Mushroom, parasitic on rye, families sporыnyevыh (Clavicipitaceae). It belongs to a class of marsupials mushrooms. For medical purposes are grown and harvested horns ergot.
Ergot – Chemical composition
Horns Ergot contains 3 group alkaloids: Group ergotamine, ergotoxine group and the group ergometrika. All alkaloids have their inactive isomers. At the moment of horns ergot allocated more 15 various alkaloids. Besides alkaloids, tyramine found in ergot, histamine, trimethylamine, methylamine and Others aminы, as well as organic acids, pigments and fatty oil.
Ergot – Pharmacological properties
The amount of biologically highly active ergot alkaloids is currently one of the most important sources of creation of various pharmacological agents of various directions and mechanism of action. Herbal medicines and its main ergot alkaloids - ergotamine and ergometrine - are of great importance for practical medicine. The main pharmacological properties of ergot drugs is considered a significant increase uterine contractions and increasing its tone.
In small doses, herbal form and especially its ergot alkaloid drugs (ergometrine, ergotamin, ergotoxine) cause in animal experiments clear strengthening of rhythmic contractions of the uterine muscle, However, with increasing doses of drugs begins to emerge and tonic effect, that at first reflected in a reduction of the amplitude reductions and increased muscle tone, and then comes a sharp spasm of smooth muscles of the uterus.
It should be noted, ergot medications that have a tonic effect on the whole on the contractility of the smooth muscle of organs, at therapeutic doses is strictly selective effect on the uterus, being most pronounced selectivity in this direction is ergometrine, but the duration of the effect on the contractile ability of the uterus championship is still necessary to give ergotoxine and ergotamine.
Equally important have vasodilating properties of ergot alkaloids, that in experiments on different animal species were accompanied by increases in blood pressure and reflex bradycardia, and even large doses resulting in damage to vascular endothelium, wherein at ergotoxine this negative effect is expressed on blood vessels in less, than other ergot.
Ergot alkaloids in the experiment showed distinct adrenoceptor blocking properties, however, the associated effect of their vasodilator, Unfortunately, It leveled a direct vasoconstrictor action myotropic. In this respect, favorably dihydrogenated ergot alkaloids (dihydroergotamine and dihydroergotoxin), who adrenoliticheskoe effect is significantly more, direct effects on vascular smooth muscle, and uterine. In this regard, they reduce blood pressure due to inhibition of the vasomotor center, and partly due to the blockade of adrenergic receptors of the vascular wall, as well as significantly more activity centers stimulate the vagus nerves. The least negative effect on the vascular wall and blood pressure has ergometrine, which is also approximately 3-4 times less toxic, than ergotoxine and ergotamine.
Ergot – Use in medicine
Ergot and its products are widely used in obstetric practice for uterine atony and associated uterine bleeding. Hemostatic effect of ergot drugs is mainly due to the compression of the walls of blood vessels while reducing the muscles of the uterus. In the postpartum period ergot drugs accelerate the regression of the uterus. Galenovo and novogalenovyh funds, prepared ergot, also used in menorrhagia (menstrual bleeding) and uterine bleeding, non-violation of the menstrual cycle.
Ergot alkaloid drugs have adrenolytic action, which is more pronounced in drugs, produced on the basis of hydrogenated alkaloids, who lose their selective effect on the uterus, but become hypotensive and sedative properties and are used in the neuroses, vascular spasm, hypertension and other diseases.
It was also found stimulating effect of hydrogenated ergot alkaloids to the process of blood coagulation.
Ergot – Contraindications and side effects
Ergot preparations are contraindicated in pregnancy and during delivery. The tonic contraction of muscles of the uterus can interfere with normal breathing and lead to asphyxia. Harmful use of ergot directly after birth, as the muscle spasm may prevent the separation of the placenta. Too prolonged use, sometimes with hypersensitivity to ergot drugs phenomenon can ergotism, associated with the narrowing of blood vessels and tissue malnutrition (especially the extremities), as well as mental disorders. Accidental or deliberate poisoning with large doses of ergot accompanied by painful abdominal pain and severe cramps, often death occurs. All preparations of ergot, as well as the whole horns, highly toxic, so it should only be used with a doctor's permission and under his control.
Ergot – Formulations, Dosing and Administration
Ergotal - The amount of ergot alkaloids in the form of phosphates. The powder is white or slightly brownish, water-soluble. The drug is available in tablets, containing 0,001 g (1 mg) total alkaloids, and a 0,05 % solution in ampoules 1 ml. Assign inside of 1 / 2-1 tablet 2-3 times a day, or under the skin and muscles of 0.5-1 ml (0,00025-0.0005 G ergotala).
Эrgometrina maleate - White or slightly yellow crystalline powder, odorless; uasteorim in iodine, it is soluble in alcohol, insoluble in ether and chloroform. Melting point 156-158 ° C.
Apply ergometrine maleate in obstetric practice for bleeding after manual removal of placenta, in the early postpartum hemorrhage, delayed involution of the uterus in the postpartum period, bleeding after cesarean section, when spotting after abortion.
Assign inside, intramuscularly and intravenously; the fastest and most powerful effect is observed when administered intravenously. A single dose when administered parenterally 0,0002 g (0,2 mg), the oral - 0,0002-0,0004 g (0,20.4 mg). In the postpartum period designate the interior of 0.2-0.4 mg 2-3 times a day until the disappearance of the risk of bleeding during --obychno 3 days; prolonged bleeding when administered once 0,2 mg vein or intramuscularly, then keep on giving the drug inside.
Ergometrine maleate is generally well tolerated; long prescribed the drug is not recommended; should be considered, that in some cases (in individuals with hypersensitivity) may develop phenomenon of ergotism.
The drug is available in tablets, containing 0,0002 g (0,2 mg) эrgometrina maleate, and ampoules 1 ml 0,02 % solution (0,2 mg).
Эrgotamina gidrotartrat used in obstetric practice for uterine atony, Postpartum hemorrhage, subinvolution uterus; gynecology - sometimes with uterine bleeding. Besides, ergotamine used for migraines. There is also evidence of its effectiveness in glaucoma.
Assign ergotamine atony of the uterus and incomplete abortion under the skin or intramuscular injection of 0.5-1 ml 0,05 % solution; emergency injected slowly into a vein 0,5 ml. If other indications designate the interior of 10-15 drops 0,1 % I-solution 3 times per day. When migraine recommend 15-20 drops a few hours before an expected attack; when administered to a migraine attack 0.5-1 mL intramuscularly.
Ergotamine should not be used for a long time; after 7 days of use in cases, requiring longer treatment, make a break (3-4 days).
"Belloid"Is available in tablets, containing 0,3 mg ergotoxine, 0,1 mg of total alkaloids of belladonna (belladonna) and 0,03 Mr. butiletilbarbiturovoy acid. Accepted at increased irritability, insomnia, Meniere's syndrome, neurodegenerative disorders, associated with menstrual irregularities, hyperthyroidism 1 tablet (drop) 3-6 Times per day.