Peringatan Keamanan

The most common adverse reactions noted with Delafloxacin were nausea (8%), diarrhea (8%), headache (3%), transaminase elevations (3%), and vomiting (2%) FDA Label. Fluoroquinolones are associated with increased frequency of tendon rupture and tendonitis, increased risk of peipheral neuropathy, excacerbation of myasthenia gravis, and development of Clostridium difficile-associated diarrhea. Fluoroquinolones are also associated with an increased risk of central nervous system reactions (CNS), including: convulsions and increased intracranial pressure (including pseudotumor cerebri) and toxic psychosis. Fluoroquinolones may also cause CNS reactions of nervousness, agitation, insomnia, anxiety, nightmares, paranoia, dizziness, confusion, tremors, hallucinations, depression, and suicidal thoughts or acts.

Delafloxacin

DB11943

small molecule approved investigational

Deskripsi

Delafloxacin is a fluoroquinolone antibiotic which has been used in trials studying the treatment and basic science of Gonorrhea, Hepatic Impairment, Bacterial Skin Diseases, Skin Structure Infections, and Community Acquired Pneumonia, among others. It was approved in June 2017 under the trade name Baxdela for use in the treatment of acute bacterial skin and skin structure infections.

Struktur Molekul 2D

Berat 440.76
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean half life of elimination of Delafloxacin is 3.7 hours after a single intravenous administration [FDA Label]. The mean half life of elimination for multple oral administrations is 4.2-8.5 hours.
Volume Distribusi The steady sate volume of distrubution of Delafloxacin is 30-48 liters [FDA Label].
Klirens (Clearance) The mean total clearance of Delafloxacin is 16.3 liters per hour [FDA Label]. Renal clearance accounts for 35-45% of total clearance.

Absorpsi

The median time to peak plasma concentration for orally administered Delafloxacin is 0.75 (0.5-4.0) hours after a single dose and 1.00 (0.5-6.0) hours for steady state dosing FDA Label. The median time to peak plasma concentration for intravenously administered Delafloxacin is 1.00 (1.0-1.2) hours for a single dose and 1.0 (1.0-1.0) hour for steady state dosing. The absolute bioavailability for orally administed Delafloxacin is 58.8%.

Metabolisme

Delafoxacin is primarily metabolized via glucuronidation mediated by UDP glucuronosyltransferase 1-1, UDP-glucuronosyltransferase 1-3, and UDP-glucuronosyltransferase 2B15 FDA Label. Less than 1% is metabolized via oxidation.

Rute Eliminasi

After a single intravenous dose, 65% of Delafloxacin was excreted in the urine either unchanged or as glucuronide metabolites with 28% excreted unchanged in the feces FDA Label. After a single oral dose, 50% of Delafloxacin was excreted in the urine either unchanged or as glucuronide metabolites with 48% excreted unchanged in the feces.

Interaksi Makanan

3 Data
  • 1. Avoid multivalent ions. Separate the administration of multivalent cations from delafloxacin by at least 6 hours before or 2 hours after delafloxacin.
  • 2. Take separate from antacids. The administration of antacids should be separated from delafloxacin by at least 6 hours before or 2 hours after delafloxacin.
  • 3. Take with or without food.

Interaksi Obat

1558 Data
Aripiprazole The metabolism of Aripiprazole can be increased when combined with Delafloxacin.
Aripiprazole lauroxil The metabolism of Aripiprazole lauroxil can be increased when combined with Delafloxacin.
Didanosine Didanosine can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Probenecid Probenecid may decrease the excretion rate of Delafloxacin which could result in a higher serum level.
Quinapril Quinapril can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium acetate Calcium acetate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Dextran Iron Dextran can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium Calcium can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium carbonate Calcium carbonate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum carbonate Lanthanum carbonate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric carboxymaltose Ferric carboxymaltose can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose Iron sucrose can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate Ferric pyrophosphate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium citrate Calcium citrate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium gluconate Calcium gluconate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate Ferric sulfate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation Ferric cation can cause a decrease in the absorption of Delafloxacin 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 Delafloxacin 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 Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium polycarbophil Calcium polycarbophil can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide Ferric oxyhydroxide can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sucralfate Sucralfate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ifosfamide The metabolism of Ifosfamide can be increased when combined with Delafloxacin.
Perampanel The metabolism of Perampanel can be increased when combined with Delafloxacin.
Warfarin The metabolism of Warfarin can be increased when combined with Delafloxacin.
Acenocoumarol The metabolism of Acenocoumarol can be increased when combined with Delafloxacin.
(R)-warfarin The metabolism of (R)-warfarin can be increased when combined with Delafloxacin.
R,S-Warfarin alcohol The metabolism of R,S-Warfarin alcohol can be increased when combined with Delafloxacin.
S,R-Warfarin alcohol The metabolism of S,R-Warfarin alcohol can be increased when combined with Delafloxacin.
(S)-Warfarin The metabolism of (S)-Warfarin can be increased when combined with Delafloxacin.
Nitrofurantoin The therapeutic efficacy of Delafloxacin can be decreased when used in combination with Nitrofurantoin.
Nelfinavir The metabolism of Delafloxacin can be increased when combined with Nelfinavir.
Zidovudine The metabolism of Delafloxacin can be increased when combined with Zidovudine.
Ritonavir The metabolism of Delafloxacin can be increased when combined with Ritonavir.
Lamotrigine The metabolism of Delafloxacin can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Delafloxacin can be increased when combined with Efavirenz.
Primidone The metabolism of Delafloxacin can be increased when combined with Primidone.
Ethinylestradiol The metabolism of Delafloxacin can be increased when combined with Ethinylestradiol.
Testosterone propionate The metabolism of Delafloxacin can be increased when combined with Testosterone propionate.
Rifampin The metabolism of Delafloxacin can be increased when combined with Rifampicin.
Desogestrel The metabolism of Delafloxacin can be increased when combined with Desogestrel.
Tipranavir The metabolism of Delafloxacin can be increased when combined with Tipranavir.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Delafloxacin.
Insulin human The therapeutic efficacy of Insulin human can be increased when used in combination with Delafloxacin.
Insulin lispro The therapeutic efficacy of Insulin lispro can be increased when used in combination with Delafloxacin.
Insulin pork The therapeutic efficacy of Insulin pork can be increased when used in combination with Delafloxacin.
Troglitazone The therapeutic efficacy of Troglitazone can be increased when used in combination with Delafloxacin.
Glimepiride The therapeutic efficacy of Glimepiride can be increased when used in combination with Delafloxacin.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be increased when used in combination with Delafloxacin.
Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Delafloxacin.
Metformin The therapeutic efficacy of Metformin can be increased when used in combination with Delafloxacin.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be increased when used in combination with Delafloxacin.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Delafloxacin.
Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Delafloxacin.
Miglitol The therapeutic efficacy of Miglitol can be increased when used in combination with Delafloxacin.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Delafloxacin.
Nateglinide The therapeutic efficacy of Nateglinide can be increased when used in combination with Delafloxacin.
Pentamidine The therapeutic efficacy of Pentamidine can be increased when used in combination with Delafloxacin.
Tolazamide The therapeutic efficacy of Tolazamide can be increased when used in combination with Delafloxacin.
Repaglinide The therapeutic efficacy of Repaglinide can be increased when used in combination with Delafloxacin.
Phenformin The therapeutic efficacy of Phenformin can be increased when used in combination with Delafloxacin.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be increased when used in combination with Delafloxacin.
Glyburide The therapeutic efficacy of Glyburide can be increased when used in combination with Delafloxacin.
Glipizide The therapeutic efficacy of Glipizide can be increased when used in combination with Delafloxacin.
Gliclazide The therapeutic efficacy of Gliclazide can be increased when used in combination with Delafloxacin.
Tolbutamide The therapeutic efficacy of Tolbutamide can be increased when used in combination with Delafloxacin.
Pioglitazone The therapeutic efficacy of Pioglitazone can be increased when used in combination with Delafloxacin.
Gliquidone The therapeutic efficacy of Gliquidone can be increased when used in combination with Delafloxacin.
Mitiglinide The therapeutic efficacy of Mitiglinide can be increased when used in combination with Delafloxacin.
Sitagliptin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Delafloxacin.
Sunitinib The therapeutic efficacy of Sunitinib can be increased when used in combination with Delafloxacin.
Exenatide The therapeutic efficacy of Exenatide can be increased when used in combination with Delafloxacin.
Mecasermin The therapeutic efficacy of Mecasermin can be increased when used in combination with Delafloxacin.
Pramlintide The therapeutic efficacy of Pramlintide can be increased when used in combination with Delafloxacin.
Glisoxepide The therapeutic efficacy of Glisoxepide can be increased when used in combination with Delafloxacin.
Insulin aspart The therapeutic efficacy of Insulin aspart can be increased when used in combination with Delafloxacin.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be increased when used in combination with Delafloxacin.
Glymidine The therapeutic efficacy of Glymidine can be increased when used in combination with Delafloxacin.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be increased when used in combination with Delafloxacin.
Buformin The therapeutic efficacy of Buformin can be increased when used in combination with Delafloxacin.
Vildagliptin The therapeutic efficacy of Vildagliptin can be increased when used in combination with Delafloxacin.
Voglibose The therapeutic efficacy of Voglibose can be increased when used in combination with Delafloxacin.
NN344 The therapeutic efficacy of NN344 can be increased when used in combination with Delafloxacin.
AMG-222 The therapeutic efficacy of AMG-222 can be increased when used in combination with Delafloxacin.
Bisegliptin The therapeutic efficacy of Bisegliptin can be increased when used in combination with Delafloxacin.
Alogliptin The therapeutic efficacy of Alogliptin can be increased when used in combination with Delafloxacin.
Dapagliflozin The therapeutic efficacy of Dapagliflozin can be increased when used in combination with Delafloxacin.
Saxagliptin The therapeutic efficacy of Saxagliptin can be increased when used in combination with Delafloxacin.
Liraglutide The therapeutic efficacy of Liraglutide can be increased when used in combination with Delafloxacin.
Gosogliptin The therapeutic efficacy of Gosogliptin can be increased when used in combination with Delafloxacin.
Linagliptin The therapeutic efficacy of Linagliptin can be increased when used in combination with Delafloxacin.
Canagliflozin The therapeutic efficacy of Canagliflozin can be increased when used in combination with Delafloxacin.
Glibornuride The therapeutic efficacy of Glibornuride can be increased when used in combination with Delafloxacin.
Benfluorex The therapeutic efficacy of Benfluorex can be increased when used in combination with Delafloxacin.
Empagliflozin The therapeutic efficacy of Empagliflozin can be increased when used in combination with Delafloxacin.
Albiglutide The therapeutic efficacy of Albiglutide can be increased when used in combination with Delafloxacin.
Dulaglutide The therapeutic efficacy of Dulaglutide can be increased when used in combination with Delafloxacin.
Lobeglitazone The therapeutic efficacy of Lobeglitazone can be increased when used in combination with Delafloxacin.
Netoglitazone The therapeutic efficacy of Netoglitazone can be increased when used in combination with Delafloxacin.

Target Protein

DNA topoisomerase 4 subunit A parC
DNA gyrase subunit A gyrA

Referensi & Sumber

Textbook
  • ISBN: 978-0-7020-3471-8
    49. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 612-614). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 9 • International brands: 0
Produk
  • Baxdela
    Tablet • 450 mg/1 • Oral • US • Approved
  • Baxdela
    Injection, powder, lyophilized, for solution • 300 mg/10.5mL • Intravenous • US • Approved
  • Quofenix
    Injection, powder, for solution • 300 mg • Intravenous • EU • Approved
  • Quofenix
    Tablet • 450 mg • Oral • EU • Approved
  • Quofenix
    Tablet • 450 mg • Oral • EU • Approved
  • Quofenix
    Tablet • 450 mg • Oral • EU • Approved
  • Quofenix
    Tablet • 450 mg • Oral • EU • Approved
  • Quofenix
    Tablet • 450 mg • Oral • EU • Approved
Menampilkan 8 dari 9 produk.

Sekuens Gen/Protein (FASTA)

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