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Actions of Ciprofloxacin in details
Ciprofloxacin is a bactericidal agent which inhibits an essential step in the reproduction of bacterial deoxyribonucleic acid (DNA), the A subunit of DNA gyrase (topoisomerase).
Ciprofloxacin is more potent and has a broader spectrum of activity than nalidixic acid, a non-fluorinated quinolone.
Spectrum: Ciprofloxacin is active against (gram-negative aerobic bacteria). Enterobacteriaceae including Escherichia coli and Citrobacter, Enterobacter, Klebsiella, Proteus, Providencia, Salmonella, Serratia, Shigella, Yersinia spp, Pseudomonas aeruginosa, Hapnia, Edwardsiella, Morganella, Acinetobacter spp, Campylobacter spp, Gardenerella vaginalis, Helicobacter pylori, Legionella spp, Aeromonas, Plesiomonas, Pasteurella multocida and Vibrio spp. Ciprofloxacin has variable activity against Brucella melitensis.
Gram-positive aerobic staphylococci bacteria including penicillinase-producing and nonproducing strains as well as some methicillin-resistant strains are susceptible to ciprofloxacin. Streptococcus pneumoniae and enterococci are less susceptible to the drug.
Ciprofloxacin is also active against Corynebacterium spp and Listeria monocytogenes.
It exerts bactericidal effect against Pseudomonas spp, Haemophilus ducreyi, H. influenzae, Moraxella (Branhamelia) catarrhalis, Neisseria gonorrhea, N. meningitidis. This is also true to β-lactamase-producing strains of H. influenzae, M. catarrhalis and N. gonorrhea.
Mycobacteria, mycoplasmas, rickettsias, Plasmodium falciparum and Clostridium difficile may be sensitive to ciprofloxacin. Moderate susceptibility to ciprofloxacin is exhibited by Chlamydia trachomatis.
Resistance: Bacteroides fragilis, C. difficile, other anaerobic bacteria, Campylobacter spp, non-typhoid Salmonella spp, multi-resistant Salmonella typhii, S. paratyphi and β-lactamase-producing gonococcus are resistant to ciprofloxacin.
Ciprofloxacin is also inactive against against fungi and the spirochete, Treponema pallidum.
Nocardia asteroides, Ureaplasma urealyticum, are usually considered to be resistant to ciprofloxacin.
During treatment with ciprofloxacin, resistant strains of Staphylococcus aureus (including methicillin-resistant strains), P. aeruginosa, Enterobacteriaceae including E. coli and Serratia marcescens were found.
Monotherapy with ciprofloxacin was reported to have caused the development of mutational resistance in mycobacteria.
Cross-resistance exists between ciprofloxacin and other fluoroquinolones.
Resistance of Staphylococcus epidermidis to ciprofloxacin may have been caused by the presence of the drug in sweat.
Effects when Given with Other Antimicrobial Agents: Enhanced effect is exhibited when ciprofloxacin is given with imipenem against P. aeruginosa. The activity of ciprofloxacin against S. aureus and P. aeruginosa is enhanced if given with aminoglycosides. The same is true against anaerobic bacteria if given concomitantly with clindamycin or cefotaxime.
Pharmacokinetics: Ciprofloxacin, upon ingestion, is readily absorbed in the gastrointestinal tract. Peak plasma concentration of 2.5 mcg/mL is reached 1-2 hrs after 500 mg oral dose. The oral bioavailability of the drug is about 70%.
Absorption of the drug may be delayed by food but it does not give significant clinical effects. The plasma half-life (t½) of ciprofloxacin is 3.5-4.5 hrs and may be delayed in patients with end-stage renal disease (8 hrs) and in the elderly. In patients with severe liver cirrhosis, t½ is slightly prolonged.
Ciprofloxacin is 20-40% protein bound. It is widely distributed in body and tissues. It may be seen in the cerebrospinal fluid, 10% in normal meninges, and is able to cross the placenta.
Ciprofloxacin is found to be excreted in breast milk but is mainly excreted in the urine by active tubular secretion and glomerular filtration which may be reduced by probenecid. Other means of elimination include hepatic metabolism, excretion in the bile where high concentration are achieved and transluminal excretion in the intestinal mucosa.
The urinary metabolite of ciprofloxacin is oxociprofloxacin and primary fecal metabolite is suphociprofloxacin.
Oral ciprofloxacin is 40-50% and 15% is excreted in the urine as unchanged drug and metabolite, respectively, within a period of 1 day. Fecal excretion involves 20-35% of ciprofloxacin taken orally.
Few amounts of the drug may be removed by dialysis.
How should I take Ciprofloxacin?
Follow all directions on your prescription label. Do not use this medicine in larger or smaller amounts or for longer than recommended.
Ciprofloxacin is injected into a vein through an IV. You may be shown how to use an IV at home. Do not self-inject this medicine if you do not understand how to give the injection and properly dispose of used needles, IV tubing, and other items used to inject the medicine.
Ciprofloxacin must be injected slowly, over at least 60 minutes.
Drink plenty of liquids while you are using ciprofloxacin.
Ciprofloxacin is usually given every 8 to 12 hours for up to 14 days. Some infections may need to be treated for 4 to 6 weeks. Anthrax exposure is usually treated for 60 days.
Follow your doctor's dosing instructions very carefully.
Use this medicine for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Ciprofloxacin will not treat a viral infection such as the flu or a common cold.
If you use this medicine long-term, you may need frequent medical tests at your doctor's office.
Store at room temperature away from moisture, heat, and light. Do not freeze.
Do not use ciprofloxacin if it has changed colors or has particles in it. Call your pharmacist for new medication.
May be taken with or without food. May be taken w/ meals to minimise GI discomfort. Do not take w/ antacids, Fe or dairy products.
Mechanism of Action
Ciprofloxacin is a member of the fluoroquinolone class of antibacterial agents.
The absolute bioavailability of ciprofloxacin when given as an oral tablet is approximately 70% with no substantial loss by first pass metabolism. Ciprofloxacin maximum serum concentrations and area under the curve are shown in the chart for the 250 mg to 1000 mg dose range (Table 10).
Maximum serum concentrations are attained 1 to 2 hours after oral dosing. Mean concentrations 12 hours after dosing with 250, 500, or 750 mg are 0.1, 0.2, and 0.4 mcg/mL, respectively. The serum elimination half-life in subjects with normal renal function is approximately 4 hours. Serum concentrations increase proportionately with doses up to 1000 mg.
A 500 mg oral dose given every 12 hours has been shown to produce an area under the serum concentration time curve (AUC) equivalent to that produced by an intravenous infusion of 400 mg CIPRO given over 60 minutes every 12 hours. A 750 mg oral dose given every 12 hours has been shown to produce an AUC at steady-state equivalent to that produced by an intravenous infusion of 400 mg given over 60 minutes every 8 hours. A 750 mg oral dose results in a Cmax similar to that observed with a 400 mg intravenous dose. A 250 mg oral dose given every 12 hours produces an AUC equivalent to that produced by an infusion of 200 mg CIPRO given every 12 hours (Table 11).
When CIPRO Tablet is given concomitantly with food, there is a delay in the absorption of the drug, resulting in peak concentrations that occur closer to 2 hours after dosing rather than 1 hour whereas there is no delay observed when CIPRO Suspension is given with food. The overall absorption of CIPRO Tablet or CIPRO Suspension, however, is not substantially affected. The pharmacokinetics of ciprofloxacin given as the suspension are also not affected by food. Avoid concomitant administration of CIPRO with dairy products (like milk or yogurt) or calcium-fortified juices alone since decreased absorption is possible; however, CIPRO may be taken with a meal that contains these products
With oral administration, a 500 mg dose, given as 10 mL of the 5% CIPRO Suspension (containing 250 mg ciprofloxacin/5mL) is bioequivalent to the 500 mg tablet. A 10 mL volume of the 5% CIPRO Suspension (containing 250 mg ciprofloxacin/5mL) is bioequivalent to a 5 mL volume of the 10% CIPRO Suspension (containing 500 mg ciprofloxacin/5mL).
The binding of ciprofloxacin to serum proteins is 20% to 40% which is not likely to be high enough to cause significant protein binding interactions with other drugs.
After oral administration, ciprofloxacin is widely distributed throughout the body. Tissue concentrations often exceed serum concentrations in both men and women, particularly in genital tissue including the prostate. Ciprofloxacin is present in active form in the saliva, nasal and bronchial secretions, mucosa of the sinuses, sputum, skin blister fluid, lymph, peritoneal fluid, bile, and prostatic secretions. Ciprofloxacin has also been detected in lung, skin, fat, muscle, cartilage, and bone. The drug diffuses into the cerebrospinal fluid (CSF); however, CSF concentrations are generally less than 10% of peak serum concentrations. Low levels of the drug have been detected in the aqueous and vitreous humors of the eye.
Four metabolites have been identified in human urine which together account for approximately 15% of an oral dose. The metabolites have antimicrobial activity, but are less active than unchanged ciprofloxacin. Ciprofloxacin is an inhibitor of human cytochrome P450 1A2 (CYP1A2) mediated metabolism. Co-administration of ciprofloxacin with other drugs primarily metabolized by CYP1A2 results in increased plasma concentrations of these drugs and could lead to clinically significant adverse events of the co-administered drug.
The serum elimination half-life in subjects with normal renal function is approximately 4 hours. Approximately 40 to 50% of an orally administered dose is excreted in the urine as unchanged drug. After a 250 mg oral dose, urine concentrations of ciprofloxacin usually exceed 200 mcg/mL during the first two hours and are approximately 30 mcg/mL at 8 to 12 hours after dosing. The urinary excretion of ciprofloxacin is virtually complete within 24 hours after dosing. The renal clearance of ciprofloxacin, which is approximately 300 mL/minute, exceeds the normal glomerular filtration rate of 120 mL/minute. Thus, active tubular secretion would seem to play a significant role in its elimination. Co-administration of probenecid with ciprofloxacin results in about a 50% reduction in the ciprofloxacin renal clearance and a 50% increase in its concentration in the systemic circulation.
Although bile concentrations of ciprofloxacin are several fold higher than serum concentrations after oral dosing, only a small amount of the dose administered is recovered from the bile as unchanged drug. An additional 1% to 2% of the dose is recovered from the bile in the form of metabolites. Approximately 20% to 35% of an oral dose is recovered from the feces within 5 days after dosing. This may arise from either biliary clearance or transintestinal elimination.
Pharmacokinetic studies of the oral (single dose) and intravenous (single and multiple dose) forms of ciprofloxacin indicate that plasma concentrations of ciprofloxacin are higher in elderly subjects (older than 65 years) as compared to young adults. Although the Cmax is increased 16% to 40%, the increase in mean AUC is approximately 30%, and can be at least partially attributed to decreased renal clearance in the elderly. Elimination half-life is only slightly (~20%) prolonged in the elderly. These differences are not considered clinically significant.
In patients with reduced renal function, the half-life of ciprofloxacin is slightly prolonged. Dosage adjustments may be required.
In preliminary studies in patients with stable chronic liver cirrhosis, no significant changes in ciprofloxacin pharmacokinetics have been observed. The kinetics of ciprofloxacin in patients with acute hepatic insufficiency, have not been fully studied.
Following a single oral dose of 10 mg/kg CIPRO suspension to 16 children ranging in age from 4 months to 7 years, the mean Cmax was 2.4 mcg/mL (range: 1.5 mcg/mL to 3.4 mcg/mL) and the mean AUC was 9.2 mcg*hr/mL (range: 5.8 mcg*hr/mL to 14.9 mcg*h/mL). There was no apparent age-dependence, and no notable increase in Cmax or AUC upon multiple dosing (10 mg/kg three times a day). In children with severe sepsis who were given CIPRO IV (10 mg/kg as a 1-hour intravenous infusion), the mean Cmax was 6.1 mcg/mL (range: 4.6 mcg/mL to 8.3 mcg/mL) in 10 children less than 1 year of age; and 7.2 mcg/mL (range: 4.7 mcg/mL to 11.8 mcg/mL) in 10 children between 1 year and 5 years of age. The AUC values were 17.4 mcg*hr/mL (range: 11.8 mcg*hr/mL to 32 mcg*hr/mL) and 16.5 mcg*hr/mL (range: 11 mcg*hr/mL to 23.8 mcg*hr/mL) in the respective age groups. These values are within the range reported for adults at therapeutic doses. Based on population pharmacokinetic analysis of pediatric patients with various infections, the predicted mean half-life in children is approximately 4 hours –5 hours, and the bioavailability of the oral suspension is approximately 60%.
Concurrent administration of antacids containing magnesium hydroxide or aluminum hydroxide may reduce the bioavailability of ciprofloxacin by as much as 90%.
Histamine H2-receptor antagonists
Histamine H2-receptor antagonists appear to have no significant effect on the bioavailability of ciprofloxacin.
The serum concentrations of ciprofloxacin and metronidazole were not altered when these two drugs were given concomitantly.
In a pharmacokinetic study, systemic exposure of tizanidine (4 mg single dose) was significantly increased (Cmax 7-fold, AUC 10-fold) when the drug was given concomitantly with CIPRO (500 mg twice a day for 3 days). Concomitant administration of tizanidine and CIPRO is contraindicated due to the potentiation of hypotensive and sedative effects of tizanidine.
In a study conducted in 12 patients with Parkinson’s disease who were administered 6 mg ropinirole once daily with 500 mg CIPRO twice-daily, the mean Cmax and mean AUC of ropinirole were increased by 60% and 84%, respectively. Monitoring for ropinirole-related adverse reactions and appropriate dose adjustment of ropinirole is recommended during and shortly after co-administration with CIPRO.
Following concomitant administration of 250 mg CIPRO with 304 mg clozapine for 7 days, serum concentrations of clozapine and N-desmethylclozapine were increased by 29% and 31%, respectively. Careful monitoring of clozapine associated adverse reactions and appropriate adjustment of clozapine dosage during and shortly after co-administration with CIPRO are advised.
Following concomitant administration of a single oral dose of 50 mg sildenafil with 500 mg CIPRO to healthy subjects, the mean Cmax and mean AUC of sildenafil were both increased approximately two-fold. Use sildenafil with caution when co-administered with CIPRO due to the expected two-fold increase in the exposure of sildenafil upon co-administration of CIPRO.
In clinical studies it was demonstrated that concomitant use of duloxetine with strong inhibitors of the CYP450 1A2 isozyme such as fluvoxamine, may result in a 5-fold increase in mean AUC and a 2.5-fold increase in mean Cmax of duloxetine.
In a study conducted in 9 healthy volunteers, concomitant use of 1.5 mg/kg IV lidocaine with CIPRO 500 mg twice daily resulted in an increase of lidocaine Cmax and AUC by 12% and 26%, respectively. Although lidocaine treatment was well tolerated at this elevated exposure, a possible interaction with CIPRO and an increase in adverse reactions related to lidocaine may occur upon concomitant administration.
Metoclopramide significantly accelerates the absorption of oral ciprofloxacin resulting in a shorter time to reach maximum plasma concentrations. No significant effect was observed on the bioavailability of ciprofloxacin.
When CIPRO was administered as a single 1000 mg dose concomitantly with omeprazole (40 mg once daily for three days) to 18 healthy volunteers, the mean AUC and Cmax of ciprofloxacin were reduced by 20% and 23%, respectively. The clinical significance of this interaction has not been determined.
MicrobiologyMechanism of Action
The bactericidal action of ciprofloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV (both Type II topoisomerases), which are required for bacterial DNA replication, transcription, repair, and recombination.
Mechanism of Resistance
The mechanism of action of fluoroquinolones, including ciprofloxacin, is different from that of penicillins, cephalosporins, aminoglycosides, macrolides, and tetracyclines; therefore, microorganisms resistant to these classes of drugs may be susceptible to ciprofloxacin. Resistance to fluoroquinolones occurs primarily by either mutations in the DNA gyrases, decreased outer membrane permeability, or drug efflux. In vitro resistance to ciprofloxacin develops slowly by multiple step mutations. Resistance to ciprofloxacin due to spontaneous mutations occurs at a general frequency of between < 10-9 to 1x10-6.
There is no known cross-resistance between ciprofloxacin and other classes of antimicrobials.
Ciprofloxacin has been shown to be active against most isolates of the following bacteria, both in vitro and in clinical infections.
Staphylococcus aureus (methicillin-susceptible isolates only)
Staphylococcus epidermidis (methicillin-susceptible isolates only)
The following in vitro data are available, but their clinical significance is unknown. At least 90 percent of the following bacteria exhibit an in vitro minimum inhibitory concentration (MIC) less than or equal to the susceptible breakpoint for ciprofloxacin (≤1 mcg/mL). However, the efficacy of ciprofloxacin in treating clinical infections due to these bacteria has not been established in adequate and well-controlled clinical trials.
Staphylococcus haemolyticus (methicillin-susceptible isolates only)
Staphylococcus hominis (methicillin-susceptible isolates only)
Susceptibility Test Methods
When available, the clinical microbiology laboratory should provide the results of in vitro susceptibility test results for antimicrobial drug products used in resident hospitals to the physician as periodic reports that describe the susceptibility profile of nosocomial and community-acquired pathogens. These reports should aid the physician in selecting an antibacterial drug product for treatment.
Quantitative methods are used to determine antimicrobial minimum inhibitory concentrations (MICs). These MICs provide estimates of the susceptibility of bacteria to antimicrobial compounds. The MICs should be determined using a standardized test method (broth and/or agar).5,6,7 The MIC values should be interpreted according to criteria provided in Table 12.
Quantitative methods that require measurement of zone diameters can also provide reproducible estimates of the susceptibility of bacteria to antimicrobial compounds. The zone size provides an estimate of the susceptibility of bacteria to antimicrobial compounds. The zone size should be determined using a standardized test method.6,7,8 This procedure uses paper disks impregnated with 5 mcg ciprofloxacin to test the susceptibility of bacteria to ciprofloxacin. The disc diffusion interpretive criteria are provided in Table 12.
A report of “Susceptible” indicates that the antimicrobial is likely to inhibit growth of the pathogen if the antimicrobial compound reaches the concentrations at the site of infection necessary to inhibit growth of the pathogen. A report of “Intermediate” indicates that the result should be considered equivocal, and, if the microorganism is not fully susceptible to alternative, clinically feasible drugs, the test should be repeated. This category implies possible clinical applicability in body sites where the drug is physiologically concentrated or in situations where high dosage of drug can be used. This category also provides a buffer zone that prevents small uncontrolled technical factors from causing major discrepancies in interpretation. A report of “Resistant” indicates that the antimicrobial is not likely to inhibit growth of the pathogen if the antimicrobial compound reaches the concentrations usually achievable at the infection site; other therapy should be selected.
Standardized susceptibility test procedures require the use of laboratory controls to monitor the accuracy and precision of supplies and reagents used in the assay, and the techniques of the individuals performing the test.5,6,7,8 Standard ciprofloxacin powder should provide the following range of MIC values noted in Table 13. For the diffusion technique using the ciprofloxacin 5 mcg disk the criteria in Table 13 should be achieved.
- EPA DSStox. "Ciprofloxacin: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/dsstox... (accessed September 18, 2017).
- NCIt. "Ciprofloxacin: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser/Con... (accessed September 18, 2017).
ReviewsThe results of a survey conducted on ndrugs.com for Ciprofloxacin are given in detail below. The results of the survey conducted are based on the impressions and views of the website users and consumers taking Ciprofloxacin. We implore you to kindly base your medical condition or therapeutic choices on the result or test conducted by a physician or licensed medical practitioners.
2 consumers reported administrationWhen best can I take Ciprofloxacin, on an empty stomach, before or after food?
ndrugs.com website users have also released a report stating that Ciprofloxacin should be taken After food. In any case, this may not be the right description on how you ought to take this Ciprofloxacin. Kindly visit your doctor for more medical advice in this regard. Click here to see other users view on when best the Ciprofloxacin can be taken.