Pazufloxacin Mesylate Injection

Pharmacological action: This product belongs to the quinolone antibacterial drug, and its main mechanism of action is to inhibit the activity of DNA gyrase and DNA topoisomerase IV of Staphylococcus aureus, hinder DNA synthesis and lead to bacterial death; it has weak inhibitory effect on human topoisomerase II. This product has the characteristics of broad antibacterial spectrum and strong antibacterial effect. It has good antibacterial activity against G bacteria such as Staphylococcus, Streptococcus, Enterococcus, and G- bacteria such as Escherichia coli, Proteus mirabilis, Klebsiella, Enterobacter cloacae, Citrobacter, Acinetobacter calcoaceticus, Haemophilus influenzae, Moraxella catarrhalis, Pseudomonas aeruginosa, etc. This product also has good antibacterial activity against some anaerobic bacteria such as Clostridium perfringens, Fusobacterium nucleatum, Propionibacterium acnes, Porphyromonas, some Peptostreptococci, Bacteroides fragilis and Prevotella. Toxicology study on repeated dose toxicity: rats were intravenously injected with 4, 13, 39 and 130 mg/kg/day for 3 consecutive months. The A/G (albumin/globulin) ratio of rats in the 130 mg/kg group increased, and cavitation of articular cartilage was observed in a few rats. However, monkeys were intravenously injected with 26, 52 and 104 mg/kg/day for 13 consecutive weeks, and no abnormal reactions caused by the drug were observed.

Pazufloxacin mesylate. Chemical name: (-)-(s)-10-(1-aminocyclopropyl)-9-fluoro-3-methyl-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de]-[1,4]benzoxazine-6-carboxylic acid methanesulfonate. Chemical structure: Molecular formula: C16H15FN2O4CH4O4S Molecular weight: 414.41

This product is light yellow-green or yellow-green clear liquid.

This product is suitable for the following infections caused by sensitive bacteria: 1. Secondary infections of chronic respiratory diseases, such as chronic bronchitis, diffuse bronchiolitis, bronchiectasis, emphysema, pulmonary interstitial fibrosis, bronchial asthma, old pulmonary tuberculosis, etc.: pneumonia, lung abscess; 2. Pyelonephritis, complicated cystitis, prostatitis; 3. Burn wound infection, surgical wound infection: 4. Cholecystitis, cholangitis, liver abscess; 5. Intra-abdominal abscess, peritonitis; 6. Reproductive organ infection, such as adnexitis, endometritis; pelvic inflammatory disease.

Usage: intravenous drip. Dosage: 0.3g once, twice a day, intravenous drip time is 30-60 minutes, and the course of treatment is 7-14 days. The dosage can be adjusted according to the patient's age and condition. Precautions for administration (1) Bacteriological examination should be performed before using this product. Generally speaking, in order to prevent bacterial resistance, after the pathogenic bacteria of the infection are identified, the administration time should be minimized while ensuring the treatment of the patient. (2) During the administration period, regardless of whether it is necessary to continue the medication, the necessity of continuing the medication should be determined 3 days after the start of administration, and whether to stop the medication or switch to other drugs should be evaluated. Generally speaking, the most commonly used treatment course of this drug is 14 days. (3) This drug should generally not be mixed with other drugs or infusions. (4) Patients with severe renal insufficiency should use it with caution or adjust the dosage or course of treatment. Reference is as follows: Renal clearance (ml/min) Dosage 44.7 0.3g once, twice a day 13.6 0.3g once, once a day Dialysis patients once 0.3g, once every 3 days

The main clinical adverse reactions of this product are diarrhea, rash, nausea, and vomiting. Laboratory tests show elevated ALT, AST, ALP, r-GTP, and increased eosinophils. 1. Clinical adverse reactions 1) Acute renal failure: may cause acute renal failure. 2) Abnormal liver function, jaundice. 3) Pseudomembranous colitis: severe enteritis with bloody stools may occur. If abdominal pain or frequent diarrhea occurs, the drug should be discontinued immediately and appropriate preventive measures should be taken. 4) Granulocytopenia, thrombocytopenia. 5) Rhabdomyolysis: If myalgia, weakness, elevated creatine phosphokinase (CPK), or elevated myosin in blood or urine occurs, the drug should be discontinued immediately. Rhabdomyolysis can also lead to acute renal failure. 6) Spasm. 7) Shock, allergic reaction. If any abnormalities such as dyspnea, edema, erythema, etc. occur, the drug should be discontinued and appropriate treatment measures should be taken. 8) Epidermal exfoliation necrosis (Lyell syndrome), eye, mucosal, and skin syndrome (Stevens Johnson syndrome). 9) Interstitial pneumonia: pneumonia with fever, cough, dyspnea, and abnormal chest X-ray. 10) Hypoglycemia: Severe hypoglycemia is prone to occur in elderly patients and patients with renal failure, and should be carefully observed. 11) Achilles tendonitis and tendon rupture. Close observation should be made during administration. If the above adverse reactions occur, the drug should be discontinued immediately and appropriate treatment measures should be taken. 2. Adverse reactions of similar drugs: PIE syndrome: PIE syndrome accompanied by fever, cough, dyspnea, abnormal chest X-ray, and eosinophilia has been reported in other new quinolone drugs used in clinical practice. If the above adverse reactions occur, the drug should be discontinued immediately and appropriate treatment measures should be taken. 3. Other adverse reactions: Take appropriate treatment measures if the following adverse reactions are observed. 1) Allergic reactions: rash, fever (incidence 0.1-5%), urticaria, itching, facial skin flushing (incidence <0.1%). 2) Kidney damage: increased BUN, proteinuria, bilirubinuria, tubular urine, occult blood in urine (incidence 0.1-5%), increased blood creatinine (incidence <0.1%). 3) Liver damage: increased ALT (GPT) (incidence ≥5%), increased AST (GOT), ALT, r-GTP, LAP, LDH and bilirubin (incidence 0.1-5%). 4) Blood: eosinophilia, leukopenia, thrombocytopenia, anemia (incidence 0.1-5%). 5) Gastrointestinal reactions: diarrhea or soft stools, nausea, vomiting (incidence 0.1-5%), upper abdominal discomfort, abdominal distension, black stools (incidence <0.1%). 6) Mental and nervous system: headache, dizziness (incidence 0.1-5%), transient impaired consciousness, transient mental disorder, mental abnormality (incidence <0.1%). 7) Others: phlebitis (incidence ≥5%), increased CK (CPK), electrolyte imbalance (incidence 0.1-5%), dry mouth, glossitis (incidence <0.1%).

Patients with a history of allergy to pazufloxacin and quinolones are contraindicated

(1) This product can inhibit the metabolism of theophylline in the liver, increasing the blood concentration of theophylline. Symptoms of theophylline poisoning, such as gastrointestinal reactions, headaches, arrhythmias, and spasms, may occur. Therefore, patients need to be closely observed. When the two drugs are used together, the blood concentration of theophylline should be closely observed. (2) When this product is used in combination with phenylacetic acid, diacetyl ketoacids, and non-steroidal anti-inflammatory analgesics, spasms may occur. Therefore, close observation is required. If symptoms occur, the drug should be discontinued immediately and antispasmodic treatment should be taken. When spasms occur, the combination of the two drugs should be terminated, the airway should be kept open, and antispasmodic drugs should be used for treatment. (3) When this product is used in combination with warfarin, it can enhance the effect of warfarin and thus prolong the coagulation time. Therefore, close observation and coagulation time test should be performed when using the drug. (4) When this product is used in combination with propanesulfonic acid, the serum half-life is prolonged and the AUC is increased, but there is no significant change in the peak blood concentration.

Keep in a dark, cool place and sealed.

2ml:0.1g