Ciprofloxacin (Pills, coated)

Active material: Ciprofloxacin
When ATH: J01MA02
CCF: Fluoroquinolone antibacterial drug
ICD-10 codes (testimony): A40, A41, H66, H70, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J42, K05, K12, K65.0, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, M00, M86, N11, N30, N34, N41, N70, N71, N72, N73.0, Z29.2
When CSF: 06.17.02.01
Manufacturer: Synthesis of (Russia)

Pharmaceutical form, composition and packaging

Pills, coated, round, lenticular, white or white with serovatam brown color.

Excipients: corn starch, krospovydon M, lactose, microcrystalline cellulose, magnesium stearate, talc.

The composition of the shell: polyethylene glycol 4000, Titanium dioxide, propylene glycol, talc, kollidon VA-64, hydroxypropylmethylcellulose.

10 PC. – packings Valium planimetric (1) – packs cardboard.

Pills, coated white or nearly white, Oval, lenticular; seen in cross-section one layer of white.

Excipients: corn starch or starch 1500, kollidon CL-M (krospovydon), lactose, microcrystalline cellulose, magnesium stearate.

The composition of the shell: hydroxypropylmethylcellulose, polyethylene glycol 4000, propylene glycol, talc, kollidon VA-64 (copolyvidonum), Titanium dioxide.

5 PC. – packings Valium planimetric (1) – packs cardboard.
5 PC. – packings Valium planimetric (2) – packs cardboard.
5 PC. – packings Valium planimetric (4) – packs cardboard.
5 PC. – plastic jars (1) – packs cardboard.
10 PC. – plastic jars (1) – packs cardboard.
20 PC. – plastic jars (1) – packs cardboard.

Pills, coated white or nearly white, Oval, lenticular; seen in cross-section one layer of white.

Excipients: corn starch or starch 1500, kollidon CL-M (krospovydon), lactose, microcrystalline cellulose, magnesium stearate, talc.

The composition of the shell: hydroxypropylmethylcellulose, polyethylene glycol 4000, propylene glycol, talc, kollidon VA-64 (copolyvidonum), Titanium dioxide.

5 PC. – packings Valium planimetric (1) – packs cardboard.
5 PC. – packings Valium planimetric (2) – packs cardboard.
5 PC. – packings Valium planimetric (4) – packs cardboard.
5 PC. – plastic jars (1) – packs cardboard.
10 PC. – plastic jars (1) – packs cardboard.
20 PC. – plastic jars (1) – packs cardboard.

Pharmacological action

Antimicrobial, fluoroquinolone derivative. Effective bactericidal. Inhibit bacterial DNA gyrase (topoisomerase II and IV, responsible for the process of supercoiling of chromosomal DNA around the nuclear RNA, that it is necessary to read the genetic information), narushaet synthetic DNA, the growth and division of bacteria, It is expressed morphological changes (incl. cell wall and membranes) and rapid death of the bacterial cell.

Bactericidal effect on gram-negative microorganisms in a rest period and dividing (tk. not only affects DNA gyrase, but also causes lysis of the cell wall), Gram-positive microorganisms - only during division.

Low toxicity to cells macroorganism's due to the lack of DNA gyrase. While receiving ciprofloxacin occurs parallel generating resistance to other antibiotics, do not belong to the Group of gyrase inhibitors, that makes the drug highly effective against bacteria, are resistant, eg, k aminoglycosides, penicillins, cephalosporins, tetracyclines and many other antibiotics.

Ciprofloxacin active against gram-negative aerobic bacteria: Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Proteus is wonderful, Proteus vulgaris, Serratia wilting, Hafnia avenue, edwardsiella tarda, Providencia spp., Morganella morganii, Vibrio spp., Yersinia spp., Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella multocida, Plesiomonas shigelloides, Campylobacter jejuni, Neisseria spp.; Gram-positive aerobic bacteria: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus man, Staphylococcus saprophyticus), Streptococcus pyogenes, Streptococcus agalactiae.

Preparation It is also active against some intracellular pathogens (Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Corynebacterium diphtheriae).

C drug moderately sensitive Streptococcus pneumoniae, Enterococcus faecalis, Mycoplasma hominis, Gardnerella spp., Mycobacterium avium-intracellular (for their high concentrations are required suppression).

C drug resistant Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroids.

Preparation activity against Trеponema pallidum.

Most Staphylococcus, resistant to metitillino, and resistant to ciprofloxacin. Resistant pathogens develop very slowly, because on the one hand, after the action of ciprofloxacin are left with persistent microorganisms, and on the other - there is no enzymes in bacterial cells, inactivating it.

Pharmacokinetics

Absorption

After oral administration ciprofloxacin is quickly absorbed from the gastrointestinal tract. The bioavailability of the drug is 50-85%. C_max in the blood plasma of healthy volunteers after oral administration (before meals) 250 mg, 500 mg, 750 mg 1000 mg, achieved through 1-1.5 h and is 0.76 ug / ml, 1.6 ug / ml, 2.5 ug / ml 3.4 ug / ml, respectively.

Distribution

After oral administration ciprofloxacin is distributed in tissues and body fluids. High drug concentrations are observed in the bile, light, kidney, liver, gallbladder, uterus, seminal fluid, Prostate tissue, tonsils, the endometrium, the fallopian tubes and ovaries. The concentration of the drug in those tissues above, than serum. Ciprofloxacin also penetrates into bone, eye fluid, bronchial secretion, spittle, skin, muscle, Plevra, bryushynu, lymph.

Accumulating ciprofloxacin concentration in blood neutrophils 2-7 times higher, than serum.

V_d the body is 2-3.4 l / kg. In preparation cerebrospinal fluid penetrates in a small amount, where its concentration is 6-10% from that in serum.

The degree of binding to plasma proteins ciprofloxacin is 30%.

Metabolism

It is metabolized in the liver (15-30%) with the formation of low metabolites (dijetilciprofloksacin, sul'fociprofloksacin, oksociprofloksacin, formilciprofloksacin).

Deduction

In patients with intact renal function T_1/2 It is usually 3-5 no.

The main route of excretion of ciprofloxacin from the body - kidneys. With urine output 50-70%, with feces – 15-30%.

Pharmacokinetics in special clinical situations

If any of the kidneys (T)_1/2 increases.

Testimony

-infektsii airways;

-infektsii otolaryngology;

-infektsii kidney and urinary tract;

-infektsii genitals;

-infektsii digestive system (incl. oral, teeth);

-infektsii gallbladder and biliary tract;

skin -infektsii, mucous membranes and soft tissues;

-infektsii musculoskeletal system;

-sepsis and peritonitis;

-profilaktika and treatment of infections in patients with reduced immunity (with immunosuppressive therapy).

Dosage regimen

ciprofloxacin dose for oral administration depend on disease severity, type of infection, condition of the body, age, Body weight and renal function in a patient.

At uncomplicated kidney and urinary tract - By 250 mg 2 times / day; in complicated cases – by 500 mg 2 times / day.

At diseases of the lower respiratory tract of moderate severity appoint 250 mg, and more severe cases - By 500 mg 2 times / day.

For the treatment of gonorrhea It recommends a single dose of ciprofloxacin at a dose 250-500 mg.

At gynecological diseases, enteritis, with severe colitis and high temperature, prostatitis, osteomielite - By 500 mg 2 times / day.

For the treatment of diarrhea appoint 250 mg 2 times / day.

The drug should be taken on an empty stomach, drinking plenty of fluids.

Patients with severe renal impairment should be given half the dose of the drug.

The duration of treatment depends on the severity of the disease, but treatment should always continue for at least another 2 the day after the disappearance of symptoms. Typically, the duration of treatment is 7-10 days.

The dosage regimen for patients with chronic renal failure It depends on creatinine clearance:

Side effect

From the digestive system: nausea, diarrhea, vomiting, abdominal pain, flatulence, anorexia, cholestatic jaundice (especially in patients with pre-existing liver disease), hepatitis, gepatonekroz.

From the central and peripheral nervous system: dizziness, headache, fatigue, anxiety, tremor, insomnia, nightmares, peripheral paralgezija (anomaly of the perception of pain), Sweating, intracranial hypertension, confusion, depression, hallucinations, as well as other manifestations of psychotic reactions (rarely progressing to the state, in which the patient may cause harm), migraine, fainting, thrombosis of cerebral arteries.

From the senses: disorders of taste and smell, blurred vision (diplopia, change of color), noise in ears, hearing loss.

Cardio-vascular system: tachycardia, abnormal heart rhythm, decrease in blood pressure, flushing.

From the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, gemoliticheskaya anemia.

From the laboratory parameters: gipoprotrombinemii, increase in liver transaminases and alkaline phosphatase, giperkreatininemiя, giperʙiliruʙinemija, giperglikemiâ.

From the urinary system: hematuria, kristallurija (particularly in alkaline urine and low diureze), glomerulonephritis, dizurija, polyuria, urinary retention, albuminuria, Urethral bleeding, hematuria, azotvydelitel'noj reduced kidney function, interstitial nephritis.

Allergic reactions: itching, hives, bullation, accompanied by bleeding, the appearance of small papules, forming scabs, drug fever, petechial hemorrhages in the skin (petechiae), swelling of the face or larynx, exudative erythema multiforme, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome).

Adverse Reactions, chemotherapy-related action: candidiasis.

If you experience pain in the joints or at the first signs of treatment should be discontinued because, that describes selected cases of inflammation and even rupture the tendons during treatment with fluoroquinolones.

Contraindications

-pregnancy;

-lactation (breast-feeding);

-Children and teens under 18 years;

-Increased susceptibility to ciprofloxacin and other drugs of fluoroquinolones group.

Pregnancy and lactation

Ciprofloxacin-ICCO is contraindicated during pregnancy and lactation (breast-feeding).

Cautions

Patients with epilepsy, convulsive seizures in history, vascular disorders and organic brain lesions, due to the threat of adverse reactions from the CNS ciprofloxacin should be used only for health reasons.

If you encounter during or after the treatment of severe and prolonged diarrhea should exclude the diagnosis of pseudomembranous colitis, that requires the immediate withdrawal of the drug and the appropriate treatment.

During treatment with ciprofloxacin is necessary to provide sufficient liquid under normal diuresis.

During treatment with ciprofloxacin should avoid contact with direct sunlight.

Effects on ability to drive vehicles and management mechanisms

Patients, receiving the drug Ciprofloxacin-Akos, Use caution when driving and other potentially hazardous activities, require increased attention and psychomotor speed reactions (especially while drinking habits).

Overdose

Data on drug overdose missing.

Treatment: spetsificheskiy antidote unknown. It is necessary to carefully monitor the patient's condition, gastric lavage, make routine emergency measures, provide sufficient flow of fluid. With hemo- or peritoneal dialysis can only be inferred slight (less 10%) the amount of drug.

Drug Interactions

Together with the use of ciprofloxacin with DDI absorption of ciprofloxacin is reduced due to the formation of complexes of ciprofloxacin with didanozine aluminium and magnesium salts.

Simultaneous administration of ciprofloxacin and theophylline may lead to increased concentrations of theophylline in the blood plasma due to competitive inhibition of the binding sites in cytochrome P₄₅₀ , which leads to an increase in T_1/2 theophylline and an increased risk of toxic action, associated with theophylline.

Admission antatsidov, as well as preparations, containing ions aluminium, Zinc, iron or magnesium, can cause reduced intake of ciprofloxacin, therefore the interval between administration of these drugs must be at least 4 no.

With simultaneous use of ciprofloxacin and bleeding time is prolonged anticoagulation.

Together with the use of ciprofloxacin and Cyclosporine amplified nefrotoksicescoe effects last.

As a result of reduced activity processes mikrosomalnogo oxidation in gepatocitah, concentration increases and lengthens T_1/2 teofillina (and other xantinov, eg, caffeine), oral hypoglycemic drugs, anticoagulants, helps reduce prothrombin index.

NSAIDs (except acetylsalicylic acid) increase the risk of seizures.

Metoclopramide accelerates the absorption of ciprofloxacin, which reduces the time to reach its maximum concentration.

Joint appointment urikozuricheskih drugs leads to slower excretion (to 50%) and increased plasma concentration of ciprofloxacin.

When combined with other antimicrobial drugs (beta-lactam antibiotics, aminoglikozidy, klindamiцin, metronidazol) usually observed synergy. It can be used in combination with ceftazidime and azlocillin in infections, caused by Pseudomonas spp.; with mezlocillinom, azlocillinom and other beta-lactam antibiotics – when streptococcal infections; a group of antibiotics oxacillin and vancomycin - with staphylococcal infections; metronidazole and clindamycin - In anaerobic infections.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

List B. The drug should be stored in the dark, inaccessible to children at temperature to 25 ° C. Shelf life - 3 year.