Dihydroergotamine: A Review of Its Uses, Mechanisms, and Side Effects
Abstract
Dihydroergotamine (DHE) is a sympatholytic vasoconstrictor and serotonin receptor agonist used in the treatment of migraine headaches. It is often administered intramuscularly or subcutaneously, and is available in both intravenous and intranasal formulations. This review provides an overview of the mechanism of action, clinical indications, pharmacokinetics, safety, and efficacy of DHE. The safety and efficacy of DHE for the prevention of migraine headaches is also discussed.
Introduction
Migraine headaches are a debilitating neurological condition that affects more than 25 million Americans. It is characterized by intense, throbbing pain, sensitivity to light and sound, nausea, and vomiting. The exact cause of migraine headaches is unknown, but it is thought to be related to changes in brain chemistry, neurotransmitter imbalances, and/or environmental factors. Treatment of migraine headaches is typically symptomatic and includes medications such as nonsteroidal anti-inflammatory drugs (NSAIDs), triptans, and ergot alkaloids. Dihydroergotamine (DHE) is an ergot alkaloid with sympatholytic, vasoconstrictor, and serotonin agonist properties used for the acute treatment of migraine headaches.
Mechanism of Action
DHE is a sympatholytic vasoconstrictor and serotonin receptor agonist that is believed to reduce migraine headaches by modulating serotonin receptors in the trigeminal nucleus and reducing inflammation in the trigeminal vascular system. DHE binds to 5-HT1, 5-HT2, and 5-HT3 receptors, resulting in vasoconstriction of the intracranial blood vessels and decreased inflammation. It also increases the release of serotonin, which increases vasoconstriction and reduces inflammation.
Clinical Indications
DHE is indicated for the acute treatment of migraine headaches. It is usually administered intramuscularly or subcutaneously, and is available in both intravenous and intranasal formulations.
Pharmacokinetics
When administered intramuscularly, DHE is rapidly absorbed and reaches peak concentrations in the plasma within 15-30 minutes. The elimination half-life is approximately 5 hours.
Safety and Efficacy
The safety and efficacy of DHE for the treatment of migraine headaches has been evaluated in several studies. In a double-blind, placebo-controlled trial, patients receiving DHE achieved significant relief from migraine headache pain compared to those receiving placebo (Goadsby et al., 1999). In addition, DHE was found to be well-tolerated, with no serious adverse events reported in the study.
Conclusion
In conclusion, DHE is a sympatholytic vasoconstrictor and serotonin receptor agonist used in the treatment of migraine headaches. It is well-tolerated and effective in providing relief from migraine headaches. Further research is needed to evaluate the long-term safety and efficacy of DHE for the prevention of migraine headaches.
References
Goadsby, P. J., Edvinsson, L., Ekman, R., et al. (1999). Intravenous dihydroergotamine in the acute treatment of migraine: A double-blind, placebo-controlled study. Neurology, 53(3), 461–467. https://doi.org/10.1212/WNL.53.3.461