Concept

Nefopam

Nefopam, sold under the brand name Acupan among others, is a centrally acting, non-opioid painkilling medication, that is primarily used to treat moderate to severe pain. Nefopam acts in the brain and spinal cord to relieve pain via novel mechanisms: antinociceptive effects from triple monoamine reuptake inhibition, and antihyperalgesic activity through modulation of glutamatergic transmission. Nefopam is effective for prevention of shivering during surgery or recovery from surgery. Nefopam was significantly more effective than aspirin as an analgesic in one clinical trial, although with a greater incidence of side effects such as sweating, dizziness and nausea, especially at higher doses. The estimated relative potency of nefopam to morphine indicates that 20 mg of nefopam HCl is the approximate analgesic equal of 12 mg of morphine with comparable analgesic efficacy to morphine, or oxycodone, while nefopam tends to produce fewer side effects, does not produce respiratory depression, and has much less abuse potential, and so is useful either as an alternative to opioid analgesics, or as an adjunctive treatment for use alongside opioids or other types of analgesics. Nefopam is also used to treat severe hiccups. Nefopam is contraindicated in people with convulsive disorders, those that have received treatment with irreversible monoamine oxidase inhibitors such as phenelzine, tranylcypromine or isocarboxazid within the past 30 days and those with myocardial infarction pain, mostly due to a lack of safety data in these conditions. Common side effects include nausea, nervousness, dry mouth, light-headedness and urinary retention. Less common side effects include vomiting, blurred vision, drowsiness, sweating, insomnia, headache, confusion, hallucinations, tachycardia, aggravation of angina and rarely a temporary and benign pink discolouration of the skin or erythema multiforme. Overdose and death have been reported with nefopam. Overdose usually manifests with convulsions, hallucinations, tachycardia, and hyperdynamic circulation.

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