Instructions Nefam solution for injection 20 mg/ml pre-filled syringe 1 ml No. 1
Composition
active ingredient: nefopam hydrochloride;
1 ml of solution for injection contains nefopam hydrochloride 20 mg;
Excipients: sodium dihydrogen phosphate, dihydrate; sodium hydrogen phosphate, dodecahydrate; water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: transparent colorless solution.
Pharmacotherapeutic group
Analgesics and antipyretics. ATX code N02B G06.
Pharmacological properties
Pharmacodynamics.
Nefam® is a central non-narcotic analgesic, structurally unlike other analgesics. In vitro experimental studies indicate a central effect consisting in the inhibition of catecholamine and serotonin reuptake at the synapse level. In vivo studies in animals have shown the antinociceptive properties of nefopam. In clinical studies, nefopam has shown a positive effect on postoperative tremor. Nefopam does not have anti-inflammatory or antipyretic effects, does not depress respiration and does not affect intestinal peristalsis. Nefopam has an anticholinergic effect.
Pharmacokinetics.
After a single dose of 20 mg intramuscularly, the time to reach maximum serum concentration (Tmax) is 30 to 60 minutes, and the maximum concentration (Cmax) is on average 25 ng/ml. The half-life is on average 5 hours. After intravenous administration of a dose of 20 mg, the half-life is 4 hours. Plasma protein binding is 71–76%.
Biotransformation is significant, three metabolites have been identified: desmethylnefopam, nefopam N-oxide, and nefopam N-glucuronide.
Desmethylnefopam and nefopam N-oxide are not conjugated and do not exhibit analgesic activity in animal studies. 87% of the administered dose is excreted by the kidneys, less than 5% of the administered dose is excreted unchanged.
Metabolites detected in urine account for 6%, 3% and 36% of the intravenously administered dose, respectively.
Indication
Postoperative analgesia as part of multimodal analgesia (nefopam also exhibits positive properties in preventing postoperative tremor).
Symptomatic treatment of acute pain conditions (injuries, pain after surgical operations, analgesia of renal and hepatic colic).
Contraindication
• Hypersensitivity to nefopam or to any other component of the drug.
• Children under 15 years of age – due to the lack of clinical studies.
• Seizures or history of them.
• Risk of urinary retention associated with urethroprostatic disorders.
• Risk of acute glaucoma attack.
• Concomitant use of MAO inhibitors.
Interaction with other medicinal products and other types of interactions
It should be taken into account that a significant number of drugs can increase the depression of the nervous system due to the additive effect and reduce alertness, namely: opiates (analgesics, antitussives, substitution drugs for the treatment of drug addiction), neuroleptics, barbiturates, benzodiazepines, non-benzodiazepine tranquilizers (meprobamate), hypnotics, antidepressants with a sedative effect (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), sedative H1-histamine receptor blockers, centrally acting antihypertensives, baclofen, thalidomide.
Application features
There is a risk of drug dependence. Nefam® is not a morphine-like drug or an opiate antagonist. Therefore, discontinuation of morphine-like drug treatment in morphine-dependent patients already taking Nefam® increases the risk of withdrawal syndrome. The risk/benefit ratio of Nefam® treatment should be constantly assessed.
Nefam® should not be prescribed for the treatment of chronic pain syndromes.
Caution should be exercised when prescribing the drug to patients with hepatic or renal insufficiency due to the risk of accumulation, which increases the likelihood of adverse reactions.
Caution should be exercised when prescribing the drug to patients with cardiovascular disease, as there is a possibility of tachycardia.
Due to the anticholinergic effect, treatment with Nefam® is not recommended for elderly patients.
The use of alcohol and medications containing alcohol should be avoided due to the increased sedative effect when consumed with alcohol.
This medicinal product contains less than 1 mmol (23 mg) sodium per dose, i.e. essentially 'sodium-free'.
Use during pregnancy or breastfeeding
Pregnancy.
There are no data on the use of the drug in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive function. For safety reasons, Nefam® should not be used during pregnancy.
Lactation.
Nefopam passes into breast milk in amounts that may affect the breastfed newborn/infants. Nefam® should not be used during breast-feeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
The risk of drowsiness during treatment with the drug should be taken into account, which may affect the ability to drive or operate other mechanisms.
Method of administration and doses
Therapy should correspond to the intensity of the pain syndrome and the patient's response. Intramuscular administration. Nefam® should be administered intramuscularly deep. A dose of 20 mg is recommended for one injection. If necessary, repeat the injection every 6 hours. The maximum daily dose is 120 mg.
Intravenous administration. Nefam® should be administered as a continuous intravenous infusion over at least 15 minutes; the patient should be in a supine position to avoid adverse reactions such as nausea, dizziness, sweating. Single dose per injection – 20 mg. If necessary, repeat the injection every 4 hours. Maximum daily dose – 120 mg.
Introduction method
Nefam® can be administered in a standard infusion solution (0.9% sodium chloride solution or 5% glucose solution). The optimal dilution ratio is 1 ampoule of the drug in 50 ml of infusion solution.
The course of treatment is no more than 8–10 days.
Children: Do not use in children under 15 years of age.
Overdose
Symptoms of anticholinergic origin: tachycardia, coma, convulsions, hallucinations.
Treatment: symptomatic treatment with cardiological and respiratory monitoring in a hospital setting.
Adverse reactions
Reported adverse reactions are classified by system organ class and frequency: very common (≥ 1/10), common (≥ 1/100,
Central nervous system: very common: drowsiness; common: dizziness*; rare: convulsions*, unknown: coma.
Cardiac disorders: common: tachycardia*, palpitations*.
Gastrointestinal: very common: nausea, vomiting; common: dry mouth*.
Renal and urinary disorders: common: urinary retention.
Immune system disorders: Rare: hypersensitivity reactions, including urticaria, angioedema, anaphylactic shock.
General disorders: very common: hyperhidrosis*; rare: malaise.
Psychiatric disorders: rare: agitation*, irritability*, hallucinations, drug dependence, drug abuse; unknown: confusion.
*Other atropine-like reactions may occur, even if they have never been reported.
Reporting of suspected adverse reactions.
Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the automated pharmacovigilance information system at the link: https//aisf.dec.gov.ua.
Expiration date
18 months.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Does not require special storage conditions. Do not freeze.
Keep out of reach of children.
Packaging
1 ml in a pre-filled glass syringe with a needle; 1 or 2 syringes with a needle in a blister; 1 blister in a pack; or 1 syringe with a needle in a tube; 1 or 10 tubes in a pack.
Vacation category
According to the recipe.
Producer
JSC "Farmak".
Location of the manufacturer and its business address
Ukraine, 04080, Kyiv, Kyrylivska St., 74.
