ACUPAN Tablet Ref.[27918] Active ingredients: Nefopam

Source: Medicines and Medical Devices Safety Authority (NZ)  Revision Year: 2018  Publisher: iNova Pharmaceuticals (New Zealand) Limited, c/- Simpson Grierson, 88 Shortland Street, Auckland 1141

5.1. Pharmacodynamic properties

Pharmacotherapeutic group: 4.7.1 Non-opioid analgesics and compound analgesic preparations
ATC code: N02BG06

ACUPAN is a centrally acting analgesic with a rapid onset of action. The main site of action appears to be in the central nervous system both at the brain and spinal levels.

In vitro experiments have shown nefopam to inhibit the re-uptake of various catecholamines (including noradrenaline, serotonin and dopamine). It is possible that the mechanism of action of nefopam is at least in part by altering the levels of these neuromodulators in the brain and at the spinal level. Nefopam has been shown to have sympathomimetic and anticholinergic actions.

ACUPAN is totally distinct from the other centrally acting analgesics such as morphine, codeine, pentazocine and propoxyphene. Unlike the narcotic agents, ACUPAN has been shown not to cause respiratory depression. There is no evidence from pre-clinical research of habituation occurring with ACUPAN.

5.2. Pharmacokinetic properties

The absorption of ACUPAN after oral administration is rapid with peak concentrations being reached in 1½ to 2 hours. The elimination from plasma occurs with a mean half-life of 6 hours. The medicine undergoes extensive metabolism by the liver and both unchanged medicine and metabolites are excreted principally in the urine, with approximately 6% in the faeces. Most of the dose is eliminated within 24 hours. A moderate to severe impairment of renal or hepatic function may reduce the elimination rate constant and cause some accumulation of ACUPAN or its metabolites.

5.3. Preclinical safety data

Not applicable.

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