Hydrastine
Also known as: Hydrastine, Benzylisoquinoline alkaloid
Overview
Hydrastine is an isoquinoline alkaloid primarily found in the root and rhizome of Goldenseal (Hydrastis canadensis L.), a herb native to North America. Traditionally used for its antimicrobial, anti-inflammatory, and antiseptic properties, hydrastine's effectiveness in treating infections and digestive issues has been recognized. It undergoes extensive phase I and phase II metabolism, involving multiple biotransformation pathways, which contributes to its pharmacokinetics. Although research has explored its metabolism, detailed studies evaluating its clinical efficacy and long-term safety are scarce, indicating the need for further investigation into its therapeutic applications.
Benefits
Evidence for the benefits of hydrastine is limited; however, Goldenseal extracts containing hydrastine have demonstrated antimicrobial activity against strains like methicillin-resistant Staphylococcus aureus (MRSA). While the anti-inflammatory properties of Goldenseal may also extend to hydrastine, specific effect sizes or clinical significance associated with hydrastine alone have not been thoroughly documented. Overall, Goldenseal has been recognized for its potential advantages in infection management, but the therapeutic effects of hydrastine remain inadequately characterized due to the absence of focused clinical trials.
How it works
Hydrastine is extensively metabolized in the body, primarily via reduction, O-demethylation, N-demethylation, hydroxylation, and glucuronidation processes. It interacts with liver enzymes, notably inhibiting CYP2D6 and CYP3A4/5, which can significantly influence the metabolism of other concurrently administered medications. Its antimicrobial activity is thought to arise from disrupting bacterial cell membranes or inhibiting bacterial enzymatic functions.
Side effects
The complete safety profile of hydrastine is not well defined, but high doses have been associated with liver toxicity, indicated by studies showing an increased incidence of hepatocellular adenomas and carcinomas in animal models. Specific common side effects (>5%) and rare side effects (<1%) remain unquantified. Due caution is warranted regarding potential interactions with CYP2D6 and CYP3A4/5, particularly with drugs metabolized by these pathways. Special populations, such as pregnant or breastfeeding women and individuals with liver conditions, should be particularly cautioned due to the risk of adverse effects. Long-term safety has not been well established.
Dosage
While there is no established minimum effective dose for hydrastine, doses in Goldenseal supplements typically include about 78 mg of hydrastine in a 2.7 g dose of Goldenseal. There is no maximum safe dose defined; however, high doses linked to liver toxicity in animal studies raise concerns about prolonged high-use scenarios. Absorption is rapid, with a peak serum concentration reached at approximately 1.5 hours post-administration. No specific timing or frequency guidelines are indicated, highlighting the need for caution in determining personal dosage.
FAQs
How long does it take to see effects?
Hydrastine is rapidly absorbed, with peak serum levels reached in about 1.5 hours, but documented clinical effects are minimal.
Is it safe for long-term use?
Long-term safety is questionable due to potential liver toxicity observed in animal studies.
Can it interact with other medications?
Yes, hydrastine can inhibit certain cytochrome P450 enzymes, which may alter the metabolism of other drugs.
What are the potential side effects?
Although specific side effects are not well-documented, liver toxicity at high doses is a concern.
Are there any contraindications?
Caution is recommended for pregnant or breastfeeding women and individuals with existing liver issues.
Research Sources
- https://pubmed.ncbi.nlm.nih.gov/25609220/ – This pharmacokinetic study involves 11 healthy subjects evaluating hydrastine absorption and metabolism, revealing rapid absorption with a Cmax of 225 ± 100 ng/mL, Tmax at 1.5 hours, and elimination half-life of about 4.8 hours.
- https://publications.iarc.fr/_publications/media/download/6703/f6ab6f33c673f0c0c896c684b06189b1c9b0ac57.pdf – An animal study assessing carcinogenicity demonstrates that high doses of Goldenseal root powder, which contains hydrastine, increased the rates of hepatocellular adenomas and carcinomas in test subjects.
- https://www.science.gov/topicpages/a/alkaloids+berberine+hydrastine – Research indicates Goldenseal extracts, containing hydrastine, exhibit potent antimicrobial activity against MRSA, attributed to numerous alkaloids and flavonoids present.
