Naloxon solution for injections ampoules 0.04% 1ml. №10

Description

Naloxon composition
active substance: naloxone;
1 ml of solution contains naloxone hydrochloride dihydrate in terms of 100% substance 0.4 mg;
Excipients: sodium chloride, dilute hydrochloric acid, water for injections.

Dosage form
Solution for injection.

Pharmacological properties
Naloxon is a competitive opiate receptor antagonist and belongs to the group of so-called “pure” opiate receptor antagonists. It blocks mainly μ-receptors and, due to its significant affinity for these receptors, displaces narcotic analgesics from binding sites, thus eliminating the symptoms of opioid overdose and eliminating the effects of both endogenous opiate peptides and exogenous opioid analgesics; to a lesser extent on other opiate receptors.
Administration of naloxone prevents, reduces or eliminates (depending on the dose and time of administration) the effects of opioid analgesics, restores respiration, reduces sedation and euphoria, reduces the hypotensive effect.
Naloxon eliminates the action of a wide group of narcotic drugs, both agonists and agonists-antagonists of opiate receptors: morphine, apomorphine, heroin, codeine, dihydrocodeine, promedol, methadone, pentazocine, fentanyl, buprenorphine.
The drug eliminates central and peripheral toxic symptoms: respiratory depression, pupillary constriction, slowed gastric emptying, dysphoria, coma and convulsions, as well as the analgesic effect of narcotic analgesics, in addition, it eliminates the toxic effects of large doses of alcohol.
Naloxon is also effective in respiratory disorders in mixed opioid poisoning in combination with barbiturates, benzodiazepines and alcohol.
Naloxon provokes withdrawal syndrome in patients with opioid dependence.
The drug has no analgesic activity, does not cause dysphoria and psychomimetic symptoms, addiction and drug dependence.

Indications
Naloxon is an opiate receptor antagonist. It blocks opioid receptors, eliminating central (including respiratory depression) and peripheral effects of opioids. Also affects the dopaminergic, GABAergic systems of the brain. Does not cause tolerance, drug dependence. In people with drug addiction, the drug provokes the development of withdrawal symptoms.
Naloxone is prescribed for overdose with narcotic analgesics.
It is prescribed to restore breathing in newborns after the administration of narcotic analgesics to a woman in labor.
In the postoperative period, it is used to accelerate the recovery from anesthesia, before the end of controlled breathing (only if narcotic analgesics were used during anesthesia).
It is used as a diagnostic tool in patients with suspected drug addiction.

Contraindications
Naloxon should not be prescribed for allergies to the components of the drug.

It is used with caution:

• with lung diseases;
• with renal / hepatic failure;
• when using narcotic analgesics in high doses;
• with physical opioid dependence;
• in childhood;
• with organic heart disease;
• when used in newborns from mothers with opioid dependence.

Children
Use in pediatric practice according to the indications and in the doses specified in the instructions.

Application during pregnancy and lactation
The use of this medication during pregnancy is acceptable if the health benefits to the mother outweigh the risks to the fetus.
It is not known whether the drug is excreted in breast milk, so its use during breastfeeding is possible only for absolute indications.

Method of administration and dosage
The solution is administered intravenously, subcutaneously, intramuscularly.
When overdosing with narcotic analgesics, 0.4–2 mg is used in adults, and 5–10 μg / kg in children. If the drug in the indicated dose does not bring the expected effect, the administration is repeated after 2-3 minutes. The maximum total dose is 10 mg / day.
In newborns, the initial dose is 0.01 mg / kg. The administration may be repeated in accordance with the guidelines for y adults.
For respiratory depression in the newborn caused by the use of opioid analgesics in the mother during childbirth, 0.1 mg / kg is administered. Ensure that the child’s airway is clear before administering the medication. Prophylactic intramuscular injection of 0.2 mg (or 0.06 mg / kg) is possible.
For the diagnosis of opioid dependence, 0.08 mg is administered intravenously.

Overdose
After the administration of the drug in doses exceeding the therapeutic ones (especially in the postoperative period in people with diseases of the cardiovascular system), the disappearance of analgesia, agitation, ventricular paroxysmal tachycardia, decrease / increase in blood pressure, ventricular fibrillation, cardiac arrest, pulmonary edema may occur.

Side effects:

• Digestive disorders: nausea, vomiting.
• Cardiovascular disorders: arrhythmia, tachycardia, increase / decrease in blood pressure.
• Neurological disorders: agitation, tremors, nervousness, irritability, convulsions, fatigue, behavioral disturbances.
• Others: increased sweating, pulmonary edema, allergic reactions.
• Possibly the development of a withdrawal syndrome in patients with opioid dependence: diarrhea, vague pains, hyperthermia, goose bumps, rhinorrhea, sneezing, sweating, vomiting, irritability, nervousness, fatigue, tremors, spasms in the supra-gastric region, weakness, tachycardia; in newborns – hyperthermia, convulsions, diarrhea, uncontrollable crying, sneezing, hyperreflexia, tremors, vomiting.

Storage conditions and periods
At 15-25 ° С. Shelf life is 4 years.