Methysergide-induced heart disease: a case of multivalvular and myocardial fibrosis.

Mason, J W; Billingham, M. E.; Friedman, Joelp .

doi:10.1161/01.cir.56.5.889

Cited by 49 publications

(13 citation statements)

References 6 publications

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“…Several case reports have found both drugs to be associated with mitral, aortic, and tricuspid valve lesions that in some cases led to rightsided HF. [239][240][241][242] The onset of these findings occurred typically after years of long-term administration, and the valve abnormalities did not completely resolve on drug discontinuation. 243 The mechanism of the valve fibrosis is thought to be related to excess serotonin activity because both methysergide and ergotamine are partial serotonin agonists.…”

Section: Antimigraine Medicationsmentioning

confidence: 99%

Drugs That May Cause or Exacerbate Heart Failure

Page¹,

O’Bryant²,

Cheng³

et al. 2016

Circulation

348

185

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Heart failure is a common, costly, and debilitating syndrome that is associated with a highly complex drug regimen, a large number of comorbidities, and a large and often disparate number of healthcare providers. All of these factors conspire to increase the risk of heart failure exacerbation by direct myocardial toxicity, drug-drug interactions, or both. This scientific statement is designed to serve as a comprehensive and accessible source of drugs that may cause or exacerbate heart failure to assist healthcare providers in improving the quality of care for these patients.

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Section: Antimigraine Medicationsmentioning

confidence: 99%

Drugs That May Cause or Exacerbate Heart Failure

Page¹,

O’Bryant²,

Cheng³

et al. 2016

Circulation

348

185

View full text Add to dashboard Cite

show abstract

“…In this regard, in the mid-1960s, researchers and physicians noticed a strong connection between the ergot agents methysergide and ergotamine and the development of fibrotic pathologies including HVD (Graham, Suby et al 1966; Graham 1967; Mason, Billingham et al 1977). Some even went as far as to note that the “similarities in chemical structure of serotonin, methysergide, and ergotamine” may “suggest a common pathophysiologic mechanism for ergot alkaloid-associated valve disease and carcinoid valve disease” (Redfield, Nicholson et al 1992).…”

Section: Serotonergic Drugs and Heart Valve Diseasementioning

confidence: 99%

Serotonin receptors and heart valve disease—It was meant 2B

Hutcheson

Setola

Roth

et al. 2011

Pharmacology & Therapeutics

192

153

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Carcinoid heart disease was one of the first valvular pathologies studied in molecular detail, and early research identified serotonin produced by oncogenic enterochromaffin cells as the likely culprit in causing changes in heart valve tissue. Researchers and physicians in the mid-1960s noted a connection between the use of several ergot-derived medications with structures similar to serotonin and the development of heart valve pathologies similar to those observed in carcinoid patients. The exact serotonergic target that mediated valvular pathogenesis remained a mystery for many years until similar cases were reported in patients using the popular diet drug Fen-Phen in the late 1990s. The Fen-Phen episode sparked renewed interest in serotonin-mediated valve disease, and studies led to the identification of the 5-HT2B receptor as the likely molecular target leading to heart valve tissue fibrosis. Subsequent studies have identified numerous other activators of the 5-HT2B receptor, and consequently, the use of many of these molecules has been linked to heart valve disease. Herein, we: review the molecular properties of the 5-HT2B receptor including factors that differentiate the 5-HT2B receptor from other 5-HT receptor subtypes, discuss the studies that led to the identification of the 5-HT2B receptor as the mediator of heart valve disease, present current efforts to identify potential valvulopathogens by screening for 5-HT2B receptor activity, and speculate on potential therapeutic benefits of 5-HT2B receptor targeting.

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“…Multiple additional case reports suggest a link between prolonged methysergide exposure and development of cardiac valvulopathy. The gross examination and histological findings from these patients reveal striking similarities to carcinoid heart disease, except that these findings predominantly involve left-sided heart valves (Table 1, refs 11, 12, 14, 15). …”

Section: Drug-induced Cardiac Valvulopathymentioning

confidence: 82%

Role of Serotoninergic Pathways in Drug-Induced Valvular Heart Disease and Diagnostic Features by Echocardiography

Smith

Fuentes²,

Dávila‐Román³

2009

Journal of the American Society of Echocardiography

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Serotonin plays a significant role in the development of carcinoid heart disease, which primarily leads to fibrosis and contraction of right-sided heart valves. Recently, strong evidence has emerged that the use of specific drug classes such as ergot alkaloids (for migraine headaches), 5-hydroxytryptamine (5-HT or serotonin) uptake regulators/inhibitors (for weight reduction), and ergot-derived dopamine agonists (for Parkinson’s disease) can result in left-sided heart valve damage that resembles carcinoid heart disease. Recent studies suggest that both right- and left-sided drug-induced heart valve disease involves increased serotoninergic activity and in particular activation of the 5-HT receptors, including the 5-HT2B receptor subtype, which mediate many of the central and peripheral functions of serotonin. G-proteins that inhibit adenylate cyclase activity mediate the activity of the 5-HT2B receptor subunit which is widely expressed in a variety of tissues including liver, lung, heart, and coronary and pulmonary arteries; and it has also been reported in embryonic mouse heart, particularly on mouse heart valve leaflets. In this review we discuss the salient features of serotoninergic manifestations of both carcinoid heart disease and drug-induced cardiac valvulopathy with an emphasis on echocardiographic diagnosis.

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Methysergide-induced heart disease: a case of multivalvular and myocardial fibrosis.

Cited by 49 publications

References 6 publications

Drugs That May Cause or Exacerbate Heart Failure

Drugs That May Cause or Exacerbate Heart Failure

Serotonin receptors and heart valve disease—It was meant 2B

Role of Serotoninergic Pathways in Drug-Induced Valvular Heart Disease and Diagnostic Features by Echocardiography

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