Forskolin extract supplements, safety, side effects, review, health benefit,
dose and dosage, 10% 100 mg, interactions and role with yohimbine, aminophylline, cAMP, cyclic AMP
January 2 2018
by Ray Sahelian, M.D.
Coleus forskohlii is an important traditional Ayurvedic herb that has been a
part of Indian medicine for centuries. It
has been used for centuries in Ayurvedic medicine to treat various diseases such as hypothyroidism, heart
disease and respiratory disorders.
In the 1970s, researchers isolated a chemically
active ingredient in the herb and called it forskolin. Now available in supplement form,
this substance has been tested in a number of conditions.
buy Forskolin extract supplement - Coleus Forskohlii
extract, 60 capsules
Modern extraction and analytical techniques are used to produce the
highest quality extract available. Each batch of coleus forskohlii extract is
analyzed and guaranteed to contain a minimum of 18% forskolin.
Buy Forskolin
extract supplement or get a free herbal remedies newsletter
Supplement Facts | ||
Serving Size: 1 Capsule | ||
Servings Per Bottle: 60 Capsules | ||
Amount Per Capsule | % DV | |
Coleus forskohlii extract (root) [standardized to 10% forskolin (10 mg)] | 100 mg | † |
† Daily Value or Recommended not established. |
Supplement facts
Coleus Forskohlii root extract 100 mg
Standardized to contain 10% forskolin (10 mg per
capsule)
The potent herbal extracts in Passion Rx sexual enhancer include Ashwagandha, Aspallum purificata, Catuaba, Cnidium, Coleus forskohlii forskolin extract, Damiana, Horny goat weed, Maca, Mucuna pruriens, Muira puama, Passion flower, Rehmannia, Rhodiola, Tongkat Ali and Tribulus.
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extract capsules
Suggested use, dosage: One capsule forskolin extract once
daily before breakfast.
Forskolin supplements and
weight loss
Body composition and hormonal adaptations associated with forskolin
consumption in overweight and obese men.
Obesity Research. 2005.
This study examined the effect of forskolin on body composition,
testosterone, metabolic rate, and blood pressure in overweight and obese
men. Thirty subjects were studied in a randomized, double-blind,
placebo-controlled study for 12 weeks. Forskolin was shown to elicit
favorable changes in body composition by significantly decreasing body
fat percentage and fat mass. There was a trend toward a significant
increase for lean body mass in the treatment group compared with the
placebo group. Oral ingestion (250 mg of 10% forskolin extract twice a day)
for a 12-week period was shown to favorably alter body composition while
concurrently increasing bone mass and serum free testosterone levels in
overweight and obese men.
Biotech Histochem. 2014. The effects of forskolin and rolipram on cAMP, cGMP and free fatty acid levels in diet induced obesity. We investigated the effects of forskolin and rolipram in the diet of animals in which obesity had been induced. We used 50 female albino Wistar rats that were assigned randomly into five groups as follows: group 1, control; group 2, high fat diet; group 3, high fat diet + forskolin; group 4, high fat diet + rolipram; and group 5, high fat diet + rolipram + forskolin. We found that both forskolin and rolipram stimulated lipolysis and inhibited body weight increase by increasing cAMP levels. Also, combination therapy using the two agents may be more effective in preventing diet induced obesity than either agent alone. We found also that these agents did not effect cellular cGMP levels in diet induced obesity.
Forskolin benefits
Over the years studies have shown that it is a
platelet aggregation inhibitor, relaxes vascular smooth muscle, decreases
intraocular pressure due to glaucoma, and has anti-allergy potential since it
inhibits IgE-mediated release of histamine and peptide leukotriene from human
basophils and mast cells. Forskolin has been shown to be a potent inhibitor of
cancer metastasis in mice injected with malignant cells. In a study
in psychiatry, researchers gave it intravenous to four depressed and five
schizophrenic patients. All four depressed patients showed a transient mood
elevation or stimulation, as did two of the five schizophrenic patients.
This substance may be beneficial as a bronchodilator and anti-allergy agent.
May reduce blood pressure.
It is a United States Food and Drug Administration non-approved vasoactive agent
that acts in synergism with prostaglandin E1 to induce smooth muscle relaxation.
In
combination with other vasoactive agents, forskolin has demonstrated preliminary safety
and efficacy in patients with vascular impotence. See Passion Rx below for a
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Dosage
Forskolin is available over the counter in pills and liquid in a variety of
dosages most commonly 50 mg coleus forskohlii herbal extract providing 9 mg forskolin
and 125 mg coleus forskohlii extract providing 12.5 mg.
Research
is limited on the appropriate dosages for different conditions.
The forskolin content of coleus root is typically 0.2% to 0.3%, therefore the content of crude coleus products may not be sufficient to produce a
pharmacological effect. It is best to use standardized extracts which have
it concentrated.
Coleus forskohlii
is available in various extract potencies, for instance 10 percent forskolin, 18
percent, and 20 percent. We are not aware of any research
that has tested various extract potencies to determine which is best to use.
Forskolin for allergy
Inhibition of IgE-mediated release of histamine and peptide leukotriene
from human basophils and mast cells by forskolin.
Biochem Pharmacol. 1987.
We
found that it caused a concentration-related
inhibition of IgE-mediated release of histamine and peptide leukotriene C4
(LTC4) from human basophils and lung mast cells. Our data suggest that it modulates the release of mediators
of immediate hypersensitivity reactions via the activation of adenylate cyclase
in human basophils and mast cells.
Forskolin for asthma
It is still not very clear to me whether this natural extract is effective for
asthma. Results of studies have not been very convincing.
J Int Med Res. 2010.
Forskolin compared with beclomethasone for prevention of asthma attacks: a
single-blind clinical trial.
Patients with mild or moderately persistent adult asthma were randomly assigned
to receive forskolin (one 10-mg capsule orally per day) or beclomethasone (two
50 microg inhalations every 12 h) for 2 months. No statistically significant
improvement occurred in any lung function parameter in the forskolin-treated
patients. There was no statistically significant difference between both treatment groups for any lung function parameter at
baseline or after treatment. None of the beclomethasone-treated patients had an
asthma attack and one forskolin-treated patient had a mild asthma attack during
the 2-month study period.
Forskolin versus sodium cromoglycate for prevention of asthma attacks: a
single-blinded clinical trial.
J Int Med Res. 2006.
Forty patients of either sex with mild persistent
or moderate persistent
asthma
were assigned randomly to 6 months of treatment
with forskolin at 10 mg a day orally (capsules) or with two inhalations of
sodium cromoglycate every 8 h, three times a day. The number of patients
who had asthma attacks during the treatment period was significantly lower among
those receiving forskolin than among those receiving sodium cromoglycate.
Relaxant effects of forskolin on guinea pig tracheal smooth muscle.
Lung. 1987.
Forskolin caused dose-dependent
relaxant effects on resting tone and on leukotriene C4, leukotriene D4, and carbachol-induced
contraction of tracheal smooth muscle. Moreover, with propranolol
pretreatment the relaxant effect on tracheal smooth muscle
did not change, whereas with the same pretreatment the relaxant effect of
isoproterenol diminished. These
results suggest that it relaxes airway smooth muscle in guinea pigs
in vitro and in vivo by raising tissue cyclic AMP levels and that its
actions are independent of beta-adrenoceptors.
Bladder, urinary tract
infections
Forskolin may boost the ability of antibiotics to kill E. coli -- the bacteria
responsible for 90 percent of bladder infections. In studies in mice, Duke
microbiologist Dr. Soman N. Abraham found that E. coli bacteria hide in cells
lining the bladder, out of reach of antibiotics. However, when the researchers
injected forskolin directly into the bladder or administered it intravenously,
it appeared to expel more than 75 percent of "hiding" E. coli, rendering it
susceptible to antibiotics. While customary antibiotic treatment kills the vast
majority of the bacteria, according to Dr. Soman Abraham, small numbers of
bacteria may survive the antibiotic bath by sneaking into the lining of the
bladder. There they lie there until the opportune moment, after antibiotic
treatment, to come out and start multiplying again. By revving up cellular
activity, forskolin helps flush out bacteria from their niches and into the
urine, where they can be killed by antibiotics. Nature Medicine,
2007.
Comments: Whether forskolin supplements taken orally help
individuals with bladder infections is not clear until human trials are done.
Cancer
Forskolin: a potential antimetastatic agent.
Int J Cancer. 1983.
Forskolin
is a potent platelet aggregation inhibitor and has been examined for its effects
on (a) tumor-induced human platelet aggregation and (b) pulmonary tumor
colonization in mice. These studies employed a subline of B16 murine melanoma,
B16-F10 (highly metastatic to lungs). Forskolin strongly inhibits the melanoma
cell-induced human platelet aggregation. A single dose administered intraperitoneally 30 or 60 min prior to tail vein
injection of cultured B16-F10 cells reduced tumor
colonization in the lungs by more than 70%. These findings raise the possibility that forskolin
could prove of value in the clinic for the prevention of cancer metastasis.
Diabetes and blood sugar
Int J Med Sci. 2014. Effect of chronic administration of forskolin on glycemia
and oxidative stress in rats with and without experimental diabetes. The
antioxidant and antiinflammatory action of forskolin is due to inhibition of
macrophage activation with a subsequent reduction in thromboxane B2 and
superoxide levels. These characteristics have made forskolin an effective
medication for heart disease, hypertension, diabetes, and asthma.
Forskolin extract and impotence
One study evaluated the role of forskolin as an injection into the
corpus cavernosum of the penis. In many cases there was improvement in rigidity
and/or erection.
Intracavernosal forskolin: role in management of
vasculogenic impotence resistant to standard 3-agent pharmacotherapy.
J Urol
1997.
We investigated forskolin, a direct adenylate
cyclase activator, as an intracavernosal vasoactive agent in management of
vasculogenic impotence. Concentration responses for forskolin and prostaglandin E1 induced relaxation of phenylephrine precontracted
strips of human corpus cavernosum smooth muscle were constructed in vitro.
Cyclic adenosine monophosphate (cAMP) synthesis was determined with papaverine,
phentolamine, prostaglandin E1 and forskolin in human corpus cavernosum smooth
muscle cell cultures. In vitro forskolin and prostaglandin E1 alone caused
concentration dependent relaxation. Clinical investigation in 31 patients showed no adverse events. Overall 61% reported improvement in rigidity and/or erection duration
using intracavernosal forskolin, papaverine, phentolamine and prostaglandin E1. Forskolin acts in synergism with prostaglandin E1 to
induce smooth muscle relaxation. In combination with other vasoactive agents,
forskolin has demonstrated preliminary safety and efficacy in patients with
vasculogenic impotence resistant to standard 3-agent pharmacotherapy.
Gastric tissue
Isolated gastric glands were used to investigate the action of forskolin,
a novel diterpene extracted from the Indian plant Coleus forskohlii. Forskolin
was found to stimulate both acid formation and pepsinogen secretion. The
stimulation was rapid, reversible and dose dependent. The efficacy of forskolin
was similar to that of more commonly used secretagogues, e.g. histamine,
carbachol, cyclic AMP derivatives. Forskolin was found to be more effective in
activating adenyl cyclase than histamine, isoproterenol or NaF. Treatment of
gastric glands with forskolin resulted in a 100-fold increase in tissue cAMP
levels, supporting the idea that forskolin activates adenyl cyclase in the
intact cell. The results are interpreted to show that forskolin stimulation of
gastric secretions is due to activation of adenyl cyclase with a consequent
increase in tissue cAMP.
Glaucoma, high intraocular pressure
J Ocul Pharmacol Ther.
2016. Oral Administration of Forskolin, Homotaurine, Carnosine, and Folic Acid
in Patients with Primary Open Angle Glaucoma: Changes in Intraocular Pressure,
Pattern Electroretinogram Amplitude, and Foveal Sensitivity. Twenty-two patients
(44 eyes) with POAG, with their IOP compensated by topical drugs, were enrolled
and randomly assigned to the food supplement or control treatment group. The
additional food supplement treatment consisted of 2 tablets per day (1 in the
morning, 1 in the evening) given for 1 year of a balanced association of
homotaurine, Coleus forskohlii root extract, L-carnosine, folic acid, vitamins
B1, B2, B6, and magnesium. We observed in treated patients a significant further
decrease of IOP. The results of the present pilot study indicate that the
components of the food supplement reach the eye in a detectable manner, as
evidenced by the effects on the IOP. Moreover, they suggest a short-term
neuroactive effect, as indicated by the improvement of foveal sensitivity in
treated, but not in control patients.
Saudi J Ophthalmol. 2015. Efficacy and safety of 1% forskolin eye drops in open angle glaucoma - An open label study. Forskolin 1% eye drops can be a safe alternative to beta blockers in glaucoma patients having concomitant asthma.
Forskolin: upcoming antiglaucoma molecule.
J Postgrad Med. 2012. Department of Pharmaceutics, R. C. Patel Institute of
Pharmaceutical Education and Research, Near Karwand Naka, Shirpur, Maharashtra,
India.
Forskolin is the first pharmaceutical drug and product derived from a plant to
be approved in India by the DCGI in 2006. It is a lipid-soluble compound that
can penetrate cell membranes and stimulates the enzyme adenylate cyclase which,
in turn, stimulates ciliary epithelium to activate cyclic adenosine
monophosphate, which decreases intraocular pressure (IOP) by reducing aqueous
humor inflow. The topical application is capable of reducing IOP in rabbits,
monkeys, and humans. In its drug interactions, it may act synergistically with
epinephrine, ephedrine and pseudoephedrine. Whereas the effects of anti-clotting
medications like warfarin, clopidogre, aspirin, anoxaparin, etc., may be
enhanced by forskolin. This medicine is contraindicated in the medications for
people with ulcers as forskolin may increase acid level.
Forskolin lowers intraocular pressure by reducing
aqueous inflow.
Invest Ophthalmol Visual Sci. 1984.
Forskolin lowers the intraocular pressure of rabbits, monkeys, and
humans. In rabbits, net aqueous humor inflow decreases, outflow facility remains
unchanged, and ciliary blood flow increases. Tolerance to the intraocular
pressure lowering effect did not occur in rabbits after topical doses given
every 6 hr for 15 days. In vitro forskolin activates adenylate cyclase of crude
particulate homogenates prepared from cultured human ciliary epithelia or from
dissected ciliary epithelial processes of rabbit or human eyes. This activation
is not blocked by timolol. The stimulation of adenylate cyclase by isoproterenol
in vitro is potentiated in the presence of forskolin. This substance represents a
potentially useful class of
glaucoma treating agents differing in molecular mechanism
of action from previously used drugs.
Q. Do you sell eye forskolin eye drops or do you know where
they can be purchased?
A. As of 2018, the eye drops are not
currently available in the USA or anyplace else that I know of except Samilabs
in India.
Q. I read that forskolin reduces intraocular pressure and
this makes me cautious about using this for erectile dysfunction. Would using it
affect my eyes in any negative way since it does this? Is it true that it does
this?
A. At this time I am not sure how much of any effect it has on
intraocular pressure when taken as a pill in the low dosages available as a
supplement.
Heart muscle
Forskolin exerts its actions on cells by directly activating the catalytic subunit of adenylatecyclases. The primary effect on heart muscles is the positive inotropic
one, at higher forskolin concentrations, an acceleration of the pacemaker
activity can be observed. External calcium is required for this augmentation of
contraction. Verapamil, prenylamine and tetrodotoxin depress these effects.
Hypertension
Does forskolin extract supplement reduce blood pressure?
We have not seen any definitive research evaluating forskolin
supplements and hypertension in humans.
Mechanism of action, how it works
Forskolin is a diterpene which
directly activates the adenylate cyclase and raises cyclic AMP levels in a variety of
tissues.
Cyclic AMP is an important cell regulating compound. Once formed it activates
many other enzymes involved in diverse cellular functions. Under normal
situations cAMP is formed when a stimulatory hormone (e.g., epinephrine) binds
to a receptor site on the cell membrane and stimulates the activation of
adenylate cyclase. This enzyme is incorporated into all cellular membranes and
only the specificity of the receptor determines which hormone will activate it
in a particular cell. Forskolin appears to bypass this need for direct hormonal
activation of adenylate cyclase. As a result of this direct activation of
adenylate cyclase, intracellular cAMP levels rise. The physiological and
biochemical effects of a raised intracellular cAMP level include: inhibition of
platelet activation; inhibition of mast cell degranulation and histamine
release; increased force of contraction of heart muscle; relaxation of the
arteries and other smooth muscles; increased insulin secretion; and increased
thyroid function.
Review and summary
With so many interesting possibilities, forskolin will likely be continued
to be studied for a long time. Unfortunately, at this point in time, we don't
know enough about forskolin to know for certain which clinical conditions it can
be used effectively and safely.
Drug interaction
Q. I am writing with a question about your review of this herbal supplement
on your site. I am 61 year old very active male, who runs, bikes and walks four
days a week. I have taken Sectral for about 20 years for a benign irregular
heart beat. I got the impression from your review that forskolin might interfere
with those types of drugs. I am incorrect?
A. It is difficult to say since I have not seen any studies
regarding its interaction with different types of prescription medications.
Topical forskolin
Treatment with forskolin can promote skin pigmentation and protect
against the UV light-induced damage. Fair-skinned individuals do not tan when
exposed to UV light due to a defective melanocortin 1 receptor (MC1R) gene --
one of several genes that regulate skin, hair and eye color. The gene plays a
key role in determining if a person has red hair, light skin and sensitivity to
UV light. However, a functional MC1R is not required to achieve skin
pigmentation. Dr. David E. Fisher, from the Dana Farber Cancer Institute in
Boston, and colleagues investigated the effects of UV light in mice lacking a
working MC1R gene. UV light exposure induced melanocyte stimulating hormone
expression in keratinocytes (skin cells) of these red / blonde-haired mice, but
pigmentation did not take place. Melanocytes are a type of skin cells that
produce pigment. Topical application of forskolin, however, caused pigmentation
to occur without the need for UV light, showing that functional MC1R is, in
fact, not required. Forskolin
treatment protected the animals from UV light-induced skin DNA damage. Nature, 2006.
Research
Induction of Drug Metabolism by Forskolin, the Role of The Pregnane X
Receptor and the PKA Signal Transduction Pathway.
J Pharmacol Exp Ther. 2004
Emails
Just want to know if there is any evidence of tolerance in the continued
administration. It seems that there are
a number of beneficial effects, including enhanced exercise tolerance. I have
been taking Tenormin for years and forskolin definitely helps. My brother in law
is a physician and he wondered if forskolin is something that I should cycle on
and off of. Can't find mention of tolerance to forskolin on the internet.
The reason there is little info is
because there is hardly any human studies published with the use of forskolin
supplements for prolonged periods, so we really don't know at this time.
Please tell me if the forskolin supplement contains
anything other than this ingredient, such as an amino acid that might increase
blood pressure.
The herb coleus forskohlii has a number of other substances
that have not been well-studied in terms of their effect on blood pressure.