|1. TYPE OF DRUG- Sparfloxacin|
|Sparfloxacin (spar FLOX a sinis a fluoroquinolone antibiotic used in the treatment of bacterial infections. It has a controversial safety profile.|
|2. INDICATIONS (USE)- Sparfloxacin|
|The bactericidal action of sparfloxacin results from inhibition of the enzymes topoisomerase II (DNA gyrase) and topoisomerase IV, which are required for bacterial DNA replication, transcription, repair, and recombination.|
|3. MECHANISM OF ACTION (MOA)- Sparfloxacin|
|Sparfloxacin, like other quinolones and fluoroquinolones, are bactericidal drugs, actively killing bacteria. Quinolones inhibit the bacterial DNA gyrase or the topoisomerase IV enzyme, thereby inhibiting DNA replication and transcription. Quinolones can enter cells easily and therefore are often used to treat intracellular pathogens such as Legionella pneumophila and Mycoplasma pneumoniae. For many gram-negative bacteria DNA gyrase is the target, whereas topoisomerase IV is the target for many gram-positive bacteria. Eukaryotic cells do not contain DNA gyrase or topoisomerase IV.|
|4. ROUTES OF ADMINISTRATION- Sparfloxacin|
|5. ONSET OF EFFECT OR ACTION- Sparfloxacin|
|Renal excretionIn humans, the portion of an erythromycin dose excreted in the urine varies from 0.02 to 20% and the
elimination half-live may be prolonged in renal disease. However, except complete renal failure, renal
impairment has only a minor impact on the pharmacokinetics of erythromycin.
Urinary excretion of erythromycin accounts for approximately 10% of an administered oral or IM dose
(Burrows, 1980). Twenty hours after administration of isotopic erythromycin in rats, 27 to 36% of the
radioactivity was recovered in the urine.
In humans, 15% of an administered dose was excreted in the bile.
In rats, erythromycin and its metabolites are excreted mainly by way of bile, but in part, also by direct
passage through the intestinal wall (Baggot and Gingerich, 1976). Two hours following intravenous
injection of isotopic erythromycin, 15.1% of the dose was excreted in the bi1e (Lee et al, 1956b).
Twenty hours following intravenous injection of isotopic erythromycin, 37-43% of the radioactivity is
recovered in the intestinal tract plus faeces. An enterohepatic recirculation may also
contribute to the high concentrations of erythromycin in faecal samples.
|6. DOSAGE (DOSING INFORMATION)- Sparfloxacin|
|(Adults) RTI:Day 1 :400mg.loading dose.Next 10 days 200mg. OD. STD:Gonococcal urethritis:200mg OD on day 1 followed by 100mg OD for 6 days.Acute bacterial sinusitis:Day 1 :400mg loading dose.200mg OD for the next 10 days.|
|7. HALF LIFE (DURATION OF ACTION)- Sparfloxacin|
|8. ADVERSE EFFECTS OR SIDE EFFECTS- Sparfloxacin|
|9. CONTRAINDICATIONS- Sparfloxacin|
|Hypersensitivity to fluoroquinolones.|
|10. DRUG INTERACTIONS- Sparfloxacin|
|Dose with vancomycin.Ceftazidime,Tobramycin,imipenem.digoxin plasma concentrations on concomitantuse.erythromycin,terfenadine,quinidine,astemizole,procanamide,disopyramide,amiodaroneSome neuroleptics and phenothiazines:potentiated QT-prolongation effect.|
|11. EXCRETION- Sparfloxacin|
|The urinary excretion