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Naratriptan - Uses, Dosage, Side Effects and Special Considerations

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Naratriptan - Uses, Dosage, Side Effects and Special Considerations

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Naratriptan is a triptan drug used to treat acute migraines in adults. Read the below article for particulars on Naratriptan.

Medically reviewed by

Dr. Abhishek Juneja

Published At July 25, 2022
Reviewed AtNovember 25, 2022

Overview:

Naratriptan is a serotonin (5-HT 1B/1D) receptor agonist or a triptan drug. It is marketed by GlaxoSmithKline and was approved for the use of migraines by the Food and Drug Administration (FDA) in 1998.

This drug is indicated for the treatment of acute migraine in adults (with or without aura).

Naratriptan belongs to the selective serotonin receptor agonist class of drugs. It narrows the brain's blood vessels and blocks pain signals from reaching it. Additionally, it can stop the release of substances that result in migraine symptoms, such as pain and nausea.

Generic versions of Naratriptan are available from various drug manufacturers across the world, particularly since the expiry of the initial patent for the production of Naratriptan in 2010.

How Does Naratriptan Work?

Migraines are thought to be a result of the dilation of the blood vessels around the brain or the release of sensory neuropeptides. Naratriptan binds to the 5-HT1B/1D receptors that are present on the blood vessels around the brain and acts as an agonist at these receptors. It also acts as an agonist to the sensory nerves of the trigeminal system. The agonist effects of Naratriptan result in the constriction of the cranial blood vessels and inhibition of the release of sensory neuropeptides, thereby stopping migraine.

5-HT Receptors (5-hydroxytryptamine Receptors): 5-HT receptors are also known as serotonin receptors and are essentially a group of receptors that couple with G protein (G protein-coupled receptors) that mediate neurotransmission of excitatory and inhibitory impulses. They are present in the central and peripheral nervous systems.

5-HT1B receptor is a protein found in humans and a subtype of the 5-HT receptors. The HTR1B gene encodes it. It affects neurotransmission and vascular effects such as vasoconstriction in the brain and lungs.

5-HT1D receptor or HTR1D receptor is a protein encoded by the HTR1D gene. Its actions on the central nervous system lead to anxiety and locomotion changes. It also causes blood vessel constriction in the brain.

Sensory Neuropeptides: Sensory neuropeptides are released from sensory nerves that innervate blood vessels. They affect the activities of inflammatory cells and have a role in cardiovascular disease.

Uses of Naratriptan:

Naratriptan is used in the treatment of acute migraine in adults (with or without aura).

Limitations:

  • Naratriptan is not a prophylactic medication and should not be taken to prevent migraines.

  • It is not indicated for the treatment of cluster headaches.

Dosage Restrictions:

Route of Administration: Oral.

Dosage Strengths:

  • 1 mg tablet.

  • 2.5 mg tablet.

Dosage Forms:

  • 1 mg Tablets: White, D-shaped, film-coated tablets debossed with GX CE3.

  • 2.5 mg Tablets: Green, D-shaped, film-coated, debossed with GX CE5.

The recommended dosage may be either 1 mg or 2.5 mg, which can be repeated after four hours if the initial dose is not completely effective. The maximum dose that may be consumed in a day is 5 mg.

Special Considerations:

  • Renal Impairment: In patients with severe renal impairment, the clearance of Naratriptan is reduced. Mild to moderate renal impairment patients should start with 1 mg and may take a maximum of 2.5 mg daily.

  • Hepatic Impairment: Naratriptan clearance is reduced in patients with severe hepatic impairment. Mild to moderate hepatic impairment patients may start with 1 mg and work up to 2.5 mg per day.

Drug Safety Concerns:

  • Pregnancy: Naratriptan may cause fetal harm and should be used with caution in pregnant women.

Warnings and Contraindications:

Contraindications:

Naratriptan is contraindicated in the following conditions:

  • Patients with hypersensitivity to Naratriptan or any of the other components of the drug formulation.

  • Patients with ischemic coronary artery disease or coronary vasospasm.

  • Patients with a history of stroke.

  • Patients who have had hemiplegic or basilar migraine episodes as they are vulnerable to strokes.

  • Uncontrolled hypertension patients.

  • Patients suffering from peripheral vascular disease.

  • Patients with ischemic bowel disease.

  • Patients who have already used an ergot type or ergotamine-containing medication, or a 5HT-agonist in the past 24 hours.

  • Patients with severe renal impairment.

  • Patients with severe hepatic impairment.

Warnings and Precautions:

  • Myocardial Ischemia or Infarction: Patients with cardiovascular risk factors, including those with Prinzmetal’s angina, should undergo cardiac evaluation and be treated cautiously.

  • Arrhythmias: If arrhythmia occurs in a patient upon administration of Naratriptan, the drug should be discontinued immediately.

  • Cerebrovascular Conditions: If a hemorrhage (cerebral or subarachnoid hemorrhage) or stroke occurs, the medicine should be immediately discontinued.

  • Pressure of the Chest, Throat, Neck, Jaw: If the patient experiences pain, tightness, heaviness, or pressure in the chest, throat, neck, or jaw, it is usually not serious and unrelated to cardiovascular illness. However, they should be evaluated for coronary artery disease if they are at high risk for the same.

  • Gastrointestinal Symptoms: If the blood supply to the gastrointestinal tract is cut off or blocked (gastrointestinal ischemia) or the patient experiences localized or diffuse blood vessel constriction in the peripheral regions (peripheral vasospastic reactions), the medicine should be discontinued.

  • Serotonin Syndrome: Serotonin syndrome is a severe drug reaction caused in response to the high build-up of serotonin in the body. If this reaction occurs in a patient, Naratriptan should be stopped.

  • Medication Overuse Headache: Also known as rebound headaches, these headaches may occur on long-term use of drugs such as migraine medication (including Naratriptan). If such headaches occur, the patient may require detoxification.

For Patients:

What Is a Migraine?

A migraine is a headache that causes severe pain on one side of the head. The pain may be throbbing or pulsing in nature and varies in intensity. It is usually accompanied by nausea, vomiting, and sensitivity to light and sound.

What Is Aura?

Sensory disturbances that occur before the onset of migraine are collectively referred to as an aura.

These disturbances may include the following:

  • Tunnel vision.

  • Blind spots or scotomas.

  • Seeing light flashes.

  • Zigzagging lines in the visual field.

  • Tingling sensation in the hands and face.

  • Numbness.

  • Dizziness.

  • Ringing in the ears.

  • Difficulty finding words.

  • Difficulty understanding words or speech.

  • Weakness on one side of the face or body.

Why Is Naratriptan Prescribed For Migraine?

Naratriptan helps treat migraine symptoms, including throbbing headaches, nausea, and sensitivity to light or sound.

This drug works in the following ways:

  • It narrows the blood vessels around the brain.

  • It blocks the transmission of pain signals to the brain.

  • It stops the release of substances that contribute to migraine symptoms like pain and nausea.

Naratriptan should be taken as soon as you sense that a migraine headache is beginning.

Facts You Should Know About Naratriptan:

  • Naratriptan comes in tablet form and can be taken multiple times a day at four-hour intervals, provided the maximum dosage taken is 5 mg per day.

  • Do not take Naratriptan as a preventive measure against migraines. The drug is intended for actual acute attacks of migraine with or without aura.

  • If your symptoms do not improve within four hours of taking Naratriptan, you may need to stop taking the drug and find an alternative option. This should only be done on the advice of your physician.

How Should You Take Naratriptan?

  • Take Naratriptan in the manner and dosage strength prescribed to you by your doctor. 5 mg per day is the maximum recommended dosage.

  • Do not crush, chew, break, or split the tablets. Swallow the tablets whole with water.

  • You may be required to take your first dose of Naratriptan in the doctor’s office to monitor any side effects.

  • Take Naratriptan tablets with water or other liquids.

  • If no relief is obtained after using Naratriptan, do not immediately take another dose. Instead, consult your doctor and follow the instructions they give you.

  • Maintain a record of when and how often you get headaches and when you take Naratriptan, so your physician knows whether the drug is effective for you.

  • If you take too many Naratriptan tablets, you may end up suffering from medication overuse headaches, in which case you may be required to stop taking the drug.

What Should You Discuss With Your Doctor Before Beginning Naratriptan Therapy?

Naratriptan

Your doctor should be aware of the medications you take, any medical conditions you may have, and other relevant details relating to you, such as being pregnant or breastfeeding.

1. Medical History: Tell your doctor if you suffer from any of the following conditions:

  • Heart conditions.

  • Kidney issues.

  • Liver problems.

  • Diabetes.

  • Hypertension or high blood pressure.

  • High cholesterol levels.

  • Weight issues (being overweight).

  • Obesity.

Apart from these, let your doctor know if you are a smoker.

2. Drug History: Inform your doctor of all the prescription and over-the-counter medications you are taking, as well as any herbal supplements and vitamins. The medications you should be particularly wary about are antidepressant drugs. Let your doctor know if you are taking antidepressants.

3. Pregnancy: If you are pregnant or plan on getting pregnant, tell the doctor about it, as it is possible that Naratriptan can cause fetal harm.

4. Lactation: If you are breastfeeding or plan to do so in the near future, inform your doctor of the same. The possible presence of Naratriptan in breastmilk is unclear, so approach your doctor for information on how best to feed your baby while on Naratriptan.

Is Naratriptan Safe?

  • While Naratriptan is typically safe when availed and consumed as per prescriptions, there may be a few rare cases where patients experience side effects similar to heart conditions. These include pain, tightness, or heaviness in the chest, jaw, neck, and throat. However, these are not serious and are usually unrelated to heart conditions.

  • In addition, overuse may lead to headaches, so taking only the prescribed amount is essential.

Is Naratriptan Effective?

Naratriptan has proven effective and well-tolerated in treating migraine, particularly at a dose of 2.5 mg.

What Side Effects Can You Expect With Naratriptan?

  • Serious cardiac events, including myocardial infarction, exist in patients without coronary artery disease (CAD) history.

  • Cardiac rhythm disturbances (arrhythmias) include ventricular tachycardia (increased heart rate in the heart's lower chambers).

  • Cerebrovascular events like stroke and hemorrhage may occur.

  • Transient blindness, permanent blindness, and partial vision loss have been reported.

  • Non-coronary vasospastic reactions such as peripheral and gastrointestinal vascular ischemia.

  • Hypertension or increased blood pressure.

  • Medication overuse headache.

  • Pain or pressure of the chest, throat, neck, or jaw.

  • Serotonin syndrome which includes symptoms like hallucinations, agitation, increased heart rate, increased body temperature, nausea, vomiting, and incoordination.

  • Excessive allergic reactions (anaphylaxis) or hypersensitivity reactions like angioedema.

Can You Stop Taking Naratriptan Without Your Doctor’s Approval?

In case of an emergency where you experience any of the following conditions after taking Naratriptan, you must immediately stop taking the drug and consult your doctor:

  • Chest discomfort that lasts over a few minutes.

  • Breathing difficulty.

  • Nausea.

  • Vomiting.

  • Pain, pressure, or tightness in the chest, neck, jaws, or throat.

  • Lightheadedness.

  • Cold sweats.

Are There Any Dietary Restrictions to Consider When Taking Naratriptan?

  • You may take Naratriptan with or without food. There are no other dietary restrictions as such relating to taking the drug.

  • The tablet should be swallowed down with water.

  • Avoid consuming alcohol if you suffer from migraines, which may worsen the headaches.

How Should You Store and Dispose of Naratriptan?

  • Store Naratriptan tablets at a controlled room temperature of 20 to 25 degrees Celsius (68 to 77 degrees Fahrenheit).

  • Do not store the drug in conditions of extreme heat or moisture.

  • Keep the medication away from children and pets, and store it in the container with the lid tightly closed.

What Should You Do in Case of Overdose?

  • In case of overdose, you may experience a medication overdose headache and need to be detoxified. Your doctor may ask you to stop taking the medication.

  • Call the doctor or the local poison control helpline in severe cases for information. Alternatively, a visit to the emergency room may become necessary.

What Should You Do If You Miss a Dose?

  • You can take Naratriptan at four-hour intervals. This drug does not follow a dosing schedule, so you may take a dose when you remember to, and ensure that you take the next dose (if necessary) only four hours after the previous one.

  • Also, remember that the maximum dose you are allowed to take in a day is 5 mg.

What Else Should You Keep in Mind?

Keep a record of the timing and frequency of your headaches and the timings that you take Naratriptan tablets, so your doctor can determine whether or not the drug is working for you.

For Doctors:

Indications:

Naratriptan is indicated for the treatment of acute migraine in adults with or without accompanying aura.

Limitations:

  • Naratriptan should only be used if the patient has a migraine. If the patient shows no signs of improvement after taking a dose of Naratriptan, an alternative diagnosis should be considered.

  • This drug is not indicated for prophylactic purposes.

  • Data on the safety and efficacy of Naratriptan for cluster headaches is unavailable. It should, therefore, not be used to treat cluster headaches.

Pharmacology:

Description: Naratriptan is a selective 5-HT1B/1D receptor agonist, present in the form of Naratriptan hydrochloride in the available tablets. The molecular weight of this drug is 371.93, and the empirical formula is C17 H25 N3O2S•HCl.

Components:

1. Active Ingredient: Naratriptan hydrochloride (present as 1.11 mg or 2.78 mg equivalent to 1 mg and 2.5 mg of Naratriptan, respectively).

2. Inactive Ingredients:

  • Croscarmellose sodium.

  • Hypromellose.

  • Lactose.

  • Magnesium stearate.

  • Microcrystalline cellulose.

  • Triacetin.

  • Titanium dioxide.

  • Iron oxide yellow (2.5 mg tablet only).

  • Indigo carmine aluminum lake (FD&C Blue No. 2) (2.5 mg tablet only) for coloring.

Mechanism of Action:

Naratriptan binds to human cloned 5-HT1B/1D receptors with a high affinity. Since migraines are thought to be the result of local cranial vasodilatation and sensory neuropeptide release, Naratriptan's agonist effects are explained. Specifically, Naratriptan has agonist effects at the 5-HT1B/1D receptors on intracranial blood vessels as well as the sensory nerves of the trigeminal system. This causes the constriction of cranial vessels and inhibition of the release of pro-inflammatory neuropeptides.

Pharmacodynamics:

  • Reduction of carotid arterial blood flow with negligible effect on the arterial blood pressure or total peripheral resistance.

  • 30 % increase in vascular resistance in the coronary arterial bed.

  • Trigeminal nerve activity inhibition.

  • 1 % to 10 % reduction in coronary artery diameter in CAD patients undergoing catheterization of the coronary artery.

Pharmacokinetics:

  1. Absorption:

Naratriptan is well-absorbed.

Bioavailability: 70 % oral bioavailability.

Peak Concentrations: Obtained within two to three hours after administration of a 2.5 mg tablet.

Cmax: Higher in women following the administration of 1 or 2.5 mg tablets (50 %). Tmax: Slower during migraine attacks (three to four hours).

Effect of Food: No effect on the drug pharmacokinetics.

2. Distribution:

  • Volume of Distribution (Steady-State): 170 L.
  • Plasma Protein Binding: 28 % to 31 % (concentration range - 50 to 1,000 ng/mL).

3. Metabolism:

The in vitro metabolization of Naratriptan is carried out by cytochrome P450 isoenzymes. It gets converted into several inactive metabolites.

4. Elimination:

Primary Elimination- Urinary elimination (50 % of the dose is recovered unchanged, and 30 % is in the form of metabolites).

Mean Elimination Half-Life- Six hours.

Systemic Clearance- 6.6 mL/min/kg.

Renal Clearance- 220 mL/min.

Special Considerations:

  • Age- Clearance is slightly decreased in elderly people compared to younger populations.

  • Renal Impairment- Patients with moderate renal impairment have demonstrated 50 % reduction in clearance.

  • Hepatic Impairment- Patients with moderate hepatic impairment have demonstrated 30 % reduction in clearance.

What Are the Drug Interactions Relating to Naratriptan?

  • Oral Contraceptives: Oral contraceptives cause a 32 % reduction in clearance and a 22 % reduction in the volume of distribution. The concentrations of Naratriptan may thus be a little higher in these cases.

  • Monoamine Oxidase: Naratriptan is not an inhibitor of monoamine oxidase (MAO) enzymes.

  • P450: Naratriptan inhibits P450 poorly.

  • Smoking: Clearance of Naratriptan increases by 30 %.

  • Alcohol: No significant changes on coadministration.

What Are the Clinical Trials Relating to Naratriptan?

A trial was conducted to evaluate the efficacy and tolerability of Naratriptine in the treatment of acute migraine.

Study Design:

  • Type of Study- Multicenter, randomized, double-blinded, placebo-controlled, parallel-group study.

  • Methods- Migraine patients (n=613) treated a single migraine attack with either Naratriptan tablets (2.5 mg, 1 mg, 0.25 mg, or 0.1 mg) or a placebo.

Primary Outcome Measures: The patients recorded the following parameters dosing and at intervals starting 30 minutes after taking the dose:

  • The severity of pain associated with the migraine attack.

  • Clinical disability.

  • Associated migraine symptoms.

Safety Measures:

  • Adverse events.

  • Physical examination.

  • Vital signs.

  • Electrocardiograms.

  • Laboratory tests.

Results:

1. Headache Relief (P < 0.05 Naratriptan 2.5 mg and 1 mg Versus Placebo, 1 mg Versus 0.1 mg, and 2.5 mg Versus 0.1 mg and 0.25 mg) at Four Hours Post Dose:

  • Naratriptan 2.5 mg: 60 % patients experienced relief from the headache.

  • Naratriptan 1 mg: 50 % patients experienced relief from the headache.

  • Naratriptan 0.25 mg: 35 % patients experienced relief from the headache.

  • Naratriptan 0.1 mg: 32 % patients experienced relief from the headache.

  • Placebo: 34 % patients reported headache relief.

2. Mild or No Clinical Disability (P < 0.05 Naratriptan 2.5 mg and 1 mg Versus Placebo, 1 mg Versus 0.1 mg, and 2.5 mg Versus 0.1 mg and 0.25 mg):

  • Naratriptan 2.5 mg: 70 % patients.

  • Naratriptan 1 mg: 63 % patients.

  • Naratriptan 0.25 mg: 47 % patients.

  • Naratriptan 0.1 mg: 48 % patients.

  • Placebo: 48 % patients.

3. Four-Hour Efficacy for Absence of Migraine-Associated Symptoms: The efficacy was similar to headache relief efficacy for each dose.

Adverse Events Profile: Similar to the placebo group.

Patient Counseling Information:

Administration Instructions-

  • Take Naratriptan only as prescribed by the doctor.

  • Naratriptan may be taken with or without food but needs to be swallowed down with water.

  • Tablets must be swallowed whole and not crushed, chewed, or split.

Complications or Side Effects:

  • Cardiovascular and Cerebrovascular Complications- Inform patients of the possibility of cardiovascular side effects like myocardial infarction and cerebrovascular side effects like stroke. Patients should also be informed on what symptoms to look for that are indicative of cardiovascular issues.

  • Medication Overuse Headache- Warn patients of the ill effects of overuse of the medication (more than ten days a month). Advise them to report to the hospital if they experience severe headaches after consistent use of Naratriptan.

  • Serotonin Syndrome- Inform patients that Naratriptan may cause serotonin syndrome, particularly if used concomitantly with selective serotonin reuptake inhibitors (SSRIs), MAO inhibitors, etc.

  • Hypersensitivity and Anaphylaxis- Caution patients (especially those with sensitivity to allergens) on the use of Naratriptan as it may result in severe anaphylactic reactions.

  • Sedation and Dizziness- Patients should be made aware of the possibility of experiencing somnolence (drowsiness) or dizziness and should therefore be discouraged from driving or operating heavy machinery until the safety of doing so while on Naratriptan has been established.

  • Pregnancy- Patients should inform their doctors if they are pregnant or planning pregnancy as the drug may cause fetal harm.

  • Lactation- Patients should inform their doctors if they are breastfeeding or planning to do so, as it is unknown whether the drug crosses into breast milk.

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Dr. Abhishek Juneja
Dr. Abhishek Juneja

Neurology

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