Ergotamine: Effects, Uses & Risks

Ergotamine, derived from ergot, is used to treat certain types of headaches (migraines, for example). Taking it constricts blood vessels in the brain and affects certain receptors.

What is ergotamine?

Ergotamine, derived from ergot, is used to treat certain types of headaches (eg, migraines). Ergotamine belongs to a group of medications called ergot alkaloids. Its use causes blood vessels in the area around the brain to constrict. Ergotamine also affects patterns of blood flow that are responsible for certain types of headaches. For example, the drug is used to treat migraines. However, ergotamine is used only in acute cases of already established migraine. It does not have any effect on the prevention of migraine nor does it reduce the number of migraine attacks. Ergotamine should not be used in the treatment of normal headaches caused by stress or exertion, nor for pain that is different from the regular migraine attacks. Ergotamine is obtained from ergot, which likewise has been used in medicine since the 16th century.

Pharmacological action

The effects of ergotamine on the body are very complex. The molecules of the drug share structural similarities with neurotransmitters such as serotonin, dopamine, ephedrine, can bind them to different receptors and act as their counterpart. The successful effect against migraine occurs through constriction of intracranial extracerebral blood vessels of 5-HT1B receptor and inhibition of trigeminal neurological transmission through 5-HT1D receptor. Ergotamine also has an effect on the receptors for dopamine and norepinephrine. The effects on D2 dopamine and the 5-HT1A receptor may cause some side effects.

Medical application and use

Ergotamine is used to treat certain types of headache (eg, migraine). It constricts certain blood vessels in the head, thereby relieving the painful symptoms. For acute treatment, a pill should be placed under the tongue as described by the doctor to dissolve slowly. The pill should not be chewed or swallowed, nor should it be combined with food or liquids while it dissolves in the mouth. Dosage depends on the type of headache and the individual’s response to the medication. Ergotamine works best when taken at the first signs of an attack starting. If the headache is already very advanced, the drug may not work completely. Ergotamine should be used only when needed. It is not intended for prolonged and daily use. The maximum dosage is 3 tablets in 24 hours and 5 tablets in 7 days. Ergotamine may cause withdrawal symptoms, especially if it has been taken regularly for a long time. In these cases, headaches begin as soon as the drug is discontinued. These headaches are likely to be different from normal headaches and may last for several days. Such symptoms should be reported to the treating physician as soon as possible. The doctor should already be informed if extreme use of ergotamine becomes noticeable, the drug no longer works successfully, the headaches become more severe or increase in frequency, or ergotamine is used for more than two attacks per week. In this case, another medication may need to be prescribed.

Risks and side effects

Dizziness and vomiting may start when taking ergotamine. If these side effects persist or worsen, a doctor should be consulted as soon as possible. The treating physician prescribed ergotamine because he or she believed that the risk of possible side effects was less than the successful effect of the drug. Many patients do not notice any side effects. A doctor should be sought quickly if the following rare but possible side effects begin: slowed or accelerated pulse; tingling or coldness in fingers or toes; blue fingers or hands with onset of numbness; muscle pain and physical weakness; severe stomach pain; lower back pain; little or no urine. Emergency medical attention should be alerted if significant chest pain sets in; blurred vision; confusion; or slurred speech.Breathing problems or a sudden onset of a rash can be signs of an allergic reaction. In this case, the emergency physician should also be alerted.