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 bacterial DNA gyrase and topoisomerase IV, thereby inhibiting the replication, transcription and repair process of bacterial DNA. The results of antibacterial experiments all 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 Staphylococci, 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 [approximately 0.13 and 0.18 times the maximum recommended dose for humans based on daily systemic exposure (AUC)]; 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 (approximately 0.81 and 0.36 times the maximum recommended dose for humans based on AUC). 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 0.74 times the maximum recommended dose for humans based on AUC), 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, once daily, 400 mg (2 tablets) each time. Table 1. Dosage Guidelines Infection (depending on the pathogen) Daily dose Course of treatment Acute exacerbation of chronic bronchitis 400 mg 7-10 days Acute sinusitis 400 mg 10 days Community-acquired pneumonia 400 mg 7-14 days Uncomplicated urinary tract infection 400 mg single dose or 200 mg 3-5 days Complicated urinary tract infection 400 mg 7-10 days Acute pyelonephritis 400 mg 7-10 days Male uncomplicated gonococcal urinary tract infection 400 mg single dose Female cervical and rectal gonococcal infection 400 mg single dose Gatifloxacin is mainly excreted through the kidneys. Patients with creatinine clearance < 40 ml/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 session. Table 2. Recommended doses of this product for patients with renal insufficiency Creatinine clearance Initial dose Maintenance dose ≥40ml/min400mg400mg/day<40ml/min400mg200mg/day Hemodialysis 400mg200mg/day Peritoneal dialysis 400mg200mg/day Maintenance dose Start from the second day of medication Patients with renal insufficiency use 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, without the need to adjust the dose of this product.

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, 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 related to the drug 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, dry skin, dysphagia, ear disease, ecchymosis, edema, epistaxis, euphoria, eye pain, facial edema, flatulence, gastritis, gastrointestinal bleeding, toothache, 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, tongue swelling, herpes, etc. The incidence of abnormal changes in laboratory tests is low, including: leukopenia, increased ALT or AST, and alkaline phosphatase, total bilirubin, serum amylase, electrolyte abnormalities, 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 there are slight pharmacokinetic differences between elderly female subjects and 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 slow down the renal excretion of gatifloxacin when used in combination with probenecid. 2. The bioavailability of gatifloxacin is reduced when ferrous sulfate, aluminum or magnesium antacids and dehydroxyglycosides (didanoxine, huituz) are used in combination with this product. 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.

0.1g

24 months

Chengdu Hengrui Pharmaceutical Co., Ltd.

• Founded in:

  2001-03-07

• Address:

  No. 18, Baicao Road, West Park, Chengdu Hi-tech Zone

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  91510100727431952L

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  29.18 million yuan

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