Trimigren - instructions for use, dosage, side effects, contraindications

Excipients - fat is solid (Witepsol (grades H 15, W 35), supposyr (brands NA 15, NAS 50)) - a sufficient amount to obtain a suppository with a mass of 1.25 g.

Description:Suppositories white or almost white, torpedo-shaped.

Pharmacotherapeutic group:Anti-migraine means.

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Trimigren® (sumatriptan) antimigraine drug for the management of migraine attacks of medium and high intensity. Trimigren® is a means of pathogenetic therapy, eliminates headache and associated nausea and vomiting, phono- and photophobia.

Trimigren® in the form of rectal suppositories has the added advantage of treating migraine in situations where accompanying nausea and vomiting restrict the use and effectiveness of the tablet form of sumatriptan, as well as other anti-migraine drugs.

Sumatriptan is a selective agonist 5-HT₁- serotonin receptors (subtype 5-HT_I_D), does not affect other subtypes of hydroxytryptamine receptors (5HT_2-7).

The mechanism of action of sumatriptan consists in vasoconstriction of intracranial extracerebral vessels, oppression of the activity of peripheral neurons of the trigeminal system with inhibition of the release of mediators of neurogenic inflammation (vasoactive intestinal peptide,substance P, etc.) and blocking the transmission in the nuclei of the trigeminal nerve.

Pharmacokinetics:

With rectal administration of sumatriptan in a dose of 25 mg, the maximum concentration (C_m_Oh) Of 27 ng / ml is achieved after 1.5 h (T_m_Oh), half-life (T_1/2) - 1.8 hours, the area under the curve "concentration-time" (AUC) - 77.8 ng * h / ml. For suppositories of 50 mg, these values are 50.1 ng / ml, 2.5 h, 2.1 h and 172.3 ng * h / ml, respectively. The connection with plasma proteins is 14 - 21%, the apparent volume of distribution is 2.4 l / kg. Sumatriptan metabolized by oxidation with the participation of monoamine oxidases (predominantly isoenzyme A) to form metabolites, the main one being indoleacetic analogue of sumatriptan and its glucuronide. Plasma clearance - 1160 ml / min, renal clearance - 260 ml / min; non-adrenal clearance - 40% (after oral administration). It is excreted by the kidneys, mainly in the form of metabolites - free acid or conjugate with glucuronic acid.

Lack of liver function and mild to moderate renal failure have no significant effect on the pharmacokinetics of sumatriptan.

Indications:

Migraine with aura and without it (relief of seizures).

Trimigren® can only be used with a reliably established diagnosis.

Contraindications:Hypersensitivity to any of the components of the drug; hemiplegia, hemiplegic, basilar or ophthalmoplegic migraine forms (see the "Special instructions" section), ischemic heart disease, myocardial infarction (including in the anamnesis), postinfarction cardiosclerosis, vasospastic angina (Prinzmetal), any arrhythmias, especially tachyarrhythmias, cardiac insufficiency, uncontrolled arterial hypertension, stroke and transient disorders of cerebral circulation (including in the anamnesis), occlusive diseases of peripheral vessels, Raynaud's syndrome; epilepsy, seizures and any conditions with a decrease in the threshold of convulsive readiness; severe hepatic and / or renal insufficiency; age under 18 years old and over 65 years of age (safety and efficacy not established), simultaneous administration of funds containing ergot alkaloids (derivatives of ergotamine, including metisergid), other 5-HT1 serotonin receptor agonists, monoamine oxidase inhibitors (MAO) (see "Interaction with other medicinal products ").

Carefully:Pregnancy and lactation; controlled arterial hypertension, diabetes mellitus, inflammatory diseases,bleeding, swelling of the rectum and anus; smoking, simultaneous use of lithium drugs, serotonin reuptake inhibitors (SSRIs), a known hypersensitivity to sulfonamide preparations (see section "Special instructions").

Pregnancy and lactation:Trimigren® during pregnancy and lactation can be used only as prescribed by the doctor; recommended use with caution. When used during lactation it is not recommended to breast-feed a child within 24 hours after taking the drug.

Dosing and Administration:

Rectally, 1 suppository, if there is a migraine attack.

The optimal single dose of sumatriptan in suppositories is 25 mg. At high

Intensity may require 50 mg.

Despite the fact that Trimigren® eliminates the headache and accompanying phenomena at any stage of the attack, it is recommended to take the drug as early as possible after the onset of the attack.

If the symptoms have decreased or gone and then resumed, you can take a second dose, observing the interval between doses of at least 2 hours and not strictly exceeding the maximum daily dose (during any 24-hour interval).If after the introduction of the first dose of elimination or alleviation of symptoms is not achieved, then again to stop the ongoing attack, Trimigren® should not be taken.

A single dose of Trimigrena® is determined by a physician, depending on the clinical course and intensity of the attack.

Unlike other dosage forms, the maximum dose of sumatriptan in rectal

suppositories should not exceed 100 mg during a 24-hour period.

Important! The total dose of sumatriptan taken during any 24- hour period, for example, if sumatriptan under other trade names in other dosage forms (aerosol, tablets, solution for injection) was administered into the body by any route (nose spray, ingestion, subcutaneous injection).

Side effects:

The incidence of adverse events is classified according to the recommendations of the World Health Organization: very often - more than 10%; often - more than 1 and less than 10%; infrequently - more than 0.1 and less than 1%; rarely - more than 0.01 and less than 0.1%; very rarely - less than 0.01%.

The most characteristic undesirable reactions associated with the treatment with sumatriptan: dizziness, nausea, drowsiness, decreased attention, pain in the chest and neck.Suppositories with sumatriptan are characterized only by drowsiness and local reactions.

From the nervous system: often - dizziness, drowsiness, sensitivity disorders, including paresthesia and decreased sensitivity; very rarely - anxiety, tremor, dystonia, nystagmus, scotoma; seizures were noted in patients who had a history of convulsions and in patients with convulsive readiness due to concomitant diseases.

From the cardiovascular system: often - a transient increase in blood pressure, "hot flashes"; very rarely - bradycardia, tachycardia, palpitations, heart rhythm disturbances, transient ECG changes of the ischemic type, spasm of the coronary vessels, angina pectoris, myocardial infarction, lowering of arterial pressure, Raynaud's syndrome.

From the respiratory system: often - shortness of breath.

From the digestive system: often - nausea, vomiting, which may be the symptoms of migraine; very rarely - dysphagia, a feeling of discomfort in the abdomen, a slight increase in the activity of "liver" transaminases, ischemic colitis, diarrhea.

From the musculoskeletal system: often - myalgia, very rarely - arthralgia, limitation of mobility of the neck.

From the sense organs: very rarely - diplopia, flickering flies before the eyes, reduced visual acuity. Communication with taking the drug is not proven, visual impairment can be associated with a migraine attack.

Allergic reactions: very rarely - from skin reactions (rash, itching, erythema, urticaria) to anaphylaxis.

Local reactions: itching and burning in the anus, more frequent defecation.

Other: often - a feeling of heaviness, squeezing or squeezing, pain, a sensation of tingling, burning, hot or cold in different parts of the body, relatively more often in the chest and throat. These symptoms, irrespective of their intensity, are transient.

Overdose:

There are no data on overdose of suppositories of Trimigren®.

It is known that sumatriptan orally in a dose of more than 400 mg, subcutaneously at a dose of 16 mg and intranasal 40 mg of any side effects other than those listed above does not.

Treatment: symptomatic; monitoring the patient's condition for at least 10 hours, if necessary - standard maintenance therapy. There are no specific antidotes and antagonists.There is no data on the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in the blood.

Interaction:

It is inadmissible simultaneous reception of funds containing ergot alkaloids (ergotamine), MAO inhibitors, other triptans (eletriptan, narrated, zolmitriptan, frevorotriptan, etc.).

Simultaneous use of serotonin reuptake inhibitors, lithium preparations is possible only with strict clinical validity and under medical supervision.

With simultaneous administration with ergotamine, a prolonged vasospasm was noted. In this connection, Trimigren® can be prescribed no earlier than 24 hours after taking medications containing ergotamine and its derivatives, including metisergide; and vice versa, preparations containing ergotamine can be administered no earlier than 24 hours after taking Trimigren®.

Trimigren® can be prescribed no earlier than 2 weeks after the abolition of monoamine oxidase inhibitors.

Admission sumatriptana against the background of preparations of St. John's wort perfumed (Hypericum perforatum) may increase the risk of developing and the severity of unwanted (adverse) drug reactions.

Simultaneous use of sumatriptan (and sumatriptan-containing drugs) and drugs from the SSRI group often causes weakness, hyperreflexia and impaired coordination. Perhaps the development of serotonin syndrome; symptoms: myoclonia, agitation, cramping abdominal pain, hyperpyrexia, increased blood pressure. There is also a risk of pharmacodynamic interaction of sumatriptan with tricyclic antidepressants (non-selective serotonin and noradrenaline reuptake inhibitors).

Interactions with propranolol, flunarizine, pisotifen and ethyl alcohol were not observed.

Special instructions:

When appointing Trimigrena® , as well as any triptans, should be limited to the minimally effective single dose, the frequency of reception no more than 10 days for 1 month, take into account significant drug interactions (see the section "Interaction ...").

Trimigren® can not be used for preventive purposes.

The purpose of the drug is possible only if the diagnosis is not in doubt, with a frequency of seizures at least five per year.

With such forms of migraine, as hemiplegic, basilar, ophthalmoplegic, triptans, including Trimigren®, are contraindicated.In order to prevent misuse of the drug, a description of the characteristic symptoms of these migraine forms is given below. It should be remembered that the diagnosis of migraines with the establishment of its form is capable only of a doctor who has a special qualification. Do not use the following information for self-diagnosis. The hemiplegic form is accompanied by motor and sensory impairments (difficulty in movement, slight weakness, awkwardness in the hand, impaired sensitivity up to paralysis), speech disorder. Basilar migraine is manifested by severe dizziness, disturbance of balance and coordination of movements (ataxia), noise in the ears, blindness to both eyes, pronunciation disorder (dysarthria), numbness, tingling, burning (paresthesia) in the extremities, sometimes short-term (15-20 seconds ) loss of consciousness. It occurs in girls during puberty. For ophthalmoplegic migraine, one-sided ptosis (ovulation of the upper eyelid), double vision (diplopia), dilated pupil on the side of pain, strabismus are characteristic. When prescribed to patients with a previously unidentified migraine or in patients with atypicalmigraine, you must exclude other serious neurological conditions (as with the use of other anti-migraine drugs). It should be borne in mind that in patients with migraine increased risk of cerebrovascular disorders, such as stroke and transient ischemic attack.

Patients with risk factors for coronary heart disease and other cardiovascular pathologies, in particular women in natural or surgical menopause, men over the age of 40, sumatriptan can be prescribed only after a preliminary examination, excluding contraindications from the cardiovascular system. Risk factors for complications from the cardiovascular system are hypercholesterolemia, smoking, obesity, diabetes mellitus, a burdened family history (the onset of heart disease in a father / brother under the age of 55, in a mother / sister under the age of 65). An increased risk of developing cardiac complications is when three or more of the above factors are combined. After applying sumatriptan in any dosage forms, including Trimigren® suppositories rectal, it is possible to develop a side effect - pain and / or a feeling of squeezing in the throat or chest. Such a reaction can last from 30 minutes to 2 hours.If the pain in the chest lasts longer, you must immediately seek medical attention, since prolonged chest pain may be a sign of coronary spasm and ischemia of the heart.

For women taking oral contraceptives, Trimigren ® should only be taken after consultation with a doctor. Special care should be taken by patients with migraine with aura, with a short history of migraine (less than 3 months) and in case of worsening of migraine symptoms.

During the treatment it is necessary to observe a diet, exclude products containing tyramine (chocolate, cocoa, nuts, citrus, beans, tomatoes, celery, cheeses), as well as alcoholic beverages (including dry, especially red, wine, champagne, beer ). When hypersensitivity to sulfonamides, the risk of developing allergic reactions is increased.

If Trimigrene® does not eliminate the headache, then "normal" analgesics may be used.

The abuse of Trimigren ®, as well as other anti-migraine drugs, leads to a chronic, so-called "abusus" headache. Abuzusnye headaches are eliminated by cancellation of the drug.

It is necessary to see a doctor in the following cases:

- If a migraine attack lasts more than 24 hours, as in the case of more than four attacks per month.

- If there are changes in the habitual symptoms of migraine, for example, the intensity of pain increased, the frequency of seizures increased, or any symptoms stop completely, despite taking medications.

- If paroxysmal headaches first appeared at the age of over 50.

- If taking Trimigren® did not eliminate the headache and it took an anesthetic.

Effect on the ability to drive transp. cf. and fur:During the use of the drug, patients should be very careful to drive and engage in other potentially hazardous activities requiring high rates of psychomotor reactions, due to possible drowsiness and visual impairment.

Form release / dosage:

Suppositories rectal 25 mg and 50 mg.

Packaging:

1, 2 or 5 suppositories in a contiguous cell package.

One contour cell pack together with instructions for medical use of the drug is placed in a pack of cardboard.

Storage conditions:Store at a temperature not exceeding 20 ° C. Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LS-002245

Date of registration:20.04.2012

The owner of the registration certificate:NIZHFARM, JSC NIZHFARM, JSC Russia

Manufacturer: & nbsp

NIZHFARM, JSC Russia

Information update date: & nbsp04.09.2015

Illustrated instructions

Instructions

Trimigren® (Trimigren®)