Naloxone

Active material: Naloxone
When ATH: V03AB15
CCF: Competitive antagonist opioid receptors
ICD-10 codes (testimony): T40.2, Z51.4
When CSF: 02.19.01
Manufacturer: WARSAW PHARMACEUTICAL WORK POLFA S.A. (Poland)

Pharmaceutical form, composition and packaging

Excipients: sodium chloride, hydrochloric acid, water d / and.

1 ml – ampoule (10) – packs cardboard.

Pharmacological action

Competitive antagonist opioid receptors. Blocks mostly Mu-receptors, to a lesser extent, affects the other opioid receptors, and eliminates both the endogenous opioid peptides, and exogenous opioid analgesics.

Introduction of naloxone prevent, weakens or eliminates (Depending on the dose and time of introduction) effects of opioid analgesics, Restores the breath, reduces sedative effect and euphoria, ters gipotenzivny effect.

On psihomimetičeskie effects and disforiu, caused by opioid analgesics group agonist-antagonists (pentazocin, butorphanol), Naloxone has no actions expressed. Inefficient as the antagonist of tramadol. Not completely eliminates the effects of buprenorphine.

Naloxone provokes withdrawal symptoms in patients with opioid dependence.

When in/with the introduction of the drug begins during the first 2 m, When the/m and s/to the introduction – through 5-15 m. Duration is 20-45 minutes after the on/in the introduction and 2.5-3 no – following in/m or m/to the introduction.

Pharmacokinetics

Metabolism and excretion

Naloxone biotransformiroetsa in the liver with the formation of glucuronides. T_1/2 is about 1 no. Report the news.

Testimony

-acute poisoning opioid analgesics (morphine, promedol, Fentanyl) and other drugs, the mechanism of toxicity that has opioid component (methadone, pentazocin, buprenorphine, butorphanol, nalʙufin) in conjunction with other hospital emergency rooms activities;

— Anesthesiology for termination of morfinopodobnyh analgesics during operation under special circumstances;

— to restore breathing in newborns after the introduction of the mother of opioid analgesics;

— as a diagnostic tool in patients with suspicion of opioid dependence (naloksonovaâ sample).

Dosage regimen

Dose and route of Administration depend on the patient's condition and the number of opioid agonist, located in the body.

At poisoning of opioid analgesics the initial dose of naloxone is 0.4-2 mg / slow (during 2-3 m), / m or s / c. When life-threatening conditions in preferred/route of administration. Repeated doses can be administered through 2-5 minutes before the emergence of consciousness and recovery of spontaneous breathing. If after entering a total dose of Naloxone 10 mg does not recover consciousness and breathing, You should think of another (neopioidnoj) because of poisoning.

The initial dose for children is 5-10 ug / kg body weight. Optionally there may be repeated injection.

To accelerate the exit of surgical anesthesia Naloxone designate smaller doses – from 100 to 200 g (1.5-3 mg / kg) every 2-3 minutes before the appearance of adequate pulmonary ventilation and the awakening of the patient, but without a distinct pain and discomfort. Dose greater than the minimum required could cause analgesia and raising HELL, as well as other symptoms – nausea, vomiting, increased sweating, discirkulâtornyj Kriz.

The initial dose of naloxone for children is 1-2 µg/kg body weight/. If the desired effect is not, Re-misleading drug in doses up to 100 µg/kg body weight every 2 m, before the advent of spontaneous breathing and restoring consciousness. When the impossibility of holding/in the injections of the drug is injected in/m or m/to fractional doses.

To Newborn starting dose is 10 ug / kg body weight. Introduction can be repeated in accordance with the principles of the adults with postoperative oppression breathing with the use of opioid analgesics.

At respiratory depression, caused by the introduction of opioid analgesics parturient mothers during anesthesia, newborns injected Naloxone in dose 1-2 µg/kg body weight/m, n / a or I /. If the desired effect is not, Re-misleading drug in the dose to 100 µg/kg body weight every 2 minutes before the appearance of spontaneous breathing and restoring consciousness. Before the introduction of the product to ensure patency of the airway in the newborn. Possibly preventive in/m introduction 200 g (60 ug / kg body weight) Naloxone.

With the aim of diagnosis of opioid dependence I / O is introduced 800 mcg Naloxone and monitor the condition of the patient, with the aim of identifying signs of the syndrome.

Side effect

Rapid reverse development drug oppression when you use Naloxone can be accompanied by various reactions.

From the digestive system: nausea, vomiting.

Cardio-vascular system: tachycardia, arterial hypertension, cardiac arrest.

CNS: tremor, convulsions.

Other: increased sweating.

When used in therapeutic doses in patients, in the body that contains no opioids, Naloxone does not usually cause side effects.

When you use Naloxone in doses in the postoperative period, exceeding the minimum required, Perhaps disappearance of analgesia and arousal, hypotension, arterial hypertension, ventricular tachycardia, fibrillation, pulmonary edema.

Syndrome in patients with opioid dependence: unspecified pain localization, diarrhea, hyperthermia, rhinorrhea, chikhaniye, “goose bumps”, Sweating, nausea, vomiting, fatigue, tremor, pain in epigastralna area; in newborn – convulsions, diarrhea, hyperthermia, unrestrained weeping, hyperreflexia, chikhaniye, tremor, expressed irritability, vomiting.

Contraindications

- Hypersensitivity to the drug.

Pregnancy and lactation

Be wary used Naloxone in pregnancy.

Unknown, is allocated whether naloxone with breast milk. Use of the drug during lactation (breast-feeding) perhaps on absolute grounds.

Cautions

The duration of some opioid analgesics may exceed the duration of action of naloxone, Therefore, patients should be under constant medical supervision and in the conditions of, allowing VENTILATION and other resuscitation.

Naloxone is inefficient when oppression breath, caused by non-opioid drugs.

The drug does not cause the development of addiction and the formation of drug dependence.

Overdose

Currently, the drug overdose Naloxone lacking.

Drug Interactions

Reduces the effect of opioid analgesics (incl. butorphanol, Fentanyl, pentazocin, nalʙufin, remifentanil) and accelerates the emergence of the syndrome.

While applying Naloxone can reduce antihypertensive action of clonidine.

Not compatible with the solution of medicines, containing bisul′faty.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. Shelf life – 4 year.