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p
Mp pp
p Digoxin (Lanoxin, Lanoxicaps,) Digitoxin
p Digitalis glycosides are composed of a steroid nucleus to which an
unsaturated lactone ring is attached at C-17. These two components, the
aglycone or genin moieties, are responsible for the inotropic activity of
glycosides.
p Digoxin has a half-life of about 1.6 days. By contrast digitoxin's half-life
is about 5 days. Digitoxin is rarely used and may no longer be readily
available in the United States.
p Digoxin is mainly excreted in the urine (85%). By contrast digitoxin is
mainly metabolized in the liver.
p £uabain is very rapidly acting (5 to 10 min onset) after i.v. injection.
p The clinical efficacy of digitalis glycosides is based on improving cardiac
contractility (positive inotropism) and on decreasing transmission through
the A-V node.
p The most important cardiac effect is the shift of the force-velocity
relationship upward.
Mp
pp
p Amrinone (Inocor) and milrinone (Primacor) are bipyridine derivatives
that are relatively selective inhibitors of cGMP-inhbited, cyclic AMP
phosphodiesterase (type III).
p These agents cause vasodilation (decreased afterload) and increase
myocardial contractility.
p Milrinone (Primacor) is the agent of choice among the phosphodiesterase
inhibitors for short-term parenteral support in severe heart failure patients.
rp £ral formulations are not used due to intolerable side-effects
including increases in mortality.
p Amrinone has been associated with a reversible thrombocytopenia.
Mp è
p
p p
p Are used for short-term inotropic support of the failing heart.
p Dobutamine (Dobutrex) is less arrhythmogenic and produces less
tachycardia compared to endogenous catecholamines or isoproterenol
(Isuprel).
p Dobutamine (Dobutrex) is a racemate that binds to and activates -1 and
-2 adrenoceptor subtypes.
Applied Therapeutics: The Clinical Use of Drugs", Sixth edition, edited by Lloyd
Lee-Young and Mary Ann Koda-Kimble, p 15-5, Applied Therapeutics, Inc., 1995,
Seattle, WA.
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