Rizatriptan benzoate

Chemical name

N,N,-Диметил-5-(1H-1,2,4-триа зол-1-илметил)-1H-индол-3 -этанамина benzoate

Gross

C15-H19-N5.C6-H5-COOH

Characteristics

Solid white crystals or almost white. Soluble in water.

Of drugs

The drugs-protivomigrenoznoe. Yes institute serotoninove 5-NT_1B/1D receptors. Big extended during migraine attack vnutricerepnae receptacles oppressing release cells reduces the transfer of the institution in trigeminalna system. Protivomigrenosny effect is 30 minutes after Priema.v experiments on animals and carcinogenic mutagenogo is not Obnaroujeno.u female rats were the estrus cycle at doses of 100 mg / kg / day (AUC in the dose 225 times greater than the person in the employment maximum recommended daily dose (MRDD), 30 mg). The male rats did not have adverse actions on fertility and reproductive function at doses of 250 mg / kg / Sut.massa body at birth and growth of body mass index from birth to the end of breast-feeding was less to the descendants of rats receiving before and during mating, for the duration of pregnancy and lactation doses of 10 and 100 mg / kg / day (AUC in these doses about 15 and 225 times, respectively, higher than the person in the employment MRDD, with the manifestations of toxicity with the females. When a breeding rats highest, toxic for them dose (250 mg / kg / day or more) increased mortality Potomkov.pri a pregnant rats and krolikam during organogeneza doses of 100 and 50 mg / kg / day, respectively, tertogennogo actions have not been identified. It has the ability to penetrate the placenta in rabbits and Kras.posle intake of a well-absorbed from the digestive tract. bioavailability-45% C_max achieved through 1-1.5 hours Linking protein is 14%. T_1/2 of plasma - 2-3 at Metaboliziruetsa with MAO type A Place predominantly gastrointestinal. Not koumouliruet.

Indications

Migraine (with fascination and without it), mild asthma.

Restrictions on the use of

Pregnancy, breast feeding, age and 18 years of age (the safety and effectiveness of the variables).

Pregnancy and lactation

Perhaps if the effect of therapy outweighs the potential risk to the foetus and the child (adequate and well-controlled studies safety of the pregnant and lactating women did not).

Contraindications

Hypersensitivity, and baziliarnaya gemiplegical migraine, arterial hypertension, ischemic heart disease (stenocardia, myocardial infarction established subclinical disease, etc.), the suspicion of disease, malnutrition koronarnaya, stenocardia Prinzmetala, simultaneous MAO inhibitors.

Side-Effects

From the nervous system and sensory organs : dizziness, headache, drowsiness or insomnia, weakness, fatigue, loss of mental activity, disorientation, anxiety, paresthesia, hyperesthesia, lack Zrenia.so the circulatory system and blood (blood, gemostaz) : enhancing AD heart, Tahikardia.so part of the intestine : dry mouth, nausea, vomiting, diarrhoea, Dispepcia.so the musculoskeletal system : muscle weakness, muscle rigidity, tremor, rigidity, �таксия.Аллергические �ection : hyperemia and itching Koji.prochie : discomfort in the throat, thirst, pain syndrome, including pain in the neck, chest, abdominalnaya pain; collapses, shortness of breath, increased sweating, tides blood to the skin person.

Patient interaction

MAO inhibitors, propranolol increase the concentration in the blood.

Overdosing

Symptoms : dizziness, drowsiness, fear, aetiology, hypertension and other cardiovascular symptoms, vomiting, incontinence Mochi.lechenie : stomach wash, the use of activated carbon, monitoring clinical condition, including ECG for 12 hours

Precautions

Not recommended simultaneous with the other agonists 5-NT_1 receptors or drugs ergotaminovogo stimulants (a range of at least 6900). Treatment can be no earlier than two weeks after receiving MAO inhibitors.

Dosing and Administration

Inside, and 10 mg, with a break of at least two hours with a maximum daily dose of 30 mg. For patients receiving prophylaxis, the initial dose of 5 mg daily to 15 mg.

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