Tracy Mechanism of Action

Pharmacology: Pharmacodynamics: Tramadol HCl is a centrally-acting analgesic compound. At least 2 complementary mechanisms appear applicable, binding of parent and M1 metabolite to u-opioid receptors and weak inhibition of reuptake of norepinephrine and serotonin. Paracetamol is another centrally-acting analgesic. The exact site and mechanism of its analgesic action is not clearly defined. When evaluated in a standard animal model, the combination of Tramadol and Paracetamol exhibited a synergistic effect.
Pharmacokinetics: Paracetamol is readily absorbed from the gastro-intestinal tract with peak plasma concentration occurring about 10-60 minutes after oral administration. Paracetamol is distributed into the most body tissues. It crosses the placenta and is present in the breast milk. Plasma protein binding is negligible at usual therapeutic concentrations but increases with increasing concentrations. The elimination half-life of Paracetamol varies from about 1 to 3 hours. Paracetamol is metabolized predominantly in the liver and excreted in the urine mainly as the glucuronide and sulphate conjugates less than 5% is excreted as unchanged Paracetamol. A minor hydroxylated metabolite (N-acetyl-p-benzoquinoneimine), which is usually produced in very small amounts by mixed function oxidases in the liver and kidney and which is usually detoxified by conjugation with glutathione may accumulate following Paracetamol overdosage and cause tissue damage.
Tramadol HCl is readily absorbed following oral administration but is subject to first-pass metabolism. Tramadol HCl is metabolized by N- and O-demethylation, glucuronidation or sulfation in the liver. The metabolite O-desmethyltramadol is pharmacologically active. Tramadol HCl is excreted mainly in the urine, predominantly as metabolites. Tramadol is widely distributed, crosses the placenta, and appears in small amounts in breast milk. The elimination half-life following oral administration is about 6 hours.