Apo-Baclofen - General Information
A gamma-aminobutyric acid derivative that is a specific agonist at GABA-B receptors (receptors, GABA-B). It is used in the treatment of spasticity, especially that due to spinal cord damage. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
Pharmacology of Apo-Baclofen
Apo-Baclofen is a muscle relaxant and antispastic. Apo-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 Apo-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, Apo-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. Apo-Baclofen is rapidly and extensively absorbed and eliminated. Absorption may be dose-dependent, being reduced with increasing doses. Apo-Baclofen is excreted primarily by the kidney in unchanged form and there is relatively large intersubject variation in absorption and/or elimination.
Apo-Baclofen for patients
Baclofen may cause dizziness or drowsiness, patient should use with caution when
driving, operating or performing other dangerous activites.
Patient should avoid alcohol while taking Baclofen.
Abrupt discontinuation of baclofen can seizures or hallucinations.
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.
IDE 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 KEMSTROTM was similar to that seen with baclofen tablets.
Tablets and Injection
Hypersensitivity to baclofen.Injection
Hypersensitivity to baclofen. Baclofen injection is not recommended for intravenous, intramuscular, or epidural administration
OVERDOSAGE for Kemsto
Signs and Symptoms
Vomiting, muscular hypotonia, drowsiness, accommodation disorders, coma, respiratory depression, and seizures.
In the alert patient, empty the stomach promptly by induced emesis followed by lavage. In the obtunded patient, secure the airway with a cuffed endotracheal tube before beginning lavage (do not induce emesis). Maintain adequate respiratory exchange, do not use respiratory stimulants. It is unknown what effect hemodialysis or peritoneal dialysis has on the serum concentration of baclofen.
CONTRAINDICATIONS for Kemsto
KEMSTRO is contraindicated in patients who are hypersensitive to any component of this product.
Additional information about Apo-Baclofen
Apo-Baclofen 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
Mechanism Of Action: Apo-Baclofen is a direct agonist at GABAB receptors. The precise mechanism of action of Apo-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 Interactions: Not Available
Food Interactions: Take without regard to meals.
Generic Name: Baclofen
Synonyms: Not Available
Drug Category: Muscle Relaxants; Skeletal Muscle Relaxants; GABA Agonists
Drug Type: Small Molecule; Approved
Other Brand Names containing Baclofen: Apo-Baclofen; Baclon; Kemstro; Lioresal; Lioresal Intrathecal; Novo-Baclofen; Nu-Baclofen; Pms-Baclofen;
Absorption: Rapidly and extensively absorbed
Toxicity (Overdose): LD50=45 mg/kg (male mice, IV); LD50=78 mg/kg (male rat, IV)
Protein Binding: 30%
Half Life: 1.51 hours
Dosage Forms of Apo-Baclofen: Tablet Oral
Chemical IUPAC Name: 4-amino-3-(4-chlorophenyl)butanoic acid
Chemical Formula: C10H12ClNO2
Baclofen on Wikipedia: http://en.wikipedia.org/wiki/Baclofen
Organisms Affected: Humans and other mammals