- Molecular NameConivaptan
- Synonymconivaptan; Conivaptan hydrochloride; YM 087; YM-087
- Weight498.586
- Drugbank_IDDB00872
- ACS_NO210101-16-9
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- LogP (experiment)5.955
- LogP (predicted, AB/LogP v2.0)4.43
- pkaN/A
- LogD (pH=7, predicted)4.41
- Solubility (experiment)0.00015 mg/ml
- LogS (predicted, ACD/Labs)(ph=7)-5.52
- LogSw (predicted, AB/LogsW2.0)0.0
- Sw (mg/ml) (predicted, ACD/Labs)0.0
- No.of HBond Donors2
- No.of HBond Acceptors6
- No.of Rotatable Bonds4
- TPSA78.09
- StatusFDA approved
- Administrationintravenous
- PharmacologyA 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), and there is some evidence it may be effective in heart failure.
- Absorption_valueN/A
- Absorption (description)N/A
- Caco_2N/A
- Bioavailability42.0
- Protein binding99.0
- Volume of distribution (VD)N/A
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmCYP3A4 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.
- Half life5 h
- ExcretionN/A
- Urinary ExcretionN/A
- CleranceN/A
- 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.
- LD50 (rat)N/A
- LD50 (mouse)N/A