BACLOFEN Uses, Side Effects, and More

 BACLOFEN

BRAND NAME :- Lioresal ,liofen 10mg ,25mg tab .

BACLOFEN is a commonly used muscle relaxer for the treatment of muscle spasms. It can be helpful for people with multiple sclerosis or spinal cord problems. Baclofen is available as oral tablets, granules, and liquid solutions.

PHARMACODYNAMIC:- 

Chemically, baclofen is a derivative of the neurotransmitter γ-aminobutyric acid (GABA). It is believed to work by activating (or agonizing) GABA receptors, specifically the GABAB receptors.[23] Its beneficial effects in spasticity result from its actions in the brain and spinal cord.

PHARMACOKINETICS:- 

The drug is rapidly absorbed after oral administration and is widely distributed throughout the body. Biotransformation is low: the drug is predominantly excreted unchanged by the kidneys.The half-life of baclofen is roughly 2–4 hours; it therefore needs to be administered frequently throughout the day to control spasticity appropriately.

PHARMACODYNAMIC:- 

Baclofen is an antispasmodic agent that induces muscle relaxation. It reduces the release of excitatory neurotransmitters in the pre-synaptic neurons and stimulates inhibitory neuronal signals in the post-synaptic neurons. Oral formulations of baclofen are the most commonly used form of the drug. In one cross-section study, intrathecal baclofen was more effective than oral baclofen in relieving spasticity directly at the level of the spinal cord. Baclofen has CNS depression properties and can cause sedation with tolerance, somnolence, ataxia, and respiratory and cardiovascular depression. Baclofen also mediates some antinociceptive effects and stimulates gastric acid secretion.

Baclofen exhibits anti-inflammatory and neuroprotective activities: it inhibits the release of pro-inflammatory cytokines from microglia and astrocytes, and decreases oxidative stress in rats.

MECHANISM OF ACTION:- 

The exact mechanism of action of baclofen is unclear. Baclofen is an agonist at the beta subunit of gamma-aminobutyric acid (GABA) receptors expressed on pre- and post-synaptic neurons.3 Upon binding to GABAB receptors, baclofen causes an influx of potassium into the neuron, leading to hyperpolarization of the neuronal membrane and decreased calcium influx at presynaptic nerve terminals. This results in a decreased rate of action potential threshold being reached by presynaptic neurons and reduced action potential of postsynaptic motor neurons that innervate the muscle spindles. Baclofen thereby inhibits the transmission of both mono- and polysynaptic reflexes at the spinal cord, relaxing spasticity. Baclofen may act on some voltage-gated calcium channels; however, the clinical significance of this is unclea.

USED:- 

Baclofen is used to treat muscle spasms caused by certain conditions (such as multiple sclerosis, spinal cord injury/disease). It works by helping to relax the muscles.

SIDE EFFECTS:- 

Drowsiness, mental confusion, weakness and ataxia; serum transminases may rise. Sudden withdrawal after chronic use may cause hallucinations, tachycardia and seizures. 

DOSE:- 10mg BD to 25mg TDS