Zolmitriptan 5mg ODT Tablets
It is used to treat migraine headaches.
Drug Class
Antimigraine agent
Pharmacologic Class
Selective serotonin 5-HT1B/1D receptor agonist
Pregnancy Category
Category C
FDA Approved
Sep 2000
DEA Schedule
Not Controlled
Overview
What is this medicine?
Zolmitriptan is a medication used to treat migraine headaches. It works by narrowing blood vessels in the brain and reducing substances that cause pain, nausea, and other migraine symptoms. It is not for preventing migraines, but for treating them once they start.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take the medication with or without food, and use it immediately after opening the packaging. When opening the foil, 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 the medication as soon as possible after your 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 the second 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 the medication more frequently than your doctor has prescribed.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take the medication with or without food, and use it immediately after opening the packaging. When opening the foil, 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 the medication as soon as possible after your 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 the second 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 the medication more frequently than your doctor has prescribed.
Lifestyle & Tips
- Take at the first sign of a migraine headache, but not for aura without headache.
- Do not take more than 10 mg in any 24-hour period.
- Do not use for more than 10 days per month to avoid medication overuse headache.
- Avoid migraine triggers (e.g., certain foods, stress, lack of sleep).
- Do not drive or operate machinery if you experience dizziness or drowsiness.
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 migraine recurs or partially responds. Max 10 mg in 24 hours.
Dose Range:
2.5 - 5 mg
Condition-Specific Dosing:
initial_dose:
2.5 mg or 5 mg
repeat_dose_interval:
2 hours
maximum_daily_dose:
10 mg
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (Safety and efficacy not established in patients under 12 years of age)
Adolescent:
Not established (Safety and efficacy not established in patients under 12 years of age)
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
No dosage adjustment necessary.
Severe:
No dosage adjustment necessary.
Hepatic Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
Consider lower initial dose (e.g., 2.5 mg). Max 5 mg in 24 hours.
Severe:
Consider lower initial dose (e.g., 2.5 mg). Max 5 mg in 24 hours.
Pharmacology
Mechanism of Action
Zolmitriptan is a selective agonist for 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptors. It is believed to exert its antimigraine effects through vasoconstriction of intracranial blood vessels, inhibition of neuropeptide release (e.g., calcitonin gene-related peptide, substance P) from trigeminal afferents, and inhibition of pain signal transmission in the trigeminal nucleus caudalis.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 40% (oral tablet), similar for ODT.
Tmax:
1.5 to 3 hours (for ODT).
FoodEffect:
Food has no significant effect on absorption.
Distribution:
Vd:
Approximately 2.4 L/kg.
ProteinBinding:
Approximately 25%.
CnssPenetration:
Yes (crosses blood-brain barrier).
Elimination:
HalfLife:
Approximately 2.5 to 3 hours (zolmitriptan and active metabolite).
Clearance:
Approximately 31 mL/min/kg.
ExcretionRoute:
Renal (65%) and fecal (30%), primarily as metabolites.
Unchanged:
Approximately 10% (renal), 1% (fecal).
Pharmacodynamics
OnsetOfAction:
Within 1 hour (for ODT).
PeakEffect:
2-3 hours.
DurationOfAction:
Up to 24 hours (migraine relief).
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Immediately
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 right away:
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 sensations, such as burning, numbness, or tingling
Serotonin syndrome, a potentially life-threatening condition, which may cause:
+ 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, including heart attack and abnormal heartbeat, which can occur rarely within a few hours of taking this medication. Seek help if you experience:
+ 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, including stroke, which can occur rarely. Seek help if you experience:
+ 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 Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical attention:
Feeling dizzy, sleepy, tired, or weak
Feeling of warmth
Feeling of heaviness or pressure
Dry mouth
Upset stomach or vomiting
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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 right away:
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 sensations, such as burning, numbness, or tingling
Serotonin syndrome, a potentially life-threatening condition, which may cause:
+ 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, including heart attack and abnormal heartbeat, which can occur rarely within a few hours of taking this medication. Seek help if you experience:
+ 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, including stroke, which can occur rarely. Seek help if you experience:
+ 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 Possible Side Effects
Like all medications, this drug can cause side effects, although many people may not experience any or may only have mild symptoms. If you notice any of the following side effects or any other symptoms that bother you or do not go away, contact your doctor or seek medical attention:
Feeling dizzy, sleepy, tired, or weak
Feeling of warmth
Feeling of heaviness or pressure
Dry mouth
Upset stomach or vomiting
Reporting Side Effects
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, 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 neck tightness (could be heart-related)
- Shortness of breath
- Weakness or numbness on one side of the body, slurred speech, sudden vision changes (signs of stroke)
- Severe stomach pain, bloody diarrhea (rare, but serious)
- Confusion, agitation, hallucinations, rapid heart rate, sweating, muscle stiffness, twitching, loss of coordination, severe nausea/vomiting/diarrhea (signs of serotonin syndrome)
- Allergic reaction (rash, hives, swelling of face/lips/tongue, 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 reactions you have experienced.
Certain health conditions, such as high blood pressure or liver disease.
A history of specific health problems, including:
+ 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, such as hemiplegic or basilar migraines
+ Abnormal heart rhythms, like Wolff-Parkinson-White syndrome
Recent use of certain depression medications, such as 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 migraines, 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 under 18 years of age, please note that this medication is not approved for use in children younger than 18 years of age.
Interactions with Other Medications and Health Conditions:
This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins.
* You must verify that it is safe to take this medication with all your other medications and health conditions. 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 reactions you have experienced.
Certain health conditions, such as high blood pressure or liver disease.
A history of specific health problems, including:
+ 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, such as hemiplegic or basilar migraines
+ Abnormal heart rhythms, like Wolff-Parkinson-White syndrome
Recent use of certain depression medications, such as 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 migraines, 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 under 18 years of age, please note that this medication is not approved for use in children younger than 18 years of age.
Interactions with Other Medications and Health Conditions:
This list is not exhaustive, and it is crucial to inform your doctor and pharmacist about all your medications, including prescription and over-the-counter drugs, natural products, and vitamins.
* You must verify that it is safe to take this medication with all your other medications and health conditions. 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. Until you understand how this drug affects you, avoid operating a vehicle or engaging in activities that require alertness. This medication is not intended to prevent or reduce the frequency of migraine headaches; it is designed to treat individual migraine episodes. If you experience a headache that is unusual or different from your typical migraine, consult your doctor before taking this medication.
Taking a higher dose or using this medication more frequently than prescribed by your doctor may lead to worsening headaches. As this type of medication can cause high blood pressure, it is crucial to have your blood pressure monitored as directed by your doctor. 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 before taking this medication, as some products contain phenylalanine. Individuals 65 years or older should use this medication with caution, as they may be more susceptible to side effects. Pregnant or breastfeeding women, or those planning to become pregnant, should discuss the potential benefits and risks of this medication with their doctor to make an informed decision.
Taking a higher dose or using this medication more frequently than prescribed by your doctor may lead to worsening headaches. As this type of medication can cause high blood pressure, it is crucial to have your blood pressure monitored as directed by your doctor. 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 before taking this medication, as some products contain phenylalanine. Individuals 65 years or older should use this medication with caution, as they may be more susceptible to side effects. Pregnant or breastfeeding women, or those planning to become pregnant, should discuss the potential benefits and risks of this medication with their doctor to make an informed decision.
Overdose Information
Overdose Symptoms:
- Sedation
- Ataxia (loss of coordination)
- Peripheral vasoconstriction (cold, pale extremities)
- Hypertension
What to Do:
Seek immediate medical attention or call 911. There is no specific antidote. Treatment is supportive and symptomatic. Monitor cardiac and respiratory function for at least 15 hours or until symptoms resolve. Call 1-800-222-1222 for Poison Control.
Drug Interactions
Contraindicated Interactions
- Monoamine Oxidase Inhibitors (MAOIs) (concurrent use or within 2 weeks of discontinuing MAOIs)
- Ergot-type medications (e.g., ergotamine, dihydroergotamine, methysergide) (concurrent use or within 24 hours)
- Other 5-HT1 agonists (e.g., sumatriptan, naratriptan, rizatriptan) (concurrent use or within 24 hours)
- Ischemic heart disease (angina pectoris, history of myocardial infarction, documented silent ischemia)
- Cerebrovascular syndromes (including stroke, transient ischemic attack)
- Peripheral vascular disease
- Uncontrolled hypertension
- Hemiplegic or basilar migraine
Major Interactions
- Selective Serotonin Reuptake Inhibitors (SSRIs) / Serotonin Norepinephrine Reuptake Inhibitors (SNRIs) (increased risk of serotonin syndrome)
- Cimetidine (increases zolmitriptan Cmax and AUC by 44% and 48% respectively, due to inhibition of CYP1A2 and MAO-A)
Moderate Interactions
- Oral Contraceptives (may increase zolmitriptan levels slightly, but generally not clinically significant)
- Propranolol (no significant interaction)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Cardiovascular assessment (history of ischemic heart disease, uncontrolled hypertension, cerebrovascular disease)
Rationale: To rule out contraindications and assess risk of serious cardiovascular events.
Timing: Prior to initiation of therapy.
Blood pressure
Rationale: To ensure hypertension is controlled, as triptans can cause transient increases in blood pressure.
Timing: Prior to initiation.
Routine Monitoring
Migraine frequency and severity
Frequency: Each visit or as needed.
Target: Reduction in headache days and pain intensity.
Action Threshold: Lack of efficacy, increasing frequency of use (medication overuse headache risk).
Adverse effects (e.g., chest pain, neck/jaw tightness, paresthesias, dizziness)
Frequency: Each visit or as needed.
Target: Absence or mild, tolerable effects.
Action Threshold: Severe or persistent adverse effects, signs of serotonin syndrome, or ischemic events.
Blood pressure (if risk factors present)
Frequency: Periodically, especially in patients with controlled hypertension.
Target: Within target range.
Action Threshold: Significant or sustained increase in blood pressure.
Symptom Monitoring
- Chest pain, tightness, or pressure (especially in the jaw, neck, or throat)
- Shortness of breath
- Weakness or numbness on one side of the body
- Slurred speech
- Sudden severe headache (different from usual migraine)
- Confusion, agitation, hallucinations, rapid heart rate, sweating, muscle rigidity, tremor, incoordination (signs of serotonin syndrome)
- Vision changes
Special Patient Groups
Pregnancy
Category C. Use only if the potential benefit justifies the potential risk to the fetus. Limited human data; animal studies show adverse effects at high doses.
Trimester-Specific Risks:
First Trimester:
Potential for increased risk of certain birth defects cannot be definitively ruled out, but data are limited and conflicting.
Second Trimester:
Not well studied, but generally considered less risky than first trimester for structural defects.
Third Trimester:
Not well studied. Risk of uterine contractions or fetal distress theoretically possible due to vasoconstrictive effects, but not established.
Lactation
Zolmitriptan and its metabolites are excreted into breast milk. Caution should be exercised when administered to a nursing woman. Consider pumping and discarding milk for 24 hours after a dose.
Infant Risk:
L3 (Moderately safe). Potential for infant exposure and adverse effects (e.g., drowsiness, poor feeding) is low but possible. Monitor infant for signs of adverse effects.
Pediatric Use
Safety and efficacy have not been established in patients under 12 years of age. Not recommended for routine use in children. Limited data in adolescents (12-17 years) suggest efficacy may be lower than in adults.
Geriatric Use
Use with caution in elderly patients (over 65 years). While pharmacokinetics are similar, elderly patients may be at higher risk for cardiovascular disease and adverse events. Consider lower initial doses and careful monitoring.
Clinical Information
Clinical Pearls
- Zolmitriptan ODT can be taken without water, making it convenient for patients with nausea or when water is not readily available.
- It is important to take zolmitriptan at the first sign of a migraine headache, but not during the aura phase if no headache follows.
- Patients should be screened for cardiovascular risk factors before initiating triptan therapy.
- Educate patients on the risk of medication overuse headache if triptans are used too frequently (more than 10 days per month).
- Advise patients to report any unusual symptoms, especially chest pain or neurological changes, immediately.
Alternative Therapies
- Non-steroidal anti-inflammatory drugs (NSAIDs) for mild to moderate migraines
- CGRP receptor antagonists (e.g., rimegepant, ubrogepant)
- Ditans (e.g., lasmiditan)
- Ergot alkaloids (e.g., ergotamine, dihydroergotamine) (less commonly used due to side effects)
- Antiemetics (e.g., ondansetron, metoclopramide) for associated nausea/vomiting
Cost & Coverage
Average Cost:
$20 - $100 per 6-12 tablets (generic 2.5mg/5mg)
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 medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.