Ofloxacin

Ofloxacin – the antimicrobic medicine of a broad spectrum of activity belonging to group of ftorkhinolon.

Form of release and structure

• Tablets, film coated: biconvex, round, a cover and a layer on cross section of almost white color (on 10 pieces in blister strip packagings, 1 packaging in a cardboard pack);
• Solution for infusions: transparent chartreuse liquid (on 100 ml in bottles of colourless or dark glass, 1 bottle in a cardboard pack);
• Oculentum of 0,3%: homogeneous substance yellow, white with a yellow shade or white color (on 5 g in tubas an aluminum, 1 tuba in a cardboard pack).

Structure of 1 tablet:

• Active ingredient: ofloxacin – 0,2 g or 0,4 g;
• Auxiliary components: cellulose microcrystallic, starch corn, talc, calcium stearate, povidone, aerosil;
• Cover: oksipropilmetiltsellyuloz (gipromelloz), titanium dioxide, talc, propylene glycol, poly(ethylene oxide) 4000 (macrogoal 4000).

Structure of 1 ml of solution:

• Active ingredient: ofloxacin – 0,002 g;
• Auxiliary components: sodium chloride, the water distilled.

Structure of 1 g of ointment:

• Active ingredient: ofloxacin – 0,003 g;
• Excipients: methylparahydroxybenzoate, пропилпарагидроксибензоат, vaseline.

Indications to use

Tablets and solution for infusions
Ofloxacin is recommended to use at infectious and inflammatory diseases of the following bodies and systems:

• Respiratory tracts (pneumonia, bronchitis);
• ENT organs (average otitis, sinusitis, laryngitis, pharyngitis);
• Skin and soft tissues;
• Skeletal system (joints and bones);
• Abdominal cavity (including digestive tract infections) and biliary tract;
• Kidneys (pyelonephritis) and urinary tract (cystitis, urethritis);
• Bodies of a small pelvis (salpingitis, oophoritis, endometritis, cervicitis, prostatitis, parametritis) and generative organs (colpitis, epididymite, orchitis).

Also drug use for treatment of a septicaemia (only solution), gonorrhoeas, clamidiosis, meningitis, and for prevention of infections at patients with disturbance of the immune status (including patients with a neutropenia).

Ointment

• Bacterial infections century, corneas and conjunctivas (bacterial ulcers and keratitis of a cornea, blepharites, blefarokonjyunktivita, conjunctivitis);
• Dacryocystitis, meibomitis (barley);
• Clamidiosis of eyes;
• Infectious complications after operative measures concerning an injury of an eye or removal of a foreign body (for prevention).

Contraindications

Absolute for all forms of release:

• Period of pregnancy and breastfeeding (lactation);
• Hypersensitivity to Ofloksatsin's components and other derivatives of a hinolon.

In addition for tablets and solution:

• Deficit glyukozo-6-fosfatdegidrogenazy;
• Reduction of the threshold of convulsive activity, including the period after a stroke, a craniocereberal injury or inflammatory diseases of the central nervous system (CNS);
• Epilepsy, including data in the anamnesis;
• Children's and teenage age up to 18 years (as growth of a skeleton is not completed yet).

In addition for ointment:

• Chronic conjunctivitis of not bacterial etiology;
• Age up to 15 years.

With care it is required to take a pill in case of atherosclerosis of vessels of a brain, disturbances of cerebral circulation (data in the anamnesis), organic lesions of TsNS, a chronic renal failure.

Route of administration and dosage

The dose and the mode of administration of drug in the form of tablets and solution for infusions are selected by individually attending physician, depending on weight of a course of an infection and its localization, and also from the general condition of the patient, sensitivity of microorganisms, and function of a liver and kidneys.

At patients with a renal failure at the clearance of creatinine (CC) of 20-50 ml/min., the single dose makes 50% from recommended (frequency rate of reception 2 times a day), or the full single dose is accepted 1 time a day. At KK <20 ml/min. the recommended dose in the first day – 0,2 g, then – on 0,1 g every other day.

Patients on haemo - and peritoneal dialysis should use 0,1 g of Ofloksatsin of 1 times a day.

In case of a liver failure the maximum daily dose – 0,4 g.

Duration of a course of therapy depends on sensitivity of the activator and a clinical picture. After disappearance of symptoms of a disease and normalization of temperature for 3 more days it is required to continue drug use.

Tablets
Pill is taken inside, entirely, before meal or during food, washing down with water.

The recommended dosing mode for adults – on 0,2-0,8 g the day divided into 2 receptions. A course of treatment – 7-10 days. It is possible to appoint a daily dose to 0,4 g in 1 reception, it is desirable in the morning.

In case of acute gonorrhea a pill is taken once in a dose of 0,4 g.

Therapy course duration: salmonelloses – 7-8 days, uncomplicated infections of the lower urinary tract – 3-5 days.

Solution for infusions
The drug is administered intravenously kapelno.

Begin therapy by Ofloksatsin with drop intravenous administration of 0,2 g within 30-60 min. In case of improvement of a condition of the patient transfer to administration of drug inside (tablets) with preservation of a dosage.

The recommended Ofloksatsin's doses depending on a disease and localization of an infection:

• Urinary tract – on 0,1 g 1-2 times a day;
• Kidneys and generative organs – on 0,1-0,2 g divided into 2 injections a day;
• Airways, ENT organs, skin and soft tissues, bones and joints, abdominal cavity, and also septic infections – on 0,2 g divided into 2 injections a day; increase in a daily dose in case of need to 0,4 g with preservation of frequency rate of reception is allowed;
• Prevention of infection at patients with the expressed decrease in immunity – on 0,4-0,6 g a day.

Ointment
Ofloxacin ointment is applied locally in ophthalmology.

It is necessary to delay carefully from top to bottom a lower eyelid of the affected eye and to enter a strip of ointment about 1 cm long into a conjunctival sac (having slightly squeezed a tube). Further to release an eyelid, to close an eye and for hypodispersion of ointment to move an eyeglobe.

The recommended dosing mode: 2-3 times a day for an eyelid put a strip of ointment 1 cm long – 0,00012 g of Ofloksatsin. For treatment of clamidiosis of eyes the number of uses increase up to 5-6 times a day.

Duration of a course of therapy should not exceed 2 weeks, for treatment of chlamydial infections the course needs to be prolonged up to 4-5 weeks.

Side effects

Tablets, solution for infusions

• Alimentary system: nausea, vomiting, a meteorism, diarrhea, anorexia, cholestatic jaundice, abdominal pains (including a gastralgia), a hyperbilirubinemia, increase in activity of hepatic transaminases, a pseudomembranous coloenteritis;
• TsNS: dizziness, headache, uncertainty of movements, spasms, tremor, numbness and paresthesias of extremities, dreadful dreams, intensive dreams, psychotic reactions, hypererethism, uneasiness, phobias, confusion of consciousness, depression, hallucinations, disturbance of color perception, increase in intracranial pressure, diplopia, disturbances of taste, hearing, sense of smell and balance;
• Musculoskeletal system: arthralgias, a tendinitis, tendosinovit, mialgiya, a rupture of a sinew;
• Cardiovascular system: collapse, vasculitis, tachycardia; for solution – a lowering of arterial pressure (ABP) (at sharp decrease in the ABP introduction is stopped);
• Integuments: petechias (dot hemorrhages), dermatitis violent hemorrhagic, vasculitis, papular rash;
• Bodies of a hemopoiesis: agranulocytosis, leukopenia, anemia, pancytopenia, thrombocytopenia, aplastic and hemolitic anemia;
• Urinary system: giperkreatininemiya, disturbance of work of kidneys, acute intersticial nephrite, increase in content of urea;
• Hypersensitivity reactions: itch, skin rash, small tortoiseshell, allergic nephrite, allergic pneumonitis, eosinophilia, Quincke's edema, fever, bronchospasm, Lyell's disease, Stephens-Johnson's syndrome, photosensitization, multiformny erythema; seldom – an anaphylaxis;
• Another: a vaginitis, superinfection, dysbacteriosis, a hypoglycemia (at patients with a diabetes mellitus);
• Local reactions (only for solution): reddening and pain in the place of an injection, thrombophlebitis.

Ointment
Local reactions: a burning sensation and discomfort in eyes, a hyperemia, an itch and dryness of a conjunctiva, a photophobia, dacryagogue, allergic reactions (in most cases these symptoms short).

Special instructions

Tablets and solution for infusions
Ofloxacin at the pneumonia caused by pneumococci is not choice drug; also it is not recommended for therapy of acute tonsillitis.

It is not necessary to use drug a course lasting more than 2 months. During therapy it is necessary to avoid influence of ultraviolet radiation, both a natural sunlight, and artificial radiation by mercury-quartz lamps and/or in a sunbed.

At emergence of side reactions from TsNS, allergic answers, pseudomembranous colitis drug needs to be cancelled. In case of the pseudomembranous colitis confirmed with kolonoskopichesky and/or histologic researches reception of Vancomycinum and metronidazole orally is recommended.

Because of the increased risk of development of vaginal candidiasis during therapy by Ofloksatsin women should not use hygienic tampons.

The tendinitis arising in rare instances can become the reason of a rupture of sinews (preferential an akhillova), especially at patients of advanced age. At the first signs of a tendinitis it is required to stop immediately therapy, to carry out an immobilization of an Achilles tendon and to address for consultation the orthopedist.

Against the background of Ofloksatsin's use the complication of a current of a myasthenia is possible, patients with predisposition have an increase of attacks of a porphyria.

As Ofloxacin interferes with Mycobacterium tuberculosis allocation, during bacteriological diagnosis of tuberculosis false-negative results are possible.

Patients with renal failures or a liver need to control Ofloksatsin's concentration in plasma. In case of a heavy liver and renal failure the risk of development of toxic reactions therefore the dose decline is necessary increases.

It is recommended to avoid reception of ethanol (alcoholic beverages) during therapy.

In pediatrics drug is used only for treatment of life-threatening heavy infections with a condition of excess of estimated clinical performance over potential risk of development of side effects when use of less toxic drugs is impossible. In that case the daily dose for children is defined depending on body weight: average – 0,0075 g/kg, maximum – 0,015 g/kg.

During therapy it is necessary to refrain from occupations potentially dangerous types of activity demanding speed of psychomotor reactions and the increased concentration of attention including from control of motor transport.

Ointment
At use of ointment carrying soft contact lenses is not recommended.

It is necessary to wear sunglasses (as development of photophobia is possible) and to avoid long effect of bright light.

Ointment Ofloxacin cannot be entered into an anterior chamber of an eye or subkonjyunktivalno.

Right after use of ointment disturbance of clearness of visual perception is possible, it can complicate process of driving of motor transport and work with difficult mechanisms. Between the beginning of such activity and use of an oculentum it is recommended to sustain an interval 15 min.

Medicinal interaction

Tablets and solution for infusions

• Antacids (foodstuff), calciferous, magnesium, aluminum, iron salts – reduce Ofloksatsin's absorption, forming insoluble complexes (not less than 2 hours between their use are required to observe an interval);
• Theophylline – Ofloxacin reduces its clearance by 25% (reduction of a dose of theophylline is recommended);
• Cimetidinum, methotrexate, furosemide and drugs blocking canalicular secretion – increase Ofloksatsin's concentration in plasma;
• Glibenclamide – Ofloxacin increases its concentration in plasma;
• Indirect anticoagulants antagonists of vitamin K – control of system of a blood coagulation is required;
• The non-steroidal anti-inflammatory drugs (NPVS) derivative of a nitroimidazole and methylxanthines – the probability of development of neurotoxic side effects increases;
• Glucocorticosteroids (GKS) – the risk of a rupture of sinews, especially at advanced age increases;
• The drugs alkalizing urine (citrates, inhibitors of a karboangidraza, sodium bicarbonate) – increase risk of development of nephrotoxic effects, crystallurias.

Solution for infusions Ofloxacin is compatible from 5% fructose solution, isotonic NaCl solution, Ringer's solution, 5% solution of a dextrose (glucose).

Ointment
In case of need simultaneous use of ointment Ofloxacin with other eye ointments / drops it is necessary to observe an interval between their use not less than 15 min., the last into a conjunctival sac enters Ofloxacin.

Terms and storage conditions

It is necessary to store Ofloxacin in the place unavailable to children. Tablets – without access of light and moisture at a temperature up to 25 °C. Solution – without light access, at a temperature of 15-25 °C not to freeze. Ointment – at a temperature from 15-25 °C.

Period of validity:

• Tablets, solution for infusions – 2 years;
• Ointment – 3 years.