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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

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
Possible involvement of cyclic adenosine monophosphate-independent mechanism in the positive chronotropic effect of norepinephrine in the isolated guinea pig right atrium.
2001 Aug
In contrast to forskolin and 3-isobutyl-1-methylxanthine, amrinone stimulates the cardiac voltage-sensitive release mechanism without increasing calcium-induced calcium release.
2001 Sep
Comparison of enoximone, amrinone, or levosimendan enriched St. Thomas' hospital cardioplegic solutions used for myocardial preservation in isolated guinea pig hearts.
2002
Intraoperative insulin therapy does not reduce the need for inotropic or antiarrhythmic therapy after cardiopulmonary bypass.
2002 Aug
Immunopharmacological potential of selective phosphodiesterase inhibition. II. Evidence for the involvement of an inhibitory-kappaB/nuclear factor-kappaB-sensitive pathway in alveolar epithelial cells.
2002 Feb
The efficacy of preemptive Milrinone or Amrinone therapy in patients undergoing coronary artery bypass grafting.
2002 Jan
[Pharmacology of inotropic agents].
2002 Jan-Mar
PDE4 inhibitors attenuate fibroblast chemotaxis and contraction of native collagen gels.
2002 Jun
[Effect of dexamethasone, aminoguanidin, amrinone on oxygen utilization in endotoxin shock rabbits].
2003 Apr
Effects of epinephrine and phosphodiesterase III inhibitors on bupivacaine-induced myocardial depression in guinea-pig papillary muscle.
2003 Jan
Interleukin-6 family of cytokines mediates isoproterenol-induced delayed STAT3 activation in mouse heart.
2003 Jun 6
Development of an in vitro model for vascular injury with human endothelial cells.
2004
Pharmacokinetics and pharmacodynamics of intravenous inotropic agents.
2004
Diminished inotropic response to amrinone in ventricular myocytes from myopathic hamsters is linked to depression of high-gain Ca2+-induced Ca2+ release.
2004 Aug
Treatment of mechanically-induced vasospasm of the carotid artery in a primate using intra-arterial verapamil: a technical case report.
2004 Jul 21
Cardiac and vascular effects of diltiazem, dobutamine and amrinone, drugs used after myocardial revascularization.
2004 Jun
Short-term fasting and lipolytic activity in rat adipocytes.
2004 Oct
Effects of dopamine, dobutamine, amrinone and milrinone on regional blood flow in isoflurane anesthetized dogs.
2004 Sep
Successful allogeneic bone marrow transplantation for acute myelogenous leukemia after drug-induced cardiomyopathy.
2004 Sep
Meta-analysis of hemodynamic optimization: relationship to methodological quality.
2005
Effects of a phosphodiesterase 3 inhibitor, olprinone, on rhythmical change in tension of human gastroepiploic artery.
2005 Dec 28
Effect of amrinone on mucosal permeability in experimental intestinal ischaemia/reperfusion injury.
2005 Jul
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
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
Contractile responses to selective phosphodiesterase inhibitors following chronic beta-adrenoreceptor activation.
2006 May
Acute heart failure: inotropic agents and their clinical uses.
2006 Nov
[Current approaches to intraoperative diagnosis and treatment of low cardiac output during cardiosurgical operations].
2006 Sep-Oct
[Protection of amrinone against lung injury induced by ischemia/reperfusion in rats].
2007 Jun
Peripartum cardiomyopathy: review of the literature.
2007 Oct 31
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
Surviving Sepsis Campaign: international guidelines for management of severe sepsis and septic shock: 2008.
2008 Jan
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
Design, synthesis and pharmacological evaluation of 6-hydroxy-4-methylquinolin-2(1H)-one derivatives as inotropic agents.
2009 Aug
Drug effect unveils inter-head cooperativity and strain-dependent ADP release in fast skeletal actomyosin.
2009 Aug 21
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
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)
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