Ashof - instructions for use, dose, side effects, contraindications

The bactericidal effect of ofloxacin is associated with the inhibition of DNA gyrase, which leads to a disruption in the replication of bacterial DNA and the death of microbial cells. Ofloxacin has a wide spectrum of antimicrobial action, including microorganisms resistant to other antibiotics, including strains that produce beta-lactamases.

Active (minimal suppressive concentration (MIC) <0.5 mg / l) against Gram-positive microorganisms: Staphylococcus aureus

(methicillin-sensitive strains), Staphylococcus spp. (coagulase-negative); Gram-negative aerobic microorganisms: Aeromonas hydrophila, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, producing and not producing beta-lactamase strains Haemophilus influenzae, Haemophilus parainfluenzae, Haemophilus ducreyi, Klebsiella oxytoca, Morganella morganii, Moraxella catarrhalis, producing and not producing beta-lactamase strains Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Proteus vulgaris, Plesiomonas spp., Salmonella enterica, Shigella spp., Serratici marcescens, Yersinia enterocolitica; other microorganisms: Chlamydia trachomatis, Chlamydia pneumoniae, Mycoplasma hominis, Legionella pneumophila, Mycoplasma pneumoniae, Ureaplasma urealyticum.

Different sensitivity to the drug has: Acinetobacter spp., Gardnerella vaginalis, Pseudomonas aeruginosa Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus hominis, Streptococcus pneumoniae (penicillin-sensitive and penicillin-resistant), Streptococcus pyogenes, Streptococcus spp. groups viridians, Streptococcus bovis, Streptococcus agalactiae, Klebsiella pneumoniae, Mycobacterium leprae, Mycobacterium tuberculosis.

Are resistant to ofloxacin: Staphylococcus aureus (methicillin-resistant strains), Nocardia asteroides, Enterococcus spp., Treponema pallidum, Listeria monocytogenes, most anaerobes, including Peptostreptococcus spp., Eubacterium spp., Fusobacterium spp., Clostridium difficile.

Pharmacokinetics:

The maximum serum concentration with a 30-minute intravenous infusion of ofloxacin is achieved at the end of the infusion. Concentrations of ofloxacin in serum after a 30-minute intravenous infusion of the drug:

Dose	Whey	Whey	Whey
	concentration	concentration	concentration
	ofloxacin after	ofloxacin through 4	ofloxacin through
	infusion	hours after infusion	12 hours after infusion
100 mg	2.9 mg / L	0.5 mg / l	0,2 mg / l
200 mg	5.2 mg / l	1.1 mg / l	0.3 mg / l

At the off-line use of ofloxacin, serum concentration does not increase significantly (the accumulation factor when administered twice a day is 1.5).

Quickly penetrates and is well distributed in many organs, tissues and fluids of the body, penetrates into cells. Therapeutically significant concentrations exceeding serum levels are noted in interstitial tissue, saliva, sputum, lung tissue, myocardium, bones, mucosa and intestinal wall, peritoneal fluid, pancreatic juice and pancreatic tissue, prostate gland, semen, female reproductive organs system, skin and subcutaneous tissue; penetrates into leukocytes and alveolar macrophages. The volume of distribution is 120 liters. It penetrates well through the blood-brain barrier, reaching therapeutic concentrations; in high concentrations passes through the hematoplacental barrier, excreted in breast milk. The connection with plasma proteins is approximately 25%.

The half-life with intravenous infusion is 5 hours,The decrease in serum concentration of ofloxacin after infusion occurs linearly. Less than 5% ofloxacin undergoes biotransformation in the liver. In the urine

two major metabolites are detected: dimethylfloxacin and N-oxide ofloxacin. Excretion by the kidneys (80-90% of the dose) in unchanged form. In small quantities is excreted through the intestine. In the bile ofloxacin is found in a glucuronated form.

In elderly patients, the elimination half-life increases; total and renal clearance decrease in proportion to the decrease in creatinine clearance (CC).

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to ofloxacin:

- lower respiratory tract, with the exception of cases of established pneumococcal infection or suspected of it (some strains Streptococcus pneumoniae are only partially sensitive to ofloxacin, therefore it should not be used as the first-choice drug for community-acquired pneumonia caused by this pathogen);

- LOP-organ (sinusitis, pharyngitis, otitis media, laryngitis, tracheitis), except in cases of acute tonsillitis,(some strains of β-hemolytic streptococcus are only partially sensitive to ofloxacin, so it should not be used as a first-choice drug for acute tonsillitis caused by β-hemolytic streptococcus);

- skin and soft tissues;

- bones (osteitis, osteomyelitis) and joints;

- organs of the abdominal cavity and bile ducts;

- kidney, urinary tract, prostate and urethra;

- genital organs and pelvic organs (pelvioperitonitis, endometritis, salpingitis, oophoritis, tubo-ovarian abscesses);

- septicemia;

- prevention of infections in patients with impaired immune status (including neutropenia).

Contraindications:

Hypersensitivity to ofloxacin, the components of the drug and other fluoroquinolones; epilepsy (including in the anamnesis), reduction of convulsive threshold (including after a craniocerebral injury, stroke or inflammatory processes in the central nervous system); children's age till 18 years; pregnancy, lactation; the defeat of the tendons in the previous treatment with fluoroquinolones.

Carefully:

Atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), chronic renal failure, hepatic insufficiency, organic diseases of the central nervous system, predisposition to convulsive reactions, myasthenia gravis, hepatic porphyria, glucose-6-phosphate dehydrogenase deficiency, diabetes mellitus, congenital lengthening interval syndrome QT, heart disease (heart failure, myocardial infarction, bradycardia), psychoses and other mental disorders in the anamnesis; simultaneous use of drugs that extend the interval QT (antiarrhythmic IA and III classes, tricyclic and tetracyclic antidepressants, neuroleptics, macrolides, antifungal, imidazole derivatives, some antihistamines, including astemizole, terfenadine, ebastine), for general anesthesia from the barbiturate group, drugs that lower blood pressure, drugs that reduce the threshold of convulsive brain readiness (fenbufen, theophylline); electrolyte imbalance (eg, hypokalemia, hypomagnesemia); elderly age.

Pregnancy and lactation:

Ofloxacin is contraindicated for use in pregnancy.

As ofloxacin excreted into breast milk, then due to the risk to the child, breast-feeding women, women should not use the drug. In case of urgent need for the drug, breastfeeding at this time should be discontinued.

Dosing and Administration:

Intravenously drip. The duration of administration of 200 mg ofloxacin is 30 minutes. Doses are selected individually depending on the location and severity of the infection, as well as the sensitivity of microorganisms and the general condition of the patient.

In patients with normal renal function, the average therapeutic single dose of ofloxacin is 200 mg, which is administered twice a day at intervals of 12 hours. For the treatment of severe infections, including in patients with impaired immune status, a single dose can be increased to 400 mg, which is administered intravenously drip 2 times a day.

Urinary tract infections - 100 mg, 1-2 times a day; infections of the kidneys and genitalia, organs - from 100 mg twice a day to 200 mg twice a day.

The daily dose to 400 mg ofloxacin can be administered once a day.In this case, it is preferable to administer the drug in the morning.

In patients with impaired renal function (with QC less than 50 ml / min), the first dose is the same as in patients with normal renal function and depends on the localization and severity of the infection. In the future, doses and dosing regimens are set taking into account the value of the SC.

Creatinine clearance, ml / min	50-20	<20	Hemodialysis or peritoneal dialysis
Single dose of the drug	100-200 mg every 24 hours	100 mg every 24 hours or 200 mg every 48 hours	100 mg every 24 hours or 200 mg every 48 hours

In severe violations of the liver (for example, with cirrhosis of the liver with ascites) it is not recommended to exceed the dose of ofloxacin 400 mg / day.

The duration of treatment depends on the severity of the disease. Like treatment with other antimicrobials, the administration of ofloxacin should continue for at least 48-72 hours after the normalization of body temperature or with confirmation of eradication of the bacterial agent.

After a few days, when the condition improves, the patient is transferred to receive the drug in a dosage form for oral administration at the same daily dose.

Side effects:

Very often -> 1/10; often from> 1/100 to <1/10; infrequently - from> 1/1000 to <1/100; rarely - from> 1/10000 to <1/1000; very rarely - from <1/10000,including individual messages; for adverse reactions, the frequency of which can not be estimated, it is indicated that the frequency is unknown.

From the digestive system: infrequently - abdominal pain, diarrhea, nausea, vomiting; rarely - enterocolitis (in some cases, hemorrhagic); very rarely - pseudomembranous colitis; frequency unknown - constipation, flatulence.

From the nervous system: infrequently - dizziness, headache; rarely - drowsiness, paresthesia, dysgeusia (a disorder of perception of taste), parosmia (a disorder of perception of smell); very rarely - peripheral sensory neuropathy, peripheral sensory-motor neuropathy, seizures, extrapyramidal symptoms, including tremor, and other disorders of muscle coordination; frequency unknown - increased intracranial pressure.

From the side of the musculoskeletal system: rarely - tendonitis; very rarely - myalgia, arthralgia, tendon rupture (Achilles tendon); individual cases - rhabdomyolysis and / or myopathy, muscle weakness, which is especially important for patients with pseudo-paralytic myasthenia, muscle ruptures.

From the sense organs: infrequent - irritation of the mucous membrane of the eye, vertigo; rarely - visual impairment, hearing impairment (ringing in the ears), hearing loss.

From the side of the cardiovascular system: often phlebitis; infrequently - lowering blood pressure, collapse (with a sharp drop in blood pressure, the introduction is discontinued); rarely - sinus tachycardia, "flushes" of blood to the skin of the face, ventricular arrhythmias, an increase in the QT interval on the cardiogram.

Allergic reactions: infrequently - skin rash, itching; rarely - angioedema, urticaria, pustular rash; very rarely, multiforme exudative erythema (including Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), drug rash, photosensitivity, vasculitis, which in exceptional cases can lead to cutaneous necrosis, anaphylactic shock / anaphylactoid shock; isolated cases - allergic pneumonitis; frequency unknown: bullous haemorrhagic dermatitis, allergic nephritis, eosinophilia, acute generalized exanthematous pustulosis.

Disturbances from the respiratory system and chest organs: infrequently - cough, nasopharyngitis; rarely shortness of breath, bronchospasm.

Disorders of the psyche: infrequently - agitation, sleep disturbances, insomnia; rarely - psychotic reactions (for example, hallucinations), anxiety, anxiety, nervousness, confusion, "nightmarish" dreams, depression; individual cases - psychotic reactions and depression with self-harm, in rare cases, up to suicidal thoughts or attempts.

From the skin: frequency unknown - point hemorrhages (petechiae).

On the part of the organs of hematopoiesis: very rarely - leukopenia, anemia (including hemolytic and aplastic), thrombocytopenia; individual cases - pancytopenia, agranulocytosis, oppression of bone marrow hematopoiesis.

From the urinary system: rarely - increased serum creatinine concentration; very rarely - acute renal failure; isolated cases - acute interstitial nephritis; frequency unknown - increased urea concentration in the blood.

From the liver and biliary tract: rarely - increased activity of "liver" transaminases, alkaline phosphatase, increased bilirubin concentration; very rarely - cholestatic jaundice; isolated cases - hepatitis, which can be severe.

Local Reactions: often - pain, hyperemia at the injection site, thrombophlebitis.

Other: infrequently - asthenia, superinfection, candidiasis; rarely - anorexia, hyperhidrosis; very rarely - hypoglycemia (in patients with diabetes mellitus), porphyria attacks in patients with porphyria; frequency unknown - intestinal dysbacteriosis, vaginitis, vaginal discharge.

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation, convulsions, drowsiness, vomiting, symptoms of irritation of the mucous membranes.

Treatment: forced diuresis, symptomatic therapy.

Interaction:

The simultaneous use of ofloxacin and barbiturates can lead to a sharp decrease in blood pressure. Therefore, while using barbiturates, for example, as an anesthetic, and ofloxacin, the function of the cardiovascular system should be monitored.

In clinical studies, no pharmacokinetic interactions of ofloxacin with theophylline have been established. However, the simultaneous use of theophylline, fenbufen and other non-steroidal anti-inflammatory drugs with ofloxacin can increase seizure activity of the brain.

Probenecid, cimetidine, furosemide, methotrexate and drugs that block tubular secretion, increase the concentration of ofloxacin in blood plasma.

Indirect anticoagulants: simultaneous application with ofloxacin leads to an increase in the activity of coumarin derivatives, which requires monitoring of the parameters of the blood coagulation system.

Glibenclamide, other hypoglycemic drugs and insulin: when used with ofloxacin, a slight increase in the level of hypoglycemic drugs and, as a consequence, hypoglycemia may occur, which requires monitoring of the glucose concentration in the blood.

When used simultaneously with glucocorticosteroids, the risk of rupture of tendons increases, especially in elderly patients.

When used with drugs that alkalinize urine (carbonic anhydrase inhibitors, citrates, sodium hydrogen carbonate), the risk of crystalluria and nephrotoxic effects increases.

Increases serum concentration of cyclosporine.

Possible lengthening interval QT when used simultaneously with drugs that extend the interval QT (see the "Caution" section).

A solution of ofloxacin should not be mixed with heparin because of the risk of precipitation in solution.

Compatible with the following infusion solutions: 0.9% solution of sodium chloride, Ringer's solution, 5% dextrose solution.

Special instructions:

Ofloxacin is not a drug of choice for diseases of the upper and lower respiratory tract caused by pneumococci.

As with other fluoroquinolones, due to possible photosensitization, it is advisable to avoid exposure to direct sunlight or ultraviolet radiation.

Rarely developing tendonitis can lead to rupture of tendons (mainly Achilles tendon), especially in elderly patients. In case of signs of tendonitis, it is necessary immediately to stop treatment, to immobilize the Achilles tendon and consult an orthopedist.

If a severe and prolonged diarrhea occurs (persistent and / or with a blood impurity), the diagnosis of pseudomembranous colitis should be ruled out, which requires immediate discontinuation of the drug and the appointment of appropriate treatment (prescription inside vancomycin or metronidazole).The use of drugs that inhibit intestinal peristalsis is contraindicated.

Ofloxacin inhibits growth Mycobacterium tuberculosis, which can lead to false-negative results of bacteriological tests in patients with tuberculosis.

Against the backdrop of treatment, the myasthenia flow may worsen, the incidence of porphyria attacks in predisposed patients; with insufficiency of glucose-6-phosphate dehydrogenase - the risk of hemolysis of erythrocytes.

If there are side effects from the central nervous system, allergic reactions need to cancel the drug.

In patients with diabetes, especially with the simultaneous use of hypoglycemic drugs, it is necessary to monitor the concentration of glucose in the blood.

In patients receiving fluoroquinolones, including ofloxacin, sensory and sensory-motor peripheral neuropathy was noted, the onset of which can be rapid. If the patient develops symptoms of neuropathy (pain, burning, tingling, numbness and / or weakness or other sensitivity disorders, including tactile, pain, temperature, vibration sensitivity and a sense of position), the use of ofloxacin should be discontinued.This minimizes the possible risk of irreversible changes.

Lengthening of the interval has been reported QT in patients who received fluoroquinolones, including ofloxacin. When using fluoroquinolones, including ofloxacin, caution should be exercised in patients with known risk factors for lengthening the interval QT: elderly age; violation of electrolyte balance (hypokalemia, hypomagnesemia); congenital lengthening syndrome QT; heart disease (heart failure, myocardial infarction, bradycardia); simultaneous administration of medications that can lengthen the interval QT.

In patients with impaired liver or kidney function, it is necessary to control the concentration of ofloxacin in the blood. In patients with renal insufficiency, dose adjustment of ofloxacin is necessary.

When determining opiates and porphyrin in urine during the use of ofloxacin, it is possible to obtain a false positive result.

For the treatment of mixed aerobic-anaerobic infections (peritonitis, endometritis and others) it is recommended to combine ofloxacin with one of the antibiotics that have antianaerobic activity.

As with the use of other antimicrobial agents, the use of ofloxacin, especially for a long time, can lead to increased reproduction of insensitive microorganisms and the development of superinfection.

Effect on the ability to drive transp. cf. and fur:During the period of treatment, it is necessary to refrain from driving vehicles and practicing other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:100 ml of the drug in a bottle of low density polyethylene with a lid of low density polyethylene. The bottle in a sealed polypropylene bag, along with the instructions for use, is placed in a cardboard box.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002474

Date of registration:22.05.2014

Expiration Date:22.05.2019

Date of cancellation:2019-05-22

The owner of the registration certificate:MANAS MED, LTD MANAS MED, LTD Russia

Manufacturer: & nbsp

AISHWARYA HEALTHCARE India

Representation: & nbspManas Med, OOOManas Med, OOO

Information update date: & nbsp23.09.2017

Illustrated instructions

Instructions

Ashof (Ashof)