|Active substance||Baclofen (C10H12ClNO2)|
|Manufacturing by||Sun Pharma|
|Strength||10mg / 25mg|
|Form release||Blister 10 tab|
|Shipping time||7 – 18 days (Depending from the Country)|
|Availability & Order||through request form|
Baclofen, sold under the brand name Lioresal among others, is a central nervous system depressant used as a skeletal muscle relaxant. It is primarily used to treat spasticity. It is also used in topical creams to help with pain.
Baclofen – a muscle relaxant central action, a derivative of gamma-aminobutyric acid (GAMKb-stimulant). By reducing the excitability of the terminal parts of afferent sensory fibers and suppressing the intermediate neurons, depresses mono-and polysynaptic transmission of nerve impulses, It reduces the prestressing muscle spindles. It has no effect on neuromuscular transmission. In neurological diseases involving spasticity of the skeletal muscles, reduces the painful spasms and clonic convulsions; increases range of motion in the joints, facilitates passive and active kinesitherapy (exercise, massage, manual therapy).
Baclofen produces its effects by activating the GABAB receptor, similar to the drug phenibut which also activates this receptor and shares some of its effects. Baclofen is postulated to block mono-and-polysynaptic reflexes by acting as an inhibitory neurotransmitter, blocking the release of excitatory transmitters. However, baclofen does not have significant affinity for the GHB receptor, and has no known abuse potential. The modulation of the GABAB receptor is what produces baclofen’s range of therapeutic properties.
Similarly to phenibut (β-phenyl-GABA), as well as pregabalin (β-isobutyl-GABA), which are close analogues of baclofen, baclofen (β-(4-chlorophenyl)-GABA) has been found to block α2δ subunit-containing voltage-gated calcium channels (VGCCs). However, it is weaker relative to phenibut in this action (Ki = 23 and 39 μM for R– and S-phenibut and 156 μM for baclofen). Moreover, baclofen is in the range of 100-fold more potent by weight as an agonist of the GABAB receptor in comparison to phenibut, and in accordance, is used at far lower relative dosages. As such, the actions of baclofen on α2δ subunit-containing VDCCs are likely not clinically-relevant.
Baclofen is prescribed inside during the meal.
-Initial dose: The following gradually increasing dosage regimen is suggested, but should be adjusted to suit individual patient requirements: 5 mg orally 3 times a day for 3 days, then 10 mg orally 3 times a day for 3 days, then 15 mg orally 3 times a day for 3 days, then 20 mg orally 3 times a day for 3 days
-Maintenance dose: Should be individualized
-Maximum dose: 80 mg/day (20 mg 4 times a day)
-The maximum dose of 80 mg/day should be administered in 4 divided doses.
Withdrawal symptoms may include auditory hallucinations, visual hallucinations, tactile hallucinations, delusions, confusion, agitation, delirium, disorientation, fluctuation of consciousness, insomnia, dizziness (feeling faint), nausea, inattention, memory impairments, perceptual disturbances, pruritus/itching, anxiety, depersonalization, hypertonia, hyperthermia, formal thought disorder, psychosis, mania, mood disturbances, restlessness, and behavioral disturbances, tachycardia, seizures, tremors, autonomic dysfunction, hyperpyrexia (fever), extreme muscle rigidity resembling neuroleptic malignant syndrome and rebound spasticity.