Details
Stereochemistry | ACHIRAL |
Molecular Formula | C10H9N3O |
Molecular Weight | 187.198 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=CC(=CNC1=O)C2=CC=NC=C2
InChI
InChIKey=RNLQIBCLLYYYFJ-UHFFFAOYSA-N
InChI=1S/C10H9N3O/c11-9-5-8(6-13-10(9)14)7-1-3-12-4-2-7/h1-6H,11H2,(H,13,14)
DescriptionSources: http://www.drugbank.ca/drugs/DB01427Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/pro/inamrinone.html
Sources: http://www.drugbank.ca/drugs/DB01427
Curator's Comment: Description was created based on several sources, including
https://www.drugs.com/pro/inamrinone.html
Inamrinone (Amrinone) is a positive inotropic cardiotonic with vasodilator properties, phosphodiesterase inhibitory activity, and the ability to stimulate calcium ion influx into the cardiac cell. Inamrinone is a phosphodiesterase inhibitor (PDE3), resulting in increased cAMP and cGMP which leads to an increase in the calcium influx like that caused by beta-agonists resulting in increased inotropic effect. Inamrinone is used in the treatment of congestive heart failure.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL241 Sources: http://www.drugbank.ca/drugs/DB01427 |
16.7 µM [IC50] | ||
Target ID: CHEMBL290 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10644042 |
31.2 µM [IC50] | ||
Target ID: GO:0070527 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14698653 |
61.0 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | AMRINONE LACTATE Approved UseFor the short-term management of congestive heart failure. Launch Date2000 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.2 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8513658/ |
0.75 mg/kg 3 times / day steady-state, intravenous dose: 0.75 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
INAMRINONE plasma | Homo sapiens population: UNKNOWN age: NEWBORN sex: FEMALE / MALE food status: UNKNOWN |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
245 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8513658/ |
0.75 mg/kg 3 times / day steady-state, intravenous dose: 0.75 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
INAMRINONE plasma | Homo sapiens population: UNKNOWN age: NEWBORN sex: FEMALE / MALE food status: UNKNOWN |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
5.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/8513658/ |
0.75 mg/kg 3 times / day steady-state, intravenous dose: 0.75 mg/kg route of administration: Intravenous experiment type: STEADY-STATE co-administered: |
INAMRINONE plasma | Homo sapiens population: UNKNOWN age: NEWBORN sex: FEMALE / MALE food status: UNKNOWN |
Doses
Dose | Population | Adverse events |
---|---|---|
198 ug/kg/min 1 times / day single, intravenous (max) Overdose Dose: 198 ug/kg/min, 1 times / day Route: intravenous Route: single Dose: 198 ug/kg/min, 1 times / day Sources: |
unhealthy, 0.208333333333333 n = 1 Health Status: unhealthy Condition: heart failure Age Group: 0.208333333333333 Sex: F Population Size: 1 Sources: |
Other AEs: Cardiac arrest... |
198 ug/kg/min 1 times / day single, intravenous (max) Overdose Dose: 198 ug/kg/min, 1 times / day Route: intravenous Route: single Dose: 198 ug/kg/min, 1 times / day Sources: |
unhealthy, 0.208333333333333 n = 1 Health Status: unhealthy Condition: heart failure Age Group: 0.208333333333333 Sex: F Population Size: 1 Sources: |
Other AEs: Death... Other AEs: Death (grade 5) Sources: |
100 mg 3 times / day multiple, oral Recommended Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: |
unhealthy, 49 n = 13 Health Status: unhealthy Condition: congestive heart failure Age Group: 49 Sex: M+F Population Size: 13 Sources: |
Disc. AE: Pulmonary edema, Cardiac arrest... AEs leading to discontinuation/dose reduction: Pulmonary edema Sources: Cardiac arrest Respiratory distress syndrome Chest pain Palpitations Ventricular ectopic beats |
200 mg 3 times / day multiple, oral Highest studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, 53 n = 32 Health Status: unhealthy Condition: congestive heart failure Age Group: 53 Sex: M+F Population Size: 32 Sources: |
Disc. AE: Diarrhea, Thrombocytopenia... AEs leading to discontinuation/dose reduction: Diarrhea Sources: Thrombocytopenia |
5.8 mg/kg/day 1 times / day multiple, intravenous (mean) Recommended Dose: 5.8 mg/kg/day, 1 times / day Route: intravenous Route: multiple Dose: 5.8 mg/kg/day, 1 times / day Sources: |
unhealthy, 59.4 (37-81) n = 43 Health Status: unhealthy Condition: congestive heart failure Age Group: 59.4 (37-81) Sex: M+F Population Size: 43 Sources: |
Disc. AE: Thrombocytopenia... AEs leading to discontinuation/dose reduction: Thrombocytopenia (18.6%) Sources: |
3 mg/kg 1 times / day single, intravenous (max) Recommended Dose: 3 mg/kg, 1 times / day Route: intravenous Route: single Dose: 3 mg/kg, 1 times / day Sources: |
unhealthy, <1 n = 6 Health Status: unhealthy Condition: pulmonary hypertension Age Group: <1 Sex: M+F Population Size: 6 Sources: |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Cardiac arrest | 198 ug/kg/min 1 times / day single, intravenous (max) Overdose Dose: 198 ug/kg/min, 1 times / day Route: intravenous Route: single Dose: 198 ug/kg/min, 1 times / day Sources: |
unhealthy, 0.208333333333333 n = 1 Health Status: unhealthy Condition: heart failure Age Group: 0.208333333333333 Sex: F Population Size: 1 Sources: |
|
Death | grade 5 | 198 ug/kg/min 1 times / day single, intravenous (max) Overdose Dose: 198 ug/kg/min, 1 times / day Route: intravenous Route: single Dose: 198 ug/kg/min, 1 times / day Sources: |
unhealthy, 0.208333333333333 n = 1 Health Status: unhealthy Condition: heart failure Age Group: 0.208333333333333 Sex: F Population Size: 1 Sources: |
Cardiac arrest | Disc. AE | 100 mg 3 times / day multiple, oral Recommended Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: |
unhealthy, 49 n = 13 Health Status: unhealthy Condition: congestive heart failure Age Group: 49 Sex: M+F Population Size: 13 Sources: |
Chest pain | Disc. AE | 100 mg 3 times / day multiple, oral Recommended Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: |
unhealthy, 49 n = 13 Health Status: unhealthy Condition: congestive heart failure Age Group: 49 Sex: M+F Population Size: 13 Sources: |
Palpitations | Disc. AE | 100 mg 3 times / day multiple, oral Recommended Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: |
unhealthy, 49 n = 13 Health Status: unhealthy Condition: congestive heart failure Age Group: 49 Sex: M+F Population Size: 13 Sources: |
Pulmonary edema | Disc. AE | 100 mg 3 times / day multiple, oral Recommended Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: |
unhealthy, 49 n = 13 Health Status: unhealthy Condition: congestive heart failure Age Group: 49 Sex: M+F Population Size: 13 Sources: |
Respiratory distress syndrome | Disc. AE | 100 mg 3 times / day multiple, oral Recommended Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: |
unhealthy, 49 n = 13 Health Status: unhealthy Condition: congestive heart failure Age Group: 49 Sex: M+F Population Size: 13 Sources: |
Ventricular ectopic beats | Disc. AE | 100 mg 3 times / day multiple, oral Recommended Dose: 100 mg, 3 times / day Route: oral Route: multiple Dose: 100 mg, 3 times / day Sources: |
unhealthy, 49 n = 13 Health Status: unhealthy Condition: congestive heart failure Age Group: 49 Sex: M+F Population Size: 13 Sources: |
Diarrhea | Disc. AE | 200 mg 3 times / day multiple, oral Highest studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, 53 n = 32 Health Status: unhealthy Condition: congestive heart failure Age Group: 53 Sex: M+F Population Size: 32 Sources: |
Thrombocytopenia | Disc. AE | 200 mg 3 times / day multiple, oral Highest studied dose Dose: 200 mg, 3 times / day Route: oral Route: multiple Dose: 200 mg, 3 times / day Sources: |
unhealthy, 53 n = 32 Health Status: unhealthy Condition: congestive heart failure Age Group: 53 Sex: M+F Population Size: 32 Sources: |
Thrombocytopenia | 18.6% Disc. AE |
5.8 mg/kg/day 1 times / day multiple, intravenous (mean) Recommended Dose: 5.8 mg/kg/day, 1 times / day Route: intravenous Route: multiple Dose: 5.8 mg/kg/day, 1 times / day Sources: |
unhealthy, 59.4 (37-81) n = 43 Health Status: unhealthy Condition: congestive heart failure Age Group: 59.4 (37-81) Sex: M+F Population Size: 43 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
Poisoning with calcium channel blockers--a case report and review of the literature. | 2001 Dec |
|
Clinical use of amrinone (a selective phosphodiesterase III inhibitor) in reconstructive surgery. | 2001 Dec |
|
Effects of the specific phosphodiesterase inhibitors on alloxan-induced diabetic rabbit cavernous tissue in vitro. | 2001 Feb |
|
Lack of role for nitric oxide in cholinergic modulation of myocardial contractility in vivo. | 2001 Jul |
|
The efficacy of preemptive Milrinone or Amrinone therapy in patients undergoing coronary artery bypass grafting. | 2002 Jan |
|
[Effects of amrinone in patients undergoing off-pump coronary artery bypass grafting]. | 2002 May |
|
Differential effects of amrinone and milrinone upon myocardial inflammatory signaling. | 2002 Sep 24 |
|
Possible contribution of acetylamrinone and its enhancing effects on platelet aggregation under shear stress conditions in the onset of thrombocytopenia in patients treated with amrinone. | 2003 |
|
Effects of preemptive therapy with milrinone or amrinone on perioperative platelet function and haemostasis in patients undergoing coronary bypass grafting. | 2003 Aug |
|
[Levosimendan: a new option in the pharmacologic management of cardiac insufficiency]. | 2003 Jan-Feb |
|
Inhibition and facilitation by pimobendan, a calcium sensitizer, of catecholamine secretion from bovine adrenal chromaffin cells. | 2003 Mar |
|
Development of an in vitro model for vascular injury with human endothelial cells. | 2004 |
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Cardiac and vascular effects of diltiazem, dobutamine and amrinone, drugs used after myocardial revascularization. | 2004 Jun |
|
The impact of slow rewarming on inotropy, tissue metabolism, and "after drop" of body temperature in pediatric patients. | 2005 Jun |
|
Bench-to-bedside review: Inotropic drug therapy after adult cardiac surgery -- a systematic literature review. | 2005 Jun |
|
A sensitive and specific high performance liquid chromatographic assay for milrinone in rat and human plasma using a commercially available internal standard and low sample volume. | 2005 Jun 24 |
|
Inotropic responses to phosphodiesterase inhibitors in cardiac hypertrophy in rats. | 2005 May 9 |
|
Effects of inotropic drugs on mechanical function and oxygen balance in postischemic canine myocardium: comparison of dobutamine, epinephrine, amrinone, and calcium chloride. | 2005 Oct |
|
Bench-to-bedside review: thrombocytopenia-associated multiple organ failure--a newly appreciated syndrome in the critically ill. | 2006 |
|
In vivo dilatation of the fetal and postnatal ductus arteriosus by inhibition of phosphodiesterase 3 in rats. | 2006 |
|
A comparison of three phosphodiesterase type III inhibitors on mechanical and metabolic function in guinea pig isolated hearts. | 2006 Jun |
|
The base exchange reaction of NAD+ glycohydrolase: identification of novel heterocyclic alternative substrates. | 2008 Nov 15 |
|
Effect of nitric oxide/cyclic guanosine mono-phosphate pathway on gallbladder relaxant response in bile duct-ligated guinea pigs. | 2009 |
|
Effects of propofol on responses of rat isolated renal arteriole to vasoactive agents. | 2009 Aug-Sep |
|
Gene expression analysis reveals new possible mechanisms of vancomycin-induced nephrotoxicity and identifies gene markers candidates. | 2009 Jan |
Patents
Sample Use Guides
Congestive heart failure
IV
Initially, 0.75 mg/kg as a slow (over 2–3 minutes) direct injection; if warranted, may administer a supplemental direct IV dose of 0.75 mg/kg 30 minutes after the initial dose.1 60 Direct IV injection is followed by an IV infusion of 5–10 mcg/kg per minute. Duration of therapy determined by clinical response and tolerance to adverse effects.
Route of Administration:
Intravenous
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/14698653
Inamrinone inhibited human platelet aggregation at 10,800 s(-1) in a dose-dependent manner with the IC(50) value of 61 +/- 8 uM (mean +/- S.D.), Inamrinone significantly inhibited platelet aggregation at 1200 s(-1) only at highest concentration tested (100 uM)
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NCI_THESAURUS |
C29707
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C744
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D000676
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CHEMBL12856
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AMRINONE
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DB01427
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ACTIVE MOIETY