Ergotamine and dihydroergotamine: A review

Abstract

The ergot alkaloids were the first specific antimigraine therapy available. However, with the advent of the triptans, their use in the treatment of migraine has declined and their role has become less clear. This review discusses the pharmacology, efficacy, and safety of the ergots. In randomized clinical trials, oral ergotamine was found to be superior to placebo, but inferior to 100 mg of oral sumatriptan. In contrast, rectal ergotamine was found to have higher efficacy (73% headache relief) than rectal sumatriptan (63% headache relief). Intranasal dihydroergotamine was found to be superior to placebo, but less effective than subcutaneous and intranasal sumatriptan. Ergotamine is still widely used in some countries for the treatment of severe migraine attacks. It is generally regarded as a safe and useful drug if prescribed for infrequent use, in the correct dose, and in the absence of contraindications; however, safer and more effective options do exist in the triptans. In patients with status migrainous and patients with frequent headache recurrence, ergotamine is still probably useful.

Acute treatment of migraine headache

“…• [22]. • After a single dose of ergotamine or DHE, the side effects include nausea and vomiting, abdominal discomfort, acroparaesthesia, and leg cramps [22].…”

“…• After a single dose of ergotamine or DHE, the side effects include nausea and vomiting, abdominal discomfort, acroparaesthesia, and leg cramps [22]. In patients with ischemic heart disease, ergotamine, given in therapeutic doses, has in a few cases caused variant angina, myocardial infarction, and cardiac arrest [22]. After chronic daily intake, unwanted symptoms include those attributable to vasospasm (such as intermittent claudication) and ergotamine-induced headache.…”

“…• Contraindications for DHE and ET are a consequence of their adverse effect profiles and include pregnancy, renal or hepatic failure, coronary, cerebral, and peripheral vascular disease, hypersensitivity reactions, sepsis, and uncontrolled hypertension [22]. These drugs should not be given to patients likely to have asymptomatic coronary artery disease based on their risk factor profiles, without an adequate workup.…”

Ergotamine and nicergoline – Facts and myths

“…One of the major chemical compounds responsible for the condition's observed effects was ergotamine. This compound was launched as a sympatholytic drug for migraine therapy in 1926 [1]. Nicergoline Ergotamine Valvunopathy 5-HT 2B agonism Biased signaling A B S T R A C T Ergotamine, being a representative of naturally occurring ergoline alkaloids, derived from D-lysergic acid, and nicergoline, a D-lumilysergic acid derivative belonging to semi-synthetic ergot-derived alkaloids, display diversified affinity for adrenergic, serotoninergic, and dopamine receptors.…”

“…In neurology, ergotamine tartrate was introduced for the treatment of vascular headaches, which are currently termed migraines or cluster headaches. Since then, the drug has consistently proven to be effective in the treatment of moderate to severe migraines [1].…”