Description
Nefopam Pharmacodynamics
Nefopam is a non-narcotic analgesic of central action, structurally different from other known analgesics.
In vitro, it inhibited dopamine, norepinephrine and serotonin reuptake in rat synaptosomes.
In vivo, in animals, nefopam exhibited antinociceptive activity, by possibly reducing glutamate release at the presynaptic level and activation of N-methyl-D-aspartate receptors at the postsynaptic level. Nefopam has shown positive effects in clinical trials for postoperative tremor. Nefopam has no anti-inflammatory or antipyretic effect, does not depress respiration and does not affect intestinal peristalsis. Nefopam has a minor m-cholinoblocking effect. A temporary and moderate increase in heart rate and blood pressure was observed during the studies.
Indications
Symptomatic treatment of acute pain syndrome, including postoperative pain.
Contraindications
– Hypersensitivity to nefopam or other drug components;
– children under 15 years of age (due to lack of clinical data);
– seizures or history of seizures, epilepsy;
– risk of urinary retention caused by urethral and/or prostate diseases;
– risk of acute glaucoma;
– pregnancy, breastfeeding (see also section “Administration during pregnancy and breastfeeding”).
Dosage and administration
- The dose should be adjusted to the intensity of the pain syndrome and the patient’s reaction.
- Intramuscular administration:
- Nefopam should be administered intramuscularly deeply. The recommended dose per injection is 20 mg. If necessary, the administration should be repeated every 6 hours. Maximum daily dose is 120 mg.
- Intravenous administration:
- Nefopam should be administered as an intravenous infusion for at least 15 minutes, the patient should be lying down to avoid such adverse events as nausea, dizziness, sweating. The recommended dose per injection is 20 mg. If necessary, the injection should be repeated every 4 hours. Maximum daily dose is 120 mg.
- The recommended dose should not be exceeded.
- Methods of administration:
- Nefopam can be administered in normal solutions for infusion (sodium chloride isotonic solution or dextrose solution). Nefopam and other injectable drugs should not be mixed in one syringe.
- The drug should be used immediately after opening the ampoule, diluted.
- The course of treatment is not more than 8-10 days.