Rhamnus cathartica (Common Buckthorn)

Rhamnus cathartica (Common Buckthorn)

Product Name: Крушина слабительная, Rhamnus cathartica, Kreuzdorn, Espino cerval de mar, Nerprun cathartique, النبق الشائع, พระเจ้าห้าพระองค์, Jiyda daraxti, Карагайды, Qarağac, Себарга, Šaltalankis, Smiltsērkšķis, Крушина проносна, כרונוס קתרטיקה

Synonyms: крушина обыкновенная, крушина пургавая, buckthorn, European buckthorn, common buckthorn, Purgier-Kreuzdorn, Espino negro, Nerprun purgatif, النبق الأوروبي, สมุนไพรระบาย, народные: сорная слива, волчья ягода

Parts Used: bark, fruits, leaves, branches, seeds, juice.

Main Indications for Use of Rhamnus cathartica: Chronic atonic constipation, constipation in hemorrhoids, constipation after rectal surgery, irritable bowel syndrome with constipation, colonic dyskinesia of the hypomotor type, proctogenic constipation, paralytic intestinal obstruction as part of symptomatic treatment.

Use of Rhamnus cathartica in Mixtures and Complexes: Chronic gastritis with hyposecretion, flatulence, atopic conditions of the digestive tract, constipation against the background of diabetes mellitus, chronic pancreatitis outside exacerbation, hypocholesterolemic disease.

Pharmacological Properties of Rhamnus cathartica: laxative, choleretic, antiseptic, moderately spasmolytic, irritating, anthelmintic, stimulating intestinal peristalsis, mildly cleansing, phytoncidal, moderately diuretic.

Dosage of Pharmaceutical Forms — Rhamnus cathartica

Powder — Rhamnus cathartica

Indications (Powder): Chronic atonic constipation, proctogenic constipation, irritable bowel syndrome with constipation, colonic dyskinesia of the hypomotor type, paralytic intestinal obstruction as part of symptomatic treatment.

Standard Dosage (Powder): 1 g of powder once daily at night, washed down with warm water. The effect is observed after 8–10 hours.

Enhanced Dosage (Powder): 2 g of powder once before bedtime for persistent atonic constipation, incomplete intestinal evacuation, and a tendency to prolonged stool retention of more than 72 hours.

Maximum Dosage (Powder): 3 g of powder once for severe persistent constipation caused by hypomotor colonic dyskinesia or in cases of bowel preparation before endoscopic examination.

Preventive Dosage (Powder): 0.5 g of powder every other day before bedtime for chronic colostasis, irritable bowel syndrome in remission, for patients with a sedentary lifestyle, and after surgery on the pelvic organs. Duration of intake — no more than 14 days, repeat the course no earlier than after 3 weeks.

Pediatric Dosage (Powder): From 12 years of age, with a body weight from 40 kg — 0.5 g of powder before bedtime, no more than once every 2 days. For younger children, not recommended due to insufficient knowledge of the toxicity of anthraquinone glycosides.

Contraindications (Powder): Ulcerative colitis, Crohn's disease, acute inflammatory bowel diseases, intestinal obstruction, hypersensitivity to anthraquinone glycosides. Data on contraindications during pregnancy, lactation, and in childhood under 12 years of age have not been scientifically registered.

Side Effects (Powder): Nausea, spastic abdominal pain, diarrhea, hypokalemia with prolonged use, darkening of the colonic mucosa (pseudomelanosis) with chronic intake.

Adjustment for Patient Body Weight (Powder): Patients with body weight up to 60 kg — initial dose of 0.5 g, increase only in the absence of effect. Patients with weight above 60 kg — standard dose of 1 g, possibly increased to 2 g in an enhanced regimen.

Preparation Method (Powder): To prepare 100 g of powder: take 100 g of dried buckthorn bark, clean of impurities, grind in a porcelain mortar or mill to a homogeneous powder (particle size no more than 1 mm). Store in an airtight glass container. Do not allow contact with metals.

Storage Conditions and Shelf Life (Powder): Store in a tightly closed glass container in a dark, dry place at a temperature of +15 to +25 °C. Avoid exposure to direct sunlight and electromagnetic radiation. Shelf life — up to 12 months. After opening the package, use within 60 days.

Dry Extract — Rhamnus cathartica

Indications (Dry Extract): Chronic constipation, colonic dyskinesia, constipation after rectal surgery, symptomatic treatment for hemorrhoids with difficult defecation.

Standard Dosage (Dry Extract): 100–150 mg of dry extract once daily in the evening, washed down with water.

Enhanced Dosage (Dry Extract): 200 mg once daily for pronounced hypomotor dyskinesia or incomplete intestinal evacuation.

Maximum Dosage (Dry Extract): 300 mg once for short-term need for urgent bowel cleansing, under medical supervision.

Preventive Dosage (Dry Extract): 50 mg once every two days for 7–10 days in patients with a sedentary lifestyle, chronic colostasis, and decreased motor activity in old age. Repeat the course no earlier than after 1 month.

Pediatric Dosage (Dry Extract): From 12 years of age, body weight from 40 kg — 50 mg no more than once every 3 days. Use under 12 years of age is contraindicated due to the possible toxicity of anthraquinone glycosides.

Contraindications (Dry Extract): Individual intolerance, acute inflammatory bowel diseases, irritable bowel syndrome with diarrhea, pregnancy. There are no scientifically registered data on use during lactation and in younger pediatric patients.

Side Effects (Dry Extract): Diarrhea, electrolyte disturbances (hypokalemia), intestinal spasms, reflex nausea, allergic reactions (skin itching, rash).

Adjustment for Patient Body Weight (Dry Extract): Up to 60 kg — 100 mg; from 60 kg — 150–200 mg. Increase the dose only if ineffective.

Preparation Method (Dry Extract): 100 g of crushed buckthorn bark are poured with 1000 ml of purified water, heated to 80 °C, and extracted for 4 hours. The liquid is evaporated at a temperature of 45–50 °C to a thick extract, then dried in a vacuum dryer to obtain a powder. The resulting dry extract is ground to a fine powder state.

Storage Conditions and Shelf Life (Dry Extract): Store in a hermetically sealed dark glass container at a temperature not exceeding +25 °C, in a dry, light-protected place. Shelf life — up to 24 months. After opening — use within 30 days.

Alcohol-Based Tincture — Rhamnus cathartica

Indications (Tincture): Atonic constipation, colonic dyskinesia, irritable bowel syndrome with constipation, chronic hemorrhoids with difficult defecation, intestinal hypotension against the background of old age.

Standard Dosage (Tincture): 15 drops of tincture diluted in 100 ml of water, taken once daily at night.

Enhanced Dosage (Tincture): 25 drops per 100 ml of water before bedtime for prolonged absence of stool of more than 48 hours, with a pronounced spastic component of constipation.

Maximum Dosage (Tincture): 30 drops once before diagnostic procedures (irrigoscopy, colonoscopy), under medical supervision.

Preventive Dosage (Tincture): 10 drops of tincture 2 times a week before bedtime for a chronic tendency to constipation in patients over 60 years of age, with impaired intestinal motility and decreased physical activity.

Pediatric Dosage (Tincture): Not used in children under 12 years of age. From 12 years — no more than 5 drops diluted in 100 ml of water, no more than once every 3 days.

Contraindications (Tincture): Pregnancy, lactation, childhood under 12 years of age, organic liver diseases, chronic alcoholism, inflammatory diseases of the colon, hypersensitivity.

Side Effects (Tincture): Nausea, heartburn, frequent stools, short-term spasms, allergic reactions (urticaria); in case of overdose — arrhythmias, dizziness, dehydration.

Adjustment for Patient Body Weight (Tincture): Up to 60 kg — start with 10 drops, increase is possible in the absence of effect. Over 60 kg — standard dosages, increase according to indications.

Preparation Method (Tincture): To prepare 100 ml of tincture: take 25 g of crushed buckthorn bark, pour 75 ml of 70% ethanol and 25 ml of purified water, place in a dark glass container with a hermetic lid. Infuse in a light-protected place at a temperature of +20…+25 °C for 10 days, shaking daily. Upon completion — strain, pour into a sterile bottle.

Storage Conditions and Shelf Life (Tincture): Store in a tightly closed dark glass bottle at a temperature of +15 to +25 °C. Avoid exposure to light, heat, and sources of EMI. Shelf life — up to 36 months. After opening — use within 60 days.

Oil Infusion — Rhamnus cathartica

Indications (Oil Infusion): Chronic constipation, hemorrhoidal disease with difficult defecation, anal fissure with a pronounced spastic component, biliary dyskinesia, constipation in endocrine disorders.

Standard Dosage (Oil Infusion): 1 teaspoon (5 ml) of oil infusion at night, internally, on an empty stomach or before bedtime, course — up to 10 days.

Enhanced Dosage (Oil Infusion): 1 tablespoon (15 ml) before bedtime in cases of prolonged constipation and persistent hypomotor dyskinesia.

Maximum Dosage (Oil Infusion): 2 tablespoons (30 ml) once for rapid bowel cleansing in preparation for procedures under specialist supervision.

Preventive Dosage (Oil Infusion): 1 teaspoon (5 ml) twice a week for chronic constipation, sedentary lifestyle, decreased bile secretion, and metabolic disorders. Course — no more than 4 weeks, repeat after 1–2 months.

Pediatric Dosage (Oil Infusion): From 6 years — 1 ml of oil infusion in food, no more than 2 times a week. From 12 years — 2–3 ml. Use in children under 6 years of age is not recommended.

Contraindications (Oil Infusion): Gallstone disease, pancreatitis in the acute phase, intestinal inflammation, individual intolerance. No data on use during pregnancy and lactation have been recorded.

Side Effects (Oil Infusion): Diarrhea, epigastric pain, increased peristalsis, bitterness in the mouth, nausea.

Adjustment for Patient Body Weight (Oil Infusion): Patients up to 60 kg — 1 teaspoon. Over 60 kg — an increase up to 15 ml is possible.

Preparation Method (Oil Infusion): 100 g of crushed dry buckthorn bark are poured with 200 ml of unrefined coconut oil, pre-melted in a water bath (to 35 °C). Infuse in a glass jar with a lid in a water bath at a temperature of 35–40 °C for 6 hours. Cool, strain through gauze. Pour into a dark glass bottle.

Storage Conditions and Shelf Life (Oil Infusion): Store in a dark, airtight glass container at a temperature of +5 to +20 °C, away from direct light and heating appliances. Avoid EMI. Shelf life — 6 months. After opening, use within 30 days.

Vaginal Suppositories — Rhamnus cathartica

Indications (Vaginal Suppositories): Atonic constipation with concomitant gynecological pathologies, proctogenic constipation with pelvic overload, pelvic venous insufficiency syndrome, dyspareunia against the background of spastic constipation, condition after gynecological operations with difficult defecation.

Standard Dosage (Vaginal Suppositories): 1 suppository at night, vaginally, course — 5–7 days.

Enhanced Dosage (Vaginal Suppositories): 2 suppositories per day (morning and evening) for severe pelvic constipation accompanied by venous stasis, for short-term use no more than 3 days.

Maximum Dosage (Vaginal Suppositories): 3 suppositories per day (every 8 hours) under medical supervision for pronounced pelvic stasis and postoperative intestinal atony.

Preventive Dosage (Vaginal Suppositories): 1 suppository 2 times a week for chronic pelvic venous congestion, hypomotor intestinal dysfunction in women over 45 years of age, and recurrent constipation against the background of hormonal changes.

Pediatric Dosage (Vaginal Suppositories): Not used in pediatric practice.

Contraindications (Vaginal Suppositories): Pregnancy, inflammatory diseases of the vagina, erosive processes, gynecological bleeding, individual intolerance to components. No data on use during lactation have been registered.

Side Effects (Vaginal Suppositories): Burning in the vagina, increased mucus secretion, local hyperemia, feeling of pressure in the lower abdomen.

Adjustment for Patient Body Weight (Vaginal Suppositories): No adjustment is required; used locally.

Preparation Method (Vaginal Suppositories): For 100 g of base: take 20 g of dry buckthorn extract, 70 g of coconut oil, 10 g of beeswax. Melt the coconut oil in a water bath to 40 °C, dissolve the extract in it, add wax, and stir thoroughly until homogeneous. Pour into molds of 2 g each and cool.

Storage Conditions and Shelf Life (Vaginal Suppositories): Store at a temperature of +2 to +8 °C, in the original packaging, in the dark. Shelf life — up to 6 months. After opening the blister — use within 7 days.

Rectal Suppositories — Rhamnus cathartica

Indications (Rectal Suppositories): Chronic atonic constipation, constipation in hemorrhoidal disease, hypomotor colonic dyskinesia, constipation after proctological operations, intestinal atony in elderly patients.

Standard Dosage (Rectal Suppositories): 1 suppository rectally at night, course — 5–10 days.

Enhanced Dosage (Rectal Suppositories): 2 suppositories per day (morning and evening) for complete stool retention of more than 48 hours or pronounced straining during defecation.

Maximum Dosage (Rectal Suppositories): 3 suppositories per day for no more than 3 days, under medical supervision, in cases of emergency bowel cleansing.

Preventive Dosage (Rectal Suppositories): 1 suppository every 2 days, course — 2 weeks for recurrent constipation, lazy bowel syndrome, and in postoperative recovery.

Pediatric Dosage (Rectal Suppositories): From 6 years — ½ suppository (1 g) once, no more than 2 times a week, only in the absence of effect from non-pharmacological agents.

Contraindications (Rectal Suppositories): Acute inflammatory processes in the rectum, anal fissures, bleeding, proctitis, rectal cancer, hypersensitivity to components. No data on use during pregnancy and lactation have been registered.

Side Effects (Rectal Suppositories): Burning, itching, false urges, mucosal hyperemia, frequent defecation, flatulence.

Adjustment for Patient Body Weight (Rectal Suppositories): Up to 60 kg — use 1 g each; over 60 kg — standard dose of 2 g.

Preparation Method (Rectal Suppositories): For 100 g of mass: take 20 g of dry buckthorn bark extract, 70 g of coconut oil, 10 g of lanolin. Melt the oil to 40 °C, add the extract and lanolin, stir thoroughly, pour into molds of 2 g each. Cool until completely solidified.

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

Nasal Drops — Rhamnus cathartica

Indications (Nasal Drops): Chronic vasomotor rhinitis with impaired vascular tone of the mucous membrane, congestive phenomena in the nose with hypotension, chronic sinusopathy with edema, hypotrophic rhinitis.

Standard Dosage (Nasal Drops): 1 drop into each nostril twice daily, course — no more than 5 days.

Enhanced Dosage (Nasal Drops): 2 drops 3 times a day for pronounced nasal congestion, hypotension of the mucosal vessels, in combination with chronic constipation.

Maximum Dosage (Nasal Drops): 3 drops into each nostril up to 4 times a day for 2 days for an acute vasomotor component, then reduce to the standard dosage.

Preventive Dosage (Nasal Drops): 1 drop into each nostril once daily, every other day, for 7 days, for a tendency to nasal hyposecretion, in elderly patients, and with systemic vegetative dysfunction.

Pediatric Dosage (Nasal Drops): From 6 years — 1 drop once daily, no more than 3 consecutive days. Under 6 years, not recommended due to the risk of mucosal irritation.

Contraindications (Nasal Drops): Acute rhinitis, allergic rhinitis, perforation of the nasal septum, pregnancy. No data on use during lactation have been registered.

Side Effects (Nasal Drops): Burning in the nose, increased sneezing, feeling of mucosal dryness, irritation, headache in case of overdose.

Adjustment for Patient Body Weight (Nasal Drops): No adjustment is required; the agent is used locally.

Preparation Method (Nasal Drops): To prepare 100 ml: 2 g of dry buckthorn extract are dissolved in 60 ml of warm purified water, 35 ml of unrefined coconut oil, 3 ml of glycerin, and 0.1 g of citric acid are added. The mixture is stirred until an emulsion is formed, filtered through gauze, and poured into sterile dropper bottles.

Storage Conditions and Shelf Life (Nasal Drops): Store at a temperature of +4 to +10 °C, in a dark place, without air access. Shelf life — up to 30 days. After opening, use within 7 days.

Ear Drops — Rhamnus cathartica

Indications (Ear Drops): Inflammatory diseases of the external auditory canal with hyposecretion, eczema of the auditory canal, chronic external otitis, initial stage of otosclerosis.

Standard Dosage (Ear Drops): 2 drops into each ear twice daily, course — 5 days.

Enhanced Dosage (Ear Drops): 3 drops three times a day for pronounced dryness of the auditory canal, peeling, and itching dermatitis of the auditory canal.

Maximum Dosage (Ear Drops): 4 drops up to 4 times a day for pronounced hyperkeratosis and epithelial fissures of the external auditory canal, no more than 3 consecutive days.

Preventive Dosage (Ear Drops): 1 drop into each ear once every 2 days, course — 10 days, for a tendency to dryness and irritation of the auditory canal, under conditions of frequent use of headphones, and with prolonged stay in a dusty environment.

Pediatric Dosage (Ear Drops): From 7 years — 1 drop into each ear no more than once daily, if necessary. Use under 7 years requires consultation with a physician.

Contraindications (Ear Drops): Perforation of the eardrum, acute purulent otitis, hypersensitivity, pregnancy. No data on use during lactation are available.

Side Effects (Ear Drops): Irritation of the auditory canal, burning, feeling of fullness, short-term hearing loss due to the oil film.

Adjustment for Patient Body Weight (Ear Drops): No adjustment is required.

Preparation Method (Ear Drops): For 100 ml of solution: take 3 g of dry buckthorn bark extract, dissolve in 20 ml of warm purified water, mix with 75 ml of coconut oil and 2 ml of calendula tincture. Heat to 35 °C, stir thoroughly. Strain and pour into sterile droppers.

Storage Conditions and Shelf Life (Ear Drops): Store in a dark, cool place at a temperature of +4…+10 °C, in a tightly closed bottle. Shelf life — 45 days. After opening — use within 7 days.

Ointment — Rhamnus cathartica

Indications (Ointment): Chronic external hemorrhoids, anal fissure, perianal dermatitis, inflammation of the skin in the perineal area, itching and peeling against the background of eczema, hyperkeratosis.

Standard Dosage (Ointment): Apply in a thin layer to the affected area twice daily — morning and at night. Course — 7–10 days.

Enhanced Dosage (Ointment): Apply 3–4 times a day for pronounced itching, bleeding, and pain syndrome, no more than 5 consecutive days.

Maximum Dosage (Ointment): Up to 6 applications per day for severe forms of inflammation of the perianal zone, under medical supervision. Do not use for more than 3 consecutive days.

Preventive Dosage (Ointment): Apply once daily in the evening to cleansed skin for 5 days for a tendency to irritation of the perianal area, in patients with a sedentary lifestyle or varicose veins of the lesser pelvis.

Pediatric Dosage (Ointment): From 3 years — apply once daily in a thin layer to no more than 5 cm² of skin. Under 3 years, do not use without a physician's prescription.

Contraindications (Ointment): Allergic dermatitis, open wounds, individual intolerance to components. No data on use during pregnancy and lactation have been registered.

Side Effects (Ointment): Local irritation, hyperemia, increased itching, development of contact dermatitis in case of individual sensitivity.

Adjustment for Patient Body Weight (Ointment): No adjustment is required.

Preparation Method (Ointment): To prepare 100 g of ointment: take 20 g of dry buckthorn bark extract, 65 g of coconut oil, 10 g of beeswax, and 5 g of lanolin. Melt the oil in a water bath, dissolve the extract in it, then add wax and lanolin, and stir until homogeneous. Cool and package into tubes or jars.

Storage Conditions and Shelf Life (Ointment): Store in a cool, light-protected place at a temperature of +5 to +15 °C. Shelf life — up to 6 months. After opening, use within 30 days.

Cream — Rhamnus cathartica

Indications (Cream): Dry skin, hyperkeratosis, skin itching against the background of neurodermatitis, peeling, mild forms of eczema, dermatosis with hypofunction of the sebaceous glands.

Standard Dosage (Cream): Apply in a thin layer twice daily to cleansed skin. Course — 10–14 days.

Enhanced Dosage (Cream): Apply up to 4 times a day for pronounced itching, peeling, and fissures, no more than 5 days.

Maximum Dosage (Cream): Up to 6 applications per day on limited skin areas (up to 100 cm²), for severe dryness and painful cracking.

Preventive Dosage (Cream): Apply once daily at night for 7–10 days for seasonal dry skin, dermatological changes in the elderly, and endocrine hypofunction.

Pediatric Dosage (Cream): From 3 years — once daily, only on small skin areas. Under 3 years — under medical supervision.

Contraindications (Cream): Weeping forms of eczema, active skin infections, hypersensitivity. There are no scientifically confirmed data on contraindications during pregnancy and lactation.

Side Effects (Cream): Burning, feeling of a film on the skin, local allergic reactions, urticaria.

Adjustment for Patient Body Weight (Cream): No adjustment is required.

Preparation Method (Cream): To prepare 100 g: take 15 g of dry buckthorn extract, 40 g of coconut oil, 10 g of jojoba oil, 30 g of distilled water, 3 g of lecithin, and 2 g of beeswax. Heat the oils and water to 40 °C in separate containers, combine with continuous stirring, add the extract, then homogenize with a mixer.

Storage Conditions and Shelf Life (Cream): Store at a temperature of +4…+8 °C, in a closed container protected from light. Shelf life — 45 days. After opening, use within 14 days.

Cosmetic Liquid Extraction — Rhamnus cathartica

Indications (Cosmetic Liquid Extraction): Dry skin, age-related thinning of the epidermis, impaired tone of skin vessels, post-inflammatory hyperpigmentation, dull complexion, skin itching of non-inflammatory nature.

Standard Dosage (Cosmetic Liquid Extraction): Used as part of creams, masks, and lotions at a concentration of 2–5% by weight. Apply to the skin 1–2 times a day.

Enhanced Dosage (Cosmetic Liquid Extraction): Use at a concentration of 5–7% for pronounced dry skin, age-related changes, and microcirculation disorders. Apply locally, course of 7–10 days.

Maximum Dosage (Cosmetic Liquid Extraction): Up to 10% in the composition of a cosmetic product. Use is limited locally and in time — no more than 5 consecutive days.

Preventive Dosage (Cosmetic Liquid Extraction): 1–2% in the composition of daily care products — creams, tonics, emulsions. Used long-term, once daily, in patients with thin dry skin, in conditions of cold climate or climatic insolation.

Pediatric Dosage (Cosmetic Liquid Extraction): Not used in children under 12 years of age. From 12 years — at a concentration up to 1% in the composition of products if necessary, course no more than 5 days.

Contraindications (Cosmetic Liquid Extraction): Hypersensitivity, active forms of dermatitis, eczema in the exacerbation stage, weeping eruptions. There are no scientifically registered data on use during pregnancy and lactation.

Side Effects (Cosmetic Liquid Extraction): Redness, burning sensation, allergic contact dermatitis in case of individual intolerance.

Adjustment for Patient Body Weight (Cosmetic Liquid Extraction): Not required.

Preparation Method (Cosmetic Liquid Extraction): For 100 ml of extract: 20 g of dry buckthorn bark are poured with a mixture of 70 ml of water and 30 ml of glycerin. Extract at a temperature of 35 °C for 6 hours. Strain, add 0.1 g of citric acid and 0.2 g of a preserving plant component (e.g., rosemary extract). Store in an airtight bottle.

Storage Conditions and Shelf Life (Cosmetic Liquid Extraction): Store in the refrigerator at a temperature of +4…+8 °C, in dark glassware. Shelf life — up to 45 days. After opening — use within 7 days.

Toxicity and Biosafety of Rhamnus cathartica

Studies on the toxicological evaluation of Rhamnus cathartica indicate the presence of active compounds, primarily anthraquinones, which in high dosages can cause intestinal irritation and electrolyte disturbances. In particular, with prolonged use, the risk of developing intestinal pseudomelanosis (pigmentation of the mucous membrane), characteristic of chronic intake of anthraquinone glycosides, was recorded.

Acute toxicological testing showed that the average lethal dose (LD50) for the aqueous extract of Rhamnus cathartica bark with oral administration to laboratory mice is 6300 mg/kg body weight, which indicates relatively low acute toxicity and allows limited therapeutic use with controlled dosing.

For fresh or under-dried fruits of Rhamnus cathartica, on the contrary, episodes of poisoning in children and animals have been recorded — with symptoms of nausea, vomiting, dehydration, and convulsions. This is due to the content of unstable saponin-like compounds, including emodin and chrysophanol in high concentrations.

Reference: https://pubmed.ncbi.nlm.nih.go...

Pharmacodynamics — Rhamnus cathartica

The pharmacodynamic action of Rhamnus cathartica is due primarily to the presence of anthracene derivatives, including anthraquinone glycosides, chrysophanol, and emodin. The main direction of action is the regulation of motility and secretion of the gastrointestinal tract. Anthraquinone glycosides, after activation by the colonic microflora, are converted into free aglycones capable of directly acting on the intestinal mucosa, activating the peristaltic wave. This is associated with an increase in the expression of water and electrolyte channels at the level of enterocytes, as well as inhibition of Na+/K+-ATPase, which leads to increased water entry into the intestinal lumen.

The pharmacological action is manifested predominantly at the level of the gastrointestinal tract, but with systemic use, nonspecific anti-inflammatory and antiseptic properties are also observed. This is due to the presence of flavonoids possessing membrane-stabilizing and antioxidant effects. In vitro studies show that components of Rhamnus cathartica bark are capable of reducing the production of pro-inflammatory cytokines and inhibiting the activity of cyclooxygenase-2, thereby exhibiting moderate anti-inflammatory activity.

Anthraquinones of the taxon are also capable of causing a reflex influence on the autonomic nervous system, increasing parasympathetic activity in the intestinal wall. At the same time, mild sedative effects are noted, probably mediated through a decrease in the spastic activity of smooth muscle.

Phenolic compounds of Rhamnus cathartica exhibit antioxidant properties, reducing the level of lipid peroxidation and protecting cell membranes from free-radical damage. This has been confirmed experimentally both with the use of aqueous extracts and under in vivo conditions.

On the skin, with local application of ointments and creams, extracts of the taxon exhibit moderate keratolytic, antipruritic, and astringent action. Such action is associated with local modulation of the skin immune response, influence on the synthesis of prostaglandins and cytokines.

Thus, the pharmacodynamics of Rhamnus cathartica is realized both through direct irritating and secretomotor action on the intestinal mucosa and through indirect participation in the regulation of autonomic and immune activity. The action is predominantly local, with possible systemic influence with prolonged use or high dosages.

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

Pharmacokinetics — Rhamnus cathartica

The pharmacokinetic properties of the active components of Rhamnus cathartica depend on the type of dosage form, the route of administration, and the degree of metabolic transformation of anthraquinones. With oral administration of powder, dry extract, or infusion, the absorption of anthraquinone glycosides in the small intestine is minimal. Most of the glycosides reach the colon unchanged, where they undergo bacterial β-glucosidase and reductase activation. The resulting aglycones (e.g., emodin) penetrate enterocytes and activate the secretion of water and ions into the intestinal lumen.

After absorption into the systemic bloodstream, active aglycones partially bind to albumins and enter the liver, where they undergo conjugation (glucuronidation, sulfation) with subsequent excretion predominantly with bile. A small amount of metabolites can be reabsorbed through enterohepatic circulation, providing a prolonged effect with repeated intake.

Excretion occurs predominantly through the intestine (biliary metabolites), as well as with urine in the form of glucuronides. Some components are found in urine in the form of colored metabolites, which can cause a temporary change in its color. With the use of ointments and creams with buckthorn extract, transdermal absorption is minimal; pharmacokinetics is limited to local action in the epidermis and dermis, with partial biotransformation in the skin.

With nasal, vaginal, and rectal administration (e.g., drops, suppositories), absorption depends on the lipophilicity of the base and the state of the mucous membrane. With the use of oil infusions, slow release of active substances, their partial entry into the bloodstream, and further detoxification in the liver are observed. In these cases, excretion occurs with urine and partially with feces.

Thus, the pharmacokinetics of Rhamnus cathartica represents a combination of local and systemic action with an active role of the colonic microflora, enzymatic transformation in the liver, and excretion predominantly through the intestine and urinary system.

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

Mechanisms of Action and Scientific Rationale — Rhamnus cathartica

The main pharmacologically active substances of Rhamnus cathartica are represented by anthraquinone glycosides, predominantly chrysophanol, emodin, and their derivatives. These compounds are activated in the colon under the action of bacterial β-glucosidases, after which the released aglycones stimulate peristalsis by irritating mucosal receptors and activating parasympathetic innervation. The action is realized through enterocytes and interstitial cells of Cajal, responsible for generating motor waves in the intestine.

At the molecular level, it has been established that anthraquinone aglycones are capable of inhibiting the activity of Na+/K+-ATPase in intestinal epithelial cells, which leads to retention of sodium ions in the lumen and subsequent osmotic attraction of water. This is accompanied by an increase in the volume of intestinal contents and activation of mechanoreceptors, which additionally stimulates the peristaltic reflex.

Emodin, contained in buckthorn bark, has been studied as a non-glycosidic modulator of the inflammatory response. It suppresses the expression of the enzyme cyclooxygenase-2 (COX-2) and the activity of the nuclear transcription factor NF-κB, which leads to a decrease in the synthesis of pro-inflammatory mediators such as interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α). At the same time, emodin inhibits MAPK signaling cascades, participating in limiting the inflammatory activation of macrophages and neutrophils.

Flavonoid components and phenolic acids present in Rhamnus cathartica have an antioxidant effect, blocking lipid peroxidation and inactivating free radicals. This may occur through suppression of the activity of NADPH oxidase enzymes and enhanced expression of endogenous antioxidant systems, including superoxide dismutase and catalase.

Some studies show the ability of Rhamnus cathartica extracts to modulate serotonin levels in the enteric nervous system, influencing 5-HT3 and 5-HT4 receptors that regulate intestinal secretion and motility. Such an effect is associated with enhanced reflex activity and normalization of the motor function of the gastrointestinal tract.

With local application (in the form of ointments and creams), buckthorn components interact with keratinocytes and Langerhans cells, exhibiting antipruritic and moderate antiseptic properties. This may be due to the influence on TRPV1 receptors, which mediate the sensation of itching and pain.

Thus, the biological activity of Rhamnus cathartica is due to the complex interaction of active metabolites with enterocytes, epithelial cells, neurons of the enteric nervous system, as well as cells of innate immunity, including macrophages and neutrophils.

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

Synergy — Rhamnus cathartica

Scientific data confirm that anthraquinone components of Rhamnus cathartica can enter into synergistic interaction with other plant metabolites, predominantly flavonoids, saponins, and essential oils, due to modulation of common biological cascades. In particular, combination with phenolic compounds (e.g., quercetin, rutin) enhances antioxidant activity, which contributes to the protection of intestinal epithelial cells from oxidative stress arising from increased secretion and motility.

In vitro studies show potentiation of anti-inflammatory action with combined use of buckthorn extract and glycosides from plants containing salicylates (e.g., Filipendula ulmaria). Such interaction is realized through joint inhibition of the activity of the COX-2 enzyme and subsequent reduction of prostaglandin E2 levels.

Combinations with essential oils possessing spasmolytic action (e.g., Mentha piperita) demonstrate synergy at the level of intestinal smooth muscle. This leads to a decrease in side effects in the form of spasms, usually arising with monotherapy with anthracene derivative agents.

With combined use with extracts containing saponins (e.g., Glycyrrhiza glabra), enhanced absorption of anthraquinones in the colon is noted, which may be associated with the effect of saponins on intestinal epithelial permeability and modulation of the microbiota. This interaction demonstrates an additive and modulating character.

A protective effect has also been confirmed with the combination of Rhamnus cathartica with substances that stabilize electrolyte metabolism (e.g., sources of potassium and magnesium), due to compensation of potential electrolyte loss with enhanced secretion.

Thus, the pharmacological synergy of Rhamnus cathartica is based on complementary mechanisms of action: joint regulation of secretion, motility, inflammation, and oxidative stress, with a potentiating and protective character of interactions.

References:
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https://pubmed.ncbi.nlm.nih.go...
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https://pubmed.ncbi.nlm.nih.go...

Geography of Use and Traditional Medicine — Rhamnus cathartica

Rhamnus cathartica is traditionally used in European, Middle Eastern, and Caucasian folk medicine. The homeland of the plant is considered to be Europe, including the Central and Eastern parts, as well as the western regions of Asia. Ethnobotanical evidence indicates its use among Slavic peoples, Germanic tribes, Celts, as well as in the medico-plant traditions of the peoples of the Caucasus and the Mediterranean.

In Slavic folk medicine, the bark and berries of buckthorn were used in the form of infusions, decoctions, and powder. Use included prolonged courses with a gradual increase in intensity, often with the addition of honey, dill, or caraway seeds. In the Bulgarian, Serbian, and Polish phytotherapeutic tradition, the use of juice of ripe fruits, pre-aged in a clay dish in the sun, has also been recorded. In Latvian and Lithuanian ritual practice, buckthorn was considered a "plant of purification," its branches were hung over the entrances to the house, and the fruits were sometimes placed in waist bags as a protective amulet.

Among Germanic peoples, the plant was associated with "forest bitterness" and is mentioned in monastery herbals starting from the 10th century. In the medical manuscripts of the Lorsch monastery (Germany), there are mentions of "Ramnus" used in the form of an alcohol extract or dried bark. In the alchemical schools of the late Middle Ages (including the works of Paracelsus), buckthorn was mentioned as the "plant of inner expulsion," symbolizing liberation.

In Arab phytotherapy of the Middle Ages, buckthorn is mentioned as "shajar al-marara," used in the form of powder mixed with vinegar or fig juice. The practices of Yemen and Hejaz used it in preparing the body for ritual purification. In the Armenian and Georgian tradition, the bark was ground into powder and rubbed into the skin in the abdominal area with the addition of warm oil — this technique was considered especially effective in winter.

In Hungarian and Czech rural medicine, the preparation of tinctures from buckthorn bark on moonshine or grape vodka was widespread. They were used as a ritual remedy during fasts, as well as a symbol of inner discipline. In the same regions, buckthorn branches were used in ritual bonfires on Ivan Kupala — it was believed that the smoke purifies the home and household from the "evil eye."

In the Caucasus, Rhamnus cathartica figures in Dagestani and Chechen herbals as a plant used in spring and autumn cleansings. It was often mixed with marshmallow root, senna leaves, and mint as part of home preparations. In some cases, the bark was used for smoking in pipes for ritual purposes: it was believed that the bitter smoke drives out "impure thoughts."

In Western Siberia and the Urals, buckthorn berries were sometimes used in the form of alcohol tinctures for rubbing the back and legs during bath ceremonies. In folklore, it is mentioned that the branches of the plant were placed in the corners of premises for protection from "disease spirits" and the evil eye.