Source: Health Products Regulatory Authority (ZA) Revision Year: 2022 Publisher: Adcock Ingram Limited, 1 New Road, Erand Gardens, Midrand, 1685, Private Bag X69, Bryanston, 2021 www.adcock.com 0860ADCOCK (232625)
A 2.8 Analgesic combinations
BESEMAX Tablets has analgesic, antipyretic and skeletal muscle relaxant properties.
Paracetamol has analgesic and antipyretic effects. It has only weak anti–inflammatory effects, and it has been thought to have a generally poor ability to inhibit COX in the presence of high concentrations of peroxides, as are found at sites of inflammation. It has been suggested that COX inhibition might be disproportionately pronounced in the brain, explaining its antipyretic efficacy.
Orphenadrine citrate is a muscle relaxant acting in the CNS, having, in general, a depressant effect Orphenadrine also has anticholinergic properties.
Oral paracetamol has excellent bioavailability. Peak plasma concentrations occur within 30–60 minutes, and the t1/2 in plasma is about 2 hours after therapeutic doses. Paracetamol is relatively uniformly distributed throughout most body fluids. Binding of the drug to plasma proteins is variable but less than with other NSAIDs; only 20–50% is bound at the concentrations encountered during acute intoxication. Some 90–100% of the drug may be recovered in the urine within the first day at therapeutic dosing, primarily after hepatic conjugation with glucuronic acid (about 60%), sulfuric acid (about 35%), or cysteine (about 3%); small amounts of hydroxylated and deacetylated metabolites have also been detected.
Orphenadrine is readily absorbed from the gastrointestinal tract and after intramuscular injection. It is almost completely metabolised to at least 8 metabolites. It is mainly excreted in the urine as metabolites and small amounts of unchanged drug. The half-life of orphenadrine has been reported to be 14 hours.
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