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Sumatriptan, a synthetic tryptamine derivative, was developed by GlaxoSmithKline in 1989 for the treatment of migraine. It is administered orally, into the nose, or by injection under the skin. Effects usually occur within the first three hours after administration. Common side effects include chest pressure, feeling tired, feeling like the world is spinning, vomiting, and tingling. Serious side effects may include serotonin syndrome, heart attacks, strokes, and seizures. Overuse of medications may result in overuse headaches. There is no reliable information on use during pregnancy or lactation. Belongs to the triptan class of drugs. The mechanism of action is not fully understood. Sumatriptan was patented in 1982 and approved for medical use in 1991.
Application in medicine
Sumatriptan is effective in stopping or relieving the intensity of migraine and cluster headaches. It is most effective when taken early after pain begins. Injected sumatriptan is more effective than other drugs. In a 2016 Cochrane review of the combination of sumatriptan and naproxen for acute migraine in adults, it was better than placebo for the relief of acute migraine in adults. The combination was better than placebo or one drug alone at relieving other migraine symptoms (nausea, sensitivity to light or sound) and reducing loss of ability to function normally. Adverse events of dizziness, tingling or burning of the skin, drowsiness (drowsiness), nausea, indigestion (dyspepsia), dry mouth, and chest discomfort were more common with sumatriptan (alone or in combination) than with placebo or naproxen. As a rule, they were mild or moderate in severity and rarely led to study refusal. The studies were conducted to a high standard and were generally large enough to produce reliable results, so that most effectiveness results were of high quality. The results for adverse events were downgraded to moderate quality because there were fewer events.
Side effect
- From the cardiovascular system: decrease or increase in blood pressure, bradycardia, tachycardia, palpitations, rarely - cardiac arrhythmias (up to ventricular fibrillation), transient ischemic ECG changes, myocardial infarction, coronary artery spasm, Raynaud's syndrome.
- From the gastrointestinal tract: nausea, vomiting, slight increase in the activity of liver transaminases, dysphagia, feeling of discomfort in the abdomen; rarely - ischemic colitis.
- From the nervous system: dizziness, feeling of a rush of blood to the head, weakness, drowsiness, fatigue (usually mild or moderate and transient), convulsive attack. Pain, tingling sensation, warmth, feeling of heaviness, pressure or compression occurring in any part of the body, usually passing quickly, blurred vision, diplopia, nystagmus.
- Allergic reactions in the form of urticaria, rash, erythema, rarely anaphylaxis.
An overdose of sumatriptan can cause sulfhemoglobinemia, a rare condition in which the blood changes from red to green due to the integration of sulfur into the hemoglobin molecule. If you stop using Sumatriptan, the condition changes within a few weeks.
Serious cardiac events, including death, may occur after injection of sumatriptan or the tablets.
Possible side effects
Imitrex may cause serious side effects, including:
- sudden severe abdominal pain;
- diarrhea with or without blood;
- severe chest pain;
- pain in the jaw or shoulder;
- shortness of breath;
- irregular heartbeat;
- seizure (convulsions);
- leg cramps;
- numbness or tingling in the legs or feet;
- burning pain in the legs or feet;
- feeling of coldness in the legs or feet;
- change in the color of the legs or feet;
- hip pain;
- nausea;
- vomit;
- sweating or shaking;
- excitement;
- hallucinations;
- heat;
- muscle stiffness;
- loss of coordination;
- sudden numbness or weakness on one side of the body;
- slurred speech;
- vision difficulties;
- poor balance;
- sudden severe headache.
Seek immediate medical attention if you have any of the symptoms listed above.
The most common side effects of Imitrex include:
- pain or tightness in the chest, throat or jaw;
- pressure in any part of the body;
- numbness or tingling;
- dizziness;
- drowsiness;
- weakness;
- unpleasant taste after using nasal medication;
- pain, burning, numbness, or tingling in your nose or throat after using a nasal medicine;
- runny or stuffy nose after using nasal medication.
Tell your doctor if you have any side effects that bother you or that do not go away.
These are not all possible side effects of Imitrex. Ask your doctor or pharmacist for more information.
Pharmacodynamics
Sumatriptan is a selective agonist of 5-HT1 receptors such as 5-HT1D, 5-HT1B and 5-HT1F, without affecting 5-HT2 - 5-HT7. By activating these receptors in the carotid artery system, it causes their narrowing (arteria basilaris, basilar artery), without affecting cerebral blood flow. Their dilatation and swelling are considered to be the cause of migraine. In addition, it inhibits the activity of the trigeminal nerve.
Pharmacokinetics
It is absorbed quite quickly both intranasally and orally. When taken orally, bioavailability is about 15% due to first-pass metabolism and incomplete absorption. Reaches Cmax after 2.5 hours when taken orally, after intranasal administration after 1.5 hours. Metabolized with the participation of monoamine oxidase, the main metabolites are the indoleacetic analogue of sumatriptan and its glucuronide. The half-life is 2.5 hours. It is excreted mainly by the kidneys with urine - 60% and with feces.
Indications for use
Relief of migraine attacks.
Directions for use and doses
Not used for the prevention of attacks, the maximum effect is when taken at the height of the attack.
Orally - 50-100 mg. The maximum daily dose when taken orally is 300 mg.
Rectally - 25 - 50 mg. The maximum daily dose for rectal administration is 100 mg.
Intranasal - 20 mg (1 dose) in one nostril. Repeated administration is possible after at least 2 hours for intranasal use - 2 doses of 20 mg each.
Subcutaneously - 6 mg. Repeated administration is possible after 1 hour. The maximum daily dose is 12 mg.
Contraindications
- Known hypersensitivity to the drug.
- Hemiplegic, basilar or ophthalmoplegic form of migraine.
- Previous myocardial infarction.
- Arrhythmias.
- IHD, angina pectoris, including Prinzmetal's angina.
- Uncontrolled arterial hypertension.
- Occlusive diseases of peripheral vessels.
- Previous strokes and transient cerebrovascular accidents.
- Epilepsy.
- Severe impairment of liver and/or kidney function.
- Simultaneous use of sumatriptan with ergotamine or its derivatives (including methysergide), as well as simultaneous use of MAO inhibitors and a period of up to 2 weeks after their withdrawal.
- Breastfeeding and pregnancy.
- Elderly age, adolescence (up to 18 years) (safety and effectiveness have not been established).
Special instructions
Not intended for the prevention of migraine, used only when diagnosed, during an attack. Use before an attack or during an aura may not stop the attack. Risks from the cardiovascular system should be taken into account and the possibility of developing stroke and myocardial infarction should be remembered.
A prerequisite is to follow a diet - 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).
Prescribe with caution to drivers and persons engaged in work requiring increased attention. Overdose Symptomatic therapy, observation for 10 hours.
Overdose
Symptomatic therapy, observation for 10 hours.
Interaction with other drugs
- Medicines containing ergot
Preparations containing ergot have been reported to cause prolonged vasospastic reactions. Because these effects may be additive, the use of drugs containing ergotamine or ergot-type drugs (eg, dihydroergotamine or methysergide) and IMITREX injections at 24-hour intervals are contraindicated.
- Monoamine oxidase-A inhibitors
MAO-A inhibitors increase systemic exposure by 2 times. Therefore, the use of IMITREX Injection in patients receiving MAO-A inhibitors is contraindicated.
- Other 5-HT1 agonists
Because their vasospastic effects may be additive, coadministration of IMITREX Injection and other 5-HT1 agonists (eg, triptans) within 24 hours of each other is contraindicated.
- Selective serotonin reuptake inhibitors/serotonin norepinephrine reuptake inhibitors and serotonin syndrome.
Storage
Store in a place protected from light at temperatures from 2° to 30°C.
Approval
In 1991, Glaxo received approval for Sumatriptan, which was the first triptan available. In the United States, it is available only by prescription (and is often limited, without prior authorization, to nine per 30-day period). This requirement for medical use also exists in Australia. However, it can be bought without a prescription in the UK (solely after consultation with a pharmacist and written confirmation that there are no contraindications) and Sweden. Several dosage forms for sumatriptan have been approved, including tablets, injection solution, and nasal inhalers.
In July 2009, the US FDA approved a disposable atomizer with Sumatriptan atomizers. The device delivers a subcutaneous injection of 6 mg sumatriptan without the use of a needle. Needle auto-injectors have previously been available in Europe and North America for several years.
Phase III studies with the iontophoretic transdermal patch (Zelrix/Zecuity) began in July 2008. This patch uses low voltage, controlled by a preprogrammed microchip, to deliver a single dose of sumatriptan through the skin over 30 minutes. Zecuity was approved by the US FDA in January 2013. Sales of Zecuity were discontinued following reports of skin burns and irritation.
Generics
Glaxo's patents on sumatriptan expired in February 2009. At the time, Imitrex sold for about $25 per tablet. On November 6, 2008, Par Pharmaceutical announced that it would immediately begin selling generic versions of sumatriptan injection (sumatriptan succinate injection), 4 and 6 mg starter kits, and 4 and 6 mg prefilled syringe cartridges. In addition, Par plans to release 6 mg vials in early 2009.
Mylan Laboratories Inc., Ranbaxy Laboratories, Sandoz (a subsidiary of Novartis), Dr. Reddy's Laboratories and other companies have received FDA approval for generic versions of sumatriptan tablets in 25, 50 and 100 mg doses since 2009. the drug is generally available in the US and European markets as Glaxo's patent protection has expired in those jurisdictions. Sumatriptan nasal spray is also available generically.
