Ciprofloxacin (When ATH J01MA02)
When ATH:
J01MA02
Characteristic.
Fluoroquinolone antibacterial agent II generation. Pale to slightly yellowish crystalline powder, insoluble in 0,1 n. hydrochloric acid, practically insoluble in water and ethanol.
Pharmacological action.
Broad-spectrum antibacterial, bactericide.
Application.
For systemic use: bacterial infection, caused by susceptible microorganisms: infection of upper respiratory tract (otitis media, genyantritis, frontit, sinusitis, mastoiditis, tonsillitis, pharyngitis), lower respiratory tract (bronchitis and acute exacerbation of chronic, pneumonia, bronchiectasis, mukovystsydoz), pelvic (cystitis, pyelonephritis, prostatitis, adnexitis, salpingitis, oophoritis, endometritis, tubular abscess, pelvioperitonit), skin and soft tissue (infected ulcers, wounds, burns, abscess, flegmona), bone and joints (osteomyelitis, septicheskiy arthritis); venereal diseases (gonorrhea, chancroid, Chlamydia), abdominal infections (bacterial infections of the gastrointestinal tract, gallbladder and biliary tract, intraperitoneal abscesses, peritonitis, salmonellosis, typhoid fever, Campylobacteriosis, iersinioz, dysenteries, cholera), bacteraemia, septicemia, severe infections due to immune deficiency and neutropenia, prevention of infections in surgical interventions.
In ophthalmology: infectious and inflammatory eye diseases (acute and subacute conjunctivitis, .Aloe, blefarokonъyunktyvyt, keratit, keratokonъyunktyvyt, bacterial corneal ulcer, chronic dacryocystitis, meybomit, infections of the eye after an injury, or the ingress of foreign bodies), before- and postoperative prevention of infectious complications in ophthalmic surgery.
In otorhinolaryngology: otitis externa, treatment of postoperative infectious complications.
Contraindications.
Hypersensitivity (incl. to other fluoroquinolones), deficiency of glucose-6-fosfatdegidrogenazы, childhood and adolescence (to 18 years, end of the period of intense growth - for systemic use); in ophthalmology: Viral keratitis, childhood (to 1 year - eyedrop, to 2 years - for ophthalmic ointment).
Restrictions apply.
Severe cerebral atherosclerosis, cerebrovascular accident, mental illness, epilepsy, epileptic syndrome, severe renal and / or hepatic insufficiency.
Pregnancy and breast-feeding.
Contraindicated in pregnancy (safety and efficacy in women during pregnancy is not established). Ciprofloxacin passes through the placenta. Displaying, that ciprofloxacin caused arthropathy in young animals. In experiments on rats and mice, receiving ciprofloxacin doses, exceeding the usual daily dose for human 6 time, adverse effects on the fetus revealed no. In experiments on rabbits, received an oral dose of ciprofloxacin 30 and 100 mg / kg, shows, that the drug causes disruption of the digestive tract, leading to weight loss in females and increases the number of abortions; but did not reveal teratogenicity. The on / in a dose up 20 mg / kg ciprofloxacin do not have toxic effects on the mother and the embryo, showed no teratogenicity.
Ciprofloxacin is excreted in breast milk, so the period of lactation should decide, stop taking ciprofloxacin, or breastfeeding, based on the degree of importance of the use of drugs for mother.
The use of local forms of ciprofloxacin during pregnancy is possible, if the expected benefit outweighs the potential risk to the fetus; used with caution during lactation (unknown, whether ciprofloxacin is excreted into breast milk when applied topically).
Side effects.
When administered systemically
From the digestive tract: nausea, vomiting, appetite disorders, diarrhea, constipation, psevdomembranoznыy colitis, epigastric and abdominal pain, abdominal discomfort, Ikotech, ulcers, dryness and soreness of oral mucosa, flatulence, bleeding in the gastrointestinal tract, pancreatitis, cholestatic jaundice, hepatitis, liver cell necrosis.
From the nervous system and sensory organs: headache, dizziness, excitation, a feeling of anxiety, insomnia, nightmares, confusion, depression, Phobias, feeling tired, blurred vision (changes in color vision, diplopia, nistagmo, sore eyes), taste disturbance, olfactory, noise in ears, transient hearing loss, mood changes, gait disturbance, intracranial hypertension, paraesthesia, Sweating, ataxia, tremor, convulsions, toxic psychosis, paranoia, hallucinations, migraine.
Cardio-vascular system and blood (hematopoiesis, hemostasis): decrease in blood pressure, cardiovascular collapse, arrhythmia, cerebral thrombosis, paroxysmal tachycardia, leukopenia, leukocytosis, anemia, thrombocytopenia, thrombocytosis, changes in the level of prothrombin.
From the respiratory system: pulmonary embolism, dyspnoea, respiratory distress, bronchospasm, pleural effusion.
On the part of the musculoskeletal system: arthralgia, myalgia, tendinitis.
With the genitourinary system: frequent urination, kristallurija, hematuria, цilindrurija, polyuria, proteinuria, Acidosis, urinary retention, hemorrhagic cystitis, jade, vaginitis, gynecomastia.
Allergic reactions: rash, petechiae, bubbles, papules, kozhnыy vasculitis, Stevens-Johnson syndrome, Lyell's syndrome, erythema multiforme exudative, exfoliative dermatitis, itching, swelling of the lips, person, Neck, conjunctiva, limbs, angioedema, hives, anaphylactic shock.
Other: giperpigmentatsiya, eozinofilija, fever, photosensitivity, transient increase in liver transaminases, Alkaline phosphatase, creatinine, urea, serum triglycerides, Glucose, Potassium, bilirubin; dysbiosis, candidiasis; on-site / in the introduction - pain, burning sensation, phlebitis.
When applied topically: allergic reactions, itch, burning, mild soreness and redness of the conjunctiva or in the eardrum; rare - swelling of the eyelids, photophobia, lacrimation, foreign body sensation in the eye, an unpleasant taste in the mouth immediately after instillation, reduced visual acuity, the appearance of a white crystalline precipitate in patients with corneal ulcer, keratit, keratopathy, stains or infiltration of the cornea, development of superinfection.
Cooperation.
Activity increased in combination with beta-lactam antibiotics, aminoglikozidami, vancomycin, klindamiцinom, metronidazolom. Sucralfate, bismuth preparations, antacids, containing aluminum ions, magnesium or calcium, cimetidine, ranitidine, vitamins with microelements, iron sulfate, zinc, didanosine (recommended for 2 hours before or after 4 hours after these drugs) reduce the absorption. Probenecid, azlocillin increase the concentration in the blood. Decreases clearance and increases plasma levels of caffeine, aminophylline and theophylline (It increases the likelihood of side effects). It enhances the effect of warfarin and other oral anticoagulants (prolongs bleeding time). Increases cyclosporine nephrotoxicity, the risk of increased excitability of the central nervous system and convulsive reactions to NSAIDs background. Preparations, alkalizing urine (tsytratы, sodium bicarbonate, carbonic anhydrase inhibitors), insolubiliser (It increases the probability of crystalluria). Ciprofloxacin Infusion solutions, ready to use, It may be combined with infusion solutions: 0,9% sodium chloride, Ringer, Ringer's lactate, 5 and 10% dextrose, 10% fructose solution, and sodium, contains 5% Dextrose 0,225 or 0,45% sodium chloride. Incompatible with solutions, having a pH above 7.
Overdose.
Symptoms: No specific symptoms.
Treatment: gastric lavage, the use of emetic drugs, introduction of a large amount of liquid, creating an acid reaction of urine, dopolnityelino-e pyeritonyealinyi dialysis and hemodialysis (It may be derived only 10% product); All events are held on the background of maintaining vital functions. Spetsificheskiy antidote unknown.
Dosing and Administration.
Inside, I /, locally. The mode set individually depending on the location and severity of the infection process, condition of the body, age, body weight, renal function. Inside (not chewing and drinking plenty of fluids) by 250 mg (in severe infections - at 500-750 mg) 23 times per day; prolonged taking shape 1 once a day. With infections of the urinary tract - 500 mg per day 2 admission, in acute gonorrheal urethritis - 0,5 g once. B / drip - for 200 mg (in severe infections - 400 mg) 2 once a day; the duration of infusion 30 min at a dose 200 mg 60 min - at a dose 400 mg.
Patients with severe renal impairment the daily dose reduced by half, elderly patients - to 30%.
In severe infections, and / or inability to taking the pills inside the treatment begins with a / Infusion. The duration of treatment depends on the severity of the disease. The average duration of treatment: 1 day - for acute uncomplicated gonorrhea and cystitis; to 7 days - infections of the kidneys, urinary tract and abdominal organs; throughout the period of neutropenia phase - in patients with weakened protective forces of the organism, but not more 2 month - osteomyelitis and 7-14 days - when all other infections. When streptococcal infections due to the risk of late complications, as well as chlamydial infection, treatment should continue for at least 10 days. In immunocompromised patients the treatment was carried out for the entire period of neutropenia.
Treatment should be for at least 3 days after the normalization of body temperature, or the disappearance of clinical symptoms.
Locally: for mild to moderate infections of eye drops instilled 1-2 drops into the conjunctival sac of the affected eye every 4 no, in severe infections - for 2 drop each hour. After improving the dose and frequency of instillation reduce.
Eye ointment for a lower eyelid of the affected eye.
Ear drops: instill 5 drops in the affected ear 3 once a day. After the disappearance of symptoms should be continued during the next 48 no.
Precautions.
Due to the threat of adverse reactions of the nervous system ciprofloxacin should be used only for health reasons in the pathology of the central nervous system in history: organic brain lesions, epilepsy, lowering the seizure threshold, severe atherosclerosis of brain vessels (the risk of circulatory disorders, stroke), in old age, with severe renal impairment and liver (requires monitoring of plasma concentrations).
In patients with allergic reactions to fluoroquinolone derivatives history may develop reactions to ciprofloxacin. During treatment should avoid sunlight and UV radiation, intense exercise, control the drinking regime, urine pH.
Cases of crystalluria, especially in patients with alkaline urine (pH 7 or higher). In order to avoid the development of crystalluria is unacceptable excess of the recommended daily dose, you also need adequate fluid intake and maintain an acid reaction of urine.
If you have pain in the tendons, or the first signs of tenosynovitis treatment should be discontinued (described isolated cases of inflammation, or tendon rupture during treatment with fluoroquinolones).
May reduce the rate of psychomotor reactions, especially against the background of alcohol, which should be considered for patients, working with potentially dangerous machinery or drive a vehicle. If you develop severe diarrhea, pseudomembranous colitis should be excluded (wherein ciprofloxacin is contraindicated). Simultaneous in / introduction of barbiturates demands the control of the cardiovascular system (Heart Rate, FROM, ECG). Adolescents 18 years shall be appointed only if the resistance of the pathogen to other chemotherapy drugs.
The solution in the form of eye drops not intended for intraocular injection. When using other ophthalmic agents interval between doses should be at least 5 m.
Cooperation
Active substance | Description of interaction |
Algeldrat + Magnesium hydroxide | FKV. Slows absorption (the interval between doses should be at least 2 no). |
Vancomycin | FMR: synergism. Increases (mutually) antibacterial activity. |
Warfarin | FMR: synergism. Against the background of enhanced effect of ciprofloxacin. |
Didanosine | FKV. Reduces the absorption of; with a joint appointment interval between doses should be at least 4 no. |
Ferrous gluconate | FKV. Significantly reduces the absorption of; the combined appointment interval between doses should be at least 6 no. |
Iron sulfate | FKV. Significantly reduces the absorption of; the combined appointment interval between doses should be at least 6 no. |
Iron fumarate | FKV. Significantly reduces the absorption of; the combined appointment interval between doses should be at least 6 no. |
Calcium carbonate | FKV. Significantly reduces the absorption of; the combined appointment interval between doses should be at least 6 no. |
Calcium chloride | FKV. Significantly reduces the absorption of; the combined appointment interval between doses should be at least 6 no. |
Klindamiцin | FMR: synergism. Increases (mutually) antibacterial effect. |
Caffeine | FKV. Against the background of ciprofloxacin reduced clearance, increased plasma levels and T1/2, It increases the likelihood of side effects. |
Magnesium oxide | FKV. Significantly reduces the absorption of; the combined appointment interval between doses should be at least 6 no. |
Metronidazol | FMR: synergism. Increases (mutually) antibacterial activity. |
Ranitidine | FKV. Reduces the absorption of; the combined appointment interval between doses should be at least 4 no. |
Rifampicin | FKV. It induces microsomal enzymes, accelerates biotransformation, reduces tissue concentrations. |
Sucralfate | FKV. Reduces the absorption of; combined use requires interval between reception of at least 4 no. |
Theophylline | FKV. FMR. Against the background of ciprofloxacin (inhibits CYP1A2) zamedlyaetsya biotransformation, Lowering, increased plasma levels and increases the likelihood of side effects. |
Phenytoin | FKV. Against the background of ciprofloxacin plasma levels may change; Simultaneous use requires caution. |
Cyclosporine | FMR. Strengthens (mutually) the risk of kidney damage. |
Zinc Sulphate | FKV. Significantly reduces the absorption of. |
Ethambutol | FMR. Strengthens (mutually) the risk of neurotoxicity. |