Hypericum perforatum

Latest Edit: Hector 2014-03-18 (EDT)

See Also	Botanical Monographs

St. John's Wort (Hypericum perforatum) is best known as a treatment for depression, yet it is also used in the treatment of pain, to help heal wounds, and for other traumas and injuries. To explore the characteristics, medicinal uses and prescribing considerations of this herb in more detail, check out the references indicated.,

Characteristics

• Common Names: St. John's wort, Millepertuis, Amber, Goatweed, Johnswort, Klamath weed, Tipton weed
• Family: Clusiaceae
• Habitat: Hypericum can be found in Europe, Western Asia, and Northern Africa
• Parts Used: Flower, aerial parts (90% alcohol)
• Constituents: anthraquinone derivatives (hypericin, isohypericin, protohypericin), flavonoids, prenylated phloroglucinols (hyperforin, adhyperforin)
• Medicinal Actions: alterative, antidepressant, vulnerary, analgesic, astringent, diuretic,

Uses

Historical Uses:

Hypericum perforatum has been used medicinally since the classical period. Hippocrates, Pliny, and Galen mention it in texts as being used for wound healing, pain, and as a diuretic. During the Renaissance and Victorian eras it was used for emotional and nervous complaints. Oil infused with St. John's wort can be applied topically and massaged into the tissue for muscle and nerve pain.

Medicinal Uses:

Internal

• Mental & Emotional Conditions

• depression, especially climacteric depression with anxiety and restlessness, mild to moderate depression (up to 4-6 weeks for effect, less effective in severe depression), neurotic depression, alcoholism, mania

• Trauma

• trauma such as spinal injury, shock, concussion, lacerations, puncture wounds with excruciating pain.

Article	Hypericum LIghts the Path Toward New Bladder Cancer Therapies, NDNR; 2012 November

• Other Conditions

• throbbing body without fever, frequent bed-wetting in older children and adults

Topically

• Digestive Conditions

• gastric ulcers (applied as oil to the skin, effect may be due to flavonoid content), inflamed colon (retention enema of warmed oil), inflamed hemorrhoids.

• Skin Conditions

• psoriasis, tattoo trauma, burns, myalgia (for the latter three, soothes skin and provides pain relief), varicose veins prone to leg ulcers (soothing pain relief, does not cure), cleans cuts and wounds from traumatic bruise/injury

Homeopathically this remedy is referred to as Hypericum.

Prescribing Considerations

The information provided is intended to augment the treatment from a naturopathic doctor or other trained medical professional. Although most herbs are generally safe, it is recommended that you avoid self-prescribing especially when there is an underlying ongoing medical condition, if you are on any prescription medications or if you are pregnant or breastfeeding.

Formulations and Preparation

• Tincture - 30 drops three times daily, then twice daily as it improves
• Fluid extract - 3-30 drops, normally 5-10 drops three times daily (0.5-1.0mL)
• Solid extract - 125-250mg solid extract (standardized to 0.3% hypericin content); 300-600mg daily after results are seen at 900-1200mg daily (in divided dose)
• Powder - 1-5g daily
• Tea - 1-2 tsp and boil briefly, 1 cup morning and night
• Oil internal - 1 Tbsp in the morning on an empty stomach or 1 tsp two to three times daily
• Oil topical - combine with linseed oil in psoriasis, tattoo trauma, burns, myalgia

Effect will be seen in 2-4 weeks; more than 3000 patients in 23 double-blind trials, 300-1000mg daily with a percentage taking hypericin

Safety

The safety and prescribing considerations for this herb include:,

• Generally regarded as safe.
• Side-effects may include photosensitivity, gastrointestinal upset and dizziness, sedation, and hypomania.
• Drug-Herb Interactions.

• In General - any drug that works at or via CYP3A4 or P-glycoprotein may be affected or interact with Hypericum.
• Alprazolam, Midazolam, and Related Triazolabenzodiazepines - Impaired drug absorption and bioavailability - Precautions Appropriate; These drugs are 3A4 substrates. St. John's wort (SJW) lowers bioavailability by inducing 3A4 enzyme production (interaction proved experimentally, no clinical reports, may be significant for IV midazolam preoperatively). Avoid.
• Amitriptyline and Related Tertiary Tricyclic Antidepressants - Impaired drug absorption and bioavailability - Avoidance Appropriate; These drugs are 3A4 and P-glycoprotein co-substrates. SJW lowers bioavailability (interaction proved experimentally, no clinical reports). Avoid.
• Anesthesia, General - Potential or theoretical adverse interaction of uncertain severity, interaction likely but uncertain occurrence and unclear implications; Potential pharmacokinetic and pharmacodynamic interactions with premedications and anesthetics (reports scarce). Cessation of SJW 1-2 weeks before procedure suggested. Disclosure essential.
• Antiretrovirals: Protease Inhibitors and Non-nucleoside Reverse Transcriptase Inhibitors - Minimal to mild adverse interaction - Vigilance Necessary, potentially harmful or serious adverse interaction - Avoid, impaired drug absorption and bioavailability - Precautions Appropriate; Most antiretroviral agents are 3A4 and P-glycoprotein co-substrates. Decreased bioavailability demonstrated (no clinical reports). Generally avoid. Co-administration requires specialist supervision and monitoring drug levels.
• Cyclosporine Immunosuppressive Agents - Potentially harmful or serious adverse interaction - Avoid, impaired drug absorption and bioavailability - Avoidance Necessary; Cyclosporine A is a co-substrate of 3A4 and P-glycoprotein. Decreased bioavailability demonstrated (numerous serious reports of graft rejection). Avoid.
• Digoxin, Digitoxin, and Related Glycosides - Potentially harmful or serious adverse interaction - Vigilance Necessary, impaired drug absorption and bioavailability - Precautions Appropriate; Drug is a P-glycoprotein substrate. Possible biphasic response, short-term increase, long-term decrease in bioavailability (isolated report of bigeminy, short term). If co-administration, ramp/taper the addition/cessation of SJW and monitor drug levels with vigilance during transition.
• Etoposide and Related Topoisomerase II Inhibitors - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Precautions Appropriate, Interaction likely but uncertain occurrence and unclear implications; Possible combination pharmacokinetic and pharmacodynamic interaction, decreased bioavailability (drug is 3A4 substrate) and interference with therapeutic action of hypericin blocking topo II inhibitors. Avoid.
• Fexofenadine, Histamine H1-receptor Antagonist Antihistamine - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Negligible Effect; Drug is P-glycoprotein substrate. Decreased bioavailability demonstrated (no clinical reports, minimal significance). Unlikely to cause problems.
• Imatinib, Tyrosine Kinase Inhibitors - Impaired drug absorption and bioavailability - Avoidance Appropriate; Gleevance is a 3A4 substrate. Decreased drug bioavailability demonstrated. Possible compromise to targeted anticancer therapy (no case reports). Avoid.
• Irinotecan, Camptothecin Analogs - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Avoidance Appropriate; Variable pharmacokinetic interaction probably. Camptothecin-11 responses subject to high inherent variability (significance unknown). Avoid.
• Omeprazole and Related Proton Pump Inhibitors - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Precautions Appropriate; Prilosec is a 3A4 and 2C19 substrate, SJW reduces bioavailability (experimentally demonstrated, no clinical reports, although large size of effect may be clinically significant). Avoid or monitor and increase dose of drug.
• Oral Contraceptives and Related estrogen-Containing and Synthetic estrogen and Progesterone Analog Medications - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Precaution Appropriate; Steroid hormones are 3A4 substrates. SJW increases breakthrough bleeding, may reduce OC compliance (OC failure not established despite theoretical risk). Avoid or adopt barrier methods during co-administration.
• Paclitaxel, Docetaxel: Taxane Microtubule-Stabilizing Agent - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Avoidance Necessary; Theoretically, induction of CYP3A4 and P-glycoprotein could influence drug disposition. Drug mostly eliminated via CYP2C8 (significance not established). Avoid.
• Paroxetine and Related Selective Serotonin Reuptake Inhibitor and Serotonin-Norepinephrine Reuptake Inhibitor (SSRI and SSRI/SNRI) Antidepressants and Nonselective Serotonin Reuptake Inhibitors (NSRIs) - Interaction likely but uncertain occurrence and unclear implications; SJW may lead to varying combined pharmacokinetic and pharmacodynamic interactions at least with some SSRI/NSRI drugs. Mild symptoms of serotonergic excess possible (several reports of varying reliability, significance not established). Avoid, except with professional monitoring during drug taper.
• Simvastatin and Related HMG-CoA Reductase Inhibitors (Statins) - Impaired drug absorption and bioavailability - Negligible Effect; Some older statins are co-substrates of 3A4 and P-glycoprotein (minimal significance, no reports available). Consider newer statins.
• Tacrolimus - Potentially harmful or serious adverse interaction - Avoid, impaired drug absorption and bioavailability - Avoidance Necessary; Cyclosporine A is a co-substrate of 3A4 and P-glycoprotein. Experimental evidence that tacrolimus is also a 3A4 substrate but no interaction reports for tacrolimus. Avoid.
• Verapamil and Related Calcium Channel Blockers - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Precautions Appropriate; Verapamil (and all calcium channel blockers) are 3A4 substrates. SJW induces intestinal 3A4 and increases drug clearance (no reports, interaction significance not established). Monitored co-adminstration unlikely to be problematic.
• Voriconazole and Related Triazole Antifungal Agents - Potential or theoretical adverse interaction of uncertain severity, impaired drug absorption and bioavailability - Precautions Appropriate; Drug is 3A4/2C19/2C9 substrate. SJW reduces bioavailability (experimentally demonstrated). Avoid.
• Warfarin and Oral Vitamin K Antagonist Anticoagulants - Mechanism not established. Possible pharmacokinetic effect, may lead to reduced INR (significance minimal to moderate, reliable clincial reports or trials unavailable). Unlikely to cause problems. If co-administerd, monitor INR once/twice weekly and titrate anticoagulant dosage when starting or stopping SJW therapy, until INR stablized.