Peringatan Keamanan

The oral LD50 of phenazopyridine in rats is 472 mg/kg.L7847

Overdose information

Administering excess phenazopyridine above the daily recommended dose in those with healthy or impaired kidney function may increase the drug concentration and predispose the patient to toxicity. When a large overdose occurs, methemoglobinemia results.A182141,A182144 To treat this condition, Methylene blue at 1 to 2 mg/kg/dose should be administered intravenously as a 1% solution as deemed necessary. Its administration is likely to cause a rapid reduction of the methemoglobinemia state and relieve the associated cyanosis. Hemolytic anemia is also a risk when an overdose occurs, and “bite cells” may be observed in a blood smear after an overdose with phenazopyridine. Red blood cell G6PD deficiency may increase the risk of hemolysis, and even normal doses can lead to methemoglobinemia in patients with this condition. Nephrotoxicity, renal failure, and hepatic impairment may also occur in a case of overdose with this drug. Administer symptomatic and supportive treatment as necessary.A182138,A182147,L7844

Phenazopyridine

DB01438

small molecule approved

Deskripsi

Phenazopyridine, also known as Pyridium, is a urinary tract analgesic used for the short-term management of urinary tract irritation and its associated unpleasant symptoms such as burning and pain during urination. In the USA, this drug was previously marked by Roche but has been discontinued by the FDA.L7832 It is still used in various parts of the world. Ingestion of phenazopyridine is found to change the appearance of the urine by imparting an orange or red color, as it is considered an azo dye.L7829

Struktur Molekul 2D

Berat 213.2385
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The mean elimination half-life of phenazopyridine is 7.35 hours in rats with healthy renal function.[A182174] The half-life in man is not readily vailable in the literature.
Volume Distribusi Small, trace quantities of phenazopyridine are thought to cross the placenta and the blood-brain barrier, reaching cerebrospinal fluid.[L7829] A pharmacokinetic study in rats determined that phenazopyridine metabolites were present in high levels in the kidney and liver.[A182174]
Klirens (Clearance) This drug is rapidly excreted by the kidneys, up to 65% of a dose administered orally may be excreted as unchanged drug in the urine. The clearance of phenazopyridine may be decreased with impaired renal or hepatic function and is contraindicated in these conditions.[L7826]

Absorpsi

Phenazopyridine is absorbed in the gastrointestinal tract.A182159,L7850 The mean Cmax is 65.00 ± 29.23 ng/mL, the mean Tmax is 2.48 ± 0.50 h, and the mean AUC(0 – ?)is 431.77 ± 87.82 ng.h/mL.A182171

Metabolisme

Phenazopyridine is metabolized in the liver, and acetaminophen has been discovered to be one metabolite of this drug.L7829 Hydroxylation is a pathway by which this drug is metabolized.A182180 In humans, 5-hydroxyl PAP is the major metabolite (48.3% of the dose) and small amounts of other hydroxy metabolites are produced.A182171,L7865 The metabolism of phenazopyridine produces aniline, which is likely associated with methemoglobinemia in some patients or in the case of an overdose. This dye accumulates in the skin, and yellow skin pigmentation has been observed when high doses of this drug have been taken.L7826 Triaminopyridine is also a metabolite of phenazopyridine.L7865 During a pharmacokinetic study, aniline contributed to approximately 6.9% of urinary metabolites. N acetyl-p-aminophenol (acetaminophen) contributes to about 18%, P-aminophenol (PAP) contributes 24%, and finally, DPP (unchanged phenazopyridine) contributes to about 41% of excreted urinary metabolites.A182159

Rute Eliminasi

Up to 65% of an oral phenazopyridine dose is quickly excreted by the kidneys as unchanged drug measured in the urine.L7829 The pharmacokinetics of this drug have not been evaluated in depth in man. In a small group of healthy research volunteers, 90% of a daily 600 mg oral dose of phenazopyridine hydrochloride was found to be excreted within 1 day, with 41% as unchanged drug and 49% as phenazopyridine metabolites.L7826 Another study in humans determined that 80.07 ± 4.54 percent of the dose was cleared in the urine within 48 hours of administration.A182156 In rats, biliary excretion was high, with 40.7% of a dose excreted in 8 hours.A182174

Interaksi Makanan

1 Data
  • 1. Take with food. Food reduces irritation.

Interaksi Obat

760 Data
Prilocaine The risk or severity of methemoglobinemia can be increased when Phenazopyridine is combined with Prilocaine.
Foscarnet The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Foscarnet.
Mannitol The risk or severity of nephrotoxicity can be increased when Mannitol is combined with Phenazopyridine.
Tenofovir disoproxil Phenazopyridine may increase the nephrotoxic activities of Tenofovir disoproxil.
Tenofovir alafenamide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Phenazopyridine.
Tenofovir Phenazopyridine may increase the nephrotoxic activities of Tenofovir.
Dapsone The risk or severity of methemoglobinemia can be increased when Dapsone is combined with Phenazopyridine.
Cyclosporine The risk or severity of nephrotoxicity can be increased when Cyclosporine is combined with Phenazopyridine.
Icosapent The risk or severity of nephrotoxicity can be increased when Icosapent is combined with Phenazopyridine.
Cefotiam The risk or severity of nephrotoxicity can be increased when Cefotiam is combined with Phenazopyridine.
Mesalazine The risk or severity of nephrotoxicity can be increased when Mesalazine is combined with Phenazopyridine.
Cefmenoxime The risk or severity of nephrotoxicity can be increased when Cefmenoxime is combined with Phenazopyridine.
Cefmetazole The risk or severity of nephrotoxicity can be increased when Cefmetazole is combined with Phenazopyridine.
Pamidronic acid The risk or severity of nephrotoxicity can be increased when Pamidronic acid is combined with Phenazopyridine.
Indomethacin The risk or severity of nephrotoxicity can be increased when Indomethacin is combined with Phenazopyridine.
Cidofovir The risk or severity of nephrotoxicity can be increased when Cidofovir is combined with Phenazopyridine.
Triamterene The risk or severity of nephrotoxicity can be increased when Triamterene is combined with Phenazopyridine.
Cefpiramide The risk or severity of nephrotoxicity can be increased when Cefpiramide is combined with Phenazopyridine.
Ceftazidime The risk or severity of nephrotoxicity can be increased when Ceftazidime is combined with Phenazopyridine.
Loracarbef The risk or severity of nephrotoxicity can be increased when Loracarbef is combined with Phenazopyridine.
Cefalotin The risk or severity of nephrotoxicity can be increased when Cefalotin is combined with Phenazopyridine.
Nabumetone The risk or severity of nephrotoxicity can be increased when Nabumetone is combined with Phenazopyridine.
Ketorolac The risk or severity of nephrotoxicity can be increased when Ketorolac is combined with Phenazopyridine.
Tenoxicam The risk or severity of nephrotoxicity can be increased when Tenoxicam is combined with Phenazopyridine.
Cefotaxime The risk or severity of nephrotoxicity can be increased when Cefotaxime is combined with Phenazopyridine.
Tolmetin The risk or severity of nephrotoxicity can be increased when Tolmetin is combined with Phenazopyridine.
Rofecoxib The risk or severity of nephrotoxicity can be increased when Rofecoxib is combined with Phenazopyridine.
Piroxicam The risk or severity of nephrotoxicity can be increased when Piroxicam is combined with Phenazopyridine.
Methotrexate The risk or severity of nephrotoxicity can be increased when Methotrexate is combined with Phenazopyridine.
Cephalexin The risk or severity of nephrotoxicity can be increased when Cephalexin is combined with Phenazopyridine.
Fenoprofen The risk or severity of nephrotoxicity can be increased when Fenoprofen is combined with Phenazopyridine.
Valaciclovir The risk or severity of nephrotoxicity can be increased when Valaciclovir is combined with Phenazopyridine.
Valdecoxib The risk or severity of nephrotoxicity can be increased when Valdecoxib is combined with Phenazopyridine.
Diclofenac The risk or severity of nephrotoxicity can be increased when Diclofenac is combined with Phenazopyridine.
Sulindac The risk or severity of nephrotoxicity can be increased when Sulindac is combined with Phenazopyridine.
Bacitracin The risk or severity of nephrotoxicity can be increased when Bacitracin is combined with Phenazopyridine.
Amphotericin B The risk or severity of nephrotoxicity can be increased when Amphotericin B is combined with Phenazopyridine.
Cephaloglycin The risk or severity of nephrotoxicity can be increased when Cephaloglycin is combined with Phenazopyridine.
Furosemide The risk or severity of nephrotoxicity can be increased when Furosemide is combined with Phenazopyridine.
Flurbiprofen The risk or severity of nephrotoxicity can be increased when Flurbiprofen is combined with Phenazopyridine.
Adefovir dipivoxil The risk or severity of nephrotoxicity can be increased when Adefovir dipivoxil is combined with Phenazopyridine.
Pentamidine The risk or severity of nephrotoxicity can be increased when Pentamidine is combined with Phenazopyridine.
Etodolac The risk or severity of nephrotoxicity can be increased when Etodolac is combined with Phenazopyridine.
Mefenamic acid The risk or severity of nephrotoxicity can be increased when Mefenamic acid is combined with Phenazopyridine.
Acyclovir The risk or severity of nephrotoxicity can be increased when Acyclovir is combined with Phenazopyridine.
Naproxen The risk or severity of nephrotoxicity can be increased when Naproxen is combined with Phenazopyridine.
Phenylbutazone The risk or severity of nephrotoxicity can be increased when Phenylbutazone is combined with Phenazopyridine.
Meloxicam The risk or severity of nephrotoxicity can be increased when Meloxicam is combined with Phenazopyridine.
Carprofen The risk or severity of nephrotoxicity can be increased when Carprofen is combined with Phenazopyridine.
Cefaclor The risk or severity of nephrotoxicity can be increased when Cefaclor is combined with Phenazopyridine.
Diflunisal The risk or severity of nephrotoxicity can be increased when Diflunisal is combined with Phenazopyridine.
Tacrolimus The risk or severity of nephrotoxicity can be increased when Tacrolimus is combined with Phenazopyridine.
Bumetanide The risk or severity of nephrotoxicity can be increased when Bumetanide is combined with Phenazopyridine.
Etacrynic acid The risk or severity of nephrotoxicity can be increased when Etacrynic acid is combined with Phenazopyridine.
Ceforanide The risk or severity of nephrotoxicity can be increased when Ceforanide is combined with Phenazopyridine.
Salicylic acid The risk or severity of nephrotoxicity can be increased when Salicylic acid is combined with Phenazopyridine.
Meclofenamic acid The risk or severity of nephrotoxicity can be increased when Meclofenamic acid is combined with Phenazopyridine.
Acetylsalicylic acid The risk or severity of nephrotoxicity can be increased when Acetylsalicylic acid is combined with Phenazopyridine.
Carboplatin The risk or severity of nephrotoxicity can be increased when Carboplatin is combined with Phenazopyridine.
Oxaprozin The risk or severity of nephrotoxicity can be increased when Oxaprozin is combined with Phenazopyridine.
Hydrochlorothiazide The risk or severity of nephrotoxicity can be increased when Hydrochlorothiazide is combined with Phenazopyridine.
Ketoprofen The risk or severity of nephrotoxicity can be increased when Ketoprofen is combined with Phenazopyridine.
Balsalazide The risk or severity of nephrotoxicity can be increased when Balsalazide is combined with Phenazopyridine.
Ibuprofen The risk or severity of nephrotoxicity can be increased when Ibuprofen is combined with Phenazopyridine.
Cefditoren The risk or severity of nephrotoxicity can be increased when Cefditoren is combined with Phenazopyridine.
Atazanavir The risk or severity of nephrotoxicity can be increased when Atazanavir is combined with Phenazopyridine.
Colistimethate The risk or severity of nephrotoxicity can be increased when Colistimethate is combined with Phenazopyridine.
Cefuroxime The risk or severity of nephrotoxicity can be increased when Cefuroxime is combined with Phenazopyridine.
Cefapirin The risk or severity of nephrotoxicity can be increased when Cefapirin is combined with Phenazopyridine.
Cefadroxil The risk or severity of nephrotoxicity can be increased when Cefadroxil is combined with Phenazopyridine.
Cefprozil The risk or severity of nephrotoxicity can be increased when Cefprozil is combined with Phenazopyridine.
Ceftriaxone The risk or severity of nephrotoxicity can be increased when Ceftriaxone is combined with Phenazopyridine.
Olsalazine The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Olsalazine.
Lumiracoxib The risk or severity of nephrotoxicity can be increased when Lumiracoxib is combined with Phenazopyridine.
Cefamandole The risk or severity of nephrotoxicity can be increased when Cefamandole is combined with Phenazopyridine.
Cefazolin The risk or severity of nephrotoxicity can be increased when Cefazolin is combined with Phenazopyridine.
Cefonicid The risk or severity of nephrotoxicity can be increased when Cefonicid is combined with Phenazopyridine.
Cefoperazone The risk or severity of nephrotoxicity can be increased when Cefoperazone is combined with Phenazopyridine.
Cefotetan The risk or severity of nephrotoxicity can be increased when Cefotetan is combined with Phenazopyridine.
Cefoxitin The risk or severity of nephrotoxicity can be increased when Cefoxitin is combined with Phenazopyridine.
Ceftizoxime The risk or severity of nephrotoxicity can be increased when Ceftizoxime is combined with Phenazopyridine.
Cefradine The risk or severity of nephrotoxicity can be increased when Cefradine is combined with Phenazopyridine.
Magnesium salicylate The risk or severity of nephrotoxicity can be increased when Magnesium salicylate is combined with Phenazopyridine.
Salsalate The risk or severity of nephrotoxicity can be increased when Salsalate is combined with Phenazopyridine.
Choline magnesium trisalicylate The risk or severity of nephrotoxicity can be increased when Choline magnesium trisalicylate is combined with Phenazopyridine.
Cefepime The risk or severity of nephrotoxicity can be increased when Cefepime is combined with Phenazopyridine.
Cefacetrile The risk or severity of nephrotoxicity can be increased when Cefacetrile is combined with Phenazopyridine.
Ceftibuten The risk or severity of nephrotoxicity can be increased when Ceftibuten is combined with Phenazopyridine.
Cefpodoxime The risk or severity of nephrotoxicity can be increased when Cefpodoxime is combined with Phenazopyridine.
Antrafenine The risk or severity of nephrotoxicity can be increased when Antrafenine is combined with Phenazopyridine.
Aminophenazone The risk or severity of nephrotoxicity can be increased when Aminophenazone is combined with Phenazopyridine.
Tiaprofenic acid The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Tiaprofenic acid.
Lopinavir The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Lopinavir.
Etoricoxib The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Etoricoxib.
Hydrolyzed Cephalothin The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Hydrolyzed Cephalothin.
Cephalothin Group The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Cephalothin Group.
Oxyphenbutazone The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Oxyphenbutazone.
Latamoxef The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Latamoxef.
Nimesulide The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Nimesulide.
Benoxaprofen The risk or severity of nephrotoxicity can be increased when Phenazopyridine is combined with Benoxaprofen.

Target Protein

Sodium channel protein type 1 subunit alpha SCN1A
Group A nerve fibers

Referensi & Sumber

Artikel (PubMed)
  • PMID: 31006341
    Shore SN, Britnell SR, Brown JN: Safety analysis of long-term phenazopyridine use for radiation cystitis. J Oncol Pharm Pract. 2019 Apr 22:1078155219842646. doi: 10.1177/1078155219842646.
  • PMID: 20196783
    Suter DM, Preynat-Seauve O, Tirefort D, Feki A, Krause KH: Phenazopyridine induces and synchronizes neuronal differentiation of embryonic stem cells. J Cell Mol Med. 2009 Sep;13(9B):3517-27. doi: 10.1111/j.1582-4934.2009.00660.x.
  • PMID: 29501712
    Rehfuss A, Mahon J, Sorokin I, Smith C, Stein BS: Phenazopyridine: A Preoperative Way to Identify Ureteral Orifices. Urology. 2018 May;115:36-38. doi: 10.1016/j.urology.2018.02.023. Epub 2018 Mar 1.
  • PMID: 16897003
    Onder AM, Espinoza V, Berho ME, Chandar J, Zilleruelo G, Abitbol C: Acute renal failure due to phenazopyridine (Pyridium) overdose: case report and review of the literature. Pediatr Nephrol. 2006 Nov;21(11):1760-4. doi: 10.1007/s00467-006-0196-1. Epub 2006 Aug 1.
  • PMID: 12901999
    Gold NA, Bithoney WG: Methemoglobinemia due to ingestion of at most three pills of pyridium in a 2-year-old: case report and review. J Emerg Med. 2003 Aug;25(2):143-8.
  • PMID: 31179913
    Murphy T, Fernandez M: Acquired methemoglobinemia from phenazopyridine use. Int J Emerg Med. 2018 Nov 12;11(1):45. doi: 10.1186/s12245-018-0208-5.
  • PMID: 25516057
    Chang LC, Kuo CW, Chau T, Lin SH: Phenazopyridine-induced hemolytic anemia in advanced kidney disease. J Am Geriatr Soc. 2014 Dec;62(12):2464-6. doi: 10.1111/jgs.13161.
  • PMID: 20976818
    Aizawa N, Wyndaele JJ: Effects of phenazopyridine on rat bladder primary afferent activity, and comparison with lidocaine and acetaminophen. Neurourol Urodyn. 2010 Nov;29(8):1445-50. doi: 10.1002/nau.20886.
Menampilkan 8 dari 13 artikel.

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Sekuens Gen/Protein (FASTA)

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