Previous name
Levofloxacin hydrochloride capsules
Pinyin Name Levofloxacin Inflammatory Capsules
Quinolones
Properties This product is a capsule.
Pharmacology and Toxicology This product has broad-spectrum antibacterial activity and strong antibacterial activity against most Enterobacteriaceae bacteria, such as Escherichia coli, Klebsiella, Proteus, Salmonella, Shigella, Haemophilus influenzae, Legionella pneumophila, Neisseria gonorrhoeae and other gram-negative bacteria. It also has antibacterial effect on gram-positive bacteria such as Staphylococcus aureus, Streptococcus pneumoniae, Streptococcus pyogenes, Mycoplasma pneumoniae and Chlamydia pneumoniae, but it has poor effect on anaerobic bacteria and enterococci. This product is levorotatory of ofloxacin, and its antibacterial activity in vitro is about twice that of ofloxacin. Its mechanism is to inhibit the activity of bacterial DNA gyrase, prevent the synthesis and replication of bacterial DNA, and lead to bacterial death.
Pharmacokinetics is completely absorbed after oral administration. After a single dose of 0.2g, the peak plasma concentration (Cmax) was about 65,438 0.6 mg/L, and the time to peak (Tmax) was about 65,438 0 hours. The half-life of blood elimination (t 1/2β) is about 6 hours. Protein binding rate is about 30% ~ 40%. After absorption, this product is widely distributed in various tissues and body fluids, and the ratio of the concentration in tonsils, prostate tissues, sputum, tears, female reproductive tract tissues, skin and saliva to the blood drug concentration is about 1. 1 ~ 2. 1. This product is mainly excreted from the kidney in its original form and rarely metabolized in the body. The urine volume within 48 hours after oral administration is about 80% ~ 90% of the dosage. This product excretes a small amount from feces in its original form, and the cumulative excretion within 72 hours after administration is less than 4% of the dose.
Indications: 1. Urinary and reproductive system infections, including simple and complex urinary tract infections, bacterial prostatitis, gonococcal urethritis or cervicitis (including infections caused by enzyme-producing strains). 2. Respiratory tract infection, including acute attack of bronchial infection and pulmonary infection caused by sensitive gram-negative bacilli. 3. Gastrointestinal infection is caused by Shigella, Salmonella, enterotoxigenic Escherichia coli, Aeromonas hydrophila and Vibrio parahaemolyticus. 4.typhoid fever. 5. Bone and joint infections. 6. Skin and soft tissue infections. 7. Systemic infection, such as septicemia.
Administration and dosage by oral administration. Adult dose: 1. Bronchial infection and pulmonary infection: 0.2g once, twice a day, or 0. 1g once, three times a day, with a course of 7 ~ 14 days. 2. Acute simple lower urinary tract infection: 0. 1g once, twice a day for 5-7 days; Complex urinary tract infection: 0.2g once, twice a day or 0. 1g once, three times a day. The course of treatment was 10 ~ 14 days. 3. Bacterial prostatitis: 0.2g once, twice a day for 6 weeks. Adults usually take 0.3~0.4g daily, divided into 2 ~ 3 times. For patients with severe infection or poor sensitivity to pathogens, such as Pseudomonas aeruginosa, the therapeutic dose can also be increased to 0.6g per day, taken in three times.
Adverse reactions 1. Gastrointestinal reaction: abdominal discomfort or pain, diarrhea, nausea or vomiting. 2. Central nervous system reactions may include dizziness, headache, drowsiness or insomnia. 3. Allergic reaction: rash, itchy skin, occasional exudative erythema multiforme and angioneurotic edema. Photosensitive reaction is rare. 4. Occasional seizures: (1), mental disorders, restlessness, confusion, hallucinations and tremors. (2) Hematuria, fever, rash and other interstitial nephritis manifestations. (3) Phlebitis. (4) Crystalline urine is more common in high-dose applications. (5) joint pain. 5. A few patients may have elevated serum transaminase, elevated blood urea nitrogen and decreased peripheral white blood cells, which are mostly mild and transient.
Contraindications are prohibited for patients who are allergic to this product and fluoroquinolones.
Note: 1. At present, the resistance of Escherichia coli to fluoroquinolones is common, so urine culture samples should be taken before drug use, and drug use should be adjusted according to the results of bacterial drug sensitivity. 2. When this product is used in large quantities or the pH value of urine is higher than 7, crystallized urine will appear. In order to avoid the occurrence of crystallized urine, it is advisable to drink plenty of water and keep the urine volume above 1200ml for 24 hours. 3. Patients with renal insufficiency need to adjust the dose according to renal function. 4. Avoid excessive sunlight when using this product. If there is photosensitive reaction or other allergic symptoms, stop taking it. 5. When liver function declines, if it is serious (ascites due to liver cirrhosis), the clearance rate of drugs can be reduced, and the blood drug concentration will increase, especially when liver and kidney function decline. It is necessary to weigh the advantages and disadvantages and adjust the dosage before application. 6. Patients with original central nervous system diseases, such as epilepsy, epilepsy history, etc., should avoid application. In the case of indications, carefully weigh the advantages and disadvantages before application. 7. Occasionally there are reports of heel arthritis or heel fracture after medication. If the above symptoms appear, you should stop taking the medicine immediately until the symptoms disappear.
Animal experiments on pregnant women and lactating women have not proved that quinolones have teratogenic effects, but there is no clear conclusion on the study of pregnant women's medication. In view of the fact that this medicine can cause joint diseases in minor animals, pregnant women are prohibited, and breastfeeding women should suspend breastfeeding when using this medicine.
The safety of this product for infants and adolescents under 18 years old has not been determined. However, when this product is used in several young animals, it can cause joint diseases. So it is not suitable for children and adolescents under 18.
Elderly patients often have decreased renal function when taking medicine. Because part of this product is excreted through the kidney, it needs to be reduced.
Drug interaction 1. Urine alkalizer will reduce the solubility of this product in urine, leading to crystalline urine and nephrotoxicity. 2. When quinolones are combined with theophylline, the liver elimination of theophylline is obviously reduced and the half-life of blood elimination is shortened due to the competitive inhibition of the binding site with cytochrome P450 (t 1/2? ) prolonged, the blood concentration increased, and theophylline poisoning symptoms appeared, such as nausea, vomiting, tremor, anxiety, excitement, convulsions, palpitations and so on. Although this product has little effect on the metabolism of theophylline, it is still necessary to determine the plasma concentration of theophylline and adjust the dose when combined. 3. The combination of this product and cyclosporine can increase the blood concentration of cyclosporine, so it is necessary to monitor the blood concentration of cyclosporine and adjust the dose. 4. Although the anticoagulant effect of warfarin is slightly enhanced when this product is used together with warfarin, the prothrombin time of patients should be closely monitored when it is used together. 5. Probenecid can reduce the secretion of this product from renal tubules by about 50%, and it can be poisoned by the increase of blood drug concentration when used together. 6. This product can interfere with caffeine metabolism, thus reducing caffeine elimination, prolonging the half-life of blood elimination (t 1/2β), and may cause central nervous system toxicity. 7. Acid-making drugs and iron agents containing aluminum and magnesium can reduce the oral absorption of this product and should not be used together. 8. When this product is used with Fenbufen, a non-steroidal anti-inflammatory drug, convulsions occasionally occur, so it is not suitable to use it with Fenbufen.