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Dihydroergotamine

Dihydroergotamine

Dihydroergotamine is a potent ergot alkaloid used for the acute treatment of migraine and cluster headaches. This FDA-approved medication operates by constricting blood vessels around the brain, significantly reducing headache symptoms by decreasing vascular inflammation and stabilizing serotonin receptors, which help control pain perception. Available in injectable forms and nasal sprays, it provides flexible dosing options tailored to the severity of the symptoms. While effective in relieving debilitating headaches, Dihydroergotamine should be used under strict medical supervision to manage dosages properly and avoid serious side effects such as cardiovascular issues or rare cases of fibrosis. Patients should adhere to dosage limits to prevent medication overuse headaches and ensure proper storage away from light and moisture. It is crucial to consult a healthcare provider before use, especially to discuss potential drug interactions and contraindications.

Product Overview

Dihydroergotamine, an ergot alkaloid, is primarily utilized in the treatment of migraines and cluster headaches. This medication functions by constricting blood vessels surrounding the brain, a process that alleviates headaches by mitigating vascular inflammation, commonly triggered during migraine episodes. Additionally, it stabilizes serotonin receptors, which helps moderate the transmission of pain signals and reduces pain perception. Approved by the FDA for these specific uses, Dihydroergotamine is effective in both preventing and aborting headaches at their onset, providing significant relief for those suffering from these debilitating conditions.

Dihydroergotamine is available in various forms, including injectable solutions and nasal sprays, allowing flexible application depending on the patient’s needs and the severity of symptoms. The standard dosage for the injectable form is 1 mg, which can be administered intramuscularly, subcutaneously, or intravenously and may be repeated hourly, up to specified daily and weekly maximums. The nasal spray typically starts with a dose of 0.5 mg per nostril, which may be repeated once. This medication is intended for use in adults and should be administered under the guidance of a healthcare provider.

Side effects of Dihydroergotamine can range from mild, such as nasal irritation or dizziness, to more severe reactions, including significant increases in blood pressure, heart problems, and rare instances of fibrosis. Patients are advised to use this medication judiciously, adhering closely to prescribed dosages to avoid potential overuse and associated complications. Important storage instructions include keeping the medication at room temperature, away from light and moisture, and ensuring it is out of reach of children. Users should be aware of the medication’s interaction potential, particularly with CYP3A4 inhibitors and other vasoconstrictors, and manage their use accordingly to mitigate risk. Regular follow-ups with a healthcare provider are recommended to monitor the drug’s effectiveness and any adverse effects.

Uses of Dihydroergotamine

  • Migraine Headaches
  • Cluster Headaches (only with the injection form)

How to Use Dihydroergotamine? 

Dosage

  • Dihydroergotamine is available as an injectable solution with a concentration of 1 mg/mL.

Recommended Dosage for Different Patients of Dihydroergotamine

For Migraine and Cluster Headaches:

Injectable (IM, IV, Subcutaneous)

  • Initial Dose: 1 mg.
  • Repeat Doses: Additional doses of 1 mg may be given at hourly intervals as needed.
  • Maximum Dosage:
    • Intravenous (IV): No more than 2 mg in 24 hours, with a limit of 6 mg per week.
    • Intramuscular (IM) or Subcutaneous: No more than 3 mg in 24 hours, with a limit of 6 mg per week.

Nasal Spray

  • Initial Dose: 0.5 mg (one spray in each nostril).
  • Repeat Dose: Another 0.5 mg in 15 minutes if needed.
  • Total Maximum Dose: 2 mg per episode.
  • Maximum Dosage: No more than 3 mg in 24 hours and no more than 4 mg within a 7-day period.

[Note: Remember these recommendations may vary depending on person to person. Discuss it with your doctor, and they’ll customize your dosage accordingly.]

How to Take It?

Dihydroergotamine Injection

  • Ensure that the injection site (usually the thigh or upper arm) is clean and free from any signs of infection.
  • The injection can be given subcutaneously (under the skin) or intramuscularly (into the muscle). Follow your healthcare provider’s instructions precisely.
  • Typically, your doctor will start with a test dose to ensure you do not have an adverse reaction before proceeding with the full treatment. Do not exceed the recommended dosage.

Dihydroergotamine Nasal Spray

  • Blow your nose gently to clear your nostrils.
  • If using the nasal spray for the first time or if it hasn’t been used for a while, prime the pump by spraying it several times into the air until a fine mist appears.
  • Tilt your head slightly forward, insert the nasal spray into one nostril, and close the other with your finger. Activate the spray as you breathe in gently through your nose. Repeat in the other nostril as directed.
  • Follow the dosage instructions provided by your healthcare provider closely. Typically, several sprays are needed in each nostril.

[Note: Your doctor will decide the right amount for you based on your condition, following guidelines and studies on the drug. They’ll adjust it as needed over time.]

How Does Dihydroergotamine Work?

Dihydroergotamine is a medication used primarily for the treatment of migraines and cluster headaches. It belongs to a class of drugs known as ergot alkaloids. Dihydroergotamine works by constricting blood vessels around the brain, which is believed to alleviate headaches by reducing vascular inflammation, a common trigger for migraine pain. Additionally, it stabilizes serotonin receptors in the brain, which helps to modulate the transmission of pain signals and reduce the perception of pain. This dual action makes Dihydroergotamine effective in preventing and stopping headaches once they have started, providing relief for individuals suffering from these debilitating conditions.

Important Safety Information

Side Effects

Common side effects of this medication include:

  • Headache: Headaches are a potential side effect when using dihydroergotamine.
  • Dizziness: Users may experience feelings of lightheadedness or dizziness.
  • Anxiety: Anxiety can occasionally manifest as a side effect.
  • Diarrhea: Diarrhea is another possible adverse effect.
  • Numbness and Tingling: Sensations of numbness or tingling may occur.
  • Increased Blood Pressure: Dihydroergotamine may cause an elevation in blood pressure.
  • Rash and Increased Sweating: Some individuals report developing a skin rash and experiencing increased sweating.
  • Flushing: Users may experience sudden warmth, redness, or a tingly sensation, known as flushing.

Serious side effects of this medication include:

  • Poor Blood Flow: Experiences pain, numbness, and a sensation of coldness, accompanied by a pale coloration in the hands or feet.
  • Heart Attack: Symptoms include chest pain or tightness, pain extending to the jaw, neck, or back, and shortness of breath.
  • Stroke: Signs of a stroke are sudden dizziness, difficulty with walking or speaking, loss of balance, confusion, and weakness or paralysis on one side of the body, affecting the face, arm, or leg.
  • High Blood Pressure: Common indicators are headaches and vision problems.

[Note: Remember, this list may not cover all possible side effects. Always consult with your healthcare giver for medical advice about side effects.]

Warnings

  • Low Blood Flow and Medication Interactions: Some medications can increase Dihydroergotamine levels in the body, leading to excessively tight blood vessels and restricted blood flow. This can cause strokes or tissue damage in the extremities. Avoid combining Dihydroergotamine with protease inhibitors (often used for HIV) or macrolide antibiotics (such as erythromycin and clarithromycin). Even less potent medications can pose risks, so always inform your healthcare provider and pharmacist about all medicines you take to avoid harmful interactions.
  • Low Blood Flow Symptoms:Problems from reduced blood flow have occurred with Dihydroergotamine use, even without drug interactions. Inform your provider if you experience symptoms like muscle pain, numbness, coldness, or pale or discolored skin, especially in your fingers or toes. Seek emergency help immediately if you suspect a stroke.
  • Heart Risks: Dihydroergotamine can constrict blood vessels in the heart, potentially causing heart attacks or dangerous arrhythmias. Do not use this medication if you have or are at risk for heart disease. Your first dose may need to be administered in a medical setting to manage any immediate complications. Regular follow-ups are crucial to monitor heart health. Seek immediate medical attention if you experience chest pain or tightness.
  • Stroke Risk: Dihydroergotamine has been linked to strokes, brain bleeds, and other neurological damage. Use this medication only for prescribed migraine relief, and strictly follow your provider’s instructions. If symptoms like sudden dizziness, confusion, imbalance, or weakness occur, get medical help immediately.
  • High Blood Pressure: This medication can elevate blood pressure, even in individuals without prior hypertension. Avoid Dihydroergotamine if your high blood pressure is uncontrolled.
  • Rebound Headaches: Frequent use of headache medications, including Dihydroergotamine, can lead to medication overuse headaches, which might worsen or become more frequent. Limit usage to less than 10 days per month unless otherwise directed by your healthcare provider.
  • Risks During Pregnancy: Dihydroergotamine is not recommended during pregnancy as it can harm the unborn baby and potentially trigger premature labor.
  • Fibrosis Risk: In rare cases, long-term use of Dihydroergotamine has been associated with fibrosis in the stomach, lungs, or heart. Use this medication only as necessary and discuss frequent headache prevention with your provider.
  • Nasal Spray Irritation: Users of Migranal and Trudhesa nasal sprays may experience nasal irritation, including stuffiness, burning, or bleeding. While these effects usually resolve within four hours, contact your provider if they become bothersome or persist.

Boxed Warnings

  • Concomitant administration with potent CYP450 3A4 inhibitors (e.g., protease inhibitors, macrolide antibiotics) can lead to serious and/or life-threatening peripheral ischemia.
  • Risk for vasospasm leading to cerebral ischemia and/or ischemia of the extremities is increased.

Precautions

  • Allergies: Inform your doctor or pharmacist if you have allergies to dihydroergotamine, other ergot alkaloids like ergotamine, or any other allergies. The product may contain inactive ingredients that can cause allergic reactions.
  • Medical History: Discuss your medical history with your healthcare provider, especially if you have:
    • Blood circulation issues (e.g., peripheral arterial disease, Raynaud’s disease)
    • Heart disease (e.g., coronary artery disease, angina, previous heart attack)
    • Stroke or a family history of heart disease
    • Diabetes
    • High blood pressure or high cholesterol
    • Liver or kidney disease
    • Severe blood infection (sepsis)
    • Recent blood vessel surgery
    • Stomach/intestinal problems (e.g., ischemic bowel syndrome)
    • Tobacco/smoking use or if you are postmenopausal
  • Dizziness: This medication may cause dizziness. Avoid alcohol and marijuana as they can exacerbate this effect. Do not drive or operate machinery until you can safely perform such activities.
  • Alcohol and Headaches: Note that alcohol can be a trigger for headaches.
  • Tobacco Use: Using tobacco/nicotine products can increase the risk of serious side effects such as heart problems and decreased blood supply to extremities. Do not use tobacco products while taking this medication, and discuss cessation methods with your doctor if you currently smoke.
  • Surgery: Inform your doctor or dentist of all products you use (including prescription/nonprescription drugs and herbal products) before surgery.
  • Pregnancy: Avoid becoming pregnant while using dihydroergotamine. It may harm an unborn baby. If you become pregnant, discuss the risks and benefits of this medication with your doctor immediately.
  • Breastfeeding: Dihydroergotamine may pass into breast milk and could harm a nursing infant. Breastfeeding is not recommended while using this drug and for three days after the last dose. Consult your doctor before breastfeeding.

Contraindications 

  • Hypersensitivity to ergot alkaloids.
  • Concomitant use of potent CYP450 3A4 inhibitors.
  • Ischemic heart disease (angina pectoris, history of myocardial infarction, or silent ischemia).
  • Coronary artery vasospasm, including Prinzmetal’s variant angina.
  • Uncontrolled hypertension.
  • Use within 24 hours of 5-HT1 agonists (e.g., sumatriptan), ergotamine-containing or ergot-type medications, or methysergide.
  • Hemiplegic or basilar migraine.
  • Peripheral arterial disease.
  • Sepsis.
  • Following vascular surgery.
  • Severe hepatic impairment.
  • Severe renal impairment.
  • Pregnancy.
  • Nursing mothers.
  • Concomitant use with peripheral and central vasoconstrictor

Missed Dose

Dihydroergotamine is taken as needed. If you are following a dosing schedule and miss a dose, skip it. Do not take a double dose. Additionally, limit your use to no more than three injections per day or six injections per week.

[Note: If you have missed a dose of your medication and are unsure about when to take the next one, immediately consult your doctor or pharmacist.]

Overdose 

If someone has overdosed and exhibits severe symptoms like unconsciousness or difficulty breathing, seek emergency medical help immediately. For less immediate concerns, contact a poison control center right away. Call the provincial poison control center at earliest. Symptoms of an overdose can include severe or sudden numbness, blue or purple coloring of the hands or feet, slow or difficult breathing, confusion, and seizures.

 

[Note: If you consumed more than recommended dose, get medical help right away, or call the Poison Help line at 1-800-222-1222.]

Storage

  • Store the medication in a sealed container at room temperature, avoiding exposure to heat, moisture, and direct sunlight.
  • Ensure the medicine does not freeze.
  • Keep the medication out of reach of children.
  • Discard any expired or no longer needed medicine.
  • Consult your healthcare professional for proper disposal methods for any unused medication.

[Note: Discuss with your healthcare professional about the proper disposal of any unused medicine and any questions you may have regarding its storage.]

Dihydroergotamine Interactions

  • Triptans (e.g., sumatriptan, zolmitriptan): Concomitant use of Dihydroergotamine with other serotonin receptor agonists like triptans can increase the risk of serotonin syndrome, a potentially life-threatening condition.
  • Strong CYP3A4 Inhibitors (e.g., ketoconazole, itraconazole, ritonavir): These medications can significantly increase Dihydroergotamine levels in the blood, leading to an increased risk of serious side effects such as vasospasm and ischemia.
  • Macrolide Antibiotics (e.g., erythromycin, clarithromycin): Similar to CYP3A4 inhibitors, macrolide antibiotics can increase the concentration of dihydroergotamine, heightening the risk of severe vasoconstriction and ischemic complications.
  • Protease Inhibitors (e.g., ritonavir): These are also potent inhibitors of CYP3A4 and can lead to high levels of dihydroergotamine, increasing the risk of ergot toxicity.
  • Beta-Blockers: The combination with Dihydroergotamine can increase the risk of peripheral ischemia and vasospastic reactions due to additive effects on blood vessel constriction.
  • Antifungal Agents (e.g., ketoconazole, itraconazole): These can inhibit the metabolism of Dihydroergotamine leading to increased plasma concentrations and potential toxicity.
  • SSRIs and SNRIs (e.g., fluoxetine, sertraline, venlafaxine): There is an increased risk of serotonin syndrome when SSRIs or SNRIs are taken with dihydroergotamine.
  • Nicotine: Smoking or using nicotine products can exacerbate the vasoconstrictive effects of dihydroergotamine.

[Note: This isn’t a complete list, and there could be other drugs that interact with Dihydroergotamine. Make sure to tell your doctor any prescription, over-the-counter medicines, and herbal products you’re taking.]

Dihydroergotamine Alternatives

[Note: Your doctor will choose what’s best for you. Don’t use any of these alternative medications without consulting your healthcare provider. Taking them by yourself may cause serious side effects.] 

Frequently Asked Questions

Is Dihydroergotamine considered a triptan?

No, Dihydroergotamine is not a triptan; it belongs to the class of medications known as ergots. While it operates similarly to triptans like sumatriptan (Imitrex) or rizatriptan (Maxalt), which are also used to treat migraines and cluster headaches, they differ in their chemical classification. Both ergots and triptans can cause similar side effects. It’s important to avoid taking Dihydroergotamine and triptan medications within 24 hours of each other to prevent the risk of dangerously high blood pressure and other severe side effects.

Can Dihydroergotamine cause rebound headaches?

Dihydroergotamine, when used as directed, typically does not cause rebound headaches, which are also known as medication-overuse headaches. This medication is effective in stopping headaches, and its effects tend to last longer than those of many other treatments, reducing the likelihood of experiencing another headache shortly thereafter. It is crucial to use this medication strictly according to your healthcare provider’s instructions. If you find that Dihydroergotamine is not effective, or if you find yourself using it more frequently than recommended, consult your healthcare provider for guidance.

What should I avoid while using Dihydroergotamine injections?

Avoid using Dihydroergotamine within 24 hours before or after taking other migraine medications. This includes other ergot medicines (such as ergotamine and methylergonovine) and triptan medications (such as almotriptan and eletriptan), as combining these can lead to serious side effects. Additionally, grapefruit and grapefruit products may interact with dihydroergotamine, potentially causing adverse effects. It is best to avoid grapefruit products while using this medication.

Can Dihydroergotamine cause drowsiness?

Dihydroergotamine is not commonly associated with causing drowsiness. In clinical studies, only about 3% of people who used the nasal spray form of this medication reported feeling drowsy. Additionally, while rare, some users may experience fatigue or a general sense of weakness. These side effects are generally uncommon.

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