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Palliative care
Published in Henry J. Woodford, Essential Geriatrics, 2022
Opiates act at receptors on the terminal end of pain fibres within the dorsal columns of the spinal cord. The medium-strength opiate agent tramadol also has non-opiate, mainly serotonergically mediated, properties (it may precipitate the serotonin syndrome when combined with other drugs – see page 163). Non-steroidal anti-inflammatory drugs (NSAIDs) act by preventing the formation of prostaglandins at sites of inflammation. The mechanism of action of paracetamol is poorly understood. Nefopam is another type of analgesic but has a high probability of anticholinergic effects and is typically not recommended for older people.7
Clinical pharmacology and therapeutics: nonopioids
Published in Nigel Sykes, Michael I Bennett, Chun-Su Yuan, Clinical Pain Management, 2008
Nefopam is a nonopioid analgesic, related to orphenadrine and diphenhydramine. It acts centrally and peripherally, with an unknown mechanism of action distinct from that of NSAIDs or opioids. It has an effect on a-2 receptors,45 demonstrates noncompetitive N-methyl-d-aspartic acid (NMDA) receptor antagonism,46 inhibits reuptake of noradrenaline, serotonin (via descending pathways47), and dopamine48 and has sympathomimetic and anticholinergic actions. Nefopam does not cause respiratory depression. Some accumulation occurs in moderate or severe renal or hepatic failure. It should be avoided in patients with histories of fits or on monoamine oxidase inhibitors.
Clinical management
Published in Alistair Burns, Michael A Horan, John E Clague, Gillian McLean, Geriatric Medicine for Old-Age Psychiatrists, 2005
Alistair Burns, Michael A Horan, John E Clague, Gillian McLean
Nefopam is a non-opioid analgesic whose mechanism of action is not fully understood, but it is likely to be in the CNS. It has a rapid onset of action, and it is more effective than paracetamol or NSAIDs in relieving pain. It is useful for both acute and chronic pain. Sympathomimetic and anticholin- ergic side-effects limit its use. Side-effects, which are dose-related, include:
Nefopam hydrochloride loaded microspheres for post-operative pain management: synthesis, physicochemical characterization and in-vivo evaluation
Published in Artificial Cells, Nanomedicine, and Biotechnology, 2018
Neelam Sharma, Sandeep Arora, Jitender Madan
The investigations in drug delivery involve sustained release of an active entity to curtail dosage frequency, diminution in toxicity though retaining therapeutic effectiveness of dosage regimen, improved bioavailability of active pharmaceutical moiety with superior safety and biocompatibility [1]. Nefopam hydrochloride (NPH) (Figure 1(a)) is non-opioid centrally acting analgesic preferred for relief of nociception in different pain syndrome such as acute traumatic, surgical operations, toothache and myalgia. Recommended oral dosage of NPH is 30–90 mg three times daily which might produce patient non-compliance and additional side effects such as dry mouth, hypersensitivity, patch necrosis of gastrointestinal mucosa, nausea and vomiting [2,3]. Therefore, development of biodegradable sustained release polymeric microspheres of NPH has been superlative methodology to reduce dosage frequency [4].
Emerging role of nanomedicine in the treatment of neuropathic pain
Published in Journal of Drug Targeting, 2020
Pankaj Bidve, Namrata Prajapati, Kiran Kalia, Rakesh Tekade, Vinod Tiwari
Nefopam hydrochloride a centrally acting non-opioid analgesic acts by inhibiting the reuptake of three neurotransmitters (serotonin (5-HT), dopamine (DA) and noradrenaline (NA)), producing an analgesic effect and also thought to mediate its action via acting on histamine H3 receptor, blocking voltage-gated sodium channel and modulating glutaminergic transmission [34–36]. But several adverse effects like nausea, vomiting, dizziness, drowsiness, sweating and patient non-complianceare reported due to frequent administration of nefopam hydrochloride. Thus, sustained release dosage form which ensures prolong drug release and decreases metabolism will provide an excellent strategy for its use in NeP.
The effect of preoperative nefopam treatment on postoperative catheter-related bladder discomfort in patients undergoing transurethral bladder tumor resection: a randomized double-blind study
Published in Scandinavian Journal of Urology, 2018
MiHye Park, Chan Hee Jee, Kyung-Hwa Kwak, Jun-Mo Park, Ji Hyo Kim
Nefopam is a non-opioid analgesic with a spinal and supraspinal action, including inhibition of dopamine, norepinephrine, and serotonin recapture. It is used to prevent postoperative pain in the context of multimodal analgesia [6]. This drug is a cyclic analog of diphenhydramine (an antihistamine), with a chemical structure resembling orphenadrine (an antimuscarinic) [7]. It also shows pre-emptive analgesic effects in a model of neuropathy, which involves the activation of N-methyl-D-aspartic acid (N.M.D.A.) receptors [8].