Methocarbamol - Methocarbamol Tablets tablet, Coated prescribing information
INDICATIONS AND USAGE
Methocarbamol tablets, USP are 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 methocarbamol has not been clearly identified, but may be related to its sedative properties. Methocarbamol does not directly relax tense skeletal muscles in man.
DOSAGE & ADMINISTRATION
Methocarbamol Tablets, USP 500 mg – Adults: Initial dosage: 3 tablets 4 times daily Maintenance dosage: 2 tablets 4 times daily Methocarbamol Tablets, USP 750 mg – Adults: Initial dosage: 2 tablets 4 times daily Maintenance dosage: 1 tablet every 4 hours or 2 tablets three times daily
Six grams a day are recommended for the first 48 to 72 hours of treatment. (For severe conditions 8 grams a day may be administered). Thereafter, the dosage can usually be reduced to approximately 4 grams a day.
CONTRAINDICATIONS
Methocarbamol tablets are contraindicated in patients hypersensitive to methocarbamol or to any of the tablet components.
ADVERSE REACTIONS
Adverse reactions reported coincident with the administration of methocarbamol include:
| Body as a whole: | Anaphylactic reaction, angioneurotic edema, fever, headache |
| Cardiovascular system: | Bradycardia, flushing, hypotension, syncope, thrombophlebitis |
| 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 |
| Skin and special senses: | Blurred vision, conjunctivitis, nasal congestion, metallic taste, pruritus, rash, Urticaria |
To report SUSPECTED ADVERSE REACTIONS, contact Granules USA, Inc. at 1-877-770-3183 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch
Drug Interactions
See WARNINGS and PRECAUTIONS for interaction with CNS drugs and alcohol.
Methocarbamol may inhibit the effect of pyridostigmine bromide. Therefore, methocarbamol should be used with caution in patients with myasthenia gravis receiving anticholinesterase agents.
DESCRIPTION
Methocarbamol tablet, USP, a carbamate derivative of guaifenesin, is a central nervous system (CNS) depressant with sedative and musculoskeletal relaxant properties.
The chemical name of methocarbamol is 1,2-Propanediol,3-(2-methoxyphenoxy)-,1-Carbamate,(±)-.(or) (±)-3-(o-Methoxyphenoxy)-1,2-Propanediol 1-carbamate and has the empirical formula C 11 H 15 NO 5 . Its molecular weight is 241.24g/mol. The structural formula is shown below.
Methocarbamol is a white powder, sparingly soluble in water and in chloroform, soluble in alcohol (only with heating), insoluble in benzene and in n-hexane.
Methocarbamol tablets, USP are available as 500 mg and 750 mg tablets for oral administration.
Methocarbamol tablets, USP 500 mg are light orange colored, round shaped film coated tablets debossed with "G" above the score line on one side and "500" on other side.
Methocarbamol tablets, USP 750 mg are light orange colored, caplet shaped film coated tablets debossed with "G" on one side and "750" on other side.
Methocarbamol tablets, USP 500 mg and 750 mg contain the following inactive ingredients: colloidal silicon dioxide, maize starch, povidone, sodium lauryl sulfate, sodium starch glycolate, and stearic acid.
The tabets are coated with Aquarius Prime which contains FD&C yellow 6, hydroxypropylcellulose, hypromellose, polysorbate 80, propylene glycol, and titanium dioxide
CLINICAL PHARMACOLOGY
The mechanism of action of methocarbamol in humans has not been established, but may be due to general central nervous system (CNS) depression. It has no direct action on the contractile mechanism of striated muscle, the motor end plate or the nerve fiber.
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. Special Populations Elderly The mean (± SD) elimination half-life of methocarbamol in elderly healthy volunteers (mean (± SD) age, 69 (± 4) years) was slightly prolonged compared to a younger (mean (± SD) age, 53.3 (± 8.8) years), healthy population (1.5 (± 0.4) hours versus 1.1 (± 0.27) hours, respectively). The fraction of bound methocarbamol was slightly decreased in the elderly versus younger volunteers (41 to 43% versus 46 to 50%, respectively).
Renally impaired The clearance of methocarbamol in 8 renally-impaired patients on maintenance hemodialysis was reduced about 40% compared to 17 normal subjects, although the mean (± SD) elimination half-life in these two groups was similar: 1.2 (± 0.6) versus 1.1 (±0.3) hours, respectively.
Hepatically impaired In 8 patients with cirrhosis secondary to alcohol abuse, the mean total clearance of methocarbamol was reduced approximately 70% compared to that obtained in 8 age- and weight-matched normal subjects. The mean (± SD) elimination half-life in the cirrhotic patients and the normal subjects was 3.38 (± 1.62) hours and 1.11 (± 0.27) hours, respectively. The percent of methocarbamol bound to plasma proteins was decreased to approximately 40 to 45% compared to 46 to 50% in the normal subjects.
HOW SUPPLIED
Methocarbamol tablets, USP 500 mg are light orange colored, roundshaped film coated tablets debossed with "G" above the score line on one side and "500" on other side.
They are supplied as follows
Bottles of 24 tablets NDC 62207-754-41
Bottles of 100 tablets NDC 62207-754-43
Bottles of 500 tablets NDC 62207-754-47
Bottles of 1000 tablets NDC 62207-754-49
Methocarbamol tablets, USP 750 mg are light orange colored, caplet shaped film coated tablets debossed with "G" on one side and"750" on other side.
Bottles of 24 tablets NDC 62207-770-41
Bottles of 100 tablets NDC 62207-770-43
Bottles of 500 tablets NDC 62207-770-47
Bottles of 1000 tablets NDC 62207-770-49
Store between 20ºC and 25ºC (68ºF and 77º F)
[see USP Controlled Room Temperature].
Dispense in tight container.
Manufactured for:
Granules USA, Inc.
Parsippany, NJ 07054
Toll-free: 1-877-770-3183
Manufactured by:
Granules India Limited
Hyderabad-500 081
Made in India
Issued: January 2017
