conivaptan 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| vasopressin receptor antagonists | 732 | 168626-94-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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 | Benet LZ, Broccatelli F, Oprea TI |
| S (Water solubility) | 0.15 mg/mL | Benet LZ, Broccatelli F, Oprea TI |
| EoM (Fraction excreted unchanged in urine) | 1 % | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 1.15 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 42 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| Vd (Volume of distribution) | 0.76 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 3 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.01 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 6.70 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 29, 2005 | FDA | CUMBERLAND PHARMS |
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 | C03XA02 | CARDIOVASCULAR SYSTEM DIURETICS OTHER DIURETICS Vasopressin antagonists |
| FDA MoA | N0000020044 | Vasopressin Receptor Antagonists |
| MeSH PA | D065092 | Antidiuretic Hormone Receptor Antagonists |
| MeSH PA | D045283 | Natriuretic Agents |
| FDA EPC | N0000178376 | Vasopressin Receptor Antagonist |
| FDA MoA | N0000190114 | Cytochrome P450 3A Inhibitors |
| CHEBI has role | CHEBI:59680 | vasopressin receptor antagonists |
| CHEBI has role | CHEBI:194423 | aquaretic agent |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Hyponatremia | indication | 89627008 | |
| Anuria | contraindication | 2472002 | DOID:2983 |
| Hypovolemia | contraindication | 28560003 | |
| Demyelination | contraindication | 32693004 | |
| Hypernatremia | contraindication | 39355002 | |
| Chronic heart failure | contraindication | 48447003 | |
| Acute nephropathy | contraindication | 58574008 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Osmotic Central Pontine Myelinolysis | 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 | 10.9 | acidic |
| pKa2 | 12.5 | acidic |
| pKa3 | 6.37 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Vasopressin V1a receptor | GPCR | ANTAGONIST | Ki | 9.37 | CHEMBL | CHEMBL | |||
| Vasopressin V2 receptor | GPCR | ANTAGONIST | Ki | 9.44 | CHEMBL | CHEMBL | |||
| Oxytocin receptor | GPCR | Ki | 7.35 | CHEMBL | |||||
| Vasopressin V2 receptor | GPCR | Ki | 8.52 | CHEMBL | |||||
| Vasopressin V1a receptor | GPCR | Ki | 9.32 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4025087 | VUID |
| N0000175346 | NUI |
| D01236 | KEGG_DRUG |
| 1294548 | RXNORM |
| 4025087 | VANDF |
| 4025088 | VANDF |
| C0966107 | UMLSCUI |
| CHEBI:681850 | CHEBI |
| CHEMBL1755 | ChEMBL_ID |
| DB00872 | DRUGBANK_ID |
| C106389 | MESH_SUPPLEMENTAL_RECORD_UI |
| 151171 | PUBCHEM_CID |
| 2203 | IUPHAR_LIGAND_ID |
| 7947 | INN_ID |
| 0NJ98Y462X | UNII |
| 20826 | MMSL |
| 73959 | MMSL |
| d05699 | MMSL |
| 011178 | NDDF |
| 011179 | NDDF |
| 421516006 | SNOMEDCT_US |
| 421858002 | SNOMEDCT_US |
| 425602003 | SNOMEDCT_US |
| CHEMBL1201108 | ChEMBL_ID |
| 210101-16-9 | SECONDARY_CAS_RN |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Vaprisol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-1601 | LIQUID | 5 mg | INTRAVENOUS | NDA | 23 sections |
| Vaprisol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0469-1602 | SOLUTION | 20 mg | INTRAVENOUS | NDA | 23 sections |
| VAPRISOL DEXTROSE IN PLASTIC CONTAINER | HUMAN PRESCRIPTION DRUG LABEL | 1 | 66220-160 | INJECTION, SOLUTION | 20 mg | INTRAVENOUS | NDA | 24 sections |