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Identification
NameConivaptan
Accession NumberDB00872  (APRD01302)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Conivaptan is a non-peptide inhibitor of antidiuretic hormone (vasopressin). It was approved in 2004 for hyponatremia (low blood sodium levels) caused by syndrome of inappropriate antidiuretic hormone (SIADH). Conivaptan inhibits both isotypes of the vasopressin receptor (V1a and V2).

Structure
Thumb
Synonyms
SynonymLanguageCode
4'-((4,5-dihydro-2-Methylimidazo(4,5-D)(1)benzazepin-6(1H)-yl)carbonyl)-2-biphenylcarboxanilideNot AvailableNot Available
ConivaptanNot AvailableNot Available
Prescription ProductsNot Available
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International Brands
NameCompany
VaprisolNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Conivaptan hydrochloride
Thumb
  • InChI Key: BTYHAFSDANBVMJ-UHFFFAOYSA-N
  • Monoisotopic Mass: 534.182253835
  • Average Mass: 535.035
DBSALT000793
CategoriesNot Available
CAS number210101-16-9
WeightAverage: 498.5744
Monoisotopic: 498.205576096
Chemical FormulaC32H26N4O2
InChI KeyIKENVDNFQMCRTR-UHFFFAOYSA-N
InChI
InChI=1S/C32H26N4O2/c1-21-33-28-19-20-36(29-14-8-7-13-27(29)30(28)34-21)32(38)23-15-17-24(18-16-23)35-31(37)26-12-6-5-11-25(26)22-9-3-2-4-10-22/h2-18H,19-20H2,1H3,(H,33,34)(H,35,37)
IUPAC Name
N-(4-{4-methyl-3,5,9-triazatricyclo[8.4.0.0²,⁶]tetradeca-1(14),2(6),3,10,12-pentaene-9-carbonyl}phenyl)-2-phenylbenzamide
SMILES
CC1=NC2=C(CCN(C(=O)C3=CC=C(NC(=O)C4=CC=CC=C4C4=CC=CC=C4)C=C3)C3=CC=CC=C23)N1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-phenylbenzamides. These are benzamides that are N-linked to a phenyl group via the carboxamide group.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzamides
Direct ParentN-phenylbenzamides
Alternative Parents
Substituents
  • N-phenylbenzamide
  • Biphenyl
  • Benzazepine
  • N-arylamide
  • Aminobenzoic acid or derivatives
  • Benzoic acid or derivatives
  • Benzoyl
  • Azepine
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of euvolemic or hypervolemic hyponatremia (e.g. the syndrome of inappropriate secretion of antidiuretic hormone, or in the setting of hypothyroidism, adrenal insufficiency, pulmonary disorders, etc.) in hospitalized patients.
PharmacodynamicsConivaptan is a nonpeptide, dual antagonist of arginine vasopressin (AVP) V1A and V2 receptors. The level of AVP in circulating blood is critical for the regulation of water and electrolyte balance and is usually elevated in both euvolemic and hypervolemic hyponatremia. The AVP effect is mediated through V2 receptors, which are functionally coupled to aquaporin channels in the apical membrane of the collecting ducts of the kidney. These receptors help to maintain plasma osmolality within the normal range by increasing permeability of the renal collecting ducts to water. Vasopressin also causes vasoconstriction through its actions on vascular 1A receptors. The predominant pharmacodynamic effect of conivaptan in the treatment of hyponatremia is through its V2 antagonism of AVP in the renal collecting ducts, an effect that results in aquaresis, or excretion of free water. Conivaptan's antagonist activity on V1A receptors may also cause splanchnic vasodilation, resulting in possible hypotension or variceal bleeding in patients with cirrhosis. The pharmacodynamic effects of conivaptan include increased free water excretion (i.e., effective water clearance [EWC]) generally accompanied by increased net fluid loss, increased urine output, and decreased urine osmolality.
Mechanism of actionConivaptan is a dual AVP antagonist with nanomolar affinity for human arginine vasopressin V1A and V2 receptors in vitro. This antagonism occurs in the renal collecting ducts, resulting in aquaresis, or excretion of free water.
AbsorptionNot Available
Volume of distributionNot Available
Protein binding99%
Metabolism

CYP3A4 is the sole cytochrome P450 isozyme responsible for the metabolism of conivaptan. Four metabolites have been identified. The pharmacological activity of the metabolites at V1a and V2 receptors ranged from approximately 3-50% and 50-100% that of conivaptan, respectively.

Route of eliminationNot Available
Half life5 hours
ClearanceNot Available
ToxicityAlthough no data on overdosage in humans are available, conivaptan has been administered as a 20 mg loading dose on Day 1 followed by continuous infusion of 80 mg/day for 4 days in hyponatremia patients and up to 120 mg/day for 2 days in CHF patients. No new toxicities were identified at these higher doses, but adverse events related to the pharmacologic activity of conivaptan, e.g. hypotension and thirst, occurred more frequently at these higher doses.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9522
Caco-2 permeable+0.5291
P-glycoprotein substrateSubstrate0.5919
P-glycoprotein inhibitor IInhibitor0.6901
P-glycoprotein inhibitor IIInhibitor0.8429
Renal organic cation transporterNon-inhibitor0.6631
CYP450 2C9 substrateNon-substrate0.7671
CYP450 2D6 substrateNon-substrate0.7534
CYP450 3A4 substrateSubstrate0.6602
CYP450 1A2 substrateInhibitor0.7008
CYP450 2C9 substrateInhibitor0.5368
CYP450 2D6 substrateNon-inhibitor0.6597
CYP450 2C19 substrateInhibitor0.8477
CYP450 3A4 substrateInhibitor0.9027
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9043
Ames testNon AMES toxic0.6672
CarcinogenicityNon-carcinogens0.8831
BiodegradationNot ready biodegradable0.9584
Rat acute toxicity2.5446 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9885
hERG inhibition (predictor II)Inhibitor0.8456
Pharmacoeconomics
Manufacturers
  • Astellas pharma us inc
Packagers
Dosage formsNot Available
Prices
Unit descriptionCostUnit
Vaprisol 20 mg/100 ml bag6.3USD ml
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States57236061999-12-152019-12-15
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilityVery slightly soluble (0.15 mg/mL at 23 °C)Not Available
logP6.3Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00175 mg/mLALOGPS
logP5.23ALOGPS
logP5.44ChemAxon
logS-5.5ALOGPS
pKa (Strongest Acidic)11.14ChemAxon
pKa (Strongest Basic)6.23ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area78.09 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity150.83 m3·mol-1ChemAxon
Polarizability55.51 Å3ChemAxon
Number of Rings6ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General Reference
  1. Ali F, Raufi MA, Washington B, Ghali JK: Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79. Pubmed
  2. Mao ZL, Stalker D, Keirns J: Pharmacokinetics of conivaptan hydrochloride, a vasopressin V(1A)/V(2)-receptor antagonist, in patients with euvolemic or hypervolemic hyponatremia and with or without congestive heart failure from a prospective, 4-day open-label study. Clin Ther. 2009 Jul;31(7):1542-50. Pubmed
  3. Ghali JK, Farah JO, Daifallah S, Zabalawi HA, Zmily HD: Conivaptan and its role in the treatment of hyponatremia. Drug Des Devel Ther. 2009 Dec 29;3:253-68. Pubmed
External Links
ATC CodesC03XA02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (145 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
ado-trastuzumab emtansineCYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Ado-Trastuzumab Emtansine. Specifically, strong CYP3A4 inhibitors may increase concentrations of the cytotoxic DM1 component.
AlfentanilMay increase the serum concentration of CYP3A4 Substrates.
AlfuzosinMay increase the serum concentration of CYP3A4 Substrates.
AlmotriptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Almotriptan.
AlosetronCYP3A4 Inhibitors (Strong) may increase the serum concentration of Alosetron.
AlprazolamMay increase the serum concentration of CYP3A4 Substrates.
AminophyllineMay increase the serum concentration of CYP3A4 Substrates.
AmiodaroneMay increase the serum concentration of CYP3A4 Substrates.
AmlodipineMay increase the serum concentration of CYP3A4 Substrates.
ApixabanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Apixaban.
AprepitantMay increase the serum concentration of CYP3A4 Substrates.
AripiprazoleMay increase the serum concentration of CYP3A4 Substrates.
armodafinilMay increase the serum concentration of CYP3A4 Substrates.
AstemizoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of Astemizole.
AtazanavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
AtorvastatinMay increase the serum concentration of CYP3A4 Substrates.
AvanafilCYP3A4 Inhibitors (Strong) may increase the serum concentration of Avanafil.
AxitinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Axitinib.
BedaquilineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Bedaquiline.
BenzphetamineMay increase the serum concentration of CYP3A4 Substrates.
BisoprololMay increase the serum concentration of CYP3A4 Substrates.
BoceprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
BortezomibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Bortezomib.
BosentanMay decrease the serum concentration of CYP3A4 Substrates.
BosutinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Bosutinib.
Brentuximab vedotinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Brentuximab Vedotin. Specifically, concentrations of the active monomethyl auristatin E (MMAE) component may be increased.
BrinzolamideCYP3A4 Inhibitors (Strong) may increase the serum concentration of Brinzolamide.
BromocriptineMay increase the serum concentration of CYP3A4 Substrates.
BuprenorphineMay increase the serum concentration of CYP3A4 Substrates.
BuspironeMay increase the serum concentration of CYP3A4 Substrates.
CabazitaxelMay increase the serum concentration of CYP3A4 Substrates.
CabozantinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Cabozantinib.
CalcitriolMay increase the serum concentration of CYP3A4 Substrates.
CarbamazepineMay increase the serum concentration of CYP3A4 Substrates.
ChlordiazepoxideMay increase the serum concentration of CYP3A4 Substrates.
ChloroquineMay increase the serum concentration of CYP3A4 Substrates.
CilostazolMay increase the serum concentration of CYP3A4 Substrates.
CinacalcetMay increase the serum concentration of CYP3A4 Substrates.
CisaprideMay increase the serum concentration of CYP3A4 Substrates.
CitalopramMay increase the serum concentration of CYP3A4 Substrates.
ClarithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
ClidiniumMay increase the serum concentration of CYP3A4 Substrates.
ClonazepamMay increase the serum concentration of CYP3A4 Substrates.
CocaineMay increase the serum concentration of CYP3A4 Substrates.
ColchicineMay increase the serum concentration of CYP3A4 Substrates.
CrizotinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Crizotinib.
Cyproterone acetateMay increase the serum concentration of CYP3A4 Substrates.
DabrafenibMay increase the serum concentration of CYP3A4 Substrates.
DantroleneMay increase the serum concentration of CYP3A4 Substrates.
DapoxetineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dapoxetine.
DarifenacinMay increase the serum concentration of CYP3A4 Substrates.
DarunavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
DasatinibMay increase the serum concentration of CYP3A4 Substrates.
DeferasiroxMay decrease the serum concentration of CYP3A4 Substrates.
DelavirdineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
DiazepamMay increase the serum concentration of CYP3A4 Substrates.
DigoxinMay increase the serum concentration of Digoxin.
DihydroergotamineMay increase the serum concentration of CYP3A4 Substrates.
DiltiazemMay increase the serum concentration of CYP3A4 Substrates.
DisopyramideMay increase the serum concentration of CYP3A4 Substrates.
DocetaxelMay increase the serum concentration of CYP3A4 Substrates.
DofetilideCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
DomperidoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Domperidone.
DoxazosinMay increase the serum concentration of CYP3A4 Substrates.
DronabinolCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dronabinol.
DronedaroneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dronedarone.
DutasterideCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dutasteride.
EletriptanMay increase the serum concentration of CYP3A4 Substrates.
EliglustatMay increase the serum concentration of CYP3A4 Substrates.
EplerenoneMay increase the serum concentration of CYP3A4 Substrates.
Ergoloid mesylateMay increase the serum concentration of CYP3A4 Substrates.
ErgonovineMay increase the serum concentration of CYP3A4 Substrates.
ErgotamineMay increase the serum concentration of CYP3A4 Substrates.
ErlotinibMay increase the serum concentration of CYP3A4 Substrates.
EscitalopramMay increase the serum concentration of CYP3A4 Substrates.
EszopicloneMay increase the serum concentration of CYP3A4 Substrates.
Ethinyl EstradiolMay increase the serum concentration of CYP3A4 Substrates.
EthosuximideMay increase the serum concentration of CYP3A4 Substrates.
EtoposideMay increase the serum concentration of CYP3A4 Substrates.
EverolimusCYP3A4 Inhibitors (Strong) may increase the serum concentration of Everolimus.
FelbamateMay increase the serum concentration of CYP3A4 Substrates.
FelodipineMay increase the serum concentration of CYP3A4 Substrates.
FentanylMay increase the serum concentration of CYP3A4 Substrates.
FesoterodineMay increase the serum concentration of CYP3A4 Substrates.
FlurazepamMay increase the serum concentration of CYP3A4 Substrates.
FlutamideMay increase the serum concentration of CYP3A4 Substrates.
Fluticasone furoateMay increase the serum concentration of CYP3A4 Substrates.
FosamprenavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
FosaprepitantMay increase the serum concentration of CYP3A4 Substrates.
GefitinibMay increase the serum concentration of CYP3A4 Substrates.
GuanfacineMay increase the serum concentration of CYP3A4 Substrates.
HalofantrineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Halofantrine.
HaloperidolMay increase the serum concentration of CYP3A4 Substrates.
HydrocodoneMay increase the serum concentration of CYP3A4 Substrates.
IfosfamideCYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Ifosfamide.
IloperidoneCYP3A4 Inhibitors (Strong) may increase serum concentrations of the active metabolite(s) of Iloperidone. Specifically, concentrations of the metabolites P88 and P95 may be increased. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Iloperidone.
ImatinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Imatinib.
IndinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
IrinotecanMay increase the serum concentration of CYP3A4 Substrates.
IsavuconazoniumMay increase the serum concentration of CYP3A4 Substrates.
Isosorbide DinitrateMay increase the serum concentration of CYP3A4 Substrates.
Isosorbide MononitrateMay increase the serum concentration of CYP3A4 Substrates.
IsradipineMay increase the serum concentration of CYP3A4 Substrates.
ItraconazoleAntifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Conivaptan. Fluconazole and isavuconazonium considerations are addressed in separate monographs.
IvacaftorMay increase the serum concentration of CYP3A4 Substrates.
IxabepiloneMay increase the serum concentration of CYP3A4 Substrates.
KetamineMay increase the serum concentration of CYP3A4 Substrates.
LacosamideCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lacosamide.
LapatinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lapatinib.
LercanidipineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lercanidipine.
LevobupivacaineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Levobupivacaine.
LevomilnacipranMay increase the serum concentration of CYP3A4 Substrates.
LomitapideCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lomitapide.
LopinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
LovastatinMay increase the serum concentration of CYP3A4 Substrates.
LULICONAZOLEMay increase the serum concentration of CYP3A4 Substrates.
LumefantrineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lumefantrine.
LurasidoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Lurasidone.
MACITENTANCYP3A4 Inhibitors (Strong) may increase the serum concentration of Macitentan.
MaravirocMay increase the serum concentration of CYP3A4 Substrates.
MefloquineMay increase the serum concentration of CYP3A4 Substrates.
MethadoneMay increase the serum concentration of CYP3A4 Substrates.
MethylergometrineMay increase the serum concentration of CYP3A4 Substrates.
MethylprednisoloneCYP3A4 Inhibitors (Strong) may increase the serum concentration of MethylPREDNISolone.
MidazolamMay increase the serum concentration of CYP3A4 Substrates.
MifepristoneMay increase the serum concentration of CYP3A4 Substrates.
MirtazapineMay increase the serum concentration of CYP3A4 Substrates.
MitotaneMay decrease the serum concentration of CYP3A4 Substrates.
ModafinilMay increase the serum concentration of CYP3A4 Substrates.
NateglinideMay increase the serum concentration of CYP3A4 Substrates.
NefazodoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
NelfinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
NifedipineMay increase the serum concentration of CYP3A4 Substrates.
NilotinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Nilotinib.
NimodipineMay increase the serum concentration of CYP3A4 Substrates.
NisoldipineMay increase the serum concentration of CYP3A4 Substrates.
OspemifeneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Ospemifene.
OxybutyninCYP3A4 Inhibitors (Strong) may increase the serum concentration of Oxybutynin.
OxycodoneMay increase the serum concentration of CYP3A4 Substrates.
PanobinostatMay increase the serum concentration of CYP3A4 Substrates.
ParicalcitolCYP3A4 Inhibitors (Strong) may increase the serum concentration of Paricalcitol.
PazopanibMay increase the serum concentration of CYP3A4 Substrates.
PimecrolimusCYP3A4 Inhibitors (Strong) may decrease the metabolism of Pimecrolimus.
PimozideCYP3A4 Inhibitors (Strong) may increase the serum concentration of Pimozide.
PipotiazineMay increase the serum concentration of CYP3A4 Substrates.
PomalidomideMay increase the serum concentration of CYP3A4 Substrates.
PonatinibCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
PosaconazoleAntifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Conivaptan. Fluconazole and isavuconazonium considerations are addressed in separate monographs.
PranlukastCYP3A4 Inhibitors (Strong) may increase the serum concentration of Pranlukast.
PrasugrelCYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Prasugrel.
PraziquantelMay increase the serum concentration of CYP3A4 Substrates.
PrednisoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of PredniSONE.
PropafenoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Propafenone.
QuetiapineMay increase the serum concentration of CYP3A4 Substrates.
QuinidineMay increase the serum concentration of CYP3A4 Substrates.
QuinineMay increase the serum concentration of CYP3A4 Substrates.
RanolazineMay increase the serum concentration of CYP3A4 Substrates.
RegorafenibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Regorafenib.
RepaglinideCYP3A4 Inhibitors (Strong) may increase the serum concentration of Repaglinide.
RetapamulinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Retapamulin.
RilpivirineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Rilpivirine.
RitonavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
RivaroxabanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Rivaroxaban. For clarithromycin, refer to more specific clarithromycin-rivaroxaban monograph recommendations.
RomidepsinCYP3A4 Inhibitors (Strong) may increase the serum concentration of RomiDEPsin.
RuxolitinibMay increase the serum concentration of CYP3A4 Substrates.
SalmeterolCYP3A4 Inhibitors (Strong) may increase the serum concentration of Salmeterol.
SaquinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
SaxagliptinMay increase the serum concentration of CYP3A4 Substrates.
SildenafilMay increase the serum concentration of CYP3A4 Substrates.
SilodosinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Silodosin.
SiltuximabMay decrease the serum concentration of CYP3A4 Substrates.
SimeprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Simeprevir.
SimvastatinMay increase the serum concentration of CYP3A4 Substrates.
SirolimusMay increase the serum concentration of CYP3A4 Substrates.
SolifenacinMay increase the serum concentration of CYP3A4 Substrates.
SorafenibCYP3A4 Inhibitors (Strong) may increase the serum concentration of SORAfenib.
SpiramycinMay increase the serum concentration of CYP3A4 Substrates.
SufentanilMay increase the serum concentration of CYP3A4 Substrates.
SulfisoxazoleMay increase the serum concentration of CYP3A4 Substrates.
SunitinibMay increase the serum concentration of CYP3A4 Substrates.
SuvorexantCYP3A4 Inhibitors (Strong) may increase the serum concentration of Suvorexant.
TadalafilMay increase the serum concentration of CYP3A4 Substrates.
TamoxifenMay increase the serum concentration of CYP3A4 Substrates.
TamsulosinMay increase the serum concentration of CYP3A4 Substrates.
TelaprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
TelithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Conivaptan.
TemsirolimusMay increase the serum concentration of CYP3A4 Substrates.
TeniposideMay increase the serum concentration of CYP3A4 Substrates.
TerfenadineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Terfenadine.
TheophyllineMay increase the serum concentration of CYP3A4 Substrates.
TiagabineMay increase the serum concentration of CYP3A4 Substrates.
TicagrelorCYP3A4 Inhibitors (Strong) may decrease serum concentrations of the active metabolite(s) of Ticagrelor. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Ticagrelor.
TocilizumabMay decrease the serum concentration of CYP3A4 Substrates.
TofacitinibMay increase the serum concentration of CYP3A4 Substrates.
TolterodineMay increase the serum concentration of CYP3A4 Substrates.
TolvaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Tolvaptan.
ToremifeneCYP3A4 Inhibitors (Strong) may enhance the adverse/toxic effect of Toremifene. CYP3A4 Inhibitors (Strong) may increase the serum concentration of Toremifene.
TrabectedinCYP3A4 Inhibitors (Strong) may increase the serum concentration of Trabectedin.
TramadolMay increase the serum concentration of CYP3A4 Substrates.
TriazolamMay increase the serum concentration of CYP3A4 Substrates.
TrimipramineMay increase the serum concentration of CYP3A4 Substrates.
UlipristalCYP3A4 Inhibitors (Strong) may increase the serum concentration of Ulipristal.
VardenafilMay increase the serum concentration of CYP3A4 Substrates.
VemurafenibCYP3A4 Inhibitors (Strong) may increase the serum concentration of Vemurafenib.
VenlafaxineMay increase the serum concentration of CYP3A4 Substrates.
VilazodoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Vilazodone.
VinblastineMay increase the serum concentration of CYP3A4 Substrates.
VincristineMay increase the serum concentration of CYP3A4 Substrates.
VinorelbineMay increase the serum concentration of CYP3A4 Substrates.
VorapaxarCYP3A4 Inhibitors (Strong) may increase the serum concentration of Vorapaxar.
VoriconazoleAntifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Conivaptan. Fluconazole and isavuconazonium considerations are addressed in separate monographs.
ZolpidemMay increase the serum concentration of CYP3A4 Substrates.
ZonisamideMay increase the serum concentration of CYP3A4 Substrates.
ZopicloneMay increase the serum concentration of CYP3A4 Substrates.
ZuclopenthixolCYP3A4 Inhibitors (Strong) may increase the serum concentration of Zuclopenthixol.
Food InteractionsNot Available

Targets

1. Vasopressin V1a receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Vasopressin V1a receptor P37288 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Ali F, Raufi MA, Washington B, Ghali JK: Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79. Pubmed
  3. Wada K, Matsukawa U, Fujimori A, Arai Y, Sudoh K, Sasamata M, Miyata K: A novel vasopressin dual V1A/V2 receptor antagonist, conivaptan hydrochloride, improves hyponatremia in rats with syndrome of inappropriate secretion of antidiuretic hormone (SIADH). Biol Pharm Bull. 2007 Jan;30(1):91-5. Pubmed
  4. Walter KA: Conivaptan: new treatment for hyponatremia. Am J Health Syst Pharm. 2007 Jul 1;64(13):1385-95. Pubmed
  5. Mao ZL, Stalker D, Keirns J: Pharmacokinetics of conivaptan hydrochloride, a vasopressin V(1A)/V(2)-receptor antagonist, in patients with euvolemic or hypervolemic hyponatremia and with or without congestive heart failure from a prospective, 4-day open-label study. Clin Ther. 2009 Jul;31(7):1542-50. Pubmed
  6. Ghali JK, Koren MJ, Taylor JR, Brooks-Asplund E, Fan K, Long WA, Smith N: Efficacy and safety of oral conivaptan: a V1A/V2 vasopressin receptor antagonist, assessed in a randomized, placebo-controlled trial in patients with euvolemic or hypervolemic hyponatremia. J Clin Endocrinol Metab. 2006 Jun;91(6):2145-52. Epub 2006 Mar 7. Pubmed
  7. Annane D, Decaux G, Smith N: Efficacy and safety of oral conivaptan, a vasopressin-receptor antagonist, evaluated in a randomized, controlled trial in patients with euvolemic or hypervolemic hyponatremia. Am J Med Sci. 2009 Jan;337(1):28-36. Pubmed
  8. Ghali JK, Farah JO, Daifallah S, Zabalawi HA, Zmily HD: Conivaptan and its role in the treatment of hyponatremia. Drug Des Devel Ther. 2009 Dec 29;3:253-68. Pubmed
  9. Ali F, Guglin M, Vaitkevicius P, Ghali JK: Therapeutic potential of vasopressin receptor antagonists. Drugs. 2007;67(6):847-58. Pubmed
  10. Hoque MZ, Arumugham P, Huda N, Verma N, Afiniwala M, Karia DH: Conivaptan: promise of treatment in heart failure. Expert Opin Pharmacother. 2009 Sep;10(13):2161-9. Pubmed

2. Vasopressin V2 receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: antagonist

Components

Name UniProt ID Details
Vasopressin V2 receptor P30518 Details

References:

  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  2. Wada K, Fujimori A, Matsukawa U, Arai Y, Sudoh K, Yatsu T, Sasamata M, Miyata K: Intravenous administration of conivaptan hydrochloride improves cardiac hemodynamics in rats with myocardial infarction-induced congestive heart failure. Eur J Pharmacol. 2005 Jan 10;507(1-3):145-51. Epub 2005 Jan 1. Pubmed
  3. Palm C, Pistrosch F, Herbrig K, Gross P: Vasopressin antagonists as aquaretic agents for the treatment of hyponatremia. Am J Med. 2006 Jul;119(7 Suppl 1):S87-92. Pubmed
  4. Ali F, Raufi MA, Washington B, Ghali JK: Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79. Pubmed
  5. Wada K, Matsukawa U, Fujimori A, Arai Y, Sudoh K, Sasamata M, Miyata K: A novel vasopressin dual V1A/V2 receptor antagonist, conivaptan hydrochloride, improves hyponatremia in rats with syndrome of inappropriate secretion of antidiuretic hormone (SIADH). Biol Pharm Bull. 2007 Jan;30(1):91-5. Pubmed
  6. Walter KA: Conivaptan: new treatment for hyponatremia. Am J Health Syst Pharm. 2007 Jul 1;64(13):1385-95. Pubmed
  7. Mao ZL, Stalker D, Keirns J: Pharmacokinetics of conivaptan hydrochloride, a vasopressin V(1A)/V(2)-receptor antagonist, in patients with euvolemic or hypervolemic hyponatremia and with or without congestive heart failure from a prospective, 4-day open-label study. Clin Ther. 2009 Jul;31(7):1542-50. Pubmed
  8. Ghali JK, Koren MJ, Taylor JR, Brooks-Asplund E, Fan K, Long WA, Smith N: Efficacy and safety of oral conivaptan: a V1A/V2 vasopressin receptor antagonist, assessed in a randomized, placebo-controlled trial in patients with euvolemic or hypervolemic hyponatremia. J Clin Endocrinol Metab. 2006 Jun;91(6):2145-52. Epub 2006 Mar 7. Pubmed
  9. Annane D, Decaux G, Smith N: Efficacy and safety of oral conivaptan, a vasopressin-receptor antagonist, evaluated in a randomized, controlled trial in patients with euvolemic or hypervolemic hyponatremia. Am J Med Sci. 2009 Jan;337(1):28-36. Pubmed
  10. Ghali JK, Farah JO, Daifallah S, Zabalawi HA, Zmily HD: Conivaptan and its role in the treatment of hyponatremia. Drug Des Devel Ther. 2009 Dec 29;3:253-68. Pubmed
  11. Ali F, Guglin M, Vaitkevicius P, Ghali JK: Therapeutic potential of vasopressin receptor antagonists. Drugs. 2007;67(6):847-58. Pubmed
  12. Hoque MZ, Arumugham P, Huda N, Verma N, Afiniwala M, Karia DH: Conivaptan: promise of treatment in heart failure. Expert Opin Pharmacother. 2009 Sep;10(13):2161-9. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Ali F, Raufi MA, Washington B, Ghali JK: Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. Cardiovasc Drug Rev. 2007 Fall;25(3):261-79. Pubmed

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12