Digoxin

Cataneo, Dollesin, Fajardo, Malabad

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 Pharmacology

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 Definition of Terms
A cardiotonic glycoside obtained mainly from
Digitalis lanata; it consists of three sugars and the
aglycone digoxigenin.
Digoxin has positive inotropic and negative
chronotropic activity. It is used to control ventricular
rate in atrial fibrillation and in the management of
congestive heart failure with atrial fibrillation.
The margin between toxic and therapeutic doses is
small.

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 Doses- Route of
Administration
TABLETS
The usual amount of digoxin tablets that a 70 kg
patient requires to achieve 8 to 12 mcg/kg peak
body stores is 750 to 1250 mcg.

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 CAPSULES
The usual amount of digoxin capsules that a 70 kg
patient requires to achieve 8 to 12 mcg/kg peak
body stores is 600 to 1000 mcg.

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 INJECTION
The usual amount of digoxin injection that a 70 kg
patient requires to achieve 8 to 12 mcg/kg peak
body stores is 600 to 1000 mcg.

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 ADME Profile
ABSORPTION
80 % absorbed after oral administration of tablets
75-80 % absorbed after administration of elixir
75-80 % absorbed from liquid filled capsule
80 % absorbed IM but not recommended

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 DISTRIBUTION
Bound tightly to muscles tissues Vd Correlated well
with lean body Tissues , very large distribution
volume Vd = 7.3 L/kg x IBW , approximately 475 to
500L
25 % protein bound
Crosses the placenta and enter the breast milk
Pregnancy category C I-Pharmacokinetics of
Digoxin

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 METABOLISM
Less than 10 % undergoes hepatic metabolism
Not dependent of the cytochrome P450 system and
it is not know to induce or inhibit it
Metabolism via stepwise cleavage of the sugar
moieties and lactone ring reduction

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 ELIMINATION
Digoxin Elimination follows first-order kinetics
50-70% is excreted almost entirely unchanged by
the kidney
Affected by some drugs interactions & diseases
conditions
Half life 36-48 hours and increase in case of renal
impairment

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Pharmacodynamics

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 Mode of Action

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 Interaction
FOOD INTERACTION

Avoid avocado
Avoid bran and high fiber foods within 2 hours of
taking this medication.
Avoid excess salt/sodium unless otherwise instructed
by your physician.
Avoid milk, calcium containing dairy products, iron,
antacids, or aluminum salts 2 hours before or 6 hours
after using antacids while on this medication.
Avoid salt substitutes containing potassium.
Limit garlic, ginger, gingko, and horse chestnut.

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 DRUG INTERACTION
The Class IA antiarrhythmic, quinidine. Similar
interactions occur with calcium-channel
blockers and nonsteroidal anti-inflammatory drugs.
Other drugs that interact with digitalis compounds
are amiodarone (Class III antiarrhythmic) and beta-
blockers.

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Pharmacokinetics

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Oral bioavailability (F) 70%

Clearance (CL) 6 L/h

Volume of distribution (Vd) 400 L

Half-life (t1/2) 40 h

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 Due to its narrow therapeutic index and the readily
available methods to measure its plasma
concentration, digoxin is a very good candidate
for therapeutic drug monitoring (TDM).

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 REFERENCE
Klabunde, Richard E. (2005-2015).Cardiac
Glycosides (Digitalis Compounds).Retrieved from
http://cvpharmacology.com/cardiostimulatory/digi
talis
Drug Bank (2016, August 17). Digoxin. Retrieved from
https://www.drugbank.ca/drugs/DB00390
Digoxin Pharmacokinetic Monitoring. Retrieved from
http://www.vhpharmsci.com/vhformulary/Tools/Dig
oxin-Pharmacokinetic-Monitoring.htm

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