Digoxin

Uses

Chemical

Sugar-Steroid-Lactone

Presentation

Main Actions

Mode of action

Indirect

Digoxin has a central effect which results in increased vagal activity. The increase in AV conductin is manifested as an increase on PR interval.

Direct

Digoxin blocks the Na/K ATP-ase, competitively binding to the K+ binding site. This has several effects:

Route of administration / Dose

10-20µg/kg 6 hourly enterally or parenterally until desired effect achieved. Must be given slowly, if parenterally (25 µg/min). Peak effects 2 hours after administration.

Effects

Toxicity / Side effects

Frequent. Anorexia, nasuea, vomiting, diarrhoea and abdo pain. Arrythmias. Exacerbated by hypokalaemia, hypernatraemia, hypercalcaemia, hypomagnesaemia, acid-base disturbance, hypoxaemia and renal failure.

Kinetics

Absorption

Highly variable GI absorption with bioavailability of 60-90%.

Distribution

20-30% protein bound in the plasma, but has a VD = 5-11 l/kg. Concentrationin cardiac tissues 15-30 times that in plasma.

Metabolism

Less than 105 undergoes hepatic metabolism

Excretion

50-70% o administered dose excreted unchanged in the urine. Elim T&fract12;=1.6 days

Special points