Naloxonum

Naloxonum – the competitive antagonist of opioid receptors.

Form of release and structure

Dosage form – solution for injections: colourless transparent liquid (on 1 ml: in glass ampoules without color, on 5 pieces in pallets from polyvinylchloride, in a cardboard pack 2 pallets; in ampoules, on 5 pieces in plastic holders, in a cardboard pack 2 holders or on 10 pieces in a cardboard pack).

Active ingredient of Naloxonum – Naloxonum a hydrochloride (in the form of dihydrate hydrochloride Naloxonum), in 1 ml – 0,4 mg.

Auxiliary components: Acidum hydrochloricum (to pH 3-5), sodium chloride, water for injections.

Indications to use

• Acute poisoning, including against the background of overdose by opioid analgetics (fentanyl, trimeperidine, morphine) and other means which toxic effect is caused by existence of an opioid component (methadone, opioid substitutes, pentazocine, буторфанол, buprenorphine, налбуфин) as a part of complex resuscitation actions;
• Postoperative use (only in case of use during operation of narcotic analgetics) – for acceleration of an exit from the general anesthesia, before completion of the managed breath;
• Recovery of breath at newborns, in case of introduction of mother of opioid analgetics at childbirth;
• Diagnostic means on opioid dependence (naloksonovy test).

Contraindications

Naloxonum is contraindicated at hypersensitivity to medicine components.

With care it is necessary to use drug at patients with an abnormal liver function and/or kidneys, at children's age and at newborns.

Appointment during pregnancy and breastfeeding is possible only at urgent need.

Route of administration and dosage

Naloxonum is intended for intravenous (in/in), intramuscular (in oil) and hypodermic (п / to) introductions.

Rate of administering is selected individually, considering reaction of the patient to drug and the previous single doses.

For infusional use it is necessary to dilute Naloxonum solution in 5% solution of a dextrose or 0,9% chloride sodium solution, observing a proportion – 1 ampoule of drug on 100 ml of the infusional environment. Prepare solution before direct use.

The dose and route of administration are appointed by the doctor, considering a condition of the patient, a look and amount of the opioid accepted by it.

The recommended dosing at acute poisoning (overdose) with opioid analgetics:

• Adults: an initial single dose – 0,4-2 mg. At life-threatening states the drug should be administered in/in slowly, within 2-3 minutes. For achievement of clinical effect repeated introduction is shown in 2-3 minutes, the procedure is repeated up to recovery of uniform breath and consciousness. If recovery of consciousness and breath did not occur after a total dose of introduction of 10 mg, it is necessary to consider not opioid reason of poisoning. It is possible to apply in oil or п / to;
• Children: an initial single dose – from calculation for 0,01 mg on 1 kg of weight of the child, it is preferable in/in introduction within 2-3 minutes. If necessary repeated introduction of a dose of 0,1 mg on 1 kg of weight in 2-3 minutes is shown. In case of impossibility in/in introductions, the drug administer fractional doses in oil or п / to with an interval of 2-3 minutes, in this case the effect is shown more slowly. For receiving more long action about 0,2 mg or on 0,06 mg on 1 kg of weight of the child are recommended single in oil or п / to introduction in a dose.

Postoperative use of Naloxonum:

• Adults: in/in on 0,1-0,2 mg at an interval of 2-3 minutes before emergence of normal lung ventilation and awakening of the patient, but in the absence of clear sensations of discomfort and pain. Increase in the arterial pressure (AP), the termination of an analgesia, sweating, nausea, vomiting, distsirkulyatorny crisis can become symptoms of exceeding of minimum necessary dose. Sometimes, especially in cases of use of opioid analgetics with long action, within 1-2 hours additional introduction of Naloxonum in oil is necessary. The drug can also be administered with the help in infusion;
• Children: in/in on 0,01 mg on 1 kg of weight, in the absence of desirable effect it is possible to enter in addition a dose of the corresponding 0,1 mg on 1 kg of weight of the child. In the absence of an opportunity in/in introductions, it is shown fractional in oil or п / to introduction every 2-3 minute. The single dose should not exceed 0,2 mg of drug. Besides, infusional introduction is shown.

In case of use of opioid analgetics at childbirth for recovery of breath at newborns it is shown in/in, in oil or п / to introduction of Naloxonum. Before introduction it is necessary to be convinced of passability of respiratory tracts of the baby. The recommended dose makes 0,01 mg on 1 kg of body weight, repetition of a dose in 2-3 minutes is possible. For prevention the newborn can once in oil enter 0,2 mg or on 0,06 mg on 1 kg of weight.

In quality diagnostic aids on narcotic (opioid) dependence use drug in the way to introductions of a dose of 0,0005 mg on 1 kg of weight of the checked patient. This dose allows to establish is caused or not difficulty of an urination and respiratory depression by opioids. After that it is possible to raise a dose a little, but not to high doses as high doses completely remove effect of opioid, including analgesic effect, cause excitement of the blood circulatory system and sympathetic system.

Side effects

Use of Naloxonum during the postoperative period can cause the following side effects: suffocation, increase or decrease in the ABP, ventricular tachycardia and fibrillation of ventricles, a fluid lungs, a cardiac standstill (the specified effects in rare instances are capable to entail a coma and encephalopathy, up to a lethal outcome). Use of the doses exceeding recommended can cause psychomotor excitement and disappearance of an analgesia.

Sudden drug withdrawal can lead to emergence of perspiration, nausea, vomiting, a fluid lungs, increase in the ABP, tachycardia, ventricular tachycardia, fibrillation of ventricles, to cause a shiver and spasms of a body, a stop of cordial activity, including with a lethal outcome.

Withdrawal symptoms at opioid dependence: weakness, nausea, vomiting, fever, perspiration, spasms in epigastric area, diarrhea, increase in the ABP, tachycardia, rhinitis, sneezing, a piloerektion, nervousness, irritability, yawning, concern, a shiver, pains of unspecified localization; newborns have an impetuous crying, spasms, a hyperreflexia.

Special instructions

Naloxonum is applied in the stationary conditions provided with a possibility of holding resuscitation actions (including cardiopulmonary) and oxygen therapy.

With care it is necessary to carry out treatment of newborns, at the instruction in the anamnesis of mother on dependence on opioids as full sudden cancellation of effect of drug can exponentiate development of an acute withdrawal.

The patient with pathology of lungs, hearts, a renal failure and/or the liver suspected or established by physical dependence on opioids during feeding pregnancy with a breast, at children's age it is recommended to use drug under careful observation of the doctor.

As the response to use of Naloxonum at therapy of respiratory depression against the background of reception of buprenorphine can be incomplete and there is a risk of decrease in respiratory activity, artificial ventilation of the lungs can be necessary for the patient.

During use of Naloxonum any activity connected with control of vehicles and mechanisms is prohibited the patient.

Medicinal interaction

At in introduction Naloxonum cannot be mixed with other means, also drug is incompatible with the solutions containing bisulphites.

Drug reduces hypotensive effect of a clonidine, action of opioid analgetics (налбуфин, буторфанол, pentazocine, remifentanit, fentanyl) that promotes acceleration of emergence of a withdrawal.

Simultaneous use of a metogeksital blocks the acute period of the abstinence which arose against the background of use of Naloxonum for patients with drug addiction.

Let's combine with dextrose solution 5%, solution of sodium of chloride of 0,9% and sterile water for injections.

Terms and storage conditions

To protect from children.

To store in the place protected from light at a temperature up to 25 °C.

Period of validity – 4 years.