Hypericum perforatum: Pharmacokinetic, Mechanism of Action, Tolerability, and Clinical Drug–Drug Interactions

  title={Hypericum perforatum: Pharmacokinetic, Mechanism of Action, Tolerability, and Clinical Drug–Drug Interactions},
  author={Emilio Russo and Francesca Scicchitano and Benjamin J. Whalley and Carmela Mazzitello and M. Lurdes F. Ciriaco and Stefania Esposito and Marinella Patan{\`e} and Roy Upton and Michela Pugliese and Serafina Chimirri and Maria Mamm{\`i} and Caterina Palleria and Giovambattista De Sarro},
  journal={Phytotherapy Research},
Hypericum perforatum (HP) belongs to the Hypericaceae family and is one of the oldest used and most extensively investigated medicinal herbs. The medicinal form comprises the leaves and flowering tops of which the primary ingredients of interest are naphthodianthrones, xanthones, flavonoids, phloroglucinols (e.g. hyperforin), and hypericin. Although several constituents elicit pharmacological effects that are consistent with HP's antidepressant activity, no single mechanism of action underlying… 

A current update on phytochemistry, pharmacology and herb–drug interactions of Hypericum perforatum

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Neuroprotective Activity of Hypericum perforatum and Its Major Components

It has been demonstrated that H. perforatum extracts and several of its major molecular components have the ability to protect against toxic insults, either directly, through neuroprotective mechanisms, or indirectly, through is antioxidant properties.

Role in depression of a multi-fractionated versus a conventional Hypericum perforatum extract.

A multi-fractionated hypericum extract has better clinical outcomes in subjects with depression without determining an increased risk of toxicity or reduced tolerability.

No effects of Hypericum-containing complex on dolutegravir plasma trough concentrations: a case report

Not surprisingly, the concomitant administration of a Hypericum-containing supplement in this HIV-infected patient had no significant effects on plasma drug trough concentrations.

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The review provides information on antidepressant, neuroprotective, nootropic, anxiolytic activity, antibacterial, cytotoxic, anti-inflammatory properties, analgesic, hypoglycaemic effects, and other effects of H. perforatum extracts, as well as its individual compounds.

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Hypericum Perforatum: A ‘Modern’ Herbal Antidepressant

Until now, the pharmacokinetic profile of the flavonoids in humans after oral administration of an alcoholic H. perforatum extract has been investigated in only one study, but more data are available for rutin and the aglycone quercetin after administration of pure substances or other flavonoid sources.

Herb–Drug Interactions with St John’s Wort (Hypericum perforatum): an Update on Clinical Observations

St John’s wort extracts, prepared from the aerial parts of Hypericum perforatum, contain numerous pharmacologically active ingredients, including naphthodianthrones, which are widely used for the treatment of mild-to-moderate depression.

A review of clinical and experimental observations about antidepressant actions and side effects produced by Hypericum perforatum extracts.

Some of the controversial evidence derived from clinical and experimental studies suggesting that H. perforatum exerts antidepressant-like actions are reviewed, and some of its side effects, such as nausea, rash, fatigue, restlessness, photosensitivity, acute neuropathy, and even episodes of mania and serotonergic syndrome when administered simultaneously with other antidepressant drugs are reviewed.

A review of the antibacterial activity of Hypericum perforatum L.

Hypericin and pseudohypericin: pharmacokinetics and effects on photosensitivity in humans.

Doses used in this study were higher than typical doses in current commercial preparations, frequency of side effects was equal to placebo medication and UV light sensitivity was not or only marginally increased, and there was no correlation between total hypericin plasma concentrations and photosensitivity.

Clinical herbal interactions with conventional drugs: from molecules to maladies.

Garlic has been shown to increase the clotting time and international normalized ratio of warfarin, cause hypoglycaemia when taken with chlorpropamide, and reduce the area under the plasma concentration-time curve (AUC) and maximum concentration of saquinavir in humans.

Antidepressant activity of hypericum perforatum and hyperforin: the neglected possibility.

The observations made during this study indicate that hyperforin is the major, but not the only antidepressive component of alcoholic extracts.

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Possible pharmacodynamic interactions with selective serotonin re-uptake inhibitors and serotonin (5-HT(1d)) receptor-agonists such as triptans used to treat migraine were identified and are associated with an increased risk of adverse reactions.

An update on clinical drug interactions with the herbal antidepressant St. John's wort.

This review highlights and updates the knowledge regarding drug interactions with SJW by a systematic review of all the available evidence, including worldwide published literature and spontaneous case reports.