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Parts used and where grown
The dried outer peel of the fruit of bitter orange, with
the white pulp layer removed, is
used medicinally. The leaves are also commonly used in many folk
traditions. The bitter orange
tree is indigenous to eastern Africa, Arabia, and Syria, and cultivated
in Spain, Italy, and
North America.
Bitter orange has been
used in connection with indegestion, loss of appetite, insomnia, and
weight loss.
Historical or
traditional use (may
or may not be supported by scientific studies)
Bitter orange is used similarly in a wide variety of
traditions. In Mexico and South
America the leaf is used as a tonic, as a laxative, as a sedative for
insomnia, and to calm
frazzled nerves.1 2 The peel of the fruit is
used for stomach aches and
high blood pressure.3 4 The Basque people in
Europe use the leaves for
stomach aches, insomnia, and palpitations and the bitter orange peel as
an
anti-spasmodic.5 In traditional Chinese medicine, the peel
of the immature fruit is
used for indigestion, abdominal pain, constipation, and dysenteric
diarrhea. Where the patient
is weak, the milder, mature fruit is used similarly.6 Bitter
orange continues to be
widely used for insomnia and indigestion in many parts of the world.7
Active constituents
Bitter orange has a complex chemical makeup, though it
is perhaps most known for the
volatile oil in the peel. The familiar oily residue that appears after
peeling citrus fruit,
including bitter orange, is this volatile oil. It gives bitter orange
its strong odor and
flavor, and accounts for many of its medicinal effects. Besides the
volatile oil, the peel
contains flavones, the alkaloids synephrine, octopamine, and
N-methyltyramine, and
carotenoids.8 9
How much is usually taken?
Usually 1 to 2 grams of dried peel is simmered for 10 to
15 minutes in a cup of water;
three cups are drunk daily. As a tincture, 2 to 3 ml (with a
weight-to-volume ratio ranging
from 1:1 to 1:5) is often recommended for use three times per day. 10
The purified
volatile oil is generally avoided for reasons discussed in the side
effects section.
Are there any side effects
or interactions?
Bitter orange oil may possibly cause light sensitivity
(photosensitivity), especially in
fair-skinned individuals.11 Generally this occurs only if
the oil is applied
directly to the skin and then exposed to bright light; in rare cases it
has also been known to
occur in people who have taken bitter orange internally. The oil should
not be applied
topically and anyone who uses it internally should avoid bright light,
including tanning
booths.
Internal use of the volatile oil of bitter orange is
also potentially unsafe and should not
be undertaken without expert guidance. Large amounts of orange peel
have caused intestinal
colic, convulsions, and death in children.12 The amounts
recommended above for
internal use should not be exceeded.
One text on Chinese medicine cautions against the use of
bitter orange in
pregnancy.13 This concern is not raised in any other
reference, and the American
Herbal Products Association classifies the herb as "class 1," an herb
that can be safely
consumed during pregnancy when used appropriately.14
Decoctions of bitter orange substantially increased
blood levels of cyclosporine in pigs,
causing toxicity.15 Bitter orange also inhibited human
cytochrome P450 3A (CYP3A)
in the test tube.16 This is an enzyme that helps the liver
get rid of numerous
toxins, and strongly affects metabolism of certain drugs. Bitter orange
might, therefore,
interact with drugs that are metabolized by CYP3A. To be on the safe
side, bitter orange
should not be combined with prescription medications, unless someone is
under the care of an
experienced natural medicine clinician.
At the time of writing, there
were no well-known drug interactions
with bitter orange.
References
1. Martinez M. Las Plantas
Medicinales de Mexico. Mexico City:
Libreria y Ediciones Botas, 1991.
2. Gonzalez-Ferrara MM. Plantas
medicinales del noreste de
Mexico. Monterey, Mexico: Grupo Vitro, 1998.
3. Gonzalez-Ferrara MM. Plantas
medicinales del noreste de
Mexico. Monterey, Mexico: Grupo Vitro, 1998.
4. Bejar E, Bussmann R, Roa C, Sharon
D. Herbs of Southern Ecuador: A
Field Guide to the Medicinal Plants of Vilcabamba. Spring Valley,
CA: LH Press, 2001.
5. Molina GV: Plantas Medicinales
en el Pais Vasco. San
Sebastian, Spain: Editorial Txertoa, 1999.
6. Bensky D, Gamble A, Kaptchuk T. Chinese
Herbal Medicine: Materia
Medica, rev. ed. Seattle: Eastland Press, Inc., 1993.
7. Hernandez L, Munoz RA, Miro G, et
al. Use of medicinal plants by
ambulatory patients in Puerto Rico. Am J Hosp Pharm
1984;41:2060–4.
8. Blumenthal M, Goldberg A,
Brinckmann J, eds. Herbal Medicine:
Expanded Commission E Monographs. Newton, MA: Integrative Medicine
Communications,
1999.
9. Dr. Duke’s Phytochemical and
Ethnobotanical Databases. Cited
2003 Jul 11. Available from URL: www.ars-grin.gov, 2002.
10. Blumenthal M, Goldberg A,
Brinckmann J, eds. Herbal Medicine:
Expanded Commission E Monographs. Newton, MA: Integrative Medicine
Communications,
1999.
11. Blumenthal M, Goldberg A,
Brinckmann J, eds. Herbal Medicine:
Expanded Commission E Monographs. Newton, MA: Integrative Medicine
Communications,
1999.
12. McGuffin M, Hobbs C, Upton R,
Goldberg A, eds. American Herbal
Products Association’s Botanical Safety Handbook. Boca Raton, FL:
CRC Press,
1998.
13. Bensky D, Gamble A, Kaptchuk T. Chinese
Herbal Medicine: Materia
Medica, rev ed. Seattle: Eastland Press, Inc., 1993.
14. McGuffin M, Hobbs C, Upton R,
Goldberg A, eds. American Herbal
Products Association’s Botanical Safety Handbook. Boca Raton, FL:
CRC Press,
1998.
15. Hou YC, Hsiu SL, Tsao CW, et al.
Acute intoxication of cyclosporine
caused by coadministration of decoctions of the fruits of Citrus
aurantium and the
pericarps of Citrus grandis. Planta Med
2000;66:653–5.
16. Guo LQ, Taniguchi M, Chen QY, et
al. Inhibitory potential of herbal
medicines on human cytochrome P450-mediated oxidation: Properties of
umbelliferous or citrus
crude drugs and their relative prescriptions. Jpn J Pharmacol
2001;85:399–408.
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