Peringatan Keamanan

Patients experiencing an overdose may present with nausea, vomiting, abdominal pain, crystalluria, nephrotoxicity, and oliguria.A178954,A178957,A178960 Ciprofloxacin overdose typically leads to acute renal failure.A178960 An overdose may progress over the next 6 days with rising serum creatinine and BUN, as well as anuria.A178957 Patients may require prednisone therapy, urgent hemodialysis, or supportive therapy.A178954,A178960 Depending on the degree of overdose, patients may recover normal kidney function or progress to chronic kidney failure.A178960

The oral LD50 in rats is >2000mg/kg.L6529

Ciprofloxacin for intratympanic injection or otic use has low systemic absorption and so it unlikely to be a risk in pregnancy or lactation.L6493 There is generally no harm to the fetus in animal studies, however high doses may lead to gastrointestinal disturbances in the mother which may increase the incidence of abortion.L6490,L6472,L6484,L6475 In human studies there was no increase in fetal malformations above background rates.L6478,L6481 The risk and benefit of ciprofloxacin should be weighed in pregnancy and breast feeding.L6490,L6472,L6484,L6478,L6481,L6487,L6475,L6469

2/8 in vitro tests and 0/3 in vivo tests of mutagenicity of ciprofloxacin have yielded a positive result.L6493,L6490,L6472,L6484,L6478,L6481,L6487,L6475,L6469

Oral doses of 200 and 300 times the maximum recommended clinical dose in rats and mice have shown no carcinogenicity or tumorigenicity.L6493,L6472,L6484,L6478,L6481,L6487,L6475,L6469

Oral doses above the maximum recommended clinical dose have shown no effects on fertility in rats.L6493,L6484,L6478,L6481,L6487,L6475,L6469

Ciprofloxacin

DB00537

small molecule approved investigational

Deskripsi

Ciprofloxacin is a second generation fluoroquinolone that has spawned many derivative antibiotics.A178870 It is formulated for oral, intravenous, intratympanic, ophthalmic, and otic administration for a number of bacterial infections.L6469,L6472,L6475,L6478,L6481,L6484,L6487,L6490,L6493

The first ciprofloxacin containing product was FDA approved on 22 October 1987.L6463

Struktur Molekul 2D

Berat 331.3415
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The average half life following a 250mg oral dose was 4.71 hours and 3.65 hours following a 100mg intravenous dose.[A178858] Generally the half life is reported as 4 hours.[Label,A178858]
Volume Distribusi Cirpofloxacin follws a 3 compartment distribution model with a central compartment volume of 0.161L/kg[A178858] and a total volume of distribution of 2.00-3.04L/kg.[A178876]
Klirens (Clearance) The average renal clearance after a 250mg oral dose is 5.08mL/min\*kg.[A178858] Following a 100mg intravenous dose, the average total clearance is 9.62mL/min\*kg, average renal clearance is 4.42mL/min\*kg, and average non renal clearance is 5.21mL/min\*kg.[A178858]

Absorpsi

A 250mg oral dose of ciprofloxacin reaches an average maximum concentration of 0.94mg/L in 0.81 hours with an average area under the curve of 1.013L/h\*kg.A178858 The FDA reports an oral bioavailability of 70-80%Label,A820 while other studies report it to be approximately 60%.A178858 An early review of ciprofloxacin reported an oral bioavailability of 64-85% but recommends 70% for all practical uses.A178876

Metabolisme

Ciprofloxacin is primarily metabolized by CYP1A2.L6481 The primary metabolites oxociprofloxacin and sulociprofloxacin make up 3-8% of the total dose each.L6487 Ciprofloxacin is also converted to the minor metabolites desethylene ciprofloxacin and formylciprofloxacin.L6487 These 4 metabolites account for 15% of a total oral dose.L6481 There is a lack of available data on the enzymes and types of reactions involved in forming these metabolites.A178822,A178819,A178828,A178831

Rute Eliminasi

27% of an oral dose was recovered unmetabolized in urine compared to 46% of an intravenous dose.A178858 Collection of radiolabelled ciprofloxacin resulted in 45% recovery in urine and 62% recovery in feces.A178876

Interaksi Makanan

3 Data
  • 1. Avoid milk and dairy products. Dairy products and calcium fortified juices decrease the absorption of ciprofloxacin.
  • 2. Limit caffeine intake.
  • 3. Take with or without food. The absorption is not significantly affected by food.

Interaksi Obat

1872 Data
Brexpiprazole The metabolism of Brexpiprazole can be decreased when combined with Ciprofloxacin.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Ciprofloxacin.
Everolimus The metabolism of Everolimus can be decreased when combined with Ciprofloxacin.
Flibanserin The metabolism of Flibanserin can be decreased when combined with Ciprofloxacin.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Ciprofloxacin.
Ivabradine The metabolism of Ivabradine can be decreased when combined with Ciprofloxacin.
Ivacaftor The metabolism of Ivacaftor can be decreased when combined with Ciprofloxacin.
Lurasidone The metabolism of Lurasidone can be decreased when combined with Ciprofloxacin.
Naloxegol The metabolism of Naloxegol can be decreased when combined with Ciprofloxacin.
Olaparib The metabolism of Olaparib can be decreased when combined with Ciprofloxacin.
Ranolazine The metabolism of Ranolazine can be decreased when combined with Ciprofloxacin.
Sonidegib The metabolism of Sonidegib can be decreased when combined with Ciprofloxacin.
Avanafil The metabolism of Avanafil can be decreased when combined with Ciprofloxacin.
Eplerenone The metabolism of Eplerenone can be decreased when combined with Ciprofloxacin.
Didanosine Didanosine can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Probenecid Probenecid may decrease the excretion rate of Ciprofloxacin which could result in a higher serum level.
Quinapril Quinapril can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium acetate Calcium acetate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron Dextran Iron Dextran can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium Calcium can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Lanthanum carbonate Lanthanum carbonate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric carboxymaltose Ferric carboxymaltose can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Iron sucrose Iron sucrose can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric pyrophosphate Ferric pyrophosphate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium citrate Calcium citrate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium gluconate Calcium gluconate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric sulfate Ferric sulfate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric cation Ferric cation can cause a decrease in the absorption of Ciprofloxacin 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 Ciprofloxacin 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 Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Calcium polycarbophil Calcium polycarbophil can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Ferric oxyhydroxide Ferric oxyhydroxide can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sucralfate Sucralfate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Ciprofloxacin.
Colchicine The metabolism of Colchicine can be decreased when combined with Ciprofloxacin.
Fentanyl The metabolism of Fentanyl can be decreased when combined with Ciprofloxacin.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Ciprofloxacin.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Ciprofloxacin.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Ciprofloxacin.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Ciprofloxacin.
Eszopiclone The metabolism of Eszopiclone can be decreased when combined with Ciprofloxacin.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Ciprofloxacin.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Ciprofloxacin.
Zolmitriptan The metabolism of Zolmitriptan can be decreased when combined with Ciprofloxacin.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Ciprofloxacin.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Ciprofloxacin.
Carbamazepine The serum concentration of Carbamazepine can be increased when it is combined with Ciprofloxacin.
Erlotinib The serum concentration of Erlotinib can be increased when it is combined with Ciprofloxacin.
Methotrexate The serum concentration of Methotrexate can be increased when it is combined with Ciprofloxacin.
Phenytoin The therapeutic efficacy of Phenytoin can be decreased when used in combination with Ciprofloxacin.
Fosphenytoin The therapeutic efficacy of Fosphenytoin can be decreased when used in combination with Ciprofloxacin.
Pirfenidone The serum concentration of Pirfenidone can be increased when it is combined with Ciprofloxacin.
Roflumilast The serum concentration of Roflumilast can be increased when it is combined with Ciprofloxacin.
Spironolactone Spironolactone may increase the arrhythmogenic activities of Ciprofloxacin.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Ciprofloxacin.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Ciprofloxacin.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Ciprofloxacin.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Ciprofloxacin.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Ciprofloxacin.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Ciprofloxacin.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Ciprofloxacin.
Nitrofurantoin The therapeutic efficacy of Ciprofloxacin can be decreased when used in combination with Nitrofurantoin.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Ciprofloxacin.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Ciprofloxacin.
Picosulfuric acid The therapeutic efficacy of Picosulfuric acid can be decreased when used in combination with Ciprofloxacin.
Insulin human The therapeutic efficacy of Insulin human can be increased when used in combination with Ciprofloxacin.
Insulin lispro The therapeutic efficacy of Insulin lispro can be increased when used in combination with Ciprofloxacin.
Insulin pork The therapeutic efficacy of Insulin pork can be increased when used in combination with Ciprofloxacin.
Troglitazone The therapeutic efficacy of Troglitazone can be increased when used in combination with Ciprofloxacin.
Glimepiride The therapeutic efficacy of Glimepiride can be increased when used in combination with Ciprofloxacin.
Sulfisoxazole The therapeutic efficacy of Sulfisoxazole can be increased when used in combination with Ciprofloxacin.
Acarbose The therapeutic efficacy of Acarbose can be increased when used in combination with Ciprofloxacin.
Metformin The therapeutic efficacy of Metformin can be increased when used in combination with Ciprofloxacin.
Sulfadiazine The therapeutic efficacy of Sulfadiazine can be increased when used in combination with Ciprofloxacin.
Rosiglitazone The therapeutic efficacy of Rosiglitazone can be increased when used in combination with Ciprofloxacin.
Acetohexamide The therapeutic efficacy of Acetohexamide can be increased when used in combination with Ciprofloxacin.
Miglitol The therapeutic efficacy of Miglitol can be increased when used in combination with Ciprofloxacin.
Chlorpropamide The therapeutic efficacy of Chlorpropamide can be increased when used in combination with Ciprofloxacin.
Nateglinide The therapeutic efficacy of Nateglinide can be increased when used in combination with Ciprofloxacin.
Pentamidine The therapeutic efficacy of Pentamidine can be increased when used in combination with Ciprofloxacin.
Tolazamide The therapeutic efficacy of Tolazamide can be increased when used in combination with Ciprofloxacin.
Repaglinide The therapeutic efficacy of Repaglinide can be increased when used in combination with Ciprofloxacin.
Phenformin The therapeutic efficacy of Phenformin can be increased when used in combination with Ciprofloxacin.
Sulfamethoxazole The therapeutic efficacy of Sulfamethoxazole can be increased when used in combination with Ciprofloxacin.
Glipizide The therapeutic efficacy of Glipizide can be increased when used in combination with Ciprofloxacin.
Gliclazide The therapeutic efficacy of Gliclazide can be increased when used in combination with Ciprofloxacin.
Tolbutamide The therapeutic efficacy of Tolbutamide can be increased when used in combination with Ciprofloxacin.
Pioglitazone The therapeutic efficacy of Pioglitazone can be increased when used in combination with Ciprofloxacin.
Gliquidone The therapeutic efficacy of Gliquidone can be increased when used in combination with Ciprofloxacin.
Mitiglinide The therapeutic efficacy of Mitiglinide can be increased when used in combination with Ciprofloxacin.
Sitagliptin The therapeutic efficacy of Sitagliptin can be increased when used in combination with Ciprofloxacin.
Exenatide The therapeutic efficacy of Exenatide can be increased when used in combination with Ciprofloxacin.
Mecasermin The therapeutic efficacy of Mecasermin can be increased when used in combination with Ciprofloxacin.
Pramlintide The therapeutic efficacy of Pramlintide can be increased when used in combination with Ciprofloxacin.
Glisoxepide The therapeutic efficacy of Glisoxepide can be increased when used in combination with Ciprofloxacin.
Insulin aspart The therapeutic efficacy of Insulin aspart can be increased when used in combination with Ciprofloxacin.
Insulin glulisine The therapeutic efficacy of Insulin glulisine can be increased when used in combination with Ciprofloxacin.
Glymidine The therapeutic efficacy of Glymidine can be increased when used in combination with Ciprofloxacin.
AICA ribonucleotide The therapeutic efficacy of AICA ribonucleotide can be increased when used in combination with Ciprofloxacin.

Target Protein

DNA topoisomerase 4 subunit A parC
DNA gyrase subunit B gyrB
Thymidylate synthase TMP1
DNA gyrase subunit A gyrA
DNA gyrase subunit A gyrA
DNA topoisomerase 2-alpha TOP2A
Voltage-gated inwardly rectifying potassium channel KCNH2 KCNH2
DNA gyrase subunit A gyrA
DNA topoisomerase 4 subunit A parC
DNA topoisomerase 4 subunit B parE
DNA gyrase subunit A gyrA
Multidrug resistance protein MdtK mdtK
Gyrase A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 3777908
    Drusano GL, Standiford HC, Plaisance K, Forrest A, Leslie J, Caldwell J: Absolute oral bioavailability of ciprofloxacin. Antimicrob Agents Chemother. 1986 Sep;30(3):444-6.
  • PMID: 16628145
    van Geijlswijk IM, van Zanten AR, van der Meer YG: Reliable new high-performance liquid chromatographic method for the determination of ciprofloxacin in human serum. Ther Drug Monit. 2006 Apr;28(2):278-81. doi: 10.1097/01.ftd.0000189823.43236.90.
  • PMID: 30030566
    Rusch M, Spielmeyer A, Zorn H, Hamscher G: Biotransformation of ciprofloxacin by Xylaria longipes: structure elucidation and residual antibacterial activity of metabolites. Appl Microbiol Biotechnol. 2018 Oct;102(19):8573-8584. doi: 10.1007/s00253-018-9231-y. Epub 2018 Jul 21.
  • PMID: 1491053
    Mack G: Improved high-performance liquid chromatographic determination of ciprofloxacin and its metabolites in human specimens. J Chromatogr. 1992 Nov 6;582(1-2):263-7.
  • PMID: 7736911
    Abadia AR, De Francesco L, Guaitani A: Disposition of ciprofloxacin in the isolated perfused rat liver. Drug Metab Dispos. 1995 Feb;23(2):197-200.
  • PMID: -
    Takács-Novák K, Józan M, Szász H: Lipophilicity of antibacterial fluoroquinolones International Journal of Pharmaceutics. 1992 Feb 1;79(1-3):89-96.
  • PMID: -
    Torniainen K, Tammilehto S, Ulvi V: The effect of pH, buffer type and drug concentration on the photodegradation of ciprofloxacin International Journal of Pharmaceutics. 1996 Apr 30;132(1):53-61.
  • PMID: 6489326
    Wingender W, Graefe KH, Gau W, Forster D, Beermann D, Schacht P: Pharmacokinetics of ciprofloxacin after oral and intravenous administration in healthy volunteers. Eur J Clin Microbiol. 1984 Aug;3(4):355-9.
Menampilkan 8 dari 16 artikel.

Contoh Produk & Brand

Produk: 809 • International brands: 12
Produk
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    Tablet • 250 mg • Oral • Canada • Approved
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    Tablet • 500 mg • Oral • Canada • Approved
  • Act Ciprofloxacin
    Tablet • 750 mg • Oral • Canada • Approved
  • Ag-ciprofloxacin
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Ag-ciprofloxacin
    Tablet • 500 mg • Oral • Canada • Generic • Approved
  • Ag-ciprofloxacin
    Tablet • 750 mg • Oral • Canada • Generic • Approved
  • Apo-ciproflox
    Tablet • 250 mg • Oral • Canada • Generic • Approved
  • Apo-ciproflox
    Tablet • 500 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 809 produk.
International Brands
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  • Ciproxin

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