Zolmitriptan 2.5mg ODT Tablets
It is used to treat migraine headaches.
Drug Class
Antimigraine agent
Pharmacologic Class
Selective serotonin (5-HT1B/1D) receptor agonist; Triptan
Pregnancy Category
C
FDA Approved
Sep 1999
DEA Schedule
Not Controlled
Overview
What is this medicine?
Zolmitriptan is a medication used to treat migraine headaches once they have started. It works by narrowing blood vessels in the brain and reducing substances that cause pain and other migraine symptoms. It is an orally disintegrating tablet, meaning it dissolves quickly in your mouth without water.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take it with or without food. When opening the foil packaging, do not push the tablet out. Instead, use dry hands to remove it and place it on your tongue, allowing it to dissolve. You do not need water, and it's essential not to swallow the tablet whole or chew, break, or crush it.
Take your medication as soon as possible after a headache starts. If your symptoms do not improve after the first dose, consult your doctor. If your headache returns, you may take a second dose if your doctor has advised you to do so. However, be sure to wait at least 2 hours after the first dose before taking another one.
Storing and Disposing of Your Medication
Store your medication at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom.
Missing a Dose
Since this medication is taken as needed, you do not need to worry about missing a dose. However, do not take it more frequently than your doctor has prescribed.
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take it with or without food. When opening the foil packaging, do not push the tablet out. Instead, use dry hands to remove it and place it on your tongue, allowing it to dissolve. You do not need water, and it's essential not to swallow the tablet whole or chew, break, or crush it.
Take your medication as soon as possible after a headache starts. If your symptoms do not improve after the first dose, consult your doctor. If your headache returns, you may take a second dose if your doctor has advised you to do so. However, be sure to wait at least 2 hours after the first dose before taking another one.
Storing and Disposing of Your Medication
Store your medication at room temperature, protected from light, and in a dry place. Avoid storing it in a bathroom.
Missing a Dose
Since this medication is taken as needed, you do not need to worry about missing a dose. However, do not take it more frequently than your doctor has prescribed.
Lifestyle & Tips
- Take at the first sign of a migraine headache, but not for prevention.
- Do not take more than 10 mg in a 24-hour period.
- Avoid driving or operating machinery if you experience dizziness or drowsiness.
- Avoid alcohol during a migraine attack as it can worsen symptoms or side effects.
- Identify and avoid migraine triggers (e.g., certain foods, stress, lack of sleep).
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
2.5 mg or 5 mg orally disintegrating tablet at the onset of migraine headache. May repeat dose after 2 hours if headache returns or only partial response. Maximum 10 mg in any 24-hour period.
Dose Range:
2.5 - 5 mg
Condition-Specific Dosing:
initialDose:
2.5 mg or 5 mg
repeatDoseInterval:
At least 2 hours after initial dose
maximumDailyDose:
10 mg within 24 hours
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (Safety and efficacy not established for patients under 12 years of age)
Adolescent:
Not established (Safety and efficacy not established for patients under 18 years of age)
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment necessary
Moderate:
No dose adjustment necessary
Severe:
Use with caution; consider 2.5 mg as initial dose and maximum daily dose
Dialysis:
Not specifically studied, but caution advised due to potential for increased exposure
Hepatic Impairment:
Mild:
No dose adjustment necessary
Moderate:
Consider 2.5 mg as initial dose and maximum daily dose
Severe:
Consider 2.5 mg as initial dose and maximum daily dose
Pharmacology
Mechanism of Action
Zolmitriptan is a selective agonist for 5-hydroxytryptamine1B (5-HT1B) and 5-hydroxytryptamine1D (5-HT1D) receptors. It is believed to exert its antimigraine effects through vasoconstriction of intracranial blood vessels and inhibition of pro-inflammatory neuropeptide release from trigeminal nerve endings.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 40% (oral tablet)
Tmax:
1.5 to 3 hours (for zolmitriptan); 3 hours (for active metabolite)
FoodEffect:
Minimal effect on absorption
Distribution:
Vd:
Approximately 2.4 L/kg
ProteinBinding:
Approximately 25%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 2.5 to 3 hours (zolmitriptan); 6 to 7 hours (N-desmethyl metabolite)
Clearance:
Approximately 31.5 mL/min/kg
ExcretionRoute:
Renal (65%), Fecal (30%)
Unchanged:
Approximately 4% (urine)
Pharmacodynamics
OnsetOfAction:
Within 15-45 minutes (ODT formulation)
PeakEffect:
1 to 2 hours
DurationOfAction:
4 to 6 hours
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Loss of eyesight (which can be long-lasting)
Diarrhea or constipation
Severe stomach pain or bloody diarrhea
Weight loss
Leg cramps
Feeling of heaviness or tightness in the leg muscles
Feeling cold
Burning or aching pain in the feet or toes
Shortness of breath
Abnormal burning, numbness, or tingling sensations
Serotonin Syndrome: A Potentially Life-Threatening Condition
There is a risk of developing serotonin syndrome, a severe and potentially deadly condition, especially when taking certain other medications. If you experience any of the following symptoms, contact your doctor immediately:
Agitation
Changes in balance
Confusion
Hallucinations
Fever
Fast or abnormal heartbeat
Flushing
Muscle twitching or stiffness
Seizures
Shivering or shaking
Excessive sweating
Severe diarrhea, upset stomach, or vomiting
Severe headache
Heart Problems: Seek Medical Help Right Away
In rare cases, this medication can cause severe and potentially deadly heart problems, including heart attack and abnormal heartbeat, within a few hours of taking the drug. If you experience any of the following symptoms, contact your doctor immediately:
Chest, throat, neck, or jaw tightness, pain, pressure, or heaviness
Cold sweat
Shortness of breath
Fast heartbeat
Abnormal heartbeat
Severe dizziness or passing out
Brain Blood Vessel Problems: Seek Medical Help Right Away
In rare cases, this medication can cause severe and potentially deadly brain blood vessel problems, including stroke. If you experience any of the following symptoms, contact your doctor immediately:
Weakness on one side of the body
Trouble speaking or thinking
Changes in balance
Drooping on one side of the face
Changes in eyesight
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor or seek medical help if you notice any of the following:
Dizziness
Drowsiness
Fatigue
Weakness
Feeling of warmth
Feeling of heaviness or pressure
Dry mouth
Upset stomach or vomiting
Reporting Side Effects
If you have questions about side effects or experience any symptoms that bother you or do not go away, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache
+ Dizziness
+ Passing out
+ Changes in eyesight
Loss of eyesight (which can be long-lasting)
Diarrhea or constipation
Severe stomach pain or bloody diarrhea
Weight loss
Leg cramps
Feeling of heaviness or tightness in the leg muscles
Feeling cold
Burning or aching pain in the feet or toes
Shortness of breath
Abnormal burning, numbness, or tingling sensations
Serotonin Syndrome: A Potentially Life-Threatening Condition
There is a risk of developing serotonin syndrome, a severe and potentially deadly condition, especially when taking certain other medications. If you experience any of the following symptoms, contact your doctor immediately:
Agitation
Changes in balance
Confusion
Hallucinations
Fever
Fast or abnormal heartbeat
Flushing
Muscle twitching or stiffness
Seizures
Shivering or shaking
Excessive sweating
Severe diarrhea, upset stomach, or vomiting
Severe headache
Heart Problems: Seek Medical Help Right Away
In rare cases, this medication can cause severe and potentially deadly heart problems, including heart attack and abnormal heartbeat, within a few hours of taking the drug. If you experience any of the following symptoms, contact your doctor immediately:
Chest, throat, neck, or jaw tightness, pain, pressure, or heaviness
Cold sweat
Shortness of breath
Fast heartbeat
Abnormal heartbeat
Severe dizziness or passing out
Brain Blood Vessel Problems: Seek Medical Help Right Away
In rare cases, this medication can cause severe and potentially deadly brain blood vessel problems, including stroke. If you experience any of the following symptoms, contact your doctor immediately:
Weakness on one side of the body
Trouble speaking or thinking
Changes in balance
Drooping on one side of the face
Changes in eyesight
Other Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to contact your doctor or seek medical help if you notice any of the following:
Dizziness
Drowsiness
Fatigue
Weakness
Feeling of warmth
Feeling of heaviness or pressure
Dry mouth
Upset stomach or vomiting
Reporting Side Effects
If you have questions about side effects or experience any symptoms that bother you or do not go away, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Sudden or severe chest pain, jaw pain, or arm pain (could be heart attack)
- Shortness of breath, wheezing
- Sudden weakness or numbness on one side of the body, slurred speech, sudden vision changes (could be stroke)
- Severe stomach pain, bloody diarrhea (could be ischemic colitis)
- Signs of serotonin syndrome: agitation, confusion, rapid heart rate, fever, sweating, muscle stiffness, twitching, loss of coordination, nausea, vomiting, diarrhea
- Allergic reaction: rash, hives, swelling of face/lips/tongue/throat, difficulty breathing
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following conditions to ensure safe use of this medication:
Any allergies you have, including allergies to this drug, its components, or other substances. Describe the allergic reaction you experienced, including any symptoms.
Certain health conditions, such as:
+ High blood pressure
+ Liver disease
A history of:
+ Chest pain or pressure
+ Diseased arteries in the legs or arms
+ Heart attack
+ Heart disease
+ Poor blood flow in the heart, brain, bowel, or kidney
+ Stroke or transient ischemic attack (TIA)
+ Certain types of migraines, including hemiplegic or basilar migraines
+ Abnormal heartbeat, such as Wolff-Parkinson-White syndrome
Recent use of certain medications for depression, including isocarboxazid, phenelzine, or tranylcypromine, within the last 14 days. Using this medication within 14 days of these drugs can cause severe high blood pressure.
Use of other medications for migraine or headache, such as almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, or sumatriptan, within the last 24 hours.
Use of ergotamine, methysergide, dihydroergotamine, or similar medications within the last 24 hours.
Special Considerations for Children:
If you are a parent or guardian, please note that this medication is not approved for use in children under 18 years of age.
Interactions with Other Medications and Health Conditions:
This is not an exhaustive list of all potential interactions. It is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. This will help ensure your safety while taking this medication. Do not start, stop, or change the dose of any medication without consulting your doctor.
It is essential to inform your doctor about the following conditions to ensure safe use of this medication:
Any allergies you have, including allergies to this drug, its components, or other substances. Describe the allergic reaction you experienced, including any symptoms.
Certain health conditions, such as:
+ High blood pressure
+ Liver disease
A history of:
+ Chest pain or pressure
+ Diseased arteries in the legs or arms
+ Heart attack
+ Heart disease
+ Poor blood flow in the heart, brain, bowel, or kidney
+ Stroke or transient ischemic attack (TIA)
+ Certain types of migraines, including hemiplegic or basilar migraines
+ Abnormal heartbeat, such as Wolff-Parkinson-White syndrome
Recent use of certain medications for depression, including isocarboxazid, phenelzine, or tranylcypromine, within the last 14 days. Using this medication within 14 days of these drugs can cause severe high blood pressure.
Use of other medications for migraine or headache, such as almotriptan, eletriptan, frovatriptan, naratriptan, rizatriptan, or sumatriptan, within the last 24 hours.
Use of ergotamine, methysergide, dihydroergotamine, or similar medications within the last 24 hours.
Special Considerations for Children:
If you are a parent or guardian, please note that this medication is not approved for use in children under 18 years of age.
Interactions with Other Medications and Health Conditions:
This is not an exhaustive list of all potential interactions. It is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, as well as any health problems you have. This will help ensure your safety while taking this medication. Do not start, stop, or change the dose of any medication without consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before engaging in activities that require alertness, such as driving, wait until you understand how this drug affects you.
This medication is not intended to prevent or reduce the frequency of migraine headaches. If you experience a headache that is different from your typical migraine, consult your doctor before taking this drug.
Adhering to your prescribed dosage is crucial, as taking more of this medication than directed (either a higher dose or more frequent doses) may worsen your headaches.
There is a risk of high blood pressure associated with this type of medication. Follow your doctor's instructions for monitoring your blood pressure.
If you have risk factors for heart disease, such as high blood pressure, high cholesterol, being overweight, having high blood sugar or diabetes, smoking cigarettes, being a male over 40 years old, having a family history of early heart disease, or being a postmenopausal female, exercise caution and discuss your individual situation with your doctor.
If you have phenylketonuria (PKU), consult your doctor, as some formulations of this medication may contain phenylalanine.
For individuals 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to both you and your baby.
This medication is not intended to prevent or reduce the frequency of migraine headaches. If you experience a headache that is different from your typical migraine, consult your doctor before taking this drug.
Adhering to your prescribed dosage is crucial, as taking more of this medication than directed (either a higher dose or more frequent doses) may worsen your headaches.
There is a risk of high blood pressure associated with this type of medication. Follow your doctor's instructions for monitoring your blood pressure.
If you have risk factors for heart disease, such as high blood pressure, high cholesterol, being overweight, having high blood sugar or diabetes, smoking cigarettes, being a male over 40 years old, having a family history of early heart disease, or being a postmenopausal female, exercise caution and discuss your individual situation with your doctor.
If you have phenylketonuria (PKU), consult your doctor, as some formulations of this medication may contain phenylalanine.
For individuals 65 years or older, use this medication with caution, as you may be more susceptible to side effects.
If you are pregnant, planning to become pregnant, or are breastfeeding, inform your doctor to discuss the potential benefits and risks to both you and your baby.
Overdose Information
Overdose Symptoms:
- Severe drowsiness
- Dizziness
- Nausea
- Vomiting
- Weakness
- Lack of coordination
- Hypertension
- Hypotension
- Tachycardia
- Bradycardia
- Respiratory depression
- Convulsions
What to Do:
Seek immediate medical attention or call 911. Contact a poison control center at 1-800-222-1222. Supportive treatment is recommended, including monitoring of cardiovascular and respiratory function.
Drug Interactions
Contraindicated Interactions
- Monoamine oxidase inhibitors (MAOIs) or within 2 weeks of discontinuing MAOIs (due to increased zolmitriptan exposure)
- Other 5-HT1 agonists (e.g., other triptans) within 24 hours
- Ergot-type medications (e.g., ergotamine, dihydroergotamine) within 24 hours
- Patients with ischemic heart disease, Prinzmetal's angina, uncontrolled hypertension, or other underlying cardiovascular conditions
Major Interactions
- SSRIs/SNRIs (increased risk of serotonin syndrome)
- Cimetidine (increases zolmitriptan Cmax and AUC by 2-fold)
Moderate Interactions
- Oral contraceptives (may increase zolmitriptan levels slightly)
- Propranolol (no significant interaction)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Cardiovascular risk assessment
Rationale: To identify patients at risk for ischemic heart disease or other cardiovascular events, as triptans are contraindicated in these conditions.
Timing: Prior to initiating therapy
Blood pressure
Rationale: To ensure hypertension is controlled, as triptans can cause transient increases in blood pressure.
Timing: Prior to initiating therapy
Liver function tests (LFTs)
Rationale: To assess hepatic impairment, which may require dose adjustment.
Timing: Prior to initiating therapy in patients with suspected hepatic dysfunction
Routine Monitoring
Migraine frequency and severity
Frequency: Ongoing, with each use
Target: Reduction in headache pain and associated symptoms
Action Threshold: If no improvement or worsening, consider alternative diagnosis or treatment; if using frequently, assess for medication overuse headache.
Blood pressure
Frequency: Periodically, especially in patients with risk factors for hypertension
Target: Within normal limits or patient's target range
Action Threshold: Significant or sustained increase may warrant discontinuation or alternative therapy.
Symptom Monitoring
- Chest pain, tightness, or pressure (may indicate cardiac ischemia)
- Shortness of breath, wheezing (may indicate hypersensitivity or cardiac event)
- Neck pain or stiffness (common triptan side effect, but monitor for severity)
- Tingling, numbness, or warmth (common triptan side effect)
- Dizziness, drowsiness, fatigue
- Signs of serotonin syndrome (agitation, hallucinations, rapid heart rate, fever, sweating, shivering, muscle stiffness or twitching, loss of coordination, nausea, vomiting, diarrhea)
- Signs of medication overuse headache (increasing headache frequency or severity with regular use)
Special Patient Groups
Pregnancy
Pregnancy Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies show adverse effects at high doses.
Second Trimester:
Limited human data; animal studies show adverse effects at high doses.
Third Trimester:
Limited human data; animal studies show adverse effects at high doses. Potential for uterine contractions.
Lactation
Zolmitriptan and its active metabolite are excreted into breast milk. Caution should be exercised when zolmitriptan is administered to a nursing woman. Consider pumping and discarding milk for 24 hours after a dose.
Infant Risk:
L3 (Moderate risk) - Potential for infant exposure and adverse effects. Monitor infant for drowsiness, poor feeding, or other signs of drug exposure.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients under 18 years of age. Use is not recommended in this population.
Geriatric Use
Use with caution in patients over 65 years of age due to a higher likelihood of underlying cardiovascular disease and potential for increased sensitivity to the drug's effects. No specific dose adjustment is generally required unless hepatic impairment is present.
Clinical Information
Clinical Pearls
- Zolmitriptan ODT is designed to dissolve on the tongue and does not require water, making it convenient for use anywhere.
- It is for acute treatment of migraine, not for prevention or for other types of headaches (e.g., hemiplegic or basilar migraine).
- Patients should be screened for cardiovascular risk factors before initiating triptan therapy.
- Risk of medication overuse headache (MOH) if used too frequently (e.g., 10 or more days per month).
- Advise patients to report any chest pain, tightness, or other concerning symptoms immediately.
Alternative Therapies
- Other triptans (e.g., sumatriptan, rizatriptan, eletriptan, frovatriptan, naratriptan)
- CGRP receptor antagonists (e.g., rimegepant, ubrogepant)
- NSAIDs (e.g., ibuprofen, naproxen)
- Acetaminophen
- Ergot alkaloids (e.g., ergotamine, dihydroergotamine)
- Anti-emetics (for associated nausea/vomiting)
Cost & Coverage
Average Cost:
Varies widely, typically $10-$50 per 6 tablets (2.5mg ODT)
Generic Available:
Yes
Insurance Coverage:
Tier 1 or Tier 2 (generic); Tier 3 or higher (brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about your medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.