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PubMed1979

Effect of ergotamine on cranial arteriovenous shunting in experiments with constant flow perfusion.

The effect of the antimigraine drug, ergotamine, was studied on the distribution of flow throughout the cranial microcirculation of the cat, using microspheres suitable in size to separate capillary flow from flow through the arteriovenous anastomoses. A constant flow perfusion experiment was used in order to eliminate the secondary effect of ergotamine on the microcirculation through a reduction in carotid blood flow per se. Under the experimental conditions, ergotamine decreased in a dose-dependent way the fraction of perfusion flow shunted through the arteriovenous anastomoses. This mode of action of ergotamine sheds new light on the so-called migraine shunt theory.

Animals↗
PubMed1984

Immunoassay of ergotamine and dihydroergotamine using a common 3H-labelled ligand as tracer for specific antibody and means to overcome experienced pitfalls.

A highly sensitive radioimmunoassay for the determination of ergotamine and dihydroergotamine is described. The limit of detection is about 9 pg/mL blood plasma for both compounds. The specificity of the gamma-globulin, which was prepared from rabbit antiserum, was investigated in the presence of compounds synthesized as possible metabolites. It was found that the tricyclic peptide moiety common to both molecules is an essential structural feature for binding to the gamma-globulin. From dilution experiments with the radioactively labelled compound it followed that ergotamine and to a lesser extent also its dihydro derivative are adsorbed on various tube wall materials using known buffer solutions. A practically insuperable obstacle is rearrangement of ergotamine under the experimental conditions, forming a stereoisomer by inversion at the C-8 position. The equilibrium of ergotamine in equilibrium ergotaminine found in human plasma remains stable under the incubation conditions of the radioimmunoassay.

Dihydroergotamine↗
PubMed1992

Identification and quantification of ergotamine in human plasma by gas chromatography-mass spectrometry.

A highly sensitive and simple gas chromatographic-mass spectrometric method is described for the identification and quantification of ergotamine in plasma or serum. Ergotamine is extracted with chloroform from the alkalinized sample and detected by electron ionization mass spectrometry. This analytical method was selected for an intense high-mass ion ideal for the specific quantification. It shows good linearity in the range from 50 pg/ml to 50 ng/ml for ergotamine in plasma. The practicability of this method is demonstrated by determining the plasma concentration of ergotamine in a sample from a patient.

Chloroform↗
PubMed1981

Plethysmographic comparison of sublingual and intramuscular ergotamine.

The peripheral vasoconstrictive effects of ergotamine, 0.25 mg intramuscularly and 2 mg sublingually, and a sublingual placebo were compared plethysmographically in 12 normal subjects. Both forms of ergotamine induced greater reductions than placebo in venous occlusion blood flow, systolic early ejection rate, systolic midtemporal ejection rate, systolic late runoff rate before aortic valve closure, diastolic runoff rate after aortic valve closure, and maximum and secondary pulse amplitudes. There were no significant differences between the ergotamine forms. The results indicate that the peripheral vasoconstrictive effects of ergotamine are equal after 0.25 mg intramuscularly and 2 mg sublingually. The two forms at those doses should be equally effective in migraine.

Administration, Oral↗
PubMed1992

Long-term ergotamine abuse: effect on adrenergically induced mydriasis.

The mydriatic action of sympathomimetic eyedrops after a therapeutic dose of ergotamine was measured in migraine patients with and without histories of long-term ergotamine abuse. Mydriasis induced by the postsynaptic alpha 1-agonist phenylephrine was similar in both groups of patients tested, whereas pupillary dilation caused by the release of noradrenaline tyramine was markedly greater in patients with histories of ergotamine abuse. The enhanced response to tyramine disappeared after drug withdrawal. These findings indicate that continuous ergotamine medication causes a reversible alterations in iris sympathetic transmission. This manifestation may reflect a central inhibition of pupillary sympathetic activity.

Adult↗
PubMed1973

Biosynthesis of ergotamine by Claviceps purpurea (Fr.) Tul.

High-yielding strains of Claviceps purpurea (Fr.) Tul, grown on a defined medium, have been used for a study of the biosynthesis of the peptide ergot alkaloid, ergotamine. l-[U-(14)C]tryptophan, dl-[2-(14)C]mevalonic acid lactone, sodium [2-(14)C]acetate, sodium [(14)C]formate and the methyl group of l-[methyl-(14)C]methionine were efficiently incorporated into the peptide alkaloids and specifically labelled the ergoline moiety of ergotamine. These results are the same as previously found for the biosynthesis of other ergot alkaloids. Time-course incubation experiments demonstrated that l-[U-(14)C]phenylalanine, l-[U-(14)C]proline and l-[U-(14)C]alanine were incorporated into the peptide ergot alkaloids. Chemical degradation of the radioactive alkaloid derived from additional precursor incubation experiments showed that phenylalanine and proline function as the most efficient precursors, and specifically label the constitutive side-chain phenylalanyl and prolyl moieties of the alkaloid. The evidence obtained from l-[U-(14)C]alanine-incorporation experiments was inconclusive. However, degradation of ergotamine isolated after incubation with dl-[1-(14)C]alanine, showed that the carboxyl group of the labelled amino acid was specifically incorporated into the alpha-hydroxy-alpha-amino acid residue of the alkaloid. This, in conjunction with the l-[U-(14)C]alanine-incorporation results, showed conclusively that all three carbon atoms of alanine were incorporated as a biosynthetic unit into the alpha-hydroxy-alpha-amino acid moiety of ergotamine.

Acetates↗
PubMed1983

General and regional haemodynamic effects of intravenous ergotamine in man.

The effect of intravenous ergotamine on general (blood pressure and cardiac output) and regional (splanchnic, renal and muscular) haemodynamics was studied immediately and 3 h after administration in seven male volunteers. Also plasma catecholamines were determined. An increase in blood pressure with a peak just after administration was observed. The cardiac output was unchanged and the pressor effect of ergotamine was due to an increase in total peripheral resistance. Plasma noradrenaline decreased 65% at the peak of the pressor effect whereas plasma adrenaline was unchanged. Hepatic blood flow decreased 34% just after ergotamine administration and was normal after 3 h. Renal blood flow decreased by 29 and 19%. Calf blood flow was unchanged. These results suggest that different vascular beds in man react differently to ergotamine.

Adult↗
PubMed1981

Effects of 5-hydroxytryptamine and ergotamine on human superficial temporal artery.

Isometric tension was recorded in ring preparations of human superficial temporal arteries contracted by noradrenaline (NA), 5-hydroxytryptamine (5-HT), and ergotamine. In contrast to NA and 5-HT, ergotamine induced long-lasting contractions refractive to additional stimulations and resistant to repeated wash-out. When tested against 5-HT, ergotamine acted as a non-competitive antagonist. When repeating the 5-HT stimulations (4.7 x 10(-5) M) the contractile response decreased indicating tachyphylaxis to this agent. As ergotamine revealed both a vasoconstrictive and a 5-HT-blocking activity, the beneficial effect in migraine may be by an interference during both the vasoconstrictory and vasodilatory phases.

Adult↗
PubMed1993

Placebo-controlled clinical trials with ergotamine in the acute treatment of migraine.

Although oral ergotamine alone or in combination with caffeine is widely used for the acute treatment of migraine, there is little evidence that it is significantly more effective than placebo. There are no placebo-controlled data to support the use of aerosol or suppository formulations. In addition, the recommended doses of ergotamine cannot be justified. Each formulation of ergotamine now should be tested in clinical studies performed according to the IHS criteria for trial design and in migraine patients fulfilling the diagnostic criteria of the IHS. Until these clinical data are available, no clear recommendations can be given for the use of ergotamine in the acute treatment of migraine.

Adolescent↗
PubMed1996

Side effects of ergotamine.

Ergotamine has been used for many years in the treatment of migraine, although there is little formal clinical evidence that it is significantly more efficacious than placebo. A number of side effects associated with ergotamine have been reported in the literature, including myocardial infarction, ischaemia of limb extremities, and fibrotic changes. Long-term use has led to reported cases of ergotamine-induced headache, vascular reactivity, and subclinical ergotism. When the safety profile of this drug is considered, coupled with its debatable efficacy from a clinical review previously published, the resulting poor risk:benefit ratio brings into question the continued use of ergotamine as a migraine treatment and calls for better controlled trials of its efficacy, or lack of, in the acute treatment of migraine.

Adverse Drug Reaction Reporting Systems↗
PubMed1997

Peripheral vascular effects and pharmacokinetics of the antimigraine compound, zolmitriptan, in combination with oral ergotamine in healthy volunteers.

Members of the new class of antimigraine compounds, 5HT1B/1D agonists, as well as ergotamine, may cause vasoconstriction through stimulation of 5HT receptors on peripheral vessels. The cardiovascular effects of 20 mg oral zolmitriptan (Zomig, formerly 311C90), 2 mg oral ergotamine and the combination were assessed in a randomized double-blind, placebo-controlled crossover study in 12 healthy subjects. Pharmacodynamic measures included oscillometric blood pressure, systolic blood pressure at the toe and arm using a strain gauge technique, stroke volume and cardiac output using bioimpedance cardiography, high-resolution ultrasound to measure brachial arterial diameter and a novel Doppler method to measure blood flow velocity. Both drugs produced small degrees of peripheral vasoconstriction, including increases in diastolic blood pressure and blood flow velocity and decreases in arterial diameter and toe-arm systolic pressure gradient. These effects were generally additive with the combination but of no clinical importance. There were no significant changes in cardiac output, stroke volume heart rate or ECG. Zolmitriptan, at eight times the likely therapeutic dose, was generally well tolerated both alone and in combination with ergotamine. Ergotamine had no clinically important effects on zolmitriptan pharmacokinetics.

Administration, Oral↗
PubMedDate not supplied

Headache caused by a sphenoid mucocele but presenting as an ergotamine-induced headache.

In a 65-year-old woman, symptomatic headache caused by a mucocele of the sphenoid sinus led to ergotamine abuse and subsequent ergotamine-induced headache. Since there were no neurological symptoms initially and the patient previously suffered from migraine, the mucocele was not recognized. Only after unsuccessful drug withdrawal therapy and an MRI, was the correct diagnosis made. Surgical removal of the mucocele led to complete relief of headache within 3 weeks. We conclude that ergotamine-induced headache can develop on the basis of symptomatic headache. In spite of the effectiveness of ergotamine tartrate, an MRI should be performed if focal neurological symptoms occur.

Aged↗
PubMed2000

Limb-threatening ischemia due to ergotamine: case report with angiographic evidence.

A 29-year-old woman presented with severe leg pain that had lasted for several weeks. During that period, she had taken painkillers in order to achieve sleep. In the week before she was admitted to hospital, she had noticed numbness and a cold feeling below her knees. There were no arterial pulsations below her groin, the skin of her legs being cold and pale. She had a history of chronic daily headache and had ingested Cafergot compound corresponding to ergotamine 2 to 3 mg daily for the previous 2 or 3 months. Angiography demonstrated severe narrowing of both superficial femoral arteries for a distance of about 5 to 6 cm and a subtotal stenosis of the right popliteal artery. After discontinuation of ergotamine, the patient's symptoms gradually disappeared within a few days. Angiography was repeated 2 days after the first examination and demonstrated regression of the spasms in the femoral arteries and reestablished flow in the distal vessels. Ergotamine tartrate can induce life-threatening ischemia of an extremity. Discontinuation of ergotamine is usually sufficient to reverse the ischemia, however, intravenous infusion of sodium nitroprusside may occasionally be necessary to avoid limb amputation.

Adult↗
PubMed2003

Ergotamine and dihydroergotamine: history, pharmacology, and efficacy.

Ergotamine and dihydroergotamine share structural similarities with the adrenergic, dopaminergic, and serotonergic neurotransmitters. As a result, they have wide-ranging effects on the physiologic processes that they mediate. Ergotamine and dihydroergotamine are highly potent at the 5-HT1B and 5-HT1D antimigraine receptors and, as a consequence, the plasma concentrations that are necessary to produce the appropriate therapeutic and physiologic effects are very low. The broad spectrum of activity at other monoamine receptors is responsible for their side effect profile (dysphoria, nausea, emesis, unnecessary vascular effects). Both ergotamine and dihydroergotamine have sustained vasoconstrictor actions. In acute migraine treatment, their mechanisms of action involve constricting the pain-producing intracranial extracerebral blood vessels at the 5-HT1B receptors and inhibiting the trigeminal neurotransmission at the peripheral and central 5-HT1D receptors. The scientific evidence for efficacy is stronger for dihydroergotamine than for ergotamine. Their wide use is based on long-term experience.

Animals↗
PubMed2005

Growth and hepatic in vitro metabolism of ergotamine in mice divergently selected for response to endophyte toxicity.

This study investigated if genetic differences exhibited in endophyte-resistant and -susceptible mouse lines had persisted after 13 generations in which the integrity of lines was maintained yet selection ceased. Experimental groups were mouse lines fed an endophyte-free (E-) or -infected (E+) diet. The in vitro metabolism of the ergot alkaloid ergotamine in mouse liver microsomes was characterized by LC-MS/MS and compared between both lines before and after exposure to E+ feed. No difference in the average daily weight gain of pups between resistant and susceptible mice was observed on the E+ diet. Thus, for the weight gain selection criterion under study, the difference established between the two lines appears not to have persisted over the extended period of relaxed selection. Microsomal incubations produced nine predominate peaks in the HPLC assay. The peaks were confirmed by LC-MS/MS to be ergotamine, ergotamine epimer, monohydroxylated metabolites (M1, M2, M1e, M2e) and dihydroxylated metabolites (M3--5). A gender difference for metabolite formation was observed on the E- diet, in that females produced a greater amount of M1, M1e and M3--5 than males. When challenged with the E+ diet, mice showed differences in concentration of M3 for line (resistant > susceptible) and gender (female > male) and of M4 and M5 for gender (female > male). Gender differences in the metabolism of ergotamine have not been shown before in these lines of mice or other species used to study ergot alkaloid metabolism. This adds a potential source of variation in the susceptibility to fescue toxicity not explored previously and would be of value to investigate further.

Animal Feed↗
PubMed1999

Molecular characterization of high affinity, high capacity clays for the equilibrium sorption of ergotamine.

Ergot alkaloids (mycotoxins) produced by Claviceps and Neotyphodium species of fungi may contaminate animal feedstuffs and results in disease in livestock. In this study, diverse phyllosilicate clays and other adsorbent materials, differing in chemical and structural characteristics, were tested for their ability to sorb ergotamine, a prevalent ergot mycotoxin, from acidic solution. Results indicated minimal binding to those sorbents possessing low surface area, cation exchange capacity and inaccessible interlayer regions. Cetyl pyridinium-exchanged montmorillonite (organoclay) exhibited decreased propensity for ergotamine in acidic solution as compared with the unexchanged hydrophilic parent clay. The highest ergotamine sorption was observed with cation exchanged montmorillonite clays; whereas, when collapsed, these same clays sorbed very little ligand. Based on initial binding experiments, calcium and sodium montmorillonite clays were prioritized for further characterization, including: capacity, affinity, and heat (enthalpy) of adsorption. Computer models of energy-minimized ergotamine isomers and clay were used to illustrate possible mechanisms of ergot alkaloid sorption at interlayer sites. Additional studies are warranted to assess the stability of ergot alkaloid/clay complexes under alkaline conditions to further understand the mechanism of adsorption.

Adsorption↗
PubMed2000

Ergotamine in the acute treatment of migraine: a review and European consensus.

Ergotamine has been used in clinical practice for the acute treatment of migraine for over 50 years, but there has been little agreement on its place in clinical practice. An expert group from Europe reviewed the pre-clinical and clinical data on ergotamine as it relates to the treatment of migraine. From this review, specific suggestions for the patient groups and appropriate use of ergotamine have been agreed. In essence, ergotamine, from a medical perspective, is the drug of choice in a limited number of migraine sufferers who have infrequent or long duration headaches and are likely to comply with dosing restrictions. For most migraine sufferers requiring a specific anti-migraine treatment, a triptan is generally a better option from both an efficacy and side-effect perspective.

Analgesics, Non-Narcotic↗
PubMed1999

Mortality of horn fly larvae (Diptera: Muscidae) in bovine dung supplemented with ergotamine and N-formyl loline.

Dung-dwelling larvae of ectoparasites of livestock such as the horn fly, Hematobia irritans (L.), may be exposed to > or = 1 different alkaloid species in dung from animals ingesting herbage of the tall fescue (Festuca arundinacea Schreb.)--endophyte association (Neotyphodium coenophialum (Morgan-Jones & W. Gams) Glenn, Bacon & Hanlin comb. nov.). First-instar horn flies were exposed to bovine dung supplemented with up to 50 microM each of N-formyl loline and ergotamine tartrate in factorial combination. In the absence of ergotamine tartrate, N-formyl loline caused a linear decline in the number of pupae recovered, and probit analysis indicated an LC50 of 36 microM. In the absence of N-formyl loline, significant quadratic responses of larvae to ergotamine tartrate were established, and probit analysis indicated a LC50 of 34 microM. An interaction (P < 0.001) was found between the 2 alkaloids for larval survival. This interaction showed that ergotamine tartrate moderated the toxicity of N-formyl loline and indicates that a membrane-bound receptor may be involved. There was no evidence of carryover of effects of alkaloids on subsequent stages of development or expressed as abnormalities of pupae or adults. Interactions between alkaloids probably are involved in other plant-herbivore relationships of endophyte-infected grasses.

Alkaloids↗