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phenazopyridine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 2120 | 94-78-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A local anesthetic that has been used in urinary tract disorders. Its use is limited by problems with toxicity (primarily blood disorders) and potential carcinogenicity.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.60 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 45.76 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
| EoM (Fraction excreted unchanged in urine) | 41 % | Hosey CM, Chan R, Benet LZ |
| S (Water solubility) | 0.03 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 60 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.316 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 0.356 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 42.462 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 32.509 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 5.680 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 21.630 | % | High | 1 |
| herg | hERG pIC50 | 4.895 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.808 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 23.878 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 6.890 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,ALK,AURKA,AURKB,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK1,CDK4,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EIF2AK3,EPHA2,EPHB4,ERBB2,FLT3,GRK2,GRK3,GSK3B,IKBKB,ITK,JAK1,JAK2,JAK3,KIT,MAP2K1,MAP2K6,MAP3K1,MAP3K10,MAP3K11,MAP3K14,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAPK1,MAPK10,MAPK12,MAPK7,MAPK8,MAPK9,MAPKAPK2,MAPKAPK5,MARK4,MELK,MET,MTOR,NTRK2,PAK4,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PLK1,PRKCD,PRKDC,SGK1,SIK2,SIK3,STK10,STK33,SYK,TEK,TGFBR1,TTK,ULK1,ULK2,ZAP70 | 82 | |||
| kinase-selectivity-class | ACVR2A,ACVR2B,AURKA,AXL,CDK4,DYRK1B,EPHB4,ERBB2,GRK2,IKBKB,MAP2K3,MAP2K6,MAP3K7,MAPK12,MAPK7,MAPK8,SIK2,STK33,SYK,TEK,TTK | 21 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 0.482 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 140.929 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 10.030 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 0.270 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 10.190 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 82.794 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 65.110 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 10.380 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 170.216 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| June 26, 2001 | FDA | ABLE |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Sulphaemoglobinaemia | 252.15 | 16.60 | 41 | 5455 | 492 | 90622459 |
| Methaemoglobinaemia | 243.62 | 16.60 | 55 | 5441 | 3960 | 90618991 |
| Urinary tract infection | 103.40 | 16.60 | 109 | 5387 | 305523 | 90317428 |
| Anaemia Heinz body | 52.27 | 16.60 | 6 | 5490 | 0 | 90622951 |
| Cystitis | 44.65 | 16.60 | 35 | 5461 | 66683 | 90556268 |
| Drug hypersensitivity | 42.01 | 16.60 | 89 | 5407 | 463520 | 90159431 |
| Dysuria | 36.13 | 16.60 | 25 | 5471 | 39376 | 90583575 |
| Haemolytic anaemia | 34.59 | 16.60 | 16 | 5480 | 11681 | 90611270 |
| Nephrolithiasis | 33.38 | 16.60 | 26 | 5470 | 49059 | 90573892 |
| Emotional distress | 30.68 | 16.60 | 22 | 5474 | 36640 | 90586311 |
| Anticholinergic syndrome | 27.09 | 16.60 | 9 | 5487 | 2734 | 90620217 |
| Micturition urgency | 26.03 | 16.60 | 13 | 5483 | 11220 | 90611731 |
| Mydriasis | 25.19 | 16.60 | 14 | 5482 | 14998 | 90607953 |
| Urinary retention | 23.53 | 16.60 | 19 | 5477 | 37725 | 90585226 |
| Respiratory alkalosis | 21.37 | 16.60 | 8 | 5488 | 3440 | 90619511 |
| Product dose omission issue | 20.79 | 16.60 | 51 | 5445 | 291636 | 90331315 |
| Uterine perforation | 18.27 | 16.60 | 9 | 5487 | 7545 | 90615406 |
| Hypoxia | 17.87 | 16.60 | 22 | 5474 | 72377 | 90550574 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Methaemoglobinaemia | 98.94 | 25.99 | 25 | 1294 | 5749 | 42614267 |
| Anticholinergic syndrome | 54.07 | 25.99 | 12 | 1307 | 1577 | 42618439 |
| Urinary tract infection | 53.61 | 25.99 | 35 | 1284 | 99249 | 42520767 |
| Nephrolithiasis | 35.72 | 25.99 | 19 | 1300 | 36811 | 42583205 |
| Mental status changes | 28.06 | 25.99 | 17 | 1302 | 42098 | 42577918 |
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Methaemoglobinaemia | 335.56 | 17.67 | 81 | 5701 | 9087 | 110574430 |
| Sulphaemoglobinaemia | 253.71 | 17.67 | 41 | 5741 | 554 | 110582963 |
| Urinary tract infection | 105.38 | 17.67 | 106 | 5676 | 326176 | 110257341 |
| Anticholinergic syndrome | 74.64 | 17.67 | 21 | 5761 | 4259 | 110579258 |
| Nephrolithiasis | 44.94 | 17.67 | 33 | 5749 | 66179 | 110517338 |
| Cystitis | 42.78 | 17.67 | 32 | 5750 | 66004 | 110517513 |
| Anaemia Heinz body | 42.58 | 17.67 | 6 | 5776 | 29 | 110583488 |
| Haemolytic anaemia | 42.18 | 17.67 | 21 | 5761 | 20899 | 110562618 |
| Dysuria | 38.59 | 17.67 | 29 | 5753 | 60202 | 110523315 |
| Urinary retention | 36.95 | 17.67 | 30 | 5752 | 69653 | 110513864 |
| Mental status changes | 28.72 | 17.67 | 27 | 5755 | 76095 | 110507422 |
| Emotional distress | 27.41 | 17.67 | 21 | 5761 | 44826 | 110538691 |
| Drug hypersensitivity | 23.35 | 17.67 | 64 | 5718 | 454026 | 110129491 |
| Uterine perforation | 20.39 | 17.67 | 9 | 5773 | 6831 | 110576686 |
| Mydriasis | 19.60 | 17.67 | 13 | 5769 | 22144 | 110561373 |
| Micturition urgency | 18.72 | 17.67 | 12 | 5770 | 19308 | 110564209 |
| Respiratory alkalosis | 18.60 | 17.67 | 8 | 5774 | 5713 | 110577804 |
| Hypoxia | 18.56 | 17.67 | 28 | 5754 | 129487 | 110454030 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G04BX06 | GENITO URINARY SYSTEM AND SEX HORMONES UROLOGICALS UROLOGICALS Other urologicals |
| CHEBI has role | CHEBI:35481 | non-narcotic analgesic |
| CHEBI has role | CHEBI:36333 | local anaesthetic |
| CHEBI has role | CHEBI:50903 | carcinogenic agent |
| CHEBI has role | CHEBI:149553 | anticoronaviral agent |
Related Drugs by ATC class:
G04BX Other urologicals 10 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dysuria | indication | 49650001 | |
| Urinary Tract Irritation | indication | ||
| Suicidal thoughts | contraindication | 6471006 | |
| Alcoholism | contraindication | 7200002 | |
| Hyperammonemia | contraindication | 9360008 | |
| Chronic obstructive lung disease | contraindication | 13645005 | DOID:3083 |
| Hepatic encephalopathy | contraindication | 13920009 | DOID:13413 |
| Severe chronic ulcerative colitis | contraindication | 14311001 | |
| Disorder of autonomic nervous system | contraindication | 15241006 | |
| Glaucoma | contraindication | 23986001 | DOID:1686 |
| Toxic megacolon | contraindication | 28536002 | DOID:1770 |
| Atony of colon | contraindication | 29479008 | |
| Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
| Depressive disorder | contraindication | 35489007 | |
| Glomerulonephritis | contraindication | 36171008 | DOID:2921 |
| Acute hepatitis | contraindication | 37871000 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Hypovolemic shock | contraindication | 39419009 | |
| Third trimester pregnancy | contraindication | 41587001 | |
| Hyperactive behavior | contraindication | 44548000 | |
| Uremia | contraindication | 44730006 | DOID:4676 |
| Conduction disorder of the heart | contraindication | 44808001 | |
| Achalasia of esophagus | contraindication | 45564002 | DOID:9164 |
| Chronic heart failure | contraindication | 48447003 | |
| Paralytic ileus | contraindication | 55525008 | DOID:8442 |
| Hepatic failure | contraindication | 59927004 | |
| Substance abuse | contraindication | 66214007 | |
| Hepatic coma | contraindication | 72836002 | DOID:12550 |
| Sleep apnea | contraindication | 73430006 | DOID:0050847 |
| Hiatal hernia | contraindication | 84089009 | DOID:12642 |
| Megaloblastic anemia due to folate deficiency | contraindication | 85649008 | DOID:14026 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Myasthenia gravis | contraindication | 91637004 | DOID:437 |
| Anemia due to enzyme deficiency | contraindication | 111577008 | |
| Deficiency of glucose-6-phosphate dehydrogenase | contraindication | 124134002 | DOID:2862 |
| Liver function tests abnormal | contraindication | 166603001 | |
| Folic acid deficiency | contraindication | 190633005 | |
| Disease of blood AND/OR blood-forming organ | contraindication | 191124002 | DOID:74 |
| Gastroesophageal reflux disease | contraindication | 235595009 | DOID:8534 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Bladder outflow obstruction | contraindication | 236645006 | |
| Pyloric obstruction | contraindication | 244815007 | |
| Sleep automatism | contraindication | 247962006 | |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Anemia | contraindication | 271737000 | DOID:2355 |
| Pregnancy, function | contraindication | 289908002 | |
| Thrombocytopenic disorder | contraindication | 302215000 | DOID:1588 |
| Neutropenic disorder | contraindication | 303011007 | DOID:1227 |
| Pseudomembranous enterocolitis | contraindication | 397683000 | |
| Respiratory insufficiency | contraindication | 409623005 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Porphyria | contraindication | 418470004 | |
| Fever greater than 100.4 Fahrenheit | contraindication | 426000000 | |
| Severe dehydration | contraindication | 450316000 | |
| Acute exacerbation of asthma | contraindication | 708038006 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.39 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Sodium channel alpha subunit | Ion channel | BLOCKER | CHEMBL | CHEMBL | |||||
| Sterile alpha and TIR motif-containing protein 1 | Enzyme | Ki | 4.16 | CHEMBL | |||||
| Snake venom metalloproteinase Bap1 | Enzyme | IC50 | 4.27 | CHEMBL | |||||
| Replicase polyprotein 1ab | Enzyme | Kd | 5.30 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4019884 | VUID |
| N0000147969 | NUI |
| D05450 | KEGG_DRUG |
| 136-40-3 | SECONDARY_CAS_RN |
| 4017768 | VANDF |
| 4019884 | VANDF |
| C0031379 | UMLSCUI |
| CHEBI:71416 | CHEBI |
| CHEMBL1242 | ChEMBL_ID |
| DB01438 | DRUGBANK_ID |
| CHEMBL1201022 | ChEMBL_ID |
| D010621 | MESH_DESCRIPTOR_UI |
| 4756 | PUBCHEM_CID |
| 7616 | IUPHAR_LIGAND_ID |
| 357 | INN_ID |
| K2J09EMJ52 | UNII |
| 203197 | RXNORM |
| 2316 | MMSL |
| 5266 | MMSL |
| 5267 | MMSL |
| d00337 | MMSL |
| 002866 | NDDF |
| 004869 | NDDF |
| 15785009 | SNOMEDCT_US |
| 370310006 | SNOMEDCT_US |
| 387119006 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Walgreens Urinary Pain Relief Maximum Strength | HUMAN OTC DRUG LABEL | 1 | 0363-0113 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| Walgreens Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 0363-0773 | TABLET | 95 mg | ORAL | unapproved drug other | 11 sections |
| Walgreens Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 0363-7775 | TABLET | 95 mg | ORAL | unapproved drug other | 11 sections |
| Walgreens Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 0363-7776 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| Wallgreens Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 0363-8455 | TABLET | 99.50 mg | ORAL | unapproved drug other | 11 sections |
| Phenazopyridine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0440-2070 | TABLET | 100 mg | ORAL | UNAPPROVED DRUG OTHER | 11 sections |
| UristatUTI Relief PakUTI Relief Pak | HUMAN OTC DRUG LABEL | 1 | 0440-8065 | TABLET | 95 mg | ORAL | UNAPPROVED DRUG OTHER | 14 sections |
| Rugby Phenazopyridine HCl Urinary Tract Analgesic | HUMAN OTC DRUG LABEL | 1 | 0536-1411 | TABLET | 95 mg | ORAL | unapproved drug other | 12 sections |
| Phenazopyridine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-620 | TABLET, FILM COATED | 100 mg | ORAL | unapproved drug other | 16 sections |
| Phenazopyridine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10135-621 | TABLET, FILM COATED | 200 mg | ORAL | unapproved drug other | 16 sections |
| Phenazopyridine HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-055 | TABLET | 100 mg | ORAL | unapproved drug other | 12 sections |
| Phenazopyridine HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-077 | TABLET | 200 mg | ORAL | unapproved drug other | 12 sections |
| Phenazopyridine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-115 | TABLET | 100 mg | ORAL | unapproved drug other | 11 sections |
| Phenazopyridine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 10544-571 | TABLET | 200 mg | ORAL | unapproved drug other | 11 sections |
| CVS Health Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-001 | TABLET | 95 mg | ORAL | unapproved drug other | 11 sections |
| Preferred Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-210 | TABLET | 99.50 mg | ORAL | unapproved drug other | 11 sections |
| Preferred Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-333 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| CVS Health Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-523 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| Preferred Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-551 | TABLET | 95 mg | ORAL | unapproved drug other | 11 sections |
| Discount Drug Mart Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-552 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| Family Wellness Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-599 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| Vexia Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 10956-703 | TABLET | 99.50 mg | ORAL | unapproved drug other | 11 sections |
| Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 11673-270 | TABLET | 99.50 mg | ORAL | unapproved drug other | 11 sections |
| Rite Aid Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 11822-3111 | TABLET | 99.50 mg | ORAL | unapproved drug other | 11 sections |
| Rite Aid Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 11822-8855 | TABLET | 95 mg | ORAL | unapproved drug other | 11 sections |
| Phenazopyridine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 12634-189 | TABLET | 200 mg | ORAL | unapproved drug other | 11 sections |
| Select Brand Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 15127-138 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| Signature Care Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 21130-523 | TABLET | 97.50 mg | ORAL | unapproved drug other | 11 sections |
| Signature Care Maximum Strength Urinary Pain Relief | HUMAN OTC DRUG LABEL | 1 | 21130-792 | TABLET | 99.50 mg | ORAL | unapproved drug other | 11 sections |
| Phenazopyridine Hydrochloride | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-301 | TABLET | 200 mg | ORAL | Unapproved drug other | 11 sections |