| Baclofen Pharmacology | |
| Baclofen | |
| About Baclofen | |
| Derivative of GABA ,Chlorophenyl derivative, Skeletal muscle relaxant,antispastic agent and in trigeminal
neuralgia. |
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| Mechanism of Action of Baclofen | |
| It inhibits both monosynaptic and polysynaptic reflexes at the spinal level by stimulating the GABA-B receptors, which inhibits the release of glutamate and aspartate. It may also act at intraspinal sites producing CNS
depression. Baclofen also exerts an antinoceptive effect |
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| Pharmacokinets of Baclofen | |
| Absorption- Rapidly and completely absorbed after oral administration
Distribution- 30% bound to the plasma proteins. Crosses the blood-brain barrier Metabolism- It is metabolized in the liver by deamination to ?- (p-chlorophenyl)-gamma-hydroxybutyric acid which is pharmacologically inactive. Excretion- Excreted through urine and feces |
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| Onset of Action for Baclofen | |
| 1 to 3 hour after administration | |
| Duration of Action for Baclofen | |
| 8 hours | |
| Half Life of Baclofen | |
| The elimination half-life is 3 to4 hours in plasma and about 5 hours in CSF | |
| Side Effects of Baclofen | |
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| Contra-indications of Baclofen | |
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| Special Precautions while taking Baclofen | |
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| Pregnancy Related Information | |
| Use with caution | |
| Old Age Related Information | |
| Use with caution | |
| Breast Feeding Related Information | |
| Use with caution. | |
| Children Related Information | |
| Use with caution | |
| Indications for Baclofen | |
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| Interactions for Baclofen | |
| N/A | |
| Typical Dosage for Baclofen | |
| Oral- Adults-
Initial dose-15 mg/day Maintenance dose – 30-75 mg/day in divided doses. Children- 0.75-2 mg/kg/day in divided doses |
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| Schedule of Baclofen | |
| N/A | |
| Storage Requirements for Baclofen | |
| Store below 30?C. Protect from heat, light, and moisture. | |
| Effects of Missed Dosage of Baclofen | |
| Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue
the regular schedule. Do not double the dose. |
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| Effects of Overdose of Baclofen | |
| Empty the stomach promptly by induced emesis followed by gastric lavage. Administer charcoal and if necessary
saline laxatives to reduce the further absorption of drugs |
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