Pharmacology of Milrinone
Pharmacology of Milrinone
| Indication | Indicated for the treatment of congestive heart failure. |
| Pharmacodynamics | 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. |
| Absorption | Milrinone is rapidly and almost completely absorbed after oral administration. Bioavailability is 92% (in healthy volunteers). |
| Volume of distribution |
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| Protein binding | 70 to 80% |
| Metabolism | 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. |
| Half life | 2.3 hours |
| Clearance |
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| Toxicity | LD50 = 0.3 mg/L in rats |
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