Naloxone

Naloxone is a narcotic antagonist that does not have a morphine-like effect.

[1], [2], [3], [4]

Indications of the naloxone

It is shown mainly to eliminate acute poisoning by opiate analgesics. In addition, it can be used in case of development of a coma caused by alcohol in a person, and at the same time with various types of shock (this action is associated with the fact that in the case of development of certain types of stress or shock, the opioid system of the human body is activated, and in addition with the fact that Naloxone may contribute to an increase in reduced BP).

Since the drug effect of the substance is short-lived, this limits the ability to use it in the treatment of drug dependence.

[5], [6]

Release form

Issued in the form of an injection solution in ampoules of 1 ml. Inside, one package contains 10 ampoules.

[7], [8]

Pharmacodynamics

The medicine helps to prevent, reduce or eliminate the effects of narcotic agonists. In addition, it reduces the euphoric and sedative effect, increases the level of blood pressure and promotes recovery of respiratory function.

[9], [10], [11], [12],

Pharmacokinetics

In case of drug administration intravenously, its effect begins already in the first 2 minutes, and with subcutaneous or intramuscular injection - after a few minutes. The duration of the drug after IV injection is 20-45 minutes, and after SC or IM injections - 2.5-3 hours.

The half-life is approximately 1 hour. Metabolism is carried out in the liver, and excretion occurs with the help of the kidneys.

[13], [14], [15], [16], [17], [18], [19]

Dosing and administration

The drug should be administered intravenously (do it slowly: 2-3 minutes), as well as by subcutaneous or intramuscular route.

In case of drug intoxication, the initial dosage is 0.4 mg. If this is necessary, it is required to enter this dose repeatedly, keeping the intervals of 3-5 minutes, until spontaneous breathing is restored, and the patient does not regain consciousness. The maximum dose is 10 mg. The initial infant dosage is 0.005-0.01 mg / kg.

To accelerate the withdrawal from anesthesia used in surgical operations, an injection of 0.1-0.2 mg (about 1.5-3 μg / kg) is necessary at intervals of 2-3 minutes. Follow the procedure until the required pulmonary ventilation appears, and the patient wakes up. The pediatric dose is intravenous, 0.001-0.002 mg / kg, and if this does not work, repeat doses of up to 0.1 mg / kg at intervals of 2 minutes (until consciousness recovers and spontaneous breathing begins). If you can not do IV administration, you need to inject subcutaneously or intramuscularly. For newborns, the initial dosage is 0.01 mg / kg.

In the case of oppression of the respiratory process in newborns, which developed due to the introduction of opiate painkillers during childbirth, an injection of 0.1 mg / kg of the drug (by way of iv, in / m or s / k) is required. In the future, it is allowed to inject LS as an intramuscular injection in the amount of 0.2 mg (or 0.06 mg / kg).

To diagnose the patient's opioid addiction, you need to inject 0.8 mg of the drug intravenously.

[25], [26], [27], [28]

Use of the naloxone during pregnancy

Pregnant is prohibited from prescribing a medicine. Also, you should not breast-feed a baby while using the solution.

Contraindications

Contraindication against the use of medicinal solution is the intolerance of its active substance.

[20], [21]

Side effects of the naloxone

The introduction of the solution can cause such side effects:

• sensory organs, as well as NS: development of seizures or severe tremor;
• organs of the cardiovascular system, as well as the processes of hemostasis and hematopoiesis: the development of tachycardia, increased blood pressure and cardiac arrest;
• organs of the digestive tract: the occurrence of vomiting, as well as nausea;
• others: development of hyperhidrosis.

[22], [23], [24]

Interactions with other drugs

Naloxone weakens the antihypertensive properties of clonidine.

The drug weakens the effects of opiate pain medications (this list includes such drugs as nalbuphine, fentanyl, butorphanol, and pentazocine with remifentanil), and, at the same time, accelerates the development of a withdrawal syndrome in a patient.

The drug is incompatible with medicinal solutions, which include hydrosulphates.

It has a pharmaceutical compatibility with sodium chloride solution (0.9%), as well as dextrose (5%), and also with sterile injectable water.

[29]

Storage conditions

The solution must be kept in a place that is closed from sunlight, and also inaccessible to children. Temperature values are within 15-25 ° C.

[30],

Shelf life

Naloxone can be used in the period of 4 years since the release of the drug solution.

[31]