Akupan-Biocodex, 10 mg/ml 2 pcs 5 pcs

Pharmacodynamics

Acupan-Biocodex is a central analgesic that is structurally different from other analgesics. Experimental studies indicate central action, which is based on inhibition of dopamine, noradrenaline and serotonin reuptake at the synaptic level.

In animals, nefopam showed antinociceptive activity, through possible reduction of glutamate release at presynaptic level and activation of N-methyl-D-aspartate receptors at 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-cholin-blocking effect.

Pharmacokinetics

After administration of a single dose of 20 mg intramuscularly, maximum serum concentration is observed after 30-60 minutes and is 25 ng/ml. The elimination half-life is on average 5 hours. After an intravenous dose of 20 mg, the half-life (T1/2) is 4 hours. Binding to plasma proteins 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 glucuronized in the liver 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 found in the urine are 6%, 3% and 36%, respectively, of the dose administered intravenously.

Indications

Pain syndrome of different etiology and intensity:

Active ingredient

Composition

1 ampoule (2 ml) contains:
active ingredient: nefopam hydrochloride 20.0 mg,
excipients: sodium dihydrophosphate dihydrate 32.215 mg, sodium hydrophosphate dodecahydrate 3.440 mg, water for injection up to 2.0 ml

How to take, the dosage

The dose should be adjusted to the intensity of the pain syndrome and the patient’s response.

Intramuscular administration: Akupan-Biocodex should be administered intramuscularly and 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: Akupan-Biocodex should be administered as an intravenous infusion of at least 15 minutes, the patient should be lying down. The recommended dose for one injection is 20 mg. If necessary, the administration should be repeated every 4 hours. Maximum daily dose is 120 mg.

Method of administration: Akupan-Biocodex can be administered in usual solution for infusion (0.9 % sodium chloride solution or 5 % dextrose solution). The optimal ratio for dilution is the contents of 1 ampoule of the drug in 50 ml of the solution for infusion.

The course of treatment – no more than 8-10 days.

The treatment period should not exceed 8-10 days.

Interaction

Inadication with sympathomimetics and m-cholinoblocking drugs that increase the side effects of the drug acupan-biocodex is contraindicated, especially in case of simultaneous administration: atropine-like antispasmodics, m-cholinoblocking antiparkinsonian drugs, imipramine antidepressants and phenothiazine neuroleptics, H1-histamine receptor blockers, disopyramide.

Special Instructions

Acupan-biocodex should not be prescribed for the treatment of chronic pain syndromes, such as headache.

Acupan-biocodex is not a narcotic analgesic or opioid antagonist. Therefore, discontinuing treatment with narcotic analgesics for addicted patients who are already receiving therapy with acupan-biocodex increases the risk of withdrawal syndrome. Moreover, acupan-biocodex does not increase patient detoxification.

The benefit/risk ratio of treatment with the drug, is subject to constant reassessment.

Possible risk of drug dependence in patients with depression or in patients with a history of any drug dependence.

It is not recommended to drive vehicles and engage in other potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

With caution:
Caution should be exercised when prescribing to patients with hepatic, renal insufficiency, elderly patients.
Caution should be exercised when prescribing to patients with tachycardia.

Side effects

Overdose

Symptoms: tachycardia, seizures, hallucinations.
Treatment: symptomatic, cardiac and respiratory monitoring under hospital conditions.