Ciprofloxacin is a broad-spectrum drug against microbes and is a derivative of fluoroquinols. Its action is based on the suppression of bacterial DNA gyrase and disruption of its reproduction, division and growth. The antibiotic causes pronounced morphological changes that affect membranes and cell walls, which contributes to the rapid death of the pathogen.
Gram-negative organisms are exposed to harmful effects during division and dormancy, while gram-positive organisms are destroyed during division. When ciprofloxacin is used in treatment, resistance to antibiotics of other groups that do not work on the principle of gyrase inhibition does not appear. Therefore, the use of this drug is especially effective against pathogens resistant to penicillins, tetracyclines, aminoglycosides, cephalosporins and others. Ciprofloxacin has a detrimental effect on the following groups of bacteria:
- enterobacteria;
- some intracellular pathogens;
- gram-positive aerobic bacteria.
Antibiotic ciprofloxacin
Forms of production
This medicine can be purchased at pharmacy kiosks in three forms:
- pills;
- solution for infusion;
- eye drops.
The solution contains ciprofloxacin hydrochloride as the main component, and is presented on pharmacy counters in bottles containing 100 ml of the active substance inside.
In tablets, the name of the active substance has not changed; it is still ciprofloxacin hydrochloride. Tablets are produced containing 250 and 500 mg of the active ingredient. For packaging for sale, cardboard boxes are used, which include 100, 60, 50, 40, 30, 20, 10 tablets.
Drops for the treatment of ear and eye diseases are used as a local preparation, sold in pharmacies in the form of bottles with a dropper containing 3 or 5 ml of ciprofloxacin hydrochloride.
Behavior of a drug in the human body
When taken orally, the substance is actively and almost completely absorbed from the stomach and intestines, most of all from the duodenum and small intestine. If the drug is drunk during meals, this somewhat slows down the absorption process, but does not change the active effect. Bioavailability for the body is about 55–84%, binds to plasma protein by 20–40%, absorption ends completely after an hour and a half .
Absorption directly depends on the amount of the drug taken:
- 250 mg – 1.2 µg/ml;
- 500 mg – 2.4 µg/ml;
- 750 ml – 4.3 µg/ml;
- 1000 ml – 5.4 µg/ml.
The substance is quickly distributed in tissues, but does not affect fatty layers and nerve endings; the concentration is more than two to ten times the content in plasma. The therapeutic dose accumulates in the tonsils, gall bladder and ducts, intestines, saliva, bile, internal organs of the peritoneum and pelvis, bones, prostate, seminal fluid, uterus, endometrium, ovaries, fallopian tubes, articular cartilage, synovial fluid, skin, peritoneal fluid , ureters and kidneys.
A small concentration is formed in the cerebrospinal fluid, its value reaches 6–10% of the amount in the blood serum. If inflammation of the meninges is present, the concentration increases to 36%. There is excellent emission of ciprofloxacin into the bronchial secretions, peritoneum, lymph, and ocular fluid through the placenta into the fetal body.
In the liver, ciprofloxacin forms metabolites with a total amount of up to 16–30%:
- sulfociprofloxacin;
- formylciprofloxacin;
- diethylciprofloxacin;
- oxociprofloxacin.
Metabolism in the liver is completed after 4 hours when administered orally and requires 5–6.5 hours when given intravenously; if renal failure is present, the metabolism time increases to 12 hours .
Excretion from the human body is carried out through the kidneys unchanged through tubular secretion or by tubular filtration (up to 50% is excreted when taken orally, intravenous use increases excretion to 70%). 10–15% of the substance is removed as metabolites, the remainder goes through the intestines.
After using the intravenous route of entry of the drug into the body, its concentration in the urine in the next two hours is 100 times greater than in the blood serum. This ability to accumulate in the urinary system makes the drug indispensable for the treatment of various genitourinary infections. But in case of renal failure, the concentration decreases, an increase in metabolism occurs and the substance is excreted from the body in the feces.
Treatment of diseases
A large number of diseases can be cured with the use of the antibiotic ciprofloxacin. Instructions for use indicate a list of bacterial diseases:
- respiratory diseases (exacerbations of chronic bronchitis, acute stages of pneumonia, cystic fibrosis, bronchiectasis)
- infectious diseases of the ear, nose and throat (sinusitis, mastoiditis, sinusitis, otitis media, pharyngitis, tonsillitis);
- infections of the urinary and genital organs (endometritis, salpingitis, oophoritis, adnexitis, pyelonephritis, cystitis, prostatitis, tubular abscess, gonorrhea, chlamydia, chancroid, pelvioperitonitis);
- diseases of the peritoneum (infections of the intestines and stomach, peritonitis, inflammation of the gallbladder and ducts, salmonellosis, cholera, yersiniosis, shigellosis, abscesses);
- infected inflammation of soft tissues (burns, ulcers, abscesses, wounds, phlegmon);
- bone infections (septic arthrosis and arthritis, osteomyelitis);
- increased intake of immunosuppressive drugs;
- preventive measures during surgical interventions;
- treatment and prophylactic treatment for anthrax diseases.
The antibiotic ciprofloxacin helps with diseases as a local disinfectant and antiseptic:
- ocular conjunctivitis with acute and chronic course, blepharoconjunctivitis and blepharitis;
- ulcers of bacterial origin in the cornea of the eye;
- keratoconjunctivitis and keratitis;
- eye diseases caused by infectious pathogens;
- as a prophylaxis before surgery in ophthalmology.
Release form and composition
- Eye drops 0.3% (in dropper tubes with a valve of 0.1 ml, in a cardboard pack 1 tube; in dropper tubes with a valve 1 ml, 1.5 ml or 2 ml, in a cardboard pack 1, 5 or 10 tubes; in dropper tubes with a screw neck, 5 or 10 ml, in a cardboard pack 1 tube);
- Eye and ear drops 0.3% (in polyethylene dropper bottles of 5 ml, 1 bottle in a cardboard pack);
- Solution for intravenous administration (100 ml in polyethylene bottles, 1 or 24 bottles in a cardboard pack);
- Solution for infusion (100 ml in dark glass or polyethylene bottles, 1 bottle in a cardboard pack);
- Film-coated tablets (10 pcs. in blister packs/blisters/strips, 1 or 2 packs in a cardboard pack; 10 or 20 pcs. in polymer jars, 1 jar in a cardboard pack).
The active ingredient of the drug is ciprofloxacin hydrochloride, its content:
- 1 ml drops – 3 mg;
- 1 ml of solution – 2 mg;
- 1 tablet – 250 or 500 mg.
Instructions for use and dosage
Antibiotic form in tablets
Ciprofloxacin helps in an amount, the calculation of which depends on the severity and course of the disease, the type of pathogen, the patient’s age, the state of the body at the time of injury, body weight and the functioning of the renal apparatus:
- if the kidneys and urinary tract have a small focus of inflammation, then give a tablet of 250 mg 2 times a day, and in case of extensive inflammatory processes, the dose is increased at the same frequency of administration;
- According to the instructions, gonorrhea is cured by a single dose of ciprofloxacin in the amount of 250–500 mg, depending on the severity;
- diseases of the female genital area, as well as colitis and enteritis with complications and high fever, osteomyelitis, prostatitis require the use of the drug 2 tablets (500 mg) twice a day, diarrhea is treated with a dose half as much;
- if the patient has a history of decreased functionality of the renal apparatus, then the dose of the medication should be halved;
- the time of treatment depends on the complications and severity of the disease, but, according to the instructions, the drug is taken for another two days after the symptoms of the disease do not appear.
Ciprofloxacin in ampoules
For IV treatment, the drug is injected into a vein, the procedure lasts half an hour at a dose of 200 mg. If the dose is doubled, to 400 mg, then the administration time is extended to an hour. Ciprofloxacin, when administered intravenously, can be combined for simultaneous administration with the following substances:
- sodium chloride solution 0.9%;
- glucose solution (dextrose) 10 and 5%;
- Ringer's solution;
- fructose solution;
- combined solution of sodium chloride 0.45 and 5% dextrose concentration.
A single dose for an uncomplicated course helps at 200 mg; for extensive inflammatory foci, this rate increases to 400 mg . Typically, the doctor prescribes intravenous administration twice a day, treatment lasts up to 2 weeks. If the patient’s condition is very serious, the duration of the procedures is increased to 3 weeks.
The acute stage of gonorrhea requires a single dose of 100 mg for treatment. Preoperative prophylaxis consists of intravenous infusion of 200–400 mg over half an hour and an hour, respectively.
Indications for use
For drops in ophthalmology:
- Preoperative and postoperative prevention of infectious complications in ophthalmic surgery;
- Keratitis;
- Blepharitis;
- Acute and subacute conjunctivitis;
- Keratoconjunctivitis;
- Blepharoconjunctivitis;
- Chronic dacryocystitis;
- Bacterial corneal ulcer;
- Meibomite (barley);
- Infectious eye lesions after exposure to foreign bodies or injuries.
For drops in otorhinolaryngology:
- Otitis externa;
- Postoperative infectious complications.
For solution and tablets:
- Respiratory tract infections;
- Kidney and urinary tract infections;
- Ear, nose and throat infections;
- Infections of the digestive system, including the teeth, mouth and jaws;
- Infections of the gallbladder and biliary tract;
- Gynecological (including adnexitis) and postpartum infections;
- Genital infections (including gonorrhea and prostatitis);
- Infections of the musculoskeletal system;
- Peritonitis;
- Infections of mucous membranes, skin and soft tissues;
- Sepsis;
- Infections in patients with reduced immunity (treatment and prevention).
Instructions for limited dosage of medication
Sometimes the patient’s condition is such that for some reason it is impossible to completely eliminate the antibiotic, in which case its dose and duration of administration are reduced to a minimum:
- when there is extensive atherosclerosis of the head vessels, and the blood supply to the brain is disrupted;
- the cardiogram shows an increased risk of increasing the QT interval, existing or developing arrhythmia;
- myocardial infarction, heart failure, bradycardia, electrolyte imbalance, hypomagnesemia, hypokalemia;
- simultaneous use of antidepressants, isoenzyme inhibitors, antipsychotics, macrolides, quinolines;
- mental illnesses and dysfunctions of the central nervous system (psychosis, depression, decreased anticonvulsant threshold, epilepsy);
- tissue damage to areas of the brain, stroke;
- liver and kidney failure;
- age of older people.
When is it indicated and what is a contraindication?
Indications for the use of Ciprofloxacin are numerous complex inflammatory infectious diseases, the causative agent of which is simply impossible to cope with without an antibiotic. Such ailments include lesions:
- Respiratory tract and their lower sections.
- ENT organs.
- Kidney and gastrointestinal tract.
- Bones and joints.
- Mucous membranes.
- Soft tissues.
- Dermis.
- Gallbladder and bile ducts.
The most dangerous diseases can be considered those that affect the genitourinary system and lead to disruption of the functionality of the female genital organs. We must not forget about the effectiveness of therapy with Ciprofloxacin if the patient has a diagnosed sexually transmitted disease.
However, despite the high effectiveness of the drug, you should not decide on your own about the possibility of using it for therapeutic measures. There are a number of contraindications to the use of broad-spectrum antibiotics, including:
- Impaired performance and severe kidney damage (renal failure).
- A pathological process that causes the death of hepatocytes (liver cells) and the development of liver failure.
- Individual intolerance or increased level of sensitivity to the components included in the drug.
- Pregnancy.
- Breastfeeding period.
- Young children's age.
If there is a need to prescribe Ciprofloxacin to a woman who is breastfeeding, then breastfeeding will have to be abandoned.
Despite the fact that a number of diseases and health conditions are not considered a contraindication to the use of Ciprofloxacin for therapeutic purposes, it is prescribed with extreme caution to those patients who suffer from:
- Mental disorders.
- Atherosclerosis of cerebral vessels.
- Poor circulation.
- Epilepsy.
- Increased convulsive readiness.
It can be said that age over 60 years is also considered a contraindication to the use of Ciprofloxacin.
Subtleties of using ciprofloxacin
If complications arise in the form of prolonged diarrhea with an ongoing course, then the patient is examined for the presence of pseudomembranous colitis . If the diagnosis is confirmed, then the drug should be immediately discontinued, without leaving any resulting colitis without appropriate treatment. Ciprofloxacin should also be discontinued if discomfort occurs in the tendons or at the first signs of tenosynovitis.
The time of antibiotic treatment should not coincide with sunbathing; direct sun rays are contraindicated. To ensure normal urine flow and normal diuresis, it is recommended to drink enough fluids. If alcoholic beverages are consumed simultaneously with ciprofloxacin, an increased hepatotoxic effect of the drug may occur.
The occurrence of side effects when taking an antibiotic
Unpleasant sensations and side effects can occur from various body systems:
- the digestive system responds with a decrease in appetite, the occurrence of flatulence, pain in the peritoneum, the appearance of cholestatic jaundice (especially with a diseased liver), hepatonecrosis, hepatitis;
- the nervous system reacts to taking the antibiotic with dizziness and headache, the appearance of terrible dreams, increased fatigue, anxiety, sleep disturbance, increased sweating, hypertension, impaired integrity of consciousness, hallucinogenic visions, depression, fainting, migraines;
- sensory organs are impaired in functioning, resulting in deterioration of vision, smell and taste reactions, incorrect color perception, hearing impairment and side tinnitus;
- on the part of the cardiac system and blood vessels, there is a disturbance in the heart rhythm, hypotension, tachycardia;
- the hematopoietic system responds to antibiotic use with anemia, granulocytopenia, blood clot formation, increased leukocyte levels, hemolytic anemia;
- the urinary system disrupts its functions in the form of crystalluria, dysuria, urinary retention, decreased nitrogen excretion in the kidneys, interstitial nephritis, glomerulonephritis, polyuria;
- Moreover, in laboratory conditions, when examining the patient, hyperbilirubinemia, increased activity of transaminases in the kidneys, hypoprothrombinemia, and hyperglycemia are revealed.
Separately, it should be noted the appearance of allergic responses of the body to treatment with ciprofloxacin. Patients experience skin itching , blisters, rashes in the form of urticaria, nodules, drug fever, swelling of the face and larynx, eosinophilia, difficulty breathing, increased reaction of the pupil to light. Those treated with ciprofloxacin notice nodular or exudative erythema multiforme on the body, necrolysis of the epidermal toxic course (Lyell's syndrome).
In addition to allergic manifestations, in patients taking an antibiotic, tenosynovitis, arthritis, arthralgia may worsen, tendon ruptures may appear, myalgia, asthenia may occur, severe infections of pseudomembranous colitis, candidiasis may develop, and a feeling of a rush of blood to the facial area may appear.
Interaction with other drugs
Due to a decrease in the activity of the microsomal oxidative process in the liver, the antibiotic increases the concentration and prolongs the elimination time of indirect anticoagulants, caffeine, theophylline, hyperglycemic agents, and reduces the prothrombin index.
Treatment simultaneously with metoclopramide promotes the absorption of ciprofloxacin and thereby reduces the time of formation of maximum concentration in the human body. Non-steroidal anti-inflammatory drugs can cause seizures when used together; this does not apply to ascorbic acid. Uricosuric drugs slow down the breakdown and elimination of the antibiotic, which significantly increases the content of ciprofloxacin in the blood plasma.
When used simultaneously with other antimicrobial drugs, synergy occurs, which makes it possible to more successfully cure diseases:
- for the treatment of pathogens Pseudomonas spp. the antibiotic is used in combination with ceftazimide and azlocillin;
- Streptococcal bacteria are actively affected when combined with mezlocillin and other beta-lactam antibiotics;
- staphylococcal pathogens are destroyed by combination with vancomycin and isoxalpenicillin;
- anaerobic bacteria cease to exist with simultaneous treatment with ciprofloxacin and metronidazole or clindamycin.
When combined in treatment with cyclosporine, constant monitoring of serum creatinine in patients is required, since ciprofloxacin increases the nephrotoxic effect of the drug . Indirect coagulants used in conjunction with an antibiotic enhance their effect.
The infusion solution of ciprofloxacin is not pharmaceutically compatible with other similar solutions that are unstable in an acidic environment, therefore the solution of the desired antibiotic cannot be combined with substances having a pH greater than 7 for intravenous administration.
What side effects may there be?
Ciprofloxacin is a fairly safe drug: there is no negative effect on healthy cells. Side effects occur in less than 10% of patients. The most adverse events after using the drug include:
- various digestive disorders;
- sleep problems;
- headache;
- skin allergic reactions.
Use of ciprofloxacin in pediatrics
It is not recommended to use ciprofloxacin in the treatment of children and adolescents under 18 years of age, since bone growth and skeletal formation occur before this time. The antibiotic is not used to treat bacterial infection in women carrying a fetus or during breastfeeding.
Similar drugs for use as antibiotics:
- Berox-plus is available in the form of simple and effervescent tablets;
- Betadine vaginal suppositories, weight 200 mg each, 10% ointment is available, a 10% solution is provided for local external use;
- Ceraxon is available in the form of a solution, used for small patients in the form of syrup, injections are given intramuscularly in doses of 500 and 100, and is also produced in the form of simple tablets;
- heptral is produced in the form of tablets of 400 mg; a solution is used for injections or used for intravenous infusion.