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methazolamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1741 | 554-57-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A carbonic anhydrase inhibitor that is used as a diuretic and in the treatment of glaucoma.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.70 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 61 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 21.16 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 100 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK2,MAP2K6,MAP3K21,MAPK10,MAPK7,MTOR,NTRK2,PDK1,PDK2,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PIM2,PRKDC,SIK2,STK33,SYK,TEK | 36 | |||
| kinase-selectivity-class | AXL,BRAF,CDK1,CDK16,CDK2,CDK3,CDK4,CDK6,CDK9,CLK4,DYRK1B,DYRK2,GRK2,GSK3B,MAP2K6,MAPK12,MAPK7,PDK1,PIK3CB,PIK3CD,PRKDC,STK10,STK33,TEK,ZAP70 | 25 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pld-class | Phospholipidosis risk class (1 = positive, 0 = negative) | 0 | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Jan. 26, 1959 | FDA | LEDERLE |
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Nerve degeneration | 80.30 | 72.32 | 11 | 563 | 194 | 42620567 |
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 |
|---|---|---|---|---|---|---|
| Nerve degeneration | 84.14 | 48.69 | 11 | 740 | 275 | 110588273 |
| Renal neoplasm | 60.73 | 48.69 | 11 | 740 | 2395 | 110586153 |
| Renal mass | 56.20 | 48.69 | 11 | 740 | 3624 | 110584924 |
| Abdominal rigidity | 56.06 | 48.69 | 11 | 740 | 3669 | 110584879 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | S01EC05 | SENSORY ORGANS OPHTHALMOLOGICALS ANTIGLAUCOMA PREPARATIONS AND MIOTICS Carbonic anhydrase inhibitors |
| MeSH PA | D002257 | Carbonic Anhydrase Inhibitors |
| MeSH PA | D004232 | Diuretics |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D045283 | Natriuretic Agents |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:39456 | antiglaucoma drug |
Related Drugs by ATC class:
S01EC Carbonic anhydrase inhibitors 4 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Open-angle glaucoma | indication | 84494001 | DOID:1067 |
| Secondary glaucoma | indication | 95717004 | |
| Angle-closure glaucoma | indication | 392291006 | DOID:13550 |
| Malignant glaucoma | off-label use | 10100008 | |
| Renal tubular acidosis | contraindication | 1776003 | DOID:14219 |
| Respiratory acidosis | contraindication | 12326000 | |
| Hyperkalemia | contraindication | 14140009 | |
| Metabolic acidosis, normal anion gap, acidifying salts | contraindication | 18104000 | |
| Diabetes mellitus type 2 | contraindication | 44054006 | DOID:9352 |
| Diabetes mellitus type 1 | contraindication | 46635009 | DOID:9744 |
| Acute nephropathy | contraindication | 58574008 | |
| Hepatic failure | contraindication | 59927004 | |
| Decreased respiratory function | contraindication | 80954004 | |
| Hyponatremia | contraindication | 89627008 | |
| Gout | contraindication | 90560007 | DOID:13189 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Disease of blood AND/OR blood-forming organ | contraindication | 191124002 | DOID:74 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Disorder of electrolytes | contraindication | 237840007 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 | |
| Recurrent Calcium Renal Calculi | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 7.28 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Carbonic anhydrase 4 | Enzyme | INHIBITOR | Ki | 6.62 | CHEMBL | CHEMBL | |||
| Carbonic anhydrase 7 | Enzyme | INHIBITOR | Ki | 8.68 | CHEMBL | CHEMBL | |||
| Carbonic anhydrase 1 | Enzyme | INHIBITOR | Ki | 7.85 | CHEMBL | CHEMBL | |||
| Carbonic anhydrase 2 | Enzyme | INHIBITOR | Ki | 8.05 | CHEMBL | CHEMBL | |||
| Carbonic anhydrase 5B, mitochondrial | Enzyme | Ki | 7.21 | CHEMBL | |||||
| Carbonic anhydrase 3 | Enzyme | Ki | 8.96 | CHEMBL | |||||
| Carbonic anhydrase 6 | Enzyme | Ki | 8 | CHEMBL | |||||
| Carbonic anhydrase 14 | Enzyme | Ki | 7.37 | CHEMBL | |||||
| Carbonic anhydrase 13 | Enzyme | Ki | 7.72 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | IC50 | 7.70 | CHEMBL | |||||
| Carbonic anhydrase V | Enzyme | Ki | 8.60 | CHEMBL | |||||
| Carbonic anhydrase 9 | Enzyme | Ki | 7.57 | CHEMBL | |||||
| Carbonic anhydrase 12 | Enzyme | Ki | 8.47 | CHEMBL | |||||
| Carbonic anhydrase 5A, mitochondrial | Enzyme | Ki | 7.19 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 6.77 | CHEMBL | |||||
| Carbonic anhydrase 13 | Enzyme | Ki | 7.72 | CHEMBL | |||||
| Carbonic anhydrase 4 | Enzyme | Ki | 7.44 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 6.85 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 4.49 | CHEMBL | |||||
| Carbonic anhydrase 15 | Enzyme | Ki | 7.19 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 6.92 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 7.85 | CHEMBL | |||||
| Probable transmembrane carbonic anhydrase (Carbonate dehydratase) (Carbonic dehydratase); Transmembrane carbonic anhydrase | Enzyme | Ki | 6.25 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 6.93 | CHEMBL | |||||
| Alpha carbonic anhydrase | Enzyme | Ki | 7.67 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 6.88 | CHEMBL | |||||
| Carbonic anhydrase 2 | Enzyme | Ki | 7.20 | CHEMBL | |||||
| Astrosclerin-3 | Enzyme | Ki | 6.49 | CHEMBL | |||||
| Beta-carbonic anhydrase 1 | Enzyme | Ki | 6.11 | CHEMBL | |||||
| Delta carbonic anhydrase | Enzyme | Ki | 6.77 | CHEMBL | |||||
| Carbonic anhydrase 2 | Enzyme | Ki | 6.18 | CHEMBL | |||||
| Carbonic anhydrase | Enzyme | Ki | 6.74 | CHEMBL | |||||
| Carbonic anhydrase, alpha family | Enzyme | Ki | 7.58 | CHEMBL | |||||
| Carbonate dehydratase | Enzyme | Ki | 8.09 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017906 | VUID |
| N0000146257 | NUI |
| D00655 | KEGG_DRUG |
| 4017906 | VANDF |
| C0025631 | UMLSCUI |
| CHEBI:6822 | CHEBI |
| MZM | PDB_CHEM_ID |
| CHEMBL19 | ChEMBL_ID |
| DB00703 | DRUGBANK_ID |
| D008704 | MESH_DESCRIPTOR_UI |
| 4100 | PUBCHEM_CID |
| 6828 | IUPHAR_LIGAND_ID |
| 882 | INN_ID |
| W733B0S9SD | UNII |
| 218699 | RXNORM |
| 2252 | MMSL |
| 5067 | MMSL |
| 921 | MMSL |
| d00640 | MMSL |
| 002289 | NDDF |
| 392575007 | SNOMEDCT_US |
| 53052005 | SNOMEDCT_US |
| W733B0S9SD | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0574-0790 | TABLET | 25 mg | ORAL | ANDA | 21 sections |
| methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0574-0791 | TABLET | 50 mg | ORAL | ANDA | 21 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-022 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-022 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-023 | TABLET | 50 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 24208-023 | TABLET | 50 mg | ORAL | ANDA | 19 sections |
| Methazolamide | Human Prescription Drug Label | 1 | 27241-246 | TABLET | 25 mg | ORAL | ANDA | 11 sections |
| Methazolamide | Human Prescription Drug Label | 1 | 27241-247 | TABLET | 50 mg | ORAL | ANDA | 11 sections |
| METHAZOLAMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42571-239 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| METHAZOLAMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42571-240 | TABLET | 50 mg | ORAL | ANDA | 19 sections |
| methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50090-3233 | TABLET | 50 mg | ORAL | ANDA | 21 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-026 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51407-027 | TABLET | 50 mg | ORAL | ANDA | 19 sections |
| METHAZOLAMIDE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-2996 | TABLET | 50 mg | ORAL | ANDA | 22 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-240 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 62559-241 | TABLET | 50 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-1986 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-1987 | TABLET | 50 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 67046-1193 | TABLET | 50 mg | ORAL | ANDA | 18 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68094-808 | TABLET | 50 mg | ORAL | ANDA | 22 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68094-908 | TABLET | 25 mg | ORAL | ANDA | 22 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 68151-3110 | TABLET | 50 mg | ORAL | ANDA | 21 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-1754 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-1755 | TABLET | 50 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72603-166 | TABLET | 25 mg | ORAL | ANDA | 19 sections |
| Methazolamide | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72603-167 | TABLET | 50 mg | ORAL | ANDA | 19 sections |