Gatifloxacin mesylate dispersible tablets

Pharmacological action Gatifloxacin is a racemic compound of 8-methoxyfluoroquinolone, which has a broad spectrum of activity against Gram-negative and Gram-positive microorganisms in vitro, and its R- and S-enantiomers have the same antibacterial activity. The antibacterial effect of this product is to inhibit the replication, transcription and repair process of bacterial DNA by inhibiting bacterial DNA gyrase and topoisomerase IV. The results of antibacterial experiments show that this product has antibacterial activity against most strains of the following microorganisms: 1. Gram-positive bacteria: Staphylococcus aureus (limited to strains sensitive to methicillin), coagulase-negative Staphylococcus, Streptococcus pneumoniae (strains sensitive to penicillin). 2. Gram-negative bacteria: Haemophilus (influenza and parainfluenza), Moraxella catarrhalis, Neisseria, Acinetobacter, Klebsiella pneumoniae, Enterobacter cloacae, Proteus (Proteus mirabilis and Proteus vulgaris), Pseudomonas aeruginosa, Citrobacter and Escherichia coli. 3. Other microorganisms: Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae. Toxicological studies Genetic toxicity: This product has no mutagenic effect on multiple strains in the Ames test, but has a mutagenic effect on Salmonella strain TA102 in vitro. The results of the gene mutation test of Chinese hamster V79 cells and the genetic test of Chinese hamster CHL/IU cells are both positive. Similar results can also be seen in other quinolone drugs, which may be due to the inhibitory effect of this product on type II DNA topoisomerase of eukaryotes at high concentrations. The results of the mouse micronucleus test, the rat oral cytogenetic test, and the rat oral DNA repair test of this product were all negative. Reproductive toxicity: The oral dose of rats was up to 200 mg/kg (equivalent to the maximum recommended dose for humans in terms of daily exposure (AUC)), and there was no adverse reaction to rat fertility and reproduction. Oral administration of 150 mg/kg and 50 mg/kg to rats and rabbits, respectively (in terms of AUC, approximately 0.7 and 1.9 times the maximum recommended dose for humans), did not show teratogenic effects. However, during the period of organogenesis, oral or intravenous administration of 200 mg/kg and 60 mg/kg to rats, respectively, can cause fetal skeletal malformations; oral or intravenous administration of ≥150 mg/kg and ≥30 mg/kg, respectively, can cause delayed fetal skeletal ossification, including the appearance of corrugated ribs. This suggests that there is mild fetal toxicity at this dose. This toxicity can also be seen in other quinolones. Rats were given an oral dose of 200 mg/kg in the initial stage of late pregnancy and continued to be administered until lactation, and increased post-implantation embryo loss and neonatal and perinatal mortality were observed. These findings suggest the fetal toxicity of this product. Since there are no adequate and rigorous studies conducted in pregnant women, this product can only be used during pregnancy when the potential clinical benefits of this product to the mother outweigh the harm to the fetus. This product can be secreted from rat milk, but it is not known whether it can be secreted from human milk. Since many drugs can be secreted from human milk, lactating women should use it with caution. Carcinogenicity: B6C3F1 mice were administered with the drug for 18 months, with the doses for female and male animals being 90 mg/kg and 81 mg/kg respectively [approximately 0.13 and 0.18 times the maximum recommended dose for humans based on daily systemic exposure (AUC)]: Fischer344 rats were administered with the drug for 2 years, with the doses for female and male animals being 139 mg/kg and 47 mg/kg respectively (approximately 0.81 and 0.36 times the maximum recommended dose for humans based on AUC). The results did not indicate that the product has the effect of promoting tumor growth. However, when the dose of male animals reached 100 mg/kg (approximately 0.74 times the maximum recommended dose for humans based on AUC), the incidence of giant granulocyte lymphoblastic (LGL) leukemia was increased compared with the control group. Although this increase was slightly higher than the range of historical controls, it cannot be considered that these findings at high doses in male animals will affect the safety of the clinical use of this product.

Molecular weight: C19H22FN3O4CH3SO3H

This product is white or off-white tablets.

This product is mainly used for various infectious diseases caused by sensitive pathogens, including acute exacerbation of chronic bronchitis, acute sinusitis, community-acquired pneumonia, simple urinary tract infection (cystitis) and complicated urinary tract infection, acute pyelonephritis, male gonococcal urinary tract inflammation or rectal infection and female gonococcal cervical infection.

This product is a dispersible tablet, which can be taken orally directly, or put an appropriate amount of this product into about 100ml of water, shake it to disperse it, and then take it orally. The dosage is once a day, 400mg each time.

Common adverse reactions in domestic and international clinical trials of this product are nausea, vaginitis, diarrhea, headache, and dizziness. Drug-related adverse events with lower incidence include: Systemic reactions: allergic reactions, chills, fever, back pain and chest pain. Cardiovascular system: palpitations. Digestive system: abdominal pain, constipation, indigestion, glossitis, candidal stomatitis, stomatitis, oral ulcers, vomiting. Metabolic and nutritional system: peripheral edema. Nervous system: dreaminess, insomnia, paresthesia, tremor, vasodilation, dizziness. Respiratory system: dyspnea, pharyngitis. Skin and skin soft tissue: rash, sweating. Special senses: abnormal vision, abnormal taste, tinnitus. Urogenital system: dysuria, hematuria.

1. This product is contraindicated for patients who are allergic to gatifloxacin or quinolones; 2. This product is contraindicated for pregnant women.

Precautions for children: Not recommended for use under 18 years of age. Precautions for pregnancy and lactation: Contraindicated for pregnant women. Precautions for the elderly: Elderly patients are more likely to suffer from reduced renal function and may also be at greater risk of toxic reactions. Therefore, care should be taken when selecting the dosage, and monitoring renal function will be helpful. After gatifloxacin was launched, it has been reported that elderly patients treated with gatifloxacin had significant abnormal blood sugar levels.

1. This product combined with probenecid can slow down the elimination of gatifloxacin through the kidney. 2. When this product is used simultaneously with digoxin, no significant changes in the pharmacokinetics of gatifloxacin are observed, but digoxin blood concentrations are found to increase in some subjects. Therefore, patients taking digoxin should be monitored for symptoms and signs of digoxin toxicity. 3. The simultaneous use of gatifloxacin and drugs that affect glucose metabolism can increase the risk of abnormal blood sugar metabolism in patients.

Keep in a dark and closed place in a cool place.

0.2g (based on C19H22FN3O4)

18 months

Jiangsu Runbang Pharmaceutical Co., Ltd.

• Founded in:

  2004-07-09

• Address:

  Building 1, No. 29, Yingbin Avenue, Huai'an Economic and Technological Development Zone

• Tax NO.:

  91320803762805163T

• Registered Funds:

  10.15 million yuan

• Email:

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