Choosing a drug for the treatment of migraine is a difficult task, since much depends on concomitant pathologies, the nature of the migraine, the use of other drugs, and the individual characteristics of the patient. A migraine attack will end in any case, even without any treatment, but it may take many hours or even several days.
In order to accurately diagnose migraines, choose the right medication and get quality help for migraines, you should visit a neurologist.
Characteristics of the substance
Latin name of the substance : Sumatriptanum
Formula : C14H21N3O2S
Chemical name : Sumatriptan, 3-[2-(Dimethylamino)ethyl]-N-methylindole-5-methanesulfonamide. The preparations contain sumatriptan succinate.
Description : Powder of white or almost white color. Easily dissolves in water and saline.
Clinical and pharmacological groups
- Serotonergic agent
- Selective 5-HT1 receptor agonist
- Drug with antimigraine activity
Action
Pharmacological action: anti-migraine .
Selective stimulation of 5-HT1 (5-hydroxytryptamine type 1) serotonin receptors causes constriction of dilated blood vessels in the brain and stops migraine attacks. Activates the sensitivity of receptors at the endings of afferent fibers of the trigeminal nerve, reducing the release and accumulation of sensory neuropeptides. Eliminates migraine-related nausea and photophobia.
Sumatriptan does not affect the 5-HT2 - 5-HT7 receptor subtypes. Does not have a direct analgesic effect.
Pharmacokinetics
Rapidly absorbed when taken orally and after intranasal administration. The maximum concentration in blood plasma when taken orally is achieved within 2–2.5 hours. Absolute bioavailability after oral administration averages 14% due to first-pass metabolism and incomplete absorption. The level of plasma protein binding is low (14–21%). Metabolized by oxidation with the participation of monoamine oxidase (MAO). The main metabolite is an indoleacetic analogue of sumatriptan, which does not have pharmacological activity against 5-HT1 and 5-HT2 receptors. Excreted by the kidneys and intestines. The half-life is 2–2.5 hours.
The clinical effect is usually noted:
- 30 minutes after oral administration of sumatriptan at a dose of 100 mg;
- 15 minutes after intranasal administration 20 mg;
- 10-15 minutes after subcutaneous injection.
Efficiency
In 50–70% of cases, sumatriptan quickly relieves a migraine attack when taken orally in a dose of 25 to 100 mg. Eliminates nausea and photophobia associated with migraine attacks. The greatest effect is observed when used at the height of an attack. In approximately a third of cases, a relapse may develop within the next 24 hours, which necessitates repeated use.
Reception and dosage
It is recommended to start taking the drug at the first manifestations of a migraine attack.
is not used for the same migraine attack . In such cases, paracetamol, acetylsalicylic acid or NSAIDs can be used to relieve an attack.
However, sumatriptan can be used to relieve subsequent migraine attacks . If the patient feels improved after the first dose and then symptoms return, a second dose may be administered within the next 24 hours, provided that the interval between doses is at least 2 hours.
Pills
Taken orally, the tablet should be swallowed whole with water. Treatment should be started as early as possible when a migraine attack occurs.
The recommended dose for adults is 50 mg, if necessary - 100 mg. The maximum daily dose is 300 mg.
Nasal spray*
This dosage form is especially indicated for migraine attacks accompanied by nausea and vomiting in children over 12 years of age, as well as for achieving an immediate clinical effect. The spray is equally effective when used at any stage of a migraine attack.
Use intranasally. The recommended dose of the drug for adults is 20 mg per nasal passage; for children 12-18 years old - 10 mg per nasal passage.
* The drug sumatriptan in the form of a spray does not have a registration certificate in the Russian Federation (excluded from the State Register of Medicines in 2021).
Introduction
Migraine is a common primary form of headache (TH), which manifests itself in the form of repeated attacks, often accompanied by nausea, vomiting, photo- and phonophobia.
The prevalence of migraine, according to various estimates, ranges from 2.6% to 21.7%, and the average rate is 14.7% [1]. In Russia, the prevalence of migraine reaches 20.8%, which is approximately more than 30 million people [2]. The prevalence of migraine in women is more than 2 times higher than that in men, and the highest prevalence of migraine within the female population occurs during reproductive age [3]. For this reason, issues of tactics for managing patients with migraine during pregnancy are of high relevance. Issues of pregnancy planning, as well as rules for taking medications for pain relief and approaches to preventive treatment of migraine during pregnancy are discussed very often.
Contraindications
- Hypersensitivity;
- hemiplegic, basilar or ophthalmoplegic form of migraine;
- myocardial infarction (including a history), uncontrolled arterial hypertension, coronary artery disease (or suspicion of it), angina pectoris, incl. Prinzmetal's angina;
- occlusive diseases of peripheral vessels (atherosclerosis, thrombosis);
- transient cerebrovascular accident (including a history), stroke (including a history);
- severe impairment of liver and/or kidney function;
- simultaneous use of sumatriptan with other serotonergic drugs (ergotamine, metisegride, triptans), serotonin reuptake inhibitors and monoamine oxidase inhibitors (up to 14 days after their discontinuation).
Sumatriptan is not used to prevent migraine attacks!
The course of migraine during pregnancy
In 50–70% of women during pregnancy, migraine without aura improves [4]. Migraine attacks become mild, extremely rare, and in most patients in this group the migraine completely disappears. Improvement occurs after the first trimester, starting from the 12th–14th week. pregnancy. This is due to the fact that by the beginning of the second trimester, the level of estrogen stabilizes and begins to increase, and its fluctuations stop (Fig. 1). Migraine with aura stops less often during pregnancy, in approximately 40% of patients.
At the same time, if headache persists during this period, it is necessary to carry out differential diagnosis and determine the form of headache. Alarming symptoms during pregnancy are:
the appearance of a new, unusual headache;
a sharp increase in migraine attacks;
the addition of new, unusual symptoms of hypertension, including visual impairment, sensitivity, aphasia, paresis of the limbs;
the appearance of migraine aura in patients with previous migraine without aura;
increased blood pressure during hypertension;
convulsions.
The presence of active migraine during pregnancy does not affect the course of pregnancy itself and the development of the fetus, but increases the risk of preeclampsia and gestational hypertension. Moreover, the persistence of active migraine, especially migraine with aura, during pregnancy increases the risk of acute cerebrovascular accidents (ACVA) by 15–17 times [5]. The prevalence of stroke during pregnancy and the early postpartum period is 34.2 cases per 100,000 births [5].
Restrictions
For diseases
with caution for epilepsy and a history of seizures, controlled arterial hypertension, in the presence of risk factors for the cardiovascular system (including smoking), impaired renal or liver function.
Age
For people under 18 and over 65 years , safety and effectiveness have not been established. The nasal spray is approved for use from 12 years of age.
Pregnancy and lactation
During pregnancy, it is possible only if the expected benefit to the mother outweighs the potential risk to the fetus (insufficient safety studies). Breastfeeding should be avoided for 24 hours after taking sumatriptan, as the substance is absorbed into breast milk.
Effect on psychomotor skills
Drivers should exercise caution , as well as during work that requires increased attention and quick reaction. With migraine, as well as during therapy with sumatriptan, drowsiness may develop.
Sumatriptan, 2 pcs., 50 mg, film-coated tablets
Sumatriptan should only be used in patients with an established diagnosis of migraine. The use of sumatriptan is not indicated for hemiplegic, basilar and ophthalmoplegic migraine.
Do not exceed recommended doses of sumatriptan. As with other medications used to treat acute migraine attacks, other potentially serious neurological pathologies should be excluded before treating a headache attack in patients who have not previously been diagnosed with migraine or in patients with atypical migraine. It should be noted that patients with migraine have an increased risk of developing certain cerebrovascular events (eg, stroke or transient ischemic attack (TIA)).
After taking Sumatriptan, transient symptoms such as pain and tightness in the chest may occur. Symptoms can be intense and extend to the neck area. If there is reason to believe that these symptoms are a manifestation of coronary heart disease (CHD), further use of sumatriptan should be discontinued and appropriate diagnostic testing should be performed.
Patients with risk factors for developing coronary heart disease, incl. Heavy smokers or patients using nicotine replacement therapy should not be prescribed sumatriptan without prior cardiovascular evaluation. Particular attention should be paid to postmenopausal women and men over 40 years of age who have these risk factors. However, testing does not always detect heart disease, and in very rare cases, serious cardiac complications have occurred in patients without underlying cardiovascular disease.
Sumatriptan should be used with caution in patients with controlled mild hypertension, as a transient increase in blood pressure and peripheral vascular resistance was observed in a small number of patients.
There are rare reports from post-marketing surveillance of the development of serotonin syndrome (including mental status disorders, autonomic lability and neuromuscular disorders) as a result of concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan. The development of serotonin syndrome has also been reported during concomitant use of sumatriptan with triptans and selective norepinephrine reuptake inhibitors (SNRIs).
If concomitant use of SSRIs and/or SNRIs is clinically warranted in a patient, the patient's condition should be carefully monitored. Sumatriptan should be used with caution in patients in whom the absorption, metabolism, or excretion of sumatriptan may be significantly altered, such as patients with hepatic impairment or impaired renal function. In patients with liver failure, the initial dose should be 50 mg.
Sumatriptan should be used with caution in patients with a history of seizures or other risk factors for lowering the seizure threshold, as cases of seizures have been reported while taking sumatriptan.
In patients with established hypersensitivity to sulfonamides, taking Sumatriptan may cause allergic reactions that range from cutaneous hypersensitivity reactions to anaphylaxis. Cross-sensitivity data are limited and caution should be exercised before administering sumatriptan to these patients.
Adverse reactions may occur more frequently with the simultaneous use of triptans and medications containing St. John's wort.
Long-term use of any type of painkiller for headaches can make them worse. If this situation occurs or is suspected, it is necessary to stop therapy and conduct additional examination. Drug overuse headache may be suspected in patients who experience recurrent or daily headaches despite regular use of headache medications.
Patients with rare hereditary lactose intolerance, lactase deficiency and glucose-galactose malabsorption should not take Sumatriptan, since it contains lactose.
Impact on the ability to drive vehicles and machinery
Patients with migraine may experience drowsiness associated both with the disease itself and with taking the drug Sumatriptan. Patients should be especially careful when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Side effect
Cardiovascular system and blood
Arterial hypotension or short-term increase in blood pressure, bradycardia or tachycardia, transient ischemic ECG changes, heart rhythm disturbances; in isolated cases - myocardial infarction, Raynaud's syndrome.
Nervous system and sensory organs
Dizziness, weakness, drowsiness, paresthesia; rarely - convulsions (if there is a predisposition), decreased visual acuity, diplopia, scotoma.
Digestive system
Nausea, vomiting, abdominal discomfort, dysphagia, rarely - ischemic colitis. Changes in liver function tests (slight increase in enzyme activity).
Allergy
Skin rash, urticaria, itching, erythema; rarely - anaphylaxis. In patients with hypersensitivity to sulfonamides, allergic reactions may develop when using sumatriptan.
Some of the symptoms listed may be symptoms of migraine. If any of the adverse reactions indicated in the instructions worsen or other adverse reactions not listed in the instructions are noticed, you must inform your doctor.
Other
Muscle pain, tingling, sensation of heat, pressure in the chest, throat and other parts of the body, rush of blood to the face, irregular breathing rhythm.
For the intranasal form: burning, nosebleeds.
Evgeniya
“My migraines usually start with an aura. It can be different. In my case, it’s as if I’m inside a soap bubble, from which, firstly, it’s very hard to hear, and secondly, the world around me shimmers with all the colors of the rainbow. In addition, olfactory hallucinations begin, and very funny ones at that. For example, from the last one: while walking my dog in the forest, I smelled smoked sausage. From time to time I smell metal or alcohol - and this is definitely a sign of an impending migraine. I learned about this symptom from American migraine groups, which I read all the time: they discussed that olfactory hallucinations are very often a precursor to migraines.
I have several types of migraines: the most common are a reaction to changes in atmospheric pressure. In addition, there are hormonal and stress migraines. After undergoing long-term therapy, I learned to regulate stress quite well. The weather is absolutely not controlled in any way. True, I have low blood pressure, and from time to time I drink a lot of coffee, which sometimes manages to pull me out of an attack. But, unfortunately, at some point the migraine may start again - already because I drank too much coffee. That is, it’s difficult to understand: your head hurts because the atmospheric pressure is jumping again or because coffee is already flowing through your veins instead of blood.
Sometimes I get migraines without pain, just an aura. In such a situation, I can’t think, I can’t work, the general condition is very unpleasant, but I can tolerate it. And the most hellish pain is hormonal migraines. Here it comes to trips to the hospital. I noticed that with hormonal migraines I do not have enough oxygen, and the doctor prescribed it to me. I have an oxygen cylinder next to my bed, and I can periodically put on an oxygen mask (the heroine lives in Sweden, editor's note).
Of the non-drug ways to combat migraines, I use heat and cold. I have gel pads that I keep in the freezer. When an attack begins, family members carry them back and forth - in our house this is called “bringing cartridges.” In addition, I have a soft toy - a sheep with filling and lavender, which can be heated in the microwave. I also read this method on the forum. If a person can lie down, then it is better to lie down, but the legs should be slightly higher than the level of the head. I place the cold at the base of the skull and the hot sheep under my feet. And this often makes my condition easier.”
special instructions
Before prescribing sumatriptan to patients with newly diagnosed or atypical migraine, other potentially dangerous neurological diseases should be excluded.
Overuse of medications intended to treat acute headaches is associated with increased headaches in sensitive patients (drug-overuse headache). In this case, the possibility of discontinuing the drug should be considered.
Before and during treatment, it is necessary to eat regularly, exclude foods containing tyramine (chocolate, cocoa, nuts, citrus fruits, beans, tomatoes, celery, cheeses), as well as alcoholic drinks (including dry drinks, especially red ones, wines, champagne , beer), lead a healthy lifestyle in order to prevent migraine attacks and reduce their frequency.
Stopping attacks
The selection of drug therapy for patients with migraine during pregnancy poses significant difficulties. The severity of migraines can be especially high during the first trimester. Full-blown, unrelieved migraine attacks are often accompanied by nausea, vomiting and lead to unnecessary suffering and dehydration, especially in patients suffering from early toxicosis. Despite the desire to avoid taking medications (especially in early pregnancy) to minimize the risk of fetal developmental disorders, many patients with hypertension begin to take analgesics uncontrollably. Therefore, the importance of preliminary counseling and education of patients on the proper control of hypertension cannot be overemphasized.
Non-pregnant women are recommended to take medications to relieve migraine attacks as early as possible, no later than 1 hour after the onset of the attack. This approach allows you to speed up relief and completely stop a migraine attack in a short time. Pregnancy is the only period in a woman’s life when this recommendation can be temporarily ignored. For patients seeking to minimize drug use, a stepwise approach may be recommended, in which treatment of mild to moderate attacks begins with non-drug methods.
If the patient decides not to use analgesics, control of nausea becomes a priority to avoid dehydration. Patients should avoid strong odors and drink more fluids, such as juices diluted 1:1 with water. Feelings of nausea can also be reduced by eating easily digestible foods, such as crackers, applesauce, bananas, rice, and pasta. Metoclopramide or ondansetron can also be used [6].
Neurostimulation methods play a major role in non-drug approaches to the treatment of migraine. The only device registered in Russia for non-invasive transcutaneous stimulation of the supraorbital nerve - Cefaly (Cefaly®) - is specially designed for the treatment of migraines and can be a good alternative to medications for relieving migraine attacks. Using the Cefaly device at the very beginning of an attack allows you to reduce the intensity of headaches and in some cases completely stop the attack. Thus, the intensity of migraine pain decreases by 4.3 points after 1 hour [7]. Cefaly can also be used in conjunction with pain medications to increase their effectiveness.
Despite the fact that, in general, paracetamol is less effective for relieving an acute attack of migraine than acetylsalicylic acid and nonsteroidal anti-inflammatory drugs (NSAIDs), its safety during pregnancy is higher [6]. Caffeine, which has the ability to enhance the analgesic effect, is an important addition to painkillers. Adding 100 mg of caffeine to the analgesic increases its effect by 1.5 times.
The safety of NSAIDs is controversial [6]. Prescribing NSAIDs in the first trimester may be associated with an increased risk of miscarriage and the development of congenital anomalies. Taking NSAIDs and aspirin in the third trimester can lead to premature closure of the ductus arteriosus
. For these reasons, the use of NSAIDs should be limited to the second trimester. It is especially important to stop taking them after the 32nd week. Taking high doses of aspirin may also increase the risk of bleeding.
Triptans are the most effective analgesics for the relief of migraine attacks. The safety of triptans during pregnancy is assessed through pregnancy registries, where a huge amount of data has now been accumulated for sumatriptan, for example. Despite the prohibition of its use during pregnancy indicated in the official instructions for the use of sumatriptan, there is no evidence of an increased risk of congenital malformations when taken by pregnant women [8]. Patients who took triptans in early pregnancy (without knowing they were pregnant) should be advised that the likelihood of adverse effects of this drug on the fetus is extremely low. Women who experience severe, disabling migraine attacks that cause vomiting may be advised to use triptans during pregnancy. To date, this information has not been included in official recommendations for the treatment of migraine, but the safety of sumatriptan is confirmed by the analysis of a huge number of observations and expert recommendations.
It should be borne in mind that the safety of triptans varies. Sumatriptan, as the most hydrophilic of the triptans, has difficulty penetrating the placental barrier, while other triptans (including eletriptan) are lipophilic.
Prednisolone can only be used as an “ambulance” remedy in the event of a prolonged and severe migraine attack [9]. The use of prednisolone is preferable to dexamethasone, since the latter penetrates the placenta better. Nuchal nerve blocks with lidocaine, bipuvacaine and/or a corticosteroid can be used as an ambulance to relieve severe attacks.
Interaction
Concomitant use is contraindicated:
- with ergotamine and ergotamine-containing drugs (prolonged vasospasm is possible, a 24-hour pause between doses is recommended);
- with monoamine oxidase inhibitors;
- with lithium salts (cases of the development of serotonin syndrome have been described);
- with drugs from the group of selective serotonin reuptake inhibitors;
- with other triptans (risk of additive hyperstimulation of serotonin receptors);
- with herbal preparations containing St. John's wort.
There was no interaction of sumatriptan with propranolol, flunarizine, pizotifen, or ethyl alcohol.
