Long-term Ergotamine Derivative Therapy for Migraine Associated with Pachymeningitis and Sixth Cranial Nerve Palsy
What is the long-term ergotamine derivative therapy for migraine associated with pachymeningitis and sixth cranial nerve palsy. How does it work? What are the side effects? Who should not use it?
Understanding Ergotamine Derivatives
Ergotamine derivatives, such as dihydroergotamine and ergotamine, are a group of headache medications that have been used to treat severe, throbbing headaches like migraines and cluster headaches since the 1940s. These drugs work by narrowing blood vessels in the brain, affecting the levels of the chemical messenger serotonin, and preventing the trigeminal nerve from releasing proteins that cause inflammation.
Ergotamine Derivative Therapy for Migraine with Pachymeningitis and Sixth Cranial Nerve Palsy
In cases where a patient experiences migraine associated with pachymeningitis (inflammation of the dura mater) and sixth cranial nerve palsy (paralysis of the abducens nerve), long-term ergotamine derivative therapy may be considered as a treatment option. This approach aims to manage the chronic, debilitating nature of the condition and provide relief for the patient.
How Does It Work?
Ergotamine derivatives, such as dihydroergotamine and ergotamine, work by constricting the blood vessels in the brain, which helps to relieve the throbbing pain associated with migraines. They also affect the levels of serotonin, a chemical messenger that plays a role in the development of migraines, and can prevent the trigeminal nerve from releasing inflammatory proteins.
When Would You Get Them?
Ergotamine derivatives are typically reserved for individuals who experience frequent or long-lasting migraines, and who have not found adequate relief from other pain medications like aspirin, ibuprofen, or acetaminophen. They may be particularly useful for patients with migraines associated with pachymeningitis and sixth cranial nerve palsy, where the chronic nature of the condition requires a more long-term management approach.
How Do You Take Them?
Ergotamine derivatives can be taken in various forms, including nasal sprays, suppositories, pills, and sublingual (under-the-tongue) tablets. The specific dosage and administration method will be determined by your healthcare provider based on your individual needs and the severity of your condition.
Side Effects
Ergotamine derivatives can cause a range of side effects, including nausea, vomiting, dizziness, and muscle cramps. In some cases, they may also lead to more severe side effects, such as cardiovascular problems or peripheral ischemia (reduced blood flow to the extremities). It’s important to discuss the potential risks and benefits with your healthcare provider before starting this type of therapy.
Who Should Not Use Ergot Alkaloids?
Ergotamine derivatives are not recommended for individuals with certain medical conditions, such as uncontrolled hypertension, peripheral vascular disease, or kidney or liver disease. Pregnant women and those with a history of heart disease or stroke should also avoid these medications. It’s crucial to inform your healthcare provider of your full medical history to ensure the safe and appropriate use of ergotamine derivatives.
Considerations for Long-Term Ergotamine Derivative Therapy
The use of ergotamine derivatives for the long-term management of migraine associated with pachymeningitis and sixth cranial nerve palsy requires careful monitoring and consideration of the potential risks and benefits. Patients should work closely with their healthcare providers to ensure the safe and effective use of these medications, and to manage any side effects that may arise.
Conclusion
Ergotamine derivatives can be a useful option for the long-term management of migraine associated with pachymeningitis and sixth cranial nerve palsy, but their use must be carefully considered and monitored by healthcare providers. By understanding how these medications work, the potential side effects, and who should not use them, patients can make informed decisions about their treatment options and work with their healthcare team to manage this complex and debilitating condition.
Ergotamine Derivative | DrugBank Online
All categories
- Name
- Ergotamine Derivative
- Accession Number
- DBCAT003327
- Description
Not Available
- Drugs
Drug Drug Description Dihydroergotamine An ergot alkaloid used in the acute treatment of migraine headache and cluster headache. Ergotamine An alpha-1 selective adrenergic agonist vasoconstrictor used to treat migraines with or without aura and cluster headaches. Dihydroergotoxine Not Annotated - Drugs & Drug Targets
Drug Target Type Dihydroergotamine 5-hydroxytryptamine receptor 1D target Dihydroergotamine 5-hydroxytryptamine receptor 1B target Dihydroergotamine Cytochrome P450 3A4 enzyme Dihydroergotamine Alpha-2A adrenergic receptor target Dihydroergotamine 5-hydroxytryptamine receptor 2B target Dihydroergotamine P-glycoprotein 1 transporter Dihydroergotamine 5-hydroxytryptamine receptor 1A target Dihydroergotamine 5-hydroxytryptamine receptor 1E target Dihydroergotamine 5-hydroxytryptamine receptor 2A target Dihydroergotamine 5-hydroxytryptamine receptor 2C target Dihydroergotamine Alpha-1 adrenergic receptors target Dihydroergotamine Alpha-2 adrenergic receptors target Dihydroergotamine Dopamine D2 receptor target Dihydroergotamine Dopamine D3 receptor target Dihydroergotamine Dopamine D4 receptor target Dihydroergotamine 5-hydroxytryptamine receptor 1F target Dihydroergotamine 5-hydroxytryptamine receptor 4 target Dihydroergotamine Beta-3 adrenergic receptor target Ergotamine Alpha-1A adrenergic receptor target Ergotamine 5-hydroxytryptamine receptor 1D target Ergotamine 5-hydroxytryptamine receptor 1B target Ergotamine 5-hydroxytryptamine receptor 2A target Ergotamine Alpha-2A adrenergic receptor target Ergotamine Dopamine D2 receptor target Ergotamine Cytochrome P450 3A4 enzyme Ergotamine Alpha-1B adrenergic receptor target Ergotamine Alpha-1D adrenergic receptor target Ergotamine P-glycoprotein 1 transporter Ergotamine D(1) dopamine receptor target Ergotamine 5-hydroxytryptamine receptor 1A target Ergotamine 5-hydroxytryptamine receptor 1F target Ergotamine 5-hydroxytryptamine receptor 2C target Ergotamine 5-hydroxytryptamine receptor 2B target Ergotamine Alpha-2C adrenergic receptor target
Migraine: Treatment With Ergot Alkaloids
Written by Stephanie Watson
Medically Reviewed by Murtaza Cassoobhoy, MD on February 10, 2023
- How Do They Work?
- When Would You Get Them?
- How Do You Take Them?
- Side Effects
- Who Should Not Use Ergot Alkaloids?
Ergot alkaloids are a group of headache medicines that include dihydroergotamine (Migranal, Trudhesa, others) and ergotamine (Cafergot, Ergomar, Ergostat, others).
These drugs are used only to treat severe, throbbing headaches like migraine and cluster headaches.
Ergot alkaloids are among the oldest headache treatments. They were developed in the 1920s, and doctors have been prescribing them to manage headaches since the 1940s.
They aren’t the same as triptans, a newer class of migraine medicine that came out in the 1990s. Triptans and ergot alkaloids work in similar ways, by narrowing blood vessels in the brain to relieve headaches. Triptans start to work faster than ergot alkaloids and cause fewer side effects. But their pain relief effects don’t last as long.
Although we don’t know the exact cause of migraine, one theory is that the pain starts with chemicals called neurotransmitters that help nerve cells communicate. Waves of brain cell activity cause changes in the levels of these chemicals, which leads to throbbing pain. These changes also cause blood vessels to dilate (widen), which makes the pain worse.
Ergot alkaloids work by narrowing blood vessels in the brain.
These drugs affect levels of the chemical messenger serotonin, which also narrows blood vessels. They also stop a nerve in the brain called the trigeminal nerve from releasing proteins that cause inflammation.
Some ergot alkaloid products add caffeine to help your body absorb the medicine better. This can help the drug start to work more quickly.
Other ergot alkaloids include an antihistamine like dimenhydrinate or diphenhydramine to relieve the nausea and vomiting that often come with a migraine. These ingredients also help you sleep.
Ergot alkaloids might not completely get rid of migraine, but they should work quickly to make these headaches less intense and more manageable.
Because ergot alkaloids can cause severe side effects, doctors often don’t prescribe them as the first treatment for migraine. Your doctor may not recommend them until after you’ve tried pain relievers like aspirin, ibuprofen (Advil, Motrin), or acetaminophen (Tylenol).
Ergot alkaloids are usually reserved for people who get frequent migraine or whose headaches last for longer than 2 days.
Ergotamine comes as a nasal spray, a suppository, a pill, and a type of pill that dissolves under your tongue (sublingual). Don’t chew or swallow the sublingual pill because it may not work as well. Start with one tablet. You can take another one in 30 minutes if your headache hasn’t improved, but don’t take more than three pills in 1 day.
Ergotamine plus caffeine comes as a tablet or suppository. You take two tablets at the first sign of a migraine. If the headache doesn’t improve, take another one or two tablets every 30 minutes until it goes away. Never take more than six tablets in any 24-hour period.
You may want to take ergotamine as a suppository if you have severe nausea and can’t keep a pill down.
To use the suppository, you first unwrap it and then dip the tip into water. To insert it, lie on your side and use a finger to gently push the suppository into your rectum. Wash your hands after you’ve inserted it and lie back down quietly to allow the medicine to work.
If your headache doesn’t improve within 1 hour, you can take another suppository.
Dihydroergotamine comes as a shot or a nasal spray. You can get the shot at your doctor’s office or a hospital, or your doctor can teach you how to inject it yourself. One advantage to the injectable and spray methods is they work quickly. But they can also cause more side effects than pills.
Ergot alkaloids work best if you take them as soon as your migraine starts. If you get aura or other warning signs before a headache, you can take the medicine even before the headache starts. After you take the medicine, lie down in a dark room for 2 hours to give it a chance to work.
Don’t take these medicines more often than your doctor recommends. Overusing ergot alkaloids can make them less effective.
Because ergot alkaloids narrow blood vessels, they can affect many parts of your body. The most common side effects from these medications include:
- Nausea and vomiting
- Dizziness
- Numbness and tingling
- High blood pressure
- Slow or fast heartbeat
- Muscle pain in the arms or legs
- Itching
Some people become dependent on ergot alkaloids and develop rebound headaches.
The medicine stops working and the headaches get worse. You may feel like you need to take more of the drug to get the same relief, but taking a higher dose than your doctor prescribed could increase the side effects and even cause death.
If you have headaches and find yourself taking an ergot alkaloid every day or every other day, talk to your doctor. To stop the rebound headaches, you’ll need to stop taking this medication. It can take some time before the rebound headaches stop.
Ergot alkaloids can interact with certain medications. Let your doctor and pharmacist know about all the prescription and over-the-counter medicines, vitamins, and supplements you take before you start taking a migraine medicine.
These medications can also interact with grapefruit. Don’t drink grapefruit juice or eat grapefruit while taking an ergot alkaloid without talking to your doctor first.
Pregnant women should not take ergot alkaloids. These medicines can harm a growing baby and increase the risk for miscarriage.
If you’re nursing, check with your doctor before taking ergot alkaloids. The medication can reduce the amount of milk you make. It can also pass into the breast milk and cause problems like these in your baby:
- Vomiting
- Diarrhea
- Seizures
- Blood pressure changes
Taking an ergot alkaloid can also be riskier for people who have had these conditions:
- Hemiplegic migraine (migraine with weakness on one side of the body)
- Heart disease
- Heart attack
- Stroke or transient ischemic attack (TIA)
- High blood pressure or high cholesterol
- Diabetes
- Raynaud’s disease
- Circulation problems
- Blood vessel or heart surgery
- Kidney, liver, or lung disease
You should not take ergot alkaloids with CYP3A4 inhibitors like some antibiotics, antifungal medicines, and HIV drugs. These medications slow the rate at which your body breaks down and removes ergot alkaloids. A buildup of medication in your body could lead to more serious side effects.
Your doctor should go over your medical history before they prescribe an ergot alkaloid for you.
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Consequences of misuse of painkillers
Pain medications (non-steroidal anti-inflammatory drugs – NSAIDs, ergotamine derivatives, analgesics) are the most popular and widely used over-the-counter drugs.
Pain medications (non-steroidal anti-inflammatory drugs – NSAIDs, ergotamine derivatives, analgesics) are the most popular and widely used OTC drugs.
At the same time, headaches (cephalgia) are very often the cause of their use. Most often it is the so-called tension headache and migraine.
The possibility of buying a drug without a doctor’s prescription in Ukraine leads to the fact that many people decide on their own which drug, at what dose and with what frequency to take. And therein lies the danger, since for each drug there are certain contraindications and restrictions for use.
First, the uncontrolled use of analgesics and NSAIDs often leads to the development of various side effects, including changes in blood composition, gastrointestinal bleeding, erosions and ulcers in the digestive tract.
And secondly, irrational (too frequent or exceeding the recommended dosage) use of painkillers for cephalalgia, including migraine, often causes the so-called drug-induced or abuse headache. Most often, such a headache occurs in chronic migraine as a result of chronic abuse of drugs for the treatment of attacks of cephalalgia.
The development of overuse headache is indicated by the use of painkillers more than 2-3 times a week (10 times a month) for 3 or more months. At the same time, the severity of headache attacks and the frequency of their occurrence can progress against the background of excessive drug intake.
Interestingly, analgesic-associated headache occurs only in patients with primary headache (80% of overbusy headache patients are migraine patients) and never develops as a result of taking the same drugs, but according to different indications (for example, osteoarthritis).
Theoretically, too frequent use of any migraine medications, including analgesics, NSAIDs, ergotamine derivatives, opioids, triptans, can lead to the development of “abuses”. However, since the fact of abuse (i.e., excessive frequency of use) of the drug is of greatest importance here, this problem most often occurs when taking NSAIDs and analgesics, given their greater availability and less effectiveness in moderate and severe forms of migraine.
As for the mechanisms of development of abusus cephalgia, it is assumed that it is based on changes in the parts of the brain responsible for conducting pain impulses that arise as a result of regular use of headache medications.
Diagnosis of overuse headache is not difficult – it is enough to analyze the entries in the headache diary of a patient who has addressed a doctor with complaints of progression of migraine or other primary headache, in which the time of onset of headache attacks and the number of pain medications taken for at least 3 months.
The superimposition of drug-induced headache on migraine symptoms significantly worsens the patient’s condition and requires proper treatment, the effectiveness of which depends on the patience and discipline of the patient. First of all, the doctor studies the treatment regimen, finds and cancels the “guilty” drug. Usually the complete withdrawal of such pain medication is sufficient intervention, however, in severe cases, inpatient treatment with antidepressants and detoxification therapy may be required.
At the second stage, a correction of the migraine treatment regimen is carried out in order to effectively prevent attacks and most sparing pain relief in the event of the development of cephalalgia. Treatment regimens with alternating periods of frequent use of the drug and relatively long periods without treatment are preferred, since the regular use of painkillers is a major risk factor for the development of abuse headaches. A necessary condition for the effective treatment of “abuses” is the refusal to take the analgesic that caused the development of abuses headache, since any therapy will be much less effective if the patient continues to use such a drug on a regular basis.
Prevention of the development of drug-induced headaches in people with migraine and other primary cephalalgias consists in refusing self-medication and strictly following the doctor’s recommendations. In particular, it is of great importance to abandon the uncontrolled increase in the doses and frequency of taking NSAIDs and analgesics, in case of their ineffectiveness, in favor of switching to triptans.
Sources:
- https://www.webmd.com/pain-management/pain-medication-side-effects#1
- https://www.healthline.com/health/opioids-and-related-disorders#symptoms
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Ergotamine (INN) and its salts
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