Witch Hazel

Introduction Overview

Generic Name

Witch Hazel

Brand Name

Hamamelis virginiana L.

Dosage Form

Topical preparations (steam distillates, semisolid creams, ointments), Rectal suppositories

Drug Class

Topical astringent, herbal phytotherapeutic agent

Pharmacokinetics

Absorption

The pharmacokinetics of witch hazel are not well characterized due to its primary topical use. The key bioactive constituents such as tannins are poorly absorbed through intact skin, which limits systemic exposure and reduces potential internal toxicity when used topically. When applied topically as witch hazel water (a steam distillate), the lack of tannins implies minimal dermal absorption of polyphenols and other active phytochemicals. Absorption may vary depending on formulation, concentration, and skin integrity. Rectal suppositories allow localized absorption at anorectal mucosa, but systemic absorption is minimal and not well studied due to limited clinical data. Oral absorption is not recommended and carries risk of tannin-related toxicity. Due to topical application, witch hazel has a low risk of systemic toxicity secondary to low dermal penetration.

Distribution

Distribution parameters remain largely unstudied given the predominant topical applications of witch hazel preparations. The phytochemicals such as polyphenols (hamamelitannin, gallotannins) and flavonoids are theoretically capable of systemic distribution if absorbed, but since systemic absorption is minimal with topical use, plasma distribution is negligible in clinical practice. The hydrophilic nature of tannins and high molecular weight likely limit their penetration beyond skin barriers. Volatile oils present in minor quantities may, if absorbed, distribute via plasma to tissues but at levels insufficient to measure clinical effects. Local dermal distribution includes penetration to epidermis and dermis where anti-inflammatory and astringent effects occur.

Metabolism

Metabolic pathways of witch hazel’s active constituents are not comprehensively defined. Tannins such as hamamelitannin and proanthocyanidins may undergo hydrolysis and biotransformation by gut microflora upon oral intake; however, oral use is discouraged due to tannin toxicity. For topical and rectal use, local metabolism by skin or mucosal enzymes is possible but not well characterized. Polyphenolic components may be metabolized by phase II conjugation enzymes such as glucuronidation or sulfation if absorbed systemically, but clinical data are scarce. Overall, the metabolic fate remains largely theoretical due to limited systemic bioavailability and clinical pharmacokinetic studies.

Elimination

Elimination details for witch hazel constituents are poorly defined in literature, primarily due to minimal systemic absorption after topical application. If absorbed, elimination of polyphenols and flavonoids is likely via renal excretion of metabolites, similar to other plant polyphenols, and biliary excretion of conjugated metabolites may occur. The volatile oil constituents such as safrole and eugenol are metabolized hepatically and excreted renally but are only present in trace quantities. No comprehensive studies have characterized elimination half-life, clearance, or toxicokinetics in humans. The safety profile is governed largely by limited systemic exposure and rapid local metabolism and elimination.

Dosage Forms

Available Dosage Forms:
- Witch hazel water: Steam distillate aqueous preparation, used either undiluted or diluted (commonly 1:3 with water) for topical application.
- Semisolid preparations (creams and ointments) containing 5% to 10% crude Hamamelis extract.
- Rectal suppositories containing witch hazel extract in doses ranging from 0.1 g to 1 g per dose.

Dosages for Adults and Adolescents:
- Topical: Application of witch hazel water either undiluted or diluted for skin conditions, with frequency varying depending on indication and product; often applied 2-3 times daily to affected areas.
- Semisolid preparations (ointments/creams) applied topically at 5%-10% concentration. Specific regimen depends on clinical scenario and product labeling.
- Rectal suppositories: Administered as needed for anorectal conditions; typical dosage ranges from 0.1 to 1 g per dose.
- Oral administration is not recommended due to lack of safety data and potential tannin toxicity.

Specific Patient Populations:
- Pregnancy and Lactation: Safety and efficacy data are lacking; use only if benefits justify potential risks after consultation with healthcare provider.
- Pediatrics: Limited data available; topical use may be employed cautiously for diaper dermatitis or minor skin irritation, avoiding oral administration.
- Hepatic or Renal Impairment: No specific dosing adjustments established; systemic absorption is minimal with topical applications but caution warranted with rectal suppositories.
- Allergy-prone individuals: Avoid use if known sensitivity or allergy to witch hazel or related Compositae family plants due to risk of allergic contact dermatitis.

Mechanism Of Action

Witch hazel exerts its pharmacological effects primarily through its rich content of polyphenols, tannins (notably hamamelitannin), flavonoids, and volatile oils. The astringent properties are mainly attributed to tannins, which precipitate proteins on the skin surface, leading to vasoconstriction and reduced capillary permeability. This results in decreased edema, inflammation, and bleeding in affected tissues. The ability of tannins to bind to proteins also contributes to their hemostatic effect in local tissues.

At the cellular level, witch hazel extracts influence inflammatory pathways. Hamamelitannin and related polyphenols demonstrate inhibitory actions on pro-inflammatory cytokines such as tumor necrosis factor-alpha (TNF-α), reducing endothelial cell apoptosis and vascular inflammation. This anti-inflammatory activity provides symptomatic relief in skin inflammation and conditions like hemorrhoids by modulating immune responses and stabilizing capillary walls.

Additionally, witch hazel exhibits antioxidant properties by scavenging reactive oxygen species and peroxynitrite radicals, thereby protecting skin cells from oxidative stress and potential UV-induced damage. This antioxidant capacity supports its clinical usefulness in dermatologic anti-aging formulations and wound healing.

Comparative with similar plant-derived astringents and anti-inflammatory agents, witch hazel’s unique composition of polyphenolic compounds offers a broad spectrum of bioactivities, including antimicrobial (against gram-positive and some gram-negative bacteria) and mild antiviral actions. Clinical studies are limited but suggest potential for symptomatic treatment of minor skin irritations, inflammation, and anorectal disorders. Extensive traditional and ethnobotanical use corroborate its safety and efficacy when applied topically.

Pharmacological Actions

Topical astringent due to high tannin content causing protein precipitation and capillary constriction
Anti-inflammatory effects via inhibition of pro-inflammatory cytokines and reduction of endothelial cell apoptosis
Antioxidant activity through scavenging of reactive oxygen and nitrogen species protecting skin cells
Mild antimicrobial effects against gram-positive bacteria and some gram-negative pathogens in vitro
Hemostatic action facilitating control of local bleeding in skin and mucous membranes
Vasoconstrictive properties reducing skin erythema, edema, and suppuration in inflammatory lesions
Skin conditioning and protective effects promoting wound healing and barrier restoration
Mild antiviral activity demonstrated in herpes labialis clinical trial settings
Reduces capillary permeability, decreasing fluid exudation and skin irritation
Potential antitumor properties through modulation of cellular oxidative stress and inflammation
Relieves itching and irritation in dermatological conditions such as diaper dermatitis and eczema
Mucosal protective effects when formulated in rectal suppositories for anorectal disorders
Supports collagen and extracellular matrix integrity in skin fibroblasts
Exhibits immunomodulatory effects contributing to skin homeostasis and repair
Non-greasy topical application with cooling effects enhances patient tolerance and compliance

Therapeutic Or Clinical Uses

Topical symptomatic treatment of minor skin irritation and inflammation including diaper dermatitis
Management of hemorrhoids and anorectal discomfort via suppository formulations
Reduction of skin erythema following ultraviolet (UV) or chemical irritant exposure
Treatment of minor skin injuries and localized inflammation in pediatric patients
Adjunctive therapy in wound healing through antioxidant and anti-inflammatory effects
Management of perineal pain and discomfort following episiotomy or childbirth trauma
Topical use for pruritus and itching associated with various dermatologic conditions
Potential use in controlling mild purulent skin infections due to vasoconstrictive and antibacterial properties
Symptomatic relief in eczema and other inflammatory skin disorders, though clinical evidence is mixed
Traditional use in treatment of tumors, eye inflammations, tuberculosis, and fever (historical/ethnobotanical)
Incorporation into tattoo ink to prevent purpuric lesions in tattooed skin (exploratory use)
Use as a component in cosmetic formulations for skin toning and anti-aging
Supportive treatment to reduce bleeding and inflammation in superficial skin lesions
Topical antiseptic applications for minor cuts and abrasions
Mouthwash additive in dental plaque control, though less effective than standard agents

Side Or Adverse Effects

Allergic contact dermatitis with topical application, especially in sensitive individuals
Cross-sensitivity reactions in patients allergic to Compositae family plants (arnica, chamomile)
Nausea, vomiting, or constipation reported with oral ingestion of witch hazel extracts
Potential hepatic damage if tannins are absorbed in significant amounts systemically
Local skin irritation or burning sensation, particularly with undiluted preparations
Rare reports of sensitization reactions and hypersensitivity
Possible mild stinging when applied to broken or damaged skin surfaces
Adverse gastrointestinal effects following accidental ingestion of witch hazel preparations
Limited systemic toxicity due to negligible systemic absorption in topical use
Unknown long-term effects from chronic topical exposure; generally considered safe
Potential interactions with skin barrier leading to dryness if overused
Minimal phototoxic risk based on current data
No substantial evidence for severe anaphylactic reactions
No documented narcotic or addictive properties
Absence of significant CNS or cardiovascular adverse effects

Precautions

Avoid internal or oral use due to potential tannin toxicity and lack of safety data
Use with caution in patients with known allergies or sensitivities to witch hazel or related plants such as arnica and chamomile
Careful application on broken, damaged, or highly inflamed skin to prevent irritation
Avoid use in pregnancy and lactation unless benefits outweigh risks, as safety data are lacking
Not recommended for children under 2 years of age without medical supervision
Test for allergic sensitivity before widespread topical application, especially in atopic individuals
Avoid prolonged or excessive use to minimize risk of skin dryness or irritation
Consult healthcare professional before combining with other topical medications
Use cautiously in patients with hepatic impairment due to theoretical risk from tannin absorption
Discontinue treatment if signs of allergic reaction occur, such as rash or swelling
Avoid use in cases of known cross-reactivity to Compositae family plants
Avoid combining with strong irritants or sensitizers that may exacerbate skin reactions
Monitor for gastrointestinal symptoms if oral ingestion occurs accidentally
Do not apply near eyes or mucous membranes unless specifically formulated for such use
Store witch hazel preparations appropriately to maintain stability and prevent contamination

Warnings

Do not use witch hazel extracts internally (oral ingestion) due to potential toxicity of tannins
Allergic reactions, including contact dermatitis, can occur with topical use; discontinue if symptoms develop
Safety in pregnancy and breastfeeding has not been established; avoid use unless directed by a healthcare provider
Use in children under 2 years has not been sufficiently studied and is generally not recommended
Avoid contamination and improper dilution of witch hazel water which may lead to adverse skin reactions
Use cautiously with other topical agents to avoid unpredictable interactions or enhanced irritation
Avoid use on open wounds or mucous membranes unless product labeling indicates safety
Not recommended for treatment of serious infections or severe dermatologic conditions without medical supervision
Potential for skin sensitization mandates caution with repeated or prolonged applications
Not a substitute for medical treatment of systemic or severe dermatological diseases
Inform healthcare providers of witch hazel use prior to surgeries or medical procedures
Discontinue use if severe skin irritation, rash, or hypersensitivity occurs and seek medical advice
Avoid combining with other astringent or irritant products to prevent cumulative skin damage
Do not apply to skin areas with active eczema or severe dermatitis without medical consultation
Keep out of reach of children to prevent accidental ingestion and misuse

Contraindication

Internal or oral use of witch hazel extracts is contraindicated due to tannin-related toxicity
Known hypersensitivity or allergy to witch hazel or related Compositae plants such as arnica and chamomile
Use contraindicated in patients with history of allergic contact dermatitis to topical astringents containing witch hazel
Contraindicated in patients with severe skin ulcers, open wounds, or mucosal lesions unless specifically indicated
Avoid use in infants under 2 years of age without explicit medical guidance due to insufficient safety data
Contraindicated in pregnancy and lactation unless benefits clearly outweigh risks as per healthcare provider
Use contraindicated in individuals with hepatic impairment if systemic absorption suspected
Contraindicated in cases where medicinal preparations are contaminated or improperly formulated
Avoid use in individuals with active severe dermatological infections requiring systemic therapy
Avoid use when sensitivity testing reveals positive reaction to witch hazel components
Contraindicated on mucous membranes not specified safe for application
Not suitable for systemic treatment of malignancies or severe internal diseases
Contraindicated in cases with known intolerance to volatile oil constituents like safrole and eugenol
Contraindicated when combined with other irritant topical agents that exacerbate skin reactions
Avoid use in patients with bleeding disorders if rectal suppositories are employed without medical supervision

Drug Interactions

No well-documented drug interactions with witch hazel topical or rectal preparations
Possible additive skin irritation or sensitization when combined with other topical irritants or astringents
Unknown interactions with systemic medications due to minimal systemic absorption; caution advised
Potential cross-reactivity with Compositae family plant allergies could influence interaction risk with herbal products
No reported interactions with anticoagulants or antiplatelet agents but caution recommended when treating hemorrhoids
Concomitant use with corticosteroids might modify therapeutic response due to different mechanisms of action
No known interference with topical antiseptics, though clinical data are limited
No significant interaction with oral drugs due to topical usage; avoid oral administration to prevent adverse interactions
Concurrent use with other plant-derived polyphenols or antioxidants requires monitoring for additive effects
No documented interactions with cosmetic dermatologic treatments; however, clinical prudence suggested
No evidence of interference with immunosuppressant or immunomodulatory drugs
No reports of interactions with vaccines or antibiotics
Potential interaction with skin barrier repair agents unknown
Limited data on interaction with herbal supplements used concurrently
Recommend disclosing witch hazel use to healthcare professionals before starting new therapies

Preparations Of The Drug

Witch hazel water: A steam distilled aqueous extract from twigs and bark, available as a topical astringent and cooling agent
Fluid extracts: Concentrated liquid extracts obtained from Hamamelis virginiana leaves and bark for topical application
Semisolid formulations: Creams, ointments, and lotions containing 5% to 10% crude Hamamelis extract for dermatological use
Rectal suppositories: Containing 0.1 to 1 g of witch hazel extract, used in anorectal conditions like hemorrhoids
Topical wipes and pads impregnated with witch hazel water for convenience in treating skin irritation
Combination products: Witch hazel included with other herbal or pharmaceutical ingredients in topical formulations
Polyphenol-enriched collagen sponges incorporating witch hazel extracts for wound healing applications
Commercially marketed witch hazel toners and facial astringents for cosmetic and dermatological use
Homeopathic dilutions and tinctures, though distinct pharmacologically, are available in some markets
Gels and antiseptic creams with witch hazel for minor skin infections and inflammation
Powdered leaf and bark extracts for use in compounding or integrative medicine herbal preparations
Essential oil preparations containing trace amounts of safrole and eugenol derived from witch hazel
Dry leaf and twig materials sold for topical infusion or herbal tea preparations (not recommended for internal use)
Phytochemical standardization preparations quantifying hamamelitannin and proanthocyanidins for quality control
Over-the-counter topical products labeled as witch hazel topical astringents in various concentrations and formulations