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Milrinone

Milrinone structure

CAS No:
78415-72-2
Formula:
C12H9N3O
Chemical Name:
Milrinone
Synonyms:
[3,4′-Bipyridine]-5-carbonitrile,1,6-dihydro-2-methyl-6-oxo-;1,6-Dihydro-2-methyl-6-oxo[3,4′-bipyridine]-5-carbonitrile;Win 47203;Milrinone;Corotrope;Primacor IV;Corotrop;Milrila;Primacor;2-Hydroxy-6-methyl-5-(pyridin-4-yl)pyridine-3-carbonitrile
Categories:
Active Pharmaceutical Ingredients > Circulatory System Drugs

Description

Milrinone is a PDE3 inhibitor, and also an inotrope and vasodilator.

Solid

Milrinone is a member of the class of bipyridines that is 2-pyridone which is substituted at positions 3, 5, and 6 by cyano, pyrid-4-yl, and methyl groups, respectively. It is used (particularly intravenously, as the lactate) for the short-term management of severe heart failure. It has a role as an EC 3.1.4.17 (3',5'-cyclic-nucleotide phosphodiesterase) inhibitor, a platelet aggregation inhibitor, a vasodilator agent and a cardiotonic drug. It is a pyridone, a nitrile and a member of bipyridines.|A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the ionotropic potency of amrinone.|Milrinone is a Phosphodiesterase 3 Inhibitor. The mechanism of action of milrinone is as a Phosphodiesterase 3 Inhibitor.|A positive inotropic cardiotonic agent with vasodilator properties. It inhibits cAMP phosphodiesterase type 3 activity in myocardium and vascular smooth muscle. Milrinone is a derivative of amrinone and has 20-30 times the inotropic potency of amrinone.

Milrinone Basic Attributes

Molecular Weight：

211.22

Exact Mass：

211.22

EC Number：

278-903-6

UNII：

JU9YAX04C7

NSC Number：

760072

DSSTox ID：

DTXSID5023324

ATC Code：

C01CE02|C - Cardiovascular system

HScode：

2933399090

Characteristics

PSA：

65.8

XLogP3：

Appearance：

off-white powder

Density：

1.3±0.1 g/cm3

Melting Point：

>300 °C

Boiling Point：

448.7ºC at 760 mmHg

Flash Point：

225.2±28.7 °C

Refractive Index：

1.622

Water Solubility：

soluble in DMSO( >10 mg/mL). Insoluble in water.

Storage Conditions：

2-8°C

Collision Cross Section：

150.4 Å² [M+H]+ [CCS Type: TW, Method: Major Mix IMS/Tof Calibration Kit (Waters)]

Safety Information

Packing level：

III

Hazard category：

6.1(b)

Transport codes：

UN 2811 6.1/PG 3

wgk germany：

hazard class code：

23/24/25-26/27/28

safety instructions：

36/37/39-45-22

RTECS Number：

DW1762000

Marks：

T,T+

Stability/Shelf Life：

Stable. Incompatible with strong oxidizing agents.

Precautionary statement(s)：

Missing Phrase - N15.00950417-P261-P280-P302 + P352 + P312-P304 + P340 + P312-P403 + P233

Hazard Statements：

H301 + H311 + H331

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P261, P264, P270, P271, P280, P301+P310, P302+P352, P304+P340, P311, P312, P321, P322, P330, P361, P363, P403+P233, P405, and P501|Aggregated GHS information provided by 106 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Toxicity

Toxicity Summary：

LD50 = 0.3 mg/L in rats

Protein Binding：

70 to 80%

Drug Information

Drug Indication：

Indicated for the treatment of congestive heart failure.|FDA Label

Pharmacology：

Milrinone, a synthetic dimethylxanthine derivative structurally related to theophylline and caffeine, is used in the treatment of peripheral vascular diseases and in the management of cerebrovascular insufficiency, sickle cell disease, and diabetic neuropathy.

MeSH：

Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. (See all compounds classified as Platelet Aggregation Inhibitors.)|Agents that have a strengthening effect on the heart or that can increase cardiac output. They may be CARDIAC GLYCOSIDES; SYMPATHOMIMETICS; or other drugs. They are used after MYOCARDIAL INFARCT; CARDIAC SURGICAL PROCEDURES; in SHOCK; or in congestive heart failure (HEART FAILURE). (See all compounds classified as Cardiotonic Agents.)|Compounds that specifically inhibit PHOSPHODIESTERASE 3. (See all compounds classified as Phosphodiesterase 3 Inhibitors.)|Drugs used to cause dilation of the blood vessels. (See all compounds classified as Vasodilator Agents.)

Absorption：

Milrinone is rapidly and almost completely absorbed after oral administration. Bioavailability is 92% (in healthy volunteers).|The primary route of excretion of milrinone in man is via the urine.|0.38 liters/kg [intravenous injections of 12.5 mcg/kg to 125 mcg/kg to congestive heart failure patients]|0.13 L/kg/hr [congestive heart failure patients, following IV injections of 12.5 mcg/kg to 125 mcg/kg]

Metabolism/Metabolites：

There are five metabolites but the O-glucuronide represents the major pathway of biotransformation.

Biological Half-Life：

2.3 hours

Mechanism of Action：

Milrinone inhibits erythrocyte phosphodiesterase, resulting in an increase in erythrocyte cAMP activity. Subsequently, the erythrocyte membrane becomes more resistant to deformity. Along with erythrocyte activity, Milrinone also decreases blood viscosity by reducing plasma fibrinogen concentrations and increasing fibrinolytic activity.

MeSH Entry Terms：

Corotrop

Milrinone Use and Manufacturing

Uses

Selective phosphodiesterase inhibitor with vasodilating and positive inotropic activity. Cardiotonic

Use Classification：

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients|Pharmaceuticals

Computed Properties

Molecular Weight:211.22
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:1
Exact Mass:211.074561919
Monoisotopic Mass:211.074561919
Topological Polar Surface Area:65.8
Heavy Atom Count:16
Complexity:419
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

Material

Cyclohexane

Pyridine

Drug Function and Efficacy

Positive inotropic and vasodilatory effects

This ingredient has been used in drugs with the following functions (note: it does not mean that the ingredient itself has the following health functions)

Related Drugs

Milrinone injection
Specifications	5ml:5mg
Manufacturer	Tongliao Huabang Pharmaceutical Co., Ltd.

Milrinone and Glucose Injection
Specifications	100ml: Milrinone 20mg and glucose 5.43g
Manufacturer	Lunan BETTER Pharmaceutical Co., Ltd.

Milrinone Lactate Injection
Ingredients	The chemical name of this product is: 2-methyl-6-oxy-1,6-dihydro-[3,4-bipyridine]-5-carbonitrile. Molecular formula: C10H9N3O Molecular weight: 211.22
Indication	1. When used together with disopyramide, it may lead to hypotension. 2. When used together with commonly used cardiotonic, diuretic and vasodilator drugs, no adverse interactions have been observed. 3. When used together with nitrates, there is an additive effect. 4. This product can enhance the positive inotropic effect of digitalis, so it is not necessary to stop using digitalis during its use.
Specifications	5 ml: 5 mg (as milrinone)
Manufacturer	Lunan BETTER Pharmaceutical Co., Ltd.

See More Related Drugs

Registered Holders

HIKMA PHARMACEUTICALS LLC

United States
Active
EMCURE PHARMACEUTICALS LTD

United States
Active
W R GRACE AND CO -CONN

United States
Active

See More Registered Holders

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