Baclofen (Lioresal) is the parachlorophenol analogue of the naturally occurring neurotransmitter y-aminobutyric acid (GABA).
Mechanism of Action
Baclofen appears to affect the neuromuscular axis by acting directly on sensory afferents, y-motor neurons,and collateral neurons in the spinal cord to inhibit both monosynaptic and polysynaptic reflexes. The principal effect is to reduce the release of excitatory neurotrans mitters by activation of presynaptic GABAB receptors.This seems to involve a G protein and second-messenger link that either increases K+ conductance or decreases Ca++ conductance.
Absorption, Metabolism, and Excretion
Baclofen is rapidly and effectively absorbed after oral administration. It is lipophilic and able to penetrate the blood-brain barrier.Approximately 35% of the drug is excreted unchanged in the urine and feces.
Clinical Uses
Baclofen is an agent of choice for treating spinal spasticity and spasticity associated with multiple sclerosis. It is not useful for treating spasticity of supraspinal origin. Doses should be increased gradually to a maximum of 100 to 150 mg per day, divided into four doses.
Adverse Effects
Side effects are not a major problem, and they can be minimized by graduated dosage increases.They include lassitude, slight nausea, and mental disturbances (in cluding confusion, euphoria, and depression). The drowsiness is less pronounced than that produced by diazepam—an important therapeutic advantage. Hypotension has been noted, particularly following overdose.Elderly patients and patients with multiple sclerosis may require lower doses and may display increased sensitivity to the central side effects.Baclofen may increase the frequency of seizures in epileptics.
Mechanism of Action
Baclofen appears to affect the neuromuscular axis by acting directly on sensory afferents, y-motor neurons,and collateral neurons in the spinal cord to inhibit both monosynaptic and polysynaptic reflexes. The principal effect is to reduce the release of excitatory neurotrans mitters by activation of presynaptic GABAB receptors.This seems to involve a G protein and second-messenger link that either increases K+ conductance or decreases Ca++ conductance.
Absorption, Metabolism, and Excretion
Baclofen is rapidly and effectively absorbed after oral administration. It is lipophilic and able to penetrate the blood-brain barrier.Approximately 35% of the drug is excreted unchanged in the urine and feces.
Clinical Uses
Baclofen is an agent of choice for treating spinal spasticity and spasticity associated with multiple sclerosis. It is not useful for treating spasticity of supraspinal origin. Doses should be increased gradually to a maximum of 100 to 150 mg per day, divided into four doses.
Adverse Effects
Side effects are not a major problem, and they can be minimized by graduated dosage increases.They include lassitude, slight nausea, and mental disturbances (in cluding confusion, euphoria, and depression). The drowsiness is less pronounced than that produced by diazepam—an important therapeutic advantage. Hypotension has been noted, particularly following overdose.Elderly patients and patients with multiple sclerosis may require lower doses and may display increased sensitivity to the central side effects.Baclofen may increase the frequency of seizures in epileptics.
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Unknown - Friday 24 June 2011
