Ofloxacin, 400 mg 10 pcs

Pharmacotherapeutic group

Antimicrobial agent, fluoroquinolone

ATX Code

S01AE01

Pharmacodynamics:

A broad-spectrum antimicrobial from the group of fluoroquinolones acts on the bacterial enzyme DNA-hydrase, which provides superspiration and thus the stability of bacterial DNA (destabilization of DNA chains leads to their death). It has a bactericidal effect.

Highly active against most gram-negative and some gram-positive microorganisms: Aeromonas hydrophila Branhamella catarrhalis Brucella spp. Clostridium perfringens Escherichia coli Salmonella spp. Enterobacter spp. Serratia spp. Citrobacter spp. Yersinia spp. Providencia spp. Haemophilus influenzae and parainfluenzae Haemophilus ducreyi Plesiomonas Legionella Shigella spp. Proteus spp. including Proteus mirabilis Proteus vulgaris (indol + indol -) Moraxella morganii Klebsiella spp. (including Klebsiella pneumonia) Helicobacter pylori Mycoplasma spp. Vibrio spp. Gardnerella vaginalis Neisseria gonorrhoeae Neisseria meningitidis Chlamydia trachomatis Staphylococcus aureus methi-S Staphylococcus coagulase negative.

Moderately sensitive to ofloxacin Acinetobacter spp. Ureaplasma urealyticum Bacteroides fragilis Mycobacterium tuberculosis Mycobacterium fortuitum Chlamidia psittaci anaerobic gram-positive cocci Enterococcus faecalis Streptococcus pneumoniae Pseudomonas spp. Streptococcus spp. (especially beta-hemolytic).

Acinetobacter braumanmii Clostridium difficile Enterococci Listeria monocytogenes Staphylococci methi-R Nocardia spp. are insensitive to Ofloxocin.

Ofloxacin is inactive against Treponema pallidum.

Pharmacokinetics:

Absorption after oral administration is fast and complete (95%). Bioavailability – over 96% plasma protein binding – 25%. Time to reach maximum concentration (TCmax) when taken orally – 1 -2 hours. Maximal concentration (Cmax) after a single dose of 100, 200, 300 and 600 mg is 1.3 4 and 6.9 mg/l, respectively, and it depends on the dose: after a single dose of 200 and 400 mg it is 2.5 and 5 mcg/ml, respectively.

Food may delay absorption but has no significant effect on bioavailability. Volume of distribution is 100 l. Distribution: cells (leukocytes alveolar macrophages) skin soft tissues bones abdominal organs and small pelvis respiratory system urine saliva bile prostate secretion; well penetrates through the blood-brain barrier placental barrier is secreted with the mother’s milk. Penetrates into cerebrospinal fluid (14-60%). Metabolized in the liver (about 5%) to form N-oxide ofloxacin and dimethylofloxacin. Half-life (T1/2) – 4.5-7 hours (regardless of the dose). Excreted by the kidneys – 75-90% (unchanged) about 4% – in the bile. Extra-renal clearance is less than 20%.

After a single use in a dose of 200 mg in the urine is detectable within 20-24 hours. With renal/hepatic insufficiency, excretion may be delayed. It does not cumulate. Hemodialysis removes 10-30% of the drug.

Indications

Treatment of infectious and inflammatory diseases caused by microorganisms sensitive to Ofloxacin:

– respiratory tract infections (except in cases of pneumococcal infection); – Ear-nose-throat infections (except in cases of acute tonsillitis);

– infections of the abdomen and biliary tract;

– infections of the kidneys of the urinary tract of the prostate urethra (including gonococcal

– infections of the pelvic organs;

– infections of bones and joints;

– infections of skin and soft tissues;

– prevention of infections in patients with compromised immune status (including neutropenia).

Infections of the skin and soft tissues.)

Active ingredient

Composition

Each tablet contains:

Active substance:

ofloxacin 400 mg;

Associates:

Corn or potato starch;

MCC;

Talc;

polyvinylpyrrolidone low molecular weight;

magnesium or calcium stearate;

aerosil

Shell composition: oxypropyl methylcellulose; talc; titanium dioxide; propylene glycol; polyethylene oxide 4000 or opider IIOfloxacin – 400 mg.

How to take, the dosage

The dose of Ofloxacin and the duration of treatment depend on the severity and type of infection, the general condition of the patient and renal function.

The average daily dose for adults is 200 mg to 600 mg. The duration of treatment is 7-10 days.

Dose up to 400 mg/day can be administered in 1 dose preferably in the morning. Doses over 400 mg/day should be divided into 2 doses at regular intervals. The tablets should be taken in whole with water both before and during meals. Simultaneous use with antacids should be avoided.

In case of severe infections or when treating overweight patients, the daily dose can be increased to 800 mg.

In uncomplicated lower urinary tract infections, the drug is prescribed in a dose of 200 mg/day for 3-5 days. In gonorrhea it is prescribed 400 mg once.

In patients with hepatic insufficiency, it is not recommended to exceed the maximum daily dose of 400 mg.

Interaction

When concomitant use of vitamin K antagonists it is necessary to monitor the blood clotting system.

Ofloxacin may slightly increase serum concentrations of glibenclamide when used concomitantly.

When high doses ofloxacin and other medications excreted by renal tubular secretion such as probenecid cimetidine furosemide or methotrexate are used, the serum concentration of ofloxacin may increase.

Significant decrease in seizure threshold may be observed when fluoroquinolones are prescribed in combination with theophylline-phenbufen or other non-steroidal anti-inflammatory drugs as well as other drugs that lower the seizure threshold.

The risk of neurotoxic effects increases with nonsteroidal anti-inflammatory drugs nitroimidazole derivatives and methylxanthines.

Concomitant administration with glucocorticosteroids increases the risk of tendon rupture especially in the elderly.

The risk of QT interval prolongation increases when co-administered with drugs that prolong the QT interval (Class IA and III antiarrhythmic drugs tricyclic antidepressants macrolides).

The risk of crystalluria and nephrotoxic effects increases when prescribed with drugs that alkalize the urine (carboanhydrase inhibitors sodium hydrocarbonate citrate).

Special Instructions

Due to the fact that ofloxacin is mainly excreted through the kidneys in patients with renal insufficiency the dose of of ofloxacin should be corrected. Due to the risk of photosensitization, exposure to sunlight and ultraviolet rays should be avoided. Occurrence of diarrhea especially in severe persistent and/or with blood admixture during or after treatment with ofloxacin may be a manifestation of pseudomembranous colitis. If pseudomembranous colitis is suspected, treatment with ofloxacin should be discontinued immediately and appropriate specific antibacterial therapy should be administered without delay. Drugs that inhibit intestinal peristalsis are contraindicated in this clinical situation.

Like other quinolones, ofloxacin should be used with particular caution in patients who are prone to epileptic seizures (patients with a history of central nervous system damage taking phenbufen and similar non-steroidal anti-inflammatory drugs or drugs that lower the seizure threshold such as theophylline).

Tendinitis occurring very rarely can sometimes lead to tendon rupture, mainly of the Achilles tendon, especially in older patients. If signs of tendinitis (inflammation of the tendon) occur, it is recommended that treatment be stopped immediately, the Achilles tendon be immobilized, and an orthopedic consultation be obtained.

Particular caution is necessary when taking fluoroquinolones including ofloxacin in patients with known risk factors for QT interval prolongation such as:

-older age;

-uncorrectable electrolyte imbalances (e.g., hypokalemia hypomagnesemia); -congenital QT interval prolongation;

– cardiovascular disease (heart failure myocardial infarction bradycardia);

– concurrent use of drugs prolonging the QT interval (Class IA and III antihypertensive drugs tricyclic antidepressants macrolides).

Ofloxacin may worsen the course of myasthenia gravis. There may be an increase in the frequency of attacks of porphyria. During treatment with Ofloxacin, false positives may occur with urinary opiates and porphyrins.

Ofloxacin prevents isolation of Mycobacterium tuberculosis leading to false-negative results in the bacteriological diagnosis of tuberculosis. It is also not recommended to consume ethanol during treatment. Ofloxacin is not the drug of choice for pneumonia caused by pneumococci. It is not indicated in the treatment of acute tonsillitis.

At the time of treatment, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities that require increased concentration and rapid psychomotor reactions.

Contraindications

– Hypersensitivity to ofloxacin to other quinolones or components of the drug;

– epilepsy;

– lesion of the central nervous system with reduced seizure threshold (after craniocerebral injury of stroke inflammatory processes in the central nervous system (CNS);

– tendon involvement in previous treatment with quinolones;

– glucose-6-phosphate dehydrogenase deficiency;

– age less than 18 years;

– pregnancy and lactation.

Side effects

Nervous system disorders: headache dizziness insecurity of movements tremor cramps numbness and paresthesias of extremities intense dreams “nightmares” psychotic reactions anxiety state agitation phobia depression confusion hallucinations increased intracranial pressure.

Musculoskeletal system: tendinitis myalgia arthralgia tendosynovitis tendon rupture.

Sense organs: color perception disorders diplopia disorders of taste, smell, hearing and balance.

Cardiovascular system disorders: tachycardia decreased blood pressure (BP)

Allergic reactions: skin rash pruritus urticaria allergic pneumonitis allergic nephritis eosinophilia fever angioedema bronchospasm; erythema multiforme (including erythema exudative).Stevens-Johnson syndrome and toxic epidermal necrolysis (Lyell’s syndrome) photosensitization vasculitis anaphylactic shock.

Skin disorders: petechial haemorrhages (petechiae) bullous hemorrhagic dermatitis papular rash with crust indicating vascular lesions (vasculitis).

Hematopoietic organs: leukopenia agranulocytosis anemia thrombocytopenia pancytopenia hemolytic and aplastic anemia.

Urinary system disorders: acute interstitial nephritis renal dysfunction hypercreatininemia increased concentration of urea.

Others: intestinal dysbacteriosis superinfection hypoglycemia (in diabetic patients) vaginitis.

Overdose

Symptoms: dizziness confusion confusion disorientation drowsiness vomiting.

In case of overdose, gastric lavage and symptomatic therapy are recommended. There is no specific antidote.

Pregnancy use

Similarities