Baclofen
Baclofen is analogue of gamma aminobutyric acid used as a muscle relaxant and antispastic. Chemically Baclofen is identified as ß-(aminomethyl)-p-chlorohydrocinnamic acid. It relaxes muscles and relieves pain and discomfort due to certain nerve disorders. Baclofen is used in the treatment of multiple sclerosis, spinal cord diseases etc. Administered orally.
Primary Characteristics
It is of Synthetic origin and belongs to Benzenepropanoic acid.
It belongs to GABA-B agonist pharmacological group on the basis of mechanism of action and also classified in Antipsychotic Agent pharmacological group. It is also classified under Muscle Relaxants .
Molecular Weight: 232 · pKa: 3.85, 9.25 · Solubility in Alcohol: 0.1 mg/ml · Non-proprietary name: Baclofen.
Pharmacokinetics
Absorption: Baclofen has an oral bioavailability is 97% (±2%).
Distribution: Baclofen has a volume of distribution is 0.81l/kg. plasma protein binding is 30%.
Elimination: it is metabolised via 15%, plasma half-life is 3-4 hr, renal excretion is 75%.
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Indications
Baclofen is primarily indicated in conditions like Hiccup due to gastric distension in palliative care, Hiccup in palliative care, Male hypersexuality, Muscle spasm in palliative care, Parkinson's disease (but not drug-induced extrapyramidal symptoms), Spasticity.
Baclofen is also indicated for secondary conditions like Hiccup, Neurogenic bladder, Refractory trigeminal neuralgia.
Contraindications
Baclofen is contraindicated in conditions like Epilepsy, Rheumatoid arthritis, Muscular spasm, Bladder sphincter hypertonia.
Dosage
Baclofen's dosage details are as follows:
| Dose | Single Dose | Frequency | Route | Instructions |
|---|---|---|---|---|
| Adult Dosage | ||||
| 17.5 mg | 17.5 mg | Every 8h | PO | Increase Dose Gradually. Max. Dose 100 mg/day |
| Paediatric Dosage (20kg) | ||||
| 4.25 mg/kg | 4.25 mg/kg | Every 8h | Oral | Gradually increase the dose |
| Neonatal Dosage (3kg) | ||||
| 3.75 mg/kg | 3.75 mg/kg | Every 8h | oral | Gradually increase the dose |
Drug Interactions
Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Side Effects
Baclofen in overdosage may give rise to further complications which include Personality disturbances , Hallucinations , Allergic reactions .
Baclofen produces potentially life-threatening effects which include Major seizures. Careful monitoring is needed with proper medical management.
The signs and symptoms that are produced after acute overdosage of Baclofen are Hypotension, Retrograde amnesia, Bradycardia, Respiratory depression, Hypotonia, Pupillary changes, Loss of reflexes, Unconsciousness, Hypothermia, Myoclonus, Major seizures.
Baclofen is known to cause more or less tolerable side effects which are usually transient. These include Blurred vision, Confusion, Diarrhea, Dizziness, Drowsiness, Dyspnea, Fatigue, Headache, Lethargy, Nausea, Sedation , VertigoX, Vomiting .
Warnings / Precautions
Available Brands
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Single Ingredient
Storage Conditions
Drug Classification
- 1.20 — Muscle relaxants and cholinesterase inhibitors