Naloxonum

General characteristics. Structure:

Active ingredient: 0,4 mg of Naloxonum of a hydrochloride (in terms of anhydrous substance) in 1 ml of solution.

Excipients: sodium chloride, dinatrium эдетат (disodium salt of ethylene diamine tetraacetic acid), Acidum hydrochloricum of 0,1 M, water for injections.

Pharmacological properties:

Pharmacodynamics. Antagonist of opioid receptors. Blocks opioid receptors, eliminates central (including respiratory depression) and peripheral effect of opioids. Influences also dofaminergichesky and Gamkergichesky systems of a brain. Does not cause tolerance and medicinal dependence. At persons with drug addiction provokes development of an abstinence syndrome.

After intravenous administration the effect develops in 1-2 min., after intramuscular - 2-5 min.; reaches a maximum in 5-15 min.; duration of effect depends on a dose and a way of introduction - at intravenous administration of 0,4 mg effect duration - 45 min., at intramuscular introduction - longer (to 4 h).

In experiments on mice and rats suppression of fertility and lack of teratogenic effect are revealed.

Pharmacokinetics. Gets through a blood-brain and placental barrier. It is metabolized in a liver. Naloxonum elimination half-life - 30-80 min. It is removed by kidneys (during 72 h 70% of the entered dose are removed).

Indications to use:

Overdose of narcotic analgetics.

Postoperative use: acceleration of an exit from the general anesthesia, before the end of the managed breath. Postoperatively drug is used only if during anesthesia narcotic analgetics were applied. Naloxonum is inefficient for treatment of the respiratory depression caused by substances, others than opioids.

Recovery of breath at newborns after introduction to the woman in labor of narcotic analgetics. As diagnostic medicine at patients with suspicion of drug addiction.

Route of administration and doses:

The drug is administered intravenously, intramusculary, subcutaneously.

At overdose of narcotic analgetics by the adult - in a dose of 0,4-2 mg, to children - 5-10 mkg/kg. If use in the specified dose does not bring the expected effect, introduction in the same dose is repeated in 2-3 min. The maximum total dose - 10 mg/days. If recovery of consciousness and breath does not occur, it is necessary to think of other (not opioid) reason of poisoning.

Postoperative introduction is carried out intravenously, in a dose of 0,1-0,2 mg, in 2-3 min. introduction of the same dose is repeated before recovery at the patient of satisfactory breath. Then in need of a current of several hours continue intramuscular introduction.

Children have intravenously initial dose of-1-2 mkg/kg. If there is no desirable effect, repeatedly enter in doses up to 0,1 mg/kg every 2 min., before emergence of spontaneous breath and recovery of consciousness. At impossibility of intravenous administration it is possible to enter intramusculary or subcutaneously fractional doses.

Newborns have an initial dose of-0,01 mg/kg. Introduction can be repeated according to the principles of use for adults.

At the respiratory depression caused by introduction of opioid analgetics of mother at the time of delivery the newborn enter 0,1 mg/kg intramusculary, subcutaneously or intravenously. Before introduction it is necessary to be convinced of passability of respiratory tracts at the newborn. Perhaps preventive intramuscular introduction of 0,2 mg (0,06 mg/kg).

Diagnosis of opioid dependence - intravenously 0,08 mg.

Features of use:

Pregnancy and lactation. Use during pregnancy is admissible if the advantage for mother exceeds risk for a fruit. It is unknown whether Naloxonum with breast milk is allocated. Use of drug during breastfeeding is possible according to absolute indications.

It can be applied as medicine to differential diagnosis of poisoning with narcotic analgetics. At use it is necessary to exercise constant medical surveillance over the patient.

Influence on ability to manage vehicles and mechanisms: it is not described.

Side effects:

From the alimentary system: nausea, vomiting.

From cardiovascular system: tachycardia, arrhythmia, increase or lowering of arterial pressure.

After introduction in the doses exceeding therapeutic (especially in the postoperative period at patients with diseases of cardiovascular system): disappearance of an analgesia and excitement, decrease/increase in arterial pressure, ventricular Bouveret's disease, fibrillation, ventricles, fluid lungs, cardiac standstill.

From TsNS: tremor, nervousness, excitement, irritability, fatigue, spasms, behavior disorder.

Others: the increased sweating, allergic reactions, a fluid lungs. A syndrome of "cancellation" at patients with opioid dependence: not clear pains, diarrhea, a hyperthermia, a rhinorrhea, sneezing, "goose-pimples", perspiration, nausea, vomiting, nervousness, fatigue, irritability, a tremor, spasms in epigastric area, tachycardia, weakness; newborns have spasms, diarrhea, a hyperthermia, impetuous crying, a hyperreflexia, sneezing, a tremor, extraordinary irritability, vomiting.

Interaction with other medicines:

Reduces hypotensive action of a clonidine.

Reduces effect of narcotic analgetics (including a butorfanola, the nalbufina, pentazocine, fentanyl, remifentanit) and accelerates emergence of a syndrome of "cancellation".

It is incompatible with solutions of the medicines containing hydrosulphates.

Pharmaceutical we will combine from 0,9% solution of sodium of chloride, 5% dextrose solution, sterile water for injections.

Contraindications:

Hypersensitivity.

With care. Organic heart diseases, diseases of lungs, a renal/liver failure, use of narcotic analgetics in high doses, physical opioid dependence, children's age, use for newborns on mothers with opioid dependence.

Overdose:

See the section "Side effect".

Storage conditions:

In the place protected from light, at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 4 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Solution for injections of 0,4 mg/ml in ampoules on 4 ml. 5 ampoules in a blister strip packaging from a film polyvinyl chloride and - a foil of the aluminum printing varnished or flexible packaging on the basis of aluminum foil, or without foil. Po1 or 2 blister strip packagings (with a foil or without foil) together with the application instruction of drug; a knife or the scarificator ampoule place in a pack from a cardboard. 20, 50 or 100 blister strip packagings with a foil together with 10, 25 or 50 application instructions of drug respectively, knives or scarificators ampoule place in a box from a cardboard or in a box from corrugated fibreboard (for a hospital). When packaging ampoules with rings or points of a break scarificators or knives ampoule do not put.