Спарфло®

General characteristics. Structure:

Active agent: спарфлоксацин - 200 mg.
Excipients: starch corn, cellulose microcrystallic, кросповидон, silicon dioxide colloid, talc, magnesium stearate; cover: gipromelloza, propylene glycol, titanium dioxide, talc, dye quinoline yellow.

Description: almost white or pale yellow oval tablets, coated, on one party - risk, on another a stamping "200".

Pharmacological properties:

Pharmacodynamics. The antimicrobic means derivative of a ftorkhinolon, inhibits bacterial DNA - a giraza, despiralizuyushchy sites of chromosomal DNA.
The hypotoxicity for cells of a macroorganism is explained by absence in them гираз.
Is bactericidal antimicrobic drug of a broad spectrum of activity, as concerning gram-positive, and gram-negative flora. Advantage of drug is big activity concerning gram-positive cocci and anaerobe bacterias in comparison with ftorkhinolona of the previous generations. Concerning gram-negative flora shows the activity close to aminoglycosides.
On gram-positive microorganisms has bactericidal effect only during division, on gram-negative organisms - and during a dormant period as influences not only on DNK-girazu, but also causes a lysis of a cell wall.
Prevents a transcription of the genetic material of bacteria necessary for their normal metabolism that leads to bystry decline in the ability of bacteria to division. Its action does not result from parallel development of resistance to other antibiotics which are not belonging to group of inhibitors of a giraza that does it highly effective in relation to bacteria which are steady, for example to aminoglycosides, penicillin, cephalosporins, tetracyclines and many other antibiotics.
To a sparfloksatsin the following pathogenic microorganisms are highly sensitive: Escherichia coli, Shigella spp., Salmonella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Serratia spp., Hafnia spp., Edwardsiella spp., Proteus spp. (an indole - positive and an indole - negative), Providencia spp., Morganella spp., Yersinia spp.; Vibrio spp., Aeromonas spp., Plesiomonas spp., Pasteurella spp., Haemophilus spp., Campylobacter spp., Pseudomonas cepacia, Pseudomonas aeruginosa, Legionella spp., Neisseria spp., Moraxella spp., Acinetobacter spp., Brucella spp.; Staphylococcus spp., Streptococcus pneumoniae, Mycoplasma pneumoniae, Listeria spp., Corynebacterium spp., Chlamydia spp., Xanthomonas maltophilia.
Sparfloksatsin is characterized by high activity concerning Mycobacterium tuberculosis, including mnozhestvennorezistentny strains.
Enterococcus faecium, Ureaplasma urealyticum, Nocardia asteroides are, as a rule, sensitive to a sparfloksatsin.
The following microorganisms have moderate sensitivity: Gardnerella spp., Flavobacterium spp., Alcaligenes spp., Streptococcus agalactiae, Enterococcus faecalis, Streptococcus pyogenes, Streptococcus viridans, Mycoplasma hominis, Mycobacterium fortuitum.
Behind some exceptions, anaerobic microorganisms are moderately sensitive (Peptococcus spp., Peptostreptococcus spp.) or steady (Bacteroides spp.). Sparfloksatsin is not effective against Treponema pallidum.
Resistance to a sparfloksatsin develops extremely slowly as, on the one hand, after its action there is practically no persistent microorganism left, and on the other hand - bacterial cells have no enzymes inactivating it.
Cross resistance to other antimicrobic drugs is noted.
Concerning Pseudomonas aeruginosa and other gram-negative bacilli on activity concedes to ciprofloxacin.
Has post-antibiotic effect: microorganisms do not breed during 0,5-4 h after disappearance of drug from plasma.

Pharmacokinetics. Absorption after intake - about 90%. Extent of absorption does not change at reception drug together with food or milk. Food slows down absorption speed, however does not change extent of absorption so the maximum of concentration of a sparfloksatsin is noted about 30 min. later, than at reception on an empty stomach.

It is well distributed in body tissues (excepting the fabric rich with fats, including nervous tissue), concentration in fabrics and liquids of the lower respiratory tracts exceeds concentration in plasma. It is found in high concentration in alveolar macrophages. Therapeutic concentration are reached in saliva, bile, intestines, abdominal organs and a small pelvis, kidneys and urinary bodies, pulmonary fabric, a bronchial secret, a bone tissue, muscles, synovial fluid and joint cartilages, peritoneal liquid, skin. In cerebrospinal and intraocular fluid it is found in 10% of concentration of drug in plasma.

0,8 l/kg, ±Препарат the large volume of distribution - 3,9 exceeding this indicator for other ftorkhinolon has. Communication with proteins of a blood plasma (preferential albumine) makes about 45%.

Time of achievement of the maximum concentration after intake of 400 mg - 3-6 h, concentration in fabrics is 2-12 times higher, than in plasma. Concentration of drug in blood serum has linear dependence on size of the accepted dose.
Activity decreases at acid PH values a little.
It is metabolized in a liver, brought with a fecal masses (30-50%) and with urine (tubular filtering and canalicular secretion) - out of them, in not changed look, about 10% of orally accepted dose. The elimination half-life - 16-30 h, at patients with a renal failure an elimination half-life is extended.
At a chronic renal failure the percent of the drug removed through kidneys decreases, but at clearance of creatinine higher than 20 ml/min. of its kumulirovaniye in an organism do not occur as parallel to it there is an increase in metabolism and removal with fecal masses.

Indications to use:

Respiratory infections: pneumonia, chronic obstructive diseases of lungs in the aggravation stages caused by sensitive microorganisms;
infections of a middle ear, adnexal bosoms of a nose, especially if they are caused by gram-negative activators, including Pseudomonas spp., or Staphylococcus spp.;
infections of eyes;
infections of kidneys and urinary tract (cystitis, not gonococcal urethritis, pyelitis);
infections of generative organs (including adnexitis, prostatitis);
infections of an abdominal cavity (bacterial infections of digestive tract, including, caused by shigellas and salmonellas, bilious ways, peritonitis);
infections of skin and soft tissues (abscess, pyoderma, furunculosis, infectious dermatitis),
infections of bones and joints (including osteomyelitis);
sepsis, infections against the background of an immunodeficiency, including against the background of treatment by immunodepressive means or at patients with a neutropenia;
diseases, sexually transmitted: gonorrhea, clamidiosis;
pulmonary tuberculosis (for treatment of drug resistant tuberculosis or at intolerance of therapy of the first line);
leprosy.

Route of administration and doses:

The adult, inside, irrespective of meal (without chewing, washing down with enough liquid).
Duration of a course of treatment depends on character and disease severity and a type of the activator.
Pneumonia, exacerbation of chronic bronchitis - in the first day of 400 mg once, further on 200 mg/days within 10 days; to patients with clearance of creatinine less than 50 ml/min. - in the first day of 400 mg once, further on 200 mg each 48 h.
Infections of ENT organs, sinusitis - in the first day of 400 mg once, further on 200 mg a day within 10 days.
At a pulmonary tuberculosis it is applied as a part of complex therapy with antitubercular drugs - in the first day of 400 mg once, further on 200 mg a day within 30 days.
Infections of urinary tract: in the first day of 200 mg once, further on 100 mg once a day within 10-14 days.
Acute gonorrheal urethritis: in the first day of 400 mg once, then it is strict in 24 hours - 1 tablet (200 mg), a course dose of 600 mg.
Not gonococcal urethritis - in the first day of 200 mg once, further on 100 mg once a day within 6 days.
Bacterial prostatitis - in the first day of 400 mg once, further on 200 mg a day within 10-14 days.
Chlamydial infections - in the first day of 400 mg, further on 200 mg within 10-14 days.
Infections of skin and soft tissues - in the first day of 400 mg once, further on 200 mg once a day within 3-9 days.
Leprosy: on 200 mg once a day during 12 weeks.

Features of use:

It is necessary to avoid ultra-violet radiation during treatment sparfloksatsiny and within 3 days after its termination.
In order to avoid development of a crystalluria, exceeding of the recommended daily dose is inadmissible, sufficient consumption of liquid and maintenance of acid reaction of urine is necessary.
There are single messages that use of ftorkhinolon is followed by ruptures of sinews of a shoulder, hands and the Achilles tendon. At emergence of complaints treatment should be stopped.
During treatment sparfloksatsiny it is necessary to abstain from occupations potentially dangerous types of activity requiring special attention and speed of mental and motor reactions.

Side effects:

From cardiovascular system: lengthening of an interval of Q-T, tachycardia, thrombosis of cerebral arteries;
From the alimentary system: a loss of appetite, nausea, vomiting, dyspepsia, pain in a stomach, a meteorism, diarrhea, cholestatic jaundice (especially at patients with the postponed liver diseases), hepatitis, гепатонекроз;
From respiratory system: asthma;
From a nervous system: dizziness, a headache, increased fatigue, drowsiness, uneasiness, a tremor, a peripheral paralgeziya (anomaly of perception of feeling of pain), the increased sweating, increase in intracranial pressure, "dreadful" dreams, confusion of consciousness, a depression, hallucinations, psychotic reactions, unconscious states;
From sense bodys: disturbances of taste and sense of smell, vision disorder (for example diplopia, change of color perception), sonitus, decrease in hearing;
From an urinary system: hamaturia; a crystalluria (first of all at alkalinuria and a hypouresis);
From a musculoskeletal system: arthralgia, adynamy, mialgiya, tendovaginitis;
Allergic reactions: itch, medicinal fever, dot hemorrhages (petechias); nodal erythema, face edema, vessels or throat, multiformny exudative erythema (including Stephens-Johnson's syndrome), toxic epidermal necrolysis (Lyell's disease);
From laboratory indicators: eosinophilia, leukopenia, granulocytopenia, anemia, thrombocytopenia; leukocytosis, thrombocytosis, hemolitic anemia, increase in activity of "hepatic" transaminases and ShchF, prothrombinopenia, giperkreatininemiya, hyperbilirubinemia, hyperglycemia;
Others: a photosensitization, "inflows" of blood to the person.

Interaction with other medicines:

Practically does not influence concentration of theophylline, peroral hypoglycemic drugs, indirect anticoagulants.
Non-steroidal anti-inflammatory drugs (excepting acetylsalicylic acid) increase risk of development of spasms.

Oral administration together with ferriferous drugs, sukralfaty and the antiacid drugs containing magnesium, aluminum, calcium, zinc, and also iron salts leads to decrease in absorption of a sparfloksatsin (it it is necessary to appoint or in 1-2 hours prior to, or, not less than in 4 hours after).

Metoclopramidum accelerates absorption of a sparfloksatsin that leads to reduction of time of achievement of its maximum concentration in plasma.

As спарфлоксацин can promote increase in duration of an interval of Q-T, the concomitant use with the drugs possessing the same action is not recommended: with antiarrhytmic means of the class Ia and III, terfenadiny, bepridily, erythromycin, astemizoly, tsizapridy, pentamidine, tricyclic antidepressants and fenotiaziny.
At a combination to other antimicrobic drugs, a synergism (beta lactams, aminoglycosides, clindamycin, metronidazole) is usually observed; спарфлоксацин it can successfully be applied in a combination with azlotsilliny and a ceftazidime at the infections caused by Pseudomonas spp.; with mezlotsilliny, azlotsilliny and others beta лактамными antibiotics - at streptococcal infections; with the penicillin steady against action беталактамаз, and Vancomycinum - at staphylococcal infections; with metronidazole and clindamycin - at mephitic gangrenes.
At simultaneous use of a sparfloksatsin with cyclosporine increase in serumal creatinine therefore at such patients control of this indicator 2 times a week is necessary is noted.

Contraindications:

Hypersensitivity to drug components, epilepsy, age up to 18 years (incomplete process of formation of a skeleton), the extended interval of Q-T or other factors promoting development of arrhythmias (a hypopotassemia, the expressed bradycardia, chronic heart failure, fibrillation of auricles), deficit glyukozo-6-fosfatdegidrogenazy, a heavy renal failure; pregnancy, lactation period.
With care:
The atherosclerosis of vessels of a brain, disturbance of cerebral circulation, epileptic syndrome, living conditions (professional activity) which are not allowing to limit insolation, a chronic renal failure.

Overdose:

Treatment: the specific antidote is unknown. Symptomatic therapy, if necessary - a hemodialysis and peritoneal dialysis.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children! Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, on 200 mg. On 6 tablets in the blister, together with the Application instruction of drug place in a pack cardboard.