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