Trade name NORFLOXACIN CAPSULES
Common name NORFLOXACIN CAPSULES
The main component of norfloxacin is 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7 - (1-piperazinyl) - 3-quinoline carboxylic acid.
Action category: This product is a prescription drug for infection caused by sensitive bacteria.
The indications are applicable to urinary tract infection, gonorrhea, prostatitis, intestinal infection, typhoid and other Salmonella infections caused by sensitive bacteria.
Adverse reactions 1. Gastrointestinal reactions are common, which can be manifested as abdominal discomfort or pain, diarrhea, nausea or vomiting.
2. The reaction of central nervous system may include dizziness, headache, drowsiness or insomnia.
3. Allergic reaction, rash, skin pruritus, and occasionally exudative erythema multiforme and angioneuroedema. A few patients have photosensitive reaction.
4. Occasionally:
(1) Seizures, mental disorders, irritability, disturbance of consciousness, hallucinations, tremors.
(2) Hematuria, fever, rash and other manifestations of interstitial nephritis.
(3) Phlebitis.
(4) Crystalline urine, mostly seen in high-dose application.
(5) Joint pain.
5. A few patients may have elevated serum aminotransferase, increased blood urea nitrogen and decreased peripheral blood leukocytes, mostly mild and transient.
Contraindication: it is forbidden for patients allergic to this product and fluoroquinolones.
It is suitable for patients with infectious diseases caused by sensitive bacteria.
It is not suitable for people who are allergic to this product.
Precautions 1. This product should be taken on an empty stomach and 250ml of water at the same time.
2. At present, there are many norfloxacin resistant Escherichia coli, so urine samples should be taken for culture before administration, and the medication should be adjusted with reference to the results of bacterial drug sensitivity.
3. Crystalline urine can occur when the product is applied in large doses or when the urine pH value is above 7. In order to avoid the occurrence of crystalline urine, it is advisable to drink more water and keep the 24-hour urine output above 1200ml.
4. For patients with decreased renal function, the dosage should be adjusted according to renal function.
5. Moderate and severe photosensitive reactions can occur with fluoroquinolones. Excessive exposure to sunlight should be avoided when using this product. In case of photosensitive reaction, the drug should be stopped.
6. Very few patients with glucose-6-phosphate dehydrogenase deficiency may have hemolysis risk when taking this product.
7. Quinolones include this product, which can aggravate the symptoms of myasthenia gravis, respiratory myasthenia and endanger life. Quinolones, including this product, should be used with special caution in patients with myasthenia gravis.
8. In case of severe liver dysfunction (cirrhotic ascites), drug clearance can be reduced, blood drug concentration can be increased, and liver and kidney functions can be decreased, especially. Weigh the advantages and disadvantages, and adjust the dose.
9. Patients with original central nervous system diseases, such as epilepsy and history of epilepsy patients, should avoid application. When there are indications, they should carefully weigh the advantages and disadvantages before application.
Pregnant women and lactating women have used monkeys for reproductive research, and the dose is up to 10 times that of humans. It is found that this product can cause abortion. The plasma peak concentration (Cmax) of this dose in monkeys is about twice that of humans. This product has not been proved to have teratogenic effect in animals. However, no suitable and well controlled study has been conducted in pregnant women, so this product is not suitable for pregnant women. Whether this product is secreted by milk is still lack of data. When 200mg of this product is applied to lactating women, the drug cannot be detected in milk. However, due to the small study dose, the secretion of other varieties of this kind of drugs through milk, and the potential serious adverse reactions to newborns and infants, lactating women should avoid using this product or stop breastfeeding during application.
Medication for children is prohibited for patients under the age of 18.
Elderly patients often have renal dysfunction. Because part of this product is discharged through the kidney, it needs to be reduced.
Drug interaction 1. Urinary Alkalizer can reduce the solubility of this product in urine, resulting in crystalline urine and nephrotoxicity.
2. When combined with theophylline, the competitive inhibition of the binding site with cytochrome P450 may significantly reduce the liver clearance of theophylline and the blood elimination half-life (T1 / 2) β) Prolonged, the blood concentration of theophylline increases, and there are symptoms of theophylline poisoning, such as nausea, vomiting, tremor, uneasiness, excitement, convulsion, palpitation, etc. Therefore, the blood concentration of theophylline should be measured and the dose should be adjusted.
3. The combination of cyclosporine and this product can increase the blood concentration of the former. The blood concentration of cyclosporine must be monitored and the dose must be adjusted.
4. This product can enhance the anticoagulant effect of warfarin when used together with anticoagulant. When used together, the prothrombin time of patients should be closely monitored.
5. Probenecid can reduce the secretion of this product from renal tubules by about 50%. When used together, it can produce toxicity due to the increase of blood concentration of this product.
6. This product has antagonistic effect with nitrofurantoin and is not recommended for combined application.
7. Multi vitamins, other preparations containing iron and zinc ions and acid making drugs containing aluminum or magnesium can reduce the absorption of this product. It is recommended to avoid using it. If it cannot be avoided, take it 2 hours before taking this product or 6 hours after taking it.
8. Didanosine (DDI) can reduce the oral absorption of this product. Because its preparation contains aluminum and magnesium, it can be chelated with fluoroquinolones, so it should not be used together.
9. This product interferes with caffeine metabolism, resulting in reduced caffeine clearance and blood elimination half-life (T1 / 2) β) Prolonged and may produce central nervous system toxicity.
The single oral dose of this product in mice and rats with drug overdose reached 4G / kg, and no lethal effect was found. In case of acute drug overdose, vomiting or gastric lavage should be carried out to promote gastric emptying, the changes of the disease should be carefully observed, symptomatic treatment and supportive therapy should be given. Appropriate fluid replacement volume must be maintained.
Drug toxicology this product is a fluoroquinolone antibacterial drug with broad-spectrum antibacterial effect, especially against aerobic gram-negative bacteria. It has good antibacterial effect on the following bacteria in vitro: most bacteria of Enterobacteriaceae, including enterobacter, Escherichia coli, Klebsiella, Proteus and Salmonella , Shigella, Vibrio, Yersinia, etc. norfloxacin also has antibacterial activity against multidrug-resistant bacteria in vitro. It also has good antibacterial effect against penicillin resistant Neisseria gonorrhoeae, Haemophilus influenzae and catamora. Norfloxacin is a bactericide, which inhibits the synthesis and replication of DNA by acting on the a subunit of bacterial DNA helicase.
Pharmacokinetics during fasting, oral absorption is rapid but incomplete, about 30% ~ 40% of the dosage; it is widely distributed in various tissues and body fluids, such as liver, kidney, lung, prostate, testis, uterus, bile, sputum, blister, blood and urine, but not in the central nervous system. The serum protein binding rate is 10% ~ 15%, and the blood elimination half-life (T1 / 2) β) It lasts for 3 ~ 4 hours, and can be extended to 6 ~ 9 hours in case of renal dysfunction. After a single oral administration of 400mg and 800mg, the blood drug concentration reaches the peak value after 1 ~ 2 hours, and the blood drug peak concentration (Cmax) is 1.4 ~ 1.6mg/l and 2.5mg/l respectively. Kidney (glomerular filtration and renal tubular secretion) And hepatobiliary system are the main excretion routes. 26% ~ 40% are excreted from urine in the form of prototype and less than 10% in the form of metabolites, and 28% ~ 30% are excreted from bile and / or feces. The pH value of urine affects the solubility of this product. The dissolution is the least when the pH value of urine is 7.5, and the dissolution increases when other pH values.
Store under shading and seal.
Executive standard: Chinese Pharmacopoeia, 2005 edition, Part 2