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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
4'-((4,5-dihydro-2-Methylimidazo(4,5-D)(1)benzazepin-6(1H)-yl)carbonyl)-2-biphenylcarboxanilide
Conivaptan
External Identifiers
  • YM 087
  • YM-087
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Vaprisol Dextrose In Plastic Containerinjection, solution20 mg/100mLintravenousCumberland Pharmaceuticals Inc.2008-10-082016-04-05Us
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
Categories
UNII0NJ98Y462X
CAS number210101-16-9
WeightAverage: 498.5744
Monoisotopic: 498.205576096
Chemical FormulaC32H26N4O2
InChI KeyInChIKey=IKENVDNFQMCRTR-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.
Related Articles
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 inhibitorInhibitor0.5368
CYP450 2D6 inhibitorNon-inhibitor0.6597
CYP450 2C19 inhibitorInhibitor0.8477
CYP450 3A4 inhibitorInhibitor0.9027
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
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Astellas pharma us inc
Packagers
Dosage forms
FormRouteStrength
Injection, solutionintravenous20 mg/100mL
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
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5723606 No1999-12-152019-12-15Us
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 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:17919259 ]
  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. doi: 10.1016/j.clinthera.2009.07.011. [PubMed:19695403 ]
  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:20054444 ]
External Links
ATC CodesC03XA02
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (145 KB)
MSDSNot Available
Interactions
Drug Interactions
Drug
ado-trastuzumab emtansineThe serum concentration of ado-trastuzumab emtansine can be increased when it is combined with Conivaptan.
AlfentanilThe serum concentration of Alfentanil can be increased when it is combined with Conivaptan.
AlfuzosinThe serum concentration of Alfuzosin can be increased when it is combined with Conivaptan.
AlitretinoinThe serum concentration of Alitretinoin can be increased when it is combined with Conivaptan.
AlprazolamThe serum concentration of Alprazolam can be increased when it is combined with Conivaptan.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Conivaptan.
AmiodaroneThe serum concentration of Amiodarone can be increased when it is combined with Conivaptan.
AmlodipineThe serum concentration of Amlodipine can be increased when it is combined with Conivaptan.
ApixabanThe serum concentration of Apixaban can be increased when it is combined with Conivaptan.
AprepitantThe serum concentration of Aprepitant can be increased when it is combined with Conivaptan.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Conivaptan.
ArmodafinilThe serum concentration of Armodafinil can be increased when it is combined with Conivaptan.
AtazanavirThe serum concentration of Conivaptan can be increased when it is combined with Atazanavir.
AtorvastatinThe serum concentration of Atorvastatin can be increased when it is combined with Conivaptan.
AvanafilThe serum concentration of Avanafil can be increased when it is combined with Conivaptan.
AxitinibThe serum concentration of Axitinib can be increased when it is combined with Conivaptan.
BenzphetamineThe serum concentration of Benzphetamine can be increased when it is combined with Conivaptan.
BexaroteneThe serum concentration of Conivaptan can be decreased when it is combined with Bexarotene.
BisoprololThe serum concentration of Bisoprolol can be increased when it is combined with Conivaptan.
BoceprevirThe serum concentration of Conivaptan can be increased when it is combined with Boceprevir.
BosentanThe serum concentration of Conivaptan can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Bosutinib can be increased when it is combined with Conivaptan.
BrexpiprazoleThe serum concentration of Brexpiprazole can be increased when it is combined with Conivaptan.
BromocriptineThe serum concentration of Bromocriptine can be increased when it is combined with Conivaptan.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Conivaptan.
BuprenorphineThe serum concentration of Buprenorphine can be increased when it is combined with Conivaptan.
BuspironeThe serum concentration of Buspirone can be increased when it is combined with Conivaptan.
CabazitaxelThe serum concentration of Cabazitaxel can be increased when it is combined with Conivaptan.
CabozantinibThe serum concentration of Cabozantinib can be increased when it is combined with Conivaptan.
CalcitriolThe serum concentration of Calcitriol can be increased when it is combined with Conivaptan.
CarbamazepineThe serum concentration of Carbamazepine can be increased when it is combined with Conivaptan.
CeritinibThe serum concentration of Conivaptan can be increased when it is combined with Ceritinib.
ChlordiazepoxideThe serum concentration of Chlordiazepoxide can be increased when it is combined with Conivaptan.
ChloroquineThe serum concentration of Chloroquine can be increased when it is combined with Conivaptan.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Conivaptan.
CinacalcetThe serum concentration of Cinacalcet can be increased when it is combined with Conivaptan.
CisaprideThe serum concentration of Cisapride can be increased when it is combined with Conivaptan.
CitalopramThe serum concentration of Citalopram can be increased when it is combined with Conivaptan.
ClarithromycinThe serum concentration of Conivaptan can be increased when it is combined with Clarithromycin.
ClonazepamThe serum concentration of Clonazepam can be increased when it is combined with Conivaptan.
ClorazepateThe serum concentration of Clorazepate can be increased when it is combined with Conivaptan.
CobicistatThe serum concentration of Conivaptan can be increased when it is combined with Cobicistat.
CobimetinibThe serum concentration of Cobimetinib can be increased when it is combined with Conivaptan.
CocaineThe serum concentration of Cocaine can be increased when it is combined with Conivaptan.
ColchicineThe serum concentration of Colchicine can be increased when it is combined with Conivaptan.
CrizotinibThe serum concentration of Crizotinib can be increased when it is combined with Conivaptan.
CyclosporineThe serum concentration of Cyclosporine can be increased when it is combined with Conivaptan.
Cyproterone acetateThe serum concentration of Cyproterone acetate can be increased when it is combined with Conivaptan.
DabrafenibThe serum concentration of Dabrafenib can be increased when it is combined with Conivaptan.
DaclatasvirThe serum concentration of Daclatasvir can be increased when it is combined with Conivaptan.
DantroleneThe serum concentration of Dantrolene can be increased when it is combined with Conivaptan.
DapsoneThe serum concentration of Dapsone can be increased when it is combined with Conivaptan.
DarifenacinThe serum concentration of Darifenacin can be increased when it is combined with Conivaptan.
DarunavirThe serum concentration of Conivaptan can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Dasatinib can be increased when it is combined with Conivaptan.
DeferasiroxThe serum concentration of Conivaptan can be decreased when it is combined with Deferasirox.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Conivaptan.
DiazepamThe serum concentration of Diazepam can be increased when it is combined with Conivaptan.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Conivaptan.
DihydroergotamineThe serum concentration of Dihydroergotamine can be increased when it is combined with Conivaptan.
DiltiazemThe serum concentration of Diltiazem can be increased when it is combined with Conivaptan.
DisopyramideThe serum concentration of Disopyramide can be increased when it is combined with Conivaptan.
DocetaxelThe serum concentration of Docetaxel can be increased when it is combined with Conivaptan.
DofetilideThe serum concentration of Dofetilide can be increased when it is combined with Conivaptan.
DomperidoneThe serum concentration of Domperidone can be increased when it is combined with Conivaptan.
DoxazosinThe serum concentration of Doxazosin can be increased when it is combined with Conivaptan.
DoxorubicinThe serum concentration of Doxorubicin can be increased when it is combined with Conivaptan.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Conivaptan.
DronedaroneThe serum concentration of Dronedarone can be increased when it is combined with Conivaptan.
EletriptanThe serum concentration of Eletriptan can be increased when it is combined with Conivaptan.
EliglustatThe serum concentration of Eliglustat can be increased when it is combined with Conivaptan.
EplerenoneThe serum concentration of Eplerenone can be increased when it is combined with Conivaptan.
Ergoloid mesylateThe serum concentration of Ergoloid mesylate can be increased when it is combined with Conivaptan.
ErgonovineThe serum concentration of Ergonovine can be increased when it is combined with Conivaptan.
ErgotamineThe serum concentration of Ergotamine can be increased when it is combined with Conivaptan.
ErlotinibThe serum concentration of Erlotinib can be increased when it is combined with Conivaptan.
ErythromycinThe serum concentration of Erythromycin can be increased when it is combined with Conivaptan.
EscitalopramThe serum concentration of Escitalopram can be increased when it is combined with Conivaptan.
EszopicloneThe serum concentration of Eszopiclone can be increased when it is combined with Conivaptan.
EthosuximideThe serum concentration of Ethosuximide can be increased when it is combined with Conivaptan.
EtoposideThe serum concentration of Etoposide can be increased when it is combined with Conivaptan.
EverolimusThe serum concentration of Everolimus can be increased when it is combined with Conivaptan.
FelbamateThe serum concentration of Felbamate can be increased when it is combined with Conivaptan.
FelodipineThe serum concentration of Felodipine can be increased when it is combined with Conivaptan.
FentanylThe serum concentration of Fentanyl can be increased when it is combined with Conivaptan.
FesoterodineThe serum concentration of Fesoterodine can be increased when it is combined with Conivaptan.
FlibanserinThe serum concentration of Flibanserin can be increased when it is combined with Conivaptan.
FluconazoleThe metabolism of Conivaptan can be decreased when combined with Fluconazole.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Conivaptan.
FlurazepamThe serum concentration of Flurazepam can be increased when it is combined with Conivaptan.
FlutamideThe serum concentration of Flutamide can be increased when it is combined with Conivaptan.
FosaprepitantThe serum concentration of Fosaprepitant can be increased when it is combined with Conivaptan.
Fusidic AcidThe serum concentration of Conivaptan can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Gefitinib can be increased when it is combined with Conivaptan.
GuanfacineThe serum concentration of Guanfacine can be increased when it is combined with Conivaptan.
HaloperidolThe serum concentration of Haloperidol can be increased when it is combined with Conivaptan.
HydrocodoneThe serum concentration of Hydrocodone can be increased when it is combined with Conivaptan.
Hydroxyprogesterone caproateThe serum concentration of Hydroxyprogesterone caproate can be increased when it is combined with Conivaptan.
IbrutinibThe serum concentration of Ibrutinib can be increased when it is combined with Conivaptan.
IdelalisibThe serum concentration of Conivaptan can be increased when it is combined with Idelalisib.
IfosfamideThe serum concentration of the active metabolites of Ifosfamide can be reduced when Ifosfamide is used in combination with Conivaptan resulting in a loss in efficacy.
ImatinibThe serum concentration of Imatinib can be increased when it is combined with Conivaptan.
IndinavirThe serum concentration of Conivaptan can be increased when it is combined with Indinavir.
IrinotecanThe serum concentration of Irinotecan can be increased when it is combined with Conivaptan.
IsavuconazoniumThe serum concentration of Isavuconazonium can be increased when it is combined with Conivaptan.
IsosorbideThe serum concentration of Isosorbide can be increased when it is combined with Conivaptan.
Isosorbide DinitrateThe serum concentration of Isosorbide Dinitrate can be increased when it is combined with Conivaptan.
Isosorbide MononitrateThe serum concentration of Isosorbide Mononitrate can be increased when it is combined with Conivaptan.
IsradipineThe serum concentration of Isradipine can be increased when it is combined with Conivaptan.
ItraconazoleThe metabolism of Conivaptan can be decreased when combined with Itraconazole.
IvabradineThe serum concentration of Ivabradine can be increased when it is combined with Conivaptan.
IvacaftorThe serum concentration of Ivacaftor can be increased when it is combined with Conivaptan.
IxabepiloneThe serum concentration of Ixabepilone can be increased when it is combined with Conivaptan.
KetamineThe serum concentration of Ketamine can be increased when it is combined with Conivaptan.
KetoconazoleThe metabolism of Conivaptan can be decreased when combined with Ketoconazole.
LapatinibThe serum concentration of Lapatinib can be increased when it is combined with Conivaptan.
LevomilnacipranThe serum concentration of Levomilnacipran can be increased when it is combined with Conivaptan.
LidocaineThe serum concentration of Lidocaine can be increased when it is combined with Conivaptan.
LomitapideThe serum concentration of Lomitapide can be increased when it is combined with Conivaptan.
LovastatinThe serum concentration of Lovastatin can be increased when it is combined with Conivaptan.
LuliconazoleThe serum concentration of Conivaptan can be increased when it is combined with Luliconazole.
LurasidoneThe serum concentration of Lurasidone can be increased when it is combined with Conivaptan.
MACITENTANThe serum concentration of MACITENTAN can be increased when it is combined with Conivaptan.
MaravirocThe serum concentration of Maraviroc can be increased when it is combined with Conivaptan.
MefloquineThe serum concentration of Mefloquine can be increased when it is combined with Conivaptan.
MethadoneThe serum concentration of Methadone can be increased when it is combined with Conivaptan.
MidazolamThe serum concentration of Midazolam can be increased when it is combined with Conivaptan.
MifepristoneThe serum concentration of Mifepristone can be increased when it is combined with Conivaptan.
MirtazapineThe serum concentration of Mirtazapine can be increased when it is combined with Conivaptan.
MitotaneThe serum concentration of Conivaptan can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Modafinil can be increased when it is combined with Conivaptan.
NaloxegolThe serum concentration of Naloxegol can be increased when it is combined with Conivaptan.
NateglinideThe serum concentration of Nateglinide can be increased when it is combined with Conivaptan.
NefazodoneThe serum concentration of Conivaptan can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Conivaptan can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Conivaptan can be increased when it is combined with Netupitant.
NicardipineThe serum concentration of Nicardipine can be increased when it is combined with Conivaptan.
NifedipineThe serum concentration of Nifedipine can be increased when it is combined with Conivaptan.
NilotinibThe serum concentration of Nilotinib can be increased when it is combined with Conivaptan.
NimodipineThe serum concentration of Nimodipine can be increased when it is combined with Conivaptan.
NisoldipineThe serum concentration of Nisoldipine can be increased when it is combined with Conivaptan.
OlaparibThe serum concentration of Olaparib can be increased when it is combined with Conivaptan.
OxycodoneThe serum concentration of Oxycodone can be increased when it is combined with Conivaptan.
PaclitaxelThe serum concentration of Paclitaxel can be increased when it is combined with Conivaptan.
PalbociclibThe serum concentration of Palbociclib can be increased when it is combined with Conivaptan.
PanobinostatThe serum concentration of Panobinostat can be increased when it is combined with Conivaptan.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Conivaptan.
PhenytoinThe metabolism of Conivaptan can be increased when combined with Phenytoin.
PimecrolimusThe metabolism of Pimecrolimus can be decreased when combined with Conivaptan.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Conivaptan.
PipotiazineThe serum concentration of Pipotiazine can be increased when it is combined with Conivaptan.
PosaconazoleThe metabolism of Conivaptan can be decreased when combined with Posaconazole.
PraziquantelThe serum concentration of Praziquantel can be increased when it is combined with Conivaptan.
PropafenoneThe serum concentration of Propafenone can be increased when it is combined with Conivaptan.
QuetiapineThe serum concentration of Quetiapine can be increased when it is combined with Conivaptan.
QuinidineThe serum concentration of Quinidine can be increased when it is combined with Conivaptan.
QuinineThe serum concentration of Quinine can be increased when it is combined with Conivaptan.
RanolazineThe serum concentration of Ranolazine can be increased when it is combined with Conivaptan.
RegorafenibThe serum concentration of Regorafenib can be increased when it is combined with Conivaptan.
RitonavirThe serum concentration of Conivaptan can be increased when it is combined with Ritonavir.
RuxolitinibThe serum concentration of Ruxolitinib can be increased when it is combined with Conivaptan.
SalmeterolThe serum concentration of Salmeterol can be increased when it is combined with Conivaptan.
SaquinavirThe serum concentration of Conivaptan can be increased when it is combined with Saquinavir.
SaxagliptinThe serum concentration of Saxagliptin can be increased when it is combined with Conivaptan.
SildenafilThe serum concentration of Sildenafil can be increased when it is combined with Conivaptan.
SilodosinThe serum concentration of Silodosin can be increased when it is combined with Conivaptan.
SiltuximabThe serum concentration of Conivaptan can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Simeprevir can be increased when it is combined with Conivaptan.
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Conivaptan.
SirolimusThe serum concentration of Sirolimus can be increased when it is combined with Conivaptan.
SolifenacinThe serum concentration of Solifenacin can be increased when it is combined with Conivaptan.
SonidegibThe serum concentration of Sonidegib can be increased when it is combined with Conivaptan.
SpiramycinThe serum concentration of Spiramycin can be increased when it is combined with Conivaptan.
St. John's WortThe serum concentration of Conivaptan can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Stiripentol can be increased when it is combined with Conivaptan.
SufentanilThe serum concentration of Sufentanil can be increased when it is combined with Conivaptan.
SunitinibThe serum concentration of Sunitinib can be increased when it is combined with Conivaptan.
SuvorexantThe serum concentration of Suvorexant can be increased when it is combined with Conivaptan.
TacrolimusThe serum concentration of Tacrolimus can be increased when it is combined with Conivaptan.
TadalafilThe serum concentration of Tadalafil can be increased when it is combined with Conivaptan.
TamoxifenThe serum concentration of Tamoxifen can be increased when it is combined with Conivaptan.
TamsulosinThe serum concentration of Tamsulosin can be increased when it is combined with Conivaptan.
TelaprevirThe serum concentration of Conivaptan can be increased when it is combined with Telaprevir.
TelithromycinThe serum concentration of Conivaptan can be increased when it is combined with Telithromycin.
TemsirolimusThe serum concentration of Temsirolimus can be increased when it is combined with Conivaptan.
TeniposideThe serum concentration of Teniposide can be increased when it is combined with Conivaptan.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Conivaptan.
TiagabineThe serum concentration of Tiagabine can be increased when it is combined with Conivaptan.
TocilizumabThe serum concentration of Conivaptan can be decreased when it is combined with Tocilizumab.
TofacitinibThe serum concentration of Tofacitinib can be increased when it is combined with Conivaptan.
TolterodineThe serum concentration of Tolterodine can be increased when it is combined with Conivaptan.
TolvaptanThe serum concentration of Tolvaptan can be increased when it is combined with Conivaptan.
TrabectedinThe serum concentration of Trabectedin can be increased when it is combined with Conivaptan.
TrazodoneThe serum concentration of Trazodone can be increased when it is combined with Conivaptan.
TriazolamThe serum concentration of Triazolam can be increased when it is combined with Conivaptan.
TrimipramineThe serum concentration of Trimipramine can be increased when it is combined with Conivaptan.
UlipristalThe serum concentration of Ulipristal can be increased when it is combined with Conivaptan.
VardenafilThe serum concentration of Vardenafil can be increased when it is combined with Conivaptan.
VemurafenibThe serum concentration of Vemurafenib can be increased when it is combined with Conivaptan.
VenlafaxineThe serum concentration of Venlafaxine can be increased when it is combined with Conivaptan.
VerapamilThe serum concentration of Verapamil can be increased when it is combined with Conivaptan.
VilazodoneThe serum concentration of Vilazodone can be increased when it is combined with Conivaptan.
VinblastineThe serum concentration of Vinblastine can be increased when it is combined with Conivaptan.
VincristineThe serum concentration of Vincristine can be increased when it is combined with Conivaptan.
VindesineThe serum concentration of Vindesine can be increased when it is combined with Conivaptan.
VinorelbineThe serum concentration of Vinorelbine can be increased when it is combined with Conivaptan.
VoriconazoleThe metabolism of Conivaptan can be decreased when combined with Voriconazole.
ZolpidemThe serum concentration of Zolpidem can be increased when it is combined with Conivaptan.
ZonisamideThe serum concentration of Zonisamide can be increased when it is combined with Conivaptan.
ZopicloneThe serum concentration of Zopiclone can be increased when it is combined with Conivaptan.
ZuclopenthixolThe serum concentration of Zuclopenthixol can be increased when it is combined with Conivaptan.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Vasopressin receptor activity
Specific Function:
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate a phosphatidyl-inositol-calcium second messenger system. Has been involved in social behaviors, including affiliation and attachment.
Gene Name:
AVPR1A
Uniprot ID:
P37288
Molecular Weight:
46799.105 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  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:17919259 ]
  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:17202666 ]
  4. Walter KA: Conivaptan: new treatment for hyponatremia. Am J Health Syst Pharm. 2007 Jul 1;64(13):1385-95. [PubMed:17592003 ]
  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. doi: 10.1016/j.clinthera.2009.07.011. [PubMed:19695403 ]
  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:16522696 ]
  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. doi: 10.1097/MAJ.0b013e31817b8148. [PubMed:19057376 ]
  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:20054444 ]
  9. Ali F, Guglin M, Vaitkevicius P, Ghali JK: Therapeutic potential of vasopressin receptor antagonists. Drugs. 2007;67(6):847-58. [PubMed:17428103 ]
  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. doi: 10.1517/14656560903173237. [PubMed:19663609 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Vasopressin receptor activity
Specific Function:
Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Involved in renal water reabsorption.
Gene Name:
AVPR2
Uniprot ID:
P30518
Molecular Weight:
40278.57 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  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:15659304 ]
  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:16843091 ]
  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:17919259 ]
  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:17202666 ]
  6. Walter KA: Conivaptan: new treatment for hyponatremia. Am J Health Syst Pharm. 2007 Jul 1;64(13):1385-95. [PubMed:17592003 ]
  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. doi: 10.1016/j.clinthera.2009.07.011. [PubMed:19695403 ]
  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:16522696 ]
  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. doi: 10.1097/MAJ.0b013e31817b8148. [PubMed:19057376 ]
  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:20054444 ]
  11. Ali F, Guglin M, Vaitkevicius P, Ghali JK: Therapeutic potential of vasopressin receptor antagonists. Drugs. 2007;67(6):847-58. [PubMed:17428103 ]
  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. doi: 10.1517/14656560903173237. [PubMed:19663609 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
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:17919259 ]
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Drug created on June 13, 2005 07:24 / Updated on May 03, 2016 02:29