Ofloxacin-Teva, 200 mg 10 pcs

Pharmacotherapeutic group: antimicrobial agent – fluoroquinolone.

ATX code: JMA0101

Pharmacological properties .

Pharmacodynamics

Ofloxacin is a synthetic antibacterial drug of broad spectrum

from the group of fluoroquinolones with bactericidal action. The main

the mechanism of action of quinolones is specific inhibition of bacterial

DNA-gyrase. DNA-gyrase is essential for replication, transcription, repair and recombination of bacterial DNA. Its inhibition leads to the unwinding and destabilization of bacterial DNA and, consequently, to the death of the microbial cell.

Highly active against most gram-negative and gram-positive 2

microorganisms.

Fluoroquinolones have concentration-dependent bactericidal activity and

moderate postantibacterial action. The ratio of AUC to minimum

suppressive concentration (MCC) or the ratio of maximum concentration to

MCC is a predictive factor for successful clinical treatment.

Sensitive microorganisms

.Non-permanently susceptible microorganisms (possibly due to acquired

resistance): Citrobacter freundii, Escherichia coli, Klebsiella oxytoca, Klebsiella

pneumoniae, Neisseria gonorrhoeae, Proteus mirabilis, Pseudomonas aeruginosa, Serratia spp,

Staphylococcus spp. (coagulazonegative strains), Staphylococcus aureus (methicillin-

sensitive strains), Staphylococcus epidermidis, Campylobacter jejuni, Enterococcus

faecalis, Streptococcus pneumoniae.

Resistant microorganisms

Acinetobacter baumannii, Bacteroides spp, Clostridium difficile, Enterococci (including

Enterococcus faecium), (methicillin-

resistant strains), Nocardia spp.

Resistance

Resistance to ofloxacin develops as a result of a stepwise process of mutations

of the genes encoding both topoisomerase type II: DNA-gyraza and topoisomerase IV. Other

resistance mechanisms, such as the mechanism for influencing the permeability of the outer

structures of the microbial cell (a mechanism characteristic of Pseudomonas aeruginosa) and

the efflux mechanism (active elimination of the antimicrobial agent from the microbial

cell) can also affect the sensitivity of microorganisms to ofloxacin.

MBC limit values

The European Committee for the Susceptibility of Antibiotics (EUCAST) approved limit values (mg/L) for ofloxacin.

Microorganisms

Sensitive (mg/L)

Enterobacteriaceae .

≤0.5

>1

Staphylococcus spp.

≤1

>1

Streptococcus pneumoniae

≤0.12

>4

Haemophilus influenzae

≤0.5

>0.5

Moraxella catarrhalis

≤0.5

>0.53

Neisseria gonorrhoeae

≤0.12

>0.25

/p>

Borderline MPC values,

not associated with a specific

microbial species

≤0.5

>1

Pharmacokinetics

After oral administration, ofloxacin is rapidly and almost completely absorbed from the

gastrointestinal tract. Bioavailability is almost 100%.

The maximum plasma concentration of ofloxacin after a single dose of 200

mg is 2.5-3 mcg/ml and is reached after 1 hour. Binding to plasma proteins

is 25%. The volume of distribution is approximately 120 liters. Less than 5% of Ofloxacin

is biotransformed.

It is excreted mainly by the kidneys (80-90% of the dose is unchanged). Two main metabolites are detected in the urine: N-desmethylofloxacin and ofloxacin

N-oxide. About 4% ofloxacin is excreted with the bile as glucuronides. The elimination half-life is 6-7 hours. Concentrations ofloxacin in the urine and in

infected urinary tract exceed concentrations ofloxacin in serum

blood by 5-100 times.

Special patient groups

Elderly patients

. Elderly patients have an increased half-life, but

the maximum concentration does not change.

Renal failure

In renal failure, the half-life is prolonged; total and renal

clearance decrease in proportion to the decrease in creatinine clearance.

Indications

Treatment of infection and inflammatory diseases caused by microorganisms sensitive to
ofloxacin:
Pyelonephritis and complicated urinary tract infections; prostatitis, epididymitis, orchitis;
pelvic organ infections (as part of combined therapy);
For treatment of the following infectious and inflammatory diseases, ofloxacin may
be used only as an alternative to other antimicrobial agents: skin and soft tissue infections;
cystitis, uncomplicated urinary tract infections;
4 bone and joint infections;
acute sinusitis;
exacerbation of chronic bronchitis, community-acquired pneumonia;
prophylaxis of infections caused by microorganisms sensitive to Ofloxacin
in patients with significant decrease of immune status
(for example, in neutropenia).
When using the drug Ofloxacin-Teva the official
national recommendations on the proper use of antibacterial
drugs, as well as the sensitivity of pathogenic microorganisms in a particular
region should be considered.

Active ingredient

Composition

How to take, the dosage

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

Adults with normal renal function (creatinine clearance greater than 50 ml/min)

The drug is indicated in a daily dose of 400 mg divided into 2 doses (every 12 hours).

The daily dose can be increased to 600-800 mg in severe infections or when treating overweight patients.

In uncomplicated lower urinary tract infections, the drug is prescribed in a dose of 200 mg daily for 3-5 days.

In gonorrhea, 400 mg is prescribed once.

The daily dose of up to 400 mg may be prescribed in 1 dose, preferably in the morning. A daily dose of more than 400 mg should be divided into 2 doses at regular intervals.

The tablets should be swallowed whole with plenty of water.

The drug can be taken both before and with meals. Concomitant use with antacids should be avoided.

Special patient groups

.Elderly patients

Patients’ age does not require dose adjustment of ofloxacin. However, when using the drug in elderly patients, special attention should be paid to renal function because if it declines, the dosing regimen may need to be adjusted accordingly.

Patients with hepatic impairment

The daily dose of Ofloxacin 400 mg should not be exceeded in patients with hepatic impairment.

Patients with impaired renal function

The following dosing regimen is recommended for impaired renal function depending on creatinine clearance:

Creatinine clearance

Strong>Dose

(mg)*

frequency of administration

50-20 ml/min

100-200

1 time per day (every 24 h)

p> < 20 mL/min**

or hemodialysis

and peritoneal dialysis

100

or

200/p>

once a day (every 24 hours)

or

once every 2 days (every 48 hours)

* As indicated.

** It is recommended that serum concentrations of ofloxacin be monitored in patients

with severe renal impairment or in patients on dialysis.

In cases where creatinine clearance (CK) cannot be determined, it can be

calculated from serum creatinine concentration using the Cockroft formula

for adults:

for men:

CK (ml/min) =

Body weight (kg) x (140 – age in years)

/p>

72 x serum creatinine (mg/dL)

or

CK (ml/min) =

Body weight (kg) x (140 – age in years)

0.814 x serum creatinine (μmol/L)

for women:

CK (ml/min) = 0.85 x index in men. Treatment duration

The duration of treatment depends on the severity of the disease. Like any treatment with antimicrobials, treatment with ofloxacin should be continued for at least 48-72 hours after normalization of body temperature or when there is confirmation of eradication of the pathogen.

Interaction

With antacids containing aluminum hydroxide, sucralfate, magnesium hydroxide, aluminum phosphate, or preparations containing zinc, iron

Special Instructions

Loss of function (disability) and potential irreversible seriousadverse reactions due to fluoroquinolones

The use of fluoroquinolones has been associated with loss of function (disability) and potentially irreversible seriousadverse reactions due to fluoroquinolones. The use of fluoroquinolones, including ofloxacin, has been associated with disability and the development of irreversible serious adverse reactions from various body systems that may develop simultaneously in the same patient. Fluoroquinolone-induced adverse reactions include tendonitis, tendon rupture, arthralgia, myalgia, peripheral neuropathy, and nervous system side effects (hallucinations, anxiety, depression, insomnia, headaches, and confusion). These reactions may develop within a few hours to a few weeks after the start of therapy with Ofloxacin. The development of these adverse reactions has been reported in patients of any age or without previous risk factors. If the first signs or symptoms of any serious adverse reactions occur, the use of of ofloxacin should be stopped immediately. The use of fluoroquinolones, including ofloxacin, should be avoided in patients who have had any of these serious adverse reactions.

Renal failure

Because of the fact that ofloxacin is mainly excreted by the kidneys, a dose adjustment of ofloxacin is necessary in patients with renal failure (see “Caution” and “Dosage and administration” sections).

Prevention of photosensitization

According to the risk of photosensitization during treatment with ofloxacin, exposure to bright sunlight and ultraviolet rays should be avoided.

Secondary infection

As with other antimicrobial agents, if used, especially long-term, ofloxacin may lead to secondary infection associated with the growth of

Contraindications

Hypersensitivity to ofloxacin, other quinolones or excipients of the drug.

Epilepsy.

Pseudoparalytic myasthenia gravis (myasthenia gravis) (see sections “Side effects” and “Precautions”).

Tendon lesions with a history of fluoroquinolones.

Childhood and adolescence before 18 years of age (the risk of cartilage bone growth zone lesions in a child cannot be completely excluded).

Pregnancy (the risk of cartilage growth zones in the fetus cannot be completely excluded).

The period of breastfeeding (the risk of damage to the cartilage growth zones of the baby cannot be completely excluded).

Hereditary lactose intolerance, lactase deficiency, glucose-galactose

malabsorption (due to the presence of lactose in the composition).

With caution

In patients who are prone to developing seizures (in patients with

Preexisting central nervous system (CNS) lesions, such as

serious cerebral atherosclerosis, impaired cerebral

a history of circulatory disorders, organic CNS lesions, a history of traumatic brain injury; patients concomitantly receiving drugs that lower the seizure threshold, such as phenbufen or other non-steroidal anti-inflammatory drugs, theophylline).

In patients with latent or manifest glucose-6-5 deficiency

Phosphate dehydrogenase (increased risk of hemolytic reactions when treated with

quinolones).

In patients with impaired renal function (mandatory monitoring of renal function is required as well as dosage adjustment, see section “How to use and doses”).

In patients with hepatic impairment (monitor liver function parameters).

In patients with porphyria (risk of exacerbation of porphyria).

In patients with risk factors for QT interval prolongation: In elderly patients; in unadjusted electrolyte disorders (hypokalemia,

hypomagnesemia); in congenital QT interval prolongation syndrome; in

heart disease (heart failure, myocardial infarction,

bradycardia); in concomitant administration of drugs capable of prolonging the QT (antiarrhythmic drugs of classes IA and III, tricyclic

antidepressants, macrolides, neuroleptics).

In patients with diabetes mellitus receiving oral hypoglycemic agents (e.g., glibenclamide) or insulin (increased risk of hypoglycemia).

In patients with severe adverse reactions to other quinolones, such as severe neurological reactions (increased risk of similar adverse reactions with

loxacin).

In patients with a history of psychosis and other psychiatric disorders.

In elderly patients.

In patients after transplantation and with concomitant use of glucocorticosteroids (increased risk of tendinitis and tendon rupture – see “Special Precautions”).

In patients with a family history of aortic aneurysm, or in patients with

diagnosed aortic aneurysm and/or aortic dissection or with other risk factors or conditions predisposing to the development of an aneurysm

/p>

Aortic aneurysm or aortic dissection (e.g., Marfan syndrome, Ehlers-

Danlos vascular syndrome, Takayasu arteritis, giant cell arteritis,

Behçet disease, arterial hypertension, atherosclerosis) (see “Indications. See section “Special Indications”).

Side effects

The information below is based on data from clinical studies and extensive post-registration experience with the drug.

The side effects listed below are presented according to the following frequency gradations: Very common (≥1/10); common (≥1/100, < 1/10); infrequent (≥1/1000, < 1/100); rare (≥1/10000, < 1/1000); very rare (< 1/10000) (including individual reports); frequency unknown (the incidence cannot be determined from available data).

Cardiac disorders

Infrequent: sensation of palpitations. Rarely: tachycardia. Frequency unknown: QT interval prolongation, pirouette-type ventricular arrhythmia (especially in patients with risk factors for QT interval prolongation).

vascular disorders

Rarely: increased blood pressure, decreased blood pressure.

Disorders of the blood and lymphatic system

Very rare:

anemia, hemolytic anemia, leukopenia, eosinophilia,

thrombocytopenia. Frequency unknown: agranulocytosis, pancytopenia, inhibition of bone

cerebral hematopoiesis.

Nervous system disorders

Infrequent: dizziness, headache. Rarely: somnia, paresthesia, dysgeusia

(taste perception disorder), parosmia (odor perception disorder). Very

frequent: peripheral sensory neuropathy, peripheral sensory-motor

neuropathy, seizures, extrapyramidal symptoms, including tremor and other disorders of muscle coordination. Frequency unknown: Ageusia, increased intracranial pressure (benign intracranial hypertension, pseudotumor of the brain).

Mental disorders

Infrequent: anxiety, sleep disorders, insomnia. Rarely: psychotic disorders

(such as hallucinations), anxiety, nervousness, confusion, nightmares,

depression. Frequency unknown: psychotic disorders and depression with self-harm, in rare cases up to suicidal thoughts or attempts, memory and attention disorders, disorientation, delirium.

Visual disorders

Infrequent: irritation of the mucous membrane of the eye, conjunctivitis. Rarely: disorders

of vision (diplopia, impaired color perception). Frequency unknown: uveitis.

Hearing organ and labyrinth disorders

Infrequent: vertigo. Very rare: disorders of hearing (tinnitus), hearing loss.

Disorders of the respiratory system, thoracic and mediastinal organs

Infrequent: cough, nasopharyngitis. Rarely: dyspnea, bronchospasm. Frequency unknown:

allergic pneumonitis, marked shortness of breath.

Disorders of the digestive system

Infrequent: abdominal pain, diarrhea, nausea, vomiting, decreased appetite. Rarely: enterocolitis

(sometimes hemorrhagic). Very rare: pseudomembranous colitis. Frequency

unknown: dyspepsia, constipation, flatulence, pancreatitis, stomatitis.

Liver and biliary tract disorders 9

Rarely:

increased activity of “hepatic” enzymes such as

alanine aminotransferase (ALT), aspartate aminotransferase (ACT), lactate dehydrogenase

(LDH), gamma-glutamyltransferase (GGT) and/or alkaline phosphatase (ALP) and/or

blood bilirubin concentrations. Very rare: cholestatic jaundice. Frequency

unknown: hepatitis, which can be severe; cases of severe hepatic failure, including acute liver failure, sometimes fatal, have been reported when using ofloxacin

(mostly in patients with impaired liver function).

Renal and urinary tract disorders

Rarely: increased serum creatinine concentration. Very rare: acute

renal failure. Frequency unknown: acute interstitial nephritis,

increased blood urea concentration.

Skin and subcutaneous tissue disorders

Infrequent: rash, rash. Rarely: crash, hyperhidrosis, pustular rash, “rushes” of blood

to the skin. Very rare: Multiform exudative erythema, toxic

epidermal necrolysis, photosensitization reactions, drug rash, vascular

purpura, vasculitis, which in exceptional cases may lead to cutaneous

necrosis. Frequency unknown: Stevens-Johnson syndrome, acute generalized

exanthematous pustulosis, exfoliative dermatitis.

Musculoskeletal and connective tissue disorders

Rarely: tendinitis. Very rare: arthralgia, myalgia, tendon rupture (e.g.,

the Achilles tendon) (as with other fluoroquinolones, this side effect

can develop within 48 hours of starting treatment and may be bilateral).

Frequency is unknown: rhabdomyolysis and/or myopathy, muscle weakness, which is especially important in patients with pseudoparalytic myasthenia gravis (myasthenia gravis), muscle tears,

muscle tears, ligament tears, arthritis.

Disorders of metabolism and nutrition

Rarely: anorexia. Frequency unknown: hyperglycemia, severe hypoglycemia, up to the development of hypoglycemic coma, especially in elderly patients, in patients with

diabetes receiving oral hypoglycemic drugs or

insulin).

Infectious and parasitic diseases

Infrequent: fungal infections, resistance of pathogens.

Immune system disorders

Rarely: anaphylactic reactions, anaphylactoid reactions, angioedema.

very rare: anaphylactic shock, anaphylactoid shock.

Congenital, .Hereditary and genetic disorders

Frequency is unknown: acute porphyria in patients with porphyria.

General disorders and disorders at the site of administration

Frequency unknown: sthenia, increased body temperature, back, chest, limb pain.

Overdose

Symptoms. The most important symptoms of overdose are CNS symptoms (such as dizziness, confusion, loss of consciousness, seizures), prolonged QT interval, and gastrointestinal reactions (such as nausea and erosions of the gastrointestinal mucosa).

Treatment. In case of overdose, gastric lavage and symptomatic therapy are recommended. Antacids may be used to protect the gastric mucosa. ECG should be monitored, because the QT interval may be prolonged. Ofloxacin fractions can be removed from the body by hemodialysis. There is no specific antidote.

Pregnancy use

Pregnancy

Ofloxacin should not be used during pregnancy (see section “Contraindications”).

The period of breastfeeding

Since ofloxacin is excreted into breast milk, due to the risks to the baby,

women who are breastfeeding should not take ofloxacin or, if

it is necessary, discontinue breastfeeding.

Similarities