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Nefopam

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Nefopam

Nefopam_IT

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Nefopam

Property Description
Active ingredient Nefopam hydrochloride
Form Tablets/Capsules, Solution for injection
Pharmacological class Centrally-acting analgesic, Non-opioid
Common use Relief of moderate to severe pain
Origin Synthetic, benzoxazocine derivative

What Type of Medicine is Nefopam? (Identity and Classification)

Nefopam is a synthetic drug classified as a centrally-acting analgesic, meaning its primary mechanism for pain relief occurs within the central nervous system, specifically the brain and spinal cord. The active pharmaceutical component is Nefopam hydrochloride. Nefopam is categorized as a non-opioid analgesic and belongs to the benzoxazocine chemical class. This structure is a key differentiator, as it provides a powerful option for managing moderate to severe pain while being chemically and pharmacologically unrelated to narcotic agents, ensuring it avoids the risk of opioid-related respiratory depression.

Understanding Nefopam's Unique Pain Relief Mechanism (General Purpose and High-Level Action)

The general purpose of Nefopam is to lessen the perception of pain by boosting the body's natural defense systems against pain signals. It works by inhibiting the reuptake of three vital neurotransmitters—serotonin, norepinephrine, and dopamine—thereby increasing their availability to modulate pain transmission. This triple neurotransmitter reuptake inhibition enhances the central descending pain control pathways. This unique mechanism provides effective relief in settings like post-operative recovery, offering a non-narcotic pathway to reduce discomfort.

Nefopam’s Available Forms and Composition (Product Entity)

Nefopam is a single-ingredient product commonly supplied as both oral solid forms (tablets or capsules) and an injectable solution. The availability of both forms, including the injectable route, provides flexibility for healthcare professionals to manage pain acutely via intravenous or intramuscular delivery, or chronically via oral administration. The active salt, Nefopam hydrochloride, is formulated with either an aqueous base for the injection or standard solid excipients for the tablet to ensure pharmaceutical stability and appropriate delivery of the active compound.

What side effects are possible with Nefopam?

Official Regulatory Safety Profile

This information details the possible side effects and safety considerations for nefopam as documented in authoritative governmental regulatory sources.

Frequency-Classified Adverse Reactions

The following are common and very common side effects reported in official documents:

Frequency System Organ Class (SOC) Adverse Reaction
Very Common (1/10) Nervous System, Gastrointestinal Somnolence (Drowsiness), Nausea, Vomiting
Common (1/100 to < 1/10) Cardiac, Nervous System, Psychiatric Tachycardia (Fast Heart Rate), Palpitations, Dizziness, Insomnia, Hyperhidrosis (Excessive Sweating)

Serious Adverse Reactions and Overdose Risk

Regulatory warnings highlight the risk of severe effects, particularly in the event of an overdose. These serious reactions include convulsions (seizures), hallucinations, and profound depression of the central nervous system (CNS) and cardiovascular function.

Safety Restrictions and Limitations

The use of nefopam is contraindicated (officially forbidden) in several specific patient groups due to known safety risks, including:

  • Children under 15 years of age.
  • Individuals with a history of epilepsy or convulsive disorders.
  • Patients at risk of angle-closure glaucoma.
  • Patients with prostatic disorders or urethropathies leading to a risk of urinary retention.
  • Use in combination with certain medications, such as MAO inhibitors, is also restricted.

Population-Specific Considerations

Caution is advised when nefopam is used in the elderly due to the increased risk of confusion, drowsiness, and anticholinergic effects like urinary retention. Patients with known hepatic (liver) or renal (kidney) insufficiency also require careful consideration due to the potential for drug accumulation.

Overdose and Emergency Response

The official regulatory profile for Nefopam overdose details a distinct pattern of severe toxicity across the central nervous system (CNS) and cardiovascular systems. Documented clinical manifestations include CNS effects such as coma, convulsions (seizures), agitation, and hallucinations. Cardiovascular effects involve tachycardia accompanied by a hyperdynamic circulation. Regulatory documents also note that older patients may be more susceptible to overdose-related CNS effects, specifically confusion.

Immediate medical attention is required for all suspected overdose cases. Official guidance mandates that emergency services (e.g., A&E) be contacted immediately if severe signs like a seizure or fit occur, or if the individual becomes unconscious. Urgent medical advice is also required for less severe but still critical symptoms such as persistent hallucinations or a very fast heartbeat.

The official labeling confirms that no specific antidote is known for Nefopam overdose. Consequently, management is officially defined as symptomatic and supportive. Procedures described in regulatory documents include the prompt removal of the ingested drug through methods like gastric lavage and the use of activated charcoal. Specific pharmacological interventions are noted, such as the use of Diazepam for the control of convulsions and Beta-adrenergic blockers to manage cardiovascular complications.

Therapeutic Uses of Nefopam

What Nefopam Treats: Main Uses and Benefits

Nefopam is commonly used to help with symptoms related to physical discomfort across conditions characterized by periods of heightened symptoms. This medication is applicable in clinical settings that involve acute or unstable symptom patterns, such as managing moderate to severe pain, including post-surgical discomfort, dental pain, and pain arising from musculoskeletal conditions.

It is generally applied in scenarios where additional management of discomfort is required, and is considered relevant in the context of persistent, specialized long-term pain. This application provides support that helps ease the overall symptom burden, supporting patients during difficult episodes by easing distress.

The medication is relevant in managing symptom clusters within multimodal pain management strategies. This approach supports therapeutic efforts to reduce the reliance on narcotic analgesics, which contributes to maintaining functional stability.

Quick Fact: Relief for Established Pain Nefopam is commonly used when symptoms intensify, providing supportive relief that is often sought when additional symptom management support is required.

Eligibility and Restrictions for Use

The official regulatory profile for Nefopam strictly defines the populations who can and cannot use the medicine.

Populations for Whom Use is Prohibited

Nefopam is contraindicated and must not be used by patients who meet the following criteria, as explicitly stated in the official regulatory labeling:

  • Patients with a history of convulsive disorders (e.g., epilepsy).
  • Patients taking Monoamine Oxidase (MAO) Inhibitors.
  • Patients with known hypersensitivity to the drug or any of its components.
  • Patients being treated for a Myocardial Infarction (heart attack).

Age-Related and Conditional Eligibility

Category Regulatory Classification
Pediatric Population Use is not recommended for children under 12 years, as safety and efficacy have not yet been established for this age group.
Older Adults Recommended starting dose is reduced, as older patients are more susceptible to certain central nervous system effects.
Kidney Impairment Patients with terminal renal insufficiency are eligible but require a reduced daily dose.
Liver Impairment Use requires caution in patients with hepatic insufficiency.

Pregnancy and Breastfeeding Eligibility

Use during pregnancy should be avoided unless the physician deems it absolutely essential, given the regulatory determination that there is no evidence of safety during human pregnancy. Since Nefopam is excreted in human milk, official labeling requires that breastfeeding must be discontinued during treatment due to the risk of adverse effects in the nursing infant.

Other Specific Restrictions

Caution is required for use in patients with or at risk of angle closure glaucoma or those with or at risk of urinary retention (e.g., due to urethroprostatic disorders).

What should I know about interactions with other medicines?

Nefopam has the potential to interact with several classes of medicinal products, primarily due to its effect on neurotransmitter reuptake and its inherent anticholinergic properties. These interactions can lead to clinically significant outcomes, including additive side effects and the risk of severe reactions.

Interacting Product Category Nature of Interaction Classification
Monoamine Oxidase (MAO) Inhibitors High risk of Serotonin Toxicity/Syndrome. Contraindicated
Tricyclic Antidepressants (TCAs) Increased risk of serotonin toxicity and additive anticholinergic effects. Use with Caution
Agents with Anticholinergic Activity Increased severity of side effects such as dry mouth and urinary retention. Additive Effect
Agents with Sympathomimetic Activity Increased severity of side effects like tachycardia and palpitations. Additive Effect

The co-administration of Nefopam with any medicine that increases serotonin availability, including MAO inhibitors, Tricyclic Antidepressants, and Selective Serotonin Reuptake Inhibitors (SSRIs), is associated with the potential for serotonin syndrome.

Additionally, Nefopam may interfere with certain laboratory screening tests for benzodiazepines and opioids, potentially leading to false positive results for individuals taking the medicine. Patients should inform healthcare providers about all concurrent medicines, including over-the-counter and herbal supplements.

Mechanism of Action

How Nefopam Works — Mechanism of Action

Nefopam is an agent that acts primarily within the central nervous system and exerts its effect through the modulation of neurotransmitter systems and influence on pain signal transmission pathways in the CNS.

It acts as a non-selective inhibitor of the Serotonin Transporter (SERT) and the Norepinephrine Transporter (NET). By blocking the reuptake of these monoamines into nerve endings, it increases their concentration in the synapse. This activity potentiates the descending inhibitory pain system.

Concurrently, Nefopam acts as a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist, which acts to reduce neuronal hyperexcitability and limit the cascade known as central sensitization. This action, combined with minor Na^+ channel blockade, contributes to antinociception via neural membrane stabilization.

This combined central action causes the suppression of ascending pain signals in the spinal cord. The resulting physiological change is antinociception.

Dosage and Administration Information

Nefopam is utilized via two primary approved routes of administration: oral (tablets or capsules) and parenteral (intravenous or intramuscular injection). This dual availability allows for use in both outpatient and supervised clinical settings.

The administration schedule is determined by the route. Oral administration is typically taken three times daily, with individual doses ranging from 30 mg up to 90 mg; the tablets may be taken either with or without food. For the injectable form, the single dose is generally 20 mg and can be repeated, with a minimum interval of four hours for the intravenous route and six hours for the intramuscular route, up to a maximum daily total of 120 mg.

The injectable form has specific procedural conditions. Intravenous doses require dilution in common solutions (such as isotonic sodium chloride) and must be administered as a slow infusion over at least 15 minutes. To facilitate proper use, the patient is generally advised to be lying down during and immediately after parenteral administration.

Important usage adjustments exist for certain populations. The starting oral regimen for older adults is commonly reduced, often advised not to exceed 30 mg three times daily. Additionally, a dose reduction is recommended for patients with severe renal impairment. Nefopam is generally not recommended for use in children under 12 years of age. Following prolonged use, a gradual dose reduction may be necessary when discontinuation is planned.

Recent Clinical Evidence

Research evidence / Overview of studies for Nefopam

Evidence for Use in Acute Postoperative Pain

Nefopam was evaluated in research exploring use in study in outcomes related to physical discomfort that arises after surgical procedures, which is a common clinical setting where acute symptoms are particularly noticeable. Research into this application primarily consists of short-term Randomized Controlled Trials (RCTs) and systematic reviews. These studies typically involved adult patients recovering from procedures such as general, orthopedic, and dental surgeries.

Studies monitored outcomes related to patient-reported perceived discomfort, focusing on how symptoms change over time in the first 24 to 48 hours following the procedure. Researchers also monitored outcomes related to the need for supplementary supplementary pain medication, such as how long it took before a patient requested additional medication, and the total amount of opioid medication required during the recovery period.

Findings describe patterns observed in the studies where research reported patterns observed in measured opioid consumption that were associated with Nefopam compared to control groups. Research examined changes measured in the time before patients needed rescue medication. However, when examining scores used to measure pain intensity, results were mixed across different studies and types of surgery. This variability across studies means that broad conclusions about pain intensity are difficult to draw based on the research.

Evidence for Use in Chronic Pain Conditions

Research has explored the use of Nefopam for study of outcomes related to chronic musculoskeletal conditions like rheumatoid arthritis or low back discomfort. The research base lacks contemporary, high-quality evidence and is largely derived from smaller, older trials and some observational reports.

Studies conducted in this area monitored patient-reported outcomes describing changes in subjective pain levels over a period of several weeks, and sometimes monitored physical measures like joint tenderness or stiffness. Findings in these research contexts involving fluctuating or unstable symptoms have been variable, particularly when compared against inactive control substances. The evidence contributes to the broader evidence landscape but certainty remains low due to the nature of the available data.

Evidence for Specialized Applications in the Peri-operative Setting

Specific research was conducted for a specialized, non-pain-related application: research exploring outcomes related to postoperative shivering. These trials, often relevant in trials assessing short-term or episodic symptom patterns immediately following anesthesia, were designed to see if Nefopam was associated with this specific outcome. Research examined the frequency and severity of shivering episodes. Studies reported how symptoms evolved in the observed populations, indicating that research measured a lower incidence of shivering that was associated with Nefopam compared to inactive substances or other control agents.

Long-Term Research and Follow-up Durations

The majority of the evidence for Nefopam is derived from research focused on short-term symptom changes, such as the immediate hours or days following a procedure. Therefore, follow-up durations were limited in most key studies. There is limited information for long-term outcomes or the durability of any observed response over extended periods. For example, research does not provide sufficient data on the effects on functional outcomes or perceived discomfort that lasts longer than a few weeks or months. This means that long-term effects are not fully established in the research record.

Evidence Gaps and Areas of Uncertainty

The research landscape for Nefopam shows several areas where more data is needed. Firstly, the evidence quality varies across studies, and many randomized trials involved sample sizes that were modest, meaning the results apply only to the populations studied. Furthermore, findings were variable when research explored direct pain intensity reduction in the acute pain setting. Data for certain groups remain insufficient, and research does not provide adequate context for populations such as older adults with multiple chronic conditions or women who are pregnant or breastfeeding. Overall, the available evidence provides context but not individual predictions, and the findings help contextualize how patients reported their experience under the specific conditions of the studies.

Frequently Asked Questions (FAQ)

Common questions about Nefopam (FAQ)

Q: What is the main medical purpose of Nefopam?

Official product information indicates that Nefopam is primarily used for the relief of acute and chronic pain.

It is distinct from many other pain relievers and acts within the central nervous system to modulate pain signals.

Q: Is Nefopam classified as an opioid or narcotic drug?

Regulatory documents state that Nefopam is a non-opioid, non-narcotic central analgesic.

It possesses a unique chemical structure and exerts its effect without binding to opioid receptors or causing respiratory depression, distinguishing it from narcotic agents.

Q: Does Nefopam carry a risk of dependence or addiction according to regulatory information?

Official warnings note that the risk is considered much lower than with opioid painkillers. However, there have been rare reports of dependence after taking it for many years.

Gradual dose reduction may be necessary following prolonged use, as prescribed by a healthcare professional.

Q: How quickly should a person expect the effects of Nefopam to start?

For the oral tablets, the effects should typically begin within 1 to 2 hours after administration.

This onset window aligns with the time required for the drug to reach its peak concentration in the bloodstream.

Q: What is the approximate duration of the effects of Nefopam?

The terminal elimination half-life of Nefopam is generally reported to be between 3 to 8 hours.

This duration is a factor in determining the appropriate interval between doses, as reflected in official prescribing information.

Q: Can Nefopam interact with common over-the-counter pain medications?

Nefopam is often prescribed when common non-prescription painkillers are not sufficient.

Regulatory guidance states the importance of informing a healthcare provider of all concurrent medications, as the drug’s side effects may be additive when taken with other agents that have anticholinergic or sympathomimetic activity.

Q: Are there any specific warnings about taking Nefopam with alcohol?

Official product warnings strongly discourage alcohol consumption while taking Nefopam.

This is because alcohol is known to increase the sedative effect of the medication, which may affect a person’s ability to drive or operate machinery safely.

Q: Is Nefopam contraindicated for people with certain heart conditions?

The drug should not be used to treat pain specifically resulting from a myocardial infarction (heart attack).

Caution is also advised for patients with other cardiovascular pathology due to the potential risk of tachycardia (a fast heart rate) which is a documented side effect.

Q: What are the official restrictions for using Nefopam during pregnancy or while breastfeeding?

According to official restrictions, Nefopam should not be used during pregnancy unless deemed absolutely essential by a healthcare professional.

Because the drug is excreted in human milk, breast-feeding should be discontinued during the course of treatment to avoid risk to the infant.

Q: Why is Nefopam sometimes confused with tricyclic antidepressants?

Official information describes Nefopam’s mechanism of action as involving the reuptake inhibition of serotonin and norepinephrine.

This specific neurochemical activity is a similarity shared with some tricyclic antidepressants, which contributes to the common confusion.

Q: Does Nefopam affect the ability to drive or operate machinery?

Official product information warns that the medication may affect the ability to drive or operate machinery due to the potential risk of drowsiness and dizziness.

Patients should use caution and assess their condition before engaging in such activities.

Q: Are there different brand names for Nefopam across various regions?

Yes, while the generic name is Nefopam, official patient information from various regions commonly cites the brand name Acupan.

This indicates that the drug is marketed under different commercial names internationally.

Q: Is Nefopam used to treat neuropathic pain?

The official indication lists are for acute and chronic pain, including post-operative and musculoskeletal pain.

Neuropathic pain (pain caused by nerve damage) is not explicitly listed on the official indication list provided by regulatory documents.

Q: Can Nefopam cause dry mouth, and is this common?

Yes, dry mouth is a frequently reported side effect of Nefopam.

Official documents classify this as a documented anticholinergic effect of the medication, which is a common action among drugs affecting the central nervous system.

Q: Is there a known withdrawal process described when stopping Nefopam treatment?

Regulatory warnings state that gradual dose reduction may be necessary when stopping treatment after long-term use.

This is advised because sudden discontinuation may result in symptoms such as tiredness or restlessness.

Q: Does Nefopam have documented side effects related to kidney or liver function?

Caution is advised for patients who have pre-existing hepatic (liver) or renal (kidney) insufficiency.

Furthermore, post-marketing reports have indicated risks of hepatocellular injury and acute kidney injury.

Q: What are the regulatory classifications of Nefopam in Europe or Canada?

Regulatory bodies classify Nefopam as a non-opioid analgesic with central stimulant properties, using the ATC code: N02BG06.

It is not scheduled as a narcotic or controlled substance in the major regions where it is licensed.

Q: Is it normal to feel a tingling sensation after taking Nefopam?

Yes, numbness or tingling in the extremities is listed as a frequently reported side effect.

This condition is described in medical terms as paraesthesia in official product information.

Q: How long does Nefopam stay in the body after the last dose?

The terminal half-life is typically between 3 to 8 hours.

Based on official pharmacokinetic data, the majority of the dose is generally eliminated from the body within 24 hours.

Q: Are there any specific official warnings about skin reactions with Nefopam use?

Official warnings detail that certain skin reactions are possible but are classified as rare.

These include swelling of the skin and soft tissue (known as angioedema) and severe allergic reactions (anaphylaxis).

Q: What types of pain are listed as the primary indications for Nefopam?

Official product information indicates that Nefopam is indicated for the relief of acute and chronic pain.

This includes post-operative pain, dental pain, musculoskeletal pain, acute traumatic pain, and pain caused by cancer.

How should Nefopam be stored and disposed of?

Storage Conditions

All Nefopam products must be stored out of the sight and reach of children.

Required storage temperature varies by labeled formulation:

  • Some tablet labels state the product does not require any special storage conditions.
  • Other product labels specify to not store above 30 C.

The medicine should not be used after the expiry date shown on the packaging. For the injection solution, official guidance specifies that the product must be immediately used after opening, reconstitution, or dilution.

Disposal Instructions

Expired or unused Nefopam must not be thrown away via wastewater or household waste; this instruction is a measure to help protect the environment.

Disposal procedures require consulting a healthcare professional: patients must ask a pharmacist how to properly throw away medicine they no longer need, in accordance with local requirements for pharmaceutical waste.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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