| Item |
Information |
|
Drug Groups
|
approved |
|
Description
|
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] |
| Indication |
Indicated for the treatment of congestive heart failure. |
| 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. |
| Toxicity |
LD50 = 0.3 mg/L in rats |
| Affected Organisms |
| • |
Humans and other mammals |
|
| Biotransformation |
There are five metabolites but the O-glucuronide represents the major pathway of biotransformation. |
| Absorption |
Milrinone is rapidly and almost completely absorbed after oral administration. Bioavailability is 92% (in healthy volunteers). |
| Half Life |
2.3 hours |
| Protein Binding |
70 to 80% |
| Elimination |
The primary route of excretion of milrinone in man is via the urine. |
| Distribution |
* 0.38 liters/kg [intravenous injections of 12.5 mcg/kg to 125 mcg/kg to congestive heart failure patients]
* 0.45 liters/kg [intravenous infusions of 0.20 mcg/kg/min to 0.70 mcg/kg/min to congestive heart failure patients] |
| Clearance |
* 0.13 L/kg/hr [congestive heart failure patients, following IV injections of 12.5 mcg/kg to 125 mcg/kg]
* 0.14 L/kg/hr [congestive heart failure patients, following infusions of 0.2 mcg/kg/min to 0.7 mcg/kg/min] |
| External Links |
|