S7/99 CASCARA SAGRADA Rhamnus purshiana - Family Rhamnaceae Synonyms Sacred Bark, California Buckthorn

Description

This tree is 5 - 8 m in height, and has reddish-brown bark, which is often covered with lichen. The leaves are alternate, dark green, elliptic to oblong - ovate, irregular, finely toothed, or often almost entire. In addition, they are rounded at the base and may be obtuse or acute at the apex. The small, greenish flowers grow in finely hirsute umbels and produce black, pea-size drupes.

Parts used

The aged, dried bark.

Constituents

The bark contains 6-9% anthraquinone glycosides, including A, B, C, D, E and F-cascarosides. The glycosides form chrysophanol and emodin complexes. The activity of Cascara is primarily due to the anthraquinones A,B,C and D-cascarosides (C-10 isomers of 8-0-B-D glucopyranosides of deoxybarbaloin and chrysophanol).(1) Cascara also contains smaller amounts of the bitter, less desirable anthracene compounds and aloins that account for the cathartic character of aloes and senna.(2) The cascarosides are found in a concentration of 6 to 9% O-glycosides and C-glycosides.(3,4) The European Pharmacopeia requires official Cascara to contain at least ``... 8% hydro-anthracene derivatives, calculated as cascaroside, of which not less than 60% consists of cascaroside A.``(5) It appears that the more irritative anthranols, dianthrones and anthranes are the likely intermediates of the anthraquinone cascarosides.(6,7) The study of these anthraquinone derivatives is complex as there may be derivatives (about a dozen in Cascara)(8) and their nature may change with age and during extraction.(9) Anthracene derivative plants have been important cathartics for hundreds of years.

Mode of Action

R. purshiana is a mild cathartic laxative(10,11) primarily used in the treatment of chronic constipation. Cascara also has tonic and stomachic properties.(15-19) In the control of habitual constipation it ``not only acts as a laxative but restores natural tone to the colon.(20) Cascara is recommended for piles as it forms a soft non-irritating stool(21) and is also suggested as a useful laxative for hemorrhoidal conditions.(22,23) Cascara is indicated as the cathartic of choice in the elderly and delicate(24) and is non-irritating. The use of Cascara has ``little tendency to produce secondary constipation.(25)

The action of Cascara Sagrada is primarily due to stimulation of increased colonic peristalsis.(26-29) Peristalsis is stimulated through the autonomic nervous system rather than through the local irritative mechanism as is sometimes proposed. The active principles are absorbed through the small intestine, enter the systemic circulation, and stimulate the Auerbach plexus thereby exciting peristalsis.(30) Cascara is mild in action and generally doesn`t cause griping. It is considered the least griping of the emodin cathartics.(31)

Therapeutic Action
Cathartic, bitter tonic, alterative, hepatic, stomachic, and febrifuge.

Energetics

Other

Holmes lists Cascara Sagrada as bitter, a bit astringent, cold and moist; with secondary qualities of stimulating, restoring, dissolving, cleansing sinking movement. It enters the Liver, Gall Bladder, Small Intestine, Stomach and Colon meridians; influencing the liver, gall bladder, stomach and small intestine. Its organism is warmth.(32) Tierra lists it as cold and bitter; influencing the spleen, stomach, liver and colon.(33)

Folklore

This herb has been applied traditionally as a laxative and also as a bitter tonic. It was also used for gallstones, liver ailments, hemorrhoids and the stimulation of digestion.(34) Cascara has been heavily recommended since the mid-1800`s by Eclectic physicians in North America.(35)

Well over a dozen Western North American Indian tribes used Cascara. Not surprisingly, they found its cathartic and laxative effect most useful.(36)

Dosage(37)

Capsules - 1-3, 2-3 times daily
Fluid extract BP - 6 drops - 1 dram (3.6 ml)
Powder extrac t - 2 -10 grains.
Cascara Sagrada powdered bark is listed as between 0.10 and 8.0 grams in the literature.(38)
Merck Index and the U.S. Dispensory - 0.60 to 2.0 grams,(39,40)
B.P.C., 1934 lists the dose as 0.10 to 4.0 grams(41)
1.0 gram Cascara extract is equal to 3.0 grams Cascara, usual dose is 300 mg.(42)
Cascara produces its action 6-8 hours after ingestion(43)

Toxicity and Contraindications

ESCOP lists contraindications for intestinal obstruction and stenosis, atony, inflammatory disease of the colon ( e.g. Crohn`s disease, ulcerative colitis), appendicitis; abdominal pain of unknown origin; severe dehydration state with water and electrolyte depletion. It is also listed not to be used by children under the age of 10 years old(44) Western herbalists often use Cascara (since 19th century) for atony and in small doses for Crohn`s and colitis (under practitioner care). In complex formulas, Cascara is used in children as young as six, if under practitioner care.

Large doses can cause extensive diarrhea accompanied by nausea, vomiting and cramping. The cascarosides are ``generally considered to be safe drugs with a minimum of side effects...``(45) Toxicity appears to be an issue in excessively large doses which may cause irritation.(46)

The Merck Index lists the upper therapeutic dose as 8 grams. Cascarosides may enter a mother`s milk and act as a laxative for some children (many practitioners have noticed this) however, experimental data suggest it should have very little or no effect.. Long term use may induce chronic diarrhea or a pseudomelanin pigmentation of the colon and rectal mucosa.(47,48) This pigmentation is completely harmless and reversible in four to twelve months after use is discontinued.(49) Some authors note that excessive doses can result in cramping, vomiting, and nausea.(50,51) These side effects are generally countered by the addition of a carminative such as ginger or fennel. The younger the bark, the more pronounced the side effects. The ratio of anthrone to anthraquinone constituents changes as the bark is stored. The less predominant and more desirable anthraquinone cascarosides become more common through a slow process of hydrolysis of the constituent glycosides.(52,53) Grieve(54) states that ``the action of the bark becomes milder and less emetic by keeping. Matured bark, three years old, is preferred for pharmaceutical purposes``.

Experimental studies as well as centuries of experience has shown that there is no undesirable or damaging effect if Cascara is taken in moderate doses during pregnancy even though several pharmacopeia suggest it should not be used during the first trimester and others suggest at any time.(55)

Official Recognition and Medical References

Cascara Sagrada has had a long history of use as an official drug. The following are just some of the official preparations of Cascara used in the past.

EXTRACTUM CASCARAE B.P. 1914, U.S.P. 1905, Fr.Codex 1908, (56)
ELIXIR CASCARAE SAGRADAE B.P., 1934(57)
EXTRACTUM CASCARAE SAGRADAE LIQUIDUM B.P.,1934(58)
P.ITAL. 1909(59) Fr.Codex, 1908, GERMAN PHARM, 1910 (60)
EXTRACTUM CASCARAE LIQUIDUM MISCIBLE B.P.C. 1911(61)
EXTRACTUM CASCARAE SAGRADAE SICCUM B.P., 1934(62)
TINCTURA CASCARAE SAGRADAE Fr.Codex, 1908, Ital. Pharm 1909(63)
ESCOP 1996 & 1997
German Commision E 5.12.84
UK General sales list Schedule 1 table A
Belgium Accepted for specific indication No. 90/22 bis.
France Accepted for specific indication
PDR for Herbal medicine

Cascara Sagrada is also currently found in many prescription and ``over-the-counter`` laxative preparations including: Bicholax, Cas-Evac, Casylium, Kordremul with Cascara and many others.

References

1. Morton, J.F., Major Medicinal Plants: Botany, Culture and Uses, Charles C. Thomas Inc, Springfield IL, 1977, p. 201.
2. Leung, A.Y., Encyclopedia of common natural ingredients used in food, drugs, and cosmetics, John Wiley & Sons Inc., New York, 1980, p. 97.
3. Trease, G.E. and Evans, W.C., Pharmacognosy 11 ed., Bailliere Tindall, London, 1978, p. 385.
4. Trease, G.E. and Evans, W.C., Ibid.
5. European Pharmacopeia (Vol. 2), Council of Europe, Maisonneuve S.A., Sainte-Ruffine, France, 1971. p. 355.
6. Tyler, V.E. et al., Pharmacognosy (7th ed.), Lea & Febiger, Phila. PA, 1976. p. 78
7. Robinson, T., The Organic Constituents of Higher Plants (4th ed.), Cordus Press, North Amherst, Mass., 1980. p. 122.
8. Tyler, V.E. et al., Ibid.
9. Robinson, T., Ibid.
10. Remington`s Pharmaceutical Sciences (16th ed.), Mack Publ. Co., Easton PA, 1980. p. 742
11. Leung, A.Y., Ibid. .
12. Spoerke, D.G., Herbal Medications, Woodbridge Press Publ. Co., Santa Barbara CA, 1980, p. 50.
13. Squire, P.W., Squire`s Companion to the Latest Edition of the British Pharmacopeia, J & A Churchill, London, 1908, p. 337.
14. Wood, H.C. and Osol, A., Dispensatory of the United States of America 23rd Ed.,J.B. Lippincott, Montreal, P.Q., 1943. p. 283.
15. Gathercoal, E.N. and Wirth, E.H., Pharmacognosy, Lea & Febiger, Phila. PA, 1936, p. 459.
16. Textbook of Pharmacognosy, J. & A. Churchill Ltd., Rahway, N.J.,1976 p. 90.
17. Wren, R.C., Potter`s New Cyclopaedia of Botanical Drugs and Preparations, Health Science Press, Rustington, Sussex, U.K., 1975. p. 68.
18. Squire, P.W., Ibid.
19. Grieve, M., A Modern Herbal, Jonathan Cape, London, 1931, p.137.
20. Tyler, V.E. et al., Ibid.
21. Martindale: The Extra Pharmacopeia, The Pharmaceutical Press, London, 1941, p. 376.
22. The British Pharmaceutical Codex 1934. The Pharmaceutical Press, London, 1934, p. 290.
23. Morton, J.F., Ibid
24. Grieve, M., Ibid.
25. The Merck Index 5th ed., Merck & Co. Inc., Rahway NJ, 1940. p. 124.
26. Wood, H.C. and Osol, A., Ibid.
27. Martindale, Ibid.
28. Spoerke, D.G.,Ibid.
29. Leung, A.Y., Ibid.
30. Remington`s Pharmaceutical Sciences (16th ed.), Ibid.
31. Remington`s Pharmaceutical Sciences (16th ed.), Ibid.
32. Holmes, P., The Energetics of Western Herbs (2 vols.), Artemis Press, Boulder CO, 1989, p. 176-178.
33. Tierra, M., Planetary Herbology, Lotus Press, Santa Fe, NM, 1988, p. 167.
34. Willard, T.W., Textbook of Modern Herbology, c.w. Progressive Publishing Inc., Calgary, AB, Can., 1988, p. 220.
35. Crellin, p.137-138, Grieves, Ibid.
36. Moerman, D.E., Medicinal Plants of Native America, University of Michigan Museum of Anthropology, Technical Reports, Number 19, Ann Arbor, Michigan, 1986, Vol.1, p. 399.
37. Santillo, H., Natural Healing with Herbs, Hohm Press, Prescott Valley, AZ, p. 98.
38. The British Pharmaceutical Codex 1934. Ibid..
39. The Merck Index 5th ed., Ibid.
40. Wood, H.C. and Osol, A., Ibid.
41. The British Pharmaceutical Codex 1934. Ibid. Grieve, M., Ibid.
42. Remington`s Pharmaceutical Sciences (16th ed.), Ibid.
43. Williams, L.O., Drug and Condiment Plants, Agricultural Handbook 172, U.S.D.A., Washington, D.C., 1960, p. 74.
44. ESCOP, Rhamni purshiani, Cascara; July 1997
45. Leung, A.Y., Encyclopedia of common natural ingredients used in food, drugs, and cosmetics, Ibid., p. 97.
46. Wood, H.C. and Osol, A., Dispensatory of the United States of America 23rd ed., Ibid..
47. Remington`s Pharmaceutical Sciences (16th ed.), Ibid.
48.Morton, J.F., Major Medicinal Plants: Botany, Culture and Uses, Charles C. Thomas Inc, Springfield IL, 1977. p. 204
49 Williams, L.O., Drug and Condiment Plants, Agricultural Handbook 172, Ibid., p. 69.
50. Spoerke, D.G., Herbal Medications, Ibid., p, 51.
51.Morton, J.F., Major Medicinal Plants: Botany, Culture and Uses, Ibid.
52. Griffenberg, G.B. and Hawkins, L.L., Handbook of Non-Prescription Drugs (1973 ed.), American Pharmaceutical Assoc., Washington, D.C., 1973. p. 122.
53. Kinglet, R., Studies in the field of Drugs containing Anthracene Derivatives XVII. The quantitative determination of the anthracene derivatives of Rhamnus purshiana bark., Lloydia Vol. 31, No.1, p. 17 - 22, 1968, p. 17
54. Grieve, M., Ibid
55. ESCOP Ibid
56. Lucus, E.W. and Stevens, H.B., The Book of Pharmacopeias, J & H Churchill, London, 1915, p. 90.
57. The British Pharmaceutical Codex 1934. Ibid., p. 291.
58. The British Pharmaceutical Codex 1934. Ibid.
59. Lucus, E.W. and Stevens, H.B., The Book of Pharmacopeias, Ibid.
60. Lucus, E.W. and Stevens, H.B., The Book of Pharmacopeias, Ibid.
61. Lucus, E.W. and Stevens, H.B., The Book of Pharmacopeias, Ibid. p. 91
62. The British Pharmaceutical Codex 1934. Ibid.
63. Lucus, E.W. and Stevens, H.B., The Book of Pharmacopeias, Ibid., p. 383.