Sumatriptan - instructions for use, dose, side effects, contraindications

Excipients: lactose monohydrate - 92.00 mg; cellulose microcrystalline - 9.00 mg; povidone (polyvinylpyrrolidone low molecular weight) - 3, C0 mg; silicon dioxide colloidal - 1.80 mg; croscarmellose sodium - 1.80 mg; magnesium stearate - 1.80 mg;

film sheath: [hypromellose - 3.00 mg, talc - 1.00 mg, titanium dioxide - 0.55 mg, mafogol 4000 (polyethylene glycol 4000) - 0.45 mg] or [dry mixture for film coating containing hypromellose (60%), talc (20%), titanium dioxide (11%), magnesium 4000 (polyethylene glycol 4000) (9%)] - 5.00 mg.

Dosage of 100 mg

active substance: sumatriptan succinate (in terms of sumatriptan) - 100 mg;

Excipients: lactose monohydrate - 184.00 mg; microcrystalline cellulose - 18.00 mg; povidone (low molecular weight polyvinylpyrrolidone) - 7.2.0 mg; silicon dioxide colloidal - 3.60 mg; croscarmellose sodium - 3.60 mg; magnesium stearate - 3.60 mg;

film sheath: [hypromellose - 6.00 mg, talc - 2.00 mg, titanium dioxide - 1.10 mg, ma tall oil 4000 (polyethylene glycol 4000) - 0.90 mg] or [dry mixture for film coating containing hypromellose (60%), talcum powder (20%), titanium dioxide (11%), macrogol 4000 (polyethylene glycol 4000) (9%)] - 10.00 mg.

Description:Round, biconvex tablets, covered with a film shell of white or almost white color. On the cross section, the nucleus is white or almost white in color.

Pharmacotherapeutic group:Anti-migraine means.

ATX: & nbsp

N.02.C Anti-migraine drugs

Pharmacodynamics:

Mechanism of action

Sumatriptan is a selective agonist of vascular 5-hydroxytryptamine-1 receptors (5-HT1D), does not affect other 5-HT receptor subtypes (5-HT2-5-HT7). Receptors 5-HT1D are located mainly in the cranial blood vessels of the brain, and their stimulation leads to a narrowing of these vessels.

In animals sumatriptan selectively acts on the vasoconstriction of the branches of the carotid artery, without affecting the blood flow in the vessels of the brain. The vascular carotid artery pool supplies extracranial and intracranial tissues (including the meninges), and it is believed that the expansion of these vessels and / or edema of their walls is the main mechanism of migraine in man. In addition, experimental data make it possible to judge that sumatriptan reduces the sensitivity of the trigeminal nerve. Both these effects can underlie the anti-migraine effect of sumatriptan.

The clinical effect is usually observed in 30 minutes after oral intake of 100 mg of the drug.

Although the recommended dose for oral administration is 50 mg, migraine attacks vary in severity in both the patient and in different patients.Doses of 25 mg to 100 mg showed greater efficacy compared with placebo in clinical studies, but a 25 mg dose was statistically significantly less effective than 50 mg and 100 mg.

Sumatriptan has been shown to be effective in treating migraine attacks, including menstrual-associated migraine, that is, a migraine without an aura that occurs between three days before and five days after the onset of menstruation.

Pharmacokinetics:

Attacks migraine, apparently, do not have a significant effect on

pharmacokinetics of sumatriptan taken internally.

Suction

After oral administration sumatriptan quickly absorbed, 70% of the maximum plasma concentration is achieved after 45 minutes.

After oral administration in a dose of 100 mg, the maximum concentration in blood plasma is an average of 54 ng / ml. Bioavailability is 14% due to presystemic metabolism and incomplete absorption.

Distribution

St.ide with plasma proteins - 14-21 %, the total volume of distribution on average is 170 l.

Metabolism

Metabolized by oxidation with the participation of monoamine oxidase (MAO) A with the formation of metabolites, the main one being the indoleacetic analogue of sumatriptan, which does not possess pharmacological activity against 5-HTU and 5-11T2-serotonin receptors.Secondary metabolites of sumatriptan were not detected.

Excretion

The half-life is approximately 2 hours. The main metabolite (indoleacetic analogue of sumatriptan) is excreted by the kidneys in the form of free acid and its glucuronide conjugate.

The clearance is 1160 ml / min; renal clearance - 260 ml / min; non-adrenal clearance - 80% (after oral administration).

Pharmacokinetics in patients of special groups

Patients with impaired renal function

In patients with renal insufficiency, no studies have been performed.

Patients with hepatic impairment In patients with impaired hepatic function, the bioavailability of the drug can be significantly increased by increasing sumatriptan in blood plasma as a result of a decrease in presystem clearance. An assessment was made of the effect of moderate hepatic impairment (class B on the Child-Pugh scale) on the pharmacokinetics of sumatriptan when administered subcutaneously. There were no significant differences in the pharmacokinetics of sumatriptan for subcutaneous administration in patients with moderate impairment of liver function compared to healthy controls in the control group.

Elderly patients

In elderly patients, in experimental studies, no significant differences in the pharmacokinetics of sumatriptan were found in comparison with the pharmacokinetics of the drug in healthy men.

Floor

Differences in the pharmacokinetics of sumatriptan (AUC, FROM_m_Oh, T_m_Oh and T_1|2) men and women are not identified.

Indications:Coping migraine attacks with or without an aura, including episodes of menstrual-associated migraine.

Contraindications:

- hypersensitivity to any of the components of the drug;

- lactose intolerance, lactase deficiency, glucose-galactose malabsorption;

- hemiplegic, basilar and ophthalmoplegic forms of migraine;

- ischemic heart disease (CHD), including angina pectoris (including Prinzmetal angina), myocardial infarction (including history), postinfarction cardiosclerosis, and the presence of symptoms suggesting the presence of IHD;

- occlusive diseases of peripheral vessels;

- stroke or transient impairment of cerebral circulation (including in history);

uncontrolled arterial hypertension;

- simultaneous administration with medications containing ergotamine or its derivatives (including metisergide), or other 5-HT 1 -receptor triptans / agonists;

- simultaneous administration with MAO inhibitors and up to 14 days after the withdrawal of these drugs;

- simultaneous reception with other 5-HT1-serotonin receptor agonists; marked renal or hepatic insufficiency;

- age 18 years or older than 65 years (safety and efficacy of sumatriptan not established).

Carefully:

- controlled arterial hypertension;

- diseases in which absorption, metabolism or excretion of sumatriptan may change (eg, impaired renal or hepatic function);

- Epilepsy (including any conditions with a decrease in the threshold of convulsive alertness);

- hypersensitivity to sulfanilamides (taking sumatriptan can cause allergic reactions, the severity of which varies from skin manifestations to anaphylaxis;

- data on cross-sensitivity are limited, but caution should be exercised when assigning sumatriptan to such patients).

Pregnancy and lactation:

Pregnancy

The use of sumatriptan in pregnancy is possible only if the intended benefit to the mother exceeds the possible risk to the fetus.The data of post-registration observation of more than 1000 women who took sumatriptan during the first trimester of pregnancy. Due to insufficient information, it is premature to make final conclusions about increasing the risk of congenital malformations. The experience of using sumatriptan in the II and III trimesters of pregnancy is limited.

The results of animal studies did not show a direct teratogenic effect of sumatriptan on the fetus or a negative effect on the peri- and postnatal development of an embryo or fetus in rats. However, there is evidence of the effect of sumatriptan on the viability of the embryo and fetus in rabbits when taking large doses of sumatriptan.

Breastfeeding period

It has been shown that after subcutaneous administration sumatriptan excreted in breast milk. Effects on the newborn can be minimized if avoiding breastfeeding for 12 hours after taking the drug.

Dosing and Administration:

A drug Sumatriptan should not be prescribed as a prophylaxis. Do not exceed the recommended dose of the drug Sumatriptan.

It is recommended to start taking the drug Sumatriptan immediately, with the first manifestations of a migraine attack, while the drug Sumatriptan is equally effective at application at any stage of a migraine attack.

The drug is used inside, swallowing the tablet whole and washing down with water. Adults

The recommended dose is 50 mg (1 tablet). Some patients may require a dose of 100 mg.

If, after taking the first dose, a migraine attack is not stopped, the second dose of the drug for cupping of the same a migraine attack should not be prescribed. In such cases, to stop the attack, you can apply paracetamol, acetylsalicylic acid or non-steroidal anti-inflammatory drugs. However, the drug Sumatriptan can be used for cupping subsequent migraine attacks.

If the patient feels better after the first dose of the drug and then the symptoms resume, a second dose can be taken, provided that the interval between doses is at least 2 hours, and no more than 300 mg is taken within a 24-hour period. Sumatriptan can be taken no earlier than 24 hours after taking medications containing ergotamine; and vice versa, preparations containing ergotamia can be used no earlier than 6 hours after taking sumatriptan.

Special patient groups

Children and teenagers (under the age of 18)

Effectiveness of the drug Sumatriptan in this group of patients has not been demonstrated.

Patients of advanced age (over 65 years)

Experience with the drug Sumatriptan in patients over 65 years of age is limited. The pharmacokinetics in patients in this population do not significantly differ from those in younger patients, but until additional clinical data are obtained, the use of sumatriptan in patients older than 65 years is not recommended.

Side effects:

Classification of the incidence of adverse events according to recommendations

World Health Organization (WHO):

very often> 1/10;

often from> 1/100 to <1/10;

infrequently from> 1/100 to <1/100;

rarely from> 1/10000 to <1/1000;

very rarely <1/10000, including individual messages;

the frequency is unknown - it is not possible to establish the frequency of occurrence from the available data.

Impaired nervous system:

often - dizziness, drowsiness, sensitivity disorders, including paresthesia and decreased sensitivity;

frequency is unknown - convulsive seizures (in a number of cases observed in patients with convulsive attacks in the anamnesis or with concomitant conditions,predisposing to the occurrence of seizures; some patients did not have risk factors), tremor, dystopia, nystagmus, scotoma, anxiety.

Disorders from the cardiovascular system:

often - a transient increase in blood pressure (soon after taking the drug), hot flashes;

the frequency is unknown - bradycardia, tachycardia, arrhythmias, signs of transient ischemia on the ECG, coronary vasospasm, angina, myocardial infarction, lowering of arterial pressure, Raynaud's syndrome.

Disturbances from the respiratory system, chest and mediastinal organs:

often - shortness of breath, mild transitory irritation of the mucous membrane or burning sensation

in the nasal cavity or throat, nosebleeds.

Disorders from the gastrointestinal tract:

often - nausea, vomiting (the cause-effect relationship is not proven);

very rarely - ischemic colitis, dysphagia, a feeling of discomfort in the abdomen, diarrhea.

Disturbances from the musculoskeletal and connective tissue:

often a feeling of heaviness (usually transient, can be intense and arise

in any part of the body, including the thorax and throat);

frequency unknown - stiff neck, arthralgia.

Disorders from the side of the organ of vision:

frequency unknown - flickering, diplopia, decreased visual acuity, loss of vision (usually transient); However, visual disturbances can be caused by the actual migraine attack.

Immune system disorders:

frequency is unknown - hypersensitivity reactions, including skin manifestations,

as well as anaphylaxis.

Laboratory indicators:

very rarely - slight deviations in the indicators of "liver" samples.

General disorders:

often, pain, a feeling of cold or heat, a feeling of pressure or constriction (usually transient, can be intense and occur in any part of the body, including the chest and throat), weakness, fatigue (usually transient, mild or moderate expression); frequency is unknown - hyperhidrosis.

Overdose:

Symptoms

When taking sumatriptan inside at a dose of up to 400 mg, there are no other adverse reactions other than those listed above.

Treatment

Gastric lavage; follow the patient's condition for 10 hours and, if necessary, carry out symptomatic therapy. There is no evidence of the effect of hemodialysis or peritoneal dialysis on the concentration of sumatriptan in blood plasma.

Interaction:

No interaction of sumatriptan with propranolol, flunarizine, pisotifen and ethyl alcohol has been observed.

With simultaneous administration with ergotamine, a prolonged vasospasm was noted. There are limited data on the interaction with preparations containing ergotamine or other tryptans / agonists of 5-HT1-serotonin receptors. Theoretically, an increased risk of coronary vasospasm, and the joint use of these drugs is contraindicated. Sumatriptan can be used no earlier than 24 hours after taking medications containing ergotamine or other tryptans / agonists of 5-H1 | -serotonin receptors; and vice versa, preparations containing ergotamine can be used no earlier than 6 hours after taking sumatriptan; other triptans / agonists of 5-HT1-serotonin receptors - not earlier than 24 hours after admission

sumatriptan.

Possible interaction between sumatriptan and MAO inhibitors, their simultaneous use is contraindicated.

There are rare reports of the development of serotonin syndrome (including mental disorders, autonomic lability and neuromuscular disorders) as a result of the concomitant use of selective serotonin reuptake inhibitors (SSRIs) and sumatriptan.Also, the development of serotonin syndrome was reported against the background of the simultaneous administration of triptans with selective serotonin and noradrenaline reuptake inhibitors (SSRIs). In case of their simultaneous application, the patient's condition should be carefully monitored.

Special instructions:

A drug Sumatriptan should be prescribed only if the diagnosis of migraine is not in doubt, and it should be used as soon as possible after the onset of a migraine attack, although it is equally effective when used at any stage of an attack.

Sumatriptan tablets can not be used for prophylactic purposes. As with the use of other anti-migraine drugs, before the appointment of sumatriptan, patients with a newly diagnosed migraine or in patients with an atypically migraine should exclude another neurological pathology. It should be noted that patients with migraine are at increased risk of developing certain cerebrovascular disorders (for example, stroke or transient cerebral circulation disorders).

Stigma in the chest and transient intense pain that spreads to the neck area that occur after taking sumatriptan may be symptoms of coronary heart disease.If there is reason to believe that these symptoms are a manifestation of CHD, it is necessary to conduct an appropriate diagnostic examination.

Sumatriptan should not be given to patients at risk of cardiovascular disease, including those who are malignant smokers or patients receiving nicotine replacement therapy, without a preliminary examination to exclude them (postmenopausal women, men over the age of 40 and patients with risk factors development of IHD).

The examination does not always make it possible to detect heart disease in some patients. In very rare cases, patients who have a history of cardiovascular disease may experience serious adverse cardiovascular reactions.

Patients with controlled arterial hypertension should be administered with caution, since in some cases there has been an increase in arterial pressure and peripheral vascular resistance, as well as in patients with diseases in which absorption, metabolism or excretion of the drug may change (eg, renal dysfunction or liver).In very rare cases, serotonin syndrome (including psychiatric disorder, autonomic lability, and neuromuscular disorders) may develop as a result of the concomitant use of SSRIs and sumatriptan. Also, the development of serotonin syndrome was reported against the background of the simultaneous administration of triptans with SSRIs. In the case of simultaneous prescription with drugs from the SSRI / SSRIs group, the patient's condition should be carefully monitored.

A drug Sumatriptan Caution should be used with caution in patients who may significantly alter absorption, metabolism, or excretion of sumatriptan, for example in patients with impaired renal or hepatic function (class A or B on the Child-Pugh scale).

A drug Sumatriptan should be used with caution in patients with epilepsy, seizures or organic brain damage in the history or having other risk factors for reducing the threshold of convulsive readiness. The concomitant use of other 5-HT1-serotonin receptor triptans / agonists with sumatriptan is not recommended. In patients with hypersensitivity to sulfonamides, taking the drug Sumatriptan can cause allergic reactions, which vary from skin manifestations to anaphylaxis. Data on cross-sensitivity are limited, but caution should be exercised in prescribing the drug to such patients. Undesirable reactions may occur more often during the simultaneous use of triptans and herbal preparations containing Hypericum perforatum (Hypericum perforatum). Abuse of medicines intended to stop migraine attacks is associated with increased headaches in sensitive patients (headache associated with drug abuse). In this case, the possibility of drug cancellation should be considered. Do not exceed the recommended dose of sumatriptan.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 50 mg and 100 mg.

Packaging:

1, 4, 6 or 10 tablets in a contoured cell pack made of a polyvinyl chloride light barrier film and aluminum foil.

2, 4, 6 or 10 tablets in a can of high-density polyethylene.

2 or 4 contour packs with 1 tablet.

1, 2, 3 or 5 contour cell packs of 2 tablets.

1 contour cell pack of 4 tablets.

1 contour cell pack of 6 tablets ,.

1 circuit cell pack of 10 tablets or one jar along with instructions for medical use in a pack of cardboard.

Storage conditions:Store in a dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002635

Date of registration:22.09.2014

The owner of the registration certificate:VERTEKS, AO VERTEKS, AO Russia

Manufacturer: & nbsp

VERTEKS, AO Russia

Information update date: & nbsp04.09.2015

Illustrated instructions

Instructions

Sumatriptan (Sumatriptan)