Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C32H26N4O2.ClH |
| Molecular Weight | 535.035 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CC1=NC2=C(N1)C3=CC=CC=C3N(CC2)C(=O)C4=CC=C(NC(=O)C5=CC=CC=C5C6=CC=CC=C6)C=C4
InChI
InChIKey=BTYHAFSDANBVMJ-UHFFFAOYSA-N
InChI=1S/C32H26N4O2.ClH/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);1H
| Molecular Formula | C32H26N4O2 |
| Molecular Weight | 498.5744 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
| Molecular Formula | ClH |
| Molecular Weight | 36.461 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionSources: https://www.drugs.com/ppa/conivaptan.htmlCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21409494 |
https://www.ncbi.nlm.nih.gov/pubmed/18926434
Sources: https://www.drugs.com/ppa/conivaptan.html
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/21409494 |
https://www.ncbi.nlm.nih.gov/pubmed/18926434
Conivaptan is an arginine vasopressin (AVP) receptor antagonist with affinity for AVP receptor subtypes V1A and V2. The antidiuretic action of AVP is mediated through activation of the V2 receptor, which functions to regulate water and electrolyte balance at the level of the collecting ducts in the kidney. Conivaptan was approved in 2004 for hyponatremia caused by syndrome of inappropriate antidiuretic hormone. Conicaptan is being evaluated for reduce intracranial pressure in patients with traumatic brain injury, and as a treatment for heart failure.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL1889 |
0.43 nM [Ki] | ||
Target ID: CHEMBL1790 |
0.36 nM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | VAPRISOL IN 5% DEXTROSE IN PLASTIC CONTAINER Approved UseVAPRISOL is a vasopressin receptor antagonist indicated to raise serum sodium in hospitalized patients with euvolemic and hypervolemic hyponatremia. Launch Date2005 |
|||
| Palliative | Unknown Approved UseUnknown |
|||
| Palliative | Unknown Approved UseUnknown |
|||
| Palliative | Unknown Approved UseUnknown |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
619 ng/mL |
40 mg/kg single, intravenous dose: 40 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
CONIVAPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
2681 ng/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/10638391 |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CONIVAPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
4813 ng × h/mL EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/10638391 |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CONIVAPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
5 h |
40 mg/kg single, intravenous dose: 40 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
CONIVAPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
|
3.1 h EXPERIMENT https://www.ncbi.nlm.nih.gov/pubmed/10638391 |
50 mg single, intravenous dose: 50 mg route of administration: Intravenous experiment type: SINGLE co-administered: |
CONIVAPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1% |
40 mg/kg single, intravenous dose: 40 mg/kg route of administration: Intravenous experiment type: SINGLE co-administered: |
CONIVAPTAN plasma | Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
80 mg 1 times / day multiple, oral Highest studied dose Dose: 80 mg, 1 times / day Route: oral Route: multiple Dose: 80 mg, 1 times / day Sources: |
unhealthy, 68.7 years (range: 35–90 years) Health Status: unhealthy Age Group: 68.7 years (range: 35–90 years) Sex: M+F Sources: |
|
120 mg 1 times / day multiple, intravenous Highest studied dose Dose: 120 mg, 1 times / day Route: intravenous Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Other AEs: Hypotension, Thirst... Other AEs: Hypotension Sources: Thirst |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
Disc. AE: Hypopituitarism, Infusion site reaction... AEs leading to discontinuation/dose reduction: Hypopituitarism (0.2%) Sources: Infusion site reaction (0.2%) Infusion site phlebitis (1.6%) Infusion related reaction (0.2%) Sepsis NOS (0.2%) Pneumonia NOS (0.2%) Blood creatinine increased (0.2%) Blood sodium increased (0.2%) Blood urea increased (0.2%) Heart rate increased (0.2%) Hypernatremia (0.8%) Epilepsy NOS (0.2%) Agitation (0.2%) Renal failure acute (0.2%) Respiratory arrest (0.2%) Respiratory failure (0.2%) Cyanosis peripheral (0.2%) Phlebitis NOS (0.2%) Phlebitis superficial (0.2%) |
12.5 mg single, intravenous Dose: 12.5 mg Route: intravenous Route: single Dose: 12.5 mg Sources: |
unhealthy |
Other AEs: Dizziness... Other AEs: Dizziness (below serious, 1 patient) Sources: |
20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
Other AEs: Coagulopathy, Cardiac failure congestive... Other AEs: Coagulopathy (serious, 1 patient) Sources: Cardiac failure congestive (serious, 2 patients) Multi-organ failure (serious, 1 patient) Hyponatraemia (serious, 1 patient) Transient ischaemic attack (serious, 1 patient) Renal failure (serious, 1 patient) Respiratory distress (serious, 1 patient) Hypocoagulable state (below serious, 1 patient) Leukocytosis (below serious, 1 patient) Arrhythmia ventricular (below serious, 1 patient) Abdominal discomfort (below serious, 1 patient) Abdominal distension (below serious, 2 patients) Abnormal bowel sounds (below serious, 1 patient) Constipation (below serious, 2 patients) Nausea (below serious, 2 patients) Fatigue (below serious, 1 patient) Hypothermia (below serious, 1 patient) Pain (below serious, 2 patients) Procedural pain (below serious, 1 patient) Breath sounds abnormal (below serious, 1 patient) Chest X-ray abnormal (below serious, 1 patient) Hypoalbuminaemia (below serious, 1 patient) Hypomagnesaemia (below serious, 2 patients) Hypophosphataemia (below serious, 1 patient) Hypovolaemia (below serious, 1 patient) Muscle spasms (below serious, 1 patient) Headache (below serious, 1 patient) Lethargy (below serious, 1 patient) Anxiety (below serious, 1 patient) Dysuria (below serious, 1 patient) Cough (below serious, 1 patient) Postnasal drip (below serious, 1 patient) Rales (below serious, 1 patient) Pruritus (below serious, 1 patient) Hypotension (below serious, 3 patients) |
20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
Other AEs: Cardiac failure congestive, Pneumonia... Other AEs: Cardiac failure congestive (serious, 1 patient) Sources: Pneumonia (serious, 1 patient) Respiratory acidosis (serious, 1 patient) Coronary artery bypass (serious, 1 patient) Hypotension (serious, 1 patient) Dry eye (below serious, 1 patient) Constipation (below serious, 2 patients) Nausea (below serious, 1 patient) Vomiting (below serious, 2 patients) Chest pain (below serious, 1 patient) Fatigue (below serious, 1 patient) Oedema peripheral (below serious, 1 patient) Bronchitis chronic (below serious, 1 patient) Contusion (below serious, 1 patient) Blood pressure decreased (below serious, 1 patient) Cardiac murmur (below serious, 1 patient) Carotid bruit (below serious, 1 patient) Heart sounds abnormal (below serious, 1 patient) Dehydration (below serious, 1 patient) Hypernatraemia (below serious, 1 patient) Hypokalaemia (below serious, 1 patient) Neck pain (below serious, 1 patient) Headache (below serious, 1 patient) Insomnia (below serious, 2 patients) Psychotic disorder (below serious, 1 patient) Haematuria (below serious, 1 patient) Pruritus (below serious, 1 patient) Haematoma (below serious, 1 patient) Thrombophlebitis (below serious, 1 patient) |
22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
Other AEs: Atrial tachycardia, Urinary tract infection... Other AEs: Atrial tachycardia (serious, 1 patient) Sources: Urinary tract infection (serious, 1 patient) Encephalopathy hepatic (serious, 1 patient) Atrial flutter (below serious, 1 patient) Nausea (below serious, 1 patient) Vomiting (below serious, 1 patient) Polydipsia (below serious, 1 patient) Back pain (below serious, 1 patient) Productive cough (below serious, 1 patient) Dry skin (below serious, 1 patient) Phlebitis (below serious, 2 patients) |
60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
Other AEs: Cardiac arrest, Atrial flutter... Other AEs: Cardiac arrest (serious, 1 patient) Sources: Atrial flutter (below serious, 1 patient) Ventricular tachycardia (below serious, 1 patient) Constipation (below serious, 1 patient) Infusion site erythema (below serious, 3 patients) Infusion site pain (below serious, 1 patient) Pyrexia (below serious, 1 patient) Heart rate increased (below serious, 1 patient) Muscle spasms (below serious, 1 patient) Pain in extremity (below serious, 1 patient) Headache (below serious, 1 patient) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Hypotension | 120 mg 1 times / day multiple, intravenous Highest studied dose Dose: 120 mg, 1 times / day Route: intravenous Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
|
| Thirst | 120 mg 1 times / day multiple, intravenous Highest studied dose Dose: 120 mg, 1 times / day Route: intravenous Route: multiple Dose: 120 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
|
| Agitation | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Blood creatinine increased | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Blood sodium increased | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Blood urea increased | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Cyanosis peripheral | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Epilepsy NOS | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Heart rate increased | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Hypopituitarism | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Infusion related reaction | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Infusion site reaction | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Phlebitis NOS | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Phlebitis superficial | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Pneumonia NOS | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Renal failure acute | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Respiratory arrest | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Respiratory failure | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Sepsis NOS | 0.2% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Hypernatremia | 0.8% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Infusion site phlebitis | 1.6% Disc. AE |
40 mg 1 times / day multiple, intravenous Recommended Dose: 40 mg, 1 times / day Route: intravenous Route: multiple Dose: 40 mg, 1 times / day Sources: |
unhealthy, adult Health Status: unhealthy Age Group: adult Sources: |
| Dizziness | below serious, 1 patient | 12.5 mg single, intravenous Dose: 12.5 mg Route: intravenous Route: single Dose: 12.5 mg Sources: |
unhealthy |
| Abdominal discomfort | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Abnormal bowel sounds | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Anxiety | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Arrhythmia ventricular | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Breath sounds abnormal | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Chest X-ray abnormal | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Cough | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Dysuria | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Fatigue | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Headache | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hypoalbuminaemia | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hypocoagulable state | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hypophosphataemia | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hypothermia | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hypovolaemia | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Lethargy | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Leukocytosis | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Muscle spasms | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Postnasal drip | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Procedural pain | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Pruritus | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Rales | below serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Abdominal distension | below serious, 2 patients | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Constipation | below serious, 2 patients | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hypomagnesaemia | below serious, 2 patients | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Nausea | below serious, 2 patients | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Pain | below serious, 2 patients | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hypotension | below serious, 3 patients | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Coagulopathy | serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Hyponatraemia | serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Multi-organ failure | serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Renal failure | serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Respiratory distress | serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Transient ischaemic attack | serious, 1 patient | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Cardiac failure congestive | serious, 2 patients | 20 mg 1 times / day multiple, intravenous Dose: 20 mg, 1 times / day Route: intravenous Route: multiple Dose: 20 mg, 1 times / day Sources: |
unhealthy |
| Blood pressure decreased | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Bronchitis chronic | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Cardiac murmur | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Carotid bruit | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Chest pain | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Contusion | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Dehydration | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Dry eye | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Fatigue | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Haematoma | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Haematuria | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Headache | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Heart sounds abnormal | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Hypernatraemia | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Hypokalaemia | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Nausea | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Neck pain | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Oedema peripheral | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Pruritus | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Psychotic disorder | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Thrombophlebitis | below serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Constipation | below serious, 2 patients | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Insomnia | below serious, 2 patients | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Vomiting | below serious, 2 patients | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Cardiac failure congestive | serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Coronary artery bypass | serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Hypotension | serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Pneumonia | serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Respiratory acidosis | serious, 1 patient | 20 mg 2 times / day multiple, intravenous Dose: 20 mg, 2 times / day Route: intravenous Route: multiple Dose: 20 mg, 2 times / day Sources: |
unhealthy |
| Atrial flutter | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Back pain | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Dry skin | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Nausea | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Polydipsia | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Productive cough | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Vomiting | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Phlebitis | below serious, 2 patients | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Atrial tachycardia | serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Encephalopathy hepatic | serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Urinary tract infection | serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy |
| Atrial flutter | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Constipation | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Headache | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Heart rate increased | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Infusion site pain | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Muscle spasms | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Pain in extremity | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Pyrexia | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Ventricular tachycardia | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Infusion site erythema | below serious, 3 patients | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
| Cardiac arrest | serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 20, 48 |
strong [IC50 0.47 uM] | yes (co-administration study) Comment: coadministration with midazolam or simvastatin significantly increased both CYP3A4 substrates Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 20, 48 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 48.0 |
weak [IC50 198.3 uM] | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 48.0 |
yes [IC50 12.6 uM] | |||
Page: 10, 48 |
yes [IC50 13.3 uM] | yes (co-administration study) Comment: coadministration with warfarin increased warfarin WUC by 14% amd Cmax by 17% Page: 10, 48 |
||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 48.0 |
yes [IC50 19.2 uM] | |||
Page: 10, 21 |
yes | yes (co-administration study) Comment: coadministration with digoxin resulted in increased Cmax by 79% and AUC by 43% Page: 10, 21 |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 21, 48 |
yes | |||
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 38.0 |
yes | yes (co-administration study) Comment: ketoconazole increased conivaptan AUC 11-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2005/021697s000_Vaprisol_BIOPHARMR.pdf Page: 38.0 |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
Page: 20, 25 |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Successful treatment of ifosfamide-induced hyponatremia with AVP receptor antagonist without interruption of hydration for prevention of hemorrhagic cystitis. | 2009-07 |
|
| AVP receptor antagonists in patients with CHF. | 2009-06 |
|
| Pharmacology of vasopressin antagonists. | 2009-06 |
|
| Hyponatremia: case vignettes. | 2009-05 |
|
| Medial septal area vasopressin receptor subtypes in the regulation of urine and sodium excretion in rats. | 2009-02 |
|
| New topics in vasopressin receptors and approach to novel drugs: research and development of conivaptan hydrochloride (YM087), a drug for the treatment of hyponatremia. | 2009-01 |
|
| Efficacy and safety of oral conivaptan, a vasopressin-receptor antagonist, evaluated in a randomized, controlled trial in patients with euvolemic or hypervolemic hyponatremia. | 2009-01 |
|
| Role of vasopressin and vasopressin receptor antagonists in type I cardiorenal syndrome. | 2009 |
|
| Conivaptan bolus dosing for the correction of hyponatremia in the neurointensive care unit. | 2009 |
|
| Conivaptan for hyponatremia in the neurocritical care unit. | 2009 |
|
| Vasopressin and vasopressin receptor antagonists in heart failure. | 2008-12-19 |
|
| Tolvaptan and its potential in the treatment of hyponatremia. | 2008-12 |
|
| Vasopressin antagonists for the treatment of acute decompensated heart failure: when, for whom, for how long, and on what standard therapy? | 2008-10 |
|
| Efficacy and safety of the vasopressin V1A/V2-receptor antagonist conivaptan in acute decompensated heart failure: a dose-ranging pilot study. | 2008-10 |
|
| Use of conivaptan to allow aggressive hydration to prevent tumor lysis syndrome in a pediatric patient with large-cell lymphoma and SIADH. | 2008-08 |
|
| [Etiology, diagnostics and therapy of hyponatremias]. | 2008-07-20 |
|
| Assessment of the efficacy and safety of intravenous conivaptan in patients with euvolaemic hyponatraemia: subgroup analysis of a randomized, controlled study. | 2008-07 |
|
| Vasopressin and vasopressin antagonists in heart failure and hyponatremia. | 2008-06 |
|
| Conivaptan: potential therapeutic implications in heart failure. | 2008-06 |
|
| Non-peptide arginine-vasopressin antagonists: the vaptans. | 2008-05-10 |
|
| Vasopressin-receptor antagonists in heart failure. | 2008-05-01 |
|
| [Pharmacology and clinical relevance of vasopressin antagonists]. | 2008-05 |
|
| Conivaptan: a step forward in the treatment of hyponatremia? | 2008-04 |
|
| The management of ascites and hyponatremia in cirrhosis. | 2008-02 |
|
| Intravenous conivaptan. | 2008 |
|
| Peptide and non-peptide agonists and antagonists for the vasopressin and oxytocin V1a, V1b, V2 and OT receptors: research tools and potential therapeutic agents. | 2008 |
|
| Mechanisms, risks, and new treatment options for hyponatremia. | 2008 |
|
| Observations regarding the use of the aquaretic agent conivaptan for treatment of hyponatremia. | 2008 |
|
| Hyponatremia in psychiatric patients: update on evaluation and management. | 2008 |
|
| Diagnosis and management of hyponatremia in cancer patients. | 2007-12 |
|
| Current issues for nurse practitioners: Hyponatremia. | 2007-11 |
|
| Hyponatremia and vasopressin antagonism in congestive heart failure. | 2007-11 |
|
| Water in health and disease: new aspects of disturbances in water metabolism. | 2007-10 |
|
| Gateways to clinical trials. | 2007-09 |
|
| [Vasopressin antagonists in treatment of hyponatremia]. | 2007-08 |
|
| Hyponatremia: clinical diagnosis and management. | 2007-08 |
|
| Conivaptan: new treatment for hyponatremia. | 2007-07-01 |
|
| Intravenous conivaptan: effects on the QTc interval and other electrocardiographic parameters in healthy volunteers. | 2007-06-15 |
|
| [Recent progress in vasopressin research on cardiovascular diseases]. | 2007-06 |
|
| Clinical practice. The syndrome of inappropriate antidiuresis. | 2007-05-17 |
|
| Hyponatremia: current treatment strategies and the role of vasopressin antagonists. | 2007-05 |
|
| New agents for managing hyponatremia in hospitalized patients. | 2007-02-01 |
|
| Recognition and treatment of hyponatremia in acutely ill hospitalized patients. | 2007-02 |
|
| Management of hyponatremia and clinical use of vasopressin antagonists. | 2007-02 |
|
| New drugs 07, part I. | 2007-02 |
|
| Conivaptan: a dual vasopressin receptor v1a/v2 antagonist [corrected]. | 2007 |
|
| Assessment of the efficacy and safety of intravenous conivaptan in euvolemic and hypervolemic hyponatremia. | 2007 |
|
| Therapeutic potential of vasopressin receptor antagonists. | 2007 |
|
| Cerebral correlates of hyponatremia. | 2007 |
|
| Vasopressin receptor antagonists in heart failure. | 2006-06 |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/ppa/conivaptan.html
IV: 20 mg infused over 30 minutes as a loading dose, followed by a continuous infusion of 20 mg over 24 hours (0.83 mg/hour) for 2 to 4 days; may increase to a maximum dose of 40 mg over 24 hours (1.7 mg/hour) if serum sodium not rising sufficiently; total duration of therapy not to exceed 4 days. Note: If patient requires 40 mg/24 hours, may administer two consecutive 20 mg/100 mL premixed solutions over 24 hours (ie, 20 mg over 12 hours followed by 20 mg over 12 hours).
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/20471258
Binding of conivaptan with recombinant human vasopressin V1a and V2 receptors was studied using [3H]-Arg-vasopressin as a radioligand. Conivaptan binds to V1a with Ki of 0.43 and to V2 receptor with Ki of 0.36 nM.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:08:32 GMT 2025
by
admin
on
Mon Mar 31 18:08:32 GMT 2025
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| Record UNII |
75L57R6X36
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| Record Status |
Validated (UNII)
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| Record Version |
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| Classification Tree | Code System | Code | ||
|---|---|---|---|---|
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NCI_THESAURUS |
C2180
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100000156313
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C65351
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216322
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LL-60
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75L57R6X36
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1294548
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75L57R6X36
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m3761
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168626-94-6
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DBSALT000793
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SUB130161
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