Ergot alkaloids are naturally occurring, active ingredients that are mainly found in the ergot fungus (Claviceps purpurea). They are used as an isolated component in various medicines due to their psychotropic as well as vascular and circulation-promoting properties.

What are ergot alkaloids?

The parasitic crescent-shaped cereal fungus grows mainly in cereal ears after an infection of the grain. Since alkaloids have a high toxicity as a secondary plant substance, in agriculture the attack is prevented by various strategies. Until the 20th century, there was regular mass poisoning from the consumption of contaminated grain, which was referred to as "ergotism". Today, the term is used for the side effects associated with chronic use of ergotamine.

Ergot alkaloids are made up of ergoline, a nitrogen-containing, organic-chemical compound whose abstracted substances are used in the treatment of migraine, hypotension, Parkinson's disease and cardiovascular disease. From the ergot fungus lysergic acid is obtained, which is used for the production of LSD (Lysergsäurediethylamid). For this reason, the delivery of the drug ergotamine is restricted by the German Basic Substance Control Act.

Already in low concentrations, the ergot alkaloids have a toxic effect on the central nervous system. Currently, the alkaloids and derivatives of cereal parasite are being discussed as neuro-psychotropic drugs. In pharmacological terms, "Dirty Drugs" refers to drugs that bind to various receptors in the brain. On the one hand, this leads to a broad spectrum of effects, but is often associated with unpredictable side effects. Science is working towards a more targeted effect.

In addition to ergot alkaloids, the British biochemist Henry Hallett Dale could detect histamine as a natural product in ergot.

Pharmacological action

Ergot alkaloids have many effects on the body. Primarily, they are called dopamine agonists. That is, they stimulate the dopamine receptors and thereby intensify the dopamine action in the body. They directly intervene in the autonomic nervous system, which coordinates our body and organ functions. This effect is used, for example, in Parkinson's disease, as the disease is mainly caused by a lack of dopamine.

Single ergot alkaloids, even at low concentrations, can cause neurological disorders and affect the central nervous system. This can lead to epileptic seizures or convulsions. Other alkaloids include a toxin that can cause limbs to die by occluding the blood vessels.

Five to ten percent of ergot can already kill an adult. Responsible for this is the composition of the various ergot alkaloids and their high concentration.

The active ingredients can both block and excite the receptors on the blood vessels. Depending on which alkaloid it is. The successful treatment of migraine is explained by its effect on the blood vessels. The binding of the substances to the alpha-receptors of the musculature also induces contractions of the uterus.

An ergot alkaloid used is ergometrine. It is a uterine tonic (has a tonic effect on the uterus) that acts alpha-sympatholytically (reversing the effects of the sympathetic) and has a direct stimulating effect on the vascular smooth muscle and the uterus. In the venous system, ergotamine in its natural form has a pronounced vasoconstrictive (narrowing) effect on venous and arterial vessels.

In addition, a serotonergic (serotonin-responsive or serotonin-containing) effect is discussed. Ergotamine derivatives are detectable in breast milk. They can cause vomiting, diarrhea and hypertension in breastfed infants.

Lysergic acid dilates the pupils and raises blood pressure, can trigger perceptual changes in the sense of time as well as in visual and acoustic stimuli. LSD is a mood-altering hallucinogen.

Furthermore, some derivatives of ergot alkaloids are used. Bromocriptine and cabergoline, for example, have dopaminergic properties and inhibit the release of the hormone prolactin. Dihydroergotamine has a blood pressure and vascular regulation. Dihydroergocryptine acts selectively on D2 receptors.

Dihydroergotoxin, in combination with other drugs, can positively affect brain function and reduce blood pressure. Lisuride and pergolide bind to dopamine and serotonin receptors. Methylergometrine has a contracting (toning) effect on the uterus.

Medical application & use

In medicine, despite their toxicity, the substances of the fungus constitute a group of highly efficient analeptics. They are therefore used in a wide variety of diseases.

Dihydroergotamine in: hypotension, fainting, cardiovascular complaints, acute migraine attacks with and without aura.

Dihydroergotoxine in: hypertension / age-related hypertension, concomitant treatment of Raynaud's syndrome, visual disturbances of vascular origin, symptomatic treatment of venous-lymphatic insufficiency, brain disorders, Alzheimer's, dementia, migraine. Even small amounts can cause nausea and vomiting. The remedy is therefore also used as an emetic.

Ergotamine in: cluster headache, migraine. Dihydroergocryptine, lisuride, cabergoline and pergolide in: Parkinson's disease. Dihydroergocryptine in: Parkinson's disease and interval treatment of migraine. Bromocriptine in: restless legs syndrome, menstrual disorders, female infertility, male hyperprolactin anemia, prolactinomas, acromegaly, benign mammary gland disorders, and Parkinson's disease.

Cabergoline in turn: hyperprolactinemic disorders. Methylergometrine in: promotions of placental ablation, treatments for uterine atony and treatment of postpartum bleeding.

Risks & Side Effects

The following side effects can occur: Headache, vomiting, in case of long-term treatment Circulatory disorders of the hands and feet up to vascular occlusion and death of the affected region, angina, gastrointestinal discomfort, loss of appetite, insomnia, restlessness, stuffy nose, constipation, slowed heartbeat, drop in blood pressure, Circulatory problems, dizziness, itching, tingling and numbness and feeling of cold in the arms and legs, anxiety, depression, skin reactions, muscle weakness, muscle pain, muscle spasms, too slow or too fast heart rate (bradycardia, tachycardia), heart valve damage, heart attack, heart stuttering, respiratory disorders, edema, Fibrosis, dyskinesias, hallucinations, hypotension, drowsiness, sweating, dry mouth, stomach pain, stomach cramps, weakness, heartburn, fluid retention in tissues, weight change, restlessness, loss of libido, tremor, tinnitus, nightmares, delusions, upper limb also complaints, indigestion, painful legs, hair loss, blurred vision, psychosis, nervousness, coordination disorders, incontinence, frequent urination, facial blanching, stroke, uterine contractile pain, hypogalactia and behavioral disorders.

Common side effects of all dopamine agonists are increased libido and hypersexuality, binge eating, obsessive-compulsive disorder and diminished impulse control. Tags: 

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