Sparbact (Tablets) Instructions for Use

Marketing Authorization Holder

Ipca Laboratories Ltd. (India)

ATC Code

J01MA09 (Sparfloxacin)

Active Substance

Sparfloxacin (Rec.INN registered by WHO)

Dosage Form

Sparbact

Coated tablets, 200 mg: 6 pcs.

Dosage Form, Packaging, and Composition

Coated tablets of greenish-yellow color, round, biconvex; the cross-section shows the tablet’s contents are yellow.

6 pcs. – blister packs (1) – cardboard packs.

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

An antimicrobial agent, a fluoroquinolone derivative, inhibits bacterial DNA gyrase, which desupercoils sections of chromosomal DNA molecules (necessary for reading genetic information). Its low toxicity to host cells is explained by the absence of gyrase in them.

It is a broad-spectrum bactericidal antimicrobial drug (primarily against gram-negative flora, in this respect it is similar to aminoglycosides). It exerts a bactericidal effect on gram-positive microorganisms only during division, and on gram-negative organisms – also during the resting phase, as it affects not only DNA gyrase but also causes lysis of the cell wall.

It prevents the transcription of bacterial genetic material necessary for their normal metabolism, leading to a rapid decrease in the bacteria’s ability to divide. As a result of its action, parallel development of resistance to other antibiotics not belonging to the group of gyrase inhibitors does not occur, making it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines, and many other antibiotics.

Highly active against Escherichia coli, Shigella spp., Salmonella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Serratia spp., Hafnia, Edwardsiella, Proteus (indole-positive and indole-negative), Providencia spp., Morganella morganii, Yersinia spp.; Vibrio spp., Aeromonas spp., Plesiomonas spp., Pasteurella spp., Haemophilus spp., Campylobacter spp., Pseudomonas cepacia, Pseudomonas aeruginosa, Legionella spp., Neisseria spp., Moraxella, Acinetobacter spp., Brucella; Staphylococcus spp., Listeria spp., Corynebacterium spp., Chlamydia spp., Xanthomonas maltophilia.

Moderately active against Gardnerella spp., Flavobacterium spp., Alcaligenes spp., Streptococcus agalactiae, Enterococcus faecalis, Streptococcus pyogenes, Streptococcus pneumoniae, Streptococcus viridans, Mycoplasma hominis, Mycoplasma pneurnoniae, Mycobacterium tuberculosis and Mycobacterium fortuitum.

Considered active against Enterococcus faecium, Ureaplasma urealyticum, Nocardia asteroides. With some exceptions, anaerobic microorganisms are moderately sensitive (e.g., Peptococcus spp., Peptostreptococcus spp.) or resistant (e.g., Bacteroides spp.).

Not active against Treponema pallidum.

Resistance to sparfloxacin develops extremely slowly, as practically no persisting microorganisms remain and bacterial cells lack enzymes that inactivate it. No cross-resistance with other antimicrobial drugs has been noted.

Against Pseudomonas aeruginosa and other gram-negative bacilli, it is less active than ciprofloxacin. T_1/2 is longer than that of ciprofloxacin, therefore Sparfloxacin can be administered once daily. Like ciprofloxacin, it does not interact with theophylline (does not inhibit the activity of liver microsomal enzymes). In terms of the ability to cause photosensitization, it is closer to lomefloxacin than to other fluoroquinolones. It has a post-antibiotic effect; microorganisms do not multiply for 0.5-4 hours after the active substance disappears from the plasma.

Pharmacokinetics

After oral administration, about 90% is absorbed. Absorption is not altered when taken with food and milk.

It is well distributed in body tissues (excluding fat-rich tissue, such as nervous tissue), the concentration in 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 achieved in saliva, bile, intestines, abdominal and pelvic organs, kidneys and urinary organs, lung tissue, bronchial secretions, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, and skin. The concentration in cerebrospinal and intraocular fluid is 10% of the plasma concentration. V_d – 2-3 L/kg, plasma protein binding – about 45%. After a single oral dose of 400 mg, C_max in blood plasma is reached in 3-6 hours, the content in tissues is 2-12 times higher than in plasma. Serum concentration shows a linear dependence on the administered dose. Activity decreases somewhat at acidic pH values.

It is metabolized in the liver, excreted in feces (30-50%) and urine (tubular filtration and tubular secretion), of which about 10% of the orally administered dose is excreted unchanged. T_1/2 – 16-30 hours, in patients with renal failure T_1/2 increases. In chronic renal failure, the percentage of renal excretion decreases, but accumulation of the active substance in the body does not occur at CrCl>20 ml/min, as metabolism and excretion via the intestine increase in parallel.

Indications

Infections of the respiratory tract, middle ear infections, paranasal sinus infections, especially if caused by gram-negative pathogens, including Pseudomonas, or Staphylococcus, eye infections, kidney and urinary tract infections, genital infections (including adnexitis), non-gonococcal urethritis, prostatitis, abdominal infections (e.g., bacterial infections of the gastrointestinal tract, biliary tract, peritonitis), skin and soft tissue infections, bone and joint infections (e.g., osteomyelitis), sepsis, infections against the background of immunodeficiency, e.g., during treatment with immunosuppressive agents or in patients with neutropenia; gonorrhea, chlamydia, leprosy.

ICD codes

Dosage Regimen

Adults, orally, regardless of meals (without chewing, with a sufficient amount of fluid). The duration of the treatment course depends on the nature and severity of the disease and the type of pathogen.

For pneumonia, exacerbation of chronic bronchitis, sinusitis – on the first day 400 mg as a single dose, then – 200 mg/day for 10 days, for patients with CrCl<50 ml/min – on the first day 400 mg as a single dose, then 200 mg every 48 hours.

For urinary tract infection – on the first day 200 mg as a single dose, then 100 mg once/day for 10-14 days.

For acute gonococcal urethritis: 200 mg as a single dose.

For non-gonococcal urethritis on the first day – 200 mg as a single dose, then – 100 mg once/day for 6 days. For leprosy – 200 mg once/day for 12 weeks.

Adverse Reactions

From the digestive system nausea, diarrhea, vomiting, dyspepsia, abdominal pain, flatulence, decreased appetite, increased activity of hepatic transaminases and alkaline phosphatase, cholestatic jaundice (especially in patients with a history of liver disease), hepatitis, hepatonecrosis.

From the CNS and peripheral nervous system dizziness, headache, increased fatigue, anxiety, tremor, drowsiness, peripheral paralgesia (abnormality in pain perception perception), sweating, intracranial hypertension, anxiety, nightmares, confusion, depression, hallucinations, psychotic reactions, migraine, general weakness.

From the cardiovascular system QT interval prolongation, cerebral artery thrombosis, tachycardia, flushing, syncope.

From the sensory organs taste and smell disturbances, visual impairment (e.g., diplopia, color vision changes), tinnitus, hearing loss.

From laboratory parameters eosinophilia, leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia, hypoprothrombinemia, hypercreatininemia, hyperbilirubinemia, hyperglycemia, hematuria, crystalluria (primarily with alkaline urine and low diuresis).

Dermatological reactions itching, drug fever, petechiae, erythema nodosum, exudative multiforme erythema, malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), photosensitivity.

From the musculoskeletal system arthralgia, arthritis, muscle pain, tenosynovitis.

Allergic reactions facial edema, vascular or laryngeal edema, shortness of breath.

Contraindications

Epilepsy, prolonged QT interval or other factors contributing to the development of arrhythmias (hypokalemia, significant bradycardia, chronic heart failure, atrial fibrillation), glucose-6-phosphate dehydrogenase deficiency, severe renal failure, pregnancy, lactation (breastfeeding), children and adolescents under 18 years of age (incomplete process of skeletal formation), hypersensitivity to sparfloxacin.

Use in Pregnancy and Lactation

Contraindicated during pregnancy and lactation.

Use in Renal Impairment

Contraindicated in severe renal failure.

Pediatric Use

Contraindicated in children and adolescents under 18 years of age.

Special Precautions

Use with caution in cerebral atherosclerosis, cerebrovascular accident, epileptic syndrome, living conditions (professional activities) that do not allow limiting sun exposure, chronic renal failure.

UV irradiation should be avoided during treatment and for 3 days after its completion. To avoid the development of crystalluria, exceeding the recommended daily dose is unacceptable, sufficient fluid intake and maintenance of acidic urine reaction are necessary.

Food slows down the rate of absorption.

Concomitant use of sparfloxacin with antiarrhythmic drugs of classes IA and III, bepridil, erythromycin, astemizole, cisapride, pentamidine, tricyclic antidepressants and phenothiazines is not recommended.

Effect on ability to drive vehicles and operate machinery

During treatment, one should refrain from engaging in potentially hazardous activities requiring increased attention and speed of psychomotor reactions.

Drug Interactions

With simultaneous use, NSAIDs (excluding acetylsalicylic acid) increase the risk of seizures.

Oral administration together with iron-containing preparations, sucralfate and antacid preparations containing magnesium, aluminum, calcium, zinc, as well as iron salts, leads to a decrease in the absorption of sparfloxacin.

Metoclopramide accelerates the absorption of sparfloxacin.

With simultaneous use with cyclosporine, an increase in serum creatinine content is noted.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.