What Is Naloxone Hydrochloride?

It is suitable for acute poisoning of narcotic analgesics and acute poisoning of alcohol. It is used for respiratory depression and coma caused by known or suspected opioid overdose. It can also be used for the differential diagnosis of opioid addicts. And it absorbs quickly, easily penetrates the blood-brain barrier, and metabolizes quickly. The effect lasts 45 to 90 minutes.

Naloxone hydrochloride

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It is suitable for acute poisoning of narcotic analgesics and acute poisoning of alcohol. It is used for respiratory depression and coma caused by known or suspected opioid overdose. And it absorbs quickly, easily penetrates the blood-brain barrier, and metabolizes quickly. The effect lasts 45 to 90 minutes.

Chinese name

Naloxone hydrochloride

Foreign name

NALOXONE HYDROCHLORIDE INJECTION

Drug alias

Suno

Character

This product is a colorless clear liquid

Drug category

Antipyretic analgesics and non-steroidal anti-inflammatory analgesics

[Drug name] Naloxone Hydrochloride

[Drug alias] Suno

[Molecular formula composition] 17-allyl-4,5-epoxy-3,14-dihydroxymorphinan-6 ketone hydrochloride

[Specifications] Injection: 1ml: 0.04mg, 1ml: 0.4mg. This product is a colorless clear liquid

[Pharmacokinetics] Orally absorbable, but the first pass effect is large. It is effective within 2min of intravenous injection, and can quickly cross the blood-brain barrier. Intramuscular, subcutaneous, sublingual or intratracheal administration is slightly later than intravenous injection. T1 / 2 is 60min 90min, and is metabolized in the liver. Intravenous and intratracheal administration of this product for 1 to 3 minutes, intramuscular injection or subcutaneous injection for 5 to 10 minutes produces effects. This product absorbs quickly, easily penetrates the blood-brain barrier, and has rapid metabolism. The effect lasts 45 to 90 minutes. Plasma half-life is 90 minutes, and oral absorption is poor.

[Indications] Acute poisoning of narcotic analgesics and acute poisoning of alcohol are the first choice for respiratory depression and coma due to known or suspected opioid overdose. It can also be used for the differential diagnosis of opioid addicts.

[Adverse reactions] There are increased blood pressure, increased heart rate, chest tightness, tremor, nausea, and vomiting.

[Usage and Dosage] Subcutaneous, intramuscular, or intravenous injection, opioid overdose, 0.4 mg (or 10 (g / kg) / time) for adults, can be repeated once in 2 to 3 minutes; postoperative caused by opioids Respiratory depression, each time according to the weight of 1.3 (g ~ 3 (g / kg.) Differential diagnosis of opioid dependence, intramuscular injection of 0.4mg / time, no response within 20 to 30 minutes can be injected again. Severe alcoholism, intramuscular Or intravenous injection of 0.8mg to 1.2mg, repeated administration of 0.4mg to 0.8mg after 1h.

Method name: Determination of Naloxone Hydrochloride-Neutralization Titration

Application range: This method uses titration to determine the content of naloxone hydrochloride.

This method is applicable to naloxone hydrochloride.

Principle of the method: Add the test solution with mercury acetate solution to dissolve, add glacial acetic acid, acetic anhydride, and crystal violet indicator solution, and titrate with perchloric acid titration solution (0.1mol / L) until the solution is blue-green, record the perchloric acid titration The amount of fluid used is calculated.

Reagent: 1. Water (new boiling to room temperature)

2. Perchloric acid titrant (0.1mol / L)

3. Crystal violet indicator liquid

Glacial acetic acid

5. Acetic anhydride

6. Glacial acetic acid

7. Mercury acetate test solution

8. Reference potassium hydrogen phthalate

equipment:

Sample preparation: 1. Perchloric acid titration solution (0.1mol / L)

Preparation: Take 750mL of anhydrous glacial acetic acid (calculated with water content, add 5.22mL acetic anhydride per 1g of water), add 8.5mL perchloric acid (70% -72%), shake well, and slowly add acetic anhydride dropwise at room temperature. 23mL, shake while adding, shake evenly after adding, let cool, add an appropriate amount of anhydrous glacial acetic acid to 1000mL, shake well, and leave for 24 hours. If the test sample is easily acetylated, the water content on this page must be determined by moisture measurement, and then the water content of this solution should be adjusted to 0.01% -0.2% with water and acetic anhydride.

Calibration: Take about 0.16g of standard potassium hydrogen phthalate dried to constant weight at 105 , accurately weigh, add 20mL of anhydrous glacial acetic acid to dissolve, add 1 drop of crystal violet indicator solution, and titrate slowly with Blue, and the results of the titration are corrected with a blank test. Each 1mL of perchloric acid titration solution (0.1mol / L) is equivalent to 20.42mg of potassium hydrogen phthalate. Calculate the concentration of this solution based on the consumption of this solution and the amount of potassium hydrogen phthalate taken.

Storage: Place in a brown glass bottle and keep tightly closed.

Crystal violet indicator liquid

Take 0.5g of crystal violet, add 100mL of glacial acetic acid to dissolve, and get.

Operation steps: Accurately weigh 0.3g of the test sample, add 10mL of mercury acetate test solution to dissolve, add 40mL of glacial acetic acid, 10mL of acetic anhydride and 1 drop of crystal violet indicator solution, and use perchloric acid titration solution (0.1mol / L) The titration solution was blue-green, and the results of the titration were corrected by a blank test. The volume of perchloric acid titrant consumed (mL) was recorded. Each 1 mL of perchloric acid titrant (0.1 mol / L) was equivalent to 36.38 mg of sodium chloride. Complex ketone (C19H21NO4 · HCl).

Note 1: "Precision weighing" means that the weighed weight should be accurate to one thousandth of the weight. Precision requirements.

References: Pharmacopoeia of the People's Republic of China, compiled by the National Pharmacopoeia Committee, Chemical Industry Press, 2005 edition, Part Two, p.524.

Pregnancy class B. For opioid-dependent persons, severe withdrawal symptoms can be promptly triggered, and the patient's medication history should be noted. This product is independent, and used with caution in patients with cardiac dysfunction and hypertension. Those who are negative in this product's identification test cannot rule out positive opioid dependence.

Used name
English 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
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
Medication for elderly patients
medicine interactions	still uncertain.
Drug overdose
Store	Keep it tightly closed in a cool and dark place.
package
Expiration date