Drug Name】Pasiniazid Tablets

Ingredients]: The main ingredient of this product is Pasiniazid.

Chemical name: 4-pyridinecarbohydrazide p-aminosalicylate.

Molecular Formula:C6H7N3O-C7H7NO3

Molecular weight:290.27

Properties]: This product is film-coated tablets.

Indications】Combined with other anti-tuberculosis drugs, it is used for the treatment of various types of pulmonary tuberculosis, endobronchial tuberculosis and extrapulmonary tuberculosis. It can also be used as a protective drug for surgery related to tuberculosis, as well as for the prevention of tuberculosis infection and recurrence of long-term or high-dose corticosteroid and immunosuppressive therapy.

Specifications】0.1g

Dosage】Orally

Treatment In combination with other anti-tuberculosis drugs, adults: 10-20mg/kg of body weight a day pediatrics: depending on the individual needs can be increased to 20-40mg/kg of body weight a day, take at once.

Prevention: 10~15mg/kg/day according to body weight, taken at once.

Adverse Reactions] Occasionally, dizziness, headache, insomnia, fever, skin rash, nausea, fatigue, gangrene, peripheral neuritis, optic neuritis and hematocrit may occur.

Contraindications

1、Patients with psychosis and epilepsy are prohibited.

2、It is forbidden for patients with severe liver dysfunction.

Precautions

1, this product should be taken at least 3 months, if there is no adverse reaction, it is not appropriate to stop the drug in the middle of the clinical diagnosis of healing before stopping the drug.

2、Pregnant women, people with liver or kidney insufficiency and people with history of mental illness, epilepsy and traumatic brain injury should be cautious.

Liver function tests should be conducted regularly during the period of use. A transient elevation of aminotransferase may occur in a few patients in the first two months of use. If the drug is continued under hepatoprotective treatment, the aminotransferase may return to normal. If it continues to rise, the drug should be discontinued.

4、If symptoms of optic neuritis appear during the course of treatment, eye examination should be conducted immediately and repeated periodically.

5、Taking vitamin B together can prevent peripheral neuritis and other neurological adverse reactions.

6, antacids, especially aluminum hydroxide, can inhibit the absorption of this product, should not be taken together.

7, this product can enhance the coumarin anticoagulant, some antiepileptic drugs, antihypertensive drugs, anticholinergics, tricyclic antidepressants, combined use should be noted.

Pregnant women and lactating women】Pregnant women and lactating women should be cautious.

For children: Follow the dosage for children strictly or as directed by the physician.

Geriatric Use] Not known.

Drug interactions] Not known.

Overdose] Not known.

Pharmacology and Toxicology

1、Pharmacology

This product is a chemical synthesis of isoniazid (INH) and p-aminosalicylic acid (PAS), INH is mainly effective against Mycobacterium bovis during the growth and reproduction period. Its mechanism of action has not been elucidated, and it may inhibit the synthesis of myolic acid (mycolic acid) in sensitive bacteria and rupture the cell wall.PAS effectively delays and blocks the acetylation process of INH in the body. As a result, it maintains a higher and longer INH concentration in the blood and reduces the toxicity to the liver. Clinically, after taking equal amount of INH and this product respectively, it was found that the blood concentration of INH at 12 hours was only 0.03mg, but this product was 2.6 mg/; at 14 hours, the blood concentration of INH was already 0, but this product was still as high as 2mg/L, which was twice as much as the MIC. This not only enhanced the bactericidal effect of the drug, but also delayed the emergence of bacterial resistance. It has been clinically proved that in the combination therapy with other anti-tuberculosis drugs, the anti-tuberculosis efficacy of this product is significantly better than INH, and the incidence of gastrointestinal reactions, hepatic impairment and leukopenia are significantly lower than the incidence of adverse reactions of FINH.

Animal experiments showed that in artificially infected mice, the anti-tuberculosis efficacy of this product was about 5 times that of INH; the therapeutic effect of this product at 10mg/kg per day was significantly better than that of the physical mixture of INH (20mg/kg per day) + PAS (200mg/kg per day).

2. Toxicology

The oral LD50 of this product is 0.4g/kg-d and 0.8~1.6g/kg in mice and mice respectively, which is 2 times of INH.

Pharmacokinetics] The product is rapidly absorbed from the gastrointestinal tract after oral administration and distributed in tissues and body fluids throughout the body, including cerebrospinal fluid and caseous tissue. In vivo, it is gradually decomposed into INH and PAS, most of which are acetylated in the liver and become inactive metabolites, and are mainly excreted through the kidneys. INH as a marker tmax=3.4h, t1/2=6.8h.

Storage] Keep in a dry place, sealed and protected from light.

Package】Plastic bottle, 100 tablets/bottle.

Expiry date]: 24 months

Execution Standard] National Drug Standard WS-10001-(HD-0322)-2002

Approval Number]: National Pharmaceutical Standard H20058553