Instructions Nefalzhik solution for injection 20 mg ampoule 2 ml No. 5
Composition
active ingredient: nefopam hydrochloride;
1 ampoule 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, odorless solution.
Pharmacotherapeutic group
Analgesics and antipyretics.
ATX code N02B G06.
Pharmacological properties
Pharmacodynamics.
Nefalzhik is a central non-narcotic analgesic, structurally unlike other analgesics.
Experimental studies in vitro indicate a central action consisting in the inhibition of catecholamine and serotonin reuptake at the synapse level.
In vivo animal studies have shown antinociceptive properties of nefopam.
Nefalzhik has shown a positive effect on postoperative tremor in clinical studies.
Nefalzhik does not have anti-inflammatory or antipyretic effects, does not depress respiration, and does not affect intestinal peristalsis.
Nefalzhik 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; 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%, respectively, of the intravenously administered dose.
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 of the other ingredients of the drug.
Children under 15 years of age, due to the lack of clinical studies.
Convulsions 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. Nefalzhik does not belong to morphine-like drugs and opiate antagonists. Therefore, discontinuation of treatment with morphine-like drugs in patients already taking Nefalzhik increases the risk of developing withdrawal syndrome. The risk/benefit ratio of treatment with Nefalzhik should be constantly assessed.
Nefalzhik 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.
Given the anticholinergic effect, treatment with Nefalzhik 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.
Use during pregnancy or breastfeeding
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 toxicity. For safety reasons, Nefalzhik should not be used during pregnancy.
Lactation: Nefopam is excreted in human milk to such an extent that exposure to the breastfed newborn/infants is likely. Nefalzhik should not be used during breast-feeding.
The ability to influence the reaction speed when driving or working with other mechanisms
The possible 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. Nefalzhik should be administered intramuscularly deep. A dose of 20 mg is recommended for one injection. If necessary, the injection is repeated every 6 hours. The maximum daily dose is 120 mg.
Intravenous administration. Nefalzhik should be administered as a continuous intravenous infusion over at least 15 minutes, with the patient in a supine position to avoid some adverse reactions such as nausea, dizziness, sweating. A single dose per injection is 20 mg. If necessary, the administration is repeated every 4 hours.
The maximum daily dose is 120 mg.
Administration method:
Nefalzhik 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.
Side effects
Reported adverse reactions are listed by system organ class and frequency: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1,000, < 1/100), rare (≥ 1/10,000, < 1/1,000), very rare (< 1/10,000), not known (frequency cannot be estimated from the available data).
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.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in a place protected from light.
Incompatibility
Do not mix the drug with other medicines in the same container.
Packaging
2 ml of solution in an ampoule. 5 ampoules on a pallet in a cardboard box.
Vacation category
According to the recipe.
Producer
1. Responsible for the release of the series: BIOCODEX, France.
2. Production: DELPHARM TOUR, France.
Address
1. 1 Avenue Blaise Pascal, 60000 Beauvais, France.
2. Paul Langevin Street, 37170 Chambray-le-Tour, France.
