Sparfloxacin

Sparfloxacin

File:Sparfloxacin.svg
Clinical data
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	Oral
ATC code	J01MA09 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	92%
Protein binding	45%
Metabolism	Hepatic glucuronidation Cytochrome P450 system not involved
Elimination half-life	16 to 30 hours
Excretion	Fecal (50%) and renal (50%)
Identifiers
IUPAC name 5-amino-1-cyclopropyl-7-[(3R,5S)3,5-dimethylpiperazin- 1-yl]-6,8-difluoro-4-oxo-quinoline-3-carboxylic acid
CAS Number	110871-86-8
PubChem CID	60464
DrugBank	APRD01231
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C19H22F2N4O3
Molar mass	392.41 g/mol

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Sparfloxacin (spar FLOX a sin), trade names Zagam® and Zagam Respipac, is a fluoroquinolone antibiotic used in the treatment of bacterial infections. Zagam is no longer available in the United States.

Sparfloxacin achieves a high degree of penetration into most tissues, except for the central .nervous system. Sparfloxacin is about 37- 45% protein boun;J) (Shimada et at., 1993; Montay,1996). Following a single 400-mg oral dose of sparfloxacin, the mean peak concentration in ~ cantharides-induced inflammatory fluid is 1.3 lA-g per ml after a mean duration of 5 h post-dose. ,J. Thus(overall sparfloxacin penetration into inflammatory fluid is 117% and the mean elimination half-life from this fluid is 19.7 h (Johnson et at., 1992). Skin penetration of sparfloxacin is.good with skin:plasma ratios of 1.00 at 4 h (time of peak plasma concentration) and 1.39 at 5 h. Following single oral doses of 100 or 200mg, concentrations in skin of 0.56 and 0.82-1.31 lA-g per g, respectively, can be expected (Nogita and Ishibashi, 1991 ). Sparfloxacin achieves excellent penetration into human polymorphonuclear leukocytes in vitro (Garcia et at., 1992). Sparfloxacin achieves high concentrations in respiratory and sinus tissues. Following an oral loading dose of 400 mg followed by 200 mg daily, mean concentrations of sparfloxacin (2.5 to 5 h after dosing) in bronchial mucosa, epithelial lining fluid and alveolar macrophages are 4.4 ug per g, 15.0 ug per ml and 53.7 ug per g, respectively. The mean sparfloxacin concentration in maxillary sinus mucosa, 2-5 h after a single 400-mg dose, is 5.8 ug/g (Wise and Honeybourne, 1996) Shimada et at. ( 1993) has summarized many of the studies published in J apanese regarding the tissue distribution of sparfloxacin. (iligh concentrations are achieved in sputu!J!, pleural fluid, skin, lung, prostate, gynecological tissues, breast milk aJ1d otolaryngological ti~sues. Salivary concentrations are 66-70% of plasma levels, while CSF penetration appears to be somewhat.limited with CSF:plasma concentration ratios of only 0.25-0.35. Sparfloxacin achieves concentrati<>ns in bile and gallbladder of 7.1- to 83-fold the concurrent serum levels;J In rabbits, sparfloxacin achieves very good penetration into the ocular vitreous (54% ), cornea (76%) and lens (36%) (Cochereau-Massin et at., 1993).

Sparfloxacin has a similar rate of adverse reactions as ciprofloxacin and other commonly used fluoroqumolones. In a review of 2081 adult patients participating in a Phase III clinical trial of sparfloxacin in community-acquired, lower respiratory tract infections, sparfloxacin (200- or 4O0-mg loading dose then 100 or 200mg daily; i.e. 200/100mg and 400/200mg) had a similar incidence of adverse events as the comparator agents (Rubinstein, 1996). The overall rates of drug-related adverse reactions for sparfloxacin 400/200mg versus comparators and 200/100mg versus the comparator (amoxycillin/clavulanic acid) were 13.7 versus 17.7%, and 9.5 versus 13.2%, respectively. However, many of these reported reactions were very minor; discontinua- tion of the antibacterial agent because of drug-related adverse reactions occured in 1.6 versus 1.6%, and 1) versus 1.1 %, respectively. Adverse reactions affecting the nervous system were reported in 5.7% of the sparfloxacin group, with insomnia and other sleep disorders the most common events. Phototoxicity was noted in 2.0% of sparfloxacin recipients, with the average delay in onset being 6.3 :t 4.5 days (range 1-14 days) after commencing sparfloxacin. Mostly this comisted of erythema on the face and hands which lasted an average of 6.4 :t 4.2 days. The incidence of phototoxicity associated with sparfloxacin appears to be higher than that observed with ciprofloxacin and ofloxacin but less than that reported for fleroxacin, pefloxacin, enoxacin and nalidixic acid. Most importantly, features of the hemolytic-uremic syndrome such as that associated with temafloxacin (p.II44) have not been reported (Ram say and Obershkova, 1974; Bowie et at., 1989; Davey, 1989; Wolf son and Hooper, 1991; Rubinstein, 1996).