Baclofen Information
Baclofen (Baclofen)
Baclofen (Baclofen) Description
Baclofen (Baclofen) USP is a muscle relaxant and antispastic.
Its chemical name is 4-amino-3-(-4-chlorophenyl)-butanoic acid. The structural formula is:
Baclofen (Baclofen) USP is a white to off-white, odorless or practically odorless crystalline powder. It is slightly soluble in water, very slightly soluble in methanol and insoluble in chloroform.
Each tablet, for oral administration, contains 10 mg or 20 mg Baclofen (Baclofen) . In addition, each tablet contains the following inactive ingredients: microcrystalline cellulose, pregelatinized starch, colloidal silicon dioxide, and magnesium stearate.
Baclofen (Baclofen) Clinical Pharmacology
The precise mechanism of action of Baclofen (Baclofen) is not fully known. Baclofen (Baclofen) is capable of inhibiting both monosynaptic and polysynaptic reflexes at the spinal level, possibly by hyperpolarization of afferent terminals, although actions at supraspinal sites may also occur and contribute to its clinical effect. Although Baclofen (Baclofen) is an analog of the putative inhibitory neurotransmitter gamma-aminobutyric acid (GABA), there is no conclusive evidence that actions on GABA systems are involved in the production of its clinical effects. In studies with animals, Baclofen (Baclofen) has been shown to have general CNS depressant properties as indicated by the production of sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen (Baclofen) is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen (Baclofen) is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.
Baclofen (Baclofen) Indications And Usage
Baclofen (Baclofen) is useful for the alleviation of signs and symptoms of spasticity resulting from multiple sclerosis, particularly for the relief of flexor spasms and concomitant pain, clonus, and muscular rigidity.
Patients should have reversible spasticity so that Baclofen (Baclofen) treatment will aid in restoring residual function.
Baclofen (Baclofen) may also be of some value in patients with spinal cord injuries and other spinal cord diseases.
Baclofen (Baclofen) is not indicated in the treatment of skeletal muscle spasm resulting from rheumatic disorders.
The efficacy of Baclofen (Baclofen) in stroke, cerebral palsy, and Parkinson's disease has not been established and, therefore, it is not recommended for these conditions.
Baclofen (Baclofen) Contraindications
Hypersensitivity to Baclofen (Baclofen) .
Baclofen (Baclofen) Warnings
Baclofen (Baclofen) has been shown to increase the incidence of omphaloceles (ventral hernias) in fetuses of rats given approximately 13 times the maximum dose recommended for human use, at a dose which caused significant reductions in food intake and weight gain in dams. This abnormality was not seen in mice or rabbits.
There was also an increased incidence of incomplete sternebral ossification in fetuses of rats given approximately 13 times the maximum recommended human dose, and an increased incidence of unossified phalangeal nuclei of forelimbs and hindlimbs in fetuses of rabbits given approximately 7 times the maximum recommended human dose. In mice, no teratogenic effects were observed, although reductions in mean fetal weight with consequent delays in skeletal ossification were present when dams were given 17 and 34 times the human daily dose. There are no studies in pregnant women. Baclofen (Baclofen) should be used during pregnancy only if the benefit clearly justifies the potential risk to the fetus.
Baclofen (Baclofen) Precautions
Safe use of Baclofen (Baclofen) in children under 12 has not been established, and it is, therefore, not recommended for use in children.
Because of the possibility of sedation, patients should be cautioned regarding the operation of automobiles or other dangerous machinery, and activities made hazardous by decreased alertness. Patients should also be cautioned that the central nervous system effects of Baclofen (Baclofen) may be additive to those of alcohol and other CNS depressants.
Baclofen (Baclofen) should be used with caution where spasticity is utilized to sustain upright posture and balance in locomotion or whenever spasticity is utilized to obtain increased function.
In patients with epilepsy, the clinical state and electroencephalogram should be monitored at regular intervals, since deterioration in seizure control and EEG have been reported occasionally in patients taking Baclofen (Baclofen) .
It is not known whether this drug is excreted in human milk. As a general rule, nursing should not be undertaken while a patient is on a drug since many drugs are excreted in human milk.
A dose-related increase in incidence of ovarian cysts and a less marked increase in enlarged and/or hemorrhagic adrenal glands was observed in female rats treated chronically with Baclofen (Baclofen) .
Ovarian cysts have been found by palpation in about 4% of the multiple sclerosis patients that were treated with Baclofen (Baclofen) for up to one year. In most cases these cysts disappeared spontaneously while patients continued to receive the drug. Ovarian cysts are estimated to occur spontaneously in approximately 1% to 5% of the normal female population.
Baclofen (Baclofen) Adverse Reactions
The most common is transient drowsiness (10 to 63%). In one controlled study of 175 patients, transient drowsiness was observed in 63% of those receiving Baclofen (Baclofen) compared to 36% of those in the placebo group. Other common adverse reactions are dizziness (5 to 15%), weakness (5 to 15%) and fatigue (2 to 4%).
Others reported:
Some of the CNS and genitourinary symptoms may be related to the underlying disease rather than to the drug therapy. The following laboratory tests have been found to be abnormal in a few patients receiving Baclofen (Baclofen) : increased SGOT, elevated alkaline phosphatase, and elevation of blood sugar.
Baclofen (Baclofen) Dosage And Administration
The determination of optimal dosage requires individual titration. Start therapy at a low dosage and increase gradually until optimum effect is achieved (usually between 40 to 80 mg daily).
The following dosage schedule is suggested:
5 mg t.i.d. for 3 days 10 mg t.i.d. for 3 days 15 mg t.i.d. for 3 days 20 mg t.i.d. for 3 days
Thereafter additional increases may be necessary but the total daily dose should not exceed a maximum of 80 mg daily (20 mg q.i.d.).
The lowest dose compatible with an optimal response is recommended. If benefits are not evident after a reasonable trial period, patients should be slowly withdrawn from the drug (see ).
Baclofen (Baclofen) How Supplied
Baclofen (Baclofen) Tablets, USP are available as a white, round, flat tablet with beveled edge debossed with LCI over 1330 with score on one side and on opposite side plain, containing 10 mg Baclofen (Baclofen) USP. Available in bottles of 100 (NDC 0527-1330-01), 500 (NDC 0527-1330-05) and 1000 (NDC 0527-1330-10).
Baclofen (Baclofen) Tablets, USP are available as a white, round, flat tablet with beveled edge debossed with LCI over 1337 with score on one side and on opposite side plain, containing 20 mg Baclofen (Baclofen) USP. Available in bottles of 100 (NDC 0527-1337-01) and 500 (NDC 0527-1337-05).
PHARMACIST: Dispense in a tight container as defined in the USP. Use child-resistant closure.
Store at 20° to 25°C (68° to 77°F) (see USP Controlled Room Temperature)
Manufactured by: Philadelphia, PA 19136
Revised: 12/07
Baclofen (Baclofen) Principal Display Panel — Mg
Baclofen (Baclofen) Principal Display Panel — Mg
