Colocynthidis fructus

Colocynthidis fructus, also known as colocynth fruits, are used in folk medicine worldwide, e.g. for urinary tract infections, also for gastrointestinal complaints, bacterial infections or diabetes.
Herbal medicinal products in Germany with colocynth fruit extract since 1914 Arhama® tincture N

Commission E: Negative monograph due to gastrointestinal side effects

Colocynthidis fructus contains as a skin active substance Cucurbitacine E, which is present in glycosidic form, with a maximum level of 0,072 % of the official drug. It contains sterols, fatty acids, flavonoids, sugars and saponins.

Coloquine fruits increase the secretion of fluid into the intestinal lumen and also have a laxative, peristaltic stimulating effect, promote the secretion of gastric juice and irritate the mucous membrane in a high dosage. Furthermore, cucurbitacin derivatives have a broad antiproliferative effect.

For the treatment of nonspecific gastrointestinal disorders with diarrhea for adults and children 12 years and older.

Dosage: Single dose of 7.5 mL; at intervals of 48 h for a maximum of 14 days (corresponding to a maximum of 7 single doses)
A colocynth fruit extract is not intended for long-term use. If necessary, the duration of intake should be limited to as few days as possible. It should not exceed 14 days at a time and 30 days in total in a calendar year.

An extract of coloquinth fruits (1: 10-13) has been approved; the extractant is ethanol 42 % V/V. Only one product is authorized, which is only available on prescription.

BfArM: Koloquinthen-Essenz-Bombastus, ENR: 3000743, approved according to § 105 AMG, prescription only, 100 g (= 105.7 ml) liquid
Indication: For short-term use in constipation in children from 12 years and adults
Dosage: 2 x daily 3 - 10 ml, corresponding to a drug equivalent of 110 mg to 475 mg daily dose.
Duration of use: Not longer than 14 days in a row and
not on more than 30 days within one year.

Cramp-like symptoms may occur, especially with irritable colon (-> dose reduction). A loss of electrolyte is to be expected with chronic use or abuse.

Chronic ingestion or abuse due to potassium deficiency increases the effect of cardiac glycosides and may influence the effect of antiarrhythmic drugs. Potassium losses can be increased by combining it with saluretics, adrenal cortex hormones or liquorice root. A simultaneous intake of anthranoid drugs may also increase the effects.

The side effects do not occur or occur only very rarely if the dose of total cucurbitacins is limited to a maximum amount (0.072%) as in the approved ethanolic extract.
Overdosage may result in painful intestinal cramps and severe diarrhoea with loss of water and electrolytes. An overdose with a toxic damage is only possible with a dosage outside the package size.

The homeopathic globules Citrullus colocynthis D6 are toxicologically harmless and a frequently prescribed homeopathic agent for colicky pain conditions associated with abdominal pain, nausea and nausea. Infants and toddlers receive as initial dose 5 globules per hour, infants 1 globule. In case of a noticeable improvement, usually after the 3rd day, 5 globules or 1 globule is reduced to 3 times daily. They can usually be discontinued after a few days.

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2. Cai Y et al (2015) Cucurbitacins: A Systematic Review of the Phytochemistry and Anticancer Activity. On J Chin Med 43:1331-1350.
3. Chawech R et al (2015) Cucurbitacins from the Leaves of Citrullus colocynthis (L.) Schrad. Molecules 20:18001-18015.
4. Chen X et al (2012) Biological activities and potential molecular targets of cucurbitacins: a focus on cancer. Anticancer Drugs 23:777-787.
5. Guo J et al (2015) The anti-melanoma efficiency of the intratumoral injection of cucurbitacin-loaded sustained release carriers: in situ-forming implants. AAPS PharmSciTech 16:973-985.
6. Schilcher H (Ed.) in, Guide to Phytotherapy, Urban & Fischer Verlag (2016) Munich, p. 192 ff.
7. Silva IT et al (2016) Cytotoxic effects of natural and semisynthetic cucurbitacins on lung cancer cell line A549. Invest New Drugs 34:139-148.
8. Wang Y et al (2014) Cucurbitacin IIb exhibits anti-inflammatory activity through modulating multiple cellular behaviors of mouse lymphocytes.PLoS One 9:e89751.