977-150-01). | ||
|storage=Store at 20°- 25°C (68°- 77°F), excursions permitted to 15°- 30°C (59°- 86°F). | |storage=Store at 20°- 25°C (68°- 77°F), excursions permitted to 15°- 30°C (59°- 86°F). | ||
|packLabel=[[File:methocarbamol injection2.png|thumb|none|400px|This image is provided by the National Library of Medicine.]] | |packLabel=[[File:methocarbamol injection2.png|thumb|none|400px|This image is provided by the National Library of Medicine.]] | ||
|fdaPatientInfo=Patients should be cautioned that methocarbamol may cause drowsiness or dizziness, which may impair their ability to operate motor vehicles or machinery. | |fdaPatientInfo=Patients should be cautioned that methocarbamol may cause drowsiness or [[dizziness]], which may impair their ability to operate motor vehicles or machinery. | ||
Because methocarbamol may possess a general CNS-depressant effect, patients should be cautioned about combined effects with alcohol and other CNS | Because methocarbamol may possess a general CNS-[[depressant]] effect, patients should be cautioned about combined effects with alcohol and other CNS [[depressant]]s. | ||
|alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication. | |alcohol=* Alcohol-{{PAGENAME}} interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication. | ||
|brandNames=*ROBAXIN ®<ref>{{Cite web | title =ROBAXIN- methocarbamol injection, solution | url = https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=1254#INV-8a66859d-61dc-4011-b76e-5f19d6e0d6c2}}</ref> | |brandNames=*ROBAXIN ®<ref>{{Cite web | title =ROBAXIN- methocarbamol injection, solution | url = https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?id=1254#INV-8a66859d-61dc-4011-b76e-5f19d6e0d6c2}}</ref> | ||
|lookAlike=* A® — B®<ref name="www.ismp.org">{{Cite web | last = | first = | title = http://www.ismp.org | url = http://www.ismp.org | publisher = | date = }}</ref> | |lookAlike=* A® — B®<ref name="www.ismp.org">{{Cite web | last = | first = | title = http://www.ismp.org | url = http://www.ismp.org | publisher = | date = }}</ref> | ||
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}} | }} | ||
<!--Pill Image--> | <!--Pill Image--> | ||
<!--Label Display Image--> | <!--Label Display Image--> | ||
<!--Category--> | <!--Category--> | ||
[[Category:Drug]] | [[Category:Drug]] | ||
Revision as of 18:20, 20 May 2015
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Shanshan Cen, M.D. [2]
Disclaimer
WikiDoc MAKES NO GUARANTEE OF VALIDITY. WikiDoc is not a professional health care provider, nor is it a suitable replacement for a licensed healthcare provider. WikiDoc is intended to be an educational tool, not a tool for any form of healthcare delivery. The educational content on WikiDoc drug pages is based upon the FDA package insert, National Library of Medicine content and practice guidelines / consensus statements. WikiDoc does not promote the administration of any medication or device that is not consistent with its labeling. Please read our full disclaimer here.
Overview
Methocarbamol (injection) is a central nervous system (CNS) [[depressant]] with [[sedative]] and musculoskeletal relaxant properties that is FDA approved for the treatment of rest, physical therapy, and can be used as an adjunct to other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. Common adverse reactions include [[dizziness]], [[headache]], lightheadedness, [[somnolence]].
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Indications
The injectable form of methocarbamol is indicated as an adjunct to rest, physical therapy, and other measures for the relief of discomfort associated with acute, painful musculoskeletal conditions. The mode of action of this drug has not been clearly identified, but may be related to its sedative properties. Methocarbamol does not directly relax tense skeletal muscles in man.
Dosage
Total adult dosage should not exceed 30 mL (3 vials) a day for more than 3 consecutive days except in the treatment of tetanus. If the condition persists, a like course may be repeated after a drug-free interval of 48 hours. Dosage and frequency of injection should be based on the severity of the condition being treated and therapeutic response noted.
For the relief of symptoms of moderate degree, one dose of 1 gram (one 10 mL vial) may be adequate. Ordinarily this injection need not be repeated, as the administration of the oral form will usually sustain the relief initiated by the injection. For the severest cases or in postoperative conditions in which oral administration is not feasible, additional doses of 1 gram may be repeated every 8 hours up to a maximum of 3 g/day for no more than 3 consecutive days.
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Methocarbamol (injection) in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Methocarbamol (injection) in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
Indications
Dosage
A minimum initial dose of 15 mg/kg or 500 mg/m2 is recommended. This dosage may be repeated every six hours, if required. The total dose should not exceed 1.8 g/m2 for 3 consecutive days. The maintenance dosage may be given by injection into tubing or by I.V. infusion with an appropriate quantity of fluid. See directions for I.V. use.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Methocarbamol (injection) in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Methocarbamol (injection) in pediatric patients.
Contraindications
ROBAXIN Injectable should not be administered to patients with known or suspected renal pathology. This caution is necessary because of the presence of polyethylene glycol 300 in the vehicle.
A much larger amount of polyethylene glycol 300 than is present in recommended doses of ROBAXIN Injectable is known to have increased pre-existing acidosis and urea retention in patients with renal impairment. Although the amount present in this preparation is well within the limits of safety, caution dictates this contraindication.
ROBAXIN Injectable is contraindicated in patients hypersensitive to methocarbamol or to any of the injection components.
Warnings
Since methocarbamol may possess a general CNS depressant effect, patients receiving ROBAXIN Injectable should be cautioned about combined effects with alcohol and other CNS depressants.
Safe use of ROBAXIN Injectable has not been established with regard to possible adverse effects upon fetal development. There have been very rare reports of fetal and congenital abnormalities following in utero exposure to methocarbamol. Therefore, ROBAXIN Injectable should not be used in women who are or may become pregnant and particularly during early pregnancy unless in the judgment of the physician the potential benefits outweigh the possible hazards.
Use in Activities Requiring Mental Alertness
Methocarbamol may impair mental and/or physical abilities required for performance of hazardous tasks, such as operating machinery or driving a motor vehicle. Patients should be cautioned about operating machinery, including automobiles, until they are reasonably certain that methocarbamol therapy does not adversely affect their ability to engage in such activities.
Use in Patients with Hypersensitivity to Latex
The vial stopper contains dry natural rubber that may cause hypersensitivity reactions when handled by or when the product is injected in persons with known or possible latex sensitivity.
Precautions
As with other agents administered either intravenously or intramuscularly, careful supervision of dose and rate of injection should be observed. Rate of injection should not exceed 3 mL per minute–i.e., one 10 mL vial in approximately three minutes. Since ROBAXIN Injectable is hypertonic, vascular extravasation must be avoided. A recumbent position will reduce the likelihood of side reactions.
Blood aspirated into the syringe does not mix with the hypertonic solution. This phenomenon occurs with many other intravenous preparations. The blood may be injected with the methocarbamol, or the injection may be stopped when the plunger reaches the blood, whichever the physician prefers.
The total dosage should not exceed 30 mL (three vials) a day for more than three consecutive days except in the treatment of tetanus.
Caution should be observed in using the injectable form in patients with suspected or known seizure disorders.
Adverse Reactions
Clinical Trials Experience
The following adverse reactions have been reported coincident with the administration of methocarbamol. Some events may have been due to an overly rapid rate of intravenous injection.
Body as a Whole Anaphylactic reaction, angioneurotic edema, fever, headache
Cardiovascular System Bradycardia, flushing, hypotension, syncope, thrombophlebitis
In most cases of syncope there was spontaneous recovery. In others, epinephrine, injectable steroids, and/or injectable antihistamines were employed to hasten recovery.
Digestive System Dyspepsia, jaundice (including cholestatic jaundice), nausea and vomiting
Hemic and Lymphatic System Leukopenia
Immune System Hypersensitivity reactions
Nervous System Amnesia, confusion, diplopia, dizziness or lightheadedness, drowsiness, insomnia, mild muscular incoordination, nystagmus, sedation, seizures (including grand mal), vertigo
The onset of convulsive seizures during intravenous administration of methocarbamol has been reported in patients with seizure disorders. The psychic trauma of the procedure may have been a contributing factor. Although several observers have reported success in terminating epileptiform seizures with ROBAXIN Injectable, its administration to patients with epilepsy is not recommended.
Skin and Special Senses Blurred vision, conjunctivitis, nasal congestion, metallic taste, pruritus, rash, urticaria
Other Pain and sloughing at the site of injection
Postmarketing Experience
There is limited information regarding Postmarketing Experience of Methocarbamol (injection) in the drug label.
Drug Interactions
Methocarbamol may inhibit the effect of pyridostigmine bromide. Therefore, methocarbamol should be used with caution in patients with myasthenia gravis receiving anticholinesterase agents.
Because methocarbamol may possess a general CNS-depressant effect, patients should be cautioned about combined effects with alcohol and other CNS depressants.
Use in Specific Populations
Pregnancy
Pregnancy Category (FDA): C Animal reproduction studies have not been conducted with methocarbamol. It is also not known whether methocarbamol can cause fetal harm when administered to a pregnant woman or can affect reproduction capacity. ROBAXIN Injectable should be given to a pregnant woman only if clearly needed.
Safe use of ROBAXIN Injectable has not been established with regard to possible adverse effects upon fetal development. There have been reports of fetal and congenital abnormalities following in utero exposure to methocarbamol. Therefore, ROBAXIN Injectable should not be used in women who are or may become pregnant and particularly during early pregnancy unless in the judgment of the physician the potential benefits outweigh the possible hazards.
Pregnancy Category (AUS): B2
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Methocarbamol (injection) in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Methocarbamol (injection) during labor and delivery.
Nursing Mothers
Methocarbamol and/or its metabolites are excreted in the milk of dogs; however, it is not known whether methocarbamol or its metabolites are excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when ROBAXIN Injectable is administered to a nursing woman.
Pediatric Use
Safety and effectiveness of ROBAXIN Injectable in pediatric patients have not been established except in tetanus.
Geriatic Use
There is no FDA guidance on the use of Methocarbamol (injection) with respect to geriatric patients.
Gender
There is no FDA guidance on the use of Methocarbamol (injection) with respect to specific gender populations.
Race
There is no FDA guidance on the use of Methocarbamol (injection) with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Methocarbamol (injection) in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Methocarbamol (injection) in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Methocarbamol (injection) in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Methocarbamol (injection) in patients who are immunocompromised.
Administration and Monitoring
Administration
- Intramuscular
- Intravenous
Monitoring
There is limited information regarding Monitoring of Methocarbamol (injection) in the drug label.
IV Compatibility
There is limited information regarding IV Compatibility of Methocarbamol (injection) in the drug label.
Overdosage
Limited information is available on the acute toxicity of methocarbamol. Overdose of methocarbamol is frequently in conjunction with alcohol or other CNS depressants and includes the following symptoms: nausea, drowsiness, blurred vision, hypotension, seizures, and coma. In post-marketing experience deaths have been reported with an overdose of methocarbamol alone or in the presence of other CNS depressants, alcohol or psychotropic drugs.
Treatment
Management of overdose includes symptomatic and supportive treatment. Supportive measures include maintenance of an adequate airway, monitoring urinary output and vital signs, and administration of intravenous fluids if necessary. The usefulness of hemodialysis in managing overdose is unknown.
Pharmacology
| |
Methocarbamol (injection)
| |
| Systematic (IUPAC) name | |
| (RS)-2-hydroxy-3-(2-methoxyphenoxy)propyl carbamate | |
| Identifiers | |
| CAS number | |
| ATC code | M03 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox |
| Mol. mass | 241.241 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | Hepatic |
| Half life | 1.14–1.24 hours[1] |
| Excretion | ? |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status |
[[Prescription drug|Template:Unicode-only]](US) OTC(Canada) |
| Routes | Oral, intravenous |
Mechanism of Action
The mechanism of action of methocarbamol in humans has not been established, but may be due to general CNS depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.
Structure
ROBAXIN (methocarbamol injection, USP) Injectable, a carbamate derivative of guaifenesin, is a central nervous system (CNS) depressant with sedative and musculoskeletal relaxant properties. It is a sterile, pyrogen-free solution intended for intramuscular or intravenous administration.
Each mL contains: methocarbamol, USP 100 mg, polyethylene glycol 300, NF 0.5 mL, Water for Injection, USP q.s. The pH is adjusted, when necessary, with hydrochloric acid and/or sodium hydroxide. The chemical name of methocarbamol is 3‑(2‑methoxyphenoxy)‑1,2-propanediol 1‑carbamate and has the empirical formula of C11H15NO5. Its molecular weight is 241.24. The structural formula is shown below:
Methocarbamol is a white powder, sparingly soluble in water and chloroform, soluble in alcohol (only with heating) and propylene glycol, and insoluble in benzene and n‑hexane.
ROBAXIN Injectable has a pH between 3.5 and 6.0.
Pharmacodynamics
There is limited information regarding Pharmacodynamics of Methocarbamol (injection) in the drug label.
Pharmacokinetics
In healthy volunteers, the plasma clearance of methocarbamol ranges between 0.20 and 0.80 L/h/kg, the mean plasma elimination half-life ranges between 1 and 2 hours, and the plasma protein binding ranges between 46% and 50%.
Methocarbamol is metabolized via dealkylation and hydroxylation. Conjugation of methocarbamol also is likely. Essentially all methocarbamol metabolites are eliminated in the urine. Small amounts of unchanged methocarbamol also are excreted in the urine.
Nonclinical Toxicology
Drug and/or Laboratory Test Interactions
Methocarbamol may cause a color interference in certain screening tests for 5‑hydroxyindoleacetic acid (5-HIAA) using nitrosonaphthol reagent and in screening tests for urinary vanillylmandelic acid (VMA) using the Gitlow method.
Carcinogenesis and Mutagenesis and Impairment of Fertility
Long-term studies to evaluate the carcinogenic potential of methocarbamol have not been performed. No studies have been conducted to assess the effect of methocarbamol on mutagenesis or its potential to impair fertility.
Clinical Studies
There is limited information regarding Clinical Studies of Methocarbamol (injection) in the drug label.
How Supplied
ROBAXIN Injectable (100 mg/mL) supplied in – 10 mL single dose vials in packages of 25 (NDC 60977-150-01).
Storage
Store at 20°- 25°C (68°- 77°F), excursions permitted to 15°- 30°C (59°- 86°F).
Images
Drug Images
{{#ask: Page Name::Methocarbamol (injection) |?Pill Name |?Drug Name |?Pill Ingred |?Pill Imprint |?Pill Dosage |?Pill Color |?Pill Shape |?Pill Size (mm) |?Pill Scoring |?NDC |?Drug Author |format=template |template=DrugPageImages |mainlabel=- |sort=Pill Name }}
Package and Label Display Panel
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Patient Counseling Information
Patients should be cautioned that methocarbamol may cause drowsiness or dizziness, which may impair their ability to operate motor vehicles or machinery.
Because methocarbamol may possess a general CNS-depressant effect, patients should be cautioned about combined effects with alcohol and other CNS depressants.
Precautions with Alcohol
- Alcohol-Methocarbamol (injection) interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
- ROBAXIN ®[2]
Look-Alike Drug Names
- A® — B®[3]
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.
- ↑ Sica DA, Comstock TJ, Davis J, Manning L, Powell R, Melikian A, Wright G. (1990). "Pharmacokinetics and protein binding of methocarbamol in renal insufficiency and normals". European Journal of Clinical Pharmacology. 39 (2): 193–4. doi:10.1007/BF00280060. PMID 2253675.
- ↑ "ROBAXIN- methocarbamol injection, solution".
- ↑ "http://www.ismp.org". External link in
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