Gatifloxacin Capsules

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 and other Streptococcus strains. 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: Oral administration of doses up to 200 mg/kg to rats (based on daily exposure (AUC), equivalent to the maximum recommended dose for humans) had no adverse effects on 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 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 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 increased neonatal and perinatal mortality were observed. These findings suggest the fetal toxicity of this product. Carcinogenicity: B6C3F1 mice were administered with the drug for 18 months, with the doses of female and male animals being 90 mg/kg and 81 mg/kg respectively [based on daily systemic exposure (AUC), approximately 0.13 and 0.18 times the maximum recommended dose for humans]; Fischer344 rats were administered with the drug for 2 years, with the doses of female and male animals being 139 mg/kg and 47 mg/kg respectively (based on AUC, approximately 0.81 and 0.36 times the maximum recommended dose for humans). 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, approximately 0.74 times the maximum recommended dose for humans), 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 this product's clinical use.

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

This product is a hard capsule, and the contents are off-white or light yellow granules.

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.

Oral administration, twice a day, 200 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: abdominal pain, constipation, indigestion, glossitis, candidal stomatitis, stomatitis, oral ulcers, vomiting. Metabolic and nutritional system: peripheral edema. Nervous system: dreaminess, insomnia, paresthesia, tremor, vasodilation, and dizziness. Respiratory system: dyspnea, pharyngitis. Skin and skin soft tissue: rash, sweating. Special senses: visual abnormalities, taste abnormalities, tinnitus. Urogenital system: dysuria, hematuria. Other rare adverse events include: abnormal thinking, irritability, alcohol intolerance, loss of appetite, anxiety, joint pain, arthritis, asthenia, asthma (bronchospasm), ataxia, bone pain, bradycardia, breast pain, cheilitis, colitis, confusion, convulsions, cyanosis, depersonalization, depression, diabetes, dry skin, dysphagia, ear disease, ecchymosis, edema, epistaxis, euphoria, eye pain, facial edema, flatulence, gastritis, gastrointestinal bleeding, toothache, etc. Gingivitis, halitosis, 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, swollen tongue, herpes, etc. The incidence of abnormal changes in laboratory tests is low, including: leukopenia, increased ALT or AST, and abnormal alkaline phosphatase, total bilirubin, serum amylase, electrolytes, etc.

This product is contraindicated 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 and lactating women have not been established. Pregnant 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) does 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 exhibit signs and symptoms of toxicity, digoxin plasma concentrations should be measured and the digoxin dose adjusted appropriately.

Keep away from light and store in airtight container.

0.2g (based on C19H22FN304)

24 months

Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.

• Founded in:

  2001-11-30

• Address:

  Luoqi Road, Linyi High-tech Industrial Development Zone, Shandong Province

• Tax NO.:

  913700002658705037

• Registered Funds:

  60.96 million yuan

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