Lioresal Information
Lioresal (Baclofen)
Lioresal (Baclofen) Description
Lioresal (Baclofen) , baclofen USP, is a muscle relaxant and antispastic, available as 10-mg and 20-mg tablets for oral administration. Its chemical name is 4-amino-3-(4-chlorophenyl)- butanoic acid, and its structural formula is
Baclofen USP is a white to off-white, odorless or practically odorless crystalline powder, with a molecular weight of 213.66. It is slightly soluble in water, very slightly soluble in methanol, and insoluble in chloroform.
Lioresal (Baclofen) Actions
The precise mechanism of action of Lioresal (Baclofen) is not fully known. Lioresal (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 Lioresal (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, Lioresal (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. Lioresal (Baclofen) is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Lioresal (Baclofen) is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.
Lioresal (Baclofen) Indications
Lioresal (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 Lioresal (Baclofen) treatment will aid in restoring residual function.
Lioresal (Baclofen) may also be of some value in patients with spinal cord injuries and other spinal cord diseases.
Lioresal (Baclofen) is not indicated in the treatment of skeletal muscle spasm resulting from rheumatic disorders.
The efficacy of Lioresal (Baclofen) in stroke, cerebral palsy, and Parkinson’s disease has not been established and, therefore, it is not recommended for these conditions.
Lioresal (Baclofen) Contraindications
Hypersensitivity to baclofen.
Lioresal (Baclofen) Precautions
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 Lioresal (Baclofen) may be additive to those of alcohol and other CNS depressants.
Lioresal (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 Lioresal (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 Lioresal (Baclofen) .
Ovarian cysts have been found by palpation in about 4% of the multiple sclerosis patients that were treated with Lioresal (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.
Lioresal (Baclofen) Pediatric Use
Safety and effectiveness in pediatric patients below the age of 12 years have not been established.
Lioresal (Baclofen) Adverse Reactions
The most common is transient drowsiness (10%-63%). In one controlled study of 175 patients, transient drowsiness was observed in 63% of those receiving Lioresal (Baclofen) compared to 36% of those in the placebo group. Other common adverse reactions are dizziness (5%-15%), weakness (5%-15%) and fatigue (2%-4%). Others reported:
Instances of rash, pruritus, ankle edema, excessive perspiration, weight gain, nasal congestion. Some of the CNS and genitourinary symptoms may be related to the underlying disease rather than to drug therapy.
The following laboratory tests have been found to be abnormal in a few patients receiving Lioresal (Baclofen) : increased SGOT, elevated alkaline phosphatase, and elevation of blood sugar.
Lioresal (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 40-80 mg daily).
The following dosage titration 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 WARNINGS
Lioresal (Baclofen) How Supplied
Tablets 10 mg – oval, white, scored (imprinted Lioresal (Baclofen) on one side and 10 twice on the scored side)
Bottles of 100………………………………………………….NDC 0028-0023-01
Unit Dose (blister pack)
Box of 100 (strips of 10)………………………………………NDC 0028-0023-61
Tablets 20 mg – capsule - shaped, white, scored (imprinted Lioresal (Baclofen) on one side and 20 twice on the scored side)
Bottles of 100………………………………………………….NDC 0028-0033-01
Unit Dose (blister pack)
Box of 100 (strips of 10)………………………………………NDC 0028-0033-61
Do not store above 30ºC (86ºF). Dispense in tight container (USP).
667794 C98-22 (Rev. 4/98)
Novartis Pharmaceuticals Corporation
East Hanover, New Jersey 07936
©1998 Novartis
