although they have yet to be characterized
for all four varieties.^15 For example, om-
buin-3-O-rutinoside was found in the leaves
of both varieties ofE. novogranatense, but not
in either variety ofE. coca.Flavonoids found
in the leaves of all four species are kaempferol
3-O-glucoside and quercetin 3-O-glucosi-
de.^16 E. novogranatense(variety not stated)
alsocontainsprocyanidinsB 1 andB 3 ,acatechin
rhamnopyranoside,^17 and a procyanidin glyco-
side (catechin 3-O-rhamnosyl-(4a!8)-
catechin).^18
PHARMACOLOGY AND BIOLOGICAL
ACTIVITIES
Oral administration of whole coca leaf extract
(E. cocafrom Peru) to rats resulted in reduced
food consumption, which could not be entirely
attributed to the content of cocaine.^19 A co-
caine-free extract of the leaves administered
intraperitoneally also reduced food consump-
tion in rats.^20
Preliminary studiesindicatethatafterchew-
ing coca leaves, chronic coca leaf chewers of
Bolivia show increased plasma levels of co-
caine and benzoylecgonine during exercise;^21
from chewing approximately 15 g of leaves, no
significant alteration in blood pressure or heart
rate during maximal^22 or prolonged submaxi-
mal exercise;^23 no change in maximal exercise
capacity;andcomparedtononchewerswithout
coca, greater ventilatory output and free fatty
acidavailabilityduringincrementalexercise.^22
At rest, after chewing approximately 50 g of
leaves for 1 h, chronic coca chewers showed a
significant increase in plasma norepinephrine,
heart rate, hematocrit, and hemoglobin con-
centration compared to nonchewers without
coca. During submaximal exercise, the same
subjects showed a significantly higher mean
arterial blood pressure and a higher heart rate
compared to the nonchewers, suggesting a
compromised circulatory adjustment during
exercise.^24 After chewing 15 g of leaves for
1 h, nonhabitual coca leaf chewers showed a
significant decrease in plasma insulin levels.
During steady-state exercise, they displayed
significant increases in heart rate, oxygen up-
take, and respiratory exchange, whereas the
decreaseinplasmainsulinandglucoseinduced
by exercise appeared to be prevented by the
coca chewing. No evidence was found of acute
coca leaf use increasing tolerance to
exercise.^25
The pharmacological activity and toxicity
of coca is generally attributed to cocaine. In
addition to its local anesthetic, central nervous
system stimulant, and addictive (similar to
amphetamines) properties, cocaine has many
other activities (GOODMAN AND GILMAN;LIST AND
HO ̈RHAMMER;MARTINDALE;MORTON3). Little is
known of the effects of the other alkaloids
present in coca leaf.^26TOXICOLOGYIn a chronic feeding in rabbits, decocainized
leaves of Trujillo coca leaves from which the
majority of cocaine-like alkaloids were re-
moved, doses of 21 or 210 mg produced no
significant signs of toxicity. Rats fed the same
leaf extract at 150 mg showed a significant
decrease in weight gain, but not from doses of
1.5 and 15 mg. At all doses, the rats showed
pyometra often with endometrial metaplasia,
renal tubular calcification, and portal triaditis
in the liver.^27 The LD 50 of a coca leaf (E. coca)
extract in male mice was 3450 mg/kg i.p.^28
Biopsies of the buccal mucosa of chronic
coca leaf chewers of Bolivia showed no evi-
dence of carcinoma or chronic ulceration.
Leukoedema was present in 76% of samples
taken from the side of the mouth that the
subjects placed their coca leaf quid and may
have resulted from the known irritant property
of the lime traditionally added to the leaves
in the course of chewing.^29
The fatal dose of cocaine in humans is
reported to be about 1.2 g, but a dose as low
as 20 mg (0.02 g) has been reported to cause
severe toxic effects (GOODMAN AND GILMAN).
Cocaine abusers show cerebral perfusion
defects, cerebral thrombosis, and high inci-
dences of neuropsychological impairment.
(HIGGINS AND KATZ;).^30Coca 213