Cascara Sagrada

Rhamnaceae

Frangula purshiana

Also known as: Cascara, Sacred Bark, Rhamnus purshiana

Pregnancy D
Lactation D

clinical_notes Clinical Summary

Cascara Sagrada (Frangula purshiana) is a North American buckthorn whose aged bark contains anthraquinone glycosides (cascarosides) producing a stimulant laxative effect within 8-12 hours.

Historically the dominant OTC laxative in the US until the FDA revoked its GRAS status in 2002.

Use should be strictly short-term (less than 1 week) in adults; contraindicated in pregnancy, lactation, children, and IBD.

Pregnancy Safety

D

Avoid in pregnancy. FDA removed cascara from OTC laxative status in 2002. Bulk-forming laxatives are preferred alternatives.

Lactation Safety

D

Contraindicated while breastfeeding. Anthraquinones cross into milk and can induce diarrhea in the infant.

warning Contraindications

  • Pregnancy (contraindicated)
    Theoretical
  • Lactation (contraindicated)
    Clinically Proven
  • Children (contraindicated)
    Clinically Proven
  • Inflammatory bowel disease (Crohn's, ulcerative colitis) (contraindicated)
    Clinically Proven
  • Use >1 week / long-term use (contraindicated)
    Clinically Proven
  • Concurrent use of cardiac glycosides (digoxin) or thiazide diuretics (avoid)
    Theoretical

vital_signs Clinical Profile

Primary Indications

  • check_circle short-term constipation
  • check_circle occasional constipation

Therapeutic Actions

stimulant laxativecholagoguebitterpurgative

System Affinities

  • check_circle digestive system
  • check_circle colon
  • check_circle hepatobiliary

labs Active Constituents

cascarosides A, B, C, D

aloin-like anthrones

emodin

chrysophanol

barbaloin

resins

tannins

history_edu Traditional Use

No TCM data available for this herb yet.

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Traditional Uses Across Healing Systems

While many herbs lack controlled clinical trials, centuries of traditional practice across cultures provide valuable insight into their therapeutic applications.

Indigenous Pacific Northwest of North America
Pre-colonial; introduced to Western medicine in 1877.

Pacific Northwest First Nations used the aged bark as a laxative for constipation.

Chinook Jargon name 'chittem bark'. Bark must be aged at least 1 year to destroy harsh anthrone compounds.

Western Herbal North America, Europe
1877 - present

Principal OTC laxative in North America for much of the 20th century; still used short-term for constipation.

Removed from FDA OTC monograph in 2002 due to lack of efficacy/safety data; still sold as dietary supplement.

spa Parts Used

bark

Constituents
cascarosides A-Demodinchrysophanolaloin-like anthrones
Indications
  • short-term constipation
Preparation

Only aged (>1 year) dried bark from trunk/branches is used - fresh bark contains free anthrones that cause violent vomiting and cramping.

shield Safety

Contraindications — Evidence Basis

Pregnancy
contraindicated Theoretical

Anthraquinone laxatives may stimulate uterine activity; insufficient safety data.

Lactation
contraindicated Clinically Proven

Anthranoids distribute into breast milk and may cause diarrhea in the nursing infant.

Children
contraindicated Clinically Proven

Increased risk of dehydration, electrolyte disturbance, and hypokalemia.

Inflammatory bowel disease (Crohn's, ulcerative colitis)
contraindicated Clinically Proven

Stimulant laxatives may aggravate mucosal inflammation and cause cramping.

Use >1 week / long-term use
contraindicated Clinically Proven

Risk of dependence, electrolyte imbalance, hypokalemia, melanosis coli, and rare hepatotoxicity.

Concurrent use of cardiac glycosides (digoxin) or thiazide diuretics
avoid Theoretical

Hypokalemia from chronic anthraquinone use potentiates cardiac glycoside toxicity.

monitoring

Monitoring Parameters

Monitor during use, especially with prolonged or high-dose therapy.

Serum potassium
If used >1 week: weekly

Risk of hypokalemia from chronic anthraquinone use.

flagThreshold: K+ <3.5 mEq/L: discontinue and replete.

Liver enzymes (ALT, AST, ALP, bilirubin)
If used long-term: at baseline, 4 weeks, and as indicated

Rare reports of cholestatic hepatitis, portal hypertension, and acute liver failure with chronic use.

flagThreshold: ALT >3x ULN or new jaundice: discontinue immediately and evaluate.

Toxicity

Toxic Dose

Use >1 week or doses above 20-30 mg hydroxyanthracene derivatives per day increase risk of toxicity. Fresh bark is toxic (emesis).

Symptoms

Severe abdominal cramping, watery diarrhea, hypokalemia, dehydration, electrolyte loss, cardiac arrhythmia, muscle weakness, melanosis coli, rare cholestatic hepatitis, acute liver failure.

Management

Discontinue immediately; rehydration and electrolyte correction; monitor potassium and liver enzymes; supportive care.

Adverse Effects

abdominal crampsnauseadiarrheaelectrolyte imbalancehypokalemiamelanosis colihepatotoxicity (rare)

CYP Metabolism

Emodin has been shown to modulate CYP3A4 in vitro; clinical relevance at therapeutic doses unclear.

swap_horiz Interactions

Digoxin

Increased Effect critical

Class: Cardiac glycoside

Mechanism

Chronic cascara use causes hypokalemia through loss of potassium in stool. Hypokalemia markedly potentiates digoxin binding to the myocardial Na+/K+-ATPase, precipitating digoxin toxicity (ventricular arrhythmias, AV block) even at therapeutic serum digoxin levels.

Clinical Guidance

Contraindicated with chronic cascara use. If short-term use unavoidable, monitor serum potassium and digoxin level; correct hypokalemia promptly.

menu_book
Evidence Source World Health Organization. WHO Monographs on Selected Medicinal Plants, Volume 2: Cortex Rhamni Purshianae View source open_in_new

Furosemide

Increased Effect high

Class: Loop diuretic

Mechanism

Additive potassium and magnesium losses via stool (cascara) and urine (loop diuretic) can precipitate clinically significant hypokalemia, hypomagnesemia and arrhythmia risk.

Clinical Guidance

Avoid chronic combined use. If combined, check serum potassium and magnesium within 1-2 weeks and supplement as needed.

menu_book
Evidence Source European Medicines Agency (HMPC). Community herbal monograph: Rhamnus purshiana bark. View source open_in_new

Hydrochlorothiazide

Increased Effect moderate

Class: Thiazide diuretic

Mechanism

Thiazides and stimulant anthraquinone laxatives both deplete potassium; combined use increases risk of hypokalemia, muscle weakness and arrhythmia.

Clinical Guidance

Limit cascara to short courses (<1-2 weeks). Monitor electrolytes every 2-4 weeks if chronic laxative use continues.

menu_book
Evidence Source Izzo AA, Ernst E. Interactions between herbal medicines and prescribed drugs: an updated systematic review. Drugs. 2009;69(13):1777-98 View source open_in_new

Prednisone

Increased Effect moderate

Class: Corticosteroid

Mechanism

Corticosteroids promote renal potassium excretion; concurrent stimulant laxative use amplifies kaliuresis and risk of hypokalemic complications (weakness, ileus, arrhythmia).

Clinical Guidance

Avoid chronic co-use. If both needed short-term, check potassium at 1 week.

menu_book
Evidence Source Müller-Lissner SA. Adverse effects of laxatives: fact and fiction. Pharmacology. 1993;47(Suppl 1):138-45 View source open_in_new

Warfarin

Increased Effect moderate

Class: Anticoagulant

Mechanism

Reports of elevated INR with chronic anthraquinone laxative use, potentially from electrolyte-mediated vitamin K-epoxide cycle disturbance, reduced vitamin K absorption due to rapid GI transit, and possible direct displacement of warfarin from albumin.

Clinical Guidance

Monitor INR closely if cascara is used >1 week alongside warfarin. Prefer bulk-forming laxatives (psyllium) in anticoagulated patients.

menu_book
Evidence Source Heck AM, DeWitt BA, Lukes AL. Potential interactions between alternative therapies and warfarin. Am J Health Syst Pharm. 2000;57(13):1221-7 View source open_in_new

Oral contraceptives (combined)

Decreased Effect moderate

Class: Hormonal contraceptive

Mechanism

Rapid intestinal transit induced by stimulant laxatives can reduce absorption of orally administered estrogens and progestogens, lowering contraceptive reliability.

Clinical Guidance

Space cascara doses at least 2 hours apart from oral contraceptive dosing. Consider backup contraception with prolonged cascara use.

menu_book
Evidence Source European Medicines Agency (HMPC). Community herbal monograph: Rhamnus purshiana bark. View source open_in_new

Licorice-containing medications (carbenoxolone)

Increased Effect high

Class: Mineralocorticoid / mucosal protectant

Mechanism

Both cascara (K loss via stool) and carbenoxolone/licorice (pseudohyperaldosteronism) reduce serum potassium; risk of severe hypokalemia and myopathy is additive.

Clinical Guidance

Do not combine. If encountered, check serum potassium immediately and discontinue laxative.

menu_book
Evidence Source Izzo AA, Ernst E. Interactions between herbal medicines and prescribed drugs: an updated systematic review. Drugs. 2009;69(13):1777-98 View source open_in_new

hub Combinations

info

Synergistic pairings can enhance therapeutic outcomes, while knowing suitable substitutes helps when specific herbs are unavailable or contraindicated.

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Possible Substitutes

2
Aloe Vera
Moderate Evidence
Rationale

Both are anthraquinone-based stimulant laxatives; aloe latex is a stronger alternative.

Clinical Evidence

Historical OTC formulations; both have similar FDA safety concerns.

Senna
Strong Evidence
Rationale

Similar anthraquinone mechanism; senna is the most commonly used clinically acceptable alternative.

Clinical Evidence

Senna has FDA approval and stronger safety data.

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Synergistic Combinations

2
Fennel
Traditional Use
Rationale

Fennel's carminative action reduces griping and abdominal cramping associated with stimulant laxatives.

Clinical Evidence

Traditional Western formulation practice to temper anthraquinone cramping.

Psyllium
Moderate Evidence
Rationale

Bulking fiber combined with stimulant laxative improves stool formation and reduces dependence risk.

Clinical Evidence

Standard combination in some OTC laxatives.

science Studies

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Cytotoxicity of Structurally Diverse Anthranoids and Correlation with Mechanism of Action and Side Effects

In Vitro
2018 |Ferro EA, Ribeiro AB, Kato L, de Oliveira CM, Rodrigues EV, Botelho FV. Food Chem Toxicol. 2018;120:498-506.

This in vitro study evaluated the cytotoxicity and apoptosis-inducing ability of structurally diverse anthraquinones including cascarosides A-F isolated from Rhamnus purshiana (cascara sagrada) bark. Cell viability was assessed in NOK-SI, HeLa, and T98G cell lines, and key apoptotic proteins were evaluated. The study found that glycosylated anthraquinones (cascarosides) showed notably reduced cytotoxicity compared to aglycone anthraquinones, providing mechanistic evidence that cascarosides-enriched cascara extract may have a safer laxative profile. The presence of glucose moieties in cascarosides appears to reduce cellular toxicity while retaining laxative activity through bacterial hydrolysis in the large intestine. These findings help explain the traditional use of cascara as a laxative at appropriate doses.

ConstipationOccasional constipation
laxativeanthraquinone mechanismstimulant laxativecolonic motility
View source open_in_new

The metabolism of anthranoid laxatives

Observational
1988 |Lemli J. Pharmacology. 1988;36 Suppl 1:126-128.

This foundational pharmacological review characterizes the metabolic fate of anthranoid laxatives including the cascarosides present in cascara sagrada. Anthranoid glycosides are demonstrated to pass through the small intestine unabsorbed, reaching the large intestine where colonic bacteria hydrolyze the sugar moiety to release active anthrone aglycones. The active metabolites then stimulate water and electrolyte secretion, promoting bowel movements. Radiochemical studies showed tissue-bound anthranoid activity clearance from most organs, with notable kidney retention. The review argues that anthrone C-glycosides (the primary active compounds in cascara) have a preferable safety profile compared to O-glycoside anthraquinones found in senna. These mechanistic insights remain the pharmacological basis for cascara's clinical use as a stimulant laxative.

ConstipationOccasional constipation
laxativeanthraquinone mechanismstimulant laxativecolonic motility
View source open_in_new

medication Dosing

capsule

Dose Range

100-300 mg dried bark extract (standardized to 20-30 mg hydroxyanthracene derivatives)

Frequency

Once at bedtime

Notes

Strictly short-term; do not exceed 7 days consecutive use. Takes effect in 8-12 hours.

tincture

Dose Range

2-6 mL fluid extract

Frequency

Once at bedtime

Notes

Short-term use only. Mild bitter action.

decoction

Dose Range

1 g dried aged bark

Frequency

Once at bedtime

Notes

Simmer 10 minutes; taken occasionally for constipation.

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Disclaimer: This information is largely AI-generated and reviewed by human experts at Evara Health. It is intended for educational and clinical reference purposes only and should not replace professional medical advice.

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