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Aphrodisiacs past and present: A historical review

Article  in  Clinical Autonomic Research · November 2001

DOI: 10.1007/BF02332975 · Source: PubMed

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Flgure 1. Chemical structure of ambrein.
have shown that this tricyclic ttiterpene alcohol increases the
concentrations of several anterior pituitary hormones and
serum testosterone, which m turn stimulate dopam~nere-
ceptor synthesis and sexual behanor [4]. Amhrein also en-
hances central noradrenergic traficking, which in turn
stimulates sexual arousal, and it can antagonize the contrac-
tile action of various agents (acetylcholine, noradrenaline,
prostaglandin, oxytocin) on smooth muscles [3].
Flgure 2. Ambra grisea: lumps found In the gut of a sperm
whale. (From Ralph RD. Ambergris: a pathfinder and annotated
bibliography. Updated 10-4-98. Available at: http://www.uncg.
edu/lis/faculty/ralphlwritings/amberg~. Accessed October
2, 2000. By permission of the author.)
304 Clinical Autonomic Research 2001, Vol 11 No 5
Saluia haematoaks has been reported ro have an anxiolytic
effect, to decrease brain serotonin synthesis, and to contain
flavonoids, which have antioxidant properties [6]. Andoxi-
dant compounds can in turn alter androgen levels.
Litbopmum aruense (bird millet) is a plant whose leaf
and seeds have androgenic, gonadotropic, and estrogenic
properties, hence its aphrodisiac effect 171. No toxicity is
known.
In Arab countries, Brmica rapa, h n u r amygdah, and
Zingiber oficinale are used for their aphrodisiac effects and
various other medical properties [8]. Animal studies have
demonstrated their androgenic activity, with toxicity lim-
ited to androgen effects (weight gain, alopecia) and mild
anemia.
Bufo toadskin and glands contain bufotenine (Fig. 3) and
its O-methylated derivative, 5-MeO-DMT (5-methoxy-
N,N-dimethyltryptamine), a putative Wudnogen conge-
ner of serotonin 191. It is the active ingredient in West
Indian "love stone" and the Chinese medication chan nr
[lo]. Its use dates to prehistoric ages, crossing many cultures
and continents. Because of its pressor and digitalis-like
properties, it was recommended as a heart medication and
diuretic and to stop bleeding diathesis [9]. Curiously, Ger-
man violinists handled toads before performances to reduce
sweat production in their palms [9]; the mechanism
thrkgh which this is achieved is unclear: no anticholinergic
property is described in toad skin secretions. The aphrodi-
siac p r o p e ~ e sare likely of central origin, as are other (psy-
choactive) effects of the drug; hence, it is listed as a hallu-
cinogen. The toad has a prominent position in mythology,
religions, occult and magic rituals, and fairy tales. How that
popularity relates to its venom is a mystery.
A nonspecific increase in sexually oriented behavior oc-
curs with the inrake of central nervous system stimulants,
such as amphetamine, cocaine, dopaminergic agents, caf-
feine, antiserotonin drugs, cannabis, and marijuana. Various
stimulants are present in beverages and chewable derivatives
of the kok nut, guarana, and betel nut, the use of which
as recreational and aphrodisiac drugs is widespread in Af-
rica, Asia, and Latin America [ll]. These nuts also contain
do
Cardenollde
Bufodlenollde
I b'
Figure 3. Chemical structures of some of the active compounds in
Bufo toad secrenons
tannin, whose carcinogenic and antinutritional propetties
are well known. The effect of ethanol is likely through
disinhibition, but it decreases potency.
Substances that increase potency (allow or
sustain erection)
The mode of action of these compounds is generally
through induction of vasodiifation, to allow for erection to
occur. Such remedies are used almost exclusively by males,
although to a lesser degree they could be efTective in women.
Sildenaiil (under the brand name Kagra; Pfmr, New York,
NY, U.S.A.)(Fig. 4), an oral drug for men with erectile
dysfunction, produces satisfactory erections and improves
sexual satisfaction without affecting sexual desire [12].
Sidenafil also may be useful for treating female sexual dys-
function [13,14]. It appears to be effective for various con-
ditions that cause impotence, such as diabetes, starus post-
prostatectomy, spinal cord injuries, drug effect, and even
psychogenic impotence [14,15]. Sildenafil competitively in-
hibits type-V cyclic guanosine monophosphate (cGMP)-
specific phosphodiesterase enzyme. Inhibition of that iso-
enzyme increases stores of cGMP, the second messenger of
nitric oxide and a mediator of vasodilatation to the penis,
which relaxes corpus cavernosal smooth muscle cells and
increases blood flow into cavernosal spaces. This leads to
increased intracavernosal pressure, which is a major factor in
producing erection.
Because of its additive vasodilating effects and potential
for a dangerous drop in blood pressure, sildenafil must not
be taken concurrently with nittate therapy, and they should
not be used within 24 hours of each other. Patients with
adrenergic autonomic dysfunction, who are unable to com-
pensate for hemodynamic perturbations, are particularly at
risk for sildenaiil's hypotensive effect. Unfomnately, such
individuals likely are a significant portion of patients who
might need sildenafii.
Flgure 4. Chemical structure of sildenafil.
ngure 5. Ginseng rwts.
Sildenafiil may produce potentially hazardous cardiovas-
cular effects for ~ettainpatients, such as those with coronary
ischemia or congestive heart failure, or patients caking mul-
tidrug antihypertensive regimens or drugs that might pro-
long the half-life of sildenafil [16,17]. Patients in dose-
escalation trials have reported seeing a blue haze and
transient increased brightness when taking sildenafil in
doses of more than 200 mg [13]. Transient abnormal vision
occurred in 3% of patients in flexible-dose trials and in 11%
of patients in bed-dose studies and was more common at
100-mg doses than at lower doses. Such a phenomenon is
due to the drug effect on retinal phosphodiestera.se, and
therefore the use of sildenafil is conttaindicated in patients
with retinitis pigmentosa or other retinal abnormality.
Headache occurred in 11% to 16% of patients in large
studies [13,14,181, and it can be severe.
Panax (panacea) ginseng is a root (Fig. 5) used in ttadi-
tional Chinese medicine [19]. It works as an antioxidant by
enhancing nitric oxide synthesis in the endothelium of
many organs [201, including the corpora cavernosa. Ginse-
nnsides also enhance acetylcholine-induced and ttansmural
nerve stimulation-activated relaxation associated with in-
creased tissue cyclic guanosine monophosphate, similar to
sildenaiil, hence the aphrodisiac properties. Ginseng's cen-
tral effect (increase in brain stem dopamine, nnrepineph-
time, cortical serotonin, attenuation of monoamine oxidase
activity) can explain its memory-enhancing and antianxiety
properties and contribute to its aphrodisiac effect. In addi-
tion, ginseng significandy increases workload and oxygen
uptake in normal subjects, and, at fixed load, it decreases
oxygen consumption and carbon dioxide and lactate pto-
duction, confirming its ergogenic properties, particularly
evident when the organism is challenged, taxed, or ex-
hausted (eg., the elderly and athletes). At the recommend-
ed doses, no toxicity is known. Inhalation of "poppers"
Clinical Autonomic Research 2001, Vol 11 No 5 305
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