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Protocols: St. John's Wort (Hypericum Perforatum)

Psychoactive

Antidepressant

Description:Bushy perennial plant with 2,400 year history of use for "nervous unrest" (Hippocrates).

Method of Action: Contains at least 10 constituents or groups of components including naphthodianthroms, flavinoids, xanthose, and bioflavinoids. Recent studies suggest it hyperforin is the primary active ingredient. Hypericum extracts show affinity for a variety of neurotransmitter receptors including: adenosine, GABA(a) and GABA(b), seritonin (5-HT - both 1a and 2a), central benzodiazepine, forskolin, inositol triphosphate, and the MAO A and B enzymes. Hypericin by itself has an affinity for the N-methyl-D-aspartate receptor. Additionally, earlier studies suggested that hypericum extracts exert an inhibitory effect on the enzymes of catecholamine metabolism, monoamine oxidase and catechol-o-methyltransferase. Primary method of action is probably not MAO-related. Evidence exists instead for inhibition of synaptosomal reuptake of serotonin, noradrenaline and dopamine and for down-regulation of B-adrenergic receptors and upregulation of 5-HT receptors.

Indications and Usage: In more than two dozen randomized placebo-controlled trials and 4 trails conducted against standard antidepressant drugs hypericum was found to have similar efficacy to standard antidepressant drugs for the treatment of Mild-Moderate Depression. Hypericum may also be useful in the treatment of Mild-Moderate Anxiety, Obsessive-Compulsive Disorder and other problems generally amenable to treatment with SSRI drugs. In double-blind study was found to be as effective as bright light therapy in treating Seasonal Affective Disorder. May be helpful in the treatment of Alcoholism and Benign Obesity. Hypericum is not effective for emergent or situational depression or anxiety. Oily hypericum preparations useful for dyspeptic complaints and external contused injuries, myalgia and first-degree burns.

Contraindications: Do not use this product if you are pregnant or lactating without first seeking advice from your physician. (Uterotonic activity has been reported in animal experiments.) Do not use while in direct sunlight for prolonged periods without skin protection. Potential for MAO inhibitor-like drug interactions. May inhibit absorption of iron and should not be used by persons in which this is contraindicated.

Dosage and Administration: 900 to 1,500 mg of dry extract (standardized to 0.3 percent hyperforin hypericin) daily taken with meals in three divided doses. Standard dose is 300 mg three time daily with meals. Begin with 300 mg at breakfast and lunch and increase as needed if no results in 14 days of continual administration. As with all serotonergic medications do not abruptly discontinue use and do not use in conjunction with other psychotropic medications without close medical supervision.

Clinical Effect In: 2 to 12 weeks depending on type and severity of condition. Average improvement of depressive symptoms is 70% after four weeks. Do not discontinue as ineffective until 12 weeks. Hypericins are absorbed within 2 hours with 14% to 21% systematically available. Plasma half-life is 24 hours allowing steady-state concentrations to be reached in 4 days. No data available on washout period for this drug.

Adverse Reactions: Serotonin syndrome can result from hypericum overdose, or combination with other SSRI and MAOI drugs. (Do not use this product without first reviewing our handout on serotonin syndrome.) Discontinue use if signs of mental or physical agitation appear. In 3.8 million patients only 32 reports of side effects were recorded. Occasionally: Agitation or restlessness (0.3%), mild GI distress (0.5%), allergic reactions (0.5%), photosensitivity (Increased sun protection is recommended only for persons with compromised immune systems or who are highly susceptible to burning). Rarely: dizziness, dry mouth, sedation, restlessness and mild constipation. Reported but possibly unrelated to drug: hyperaesthesia, dyspnoea, flushing, headache, hyperventilation, mydriasis, pain, palpitations, rhinitis, tremor, decreased cyclosporin levels. No CNS problems that would impair reaction time or coordination have been reported. No long-term studies but in long history of use no evidence of long-term side effects, carcinogenicity or mutingenicity. If you suspect that an herb or other supplement is making you sick, call the FDA's MedWatch hotline at 800-332-1088 or contact the agency via its website at http://www.fda.gov/medwatch.

Known Interactive Effects: Should not be used concurrently by persons taking photosensitizing agents (e.g. piroxicam, tetracycline hydrochloride), MAO Inhibitors or other antidepressant drugs without qualified medical supervision. No reports of drug-drug interactions other than potentiation of other serotonergic drugs (Wait 4 weeks after discontinuing MAO Inhibitor.) Should not be used in conjunction with another SSRI drug. (Slowly reduce current SSRI while gradually increasing Hypericum extract to 300 mg level.) Caffeine and theophylline, when taken with Hypericum may increase anxiety levels.

Additional Considerations: Because the mechanisms of action have not been delineated, standardization by hypericum content confers no guarantee of the pharmacologic equivalence of products. Potency of products varies widely even among those that are "standardized". Look for "research-grade, stabilized hyperforin-rich" extract from the flower portion of the plant (versus leaf or aerial plant parts). Hyperforin is unstable so it's potency is largely lost by the time you buy a St. John's Wort product. Vitamin World, Nature's Bounty, Nutrilite, and Nature's Way or LI160 (Jarsin 300) comparable products are currently receiving the best ratings by independent laboratories.

Warnings: The information above is provided for educational purposes and may not be construed as a medical prescription or as a substitute for the advice of your physician. Do not use this product without first consulting your physician especially if you are pregnant or lactating. Be advised that some herbs and dietary supplements can cause severe allergic reactions in some individuals and may also have an adverse result in conjunction with other medications, or treatments. You should regularly consult your physician in matters regarding your health and particularly in respect to symptoms and conditions, which may require diagnosis or medical attention. Reevaluate use of this product after 6 months.

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