Dihydroergotamine (Dihydroergotaminum) (DHE) is an ergot alkaloid used to treat migraine. This is a derivative of ergotamine. Dihydroergotamine - alpha-blocker. Available in the form of methanesulfonate (mesylate). It is applied as a nasal spray or injection and has an efficacy similar to that of sumatriptan. Nausea is a common side effect.
It acts similarly to triptans, acting as an agonist of serotonin receptors and causing vasoconstriction of intracranial blood vessels, but also centrally interacts with dopamine and adrenergic receptors. It can be used for the treatment of acute irresistible headache or refusal of analgesics.
Content
Medical use
Subcutaneous and intramuscular injections are generally more effective than the nasal spray, and patients can take them on their own. Intravenous injection is considered very effective in severe migraine or migraine status. DHE is also used to treat headache with excessive use of medications.
Side Effects
When taking the drug inside possible nausea, vomiting, weakness, drowsiness, in rare cases - paresthesia, diarrhea. With parenteral administration and hypersensitivity, the possibility of a collaptoid reaction should be considered. After intramuscular injections, the patient must be in a supine position for some time. Nausea is a common side effect of intravenous administration and is less common in other regimens. Antiemetics can be given before DHE to counteract nausea. Risks and contraindications are similar to triptans. DGE and triptans should never be taken within 24 hours of each other due to possible coronary artery spasm. DHE is not addictive.
Mechanism of Action
The antimigraine activity of DHE is due to its action as an agonist of serotonin receptors (5-HT) -1B, -1D and -1F. It also interacts with other serotonin, adrenergic and dopamine receptors. The main pharmacological properties of the drug is a-adrenoblokiruyuschaya activity, extending to a1- and a2- adrenergic receptors . It has affinity for various types of serotonin receptors. [one]
Indications for use
Applied mainly for migraine , Raynaud's disease and other peripheral circulatory disorders.
Release form
Available for ingestion in the form of a solution containing in 1 ml 0.002 g (2 mg) of dihydroergotamine methanesulfonate, as well as tablets containing 0.0025 g (2.5 mg) of the drug, and for injection in 1 ml ampoules containing 0.001 g (1 mg) of the drug.
Dosing regimen
It is usually taken orally with 10-20 drops (1/2 cup of water) 1-3 times a day. In severe forms of migraine is administered immediately after the first signs of 1 ml intramuscularly, and, if necessary, administered in the same dose again. For the prevention of migraine and headache of vascular genesis, take 1 tablet (2.5 mg) in the morning and evening or 20 drops of a 0.2% solution (2 mg) 2-3 times a day. The optimal dose is selected individually.
Contraindications
The drug is contraindicated in hypotension, severe atherosclerosis , organic heart disease, angina , impaired liver and kidney function, in old age, as well as during pregnancy and breastfeeding of the child.
History
Dihydroergotamine (DHE) is a semi-synthetic form of ergotamine approved in the United States in 1946.
Society and Culture
Accessibility
Oral bioavailability is poor and not available orally in the United States. DHE is available as a nasal spray and in ampoules for subcutaneous, intramuscular and intravenous injections. Efficacy varies in the form of a nasal spray with a bioavailability of 32% from injecting.
European Union
In 2013, the European Medicines Agency for Human Medicines (CHMP) Committee recommended that drugs containing ergot derivatives should no longer be used to treat a number of conditions related to problems with memory, sensation or circulation, or to prevent migraine due to the risk of (increased risk of fibrosis and ergotism), reportedly higher than the benefit of these indications.
Synonyms
Ditamin, Klavivrenin, Agit, Angionorm, Clavigrenin, Cornhidral; DH-Ergotamin, Diergotan, Diidergot, Dihydergot, Dihydroergotamine mesilate, Dihytamin, Ditamin, Ergomimet, Ergovasan, Ikaran, Migretil, Migrifen, Tonopress, Vasogin, Verteblan, etc.