Zolmitriptan

Coming from the triptan family of tryptamine-based drugs, Zolmitriptan is an abortive medication for the treatment of migraines in adults, triggering the release of serotonin 5-HT1B and 5-HT1D receptors in nerve endings and blood vessels in the brain.

Overview

Zolmitriptan is a tryptamine-based painkiller from the triptan family of pharmaceuticals and is used to relieve the symptoms of acute migraine headaches. As a triptan, its function is the alleviation and cessation of pain in the sufferer, it is not intended for preventative use. Likewise, zolmitriptan is not an appropriate medication for cluster headaches.

Zolmitriptan affects blood vessels and nerve endings in the brain to provide relief from migraine headaches by stimulating the release of serotonin 5-HT1d and 5-HT1B receptors in that location.

Many people discover that their migraine headaches cease entirely after taking zolmitriptan. Others find that their symptoms remain, but at a greatly reduced rate and that they can resume their day-to-day activities, even though their migraine headache has not completely abated. As well as relieving the headache itself, zolmitriptan often assists in relieving other symptoms that occur along with a migraine headache. Common symptoms found to be affected include sensitivity to light and sound, vomiting and nausea. It should be stated that zolmitriptan is not an appropriate treatment for those symptoms on their own, only if the underlying cause is a migraine headache.

Indeed, zolmitriptan should only ever be prescribed for the specific relief of migraine headaches, as it is not a regular form of pain relief. It is most often prescribed to patients who cannot treat their headaches appropriately with aspirin, acetaminophen, or other forms of painkiller.

The reason it is only prescribed for one particular ailment, and then only because other medicine has proven ineffective, lies in zolmitriptan causing several serious side effects in certain cases.

Conditions treated:

  • migraine headaches
  • nausea
  • vomiting
  • sensitivity to light
  • sensitivity to sound

Type of Medicine:

  • painkiller
  • triptan

Side Effects

Zolmitriptan has been the cause of several serious side effects in certain patients with blood vessel or heart disease.

The more common side effects reported include severe chest pains, as well as a heaviness, a tightness, or a pressure in the neck or chest. Other side effects commonly reported are different sensations such as burning, warmth and heat, or numbness, tightness, or tingling in people taking zolmitriptan.

These side effects only seem to occur in patients who already suffer from issues with their circulatory system, such as angina pectoris or hypertension. In such cases, these are expected side effects and the dosage prescribed should take them into consideration. Any patient who experiences these effects without a known history of heart disease or blood vessel disease should consult their doctor if such symptoms occur.

Users of zolmitriptan may also experience a serious, and occasionally fatal, disorder known as serotonin syndrome, due to the drug’s stimulation of serotonin release in the brain. Symptoms include a change in balance, agitation, hallucinations, fever, twitching or stiffness of muscles, excessive sweating, seizures, fever, abnormal heart rate, very bad diarrhea, and very bad headaches. Anyone exhibiting such symptoms while taking zolmitriptan should immediately contact their doctor. Risk may be exacerbated if taking this drug alongside anti-depressants and other migraine medication.

Both heart attacks and strokes have been reported in patients prescribed zolmitriptan, usually if they are susceptible to such events already.

There are several other side effects that can occur when taking zolmitriptan that are less common, but reported often enough to justify their discussion.

These include severe stomach or abdominal pain, caused by the drug’s effect on the production of stomach acid. Connected side effects include nausea and loss of appetite, as well as diarrhea and difficult or painful urination. Pains to the side and lower back are also reported.

Given the drug’s impact on the circulatory system, it is perhaps not surprising that patients complain of an irregular or a fast heartbeat and tightness in the chest. Similarly, a generalised weakness has been reported by patients, as well as difficulty breathing, a chill or fever, and associated hoarseness and coughing.

Other common side effects impact the skin, including hives, skin rashes, and other causes of itching, a puffiness around the patient’s eyes, face, or lips, and can even result in changes to the color of the patient’s facial skin.

Other side effects, of less immediate concern, include blurred vision, a pounding in the ears, and headaches. Nervousness, confusion, dizziness, fainting and an unusual weakness or tiredness have also been reported, as has a frequent increased or strong urge to urinate, combined with an increased volume of diluted, pale urine and difficulty swallowing.

Any patients persistently exhibiting these side effects should consult their doctor for advice.

There have been other common side effects reported with this drug, which usually do not require medical attention. In most cases, these side effects go away during appropriate treatment as the patient’s body adapts to the medication. Common side effects include a loss or lack of strength, unusual drowsiness or sleepiness and a cold or warm sensation. Less common side effects include lightheadedness or dizziness, dry mouth, a sensation of spinning, or a feeling that you or your surroundings are in constant motion.

Rarer side effects have been reported that normally don’t require the attention of a doctor. These include crying, anxiety, depression, depersonalization, euphoria, dysphoria, irritability, hyperventilation, paranoia, loss of or problems with memory, quickness to react, or overreact, emotionally, redness of the skin, rapidly changing moods, trouble sleeping, welts, shaking, and feeling, hearing, or seeing things that aren’t there.

Dosage

Patients should follow the orders of their prescribing doctor, or the directions printed on the label, as the required dose of zolmitriptan will be different for any two individuals. The information that follows only includes the average doses of zolmitriptan. If your doctor prescribes a different dosage, then you should not change it unless advised to by the prescribing doctor.

The amount of zolmitriptan you are expected to take depends on the potency of the drug prescribed. Oral zolmitriptan comes it two forms – oral tablets and oral disintegrating tablets.

For oral tablets

Adults: 2.5 milligram (mg) zolmitriptan oral tablets may be broken in half before administration. Initially, 1.25 or 2.5 mg, taken as a single dose. Should the migraine return after having been relieved, the patient may take another dose, so long as a minimum two hours have passed since the initial dose. No more than 5 mg of zolmitriptan should be taken in any single dose, nor should any more than 10 mg of the drug be taken over a single 24-hour period.

Children: Zolmitriptan oral tablets are not recommended for use by children.

For oral disintegrating tablets

Adults: 2.5 zolmitriptan oral disintegrating tablet placed on the tongue as a single dose. If the migraine returns having initially been relieved, the patient can take another dose, assuming that at least two hours have gone by since the first. No more than 10 mg of zolmitriptan should be taken over a 24-hour period, nor should any more than 5 mg of the drug be administered in one single dose.

Children: The use of zolmitriptan oral disintegrating tablets is not recommended for children.

Interactions with other drugs

Certain medications should never be used together, as they have known side effects when the two interact with one another. On the other hand, there are other medicines that might be used together, even though they have a known interaction. In cases like this, your prescribing doctor may choose to alter the dosage, or may decide that other precautions are necessary before your course of zolmitriptan begins. Therefore, it is essential when prescribed zolmitriptan that you alert your healthcare professional to the fact that you are taking any of the drugs listed below.

The following lists of known interactions are included here based on their potential significance, and it should not be assumed that they are exhaustive.

Using zolmitriptan with any of the following drugs is not recommended. Your prescribing doctor may choose to change some of the medication you take before giving you zolmitriptan, or may decide not to treat you with it at all.

  • Almotriptan
  • Mesoridazine
  • Cisapride
  • Methylene Blue
  • Dihydroergotamine
  • Methylergonovine
  • Eletriptan
  • Methysergide
  • Ergoloid Mesylates
  • Naratriptan
  • Ergonovine
  • Phenelzine
  • Ergotamine
  • Procarbazine
  • Frovatriptan
  • Rizatriptan
  • Isocarboxazid
  • Safinamide
  • Levomethadyl
  • Sumatriptan
  • Linezolid
  • Thioridazine
  • Terfenadine
  • Tranylcypromine

Using zolmitriptan with any of the following drugs is usually not recommended, but might be necessary in certain cases. If both medications are prescribed at the same time, your doctor may choose to change either the dosage or the regularity of intake of one or both of the drugs.

  • Acecainide
  • Ziprasidone
  • Ajmaline
  • Vortioxetine
  • Amiodarone
  • Vilazodone
  • Amitriptyline
  • Venlafaxine
  • Amoxapine
  • Vasopressin
  • Aprindine
  • Trimipramine
  • Azimilide
  • Trifluoperazine
  • Bretylium
  • Trazodone
  • Buprenorphine
  • Tramadol
  • Chloroquine
  • Tedisamil
  • Citalopram
  • Tapentadol
  • Desipramine
  • St John's Wort
  • Desvenlafaxine
  • Spiramycin
  • Dibenzepin
  • Sotalol
  • Disopyramide
  • Sibutramine
  • Dofetilide
  • Sertraline
  • Dolasetron
  • Sematilide
  • Doxepin
  • Reboxetine
  • Droperidol
  • Quinidine
  • Duloxetine
  • Protriptyline
  • Erythromycin
  • Propafenone
  • Escitalopram
  • Prochlorperazine
  • Fentanyl
  • Procainamide
  • Flecainide
  • Probucol
  • Fluconazole
  • Prajmaline
  • Fluoxetine
  • Pixantrone
  • Fluvoxamine
  • Pirmenol
  • Foscarnet
  • Pentamidine
  • Gemifloxacin
  • Paroxetine
  • Granisetron
  • Palonosetron
  • Halofantrine
  • Oxycodone
  • Hydroquinidine
  • Octreotide
  • Ibutilide
  • Nortriptyline
  • Imipramine
  • Nefazodone
  • Isradipine
  • Mirtazapine
  • Levomilnacipran
  • Milnacipran
  • Lidoflazine
  • Meperidine
  • Lorcainide
  • Mefloquine
  • Lorcaserin

Using zolmitriptan with the following medication might cause an increase in the risk of certain side effects. However, using both drugs in unison might be the best treatment for you. If your doctor prescribes both medicines together, they will likely alter how often you are required to administer one or both medications, and the dosage for each administration.

  • Cimetidine

Other Interactions

With the pronounced potential side effects that zolmitriptan has been reported to have on both the circulatory system and the lungs and chest, it is recommended that it should not be taken in conjunction with tobacco.

Warnings

Before being prescribed any medication, including zolmitriptan, it is important that you and your doctor have a frank and open discussion, weighing the good which the drug will do for your condition against the potential risks involved in taking it.

You should inform your doctor immediately if you have ever had an unusual or allergic reaction to zolmitriptan before, or any other medication. You should also tell your doctor about any other allergies you might suffer from, even if you do not immediately see the significance or connection to your medicine. This can include preservatives, animals, dyes, foods, or anything else.

Geriatric

To date, none of the appropriate studies performed have managed to demonstrate specific issues that might limit zolmitriptan’s usefulness among the elderly. That being said, age-related heart conditions and high blood pressure are more likely among elderly patients. Given zolmitriptan's known potential side effects, which affect the heart, circulatory and respiratory systems in adults, geriatric patients may need their dosage of the drug altered in order to mitigate the risk.

Pregnancy – all trimesters

No adequate studies have been conducted to determine whether taking zolmitriptan during pregnancy will have an adverse effect on either mother or baby. It will be up to you and your health professional to weigh the possible risks against the potential benefits, before choosing to undergo a course of this medication while pregnant.

Breastfeeding

There have been no adequate studies conducted that determine whether taking zolmitriptan while breastfeeding will have an effect on either mother or baby. It is between your health professional and you to decide if the possible benefits outweigh the potential risks, before you agree to a course of these drugs while breastfeeding.

Children

Zolmitriptan has not been declared as suitable for use in children suffering these symptoms, so an alternative medical solution should be used in these cases.

Other Medical Problems

Whenever determining a new course of medication with your doctor, you should always inform them of any existing medical conditions. If the medication in question is zolmitriptan, it is especially important that you advise your health professional of any of the following problems, as they are often exacerbated by the drug:

  • angina (chest pain)
  • arrhythmia (irregular rhythm of the heartbeat)
  • a history of basilar migraine (a migraine that includes attendant hearing and vision problems)
  • a history of heart attacks
  • heart disease
  • blood vessel disease
  • a history of hemiplegic migraine (a migraine that includes attendant paralysis)
  • uncontrolled hypertension (high blood pressure)
  • ischemic bowel disease (low supply of blood to the bowels)
  • peripheral vascular disease (clogged arteries)
  • a history of strokes
  • a history of transient ischemic attack
  • Wolff-Parkinson-White Syndrome (a heart rhythm problem)
  • a family history of coronary artery disease, diabetes, hypertension, obesity, or Raynaud's syndrome
  • any heart rhythm problems, including ventricular fibrillation and ventricular tachycardia)
  • moderate to severe liver disease – the use of zolmitriptan oral disintegrating tablets is not recommended for patients with this condition, as you should not break these tablets in half.
  • Phenylketonuria (PKU) – the use of zolmitriptan oral disintegrating tablets is not recommended for patients with this condition, as they contain phenylalanine, which can react unfavourably with the condition.

It is essential that regular visits take place with your health professional to enable them to check your progress. This will allow your prescribing doctor to determine that your course of medication is having the desired effect, and to decide whether you should continue with the treatment, or have your prescription altered or stopped.

Zolmitriptan is a powerful member of the triptan family of drugs, so-called because they all have a tryptamine base. The group as a whole is for the cessation of migraine and cluster headaches although some (like zolmitriptan itself) are only appropriate for one or the other (migraines, in this instance). Different triptans have different types of impact on the body, and using more than one at the same time, without medical clearance, can lead to an exacerbation of the effects.

Therefore, you should not take zolmitriptan if you have taken other triptan or ergot-type medication for your migraine in the last 24 hours.

Some common triptan drugs include almotriptan, eletriptan, frovatriptan, naratriptan), or sumatriptan.

Some common ergot-type medications include dihydroergotamine, ergotamine, and methysergide.

Many of these drugs are available under a registered brand name, so be sure to check the label of any migraine medication to determine whether they include such drugs.

Zomlitriptan should not be taken within two weeks of taking a Monoamine oxidase (MAO) inhibitor, often found in anti-depression medication. Common MAO inhibitors include phenelzine and tranylcypromine.

The effect of zolmitriptan is to cause a swift cessation or reduction of the pain symptoms from a migraine headache. If, upon taking the drug, your migraine does not lessen its severity or go away, or if it started occurring with greater regularity, or if the intensity of the migraine increased, you should speak with your prescribing doctor immediately to determine if there is an underlying issue causing these unwanted effects.

With its known impact on the circulartory system in certain individuals, zolmitriptan can increase your risk of abnormal heart rhythm, angina, heart attack, or stroke. If you or a family member have an existing heart disease condition, this risk is increased through the use of this drug. If you have existing high blood pressure, diabetes, or if you are a smoker your risk is similarly enhanced.

You should call your doctor immediately if you start to exhibit symptoms of a heart condition, including chest pain or discomfort, an irregular or uneven heartbeat, vomiting or nausea, discomfort or pain in the back, neck, arms, shoulders, or jaw, sweating, or shortness of breath.

You should call your doctor immediately if you begin to display any symptoms of a stroke. These can include difficulty with speaking, confusion, double vision, an inability to move legs, arms, or facial muscles, slow speech, or an inability to speak.

If you have chest discomfort, neck or jaw tightness once you start taking zolmitriptan, you should check with your doctor straight away. You should also tell your prescribing doctor if you start having severe or sudden stomach or abdominal pain, or bloody diarrhea once you started using this medication.

You should check with your doctor immediately if you start having difficulty with reading, blurred vision, or any change in vision whilst taking this medicine.

Once again, you should ensure your doctor knows all the other medication you are taking. Zolmitriptan oral tablets have been linked to a serious medical condition called serotonin syndrome when taken in conjunction with certain other drugs, notably those used to treat depression. Reported drugs known to trigger this effect include citalopram, duloxetine, escitalopram, fluoxetine, fluvoxamine, olanzapine, paroxetine, sertraline, or venlafaxine. Symptoms of serotonin syndrome include agitation, excitement while talking that is not normal, confusion, fever, diarrhea, poor coordination, overactive reflexes, shaking, restlessness, sweating, shivering, trembling, or twitching that you can’t control. If you start exhibiting any of these symptoms after taking zolmitriptan, it is essential that you contact your prescribing doctor immediately.

Zolmitriptan can cause dizziness or drowsiness in some people, and it is generally nothing to be concerned about. For as long as you do feel drowsy or dizzy, you should not drive, use machinery, or perform any other activity that could be dangerous.

Drinking alcohol can cause the intensity of headaches to increase. People suffering from severe headaches are advised to avoid alcoholic beverages during a headache.

Storage

Zolmitriptan should always be stored at room temperature, in a closed container. It should be kept away from direct light, moisture, and heat, and you should also keep it from freezing.

Zolmitriptan should always be kept beyond the reach of children.

You should not keep any medicine that is not longer required, or which is outdated. It is recommended that you consult your prescribing doctor, or other healthcare professional how to dispose of any unused medicine.

Zolmitriptan comes in sealed blister packs. You should always keep the tablets in those blister packs. Any medicine removed from the packs and subsequently unused should be disposed of.

Summary

While zolmitriptan has been proven to be a very effective treatment for the condition of acute migraine headaches, it has several extreme side effects which must be taken into consideration before taking. As a tryptamine-based drug, it affects the blood vessels and nerve endings in the brain, triggering the release of serotonin to reduce the impact of the migraine headache from which the patient is suffering. The nature of the medication, and the side effects it promotes in certain individuals means that it is rarely administered except where other remedies such as aspirin have proven ineffective.

The side effects reported by users of zolmitriptan range from slight irritation of the skin and an increased need to urinate, down to potentially fatal conditions including serotonin syndrome, heart attack and strokes. These conditions are caused by the drug’s impact on the circulatory system and brain.

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Last Reviewed:
December 23, 2017
Last Updated:
December 22, 2017
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