Universal reference book for medicines
Name of the preparation: NALOXON (NALOXON)

Active substance: naloxone

Type: Competitive opioid receptor antagonist

Manufacturer: WARSAW PHARMACEUTICAL WORK POLFA (Poland)
Composition, form of production and packaging
Solution for injection is
colorless, transparent.

1 ml

naloxone hydrochloride (in the form of naloxone hydrochloride dihydrate) 400 μg

Excipients: sodium chloride - 8.55 mg, hydrochloric acid (up to pH 3-5), water d / u (up to 1 ml).

1 ml - ampoules of colorless glass (5) - pallets made of PVC (2) - cardboard packs.

INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2012.

PHARMACHOLOGIC EFFECT

Naloxone is a specific antagonist of opioid receptors.
Competitively communicates with the main types of opioid receptors and prevents or eliminates central (including respiratory depression) and peripheral effects of both endogenous opioid peptides and exogenous opioids (opioid analgesics and their surrogates).
It also affects the dopaminergic and GABA -ergic system of the brain.
Restores breathing, reduces sedation and euphoria, weakens the hypotensive effect.
The psychotomimetic effects and dystrophy caused by opioid analgesics of the agonist-antagonist group (pentazocine, butofanol), Naloxone has no pronounced effect.
It is not effective as a tramadol antagonist. Completely does not eliminate the effects of buprenorphine.
Naloxone provokes withdrawal syndrome in patients with drug dependence to opioids.
Does not cause addiction and drug dependence.
With IV introduction, the effect develops within the first 2 minutes, with a / m and / or injection - after 2-5 minutes and reaches a maximum after 5-15 minutes.
The duration of action is from 20-45 minutes after intravenous administration and 2.5-3 hours after IM and / or injection.
PHARMACOKINETICS

Distribution and Metabolism

It penetrates the GEB and the placental barrier.

Naloxone is metabolized in the liver with the formation of predominantly glucuronides.

Excretion

T 1/2 - about 1 hour (30-80 min).
In adults T 1/2 - about 64 ± 12 min; in newborns (after injection into the umbilical vein) - about 3.1 ± 0.5 h; in preterm infants - about 51.8 ± 9.2 min.
It is excreted through the kidneys.
Within 72 hours, 70% of the dose administered is excreted.
INDICATIONS

- acute poisoning (overdosage) of opioid analgesics (morphine, trimperidine, fentanyl) and other drugs in the mechanism of toxic effect of which there is an opioid component (opioid substitutes, methadone, pentazocine, buprenorphine, butorphanol, nalbuphine and others) in combination with other resuscitation measures;

- postoperative application: acceleration of the exit from general anesthesia, before the end of controlled breathing (the drug is used only if narcotic analgesics were used during the operation);

- to restore respiration in newborns after the introduction of opioid analgesics to the mother;

- as a diagnostic tool in patients with suspected opioid dependence (naloxone test).

DOSING MODE

The rate of Naloxone administration should be selected individually, depending on the patient's response to the use of naloxone and previously administered single doses.

Naloxone is used iv, in / m or s / k.

In case of infusion, Naloxone solution is diluted in 0.9% sodium chloride solution or in 5% dextrose solution as follows: 2 mg (5 ml of solution containing 400 μg / ml naloxone) is added to 500 ml of infusion medium.

The solution obtained after dilution contains 4 μg of naloxone in 1 ml.
The solution is prepared immediately before use.
The dose of Naloxone and the method of administration depend on the patient's condition, type and amount of opioid taken.

Acute poisoning (overdose) of opioid analgesics

Adults

The initial single dose is 400-2000 μg, which is injected iv slowly (within 2-3 min).
If necessary, the dose can be re-introduced after 2-3 minutes, until recovery of consciousness and even breathing. If after the introduction of a total dose of 10 mg there was no recovery of consciousness and breathing, we should assume another (non-opioid) cause of poisoning.
Naloxone can also be used in / m or s / k.
In menacing states of life, the IV route is preferred.
Children

The initial single dose is 10 μg / kg, which is injected iv slowly (for 2-3 min).
If necessary, an additional dose of 100 μg / kg can be administered after 2-3 minutes.
If it is impossible to apply naloxone IV, it is administered in / m or n / k fractional doses at intervals of 2-3 min.
With the / m introduction the effect of the drug manifests itself more slowly. Once a dose of about 200 μg (i.e., about 60 μg / kg) can be administered once, giving a longer duration of action.
Postoperative use: to accelerate the recovery from general anesthesia (if narcotic analgesics were used during the operation)

Adults

IV injection of the drug in a dose of 100-200 μg (1.5-3 μg / kg) every 2-3 minutes until the appearance of adequate pulmonary ventilation and awakening of the patient, but without distinct pain and discomfort.
A dose that exceeds the minimum required may cause analgesia to stop and increase blood pressure, as well as other symptoms: nausea, vomiting, increased sweating, discirculatory crisis. In some cases, especially after taking opioid analgesics with a long duration of action, an additional dose of naloxone should be given in / m for 1-2 hours. The drug is also injected with an IV infusion.
Children

In / in the drug administered at a dose of 10 mcg / kg.
If necessary, an additional dose of 100 mcg / kg can be administered.
If it is impossible to apply naloxone IV, it is administered in / m or n / k fractional doses at intervals of 2-3 min.
With the / m introduction the effect of the drug manifests itself more slowly. Once a dose of about 200 μg (i.e., about 60 μg / kg) can be administered once, giving a longer duration of action. The drug is also administered by IV infusion.
Restoration of respiration in newborns after the introduction of opioid analgesics to the mothers

Newborns

Before the introduction of the drug, it is necessary to check the patency of the respiratory tract of the newborn.

The drug is administered iv, in / m or s / c at a dose of 10 mcg / kg.
If necessary, the dose can be repeated after 2-3 minutes.
After the birth of a child, he can once in order to prevent the introduction of a 200 mcg (ie, about 60 mcg / kg) of naloxone.

As a diagnostic tool in patients with suspected drug (opioid) dependence

In / in a dose of 0.5 mcg / kg, it is possible to decide whether respiratory depression or difficulty in urinating with opioids is caused.
Then the dose of naloxone can be increased by avoiding too large doses. Large doses remove any action of the opioid, incl. and analgesic, and also lead to the excitation of systems of the sympathetic system and circulatory system.
SIDE EFFECT

When using the drug in the postoperative period: a decrease or increase in blood pressure, ventricular tachycardia and ventricular fibrillation, choking, pulmonary edema, cardiac arrest.
These effects sometimes lead to death, coma and encephalopathy. When using doses of the drug that exceed the minimum required, the disappearance of analgesia and psychomotor agitation may occur.
In case of sudden withdrawal of opioids, nausea, vomiting, sweating, tachycardia, increased blood pressure, tremors, convulsions, ventricular tachycardia and ventricular fibrillation, pulmonary edema and cardiac arrest may occur, which can lead to death.

The withdrawal syndrome in patients with opioid dependence: nausea, vomiting, diarrhea, weakness, tachycardia, increased blood pressure, fever, rhinitis (rhinitis), sneezing, goosebump (piloorexia), sweating, yawning, nervousness, anxiety, irritability, trembling, spasms in the epigastric region, pain of unclear localization;
in newborns - cramps, unrestrained crying, hyperreflexia.
CONTRAINDICATIONS

- Hypersensitivity to naloxone.

PREGNANCY AND LACTATION

During pregnancy and during breastfeeding, the drug should be used only in cases of acute need.

APPLICATION FOR FUNCTIONS OF THE LIVER

Caution should be exercised when using Naloxone in patients with impaired renal function.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

Caution should be exercised when using Naloxone in patients with impaired hepatic function.

APPLICATION FOR CHILDREN

Possible use according to the indications and in doses that take into account the age of the child.

Caution should be exercised when using Naloxone in childhood, as well as in newborns whose mothers have been shown to have an opioid dependence in history (sudden and complete withdrawal of the drug may cause an acute withdrawal syndrome).

SPECIAL INSTRUCTIONS

When Naloxone is used, oxygen therapy and resuscitation should be provided, as well as access to equipment that allows cardiopulmonary resuscitation.

Caution should be exercised when using Naloxone in patients with heart, lung, liver and / or kidney problems, pregnancy, lactation, childhood, in persons with established or suspected physical dependence on opioids, and in newborns whose mothers have been indicated in the anamnesis dependence on opioids (sudden and complete abolition of narcotic effect can cause acute withdrawal syndrome).

Carefully apply Naloxone in the treatment of respiratory depression caused by the use of buprenorphine.
response to the use of the drug may be incomplete. In this case, you should use mechanical ventilation. Because the duration of action of Naloxone is shorter than the duration of opioids, there is a risk of a decrease in respiratory activity.
Sudden abolition of opioids after surgery can cause nausea, vomiting, sweating, tremors, tachycardia and other symptoms.

Impact on the ability to drive vehicles and manage mechanisms

When using the drug, it is forbidden to operate vehicles and other moving mechanical devices.

OVERDOSE

There were no cases of acute overdose with Naloxone.

However, when the drug is administered at high doses (4 mg / kg and above), nausea, vomiting, chills, hyperventilation, convulsions, marked increase or decrease in blood pressure and / or bradycardia may occur.

When these symptoms appear, conservative treatment is recommended (in intensive care settings).

Doses of 2 mg / kg can cause cognitive impairment and behavioral symptoms, incl.
irritability, anxiety, tension, suspicion, depression, difficulty concentrating and lack of appetite. Behavioral symptoms can last 2-3 days.
Somatic symptoms can also be observed, such as dizziness, sweating, nausea and stomach pain, a feeling of heaviness.

Treatment is symptomatic.

DRUG INTERACTION

The drug reduces the hypotensive effect of clonidine.

Reduces the effect of opioid analgesics (including butorphanol, nalbuphine, pentazocine, fentanyl, remifentanil) and speeds up the appearance of withdrawal syndrome.

Methohexital (a short-acting barbituric acid derivative) blocks the acute onset of withdrawal caused by Naloxone in persons with drug dependence.

Naloxone should not be used iv with other drugs.

Incompatible with solutions of drugs containing bisulfites.

Pharmaceutically compatible with 0.9% sodium chloride solution, 5% dextrose solution, sterile water for injection.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.
It is used in a hospital.
TERMS AND CONDITIONS OF STORAGE

The drug should be stored in a place protected from light, inaccessible to children, at a temperature of no higher than 25 ° C.
Shelf life - 4 years.
Alphabetical index of medicines:
A  B  V  G  D  E  J
Z  I  Y  K  L  M  N
O  P  R  S  T  U  F
H  C  CH  SH  E  U  Y
Rambler's Top100
Privacy policy:
Copyright 2009 - 2017. Universal reference book of medicines. All rights reserved.
When using site materials, an active hyperlink is required!