Pharmacokinetics of methysergide and its metabolite methylergometrine in man

  title={Pharmacokinetics of methysergide and its metabolite methylergometrine in man},
  author={Ulf Bredberg and G. S. Eyjolfsdottir and Lennart K. Paalzow and Peer Tfelt-Hansen and V. Tfelt-Hansen},
  journal={European Journal of Clinical Pharmacology},
SummaryFive healthy men were given 1.0 mg methysergide maleate intravenously and 2.7 mg methysergide maleate orally in a cross-over study.The systemic availability of methysergide was only 13%, most probably due to a high degree of first-pass metabolism to methylergometrine. We also found evidence of extrahepatic clearance of methysergide.After oral administration the plasma concentrations of the metabolite were considerably higher than those of the parent drug and the area under the plasma… 

Variation in Bioavailability of Oral Methylergometrine in Healthy Male Volunteers

This study with oral methylergometrine demonstrated such large interindividual variability in bioavailability that from a pharmacokinetic point of view the oral route of administration does not appear to be the most reliable way for accurate dosing in the prevention of postpartum haemorrhage.

Pharmacokinetics and bioavailability of oral ergometrine in male volunteers

This study with oral ergometrine shows such a large interindividual variability in bioavailability that the oral route of administration does not seem not to be the most reliable means of accurate dosing in preventing post‐partum haemorrhage.

Comparison of Pharmacodynamic Effects and Plasma Levels of Oral and Rectal Ergotamine

It is suggested that a rectal dose of 1 mg ergotamine tartrate should be tried as the initial dose in the treatment of migraine attacks because it is more biologically active, for the factor used, than oral ergotamines.


Methysergide can induce retroperitoneal fibrosis and pleural and heart valve fibrosis with an estimated incidence of 1 in 5,000 treated patients, therefore, it should be reserved for severe cases in which other migraine preventive drugs are not effective.

Methylergometrine antagonizes 5 HT in the temporal artery

It is suggested that methylergometrine is the “active” drug when methysergide is used in migraine prophylaxis, and that the two compounds should be compared in Prophylactic trials in migraine.

History of Methysergide in Migraine

The rise, fall and subsequent use of methysergide as a third-choice drug of the first effective migraine prophylactic, methylergometrine, is described.

Efficacy and tolerability of intravenous methylergonovine in migraine female patients attending the emergency department: a pilot open-label study

The data suggest that intravenous methylergonovine can be an effective and safe drug in the management of severe migraine attacks in the emergency room.

Neural and cardiac toxicities associated with 3,4-methylenedioxymethamphetamine (MDMA).

Serotonergic drugs and valvular heart disease

A more likely cause of fenfluramines-induced valvulopathy is activation of 5-HT2B receptors on heart valves by the metabolite norfenfluramine, and future serotonergic medications should be designed to lack 5- HT2B agonist activity.



Metabolism of methysergide and retroperitoneal fibrosis.

Subjects and patients did not differ in regard to serum radioactivity data or urinary excretion of total radioactivity and methysergide radioactivity, and excreted radioactive carbon dioxide into the expired air at similar rates, suggesting that both groups were able to demethylate methysERGide to form methergine.

Metabolite pharmacokinetics: The area under the curve of metabolite and the fractional rate of metabolism of a drug after different routes of administration for renally and hepatically cleared drugs and metabolites

  • K. Pang
  • Biology, Medicine
    Journal of Pharmacokinetics and Biopharmaceutics
  • 2005
A model includes renal and hepatic eliminatory mechanisms for both drug and metabolite as long as the metabolite is formed only by the liver, and it is found that when competing renal eliminatory pathways exist for a drug, the area under the curve for the metabolites will change according to the route of drug administration.

Determination of ergot alkaloids in plasma by high-performance liquid chromatography and fluorescence detection.

  • P. Edlund
  • Chemistry
    Journal of chromatography
  • 1981

Ergot Alkaloids and Related Compounds

I Introduction to the Pharmacology of Ergot Alkaloids and Related Compounds as a Basis of Their Therapeutic Application and theories on the Mechanism of Noradrenaline "Overflow".

Introduction to the Pharmacology of Ergot Alkaloids and Related Compounds as a Basis of Their Therapeutic Application

This chapter, rather unorthodox for a volume of the Handbook of Experimental Pharmacology, is an attempt at a compact synopsis to help those teaching pharmacology or writing a textbook of pharmacology not to overlook the essential chemical and biological basis of the therapeutically most important compounds and those of their activities which are believed to be relevant for their therapeutic effects.