Peringatan Keamanan

Single doses of sparfloxacin were relatively non-toxic via the oral route of administration in mice, rats, and dogs. No deaths occurred within a 14-day post-treatment observation period at the highest oral doses tested, up to 5000 mg/kg in either rodent species, or up to 600 mg/kg in the dog. Clinical signs observed included inactivity in mice and dogs, diarrhea in both rodent species, and vomiting, salivation, and tremors in dogs.

Sparfloxacin

DB01208

small molecule approved investigational withdrawn

Deskripsi

Sparfloxacin is a fluoroquinolone antibiotic indicated for bacterial infections. Sparfloxacin exerts its antibacterial activity by inhibiting DNA gyrase, a bacterial topoisomerase. DNA gyrase is an essential enzyme which controls DNA topology and assists in DNA replication, repair, deactivation, and transcription.

Struktur Molekul 2D

Berat 392.3998
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Mean terminal elimination half-life of 20 hours (range 16-30 hours). Prolonged in patients with renal impairment (creatinine clearance <50 mL/min).
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Well absorbed following oral administration with an absolute oral bioavailability of 92%. Unaffected by administration with milk or food, however concurrent administration of antacids containing magnesium hydroxide and aluminum hydroxide reduces the oral bioavailability of sparfloxacin by as much as 50%.

Metabolisme

Hepatic. Metabolized primarily by phase II glucuronidation to form a glucuronide conjugate. Metabolism does not utilize or interfere with the cytochrome P450 enzyme system.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

847 Data
Didanosine Didanosine can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Probenecid Probenecid may decrease the excretion rate of Sparfloxacin which could result in a higher serum level.
Quinapril Quinapril can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium acetate Calcium acetate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Dextran Iron Dextran can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium Calcium can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum carbonate Lanthanum carbonate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric carboxymaltose Ferric carboxymaltose can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose Iron sucrose can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate Ferric pyrophosphate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium citrate Calcium citrate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium gluconate Calcium gluconate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate Ferric sulfate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation Ferric cation can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Tetraferric tricitrate decahydrate Tetraferric tricitrate decahydrate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum III cation Lanthanum III cation can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium polycarbophil Calcium polycarbophil can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide Ferric oxyhydroxide can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sucralfate Sucralfate can cause a decrease in the absorption of Sparfloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Sparfloxacin.
Nitrofurantoin The therapeutic efficacy of Sparfloxacin can be decreased when used in combination with Nitrofurantoin.
Mycophenolic acid The serum concentration of Mycophenolic acid can be decreased when it is combined with Sparfloxacin.
Mycophenolate mofetil The serum concentration of Mycophenolate mofetil can be decreased when it is combined with Sparfloxacin.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Sparfloxacin.
Insulin human The therapeutic efficacy of Insulin human can be increased when used in combination with Sparfloxacin.
Insulin lispro The therapeutic efficacy of Insulin lispro can be increased when used in combination with Sparfloxacin.
Insulin pork The therapeutic efficacy of Insulin pork can be increased when used in combination with Sparfloxacin.
Troglitazone The therapeutic efficacy of Troglitazone can be increased when used in combination with Sparfloxacin.
Glimepiride The therapeutic efficacy of Glimepiride can be increased when used in combination with Sparfloxacin.
Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Sparfloxacin.
Metformin The therapeutic efficacy of Metformin can be increased when used in combination with Sparfloxacin.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be increased when used in combination with Sparfloxacin.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Sparfloxacin.
Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Sparfloxacin.
Miglitol The therapeutic efficacy of Miglitol can be increased when used in combination with Sparfloxacin.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Sparfloxacin.
Nateglinide The therapeutic efficacy of Nateglinide can be increased when used in combination with Sparfloxacin.
Tolazamide The therapeutic efficacy of Tolazamide can be increased when used in combination with Sparfloxacin.
Repaglinide The therapeutic efficacy of Repaglinide can be increased when used in combination with Sparfloxacin.
Phenformin The therapeutic efficacy of Phenformin can be increased when used in combination with Sparfloxacin.
Glyburide The therapeutic efficacy of Glyburide can be increased when used in combination with Sparfloxacin.
Glipizide The therapeutic efficacy of Glipizide can be increased when used in combination with Sparfloxacin.
Gliclazide The therapeutic efficacy of Gliclazide can be increased when used in combination with Sparfloxacin.
Tolbutamide The therapeutic efficacy of Tolbutamide can be increased when used in combination with Sparfloxacin.
Pioglitazone The therapeutic efficacy of Pioglitazone can be increased when used in combination with Sparfloxacin.
Bromocriptine The therapeutic efficacy of Bromocriptine can be increased when used in combination with Sparfloxacin.
Gliquidone The therapeutic efficacy of Gliquidone can be increased when used in combination with Sparfloxacin.
Mitiglinide The therapeutic efficacy of Mitiglinide can be increased when used in combination with Sparfloxacin.
Sitagliptin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Sparfloxacin.
Exenatide The therapeutic efficacy of Exenatide can be increased when used in combination with Sparfloxacin.
Mecasermin The therapeutic efficacy of Mecasermin can be increased when used in combination with Sparfloxacin.
Pramlintide The therapeutic efficacy of Pramlintide can be increased when used in combination with Sparfloxacin.
Glisoxepide The therapeutic efficacy of Glisoxepide can be increased when used in combination with Sparfloxacin.
Insulin aspart The therapeutic efficacy of Insulin aspart can be increased when used in combination with Sparfloxacin.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be increased when used in combination with Sparfloxacin.
Glymidine The therapeutic efficacy of Glymidine can be increased when used in combination with Sparfloxacin.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be increased when used in combination with Sparfloxacin.
Buformin The therapeutic efficacy of Buformin can be increased when used in combination with Sparfloxacin.
Vildagliptin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Sparfloxacin.
Voglibose The therapeutic efficacy of Voglibose can be increased when used in combination with Sparfloxacin.
NN344 The therapeutic efficacy of NN344 can be increased when used in combination with Sparfloxacin.
AMG-222 The therapeutic efficacy of AMG-222 can be increased when used in combination with Sparfloxacin.
Bisegliptin The therapeutic efficacy of Bisegliptin can be increased when used in combination with Sparfloxacin.
Alogliptin The therapeutic efficacy of Alogliptin can be increased when used in combination with Sparfloxacin.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Sparfloxacin.
Saxagliptin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Sparfloxacin.
Liraglutide The therapeutic efficacy of Liraglutide can be increased when used in combination with Sparfloxacin.
Gosogliptin The therapeutic efficacy of Gosogliptin can be increased when used in combination with Sparfloxacin.
Linagliptin The therapeutic efficacy of Linagliptin can be increased when used in combination with Sparfloxacin.
Canagliflozin The therapeutic efficacy of Canagliflozin can be increased when used in combination with Sparfloxacin.
Glibornuride The therapeutic efficacy of Glibornuride can be increased when used in combination with Sparfloxacin.
Benfluorex The therapeutic efficacy of Benfluorex can be increased when used in combination with Sparfloxacin.
Empagliflozin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Sparfloxacin.
Albiglutide The therapeutic efficacy of Albiglutide can be increased when used in combination with Sparfloxacin.
Dulaglutide The therapeutic efficacy of Dulaglutide can be increased when used in combination with Sparfloxacin.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Sparfloxacin.
Netoglitazone The therapeutic efficacy of Netoglitazone can be increased when used in combination with Sparfloxacin.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be increased when used in combination with Sparfloxacin.
Ciglitazone The therapeutic efficacy of Ciglitazone can be increased when used in combination with Sparfloxacin.
Lixisenatide The therapeutic efficacy of Lixisenatide can be increased when used in combination with Sparfloxacin.
Insulin beef The therapeutic efficacy of Insulin beef can be increased when used in combination with Sparfloxacin.
Insulin degludec The therapeutic efficacy of Insulin degludec can be increased when used in combination with Sparfloxacin.
Insulin peglispro The therapeutic efficacy of Insulin peglispro can be increased when used in combination with Sparfloxacin.
Insulin tregopil The therapeutic efficacy of Insulin tregopil can be increased when used in combination with Sparfloxacin.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be increased when used in combination with Sparfloxacin.
Dutogliptin The therapeutic efficacy of Dutogliptin can be increased when used in combination with Sparfloxacin.
Allicin The therapeutic efficacy of Allicin can be increased when used in combination with Sparfloxacin.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be increased when used in combination with Sparfloxacin.
2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Sparfloxacin.
Teneligliptin The therapeutic efficacy of Teneligliptin can be increased when used in combination with Sparfloxacin.
Omarigliptin The therapeutic efficacy of Omarigliptin can be increased when used in combination with Sparfloxacin.
Carmegliptin The therapeutic efficacy of Carmegliptin can be increased when used in combination with Sparfloxacin.
Gemigliptin The therapeutic efficacy of Gemigliptin can be increased when used in combination with Sparfloxacin.
Anagliptin The therapeutic efficacy of Anagliptin can be increased when used in combination with Sparfloxacin.
Evogliptin The therapeutic efficacy of Evogliptin can be increased when used in combination with Sparfloxacin.
Sotagliflozin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Sparfloxacin.
Balaglitazone The therapeutic efficacy of Balaglitazone can be increased when used in combination with Sparfloxacin.
Remogliflozin etabonate The therapeutic efficacy of Remogliflozin etabonate can be increased when used in combination with Sparfloxacin.

Target Protein

DNA gyrase subunit A gyrA
DNA gyrase subunit B gyrB
DNA gyrase subunit A gyrA
DNA topoisomerase 4 subunit A parC
DNA topoisomerase 2-alpha TOP2A

Referensi & Sumber

Synthesis reference: Guillaume Conrath, "Solution of sparfloxacin, its preparation and salt of which it is composed." U.S. Patent US5478829, issued May, 1987.

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