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Relpax (Eletriptan) Side Effects & Adverse Reactions (List)

Relpax (Eletriptan) is a medication manufactured by Pfizer Inc. for the acute treatment of migraine headaches (with or without aura) in adults.  It was initially approved by the FDA in 2002 and is regarded as a highly effective abortive agent, engineered to attenuate already-occurring migraine attacks.  Chemically, Relpax is classified as a second generation triptan (or tryptamine-based substance), and like other triptans, functions principally as a serotonin receptor agonist.

Specifically, Relpax has highest affinity for 5-HT1B, 5-HT1D, and 5-HT1F receptor sites.  Agonism of the aforestated serotonergic receptors is thought to facilitate a vasoconstrictive response within intracranial blood vessels to offset the excessive vasodilation implicated in migraines.  Moreover, 5-HT receptor agonism may inhibit the release of proinflammatory neuropeptides such as Substance P and CGRB from trigeminal nerve fibers, ultimately preventing pain and exacerbation of a migraine attack resulting from neurogenic inflammation.

Some speculate that up to 80% of patients will derive symptomatic relief from Relpax (and other triptans) within approximately 30 to 90 minutes of administration.  Although there’s no denying the proven efficacy of Relpax as an abortive antimigraine agent, it is not devoid of side effects.  As a result, a subset of Relpax users will end up discontinuing treatment because they are unable to tolerate and/or are dissatisfied with side effects.

Relpax (Eletriptan) Side Effects & Adverse Reactions (List)

Included below is a comprehensive list of side effects associated with Relpax.  Keep in mind that specific side effects, total number of side effects, as well as their respective severities will be subject to significant individual variation.  In other words, you may report a completely different set of side effects while taking Relpax than another user.  Nonetheless, some side effects are reportedly more common than others, including: dizziness, headaches, nausea, pressure sensation, tingling, and weakness.

Allergic reactions: An allergic reaction to Relpax is considered extremely rare, but can occur in a small percentage of users.  Individuals allergic to the medication may experience an array of unpleasant symptoms including: difficulty breathing, hives, and swelling of body parts.  Most commonly, those allergic tend to notice a prominent rash throughout their body along with a swollen face, lips, throat, and/or tongue.

Thankfully most signs of an allergic reaction are obvious enough for users to sense a tolerability issue.  Nonetheless, it is necessary to consult a doctor to treat an allergic reaction to ensure that no physiological damage ensues.  Those allergic to Relpax should be able to switch to a more tolerable medication that provides equipotent migraine relief.

Balance / coordination problems: You may notice that once Relpax fully kicks in, you are unable to maintain balance and appear uncoordinated.  Some users have reported significant changes in gait (manner of walking) due to the fact that they feel drowsy, heavy, and weak.  Balance and coordination impairment may be most noticeable among elderly individuals using Relpax, but can occur in users of any age.

If your balance or coordination is compromised from Relpax, you may want to lie low and avoid exercise, operating heavy machinery, or driving a motor vehicle until the medication has been eliminated from systemic circulation.  Realize that engaging in any activity that requires optimal coordination may be putting yourself and/or others at risk of injury and/or death.  Usually balance and coordination impairment is more prominent at higher doses compared to lower.

Bodily pressure: An extremely common side effect of Relpax is increased bodily pressure.  The pressure may be extreme in some individuals to the extent that they feel as if they’re about to explode or even faint.  Others may experience a milder increase in bodily pressure and may not necessarily consider it bothersome.

The pressurized sensation may be isolated to a particular region or may be widespread throughout the body.  Pressure in the body may also be accompanied by feelings of perceived heaviness as well as weakness.  Most users are willing to deal with the pressure as long as they get migraine relief.  In some cases, a slight reduction in dosage may be helpful for decreasing pressure sensations.

Brain fog: Though its difficult to think clearly when you’re in the midst of a full-blown migraine attack, it may be even tougher to maintain mental clarity after administering a Relpax.  Most users report significant brain fog or a “spaced out feeling” that lasts at least a few hours after taking the drug – sometimes longer.  The brain fog may directly result from extensive modulation of serotonergic systems, but could also be related to altered trigeminal processes.

This brain fog may make it challenging to function in a variety of academic, occupational, and/or social settings.  It is possible that the brain fog may be exacerbated with higher doses compared to lower ones.  If the brain fog is considered severe, you may want to discuss potential ameliorative adjuncts with a medical professional to offset “cloudy thinking.”

Changes in body temperature: Many users notice fluctuations in bodily temperature while taking Relpax.  These temperature changes may result from altered function of thermoregulatory systems under the influence of Relpax.  The most common temperature change reported is warmth or sensation of heat, which may be accompanied by facial flushing, hot flashes, and/or sweating.

Others may perceive a dip in body temperature and feel constantly chilled after taking their medication.  Another set of individuals may experience sensations of hot and cold – alternating back and forth.  Though these temperature changes may be relatively unpleasant, they are generally not unpleasant enough for users to discontinue treatment.

Chest pain: Many people taking Relpax and other triptans often experience significant chest pain for several hours after administration. Most individuals that experience chest pain mention feeling tightness, pressure, and/or discomfort throughout their chest region.  Although the chest pain may be highly uncomfortable and anxiety-provoking, it usually fades after several hours.

Furthermore, most are willing to trade their migraine pain for the chest pain that accompanies medication usage.  Obviously if the chest pain associated with Relpax outweighs the migraine pain, then a medication switch will be necessary.  All that said, since chest pain experienced as a side effect may be somewhat similar to an actual heart attack, it is important to consult a cardiologist to rule out cardiac abnormalities and ensure your safety on this medication.

Cognitive deficits: Assuming you experience a migraine midday at work and/or school and decide to pop a Relpax, you may end up regretting it due to the ensuing cognitive deficits.  You may find it difficult to sustain attentional focus and/or notice that your working memory function seems impaired.  Thoughts may seem disorganized and you may find it challenging to verbalize coherent sentences.

These deficits may be caused by modulation in neurotransmission, blood vessel size, trigeminal nerve activation, and/or other side effects such as drowsiness.  While the cognitive deficits resulting from Relpax are transient and should subside within several hours after administration, they may significantly interfere with cognitively-demanding academic and/or occupational tasks.  For this reason, you may want to discuss some possible ways in which you can reduce the impairment (e.g. dosage reduction, caffeine, etc.) with your doctor.

Dizziness: Among the most common side effects of Relpax is dizziness.  When the drug takes effect, you may feel moderately dizzy or perhaps extremely dizzy to the extent that you feel drunken and/or like the room is spinning.  Those that experience moderate to severe dizziness may find it helpful to simply lie down, sit comfortably, and/or relax with eyes closed for a few hours until the migraine is over and medication is out of systemic circulation.

Those that experience mild dizziness don’t usually have a difficult time tolerating it as a side effect.  However, if the dizziness is overwhelming, you should discuss it with your doctor and determine whether there are alternative antimigraine interventions without this side effect.  In most cases, the dizziness isn’t considered an overly problematic reaction.

Drowsiness: After taking Relpax, you may feel extremely drowsy, making it difficult to maintain alertness and/or vigilance.  As a result of this drowsiness, you want to just “chill” or relax for awhile until your energy returns.  The transient drowsiness that occurs from the medication may make it difficult to exercise and stay productive, and is commonly implicated in balance/coordination problems.

To offset the drowsiness from Relpax, a stimulatory or wakefulness-promoting agent such as caffeine may be helpful, however, you should confirm the safety of any adjunctive agent with your doctor.  Assuming you don’t need to operate a motor vehicle, heavy machinery, or solve a complex equation – the drowsiness shouldn’t be too problematic.  That said, you may want to discuss a dosage reduction with your doctor as lower doses may yield less drowsiness.

Dry mouth: A side effect that is reported in some Relpax users is xerostomia or dry mouth.  Relpax may interfere with the production of saliva by the salivary glands, leading to a parched oral mucosa.  In addition to the dry mouth that may occur while taking this medication, you may also develop halitosis (or bad breath).

The halitosis may occur due to the fact that a lack of salivary lubrication within the oral mucosa makes it easier for bad bacteria to proliferate.  For this reason, if you experience dry mouth, you may want to drink extra water to keep the inside of your mouth as moist as possible – this could ease some of the discomfort and prevent halitosis.  That said, compared to other side effects, most individuals aren’t as concerned with dry mouth.

Fatigue: You may experience a stark contrast in your energy level prior to taking Relpax compared to after administration. When Relpax initially takes effect, you may notice an onset of fatigue – both physically and mentally.  As a result of this fatigue, it may be challenging for you to accomplish menial tasks such as doing the laundry, making your bed, cleaning the dishes, etc.

It may be even more difficult to engage in complex thinking, problem solving, etc.  Some of the fatigue should be expected and will gradually subside as the drug is broken down and eliminated from your system.  On the other hand, it may be helpful to discuss dosage adjustments and/or adjunct interventions to offset Relpax-induced fatigue.

Headaches: Ironically, those taking Relpax for migraines may experience mild headaches as a side effect.  It is unclear as to why Relpax is likely to cause headaches in some individuals, but since it facilitates vasoconstriction of intracranial blood vessels, it is possible that excessive vasoconstriction may be the cause.  Hypothetically assuming that excessive vasoconstriction is the cause of mild headaches, it could be that an individual is taking too high of a dose.

At the optimal dose, Relpax may reverse vasodilation of intracranial blood vessels just enough to combat the migraine symptoms, but not too much as to provoke a headache.  Those that experience headaches as a side effect may want to discuss slightly tweaking their dosage with a doctor to determine whether it helps.  It could also be that modulation of trigeminal nerve function causes mild headaches for some, but thankfully these headaches aren’t usually debilitating like migraines.

Heaviness sensation: A fairly typical Relpax side effect is a sensation of heaviness throughout the entire body or isolated within specific regions.  The heaviness may compel you to lie down and/or relax and may be accompanied by extreme muscle weakness or numbness.  Some have reported that when the heaviness is felt, it becomes challenging to move their arms, neck, and head.

Most individuals can learn to cope with the heaviness sensation that is experienced while taking this medication.  Unfortunately, most drugs within the triptan classification tend to cause sensations of heaviness throughout the body as a side effect.  If you cannot cope with this side effect, you may need to switch to a medication of another classification.

High blood pressure: Certain individuals may experience a spike in blood pressure as a result of taking Relpax.  Those with a history of prehypertension or hypertension should regularly monitor blood pressure throughout treatment to ensure that it stays within a normative, healthy range.  If a person is taking Relpax regularly and blood pressure is spiking within an abnormally high range, this could lead to serious health problems – especially over a long-term.

Over a long-term, unchecked high blood pressure is associated with coronary artery disease, heart failure, kidney disease, and stroke.  For most individuals, blood pressure won’t fluctuate significantly during treatment, but everyone should be cognizant of this possible side effect.

Hot flashes: The serotonin system is known to influence thermoregulation, and when altered, hot flashes may occur.  Relpax elicits a significant effect upon serotonin receptors as an agonist, and the summation of these effects may provoke a sudden feeling of intense heat – or hot flash.  Though nobody likes to experience a hot flash, nor the sweating and/or flushing of the face that accompanies them, however, most would consider them a small price to pay for migraine relief.

Keep in mind that some individuals may attribute a hot flash to their medication when its really caused by another factor (e.g. menopause).  Obviously if the hot flashes occur only after you take Relpax, then it’s probably the medication.  However, if you were experiencing hot flashes prior to Relpax usage, it could be that another factor is more culpable for this effect.

Jaw pain: Users have reported that after each dose of Relpax, their jaw locks up with mild pain and/or pressure.  If you experience lockjaw (trismus) or any pain, it could be a result of excess jaw rigidity induced by vasoconstriction.  It could also simply be an adverse neurophysiological reaction associated with serotonergic modulation provided by Relpax; this speculation is based on the fact that certain medications altering serotonin transmission can cause lockjaw.

To ensure that you don’t have any alternative conditions that are causing jaw pain, you may want to consult a dentist and/or neurologist.  Some individuals have had to quit taking Relpax because the jaw pain induced by the medication was equally as debilitating as the migraine it was treating.  Understand that although transient jaw pain isn’t a common reaction to Relpax, it can occur.

Lightheadedness: After taking Relpax you may feel extremely lightheaded, possibly as if you’re about to faint or enter some sort of twilight zone.  The lightheadedness can be significant for several hours and is often accompanied by dizziness, but will eventually subside.  Most individuals are able to tolerate the drug-induced lightheadedness, but some find that lying down or avoiding strenuous physical activity helps them to cope.

It isn’t fully understood as to why lightheadedness occurs, but it is understood that possible alteration of blood pressure, neurotransmission, blood vessel constriction, and/or trigeminal nerve activity could play a role.  If the lightheadedness is extreme enough that it causes you to faint, it may be a sign that Relpax isn’t a good fit for you.  On the other hand, sometimes a slight dosage reduction may effectively ameliorate some of the lightheadedness – making it easier to cope with.

Nausea: After taking Relpax you may become nauseous, possibly to the degree that you feel as if you’re about to vomit.  In fact, a small percentage of individuals taking Relpax will end up feeling so nauseous that they actually do vomit.  Though most Relpax users aren’t likely to experience extreme nausea to the extent of vomiting, they may find that the nausea suppresses their appetite.

Some have noted that nausea is often most problematic during the first few times of using Relpax and lessens with continued administration.  You may want to discuss taking an adjunct antiemetic agent and/or dosage reduction with your doctor to determine whether it helps the nausea.  Sometimes simply taking Relpax along with food (as opposed to taking it on an empty stomach) can reduce nausea.

Numbness: An extremely common side effect of this drug is numbness in certain regions of the body.  The numbness may result from neurological changes induced by Relpax, but could also be related to alterations in peripheral nerve function and/or blood flow restriction.  After administration of Relpax, patients have reported numbness most frequently in the following areas: arms, face, fingers, hands, and joints.

The numbness that occurs may be also accompanied by tingling sensations and/or pressure.  Though many users experience numbness in only one specific body area (e.g. the hands), the particular area affected in one person generally differs from that of another.  Most would not consider the numb feeling itself to be painful, but it is certainly a bizarre and unwanted reaction.

Rapid heart rate: A less common adverse effect that may occur among Relpax users is tachycardia or rapid heart rate.  If you notice that your heart rate speeds up (out of your normal range) after taking Relpax, it should be reported to a medical professional.  Additionally, those with cardiac problems and/or at risk for a heart attack should monitor both heart rate and blood pressure during treatment.

That said, those without any major cardiac problems may be experiencing relatively benign heart palpitations.  Heart palpitations are characterized as irregular or abnormally strong heartbeats resulting from neurophysiological anxiety, illness, or medications.  A medical professional will be able to distinguish between serious drug-induced tachycardia and benign palpitations.

Skin redness: Although uncommon, redness of the skin may occur as a result of Relpax treatment.  Skin redness may be a sign of an adverse allergic reaction, especially if accompanied by hives and/or swelling of body parts (e.g. neck, tongue, etc.).  However, it may also occur in certain regions as a result of temperature changes, particularly in the facial area following a drug-induced hot flash.

If you suspect that Relpax has caused a skin rash, redness, or any sort of discoloration – immediately contact your doctor.  Consultation with a dermatologist may also be useful to rule out any potential confounding causes of this redness (e.g. seasonal allergies).  Sometimes minor skin redness may not be a major issue – especially if hives, swelling, and/or rashes aren’t present.

Stomach aches: In addition to pains in the upper chest, many individuals experience stomach aches, cramps, and/or pains during Relpax treatment.  Stomach aches may be caused by irritation of the gastrointestinal tract and/or indigestion that can occur following administration of the drug.  To reduce the likelihood of stomach aches, it may be helpful to take Relpax along with some food as opposed to on an empty stomach.

This is a side effect that many Relpax users experience, and although mildly irritating, it is usually less painful than the migraine being treated.  Many other medications also cause upset stomach, so don’t assume Relpax is somehow unique in this regard.  All that said, increasing fluid intake may be helpful for mitigating stomach aches, especially if some of the stomach pain attributed to Relpax is a byproduct of dehydration.

Sweating: Many individuals taking Relpax document profuse sweating (or “hyperhidrosis”) as a side effect.  The sweating may be most noticeable in the armpits, palms, and soles of your feet. You may also experience sweats dripping down your forehead, as well as in other regions of your body as you would if you just finished a workout at the gym.

Sweats are usually regarded as a small price to pay for migraine relief, however, if the sweats are severe, they may soak your work clothes and/or be embarrassing if noticed by others.  These sweats may also be accompanied by perceived changes in bodily temperature (e.g. warmth), hot flashes, and flushing of the face.  The causative mechanisms facilitating increased sweat production as a side effect aren’t clear, but Relpax likely exerts an effect that ramps up sweat gland activity (in certain users).

Throat pain: If you’re taking Relpax and feel as if your throat is constricted or swollen, and feels somewhat painful, it’s likely a side effect of the medication.  Obviously if the throat is fully swollen, it could be a sign that you’re experiencing an allergic reaction.  For this reason, anyone with throat pain while taking the drug should report it as soon as possible to their doctor.

Some people have claimed that the throat pain caused by the drug is so severe that they cannot drink or eat because it hurts to swallow.  Others have described the throat pain as more of a burning sensation [akin to drinking acid] that is exacerbated with fluid intake – particularly hot drinks.  This throat pain may be accompanied by discomfort within the entire neck region.  In some cases, a dosage reduction may help reduce the pain, but in others, it may be an inevitable ongoing side effect.

Tingling: A side effect associated with many triptans is tingling after administration.  Usually this tingling is isolated to a specific region such as the chest or jaw, but in other cases, it occurs throughout the entire body (e.g. all of the joints).  If you experience an increase in bodily tingling, realize that it was likely caused by the Relpax and know that it will fade once the drug has been eliminated from systemic circulation.

The tingling may be accompanied by other sensations such as tightness, heaviness, and numbness.  At this time, it isn’t understood as to why tingling occurs in some users, as well as why the tingling may occur in a different region within one person compared to another.  That said, tingles may be a result of nerve fiber signaling alterations within the peripheral nervous system induced by Relpax.

Tiredness: In a subset of those taking Relpax, the tiredness induced by the drug is so extreme that they end up switching to another medication.  The extent to which a person feels tired after taking the drug may be largely a result of the dosage that’s ingested.  Sometimes tiredness and fatigue can be minimized by simply reducing the dose, while in other cases, dosage reduction plus a stimulatory adjunct may be useful.

While not everyone may find the tiredness as a side effect to be problematic, those engaged in high-performance occupational pursuits and/or advanced education may need to remain highly alert and vigilant at all times.  The tiredness may also be a detrimental side effect among those who are operating a motor vehicle – increasing likelihood of an accident.  Assuming you don’t need to remain productive, operate machinery, or a drive motor vehicle – you may be able to put up with a little tiredness.

Vomiting: In extreme cases, certain Relpax users may end up vomiting after taking their medication.  Vomiting is usually preceded by intense nausea, but may also be associated with significant dizziness.  Some users that end up vomiting report that their vomiting was caused by feeling extremely dizzy and/or a sensation of vertigo such as if the room was spinning.

To reduce the likelihood that you’ll end up vomiting, you may want to talk to your doctor about starting with a low dose.  You may want to experiment with taking the drug on an empty stomach and/or along with food to determine whether either reduces your inclination to vomit.  Since vomiting is an extreme adverse reaction and does not occur with every medication, if you regularly vomit from Relpax, realize that other interventions may be more tolerable.

Weakness: Feeling physically weak or losing strength (asthenia) is another well-documented side effect of Relpax.  The drug tends to cause drowsiness while simultaneously inducing the sensation of heaviness and/or pressure throughout the body.  This means you probably will want to avoid attempting any sort of physically-demanding activity such as jogging, weight lifting, and/or playing sports after you’ve ingested Relpax.

The weakness may render you completely useless for awhile, leaving you confined to your chair and/or the bed.  In time, as the drug leaves your system your strength will eventually return.  Still, if the muscle weakness is a problematic side effect (such as it could be among “blue collar” workers required to lift things and operate equipment), it should be discussed with your doctor.

Note: If you have any questions or concerns regarding any of the aforementioned Relpax side effects, it is recommended to contact a medical professional.

Variables that influence Relpax (Eletriptan) side effects

The specific side effects, number of side effects, and severity of side effects that occur during treatment with Relpax will be subject to interindividual variation – this was already mentioned.  However, not everyone realizes that certain variables are likely to heavily influence the side effects that they experience.  The most influential variables of Relpax side effects include: dosage, co-administered agents, frequency/duration of usage, CYP3A4 metabolism, and individual factors.

  1. Dosage (High vs. Low)

When administered as an abortive antimigraine agent, Relpax is typically administered to adults at either a dosage of 20 mg or 40 mg.  In clinical trials, both of these doses were regarded as being highly effective in the attenuation of migraine symptoms.  There is some evidence to suggest that (on average) the 40 mg dose is more effective than the 20 mg dose.

As a general rule of thumb, the greater the dosage ingested, the more likely you are to experience side effects.  High doses of Relpax not only can increase severity of certain side effects, but may provoke certain side effects that wouldn’t otherwise have occurred at a lower dose.  This is due to the fact that when ingested at high doses, the drug is exerting a greater effect upon the user’s neurophysiology; it’s disrupting homeostatic function to a more significant degree.

Disruption of homeostasis leads to a slight backlash of side effects.  It should also be mentioned that higher dose users will need to absorb, metabolize, and excrete a greater quantity of the drug, and as a result of the higher doses – these processes are less efficient.  At a lower dose, the body has an easier time metabolizing and excreting the drug because there’s a smaller amount.

If you are taking just 20 mg of Relpax, expect to experience less side effects than you would if you took the 40 mg dose and vice-versa.  Someone taking less than 20 mg and still getting antimigraine relief will likely have even fewer side effects than had they taken 20 mg.  On the other hand, someone exceeding the 40 mg recommended single-dose threshold may end up with severe side effects.

  1. Co-administered agents

If you’re taking Relpax, but also using other agents (medications or supplements), it is important to consider that the co-administered substances may alter the side effects you experience.  With any co-administered agent, there are two primary ways in which side effects are influenced: pharmacokinetically and pharmacodynamically.  Substances that interact with Relpax’s pharmacokinetic profile tend to act on the CYP3A4 isoenzyme.

There are many known CYP3A4 inducers which expedite the metabolism of Relpax including: Butalbital, Carbamazepine, Oxcarbazepine, Phenytoin, St. John’s Wort, etc.  Administration of these agents along with Relpax may affect not only its efficacy, but side effects.  Other substances known as CYP3A4 inhibitors could significantly increase side effects of Relpax because they interfere with its hepatic breakdown via CYP3A4.

Some examples of CYP3A4 inhibitors include: Clarithromycin, Indinavir, Ketoconazole, Ritonavir, etc.  So, assuming anyone is taking a CYP3A4 inducer or inhibitor with Relpax, understand that side effects may be exacerbated and/or differ compared to had they taken it as a standalone agent.  Additionally, some substances may simply provoke side effects as a result of modulating the serotonin system at the same time as Relpax.

If any serotonergic agent (e.g. an SSRI) is taken simultaneously along with Relpax, there’s a possibility that a user may experience serotonin syndrome – a side effect that wouldn’t occur if Relpax was taken alone.  It is also important to highlight the fact that some drugs/supplements may cause side effects of their own that a user may mistakenly believe to be caused by Relpax.  Unless Relpax is taken alone for awhile, it may be difficult to automatically assume that it is the culprit for certain side effects you experience.

Furthermore, we must consider the possibility that co-administered substances may entirely offset certain side effects resulting from Relpax.  For example, someone who drank a pot of coffee and then takes Relpax may feel less drowsy than had they not ingested any caffeine.  In a number of users, concurrently ingested substances are reducing unwanted Relpax side effects.

  1. Frequency/Duration of Administration

The frequency at which you administer Relpax refers to the number of times you ingest it on a daily or weekly basis.  Medical literature recommends that users not exceed 80 mg in dosing per day and that its safety when treating over 3 migraine attacks per day hasn’t been established.  It is important to understand that highly-frequent users may experience an entirely different set of side effects than infrequent users.

This may be due to the fact that the neurophysiology of a person taking the drug on a daily basis will eventually come to expect its administration and/or adapt to its influence.  As a result, the daily user may experience fewer side effects because the nervous system is no longer shocked each time the drug is administered.  On the other hand, someone using the drug once per week or every other week may experience the full set of side effects because the nervous system is not expecting the drug each time its administered.

Therefore, a lower frequency user may be more prone to side effects than a higher frequency one.  However, it could be that a high frequency (chronic) user may build up some sort of tolerance to Relpax and/or necessitate a dosage increase and that the low frequency (infrequent) user may be using a subtherapeutic dose with good success.  In this example, the high frequency user may actually experience more side effects than the lower frequency one.

In addition to frequency, it may be useful to consider total term of administration (e.g. weeks, months, years).  Someone that’s been taking Relpax for a long-term may have not only adapted to its effects (and experience fewer side effects), but may have tolerated it better from the beginning (hence the long-term use).  On the other hand, a short-term user may not have yet adapted to Relpax and may experience more side effects.

  1. Metabolism (CYP3A4)

Most evidence suggests that Relpax (eletriptan) is metabolized (N-demethylation) through the CYP3A4 isoenzyme.  Although the CYP3A4 gene that encodes for CYP3A4 isoenzyme expression won’t significantly alter Relpax metabolism in most of the population, approximately 5% of individuals of European descent are intermediate metabolizers, differing from the majority of the population (extensive metabolizers).  Intermediate metabolism indicates that the drug is still metabolized, but at a slightly slower pace than usual.

As a result of the slower metabolic breakdown and the fact that it’ll remain unmetabolized for a longer duration (than in extensive metabolizers), you’ll likely experience more severe side effects.  To determine whether you have a CYP3A4 variant that may result in intermediate metabolism of Relpax, you could consider a test such as GeneSight.  Realize that if you are among the small percentage of those with this variant, it may exacerbate side effect severity at higher doses.

  1. Individual factors

In addition to your dosage, whether you use other medications, frequency of usage, and CYP3A4 metabolism, there are still other miscellaneous individual factors that may influence side effects.  Multiple people could end up taking the same dosage of Relpax for the first time (with no other substances) with CYP3A4 extensive metabolism – yet different side effects may result.  These differences may be related to individual factors such as: administration specifics, genetics, medical conditions, sleep, and stress.

  • Administration specifics: Though you cannot control the time of day your migraine occurs, the time of day at which you administer Relpax may result in slightly different side effects. For example, someone who takes Relpax late at night may already be tired and find that the existing tiredness is potentiated by Relpax.  In addition to time of day, whether the drug is taken with or without food may make a difference in terms of altering side effects such as: fatigue, nausea, stomach aches, vomiting, etc.
  • Genetics/epigenetics: As was mentioned, the small percentage of people of European descent with a CYP3A4 polymorphism may metabolize the drug slightly slower than usual and experience more side effects at standard doses. However, other genes as well as epigenetic signatures may be more associated with certain side effects, while others may be protective against side effects.  Consider that your unique genetic code will influence whether you’re able to tolerate Relpax.
  • Medical conditions: Individuals with medical conditions other than migraines may respond differently to Relpax as a result. Not only are individuals dealing with medical conditions more likely to be using another medication (that may interact with Relpax), but side effects of treatment may be exacerbated as a result of neurophysiological changes associated with the particular condition.  For example, patients that have dealt with hypertension, heart problems, renal/hepatic impairment – are recommended to avoid Relpax due to the fact that it may worsen the underlying condition.
  • Sleep / Stress: Whether a person has been getting quality/sufficient sleep and their stress level could influence the side effects experienced while taking Relpax. Individuals that are under significant stress may find that there’s some synergism between symptoms of a stress response (e.g. irregular heartbeat, sweating, etc.) and side effects of Relpax.  Additionally, suboptimal or poor sleep hygiene may lead a person to perceive drug-related side effects as being more severe due to an overlap of sleep deprivation symptoms.

Relpax (Eletriptan): Do the benefits outweigh the side effects?

Whenever taking Relpax (or any antimigraine medication), it is important to communicate with your doctor and discuss whether its therapeutic benefits outweigh the side effects.  A subset of Relpax users may experience significant therapeutic benefits from the drug without any noticeable or unwanted side effects.  Among these users, continued usage of Relpax on an “as-needed” basis is certainly justified; it doesn’t get any better than symptomatic attenuation with perfect tolerability.

Other Relpax users may experience the exact opposite of the aforestated utopian responder.  These users may test out both the 20 mg and 40 mg dose, yet derive zero therapeutic benefit from the drug and may also experience debilitating side effects.  Even when taking it in accordance with their doctor’s instructions, they may experience major adverse reactions such as vomiting, hives, swollen body parts, etc. – and if the drug doesn’t provide symptomatic relief – it’s a no-brainer to opt for a more effective and tolerable solution.

Most individuals taking Relpax will fall somewhere in the middle between extremes of utopian (benefit plus no side effects) and dystopian (no benefit with lots of side effects) responders.  For example, most users will experience relief from migraine symptoms but also experience some unwanted side effects.  The drug may eliminate the migraine, but the side effect cost may be dizziness, nausea, muscle weakness, and chest pressure.

It is ultimately a personal decision as to whether you should continue using the medication or pursue an alternative intervention.  A helpful question to ask yourself during treatment is: “Would I rather have the migraine pain than the side effects of Relpax?” – if the answer is “Yes,” then this should be conveyed to your doctor.  You may also find it helpful to write about your experience with Relpax in a journal to document how well it works (efficacy) and any unfavorable reactions (side effects) you’ve experienced during treatment.

Possible ways to reduce Relpax side effects

There are some possible ways in which you may be able to reduce side effects resulting from Relpax.  Prior to implementing any of the strategies listed below, their safety and alleged efficacy should be discussed with a medical professional.  That said, some logical ways by which Relpax side effects could be reduced include: dosage reduction, co-supplementation, taking with food, avoiding using unnecessary substances, and/or continue using.

  1. Dosage reduction: Those experiencing severe side effects of Relpax may want to consider reducing their dosage. It is understood that side effects are often most severe at high doses due to the fact that the neurophysiological effect exerted by the drug is more substantial. Some individuals may derive antimigraine benefit from a subtherapeutic dose (e.g. 10 mg) and find that side effects are more tolerable at this lower level.  The easiest way to ensure that you aren’t experiencing unnecessary side effects is to take the minimal effective dose or just enough of the drug to alleviate your migraine but no more.
  2. Adjunctive interventions: If you’re experiencing severe side effects from Relpax, but it’s working well for migraine management, you may want to discuss introducing a potential adjunct with your doctor. For example, someone who’s feeling drowsy as a result of Relpax may benefit from adjunctive administration of a stimulatory agent such as caffeine. Those that feel dizzy, nauseous, and/or vomit – may want to consider antiemetics.  In many cases there is a safe adjunct that can be taken to attenuate certain side effects.
  3. Take with food: Sometimes individuals feel sick when taking Relpax on an empty stomach. Some of these individuals may benefit from eating a meal (or snack) with the drug. Others that get an upset stomach when taking Relpax with food may want to try taking it on an empty stomach.  While this intervention may not make a huge difference for most users, it could help slightly with any drug-induced gastrointestinal discomfort.
  4. Avoid other substances: In some cases, individuals may be ingesting an array of supplements and medications along with Relpax and would benefit from cutting back. Substances that are metabolized by CYP3A4 may be especially problematic to take along with Relpax. You may want to try avoiding unnecessary substances and determine whether avoidance ameliorates certain side effects.
  5. Continue using: As was mentioned, certain individuals may experience more prominent side effects with their first couple uses of Relpax, but these may diminish with continued regular administration. It may take a few weeks for your body to fully adjust to the intermittent effects of the drug. Sometimes continued usage is all that’s necessary for some side effects to abate.

Have you experienced Relpax (Eletriptan) side effects?

If you’ve taken Relpax, feel free to share a comment mentioning whether you experienced any side effects.  For those that experienced side effects, mention the specific side effects you experienced and their respective severities (e.g. on a scale from 1 to 10).  Would you say that the therapeutic antimigraine effect derived from Relpax outweighed these side effects?

To help others get a better understanding of your situation, mention your: Relpax dosage, how often you take it, whether you use other substances (medications, supplements, etc.), and whether you have other medical conditions.  Among individuals that are taking multiple substances along with Relpax – are you sure that the side effects are solely from Relpax?  Do you have any strategies that you’ve used to help you cope with certain side effects?

Understand that no abortive antimigraine intervention is regarded as universally optimal.  Some individuals will tolerate Relpax well, while others will find other treatments to be more effective and tolerable.  Always listen to your body by monitoring reactions to Relpax and communicate them to your doctor – if you don’t respond well, realize there are a host of viable alternatives.

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