U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry UNKNOWN
Molecular Formula C10H9N3O.C3H6O3
Molecular Weight 277.2759
Optical Activity ( + / - )
Defined Stereocenters 0 / 1
E/Z Centers 0
Charge 0
Stereo Comments LACTATE

SHOW SMILES / InChI
Structure of INAMRINONE LACTATE

SMILES

CC(O)C(O)=O.NC1=CC(=CNC1=O)C2=CC=NC=C2

InChI

InChIKey=DOSIONJFGDSKCQ-UHFFFAOYSA-N
InChI=1S/C10H9N3O.C3H6O3/c11-9-5-8(6-13-10(9)14)7-1-3-12-4-2-7;1-2(4)3(5)6/h1-6H,11H2,(H,13,14);2,4H,1H3,(H,5,6)

HIDE SMILES / InChI

Molecular Formula C3H6O3
Molecular Weight 90.0779
Charge 0
Count
Stereochemistry RACEMIC
Additional Stereochemistry No
Defined Stereocenters 0 / 1
E/Z Centers 0
Optical Activity ( + / - )

Molecular Formula C10H9N3O
Molecular Weight 187.198
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
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

Targets

Primary TargetPharmacologyConditionPotency
16.7 µM [IC50]
31.2 µM [IC50]
61.0 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
AMRINONE LACTATE

Approved Use

For the short-term management of congestive heart failure.

Launch Date

2000
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
5.2 μg/mL
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

AUC

ValueDoseCo-administeredAnalytePopulation
245 μg × h/mL
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

T1/2

ValueDoseCo-administeredAnalytePopulation
5.4 h
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

Doses

DosePopulationAdverse 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...
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
Cardiac arrest
Respiratory distress syndrome
Chest pain
Palpitations
Ventricular ectopic beats
Sources:
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
Thrombocytopenia
Sources:
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

AEs

AESignificanceDosePopulation
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:
Sourcing

Sourcing

Vendor/AggregatorIDURL
PubMed

PubMed

TitleDatePubMed
Amrinone for refractory cardiogenic shock following chloroquine poisoning.
1991
[Randomized controlled trial for the effect of amrinone and aprotinin on proinflammatory cytokine release in patients with prosthetic valve replacement during perioperative period].
2001 Jun
Comparison of enoximone, amrinone, or levosimendan enriched St. Thomas' hospital cardioplegic solutions used for myocardial preservation in isolated guinea pig hearts.
2002
[Randomized controlled trial for the effect of amrinone and aprotinin on expression leukocyte adhesion molecule in patients with prosthetic valve replacement during perioperative period].
2002 Apr
Effects of amrinone on bilateral renal ischemia/reperfusion injury.
2002 Jul
Cyclooxygenase-2 and adenylate cyclase/protein kinase A signaling pathway enhances angiogenesis through induction of vascular endothelial growth factor in rat sponge implants.
2002 Mar
Effects of cAMP modulators on long-chain fatty-acid uptake and utilization by electrically stimulated rat cardiac myocytes.
2002 Nov 1
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
[Effect of dexamethasone, aminoguanidin, amrinone on oxygen utilization in endotoxin shock rabbits].
2003 Apr
The effect of chronic renal failure on phosphodiesterase inhibitor-induced relaxation responses in rabbit cavernosal strips.
2003 Feb 21
Effects of epinephrine and phosphodiesterase III inhibitors on bupivacaine-induced myocardial depression in guinea-pig papillary muscle.
2003 Jan
Congenital junctional ectopic tachycardia: presentation and outcome.
2003 Jul 1
Development of an in vitro model for vascular injury with human endothelial cells.
2004
Pharmacokinetics and pharmacodynamics of intravenous inotropic agents.
2004
Cardiac and vascular effects of diltiazem, dobutamine and amrinone, drugs used after myocardial revascularization.
2004 Jun
Meta-analysis of hemodynamic optimization: relationship to methodological quality.
2005
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
Protective effects of different antioxidants and amrinone on vancomycin-induced nephrotoxicity.
2005 Nov
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
Bench-to-bedside review: hyperinsulinaemia/euglycaemia therapy in the management of overdose of calcium-channel blockers.
2006
In vivo dilatation of the fetal and postnatal ductus arteriosus by inhibition of phosphodiesterase 3 in rats.
2006
Alkaline Phosphatases : Structure, substrate specificity and functional relatedness to other members of a large superfamily of enzymes.
2006 Jun
Effect of combining phosphodiesterase III inhibitors with St Thomas Hospital's solution used as transplantation preservative solution in isolated rat hearts.
2006 Jun
A comparison of three phosphodiesterase type III inhibitors on mechanical and metabolic function in guinea pig isolated hearts.
2006 Jun
Contractile responses to selective phosphodiesterase inhibitors following chronic beta-adrenoreceptor activation.
2006 May
Acute heart failure: inotropic agents and their clinical uses.
2006 Nov
Coronary bypass grafting using crossclamp fibrillation does not result in reliable reperfusion of the myocardium when the crossclamp is intermittently released: a prospective cohort study.
2006 Nov 21
Treatment of poisoning caused by beta-adrenergic and calcium-channel blockers.
2006 Oct 1
Proper use of phosphodiesterase inhibitors according to the situations.
2006 Sep
[Current approaches to intraoperative diagnosis and treatment of low cardiac output during cardiosurgical operations].
2006 Sep-Oct
Investigation of binding proteins for anti-platelet agent K-134 by Drug-Western method.
2007 Feb 23
[Protection of amrinone against lung injury induced by ischemia/reperfusion in rats].
2007 Jun
Inotropic and chronotropic effects of 6-hydroxy-4-methylquinolin-2(1H)-one derivatives in isolated rat atria.
2008 Apr
Tadalafil in the treatment of erectile dysfunction.
2008 Dec
Comparison of the initial hospitalization costs between the patients treated with dobutamine and the patients treated with amrinone for acute decompensated heart failure in a Japanese institute.
2008 Mar
Labetalol infusion for refractory hypertension causing severe hypotension and bradycardia: an issue of patient safety.
2008 May 27
The base exchange reaction of NAD+ glycohydrolase: identification of novel heterocyclic alternative substrates.
2008 Nov 15
Vesnarinone represses the fibrotic changes in murine lung injury induced by bleomycin.
2009
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
Agents with inotropic properties for the management of acute heart failure syndromes. Traditional agents and beyond.
2009 Dec
Gene expression analysis reveals new possible mechanisms of vancomycin-induced nephrotoxicity and identifies gene markers candidates.
2009 Jan
Effects of amrinone in an experimental model of hepatic ischemia-reperfusion injury.
2009 Jan
Evaluation of preoperative intra-aortic balloon pump in coronary patients with severe left ventricular dysfunction undergoing OPCAB surgery: early and mid-term outcomes.
2009 Jul 27
The role of phosphodiesterase 3 in endotoxin-induced acute kidney injury.
2009 Jun 1
Pharmacological interventions for ischaemia reperfusion injury in liver resection surgery performed under vascular control.
2009 Oct 7
Pharmacological interventions versus no pharmacological intervention for ischaemia reperfusion injury in liver resection surgery performed under vascular control.
2009 Oct 7
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
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)
Substance Class Chemical
Created
by admin
on Fri Dec 15 16:21:23 GMT 2023
Edited
by admin
on Fri Dec 15 16:21:23 GMT 2023
Record UNII
I229274Y5B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
INAMRINONE LACTATE
ORANGE BOOK   VANDF  
Common Name English
Amrinone lactate [WHO-DD]
Common Name English
INOCOR
Brand Name English
INAMRINONE LACTATE [ORANGE BOOK]
Common Name English
PROPANOIC ACID, 3-HYDROXY-, COMPD. WITH 5-AMINO(3,4'-BIPYRIDIN)-6(1H)-ONE
Common Name English
INAMRINONE LACTATE [VANDF]
Common Name English
5-AMINO(3,4'-BIPYRIDIN)-6(1H)-ONE LACTATE
Systematic Name English
AMRINONE LACTATE [MART.]
Common Name English
AMRINONE LACTATE
MART.   VANDF   WHO-DD  
Common Name English
AMRINONE LACTATE [VANDF]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C744
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
Code System Code Type Description
WIKIPEDIA
Inamrinone lactate
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
SMS_ID
100000085162
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
DRUG BANK
DBSALT001311
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
RXCUI
91236
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY RxNorm
CAS
75898-90-7
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
EVMPD
SUB00512MIG
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
FDA UNII
I229274Y5B
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
ChEMBL
CHEMBL12856
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
NCI_THESAURUS
C77833
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
PUBCHEM
3035194
Created by admin on Fri Dec 15 16:21:23 GMT 2023 , Edited by admin on Fri Dec 15 16:21:23 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY