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Article about Zagam

Description of the dosage form

The tablets are coated with an almost white or light yellow, oval shell with a notch on one side and an embossed "200" on the other.

Pharmacological action

Broad spectrum antimicrobial bactericidal drug from the fluoroquinolone group. Inhibits bacterial DNA gyrase, inhibiting the replication of bacterial DNA. It has a bactericidal effect on gram-positive microorganisms only during the division period, on gram-negative microorganisms - during the division period and at rest, because not only affects DNA gyrase, but also causes lysis of the cell wall. The drug prevents the transcription of the bacteria's genetic material necessary for their normal metabolism, which results in a rapid decrease in the bacteria's ability to divide. Due to the action of the drug, there is no development of cross-resistance to other antibiotics that do not belong to the group of DNA gyrase inhibitors, which makes it very active against resistant bacteria aminoglycosides, penicillins, cephalosporins, tetracyclines.

Low toxicity to macro-organisms due to the absence of gyrase in them. Zagam is active against gram-positive and gram-negative bacteria. The advantage of the drug is a more pronounced activity against cocci and Gram-positive anaerobes compared to fluoroquinolones of previous generations. Regarding gram-negative bacteria, it has an activity similar to aminoglycosides.

Are resistant to the drug. Zagam is not active against Treponema pallidum. As for Pseudomonas aeruginosa and other Gram-negative bacteria, sparfloxacin has lower activity than ciprofloxacin. No cross-resistance to other antimicrobials has been observed. Resistance to sparfloxacin develops extremely slowly, because after its action there are practically no persistent microorganisms and the bacterial cells do not have enzymes which inactivate it. It has a post-antibiotic effect: microorganisms do not multiply within 0.5 to 4 hours after the drug has disappeared from the plasma.

Pharmacokinetics

Absorption: Absorption after oral administration is approximately 90%. After ingestion of the drug at a dose of 400 mg Cmax is reached after 3-6 hours, the concentration in the tissues is 2-12 times higher than in plasma.

The concentration of the drug in the serum depends linearly on the size of the dose taken. The degree of absorption does not change when taking the drug with food or milk, however, the rate of absorption slows down, so that the maximum concentration of sparfloxacin is noted about 30 minutes later than when taking the drug on an empty stomach. The activity of the drug decreases slightly at acid pH values. Distribution Binding to plasma proteins (mainly albumin) is 45%. Vd - 3.9 ± 0.8 L / kg. Sparfloxacin is well distributed in body tissues (excluding tissues rich in fat and nervous tissue), the concentration in the tissues and fluids of the lower respiratory tract exceeds the concentration in plasma.

It is found in high concentrations in alveolar macrophages. Therapeutic concentrations are reached in saliva, bile, intestines, abdominal and pelvic organs, kidneys and urinary organs, lung tissue, bronchial secretion, bone tissue, muscles, synovial fluid, joint cartilage , peritoneal fluid, skin. In cerebrospinal and intraocular fluid, 10% of the concentration of the drug in the blood plasma is found. Metabolism Sparfloxacin is metabolized in the liver.

Excretion Sparfloxacin is excreted in the faeces (30 to 50%) and urine (by tubular filtration and tubular secretion) - of which approximately 10% of the oral dose is unchanged. T1 / 2 is from 16 to 30 hours Pharmacokinetics in special clinical cases In patients with renal insufficiency, T1 / 2 is lengthened. In chronic renal failure, the percentage of drug excreted by the kidneys decreases. With CC> 20 ml / min, the accumulation of sparfloxacin in the body does not occur, since there is an increase in metabolism and excretion with feces.

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Special conditions

During treatment with Zagam and for 3 days after the end of treatment, patients should avoid UV rays. There are isolated reports that the use of fluoroquinolones has been accompanied by tendon ruptures. If complaints arise, treatment should be stopped. To avoid the development of crystalluria, exceeding the recommended daily dose is unacceptable. It is necessary to provide the patient with sufficient fluid intake and the maintenance of an acidic urinary reaction. Influence on the ability to drive and control mechanisms During treatment, Zagam must refrain from engaging in potentially dangerous activities which require increased attention and speed of psychomotor reactions.

The composition

1 tab sparfloxacin 200 mg Excipients: corn starch, microcrystalline cellulose, crospovidone, colloidal silicon dioxide, talc, magnesium stearate. Shell composition: hypromellose, propylene glycol, titanium dioxide, talc, quinoline yellow dye.

Zagam Indications

Infectious and inflammatory diseases caused by drug-sensitive microorganisms:

  • respiratory tract infections (including pneumonia, chronic obstructive pulmonary disease caused by exacerbation;
  • middle ear, sinus infections;
  • eye infections;
  • kidney and urinary tract infections (including cystitis, non-gonococcal urethritis, pyelitis);
  • genital infections (including adnexitis, prostatitis);
  • infections of the abdominal cavity (including the bile ducts);
  • bacterial infections of the gastrointestinal tract (including shigellosis, salmonellosis);
  • skin and soft tissue infections (including abscess, pyoderma, furunculosis, infectious dermatitis);
  • bone infections

Zagam contraindications

  • epilepsy;
  • prolonged QT interval or other factors contributing to the development of arrhythmias (hypokalaemia, severe bradycardia, congestive heart failure, atrial fibrillation);
  • glucose-6-phosphate dehydrogenase deficiency;
  • severe renal failure;
  • pregnancy;
  • lactation (breastfeeding);
  • age up to 18 years (because the skeleton formation process is incomplete);
  • Hypersensitivity to the components of the drug.

With caution, a drug should be prescribed for atherosclerosis of the cerebral vessels, cerebrovascular accidents, convulsive syndrome, chronic renal failure, living conditions or professional activities which do not limit sunstroke.

Zagam side effects

From the digestive system: decreased appetite, nausea, vomiting, dyspepsia, abdominal pain, flatulence, increased activity of liver transaminases, alkaline phosphatase, hyperbilirubinemia, cholestatic jaundice (especially in patients with previous liver diseases ), hepatitis, hepatonecrosis.

From the central nervous system and the peripheral nervous system: dizziness, headache, fatigue, anxiety, tremors, drowsiness, peripheral paralgesia (abnormality in the perception of pain), increased intracranial pressure, nightmares, confusion, depression, hallucinations, migraine, fainting, psychotic reactions. On the part of the sensory organs: alteration of taste and smell, alteration of vision (diplopia, change in color perception), tinnitus, hearing loss. On the side of the cardiovascular system: prolongation of the QT interval, tachycardia, cerebral artery thrombosis, flushing.

From the hematopoietic system: eosinophilia, leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia.

From the urinary system: hematuria, crystalluria (with an alkaline urine reaction and weak diuresis), hypercreatininemia. From the musculoskeletal system: arthralgia, myalgia, arthritis, tendovaginitis.

Dermatological reactions: photosensitization, Allergic reactions: pruritus, drug fever, knotty erythema, exudative polymorphic erythema (including Stevens-Johnson syndrome).

Drug interaction

NSAIDs (excluding acetylsalicylic acid) associated with simultaneous use with Zagam increase the risk of seizures. Since sparfloxacin prolongs the QT interval, its use should be avoided in patients receiving drugs that prolong the QT interval (terfenadine, bepridil, astemizole, erythromycin, class IA and III antiarrhythmics, cisapride, pentamidine, tricyclic antidepressants , phenothiazine).

When combined with other antimicrobials, synergism is generally observed (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole): with azlocillin and ceftazidime - for infections caused by Pseudomonas spp .; with meslocillin, azlocillin and other beta-lactam antibiotics - with streptococcal infections; with penicillins resistant to α-lactamase and vancomycin for staphylococcal infections; with metronidazole and clindamycin - with anaerobic infections.

Overdose

There is no specific antidote. In case of accidental overdose, symptomatic treatment is recommended, if necessary, hemodialysis and peritoneal dialysis.

200 mg 180 pills$ 1.38
200 mg 120 pills$ 1.53
200 mg 90 pills$ 1.70
200 mg 60 pills$ 1.89
200 mg 30 pills$ 2.36