Sumatriptan instructions for use: indications, dosage

Instructions for use of sumatriptan are required to be read in the same way as consultation with a specialist. Choosing a drug for the treatment of migraine is a very difficult task; 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.

Description 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 of sumatriptan

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.

pharmachologic effect

Serotonin 5-HT1 receptor agonist. A drug with antimigraine activity.

Pharmacokinetics

After oral administration, it is quickly absorbed. 70% of the maximum plasma concentration is achieved after 45 minutes. Cmax in blood plasma is 54 ng/ml. Bioavailability - 14% (due to first-pass metabolism and incomplete absorption). Plasma protein binding is 14-21%.

Metabolized by oxidation with the participation of monoaminoxylase (mainly isoenzyme A) with the formation of metabolites, the main of which are the indoleacetic analogue of sumatriptan, which does not have pharmacological activity against 5-HT1-serotonin receptors, and its glucuronide. It is excreted by the kidneys, mainly in the form of metabolites.

Pharmacodynamics

Sumatriptan is a specific selective agonist of 5-HT1-serotonin receptors, localized primarily in the blood vessels of the brain and their stimulation leads to a narrowing of these vessels. Does not affect other subtypes of 5-HT-serotonin receptors (5-HT2-7). Activates the sensitivity of trigeminal nerve receptors. The therapeutic effect usually occurs 30 minutes after administration.

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 2022).

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!

Contraindications to the use of Sumatriptan

hemiplegic, basilar or ophthalmoplegic forms of migraine;
IHD or the presence of symptoms suggesting its presence;
history of myocardial infarction;
pharmacologically uncontrolled arterial hypertension;
occlusive diseases of peripheral vessels;
stroke or transient cerebrovascular accident (including history);
severe dysfunction of the liver and kidneys;
simultaneous use with ergotamine or its derivatives and within 24 hours after their administration;
use while taking monoamine oxidase inhibitors or earlier than 2 weeks after discontinuation of these drugs;
age under 18 and over 65 years (efficacy and safety have not been established);
pregnancy;
breastfeeding (breastfeeding is possible no earlier than 24 hours after taking the drug;
congenital galactosemia, glucose/galactose malabsorption syndrome, congenital lactose deficiency;
hypersensitivity to any of the components of the drug.

With caution: epilepsy (including any conditions with a reduced epileptic threshold), pharmacologically controlled arterial hypertension, impaired liver or kidney function, hypersensitivity to sulfonamides (administration of sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis) .

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.

A neurologist named common mistakes in the fight against migraine

When people in any country in the world are asked what spoils their health most often, the undisputed leader emerges: headaches. It can begin after vaccination against coronavirus and is painful when contracting covid. Pierces during strokes and torments during brain tumors. However, in the vast majority of cases, there are two types of so-called primary headaches, that is, not associated with other diseases (as opposed to secondary pain, for example, with tumors or vascular accidents). These are tension headaches and migraines. The latter, according to the World Health Organization, affects more than a billion people, or every seventh inhabitant of the Earth. Every September there is a special International Migraine Awareness Week. What scientists and doctors have learned about this scourge recently and what misconceptions about migraine and its treatment are most common today, Margarita Naprienko, the head physician of the Academician Wayne Clinic for Headache and Autonomic Disorders, neurologist, Doctor of Medical Sciences, Professor at Sechenov University, told reporters.

PROBLEM 1: THIS IS NOT A DISEASE “Traditionally, in Soviet times, and I was still in this period, we practically did not treat headaches,” says Professor Naprienko. - On the one hand, there was such a disease, everyone knew it. On the other hand, it was as if it did not exist, because our patients could not receive sick leave. There were common expressions like “Migraine - too lazy to work”, they are still tenacious. And many patients do not come to specialists for precisely this reason. According to epidemiological data, with episodic migraine, which occurs up to eight times a month, only every fourth person consults a doctor. If headaches occur more often, only half, every second, go to specialists.

In fact, migraine, of course, is a full-fledged independent disease, the expert explains. Although, even today this disease remains a mystery for scientists and doctors.

PROBLEM 2: WHERE DOES IT COME FROM - The final theory of the origin of migraine and the development of the attack has not been formed. Great steps have been taken in this direction; some of the processes are clear to specialists, but the mechanism has not yet been fully studied,” says Margarita Naprienko. “We know that there are people with a certain functioning of the brain: they are susceptible to easy arousal under the influence of a variety of provoking factors. Against the background of such provocateurs, certain neurochemical processes in the brain are triggered, during which the levels of various substances change. Among them is serotonin, popularly known as the “pleasure hormone.”

Under the influence of the ongoing processes during migraine, the so-called “cortical spreading depression” develops, the doctor continues. It manifests itself in a decrease in the electrical activity of brain cells. “This wave travels through the brain tissue, causing vasoconstriction, which leads to decreased blood flow to the brain. During this period, people may experience a headache precursor such as an aura (see details below), says the professor. “However, this wave passes quickly enough, and the vessels begin to expand. Inflammation develops in them, blood flows into the inflamed wall of the vessel, and during this period people begin to feel pain.”

With migraine with aura, a cascade of different neurological symptoms is observed before the headache attack.

- These may be changes in vision, sensitivity, speech impairment. But it is very important that these changes are reversible, that is, they can last from five minutes to an hour, and must pass without fail, emphasizes Dr. Naprienko. “When this happens for the first time, patients get very scared, and doctors can’t always figure it out. Such reversible symptoms may be mistaken for acute cerebrovascular accidents (stroke).

PROBLEM 3: THERE IS NO LIFE THREATENING, BUT ITS QUALITY IS RADICALLY DECREASING Migraine is not a life-threatening disease, explains Margarita Naprienko. And because of this, patients often encounter misunderstandings from acquaintances, loved ones, colleagues and employers.

- The person seems to be healthy, his arms and legs are in place, he stands, he can work from the point of view of others. And at the same time he says that he cannot do anything. I am not aware of any cases where employers fired people because of migraines in Russia. But families in which migraine caused serious problems in relationships met at the reception. It was even necessary to write ridiculous certificates stating that the patient might actually be poorly able to work or completely incapacitated for a certain period of time. And, accordingly, during this period they are recommended to have relative peace.

What will happen if you do not engage in special treatment for migraines, endure attacks, and in the case when they are completely unbearable, call an ambulance? This is the approach that most patients practice, the doctor confirms.

- Of course, you can endure it, understanding that the attack will end. But it’s one thing if a person is not burdened with anything, does not work, and has no children requiring supervision. Then, perhaps, he can lie down in a dark room and wait for the torment to pass. But if continuous vomiting and a bursting headache begin, then people call an ambulance. Alas, in fact, it cannot greatly alleviate the condition of migraines, explains Professor Naprienko. — Yes, against the background of severe pain, a person’s blood pressure may jump and panic may begin, then sedatives will be administered to normalize the pressure. But the ambulance does not have the resources to act on the pain attack itself during a migraine.

PROBLEM 4: HOW TO BE TREATED? There are two approaches, the expert says. For episodic migraines (attacks no more than 8 times a month), medications are used to relieve headache attacks. If migraine occurs frequently, then preventive therapy is prescribed - it makes attacks less frequent and reduces pain.

“It is impossible to completely recover from migraine, because it is a genetically determined disease,” explains Margarita Naprienko. “But today it is quite possible to make attacks rare and not severe, which most patients do not know about.

The gold standard for treating a migraine attack is taking aspirin, the professor continues. “Better than effervescent, always in a large dosage, 1,000 mg (pay attention to contraindications! - Ed.). Anti-nausea medications may also be added if present. Very often, during a migraine attack, medications are poorly absorbed in the stomach, and then we prescribe drugs that enhance peristalsis. And we recommend low doses of caffeine. This could be a cup of sweet tea, coffee or even Coca-Cola.

An important point: if a person has a headache, it is extremely undesirable to immediately take a pill, emphasizes Dr. Naprienko. The body has a system to counteract pain and it is quite possible that it will cope without allowing an attack to develop. The same tea, coffee or cola can help. Taking painkillers too often and too quickly can lead to the development of so-called drug-induced headaches, warns a neurologist.

- If an hour has passed and your head still hurts, then you need to take triptans. They were created specifically for the relief of migraine attacks and made a real revolution (the first medicine of this class was registered back in 1991 - Ed.). Just keep in mind that triptans cause vasoconstriction, so they are not recommended for use during a migraine aura (see above) - if a person develops this condition, it is advisable to take aspirin first. Perhaps it will allow you to avoid an attack altogether. If not, then after the aura disappears, a triptan is taken.

PROBLEM 5: ADDITION TO MEDICINES “Triptans, which quickly relieve an attack and return a person to work, have a peculiarity: if used incorrectly, addiction to them can quickly develop,” notes Professor Naprienko. “That’s why we always warn patients: they need to strictly control the amount of medications they take. As soon as the figure exceeds 8 doses per month for triptans and 10-12 for simple analgesics (aspirin, citramone, paracetamol, ibuprofen, etc.), this is a direct indication for contacting a specialist. So that the patient is prescribed adequate therapy and preventive treatment is selected.

If you continue to swallow painkillers in huge doses and in huge quantities, then the aforementioned drug-induced headache develops, and the person ends up in a vicious circle, the doctor explains.

For the treatment of frequent, chronic migraines, botulinum toxin type A drugs are used as a preventive treatment, as well as new generation drugs based on monoclonal antibodies. The latter appeared in our country quite recently, about a year ago, and only a doctor can select and prescribe them.

STAY IN THE KNOW How to recognize a migraine

To make a diagnosis, doctors interview the patient. You can check yourself yourself. Here are the main signs of migraine:

- headache attacks last from 4 to 72 hours and are repeated;

- pain has at least two characteristics from the list: strong, throbbing, one-sided, makes you move less (intensifies with bending over, physical activity);

- there is also at least one of these symptoms: nausea, irritation by light and (or) sounds.

Link to publication: kp.ru

Side effects of sumatriptan

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.

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.

Sumatriptan

The drug should be prescribed only if the diagnosis of migraine is beyond doubt.

The drug is contraindicated for use in hemiplegic, basilar and ophthalmoplegic forms of migraine.

Before starting treatment, it is necessary to exclude types of potentially dangerous neurological pathology (for example, stroke, transient ischemic attacks) in the case where the patient has atypical symptoms, or when the patient has not been diagnosed with a condition requiring the use of sumatriptan.

After taking the drug, transient symptoms may occur, including pain and tightness in the chest, which may be intense and extend to the neck area. If there is reason to believe that these symptoms are a manifestation of coronary artery disease, it is necessary to conduct an appropriate diagnostic examination.

The drug should not be used in patients with risk factors for the development of coronary artery disease, including heavy smokers or users of nicotine replacement therapy, without prior examination of the cardiovascular system.

Particular attention should be paid to postmenopausal women and men over 40 years of age with these risk factors. However, the examination does not always reveal heart disease in every patient. In very rare cases, serious adverse reactions from the cardiovascular system may occur in patients with no history of cardiovascular pathology.

The drug should be used with caution in patients with controlled arterial hypertension, since 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 disorders, autonomic lability and neuromuscular disorders) as a result of simultaneous use of SSRIs and sumatriptan. The development of serotonin syndrome has also been reported during concomitant use of triptans with SNRIs.

In case of simultaneous use with drugs from the SSRI/SNRI group, the patient's condition should be carefully monitored.

The drug should be used with caution in patients with a history of seizures or other risk factors for lowering the seizure threshold.

In patients with known hypersensitivity to sulfonamides, taking the drug may cause allergic reactions that range from skin manifestations of hypersensitivity to anaphylaxis. Cross-sensitivity data are limited, but caution should be exercised before initiating sumatriptan in these patients.

Adverse reactions may occur more frequently during concomitant use of triptans and herbal preparations containing St. John's wort ( Hypericum perforatum

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.