Risperidone

Chemical name

3-[2-[4-(6-Фтор-1,2-бензизок сазол-3-ил)пиперидино]��тил]-6,7,8,9-тетрагидро-2- метил-4Н-пиридо[1,2-a]пир имидин-4-он

Gross

C23-H27-F-N4-O2

Characteristics

Derived бензизоксазола. White with brown Judean powder nerastvorim almost in the water, easily soluble in metilenhloride, methanol, and 0.1 g. hydrochloric acid.

Of drugs

Drugs, the neuroleptic, antipsihoticescoe. Yes blocks (high affinnostew) 5-ht_2-serotoninergicakie, D_2-dofaminergicakie, alfa_1-adrenergicakie, to a lesser extent альфа_2-адренергическ��е and gistaminove H_1-retseptora in the CNS. And weak аффинностью to 5-НТ_1А-, 5-НТ_1С-, 5-НТ_1D-серотонинергическим, D_1-дофаминергическим receptors and галоперидол-чувствит��льным Binding sites sigma, small affinnostew to 5-NT_1V- and 5-nt_3-retseptoram. It has the ability to interact with and m-holinergicakimi beta_1-, бета_2-адренергически��и �ецепторами.Оказывает �ntipsihoticescoe, sedative, and protivorvotnoe gipotermicescoe effect. Antipsihoticeski effect of the blockade was D_2-dofaminergicakih receptors mezolimbicescoy and mezokorticalna systems. Sedative effect is a consequence of the blockade adrenoretseptorov retikuliarna formations barrel brain protivorvotnoe-blockade D_2-dofaminergicakih receptors trigger a vomitoxin point gipotermicescoe-blockade dofamine receptors hypothalamus. Suppress delirium, hallucinations, reduces fear weakens aggressiveness. To a lesser extent than classical neiroleptiki, oppressing motor activity produces katalepshiyu and less triggering extrapiramidale symptoms. Can lead giperprolaktinemia, gipersecretia exists. Changes of sleep, increases medlennovolnova deep sleep (antiserotoninovoe effect). Withholding alfa-adrainoretseptora is dozozawisimuu hypotension and tachycardia fence. And proaritmogennym potential effect because lengthens the QT interval. There is evidence reducing or suppressing risperidonom saliva glands, thus contributing to the development of caries, periodontal diseases and candidiasis of the oral cavity; But some patients experienced Gipersalivacia.posle intake of rapidly and completely absorbed, the speed and completeness of removals do not depend on the meals. Relative bioavailability to the reception tablets compared to the solution, 94%, and absolute bioavailability when administered by 70%. C_max achieved in 1-2 hours Quickly and well distributed in the body. The distribution in a steady state of 1-2 l / kg Extensive metabolised in the liver, with the participation of enzymes zitohroma IID6 R450. The way biotransformation gidrauxilirovnie - with the formation of the active metabolita 9-гидрокси-рисперидон�� (on the spectrum and potency, and safety comparable to risperidonom). Another way biotransformation with minimum value N-dealkilirovanie. The gidrauxilirovania risperidona genetically determined (up to 6-8% of them white, and very few members of the Asian race is either lack of or very low metaboliziruta activity). Therefore, in patients with a high level of metabolism plasma concentration risperidona below, and 9-гидрокси-рисперидон�� - above (S_max risperidona achieved after 3 h, 9 -гидрокси-рисперидона - within 17 hours), compared with those who are characterized by a low ekstensivnostthew biotransformation. However, the status of metabolic phenotype has little clinical importance since major metabolite has specific activity. Linking plasma protein is 88% (risperidon), and 77% (9-гидрокси-рисперидон ). For high and low metabolism T_1/2 and risperidona 9-гидрокси-рисперидон�� are respectively 3 and 21 h, 20 and 30 hours Stable risperidona concentration achieved within 1 or 5 days in the face of high and low speed biotransformation respectively. The extensive metabolizantov stable concentration 9-гидрокси-рисперидон�� registered through 5-6 days. Risperidon and 9-gidroksi-risperidon a pharmacologically active leadership, a stable concentration is achieved through 5-6 days, and T_1/2 is 20 hours Report mostly kidneys (70%) and faeces (15%). If any of kidney average

Indications

Schizophrenia (acute or chronic) and other psychotic state with a predominance of productive (delirium, hallucinations, aggressiveness), negative (prituplenny passion, emotional and social otreshennosti, the scarcity of speech), or affective (depression disturbing) syndrome; Behavioral disorders in the face of dementia (regardless of the symptoms of aggressiveness, violations or Psychotic symptoms) or retardation or reduced level of intelligence (with dominance destructive behaviour); obsession with bipolar disorders (secondary treatment).

Restrictions on the use of

Heart failure, heart attack, AV blockade and other violations conductivity, the cerebral circulation and / or liver and kidney, breast cancer, gipovolemia, Parkinson's disease, epilepsy, pregnancy, breast-feeding, age and 15 years of age (no experience).

Pregnancy and lactation

During pregnancy is possible if the intended benefits to the mother outweighs the potential risk to the fetus. At the time of treatment should abandon breastfeeding.

Contraindications

Гиперчувствительност ь.

Side-Effects

From the nervous system and sensory organs : sleeping, including insomnia or drowsiness, anxiety, fatigue, the attention, concern, anxiety, headache, dizziness, ekstrapiramidnye disorders (rigidity, hypokinesia, gipersalivacia, akatizia, the acute distonia) later diskinesia, neirolepticeski malignant syndrome, the moisture, apnoea seizures, stroke (at the prone patients older), the ambiguity of Zrenia.so the circulatory system and blood (blood, gemostaz) : ortostatical gipotenzia, reflected tachycardia, arterial hypertension, and the stoichiometric тромбопения, тромбоцитопеническая пурпура.Со part of the intestine : nausea, vomiting, diarrhoea phenomenon pain in the abdomen, constipation, increased liver трансаминаз.Со the urogenital system : дисменорея, аменорея, impotence, the erection and ejaculate, аноргазмия, reduced libido, приапизм, полиурия, urinary, отеки.Аллергические reactions : skin rash, ангионевротический отек.Прочие : rhinitis, галакторея, гинекомастия, increased body mass index, gipervolemia (due polidipsii syndrome or inadequate secreta ADU), giperglikemia (for the diabetes).

Patient interaction

Decreases effect of levodopa and dopamine antagonists. Fenotiazina, Tricyclic antidepressants, fluoxetin, beta-adrenoblokatora may strengthen concentration risperidona plasma. Together with the application carbamazepinom, other inductorami liver enzymes (including PP, metabolizirutmisa involving enzymes zitohroma R450) reduced the concentration of active antipsihoticescoy fraction (risperidon and active metabolite) in plasma (a correction dose in the event of the lifting of PP). With long-term use increases carbamazepina risperidona down in the long admission clozapina will diminish. Benzodiazepines, alcohol and means of a person's central nervous system, increasing sedative effect antagonists dofamine receptors increase the risk of developing psoriasis later. Together admission antigipertenziveh funds may increase gipotenzivnogo risperidona effect.

Overdosing

Symptoms : strengthening of the sedative, drowsiness, tachycardia, arterial gipotenzia, ekstrapiramidnye disorders extension interval Qt.lechenie : washing stomach reception activated charcoal, laxatives funds, the maintenance of vehicles respiratory tract, ECG monitor, symptomatic and supportive therapy, continuous medical monitoring. When extrapiramidale symptoms Introduction antiholinergicakih funds.

Precautions

In the late psoriasis should consider lifting risperidona, and with neirolepticski malignant syndrome (hyperthermia, muscle rigidity, violation of consciousness raising CPK) to stop treatment. It should not be used in conjunction with the drivers of vehicles and people whose work involves the higher concentration and requires speed motor reactions. During the therapy should be avoided reception alcohol. At the same time as the treatment risperidonom necessary for the pre-lift antipsihoticalkie other means. Be wary combined with other means influencing the central nervous system. During treatment advised to refrain from over - at the possibility of an increase in body mass index.

Dosing and Administration

Inside, in 1-2 reception. Primary and optimal dose : with schizophrenia and bipolar disorder-2 mg / day and 2 mg / day, respectively, and disorders of the 0.25 mg and 0.5 mg twice a day in elderly patients and in the face of the liver and kidney of 0.5 mg and 1 mg twice a day, respectively.

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