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Imigran
Imigran - a remedy for migraines, is an selective agonist of serotonin 5HT1 receptors.
Pharmacodynamics
Sumatriptan is a selective agonist of 5HT receptors (1D), without affecting other 5HT receptors. The end data is located mainly inside the cranial-cerebral vessels.
During the experimental tests, it was found that sumatriptan has a selective vasoconstrictive effect on the vessels located inside the carotid artery system, without acting on the blood circulation in the brain. Through the carotid arteries, the blood reaches intra-, as well as extracranial tissues (for example, to the membranes of the brain), the expansion of the vessels of which leads to the appearance of a migraine.
With the help of experimental tests it was possible to additionally reveal the inhibitory properties of the active component relative to the function of the trigeminal nerve. It is through these two mechanisms that anti-migraine action of sumatriptan appears.
The drug effect begins half an hour after oral administration of drugs (in the amount of 100 mg).
Pharmacokinetics
When taken orally, the component is rapidly absorbed, after 45 minutes reaching 70% of the peak level. On average, the maximum plasma index at a dosage of 100 mg is 45 ng / ml. The bioavailability level with internal tablet intake is 14% (in part because of the systemic process of metabolism, and partly due to incomplete absorption).
With plasma protein, the synthesis is weak (14-21%), and the average level of the distribution volume is 17 liters. The average total clearance is about 1160 ml / minute, and in the kidneys the average is about 260 ml / minute.
The clearance outside the kidneys is about 80% of the total, which allows the determination of sumatriptan excretion mainly in the form of decay products. The main one is an indole acetic analogue of the active ingredient. It is excreted in the urine (in it it is defined as a free acid, as well as glucuronide conjugated with the substance) and does not have the activity of 5HT1, as well as 5HT2. Other decay products are not identified.
The pharmacokinetic properties of the administered sumatriptan vary slightly during the migraine attack.
Use of the immigraine during pregnancy
Prescribe to pregnant women is allowed only taking into account the possible help of the mother in relation to the risk of developing negative symptoms in the fetus.
It is known that when n / to the introduction of the active substance, it penetrates into the mother's milk. Reduce the impact on the child can be if within 12 hours after eating drugs do not breastfeed.
Contraindications
Among the contraindications of drugs:
- intolerance of the constituent elements of the medicine;
- a history of myocardial infarction, and in addition spontaneous angina, coronary artery disease, peripheral vascular pathology, or signs that are characteristic of IHD;
- a history of a temporary circulatory disorder in the brain or a stroke;
- severe or moderate degree of elevation of blood pressure or a mild form of uncontrolled increase in blood pressure;
- severe liver failure;
- taking concomitantly with MAO inhibitors - starting the use of Imigran is allowed at least 2 weeks after stopping the intake of inhibitors;
- children and adolescence, as there is no information about the safety and effectiveness of drug use in the category of people treated above.
Side effects of the immigraine
According to clinical trials, such adverse reactions were identified:
- organs of the National Assembly: often a feeling of drowsiness or dizziness, and in addition a sensitivity disorder (including hypoesthesia, as well as paresthesia);
- organs of the CCC: often a transient increase in the level of blood pressure (immediately after the use of the pill), and in addition a rush of blood;
- respiratory organs: dyspnea often occurs;
- digestive system: often in some patients developed vomiting with nausea, although the association with drug use has not yet been identified;
- connective tissue, musculature and skeleton: basically these manifestations are temporary, although they can be intense and affect various parts of the body (among them the throat and sternum) - often there are muscle pains or a feeling of heaviness;
- common disorders: often there are painful sensations, a feeling of tension, contraction, and also of cold or heat (manifestations are usually temporary, although sometimes they are intense and capable of affecting different parts of the body (among them, the throat with the sternum)). Often there is severe fatigue or a feeling of weakness (these manifestations are also temporary and usually have a moderate or mild degree of severity);
- The results of the analyzes: there were only small changes in the indicators of functional liver studies.
Results of postmarketing research:
- immunity: increased sensitivity (from skin reactions to cases of anaphylaxis);
- organs of the National Assembly: the appearance of seizures. In some cases, such symptoms appeared in people with a tendency to convulsions or with the presence in the anamnesis of conditions capable of leading to such attacks; In addition, also the development of dystonia, tremor, nystagmus, or scotoma;
- visual organs: development of diplopia or flicker, deterioration of visual acuity, and also loss of vision (it is usually temporary). But similar disorders can also occur due to the very attack of migraine;
- CAS organs: development of tachycardia, angina pectoris or bradycardia, increased heart rate, rhythm disorder, temporary ischemic changes in ECG parameters, spasms of coronary vessels, lowering of blood pressure, myocardial infarction, Raynaud's syndrome;
- digestive organs: the development of diarrhea or ischemic form of colitis;
- connective tissue, skeleton and musculature: joint pain, cervical sciatica;
- mental disorders: a sense of excitement;
- subcutaneous tissue and skin: the development of hyperhidrosis.
Dosing and administration
It is forbidden to drink tablets as a prophylactic against an attack. It is also forbidden to exceed the recommended dosage.
The best time to take the pill - immediately after the onset of an attack, but the medicine will be effective at any stage of it.
Usually, the drug is prescribed in a dose of 50 mg (the size of the first pill). Sometimes it is permitted to increase the dosage to 2 tablets (100 mg).
If there is no effect, you can not take a new dose during the same migraine attack. The next tablet can be taken only after the onset of a new attack.
In the presence of a reaction to the first dosage, but with the subsequent resumption of migraine manifestations, the 2nd pill is allowed to be used for the next 24 hours, with a minimum interval between doses of 2 hours. In general, a day (within 24 hours) can take no more than 300 mg of the drug.
Take the pill completely, while washing them with water.
Overdose
When oral doses of more than 400 mg, only symptoms of adverse reactions occurred. When developing an overdose, it takes at least 10 hours to observe the patient, while carrying out standard support procedures.
There is no information on the effects of peritoneal dialysis or hemodialysis on the parameters of the active component of the drug.
Interactions with other drugs
There is no information on the interaction of the drug with alcoholic beverages, but also with flunarizine, propranolol, and also pizotifenom.
Limited information is available on combined use with drugs that contain ergotamine or other 5-HT1 receptor / tryptone agonists. In theory, prolonged vasospastic action may develop, as a result of which it is forbidden to combine such drugs. It is not known what the duration should be in the interval between the reception of these drugs - it depends on the type of drugs, as well as their dosages. Since the properties of ergotamine and the agonists of 5-HT1 tryptans / receptors can be enhanced by Imigran, after them a 24-hour interval should be observed before receiving the latter.
In this case, medicines containing ergotamine are forbidden to use for 6 hours after ingestion of Imigran, and agonists of tryptans / receptors 5-HT1 - within 24 hours after using Imigran.
There are single postmarketing mentions that patients developed serotonin intoxication (among manifestations of neuromuscular disorders, changes in the state of the psyche and visceral instability) when the drug is combined with selective inhibitors of reverse serotonin capture. There are also data on the appearance of the aforementioned pathology in the combination of triptans with noradrenaline and inhibitors of reverse serotonin capture.