Baclofen
Therapeutic Class: Centrally acting striated muscle Relaxants
Indications :
Baclofen is indicated in-
- Spasm.
- Reflex muscle contractions.
- Indirect effects of treatment with Baclofen include improved sleep patterns, improvement in bladder and sphincter function, and helps within the prevention and healing of decubitus ulcers.
- Spasticity resulting from MS.
- Spinal cord injuries and other medulla spinalis diseases.
- Muscle spasm of cerebral origin especially infantile spastic paralysis.
- Cerebrovascular accidents or neoplastic or degenerative brain disorders.
- Tension-type headache.
Description :
Baclofen may be a centrally acting striated muscle relaxant and an antispastic agent with a spinal site of action.
Pharmacology :
Baclofen is an efficient relaxant and antispastic agent with a spinal site of action. Its mode of action isn't fully understood. Baclofen inhibits both monosynaptic and polysynaptic reflexes at the spinal level by stimulating the GABAB-receptors, which inhibit the discharge of glutamate and aspartate. it's going to also act at intraspinal sites producing CNS depression. Neuromuscular transmission isn't suffering from Baclofen. Baclofen also exerts an antinociceptive effect but the clinical significance of this is often unknown.
Dosage & Administration :
Baclofen should be taken during meals with a touch liquid. Baclofen should tend in divided doses preferably 3 times daily for adults and 4 times daily for children. rock bottom dose compatible with an optimal response is suggested. If benefits aren't evident after a 6 to the eight-week test period, patients should be slowly withdrawn from the drug.
Adults: Start therapy at a low dosage and increase gradually until optimum effect is achieved (usually between 30-80mg daily). the subsequent dosage titration schedule is suggested:
- 5 mg 3 times each day for 3 days
- 10 mg 3 times each day for 3 days
- 15 mg 3 times each day for 3 days
- 20 mg 3 times each day for 3 days
Thereafter additional increases could also be necessary, but the entire daily dose should usually not exceed a maximum of 80 mg, although in hospitalized patients daily doses of 100-120 mg may occasionally be necessary.
Children: Treatment should be started at a really low dose e.g. 0.3 mg/kg per day in divided doses. The dosage should be raised cautiously at 1-2 week intervals until it's sufficient for the child's individual needs. the standard dosage range for maintenance therapy is 0.75 to 2 mg/kg weight per day. In children aged over 10 years, a maximum daily dose of two .5mg/kg weight could also be given.
Interaction :
Increased sedation may occur if Baclofen is crazy agents working on the central systema nervosum, alcohol, or synthetic opiates. the danger of respiratory depression is additionally increased.
Combined treatment with Baclofen and antihypertensives is probably going to extend the autumn in blood pressure; therefore the dosage of antihypertensive medication should be adjusted accordingly.
The concomitant administration of Baclofen and tricyclic antidepressants may potentiate the pharmacological effects of Baclofen leading to pronounced muscular hypotonia.
In patients with Parkinson's' disease receiving treatment with Baclofen and levodopa and carbidopa, there are several reports of confusion, hallucinations, headaches, nausea, and agitation.
The concurrent use of MAO inhibitors and Baclofen may end in increased CNS depressant effects. Caution is suggested and therefore the dosage of 1 or both agents should be adjusted accordingly.
Caution should be exercised when administering Baclofen and magnesium sulfate or other neuromuscular blocking agents since a synergistic effect may theoretically occur.
Contraindications :
Baclofen is contraindicated in patients with hypersensitivity to any component of this product.
Side Effects :
The most common adverse reactions related to Baclofen are transient drowsiness, daytime sedation, dizziness, weakness, and fatigue.
- Central Nervous System: Headache (<10%), insomnia (<10%), and infrequently, euphoria, excitement, depression, confusion, hallucinations, paraesthesia, nightmares, muscle pain, tinnitus, slurred speech, coordination disorder, tremor, rigidity, dystonia, ataxia, blurred vision, nystagmus, strabismus, miosis, mydriasis, diplopia, dysarthria, epileptic seizures, respiratory depression.
- Cardiovascular: Hypotension (<10%), rare instances of dyspnoea, palpitation, pain , syncope.
- Gastrointestinal: Nausea (approximately 10%), constipation (<10%) and infrequently, dry mouth, anorexia, taste disorder, abdominal pain, vomiting, diarrhea, and a positive test for occult blood in the stool.
- Genitourinary: Urinary frequency (<10%) and infrequently, enuresis, retentiveness, dysuria, impotence, inability to ejaculate, nocturia, haematuria.
- Other: Instances of rash, pruritus, ankle edema, excessive perspiration, weight gain, nasal congestion, visual disturbances, hepatic function disorders, and paradoxical increase in spasticity. Muscular hypotonia of a degree sufficient to form walking or movement difficult may occur but is typically relieved by readjusting the dosage. For this purpose, the daytime dosage could also be reduced and therefore the evening dosage increased.
Pregnancy & Lactation :
Pregnancy category B3. The safe use of Baclofen during pregnancy has not been established. Baclofen crosses the placental barrier. Baclofen should only be administered to pregnant women when within the judgment of the physician concludes that the potential benefits outweigh the possible hazards. Baclofen is excreted in breast milk however evidence so far suggests that the quantities are so small that no undesirable effects on the infant would be expected.
Precautions & Warnings :
- Lower doses (approximately 5 mg per day) should be used for patients with impaired renal function or those undergoing chronic hemodialysis.
- Patients suffering not only from spasticity but also from psychotic disorders, schizophrenia, depressive or manic disorders, or confusional states should be treated cautiously and closely monitored as exacerbations of those disorders may occur.
- In patients with epilepsy and muscle spasticity, Baclofen could also be used under appropriate supervision and as long as adequate anticonvulsive therapy is sustained. Lowering of the convulsion threshold may occur and seizures are reported after the cessation of Baclofen therapy or with overdose.
- Baclofen should be used with caution in patients with or with a history of peptic ulcers, cerebrovascular diseases, or hepatic, renal, or respiratory failure.
- Careful monitoring of respiratory and cardiovascular function is important especially in patients with cardiopulmonary disease and respiratory muscle weakness.
- During treatment with Baclofen, neurogenic disturbances affecting the emptying of the bladder may improve. However, in patients with preexisting sphincter hypertonia, acute retention of urine may occur. Baclofen should be used with caution in these circumstances.
- Baclofen has not significantly benefited patients with stroke. These patients have also shown poor tolerance to the drugs.
- Appropriate laboratory tests should be performed periodically in patients with hepatic diseases or DM to make sure that no medicine-induced changes in these underlying diseases have occurred.
Overdose :
Symptoms of a Baclofen overdose include vomiting, weakness, drowsiness, slow breathing, seizures, unusual pupil size, and coma.
Storage :
Keep below 30°C temperature, far away from light & moisture. exclude the reach of children.
Brand Names
Brand Name | Company | Strength |
| Myorel Tablet | Healthcare Pharmaceuticals Ltd. | 5mg, 10 mg |
| Bacmax Tablet | Drug International Ltd. | 5mg, 10 mg |
| Skelofen Tablet | ACME Laboratories Ltd. | 5mg, 10 mg |
| Lospan Tablet | Beximco Pharmaceuticals Ltd. | 5mg, 10 mg |
| Beclovan Tablet | Aristopharma Ltd. | 5mg, 10 mg |