Naloxone Hydrochloride for Injection
Function and Efficacy
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.
Ingredients
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
| Name | Description | Content | CAS NO. | Manufacturer |
|---|---|---|---|---|
| Naloxone hydrochlorideIngredients |
This product is an opioid receptor antagonist, which has almost no pharmacological activity itself, but can competitively antagonize various opioid receptors and has a strong affinity for m receptors. It can completely or partially correct the central inhibitory effects of opioid substances, such as respiratory depression, sedation and hypotension; it has a wake-up effect on animals with acute ethanol poisoning; it is a pure opioid receptor antagonist and does not cause respiratory depression, psychotomimetic reactions or miotic reactions; there is no drug resistance, nor physiological or mental dependence. More |
357-08-4 | 32 | |
| MannitolExcipients |
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. More |
87-78-5 | 31 | |
| Sodium dihydrogen phosphateExcipients |
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. More |
89140-32-9 | 9 | |
| Sodium Phosphate, DibasicExcipients |
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. More |
7558-79-4 | 20 |
Indication
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.
Usage and Dosage
Because this product has obvious individual differences, the dosage and whether multiple doses are needed should be determined by the doctor based on the patient's specific situation. This product can be administered by intravenous infusion, injection or intramuscular injection. Intravenous injection is the fastest and is suitable for use in emergencies. Because the duration of action of some opioids may exceed that of this product, the patient should be monitored continuously and the product should be given repeatedly if necessary. Intravenous infusion This product can be diluted with normal saline or glucose solution. Add 2 mg of this product to 500 ml of any of the above liquids to a concentration of 0.004 mg/ml. The mixed solution should be used within 24 hours, and any 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 adult use: This product can be injected intravenously for the first time in the event of an opioid overdose.
Adverse Reactions
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.
Precautions
Patients who are allergic to this product are contraindicated.
Drug Interactions
Postoperatively, patients occasionally experience adverse reactions to this drug: hypotension, hypertension, ventricular tachycardia and ventricular fibrillation, dyspnea, pulmonary edema and cardiac arrest. Sequelae such as death, coma and encephalopathy have been reported. Overdose of this drug in postoperative patients may reverse analgesia and cause patient agitation. Reversal of opioid inhibition. 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. Patients who are physically dependent on opioids and suddenly have their opioid effects reversed may experience acute withdrawal syndrome, including but not limited to the following symptoms and signs: body pain, fever, sweating, runny nose, sneezing, piloerection, yawning.
Storage
Keep in a sealed container
Packaging Specification
0.8mg
Manufacturer
Sinopharm A-Think Pharmaceutical Co., Ltd.
-
Founded in:
1997-12-10 -
Address:
No. 111, Yixin Road, Shuangyang Economic Development Zone, Changchun -
Tax NO.:
912201012440638092 -
Registered Funds:
100 million yuan -
Website:
-
Email: