Triptans: Uses, common brands, and safety info

The acute treatment of migraines can include analgesics and nonsteroidal anti-inflammatory drugs (NSAIDs) as well as a group of drugs known as selective serotonin agonists, more often referred to as triptans. While NSAIDs such as aspirin, ibuprofen, or naproxen are usually adequate treatment for mild migraine symptoms, triptans are the preferred treatment for moderate to severe migraines or mild migraines that do not respond to other types of treatment. This article will discuss how triptans work, their safety, and things you should know before taking a triptan drug.

Other triptans

• Imitrex Statdose (sumatriptan)

• Zomig ZMT (zolmitriptan)

• Maxalt MLT (rizatriptan)

• Zecuity (sumatriptan)

• Alsuma (sumatriptan)

• Zembrace SymTouch (sumatriptan)

What are triptans?

Triptans, or selective serotonin receptor agonists, are a class of antimigraine drugs used in the treatment of moderate to severe migraines, or mild migraines that have not responded to other forms of treatment. The use of the word triptan to describe the class is derived from the fact that each drug in the class has a chemical name that ends in “-triptan”. The triptan class offers a variety of different dosage formulations such as regular oral tablets, oral dissolving tablets, nasal sprays, and injections. Nausea and vomiting associated with migraines may prevent the use of traditional oral dosage forms, but fortunately, there are alternatives for effective drug delivery in this class. Triptans first became available as a migraine treatment in the early nineties, and their development has continued as we seek better treatment options for migraine patients. 

How do triptans work?

Triptans are active at two specific types of serotonin receptors, 5-HT1B and 5-HT1D. The stimulation of these two receptor sites are responsible for several types of actions that help alleviate migraine headaches. 5-HT1D receptor stimulation is responsible for inhibiting dural vasodilation and inflammation. Dilation of blood vessels in the dura matter is thought to underlie headache pain as blood rushes to fill the dilated vessels and creates a pulsing or throbbing sensation. 5-HT1B stimulation is responsible for the vasoconstriction of dilated intracranial extracerebral blood vessels. Agonism at both receptor types inhibits neurotransmission responsible for sensation in and around the face. Triptans have no affinity for other types of serotonin receptors in the body.

What are triptans used for?

As mentioned earlier, triptans are the preferred treatment for migraines. Here’s a little more about migraines. 

Migraine headaches are a specific type of headache that occurs repeatedly over time. Migraines differ from tension headaches or other intermittent types of headaches because they are typically accompanied by nausea, vomiting, and sensitivity to light. 

Migraines may also be accompanied by an aura. An aura may present as dizziness, ear ringing, and sensations of flashing lights or lines. They typically precede the start of a migraine. Migraines are thought to be caused by an increased excitability of the central nervous system. Migraines are a disabling illness and can affect your work, social, and family life if inadequately treated. 

Triptans can also treat cluster headaches (sumatriptan only).

Who can take triptans?

Adults 

All triptans are approved for use in adults. Adults who have impaired renal or liver function may require a dose adjustment of certain triptans. Patients with pre-existing coronary artery disease (CAD) or risk factors for CAS may not be candidates for triptan therapy. These risk factors include hypertension, hypercholesterolemia, smoking, obesity, diabetes, family history of CAD, menopausal women, or men over 40 years of age.

Seniors

Menopausal women and men over 40 carry an additional risk for cardiovascular disease. As a precaution, patients would need clinical evidence that they are in good cardiac health prior to initiating triptan therapy. If liver or kidney functions have declined, dose adjustments may be necessary. As a general rule, the seniors should not take triptans.

Children

Axert (almotriptan) and Maxalt (rizatriptan) are the only drugs in the class approved by the Food and Drug Administration (FDA) for use in children. Axert is approved for children 12 years and older, while Maxalt is approved for children 6 years and older. The American Academy of Neurology also makes a recommendation for the use of nasal sumatriptan in children.

Are triptans safe?

Recalls

• Pfizer Inc., Voluntary recall of 2 lots of Relpax 40mg tablets due to contamination, August 2019

Restrictions

Do not take triptans if you have had a known hypersensitivity reaction to any triptan medication in the past.

Triptans are contraindicated in patients with coronary artery disease, peripheral arterial disease, cerebrovascular disease, or uncontrolled hypertension (high blood pressure). A physician will screen for the presence of these contraindications before prescribing triptans.

While they are rare, there are serious adverse events associated with triptan use. These include myocardial infarction (heart attack), ventricular tachycardia, ventricular fibrillation, hypertensive crisis, stroke, cerebral hemorrhage, peripheral vascular ischemia, and seizures. This is why it is important for your healthcare provider to do the proper screenings for heart disease and to determine if triptan usage is safe for you.

Geriatric patients and children are generally not good candidates for triptan use. The only exceptions are FDA approved use of almotriptan and rizatriptan in children when deemed necessary.

The use of triptans with monoamine oxidase inhibitors (MAOIs) is contraindicated. You should be off of all MAOI therapy for at least two weeks prior to initiating triptan therapy.

Triptans should not be taken within 24 hours of the administration of another triptan or ergot derivative drug, such as ergotamine, due to the increased risk of vasospasm.

Other serotonergic drugs, such as the antidepressant class known as selective serotonin reuptake inhibitors (SSRIs), may have an increased potential to cause serotonin syndrome when triptans are taken. Talk to your pharmacist about this and other potential drug interactions.

There is a phenomenon known as medication-overuse headache which can occur from taking triptans too often. Triptans have dosing limits which should be explained by your prescriber and strictly adhered to.

Triptans are not approved for migraine prevention and should only be used in the acute treatment of moderate to severe migraines. They are most effective when taken as soon after the onset of the migraine as possible.

Can you take triptans while pregnant or breastfeeding?

All triptans are pregnancy category C as determined by the FDA. While there is no proof that they may cause birth defects, there is no evidence as to their safety either. The use of triptans should only be considered as a last resort, and physicians are encouraged to register their patients for monitoring if they choose to prescribe a triptan during pregnancy.

All triptans are excreted into the breast milk, though levels are generally low. The American Academy of Pediatrics recommends the use of oral sumatriptan if a triptan is necessary while breastfeeding because it has the lowest oral bioavailability (absorption).

Are triptans controlled substances?

No, triptans are not controlled substances.

Common triptans side effects

There are a great deal of potential adverse effects to triptan consumption, though not all, if any,  will happen when you take a triptan. The potential for adverse events and their severity vary between each specific triptan, and tolerability is unique to each patient. 

Here is a list of the most common side effects:

• Paresthesia

• Hot sensation

• Cold sensation

• Malaise

• Fatigue

• Chest pain or discomfort

• Neck pain or discomfort

• Throat pain or discomfort

• Jaw pain or discomfort

• Dizziness

• Vertigo

Subcutaneous injectable triptan dosing carries the risk of additional side effects which include:

• Injection site reaction

• Flushing

• Weakness

• Sedation

• Drowsiness

• Diaphoresis

How much do triptans cost?

All traditional oral dosage forms are now available generically and are generally affordable. SingleCare offers coupon savings that can reduce the cost by up to 80% from participating local pharmacies. Oral triptans range in price from about $12 to $40 for a standard prescription amount. Imitrex (sumatriptan) tends to be the most affordable option as you are able to get nine 100 mg tablets for just under $12 using a SingleCare prescription discount card. 

Insurance coverage of triptans may vary a great deal between plans and network pharmacies. Your plan may have a preferred triptan, or may have an authorization process required for coverage. Y