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Digoxin
Digoxin
ory, the increased force of contraction should lead to improved pumping function of the heart, but its eect on
prognosis is disputable, and other eective treatments
are now available. Digoxin is no longer the rst choice
for congestive heart failure, but can still be useful in patients who remain symptomatic despite proper diuretic
and ACE inhibitor treatment.
Digoxin INN (/ddksn/[1] ) is a puried cardiac glycoside similar to digitoxin extracted from the foxglove
plant, Digitalis lanata.[2] Its corresponding aglycone is
digoxigenin, and its acetyl derivative is acetyldigoxin.
Digoxin is widely used in the treatment of various heart
conditions, namely atrial brillation, atrial utter and Digitalis/digoxin has recently fallen out of favor because
sometimes heart failure that cannot be controlled by other it did not demonstrate a mortality benet in patients with
congestive heart failure; however, it did demonstrate a remedication.
[7]
Digoxin preparations are marketed under the trade duction in hospitalizations for this condition. Because
names Cardigox; Cardiogoxin; Cardioxin; Cardoxin; other therapies have shown a mortality benet in congesCoragoxine; Digacin; Digicor; Digomal; Digon; Digosin; tive heart failure, maximizing other therapies (e.g., beta
Digoxine Navtivelle; Digoxina-Sandoz; Digoxin-Sandoz; blockers) rst is recommended before using digoxin.
Digoxin-Zori; Dilanacin; Eudigox; Fargoxin; Grexin;
Lanacordin; Lanacrist; Lanicor; Lanikor; Lanorale;
Lanoxicaps; Lanoxin; Lanoxin PG; Lenoxicaps;
Lenoxin; Lifusin; Mapluxin; Natigoxin; Novodigal;
Purgoxin; Sigmaxin; Sigmaxin-PG; Toloxin.
2 Adverse eects
Derivatives of plants of the genus Digitalis have a long history of medical use. The British physician William Withering is credited with the rst published description of the
use of digitalis derivatives in his 1785 book An Account
of the Foxglove and some of its Medical Uses With Practical Remarks on Dropsy and Other Diseases.[4]
Today, the most common indications for digoxin are
atrial brillation and atrial utter with rapid ventricular
response, though beta blockers and/or calcium channel
blockers are a better rst choice.[5][6] High ventricular
rate leads to insucient diastolic lling time. By slowing down the conduction in the AV node and increasing
its refractory period, digoxin can reduce the ventricular
rate. The arrhythmia itself is not aected, but the pumping function of the heart improves owing to improved lling.
The use of digoxin in heart problems during sinus rhythm
was once standard, but is now controversial. In the1
4 MECHANISMS OF ACTION
for a reduction in dose or a switch to a dierent glycoside, such as digitoxin (not available in the United States),
which has a much longer elimination half-life of around
seven days, elimination is mainly by renal excretion and
involves P-glycoprotein which leads to signicant clinical
interactions with other drugs commonly used in patients
with heart problems. These include: spironolactone, verapamil and amiodarone. ( Inhibit P-glycoprotein that is
mainly responsible for Digoxin Clearance )
Eective plasma levels vary depending on the medical indication. For congestive heart failure, levels between 0.5
and 1.0 ng/ml are recommended.[19] This recommendation is based on post hoc analysis of prospective trials,
suggesting higher levels may be associated with increased
mortality rates. For heart rate control (atrial brillation),
plasma levels are less dened and are generally titrated
to a goal heart rate. Typically, digoxin levels are considered therapeutic for heart rate control between 1.0 and 2.0
ng/ml. In suspected toxicity or ineectiveness, digoxin
levels should be monitored. Plasma potassium levels also
need to be closely controlled (see side eects below).
digoxin
should
avoid
taking
Pharmacokinetic properties
4 Mechanisms of action
Digoxins primary mechanism of action involves inhibition of the Na+/K+ ATPase, mainly in the myocardium.
This inhibition causes an increase in intracellular sodium
levels, resulting in a reversal of the action of the sodiumcalcium exchanger, which normally imports three extracellular sodium ions into the cell and transports one intracellular calcium ion out of the cell. The reversal of
this exchange causes an increase in the intracellular calcium concentration that is available to the contractile proteins, resulting in an increase in the force of myocardial
contraction. The inhibition of the sodium pump may
also improve baroreceptor sensitivity in HF and may explain some of the neurohormonal eects of digoxin.[20]
Digoxin also has important parasympathetic eects, par-
3
ticularly on the atrioventricular node.[21]
6 Predecessors
7 References
[1] OED
[2] Hollman A (1996). Digoxin comes from Digitalis
lanata". British Medical Journal 312 (7035): 912.
doi:10.1136/bmj.312.7035.912.
[3] WHO Model List of EssentialMedicines. World Health
Organization. October 2013. Retrieved 22 April 2014.
[4] Withering, William (1785). An Account of the Foxglove
and some of its Medical Uses With Practical Remarks on
Dropsy and Other Diseases.
REFERENCES
[6] Hallberg P, Lindbck J, Lindahl B, Stenestrand U, Melhus H (October 2007). Digoxin and mortality in
atrial brillation: a prospective cohort study. European Journal of Clinical Pharmacology 63 (10): 959971.
doi:10.1007/s00228-007-0346-9. PMID 17684738.
[19] Hunt SA, Abraham, WT, Chin, MH et al. (September 2005). ACC/AHA 2005 Guideline Update for
the Diagnosis and Management of Chronic Heart Failure in the Adult: a report of the American College of Cardiology/American Heart Association Task
Force on Practice Guidelines (Writing Committee to
Update the 2001 Guidelines for the Evaluation and
Management of Heart Failure): developed in collaboration with the American College of Chest Physicians and the International Society for Heart and
Lung Transplantation: endorsed by the Heart Rhythm
Society (pdf). Circulation 112 (12): e154e235.
doi:10.1161/CIRCULATIONAHA.105.167586. PMID
16160202.
[7] The eect of digoxin on mortality and morbidity in patients with heart failure.
The Digitalis
Investigation Group.
The New England Journal
February 1997.
of Medicine 336 (8): 525533.
doi:10.1056/NEJM199702203360801. PMID 9036306.
[8] Rossi S, ed. (2006). Australian Medicines Handbook
2006. Adelaide. ISBN 0-9757919-2-3.
[9] Tripathi KD (ed.). Essentials of Medical Pharmacology
(6th ed.). New Delhi: Jaypee Publications. ISBN 818448-085-7.
[10] Moscovitz T, Aldrighi JM, Abrahanshon PA et al. (April
2005). Repercussions of digoxin, digitoxin and estradiol on the endometrial histomorphometry of oophorectomized mice. Gynecology and Endocrinology 20 (4):
213220. doi:10.1080/09513590400021219. PMID
16019364.
[11] Thompson DF, Carter JR (1993). Drug-induced gynecomastia. Pharmacotherapy 13 (1): 3745. PMID
8094898.
[12] Doering W, Knig E, Sturm W (1977). "(title in German)" [Digitalis intoxication: specicity and signicance of cardiac and extracardiac symptoms. part I: Patients with digitalis-induced arrhythmias (authors transl)].
Zeitschrift fr Kardiologie (in German) 66 (3): 121128.
PMID 857452.
[13] Goldfrank LW (2006). Goldfranks Toxicologic Emergencies (8th ed.). New York: McGraw-Hill.
[14] Leden I (1982). Digoxin-hydroxychloroquine interaction?". Acta Medica Scandinavica 211 (5): 411
412. doi:10.1111/j.0954-6820.1982.tb01971.x. PMID
7113754.
[15] Flanagan RJ, Jones AL (2004). Fab Antibody Fragments: Some Applications in Clinical Toxicology. Drug
Safety 27 (14): 11151133. doi:10.2165/00002018200427140-00004. PMID 15554746.
[16] Kaplanski J, Weinhouse E, Topaz M, Genchik G (1983).
Verapamil and digoxin: interactions in the rat. Research
Communications in Chemical Pathology and Pharmacology 42 (3): 377388. PMID 6665298.
[17] Dasgupta A, Kidd L, Poindexter BJ, Bick RJ. Interference
of hawthorn on serum digoxin measurements by immunoassays and pharmacodynamic interaction with
digoxin. Arch Pathol Lab Med. 2010 Aug;134(8):118892.
Further reading
Rang HP, Dale MM, Ritter JM, Moore PK (2003).
Pharmacology (5th ed.). Edinburgh: Churchill Livingstone. ISBN 0-443-07145-4.
Summary of Product Characteristics, Digoxin 0,125
mg, Zentiva a.s.
Lllmann (2003). Pharmakologie und Toxikologie
(15th ed.). Georg Thieme Verlag. ISBN 3-13368515-5.
Lanatoside C (isolanid, Cedilanid - four glycoside
analog), Digoxigenin (aglycone analog)
Goldberger AD, Alexander GC. Retting the Foxglove: Digoxin Use in Contemporary Clinical
External links
Lanoxin
U.S. National Library of Medicine: Drug Information Portal Digoxin
Commonly used website to calculate empiric
digoxin doses for medical purposes for heart problems
1. Protein Data Bank entry (useful for computational molecular dynamics): http://www.rcsb.org/
pdb/explore.do?structureId=3B0W
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