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

active substance: ofloxacin - 2 g (in 1 ml of the solution contains 2 mg ofloxacin). Excipients: sodium chloride, water for injection - up to 1 liter.

Description:clear liquid of light yellow color.

Pharmacotherapeutic group:antimicrobial agent, fluoroquinolone

ATX: & nbsp

S.01.A.E.01 Ofloxacin

J.01.M.A.01 Ofloxacin

Pharmacodynamics:

Ofloksatsin - a broad-spectrum antimicrobial agent from the group of fluoroquinolones, acts on the bacterial DNA-gyrase enzyme, which provides supercoiling and, thus,stability of bacterial DNA (destabilization of DNA chains leads to their death). Has a bactericidal effect. It is active against microorganisms producing beta-lactamase and fast-growing atypical mycobacteria. Sensitive: Staphylococcus aureus, Staphylococcus epidermidis, Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Citrobacter spp., Klebsiella spp. (including Klebsiella pneumonia), Enterobacter spp., Proteus spp. (including Proteus mirabilis, Proteus vulgaris - indole-positive and indolotric), Salmonella spp., Shigella spp. (including Shigella sonnei), Yersinia enterocolitica, Campilobacter jejuni, Aeromonas hydrophila, Plesiomonas shigelloides, Vibrio cholerae, Vibrio parahaemolyticus, Haemophilus influenzae, Chlamydia spp., Legionella spp., Serratia spp., Providencia spp., Haemophilus ducreyi, Bordetella parapertussis, Bordetella pertussis, Moraxella catarrhalis, Propionibacterium acnes, Brucella spp.

Different sensitivity to the drug has: Enterococcus faecalis, Streptococcus pyogenes, pneumoniae and viridans, Serrratio marcescens, Pseudomonas spp., Acinetobacter spp., Mycoplasma hominis, Mycoplasma pneumoniae, Mycobacterium tuberculosis, Mycobacterium fortuitum, Ureaplasma urealyticum, Clostridium perfringens, Corynebacterium spp., Helicobacter pilori, Listeria monocytogenes, Gardnerella vaginalis.

Insensitive to ofloxacin in most cases: Nocardia asteroides, anaerobic bacteria (for example, Bacteroides spp., Peptococcus spp., Peptostreptococcus spp., Eubacter spp., Fusobactcrium spp, Clostridium difficile). He acts on Treponema pallidum.

Pharmacokinetics:

Distribution

After a single infusion of the drug at a dose of 200 mg for 60 minutes, the maximum concentration in the blood plasma is 2.7 μg / ml, 12 hours after the administration, the concentration of ofloxacin in the blood plasma is 0.3 μg / ml.

Equilibrium concentrations are achieved after 4 infusions of the drug. With intravenous

the administration of ofloxacin at a dose of 200 mg every 12 hours for 7 days, the average maximum and minimum equilibrium concentrations are 2.9 and 0.5 μg / ml, respectively. Binding to plasma proteins is 20-25%.

The distribution of ofloxacin: cells (leukocytes, alveolar macrophages), skin, soft tissues, bones, abdominal and pelvic organs, respiratory system, urine, saliva, bile, the secret of the prostate gland, penetrates well through the blood-brain barrier, the placental barrier, is secreted with the mother's milk.

It penetrates into the cerebrospinal fluid (14-60%).

Metabolism and excretion

Ofloxacin partially (5%) is biotransformed in the liver. The half-life is 6-7 hours.

Up to 80% of the dose is excreted by the kidneys unchanged, a small part through the gastrointestinal tract.

With hemodialysis, 10-30% of the drug is removed. In patients with impaired renal function (creatinine clearance 50 ml / min or less), the half-life of ofloxacin increases.

Do not cumulate.

Indications:

Respiratory tract infections (bronchitis, pneumonia), LOP(sinusitis, pharyngitis, otitis media, laryngitis, tracheitis), skin, soft tissues, bones, joints, infectious and inflammatory diseases of the abdominal cavity and bile ducts, kidneys (pyelonephritis), urinary tract (cystitis, urethritis), pelvic organs (endometritis, salpingitis, oophoritis, cervicitis, parametritis, prostatitis),genital organs (colpitis, orchitis, epididymitis), gonorrhea, chlamydia; sepsis, meningitis; prevention of infections in patients with impaired immune status (including neutropenia).

Contraindications:

Hypersensitivity to the components of the drug, as well as to other antibiotics of the group of fluoroquinolones, a deficiency of glucose-6-phosphate dehydrogenase, epilepsy (including in the anamnesis), a decrease in the convulsive threshold (including after craniocerebral trauma, stroke or inflammatory processes in the central nervous system); defeat of tendons in the previously conducted treatment with fluoroquinolones, age to 18 years, pregnancy, lactation.

Carefully:

atherosclerosis of cerebral vessels, cerebral circulatory disorders (in the anamnesis), chronic renal failure, organic lesions of the central nervous system.

Pregnancy and lactation:contraindicated

Dosing and Administration:

Apply ofloxacin in the form of intravenous infusion. Ofloksatsina dose for intravenous administration should not differ from the dose for oral administration.

The introduction begins with a single dose of 200 mg, which is administered drip, slowly for 30-60 minutes.When the patient's condition is improved, they are transferred to oral intake of the drug at the same daily dose.

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

respiratory tract infections, as well as ENT organs, skin and soft tissue infections, infections of bones and joints, infections of the abdominal cavity, septic infections - 200 mg 2 times a day. If necessary, increase the dose to 400 mg twice a day.

For the prevention of infections in patients with a marked decrease in immunity - 400-600 mg / day.

In patients with impaired renal function (when creatinine clearance is 50-20 ml / min), a single dose should be 50% of the average dose with a multiplicity of 2 times per day,

or a full single dose is administered once a day. When creatinine clearance is less than 20 ml / min, the first dose is 200 mg, then 100 mg / day every other day. With hemodialysis and peritoneal dialysis - 100 mg every 24 hours. The maximum daily dose for liver failure is 400 mg / day.

The duration of treatment is determined by the sensitivity of the pathogen and the clinical picture; treatment should continue for at least 3 more days after the disappearance of the symptoms of the disease and complete normalization of temperature.

Side effects:

From the digestive system: gastralgia, decreased appetite, nausea, vomiting, diarrhea, flatulence, abdominal pain, increased activity of "hepatic" transaminases, hyperbilirubinemia, cholestatic jaundice, pseudomembranous enterocolitis.

From the nervous system: headaches, dizziness, motion uncertainty, tremors, convulsions, numbness and paresthesia of the limbs, intense dreams, nightmarish dreams, psychotic reactions, anxiety, arousal, phobias, depression, confusion, hallucinations, increased intracranial pressure.

From the musculoskeletal system: tendonitis, myalgia, arthralgia, tendosynovitis, tendon rupture.

From the sense organs: violation of color perception, diplopia, violation of taste, smell, hearing and balance

From the cardiovascular system: tachycardia, lowering blood pressure, collapse (with a sharp decrease in blood pressure, the drug is stopped).

Allergic reactions: skin rash, itching, hives, allergic pneumonitis, allergic nephritis, eosinophilia, fever, Quincke's edema, bronchospasm; exudative erythema multiforme (incl.Stevens-Johnson syndrome) and toxic epidermal necrolysis (Lyell's syndrome), photosensitivity, vasculitis, anaphylactic shock.

From the skin: point hemorrhages (petechiae), bullous hemorrhagic dermatitis, papular rash with a cortex - indicating the damage of blood vessels.

From the hematopoiesis: leukopenia, agranulocytosis, anemia, thrombocytopenia, pancytopenia, hemolytic and aplastic anemia.

From the urinary system: acute interstitial nephritis, impaired renal function, hypercreatininemia, increased urea levels.

Other: dysbacteriosis of the intestine, superinfection, hypoglycemia (in patients with diabetes mellitus), vaginitis.

Local reactions: hyperemia at the injection site, thrombophlebitis.

Overdose:

Symptoms: dizziness, confusion, inhibition, disorientation,

drowsiness, vomiting.

Treatment: symptomatic therapy.

Interaction:

Reduces the clearance of theophylline by 25% (with simultaneous use should reduce the dose of theophylline).

Increases the concentration of glibenclamide in plasma.

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

At simultaneous admission with antagonists of vitamin K, it is necessary to control the blood coagulation system.

When administered with non-steroidal anti-inflammatory drugs, derivatives of nitroimidazole and methylxanthines, the risk of neurotoxic effects increases.

At simultaneous appointment with glucocorticosteroids, the risk of rupture of tendons increases, especially in the elderly.

When administered with drugs that alkalinize urine (inhibitors of carbonic anhydrase, citrates, sodium bicarbonate), the risk of crystalluria and nephrotoxic effects increases. Compatible with the following infusion solutions: 0.9% solution of sodium chloride, Ringer's solution, 5% fructose solution, 5% solution dextrose.Do not mix with heparin (risk of precipitation)!

Special instructions:

Ofloxacin is not a drug of choice for pneumonia caused by pneumococci.

Not indicated in the treatment of acute tonsillitis.

It is not recommended to use the preparation for more than 2 months, to be exposed to sunlight, to UV rays (mercury quartz lamps, solarium).

In the event of side effects from the central nervous system, allergic reactions, pseudomembranous colitis, drug withdrawal is necessary.

With pseudomembranous colitis, confirmed colonoscopically and / or histologically, oral administration of vancomycin and metronidazole is indicated.

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

During the treatment period it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

During the period of treatment can not be consumed ethanol.

When using the drug, women are not recommended to use hygiene tampons, due to the increased risk of thrush development.

Against the backdrop of treatment, myasthenia flow may worsen, and porphyria attacks may be more frequent in predisposed patients.

Can lead to false-negative results in the bacteriological diagnosis of tuberculosis (prevents the isolation Mycobacterium tuberculosis).

In patients with impaired liver or kidney function, it is necessary to monitor the concentration of ofloxacin in the blood plasma. In severe renal and hepatic insufficiency, the risk of toxic effects increases (a decreasing dose adjustment is required).

Form release / dosage:

Solution for infusions 2 mg / ml.

Packaging:

100 ml in bottles of glass. Bottle with instructions for use in the pack.

For hospital:

48 bottles without bundles with 5 instructions for use in a box of corrugated cardboard.

1 bottle with instructions for use

(from 1 to 48 bottles with an equal number of instructions for use) without a bundle in a box of corrugated cardboard.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Freezing is not allowed.

Keep out of the reach of children.

After the expiry date of the drug, unused bottles should be carefully opened, contents drained into the sewer.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-008195/08

Date of registration:16.10.2008

The owner of the registration certificate:KRASFARMA, JSC KRASFARMA, JSC Russia

Manufacturer: & nbsp

KRASFARMA, JSC Russia

Information update date: & nbsp26.03.2012

Illustrated instructions

Instructions

Ofloxacin (Ofloxacin)