Akupan

General characteristics. Structure:

Active component: 1 ampoule contains 20 mg of a nefopam of a hydrochloride

excipients: sodium dihydrophosphate a dihydrate, sodium hydrophosphate dodecahydrate, water for injections.

Pharmacological properties:

Pharmacodynamics. Analgeziruyushchy central acting agent structurally different from other analgetics. Pilot studies indicate the central action which is based in inhibition of the return capture of dopamine, noradrenaline and serotonin at the level of synapses.
At animals to nefopa showed anti-nociceptive activity, by possible decrease in release of a glutamate at the presynaptic level and activation of receptors of N-methyl-D-aspartate at the postsynaptic level. Nefopam in clinical trials showed positive effect at a postoperative shiver. Nefopam has no antiinflammatory or febrifugal effect, breath does not oppress and does not influence an intestines peristaltics. Nefopam possesses insignificant m-holinoblokiruyushchim effect.

Pharmacokinetics. After introduction of one dose of 20 mg intramusculary, the maximum concentration in serum is observed in 30-60 minutes, and makes 25 ng/ml. The elimination half-life averages 5 hours. After intravenous administration of a dose of 20 mg, the elimination half-life (T1/2) makes 4 hours. Linkng with proteins of plasma makes 71-76%. Biotransformation is considerable, three metabolites are identified: to desmetilnefopa; to nefopa N-oxide; N-glucuronide of a nefopam. Desmetilnefopam and to nefopa N-oxide do not glyukuronizirutsya in a liver, do not show analgeziruyushchy activity in researches on animals. 87% of the entered dose are removed by kidneys, less than 5% of the entered dose are removed in not changed look.
The metabolites found in urine make 6%, 3% and 36% respectively of the dose entered intravenously.

Indications to use:

Pain syndrome of a different etiology and intensity:

- a pain syndrome at injuries,
- a pain syndrome after surgeries,
- labor pain relief,
- dentagra,
- mialgiya,
- renal and hepatic gripes,
- premedication before painful medical procedures.

Route of administration and doses:

The dose has to correspond to intensity of a pain syndrome and reaction of the patient.

Intramuscular introduction: акупан®-биокодекс it is necessary to enter intramusculary deeply. The recommended dose on one introduction - 20 mg. If necessary introduction is repeated by each 6 hours. The maximum daily dose - 120 mg.

Intravenous administration: акупан® - the biocode should be entered in the form of intravenous infusion lasting not less than 15 minutes, the patient has to be in a prone position. The recommended dose on one introduction - 20 mg. If necessary introduction is repeated by each 4 hours. The maximum daily dose - 120 mg.

Introduction technique: акупан®-биокодекс it is possible to enter in usual solution for infusions (0,9% solution of sodium of chloride or 5% of solution of a dextrose). An optimum ratio at cultivation - contents of the 1st ampoule of drug in 50 ml of solution for infusions.

Course of treatment - no more than 8-10 days.

Features of use:

Akupan - the biocode does not treat narcotic analgetics and antagonists of opioids. Thus, the treatment termination by narcotic analgetics of patients, dependent on them, which already receive therapy by drug акупан®-биокодекс increases risk of development of a withdrawal. Moreover, акупан®-биокодекс does not increase desintoxication of the patient.
The ratio advantage/risk at treatment by drug, is subject to constant revaluation.
акупан®-биокодекс it is not necessary to appoint for treatment of chronic pain syndromes, such as a headache.
Possible risk of medicinal dependence at patients with a depression or at patients with any medicinal dependence in the anamnesis.

During treatment it is not recommended to manage vehicles and to be engaged in other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Perspiration, drowsiness, nausea, vomiting, atropinopodobny reactions (dryness in a mouth, a syncope, an ischuria, irritability, excitement), tachycardia and increase in arterial pressure, hypersensitivity, a small tortoiseshell, a Quincke's edema, an acute anaphylaxis, spasms, hallucinations, medicinal dependence.

Interaction with other medicines:

Reception with sympathomimetics and m-holinoblokiruyushchimi drugs which strengthen side effects of drug акупан®-биокодекс, especially in case of simultaneous introduction is contraindicated: atropinopodobny spasmolysants, m-holinoblokiruyushchikh of protivoparkinsonichesky drugs, imipraminovy antidepressants and fenotiazinovy neuroleptics, H1 blockers - histamine receptors, Disopyramidum.

Contraindications:

- Hypersensitivity to a nefopam or other components of drug,
- Age up to 12 years,
- Spasms or their existence in the anamnesis, epilepsy,
- Risk of the ischuria caused by damage of an urethra and prostate
- Risk of development of acute glaucoma,
- Pregnancy, breastfeeding period.

With care:
It is necessary to be careful at appointment to patients with a liver, renal failure, to patients of advanced age.
It is necessary to be careful at appointment to patients with tachycardia.

 

Overdose:

Symptoms: tachycardia, spasms, hallucinations.

Treatment: symptomatic, cardiological and respiratory monitoring in the conditions of a hospital.

Storage conditions:

To store at a temperature not above 25 °C, in the place protected from light.
To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Solution for infusions and intramuscular introduction of 10 mg/ml. On 2 ml in ampoules of colourless transparent glass (type I) with a point of a break and a quoted strip of blue color. On 5 ampoules on the plastic pallet, together with the instruction, place in a pack cardboard.