Isoniazid Injection

[Pharmacology and Toxicology] This product is an anti-tuberculosis drug. Isoniazid has a highly selective antibacterial effect on all types of Mycobacterium tuberculosis. It is the synthetic antibacterial drug with the strongest bactericidal effect among the current anti-tuberculosis drugs, and has almost no effect on other bacteria. It has a strong effect on Mycobacterium tuberculosis in the growth and reproduction period, and a weak and slow effect on the dormant period. Its mechanism of action may be to inhibit the synthesis of mycolic acid in sensitive bacteria and cause cell wall rupture. [Pharmacokinetics] This product is rapidly absorbed from the gastrointestinal tract after oral administration. It can be widely distributed in tissues and body fluids throughout the body and can pass through the placental barrier. The concentration in normal cerebrospinal fluid can reach 20% of the blood drug concentration. When the meninges are inflamed, the cerebrospinal fluid concentration is almost equal to the blood drug concentration. This product can penetrate into tuberculosis cavities and cheesy substances. This product can quickly enter the fetal circulation, and the concentration in breast milk is almost equal to the blood drug concentration. The concentration is also high in the liver and skin, and it is also easy to enter pleural effusion, ascites, saliva, and bile. The protein binding rate is 0-10%. This product is mainly acetylated in the liver to form inactive metabolites, some of which are hepatotoxic. 70% of the dose is excreted through the kidneys within 24 hours, most of which are inactive metabolites. 93% of the fast acetylated metabolites are excreted from the urine in the acetylated form, and 63% of the slow acetylated metabolites. It can also be excreted from breast milk, saliva, sputum and feces. A considerable amount of this product can be removed by hemodialysis and peritoneal dialysis.

The main ingredient of this product is isoniazid.

This product is a colorless or slightly yellow clear liquid.

It is used in combination with other anti-tuberculosis drugs to treat various types of tuberculosis and some non-tuberculous mycobacterial diseases.

1. Intramuscular injection, intravenous injection or intravenous drip: Intramuscular injection is rarely used in China. Generally, intravenous drip is used during the intensive period or for patients with severe illness or who cannot take oral medication. It is used after dilution with sodium chloride injection or 5% glucose injection. (1) Adults 0.3-0.4g or 5-10mg/kg per day; children 10-15mg/kg per day according to body weight, not more than 0.3g per day. (2) For patients with acute miliary tuberculosis or tuberculous meningitis, adults 10-15mg/kg per day, not more than 0.9g per day. (3) When using intermittent therapy, adults 0.6-0.8g each time, 2-3 times a week. 2. Local medication (1) Nebulization inhalation: 0.1-0.2g each time, twice a day.

The incidence of adverse reactions at commonly used doses is low. When the dose is increased to 6 mg/kg, the incidence of adverse reactions increases significantly, mainly peripheral neuritis and liver toxicity. Although the addition of vitamin B6 can reduce toxic reactions, it can also affect the efficacy. 1. Liver toxicity: This product can cause mild transient liver damage such as elevated serum aminotransferase and jaundice, with an incidence of about 10% to 20%. Liver toxicity is related to the metabolite of this product, acetylhydrazine. For those who are fast acetylated, acetylhydrazine accumulates more in the liver, so it is easy to cause liver damage. Drinking alcohol during medication can increase liver damage. Toxic reactions are manifested as poor appetite, abnormal fatigue or weakness, nausea or vomiting (prodromal symptoms of liver toxicity) and dark urine, yellow eyes or skin (liver toxicity). 2. Nervous system toxicity: Peripheral neuritis is more common in those who are slow acetylated, and has a significant relationship with the dose. Many patients show unsteady gait, numbness, tingling, burning sensation or pain in the hands and feet. This reaction is more likely to occur in lead poisoning, arteriosclerosis, hyperthyroidism, diabetes, alcohol poisoning, malnutrition and pregnant women. Other toxic reactions such as excitement, euphoria, insomnia, loss of autonomy, toxic encephalopathy or toxic psychosis are rare, and severe toxic reactions such as optic neuritis and atrophy are occasionally reported. 3. Allergic reactions include fever, polymorphic rash, lymphadenopathy, vasculitis, etc. Once they occur, the drug should be stopped immediately. If it is necessary to use it again, it should be started with a small dose and gradually increased. 4. The blood system may have granulocytopenia, eosinophilia, thrombocytopenia, methemoglobinemia, etc. 5. Others such as dry mouth, vitamin B6 deficiency, hyperglycemia, metabolic acidosis, endocrine dysfunction, etc. are occasionally reported.

Patients who are allergic to this product are contraindicated.

Precautions for children: The acetylation capacity of the liver of newborns is poor, and the elimination half-life of this product may be prolonged. Adverse reactions should be closely observed when using the drug in newborns. Precautions for pregnancy and lactation: 1. This product can cross the placenta, resulting in a higher fetal blood concentration than the maternal blood concentration. Experiments on rats and rabbits have confirmed that isoniazid can cause stillbirth. Although it has not been confirmed to be a problem in humans, pregnant women should avoid using it. If there is an indication for its use, the pros and cons must be fully weighed. 2. The concentration of this product in breast milk can reach 12mg/L, which is similar to the blood concentration; although it has not been confirmed to be a problem in humans, it should be used during lactation after fully weighing the pros and cons to decide whether to use the drug. If the drug is used, breastfeeding should be stopped. Precautions for the elderly: The incidence of hepatitis caused by this product in patients over 50 years old is higher, so the elderly need to pay close attention to changes in liver function when receiving isoniazid treatment, and reduce the dose if necessary or use liver protection preparations at the same time as appropriate.

1. Drinking alcohol every day while taking isoniazid can easily cause liver toxicity induced by this product and accelerate the metabolism of this product. Therefore, the dosage of this product must be adjusted and signs of liver toxicity must be closely observed. Patients should be advised to avoid alcoholic beverages during medication. 2. When used in combination with adrenal cortical hormones (especially prednisolone), it can increase the metabolism and excretion of this product in the liver, resulting in a decrease in the blood concentration of this product and affecting the efficacy, which is more significant in fast acetylation. The dosage should be adjusted appropriately. 3. When anticoagulants (such as coumarin or indandione derivatives) are used in combination with this product, the anticoagulant effect is enhanced due to the inhibition of the enzyme metabolism of the anticoagulant. 4. Isoniazid is an antagonist of vitamin B6, which can increase the amount of vitamin B6 excreted through the kidneys and easily cause peripheral neuritis. Those who take vitamin B6 at the same time need to increase the dosage as appropriate. 5. This product should not be used in combination with other neurotoxic drugs to avoid increasing neurotoxicity. 6. When used in combination with cycloserine, it may increase adverse reactions of the central nervous system (such as dizziness or drowsiness), and the dosage needs to be adjusted, and signs of central nervous system toxicity should be closely observed, especially for patients who are engaged in work that requires high sensitivity. 7. When used in combination with other hepatotoxic anti-tuberculosis drugs such as ethionamide, pyrazinamide, and rifampicin, the hepatotoxicity of this product may be increased, especially for those with liver damage or those who are fast acetylation of isoniazid. Therefore, it should be avoided as much as possible or closely followed up for signs of hepatotoxicity in the first 3 months of the course of treatment. 8. This product can inhibit the metabolism of carbamazepine, increase its blood concentration, and cause toxic reactions; carbamazepine can induce the microsomal metabolism of isoniazid, and the formation of hepatotoxic intermediate metabolites increases. 9. When used in combination with acetaminophen, because isoniazid can induce hepatic cytochrome P-450, the amount of toxic metabolites formed by the former increases, which can increase liver toxicity and renal toxicity. 10. When used in combination with alfentanil, isoniazid can prolong the effect of alfentanil because it is a liver drug enzyme inhibitor; when used in combination with disulfiram, it can enhance its central nervous system effects, causing dizziness, incoordination, irritability, insomnia, etc.; when used in combination with enflurane, it can increase the formation of inorganic fluorine metabolites with nephrotoxicity. 11. This product should not be used in combination with ketoconazole or miconazole, because it can reduce the blood concentration of the latter two. 12. When used in combination with phenytoin sodium or aminophylline, it can inhibit the metabolism of the two in the liver, resulting in an increase in the blood concentration of phenytoin sodium or aminophylline. Therefore, when this product is used successively or in combination with the two, the dose of phenytoin sodium or aminophylline should be appropriately adjusted. 13. It should not be taken at the same time with ephedrine or belladonna to avoid or increase adverse reactions.

Keep away from light and store in a sealed container.

2ml:0.1g

24 months

Suicheng Pharmaceutical Co., Ltd.

• Founded in:

  1997-10-17

• Address:

  No. 219, Qing'an Road, Xinzheng City

• Tax NO.:

  91410100712635557P

• Registered Funds:

  111.68 million yuan

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