Zolmitriptan 2.5mg Tablets

Manufacturer GLENMARK Active Ingredient Zolmitriptan Tablets(zohl mi TRIP tan) Pronunciation ZOHL-mi-TRIP-tan
It is used to treat migraine headaches.
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Drug Class
Antimigraine agent
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Pharmacologic Class
Selective serotonin (5-HT1B/1D) receptor agonist
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Pregnancy Category
Category C
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FDA Approved
Oct 1997
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Zolmitriptan is a medication used to treat migraine headaches. It works by narrowing blood vessels in the brain and affecting certain nerves, which helps to relieve migraine pain and other symptoms like nausea and sensitivity to light and sound. It is not used to prevent migraines, but to treat them once they have started.
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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 this medication with or without food. If needed, you can break the tablet in half, but do not chew or crush it. Take the medication with a liquid as soon as possible after your headache symptoms start.

If your headache does 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 dose.

Storing and Disposing of Your Medication

Store your medication at room temperature, away from light and moisture. Keep it in a dry place, avoiding storage 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 more frequent doses than prescribed by your doctor.
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Lifestyle & Tips

  • Take Zolmitriptan as soon as your migraine symptoms start, but not before the headache begins (e.g., during the aura phase).
  • Do not take more than the prescribed dose or more than two doses in 24 hours.
  • If your headache returns after the first dose, you can take a second dose after 2 hours.
  • Avoid driving or operating machinery if you experience dizziness or drowsiness.
  • Limit alcohol consumption, as it can worsen headaches or interact with the medication.
  • Discuss all other medications, including over-the-counter drugs, supplements, and herbal products, with your doctor to avoid potential interactions.

Dosing & Administration

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Adult Dosing

Standard Dose: 2.5 mg or 5 mg orally at the onset of migraine headache. May repeat dose after 2 hours if headache recurs. Maximum 10 mg in any 24-hour period.
Dose Range: 2.5 - 5 mg

Condition-Specific Dosing:

acute_migraine: Initial dose 2.5 mg or 5 mg. If headache recurs, a second dose may be administered after 2 hours. Max 10 mg/24 hours.
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Pediatric Dosing

Neonatal: Not established
Infant: Not established
Child: Not established (safety and efficacy not established for children under 12 years of age)
Adolescent: For adolescents 12 to 17 years of age: 2.5 mg orally at the onset of migraine headache. May repeat dose after 2 hours if headache recurs. Maximum 5 mg in any 24-hour period.
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Dose Adjustments

Renal Impairment:

Mild: No dose adjustment needed.
Moderate: No dose adjustment needed.
Severe: Use with caution. Consider lower initial doses and monitor for adverse effects.
Dialysis: Not specifically studied, but caution advised due to potential for accumulation of metabolites. Consider lower doses.

Hepatic Impairment:

Mild: No dose adjustment needed.
Moderate: Maximum single dose should not exceed 2.5 mg, and maximum daily dose should not exceed 5 mg.
Severe: Maximum single dose should not exceed 2.5 mg, and maximum daily dose should not exceed 5 mg.

Pharmacology

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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 selective vasoconstriction of intracranial blood vessels (which are dilated during a migraine attack) and inhibition of pro-inflammatory neuropeptide release from trigeminal nerve endings.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 40-48% (oral tablet)
Tmax: 1.5 to 3 hours
FoodEffect: Food has no significant effect on the absorption or pharmacokinetics of zolmitriptan.

Distribution:

Vd: Approximately 7 L/kg
ProteinBinding: Approximately 25%
CnssPenetration: Yes

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 (approximately 65%), Fecal (approximately 30%)
Unchanged: Approximately 4% (urine)
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Pharmacodynamics

OnsetOfAction: Within 45 minutes to 1 hour
PeakEffect: Approximately 2 to 3 hours
DurationOfAction: Up to 24 hours (though headache recurrence is possible)

Safety & Warnings

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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)
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 or coordination
+ Confusion
+ Hallucinations
+ Fever
+ Fast or abnormal heartbeat
+ Flushing
+ Muscle twitching or stiffness
+ Seizures
+ Shivering or shaking
+ Excessive sweating
+ Severe diarrhea, nausea, or vomiting
+ Severe headache
Heart problems, including heart attack and abnormal heartbeat, which may cause:
+ Chest, throat, neck, or jaw tightness, pain, pressure, or heaviness
+ Cold sweats
+ Shortness of breath
+ Fast or abnormal heartbeat
+ Severe dizziness or fainting
Brain blood vessel problems, including stroke, which may cause:
+ 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
* Nausea or vomiting

If you experience any of these side effects or any other unusual symptoms, 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.
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Seek Immediate Medical Attention If You Experience:

  • Severe chest pain, tightness, or pressure (could be heart attack or stroke symptoms)
  • Shortness of breath
  • Sudden severe stomach pain or bloody diarrhea (rare, but could indicate ischemic colitis)
  • Weakness or numbness on one side of the body
  • Slurred speech or vision changes
  • Signs of serotonin syndrome: agitation, hallucinations, rapid heart rate, fever, sweating, shivering, muscle stiffness or twitching, loss of coordination, nausea, vomiting, diarrhea (especially if taking with SSRIs/SNRIs)
  • Allergic reactions: rash, hives, swelling of face/lips/tongue, difficulty breathing
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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 treatment:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Describe the allergic reaction you experienced, including the 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, like 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. Taking 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 under 18 years of age, inform your doctor. This medication is not approved for use in children younger than 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.
* Before starting, stopping, or changing the dose of any medication, consult with your doctor to ensure it is safe to take this medication with your other medications and health conditions.
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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 differs 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 drugs similar to this one have been associated with high blood pressure, it is crucial to monitor your blood pressure as advised 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 are 65 years or older, use this medication with caution, as you may be more susceptible to side effects. Pregnant women, those planning to become pregnant, or breastfeeding mothers should consult their doctor to weigh the benefits and risks of using this medication to themselves and their baby.
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Overdose Information

Overdose Symptoms:

  • Sedation
  • Ataxia (loss of coordination)
  • Transient increase in blood pressure
  • Other symptoms related to excessive serotonergic activity

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Treatment is supportive, including monitoring of cardiovascular and respiratory function.

Drug Interactions

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Contraindicated Interactions

  • Ergot-type drugs (e.g., ergotamine, dihydroergotamine) within 24 hours of zolmitriptan
  • Other 5-HT1B/1D agonists (triptans) within 24 hours of zolmitriptan
  • Monoamine Oxidase-A (MAO-A) inhibitors (e.g., phenelzine, tranylcypromine, moclobemide) within 2 weeks of zolmitriptan
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Major Interactions

  • Selective Serotonin Reuptake Inhibitors (SSRIs) and Serotonin Norepinephrine Reuptake Inhibitors (SNRIs) - increased risk of serotonin syndrome
  • Cimetidine - significantly increases zolmitriptan plasma concentrations
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Moderate Interactions

  • Propranolol - may slightly increase zolmitriptan Cmax and AUC (clinical significance generally minor)
  • Oral contraceptives - may slightly increase zolmitriptan Cmax and AUC (clinical significance generally minor)

Monitoring

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Baseline Monitoring

Diagnosis of migraine

Rationale: Ensure appropriate indication and rule out other neurological conditions.

Timing: Prior to initiation of therapy

Cardiovascular risk assessment

Rationale: Zolmitriptan is contraindicated in patients with ischemic heart disease, uncontrolled hypertension, or other significant cardiovascular conditions.

Timing: Prior to initiation of therapy

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Routine Monitoring

Efficacy of headache relief

Frequency: With each dose

Target: Significant reduction or complete resolution of migraine symptoms

Action Threshold: If no relief or worsening of symptoms, re-evaluate diagnosis or treatment plan.

Adverse effects (e.g., chest pain, tightness, paresthesias, dizziness, somnolence)

Frequency: With each dose and during follow-up

Target: Absence or mild, tolerable side effects

Action Threshold: Severe or persistent adverse effects, especially chest pain, warrant immediate medical attention and discontinuation.

Blood pressure (in patients with hypertension)

Frequency: Periodically, especially if hypertension is a concern

Target: Within target range

Action Threshold: Significant increase in blood pressure may require discontinuation or adjustment of antihypertensive therapy.

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Symptom Monitoring

  • Headache intensity and duration
  • Associated symptoms (nausea, vomiting, photophobia, phonophobia)
  • Recurrence of headache
  • Presence of chest pain, tightness, or pressure
  • Tingling, numbness, or paresthesias
  • Dizziness or somnolence
  • Neck pain or stiffness
  • Flushing or warmth sensation

Special Patient Groups

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Pregnancy

Category C. Should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Limited human data available.

Trimester-Specific Risks:

First Trimester: Limited data, potential for increased risk of certain birth defects not definitively established but cannot be ruled out.
Second Trimester: Limited data, no clear evidence of increased risk.
Third Trimester: Limited data, no clear evidence of increased risk. Potential for uterine effects (vasoconstriction) theoretically possible but not well-studied.
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Lactation

Zolmitriptan and its metabolites are excreted into breast milk. Caution should be exercised when zolmitriptan is administered to a nursing woman.

Infant Risk: L3 (Moderately safe). Potential for infant exposure. Consider pumping and discarding breast milk for 24 hours after a dose to minimize infant exposure, especially with repeated dosing.
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Pediatric Use

Approved for acute treatment of migraine with or without aura in adolescents 12 to 17 years of age. Safety and efficacy not established for children younger than 12 years.

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Geriatric Use

Use with caution. Elderly patients may be more sensitive to the effects of triptans, particularly cardiovascular effects. Consider lower initial doses and monitor closely for adverse reactions due to potential for decreased renal, hepatic, or cardiac function, and concomitant disease or other drug therapy.

Clinical Information

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Clinical Pearls

  • Zolmitriptan is for acute migraine treatment, not for prevention or for cluster headaches.
  • It should not be used for hemiplegic or basilar migraine due to lack of efficacy data and potential for increased risk of adverse events.
  • Patients should be screened for cardiovascular risk factors before starting triptan therapy.
  • Risk of serotonin syndrome is increased when co-administered with SSRIs, SNRIs, or other serotonergic drugs. Educate patients on symptoms.
  • Do not use within 24 hours of other triptans or ergot-type medications.
  • Oral disintegrating tablets (ODT) are available for patients who have difficulty swallowing or experience nausea/vomiting.
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Alternative Therapies

  • Other Triptans (e.g., Sumatriptan, Rizatriptan, Eletriptan, Frovatriptan, Naratriptan)
  • CGRP Receptor Antagonists (Gepants, e.g., Ubrogepant, Rimegepant)
  • Serotonin 5-HT1F Receptor Agonists (Ditans, e.g., Lasmiditan)
  • NSAIDs (e.g., Ibuprofen, Naproxen)
  • Acetaminophen
  • Combination analgesics (e.g., Excedrin Migraine)
  • Antiemetics (e.g., Metoclopramide, Prochlorperazine) for associated nausea/vomiting
  • Ergot alkaloids (e.g., Ergotamine, Dihydroergotamine - generally less preferred due to side effects and interactions)
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Cost & Coverage

Average Cost: $15 - $50 per 6 tablets (2.5mg)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (Generic), Tier 3 (Brand)
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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 happened.