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Forskolin - Coleus Forskohlii

Forskolin (7 beta-acetoxy-8, 13-epoxy-1 alpha,6 beta,9 alpha-trihydroxy-labd-14-ene-11-one) is the main active ingredient in the Ayurvedic herb Coleus forskohlii. Coleus is a member of the mint family and grows in subtropical areas in India, Burma, and Thialand. Forskolin has been researched in the medical field for use in the treatment of allergies, respiratory problems, cardiovascular diseases, glaucoma, psoriasis, hypothyroidism and weight loss. Forskolin increases Cyclic AMP and appears to have additional actions that are due to its ability to alter a number of membrane transport proteins.

Effects of Forskolin (coleus forskohlii) on Cyclic AMP

Increased cellular cyclic AMP results in inhibition of platelet activation, decreased likelihood of blood clots, reduced release of histamine, decreased allergy symptoms, increased force of contraction of the heart, relaxation of the arteries and other smooth muscles, increased thyroid function, increased fat metabolism, increased energy and possibly weight loss. Cyclic AMP and the chemicals it activates comprise a second messenger system that is responsible for carrying out the complex and powerful effects of hormones in the body.

In addition, asthma, eczema, psoriasis, angina, obesity and hypertension are believed to be associated with decreased Cyclic AMP.

Forskolin (coleus forskohlii) and Glaucoma

Glaucoma is a condition in which the pressure in the eye is too high, due to an imbalance between the formation of aqueous humor in the eye and its absorption in or drainage out of the eye. Eventually, as the pressure builds up, the blood vessels nourishing the optic nerve are constricted, resulting in irreversible damage to the nerve and impaired vision culminating in blindness, if left untreated.

While there are no clinically proven alternative therapies for glaucoma, there are several treatments that may be beneficial and forskolin is one of them. Clinical studies have shown that topical application of one percent forskolin eye drops resulted in significant decreases in intraocular pressure for up to five hours. Limited clinical experience suggests that oral forskolin appears to offer some potential for sufferers of glaucoma.

Because untreated glaucoma can cause permanent vision loss, anyone experiencing this condition should be under the care of a physician and medical advice regarding therapeutic options should be followed.

Forskolin (coleus forskohlii) and Depression

Depression is believed to be associated with an imbalance of neurotransmitters in the brain, serotonin and dopamine primarily. Where there is a shortage of serotonin, the supplements 5-HTP or tryptophan or the SSRI drugs like prozac or Zoloft may be beneficial. If the catecholamine neurotransmitters (epinephrine, norephinephrine) are deficient the amino acids L-Phenylalanine or L-Tyrosine, or monoamine oxidase inhibitors like GeroVital (GH3) or Deprenyl may be helpful. Recent research has also been evaluating drugs that increase Cyclic AMP as a means of elevating the catecholamines. Since forskolin elevates Cyclic AMP, it may improve neurotransmitter function. It has been hypothesized that using forskolin to improve neurotransmitter levels may also be beneficial in the treatment of depression. Clinical trials using forskolin to treat depression have not been done.

Treatment of depression should be done under a physicians guidance.

Forskolin (coleus forskohlii) with Asthma and Allergies

Forskolin is a smooth muscle relaxer. The bronchioles in the respiratory tract are lined with smooth muscles. Therefore, forskolin may be able to relax these smooth muscles and improve bronchodilation, decreased airway resistance, increased vital capacity and increased forced expiratory volume. This could explain why forskolin has been used in folk medicine to treat asthma. This action is the result of the increase in Cyclic AMP caused by forskolin. Many asthma medications increase Cyclic AMP by inhibiting the enzymes that cause its breakdown. Thus, coleus and the traditional asthma drugs are likely to act synergistically. Therefore, one should consult their physician before combining them.

Forskolin (coleus forskohlii) and Weight Loss

In vitro (studies done in the lab as opposed to in living people) studies show that coleus stimulates fat metabolism. Researchers have found that many obese people have lower than normal Cyclic AMP production. Because of these considerations, coleus may, theoretically, be a weight loss agent, especially for those with reduced Cyclic AMP production. In a recent study, six overweight women took 25 mg of coleus (250 mg capsules of 10% standardized forskolin extract) twice daily for eight weeks. At the end of the eight-week trial, the participants lost a mean of ten pounds, and reduced their percentage of body fat by nearly 8%. Blood pressure levels also trended lower during the trial.

There has been a lot of hype in some media promoting the use of forskolin as a weight loss agent.

The truth is that there are no magic pills or potions that can, on their own, produce satisfactory and consistent weight loss. If one engages in diet, exercise and life style changes that can result in weight loss on their own, then one may improve their results by using forskolin and certain other supplements, in some cases.

Forskolin (coleus forskohlii) and Hypothyroidism

Forskolin has demonstrated the ability to increase thyroid hormone production and stimulate thyroid hormone release. This is likely because of forskolin's ability to increase Cyclic AMP levels. Forskolin alone should not be considered as a treatment for hypothyroidism or other thyroid conditions. For all thyroid conditions iodine nutrition should also be given particular attention.

Thyroid disorders are complex and should be evaluated by a health care professional. Treatment of thyroid disorders should be done under the care of a health care professional.

Forskolin (coleus forskohlii) and Cancer Metastases

Reserch has shown forskolin to be an inhibitor of tumor colonization in mice. This does not mean that it would be an effective therapy in humans, but it does raise the question.

Forskolin (coleus forskohlii) and Immune Enhancement

Forskolin appears to exhibit immune system enhancement by activating macrophages and lymphocytes.

Forskolin (coleus forskohlii) and Psoriasis

In psoriasis, cells divide about 1,000 times faster than normal. Coleus helps to alleviate psoriasis by normalizing the cAMP /cGMP ratio.

Cardiovascular Effects of Forskolin (coleus forskohlii)

Coleus forskohlii has been used in folk medicine to treat hypertension, congestive heart failure, and angina. Coleus's basic cardiovascular action is to lower blood pressure, while simultaneously increasing the contractility of the heart. This is believed to be due to forskolin's Cyclic AMP-elevating ability, which results in relaxation of the arteries, and increased force of contraction of the heart muscle. A preliminary trial found that coleus reduced blood pressure and improved heart function in people with cardiomyopathy. Coleus also increases cerebral blood flow, indicating that it may be beneficial in cerebral vascular insufficiency, and in enhancing post-stroke recovery. The platelet aggregation-inhibiting effects of coleus also adds to its value in cardiovascular disorders.

Drug Interactions with Forskolin (coleus forskohlii)

There is some evidence that forskolin may enhance the effects of beta-agonists such as albuterol. Forskolin may also act synergistically with epinephrine, ephedrine and pseudoephedrine. It is possible that the use of forskolin may decrease the needed dosages of beta-agonists. Anyone taking these drugs should consult their physician if they want to also use forskolin.

Because forskolin inhibits platelet aggregation and clotting, it may enhance the effects of anti-clotting medications such as warfarin, clopidogre, aspirin, enoxaparin, and dalteparin. Anyone taking any anti-clotting medications or supplements should consult their physician before adding forskolin to their regimen.

Forskolin (coleus forskohlii) Dosage

There is very limited information from clinical studies on the safe and effective dosages of forskolin. Based on the human studies for weight loss, 50 to 100 mg of forskolin taken in divided doses during the day appears to be an appropriate dose for the conditions discussed above.

Forskolin (coleus forskohlii) Supplements

Forskolin (coleus forskohlii) from the Life Extension Foundation

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Additional Information

Forskolin  PubMed references to recent research on Forskolin.

Glaucoma  Life Extension Protocols chapter on Glaucoma.

Depression  Life Extension Protocols chapter on Depression.

Asthma  Life Extension Protocols chapter on Asthma.

Allergies  Life Extension Protocols chapter on Allergies.

Weight Management  Life Extension Protocols chapter on Weight Management.

Hypothyroidism  Life Extension Protocols chapter on Hypothyroidism.

Cancer Adjuvant Therapy  Life Extension Protocols chapter on Cancer Adjuvant Therapy.

Psoriasis  Life Extension Protocols chapter on Psoriasis.

High Blood Pressure  Life Extension Protocols chapter on High Blood Pressurea.

Blood Clots  Life Extension Protocols chapter on Blood Clots.

Congestive Heart Failure  Life Extension Protocols chapter on Congestive Heart Failure.

Forskolin  Wikipedia Entry on Forskolin.

Forskolin References

Click to Expand References

(1) Ammon HP, Muller AB. Forskolin: From a ayurvedic remedy to a modern agent. Planta Med 1985;6:473-7.

(2) Caprioli J, Sears M, Bausher L, et al. Forskolin lowers intraocular pressure by reducing aqueous inflow. Invest Ophthalmol Vis Sci 1984;25:268-77.

(3) Burstein NL, Sears ML, Mead A. Aqueous flow in human eyes is reduced by forskolin, a potent adenylate cyclase activator. Exp Eye Res 1984;39:745-9.

(4) Brubaker RF, Carlson KH, Kullerstrand LJ, et al. Topical forskolin (colforsin) and aqueous flow in humans. Arch Ophthalmol 1987;105:637-41.

(5) Seto C, Eguchi S, Araie M, et al. Acute effects of topical forskolin on aqueous humor dynamics in man. Jpn J Ophthalmol 1986;30:238-44.

(6) Pescosolido N, Librando A. Oral administration of an asociation of forskolin, rutin and vitamins B1 and B2 potentiates the hypotonising effects of pharmacologic treatments in POAG patients. Clin Ter 2010;161(3):e81-5.

(7) Vetrugno M, Uva M, Russo V, et al. Oral administration of forskolin and rutin contributes to Intraocular Pressure Control in Primary Open Angle Glaucoma Patients Under Maximum Tolerated Medical Therapy. J ocul Pharmacol Ther 2012;28(5):536-41.

(8) Nebbioso M, Rusciano D, Pucci B, et al. Treatment of glaucomatous patients by means of food supplement to reduce the ocular discomfort: a double blind randomized trial. Eur Rev Med Pharmacol Sci 2013;17(8):1117-1122.

(9) Brubaker RF, Carlson KH, Kullerstrand LJ, et al. Topical forskolin (colforsin) and aqueous flow in humans. Arch Ophthalmol 1987;105:637-41.

(9) Agarwal KC, Zielinski BA, Maitra RS. Significance of plasma adenosine in the antiplatelet activity of forskolin: potentiation by dipyridamole and dilazep. Thromb Haemost 1989;61:106-10.

(10) Christenson JT, Thulesius O, Nazzal MM. The effect of forskolin on blood flow, platelet metabolism, aggregation and ATP release. Vasa 1995;24:56-61.

(9) Lindner E, Dohadwalla AN, Bhattacharya BK. Positive inotropic and blood pressure lowering activity of a diterpene derivative isolated from Coleus forskohli: Forskolin. Arzneimittelforschung 1978;28(2):284-289.

(10)Schlepper M, Thormann J, Mitrovic V. Cardiovascular effects of forskolin and phosphodiesterase-III inhibitors. Basic Res Cardiol 1989;84 Suppl 1:197-212.

(11) Lindner E, Metzger H. The action of forskolin on muscle cells is modified by hormones, calcium ions and calcium antagonists. Arzneimittelforschung 1983;33:1436-41.

(12) Kramer W, Thormann J, Kindler M, Schlepper M. Effects of forskolin on left ventricular function in dilated cardiomyopathy. Arzneimittelforschung 1987;37:364-7.

(13) Baumann G, Felix S, Sattelberger U, Klein G. Cardiovascular effects of forskolin (HL-362) in patients with idiopathic congestiv cardiomyopathy. A comparative study with dobutamine and sodium nitroprusside. J Cardiovasc Pharmacol 1990;16:93-100.

(14) Caprioli J, Sears M. Forskolin lowers intraocular pressure in rabbits, monkeys, and man. Lancet 1983;1:958-60.

(15) Seto C, Eguchi S, Araie M, et al. Acute effects of topical forskolin on aqueous humor dynamics in man. Jpn J Ophthalmol 1986;30:238-44.

(16) Meyer BH, Stulting AA, Muller FO, et al. The effects of forskolin eye drops on intra-ocular pressure. S Afr Med J 1987;71:570-1.

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