Use of Hawthorn Extract (Crataegus) for the Management of CHF
August 1998; Volume 1: 88-90
By David L. Diehl, MD
Congestive heart failure (chf) is one of the most common conditions affecting cardiac health in the United States. The American Heart Association reports that more than 400,000 new cases are diagnosed annually, and there are a total of 4.7 million people with CHF in this country.
One of the earliest and most well-known examples of the adaptation of herbal medicine to the Western formulary was the use of extracts of foxglove (Digitalis purpurea) to treat "dropsy," or congestive heart failure. If foxglove is on one side of the spectrum of clinical indications of herbal medicine ("potent and potentially dangerous"), hawthorn extract (Crataegus) may be on the other. Now used widely in Europe as a cardiac tonic, it is less potent but far safer than digoxin.
Natural History and Cultural Tradition
The Chinese herbal literature, which dates back hundreds and even thousands of years, describes use of Crataegus pinnatifida berries, known as Shan Zha, mainly for digestive ailments such as bloating, indigestion, flatulence, and diarrhea. The well-known physician and herbalist Dioscorides knew of some of the effects of hawthorn in the first century A.D. Reports of the use of Crataegus species for heart ailments were first noted in Europe in the 17th century, with English herbalist Nicholas Culpeper declaring it "a singular remedy for the [kidney] stone, and no less effective for dropsy." In the 19th century, an Irish doctor became known for his "Secret Remedy for Heart Disease," which was revealed by his daughter (1894) after his death to be hawthorn berry tincture.
According to the German Kommission E, hawthorn is indicated for "declining cardiac performance consistent with New York Heart Association [NYHA] stage II failure." It is also used in Europe for hypertension, cardiac arrhythmias, arteriosclerosis, and Buerger's disease.
Pharmacology
The leaves, flowers, and berries of hawthorn are used, but the flowers have the most cardioactive activity; C. monogyna, C. oxycantha, and C. laevigata are generally used. Crataegus extracts contain a variety of flavonoids (flavones and flavonols) including hyperoside, vitexin, vitexin rhamnoside, and rutin. Oligomeric procyanidins (precursors to flavonoids), pentacyclic triterpenes, and catechin/epicatechin are also present. The oligomeric procyanidins and flavonoids have been shown in animal studies to contribute the most to the pharmacological activity of the whole extract.1
Mechanism of Action
The beneficial effects of hawthorn extract on cardiac function have been demonstrated in isolated animal hearts and in animal physiologic studies. Positive inotropic effects and decreased afterload with consequent improvement in cardiac output and increased cardiac performance have all been shown.2 These effects are not blocked by propanolol, and some may be related to cyclic AMP phosphodiesterase-inhibitory properties.3 In isolated rat hearts, Crataegus extracts can attenuate myocardial damage from coronary occlusion.4 Improved myocardial blood flow in dogs has also been reported.5 Extracts also lower serum cholesterol by increasing LDL-receptor activity on hepatic plasma membranes.
Clinical Studies
In physiologic (non-randomized) studies in patients with NYHA class II heart failure (mild limitation of exercise tolerance, symptoms only with exercise) and class III failure (severe limitation of exercise tolerance), Crataegus extracts have been shown to increase ejection fraction, reduce blood pressure, and reduce the pressure/rate product, a reflection of myocardial oxygen consumption.7 Increase in work tolerance as measured with a bicycle ergometer has also been shown.8
There are a number of clinical studies of the effect of hawthorn in patients with NYHA stage II congestive heart failure, with some NYHA stage III patients included in one non-controlled study. Several of the studies were placebo-controlled and double-blinded. One study compared hawthorn (900 mg/d) with captopril (37.5 mg/d) in a double-blind study design.9
Of five placebo-controlled studies, four showed subjective improvement in symptoms by patient and physician report.10 The captopril controlled study above showed improved exercise tolerance in both groups and no statistical difference between captopril and hawthorn.9 All six studies demonstrated improvement in objective measures, either pressure-rate product, or improved left ventricular ejection fraction.
There are no head-to-head studies comparing hawthorn and digoxin for management of CHF. While the two agents not uncommonly are used adjunctively, studies with hawthorn typically study patients with more mild CHF, typically NYHA class II.11
Formulation/Doses
The preferred form for clinical usage is standardized extracts, given in capsule form or as a tincture. Infusions ("teas") of dried flowers have also been used, but it is important to obtain standardized extracts, since the quality of hawthorn product can vary. Extracts are typically prepared with a defined content of flavonoids (2.2%), oligomeric procyanidins (18.75%), or total flavonoids (adjusted to 10 mg).
Standardized extracts that have a defined amount of flavonoids or oligomeric procyanidins derived from the leaves and flowers have been used for the reported controlled clinical studies. The dose range is 160-900 mg of standardized extract, given in the clinical studies in divided doses (usually bid or tid) for 4-8 weeks. The higher dose range is favored in most clinical studies. Several weeks to months of treatment are recommended. The effects of hawthorn develop slowly, so it is not useful for acute attacks of angina or acute exacerbations of CHF.
Adverse Effects
Hawthorn extracts are exceedingly safe in clinical practice. Review of clinical studies has shown that 3.4% of study participants reported non-specific adverse effects; this was similar to the frequency of adverse effects in the placebo group (4.4%).10 No specific toxicities of hawthorn extracts has been reported.10
Drug Interactions
Some herbalists advise monitoring digoxin levels in patients on this medication who are then started on hawthorn extract. Hawthorn has been used in combination with plants containing cardiac glycosides besides foxglove, including Cereus grandifloris, and Convallaria majalis.
Conclusion
Crataegus extracts may well fill a niche in the management of symptoms of mild to moderate CHF. For example, it may be useful in patients with mild symptoms of CHF or hypertensive heart disease in which the physician wants to try other measures prior to use of digoxin. It has been shown in several prospective randomized controlled trials to have positive effects on subjective symptoms such as shortness of breath and post-exercise fatigue, as well as objective physiologic end points such as pressure-rate-product or bicycle ergometer function. Importantly, it is apparently free of adverse effects. In Europe, where usage is more widespread than in the United States, it may be given before digitalis is tried, or it may be given in addition to digitalis in the management of CHF. Physicians in North America should consider use of standardized extracts of hawthorn in the management of symptoms of mild to moderate congestive heart failure.
References
1. Hobbs C, Foster S. Hawthorn-A literature review. HerbalGram 1990;22:19-33.
2. Ammon HPT, Kaul R. Cardiovascular effects of Crataegus extracts, flavonides, and proanthocyanidins. Part 2, Effects on the heart. DAZ 1994;27:21-35.
3. Petkov E, Nikolov N, Uzunov P. Inhibitory effects of some flavonoids and flavonoid mixtures on cyclic AMP phosphodiesterase activity of rat heart. Planta Medica 1981;43:183-186.
4. Nasa Y, et al. Protective effect of Crataegus extract on the cardiac mechanical dysfunction in isolated perfused working rat heart. Arzneimittel-Forschung 1993;43:945-949.
5. Mavers VWH, Hensel H. Changes in local myocardial blood flow following oral administration of a Crataegus extract to non-anesthetized dogs. Arzneimittel-Forschung 1974;24:783-785.
6. Rajendran S, Deepalakshmi PD, Parasakthy K, et al. Effect of tincture of Crataegus on the LDL-receptor activity of hepatic plasma membrane of rats fed an atherogenic diet. Atherosclerosis 1996;123:235-241.
7. Schussler M, Holzl J, Fricke U. Myocardial effects of flavonoids from Crataegus species. Arzneimittel-Forschung 1995;45:842-845.
8. Schmidt U, Kuhn U, Ploch M, et al. Efficacy of the hawthorn (Crataegus) preparation LI 132 in 78 patients with chronic congestive heart failure defined as NYHA functional class II. Phytomedicine 1994;1: 17-24.
9. Tauchert M, Ploch M, Hubner WD. Effectiveness of the hawthorn extract LI 132 compared with the ACE inhibitor captopril: Multicenter double-blind study with 132 NYHA stage II patients. Munch Med 1994;136(suppl 1):S27-33.
10. Busse W. Standardized Crataegus extract clinical monograph. Quarterly Rev Nat Med 1996;Fall: 189-197.
11. Weikl A, et al. Crataegus Special Extract WS 1442. Assessment of objective effectiveness in patients with heart failure (NYHA II). Fortschritte der Medizin 1996;114:291-296.
12. Toxicity of Crataegus (Hawthorn) extract (WS 1442). J Am Coll Toxicol 1994;13:103-111.
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