Nefopam-zdorovya

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT NEFOPAM-ZDOROV'YA (NEFOPAM-ZDOROVYE)

Composition:

Active substance: nefopam hydrochloride;

1 ampoule (2 ml) of the medicinal product contains 20 mg of nefopam hydrochloride;

1 vial (2 ml) of the medicinal product contains 20 mg of nefopam hydrochloride;

Excipients: sodium hydrogen phosphate, anhydrous sodium dihydrogen phosphate, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear, colorless solution.

Pharmacotherapeutic group. Analgesics. Other analgesics and antipyretics. Nefopam.

ATC code N02BG06.

Pharmacological Properties

Pharmacodynamics

A central non-narcotic analgesic, structurally unrelated to other analgesics.

In vitro experimental studies indicate a central effect involving inhibition of the reuptake of catecholamines and serotonin at the synaptic level.

In vivo studies in animals demonstrated the antinociceptive properties of nefopam.

There is evidence of a beneficial effect on postoperative shivering.

The drug has no anti-inflammatory or antipyretic activity, does not depress respiration, and does not affect intestinal peristalsis. It has anticholinergic effects.

Pharmacokinetics

After intramuscular administration of a single 20 mg dose, the time to reach maximum plasma concentration (Tmax) is 30 to 60 minutes, and the maximum concentration (Cmax) averages 25 ng/mL. The elimination half-life (T½) averages 5 hours. After intravenous administration of a 20 mg dose, T½ is 4 hours. Plasma protein binding ranges from 71% to 76%. Extensive biotransformation occurs, with three metabolites identified: desmethylnefopam, nefopam N-oxide, and nefopam N-glucuronide.

Desmethylnefopam and nefopam N-oxide are non-conjugated and have shown no analgesic activity in animal studies. Approximately 87% of the administered dose is excreted by the kidneys, with less than 5% excreted unchanged.

Metabolites found in urine account for 6%, 3%, and 36% of the intravenously administered dose, respectively.

Clinical characteristics.

Indications.

Postoperative analgesia as part of multimodal analgesia (nefopam also demonstrates a beneficial effect in preventing postoperative shivering).

Symptomatic treatment of acute pain conditions (injuries, post-surgical pain, relief of renal and hepatic colic pain).

Contraindications.

• Hypersensitivity to nefopam or to other components of the medicinal product.
• Pediatric age under 15 years, due to lack of clinical studies.
• Seizures or history of seizures.
• 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 forms of interaction.

It should be noted that a significant number of medicinal products may enhance central nervous system depression due to additive effects and reduce alertness, namely: opioids (analgesics, antitussives, opioid substitution therapy agents), neuroleptics, barbiturates, benzodiazepines, non-benzodiazepine tranquilizers (meprobamate), hypnotics, antidepressants with sedative effect (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), sedative H1-histamine receptor blockers, centrally acting antihypertensives, baclofen, thalidomide.

Special precautions for use

There is a risk of developing dependence on the medicinal product. Neofopam does not belong to opioid-like drugs or opioid antagonists. Therefore, discontinuation of opioid therapy in patients dependent on such drugs, who are already receiving neofopam, increases the risk of withdrawal syndrome development. The risk-benefit ratio of treatment with this medicinal product should be continuously evaluated.

The drug should not be used 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 is advised when administering the drug to patients with cardiovascular disorders, as tachycardia may occur.

Due to the anticholinergic effect, treatment with this drug is not recommended in elderly patients.

Alcohol and medicinal products containing alcohol should be avoided, as alcohol consumption may enhance the sedative effect.

This medicinal product contains less than 1 mmol (23 mg)/dose of sodium, i.e., it is practically sodium-free.

Use during pregnancy or breastfeeding

There are no data on the use of this medicinal product in pregnant women. Animal studies do not indicate a direct or indirect harmful effect on reproductive toxicity. For safety reasons, the drug should not be used during pregnancy.

Lactation. The drug passes into breast milk to such an extent that effects on newborns or infants who are breastfed are probable. The drug should not be used during breastfeeding.

Ability to affect reaction speed when driving vehicles or operating machinery

The possible risk of drowsiness during treatment with this drug should be taken into account, as it may impair the ability to drive vehicles or operate other machinery.

Method of Administration and Dosage

The therapy should be adjusted according to the intensity of pain and the patient's response.

Intramuscular administration. The medicinal product should be administered deep intramuscularly. The recommended dose per administration is 20 mg. If necessary, repeat the administration every 6 hours. The maximum daily dose is 120 mg.

Intravenous administration. The medicinal product should be administered as a prolonged intravenous infusion over at least 15 minutes. The patient should be in a lying position to avoid certain adverse reactions such as nausea, dizziness, and sweating. The dose per administration is 20 mg. If necessary, repeat the administration every 4 hours.

The maximum daily dose is 120 mg.

Administration technique. The drug may be administered diluted in a standard infusion solution (0.9% sodium chloride solution or 5% glucose solution). The optimal dilution ratio is 1 ampoule/bottle of the drug in 50 ml of infusion solution.

Duration of treatment: not more than 8–10 days.

Children. Do not use in children under 15 years of age.

Overdose.

Anticholinergic symptoms: tachycardia, coma, seizures, hallucinations.

Treatment: symptomatic treatment with cardiac and respiratory monitoring in a hospital setting.

Adverse Reactions.

Reported adverse reactions are classified by system-organ classes and frequency: very common (≥ 1/10), common (≥ 1/100, < 1/10), uncommon (≥ 1/1000, < 1/100), rare (≥ 1/10000, < 1/1000), very rare (< 1/10000), not known (frequency cannot be determined from available data).

Central nervous system disorders: very common – somnolence; common – dizziness*; rare – seizures*; not known – coma.

Cardiac disorders: common – tachycardia*, palpitations*.

Gastrointestinal disorders: very common – nausea, vomiting; common – dry mouth*.

Renal and urinary disorders: common – urinary retention.

Immune system disorders: rare – hypersensitivity reactions, including urticaria, angioedema (Quincke's edema), anaphylactic shock.

General disorders: very common – hyperhidrosis*; rare – malaise.

Psychiatric disorders: rare – excitement*, irritability*, hallucinations, drug dependence, drug abuse; not known – confusion.

* Other anticholinergic-like reactions may occur, even if they have never been reported.

Reporting of adverse reactions.

Reporting suspected adverse reactions after drug approval is important. It allows continuous monitoring of the benefit-risk balance of the medicinal product. Healthcare and pharmacy professionals, as well as patients or their legal representatives, are encouraged to report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at the following link: https://aisf.dec.gov.ua.

Shelf life. 2 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C. Keep out of reach of children.

Incompatibilities. The medicinal product must not be mixed with other medicinal products in the same container.

Packaging. 2 ml in a vial; 5 vials in a cardboard box with partition.

2 ml in a vial; 5 vials in a blister; 1 blister in a cardboard box.

2 ml in a bottle; 5 bottles in a contour cell pack; 1 contour cell pack in a cardboard box.

Prescription status. Prescription only.

Manufacturer.

LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVYA".

Limited Liability Company "FARMEKS GROUP".

Manufacturer's address and location of its business activities.

Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenko Street, 22.

(LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVYA")

Ukraine, 08301, Kyiv region, city of Boryspil, Shevchenko Street, 100.

(Limited Liability Company "FARMEKS GROUP")