Gatifloxacin Tablets

Gatifloxacin is a racemic compound of 8-methylfluoroquinolone, which has a broad spectrum of activity against Gram-negative and Gram-positive microorganisms in vitro. Its R- and S-enantiomers have the same antibacterial activity. The antibacterial effect of this product is through inhibiting bacterial DNA gyrase and topoisomerase 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. Toxicological studies Genetic toxicity: This product has no mutagenic effect on multiple strains in the Ames test. However, it has a mutagenic effect on Salmonella strain TA102 in vitro. The results of gene mutation tests in Chinese hamster V79 cells and genetic tests in Chinese hamster CHL/IU cells were 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 in eukaryotes at high concentrations. The results of the mouse micronucleus test, rat oral cytogenetic test, and 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 based on daily systemic exposure [AUC]), and there was no adverse effect on rat fertility and reproduction. The oral doses of rats and rabbits reached 150 mg/kg and 50 mg/kg, respectively (based on AUC, approximately 0.7 and 1.9 times the maximum recommended dose for humans in clinical practice), 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. Carcinogenicity: B6C3F1 mice were administered with the drug by mixing it with food for 18 months, with the doses of female and male animals being 90 mg/kg and 81 mg/kg respectively (based on AUC, it is approximately 0.13 and 0.18 times the maximum recommended dose for humans in clinical practice); Fischer344 rats were administered with the drug by mixing it with food for 2 years, with the doses of female and male animals being 139 mg/kg and 47 mg/kg respectively (based on AUC, it is 0.81 and 0.36 times the maximum recommended dose for humans in clinical practice). 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 (based on AUC, it is approximately 0.74 times the maximum recommended dose for humans), the incidence of giant granulocyte lymphoblastic (1GL) 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 this product in clinical use.

The main ingredient of this product is gatifloxacin, and its chemical name is (±)-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid.

This product is a film-coated tablet, which appears off-white or light yellow after removing the film coating.

This product is used to treat infections caused by the following sensitive strains: Acute exacerbation of chronic bronchitis: caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Staphylococcus aureus. Acute sinusitis: caused by Streptococcus pneumoniae and Haemophilus influenzae. Community-acquired pneumonia: caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Staphylococcus aureus, Chlamydia pneumophila, Mycoplasma pneumophila, Legionella pneumophila. Uncomplicated and complicated urinary tract infections (cystitis) caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis. Pyelonephritis: caused by Escherichia coli. Uncomplicated urinary tract infections in men: caused by Neisseria gonorrhoeae. Uncomplicated cervical and rectal infections in women: caused by Neisseria gonorrhoeae.

Oral administration, once a day, 400 mg 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: diarrhea, 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. Other rare adverse events include: abnormal thinking, irritability, alcohol intolerance, loss of appetite, anxiety, arthralgia, arthritis, asthenia, asthma (bronchospasm), ataxia, bone pain, bradycardia, breast pain, cheilitis, colitis, confusion, convulsions, cyanosis, depersonalization, depression, diabetes, hypertension, dry skin, dysphagia, ear disease, ecchymosis, edema, epistaxis, euphoria, eye pain, facial edema, flatulence, gastritis, gastrointestinal bleeding, Gingivitis, bad breath, hallucination, hematemesis, hostility, hyperesthesia, hyperglycemia, hypertension, increased muscle tension, hyperventilation, hypoglycemia, leg cramps, lymphadenopathy, maculopapular rash, uterine bleeding, migraine, mouth edema, myalgia, muscle weakness, neck pain, nervousness, panic, paranoia, parosmia, pruritus, pseudomembranous colitis, psychosis, ptosis, rectal bleeding, drowsiness, tension, substernal chest pain, tachycardia, loss of taste, dry mouth, tongue swelling, herpes, etc. The incidence of abnormal changes in laboratory tests is low, including: leukopenia, thrombocytopenia, increased ALT or AST, and alkaline phosphatase, total bilirubin, serum amylase, electrolyte abnormalities, etc.

This product is contraindicated for use in patients who are allergic to gatifloxacin or quinolones.

Precautions for children: The efficacy and safety of this product for children and adolescents (under 18 years old) have not been established, and its use is not recommended at present. Precautions for pregnancy and lactation: The efficacy and safety of gatifloxacin for pregnant women and lactating women have not been established. Pregnant women and lactating women should use this product with caution, and it should only be considered when the benefits of using this product outweigh the possible risks to the fetus and infant. Precautions for the elderly: Although elderly female subjects have slight pharmacokinetic differences compared with young women, this difference is mainly due to the physiological decline of renal function with age, and the dosage should be determined according to their renal function.

1. This product can be used in combination with probenecid to slow down the renal excretion of gatifloxacin. 2. When ferrous sulfate, aluminum or magnesium antacids and dehydroxyglycosides (didanoxine, Huituz) are used in combination with this product, the bioavailability of gatifloxacin is reduced. However, taking this product 4 hours before taking ferrous sulfate, dietary supplements containing zinc, magnesium, iron, etc. (such as multivitamins), or aluminum/magnesium antacids or dehydroxyglycosides (didanoxine, Huituz) will not affect the pharmacokinetic process of gatifloxacin. 3. No interaction was observed when milk, calcium carbonate, cimetidine, theophylline, warfarin, glyburide or midazolam were taken at the same time with this product. 4. When this product was taken at the same time with digoxin, no significant changes in the pharmacokinetic parameters of gatifloxacin were observed, but the blood concentration of digoxin was found to be increased in some subjects. Therefore, the symptoms and signs of digoxin toxicity should be monitored in patients taking digoxin. For patients who show signs and symptoms of toxicity, the blood concentration of digoxin should be measured and the digoxin dose should be adjusted appropriately. However, it is not recommended to adjust the dose of the two drugs in advance.

Keep away from light, sealed and stored in a dry place.

0.2 g

24 months

Hubei Qianjiang Pharmaceutical Co., Ltd.

• Founded in:

  2009-09-18

• Address:

  No. 1, Zhanghua South Road, Qianjiang City

• Tax NO.:

  91429005695102248D

• Registered Funds:

  300 million yuan

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