How Effective Is Ciprofloxacin for Cystitis?

Ciprofloxacin sustained-release tablets, the indication is that this product can be used to treat urinary tract infections caused by the following sensitive bacteria, including acute simple pyelonephritis, this product and ciprofloxacin immediate-release tablets are not interchangeable. Simple urethral infection (acute cystitis): caused by E. coli, Proteus mirabilis, Enterococcus faecalis, and Staphylococcus saprophytic ^a . Complex urinary tract infection: caused by E. coli, Klebsiella pneumoniae, Enterococcus faecalis, Proteus mirabilis, Pseudomonas aeruginosa ^a . Acute simple pyelonephritis: Caused by E. coli. a: In studies treating organ infections caused by this pathogen, there were fewer than 10 subjects. The safety and effectiveness of this product for the treatment of infections other than urinary tract infections have not been proven. Bacterial culture and drug sensitivity tests should be performed before drug treatment to isolate and identify the bacteria that cause the infection and determine whether they are sensitive to ciprofloxacin. This product may have been used before the test results come out. Once the results are available, only those who are suitable for ciprofloxacin treatment should continue to use it. Regular bacterial cultures and susceptibility tests during treatment not only provide information on the effectiveness of the treatment, but also the possibility of bacterial tolerance.

Drug Name: Ciprofloxacin sustained-release tablets

Drug type: prescription
Use classification: Synthetic antibacterials

Ciprofloxacin sustained release tablets ingredients

The main ingredient of this product is ciprofloxacin. Its chemical name is: 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7- (1-piperazinyl) -3-quine Porphyrin carboxylic acid.
Molecular formula: C ₁₇ H ₁₈ FN ₃ O ₃
Molecular weight: 331.346.

Ciprofloxacin sustained release tablets

This product is a white to off-white film-coated tablet, which appears white or off-white except for the coating.

Ciprofloxacin sustained-release tablets indications

This product can be used to treat urinary tract infections caused by the following sensitive bacteria, including acute simple pyelonephritis. This product and ciprofloxacin immediate-release tablets are not interchangeable.
Simple urethral infection (acute cystitis): caused by E. coli, Proteus mirabilis, Enterococcus faecalis, Staphylococcus saprophyticus [sup] a [/ sup].
Complex urinary tract infection: caused by E. coli, Klebsiella pneumoniae, Enterococcus faecalis, Proteus mirabilis, Pseudomonas aeruginosa [sup] a [/ sup].
Acute simple pyelonephritis: Caused by E. coli.
a: In studies treating organ infections caused by this pathogen, there were fewer than 10 subjects.
The safety and effectiveness of this product for the treatment of infections other than urinary tract infections have not been proven.
Bacterial culture and drug sensitivity tests should be performed before drug treatment to isolate and identify the bacteria that cause the infection and determine whether they are sensitive to ciprofloxacin. This product may have been used before the test results come out. Once the results are available, only those who are suitable for ciprofloxacin treatment should continue to use it. Regular bacterial cultures and susceptibility tests during treatment not only provide information on the effectiveness of the treatment, but also the possibility of bacterial tolerance.

Ciprofloxacin sustained-release tablets specifications

500mg

Ciprofloxacin sustained-release tablets

This product is not interchangeable with ciprofloxacin immediate release tablets, and should be taken orally as shown in the table below. This product should be taken immediately after meals. It must be taken whole and not taken apart, crushed or chewed. .
Recommended dose:
Simple urethral infection (including acute cystitis) 500 mg once a day for 3 days.
Complex urethral infection 1000 mg once a day for 7-14 days.
Acute simple pyelonephritis 1000 mg once a day for 7-14 days.
Patients with urinary tract infections treated with ciprofloxacin immediate release tablets can switch to this product under the guidance of a physician.
If taking antacids containing magnesium / aluminum, sucralfate, VIDEX chew / buffer tablets or pediatric granules, calcium, iron, zinc and other high-buffering drugs, they should be taken 2 hours before or 6 hours later. Take. This product should be avoided with milk, calcium-rich fruit juice and other foods, so as not to affect its absorption. It is recommended to take at least 2 hours between taking this product and ingesting calcium and other substances.
Ciprofloxacin is mainly eliminated by renal secretion in patients with renal insufficiency. It can also be metabolized by the bile system and partially cleared from the intestine. These pathways can reduce the decrease of renal excretion due to renal insufficiency. Patients with simple urethral infection do not need to adjust the dose when taking 500 mg of this product; while for patients with complex urethral infection and acute simple pyelonephritis, the dose of this product should be changed from less than 30 ml / min. 1000 mg per day to 500 mg per day; for patients undergoing hemodialysis or peritoneal dialysis, this product can be taken after the dialysis process.
Patients with hepatic insufficiency have no need to adjust the dose when taking this product in patients with liver cirrhosis compensatory stage, but for patients with acute liver insufficiency, the pharmacokinetics of ciprofloxacin have not been fully explained.

Ciprofloxacin sustained-release tablets adverse reactions

In clinical trials of 961 patients with urethral infection receiving 500 mg or 1000 mg of this product, most of the adverse reactions were mild to moderate, and no treatment was needed. The types and distribution of adverse reactions at two dose levels were similar.
In the clinical trial of simple urethral infection, 444 patients received 500 mg of this product once a day, and 447 patients received ciprofloxacin immediate-release tablets 250 mg, BID for 3 days due to drug-related adverse reactions. Among the discontinued patients, 0.2% (1/444) of the ciprofloxacin sustained-release tablet group and 0% (1/447) of the control group.
In clinical trials of complex urinary tract infections and acute simple pyelonephritis, 517 patients received 500 mg of this product once a day, and 518 patients received ciprofloxacin immediate-release tablets 250 mg, BID, a total of 7-14 Of the patients discontinued due to drug-related adverse reactions, 3.1% (16/517) of the ciprofloxacin sustained-release tablet group and 2.3% (12/518) of the control group. The common causes of drug withdrawal in the test group were nausea, vomiting (4 cases), and dizziness (3 cases), while the common causes in the control group were nausea and vomiting (3 cases).
In these clinical trials, whether related to the drug or not, the incidence of adverse reactions in the ciprofloxacin sustained-release tablet group was 2%: nausea (4%), headache (3%), dizziness (2%), and diarrhea ( 2%), vomiting (2%), vaginal candidiasis (2%).
Among all patients in the 1000 mg ciprofloxacin sustained-release tablet group, researchers determined that the incidence of at least 31% of possible adverse reactions associated with the drug was: nausea (3%), headache (1%), and dizziness (1%). , Diarrhea (2%), vomiting (1%), indigestion (1%), vaginal candidiasis (1%).
Other infrequent adverse reactions that may be related to the drug, the incidence of patients in the ciprofloxacin sustained-release tablet group is less than 1%:
Systemic reactions: abdominal pain, weakness, cachexia, phototoxic cardiovascular: slow heartbeat, migraine, syncope digestion: loss of appetite, constipation, dry mouth, bloating, abnormal liver function, thirst blood / lymph: thrombin lowers central nervous system System: Nightmares, Split Personality, Depression, Hypertension, Disorders, Insomnia, Tremor, Dizziness Metabolism: Hyperglycemia Skin / Accessories: Dry skin, maculopapular, pruritus, rash, skin disorders, rubella, macrovascular herpes Special senses: diplopia, reversed taste, urogenital: dysmenorrhea, hematuria, renal dysfunction, candidiasis. The following adverse reactions are derived from clinical trials of ciprofloxacin and global post-marketing data (including all dosage forms, doses, courses and symptoms) There is no particular correlation between the ranking and the relationship between symptoms and drugs. Because this report is from an uncertain population, it is not entirely possible to reliably assess the incidence of adverse reactions and the correlation with medications. Reported adverse reactions include: pain, acidosis, anxiety, agranulocytosis, allergic reactions (rubella to allergic reactions), anemia, angina pectoris, edema, anorexia, anxiety, arrhythmia, joint pain, ataxia, atrial Flutter, bleeding quality, blurred vision, bronchospasm, refractory diarrhea, candidiasis (skin and mouth), candidiasis, cardiac murmur, cardiopulmonary arrest, cardiovascular shock, cerebral thrombosis, chills, jaundice, insanity , Convulsions, forgetfulness, drowsiness, difficulty swallowing, speech disorders, dyspnea, edema (conjunctiva, face, hands, throat, tongue, lower limbs, neck, lungs), nosebleeds, multiple rashes, nodular erythema, exfoliative Dermatitis, fever, flushing, gastrointestinal bleeding, gout (sudden attack), male and female breasts, hallucinations, hearing loss, hemolytic anemia, hemoptysis, hemorrhagic cystitis, liver gangrene, hiccup, hyperpigmentation, high Blood pressure, hypotension, intestinal obstruction, interstitial nephritis, intestinal perforation, joint sclerosis, lethargy, mild headache, lymphadenopathy, manic reaction, myalgia, myasthenia (May worsen), myocardial infarction, myoclonus, nephritis, nightmares, nystagmus, mouth ulcers, pain (arm, back, fore chest, thorax, upper abdomen, eyes, feet, jaw, neck, oral mucosa), Palpitations, pancreatitis, paranoia, paresthesia, perspiration (increased), phobia, pleural effusion, polyuria, kidney stones, renal failure, apnea, respiratory distress syndrome, restlessness, Stevens-Johnson syndrome, heartbeat Speeding, loss of taste, tendinitis, tendon fissure, tinnitus, toxic epidermal necrosis, toxic psychosis, dullness, urethral bleeding, urinary retention, frequent urination, vaginal pruritus, vasculitis, ventricular ectopic, blistering, decreased visual acuity , Visual impairment (astigmatism, change in color resolution, fear of light).
Changes in laboratory test values After using ciprofloxacin (including all dosage forms, dosages, treatment courses, and symptoms), whether related to the drug or not, the following adverse laboratory changes have been reported:
Decreased: blood glucose, BUN, hematocrit, hemoglobin, white blood cell count, platelet count, prothrombin time, serum albumin, serum sodium, total protein, increased uric acid: alkaline phosphatase, ALT (SGPT), AST (SGOT), atypical lymphocyte count, blood glucose, monocytes, BUN, cholesterol, eosinophil count, LDH, platelet count, prothrombin time, erythrocyte sedimentation rate, serum amylase, serum bilirubin, serum calcium , Serum cholesterol, serum creatinine kinase, serum creatinine, GGT, blood sodium, serum theophylline (if combined), serum triglycerides, uric acid, etc. Other: proteinuria, changes in phenytoin concentration, crystal urine, cast urine, immature white blood cells , Leukocytosis, macroglobulinemia, pancytopenia.

Ciprofloxacin sustained-release tablets contraindications

This product is contraindicated in people with a history of allergies to ciprofloxacin or any other quinolone.

Precautions for ciprofloxacin sustained-release tablets

The effectiveness and safety of this product for children and adolescents (under 18 years of age), pregnant women, and lactating women have not been established. Ciprofloxacin can cause lameness in juvenile dogs. Histological examination revealed permanent cartilage defects in the dog's load-bearing joints. Related quinolone drugs can also cause load-bearing articular cartilage erosion and other joint diseases in different kinds of juvenile animals.
It has been reported that patients taking quinolone (including ciprofloxacin) can cause convulsions, increased intracranial pressure, and psychosis. Ciprofloxacin can also cause CNS toxic reactions, including: dizziness, confusion, tremor, visual abnormalities, mental depression, and depression. Rare suicidal tendencies, etc. These reactions may occur at the first dose. If these reactions occur in patients taking ciprofloxacin, the drug should be discontinued and appropriate measures taken. Ciprofloxacin, like all quinolones, is known or has a history of suspected CNS disorders, possible seizures or very low seizure thresholds (such as severe cerebral arteriosclerosis and a history of epilepsy), and may cause seizures or reductions Patients with seizure threshold risk factors (such as certain medications, renal failure) should be used with caution.
There are also reports of severe and fatal reactions when ciprofloxacin is combined with theophylline. These reactions include: cardiac arrest, seizures, status epilepticus, and respiratory failure. Although these reactions can also occur with theophylline alone, they are more likely to occur when combined with ciprofloxacin. If the two must be combined, the theophylline concentration must be monitored and appropriate dose adjustments made.
When taking quinolone for the first time, severe (sometimes fatal) allergic reactions such as cardiovascular failure, loss of will, tingling sensation, edema of the pharynx or face, dyspnea, rubella, and itching can also occur. Only a few patients have such allergic reactions. When severe allergic reactions occur, adrenaline, oxygen, hormones should be given immediately and the airway should be kept open (including tracheal intubation).
Severe severe allergic reactions are: rash, fever, eosinophilia, jaundice, and liver necrosis. These reactions may be related to the inability of ciprofloxacin to be excreted. When a rash or other allergic symptoms occur, the drug should be discontinued immediately.
Pseudomembranous colitis can occur after taking all types of antibiotics, including ciprofloxacin, and some are milder and some are life-threatening. Therefore, when diarrhea occurs after taking antibiotics, we must pay attention to consider this diagnosis.
Antibiotic treatment can change the normal flora in the colon, causing Clostridium to overgrow, and one of its toxic products is one of the causes of "antibiotic-associated colitis".
Once pseudomembranous colitis is confirmed, it must be treated immediately. Many patients only need to stop the drug. For moderate to severe patients, consider infusion, electrolyte and protein supplementation, and use antibiotics against Clostridium colitis.
Ciprofloxacin and other quinolones can also cause rupture of the Achilles tendon and other tendons, resulting in disability and must be repaired surgically. If the patient has tendon pain, inflammation or rupture, the drug should be stopped immediately.
Be wary of general conditions: Ciprofloxacin crystals are rarely observed in human urine, but they are often found in laboratory animals, because animal urine is usually alkaline. Ciprofloxacin-related crystals have rarely been found in human urine because human urine is acidic. Therefore, after the application of ciprofloxacin, alkaline urine should be avoided, and patients should drink plenty of water to prevent the urine from being too concentrated.
Quinolones (including ciprofloxacin) can also cause CNS toxic reactions, including: restlessness, agitation, insomnia, irritability, nightmares, and delusions.
Phototoxicity can also occur after quinolone is used in patients. When patients are exposed to sunlight, such drugs can aggravate sunlight burns, so excessive sunlight should be avoided. The drug should be discontinued in patients with phototoxicity.
Information for patients As with other quinolones, avoid taking them with antacids containing magnesium or aluminum, sucralfate, VIDEX) chew / buffer tablets or pediatric granules, metal cations such as iron, and vitamin preparations containing zinc. This product should be taken 2 hours before or 6 hours after taking the above preparation. This product should be avoided with dairy products (milk, yogurt), calcium-rich fruit juice and other foods, because it can reduce the absorption of ciprofloxacin, but this product can be taken at the same time with foods containing such products.
If you forget to take the medicine on time, you can take it on the same day, but the maximum daily dose does not exceed 2 tablets. Swallow this product whole, do not break, crush or chew this product.
Ciprofloxacin can cause allergic reactions, even in a single dose, this product should be discontinued once a rash or other allergic reaction is found.
After taking this product, avoid excessive sunlight or artificial ultraviolet light. If phototoxic reaction is found, stop using this product.
If the patient has pain, inflammation or tendon fissure, treatment should be stopped and the physician should be informed that the patient should rest and avoid exercise.
This product can cause dizziness or a slight headache, but patients should know how they respond to this product before driving, operating machines or performing delicate actions that require alertness or coordination.
This product can increase the effect of theophylline and caffeine. When taking quinolones with caffeine-containing products, caffeine accumulation may occur.
It has been reported that taking quinolone (including ciprofloxacin) can cause epilepsy. If the patient has epilepsy, the physician should be notified before taking this product.

Ciprofloxacin sustained-release tablets for pregnant and lactating women

Medication for pregnant women:
There are no adequate and well-controlled studies of medications in pregnant women. The literature reports that a trial of ciprofloxacin in pregnant women by TERIS (teratogenic information system) has shown that it is not possible to produce a substantial teratogenic risk at therapeutic doses during pregnancy, but the data are insufficient to show that it is not harmful.
A controlled prospective observational trial included a total of 200 women who used fluoroquinolones during pregnancy (52.5% used ciprofloxacin and 68% took the drug during the first 3 months of pregnancy). Exposure to fluoroquinolones in the womb during embryogenesis did not increase the risk of major malformations. The major congenital malformations in the fluoroquinolone group and the control group were 2.2% and 2.6% (typically 1-5%). There were no differences in the rates of automatic abortion, preterm birth and underweight between the two groups, and no significant clinically significant skeletal or muscular disorders were found when the child was 1 year old.
Another prospective in-depth study reported that 549 pregnant women used fluoroquinolones (93% in the first 3 months of pregnancy) and a total of 70 pregnant women took ciprofloxacin in the first 3 months of pregnancy. The deformity rates of the ciprofloxacin group and the fluoroquinolone group were within the normal range. No congenital malformations were found. This study did not find any significant adverse reactions caused by factor palace exposure to ciprofloxacin.
Pregnancy, spontaneous abortion, and low birth weight were not significantly changed in pregnant women who used ciprofloxacin. However, these small post-marketing epidemiological studies (most of which are short-term studies-initial 3 months) cannot fully evaluate the harm of non-general defects or draw authoritative conclusions about the safety and reliability of ciprofloxacin for pregnant women and fetuses. Pregnant women should avoid taking ciprofloxacin unless the potential significance to the mother and child is greater than the potential harm.
Ciprofloxacin has been studied for preterm birth toxicity in mice and rats at an oral dose of 100 mg / kg (based on body surface area, 0.7 and 0.4 times the maximum daily human dose of 1000 mg, respectively). No serious harm to the fetus was found. Ciprofloxacin (orally administered 30 and 100 mg / kg) caused gastrointestinal disturbances in rabbits in toxicity tests, causing maternal weight loss and increasing abortion rates, but no teratogenicity was found in each dose group toxicity. Intravenous administration of 20 mg / kg to rabbits did not cause rabbit maternal toxicity, and no teratogenic and embryonic toxicity were found.
Medication for lactating women: Ciprofloxacin is secreted through breast milk. The amount of ciprofloxacin absorbed by infants through breast milk is unknown. Because the mother is taking ciprofloxacin for its potentially serious harm to the nursing infant, the importance of the drug to the mother should be considered to decide whether to discontinue breastfeeding or discontinue medication.

Ciprofloxacin sustained-release tablets for children

The effectiveness and safety of this product for children and adolescents (under 18 years) have not been established. Ciprofloxacin can cause joint disease in young animals.

Ciprofloxacin sustained-release tablets for elderly

In a large, prospective, randomized clinical study of this product for the treatment of complex urethral infections, 49% (509/1035) patients are over 65 years old (including 65 years old), and 30% (308/1035) patients are over 75 years old ( 75 years old). There is no general difference in safety and effectiveness between elderly patients and young patients, and clinical trials with other preparations of ciprofloxacin have not proven the difference between the two, but it does not rule out that some elderly patients have higher sensitivity Sex. Ciprofloxacin is known to be excreted mainly through the kidney, so patients with impaired renal function have a higher risk of adverse reactions. Elderly patients with normal renal function (65 years of age) do not need to adjust the dosage. However, some elderly patients' renal function declines with age. Careful choice of dosage and renal function monitoring should be performed.

Ciprofloxacin sustained-release tablets drug interactions

Similar to other quinolones, ciprofloxacin and theophylline can increase the serum concentration of theophylline and prolong the elimination half-life, which may increase the adverse reactions related to theophylline. If necessary, the concentration of theophylline must be monitored and appropriate dosage adjustments made.
Some quinolones (including ciprofloxacin) can also affect the metabolism of caffeine, thereby reducing the clearance of caffeine and extending its serum half-life.
It is possible to take quinolones (including ciprofloxacin) with polyvalent cationic preparations (such as antacids containing magnesium or aluminum), sucralfate, VIDEX chew / buffer tablets or children's granules, and calcium / zinc ion preparation Affect the absorption of quinolone, resulting in lower serum and urine concentrations of traditional Chinese medicine. This product should be taken 2 hours before or 6 hours after taking antacids containing magnesium or aluminum, sucralfate, VIDEX chew / buffer tablets or pediatric granules, metal cations such as iron, and vitamin preparations containing zinc.
Histamine H ₂ receptor antagonists may not have a significant effect on the bioavailability of ciprofloxacin.
When combined with omeprazole, the absorption of ciprofloxacin is slightly reduced (20%). However, the clinical significance of this interaction has not been proven.
When ciprofloxacin was used in combination with phenytoin, changes in serum phenytoin concentrations (increased or decreased) in patients were reported.
Severe allergic reactions have been reported when this product is used in combination with glibenclamide (very rare).
Some quinolones (including ciprofloxacin) combined with cyclosporine can cause a transient increase in serum creatinine.
It has been reported that quinolones can enhance the effect of the oral anticoagulant warfarin or its derivatives. When combined with such drugs, the clotting time should be closely monitored or other appropriate clotting tests should be performed.
Probenecid can affect the secretion process of ciprofloxacin in the renal tubules and increase its plasma concentration. This should be considered if the patient is taking both drugs together.

Ciprofloxacin sustained-release tablets overdose

In the event of an acute overdose, the stomach must be emptied by vomiting or gastric lavage. Patients should be carefully observed and given supportive treatment, including antacids containing magnesium or calcium, to reduce the absorption of ciprofloxacin, and to maintain a proper fluid. Hemodialysis or peritoneal dialysis can only excrete small amounts of ciprofloxacin.
In mice, rats, rabbits, and dogs, when ciprofloxacin is at a concentration of 125-300 mg / kg, obvious toxic effects can occur, including tonicity / intermittent seizures.
Ciprofloxacin was administered orally in a single dose and was relatively less toxic to mice, rats, and dogs. No deaths were found within 14 days of treatment in the highest dose group (5,000 mg / kg for rodents, 2500 mg / kg for dogs), but within two days Reduced activity and cyanosis were observed in this rodent species, and severe vomiting was observed in dogs; in rabbit experiments, ciprofloxacin reached a high mortality rate of 2500 mg / kg, but after 10-14 days of administration, These animals have reduced mortality.

Clinical trial of ciprofloxacin sustained-release tablets

Simple urethral infections (including acute cystitis):
A randomized, double-blind, controlled clinical trial of CIPRO XR in the treatment of simple urethral infections was performed in the United States. This trial evaluated CIPRO XR 500 mg OD and ciprofloxacin immediate-release 250 mg, BID in 905 patients. In the effect, there were 452 people in the CIPRO XR group and 453 people in the control group. The main evaluation index was the elimination of baseline bacteria during the cure test (4-11 days after treatment), and there were no new infections or secondary infections.
The results showed that bacterial clearance and clinical effectiveness were similar between the two groups. The clearance rate, clinical effectiveness, and 95% confidence interval of the two (CIPRO XR group minus the control group) are as follows:

Complex urethral infections and acute simple pyelonephritis:
A randomized double-blind, controlled clinical trial in the United States and Canada evaluated the efficacy of CIPRO XR for complex urethral infection (cUTI) and acute simple pyelonephritis (AUP). The trial enrolled 1042 patients, of whom 521 were in the treatment group. CIPRO XR (1000 mg once a day for 7 to 14 days) was compared with ciprofloxacin immediate-release tablets (500 mg twice a day for 7 to 14 days). Days). The primary criterion for judging the endpoint of treatment (TOC) was the baseline bacterial clearance of patients treated with the protocol (PP) and modified protocol (MITT) without new or repeated infections from 5 to 11 days after treatment.
The population treated according to the plan is defined as patients diagnosed with cUTI or AUP. The pathogenic bacteria at baseline are 10 [sup] 5 [/ sup] CFU / mL, which does not violate the selection criteria. It is positive by urine culture. The drug is sensitive, there is no withdrawal or loss of follow-up, and follow the medication regulations. Compared with the control group, more patients in the treatment group were excluded. The reason should be explained in the results. The reasons for the large discrepancy between the two groups were that there were no effective urine culture results, bacteria were resistant to the drug, and treatment was discontinued due to adverse reactions.
All patients who were able to isolate pathogens and take test drugs at baseline were defined as the MITT population, including 342 in the CIPRO XR group and 324 in the control group. Lost follow-up patients were considered invalid cases in the analysis. In the MITT analysis of cUTI patients, the bacterial clearance rates of CIPRO XR and the control group were 160/271 (59.0%) and 156/248 (62.9%) [97.5% CI * (-13.5%, 5.7%)]. The clinical cure rates of CIPRO XR and the control group were 184/271 (67.9%) and 182/248 (73.4%) [97.5% CI * (-26.8%, 6.5%)]. In the MITT analysis, the bacterial clearance of CIPRO XR and the control group of AUP patients was 47/71 (66.2%) and 58/76 (76.3%), [97.5% CI * (-26.8%, 6.5%)], the clinical cure rates were 50/71 (70.4%) and 58/76 (76.3%), [97.5% CI * (-22.0%, 10.4%)].
*: Difference rate confidence interval (CIPRO XR minus control group)
In the PP population, the difference in bacterial clearance between the CIPRO XR group and the control group at the time of TOC follow-up was inconsistent among AUP and cUTI patients. In cUTI patients, the CIPRO XR group was higher than the control group, while in AUP patients, the CIPRO XR group was lower than the control group. This discrepancy was not reflected in the cure rates of the two groups. The clinical cure rates of CIPRO XR and control group were 96.1% (198/206) and 92.1% (211/229).
At the time of TOC follow-up, according to the infection classification, in the PP population, the corresponding 97.5% confidence intervals for the bacterial clearance rate and clinical cure rate and difference rate (CIPRO XR minus control group) in the CIPRO XR group and the control group are shown in the following table:

Of the 166 patients taking this product for complex urethral infections, 148 (89%) of the pathogens were cleared, 8 (5%) were not cleared, 5 (3%) had repeated infections, and 5 ( 3%) new infections occurred. Of the 177 patients in the control group, 144 (81%) were cleared of pathogenic bacteria, 16 (9%) were not cleared, 3 (2%) had repeated infections, and 14 (8%) had new infections. . Of the 40 patients taking this product to treat AUP infection, 35 (87.5%) of the pathogenic bacteria were cleared, 2 (5%) were not cleared, and 3 (7.5%) developed new infections. In TOC, 5 cases of patients taking this product for AUP did not find bacterial clearance, and 4 cases were considered clinically cured without antibiotic replacement therapy. Of the 52 controls, 51 (98%) were cleared of pathogenic bacteria, and 1 (2%) was not cleared.

Ciprofloxacin sustained-release tablets pharmacology and toxicology

Pharmacological effects: This product has a broad-spectrum antibacterial effect, especially high antibacterial activity against aerobic gram-negative bacilli, and has good antibacterial effect on the following bacteria in vitro: most bacteria of the family Enterobacteriaceae, including Citrobacter, cloaca , Enterobacter, such as Enterobacter aerogenes, Escherichia coli, Klebsiella, Proteus, Salmonella, Shigella, Vibrio, Yersinia, etc. Often has antibacterial activity against multiple drug-resistant bacteria. Penicillin-resistant Neisseria gonorrhoeae, H. influenzae, and Moraxella all have high antibacterial activity. It has antibacterial effect on most strains of Pseudomonas, such as Pseudomonas aeruginosa. This product has antibacterial activity against methicillin-sensitive Staphylococcus, and only moderate antibacterial activity against Streptococcus pneumoniae, Streptococcus hemolyticus and Enterococcus faecalis. It has good anti-microbial effect on Chlamydia trachomatis, Mycoplasma and Legionella, and it also has antibacterial activity against Mycobacterium tuberculosis and atypical Mycobacterium. Poor antibacterial activity against anaerobic bacteria.
Ciprofloxacin is a fungicide that acts on the A subunit of bacterial DNA helicase to inhibit DNA synthesis and replication and cause bacterial death.
Toxicology research:
Carcinogenicity and mutagenicity: 8 in vitro mutagenicity tests have been performed on ciprofloxacin, and 2 of them were positive (rat liver cell DNA repair test and mouse lymphoma cell back mutation test). But in vitro tests of rat liver cell DNA repair test, micronucleus test (mouse), and dominant lethal test (mouse) were negative. Long-term carcinogenicity in vivo tests on rats and mice have been completed. After daily oral administration for 2 years, ciprofloxacin was not found to have any carcinogenic and tumorigenic effects.
Reproductive toxicity: Reproductive studies with rats and mice taking 6 times the usual daily dose of humans have not been found to be harmful to the fetus or cause fertility impairment. Ciprofloxacin has gastrointestinal disturbances when used in rabbits (30 and 100 mg / kg orally) resulting in weight loss and miscarriage in female rabbits. However, no teratogenic effect was observed at both doses. After intravenous administration of up to 20 mg / kg, there was no maternal toxicity, embryo toxicity or teratogenic effects. However, adequate, well-controlled studies have not been conducted in pregnant women. Ciprofloxacin should only be used for pregnant women if its potential benefits outweigh the potential danger to the fetus.

Pharmacokinetics of Ciprofloxacin Sustained-release Tablets

Compared with the immediate release tablets, the absorption of this product is a preparation of slow-release drugs.
After taking this product, the time to reach the peak plasma concentration of ciprofloxacin is 1-5 hours. Compared with ciprofloxacin immediate-release tablets 250 mg twice daily, this product is 500 mg once daily. The peak concentration is higher, and the 24-hour AUC of the immediate-release tablets and the sustained-release tablets is equal.
The following table compares the steady-state pharmacokinetic parameters of ciprofloxacin sustained-release tablets 500 mg once daily and ciprofloxacin immediate-release tablets 250 g twice daily.

The volume of distributed ciprofloxacin is about 2.1-2.7 L / Kg. Studies have shown that ciprofloxacin can penetrate into a variety of tissues, whether oral or intravenous. Ciprofloxacin has a serum protein binding rate of 20-40%, and there is insufficient evidence to suggest that protein binding rates are related to interactions with other drugs.
Metabolic ciprofloxacin has four metabolites in human urine. These metabolites also have antibacterial activity, but are lower than the prototype ciprofloxacin. The main metabolites are oxociprofloxacin (M3) and thiociprofloxacin (M2), each of which is about 3-8% of the total dose. The other secondary metabolite is desethylciprofloxacin. (M1) and formylciprofloxacin (M4). Drugs and metabolites are in the same proportions in serum as in urine, and these metabolites are almost completely excreted 24 hours after taking the drug.
Elimination kinetics of ciprofloxacin immediate-release tablets and sustained-release tablets are similar. In a comparative study of the two, both were about 35% of the oral doses excreted from the urine as prototypes and were completely excreted 24 hours after oral administration. The renal clearance of ciprofloxacin is 300 ml / min, which exceeds the normal glomerular filtration rate of 120 ml / min. Therefore, the active secretion of glomeruli plays a significant role in the excretion process. When ciprofloxacin immediate release tablets are taken with probenecid, the renal clearance of ciprofloxacin can be reduced by 50%, and the blood concentration can be increased by 50%. After taking ciprofloxacin immediate-release tablets, although the concentration of ciprofloxacin in the bile was several times higher than that in the serum, there were only a few prototype drugs in the bile. In addition, metabolites were found in bile at 1-2% of the dose taken. Within 5 days after oral immediate-release tablets, about 20-35% of the drug is excreted in the feces, that is, biliary or intestinal elimination is formed.
Pharmacokinetic tests of ciprofloxacin immediate-release tablets (single-dose) and intravenous preparations (single-dose and multiple-dose) in special populations show that the elderly have higher blood concentrations and Cmax than young The increase of 16-40%, with an average AUC increase of about 30%, is at least partly due to reduced renal clearance in the elderly. The elimination half-life of the elderly is slightly extended (approximately 20%), and these differences are not clinically significant.
For patients with low renal function, the half-life of ciprofloxacin is slightly extended. Patients with simple urinary tract infections do not need to adjust the dose if taking 500 mg of this product. For patients with complex urinary tract infections and acute simple pyelonephritis, taking 1000 mg is also appropriate. When the creatinine clearance is below 30 ml / min, the dosage of this product can be reduced to 500 mg once a day.
For patients with compensatory cirrhosis, the pharmacokinetics of ciprofloxacin did not change significantly, but for patients with acute liver damage, no adequate studies have been performed.

Storage of Ciprofloxacin Sustained-release Tablets

Shaded and sealed.

Ciprofloxacin sustained release tablets packaging

Packed in aluminum foil, 4 pcs / board, 5 pcs / board, 6 pcs / board, 1 pc / box.

Expiration Date of Ciprofloxacin Sustained Release Tablets

24 months ^[1]