Digoxin
Clinical data | |
---|---|
Pronunciation | /dɪˈdʒɒksɪn/[1][2] |
Trade names | Lanoxin, others |
AHFS/Drugs.com | Monograph |
MedlinePlus | a682301 |
License data | |
Pregnancy category |
|
Routes of administration | By mouth, intravenous |
ATC code | |
Legal status | |
Legal status | |
Excretion | Kidney |
Identifiers | |
| |
JSmol) | |
Melting point | 249.3 °C (480.7 °F) |
Solubility in water | 0.0648 mg/mL (20 °C) |
| |
| |
(verify) |
Digoxin (better known as Digitalis), sold under the brand name Lanoxin among others, is a medication used to treat various
Common side effects include
Digoxin is in the
Medical uses
Irregular heartbeat
The most common indications for digoxin are atrial fibrillation and atrial flutter with rapid ventricular response,[12][13] especially in older or less active patients,[14] though beta blockers and/or calcium channel blockers may be preferred in some patients, such as younger more active ones, or those without heart failure or hemodynamic instability.[15]
Early observational studies showed an increased risk of death in patients taking digoxin, despite an attempt to allow for other risk factors for death (so-called
Heart failure
Abortion
Digoxin is also used intrafetally or amniotically during
Side effects
The occurrence of
Digoxin can lead to cardiac arrhythmias when given with thiazides and loop diuretics. This is because co-administration of Digoxin with drugs such as thiazides and loop diuretics which can cause hypokalemia, low serum levels of potassium in the blood. This exacerbates the potential for cardiac arrythmias because the low levels of potassium reduces the amount of K+ at the ATPase pump and increase calcium levels too much which leads to these arrythmias.[29] It can also cause visual disturbances as well as dizziness or fainting.
Several other drugs associated with ADRs in concommitant use include verapamil, amiodarone, quinidine, tetracycline, and erythromycin.
Overdose
In overdose, the usual supportive measures are needed. If
Pharmacology
Pharmacodynamics
Digoxin's primary mechanism of action involves inhibition of the sodium potassium adenosine triphosphatase (
The inhibition of the
Digoxin also has important
Overall, the heart rate is decreased while
Other electrical effects include a brief initial increase in
The conduction velocity increases in the atria, but decreases in the AV node. The effect upon
Digoxin is also an
Pharmacokinetics
Digoxin is usually given orally, but can also be given by
Digoxin elimination is mainly by
Effective
Quinidine, verapamil, and amiodarone increase plasma levels of digoxin (by displacing tissue binding sites and depressing renal digoxin clearance), so plasma digoxin must be monitored carefully when coadministered.[citation needed]
A study which looked to see if digoxin affected men and women differently found that digoxin did not reduce deaths overall, but did result in less hospitalization. Women who took digoxin died "more frequently" (33%) than women who took placebo (29%). Digoxin increased the risk of death in women by 23%. There was no difference in the death rate for men in the study.[38]
Digoxin is also used as a standard control substance to test for P-glycoprotein inhibition.[39]
Digoxin appears to be a peripherally selective drug due to limited brain uptake caused by binding to P-glycoprotein.[40][41]
Pharmacomicrobiomics
The bacteria Eggerthella lenta has been linked to a decrease in the toxicity of Digoxin.[42] These effects have been studied through comparisons of North Americans and Southern Indians, in which a reduced digoxin metabolite profile correlates with E. lenta abundance.[43] Further studies have also revealed an increase in digoxin toxicity when used alongside erythromycin or tetracycline, the researches attributed this to the decrease in the E. lenta population.[44]
History
Derivatives of plants of the genus
In 1930, Digoxin was first isolated by Dr. Sydney Smith from the
Society and culture
Charles Cullen admitted in 2003 to killing as many as 40 hospital patients with overdoses of heart medication—usually digoxin—at hospitals in New Jersey and Pennsylvania over his 19-year career as a nurse. On March 10, 2006, he was sentenced to 18 consecutive life sentences and is not eligible for parole.[51]
On April 25, 2008, the U.S.
On March 31, 2009, the FDA announced another generic digoxin pill recall by posting this company press release on the agency's web site: "Caraco Pharmaceutical Laboratories, Ltd. Announces a Nationwide Voluntary Recall of All Lots of Digoxin Tablets Due to Size Variability". A March 31 press release from Caraco, a generic pharmaceutical company, stated:
[All] tablets of Caraco brand Digoxin, USP, 0.125 mg, and Digoxin, USP, 0.25 mg, distributed prior to March 31, 2009, which are not expired and are within the expiration date of September, 2011, are being voluntarily recalled to the consumer level. The tablets are being recalled because they may differ in size and therefore could have more or less of the active ingredient, digoxin.[citation needed]
A 2008 study suggested digoxin has beneficial effects not only for the heart, but also in reducing the risk of certain kinds of cancer.[55] However, comments on this study suggested that digoxin is not effective at reducing cancer risk at therapeutic concentrations of the drug,[56] so the results need further investigation.[57]
Brand names
Digoxin preparations are marketed under the
Digoxin and cancer
Cardiac glycosides, particularly digoxin, have been conventionally used for treatment of common cardiac problems, mainly heart failure and cardiac arrhythmias. The interaction of digoxin and cancer has also been studied. Despite existence of numerous preclinical studies that investigated the anticancer effects of digoxin, there are no solid and conclusive results so far.
Several studies have suggested that digoxin may have anticancer properties,[60] others not.[61]
Digoxin, as a cardiac glycoside, has a chemical structure basically similar to that of estradiol. Digoxin has the ability to bind oestrogen receptors, and therefore it has been proposed that it might increase the risk of oestrogen-sensitive breast and uterine cancers.[62] A large Danish study found a complicated picture, with slightly increased risk of breast cancer amongst women taking digoxin, but better prognostic features.[63] The Nurses' Health Study found a similar slight increase of risk.[64]
Digoxin inhibits the proliferation of many cancerous cell lines in vitro,[65][66] but its relevance to cancer in vivo remains unclear.
References
- ^ "Digoxin". Digoxin | Definition of Digoxin by Lexico. Lexico. Archived from the original on 27 October 2019. Retrieved 28 October 2019.
- ^ "digoxin". WordReference. Retrieved 28 October 2019.
- ^ a b "Digoxin Use During Pregnancy". Drugs.com. Archived from the original on 21 December 2016. Retrieved 14 December 2016.
- ^ a b c d e "Digoxin". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
- ^ S2CID 218950180.
- ^ ISBN 9789241547659.
- ^ ISBN 9781317039792. Archivedfrom the original on 2017-09-08.
- ^ PMID 8611904.
- hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
- ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
- ^ "Digoxin - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
- S2CID 127927.
- S2CID 30951337.
- ISBN 9780702066009.
- S2CID 59304609.
- PMID 25660972.
- PMID 25939649.
- PMID 29518134.
- PMID 26321114.
- PMID 26321114.
- ISBN 9780702066009.
- ^ Withering W (1785). An Account of the Foxglove and some of its Medical Uses. Birmingham, England: M. Swinney.
- ^ PMID 34447992.
- PMID 29111106.
- ISBN 9781444358476. Archivedfrom the original on 2017-09-08.
- S2CID 22855158.
- S2CID 30322620.
- PMID 857452.
- ISBN 978-0-340-90046-8.
- S2CID 40869324. Archived from the originalon January 16, 2013. Retrieved July 16, 2007.
- ISBN 978-81-8448-085-6.
- PMID 2344687.
- S2CID 33752611.
- ISBN 978-0-323-47870-0. Archivedfrom the original on 2021-04-20. Retrieved 2021-03-28.
- PMID 29493947. Retrieved 7 May 2023.
- PMID 16160202.
- ISBN 978-0-7817-2845-4. Archived from the originalon 2017-09-08. Retrieved 2016-12-15.()
- PMID 12409542.
- PMID 20190787.
- PMID 10706193.
- PMID 10837715.
- ^ "PharmacoMicrobiomics". pharmacomicrobiomics.com. Archived from the original on 2021-06-02. Retrieved 2020-08-13.
- PMID 2759492.
- PMID 7266632.
- ^ Culpeper N (1652). The English Physician, Etc (1st ed.). London: William Bentley. pp. 97–98. Retrieved 22 January 2023.
- ^ Withering W (1785). An Account of the Foxglove and some of its Medical Uses With Practical Remarks on Dropsy and Other Diseases. Archived from the original on 2017-09-08.
- ISBN 0192615017.
- S2CID 9025850.
- ^ "digoxin". Wiktionary. Wikimedia. 16 January 2023. Retrieved 21 January 2023.
- ^ from the original on 2021-06-02. Retrieved 2020-10-22.
- ^ "Victims' families set to confront killer". USA Today. 2006-01-01. Archived from the original on 2006-01-04.
- ^ "Recalls, Market Withdrawals & Safety Alerts". Federal Drugs Administration. 2008-10-15. Archived from the original on 2008-05-02. Retrieved 2011-11-08.
- ^ "Urgent Digitek Digoxin Recall". U.S. Recall News. 2008-04-28. Archived from the original on 2008-05-04. Retrieved 2009-07-25.
- ^ "Patients Sue Icelandic Drugmaker Over Recalled Heart Drug". The Wall Street Journal. 2008-05-09. Archived from the original on 2009-04-13. Retrieved 2009-07-25.
- PMID 19020076.
- PMID 19240208.
- PMID 2651280.
- ^ "Digoxin: a medicine to treat heart problems". nhs.uk. 2021-09-15. Retrieved 2024-01-24.
- ^ "Digoxin Tablets: Uses & Side Effects". Cleveland Clinic. Retrieved 2024-01-24.
- PMID 31719612.
- PMID 27755533.
- PMID 21422417.
- PMID 23421975.
- PMID 24573543.
- PMID 30183476.
- PMID 28496002.
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.
- Lüllmann H, Kuschinsky G, Mohr K, Wehling M (2003). Pharmakologie und Toxikologie (15th ed.). Georg Thieme Verlag. ISBN 3-13-368515-5.
- Lanatoside C (isolanid, Cedilanid – four glycoside analog), Digoxigenin (aglycone analog)
- Goldberger ZD, Alexander GC (January 2014). "Digitalis use in contemporary clinical practice: refitting the foxglove". JAMA Internal Medicine. 174 (1): 151–154. PMID 24217624.