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Naloxon (Solution) Instructions for Use

ATC Code

V03AB15 (Naloxone)

Active Substance

Naloxone (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Competitive opioid receptor antagonist

Pharmacotherapeutic Group

Opioid receptor antagonist

Pharmacological Action

Opioid receptor antagonist. It blocks opioid receptors, eliminating the central (including respiratory depression) and peripheral effects of opioids. It also affects the dopaminergic and GABAergic systems of the brain. It does not cause tolerance or drug dependence. In individuals with drug dependence, it provokes the development of withdrawal syndrome.

After IV administration, the effect develops within 1-2 minutes; after IM administration, within 2-5 minutes; it reaches its maximum within 5-15 minutes. The duration of the effect depends on the dose and route of administration – with IV administration of 0.4 mg, the duration of the effect is 45 minutes; with IM administration, it is longer (up to 4 hours).

Experiments on mice and rats revealed suppression of fertility and the absence of a teratogenic effect.

Pharmacokinetics

It penetrates the blood-brain barrier and the placental barrier. It is metabolized in the liver. The T1/2 of naloxone is 30-80 minutes. It is excreted by the kidneys (70% of the administered dose is excreted within 72 hours).

Indications

Overdose of narcotic analgesics.

Postoperative use: acceleration of recovery from general anesthesia, before the end of controlled respiration. Postoperatively, the drug is used only if narcotic analgesics were used during anesthesia. Naloxone is ineffective for treating respiratory depression caused by substances other than opioids.

Restoration of breathing in newborns after administration of narcotic analgesics to the mother in labor.

As a diagnostic agent in patients with suspected drug dependence.

ICD codes

ICD-10 code Indication
F11 Mental and behavioral disorders due to opioid use
P04.0 Fetus and newborn affected by maternal anesthesia and analgesia in pregnancy, labor and delivery
T40 Poisoning by narcotics and psychodysleptics [hallucinogens]
T88.5 Other complications of anesthesia
ICD-11 code Indication
6C43.Z Disorders due to opioid use, unspecified
KA06.0 Fetus or newborn affected by maternal use of anesthesia or analgesic drugs during pregnancy, labor and delivery
NE60 Poisoning by drugs, medicaments or biological substances, not elsewhere classified
NE8Z Injury or harm caused as a result of surgical or therapeutic interventions, not elsewhere classified, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Solution

The drug is administered intravenously, intramuscularly, or subcutaneously.

For overdose of narcotic analgesics, adults are given a dose of 0.4-2 mg, children – 5-10 mcg/kg. If the use of the indicated dose does not bring the expected effect, the administration is repeated at the same dose after 2-3 minutes. The maximum total dose is 10 mg/day. If restoration of consciousness and breathing does not occur, another (non-opioid) cause of poisoning should be considered.

Postoperative administration is performed intravenously, at a dose of 0.1-0.2 mg; after 2-3 minutes, the same dose is repeated until the patient’s satisfactory breathing is restored. Then, if necessary, intramuscular administration is continued for several hours.

In children, the initial IV dose is 1-2 mcg/kg. If the desired effect is not achieved, it is re-administered in doses of up to 0.1 mg/kg every 2 minutes, until spontaneous breathing appears and consciousness is restored. If IV administration is not possible, it can be administered IM or subcutaneously in fractional doses.

In newborns, the initial dose is 0.01 mg/kg. Administration can be repeated in accordance with the principles of use in adults.

For respiratory depression caused by the administration of opioid analgesics to the mother during childbirth, newborns are given 0.1 mg/kg intramuscularly, subcutaneously, or intravenously. Before administration, it is necessary to ensure the patency of the newborn’s airways. Prophylactic IM administration of 0.2 mg (0.06 mg/kg) is possible.

Diagnosis of opioid dependence – IV 0.08 mg.

Adverse Reactions

From the digestive system: nausea, vomiting.

From the cardiovascular system: tachycardia, arrhythmia, increase or decrease in blood pressure.

After administration in doses exceeding the therapeutic dose (especially in the postoperative period in patients with cardiovascular diseases): disappearance of analgesia and agitation, decrease/increase in blood pressure, ventricular paroxysmal tachycardia, ventricular fibrillation, pulmonary edema, cardiac arrest.

From the CNS: tremor, nervousness, agitation, irritability, fatigue, convulsions, behavioral disturbance.

Other: increased sweating, allergic reactions, pulmonary edema.

Withdrawal syndrome in patients with opioid dependence: vague pains, diarrhea, hyperthermia, rhinorrhea, sneezing, “goosebumps”, sweating, nausea, vomiting, nervousness, fatigue, irritability, tremor, spasms in the epigastric region, tachycardia, weakness; in newborns – convulsions, diarrhea, hyperthermia, uncontrollable crying, hyperreflexia, sneezing, tremor, unusual irritability, vomiting.

Contraindications

Hypersensitivity.

With caution. Organic heart diseases, lung diseases, renal/hepatic insufficiency, use of narcotic analgesics in high doses, physical opioid dependence, childhood, use in newborns from mothers with opioid dependence.

Use in Pregnancy and Lactation

Use during pregnancy is acceptable if the benefit to the mother outweighs the risk to the fetus. It is not known whether Naloxone is excreted in breast milk. Use of the drug during breastfeeding is possible for absolute indications.

Use in Hepatic Impairment

With caution: hepatic insufficiency.

Use in Renal Impairment

With caution: renal insufficiency.

Pediatric Use

With caution: childhood, use in newborns from mothers with opioid dependence.

Special Precautions

It can be used as a drug for the differential diagnosis of poisoning with narcotic analgesics. When used, constant medical supervision of the patient is necessary.

Drug Interactions

It reduces the hypotensive effect of clonidine.

It reduces the effect of narcotic analgesics (including butorphanol, nalbuphine, pentazocine, fentanyl, remifentanil) and accelerates the onset of withdrawal syndrome.

It is incompatible with solutions of medicinal products containing hydrosulfates. It is pharmaceutically compatible with 0.9% sodium chloride solution, 5% dextrose solution, and sterile water for injection.

Storage Conditions

Store the drug in a place protected from light, at a temperature not exceeding 25°C (77°F). Keep out of the reach of children.

Shelf Life

Shelf life – 4 years. Do not use after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

Kern Pharma S.L. (Spain)

Labeled By

SINTEZ, PAO (Russia)

Dosage Form

Bottle Rx Icon Naloxone Solution for injection 0.4 mg/1 ml: amp. 10, 500, 1000 or 2500 pcs., bottles 50 ml, 100 ml or 200 ml

Dosage Form, Packaging, and Composition

Solution for injection 1 ml
Naloxone hydrochloride (as naloxone hydrochloride dihydrate) 400 mcg

1 ml – ampoules (5) – plastic trays (2) – cardboard packs.
1 ml – ampoules (5) – plastic trays (100) – cardboard boxes.
1 ml – ampoules (5) – plastic trays (200) – cardboard boxes.
1 ml – ampoules (5) – plastic trays (500) – cardboard boxes.
50 ml – polyethylene bottles.
100 ml – polyethylene bottles.
200 ml – polyethylene bottles.

Marketing Authorization Holder

Kern Pharma S.L. (Spain)

Labeled By

COMPANY DEKO, LLC (Russia)

Dosage Form

Bottle Rx Icon Naloxone Solution for injection 0.4 mg/1 ml: amp. 10, 500, 1000 or 2500 pcs., bottles 50 ml, 100 ml or 200 ml

Dosage Form, Packaging, and Composition

Solution for injection 1 ml
Naloxone hydrochloride (as naloxone hydrochloride dihydrate) 400 mcg

1 ml – ampoules (5) – plastic trays (2) – cardboard packs.
1 ml – ampoules (5) – plastic trays (100) – cardboard boxes.
1 ml – ampoules (5) – plastic trays (200) – cardboard boxes.
1 ml – ampoules (5) – plastic trays (500) – cardboard boxes.
50 ml – polyethylene bottles.
100 ml – polyethylene bottles.
200 ml – polyethylene bottles.

Marketing Authorization Holder

Kern Pharma S.L. (Spain)

Dosage Form

Bottle Rx Icon Naloxone Solution for injection 0.4 mg/1 ml: amp. 10, 500, 1000 or 2500 pcs., bottles 50 ml, 100 ml or 200 ml

Dosage Form, Packaging, and Composition

Solution for injection 1 ml
Naloxone hydrochloride (as naloxone hydrochloride dihydrate) 400 mcg

1 ml – ampoules (5) – plastic trays (2) – cardboard packs.
1 ml – ampoules (5) – plastic trays (100) – cardboard boxes.
1 ml – ampoules (5) – plastic trays (200) – cardboard boxes.
1 ml – ampoules (5) – plastic trays (500) – cardboard boxes.
50 ml – polyethylene bottles.
100 ml – polyethylene bottles.
200 ml – polyethylene bottles.

Marketing Authorization Holder

Moscow Endocrine Plant FSUE (Russia)

Dosage Form

Bottle Rx Icon Naloxone Solution for injection 400 mcg/1 ml: amp. 5, 10 or 100 pcs.

Dosage Form, Packaging, and Composition

Solution for injection colorless, transparent.

1 ml
Naloxone hydrochloride 400 mcg

Excipients: sodium chloride, hydrochloric acid, water for injection.

1 ml – ampoules (5) – plastic holders (1) – cardboard packs.
1 ml – ampoules (10) – plastic holders (1) – cardboard packs.
1 ml – ampoules (100) – plastic holders (1) – cardboard packs.

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