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Pharmacology: Pharmacodynamics: BIOCALM is a centrally acting muscle relaxant. It exerts muscle relaxant activity through blocking gamma pathway descending from the brain stem and exhibiting nonspecified inhibitory activity at the spinal levels.
Pharmacokinetics: After oral administration absorption and distribution of tolperisone is rapid with large variation in AUC (area under curve) and Cmax (peak concentration). Tolperisone is mainly metabolised by p450-mediated CYP2D6 metabolic pathway into its active metabolite hydroxymethyl tolperisone. The half life of the drug is 1.5 hours, it undergoes extensive metabolism and only 0.1% of total dose appears in urine over a period of 24 hours. The inter-individual variation in the plasma concentration is due to the genetic polymorphism of the drug metabolizing enzymes.
