Buy Lioresal (Baclofen) muscle relaxant medication
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LIORESAL (BACLOFEN) TABLETS PHARMACOLOGY
Lioresal is an effective antispastic agent with a spinal site of action. Its mechanism of action and pharmacological properties are different from those of other antispastic agents.
Baclofen also has central sites of action given the adverse event profile and general CNS depressant properties.
Baclofen depresses monosynaptic and polysynap tic reflex transmission, probably by various actions, including stimulation of GABA-beta-receptors. This stimulation in turn inhibits the
release of excitatory amino acids (glutamate and aspartate) in guinea pig preparations. Neuromuscular transmission is not affected by baclofen.
Baclofen exerts an antinociceptive effect. The clinical significance of this awaits clarification. In neurological diseases associated with spasm of the skeletal muscles, the clinical effects of Lioresal take the form of a beneficial action on reflex muscle contractions and of marked relief from painful spasm, automatism and clonus. Lioresal, where indicated, improves the patient's mobility, making for greater independence and facilitating passive and active physiotherapy. Baclofen stimulates gastric acid secretion.
Baclofen is rapidly and completely absorbed from the gastro-intestinal tract. Maximum concentrations of unchanged drug are attained in plasma in 2 to 4 hours after an oral dose. The bioavailability of oral baclofen is 70 to 80%.
Following oral administration of a single dose of 40 mg baclofen, peak serum concentrations of 500 to 600 nanogram/mL are reached. The serum concentration remains above 200 nanogram/mL for 8 hours. The onset of action is highly variable and may range from hours to weeks.
The distribution volume of baclofen amounts to 0.7 litre/kg. In cerebrospinal fluid, the active substance attains concentrations approx. 8.5 times lower than in the plasma. Baclofen is bound to plasma proteins to the extent of about 30%.
About 15% of a dose of baclofen is metabolised in the liver. Deamination yields the main metabolite, beta-chlorophenyl-gamma-hydroxybutyric acid, which is pharmacologically inactive.
Approximately 70% of baclofen is eliminated in the urine in unchanged form. The plasma elimination half-life of baclofen averages 3 to 4 hours. Within 72 hours, approximately 75% of the dose is excreted via the kidneys, approximately 5% of this quantity being in the form of metabolites. The remainder of the dose, including 5% as metabolites, is excreted in the faeces.
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