terlipressin 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasopressin analogues | 2967 | 14636-12-5 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Terlipressin is a synthetic vasopressin analogue with twice the selectivity for vasopressin V1 receptors versus V2 receptors. Terlipressin acts as both a prodrug for lysine-vasopressin, as well as having pharmacologic activity on its own. Terlipressin is thought to increase renal blood flow in patients with hepatorenal syndrome by reducing portal hypertension and blood circulation in portal vessels and increasing effective arterial volume and mean arterial pressure (MAP). It is used to control bleeding of ESOPHAGEAL VARICES and for the treatment of HEPATORENAL SYNDROME.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 12 | mg | P |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 0.24 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 8.20 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 0.90 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Sept. 14, 2022 | FDA | MALLINCKRODT |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
None
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | H01BA04 | SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES POSTERIOR PITUITARY LOBE HORMONES Vasopressin and analogues |
| MeSH PA | D000959 | Antihypertensive Agents |
| MeSH PA | D002317 | Cardiovascular Agents |
| MeSH PA | D014662 | Vasoconstrictor Agents |
| FDA EPC | N0000194045 | Vasopressin Receptor Agonist |
| FDA MoA | N0000194046 | Vasopressin Receptor Agonists |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hepatorenal syndrome | indication | 51292008 | DOID:11823 |
| Ischemia | contraindication | 52674009 | DOID:326 |
| Hypoxia | contraindication | 389086002 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.65 | acidic |
| pKa2 | 11.89 | acidic |
| pKa3 | 12.32 | acidic |
| pKa4 | 12.71 | acidic |
| pKa5 | 12.98 | acidic |
| pKa6 | 13.08 | acidic |
| pKa7 | 13.57 | acidic |
| pKa8 | 13.58 | acidic |
| pKa9 | 13.67 | acidic |
| pKa10 | 13.96 | acidic |
| pKa11 | 10.31 | Basic |
| pKa12 | 7.93 | Basic |
Orange Book patent data (new drug applications)
None
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 0.85MG BASE/VIAL | TERLIVAZ | MALLINCKRODT IRELAND | N022231 | Sept. 14, 2022 | RX | POWDER | INTRAVENOUS | Sept. 14, 2027 | NEW CHEMICAL ENTITY |
| EQ 0.85MG BASE/VIAL | TERLIVAZ | MALLINCKRODT IRELAND | N022231 | Sept. 14, 2022 | RX | POWDER | INTRAVENOUS | Sept. 14, 2029 | TO IMPROVE KIDNEY FUNCTION IN ADULTS WITH HEPATORENAL SYNDROME WITH RAPID REDUCTION IN KIDNEY FUNCTION |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Vasopressin V1a receptor | GPCR | AGONIST | Ki | 5.96 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Vasopressin V2 receptor | GPCR | AGONIST | Ki | 5.16 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| D06672 | KEGG_DRUG |
| 4041761 | VANDF |
| C0145185 | UMLSCUI |
| CHEBI:135905 | CHEBI |
| CHEMBL2135460 | ChEMBL_ID |
| D000077585 | MESH_DESCRIPTOR_UI |
| DB02638 | DRUGBANK_ID |
| 11241 | IUPHAR_LIGAND_ID |
| 5114 | INN_ID |
| 7Z5X49W53P | UNII |
| 72081 | PUBCHEM_CID |
| 57048 | RXNORM |
| 29210 | MMSL |
| d04932 | MMSL |
| 004053 | NDDF |
| 013118 | NDDF |
| 325927008 | SNOMEDCT_US |
| 395899009 | SNOMEDCT_US |
| 734453002 | SNOMEDCT_US |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Terlivaz | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43825-200 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 0.85 mg | INTRAVENOUS | NDA | 30 sections |
| Terlivaz | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43825-200 | INJECTION, POWDER, LYOPHILIZED, FOR SOLUTION | 0.85 mg | INTRAVENOUS | NDA | 30 sections |