Ciprofloxacin Actions

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Actions of Ciprofloxacin in details

infoThe action of the drug on the human body is called Pharmacodynamics in Medical terminology. To produce its effect and to change the pathological process that is happening the body and to reduce the symptom or cure the disease, the medicine has to function in a specific way. The changes it does to the body at cellular level gives the desired result of treating a disease. Drugs act by stimulating or inhibiting a receptor or an enzyme or a protein most of the times. Medications are produced in such a way that the ingredients target the specific site and bring about chemical changes in the body that can stop or reverse the chemical reaction which is causing the disease.
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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?

Take ciprofloxacin only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.

ciprofloxacin comes with a Medication Guide. Read and follow the instructions carefully. Ask your doctor if you have any questions.

ciprofloxacin works best when there is a constant amount in the blood or urine. To help keep the amount constant, do not miss any doses. Also, it is best to take the doses at evenly spaced times, day and night. For example, if you are to take one dose a day, try to take it at the same time each day.

If you need to take ciprofloxacin for anthrax infection, your doctor will want you to begin taking it as soon as possible after you are exposed to anthrax.

Swallow the extended-release tablet whole. Do not crush, split, or chew it.

Shake the oral liquid for at least 15 seconds just before each use. The oral liquid has small microcapsules floating in it. These microcapsules may look like bubbles or small beads. Do not chew the microcapsules when you take the oral liquid. Measure the oral liquid with the marked measuring spoon that comes with the bottle.

You may take ciprofloxacin with or without food. However, Proquin® XR tablets should be taken with a main meal, preferably the evening meal.

Drink plenty of fluids while you are taking ciprofloxacin. Drinking extra water will help prevent some unwanted effects of ciprofloxacin.

Do not take ciprofloxacin alone with milk, yogurt, or other dairy products. Do not drink any juice with calcium added when you take ciprofloxacin. It is okay to have dairy products or juice as part of a larger meal when you take ciprofloxacin.

If you are taking aluminum or magnesium-containing antacids, iron supplements, multivitamins, didanosine (Videx®), lanthanum carbonate (Fosrenol®), sevelamer (Renagel®), sucralfate (Carafate®), or any products containing calcium or zinc, do not take them at the same time that you take ciprofloxacin. It is best to take these medicines at least 2 hours before or 4 to 6 hours after taking ciprofloxacin. These medicines may keep ciprofloxacin from working properly.

Keep using ciprofloxacin for the full treatment time, even if you feel better after the first few doses. Your infection may not clear up if you stop using the medicine too soon.

Dosing

The dose of ciprofloxacin will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of ciprofloxacin. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (extended-release tablets):
    • For uncomplicated urinary tract infections (acute cystitis):
      • Adults—500 milligrams (mg) once a day for 3 days.
      • Children—Use and dose must be determined by your doctor.
    • For complicated urinary tract infections:
      • Adults—1000 milligrams (mg) once a day.
      • Children—Use and dose must be determined by your doctor.
    • For acute uncomplicated pyelonephritis:
      • Adults—1000 milligrams (mg) once a day.
      • Children—Use and dose must be determined by your doctor.
  • For oral dosage forms (suspension or tablets):
    • For infections:
      • Adults—250 to 750 milligrams (mg) two times a day, taken every 12 hours.
      • Children—Use and dose must be determined by your doctor.
    • For urinary tract or serious kidney infections:
      • Adults—250 to 500 milligrams (mg) two times a day, taken every 12 hours.
      • Children—Dose is based on body weight and must be determined by your doctor. The dose is usually 10 to 20 milligrams (mg) per kilogram (kg) of body weight every 12 hours. However, the dose is usually not more than 750 mg per day.
    • For gonorrhea:
      • Adults—250 milligrams (mg) taken as a single dose.
      • Children—Use and dose must be determined by your doctor.
    • For anthrax infection (post-exposure):
      • Adults—500 milligrams (mg) two times a day, taken every 12 hours.
      • Children—Dose is based on body weight and must be determined by your doctor. The dose is usually 15 milligram (mg) per kilogram (kg) of body weight every 12 hours. However, the dose is usually not more than 500 mg per day.

Missed Dose

If you miss a dose of ciprofloxacin, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Do not take more than one extended-release tablet each day.

Storage

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

You may store the oral liquid at room temperature or in the refrigerator. Do not freeze the bottle. Do not keep the mixed oral liquid for more than 14 days. Throw away any unused liquid after 14 days.

Ciprofloxacin administration

infoAdministration of drug is important to know because the drug absorption and action varies depending on the route and time of administration of the drug. A medicine is prescribed before meals or after meals or along with meals. The specific timing of the drug intake about food is to increase its absorption and thus its efficacy. Few work well when taken in empty stomach and few medications need to be taken 1 or 2 hrs after the meal. A drug can be in the form of a tablet, a capsule which is the oral route of administration and the same can be in IV form which is used in specific cases. Other forms of drug administration can be a suppository in anal route or an inhalation route.
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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.

Ciprofloxacin pharmacology

infoPharmacokinetics of a drug can be defined as what body does to the drug after it is taken. The therapeutic result of the medicine depends upon the Pharmacokinetics of the drug. It deals with the time taken for the drug to be absorbed, metabolized, the process and chemical reactions involved in metabolism and about the excretion of the drug. All these factors are essential to deciding on the efficacy of the drug. Based on these pharmacokinetic principles, the ingredients, the Pharmaceutical company decides dose and route of administration. The concentration of the drug at the site of action which is proportional to therapeutic result inside the body depends on various pharmacokinetic reactions that occur in the body.

Absorption

Ciprofloxacin given as an oral tablet is rapidly and well absorbed from the gastrointestinal tract after oral administration. The absolute bioavailability 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.

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 ciprofloxacin 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 IV dose. A 250 mg oral dose given every 12 hours produces an AUC equivalent to that produced by an infusion of 200 mg ciprofloxacin given every 12 hours.

Distribution

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.

Metabolism

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. Coadministration 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 coadministered drug.

Excretion

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.

With oral administration, a 500 mg dose, given as 10 mL of the 5% ciprofloxacin for oral suspension (containing 250 mg ciprofloxacin/5mL) is bioequivalent to the 500 mg tablet. A 10 mL volume of the 5% ciprofloxacin for oral suspension (containing 250 mg ciprofloxacin/5mL) is bioequivalent to a 5 mL volume of the 10% ciprofloxacin for oral suspension (containing 500 mg ciprofloxacin/5mL).

Drug-Drug Interactions

When Ciprofloxacin Hydrochloride 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 ciprofloxacin for oral suspension is given with food. The overall absorption of ciprofloxacin hydrochloride tablet or ciprofloxacin for oral suspension, however, is not substantially affected. The pharmacokinetics of ciprofloxacin given as the suspension are also not affected by food. Concurrent administration of antacids containing magnesium hydroxide or aluminum hydroxide may reduce the bioavailability of ciprofloxacin by as much as 90%.

The serum concentrations of ciprofloxacin and metronidazole were not altered when these two drugs were given concomitantly.

Concomitant administration with tizanidine is contraindicated. Concomitant administration of ciprofloxacin with theophylline decreases the clearance of theophylline resulting in elevated serum theophylline levels and increased risk of a patient developing CNS or other adverse reactions. Ciprofloxacin also decreases caffeine clearance and inhibits the formation of paraxanthine after caffeine administration.

Special Populations

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 (> 65 years) as compared to young adults. Although the Cmax is increased 16-40%, 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.

Patients with Renal Impairment

In patients with reduced renal function, the half-life of ciprofloxacin is slightly prolonged. Dosage adjustments may be required.

Patients with Hepatic Impairment

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, however, have not been fully elucidated.

Pediatrics

Following a single oral dose of 10 mg/kg ciprofloxacin suspension to 16 children ranging in age from 4 months to 7 years, the mean Cmax was 2.4 mcg/mL (range: 1.5 to 3.4 mcg/mL) and the mean AUC was 9.2 mcg*h/mL (range: 5.8 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 TID). In children with severe sepsis who were given intravenous ciprofloxacin (10 mg/kg as a 1-hour infusion), the mean Cmax was 6.1 mcg/mL (range: 4.6 to 8.3 mcg/mL) in 10 children less than 1 year of age; and 7.2 mcg/mL (range: 4.7 to 11.8 mcg/mL) in 10 children between 1 and 5 years of age. The AUC values were 17.4 mcg*h/mL (range: 11.8 to 32.0 mcg*h/mL) and 16.5 mcg*h/mL (range: 11.0 to 23.8 mcg*h/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 to 5 hours, and the bioavailability of the oral suspension is approximately 60%.


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References

  1. 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).
  2. 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).

Reviews

The 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.

User reports

2 consumers reported administration

When 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 With a meal. 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.
Users%
With a meal1
50.0%
After food1
50.0%


Consumer reviews

Elias08 May 2015 09:45
its hard to find. have been to so many chemists all in vain


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