Absorption :   Sparfloxacin is well absorbed following oral administration with an absolute oral bioavailability of 92%. The mean maximum plasma sparfloxacin concentration following a single 400-mg oral dose was approximately 1.3 (±0.2) µg/mL. The area under the curve (mean AUC _{O ->(infinity)} ) following a single 400-mg oral dose was approximately 34 (±6.8) µg·hr/mL.

Steady-state plasma concentration was achieved on the first day by giving a loading dose that was double the daily dose. Mean (±SD) pharmacokinetic parameters observed for the 24-hour dosing interval with the recommended dosing regimen are shown below:

Maximum plasma concentrations for the initial oral 400-mg loading dose were typically achieved between 3 to 6 hours following administration with a mean value of approximately 4 hours. Maximum plasma concentrations for a 200-mg dose were also achieved between 3 to 6 hours after administration with a mean of about 4 hours.

Oral absorption of sparfloxacin is unaffected by administration with milk or food, including high fat meals. Concurrent administration of antacids containing magnesium hydroxide and aluminum hydroxide reduces the oral bioavailability of sparfloxacin by as much as 50%. (See PRECAUTIONS , Information for Patients , and Drug Interactions .)

Distribution:   Upon reaching general circulation, sparfloxacin distributes well into the body, as reflected by the large mean steady-state volume of distribution (Vd _ss ) of 3.9 (±0.8) L/kg. Sparfloxacin exhibits low plasma protein binding in serum at about 45%.

Sparfloxacin penetrates well into body fluids and tissues. Results of tissue and body fluid distribution studies demonstrated that oral administration of sparfloxacin produces sustained concentrations and that sparfloxacin concentrations in lower respiratory tract tissues and fluids generally exceed the corresponding plasma concentrations. The concentration of sparfloxacin in respiratory tissues (pulmonary parenchyma, bronchial wall, and bronchial mucosa) at 2 to 6 hours following standard oral dosing was approximately 3 to 6 times greater than the corresponding concentration in plasma. Concentrations in these respiratory tissues increase at up to 24 hours following dosing. Sparfloxacin is also highly concentrated into alveolar macrophages compared to plasma. Tissue or fluid to plasma sparfloxacin concentration ratios for respiratory tissues and fluids are:

Tissue to Plasma Sparfloxacin Concentration Mean Ratio (%CV) *

Respiratory tissues and fluids	n ** value	Time of Collection Postdose
		2 to 6 hour		12 to 24 hour
alveolar macrophage	6/5	51.8	(88.7%)	68.1	(47.9%)
epithelial lining fluid	10/10	12.3	(26.7%)	17.6	(35.3%)
pulmonary parenchyma	8/7	5.9	(15.0%)	15.8	(32.0%)
bronchial wall	8/7	2.8	(16.0%)	5.7	(25.0%)
bronchial mucosa	6/5	2.7	(11.5%)	3.1	(11.6%)
* % CV (percent coefficient of variation)
** For tissues with two values, the first n is for 2 to 6 hours and the second n is for 12 to 24 hours.

Brand Name: Zagam
Generic Name: Sparfloxacin

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