Ofloxacin: Instructions for use, price, reviews and analogues

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Is ofloxacin an antibiotic or not? This is not an antibiotic , but an antibacterial agent from the group of fluorinated quinolones , which is not the same thing. Differs from antibiotics in structure and origin. Fluoroquinolones have no analogues in nature, and antibiotics are products of natural origin.

The bactericidal effect is associated with inhibition of DNA gyrase, which leads to disruption of DNA synthesis and cell division, changes in the cell wall, cytoplasm and cell death. The inclusion of a fluorine atom in the quinoline molecule changed the spectrum of antibacterial action - it has expanded significantly and also includes microorganisms that are resistant to antibiotics and strains that produce beta-lactamases.

Gram-positive and gram-negative microorganisms, as well as chlamydia , ureaplasma , mycoplasma , gardnerella . Suppresses the growth of Mycobacterium tuberculosis . Does not affect Treponema pallidum. Microflora resistance develops slowly. A pronounced post-antibiotic effect is characteristic.

Pharmacokinetics

Absorption after oral administration is good. Bioavailability 96%. A small part of the drug binds to proteins. The maximum concentration is determined after 1 hour. It is well distributed in tissues, organs and fluids, penetrates into cells. Significant concentrations are observed in saliva, sputum, lung, myocardium, intestinal mucosa, bones, prostate tissue, female genital organs, skin and fiber.

Penetrates well through all barriers and into the cerebrospinal fluid. About 5% of the dose is biotransformed in the liver. The half-life is 6-7 hours. With repeated administration, cumulation is not pronounced. It is excreted by the kidneys (80-90% of the dose) and a small part with bile. In renal failure, T1/2 increases. With liver failure, excretion may also slow down.

Pharmacological properties of the drug Ofloxacin

Ofloxacin is an antimicrobial agent of the fluoroquinolone group. The bactericidal effect of ofloxacin, like other fluorinated quinolones, is due to its ability to block the bacterial enzyme DNA gyrase. The antibacterial spectrum of ofloxacin covers microorganisms resistant to penicillins, aminoglycosides, cephalosporins, as well as microorganisms with multiple resistance. The spectrum of action of ofloxacin includes the following types of microorganisms: Aerobic gram-negative bacteria - E. coli, Klebsiella spp., Salmonella spp., Proteus spp., Shigella spp., Yersinia spp., Enterobacter spp., Morganella morganii, Providencia spp., Vibrio spp. , Citrobacter spp., Serratia spp., Campylobacter spp., Pseudomonas aeruginosa, P. cepacia, Neisseria gonorrhoeae, N. meningitidis, Haemophilus influenzae, H. ducreyi, Acinetobacter spp., Moraxella catarrhalis, Gardnerella vaginalis, Pasteurella multocida, Helicobacter pylori. Aerobic gram-positive bacteria - staphylococci, including penicillinase-producing and methicillin-resistant strains, streptococci (especially Streptococcus pneumoniae ), Listeria monocytogenes, Corynebacterium spp. Ofloxacin is more active than ciprofloxacin against Chlamydia trachomatis . It is also active against Mycobacterium leprae and Mycobacterium tuberculosis and several other Mycobacterium . There are reports of a synergistic effect against M. leprae of ofloxacin and rifabutin. Treponema pallidum , viruses, fungi and protozoa are not susceptible to ofloxacin. Quickly and almost completely absorbed from the digestive tract. The absolute bioavailability of ofloxacin is 96% after oral administration. Plasma concentrations reach a level of 3–4 mcg/ml 1–2 hours after administration of a dose of 400 mg. Eating does not reduce the absorption of ofloxacin, but may slightly slow down the rate of absorption. The half-life is 5–8 hours. Since ofloxacin is mainly excreted by the kidneys, its pharmacokinetics changes significantly in patients with impaired renal function. Hemodialysis slightly reduces the concentration of ofloxacin in the blood serum. Ofloxacin is widely distributed in tissues and body fluids, including CSF; volume of distribution - from 1 to 2.5 l/kg. About 25% of ofloxacin is bound to plasma proteins. Ofloxacin crosses the placenta and into breast milk. Reaches high concentrations in most tissues and biological fluids of the body, including ascitic fluid, bile, saliva, bronchial secretions, gallbladder, lungs, prostate gland, bone tissue. It is mainly excreted unchanged in the urine, with 75–80% within 24–48 hours. Less than 5% of the dose is excreted in the urine as a metabolite. From 4 to 8% of the dose taken is excreted in the feces. The maximum concentration of ofloxacin in blood plasma (after intravenous administration at a dose of 200 mg for 30 minutes) is achieved almost immediately.

Indications for use

bronchitis , pneumonia ;
diseases of ENT organs ( pharyngitis , sinusitis , otitis media , laryngitis );
diseases of the kidneys and urinary tract ( pyelonephritis , urethritis , cystitis );
infections of the skin, soft tissues, bones;
endometritis , salpingitis , parametritis , oophoritis , cervicitis , colpitis , prostatitis , epididymitis , orchitis ;
gonorrhea , chlamydia ;
corneal ulcers, blepharitis , conjunctivitis , keratitis , stye , chlamydial eye lesions, prevention of infection after injuries and operations (for ointment).

Indications for use of the drug Ofloxacin

Infections caused by microorganisms sensitive to ofloxacin: genitourinary system - acute and chronic pyelonephritis, prostatitis, cystitis, epididymitis, surgical urinary tract infections, complicated or recurrent urinary tract infections, infections caused by Pseudomonas aeruginosa and other multidrug-resistant microorganisms, nosocominal urinary tract infections; respiratory tract infections - pneumonia, pleurisy, pleural empyema, infected bronchiectasis, chronic bronchitis in the acute phase, lung abscess, cystic fibrosis; infections of the ENT organs, including otitis media, sinusitis, tonsillitis, etc.; skin and soft tissue infections; sexually transmitted diseases - infections of the urethra, cervix, rectum, pharynx caused by penicillin-resistant gonococci, chlamydia and other microorganisms; pelvic organ infections; other infectious diseases - typhoid fever, salmonellosis, shigellosis, infections of the abdominal cavity and biliary tract; in the complex treatment of septicemia, endocarditis, osteomyelitis, mycobacterial infections, leprosy; prevention of infectious complications in patients with immunodeficiency or in patients with neutropenia; perioperative prevention or postoperative treatment of surgical infections. Eye ointment, eye/ear drops: bacterial corneal ulcers, conjunctivitis, blepharitis, stye, dacryocystitis, keratitis, chlamydial eye infections, external otitis of bacterial etiology.

Contraindications

age under 18 years;
increased sensitivity;
pregnancy;
breast-feeding;
epilepsy or increased convulsive readiness after traumatic brain injury, cerebrovascular accidents and other diseases of the central nervous system;
previously noted tendon damage after taking fluoroquinolones ;
peripheral neuropathy;
lactose intolerance ;
age up to 1 year (for ointment).

It is prescribed with caution for organic diseases of the brain, myasthenia gravis , severe dysfunction of the liver and kidneys, hepatic porphyria , heart failure , diabetes mellitus , myocardial infarction , paroxysmal ventricular tachycardia , bradycardia , and in old age.

Side effects

Most common adverse reactions:

nausea , loss of appetite;
vomit;
diarrhea , abdominal pain;
flatulence.

Less common and very rare adverse reactions:

transaminase activity , cholestatic jaundice ;
hepatitis , hemorrhagic colitis , pseudomembranous colitis ;
headache , dizziness ;
anxiety, irritability;
insomnia , intense dreams;
anxiety, phobias;
depression;
tremor , convulsions;
paresthesia of the limbs , peripheral neuropathy;
conjunctivitis;
tinnitus, hearing loss ;
color vision disturbance, double vision;
taste disturbances;
tendonitis , myalgia , arthralgia , pain in the extremities;
tendon rupture;
palpitations, ventricular arrhythmia , hypertension ;
dry cough , shortness of breath , bronchospasm ;
petechiae;
leukopenia , anemia , thrombocytopenia ;
renal dysfunction, dysuria , urinary retention ;
rash, itchy skin, urticaria ;
intestinal dysbiosis.

Instructions for use of Ofloxacin (Method and dosage)

Ofloxacin ointment, instructions for use

Apply 1-1.5 cm of ointment to the lower eyelid 3 times a day. In the presence of chlamydial eye lesions - 5 times a day. Treatment is carried out for no more than 2 weeks. When using several drugs simultaneously, the ointment is used last.

Ofloxacin tablets, instructions for use

The tablets are taken orally, whole, before or during meals. The dose is selected depending on the severity of the infection, liver and kidney function. The usual dose is 200-600 mg per day, divided into 2 doses. For severe infections and if the patient is overweight, the daily dose is increased to 800 mg. For gonorrhea , 400 mg is prescribed in one dose, once, in the first half of the day.

It is prescribed to children for health reasons, if there is no replacement with other means. The daily dose is 7.5 mg per kg of weight.

For patients with impaired renal function, the dosage regimen is adjusted. In patients with severe liver dysfunction, the daily dose should be no more than 400 mg. The duration of treatment is determined by the severity of the disease. Treatment is continued for another 3 days after the temperature has normalized or after laboratory tests confirming the eradication of the microorganism . Most often, the duration of treatment is 7-10 days, for salmonellosis - 7 days, for urinary tract infections - up to 5 days. Treatment should not last more than 2 months. In the treatment of certain diseases, Ofloxacin is first prescribed intravenously 2 times a day, followed by oral administration.

Drops with the active substance ofloxacin are available under the names Dancil , Floxal , Uniflox . See instructions for use of these drugs.

Instructions for use OFLOXACIN

It is not the drug of choice for pneumonia caused by pneumococci. Not indicated for the treatment of acute tonsillitis.

It is not recommended to use the drug for more than 2 months. Avoid exposure to sunlight and ultraviolet rays (mercury-quartz lamps, solarium).

In case of side effects from the central nervous system, allergic reactions, pseudomembranous colitis, discontinuation of the drug is necessary. For pseudomembranous colitis confirmed by colonoscopy and/or histology, oral administration of vancomycin and metronidazole is indicated.

It should be borne in mind that when using Ofloxacin-Borimed, rare tendinitis can lead to tendon rupture (mainly the Achilles tendon), especially in elderly patients. If symptoms of tendinitis occur, you should immediately stop treatment, immobilize the Achilles tendon and consult an orthopedist.

When using the drug, women are not recommended to use Tampax-type tampons, due to the increased risk of developing vaginal candidiasis.

During treatment, the course of myasthenia gravis may worsen and attacks of porphyria may increase in predisposed patients.

When using the drug, false negative results are possible in the bacteriological diagnosis of tuberculosis (prevents the isolation of Mycobacterium tuberculosis).

In patients with impaired liver or kidney function, monitoring of plasma concentrations of ofloxacin is necessary. In case of severe renal and hepatic insufficiency, the risk of developing toxic effects increases (dose adjustment is required).

During treatment with the drug, you should avoid drinking alcohol.

Use in pediatrics

In children, Ofloxacin-Borimed is prescribed only when there is a threat to life, taking into account the expected benefits and the potential risk of side effects, when it is impossible to use other, less toxic drugs.

Impact on the ability to drive vehicles and operate machinery

During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

The drug should be prescribed with caution in case of atherosclerosis of cerebral vessels, cerebrovascular accidents (history), chronic renal failure, QT prolongation, organic lesions of the central nervous system.

Interaction

When prescribing sucralfate , antacids and drugs containing aluminum, zinc, magnesium or iron, the absorption of ofloxacin . There is an increase in the effectiveness of indirect anticoagulants when taken with this drug. Control of the coagulation system is necessary.

The risk of neurotoxic effects and convulsive activity increases with the simultaneous administration of NSAIDs, nitroimidazole and methylxanthines .

When used with Theophylline, its clearance decreases and its half-life increases.

The simultaneous use of hypoglycemic agents may lead to hypo- or hyperglycemic states.

When used with Cyclosporine, an increase in its concentration in the blood and half-life is observed.

Probenecid , Furosemide , Cimetidine and Methotrexate reduce the tubular secretion of the active substance, which leads to an increase in its concentration in the blood plasma.

A sharp decrease in blood pressure is possible when using barbiturates and antihypertensive drugs .

When used with glucocorticosteroids, there is a risk of tendon rupture.

It is possible to prolong the QT interval when using antipsychotics, antiarrhythmic drugs, tricyclic antidepressants, macrolides, imidazole derivatives, astemizole , terfenadine , ebastine .

The use of carbonic anhydrase inhibitors, sodium bicarbonate and citrates, which alkalinize the urine, increases the risk of crystalluria and nephrotoxicity.

Ofloxacin film-coated tablets 400 mg No. 10

Release form

Due to the fact that ofloxacin is excreted mainly through the kidneys, dosage adjustment of ofloxacin is necessary in patients with renal failure.
Due to the risk of photosensitivity, exposure to sunlight and ultraviolet rays should be avoided. The appearance of diarrhea, especially severe, persistent and/or bloody diarrhea, during or after treatment with ofloxacin may be a manifestation of pseudomembranous colitis. If the development of pseudomembranous colitis is suspected, treatment with ofloxacin should be stopped immediately and appropriate specific antibacterial therapy should be prescribed without delay. In this clinical situation, drugs that suppress intestinal motility are contraindicated. Like other quinolones, ofloxacin should be administered with extreme caution to patients predisposed to the development of epileptic seizures (patients with a history of damage to the central nervous system, taking fenbufen and similar non-steroidal anti-inflammatory drugs or drugs that lower the seizure threshold, for example, theophylline).

Tendonitis, which is very rare, can sometimes lead to tendon rupture, predominantly the Achilles tendon, especially in older patients. If signs of tendonitis (inflammation of the tendon) appear, it is recommended to immediately stop treatment, immobilize the Achilles tendon and consult an orthopedic surgeon.

Some caution is warranted when taking fluoroquinolones, including ofloxacin, in patients with known risk factors for QT prolongation, such as:

-elderly age,

- uncorrectable electrolyte imbalance (for example, hypokalemia, hypomagnesemia), - congenital prolongation of the QT interval,

- diseases of the cardiovascular system (heart failure, myocardial infarction, bradycardia),

- simultaneous use of drugs that prolong the QT interval (classes IA and III antiarthmic drugs, tricyclic antidepressants, macrolides).

Ofloxacin may worsen myasthenia gravis. Possible increased frequency of porphyria attacks. During treatment with ofloxacin, false-positive results may occur when determining opiates and porphyrins in urine.

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

Ofloxacin analogs

Level 4 ATX code matches:
Siflox

Hyleflox

Leflobakt

Lefoccin

Gatifloxacin

Faktiv

Tigeron

Lebel

Zanotsin

Lomefloxacin

Eleflox

Lomflox

Pefloxacin

Tsiprobay

Sparflo

Tariwid

Zoflox

Abaktal

Moxifloxacin

Levofloxacin

Tablet preparations: Zanotsin , Zoflox , Ofloxin .

Solutions for infusions: Oflo , Tarivid , Ofloxabol .

An analogue of Ofloxacin, produced in the form of an eye ointment - Floxal , in the form of eye/ear drops - Dancil , Uniflox .

Reviews about Ofloxacin

Fluoroquinolones occupy a leading place among antimicrobial agents and are considered as an alternative to highly active antibiotics in the treatment of severe infections. Currently, the monofluorinated representative of the second generation, ofloxacin .

The advantage of this drug over other fluoroquinolones is its very high bioavailability, as well as the slowly and rarely developing resistance of microorganisms to it.

Given its high activity against STI pathogens, this drug is widely used in dermatovenerology in the treatment of STIs: urogenital chlamydia , gonorrhea , gonorrheal-chlamydial, mycoplasma and ureaplasma infections. Eradication of chlamydia is observed in 81-100% of cases and it is considered the most effective of all fluoroquinolones. This is evidenced by reviews of Ofloxacin:

“... I took this drug and treated mycoplasma and ureaplasma. Effective";
“... It helped me, I drank it for cystitis, there were no side effects. The drug is inexpensive and effective.”

A wide spectrum of action, good penetration into the tissues of the genital organs, urinary system, prostate secretions, long-term preservation of concentrations in the lesion determines its use for urological and gynecological diseases. Thus, there are reviews that taking this remedy for 3 days has shown high effectiveness for recurrent cystitis in women. It was prescribed for prophylactic purposes after diathermocoagulation of cervical erosions after the introduction of intrauterine contraceptives , after abortions , and was successfully used for prostatitis and epididymitis .

Not being an antibiotic, it does not affect the vaginal and intestinal flora and does not cause dysbacteriosis . According to patients, this drug is poorly tolerated. Most often, side effects were observed from the gastrointestinal tract, less often - from the central nervous system and skin allergic reactions, and very rarely - transient changes in liver test parameters. The drug does not have hepato-, nephro- and ototoxic effects.

“... there was nausea, my stomach was churning, there was no appetite”;
“... I felt very sick, I couldn’t eat anything, but I finished the course of treatment”;
“... After taking it, insomnia appeared. I suspect it’s from the drug, since I slept well before”;
“...felt hot and cold in a sweat, and panic appeared.”

Many patients with conjunctivitis , blepharitis and keratitis were prescribed eye drops with the active ingredient ofloxacin ( Uniflox , Floxal , Dancil ), reviews of which were positive. Patients used them 4-5 times a day for blepharitis and conjunctivitis and noted significant improvement within 2-3 days. Due to the high bioavailability of the active substance, drops can also be used for deeper lesions - uveitis , scleritis and iridocyclitis .

Use of the drug Ofloxacin

The dose depends on the type of microorganism and the severity of the infection, age, body weight and kidney function of the patient. In most cases, the course of treatment is 7-10 days, treatment must be continued for another 2-3 days after the symptoms of the infection have resolved. For severe and complicated infections, therapy can be extended. The oral dose ranges from 200 mg/day to 400 mg in 2 divided doses. A dose of 400 mg can be taken at one time, preferably in the morning. A single dose of 400 mg can be recommended for acute uncomplicated gonorrhea. A dose of 400 mg is recommended by WHO for the treatment of leprosy. Depending on the severity of the infection, adults are administered IV drips from 200 to 400 mg 2 times a day. The average duration of treatment is 7–10 days. If renal function is impaired, ofloxacin is first administered at a dose of 200 mg, then - taking into account creatinine clearance (with creatinine clearance 20-50 ml/min - 100 mg every 24 hours, with creatinine clearance less than 20 ml/min - 100 mg every 48 h). Eye/ear drops: 1–2 drops of 0.3% solution into the conjunctival sac or external auditory canal every 2–4 hours for 2 days, then 4 times a day (up to 5 days). When using the drug in the form of an eye ointment, 1.5 cm strips of ointment are placed behind the lower eyelid of the affected eye 2-3 times a day; in case of chlamydial infection - 5 times a day. A combination of eye drops and ointment is possible. When using more than one drug simultaneously, the ointment should be used last.

Ofloxacin price, where to buy

You can purchase the drug at any pharmacy. The cost depends on the manufacturer. The price of Ofloxacin in tablets of 200 mg produced in Russia (Ozon, Makiz Pharma, Sintez OJSC) ranges from 26 rubles. up to 30 rub. for 10 tablets, and the cost of tablets 400 mg No. 10 is from 53 to 59 rubles. Ofloxacin Teva, produced only in 200 mg tablets, is more expensive - 163-180 rubles. Eye ointment (Kurgan OJSC Sintez) costs from 38 to 64 rubles. in different pharmacies.

The price of Ofloxacin in Ukraine is 11-14 UAH. (tablets), 35-40 UAH. (solution for infusion).

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine
Online pharmacies in KazakhstanKazakhstan

ZdravCity

Ofloxacin tablets p.p.o.
200 mg 10 pcs. Ozone LLC 51 rub. order
Ciprofloxacin tablets p.p.o. 500 mg 10 pcs. Ozone LLC
39 RUR order
Ciprofloxacin tablets p.p.o. 500 mg 10 pcs Rapharma JSC
74 RUR order
Levofloxacin eye drops 0.5% 5 mlFGUP "Moscow Endocrine Plant"
160 rub. order
Levofloxacin tablets p.p.o. 500 mg 10 pcs Rapharma JSC
516 RUR order

Pharmacy Dialogue

Levofloxacin-Teva tablets 500 mg No. 7Teva Pharmaceutical
RUB 332 order
Ofloxacin (tablet p/o 200 mg No. 10) Teva
RUB 187 order
Levofloxacin-Teva tablets 500 mg No. 14Teva Pharmaceutical
RUR 693 order
Levofloxacin (dose solution, 5 mg/ml, container 100 ml No. 1 (ind. pack)) Kraspharma PJSC
RUB 279 order
Ciprofloxacin (tab.p.pl/vol. 500 mg No. 10) Ozone LLC
39 RUR order

Pharmacy24

Ofloxacin-Darnitsa 0.2 No. 10 tablets PrAT" Pharmaceutical company "Darnitsa", Ukraine
19 UAH. order
Ofloxacin 0.2 g No. 10 tablets AT "Lekhim-Kharkiv", Ukraine
19 UAH order
Ofloxacin 200 mg 100 ml No. 1 solution Eurolife Healthcare Pvt. Ltd., India
45 UAH order
Ciprofloxacin 0.2% 100 ml solution
30 UAH order
Ciprofloxacin 0.25 No. 10 tablets PrAT "Technolog", Uman, Cherkasy region, Ukraine
15 UAH order

PaniPharmacy

Enrofloxacin-50 100ml Ukraine, Kharkov-Product
82 UAH order
LEVOFLOXACIN tablets Levofloxacin film-coated tablets 500 mg No. 10 Ukraine, Health LLC
145 UAH order
Ciprofloxacin infusion Ciprofloxacin infusion solution 0.2% 100ml Ukraine, Novofarm-Biosintez LLC
18 UAH order
Ciprofloxacin infusion Ciprofloxacin infusion solution 0.2% 100ml Ukraine, Yuria-Pharm LLC
37 UAH order
LEVOFLOXACIN tablets Levofloxacin film-coated tablets 500 mg No. 10 Ukraine, Tekhnolog ChAO
122 UAH order