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

Active substanceGatifloxacinGatifloxacin

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Gatispan

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Zarquin

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FARMASINTEZ, JSC (Irkutsk) Russia

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Dosage form: & nbspfilm coated tablets

Composition:

Tablets 200 mg

Active substance: gatifloxacin 200 mg.

ExcipientsCalcium hydrogen phosphate, corn starch ,, carmellose, colloidal silica, polyvinylpyrrolidone, magnesium stearate, talc, sodium lauryl sulfate, hydroxypropylmethyl cellulose, ethylcellulose, PEG 6000, propylene glycol, titanium dioxide, yellow iron oxide colorant.

Tablets 400 mg

Active substance: gatifloxacin 400 mg.

ExcipientsCalcium hydrogen phosphate, corn starch, carmellose, colloidal silica, polyvinylpyrrolidone, magnesium stearate, talc, sodium lauryl sulfate, hydroxypropylmethyl cellulose, ethylcellulose, PEG 6000, propylene glycol, titanium dioxide.

Description:

Tablets 200 mg: oval pills of light yellow color, convex form on both sides, covered with a film membrane with an impression PPL one side.

Tablets 400 mg: oval tablets of white color, convex form on both sides, film-coated with impression PPL one side.

Pharmacotherapeutic group:Antimicrobial agent - fluoroquinolone

ATX: & nbsp

J.01.M.A.16 Gatifloxacin

S.01.A.E.06 Gatifloxacin

Pharmacodynamics:

Gatifloxacin acts bactericidal, affecting the replication of bacterial DNA (the target are topoisomers II and IV, which change the spatial configuration of the DNA molecule at various stages of its replication). Interacting with topoisomerase IV, causes the rupture of the DNA molecule after replication. It is active against many strains of microorganisms both in conditions in vitro, and in vivo. Gatifloxacin Active against gram-negative aerobic bacteria: Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella oxytoca, Klebsiella pneumoniae, Moraxella catarrhalis, Neisseria gonorrhoeae, Proteus mirabilis, Acinetobacter lwoffii, Citrobacter koseri, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Morganella morganii, Proteus vulgaris, Salmonella spp., Shigella spp .; at respect Gram-positive aerobic bacteria: Staphylococcus aureus, Staphylococcus saprophyticus, Streptococcus pneumoniae, Streptococcus pyogenes; for anaerobic bacteria: Peptostreptococcus spp., Bacteroides spp., Clostridium spp., Prevotella spp., Peptococcus spp., as well as in relation to Chlamydia pneumoniae, Legionella pneumoniae, Mycoplasma pneumoniae.

Pharmacokinetics:

Gatifloxacin is well absorbed from the gastrointestinal tract, food intake does not affect the absorption of the drug. Bioavailability is 96%. After ingestion of a single dose of 400 mg, the maximum concentration in the plasma is achieved through 1-2 hours and is 4.2 mg / l. Constant concentration in the plasma is achieved on the third day of treatment.The median sustained peak and lowest plasma concentrations of 400 mg once a day are approximately 4.2 mg / ml and 0.4 mg / ml, respectively. The binding of gatifloxacin to plasma proteins is approximately 20% and is independent of the concentration of the drug. Due to the low association with proteins, the concentration of gatifloxacin in saliva is approximately equal to the concentration in the plasma. The average volume of gatifloxacin distribution ranges from 1.5 to 2.0 l / kg. Gatifloxacin well penetrates into many tissues and body fluids (including alveolar and pulmonary tissue, genital organs, saliva).

Gatifloxacin in humans undergoes limited biotransformation, less than 1% of the accepted dose is excreted by the kidneys in the form of metabolites - ethylenediamine and methylethylenediamine.

More than 70% of the dose after ingestion is excreted within 48 hours in an unchanged form by the kidneys and 5% through the gastrointestinal tract. The half-life of gatifloxacin ranges from 7 to 14 hours and is independent of the dose and route of administration of the drug. Kidney clearance is independent of the dose, the average value is from 124 to 161 ml / min.

Pharmacokinetics in special clinical cases

With a moderate violation of liver function, dose adjustment is not required. However, given that gatifloxacin is mainly excreted by the kidneys, patients with creatinine clearance less than 40 ml / min, as well as patients on hemodialysis or permanent peritoneal ambulatory dialysis, require a reduction dose. Information on how the pharmacokinetics of gatifloxacin in severe liver damage are absent.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to the preparation:

- exacerbation of chronic bronchitis;

- community acquired pneumonia.

Contraindications:

- Pincreased sensitivity to gatifloxacin, other members of the quinolone class, or other components of the drug;

- diabetes;

- interval lengthening QT;

- simultaneous reception of antiarrhythmic drugs class IA (incl. quinidine, procainamide) or class III (including, amiodarone, sotalol);

- uncontrolled hypokalemia;

- children and adolescence (up to 18 years);

- pregnancy;

- lactation period.

Carefully:

- In diseases of the central nervous system (pronounced atherosclerosis of cerebral vessels, cerebral circulation disorders, epilepsy), predisposing to the occurrence of convulsive seizures and lowering the threshold of convulsive readiness;

- elderly patients;

- at the conditions predisposing to an arrhythmia (including a bradycardia, an acute ischemia of a myocardium),

- in patients taking antipsychotic drugs, tricyclic antidepressants, as well as drugs that can lengthen the interval QT (including cisapride, erythromycin), t. an additive effect is possible, and relevant pharmacokinetic studies have not been carried out to date;

- with renal insufficiency (creatinine clearance <40 ml / min).

Dosing and Administration:

Inside, 400 mg once a day, regardless of food intake.

The course of treatment is 7-10 days.

The maximum single dose: 400 mg. The maximum daily dose: 400 mg.

For patients with impaired renal function, dosage adjustment is necessary.

With the clearance of creatinine to 40 ml / min - the initial dose is 400 mg. Subsequent doses, starting from the second day of treatment - 400 mg daily.

When the creatinine clearance is <40 ml / min, the initial dose is 400 mg for patients on hemodialysis, permanent ambulatory peritoneal dialysis.Subsequent doses, starting from the second day of treatment, are 200 mg daily.

In patients on hemodialysis, the drug is taken after the completion of the procedure for hemodialysis.

Side effects:

Most often (more than 3%) there are: nausea, diarrhea, headache, dizziness, vaginitis.

With a frequency of 0.1-3%:

from the nervous system: excitation, anxiety, paresthesia, insomnia, drowsiness, tremor, anxiety, excitement.

From the skin: dry skin, rash, itching.

From the urinary system: painful urination.

From the side of the musculoskeletal system: the risk of tendonitis or rupture of the tendon increases, arthralgia.

From the digestive system: anorexia, dyspepsia, abdominal pain, gastritis, flatulence, constipation, glossitis, stomatitis, tongue ulcers, candidiasis.

From the respiratory system: shortness of breath, pharyngitis.

From the sense organs: impaired vision, perversion of taste, ringing in the ears.

Co cardiovascular system: increase of arterial pressure, heart palpitations.

Allergic reactions: urticaria, angioedema, itching, bronchospasm, Stevens-Johnson syndrome, anaphylactic shock.

Other: chills, fever, swelling of the face and extremities, sweating, asthenia, back pain, breast, hypo- or hyperglycemia.

With a frequency of less than 0.1%:

from the nervous system: ataxia, convulsions, depersonalization, depression, hallucinations, hostility, hyperesthesia, migraine, euphoria, attacks of fear.

From the skin: maculopapular rash, vesicular rash.

From the genitourinary system: hematuria, metrorrhagia.

From the side of the musculoskeletal system: arthritis, ossalgia, myalgia, myasthenia gravis.

From the digestive system: dysphagia, gingivitis, bad breath, swelling of the tongue, colitis (including pseudomembranous), gastrointestinal bleeding (including rectal).

From the respiratory system: bronchospasm, hyperventilation.

From the sense organs: parosmia, ptosis, taste disorders (including its loss), pain in the ears, eyes, photophobia.

From the side of the cardiovascular system: bradycardia, enhancement arterial pressure, retrosternal pain.

From the endocrine system: hypoglycemia, hyperglycemia, diabetes mellitus.

Laboratory indicators: neutropenia, increased levels alanine, asparagintransferazy, alkaline phosphatase, amylase, hyperbilirubinemia, electrolyte disturbances.

Other: etdaola intolerance, cyanosis, lymphadenopathy, pain in the neck.

Overdose:

Symptoms: nausea, vomiting, diarrhea; in more severe cases - tachypnea, tremor, convulsions, agitation.

Treatment: gastric lavage (the first two hours after poisoning), observation, symptomatic therapy with ECG monitoring. There is no specific antidote. It is necessary to ensure a sufficient supply of fluid in the body while maintaining the appropriate diuresis. With hemodialysis and peritoneal dialysis is withdrawn slightly.

Interaction:

With the simultaneous use of gatifloxacin and:

- antiarrhythmic drugs (including quinidine, procainamide, amiodarone, sotalol), tricyclic antidepressants (including amitriptyline, imipramine, nortriptyline, doxepin, amoxapine), phenothiazine derivatives (including chlorpromazine, fluphenazine, perphenazine , mesoridazine, thioridazine), erythromycin, cisapride increases the risk of cardiac arrhythmias;

- Glibenclamide or insulin increases the risk of hypo- or hyperglycemia;

- warfarin changes in the pharmacokinetics of both drugs are not observed, prothrombin time does not change. However, due to the fact that some quinolones increase the effect of warfarin and similar agents, control of prothrombin time is required;

- digoxin showed no significant changes in the pharmacokinetics of gatifloxacin, but in some patients there was an increase in the level of digoxin concentration in the blood. It is required to control the concentration of digoxin in the blood serum and, if necessary, dose adjustment of digoxin;

- probenicida systemic exposure of gatifloxacin may be increased;

- cimetidine, taken 1 hour before taking gatifloxacin, there was no change in the pharmacokinetics of the latter.

Preparations containing ions of zinc, magnesium, iron and aluminum, didanosine reduce the effectiveness of gatifloxacin (should be taken at an interval of 4 hours).

With the simultaneous use of quinolones and theophylline, it is possible to increase the concentration of theophylline in the blood plasma and increase the risk of developing toxic effects associated with theophylline.

With the simultaneous administration of quinolones and cyclosporine, the nephrotoxic effect of cyclosporin can be enhanced.

With simultaneous use of quinolones and non-steroidal anti-inflammatory drugs, the risk of side effects from the central nervous system, including convulsions, may increase.

When combined quinolones with other antimicrobial agents (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergy is usually observed.

Special instructions:

Gatifloxacin can cause neurological side effects, so people on treatment with the drug should not drive motor vehicles or other mechanisms that require increased attention and coordination.

It is necessary to monitor the concentration of glucose in the blood plasma, especially in patients with risk factors for diabetes mellitus, chronic renal failure, in elderly patients, while taking with hypoglycemic drugs.

During the period of treatment, ECG monitoring is required (lengthening of the interval QT, ventricular arrhythmias). Degree of lengthening interval QT may increase with increasing drug concentration, therefore, do not exceed the recommended dose. Interval lengthening QT is associated with an increased risk of ventricular arrhythmias, including flicker-flutter.

Against the background of therapy with fluoroquinolones, including gatifloxacin, especially in elderly patients receiving glucocorticosteroids, tendonitis and tendon rupture are possible. At the first symptoms of pain or inflammation at the site of damage, taking the drug should stop and unload the affected limb.

The use of broad-spectrum antibacterial drugs is associated with a risk of developing pseudomembranous colitis. This diagnosis should be borne in mind in patients who have severe diarrhea on the background of treatment with gatifloxacin. In this case, appropriate therapy should be given immediately.

In some cases, after the first use of the drug may develop hypersensitivity and allergic reactions. Very rarely allergic reactions can progress to a life-threatening anaphylactic shock even after the first use of the drug. In these cases gatifloxacin it is necessary to cancel and carry out the necessary measures (including anti-shock).

Patients receiving the drug should avoid direct sunlight and UV radiation.

Form release / dosage:

Tablets, film-coated, 200 mg, 400 mg.

Packaging:5 tablets per blister of PVC film and aluminum foil. For 1 blister in a cardboard box with instructions for use.

Storage conditions:

Store in a dry, dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003687/09

Date of registration:15.05.2009 / 13.02.2017

Expiration Date:Unlimited

The owner of the registration certificate:FARMASINTEZ, JSC (Irkutsk) FARMASINTEZ, JSC (Irkutsk) Russia

Manufacturer: & nbsp

FARMASINTEZ, JSC (Irkutsk) Russia

Information update date: & nbsp10.10.2017

Illustrated instructions

Instructions

Zarquin (Zarquin)