|Accession Number||DB00235 (APRD00010)|
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. [PubChem]
|External IDs||WIN 47,203-2|
|Approved Prescription Products|
|Approved Generic Prescription Products|
|Approved Over the Counter Products||Not Available|
|Unapproved/Other Products||Not Available|
|Brand mixtures||Not Available|
|Weight||Average: 211.2194 |
Indicated for the treatment of congestive heart failure.
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.
|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.
Milrinone is rapidly and almost completely absorbed after oral administration. Bioavailability is 92% (in healthy volunteers).
|Volume of distribution|
70 to 80%
There are five metabolites but the O-glucuronide represents the major pathway of biotransformation.
|Route of elimination|
The primary route of excretion of milrinone in man is via the urine.
LD50 = 0.3 mg/L in rats
|Pharmacogenomic Effects/ADRs||Not Available|
|Food Interactions||Not Available|
|Synthesis Reference||Not Available|
|General References||Not Available|
|ATC Codes||C01CE02 — Milrinone|
|PDB Entries||Not Available|
|FDA label||Download (491 KB)|
|MSDS||Download (34.8 KB)|
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
|Predicted ADMET features|
|Mass Spec (NIST)||Not Available|
|Description||This compound belongs to the class of chemical entities known as bipyridines and oligopyridines. These are organic compounds containing two pyridine rings linked to each other.|
|Super Class||Organic compounds|
|Sub Class||Pyridines and derivatives|
|Direct Parent||Bipyridines and oligopyridines|
|Alternative Parents||3-pyridinecarbonitriles / Methylpyridines / Hydroxypyridines / Heteroaromatic compounds / Nitriles / Azacyclic compounds / Organopnictogen compounds / Organooxygen compounds / Hydrocarbon derivatives|
|Substituents||Bipyridine / 3-pyridinecarbonitrile / Methylpyridine / Hydroxypyridine / Heteroaromatic compound / Azacycle / Nitrile / Carbonitrile / Organic nitrogen compound / Organic oxygen compound|
|Molecular Framework||Aromatic heteromonocyclic compounds|
|External Descriptors||nitrile, pyridone, bipyridines (CHEBI:50693 )|
- Pharmacological action
- General Function:
- Metal ion binding
- Specific Function:
- Cyclic nucleotide phosphodiesterase with a dual-specificity for the second messengers cAMP and cGMP, which are key regulators of many important physiological processes.
- Gene Name:
- Uniprot ID:
- Uniprot Name:
- cGMP-inhibited 3',5'-cyclic phosphodiesterase A
- Molecular Weight:
- 124978.06 Da
- Cone J, Wang S, Tandon N, Fong M, Sun B, Sakurai K, Yoshitake M, Kambayashi J, Liu Y: Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504. [PubMed:10511123 ]
- Kuthe A, Magert H, Uckert S, Forssmann WG, Stief CG, Jonas U: Gene expression of the phosphodiesterases 3A and 5A in human corpus cavernosum penis. Eur Urol. 2000 Jul;38(1):108-14. [PubMed:10859452 ]
- Lefievre L, de Lamirande E, Gagnon C: Presence of cyclic nucleotide phosphodiesterases PDE1A, existing as a stable complex with calmodulin, and PDE3A in human spermatozoa. Biol Reprod. 2002 Aug;67(2):423-30. [PubMed:12135876 ]
- Zhang W, Ke H, Colman RW: Identification of interaction sites of cyclic nucleotide phosphodiesterase type 3A with milrinone and cilostazol using molecular modeling and site-directed mutagenesis. Mol Pharmacol. 2002 Sep;62(3):514-20. [PubMed:12181427 ]
- Shakur Y, Fong M, Hensley J, Cone J, Movsesian MA, Kambayashi J, Yoshitake M, Liu Y: Comparison of the effects of cilostazol and milrinone on cAMP-PDE activity, intracellular cAMP and calcium in the heart. Cardiovasc Drugs Ther. 2002 Sep;16(5):417-27. [PubMed:12652111 ]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]