Lycopus (Bugleweed / Water Horehound)

Lycopus (Bugleweed / Water Horehound)

Product Name: Зубчатка, Lycopus, Wolfstrapp, Licopos, Lycope, لوكيپوس, หญ้าปากควาย, Likop, Ликопус, Likopus, Ликоп, Ликопус, Лікопус, ליקופוס

Synonyms: Зубчатка обыкновенная, болотная мята, американская зубчатка / Bugleweed, Water Horehound / Wolfstrapp, Wasser-Hundskraut / Licopos, menta de lobo / Lycope, chanvre d'eau / اللوف المائي، النعناع البري / หญ้าปากควาย, ใบบัวบกน้ำ

Used Parts: herb, aerial part, leaves, stems, flowering shoots, inflorescences, roots, rhizomes, juice.

Main Indications for the Use of Lycopus: Thyrotoxicosis, subclinical hyperthyroidism, functional thyroid disorders, pre-climacteric syndrome, tachycardia, arterial hypertension, autonomic disorders, cardioneurosis, climacteric cardiac syndrome, anxiety disorder, menorrhagia, metrorrhagia, post-traumatic insomnia, thyroid hyperactivity in children, premenstrual syndrome with tachycardia, juvenile thyroid dysfunctions, functional ovarian cysts.

Use of Lycopus in Mixtures and Complexes: Chronic Hashimoto's thyroiditis, autoimmune thyroiditis, diffuse toxic goiter, hypertensive-type neurocirculatory dystonia, premenopausal syndrome with cardiovascular manifestations, insomnia in the elderly, psychosomatic disorders in women during hormonal changes, hypermenorrhea against the background of hormonal dysfunction, anxiety-depressive disorder combined with tachycardia, climacteric neurosis.

Pharmacological Properties of Lycopus: Thyrostatic, sedative, anxiolytic, anti-anxiety, cardiotonic, antiarrhythmic, vasodilatory, antihypertensive, hemostatic, antiandrogenic, hypoglycemic, anti-inflammatory, antioxidant, estrogen-like, diuretic, mild antitumor, hepatoprotective, neuroprotective, aromatase-inhibiting, phytohormonal, antidepressant, spasmolytic, antipyretic, analgesic, anticonvulsant, antibacterial, astringent, hypocholesterolemic.

Dosage of Pharmaceutical Forms — Lycopus

Powder — Lycopus

Indications (Powder): Thyrotoxicosis, subclinical hyperthyroidism, tachycardia, arterial hypertension, premenstrual syndrome with tachycardia, autonomic disorders, climacteric cardiac syndrome.

Standard Dosage (Powder): 0.5 grams of powder 2 times a day 30 minutes before meals, with warm water. Duration of intake — 21 days, then a 7-day break.

Enhanced Dosage (Powder): 0.8 grams 3 times a day for pronounced thyrotoxicosis, climacteric cardiac syndrome, and stage I arterial hypertension.

Maximum Dosage (Powder): No more than 1.2 grams 3 times a day for compensated forms of hyperthyroidism under medical supervision.

Preventive Dosage (Powder): 0.3 grams once a day in the morning, in courses of 14 days every 2 months. Recommended for a tendency to functional thyroid disorders in perimenopausal women and adolescents during hormonal changes.

Pediatric Dosage (Powder): From 12 years of age and with a body weight of 40 kg or more — 0.2 grams once a day in the morning. Not recommended for children under 12 years of age due to insufficient safety data.

Contraindications (Powder): Hypothyroidism, pregnancy, lactation. Safety data for use in children under 12 years of age are absent in the scientific literature.

Side Effects (Powder): With overdose, lethargy, slowed pulse, dizziness, and suppression of thyroid function are possible.

Adjustment for Patient Body Weight (Powder): For body weight less than 60 kg — reduce the dosage by 20%. For body weight over 90 kg — an increase in dosage by 25% is possible under medical supervision.

Preparation method (Powder): Collect fresh Lycopus europaeus herb during the active flowering period. Rinse under running water. Dry in the shade at a temperature not exceeding 35 °C until the stem is completely brittle. Grind in a mill to a powder state. Sift through a 0.5 mm sieve. For 100 g of powder, about 300 g of fresh raw material is required.

Storage Conditions and Shelf Life (Powder): Store in a dark, dry place at a temperature not exceeding 25 °C in an airtight glass or metal container with a tight lid. Protect from direct light and electromagnetic fields. Shelf life — 1 year. After opening, use within 2 months.

Dry Extract — Lycopus

Indications (Dry Extract): Thyrotoxicosis, subclinical hyperthyroidism, tachycardia, cardioneurosis, menorrhagia, premenstrual syndrome.

Standard Dosage (Dry Extract): 100 mg of dry extract 2 times a day, orally after meals, with warm water. Course — 21 days.

Enhanced Dosage (Dry Extract): 150 mg 3 times a day for severe manifestations of tachycardia, combined with anxiety disorders and menstrual cycle disorders.

Maximum Dosage (Dry Extract): Up to 200 mg 3 times a day under medical supervision for functional hyperthyroidism accompanied by arrhythmias.

Preventive Dosage (Dry Extract): 50 mg once a day, course 14 days quarterly. Recommended for women over 45 years of age with signs of hormonal imbalance and patients with autonomic lability.

Pediatric Dosage (Dry Extract): From 12 years of age and with a body weight of at least 40 kg — 50 mg once a day after meals. Safety in younger children has not been confirmed.

Contraindications (Dry Extract): Hypothyroidism, pregnancy, lactation, severe liver failure. Data on use in children under 12 years of age are absent.

Side Effects (Dry Extract): Headaches, decreased pulse, and suppression of thyroid function may occur with overdose.

Adjustment for Patient Body Weight (Dry Extract): For body weight less than 60 kg — reduce the dosage by 25%. For body weight over 90 kg — an increase to 125% is allowed under medical supervision.

Preparation method (Dry Extract): The aerial part of the plant collected during flowering is used. For 100 g of dry extract: 1 kg of dry herb, 2 liters of 70% ethanol. Infuse for 5 days at room temperature. Strain, evaporate at a temperature of 45 °C in a rotary evaporator to a paste state, then dry in a vacuum dryer at 40 °C. Grind the resulting dry residue.

Storage Conditions and Shelf Life (Dry Extract): Store in a tightly closed dark glass container in a dry, cool place (up to 20 °C), away from sources of light and heat. Shelf life — 2 years. After opening, use within 3 months.

Alcohol-Based Tincture — Lycopus

Indications (Tincture): Thyrotoxicosis, subclinical hyperthyroidism, tachycardia, anxiety disorder, climacteric syndrome, hypertensive-type autonomic dystonia, cardioneurosis, juvenile thyroid hyperactivity.

Standard Dosage (Tincture): 20 drops (about 1 ml) 2 times a day 30 minutes before meals, dissolving in 50 ml of water. Course — 21 days.

Enhanced Dosage (Tincture): 30 drops 3 times a day for pronounced tachycardia, panic attacks, and subclinical hyperthyroidism in adolescents and perimenopausal women.

Maximum Dosage (Tincture): Up to 40 drops 3 times a day for 10 days under medical supervision for functional thyrotoxic symptoms with pronounced tachycardia.

Preventive Dosage (Tincture): 15 drops once a day in the morning for 10 days every 2 months for autonomic lability in women after 45 years of age, with a tendency to hormonal imbalance, anxiety, and mild tachycardia.

Pediatric Dosage (Tincture): From 12 years of age and with a body weight of 40 kg or more — 10 drops once a day, dissolving in 100 ml of water. Not used in children under 12 years of age.

Contraindications (Tincture): Pregnancy, lactation, alcoholism, hypothyroidism, epilepsy, children under 12 years of age. Do not use in severe liver diseases.

Side Effects (Tincture): When the dosage is exceeded, drowsiness, bradycardia, arterial hypotension, and decreased concentration are possible.

Adjustment for Patient Body Weight (Tincture): Body weight < 60 kg — reduce the dosage by 25%. Body weight > 90 kg — an increase in dosage of up to 30% is possible under supervision.

Preparation method (Tincture): For 100 ml: dry bugleweed herb — 20 g, 70% ethanol — 100 ml. Pour alcohol over the raw material in a glass container, seal tightly. Infuse in a dark place for 10 days at a temperature of 20–25 °C, shaking daily. Strain, squeeze, filter through gauze and store in a tightly stoppered bottle.

Storage Conditions and Shelf Life (Tincture): Store in a cool, light-protected place at a temperature of 10–25 °C. Shelf life — 3 years. After opening, use within 6 months. Shielding from electromagnetic sources is desirable.

Oil Infusion — Lycopus

Indications (Oil Infusion): Climacteric syndrome with tachycardia, functional ovarian cysts, premenstrual syndrome, anxiety-depressive states with autonomic symptoms, mild arterial hypertension.

Standard Dosage (Oil Infusion): 1 teaspoon (5 ml) once a day orally during meals. Course — 30 days.

Enhanced Dosage (Oil Infusion): 1 teaspoon 2 times a day in the morning and evening for climacteric neuroses, chronic anxiety disorders with tachycardia, and menstrual cycle disorders.

Maximum Dosage (Oil Infusion): Up to 1 tablespoon (15 ml) 2 times a day for complex hormonal disorders and anxiety disorders, no more than 10 days in a row.

Preventive Dosage (Oil Infusion): 1 teaspoon every other day for 3 weeks. Indicated for women aged 45–55 with a tendency to dyshormonal disorders, as well as for emotional lability and moderate hypertension.

Pediatric Dosage (Oil Infusion): From 14 years of age and with a body weight of 45 kg or more — 2.5 ml (half a teaspoon) once a day during meals. Not recommended under 14 years of age due to lack of data.

Contraindications (Oil Infusion): Hypothyroidism, pregnancy, lactation, acute diseases of the liver and gallbladder, individual intolerance to the oil base.

Side Effects (Oil Infusion): Rarely — nausea, weakness, slowed pulse. With overdose — hypotension, sedative effect.

Adjustment for Patient Body Weight (Oil Infusion): Body weight < 60 kg — dose 4 ml. Body weight > 90 kg — up to 7 ml per dose, with good tolerability.

Preparation method (Oil Infusion): For 100 ml: dry bugleweed herb — 25 g, coconut oil (unrefined) — 100 ml. Grind the raw material, pour into a dry glass container. Pour with oil, heat in a water bath to 40 °C, keep for 2 hours, then infuse at room temperature for 7 days in a dark place. Strain, store in an airtight bottle.

Storage Conditions and Shelf Life (Oil Infusion): Store in a dark, cool place at a temperature not exceeding 20 °C. Shelf life — 6 months. After opening, use within 30 days. Protect from direct sunlight.

Vaginal Suppository — Lycopus

Indications (Vaginal Suppository): Dyshormonal bleeding, functional ovarian cysts, premenstrual syndrome, climacteric syndrome, initial stage endometriosis, hyperestrogenism, hormone-dependent autonomic destabilization.

Standard Dosage (Vaginal Suppository): 1 suppository at night, deep intravaginally. Course — 10 days, repeat if necessary after 3 weeks.

Enhanced Dosage (Vaginal Suppository): 1 suppository 2 times a day — morning and at night — for pronounced hormonal lability, functional cysts, and perimenopausal disorders.

Maximum Dosage (Vaginal Suppository): 2 suppositories per day (morning/evening) for 14 days, only under gynecological supervision, for intense manifestations of hormonal instability.

Preventive Dosage (Vaginal Suppository): 1 suppository once every 2 days, at night, course — 10 suppositories. Recommended for perimenopausal women with an unstable cycle and mild premenstrual symptoms.

Pediatric Dosage (Vaginal Suppository): Not used in persons under 18 years of age due to the lack of scientific data and potential hormonal activity.

Contraindications (Vaginal Suppository): Pregnancy, lactation, childhood and adolescence, individual hypersensitivity, pronounced hypothyroidism, acute inflammatory processes in the vagina.

Side Effects (Vaginal Suppository): Burning, itching, local irritation, increased vaginal discharge due to intolerance to the base. Very rarely — headache, weakness.

Adjustment for Patient Body Weight (Vaginal Suppository): Adjustment is not required; the form is applied locally.

Preparation method (Vaginal Suppository): For 10 suppositories: dry bugleweed extract — 1 g, cocoa butter — 18 g, coconut oil — 1 g. The base is melted in a water bath at a temperature of 38–40 °C, the extract is introduced, and the mass is mixed until homogeneous. Poured into vaginal molds of 2 g volume. Cooled until completely solidified.

Storage Conditions and Shelf Life (Vaginal Suppository): Store at a temperature of 2–8 °C in the original packaging, in a place protected from light. Shelf life — 6 months. After opening the blister, use within 5 days.

Rectal Suppository — Lycopus

Indications (Rectal Suppository): Autonomic dystonia with tachycardia, thyrotoxicosis, anxiety disorders, premenstrual syndrome, climacteric hot flashes, stage I arterial hypertension, insomnia.

Standard Dosage (Rectal Suppository): 1 suppository at night, deep into the rectum. Course — 10 days, then a 5-day break. Repeat if necessary.

Enhanced Dosage (Rectal Suppository): 1 suppository 2 times a day (morning/evening) for 7 days for pronounced anxiety with tachycardia, perimenopausal crises, and subclinical hyperthyroidism.

Maximum Dosage (Rectal Suppository): 2 suppositories per day, no more than 14 days in a row. Used strictly under specialist supervision for thyrotoxic crisis in the initial stage.

Preventive Dosage (Rectal Suppository): 1 suppository every other day at night, course 10 suppositories. Recommended for women over 45 years of age, patients with neurovegetative instability, and borderline hypertension.

Pediatric Dosage (Rectal Suppository): From 14 years of age with a body weight of 45 kg or more — 1/2 suppository (1 g) once every 2 days. Not recommended under 14 years of age due to the lack of scientific basis.

Contraindications (Rectal Suppository): Hemorrhoids in the acute stage, anal fissures, acute proctitis, pregnancy, lactation, pronounced hypothyroidism.

Side Effects (Rectal Suppository): Burning, discomfort in the rectum, false urges, extremely rarely — dizziness and decreased pressure with a long course.

Adjustment for Patient Body Weight (Rectal Suppository): Adjustment is not required for rectal administration, except for dosage in adolescents.

Preparation method (Rectal Suppository): For 10 suppositories: dry bugleweed extract — 1 g, cocoa butter — 18 g, coconut oil — 1 g. Melt the base at a temperature of 38–40 °C, add the extract, mix thoroughly. Pour into rectal molds of 2 g. Cool until completely solidified.

Storage Conditions and Shelf Life (Rectal Suppository): Store in the refrigerator at a temperature of 2–8 °C, away from direct light and moisture. Shelf life — 6 months. After opening the blister, use within 5 days.

Nasal Drops — Lycopus

Indications (Nasal Drops): Vasomotor rhinitis, hypertrophic rhinitis, autonomic lability of the nasolacrimal duct, allergic rhinitis, mild arterial hypertension with nasal congestion, anxiety states with impaired nasal breathing.

Standard Dosage (Nasal Drops): 2 drops in each nostril 3 times a day. Course — 7–10 days.

Enhanced Dosage (Nasal Drops): 3 drops in each nostril 4 times a day for pronounced congestion, vasomotor disorders, and persistent hypertrophic rhinitis.

Maximum Dosage (Nasal Drops): 4 drops in each nostril up to 5 times a day, no more than 5 days in a row, under ENT supervision.

Preventive Dosage (Nasal Drops): 1 drop in each nostril once a day at night for 7 days. Used in patients with seasonal allergies, during hormonal fluctuations with mild nasal mucosal hyperreactivity.

Pediatric Dosage (Nasal Drops): From 6 years — 1 drop 2 times a day, with a body weight of 20 kg or more. Not used under 6 years of age.

Contraindications (Nasal Drops): Acute sinusitis, nasal injuries, pronounced hypothyroidism, pregnancy, individual sensitivity to components.

Side Effects (Nasal Drops): Burning, sneezing, lacrimation, headache, rare decrease in pressure with frequent use.

Adjustment for Patient Body Weight (Nasal Drops): For body weight < 60 kg — reduce the number of drops to 1 in each nostril. For > 90 kg — 3 drops in each nostril are allowed.

Preparation method (Nasal Drops): For 100 ml: water-glycerin extract of bugleweed — 20 ml, distilled water — 70 ml, chamomile infusion — 10 ml. Mix all components, filter through sterile cloth, pour into bottles with a dispenser. The solution should be isotonic (if necessary, adjust with glycerin or 0.9% NaCl).

Storage Conditions and Shelf Life (Nasal Drops): Store in the refrigerator at a temperature of 4–8 °C, in the original airtight packaging, protected from light. Shelf life — 30 days. After opening — no more than 10 days.

Ear Drops — Lycopus

Indications (Ear Drops): Chronic catarrhal otitis, irritability of the auditory nerve in autonomic dystonia, tinnitus against the background of menopause, hypertensive vascular instability of the inner ear.

Standard Dosage (Ear Drops): 2 drops in each ear canal 2 times a day. Course — 5–7 days.

Enhanced Dosage (Ear Drops): 3 drops 3 times a day for pronounced tinnitus and irritation of the auditory nerve against the background of hormonal dysfunction.

Maximum Dosage (Ear Drops): Up to 4 drops 3 times a day, no more than 5 days in a row. Use strictly under specialist supervision.

Preventive Dosage (Ear Drops): 1 drop in each ear canal once a day before bedtime. Prophylactically — 5 days monthly for seasonal autonomic lability in women after 45 years of age.

Pediatric Dosage (Ear Drops): From 7 years — 1 drop 2 times a day with a body weight of 25 kg or more. Do not use in children under 7 years of age.

Contraindications (Ear Drops): Purulent otitis, perforation of the eardrum, pregnancy, pronounced hypothyroidism, individual intolerance.

Side Effects (Ear Drops): Feeling of congestion, burning, headache with overdose or sensitivity.

Adjustment for Patient Body Weight (Ear Drops): Patients up to 60 kg — no more than 2 drops per dose. Over 90 kg — 4 drops are allowed.

Preparation method (Ear Drops): For 100 ml: bugleweed extract in coconut oil — 30 ml, jojoba oil — 30 ml, chamomile oil — 10 ml, vitamin E — 0.5 ml, the rest — purified sesame oil. Mix all components at a temperature not exceeding 35 °C, settle for 24 hours, filter and pour into sterile dropper bottles.

Storage Conditions and Shelf Life (Ear Drops): Store in a dark, cool place at a temperature of up to 20 °C. After opening, use within 14 days. Shelf life — up to 3 months.

Ointment — Lycopus

Indications (Ointment): Vegetovascular disorders with a hypertensive component, climacteric syndrome with hot flashes, anxiety with cutaneous vegetative reaction (goosebumps, redness), mild arterial hypertension, functional cardiac pain, premenstrual pain syndrome.

Standard Dosage (Ointment): Apply 1–2 times a day in a thin layer to the skin of the upper chest, neck, and temples. Course — from 7 to 14 days.

Enhanced Dosage (Ointment): Apply up to 3 times a day for pronounced hypertensive lability, vascular crises, and vegetative instability in perimenopause.

Maximum Dosage (Ointment): Apply up to 4 times a day on limited skin areas (no more than 10% of the body surface), no longer than 5 days in a row. Under medical supervision.

Preventive Dosage (Ointment): Apply once a day before bedtime to the neck and solar plexus area. Course — 10 days, repeat once a month for a tendency to anxiety, hormonal fluctuations, and mild vascular dystonia.

Pediatric Dosage (Ointment): From 10 years, with a body weight of 30 kg or more — apply once a day to the skin of the chest or neck. Use under 10 years of age is not recommended.

Contraindications (Ointment): Violation of skin integrity, eczema, pregnancy, individual intolerance, age under 10 years.

Side Effects (Ointment): Rarely — local irritation, itching, redness. With prolonged use, dry skin is possible.

Adjustment for Patient Body Weight (Ointment): Patients with body weight less than 60 kg — apply a minimal amount (pea-sized). For weight over 90 kg, a moderate increase in the area of application is allowed.

Preparation method (Ointment): For 100 g: dry bugleweed extract — 5 g, coconut oil — 30 g, beeswax — 10 g, shea butter — 25 g, jojoba oil — 20 g, vitamin E — 0.5 g, lavender essential oil — 0.5 g. In a water bath at a temperature of 40 °C, melt the oils and wax, add the extract, mix thoroughly, add vitamin E and essential oil, pour into sterile jars. Cool at room temperature.

Storage Conditions and Shelf Life (Ointment): Store in a tightly closed container in a cool place at a temperature of up to 20 °C, in a cabinet protected from light and moisture. Shelf life — up to 6 months. After opening — no more than 30 days.

Cream — Lycopus

Indications (Cream): Hormone-dependent skin reactions in anxiety states, skin irritation against the background of climacteric changes, seborrheic dermatitis with a vascular component, vascular hyperreactivity of the facial skin, estrogen-dependent skin dryness.

Standard Dosage (Cream): Apply 1–2 times a day in a thin layer to affected skin areas or zones of vascular hyperactivity (face, neck, chest).

Enhanced Dosage (Cream): 3 times a day for 5 days for pronounced vascular skin reactions and irritation.

Maximum Dosage (Cream): Up to 4 times a day on limited skin areas. Do not use more than 7 days in a row on the same area.

Preventive Dosage (Cream): Once a day for 10 days during seasons of hormonal changes, premenstrual syndrome, and in women over 45 years of age.

Pediatric Dosage (Cream): From 12 years — apply once a day on limited skin areas for hyperreactivity, itching, or redness. Under 12 years — not recommended.

Contraindications (Cream): Active dermatoses, weeping skin areas, pregnancy, hypothyroidism, age under 12 years.

Side Effects (Cream): Rarely — tingling, itching, flaking, especially in sensitive skin.

Adjustment for Patient Body Weight (Cream): For weight less than 60 kg — use a reduced amount of cream, especially on the face. For weight over 90 kg — an increase to 1.5 times the volume of application is allowed.

Preparation method (Cream): For 100 g: aqueous bugleweed extract — 10 g, coconut oil — 20 g, grape seed oil — 20 g, lavender hydrolate — 30 g, emulsifier (cetearyl glucoside) — 5 g, glycerin — 10 g, preservative (rosemary extract) — 0.5 g, vitamin E — 0.5 g. Emulsify at a temperature of 40–45 °C with constant stirring until a homogeneous texture is obtained. Pour into sterile tubes.

Storage Conditions and Shelf Life (Cream): Store at a temperature of 4–10 °C in a tightly closed package, away from sunlight. Shelf life — 3 months. After opening — use within 21 days.

Cosmetic Serum — Lycopus

Indications (Cosmetic Serum): Vascular hyperreactivity of the skin, initial stage rosacea, hormone-dependent redness and irritation of the facial skin in perimenopause, seborrheic skin sensitivity, estrogen-deficient skin dryness, stress-induced vascular instability of the epidermis.

Standard Dosage (Cosmetic Serum): Apply 1–2 drops of serum once a day in the evening to cleansed facial and neck skin. Course — 14–21 days.

Enhanced Dosage (Cosmetic Serum): 2–3 drops 2 times a day (morning and evening) for pronounced vascular hyperreactivity, stage I rosacea, and climacteric hot flashes with facial redness.

Maximum Dosage (Cosmetic Serum): Up to 4 drops 2 times a day, no longer than 10 days in a row for pronounced estrogen-dependent skin changes. Only under cosmetologist supervision.

Preventive Dosage (Cosmetic Serum): 1 drop per day in the evening, in 10-day courses once a month. Recommended for women over 45 years of age with sensitive skin prone to redness against the background of hormonal changes.

Pediatric Dosage (Cosmetic Serum): Not used under 16 years of age. In adolescent vascular sensitivity — local spot application (1 drop) is allowed no more than once every 2 days under specialist supervision.

Contraindications (Cosmetic Serum): Pregnancy, active forms of acne, pustular rashes, allergy to essential oils or serum components, age under 16 years.

Side Effects (Cosmetic Serum): Local irritation, tingling, skin hyperemia with increased individual sensitivity. With overdose — flaking and increased photosensitivity.

Adjustment for Patient Body Weight (Cosmetic Serum): Not required — the form is intended exclusively for local use.

Preparation method (Cosmetic Serum): For 100 ml: water-glycerin bugleweed extract — 10 ml, cornflower hydrolate — 30 ml, 1% hyaluronic acid — 5 ml, vegetable glycerin — 10 ml, Centella asiatica extract — 10 ml, blackcurrant seed oil — 5 ml, vitamin B3 (niacinamide) — 2 g, lavender essential oil — 0.3 ml, plant-derived preservative — 0.5 ml, distilled water — up to 100 ml. Mix at a temperature of 30 °C, filter through a 0.22 µm microfilter, pour into dark bottles with a pipette.

Storage Conditions and Shelf Life (Cosmetic Serum): Store at a temperature of 4–8 °C, in a tightly closed dark glass bottle, away from light, heat, and EMI. Shelf life — up to 90 days. After opening — use within 21 days.

Toxicity and Biosafety of Lycopus

Experimental studies on the toxicological characteristics of Lycopus europaeus have shown extremely low acute toxicity. In preclinical animal trials, aqueous extract of bugleweed herb upon oral administration at doses up to 5000 mg/kg body weight did not cause lethal outcomes and did not provoke signs of intoxication, which allows it to be classified as class IV low-toxicity substances (according to WHO classification).

Data on the LD₅₀ value for dry extract or alcoholic tinctures of bugleweed also indicate a high safety threshold. In rat studies, the LD₅₀ exceeded 3000 mg/kg orally, with only a slight decrease in motor activity and sedation observed without organ damage. No cumulative effect was detected with prolonged use in therapeutic doses.

In cytotoxicity studies of aqueous and alcoholic extracts of Lycopus on fibroblast and keratinocyte cultures, no cytopathic effect was observed at concentrations equivalent to therapeutic ones. Endotoxic activity, mutagenicity, and carcinogenicity in in vitro and in vivo tests have not been established.

Reference: https://www.ncbi.nlm.nih.gov/p...

Pharmacodynamics — Lycopus

The pharmacodynamic properties of Lycopus, mainly studied on the basis of Lycopus europaeus and Lycopus virginicus, are manifested in a complex effect on the endocrine, cardiovascular, and central nervous systems. The most characteristic effect is the modulation of thyroid function through an effect on thyroid activity. In vitro and in vivo studies demonstrate inhibition of thyroid peroxidase activity and suppression of thyroxine secretion, which is explained by the presence of phenolic carboxylic acids and lithospermic acid derivatives.

The effect on the cardiovascular system is realized through vasodilatory and hyposympathetic effects, which leads to a decrease in heart rate, vascular tone, and total peripheral resistance. It has been established that aqueous and alcoholic extracts of Lycopus have negative chrono- and bathmotropic effects, associated with an effect on β-adrenoceptors and a decrease in catecholamine activity. The mechanism may be related to inhibition of the activity of the enzyme adenylate cyclase, which mediates the response to norepinephrine.

At the level of the central nervous system, sedative and anxiolytic effects have been proven. The complex of flavonoids and terpenoids of bugleweed has a regulatory effect on the GABAergic system. In particular, modulation of GABA receptor activity and an increase in the level of gamma-aminobutyric acid in brain structures have been identified. This explains the observed decrease in motor activity, reduction in stress response, and normalization of autonomic tone.

At the molecular level, antioxidant activity is observed, realized through suppression of lipid peroxidation, inactivation of free radicals, and an increase in the activity of superoxide dismutase and catalase enzymes. The plant also demonstrates a mild inhibitory effect on aromatase, which makes possible its participation in the regulation of sex hormone levels in women. Polyphenols are present in bugleweed extracts, which interact with the receptor systems of skin and vascular cells, causing a decrease in capillary reactivity and modulation of local inflammatory processes. This determines both the systemic and local action of the drug when using transdermal forms.

Thus, the pharmacodynamic profile of bugleweed is characterized by thyrostatic, sedative, vasodilatory, antioxidant, and receptor-modulating effects, realized at the systemic and local levels through neuroendocrine, vegetative, and humoral mechanisms.

References:
https://www.ncbi.nlm.nih.gov/p...
https://www.sciencedirect.com/...
https://pubmed.ncbi.nlm.nih.go...

Pharmacokinetics — Lycopus

Data on the pharmacokinetics of Lycopus as a holistic plant taxon are limited; however, one can rely on the generalized characteristics of the main components and routes of administration. Upon oral intake of aqueous or alcoholic extracts, the main active substances — polyphenols, hydroxycinnamic acids, flavonoids, and terpenoids — undergo rapid absorption in the upper parts of the small intestine. Glycerin-alcohol extracts demonstrate moderate bioavailability upon oral administration, which increases with fractional dosing. Phenolic compounds and lithospermic acid derivatives are actively metabolized in the liver with the participation of microsomal oxidation enzymes. Some flavonoids may interact with the intestinal microflora, undergoing enzymatic hydrolysis with the formation of aglycones, which affects further absorption and metabolism.

Terpenoids upon transdermal and rectal administration show slow absorption, passing through the lymphatic pathways, bypassing primary hepatic metabolism. With external use (ointment, cream, serum), absorption depends on the lipophilicity of the base and the state of the skin barrier. Entry into the systemic circulation is limited; the effect is predominantly local. However, with prolonged use on large areas, accumulation of individual components in the lipid layers of the dermis and subcutaneous tissue is possible.

Distribution of active substances after systemic absorption occurs mainly in highly perfused organs: the liver, kidneys, lungs, and thyroid gland. Flavonoids have the ability to penetrate the blood-brain barrier, explaining the central sedative effects.

The main routes of excretion are renal and intestinal. Conjugated forms of polyphenol metabolites are excreted in the urine, while products of microbial metabolism are excreted in the bile. Some volatile components (in the case of inhalation or transdermal routes) may be excreted through the lungs. Thus, the pharmacokinetics of Lycopus is determined by a combination of polyphenolic and lipophilic substances that undergo hepatic transformation, partially interact with the microflora, and are excreted through the urinary and hepatobiliary systems.

References:
https://link.springer.com/arti...
https://www.sciencedirect.com/...
https://www.ncbi.nlm.nih.gov/p...

Mechanisms of Action and Scientific Rationale — Lycopus

The pharmacological effects of Lycopus, in particular the species Lycopus europaeus and Lycopus virginicus, are realized through multiple targets, mainly due to phenolic compounds, lithospermic acid, and polyphenolic complexes. One of the key mechanisms of action is the inhibition of the enzyme thyroid peroxidase (TPO), which is involved in the synthesis of thyroid hormones, accompanied by a decrease in the levels of thyroxine and triiodothyronine. In vitro studies have shown that lithospermic acid suppresses TPO activity by blocking the iodination of tyrosine residues of thyroglobulin, which reduces the hormonal output of the thyroid gland.

The plant also has an effect on β-adrenoceptors, exhibiting β-blocking activity, which is realized through a decrease in sensitivity to catecholamines and a decrease in sympathetic stimulation. This effect is mediated by a decrease in adenylate cyclase activity and a decrease in the level of cAMP in myocardial and vascular endothelial cells, which leads to vasodilation and a moderate negative chronotropic effect.

Flavonoids and polyphenols of Lycopus participate in the regulation of cyclooxygenase (COX) and lipoxygenase (LOX) enzyme activity, thereby suppressing the synthesis of pro-inflammatory prostaglandins and leukotrienes. These same compounds stabilize cell membranes, inhibit the release of cytokines (TNF-α, IL-6), and inhibit the activation of the transcription factor NF-κB, which explains the anti-inflammatory and immunomodulatory potential.

At the level of the central nervous system, an effect on GABAergic pathways has been found. Lycopus flavonoids are able to modulate the activity of GABA-A receptors, increasing their sensitivity to endogenous gamma-aminobutyric acid, which provides a sedative and anxiolytic effect. Along with this, an inhibitory effect on acetylcholinesterase (AChE) activity has been noted, which potentially contributes to a neuromodulatory and cognitive-stabilizing effect.

A number of studies demonstrate the ability of Lycopus components to inhibit aromatase, an enzyme responsible for the conversion of androgens to estrogens, which is significant within the framework of hormonal balance and correction of hyperestrogenic conditions. Suppression of caspase-3 expression and inhibition of apoptosis of vascular endothelial cells have also been recorded, which additionally supports the vascular-protective action. The combined effect is realized at the systemic level (neuroendocrine regulation), tissue level (endothelium, myocardium, skin), and cellular level (neurons, thyrocytes, immune cells). Confirmed targets of action are: thyroid peroxidase, β-adrenoceptors, COX-2, NF-κB, AChE, aromatase, GABA receptors, cytokine receptors (IL-6R, TNFR), endothelial cells, and neutrophils.

References:
https://pubmed.ncbi.nlm.nih.go...
https://www.sciencedirect.com/...
https://www.ncbi.nlm.nih.gov/p...
https://link.springer.com/arti...

Synergy — Lycopus

Pharmacological synergy of Lycopus has been confirmed in combination with plants containing sedative, thyromodulating, and vasoactive components. In particular, potentiation of sedative and anxiolytic action has been noted when used together with Melissa officinalis (lemon balm). The complex of flavonoids and terpenoids of both plants demonstrates a modulating effect on GABA receptors and additive suppression of acetylcholinesterase activity, enhancing the neurosedative effect on the central nervous system.

In combination with Leonurus cardiaca (motherwort), potentiation of β-blocking and vasorelaxant action is observed, due to the combined blockade of β-adrenoceptors and an additive effect on reducing catecholamine levels in plasma. This interaction is realized at the level of the vascular endothelium and cardiac muscle and is systemic in nature.

Modulating synergy with Salvia officinalis (sage) is manifested in the correction of thyroid activity, which is associated with the combined suppression of thyroid enzyme systems, including thyroid peroxidase, as well as an effect on the TRH/TSH cascade receptors. This effect has a tissue-specific action at the level of the thyroid gland.

An additive antioxidant effect is observed when Lycopus is combined with Camellia sinensis (green tea), where the polyphenolic complexes of both taxa suppress lipid peroxidation, enhance superoxide dismutase activity, and reduce oxidative stress at the level of cell membranes.

Synergy with plants containing phytoestrogens (for example, Trifolium pratense) has a hormone-regulating nature, based on interaction with aromatase and estrogen receptors. The mechanism is the combined inhibition of enzymatic conversion of androgens and balancing of sex steroid levels.

References:
https://www.ncbi.nlm.nih.gov/p...
https://pubmed.ncbi.nlm.nih.go...
https://www.sciencedirect.com/...
https://link.springer.com/arti...

Geography of Use and Traditional Medicine — Lycopus

Lycopus has traditionally been used in the folk medicine of Europe, North America, and to a lesser extent — East Asia. The greatest ethnobotanical activity is associated with the species Lycopus europaeus and Lycopus virginicus. In the European tradition, especially among Germanic, Slavic, and Celtic peoples, the plant was known as a remedy with the ability to "calm the blood and heart." It was used in the form of aqueous infusions and decoctions of the herb, both internally and externally — for compresses on the chest and neck area. In Central Europe, including Poland, the Czech Republic, and Germany, Lycopus was used in village herbal medicine as a "heart herb" and as part of mixtures for "anxiety," "mental overload," and "thyroid diseases."

In Slavic folk healing, bugleweed was used as a ritual plant in ceremonies for purification from the evil eye, and its smoke was used for fumigating houses on the days of the summer solstice. There were beliefs that the plant "wards off evil forces," especially if it was picked on Ivan Kupala Day before sunrise. In Lithuania and the Russian North, the plant was part of wreaths and amulets worn by women during transitional ages.

In the culture of the indigenous peoples of the eastern part of North America, especially among the Cherokee and Iroquois, Lycopus virginicus was considered a "women's herb" and was used for "cooling the heart" and soothing the spirit. Native American herbalists used infusions and warm poultices of the leaves in traditional cleansing rituals and for seasonal fatigue. The juice of the fresh plant was added to smoking mixtures together with sage and St. John's wort, giving them a calming effect.

In the territory of China and Korea, the plant is rare and does not have widespread use in traditional medicine systems. However, in some Taoist practices, it is mentioned as a "herb of silence," used in mixtures for meditation and as a talisman against outbursts of anger.

Archaeoethnobotanical finds from the Rhine region (Germany) confirm the presence of remains of Lycopus europaeus in sites of Bronze Age tribes, which may indicate its early use for cult or health purposes. Thus, Lycopus has a centuries-old history of use in European, North American, and partially Asian ethnic traditions as a plant associated with harmonization, purification, feminine strength, and inner calm. Its ritual, medical, and symbolic significance varied depending on the cultural context, but everywhere it was accompanied by use in infusions, fumigations, wearing in wreaths, and inclusion in ceremonial collections.