Sparflo^® (Tablets) Instructions for Use

Marketing Authorization Holder

Dr. Reddy’s Laboratories Ltd. (India)

Contact Information

DR. REDDY’S LABORATORIES LTD. (India)

ATC Code

J01MA09 (Sparfloxacin)

Active Substance

Sparfloxacin

Dosage Form

Sparflo®

Coated tablets, 200 mg: 6 pcs.

Dosage Form, Packaging, and Composition

Coated tablets almost white or light yellow in color, oval, with a score on one side and an imprint “200” on the other.

Excipients: corn starch – 15 mg, microcrystalline cellulose – 65 mg, crospovidone – 5 mg, colloidal silicon dioxide – 6 mg, talc – 3 mg, magnesium stearate – 6 mg.

Shell composition: hypromellose – 5.36 mg, propylene glycol – 1.32 mg, titanium dioxide (E171) – 2.19 mg, talc – 1.11 mg, quinoline yellow dye (E104) – 0.03 mg.

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

Clinical-Pharmacological Group

Antibacterial drug of the fluoroquinolone group

Pharmacotherapeutic Group

Antimicrobial agent – fluoroquinolone

Pharmacological Action

Broad-spectrum antimicrobial bactericidal drug from the fluoroquinolone group. It inhibits bacterial DNA gyrase, preventing the replication of bacterial DNA. It exerts a bactericidal effect on gram-positive microorganisms only during the division period, and on gram-negative microorganisms during both the division and resting periods, as it affects not only DNA gyrase but also causes lysis of the cell wall.

The drug prevents the transcription of the genetic material of bacteria necessary for their normal metabolism, which leads to a rapid decrease in the ability of bacteria to divide. As a result of the drug’s action, the development of cross-resistance to other antibiotics not belonging to the group of DNA gyrase inhibitors is not observed, making it highly active against bacteria resistant to aminoglycosides, penicillins, cephalosporins, and tetracyclines.

Low toxicity to macroorganisms is explained by the absence of gyrases in them.

Sparflo^®is active against gram-positive and gram-negative bacteria. An advantage of the drug is its more pronounced activity against gram-positive cocci and anaerobes compared to previous generations of fluoroquinolones. Against gram-negative bacteria, it exhibits activity close to that of aminoglycosides.

Highly susceptible to the drug are Staphylococcus spp., Streptococcus pneumoniae, Escherichia coli, Salmonella spp., Shigella spp., Citrobacter spp., Klebsiella spp., Enterobacter spp., Serratia spp., Hafnia spp., Edwardsiella spp., Proteus spp. (indole-positive and indole-negative strains), Providencia spp., Morganella spp., Yersinia spp., Vibrio spp., Aeromonas spp., Plesiomonas spp., Pasteurella spp., Campylobacter spp., Haemophilus spp., Pseudomonas aeruginosa, Pseudomonas cepacia, Legionella spp., Neisseria spp., Moraxella spp., Acinetobacter spp., Brucella spp., Mycoplasma pneumoniae, Listeria spp., Corynebacterium spp., Chlamydia spp., Xanthomonas maltophilia.

The drug is also highly active against Mycobacterium tuberculosis (including multidrug-resistant strains).

Generally sensitive to the drug are Ureaplasma urealyticum, Nocardia asteroides.

The drug is moderately active against Gardnerella spp., Flavobacterium spp., Alcaligenes spp., Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus viridans, Enterococcus faecalis, Mycoplasma hominis, Mycobacterium fortuitum, Peptococcus spp., Peptostreptococcus spp.

Resistant to the drug are Bacteroides spp.

Sparflo^®is not active against Treponema pallidum.

Against Pseudomonas aeruginosa and other gram-negative bacteria, Sparfloxacin is less active than ciprofloxacin.

No cross-resistance to other antimicrobial drugs has been noted.

Resistance to sparfloxacin develops extremely slowly because after its action, practically no persisting microorganisms remain, and bacterial cells lack enzymes that inactivate it.

It has a post-antibiotic effect: microorganisms do not multiply for 0.5-4 hours after the drug disappears from the plasma.

Pharmacokinetics

Absorption

Absorption after oral administration is about 90%. After oral administration of the drug at a dose of 400 mg, C_max is reached in 3-6 hours, the concentration in tissues is 2-12 times higher than in plasma. The concentration of the drug in blood serum has a linear dependence on the size of the administered dose.

The degree of absorption does not change when the drug is taken with food or milk; however, the rate of absorption slows down, so the maximum concentration of sparfloxacin is noted approximately 30 minutes later than when the drug is taken on an empty stomach.

The activity of the drug decreases somewhat at acidic pH values.

Distribution

Binding to plasma proteins (mainly albumin) is 45%. V_d – 3.9±0.8 L/kg. Sparfloxacin is well distributed in the body’s tissues (excluding fat-rich tissue, nervous tissue), concentrations in the tissues and fluids of the lower respiratory tract exceed 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, articular cartilage, peritoneal fluid, and skin. In cerebrospinal and intraocular fluid, 10% of the drug concentration in blood plasma is detected.

Metabolism

Sparfloxacin is metabolized in the liver.

Excretion

Sparfloxacin is excreted in feces (30-50%) and in urine (by tubular filtration and tubular secretion) – of which about 10% of the orally administered dose is excreted unchanged. T_1/2 is 16-30 hours.

Pharmacokinetics in special clinical cases

In patients with renal failure, T_1/2 is prolonged. In chronic renal failure, the percentage of the drug excreted through the kidneys decreases. With CrCl>20 ml/min, accumulation of sparfloxacin in the body does not occur, as metabolism and excretion in feces increase.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug

• Respiratory tract infections (including pneumonia, chronic obstructive pulmonary disease in the acute stage, caused by Streptococcus pneumonia, Staphylococcus spp., Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Klebsiella pneumoniae, Enterobacter cloacae, Mycoplasma pneumonia, Chlamydia pneumoniae);
• Middle ear infections, paranasal sinus infections (especially those caused by gram-negative pathogens, including Pseudomonas spp. or Staphylococcus spp.);
• Eye infections;
• Kidney and urinary tract infections (including cystitis, nongonococcal urethritis, pyelitis);
• Genital infections (including adnexitis, prostatitis);
• Abdominal infections (including biliary tract infections);
• Bacterial gastrointestinal infections (including shigellosis, salmonellosis);
• Skin and soft tissue infections (including abscesses, pyoderma, furunculosis, infectious dermatitis);
• Bone and joint infections (including osteomyelitis);
• Sexually transmitted infections (gonorrhea, chlamydia);
• Pulmonary tuberculosis (in case of intolerance to first-line therapy or for the treatment of drug-resistant tuberculosis);
• Leprosy;
• Infections in patients with immunodeficiency (including against the background of treatment with immunosuppressive drugs or in patients with neutropenia).

ICD codes

Dosage Regimen

The drug is administered orally, regardless of food intake. The duration of treatment depends on the severity of the disease, clinical course, and the results of bacteriological examination.

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

For ENT infections (including sinusitis), 400 mg is prescribed as a single dose on the first day, then – 200 mg/day for 10 days.

For pulmonary tuberculosis as part of combination therapy with anti-tuberculosis drugs, 400 mg is prescribed as a single dose on the first day, then – 200 mg/day for 30 days.

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

For acute gonococcal urethritis, 400 mg is prescribed as a single dose on the first day, then – after 24 hours – 200 mg. The total course dose is 600 mg.

For nongonococcal urethritis, 200 mg is prescribed as a single dose on the first day, then – 100 mg once/day for 6 days.

For bacterial prostatitis, 400 mg is prescribed as a single dose on the first day, then – 200 mg/day for 10-14 days.

For chlamydial infections, 400 mg is prescribed as a single dose on the first day, then 200 mg/day for 10-14 days.

For skin and soft tissue infections, 400 mg is prescribed as a single dose on the first day, then 200 mg once/day for 3-9 days.

For leprosy, 200 mg is prescribed once/day for 12 weeks.

The tablets should be swallowed without chewing, with a sufficient amount of liquid.

Adverse Reactions

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

From the central and peripheral nervous system: dizziness, headache, increased fatigue, anxiety, tremor, drowsiness, peripheral paralgesia (abnormality of pain perception), increased intracranial pressure, nightmares, confusion, depression, hallucinations, migraine, fainting, psychotic reactions.

From the sensory organs: impaired taste and smell, visual impairment (diplopia, altered color perception), tinnitus, hearing loss.

From the cardiovascular system: QT interval prolongation, tachycardia, cerebral artery thrombosis, flushing of the skin of the face.

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

From the urinary system: hematuria, crystalluria (with alkaline urine reaction and low diuresis), hypercreatininemia.

From the musculoskeletal system: arthralgia, myalgia, arthritis, tenosynovitis.

Dermatological reactions photosensitivity,

Allergic reactions skin itching, drug fever, erythema nodosum, exudative erythema multiforme (including Stevens-Johnson syndrome), toxic epidermal necrolysis ( Lyell’s syndrome), facial edema, laryngeal edema.

Other dyspnea, general weakness, increased sweating, hypoprothrombinemia, hyperglycemia, petechiae.

Contraindications

• Epilepsy;
• Prolonged QT interval or other factors contributing to the development of arrhythmias (hypokalemia, severe bradycardia, congestive heart failure, atrial fibrillation);
• Glucose-6-phosphate dehydrogenase deficiency;
• Severe renal failure;
• Pregnancy;
• Lactation (breastfeeding);
• Age under 18 years (due to incomplete skeletal formation process);
• Hypersensitivity to the drug components.

With caution the drug should be prescribed for cerebral atherosclerosis, cerebrovascular disorders, convulsive syndrome, chronic renal failure, living conditions or professional activities that do not allow limiting insolation.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Special Precautions

During treatment with Sparflo^® and for 3 days after treatment completion, patients should avoid UV radiation.

There are isolated reports that the use of fluoroquinolones has been accompanied by tendon ruptures. If complaints appear, treatment should be discontinued.

To avoid the development of crystalluria, exceeding the recommended daily dose is unacceptable. It is necessary to ensure sufficient fluid intake for the patient and maintenance of acidic urine reaction.

Effect on ability to drive vehicles and mechanisms

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

Overdose

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

Drug Interactions

NSAIDs (excluding acetylsalicylic acid) when used concomitantly with Sparflo^® increase the risk of seizures.

Since Sparfloxacin contributes to QT interval prolongation, its use should be avoided in patients receiving drugs that promote QT interval prolongation (terfenadine, bepridil, astemizole, erythromycin, class I A and III antiarrhythmic drugs, cisapride, pentamidine, tricyclic antidepressants, phenothiazine).

When combined with other antimicrobial drugs, synergism is usually observed (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole): with azlocillin and ceftazidime – for infections caused by Pseudomonas spp.; with mezlocillin, azlocillin and other beta-lactam antibiotics – for streptococcal infections; with beta-lactamase-resistant penicillins and vancomycin – for staphylococcal infections; with metronidazole and clindamycin – for anaerobic infections.

With concomitant use of sparfloxacin and cyclosporine, an increase in serum creatinine is noted, therefore, in patients taking this combination, monitoring of this indicator 2 times a week is necessary.

Pharmacokinetic interaction

With concomitant use, Sparfloxacin has practically no effect on the concentration of theophylline, oral hypoglycemic drugs, indirect anticoagulants.

With concomitant use of Sparflo^® with iron-containing drugs, sucralfate and antacid drugs containing magnesium, aluminum, calcium, zinc, iron salts, a decrease in the absorption of sparfloxacin is noted. In this regard, Sparflo^® should be administered 1-2 hours before or not less than 4 hours after taking the specified drugs.

With concomitant use, metoclopramide accelerates the absorption of sparfloxacin, which leads to a decrease in the time to reach its maximum plasma concentration.

Storage Conditions

The drug should be stored out of the reach of children, in a dry, light-protected place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

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.