Gatifloxacin eye drops

1. 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 through inhibiting bacterial DNA gyrase and topoisomerase I and IV, thereby inhibiting bacterial DNA replication, transcription and repair processes. In vitro tests and clinical use results have shown 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), Streptococcus pneumoniae (strains sensitive to penicillin). (2) Gram-negative bacteria: Escherichia coli, Haemophilus influenzae and parainfluenzae, Klebsiella pneumoniae, Moraxella catarrhalis, Neisseria gonorrhoeae, Proteus mirabilis. (3) Other microorganisms: Chlamydia pneumoniae, Legionella pneumophila, Mycoplasma pneumoniae. 2. Toxicological studies (1) Genotoxicity: 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 I and II DNA topoisomerase of eukaryotes at high concentrations. The results of the mouse micronucleus test, rat cytogenetic test and rat DNA repair test of this product administered orally and intravenously were all negative. (2) Reproductive toxicity: The oral dose of rats was up to 200 mg/kg (about 4500 times the maximum dose recommended by ophthalmologists), and there was no adverse effect on rat fertility and reproduction. The oral dose of rats and rabbits was up to 50 mg/kg (about 1000 times the maximum dose recommended by ophthalmologists), and no teratogenic effect was observed. However, during the organogenesis period, oral or intravenous administration of 200 mg/kg and 60 mg/kg, respectively, can cause fetal skeletal malformations in rats; oral or intravenous administration of ≥150 mg/kg and ≥30 mg/kg, respectively, can cause delayed fetal skeletal ossification, including the appearance of wavy ribs. This suggests that at this dose, there is mild fetal toxicity. This toxicity can also be seen in other quinolones. Rats were given oral doses of 200 mg/kg in the initial stage of late pregnancy and continued to be administered until lactation. Increased post-implantation embryo loss and increased mortality in newborn rats and perinatal periods were observed. These findings also suggest the fetal toxicity of this product. (3) Carcinogenicity: B6C3F1 mice were administered with the drug by mixing it with their food for 18 months, with the doses for female and male animals being 90 mg/kg and 81 mg/kg respectively (approximately 2000 times the maximum dose recommended by ophthalmologists); Fischer344 rats were administered with the drug by mixing it with their food for 2 years, with the doses for female and male animals being 139 mg/kg and 47 mg/kg respectively (approximately 3000 times and 1000 times the maximum dose recommended by ophthalmologists). The results did not indicate that this product has the effect of promoting tumor growth. However, when the dose of male animals reached 100 mg/kg (approximately 1000 times the maximum dose recommended by ophthalmologists), 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 existing historical controls, it cannot be considered that these findings at high doses in male animals will affect the safety of this product in clinical use.

The main ingredient of this product is gatifloxacin. Chemical name: 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid Chemical structure: Molecular formula: C19H22FN3O4 Molecular weight: 375.40

This product is a yellowish green clear liquid.

The following infections caused by Staphylococcus, Streptococcus, Pneumococcus, Bacteria, Corynebacterium, Bacterium Burkholderia, Pseudomonas, Haemophilus influenzae, etc. that are sensitive to gatifloxacin: blepharitis, sty, dacryocystitis, conjunctivitis, tarsal gland inflammation, keratitis, corneal ulcer, etc.

Day 1-2: When awake, take 1 drop every 2 hours, 8 times a day. Day 3-7: When awake, take 1 drop 4 times a day.

Occasionally, there may be transient irritation symptoms

It is contraindicated in patients who are allergic to gatifloxacin or other quinolones.

Precautions for children: The safety and effectiveness of this product for infants under 1 year old have not been established, so use with caution in infants. Precautions for pregnancy and lactation: No teratogenic effects were found in rats and rabbits taking 50 mg/Kg/day of gatifloxacin orally. However, taking 150 mg/Kg/day orally in rats can cause fetal skeletal/craniofacial malformations or delayed ossification, anterior chamber hypertrophy, and weight loss. Taking 200 mg/Kg/day orally during the perinatal period can cause miscarriage and increased perinatal mortality in fetal rats. Due to the lack of research data on the use of gatifloxacin in pregnant women, pregnant women should consult a doctor before using this product and only use it after weighing the pros and cons. Gatifloxacin can be secreted in the milk of rats, but it is not clear whether it is secreted in human milk. Lactating women should be cautious. Precautions for the elderly: It is not yet clear.

The interaction between gatifloxacin eye drops and other drugs is still unclear. However, systemic administration of quinolone antibiotics can increase the plasma concentration of theophylline, affect the metabolism of caffeine, enhance the efficacy of oral anticoagulants such as warfarin and its derivatives, and cause a transient increase in the plasma inosine level in patients taking cyclosporine. Please follow the doctor's advice when using the above drugs in combination.

Keep in dark, airtight, cool place

0.3%(g/ml)

24 months

Anhui Shuangke Pharmaceutical Co., Ltd.

• Founded in:

  2000-12-11

• Address:

  No. 80, Science Avenue, High-tech Zone, Hefei City, Anhui Province

• Tax NO.:

  913401007255479354

• Registered Funds:

  2 million yuan

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