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).
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.
Sumatriptan-OBL, 100 mg, film-coated tablets, 2 pcs.
Sumatriptan is not intended for the prevention of migraine. Sumatriptan should only be taken if the diagnosis of migraine is certain. Sumatriptan should be used as soon as possible after the onset of a migraine attack, but the drug is equally effective at any stage of the attack. If there is no effect from the first dose, the diagnosis should be clarified. When using sumatriptan to relieve headaches in patients with previously undiagnosed migraine or migraine with atypical symptoms, other potentially dangerous neurological diseases should be excluded. It must be borne in mind that patients with migraine are at risk of developing cerebrovascular complications (including stroke or transient cerebrovascular accident). Sumatriptan should be taken with caution in case of epilepsy and any other conditions accompanied by a decrease in the seizure threshold. In case of simultaneous use with SSRIs/SNRIs, the patient's condition should be carefully monitored.
Before using sumatriptan, patients should exclude the presence of cardiovascular disease, especially in patients at risk. These patients include postmenopausal women, men over 40 years of age, and patients with risk factors for coronary artery disease. The examination does not always reveal cardiovascular disease in some patients. In very rare cases, transient side effects such as chest pain and tightness may occur after taking sumatriptan. The pain can be intense and radiate to the neck (pharynx). If there is reason to believe that these symptoms may be a manifestation of coronary artery disease, it is necessary to stop taking the drug and perform a diagnostic examination. Treatment with sumatriptan should be carried out with caution in patients with controlled arterial hypertension, since in some cases an increase in blood pressure and peripheral vascular resistance may be observed. Sumatriptan should be used with caution in patients with diseases that may significantly alter the absorption, metabolism or excretion of sumatriptan, such as impaired renal or hepatic function. In patients with hypersensitivity to sulfonamides, when using sumatriptan, allergic reactions may develop, which range from skin manifestations to anaphylactic shock. Cross-sensitivity data are limited, but caution is warranted when administering sumatriptan to these patients. Overuse of medications intended to treat migraine attacks is associated with increased headaches in sensitive patients (drug overuse headache). In this case, the possibility of discontinuing the drug should be considered.
Effect on the ability to drive vehicles and control equipment During migraine, as well as during therapy with sumatriptan, drowsiness may develop. Therefore, during the period of use of sumatriptan, care must be taken 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.
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
).
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.
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.
Sumatriptan 100 mg
Sumatriptan should only be used in patients with an established diagnosis of migraine. The use of sumatriptan is not indicated for hemiplegic, basilar and ophthalmo-plegic 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 Sumatrintan, 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 examination of the cardiovascular system. 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 Sumatrintan, as 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.
