Source: Υπουργείο Υγείας (CY) Revision Year: 2022 Publisher: Remedica Ltd., Aharnon Str., Limassol Industrial Estate, 3056 Limassol, Cyprus
Pharmacotherapeutic group: Analgesics, Other Analgesics and Antipyretics, Anti-Inflammatory
ATC code: N02BE01
Paracetamol has analgesic and antipyretic effects that do not differ significantly from those of aspirin. However it has only weak anti-inflammatory effects. It is only a weak inhibitor of prostaglandin biosynthesis although there is some evidence to suggest it may be more effective against enzymes in the central nervous system than in the periphery. This may in part account for its activity profile.
Paracetamol is rapidly and almost completely absorbed from the gastro-intestinal tract with peak plasma concentrations occurring 0.5-2 hours after dosing. The plasma half-life is approximately 2 hours after therapeutic doses in adults but is increased in neonates to about 5 hours. It is widely distributed through the body. Metabolism is principally by the hepatic microsomal enzymes and urinary excretion accounts for over 90% of the dose within 1 day. Virtually no paracetamol is excreted unchanged, the bulk being conjugated with glucoronic acid (60%), sulphuric acid (35%) or cysteine (3%). Children have less capacity for glucuronidation of the drug than adults.
There are no studies relating to the mutagenic potential of paracetamol Suspension.
In vivo mutagenicity tests of paracetamol in mammals are limited and show conflicting results. Therefore, there is insufficient information to determine whether paracetamol poses a mutagenic risk to man.
Paracetamol has been found to be non-mutagenic in bacterial mutagenicity assays, although a clear clastogenic effect has been observed in mammalian cells in vitro following exposure to paracetamol (3 and 10 mM for 2h).
There are no studies to the carcinogenic potential of paracetamol suspension.
There is inadequate evidence to determine the carcinogenic potential of paracetamol in humans. A positive association between the use of paracetamol and cancer of the ureter (but not of other sites in the urinary tract) was observed in a case-control study in which approximate lifetime consumption of paracetamol (whether acute or chronic) was estimated. However, other similar studies have failed to demonstrate a statistically significant association between paracetamol and cancer of the urinary tract, or paracetamol and renal cell carcinoma.
There is limited evidence for the carcinogenicity of paracetamol in experimental animals. Liver cell tumours can be detected in rats following chronic feeding of 500 mg/kg/day paracetamol.
There is no information relating to the teratogenic potential of paracetamol Suspension. In humans, paracetamol crosses the placenta and attains concentrations in the foetal circulation similar to those in the maternal circulation. Intermittent maternal ingestion of therapeutic doses of paracetamol are not associated with teratogenic effects in humans.
Paracetamol has been found to be foetotoxic to cultured rat embryo.
There is no information relating to the effects of paracetamol Suspension. A significant decrease in testicular weight was observed when male Sprague-Dawley rats were given daily high doses of paracetamol (500 mg/kg/body weight/day) orally for 70 days.
Conventional studies using the currently accepted standards for the evaluation of toxicity to reproduction and development are not available.
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