Lioresal: profile and news

Eyesight, toxin connection 12 Dec 2005
...been tried, some of which include Artane (trihexyphenidyl), Cogentin (benztropine), Valium (diazepam), Klonapin (clonazepam), Lioresal (baclofen), Tegretol ... - Inland Valley Daily Bulletin,

XenoPort trials potential new digestive disorder treatment Oct 28, 2005
XP19986 is designed to overcome the deficiencies of baclofen, a generic drug approved for the treatment of spasticity and marketed by Novartis as Lioresal. ... - Pharmaceutical Business Review

Tourette Syndrome Jul 19, 2005
These medications may have serious side effects, so researchers are studying baclofen (Lioresal) and botulinum toxin type A (Botox) used together, as well as ... - rarediseases.about.com <**results**>

Updated ACG Guidelines for Diagnosis and Treatment of GERD Jun 26, 2005
Available promotility agents (eg, tegaserod [Zelnorm], baclofen [Lioresal] ) may be useful in select patients with GERD, particularly as an adjunctive acid ... - RedNova.com,

Psychiatric Times February 2005 Vol. XXII Issue 2 Feb 28, 2005
Some promising GABA-ergic medications include baclofen (Lioresal) and topiramate (Topamax). Baclofen is a GABA-B agonist that is used as a muscle relaxant. ... - Psychiatric Times,

Other information

Indication
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

Pharmacology
Baclofen is a muscle relaxant and antispastic. 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. Although 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 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 is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.

Mechanism Of Action
Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Baclofen is not fully known. It 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.

Drug Category
Muscle Relaxants; Skeletal Muscle Relaxants; GABA Agonists; ATC:M03BX01

Brand Names/Synonyms
Apo-Baclofen; Ba 34647; Baclofen; Baclon; C 34647ba; Kemstro; Lioresal; Lioresal Intrathecal; Novo-Baclofen; Nu-Baclofen; Pms-Baclofen

Dosage Forms
TABLET; INTRATHECAL INJECTION;

Absorption
Rapidly and extensively absorbed

Interactions
-->Interactions for Baclofen:
Injection

There is inadequate systematic experience with the use of baclofen injection in combination with other medications to predict specific drug-drug interactions. Interactions attributed to the combined use of baclofen injection and epidural morphine include hypotension and dyspnea.

SIDE EFFECTS (KEMSTRO)

The most common adverse reaction during treatment with baclofen is transient drowsiness (10-63%).

In one controlled study of 175 patients, transient drowsiness was observed in 63% of those receiving baclofen tablets 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:

Neuropsychiatric: Confusion (1-11%), headache (4-8%), insomnia (2-7%); and, rarely, euphoria, excitement, depression, hallucinations, paresthesia, muscle pain, tinnitus, slurred speech, coordination disorder, tremor, rigidity, dystonia, ataxia, blurred vision, nystagmus, strabismus, miosis, mydriasis, diplopia, dysarthria, epileptic seizure.

Cardiovascular: Hypotension (0-9%). Rare instances of dyspnea, palpitation, chest pain, syncope.

Gastrointestinal: Nausea (4-12%), constipation (2-6%); and, rarely, dry mouth, anorexia, taste disorder, abdominal pain, vomiting, diarrhea, and positive test for occult blood in stool.

Genitourinary: Urinary frequency (2-6%); and, rarely, enuresis, urinary retention, dysuria, impotence, inability to ejaculate, nocturia, hematuria.

Other: 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 baclofen: increased SGOT, elevated alkaline phosphatase, and elevation of blood sugar.

The adverse experience profile seen with KEMSTRO^TM was similar to that seen with baclofen tablets.

Chemical IUPAC Name
4-amino-3-(4-chlorophenyl)-butanoic acid

Chemical Formula
C10H12ClNO2

Half Life
1.51 hours

Drug Type
Approved Drug

# Accession No
APRD00551

CAS Registry Number
1134-47-0