Zolmitriptan 5mg Nasal Spray
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
Nov 2003
DEA Schedule
Not Controlled
Overview
What is this medicine?
Zolmitriptan nasal spray 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
Proper Use of This Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to use this medication as directed.
This medication is for nasal use only. Do not take it by mouth.
Before using, blow your nose to ensure the nasal passage is clear.
To administer, spray a single dose into one nostril as soon as possible after the onset of an attack.
If your headache does not improve after the first dose, consult your doctor. If your headache recurs, you may take a second dose if advised by your doctor. However, you must wait at least 2 hours after the first dose before taking the second dose.
Storage and Disposal
To maintain the medication's effectiveness, store it:
At room temperature
Protected from light
In a dry place
Avoid storing in a bathroom
Missed Dose
Since this medication is taken as needed, there is no scheduled dosing. Do not use it more frequently than recommended by your doctor.
To use this medication correctly, follow your doctor's instructions and read all the information provided. It is essential to use this medication as directed.
This medication is for nasal use only. Do not take it by mouth.
Before using, blow your nose to ensure the nasal passage is clear.
To administer, spray a single dose into one nostril as soon as possible after the onset of an attack.
If your headache does not improve after the first dose, consult your doctor. If your headache recurs, you may take a second dose if advised by your doctor. However, you must wait at least 2 hours after the first dose before taking the second dose.
Storage and Disposal
To maintain the medication's effectiveness, store it:
At room temperature
Protected from light
In a dry place
Avoid storing in a bathroom
Missed Dose
Since this medication is taken as needed, there is no scheduled dosing. Do not use it more frequently than recommended by your doctor.
Lifestyle & Tips
- Use at the first sign of a migraine headache, but it can be used at any time during a migraine attack.
- Do not use for more than 10 days per month to avoid medication overuse headache.
- Avoid known migraine triggers (e.g., certain foods, stress, lack of sleep, strong smells).
- Maintain a regular sleep schedule and healthy lifestyle.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
Initial dose 2.5 mg or 5 mg. May repeat after 2 hours if needed. Maximum 10 mg in any 24-hour period.
Dose Range:
2.5 - 10 mg
Condition-Specific Dosing:
initial_dose:
2.5 mg or 5 mg
repeat_dose_interval:
After 2 hours
max_24_hours:
10 mg
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established (safety and efficacy not established for children under 12 years)
Adolescent:
For adolescents 12 years and older: Initial dose 2.5 mg. May repeat after 2 hours if needed. Maximum 5 mg in any 24-hour period.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed
Moderate:
No dose adjustment needed
Severe:
No dose adjustment needed
Dialysis:
No specific recommendations; use with caution due to potential for accumulation of metabolites.
Hepatic Impairment:
Mild:
No dose adjustment needed
Moderate:
Maximum 5 mg in any 24-hour period
Severe:
Maximum 5 mg in any 24-hour period
Pharmacology
Mechanism of Action
Zolmitriptan is a selective agonist for 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptors. Its therapeutic action in migraine is thought to be due to selective constriction of cranial blood vessels, inhibition of pro-inflammatory neuropeptide release from trigeminal nerve endings, and inhibition of pain signal transmission in the trigeminal system.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 40% (nasal)
Tmax:
3 hours (nasal spray)
FoodEffect:
Not clinically significant for nasal spray
Distribution:
Vd:
2.4 L/kg
ProteinBinding:
Approximately 25%
CnssPenetration:
Yes
Elimination:
HalfLife:
2.5-3 hours (zolmitriptan); 5.7-6.1 hours (active N-desmethyl metabolite)
Clearance:
Not available (systemic clearance is approximately 31.5 mL/min/kg)
ExcretionRoute:
Primarily renal (65%), fecal (30%)
Unchanged:
Approximately 4% (urine), approximately 1% (feces)
Pharmacodynamics
OnsetOfAction:
As early as 15 minutes (nasal spray)
PeakEffect:
1-3 hours
DurationOfAction:
Up to 24 hours for migraine relief
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 immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness or swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache or dizziness
+ Fainting or changes in vision
Vision changes or loss of eyesight (which can be long-lasting)
Severe stomach pain or bloody diarrhea
Weight loss
Leg cramps or a 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 or coordination
+ Confusion
+ Hallucinations
+ Fever
+ Abnormal heartbeat or flushing
+ Muscle twitching or stiffness
+ Seizures
+ Shivering or shaking
+ Excessive sweating
+ Severe diarrhea, nausea, or vomiting
+ Severe headache
Heart problems, including:
+ Heart attack
+ Abnormal heartbeat
+ Chest, throat, neck, or jaw tightness, pain, pressure, or heaviness
+ Cold sweats
+ Shortness of breath
+ Fast or irregular heartbeat
+ Severe dizziness or fainting
Brain blood vessel problems, including:
+ Stroke
+ Weakness on one side of the body
+ Difficulty speaking or thinking
+ Changes in balance or coordination
+ Drooping on one side of the face
+ Changes in vision
Other Possible 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 if you notice any of the following:
Dizziness, drowsiness, tiredness, or weakness
Feeling of warmth or heaviness
Dry mouth
Upset stomach or vomiting
Changes in taste
* Nose irritation
If you experience any side effects that bother you or do not go away, contact your doctor for advice. 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 immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness or swelling of the mouth, face, lips, tongue, or throat
Signs of high blood pressure, including:
+ Severe headache or dizziness
+ Fainting or changes in vision
Vision changes or loss of eyesight (which can be long-lasting)
Severe stomach pain or bloody diarrhea
Weight loss
Leg cramps or a 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 or coordination
+ Confusion
+ Hallucinations
+ Fever
+ Abnormal heartbeat or flushing
+ Muscle twitching or stiffness
+ Seizures
+ Shivering or shaking
+ Excessive sweating
+ Severe diarrhea, nausea, or vomiting
+ Severe headache
Heart problems, including:
+ Heart attack
+ Abnormal heartbeat
+ Chest, throat, neck, or jaw tightness, pain, pressure, or heaviness
+ Cold sweats
+ Shortness of breath
+ Fast or irregular heartbeat
+ Severe dizziness or fainting
Brain blood vessel problems, including:
+ Stroke
+ Weakness on one side of the body
+ Difficulty speaking or thinking
+ Changes in balance or coordination
+ Drooping on one side of the face
+ Changes in vision
Other Possible 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 if you notice any of the following:
Dizziness, drowsiness, tiredness, or weakness
Feeling of warmth or heaviness
Dry mouth
Upset stomach or vomiting
Changes in taste
* Nose irritation
If you experience any side effects that bother you or do not go away, contact your doctor for advice. 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 or angina)
- Shortness of breath
- Weakness or numbness on one side of the body
- Sudden vision changes or loss of vision
- Slurred speech or difficulty speaking
- Confusion or hallucinations
- Fever, sweating, fast heartbeat, muscle stiffness, twitching, loss of coordination, nausea, vomiting, or diarrhea (signs of serotonin syndrome)
- Severe stomach pain or bloody diarrhea (rare, but could indicate ischemic colitis)
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:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction and its symptoms.
Certain health conditions, including:
+ High blood pressure
+ Liver disease
A history of specific health problems, such as:
+ 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 heart rhythms, such as Wolff-Parkinson-White syndrome
Recent use of certain medications for depression, including isocarboxazid, phenelzine, or tranylcypromine, within the last 14 days. Taking 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.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. Ensure 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:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction and its symptoms.
Certain health conditions, including:
+ High blood pressure
+ Liver disease
A history of specific health problems, such as:
+ 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 heart rhythms, such as Wolff-Parkinson-White syndrome
Recent use of certain medications for depression, including isocarboxazid, phenelzine, or tranylcypromine, within the last 14 days. Taking 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.
This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. Ensure 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. 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 exacerbate your headaches.
Regular blood pressure monitoring is recommended, as medications like this one can cause high blood pressure. Follow your doctor's instructions for blood pressure checks.
If you have risk factors for heart disease, such as high blood pressure, high cholesterol, being overweight, having high blood sugar or diabetes, smoking, 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.
For individuals 65 years or older, it is crucial to use this medication with caution, as you may be more susceptible to side effects.
This medication is not approved for use in children under 12 years old; consult with your doctor to discuss potential alternatives.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to weigh the benefits and risks of this medication for 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 exacerbate your headaches.
Regular blood pressure monitoring is recommended, as medications like this one can cause high blood pressure. Follow your doctor's instructions for blood pressure checks.
If you have risk factors for heart disease, such as high blood pressure, high cholesterol, being overweight, having high blood sugar or diabetes, smoking, 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.
For individuals 65 years or older, it is crucial to use this medication with caution, as you may be more susceptible to side effects.
This medication is not approved for use in children under 12 years old; consult with your doctor to discuss potential alternatives.
If you are pregnant, plan to become pregnant, or are breastfeeding, inform your doctor to weigh the benefits and risks of this medication for both you and your baby.
Overdose Information
Overdose Symptoms:
- Sedation
- Ataxia (loss of coordination)
- Mild to moderate increases in heart rate
- Mild to moderate increases in blood pressure
What to Do:
Seek immediate medical attention. There is no specific antidote. Treatment should be supportive and symptomatic. Monitor ECG and blood pressure. Call 1-800-222-1222 (Poison Control Center) for further guidance.
Drug Interactions
Contraindicated Interactions
- Monoamine oxidase-A (MAO-A) inhibitors (within 2 weeks of use)
- Ergot-type medications (e.g., ergotamine, dihydroergotamine) (within 24 hours)
- Other 5-HT1 agonists (e.g., other triptans) (within 24 hours)
Major Interactions
- Selective serotonin reuptake inhibitors (SSRIs) and serotonin norepinephrine reuptake inhibitors (SNRIs) (increased risk of serotonin syndrome)
- Cimetidine (increases zolmitriptan Cmax and AUC)
Moderate Interactions
- Propranolol (increases zolmitriptan Cmax and AUC)
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Cardiovascular risk assessment
Rationale: To identify underlying cardiovascular disease or risk factors (e.g., hypertension, hypercholesterolemia, smoking, obesity, diabetes, family history of CAD) before initiating therapy, as triptans can cause coronary vasospasm.
Timing: Prior to initiation of therapy
Routine Monitoring
Efficacy of migraine relief
Frequency: As needed with each migraine episode
Target: Significant reduction or elimination of migraine pain and associated symptoms
Action Threshold: Lack of efficacy after appropriate dosing may warrant consideration of alternative treatments.
Adverse effects (e.g., chest pain, paresthesias, dizziness, neck/throat tightness)
Frequency: With each dose and during follow-up
Target: Absence or mild, transient nature of adverse effects
Action Threshold: Persistent, severe, or new onset of adverse effects, especially chest pain or neurological symptoms, requires immediate medical evaluation.
Symptom Monitoring
- Chest pain, tightness, or pressure (may indicate cardiac ischemia or vasospasm)
- Shortness of breath
- Palpitations
- Dizziness, vertigo
- Paresthesias (tingling, numbness)
- Neck or throat tightness/pressure
- Weakness, fatigue
- Signs of serotonin syndrome: agitation, hallucinations, delirium, tachycardia, labile blood pressure, hyperthermia, hyperreflexia, incoordination, nausea, vomiting, diarrhea
- Signs of stroke or transient ischemic attack (TIA): sudden numbness or weakness, vision changes, speech difficulty, confusion, severe headache
Special Patient Groups
Pregnancy
Zolmitriptan is classified as Pregnancy Category C. Studies in animals have shown adverse effects on the fetus, but there are no adequate and well-controlled studies in pregnant women. It should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Potential for developmental toxicity observed in animal studies. Use only if clearly needed.
Second Trimester:
Potential for developmental toxicity observed in animal studies. Use only if clearly needed.
Third Trimester:
Potential for developmental toxicity observed in animal studies. Use only if clearly needed. Consider potential for vasoconstrictive effects on uterine blood flow.
Lactation
Zolmitriptan and its active metabolite are excreted into breast milk. The amount is generally low, and adverse effects in breastfed infants are unlikely. However, caution is advised.
Infant Risk:
Low risk. Monitor infant for drowsiness, poor feeding, or unusual irritability. Consider waiting 24 hours after a dose before breastfeeding to minimize infant exposure, though this is often not necessary based on current data.
Pediatric Use
Approved for acute treatment of migraine with or without aura in adolescents 12 years of age and older. Safety and efficacy have not been established for children younger than 12 years.
Geriatric Use
Use with caution in elderly patients (over 65 years) due to a higher likelihood of underlying cardiovascular disease and potential for increased sensitivity to adverse effects. A cardiovascular evaluation is recommended prior to initiation.
Clinical Information
Clinical Pearls
- Zolmitriptan nasal spray is effective for acute migraine treatment, including those with aura or without.
- It can be administered at any time during a migraine attack, but is generally most effective when taken at the first sign of migraine symptoms.
- Do not use for basilar or hemiplegic migraine due to lack of established efficacy and potential for increased risk of adverse events.
- Patients should be advised on the proper administration technique for the nasal spray to ensure optimal absorption.
- Counsel patients on the risk of medication overuse headache if used too frequently (more than 10 days per month).
Alternative Therapies
- Other triptans (e.g., sumatriptan, rizatriptan, eletriptan, frovatriptan, naratriptan, almotriptan)
- CGRP receptor antagonists (e.g., ubrogepant, rimegepant, zavegepant)
- Non-steroidal anti-inflammatory drugs (NSAIDs) (e.g., ibuprofen, naproxen)
- Acetaminophen
- Ergot alkaloids (e.g., ergotamine, dihydroergotamine)
- Anti-emetics (e.g., metoclopramide, prochlorperazine) for associated nausea/vomiting
Cost & Coverage
Average Cost:
Varies widely, typically $50-$200 per 6 nasal spray devices (5mg)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (for generic), Tier 3 or Tier 4 (for brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is 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 it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this 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 overdose, including the medication taken, the amount, and the time it occurred.