Details
Stereochemistry | ACHIRAL |
Molecular Formula | C32H26N4O2 |
Molecular Weight | 498.5756 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cc1nc2CCN(c3ccccc3-c2[nH]1)C(=O)c4ccc(cc4)NC(=O)c5ccccc5-c6ccccc6
InChI
InChIKey=IKENVDNFQMCRTR-UHFFFAOYSA-N
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)
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 Date1.13581438E12 |
|||
Palliative | Unknown Approved UseUnknown |
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Palliative | Unknown Approved UseUnknown |
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Palliative | Unknown Approved UseUnknown |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
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 |
|
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 |
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 |
---|---|---|---|---|
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 |
|
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 |
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) n = 27 Health Status: unhealthy Condition: euvolemic hyponatremia | hypervolemic hyponatremia Age Group: 68.7 years (range: 35–90 years) Sex: M+F Population Size: 27 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 Condition: Congestive heart failure 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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
Disc. AE: Hypopituitarism, Infusion site reaction... AEs leading to discontinuation/dose reduction: Hypopituitarism (0.2%) Sources: Page: p. 64Infusion 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 n = 6 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 6 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
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 n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
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 Condition: Congestive heart failure 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 Condition: Congestive heart failure 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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
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: Page: p. 64 |
unhealthy, adult n = 445 Health Status: unhealthy Age Group: adult Population Size: 445 Sources: Page: p. 64 |
Dizziness | below serious, 1 patient | 12.5 mg single, intravenous Dose: 12.5 mg Route: intravenous Route: single Dose: 12.5 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 6 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 20 Health Status: unhealthy Condition: Euvolemic or Hypervolemic Hyponatremia Population Size: 20 Sources: |
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 n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
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 n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
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 n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
Nausea | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
Polydipsia | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
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 n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
Vomiting | below serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
Phlebitis | below serious, 2 patients | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
Atrial tachycardia | serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
Encephalopathy hepatic | serious, 1 patient | 22.5 mg single, intravenous Dose: 22.5 mg Route: intravenous Route: single Dose: 22.5 mg Sources: |
unhealthy n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
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 n = 9 Health Status: unhealthy Condition: Liver Cirrhosis Population Size: 9 Sources: |
Atrial flutter | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Constipation | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Headache | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Heart rate increased | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Infusion site pain | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Muscle spasms | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Pain in extremity | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Pyrexia | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Ventricular tachycardia | below serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Infusion site erythema | below serious, 3 patients | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
Cardiac arrest | serious, 1 patient | 60 mg single, intravenous Dose: 60 mg Route: intravenous Route: single Dose: 60 mg Sources: |
unhealthy n = 6 Health Status: unhealthy Condition: Acute Decompensated Heart Failure Population Size: 6 Sources: |
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 |
---|---|---|
Molecular modeling of interactions of the non-peptide antagonist YM087 with the human vasopressin V1a, V2 receptors and with oxytocin receptors. | 2001 Dec |
|
Neurohormonal antagonism in heart failure; beneficial effects of vasopressin V(1a) and V(2) receptor blockade and ACE inhibition. | 2002 Apr |
|
Effect of the vasopressin receptor antagonist conivaptan in rats with heart failure following myocardial infarction. | 2002 Aug 23 |
|
Body compartment volumes and composition after giving a vasopressin antagonist: changes are revealed by a tonicity balance. | 2002 Feb |
|
Conivaptan (Yamanouchi). | 2002 Jan |
|
[Treatment of heart failure: an update]. | 2002 Jul |
|
Effect of conivaptan, a combined vasopressin V(1a) and V(2) receptor antagonist, on vasopressin-induced cardiac and haemodynamic changes in anaesthetised dogs. | 2002 Nov |
|
Vasopressin: a new target for the treatment of heart failure. | 2003 Jul |
|
Therapeutic role of vasopressin receptor antagonism in patients with liver cirrhosis. | 2003 Jul |
|
Effect of the V1a/V2-AVP receptor antagonist, Conivaptan, on renal water metabolism and systemic hemodynamics in rats with cirrhosis and ascites. | 2003 Jun |
|
2,5-disubstituted 3,4-dihydro-2H-benzo[b][1,4]thiazepines as potent and selective V2 arginine vasopressin receptor antagonists. | 2003 Nov 17 |
|
Gateways to clinical trials. | 2004 Jul-Aug |
|
Gateways to clinical trials. | 2005 Jan-Feb |
|
Conivaptan Yamanouchi. | 2005 Mar |
|
Vasopressin antagonism: a future treatment option in heart failure. | 2005 Mar |
|
Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. | 2005 Mar |
|
Vasopressin receptor antagonists: pharmacological tools and potential therapeutic agents. | 2006 Apr |
|
Vasopressin antagonists. | 2006 Aug |
|
Pharmacologic chaperones as a potential treatment for X-linked nephrogenic diabetes insipidus. | 2006 Jan |
|
Hyponatremia and heart failure--treatment considerations. | 2006 Jan-Feb |
|
Vasopressin antagonists as aquaretic agents for the treatment of hyponatremia. | 2006 Jul |
|
Conivaptan: a selective vasopressin antagonist. | 2006 Jun |
|
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. | 2006 Jun |
|
Conivaptan (Vaprisol) for hyponatremia. | 2006 Jun 19 |
|
Hyponatremia in cirrhosis: clinical features and management. | 2006 Oct |
|
New drugs: rasagiline mesylate, conivaptan hydrochloride, and sunitinib malate. | 2006 Sep-Oct |
|
Therapeutic potential of vasopressin receptor antagonists. | 2007 |
|
Cerebral correlates of hyponatremia. | 2007 |
|
[Vasopressin antagonists in treatment of hyponatremia]. | 2007 Aug |
|
New drugs 07, part I. | 2007 Feb |
|
New agents for managing hyponatremia in hospitalized patients. | 2007 Feb 1 |
|
[Arginine vasopressin antagonism--new treatment option in chronic heart failure]. | 2007 Jan 18 |
|
Hyponatremia: current treatment strategies and the role of vasopressin antagonists. | 2007 May |
|
Current issues for nurse practitioners: Hyponatremia. | 2007 Nov |
|
Gateways to clinical trials. | 2007 Sep |
|
Mechanisms, risks, and new treatment options for hyponatremia. | 2008 |
|
Observations regarding the use of the aquaretic agent conivaptan for treatment of hyponatremia. | 2008 |
|
Use of conivaptan to allow aggressive hydration to prevent tumor lysis syndrome in a pediatric patient with large-cell lymphoma and SIADH. | 2008 Aug |
|
Tolvaptan and its potential in the treatment of hyponatremia. | 2008 Dec |
|
The management of ascites and hyponatremia in cirrhosis. | 2008 Feb |
|
Vasopressin-receptor antagonists in heart failure. | 2008 May 1 |
|
Non-peptide arginine-vasopressin antagonists: the vaptans. | 2008 May 10 |
|
Vasopressin antagonists for the treatment of acute decompensated heart failure: when, for whom, for how long, and on what standard therapy? | 2008 Oct |
|
Role of vasopressin and vasopressin receptor antagonists in type I cardiorenal syndrome. | 2009 |
|
Conivaptan for hyponatremia in the neurocritical care unit. | 2009 |
|
Medial septal area vasopressin receptor subtypes in the regulation of urine and sodium excretion in rats. | 2009 Feb |
|
Efficacy and safety of oral conivaptan, a vasopressin-receptor antagonist, evaluated in a randomized, controlled trial in patients with euvolemic or hypervolemic hyponatremia. | 2009 Jan |
|
Vasopressin and vasopressin receptor antagonists in heart failure. | 2009 Jan-Feb |
|
AVP receptor antagonists in patients with CHF. | 2009 Jun |
|
Hyponatremia: case vignettes. | 2009 May |
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.
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Classification Tree | Code System | Code | ||
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NDF-RT |
N0000009945
Created by
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WHO-ATC |
C03XA02
Created by
admin on Sat Jun 26 11:07:18 UTC 2021 , Edited by admin on Sat Jun 26 11:07:18 UTC 2021
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|
WHO-VATC |
QC03XA02
Created by
admin on Sat Jun 26 11:07:18 UTC 2021 , Edited by admin on Sat Jun 26 11:07:18 UTC 2021
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NDF-RT |
N0000178376
Created by
admin on Sat Jun 26 11:07:18 UTC 2021 , Edited by admin on Sat Jun 26 11:07:18 UTC 2021
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||
|
NCI_THESAURUS |
C2180
Created by
admin on Sat Jun 26 11:07:18 UTC 2021 , Edited by admin on Sat Jun 26 11:07:18 UTC 2021
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Code System | Code | Type | Description | ||
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210101-16-9
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PRIMARY | |||
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SUB32706
Created by
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PRIMARY | |||
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732
Created by
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PRIMARY | |||
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210101-16-9
Created by
admin on Sat Jun 26 11:07:18 UTC 2021 , Edited by admin on Sat Jun 26 11:07:18 UTC 2021
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PRIMARY | |||
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C106389
Created by
admin on Sat Jun 26 11:07:18 UTC 2021 , Edited by admin on Sat Jun 26 11:07:18 UTC 2021
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PRIMARY | |||
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CONIVAPTAN
Created by
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PRIMARY | |||
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302285
Created by
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PRIMARY | RxNorm | ||
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0NJ98Y462X
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PRIMARY | |||
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2203
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PRIMARY | |||
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7947
Created by
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PRIMARY | |||
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M3761
Created by
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PRIMARY | Merck Index | ||
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CHEMBL1755
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PRIMARY | |||
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C74428
Created by
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PRIMARY | |||
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151171
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PRIMARY | |||
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DB00872
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PRIMARY |
ACTIVE MOIETY
SALT/SOLVATE (PARENT)