metyrapone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 1791 | 54-36-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Bocci G, Oprea TI, Benet LZ |
| S (Water solubility) | 0.43 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 4, 1961 | FDA | HRA PHARMA |
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 |
|---|---|---|---|---|---|---|
| Premature delivery | 77.71 | 46.26 | 23 | 601 | 30258 | 63458140 |
| Cortisol increased | 75.64 | 46.26 | 11 | 613 | 418 | 63487980 |
| Cortisol free urine increased | 61.38 | 46.26 | 7 | 617 | 34 | 63488364 |
| Pneumocystis jirovecii pneumonia | 57.44 | 46.26 | 16 | 608 | 16898 | 63471500 |
| Adrenal insufficiency | 56.53 | 46.26 | 16 | 608 | 17899 | 63470499 |
| Blood corticotrophin decreased | 46.47 | 46.26 | 7 | 617 | 338 | 63488060 |
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 |
|---|---|---|---|---|---|---|
| Pneumocystis jirovecii pneumonia | 46.66 | 42.05 | 15 | 436 | 19695 | 34936785 |
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 |
|---|---|---|---|---|---|---|
| Pneumocystis jirovecii pneumonia | 96.74 | 41.72 | 29 | 929 | 32479 | 79710951 |
| Adrenal insufficiency | 78.65 | 41.72 | 24 | 934 | 28463 | 79714967 |
| Cortisol free urine increased | 77.22 | 41.72 | 9 | 949 | 43 | 79743387 |
| Premature delivery | 74.39 | 41.72 | 22 | 936 | 23445 | 79719985 |
| Cortisol increased | 63.37 | 41.72 | 10 | 948 | 535 | 79742895 |
| Premature rupture of membranes | 43.31 | 41.72 | 10 | 948 | 4059 | 79739371 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | V04CD01 | VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Tests for pituitary function |
| MeSH PA | D000963 | Antimetabolites |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D009676 | Noxae |
| FDA MoA | N0000175921 | Adrenal Steroid Synthesis Inhibitors |
| FDA EPC | N0000175928 | Adrenal Steroid Synthesis Inhibitor |
| CHEBI has role | CHEBI:33295 | diagnostic aid |
| CHEBI has role | CHEBI:35221 | antimetabolite |
| CHEBI has role | CHEBI:76798 | cytochrome p450 XIB1 inhibitor |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Diagnostic Test for Secondary Adrenocortical Insufficiency | indication | ||
| Hypercortisolism | off-label use | 47270006 | |
| Primary adrenocortical insufficiency | contraindication | 373662000 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 4.64 | Basic |
| pKa2 | 1.71 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Cytochrome P450 11B1, mitochondrial | Enzyme | INHIBITOR | IC50 | 7.84 | CHEMBL | DRUG LABEL | |||
| Cytochrome P450 3A4 | Enzyme | IC50 | 6.10 | DRUG MATRIX | |||||
| Cytochrome P450 11B2, mitochondrial | Enzyme | IC50 | 7.38 | CHEMBL | |||||
| Cytochrome P450 11B1 | Enzyme | Ki | 6.24 | CHEMBL | |||||
| Cytochrome P450 11B1, mitochondrial | Enzyme | IC50 | 5.34 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018788 | VUID |
| N0000147091 | NUI |
| D00410 | KEGG_DRUG |
| 4018788 | VANDF |
| C0025876 | UMLSCUI |
| CHEBI:44241 | CHEBI |
| MYT | PDB_CHEM_ID |
| CHEMBL934 | ChEMBL_ID |
| DB01011 | DRUGBANK_ID |
| D008797 | MESH_DESCRIPTOR_UI |
| 4174 | PUBCHEM_CID |
| 5224 | IUPHAR_LIGAND_ID |
| 1404 | INN_ID |
| ZS9KD92H6V | UNII |
| 203002 | RXNORM |
| 10389 | MMSL |
| 5107 | MMSL |
| d00592 | MMSL |
| 002120 | NDDF |
| 395794007 | SNOMEDCT_US |
| 53848009 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Metopirone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76336-455 | CAPSULE, GELATIN COATED | 250 mg | ORAL | NDA | 32 sections |
| Metopirone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76336-455 | CAPSULE, GELATIN COATED | 250 mg | ORAL | NDA | 32 sections |
| Metopirone | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76336-455 | CAPSULE, GELATIN COATED | 250 mg | ORAL | NDA | 32 sections |