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Naloxone Hydrochloride Injection

Function and Efficacy

This product is a pure opioid receptor antagonist and has no intrinsic activity. However, it can competitively antagonize various opioid receptors and has a strong affinity for μ receptors. Naloxone takes effect quickly and has a strong antagonistic effect. Naloxone also reverses all effects of opioid agonists, including analgesia. In addition, it also has a recovery effect that is not related to antagonizing opioid receptors. It can quickly reverse the respiratory depression caused by opioid analgesics, cause high excitement, and cause cardiovascular hyperfunction. This product also has an anti-shock effect. It does not produce morphine-like dependence, withdrawal symptoms, and respiratory depression. Acute toxicity LD50 (mg/kg): mice, oral 565.

Ingredients

The main ingredient of this product is naloxone hydrochloride

Name Description Content CAS NO. Manufacturer
Naloxone hydrochlorideIngredients

A pure opioid receptor antagonist that competitively antagonizes all types of opioid receptors, has a strong affinity for μ receptors, can rapidly reverse the respiratory depression caused by opioid analgesics, induce high excitement, hyperactivity of cardiovascular function, has an anti-shock effect, and does not produce morphine-like dependence, withdrawal symptoms, and respiratory depression.

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357-08-4 32

Appearance

This product is a colorless clear liquid.

Indication

This product is the most widely used opioid receptor antagonist in clinical practice. It is mainly used for: 1. Rescue acute poisoning by narcotic analgesics, antagonize the respiratory depression of this type of drug, and awaken the patient. 2. Antagonize the residual effects of narcotic analgesics. Newborns are affected by narcotic analgesics in their mothers and suffer respiratory depression, which can be antagonized by this product. 3. Rescue acute ethanol poisoning: intravenous injection of naloxone 0.4-0.6mg can awaken the patient. 4. For those suspected of being addicted to narcotic analgesics, intravenous injection of 0.2-0.4mg can stimulate withdrawal symptoms and has diagnostic value. 5. Awakening effect, which may activate the physiological awakening system through cholinergic effects to awaken the patient, and is used for general anesthesia awakening and anti-shock and some comatose patients.

Usage and Dosage

Common dosage: naloxone 5μg/kg, wait 15 minutes and then intramuscularly inject 10μg/kg. Or first give a loading dose: 1.5-3.5μg/kg, and maintain at 3μg/kg/h. In detoxification treatment, intramuscular or intravenous injection: 0.4-0.8mg each time. In the process of quitting with methadone, you can try a small dose of methadone (5-10mg per day), give naloxone 1.2mg every half hour for several hours (3-6 hours), and then switch to naloxone. Use it 3 times a week to achieve the purpose of quitting.

Adverse Reactions

Adverse reactions to this product are rare, but may occasionally cause drowsiness, nausea, vomiting, tachycardia, hypertension and irritability.

Precautions

Not yet clear

Special Population Medication

Precautions for children: Using this product on sick children or newborns can reverse the effects of opioids. Children with opioid poisoning react strongly to this product, so they need to be closely monitored for at least 24 hours until the product is completely metabolized. Precautions during pregnancy and lactation: 1. The doses of reproductive toxicity tests on mice and rats were 4 to 8 times the usual human dose, and the results did not show that naloxone was embryotoxic or teratogenic. Since there are no sufficient and effective studies in pregnant women, pregnant women should only consider using the drug when necessary. 2. Maternal dependence is often accompanied by fetal dependence, so the risk to the fetus should be considered before using this product on women with known or suspected opioid dependence. Naloxone can cross the placenta and induce withdrawal symptoms in the mother and fetus. Patients with mild to moderate hypertension should be closely monitored when using naloxone during labor to avoid severe hypertension. 3. It is not clear whether this product will affect labor and/or delivery time. However, published studies have shown that the use of naloxone during labor will not have adverse effects on mothers and newborns. 4. It is not clear whether this product will be secreted through human milk. Because the drug may be secreted into human milk, this product should be used with caution in breastfeeding women. Elderly precautions: There are not enough clinical trials of this product in patients aged 65 years and over, and no difference in the response of elderly patients to naloxone was found between younger patients and elderly patients. In general, the dose selection for elderly patients should be cautious, and the drug should be started at a low dose, considering the high probability of decreased liver, kidney or heart function and concomitant diseases or other drug treatments.

Drug Interactions

Not yet clear

Storage

Seal and store in a cool place.

Packaging Specification

1ml:0.4mg

Validity Period

24 months

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