ULTRAFLEX V. I.

Instructions for medical use

medicine

ULTRAFLOX V.I.

Registration number : B-250-95 60205/11

Trade name of the drug : Ultraflox V.I.

International nonproprietary name : ciprofloxacin.

Dosage form : solution for infusion.

Composition : 100 ml solution for infusion contains 200 mg ciprofloxacin.

Description : transparent colorless solution.

Pharmacotherapeutic group: antimicrobial agents – fluoroquinolones.

Code ATH: J01MA02

Pharmacological properties

Pharmacodynamics

A broad-spectrum antimicrobial drug from the group of fluoroquinolones. Acts bactericidal. The drug inhibits bacterial DNA gyrase, as a result of which DNA replication and the synthesis of bacterial cellular proteins are disrupted. Ciprofloxacin acts on both reproducing and dormant microorganisms.

Gram-negative aerobic bacteria are sensitive to ciprofloxacin: Escherichia coli, Salmonella spp., Shigella spp., Citobacter spp., Klebsiella spp., Enterobacter spp., Proteus mirabilis, Proteus vulgaris, Serratia marcescens, Hafniaalvei, Edwardsiellatarda, Providencia spp., Morganella morganii, Vibrio spp., Yersinia spp., other gram-negative bacteria: Haemophilus spp., Pseudomonas aeruginosa, Moraxella catarrhalis, Aeromonas spp., Pasteurella miltocida, Plesimonas shigelloides, Campylobacter jejuni, Neisseria spp.; some intracellular pathogens: Legionella pneunophila, Brucella spp., Chlamydia tracomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium-intraacellulare.

Gram-positive aerobic bacteria are also sensitive to ciprofloxacin: Staphylococcus spp. (Staphylococcus aureus, Staphylococcus haemolyticus, Staphylococcus hominis, Staphylococcus saprophyticus), Streptococcus spp. (Streptococcus pyogenes, Streptococcus agalactiae).

Most staphylococci resistant to methicillin are also resistant to ciprofloxacin.

The sensitivity of bacteria Streptococcus pneumoniae and Enterococcus faecalis is moderate.

Both in vitro and according to studies of drug concentrations in blood plasma (as a surrogate marker), Bacillus anthracis is also sensitive to ciprofloxacin. The following are resistant to the drug: Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroids. The effect of the drug against Treponema pallidum has not been sufficiently studied.

Pharmacokinetics

After intravenous administration of the drug, ciprofloxacin is distributed in the tissues and fluids of the body. High concentrations of the drug are found in the liver, bile, gall bladder, lungs, kidneys, uterus, seminal fluid, prostate tissue, tonsils, endometrium, fallopian tubes and ovaries. The concentration of the drug in these tissues is higher than in the blood serum. Ciprofloxacin also penetrates well into bones, ocular fluid, bronchial secretions, saliva, skin, muscles, pleura, peritoneum and lymph. The concentration of ciprofloxacin accumulated in blood neutrophils is 2-7 times higher than in blood serum.

The volume of distribution in the body is 2-3.5 l/kg. The drug penetrates the cerebrospinal fluid in small quantities, where its concentration is usually 6-10% of the serum.

The binding of ciprofloxacin to plasma proteins is 30%. In patients with unchanged renal function, the half-life is usually 3-5 hours. If renal function is impaired, the half-life increases.

Ciprofloxacin is excreted from the body mainly by the kidneys (50-70%) and the gastrointestinal tract (10-30%)

Indications for use

Infectious and inflammatory diseases caused by microorganisms sensitive to ciprofloxacin:

• respiratory tract;
• ear, nose and throat;
• kidneys and urinary tract;
• genitals;
• digestive system (including mouth, teeth, jaws);
• gallbladder and bile ducts;
• skin, mucous membranes, soft tissues;
• musculoskeletal system.

Ciprofloxacin is indicated for the treatment of sepsis and peritonitis, as well as for the prevention and treatment of infections in patients with reduced immunity (during treatment with immunosuppressants). The drug is also indicated for the prevention and treatment of pulmonary anthrax (Bacillus anthracis infection)

Ciprofloxacin, in addition to the prevention and treatment of pulmonary anthrax (Bacillus anthracis infection) in children under 18 years of age and the treatment of complications caused by Pseudomonas aeruginosa, in children from 5 to 17 years of age with pulmonary cystic fibrosis, is not recommended for the treatment of other infectious diseases.

Directions for use and doses

Dose of Ultraflox V.I. the solution for infusion depends on the severity of the disease, the type of infection and its location, the patient’s condition and is administered intravenously 100-200 ml (200-400 mg) 2 times a day. The duration of treatment is 1-2 weeks; if necessary, you can continue the course of treatment. Can be administered intravenously as a bolus, but it is recommended to administer drip over 30 minutes (100 ml).

Side effects

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, flatulence, loss of appetite, cholestatic jaundice (especially in patients with liver disease), hepatitis, hepatonecrosis.

From the central nervous system: dizziness, vertigo, headache, increased fatigue, anxiety, agitation, tremor, insomnia, “nightmare” dreams, peripheral paralgesia (abnormalities of pain sensitivity), paraesthesia, dysesthesia, hypoesthesia, hyperesthesia, peripheral neuropathy, polyneuropathy, sweating, increased intracranial pressure, disorientation, confusion, depression and hallucinations, as well as other manifestations of psychotic reactions (sometimes developing to states where the patient can harm himself), migraine, fainting, thrombosis of the cerebral arteries, convulsions, impaired coordination of movement.

From the senses: impaired taste and smell, visual impairment (diplopia, changes in color perception), tinnitus, decreased hearing, hearing loss.

From the cardiovascular system: tachycardia, cardiac arrhythmia, prolongation of the QT interval, gastric arrhythmias (including pirouette type), decreased blood pressure, flushing of the face.

From the respiratory system: respiratory failure (including bronchospasm).

From the hematopoietic system: leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia, neutropenia, agranulocytosis, pancytopenia, impaired hematopoiesis in the bone marrow.

From the urinary system: hematuria, crystalluria (primarily with alkaline urine and low diuresis), glomerulonephritis, dysuria, polyuria, urinary retention, albuminuria, urethral bleeding, impaired nitrogen excretory function of the kidneys, interstitial nephritis, renal failure.

From the musculoskeletal system: arthralgia, arthritis, tendovaginitis, tendon rupture (Achilles), myalgia, increased muscle tone, muscle cramps, muscle weakness, increased symptoms of myasthenia gravis.

Allergic reactions : skin rashes, urticaria, drug fever, pinpoint bleeding into the skin (petechiae), swelling of the face or larynx, shortness of breath, eosinophilia, vasculitis, erythema nodosum, erythema multiforme exudative, serum sickness, Stevens — Johnson syndrome (erythema malignant exudative ), toxic epidermal necrolysis (Lyell’s syndrome).

Other: increased sensitivity to light, general weakness, superinfection (candidiasis, pseudomembranous colitis), gait disturbance.

From laboratory parameters: hypoprothrombinemia, increased activity of “liver” transaminases and alkaline phosphatase, hypercreatininemia, hyperbilirubinemia, hyperglycemia, increased amylase activity.

Contraindications

• hypersensitivity to ciprofloxacin or to other drugs of the fluoroquinolone group;
• simultaneous use with tizanidine (risk of a pronounced decrease in blood pressure, drowsiness);
• pregnancy;
• lactation period;
• children and adolescents up to 18 years of age;
• pseudomembranous colitis.

With caution — severe cerebral atherosclerosis,cerebrovascular accident, mental illness, epilepsy, severe renal and/or liver failure, in patients with a history of tendon diseases associated with taking quinolones, old age, long QT syndrome, heart disease (heart failure, myocardial infarction, bradycardia), electrolyte imbalance (hypokalemia, hyponatremia), simultaneous use with drugs that prolong the QT interval (including class IA and III antiarrhythmics), simultaneous use with drugs (including theophylline, caffeine, duloxetine, clozapine) metabolized by isoenzymes CYP450 1A 2. .

Overdose

A reversible toxic effect on the kidneys has been determined. A specific antidote is unknown. It is necessary to carefully monitor the patient’s condition, carry out routine emergency measures, and ensure sufficient fluid intake. Using heme peritoneal dialysis, only a small (less than 10%) amount of the drug can be released.

Interaction with other drugs

Due to a decrease in the activity of microsomal oxidative processes in hepatocytes, it prolongs T1/2 of theophylline (other xanthines, for example, caffeine), oral hypoglycemic drugs, and helps to lower the prothrombin index.

When combined with other antimicrobial drugs (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergism is usually observed. For infections caused by Pseudomonas spp. in combination with azocillin and ceftazidime; for staphylococcal infections — mezocillin and azocillin and other beta-lactam antibiotics; for anaerobic infections — with metronidazole and clindamycin can be used with success.

It enhances the nephrotoxic effect of cyclosporine, there is an increase in serum creatinine; in such patients it is necessary to monitor this indicator 2 times a week.

When used simultaneously, it enhances the effect of indirect anticoagulants.

Non-steroidal anti-inflammatory drugs (except acetylsalicylic acid) increase the risk of developing seizures.

The combined use of uricosuric drugs leads to a slower elimination (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

Increases the Cmax of tizanidine by 7 times (from 4 to 21 times) and the area under the pharmacological curve “concentration time” (AUC) by 10 times (from 6 to 24 times), increases the risk of a pronounced decrease in blood pressure and drowsiness. Concomitant use with drugs that prolong the QT interval (class IA and III antiarrhythmics), the QT interval may lengthen.

Concomitant use of ropirinol and ciprofloxacin leads to an increase in the Cmax and AUC of ropirinol by 60% and 84%, respectively. During combined use with ciprofloxacin and after completion of combination treatment, it is necessary to monitor the side effects of ropirinol.

With simultaneous use of clozapine and ciprofloxacin, the serum concentration of clozapine and N-desmethylclozapine may increase by 29% and 31%, respectively (during its use with cyclosporine and after completion of combination treatment, a dose adjustment of clozapine is necessary for a short time).

special instructions

Ciprofloxacin is not the drug of choice for suspected or established pneumonia caused by Streptococcus pneumoniae.

To avoid the development of crystalluria, the recommended daily dose should not be increased, and it is also necessary to consume a sufficient amount of fluid and maintain an alkaline urine reaction.

For patients with epilepsy who have a history of seizures, convulsions, vascular diseases and organic diseases of the brain, due to the risk of developing adverse reactions from the central nervous system, ciprofloxacin should be prescribed only for “vital” indications.

If severe and prolonged diarrhea occurs during or after treatment with ciprofloxacin, the diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and the appointment of appropriate treatment.

If there is pain in the tendons or the first signs of tenosynovitis appear, it is necessary to suspend treatment (during treatment with fluoroquinolones, isolated cases of inflammation and even tendon rupture have been described).

During treatment, UV exposure (including contact with direct sunlight) should be avoided. When treating severe infections, staphylococcal infections and infections associated with anaerobic bacteria, ciprofloxacin must be used in combination with appropriate antibacterial agents.

If infections caused by fluoroquinolone-resistant strains of Neisseria gonorrhoeae are suspected, local data on resistance to ciprofloxacin should be considered and the susceptibility of the pathogen should be confirmed in laboratory tests.

In rare cases, after the first use, anaphylactic reactions up to anaphylactic shock may occur. In such cases, it is necessary to immediately stop the use of ciprofloxacin and carry out appropriate treatment.

In elderly patients with tendon diseases or previously treated with corticosteroids, cases of tendon rupture (mainly Achilles tendon) may occur.

When using the drug for the first time, adverse reactions from the central nervous system may occur. In rare cases, they may manifest as psychosis and suicide attempts. In such cases, you must immediately stop taking the drug and inform your doctor. Ciprofloxacin is a moderate inhibitor of the CYP450 1A 2 isoenzyme. With simultaneous use of ciprofloxacin and drugs metabolized by these isoenzymes (including theophylline, caffeine, fluoxetine, clozapine), caution must be exercised because ciprofloxacin-related inhibition of their metabolism increases the concentration of drugs in the blood serum , may cause specific adverse reactions.

In vitro in laboratory tests, ciprofloxacin inhibits the growth of Mycobacterium spp., which in patients receiving ciprofloxacin in the diagnosis of this pathogen can lead to false negative results.

Effect on the ability to drive vehicles and operate machinery.

Patients receiving ciprofloxacin should be careful when driving or engaging in other potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Release form

Solution for infusion, 100 ml in plastic bottles. 1 bottle along with instructions for use in a cardboard box.

Food conditions

Store in a cool, dark place at temperatures below 30ºC

Keep out of the reach of children. Do not freeze!

Best before date

3 years. Do not use after the expiration date!

Conditions for dispensing from pharmacies

Dispensed with a doctor’s prescription.

Manufacturer : BAL PHARMA LTD, India.