Active Ingredient: Ciprofloxacin
Form of issue
Eye and ear drops 0,3%.
Concentrate for infusion therapy 2 mg / ml.
Pills coated with a film coat 250 mg, 500 mg, 1000mg and 750 mg.
Ointment ophthalmic 0,3%.
Ear and eye drops of Ciprofloxin contain Ciprofloxin hydrochloride at a concentration of 3 mg / ml (in terms of a pure substance), Trilon B, benzalkonium chloride, sodium chloride, purified water.
In the ophthalmic ointment, the active substance is also contained in a concentration of 3 mg / ml.
Pills Ciprofloxin: 250, 500, and 750 mg 1000mg mg Ciprofloxin, MCC, potato starch, corn starch, hypromellose, croscarmellose sodium, talc, magnesium stearate, colloidal anhydrous silica, macrogol 6000, additive E171 (titanium dioxide), polysorbate 80.
The infusion solution contains the active substance at a concentration of 2 mg / ml. Excipients: sodium chloride, edetate disodium, lactic acid, dilute hydrochloric acid, water d / u.
↘ Pharmacodynamics and pharmacokinetics ↙
Ciprofloxin is an anti-biotics or not?
Antibiotic Ciprofloxin is an early fluoroquinolone (1st generation drug) and is used primarily for hospital infections. The agent penetrates well into cells and tissues (including cells of bacteria and macroorganisms) and has good pharmacokinetic parameters.
The mechanism of action of the drug is due to the ability to inhibit DNA-gyrase (enzyme of bacterial cells) with a violation of DNA synthesis, division and growth of microorganisms.
Wikipedia indicates that against the background of the use of the drug, resistance to other non-group inhibitors of gyrase, antibiotics is not developed. This makes Ciprofloxin highly effective against bacteria resistant to the action of penicillins, kaminoglikozidov, tetracyclines, cephalosporins and a number of other antibiotics.
The most active activity is with Gram (-) and Gram (+) aerobes:
H. influenzae, N. gonorrhoeae, Salmonella spp., P. aeruginosa, N. meningitidis, E. coli, Shigella spp.
Effective in infections caused by: strains of staphylococci (including those producing penicillinase), individual strains of enterococci, legionella, campylobacteria, chlamydia, mycoplasmas, mycobacteria.
It is active against the producing beta-lactamase microflora.
Anaerobes are moderately sensitive or resistant to the drug. Therefore, in patients with mixed anaerobic and aerobic infections, Ciprofloxin treatment should be supplemented with the administration of lincosamides or metronidazole.
Resistant to the antibiotic are: Ureaplasma urealyticum, Streptococcus faecium, Treponema pallidum, Nocardia asteroides.
After taking the pill, the drug is quickly and completely absorbed in the digestive tract.
Main pharmacokinetic parameters:
▶ bioavailability – 70%;
▶ TSmax in blood plasma – 1-2 hours after administration;
▶ T½ – 4 hours.
Plasma proteins bind from 20 to 40% of the substance. Ciprofloxin is well distributed in body fluids and tissues, and its concentration in tissues and liquids can significantly exceed the plasma one.
Through the placenta penetrates the cerebrospinal fluid, excreted into breast milk, high concentrations are fixed in the bile. Up to 40% of the dose taken is eliminated within 24 hours in unchanged form by the kidneys, part of the dose is excreted with bile.
➡Indications for use Ciprofloxin
Ciprofloxin – from what these pills / solution?
Ciprofloxin is prescribed for the treatment of infectious diseases of the ENT organs, pelvic organs, bones, skin, joints, abdominal cavity, respiratory tract, urogenital and postoperative infections caused by a flora sensitive to the drug.
The drug can be used in patients with immunodeficiency states (including in conditions that develop with neutropenia, or due to the use of immunosuppressors).
Ciprofloxin (like other early fluoroquinolones) is the preferred drug in the treatment of UTI, including, among others, hospital infections.
Due to the ability to penetrate well into tissues and, in particular, into prostate tissue, fluoroquinolones have practically no alternative in the treatment of bacterial prostatitis.
Being highly active against the most likely pathogens of hospital pneumonia (Staphylococcus aureus, enterobacteria and Pseudomonas aeruginosa), it is important for pneumonia associated with the need for artificial ventilation.
If the causative agent of the disease is P. aeruginosa, before prescribing the drug, its sensitivity to Ciprofloxin should be established. This is due to the fact that in intensive care units more than a third of the Pseudomonas aeruginosa strains are resistant to the drug.
Importance of the drug has with intra-abdominal surgical infections and infections of the hepatobiliary system. To prevent infection, he can be assigned to a patient with pancreatic necrosis.
Fluoroquinolones are not used for CNS infections. This is due to their low penetration (penetration) into the cerebrospinal fluid. In this case, they are effective in meningitis, the causative agents of which are resistant to cephalosplorins of the third generation of Gram (-) bacteria.
The presence of several dosage forms allows the use of the drug for the stepwise therapy. When switching from Ciprofloxin IV administration to oral intake in order to maintain therapeutic concentration, the dose for oral administration should be increased.
So, if the patient was prescribed the administration of 100 mg intravenously, then he should take 250 mg inside, and if 200 mg was administered to the vein, then 500 mg.
What is the medicine in the form of eye / ear drops?
In ophthalmology it is used for superficial bacterial infections of the eye (eye) and its appendages, as well as for ulcerative keratitis.
Indications for use Ciprofloxin in otology: acute bacterial otitis of the external ear and acute bacterial otitis of the middle ear in patients with a tympanostomy tube.
Contraindications in systemic application:
➲ severe renal / hepatic dysfunction;
➲ indications of a history of chronic tendonitis caused by the use of quinolones.
Drops for eyes and ears are contraindicated in fungal and viral infections of the eyes / ears, with intolerance to Ciprofloxin (or other quinolones), during pregnancy and lactation.
For children, pills and a solution for intravenous administration can be prescribed from the age of 12, eye and ear drops from 15 years.
▶ Side effects
The drug is good tolerability.
The most common side effects with intravenous administration and ingestion:
In Vidal’s handbook it is reported that in single cases the patients were recorded:
➲ violation of gait;
➲ peripheral sensory disorders;
➲ intracranial hypertension;
➲ feeling of fear;
➲ visual impairment;
➲ stomach ache;
➲ nausea, vomiting;
➲ necrosis of hepatocytes;
➲ arterial hypertension (rarely);
➲ the appearance of rashes on the skin.
Exceptionally rare side effects: bronchospasm, anaphylactic shock, Quincke’s edema, arthralgia, petechiae, malignant erythema exudative, vasculitis, Lyell’s syndrome, leuko- and thrombocytopenia, eosinophilia, anemia, hemolytic anemia, thrombotic or leukocytosis, increased plasma LDH concentration, bilirubin, LF, transaminase of the liver, creatinine.
Application in ophthalmology is accompanied by:
⓵. often – a sense of discomfort and / or foreign body presence in the eye, the appearance of white plaque (usually in patients with ulcerative keratitis and with frequent use of drops), the formation of crystallites / scales, supergiosis and conjunctival hyperemia, tingling and burning;
⓶. in isolated cases – keratitis / keratopathy, eyelid edema, corneal staining, hypersensitivity reactions, lacrimation, decreased visual acuity, photophobia, corneal infiltration.
Side effects that are associated with or possibly related to the use of the drug are usually mild, do not pose a threat and go untreated.
In patients with ulcerative keratitis, the emerging white coating does not adversely affect the treatment of the disease and the parameters of vision and disappears on its own. As a rule, it appears in the period from 1-7 days after the beginning of the course of application of the drug and disappears immediately or within 13 days after its termination.
Neofthalmological disorders when using drops: the appearance of an unpleasant aftertaste in the mouth, in rare cases – nausea, dermatitis.
When used in otology, the following are possible:
- often – a run-off in the ear;
- in some cases – ringing in the ears, headache, dermatitis.
Pills Ciprofloxin: instructions for use
The daily dose for an adult varies from 500 mg to 1.5 g / day. It should be divided into 2 receptions with an interval of 12 hours.
To prevent the crystallization of salts in the urine, the antibiotic should be taken with a large volume of liquid.
A single dose is selected depending on the diagnosis:
☞ urogenital infections – from 2 * 250 to 2 * 500 mg with uncomplicated acute, from 2 * 500 to 2 * 750 mg with complicated;
☞ cystitis in women before menopause – 500 mg (once);
☞ infection of the respiratory tract (depending on the pathogen and severity of the disease) – from 2 * 500 to 2 * 750 mg;
☞ gonorrhea – 500 mg once for acute uncomplicated and from 2 * 500 to 2 * 750 mg mg, if the patient is diagnosed with an extragenital form of the disease, and also in cases when the disease occurs with complications;
☞ joint and bone lesions, severe, life-threatening patients, infections, septicemia, peritonitis (in particular, in the presence of Pseudomonas, Streptococcus or Staphylococcus) – 2 * 750 mg;
☞ gastrointestinal infections – from 2 * 250 to 2 * 500 mg;
Inhalation form of anthrax – 2 * 500 mg;
prevention of invasive infections caused by N. meningitidis – 1 * 500 mg.
The treatment continues until clinical symptoms stop, and a few more days after their disappearance and the normalization of body temperature. In most cases, the course lasts from 5 to 15 days, with lesions of joints and bone tissue it is prolonged to 4-6 weeks, with osteomyelitis – up to 2 months.
Patients with renal dysfunction require a dose adjustment and / or duration of the interval.
Application of ampoules
Ciprofloxin in ampoules is recommended to be administered intravenously in the form of a drop infusion. The dose for an adult is 200-800 mg / day. The duration of the course is on average from 1 week to 10 days.
With urogenital infections, joints and bones or ENT disorders, a patient is administered 200-400 mg twice a day during the day. With infections of the respiratory tract, intra-abdominal infections, septicemia, soft tissue and skin lesions, a single dose at the same multiplicity of applications is 400 mg.
With kidney dysfunction, the starting dose is 200 mg, and subsequently it is adjusted for Clcr.
In the case of the use of ampoules in a dose of 200 mg, the duration of the infusion is 30 minutes, with the administration of the drug at a dose of 400 mg – 1 hour.
Ciprofloxin injections are not prescribed.
Ear and Eye Drops Ciprofloxin: Instructions for Use
With ulcerative keratitis, the treatment is carried out according to the following scheme:
✹ ➊ day – during the first 6 hours of the conjunctival cavity is administered 2 drops of the solution every 15 minutes, then the interval between instillation increased to half (a single dose of the same – 2 drops);
✹ ➋ days – 2 drops with an interval between instillations of 60 minutes;
3-14 days – 2 drops with an interval between instillations of 4 hours.
Treatment for ulcerative keratitis can last longer than 14 days. The treatment plan is selected individually by the attending physician.
With superficial bacterial infections of the eye and its appendages, the standard dose is 1-2 drops with a multiplicity of applications of 4 r. / Day. In especially severe cases, in the first 48 hours the patient is instilled with 1-2 drops every 2 hours.
Treatment lasts from 7 to 14 days.
After instillation, a nasolacrimal occlusion is recommended to reduce systemic absorption of the drug administered into the eye.
In the case of concomitant treatment with other drugs for ophthalmic topical use should withstand 15-minute time intervals between their administration and administration of Ciprofloxin.
In otology, the standard dose of the drug is 4 drops in the previously cleared auditory canal of the affected ear 2 r. / Day.
Patients who use ear pads, the dose is increased only with the first use of the drug: children are administered 6, adults – 8 drops.
The course should not last more than 10 days. If it is necessary to extend it, determine the sensitivity of the local flora.
In case of using other agents for topical application between their administration and administration of Ciprofloxin, it is necessary to maintain an interval of 10-15 minutes.
Dosage for children from 15 years: 3 drops twice a day.
The effect of renal / hepatic dysfunction on the pharmacokinetic parameters of the drug in the form of ear and eye drops has not been studied.
To avoid vestibular stimulation, the solution is warmed to body temperature before insertion into the auditory canal.
The patient should lie on the opposite side of the affected ear. In this position, it is recommended to stay for 5-10 minutes after instillation of the solution.
It is also permissible after local cleaning to insert for 1-2 days in the ear canal a tampon moistened with a solution of hygroscopic cotton wool or gauze. To saturate the drug, it should be moistened twice a day.
To avoid contamination of the tip of the dropper bottle and the solution, do not touch the dropper to the eyelids, the pinna, the external auditory canal, outdoor areas and any other surfaces.
Fundamental difference in how to take drugs from different manufacturers, no: instructions for use Ciprofloxin-Akos similar to the instructions on the Ciprofloxin-FPO, Ciprofloxin, Promed, Vero Ciprofloxin or Ciprofloxin-Teva.
For children and adolescents under the age of 18, the drug should be prescribed only if the pathogen is resistant to other chemotherapeutic agents.
Specific symptoms with an overdose of Ciprofloxin not. The patient is shown gastric lavage, taking emetic drugs, creating an acidic urine reaction, introducing a large volume of fluid. All activities should be conducted against the backdrop of maintaining the function of vital systems and organs.
Peritoneal dialysis and hemodialysis contribute to the elimination of 10% of the dose.
There is no specific antidote for the drug.
The use in combination with Teofillinum promotes an increase in plasma concentration and an increase in T1 / 2 of the latter.
Al / Mg-containing antacids help to slow the absorption of Ciprofloxin and thereby reduce its concentration in urine and blood. Between the methods of these drugs should be maintained intervals of at least 4 hours.
Probenecid delayed excretion of the drug.
Ciprofloxin increases the effect of coumarin anticoagulants.
The interaction of Ciprofloxin for use in otology and ophthalmology with other drugs has not been studied.
▶ Storage conditions
Store the drug at room temperature, in a place inaccessible to children.
▶ Shelf life
For solution, ear and eye drops – 2 g (the contents of the opened vial should be used for 28 days), for pills – 3 g.
▶ Special instructions
Because of the possibility of occurrence of side effects from the side of the central nervous system in patients with a history of its pathology, the drug can be used exclusively for life indications.
Ciprofloxin is cautiously prescribed when lowering the threshold of convulsive readiness, epilepsy, brain damage, severe cerebrosclerosis (increased risk of blood flow and stroke), serious violations of the liver / kidney function, in old age.
During treatment it is recommended to avoid UV and solar irradiation and increased physical activity, to control urine acidity and drinking regimen.
In patients with an alkaline urine reaction, cases of crystalluria were recorded. To avoid its development, it is inadmissible to exceed the therapeutic dose of the drug. In addition, the patient requires a lot of drinking and maintaining an acid reaction of urine.
Pain in the tendons and the appearance of signs of tendovaginitis are a signal to stop treatment, as the possibility of inflammation / rupture of the tendon is not ruled out.
Ciprofloxin can inhibit the rate of psychomotor reactions (especially against the background of alcohol), which should be remembered for patients working with potentially dangerous devices.
With the development of severe diarrhea, pseudomembranous colitis should be ruled out. this disease is a contraindication to the use of the drug.
If necessary, simultaneous in / in the introduction of barbiturates should monitor the function of SSS: in particular, the parameters of ECG, heart rate, blood pressure.
The liquid ophthalmic form of the drug is not intended for intraocular injections.