Gatifloxacin Lactate Sodium Chloride Injection

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 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, 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 eukaryotic organisms 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 in terms of daily systemic exposure [AUC]), and there was no adverse reaction to rat fertility and reproduction. The oral doses of rats and rabbits reached 150 mg/kg and 50 mg/kg, respectively (in terms of AUC, about 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 for 18 months, with the doses for female and male animals being 90 mg/kg and 81 mg/kg respectively (based on AUC, approximately 0.13 and 0.18 times the maximum recommended human dose in clinical practice); 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 (based on AUC, approximately 0.81 and 0.36 times the maximum recommended human dose in clinical practice); the results did not indicate that this product has the effect of promoting tumor growth, but when the dose of male animals reached 100 mg/kg (based on AUC, approximately 0.74 times the maximum recommended human dose), 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 in clinical use.

The main ingredient of this product is gatifloxacin lactate. Chemical name: 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazine)-4-oxo-3-quinolinecarboxylic acid lactate. Chemical structure: Molecular formula: C19H22FN3O4·C3H6O3 Molecular weight: 465.48

This product is a yellowish green clear liquid.

Used to treat the following infectious diseases of moderate severity or above caused by sensitive strains: Acute exacerbation of chronic bronchitis: caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis or Staphylococcus aureus. Acute sinusitis: caused by Streptococcus pneumoniae, Haemophilus influenzae, etc. Community-acquired pneumonia: caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Staphylococcus aureus, Chlamydia pneumophila, Mycoplasma pneumophila, or Legionella pneumophila. Simple or complicated urinary tract infection (cystitis): caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, etc. Pyelonephritis: caused by Escherichia coli, etc. Simple urethral and cervical gonorrhea: caused by Neisseria gonorrhoeae. Acute simple rectal infection in women: caused by Neisseria gonorrhoeae. Before treatment, appropriate culture and sensitivity tests should be performed to isolate and identify the pathogenic microorganisms and determine their sensitivity to gatifloxacin. However, treatment with this product can be started before the results of the bacteriological examination are obtained. After the results of the bacteriological examination are obtained, appropriate treatment can be continued.

Intravenous drip, 400 mg each time, once a day, refer to the table below (Table 1) for details. This product is bioequivalent to oral tablets. During the course of treatment, it can be changed from intravenous administration to oral tablets according to the doctor's decision, without adjusting the dose. Table 1. Dosage Guidelines for Gatifloxacin Gatifloxacin is mainly excreted through the kidneys. Patients with creatinine clearance <40ml/min, including hemodialysis and long-term peritoneal dialysis patients, should adjust the dose of this product. Hemodialysis patients should take the drug after each hemodialysis. Refer to the table below (Table 2) for usage and dosage for patients with renal insufficiency. Table 2. Recommended dose of this product for patients with renal insufficiency Patients with renal insufficiency do not need to adjust the dose of this product when using a single dose of 400mg to treat simple urinary tract infection or gonorrhea, and 200mg daily for 3 days to treat simple urinary tract infection.

Adverse reactions seen in clinical trials were mostly mild, mainly in the intravenous administration site and the gastrointestinal tract and nervous system, including phlebitis, nausea, vomiting, diarrhea, headache and dizziness. Other rare clinically related adverse events include: Systemic reactions: allergic reactions, chills, fever, back pain, chest pain, weakness and facial edema. Cardiovascular system: hypertension, palpitations. Digestive system: abdominal pain, constipation, indigestion, glossitis, candidal stomatitis, stomatitis, oral ulcers, vomiting, loss of appetite, gastritis and flatulence. Metabolic and nutritional system: peripheral edema, hyperglycemia and thirst. Musculoskeletal system: joint pain, painful cramps in the lower limbs. Nervous system: dreaminess, insomnia, paresthesia, tremor, vasodilation, dizziness, agitation, anxiety, confusion and tension. Respiration

This product is contraindicated for patients who are allergic to gatifloxacin or quinolones. It is contraindicated for patients with diabetes.

Precautions for children: The efficacy and safety of this product for children and adolescents (under 18 years old) have not been established, and it is recommended not to use this product. Precautions for pregnancy and lactation: The safety of the efficacy of gatifloxacin for pregnant and lactating women has not been established. Pregnant women should avoid using this product, and lactating women should suspend breastfeeding when discontinuing the use of this product. Precautions for the elderly: Elderly patients are more likely to suffer from reduced renal function. And the risk of toxic reactions may also be greater, so caution should be exercised when choosing the dosage, and monitoring renal function will be helpful. After gatifloxacin was launched, there have been reports of abnormal blood sugar in elderly patients treated with gatifloxacin. Elderly patients may have future-detected diabetes, age-related reduced renal function, underlying diseases, and/or are taking concomitant medications that affect glucose metabolism, which may pose a special risk for abnormal blood sugar. When preparing to use gatifloxacin for patients, it is recommended that doctors discuss with patients who may be at risk of hypoglycemia and/or hyperglycemia (abnormal blood sugar metabolism events) so that patients know how to monitor their blood sugar changes and what measures should be taken when such changes occur.

1. This product can be used in combination with probenecid to 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 an increase in the blood concentration of digoxin is found in some subjects. Therefore, the symptoms and signs of digoxin toxicity in patients taking digoxin should be monitored. For patients who show symptoms and signs 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. 3. The simultaneous use of gatifloxacin and drugs that affect glucose metabolism can increase the risk of abnormal blood glucose metabolism in patients (see Contraindications and Warnings: Abnormal Blood Glucose). Antidiabetic drugs: Pharmacodynamic changes that affect glucose metabolism have been observed after the combined use of glibenclamide and other hypoglycemic drugs. No significant pharmacokinetic interactions were observed when glibenclamide was used in combination with gatifloxacin.

Keep away from light and store in airtight container.

100ml: Gatifloxacin 0.2g and sodium chloride 0.9g

24 months

Shijiazhuang No.4 Pharmaceutical Co., Ltd.

• Founded in:

  1994-06-28

• Address:

  No. 518, Huaian East Road, Shijiazhuang High-tech Industrial Development Zone

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  911301001044060055

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  950 million yuan

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