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methylergometrine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| ergot alkaloid derivatives | 1764 | 113-42-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A homolog of ERGONOVINE containing one more CH2 group. (Merck Index, 11th ed)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 0.20 | mg | O |
| 0.20 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Benet LZ, Broccatelli F, Oprea TI |
| BA (Bioavailability) | 60 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.96 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 7.18 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 1.85 hours | Lombardo F, Berellini G, Obach RS |
| S (Water solubility) | 11.39 mg/mL | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 1.884 | Moderate | 0.73 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 58.614 | Moderate | 0.73 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 1.503 | 10^-6 cm/s | Moderate | 0.73 |
| dh-clint | Dog hepatocyte intrinsic clearance | 3.041 | uL/min/10^6 cells | Moderate | 0.73 |
| dppb | Dog plasma protein binding (% unbound) | 30 | % | Moderate | 0.73 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 48.450 | % | Moderate | 0.73 |
| herg | hERG pIC50 | 4.351 | pIC50 | Moderate | 0.73 |
| hh-clint | Human hepatocyte intrinsic clearance | 2.065 | uL/min/10^6 cells | Moderate | 0.73 |
| hlm-clint | Human liver microsomal intrinsic clearance | 31.477 | uL/min/mg protein | Moderate | 0.73 |
| hppb | Human plasma protein binding (% unbound) | 32.370 | % | Moderate | 0.73 |
| kinase-safety-class | ACVR2B,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,ITK,JAK3,KDR,MAP2K6,MAP3K7,MAPK10,MAPK7,MET,NTRK2,PDK1,PDK2,PDK4,PIK3CA,PIK3CB,PIM2,PRKDC,SIK2,SIK3,STK33,TEK,TGFBR1,ZAP70 | 39 | |||
| kinase-selectivity-class | AXL,BRAF,CDK9,EIF2AK3,MAP2K6,MAP3K21,PDK1 | 7 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 19.543 | Moderate | 0.73 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 26.062 | Moderate | 0.73 | |
| mppb | Mouse plasma protein binding (% unbound) | 26.460 | Moderate | 0.73 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 24.044 | Moderate | 0.73 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 46.380 | % | Moderate | 0.73 |
| rh-clint | Rat hepatocyte intrinsic clearance | 16.827 | uL/min/10^6 cells | Moderate | 0.73 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 70.670 | % | Moderate | 0.73 |
| rppb | Rat plasma protein binding (% unbound) | 32.370 | % | Moderate | 0.73 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 933.254 | uM | Moderate | 0.73 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 19, 1946 | FDA | EDISON THERAPS LLC |
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 |
|---|---|---|---|---|---|---|
| Wrong product administered | 76.85 | 39.19 | 18 | 1092 | 7647 | 90619690 |
| Cyanosis | 43.35 | 39.19 | 14 | 1096 | 19441 | 90607896 |
| Postpartum haemorrhage | 42.58 | 39.19 | 9 | 1101 | 2392 | 90624945 |
| Disseminated intravascular coagulation | 41.95 | 39.19 | 14 | 1096 | 21524 | 90605813 |
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 |
|---|---|---|---|---|---|---|
| Wrong product administered | 199.38 | 88.60 | 32 | 143 | 6194 | 42614966 |
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
| 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 |
|---|---|---|---|---|---|---|
| Wrong product administered | 142.27 | 104.03 | 27 | 99 | 25 | 113802 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G02AB01 | GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS UTEROTONICS Ergot alkaloids |
| ATC | G02AC01 | GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS UTEROTONICS Ergot alkaloids and oxytocin incl. analogues, in combination |
| FDA CS | M0007652 | Ergolines |
| MeSH PA | D010120 | Oxytocics |
| MeSH PA | D012102 | Reproductive Control Agents |
| CHEBI has role | CHEBI:176497 | geroprotector |
| FDA EPC | N0000175827 | Ergot Derivative |
Related Drugs by ATC class:
G02AB Ergot alkaloids 1 drug
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Postpartum hemorrhage | indication | 47821001 | |
| Postabortal Hemorrhage | indication | ||
| Incomplete miscarriage | off-label use | 156072005 | |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Pregnancy-induced hypertension | contraindication | 48194001 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Seizure disorder | contraindication | 128613002 | |
| Cerebrovascular accident | contraindication | 230690007 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Sepsis syndrome | contraindication | 238150007 | |
| Pregnancy, function | contraindication | 289908002 | |
| Arteriosclerosis obliterans | contraindication | 361133006 | DOID:5160 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 12.56 | acidic |
| pKa2 | 13.6 | acidic |
| pKa3 | 7.01 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| D(1A) dopamine receptor | GPCR | ANTAGONIST | Ki | 6.27 | DRUG MATRIX | CHEMBL | |||
| D(2) dopamine receptor | GPCR | Ki | 6.56 | DRUG MATRIX | |||||
| Alpha-2A adrenergic receptor | GPCR | Ki | 6.23 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.63 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | AGONIST | Ki | 9.40 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2B | GPCR | PARTIAL AGONIST | Ki | 9.10 | CHEMBL | ||||
| 5-hydroxytryptamine receptor 2C | GPCR | AGONIST | Ki | 8.30 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 6 | GPCR | Ki | 8.93 | DRUG MATRIX | |||||
| Alpha-2B adrenergic receptor | GPCR | Ki | 6.68 | DRUG MATRIX | |||||
| D(3) dopamine receptor | GPCR | Ki | 7.24 | DRUG MATRIX | |||||
| Cytochrome P450 2D6 | Enzyme | IC50 | 6.70 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1F | GPCR | ANTAGONIST | Ki | 7.50 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1E | GPCR | ANTAGONIST | Ki | 7.20 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 1B | GPCR | Ki | 8.03 | DRUG MATRIX | |||||
| 5-hydroxytryptamine receptor 1A | GPCR | IC50 | 8.39 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2A | GPCR | AGONIST | Ki | 7.90 | IUPHAR | ||||
| 5-hydroxytryptamine receptor 2C | GPCR | AGONIST | Ki | 7.90 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| 4018757 | VUID |
| N0000179466 | NUI |
| D00680 | KEGG_DRUG |
| 57432-61-8 | SECONDARY_CAS_RN |
| 4018757 | VANDF |
| 4019831 | VANDF |
| CHEBI:749414 | CHEBI |
| H8D | PDB_CHEM_ID |
| CHEMBL1201356 | ChEMBL_ID |
| CHEMBL1200843 | ChEMBL_ID |
| DB00353 | DRUGBANK_ID |
| 227555 | RXNORM |
| 160889 | MMSL |
| 5091 | MMSL |
| 967 | MMSL |
| d00587 | MMSL |
| 001306 | NDDF |
| 004941 | NDDF |
| 126074008 | SNOMEDCT_US |
| 126075009 | SNOMEDCT_US |
| 40562000 | SNOMEDCT_US |
| C0025760 | UMLSCUI |
| D008755 | MESH_DESCRIPTOR_UI |
| 8226 | PUBCHEM_CID |
| 150 | IUPHAR_LIGAND_ID |
| 2900 | INN_ID |
| W53L6FE61V | UNII |
| W53L6FE61V | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0093-3655 | TABLET | 0.20 mg | ORAL | ANDA | 20 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-0740 | INJECTION, SOLUTION | 0.20 mg | INTRAMUSCULAR | ANDA | 21 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0904-7282 | TABLET | 0.20 mg | ORAL | ANDA | 22 sections |
| METHERGINE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 12634-179 | TABLET, COATED | 0.20 mg | ORAL | NDA | 21 sections |
| Methylergonovine Maleate | Human Prescription Drug Label | 1 | 16571-735 | TABLET | 0.20 mg | ORAL | ANDA | 22 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 17856-3655 | TABLET | 0.20 mg | ORAL | ANDA | 20 sections |
| Methergine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 27437-050 | TABLET | 0.20 mg | ORAL | ANDA | 18 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 40032-140 | TABLET | 0.20 mg | ORAL | ANDA | 21 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43386-140 | TABLET | 0.20 mg | ORAL | ANDA | 19 sections |
| METHYLERGONOVINE MALEATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1556 | INJECTION | 0.20 mg | INTRAVENOUS | ANDA | 13 sections |
| METHYLERGONOVINE MALEATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51662-1668 | INJECTION, SOLUTION | 0.20 mg | INTRAVENOUS | ANDA | 11 sections |
| METHYLERGONOVINE MALEATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 51991-144 | INJECTION | 0.20 mg | INTRAVENOUS | ANDA | 28 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-813 | TABLET | 0.20 mg | ORAL | ANDA | 21 sections |
| METHYLERGONOVINE MALEATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63629-2074 | INJECTION | 0.20 mg | INTRAVENOUS | ANDA | 22 sections |
| METHYLERGONOVINE MALEATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63704-004 | INJECTION, SOLUTION | 0.20 mg | INTRAVENOUS | ANDA | 27 sections |
| methylergonovine maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 63704-006 | TABLET | 0.20 mg | ORAL | ANDA | 23 sections |
| Methergine | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66336-402 | TABLET, COATED | 0.20 mg | ORAL | NDA | 22 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69238-1605 | TABLET | 0.20 mg | ORAL | ANDA | 22 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70010-786 | TABLET | 0.20 mg | ORAL | ANDA | 22 sections |
| METHYLERGONOVINE MALEATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72162-1592 | INJECTION | 0.20 mg | INTRAVENOUS | ANDA | 22 sections |
| Methylergonovine Maleate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 83400-100 | TABLET | 0.20 mg | ORAL | ANDA | 21 sections |