Gatifloxacin Mesylate and Glucose Injection

1. Pharmacological action Gatifloxacin is a racemic compound of the 8-methoxyfluoroquinolone class. It 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 the replication, transcription and repair process of bacterial DNA. Both in vitro tests and clinical use results 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), 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 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 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 (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 were 150 mg/kg and 50 mg/kg respectively (about 0.7 and 1.9 times the maximum recommended dose for humans based on AUC), and no teratogenic effect was observed. However, during the period of organogenesis, 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 corrugated ribs. This indicates that there is mild fetal toxicity at this dose. 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, and increased post-implantation embryo loss and neonatal and perinatal mortality were observed. These findings also 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, it should be used with caution in breastfeeding women. (3) 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 daily systemic exposure (AUC), approximately 0.13 and 0.18 times the maximum recommended human dose]; 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). 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 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 mesylate, its chemical name is: (±) 1-cyclopropyl-6-fluoro-7-(3-methyl-1-piperazinyl)-8-methoxy-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid methanesulfonate, its structural formula is: Molecular formula: C19H22FN3O4·CH3SO3H Molecular weight: 471.51

This product is a colorless or slightly yellowish green clear liquid.

Used to treat the following infectious diseases with a degree of infection 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, etc. Simple or complicated urinary tract infection (cystitis): caused by Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis, etc. Pelvic nephritis: caused by Escherichia coli, etc. Simple urethral and cervical gonorrhea: caused by Neisseria gonorrhoeae. Acute simple straight

Intravenous drip: 200 mg each time, twice a day, refer to the table below (Table 1) for details. This product is bioequivalent to oral tablets. During the course of treatment, the intravenous administration can be changed to oral tablets according to the doctor's decision, and no dosage adjustment is required. Table 1 Dosage Guide 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. For renal insufficiency, please refer to the table below (Table 2) for usage and dosage. 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 are mostly mild, mainly seen in the intravenous administration site and the gastrointestinal tract and nervous system, including phlebitis, nausea, vomiting, diarrhea, headache and dizziness. Other rare clinically relevant adverse events include: 1. Systemic reactions: allergic reactions, chills, fever, back pain, chest pain, weakness and facial edema. 2. Cardiovascular system: hypertension, palpitations. 3. Digestive system: abdominal pain, constipation, indigestion, glossitis, candidal stomatitis, stomatitis, oral ulcers, vomiting, loss of appetite, gastritis and flatulence. 4. Metabolic and nutritional system: peripheral edema, hyperglycemia and thirst. 5. Musculoskeletal system: joint pain, painful cramps in the lower limbs. 6. Nervous system: dreaminess, insomnia, paresthesia, tremor, vasodilation, dizziness, agitation, anxiety, confusion and tension. 7. Respiratory system: dyspnea, pharyngitis. 8. Skin and skin soft tissue: rash, sweating, dry skin and itching. 9. Special senses: visual abnormalities, taste abnormalities, tinnitus. 10. Urinary and reproductive system: difficulty urinating. Rare related adverse events include: abnormal thinking, alcohol intolerance, arthritis, weakness, asthma (bronchospasm), ataxia, bone pain, bradycardia, chest pain, cheilitis, colitis, confusion, convulsions, cyanosis, depersonalization, depression, diabetes, dysphagia, ear pain, ecchymosis, edema, epistaxis, euphoria, eye pain, photosensitivity, generalized edema, gastrointestinal bleeding, gingivitis, halitosis, hallucinations, hematemesis, hematuria, hostility, hyperesthesia, hyperglycemia, increased muscle tension, hyperventilation, hypoglycemia, lymphadenopathy, maculopapular rash, uterine bleeding, migraine, oral edema, myalgia, muscle weakness, neck pain, panic, paranoia, smell perversion, photophobia, pseudomembranous enterocolitis, psychosis, ptosis, rectal bleeding, tension, substernal chest pain, tachycardia, loss of taste, tongue swelling, herpes, etc. The incidence of abnormal changes in laboratory tests is low, including: leukopenia, neutropenia, decreased hemoglobin, increased ALT and/or AST, as well as alkaline phosphatase, total bilirubin, blood sugar, serum amylase and electrolyte disorders.

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 it is recommended not to use this product. Precautions for pregnancy and lactation: The efficacy and safety of gatifloxacin for pregnant and lactating women have not been established. Pregnant women should avoid using this product, and lactating women should suspend breastfeeding when using it.

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 the blood concentration of digoxin is found to be increased 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 doses of the two drugs in advance.

Seal tightly and store in a cool, dark place.

100ml: Gatifloxacin mesylate (calculated as gatifloxacin) 0.2g and glucose 5g

Tentative 18 months

Jiangsu Embrace Sicence & Technology Development Co., Ltd.

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