Naloxone Hydrochloride for Injection

This product is an opioid receptor antagonist. It has almost no pharmacological activity itself, but it can competitively antagonize various opioid receptors and has a strong affinity for m receptors. (I) Pharmacological action 1. Completely or partially correct the central inhibitory effects of opioids, such as respiratory depression, sedation and hypotension. 2. It has a wake-promoting effect on acute ethanol poisoning in animals. 3. It is a pure opioid receptor antagonist, that is, it does not have the "excitability" or morphine-like effects of other opioid receptor antagonists; it does not cause respiratory depression, psychotomimetic reactions or pupil constriction reactions. 4. No drug resistance is observed, nor is there any physiological or mental dependence. 5. Although the mechanism of action is not yet fully understood, there is sufficient evidence to show that it antagonizes the effects of opioids by competing for the same receptor sites. (II) Clinical pharmacology In a clinical study organized by the Chinese Society of Neurosurgery and the Chinese Journal of Neurosurgery, 18 large hospitals across the country (including neurological specialty hospitals) conducted a double-blind randomized controlled clinical study on the treatment of acute craniocerebral injury with naloxone injection. A total of more than 500 cases were completed. The experimental group added this product to the basic treatment plan. The dosage was 0.3mg/kg/body weight/day. After diluting it to 500ml with normal saline or balanced solution, it was continuously dripped for 24 hours using an infusion pump. After 3 consecutive days of use, the dosage was uniformly reduced to 4.8mg/day, and the drug was stopped after 7 consecutive days. Results Compared with the placebo control group that did not add this product but only used basic treatment, the mortality rate of the experimental group was 12.5%, and that of the placebo control group was 17.3%. There was a significant difference between the two groups, and the GCS score, GOS score, language motor function and quality of life score of the experimental group were significantly better than those of the placebo group. During the treatment period, a total of 8 patients developed liver and kidney dysfunction to varying degrees after taking the medicine, but there was no evidence to prove that it was related to the medicine. (III) Toxicology 1. For single-dose intravenous administration, the LD50 of rats and mice is 150mg/kg and 109mg/kg respectively; for single-dose subcutaneous injection, the LD50 of newborn rats is 260mg/kg. 2. No animal experiments have been conducted to evaluate the carcinogenicity of this product. 3. Fertility experiments on mice and rats with 50 times the human dose of this product showed no impairment of fertility.

Main ingredients: Naloxone hydrochloride, auxiliary materials are mannitol, sodium dihydrogen phosphate, disodium hydrogen phosphate. Chemical name: 17-allyl-4,5a-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride dihydrate. Chemical structure: Molecular formula: C19H21NO4·HCl·2H2O Molecular weight: 399.87

This product is an opioid receptor antagonist. 1. Used after opioid combined anesthesia to antagonize the respiratory depression caused by such drugs and promote patient awakening. 2. Used for opioid overdose to completely or partially reverse the respiratory depression caused by opioids. 3. Rescue acute ethanol poisoning. 4. Used for the diagnosis of acute opioid overdose.

Because this product has obvious individual differences, the dosage and whether multiple administrations are required should be determined by the doctor according to the specific situation of the patient. This product can be administered by intravenous infusion, injection or intramuscular injection. Intravenous injection is the fastest and is suitable for emergency use. Because the duration of action of some opioids may exceed that of this product, the patient should be continuously monitored and the product should be given repeatedly if necessary. Intravenous infusion This product can be diluted with normal saline or glucose solution. Add 2mg of this product to 500ml of any of the above liquids to a concentration of 0.004mg/ml. The mixed solution should be used within 24 hours, and the remaining mixed solution that has not been used for more than 24 hours must be discarded. Control the drip rate according to the patient's response. For adults who use opioids for the first time, 0.4mg~2mg of this product can be injected intravenously. If the ideal antagonism and improvement of respiratory function are not achieved, the injection can be repeated every 2~3 minutes. If there is no reaction after giving 10mg, this diagnostic problem should be considered. If intravenous administration is not possible, intramuscular administration can be used. Postoperative opioid inhibitory effect Partial correction of the opioid inhibitory effect after the use of opioids in surgery, usually a smaller dose of this product is effective. The dosage of this product should be determined according to the patient's response. When correcting respiratory depression for the first time, 0.1mg~0.2mg should be injected intravenously every 2~3 minutes until the ideal effect is achieved, that is, unobstructed breathing and wakefulness, without obvious pain and discomfort. This product can significantly reverse analgesia and increased blood pressure when it is greater than the necessary dose. Similarly, reversal too quickly can cause nausea, vomiting, sweating or increased circulatory burden. The amount of this product that needs to be repeated within a time interval of 1 to 2 hours depends on the dose of the last opioid used, the type of administration (short-acting or long-acting) and the interval. Severe ethanol poisoning 0.8mg~1.2mg, repeated administration of 0.4mg~0.8mg after one hour. The first dose of pediatric intravenous injection of opioid overdose is 0.01mg/kg. If this dose does not achieve a satisfactory effect in clinical practice, 0.1mg/kg should be given next. If intravenous injection is not possible, intramuscular injection can be given in divided doses. For postoperative opioid depressant effects, refer to the recommendations and precautions under adult postoperative opioid depressant. When correcting respiratory depressant effects for the first time, 0.005 mg to 0.01 mg of this product is injected intravenously every 2 to 3 minutes until the desired degree of reversal is achieved. The usual initial dose of opioid-induced depression for neonatal use is 0.01 mg per kilogram of body weight by intravenous, intramuscular or subcutaneous injection. This dose can be repeated according to the instructions for postoperative opioid depressant in adults. The naloxone challenge test is used to diagnose suspected opioid tolerance or acute opioid overdose. Inject 0.2 mg of this product intravenously and observe for 30 seconds to see if symptoms and signs of opioid withdrawal appear. If not, inject 0.6 mg each time and observe for another 20 minutes. This product should not be given to patients with obvious withdrawal symptoms and signs, or patients with opioids in the urine. Some patients, especially opioid-tolerant patients, react to low doses of this product, and intravenous injection of 0.1 mg of this product can play a diagnostic role.

Adverse reactions of this product in postoperative patients are occasionally: hypotension, hypertension, ventricular tachycardia and ventricular fibrillation, dyspnea, pulmonary edema and cardiac arrest. The sequelae of death, coma and encephalopathy have been reported. Overdose of this product in postoperative patients may reverse analgesia and cause patient agitation. Reversal of opioid inhibition A sudden reversal of opioid inhibition may cause nausea, vomiting, sweating, palpitations, increased blood pressure, shivering, seizures, ventricular tachycardia and ventricular fibrillation, pulmonary edema and cardiac arrest, and may even lead to death. Opioid dependence A sudden reversal of the opioid effect in patients who are physically dependent on opioids may cause acute withdrawal syndrome, including but not limited to the following symptoms and signs: body pain, fever, sweating, runny nose, sneezing, piloerection, yawning, weakness, chills or tremors, nervousness, restlessness or irritability, dysentery, nausea or vomiting, abdominal cramps, increased blood pressure, palpitations. In neonates, symptoms of opioid withdrawal may include: convulsions; excessive crying; hyperreflexia. Adverse reactions to postoperative use of this drug and dose reduction are classified by organ system as follows: Cardiac: pulmonary edema, cardiac arrest or failure, hypercardia, ventricular fibrillation, and ventricular tachycardia. Death, coma, and encephalopathy have been reported as sequelae. Gastrointestinal: vomiting, nausea. Nervous: convulsions, paresthesias, grand mal seizures. Psychiatric: agitation, hallucinations, tremors. Respiratory, thoracic, and diaphragmatic: dyspnea, respiratory depression, hypoxia. Skin and subcutaneous injections: nonspecific injection site reactions, sweating. Vascular disorders: hypertension, hypotension, hot flashes or redness.

Patients who are allergic to this product are contraindicated.

Precautions for children: 1. The use of this product in children or newborns can reverse the effects of opioids. Children with opioid poisoning have a strong reaction to this product, so they need to be closely monitored for at least 24 hours until the product is completely metabolized. 2. If this product is used for mothers shortly after delivery, the effect on prolonging the life of newborns can only last for 2 hours. If necessary, this product can be used directly for newborns after delivery. Precautions during pregnancy and lactation: 1. The doses of reproductive toxicity tests on mice and rats are 4 to 8 times the usual human dose. The results did not show that naloxone has embryotoxicity or teratogenicity. Since there are no sufficient and effective studies in pregnant women, pregnant women should consider using the drug only when necessary. 2. Maternal dependence is often accompanied by fetal dependence, so the risk to the fetus should be considered before using this product in pregnant women with known or suspected opium dependence. Naloxone can cross the placenta and induce withdrawal symptoms in mothers and fetuses. Patients with mild to moderate hypertension who use naloxone during labor should be closely monitored 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 is secreted through human milk. Because the drug may be secreted into human milk, breastfeeding women should use this product with caution. Elderly precautions: There are not enough clinical trials of this product in patients aged 65 and over. No difference in the response of elderly patients to naloxone was found between young patients. In general, the dose selection for elderly patients should be cautious, considering the higher probability of reduced liver, kidney or heart function and concomitant diseases or other drug treatments. The medication should be started at a low dose.

1. The low binding rate and slow dissociation rate of buprenorphine to opioid receptors determine its long duration of action. Therefore, a large dose of naloxone should be used to antagonize the effects of buprenorphine. The antagonism of buprenorphine needs to be gradually enhanced to reverse the effect and shorten the duration of respiratory depression. 2. Methynilbarbital can block the acute withdrawal symptoms induced by naloxone in opioid addicts. 3. This product should not be mixed with preparations containing sodium bisulfate, sodium bisulfite, long-chain polymer anions or any alkaline. Before adding drugs or chemical reagents to the solution of this product, its effect on the chemical and physical stability of the solution should be determined first.

Keep away from light and store in a sealed container.

1mg

24 months

Chengdu Easton Bio Pharmaceuticals Co., Ltd.

• Founded in:

  2009-06-01

• Address:

  No. 8, Xiyuan Avenue, Chengdu Hi-tech Zone

• Tax NO.:

  91510100689030428K

• Registered Funds:

  176.532256 million yuan

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