Sparfloxacin

The 5-position of quinolones can be substituted by small groups such as halogens, hydroxyl, or amino (54—56). The amino group at this position can be advantageous, particularly when appHed to 6,8-difluoro-7-piperazinyl or 6,8-difluoro-7-pyrrohdinyl quinolones. In contrast to 6,8-difluoro quinolones, when this replacement is appHed to ofloxacin, the resulting derivative has reduced antibacterial activity (57). Replacement of the 5-amino group with methylamine or dimethylamine causes activity to drop substantially. Sparfloxacin [110871-86-8] (21), a representative of 5-amino-6,8-difluoro quinolones, affords modest improvements in gram-positive activity as well as increased in vivo potency when compared with both ciprofloxacin and ofloxacin (54). 

The fluoroquinolones include ciprofloxacin (Cipro), enoxacin (Penetrex), gatifloxacin (Tequin), lome-floxacin (Maxaquin), moxifloxacin (Avelox), ofloxacin (Floxin), and sparfloxacin (Zagain). 

The more common adverse effects seen with the administration of these dm include nausea, diarrhea, headache, abdominal pain or discomfort, and dizziness. A more serious adverse reaction seen with the administration of the fluoroquinolones, especially lomefloxacin and sparfloxacin, is a photosensitivity reaction. This is manifested by an exaggerated sunburn reaction when the skin is exposed to the ultraviolet rays of sunlight or sunlamps. 

All fluoroquinolone drugs can cause pain, inflammation, or rupture of a tendon. The Achilles tendon is particularly vulnerable. This problem can be so severe tiiat prolonged disability results, and, at times, surgical intervention may be necessary to correct die problem, hi addition, the fluoroquinolone drugs, particularly sparfloxacin and lomefloxacin, cause dangerous photosensitivity reactions. Fhtients have experienced severe reactions even when sunscreens or sunblocks were used. 

C7H()N 100-46-9) see Amosulalol Bamidipine Beclamide Benperidol Betanidine Biotin Cisapride Dilevalol Guanoxan Moxifloxacin hydrochloride NebivOlol Nialamide Reproterol Sparfloxacin Sulbentine Viloxazine benzylamine hydrochloride (C7H,()C1N 3287-99-8) see Benzyl mustard oil 2-benzylaminoethanol... 

C3H7N 765-30-0) see Abacavir Ciprofloxacin Grepafloxacin Moxifloxacin hydrochloride Nevirapine Sparfloxacin... 

This class of compounds comprises a series of synthetic agents patterned after nalidixic acid, a naphthyridine derivative introduced in 1963 for the treatment of urinary tract infections. Isosteric heterocyclic groupings in this category include the quinolones (e.g., norfloxacin, ciprofloxacin, lome-floxacin, gatifloxacin, sparfloxacin, moxifloxacin, and ofloxacin), the naph-thyridones (e.g., nalidixic acid, enoxacin, and trovafloxacin), and the cin-nolones (e.g., cinnoxacin) [2] (Fig. 1). 

Thus quinolone antibacterial agents, such as ciprofloxacin CPFX 143 [201], ofloxacin OFLX144 [202],sparfloxacin SPFX145 [203] and trovaflaxin 146 [204] are members of a major class of antibacterial drugs. These fluoroquinolones show broad-spectrum antibacterial activity and are widely used to treat patients with infections, Eq. (58). 

Drugs that may be affected by tricyclic compounds include anticholinergics, carbamazepine, clonidine, dicumarol, grepafloxacin, guanethidine, levodopa, quinolones, sparfloxacin, and sympathomimetics. 

Phenothiazines Cisapride or sparfloxacin because of possible additive QT interval prolongation... 

SPARFLOXACIN Sparfloxacin may be taken with or without food. 

Sparfloxacin - Sparfloxacin is well absorbed following oral administration. Steady-state concentration was achieved on the first day by giving a loading dose that was double the daily dose. Oral absorption of sparfloxacin is unaffected by administration with milk or food, including high-fat meals. Sparfloxacin distributed well into the body. It penetrates well into body fluids and tissues. Sparfloxacin is metabolized by the liver. It is excreted in the feces (50%) and urine (50%). 

Phototoxicity Moderate-to-severe phototoxic reactions have occurred in patients exposed to direct or indirect sunlight or to artificial ultraviolet light (eg, sunlamps) during or following treatment with lomefloxacin, sparfloxacin, or ofloxacin. 

Increases in the QTc interval have been observed in healthy volunteers treated with sparfloxacin. 

Chiidren Safety and efficacy of gatifloxacin, levofloxacin, lomefloxacin, moxifloxacin, norfloxacin, ofloxacin, and sparfloxacin in children younger than 18 years of age have not been established. 

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