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Name | NALOXONE HYDROCHLORIDE INJECTION |
Pinyin name | YANSUAN NALUOTONG ZHUSHEYE |
Drug category | Antipyretic analgesics and non-steroidal anti-inflammatory analgesics |
Character | This product is a colorless clear liquid. |
Pharmacology and toxicology | This product is a pure opioid receptor antagonist and has no intrinsic activity. But it can competitively antagonize various opioid receptors and has a strong affinity for receptors. Naloxone works quickly and has strong antagonistic effects. Naloxone simultaneously reverses all the effects of opioid agonists, including analgesia. In addition, it also has an estrogen effect that is not related to antagonizing opioid receptors. It can quickly reverse the respiratory depression caused by opioid analgesics, can cause high excitement, and increase cardiovascular function. This product still has anti-shock effect. Does not produce morphine-like dependence, withdrawal symptoms, and respiratory depression. Acute toxicity LD50 (mg / kg): Mice, 565 orally. |
Pharmacokinetics | This product is not effective orally and must be administered by injection. The maximum effect is 1 to 3 minutes after intravenous injection, which lasts 45 minutes; the maximum effect is 5 to 10 minutes after intramuscular injection, which lasts 2.5 to 3 hours. This product absorbs quickly, easily penetrates the blood-brain barrier, and has rapid metabolism. The T1 / 2 of human plasma is 30 to 78 minutes. It is mainly biotransformed in the liver, and the product is excreted with urine. |
Indication | This product is currently the most widely used opioid receptor antagonist. Mainly used for: 1. Rescue acute poisoning of narcotic analgesics, antagonize the respiratory depression of such drugs, and make patients awake. 2. Antagonistic Residual Effects of Narcotic Analgesics. Respiratory depression in newborns affected by narcotic analgesics in their mothers can be antagonized with this product. 3 Rescue acute alcoholism: Intravenous naloxone 0.4 0.6mg can make patients awake. 4 For suspected narcotic analgesics addicts, intravenous injection of 0.2 to 0.4 mg can stimulate withdrawal symptoms, which has diagnostic value. 5. Arousal effect, may activate the physiological arousal system through cholinergic effect to make patients awake, used for general anesthesia and anti-shock and some coma patients. |
Dosage | Commonly used dose: 5 g / kg of naloxone, 15 g / kg intramuscularly after 15 min. Or first load: 1.5 ~ 3.5g / kg, maintained at 3g / kg · h. Intramuscular injection or intravenous injection: 0.4 0.8mg each time. In the process of withdrawal from methadone, you can try a small dose of methadone (5-10mg per day), give 1.2mg of naloxone every half hour for several hours (3-6 hours), and then switch to naloxone and use it weekly Rejection can be achieved 3 times. |
Adverse reactions | Adverse reactions to this product are rare, and occasionally drowsiness, nausea, vomiting, tachycardia, hypertension and irritability may occur. |
Contraindications |
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Precautions | 1. After applying naloxone to antagonize high-dose narcotic analgesics, high levels of excitement can occur as the pain returns. It is manifested by increased blood pressure, increased heart rate, arrhythmia, and even pulmonary edema and ventricular fibrillation. 2. Due to the short duration of action of this drug, once the effect of the drug has disappeared, the patient can fall into lethargy and respiratory depression again. Care should be taken to maintain the efficacy of the medication. 3 Use with caution in patients with cardiac insufficiency and hypertension. |
Medication for pregnant and lactating women | still uncertain. |
Medication for children |
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Medication for elderly patients |
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medicine interactions | still uncertain. |
Drug overdose |
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Store | Keep it tightly closed in a cool and dark place. |
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Expiration date |
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