Mild and moderate acute pain (including postoperative), not very severe chronic and cancer pain.
Composition:
1 tabl powl. contains 30 mg of nefopam hydrochloride.
Action:
Non-opiate analgesic, also showing cholinolytic, antihistamine and local anesthetic effects. It does not have anti-inflammatory, antipyretic, breathtaking effect, does not inhibit the respiratory center. A potent serotonin and norepinephrine reuptake inhibitor: the assumed point of analgesic handle is descending serotoninergic pathways, but the precise mechanism of action of the drug is unknown. By increasing the concentration of catecholamines in the synapses, it also acts chronically and inotropically positive. In terms of impact on o.u.n. can cause both euphoria and agitation as well as sedation. The analgesic effect corresponds to about 1/3 of the equilibrium dose of morphine, thus it is about 10 times stronger than ASA. It is well absorbed from the gastrointestinal tract (absorption 95-100%), reaching Cmax in the blood after about 1-3 h. In 71-76% bound to plasma proteins, the unbound part is rapidly distributed to tissues and body fluids, including the cerebrospinal fluid (reaches there about 25% Cmax in blood). It is metabolized in the liver by N-desmethylation and N-oxidation to 7 metabolites, of which 5 have no analgesia, and 2 have an effect that exceeds the action of the starting material by about 2%. T0,5 in the blood of nefopam is about 4 h (3-8 h); T0,5 metabolites: 2.2-9.2 h. Metabolites are excreted in urine (87%) and faeces (8%) in the form of glucuronide linkages. About 5% of the dose is excreted unchanged. The drug is excreted in breast milk.
Contraindications:
Hypersensitivity to the components of the preparation, epilepsy. Do not use in children under 12 years of age. Do not use simultaneously with MAO inhibitors and up to 3 weeks after discontinuation.
Precautions:
Use with caution in patients with liver or kidney disease, in the elderly, in patients with prostatic hyperplasia and difficulty in urinating.
Pregnancy and lactation:
The safety of use during pregnancy has not been established. The medicine can only be given when its use is absolutely necessary and the use of another medicine is contraindicated or impossible. Nefopam passes into breast milk (the infant receives approximately 3% of the dose taken by the mother) - do not use during breastfeeding.
Side effects:
In 10-30% of treated patients may cause nausea (without vomiting), dry mouth, difficulty swallowing. There may be: excessive sweating (in 10-30% of patients treated), dizziness, distraction, excessive agitation, insomnia, anxiety, loss of appetite, tachycardia, visual disturbances, difficulty passing urine, skin rashes. Elderly people have had hallucinations and confusion. It is believed that the drug may cause an amphetamine-like psychic dependence, which has not been proven.
Dosage:
Oral: usually 1-3 tabl. up to 3 times a day depending on the patient's reaction. The recommended starting dose - 60 mg three times a day. In the elderly, use lower doses (30 mg to 3 times a day). Take tablets when eating or after meals.
(C)
