Cas:54-85-3 Isoniazid powder
| product name |
Isoniazid |
| cas number |
54-85-3 |
| apperance |
White powder |
| Density |
1.2±0.1 g/cm3 |
| MF |
C6H7N3O |
| MW |
137.139 |
Isoniazid, also known as 4-picolinic acid hydrazide and isoniazid hydrazide, has a molecular formula of C6H7N3O, which is the hydrazide of isonicotinic acid. It is colored crystal or white crystalline powder, slightly bitter, stable in nature, and easily soluble in water.
Isoniazid was invented in 1952. The invention of Isoniazid made a fundamental change in the treatment of tuberculosis. In this nearly 50-year history of use, although the tuberculosis bacterium infected by some patients has developed drug resistance, most doctors still believe that it is an indispensable main drug for the treatment of tuberculosis. It is the same first-line anti-tuberculosis drug with rifampicin, ethambutol and pyrazinamide.
Anti tuberculosis
It has inhibitory and killing effects on Mycobacterium tuberculosis, and its biomembrane penetration is good. Because of its good curative effect, low toxicity, low price, and convenient oral administration, it is listed as the first anti-tuberculosis drug. [2] The oral absorption rate of isoniazid is 90%; the serum drug concentration can reach a peak 1 to 2 hours after taking it; Vd is 0.61±0.11 L/kg, and the protein binding rate is very low. This product is mainly metabolized in the body through acetylation and partial hydrolysis. Due to genetic differences, the population can be divided into fast acetylation and slow acetylation. There is a significant difference in their half-life, and the average t1/2 of those with fast acetylation is 1.1 hours. Slow acetylation takes 3 hours. The product easily passes through the blood-brain barrier. It is mainly used for various types of pulmonary tuberculosis in the advanced stage, dissolution and dissemination stage, and absorption improvement stage. It can also be used for tuberculous meningitis and other extrapulmonary tuberculosis. This product is often used in combination with other anti-tuberculosis drugs to enhance the efficacy and overcome drug-resistant bacteria. In addition, it has a certain effect on dysentery, whooping cough, and sty.
Antidepressant
Isoniazid was also the first antidepressant drug, but it withdrew from the market because of its strong liver toxicity.
Antibacterial
Isoniazid is highly selective for Mycobacterium tuberculosis and has a strong antibacterial effect. The concentration of 0.025~0.05mg/L in the test tube can inhibit the bacteria, and the higher concentration of 10mg/L has a bactericidal effect on the bacteria during the breeding period. For tubercle bacilli in the stationary phase, increasing the drug concentration or prolonging the contact time can also have a bactericidal effect. It has the same killing effect on Mycobacterium tuberculosis inside and outside the cell. Isoniazid alone is easy to produce drug resistance, and combined use can delay the development of drug resistance and enhance the efficacy. Isoniazid has no cross-resistance to other anti-tuberculosis drugs.
Although people have done detailed research on the mechanism of isoniazid, it is still not very clear. One theory is that isoniazid is converted to isonicotinic acid. Isonicotinic acid acts as an anti-metabolite of niacin instead of nicotinic acid and binds to NAD+. The deceived NAD+ cannot catalyze the normal redox reaction. Another theory is that by blocking the action of desaturase, isoniazid inhibits the conversion of C24 and C26 saturated fatty acids to C24 and C26 unsaturated fatty acids, and these unsaturated fatty acids are most likely the precursors of mycolic acid, which is It is a key component of the bacterial cell wall. Inhibiting the biosynthesis of mycolic acid will make the bacteria lose acid resistance. This mechanism fully illustrates the selectivity of isoniazid on the cell wall of Mycobacterium tuberculosis.
clinical
This product is the first choice for the treatment of tuberculosis, suitable for various types of tuberculosis, such as tuberculosis of lung, lymph, bone, kidney, intestine, tuberculous meningitis, pleurisy and peritonitis. In order to prevent and delay the emergence of drug resistance, it should be combined with other first-line anti-tuberculosis drugs. For acute miliary tuberculosis and tuberculous meningitis, the dose should be increased, and intravenous drip should be used when necessary. Isoniazid can be used to prevent people who come into contact with patients with active tuberculosis.
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