Chemical diagram hereŠDescription:
Methysergide is an oral, synthetic ergot alkaloid, structurally related to the oxytocic agent methylergonovine and to the potent hallucinogen LSD. Methysergide is used prophylactically to reduce the frequency and intensity of severe vascular headaches. Although methysergide is an ergot alkaloid, it is a weak vasoconstrictor and oxytocic. Methysergide is a more potent antagonist of peripheral serotonin receptors than other ergot alkaloids. Although methysergide and sumatriptan both stimulate serotonin receptors centrally, methysergide is intended for prophylaxis while sumatriptan is indicated for treatment of an acute attack. Methysergide was approved by the FDA in 1962.
Mehtysergide can inhibit the positive inotropic and chronotropic effects mediated by 5-HT peripherally. Vascular insufficiency can exacerbate coronary artery disease or angina contraindicating use of methysergide. Vascular insufficiency also contraindicates use of methysergide when the patient has an existing peripheral vascular disease, severe arteriosclerosis, collagen-vascualr disease, thrombophlebitis, severe hypertension (although 5-HT normally does not regulate blood pressure, methysergide can exacerbate hypertension in certain patients), or sepsis. Elderly patients should be treated with caution as they are more likely to have peripheral vascular disease and to be more affected by the vasoconstrictive actions of methsergide than younger patients.
Methysergide can interact with nicotine by adding to its vasoconstricting effect, thus increasing the risk of developing peripheral vascular ischemia. Patients who are receiving methysergide should avoid tobacco smoking.
Methysergide can cause fibrotic changes and can produce inflammatory fibrosis. Use of methysergide is contraindicated in patients with existing pulmonary disease, rheumatoid arthritis, or valvular heart disease. Use of methysergide in children is contraindicated because it can cause pulmonary fibrosis.
Ergot alkaloids are excreted into breast milk. They inhibit lactation and can cause symptoms of ergot poisoning in infants. Use of methysergide during breast-feeding is contraindicated.
Methysergide use during pregnancy has not been evaluated. Ergot alkaloids and related compounds, however, are generally rated pregnancy category X because of their oxytocic potential, so use during pregnancy is contraindicated.
Patients with hepatic disease who receive methysergide can develop symptoms of ergot poisoning because of impaired hepatic metabolism.
Methysergide can increase gastric hydrochloric acid concentration, so its use is contraindicated in patients with peptic ulcer disease.
Use of methysergide in patients with renal disease is contraindicated.
Commercial preparations contain tartrazine dye and should be used with caution in patients with tartrazine dye hypersensitivity. Patients with aspirin hypersensitivity are more likely to be at risk.
Methysergide, combined with other ergot alkaloids, increases the possibility of ergot toxicity.
Methysergide produces a wide variation in sensitivity to vasoconstrictor effects, but these effects can be additive with concurrent use of cocaine, epinephrine, methoxamine, norepinephrine, or phenylephrine.
Methysergide can interact with nicotine by adding to its vasoconstricting effect, thus increasing the risk of developing peripheral vascular ischemia.
Inflammatory fibrosis is a rare, but potentially serious, adverse reaction associated with prolonged use of methysergide. Retroperitoneal fibrosis, pulmonary fibrosis, or fibrosis in cardiac tissue can occur. Drug withdrawal usually reverses the condition, so treatment should be interrupted for at least a 3-week interval every 6 months. Occasionally, cardiac valvular damage can be irreversible.
Adverse GI effects are common during therapy with methysergide and include nausea/vomiting, diarrhea, pyrosis (heartburn), and abdominal pain. Gradual dosage increase and administration with food help to minimize these reactions.
Ischemia, resulting from peripheral vasoconstriction or vasospasm during therapy with methysergide, can manifest as itching; numbness or tingling of fingers, toes, or face; limb pain; cold hands/feet; or leg weakness. Drug withdrawal is indicated if there are signs of impaired circulation. Vasoconstriction also can precipitate chest (angina) or abdominal pain.
Methysergide is structurally similar to the hallucinogen lysergic acid diethylamide (LSD). Mild CNS stimulation, mild CNS depression, or even an LSD-like reaction can occur during therapy with methysergide.
Methysergide exerts more potent peripheral antagonism of serotonin (especially in smooth muscle) than other ergot alkaloids. Orthostatic hypotension can occur during therapy with methysergide. Sinus tachycardia has also been reported.
Rebound headaches can occur if methysergide is abruptly withdrawn. A gradual withdrawal over 2--3 weeks is recommended.
Other adverse reactions reported with methysergide include weight gain, weakness, myalgia, and arthralgia. Neutropenia and eosinophilia have rarely been reported.
What do methysergide tablets do?
METHYSERGIDE (Sansert®) is one of a group of medicines known as ergot alkaloids. Methysergide helps to prevent certain kinds of throbbing headaches such as migraine and cluster headaches. It is not helpful once the headache has started. Generic methysergide tablets are not yet available.
What should my health care professional know before I take methysergide?
They need to know if you have any of these conditions:
How should I take this medicine?
Take methysergide tablets by mouth. Follow the directions on the prescription label. Swallow the tablets with a drink of water. It is best to take methysergide with food. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your doctor's advice.
Special precautions for use in children: This medicine is not for children.
What if I miss a dose?
If you miss a dose, skip that dose. Return to your normal schedule. Do not take double or extra doses.
What other medicines can interact with methysergide?
Tell your doctor or pharmacist: about all other medicines you are taking, including non-prescription medicines; if you are a frequent user of drinks with caffeine or alcohol; if you smoke; or if you use illegal drugs. These may affect the way your medicine works. Check before stopping or starting any of your medicines.
What side effects may I notice from taking methysergide?
Serious side effects with methysergide include:
Call your doctor as soon as you can if you get any of these side effects.
Minor side effects with methysergide include:
Let your doctor know about these side effects if they do not go away or if they annoy you.
What do I need to watch for while I take methysergide?
Check with your doctor if you do not get relief from your headaches after the first 3 weeks. Carrying on taking methysergide will not be likely to help.
It is important to tell your doctor as soon as you can if you get any of the following side effects: cold, numb, or painful hands or feet; leg cramps when walking; any type of pain around your chest, stomach or in your side.
Methysergide decreases the circulation of blood to your skin, fingers, and toes. You may get more sensitive to the cold. Elderly patients are more likely to feel this effect. Dress warmly and avoid long exposure to the cold.
You may get dizzy or drowsy. Do not drive, use machinery, or do anything that needs mental alertness until you know how methysergide affects you. To reduce the risk of dizzy or fainting spells, do not stand or sit up quickly, especially if you are an older patient.
Alcohol can make headaches worse or bring on a new headache. Avoid alcoholic drinks. Smoking can increase side effects of methysergide; avoid smoking.
After 6 months of treatment you must give your body a 3 to 4 week rest period without methysergide. Before you stop taking this medicine you must gradually reduce the dose over 2 to 3 weeks so that you do not get a headache rebound effect. Ask your doctor for a schedule.
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 15 and 30°C (59 and 86°F). Keep container tightly closed.
Relative Drug Costs
Total Cost of Therapy
Available as 2 mg of methysergide maleate.