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.
Compound
One tablet of Imigran contains 50 or 100 mg sumatriptan ( sumatriptan succinate ) + lactose anhydrous, croscarmellose sodium, Opadry pink food coloring (100 mg dosage contains white coloring), titanium dioxide, red iron oxide, methylhydroxypropylcellulose, lactose monohydrate, croscarmellose sodium, magnesium stearate , triacetin.
Imigran spray contains per dose 20 or 10 mg of the active ingredient sumatriptan + anhydrous disubstituted sodium phosphate, sodium hydroxide, monopotassium phosphate, sulfuric acid, purified water.
Release form
The medicine is produced in the form of pink (50 mg) or white (100 mg) oval convex tablets. On one side there is an engraving “IMIGRAN”, on the other there is an inscription 50 (or only 50), on tablets with a dosage of 100 mg there is an engraving “GLAХO” on one side and “IMIGRAN” (or 100) on the other. If you break the tablet in half, the inside will be white or almost white. The product is sold in blisters of 1 or 2 pieces, in a cardboard pack one or 2 blisters.
The drug is also sold in disposable bottles with a dispenser, with a capacity of 20 or 10 mg, in a cardboard box there are 1 or 2 bottles. The liquid is clear, dark or light yellow.
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
Pharmacodynamics and pharmacokinetics
The active substance of the drug sumatriptan constricts blood vessels in the carotid artery system, without changing the intensity of cerebral blood flow . This occurs due to the ability of the substance to act on 5HT1 receptors without affecting the activity of other 5HT receptors . The drug also reduces the activity of the trigeminal nerve . These two mechanisms determine the anti-migraine effect of the drug.
After intranasal administration, the active components of the drug quickly penetrate the systemic bloodstream. The maximum concentration is achieved within 40 minutes - 1.5 hours. The effect occurs within 15 minutes.
When taking tablets, the absolute bioavailability is 14%, since the active substance is not completely absorbed and undergoes first-pass metabolism . Improvements in the patient's condition occur after half an hour.
The degree of binding to blood plasma is up to 21%. The half-life is 120 minutes.
With excess body weight, volume of distribution and clearance increase. The drug undergoes oxidative metabolism with the participation of MAO . The medicine is excreted in the form of metabolites through the kidneys.
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.
Contraindications
The drug is not recommended for use:
- if you are allergic to its components;
- if the patient has previously had a stroke or cases of severe cerebrovascular accident;
- after myocardial infarction ;
- for coronary heart disease , peripheral vascular diseases, Prinzmetal's angina ;
- under 18 years of age, over 65 years of age;
- persons suffering from severe liver dysfunction;
- during therapy with MAO inhibitors (at least 14 days must pass), ergotamine or its derivatives, 5-HT1 receptor agonists .
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.
Side effects
During clinical studies, the following adverse reactions were identified:
- burning or irritation in the nasal cavity or throat (for spray), shortness of breath , nosebleeds ;
- dizziness , paresthesia , decreased sensitivity, drowsiness ;
- hot flashes, increased blood pressure ;
- decreased blood , bradycardia , tachycardia , nausea;
- vomiting, feeling hot or cold, or a feeling of squeezing, heaviness, or tightness in various parts of the body, including the throat or chest;
- weakness, fatigue.
As a result of post-marketing observations, the following were identified:
- tremor , convulsions , nystagmus , dystonia ;
- decreased visual acuity, blindness that passes over time, diplopia , scotoma ;
- cardiac arrhythmias , changes in the electrocardiogram , Raynaud's syndrome ;
- dysphagia , epigastric (for tablets), ischemic colitis ; allergic skin rashes, anaphylaxis .
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.
Instructions for use of Imigran (method and dosage)
Tablets and spray cannot be used to prevent migraines.
Despite the fact that the drug remains effective both in the early stages of an attack and at its height, it is recommended to take the medicine at the first signs of migraine.
Instructions for use of Imigran tablets
Take it whole, wash it down with water.
A single dosage for an adult is 50 or 100 mg of the drug. If taking one tablet is not effective enough, then you should not take another dose of the medicine.
You can take the pill next time only after 2 hours. The maximum daily dosage is 300 mg.
Instructions for the spray
Intranasally. Prescribe one dose (20 mg) in each nostril.
In different groups of patients, depending on the individual characteristics of the body, the effectiveness of the same dosage varies. Sometimes taking 10 mg of the drug is enough.
Within 24 hours after the first attack has stopped, you can take another dose of the drug. The interval between doses should be at least 2 hours.
The maximum daily dosage is 40 mg of the drug.
Before using the spray, it is recommended to take a comfortable position and clean the nasal cavity, then remove the packaging and point the dispenser tip into one of the nasal passages, close the second nostril with your finger, and breathe through your mouth. You need to press the blue button while inhaling. Then you can breathe calmly and shallowly. Inhale through the nose, exhale through the mouth (continue for about 20 seconds). The dispenser cannot be reused.
It should be remembered that you can only press the blue button once, you cannot press it in advance.
Interaction
The drug can be taken with Propranolol, Pizotifen, ethanol and Flunarizine .
Combining the drug with Ergotamine can lead to vasospasm. It is necessary to maintain a 24-hour interval between doses.
Imigran cannot be combined with MAO inhibitors .
selective serotonin reuptake inhibitors caution may develop: weakness, impaired coordination of movements, and hyperreflexia .
special instructions
The drug can be taken only after consultation with a doctor, after confirmation of the diagnosis. Before taking Imigran, other neurological diseases (to avoid stroke , cerebral circulatory disorders).
The medicine is used to relieve migraine and as emergency therapy.
If the patient has previously had allergic reactions to sulfonamide antibiotics , then the risk of developing such reactions to sumatriptan increases.
If after using the remedy there is no improvement in the patient’s condition, it is necessary to clarify the diagnosis.
The drug is not recommended for use by women after menopause, men over 40 years of age, patients with coronary artery , hypertensive patients , or with a decrease in the seizure threshold ( epilepsy, organic brain damage ).
Caution must be observed in case of disorders of the liver and kidneys.
Do not exceed the recommended daily dosage of the product.
After taking the medicine, it is recommended to refrain from driving and performing potentially hazardous activities.
Very rarely, the combination of sumatriptan with selective serotonin reuptake inhibitors has led to the development of serotonin syndrome . Therefore, special care should be taken with this combination.
Imigran 20 mg 1 pc. dosed nasal spray glaxosmithkline manufacturing spa
pharmachologic effect
Interacts with 5-HT1 receptors (does not affect 5-HT2 - 5-HT7 receptor subtypes), mainly in the blood vessels of the brain (their stimulation leads to vasoconstriction).
Composition and release form Imigran 20 mg 1 pc. dosed nasal spray glaxosmithkline manufacturing spa
Film-coated tablets - 1 tablet.
- Active substance: sumatriptan (in the form of sumatriptan succinate) - 50 or 100 mg;
- Excipients: lactose monohydrate; lactose anhydrous; MCC; croscarmellose sodium; magnesium stearate;
- Tablet shell: for a dosage of 50 mg - Opadry pink YS-1-1441-G; methylhydroxypropylcellulose; titanium dioxide; triacetin; iron oxide red; for a dosage of 100 mg - Opadry white OY-S-7393; titanium dioxide; methylhydroxypropylcellulose.
There are 2 pcs in a blister; 1 blister in a box.
Spray for nasal use - 1 dose:
- Active substance: sumatriptan - 10 or 20 mg;
- Excipients: monosubstituted potassium phosphate; sodium phosphate disubstituted anhydrous; sulfuric acid; sodium hydroxide; purified water.
In disposable bottles, with a dosing device; There are 1 or 2 bottles in a box.
Description of the dosage form
50 mg tablets: pink, oval, biconvex, film-coated tablets engraved with “IMIGRAN” on one side and “50” on the other (or plain on one side and engraved “50” on the other). Tablet dimensions: 12×6.5 mm. Two layers are visible on the fracture: the inner layer (tablet core) is white or almost white; the outer layer (tablet shell) is pink. 100 mg tablets: White or off-white, oval, biconvex, film-coated tablets engraved with "GLAXO" on one side and "IMIGRAN" on the other (or plain on one side and engraved "100" on the other). Tablet dimensions: 12×6.5 mm. At the break, the tablets are white or almost white. Nasal spray: clear liquid from light yellow to dark yellow.
Characteristic
Selective 5-HT1 receptor agonist (5-HT1D).
Directions for use and doses
Tablets: the drug is recommended to be used as soon as possible after the onset of a migraine attack. The recommended dose for adults when taken orally is 100 mg. The maximum daily dose is 300 mg. The tablet should be swallowed whole with water. Injections: it is recommended to start treatment when the first signs of a headache or “aura” appear - nausea, vomiting, photophobia. The injections should be administered subcutaneously using an autoinjector. For migraine, the recommended dose for adults is 6 mg as a single subcutaneous injection. If symptoms recur, an additional 6 mg may be given at any time over the next 24 hours, but not earlier than one hour after the first dose. The maximum permissible daily dose is two injections of 6 mg (12 mg).
Pharmacodynamics
In animals, sumatriptan selectively constricts blood vessels in the carotid artery system but does not alter cerebral blood flow. It is believed that dilation of these vessels and/or swelling of their walls is the main mechanism of migraine in humans. In addition, it has been experimentally established that sumatriptan inhibits the activity of the trigeminal nerve. Both of these effects may underlie the antimigraine action of sumatriptan.
Pharmacokinetics
Sumatriptan is rapidly absorbed after oral administration and after intranasal administration. When taken orally, 70% of Cmax in plasma is achieved after 45 minutes; when taken at a dose of 100 mg, Cmax in plasma averages 54 ng/ml. After intranasal administration, Cmax in plasma is reached after 1-1.5 hours and is 12.9 ng/ml. The average absolute bioavailability after oral administration is 14% due to first-pass metabolism and incomplete absorption. Due to first-pass metabolism, the average absolute bioavailability with intranasal administration is 15.8% of that with subcutaneous administration. In patients with impaired liver function, increased plasma levels of sumatriptan should be expected as a result of decreased presystemic clearance. The degree of binding to plasma proteins is low (14-21%), the total volume of distribution averages 170 l, T1/2 - approximately 2 hours. Total plasma Cl averages 1160 ml/min, renal Cl - 260 ml/min, extrarenal clearance - about 80% of the total clearance. In adolescents (12-17 years old), the average Cmax in plasma is 13.9 ng/ml, the average T1/2 is about 2 hours. In adolescents with excess body weight, there is an increase in clearance and volume of distribution of the drug, therefore, with a lower body weight, they have a higher exposure to sumatriptan. The main mechanism for the elimination of sumatriptan is oxidative metabolism, which is carried out under the action of the enzyme MAO type A. The main metabolite, the indoleacetic analogue of sumatriptan, is excreted primarily in the urine, where it is found in the form of a free acid and a glucuronide conjugate. This metabolite has no activity at the 5-HT1 or 5-HT2 receptors. No minor metabolites have been identified. Migraine attacks do not appear to have a significant effect on the pharmacokinetics of sumatriptan administered orally or intranasally.
Indications for use Imigran 20 mg 1 pc. dosed nasal spray glaxosmithkline manufacturing spa
For quick relief of migraine attacks.
Contraindications
- angina pectoris or myocardial infarction in the past;
- impaired liver and kidney function;
- epilepsy;
- old age (over 60 years);
- hypersensitivity to the drug.
Application Imigran 20 mg 1 pc. dosed nasal spray glaxosmithkline manufacturing spa during pregnancy and breastfeeding
Contraindicated during pregnancy, breastfeeding and childhood.
special instructions
Imigran cannot be used for prophylactic purposes. The drug should be prescribed only if the diagnosis is beyond doubt. As with the use of other antimigraine drugs, when prescribing Imigran in patients with previously undiagnosed migraine or in patients with atypical migraine, it is necessary to exclude other potentially serious neurological conditions. It should be taken into account that patients with migraine have an increased risk of developing certain cerebrovascular disorders (for example, stroke or transient cerebrovascular accident). Sumatriptan should not be prescribed to patients with suspected heart disease without prior evaluation to exclude cardiovascular pathology. These patients include postmenopausal women, men over 40 years of age, and patients with risk factors for coronary artery disease. Although testing may not always detect heart disease in some patients, in very rare cases they develop cardiovascular side effects. After taking sumatriptan, transient intense pain and tightness in the chest may occur, spreading 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. In patients with controlled arterial hypertension, sumatriptan should be prescribed with caution, because in some cases, a transient increase in blood pressure and peripheral vascular resistance was observed. In case of simultaneous administration with drugs from the SSRI group, the patient's condition should be carefully monitored. Sumatriptan should be used with caution in patients suffering from diseases in which the absorption, metabolism or elimination of this drug may be significantly altered (for example, impaired renal or hepatic function). Caution should be exercised in patients with a history of epilepsy or structural brain damage that lowers the seizure threshold. In patients with hypersensitivity to sulfonamides, administration of sumatriptan may cause allergic reactions that range from skin manifestations to anaphylaxis. Cross-sensitivity data are limited, but caution should be exercised when prescribing sumatriptan to such patients. Clinical experience with the use of Imigran in elderly patients (over 65 years of age) is limited. There are no significant differences in the pharmacokinetic parameters of sumatriptan in elderly people and in young patients, however, until additional data from clinical studies are available, it is not recommended to prescribe Imigran to patients over 65 years of age. Patients with migraine may experience drowsiness associated both with the disease itself and with taking Imigran, so they should be especially careful when driving and working with moving machinery. The recommended dose of Imigran should not be exceeded.
Overdose
Taking Imigran orally at a dose of more than 400 mg, or a single subcutaneous administration at a dose of 16 mg, or administering Imigran once at a dose of 40 g intranasally did not cause any side effects other than those listed above. Treatment: observation of the patient’s condition for at least 10 hours, if necessary, standard supportive therapy. There are no data on the effect of hemodialysis or peritoneal dialysis on plasma concentrations of sumatriptan.
Side effects Imigran 20 mg 1 pc. dosed nasal spray glaxosmithkline manufacturing spa
- tingling and warm sensation;
- dizziness and feeling of weakness, drowsiness;
- decreased blood pressure, palpitations;
- nausea and vomiting;
- rash and itching.
Drug interactions
There was no interaction of sumatriptan with propranolol, flunarizine, pizotifen and ethyl alcohol. When taken simultaneously with ergotamine, prolonged vasospasm was observed (sumatriptan can be prescribed no earlier than 24 hours after taking drugs containing ergotamine, and drugs containing ergotamine can be prescribed no earlier than 6 hours after taking sumatriptan). Interaction between sumatriptan and MAO inhibitors is possible; their simultaneous use is contraindicated. There are isolated reports of the development of weakness, hyperreflexia and loss of coordination in patients after concomitant use of sumatriptan and drugs from the group of selective serotonin reuptake inhibitors (SSRIs). If sumatriptan and SSRIs are co-administered, the patient's condition should be carefully monitored.
Analogs
Level 4 ATC code matches:
Zolmitriptan
Rapidmed
Zomig
Relpax
Sumamigren
Amigrenin
Sumatriptan
Algomax, Migranol, Stopmigren, Sumatriptan, Amigrenin, Zomig, Rapimog, Rizamigren, Relpax, Frovamigran, Sumamigren.
Reviews
They respond very well to the medicine. Adverse reactions from taking tablets or using a spray occur infrequently. Some complain that the medicine can be difficult to obtain.
Reviews of Imigran spray and tablets:
- “... A very good drug. A Korean neurologist prescribed him. During the attack I drank, after 1.5 hours I felt relief, after 2 hours the pain completely disappeared”;
- “...I was prescribed this drug for cluster headaches by a neurologist. To be honest, I used to think that these headaches cannot be relieved by anything - you just need to wait and clench your fists, but Imigran nasal spray really helps after about 15-20 minutes, so the drug is not bad. The only “but” is its price and the fact that there is only one dose in the package. Unfortunately, you can’t find it in every pharmacy and there is a maximum of 3 doses available.”
