Peringatan Keamanan

The LD50 following oral administration in mice and rats is 1803 mg/kg and 1478 mg/kg, respectively.L11725

Levofloxacin exhibits low potential for acute toxicity - following a single high dose of levofloxacin in several different test animals (e.g. mice, rats, monkeys) observed symptoms included ataxia, ptosis, decreased motor activity, dyspnea, tremors, and convulsions.L11638 Treatment of acute overdosage should involve stomach emptying (e.g. with activated charcoal) and general supportive measures. Consider monitoring of the patient's ECG to ensure QTc values remain within range.L11692 Levofloxacin is not efficiently removed by dialysis (peritoneal or hemodialysis) and is therefore of little benefit in cases of overdose.L11638

Levofloxacin

DB01137

small molecule approved investigational

Deskripsi

Levofloxacin is a fluoroquinolone antibiotic and the optical S-(-) isomer of racemic ofloxacin.A190663 It reportedly carries 8 to 128-fold more activity against both gram-negative and gram-positive bacteria compared to R-(+)-ofloxacinA190663 and remains stereochemically stable following administration (i.e. it does not invert to the inactive isomer).L11638 Levofloxacin, along with other quinolones such as gatifloxacin and moxifloxacin, is a member of the third generation of fluoroquinolones, colloquially referred to as the "respiratory quinolones" due to improved activity against gram-positive bacteria commonly implicated in respiratory infections.A31453,A190756

Levofloxacin was first approved by the FDA in 1996, and was approved in Canada and several South American countries soon after.A190663

Struktur Molekul 2D

Berat 361.3675
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average terminal elimination half-life of levofloxacin is 6-8 hours.[A190663,L11638]
Volume Distribusi Levofloxacin is widely distributed in the body, with an average volume of distribution following oral administration between 1.09-1.26 L/kg (~89-112 L).[A190663,L11638] Concentrations in many tissues and fluids may exceed those observed in plasma.[A190663] Levofloxacin is known to penetrate well into skin tissue, fluids (e.g. blisters), lung tissue, and prostatic tissue, amongst others.[A190663]
Klirens (Clearance) The average apparent total body clearance of levofloxacin ranges from 8.64-13.56 L/h, and its renal clearance ranges from 5.76-8.52 L/h.[A190663,L11638] The relative similarity of these ranges indicates a small degree of non-renal clearance.[A190663]

Absorpsi

Absorption of levofloxacin following oral administration is rapid and essentially complete, with an oral bioavailability of approximately 99%.L11638 Due to its nearly complete absorption, the intravenous and oral formulations of levofloxacin may be interchangeable.L11692 The Tmax is generally attained 1-2 hours following administration and the Cmax is proportional to the given dose - an intravenous dose of 500mg infused over 60 minutes resulted in a Cmax of 6.2 ± 1.0 µg/mL whereas a 750mg dose infused over 90 minutes resulted in a Cmax of 11.5 ± 4.0 µg/mL.L11638 Oral administration with food prolongs the Tmax by approximately 1 hour and slightly decreases the Cmax, but these changes are not likely to be clinically significant.L11638 Systemic absorption following oral inhalation is approximately 50% lower than that observed following oral administration.L11689

Metabolisme

Only 2 metabolites, desmethyl-levofloxacin and levofloxacin-N-oxide, have been identified in humans, neither of which appears to carry any relevant pharmacological activity.L11638 Following oral administration, less than 5% of the administered dose was recovered in the urine as these metabolites, indicating very little metabolism of levofloxacin in humans.L11638 The specific enzymes responsible for the demethylation and oxidation of levofloxacin have yet to be ascertained.

Rute Eliminasi

The majority of administered levofloxacin is excreted unchanged in the urine.L11638 Following the administration of a single oral dose of levofloxacin, approximately 87% was eliminated unchanged in the urine within 48 hours and less than 4% was eliminated in the feces within 72 hours.L11638

Interaksi Makanan

1 Data
  • 1. Take with or without food. Food slightly alters kinetics but not to any clinically significant extent.

Interaksi Obat

1410 Data
Ivabradine Ivabradine may increase the QTc-prolonging activities of Levofloxacin.
Didanosine Didanosine can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Quinapril Quinapril can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium acetate Calcium acetate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Dextran Iron Dextran can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium Calcium can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum carbonate Lanthanum carbonate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric carboxymaltose Ferric carboxymaltose can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose Iron sucrose can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate Ferric pyrophosphate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate Ferric sulfate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation Ferric cation can cause a decrease in the absorption of Levofloxacin 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 Levofloxacin 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 Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide Ferric oxyhydroxide can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sucralfate Sucralfate can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Levofloxacin.
Nitrofurantoin The therapeutic efficacy of Levofloxacin can be decreased when used in combination with Nitrofurantoin.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Levofloxacin.
Insulin human The therapeutic efficacy of Insulin human can be increased when used in combination with Levofloxacin.
Insulin lispro The therapeutic efficacy of Insulin lispro can be increased when used in combination with Levofloxacin.
Insulin pork The therapeutic efficacy of Insulin pork can be increased when used in combination with Levofloxacin.
Troglitazone The therapeutic efficacy of Troglitazone can be increased when used in combination with Levofloxacin.
Glimepiride The therapeutic efficacy of Glimepiride can be increased when used in combination with Levofloxacin.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be increased when used in combination with Levofloxacin.
Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Levofloxacin.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be increased when used in combination with Levofloxacin.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Levofloxacin.
Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Levofloxacin.
Miglitol The therapeutic efficacy of Miglitol can be increased when used in combination with Levofloxacin.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Levofloxacin.
Nateglinide The therapeutic efficacy of Nateglinide can be increased when used in combination with Levofloxacin.
Pentamidine The therapeutic efficacy of Pentamidine can be increased when used in combination with Levofloxacin.
Tolazamide The therapeutic efficacy of Tolazamide can be increased when used in combination with Levofloxacin.
Repaglinide The therapeutic efficacy of Repaglinide can be increased when used in combination with Levofloxacin.
Phenformin The therapeutic efficacy of Phenformin can be increased when used in combination with Levofloxacin.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be increased when used in combination with Levofloxacin.
Glyburide The therapeutic efficacy of Glyburide can be increased when used in combination with Levofloxacin.
Glipizide The therapeutic efficacy of Glipizide can be increased when used in combination with Levofloxacin.
Gliclazide The therapeutic efficacy of Gliclazide can be increased when used in combination with Levofloxacin.
Tolbutamide The therapeutic efficacy of Tolbutamide can be increased when used in combination with Levofloxacin.
Pioglitazone The therapeutic efficacy of Pioglitazone can be increased when used in combination with Levofloxacin.
Gliquidone The therapeutic efficacy of Gliquidone can be increased when used in combination with Levofloxacin.
Mitiglinide The therapeutic efficacy of Mitiglinide can be increased when used in combination with Levofloxacin.
Sitagliptin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Levofloxacin.
Sunitinib The therapeutic efficacy of Sunitinib can be increased when used in combination with Levofloxacin.
Exenatide The therapeutic efficacy of Exenatide can be increased when used in combination with Levofloxacin.
Mecasermin The therapeutic efficacy of Mecasermin can be increased when used in combination with Levofloxacin.
Pramlintide The therapeutic efficacy of Pramlintide can be increased when used in combination with Levofloxacin.
Glisoxepide The therapeutic efficacy of Glisoxepide can be increased when used in combination with Levofloxacin.
Insulin aspart The therapeutic efficacy of Insulin aspart can be increased when used in combination with Levofloxacin.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be increased when used in combination with Levofloxacin.
Glymidine The therapeutic efficacy of Glymidine can be increased when used in combination with Levofloxacin.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be increased when used in combination with Levofloxacin.
Buformin The therapeutic efficacy of Buformin can be increased when used in combination with Levofloxacin.
Vildagliptin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Levofloxacin.
Voglibose The therapeutic efficacy of Voglibose can be increased when used in combination with Levofloxacin.
NN344 The therapeutic efficacy of NN344 can be increased when used in combination with Levofloxacin.
AMG-222 The therapeutic efficacy of AMG-222 can be increased when used in combination with Levofloxacin.
Bisegliptin The therapeutic efficacy of Bisegliptin can be increased when used in combination with Levofloxacin.
Alogliptin The therapeutic efficacy of Alogliptin can be increased when used in combination with Levofloxacin.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Levofloxacin.
Saxagliptin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Levofloxacin.
Liraglutide The therapeutic efficacy of Liraglutide can be increased when used in combination with Levofloxacin.
Gosogliptin The therapeutic efficacy of Gosogliptin can be increased when used in combination with Levofloxacin.
Canagliflozin The therapeutic efficacy of Canagliflozin can be increased when used in combination with Levofloxacin.
Glibornuride The therapeutic efficacy of Glibornuride can be increased when used in combination with Levofloxacin.
Benfluorex The therapeutic efficacy of Benfluorex can be increased when used in combination with Levofloxacin.
Empagliflozin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Levofloxacin.
Albiglutide The therapeutic efficacy of Albiglutide can be increased when used in combination with Levofloxacin.
Dulaglutide The therapeutic efficacy of Dulaglutide can be increased when used in combination with Levofloxacin.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Levofloxacin.
Netoglitazone The therapeutic efficacy of Netoglitazone can be increased when used in combination with Levofloxacin.
Rivoglitazone The therapeutic efficacy of Rivoglitazone can be increased when used in combination with Levofloxacin.
Ciglitazone The therapeutic efficacy of Ciglitazone can be increased when used in combination with Levofloxacin.
Lixisenatide The therapeutic efficacy of Lixisenatide can be increased when used in combination with Levofloxacin.
Insulin beef The therapeutic efficacy of Insulin beef can be increased when used in combination with Levofloxacin.
Insulin degludec The therapeutic efficacy of Insulin degludec can be increased when used in combination with Levofloxacin.
Insulin peglispro The therapeutic efficacy of Insulin peglispro can be increased when used in combination with Levofloxacin.
Insulin tregopil The therapeutic efficacy of Insulin tregopil can be increased when used in combination with Levofloxacin.
Ipragliflozin The therapeutic efficacy of Ipragliflozin can be increased when used in combination with Levofloxacin.
Dutogliptin The therapeutic efficacy of Dutogliptin can be increased when used in combination with Levofloxacin.
Allicin The therapeutic efficacy of Allicin can be increased when used in combination with Levofloxacin.
Tofogliflozin The therapeutic efficacy of Tofogliflozin can be increased when used in combination with Levofloxacin.
2,4-thiazolidinedione The therapeutic efficacy of 2,4-thiazolidinedione can be increased when used in combination with Levofloxacin.
Teneligliptin The therapeutic efficacy of Teneligliptin can be increased when used in combination with Levofloxacin.
Omarigliptin The therapeutic efficacy of Omarigliptin can be increased when used in combination with Levofloxacin.
Carmegliptin The therapeutic efficacy of Carmegliptin can be increased when used in combination with Levofloxacin.
Gemigliptin The therapeutic efficacy of Gemigliptin can be increased when used in combination with Levofloxacin.
Anagliptin The therapeutic efficacy of Anagliptin can be increased when used in combination with Levofloxacin.
Evogliptin The therapeutic efficacy of Evogliptin can be increased when used in combination with Levofloxacin.
Sotagliflozin The therapeutic efficacy of Sotagliflozin can be increased when used in combination with Levofloxacin.
Balaglitazone The therapeutic efficacy of Balaglitazone can be increased when used in combination with Levofloxacin.
Remogliflozin etabonate The therapeutic efficacy of Remogliflozin etabonate can be increased when used in combination with Levofloxacin.
Carbutamide The therapeutic efficacy of Carbutamide can be increased when used in combination with Levofloxacin.
Guar gum The therapeutic efficacy of Guar gum can be increased when used in combination with Levofloxacin.
Metahexamide The therapeutic efficacy of Metahexamide can be increased when used in combination with Levofloxacin.
Semaglutide The therapeutic efficacy of Semaglutide can be increased when used in combination with Levofloxacin.
Taspoglutide The therapeutic efficacy of Taspoglutide can be increased when used in combination with Levofloxacin.

Target Protein

DNA gyrase subunit A gyrA
DNA gyrase subunit B gyrB
DNA gyrase subunit A gyrA
DNA topoisomerase 4 subunit A parC

Referensi & Sumber

Synthesis reference: Valerie Niddam-Hildesheim, "Preparation of levofloxacin and forms thereof." U.S. Patent US20030130507, issued July 10, 2003.
Artikel (PubMed)
  • PMID: 9068926
    Fish DN, Chow AT: The clinical pharmacokinetics of levofloxacin. Clin Pharmacokinet. 1997 Feb;32(2):101-19. doi: 10.2165/00003088-199732020-00002.
  • PMID: 27853934
    Giri P, Naidu S, Patel N, Patel H, Srinivas NR: Evaluation of In Vitro Cytochrome P450 Inhibition and In Vitro Fate of Structurally Diverse N-Oxide Metabolites: Case Studies with Clozapine, Levofloxacin, Roflumilast, Voriconazole and Zopiclone. Eur J Drug Metab Pharmacokinet. 2017 Aug;42(4):677-688. doi: 10.1007/s13318-016-0385-7.
  • PMID: 28550055
    Sato T, Mishima E, Mano N, Abe T, Yamaguchi H: Potential Drug Interactions Mediated by Renal Organic Anion Transporter OATP4C1. J Pharmacol Exp Ther. 2017 Aug;362(2):271-277. doi: 10.1124/jpet.117.241703. Epub 2017 May 26.
  • PMID: 27550354
    Parvez MM, Kaisar N, Shin HJ, Jung JA, Shin JG: Inhibitory Interaction Potential of 22 Antituberculosis Drugs on Organic Anion and Cation Transporters of the SLC22A Family. Antimicrob Agents Chemother. 2016 Oct 21;60(11):6558-6567. doi: 10.1128/AAC.01151-16. Print 2016 Nov.
  • PMID: 17274666
    Maeda T, Takahashi K, Ohtsu N, Oguma T, Ohnishi T, Atsumi R, Tamai I: Identification of influx transporter for the quinolone antibacterial agent levofloxacin. Mol Pharm. 2007 Jan-Feb;4(1):85-94. doi: 10.1021/mp060082j.
  • PMID: 22970772
    Nies AT, Damme K, Schaeffeler E, Schwab M: Multidrug and toxin extrusion proteins as transporters of antimicrobial drugs. Expert Opin Drug Metab Toxicol. 2012 Dec;8(12):1565-77. doi: 10.1517/17425255.2012.722996. Epub 2012 Sep 13.
  • PMID: 21261881
    Fabrega A, Madurga S, Giralt E, Vila J: Mechanism of action of and resistance to quinolones. Microb Biotechnol. 2009 Jan;2(1):40-61. doi: 10.1111/j.1751-7915.2008.00063.x. Epub 2008 Oct 13.
  • PMID: 15482135
    Fish DN: Levofloxacin: update and perspectives on one of the original 'respiratory quinolones'. Expert Rev Anti Infect Ther. 2003 Oct;1(3):371-87. doi: 10.1586/14787210.1.3.371.

Contoh Produk & Brand

Produk: 497 • International brands: 11
Produk
  • Act Levofloxacin
    Tablet • 250 mg • Oral • Canada • Approved
  • Act Levofloxacin
    Tablet • 500 mg • Oral • Canada • Approved
  • Act Levofloxacin
    Tablet • 750 mg • Oral • Canada • Approved
  • Apo-levofloxacin
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Apo-levofloxacin
    Tablet • 500 mg • Oral • Canada • Generic • Approved
  • Apo-levofloxacin
    Tablet • 750 mg • Oral • Canada • Generic • Approved
  • Auro-levofloxacin
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Auro-levofloxacin
    Tablet • 500 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 497 produk.
International Brands
  • Cravit
  • Elequine
  • Floxel
  • Leroxacin
  • Levokacin
  • Levox
  • Levoxacin
  • Mosardal
  • Nofaxin
  • Reskuin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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