natgillin/translations-raw huggingface dataset:
The risk/ benefit of further treatment with RISPERDAL CONSTA should be assessed if clinically relevant orthostatic hypotension persists.
Če klinično pomembna hipotenzija ne izgine, je pred nadaljnjim zdravljenjem z zdravilom RISPERDAL CONSTA potrebno oceniti razmerje med koristjo in tveganjem.
Tardive dyskinesia/ extrapyramidal symptoms (TD/ EPS)
Tardivna diskinezija/ ekstrapiramidni simptomi (TD/ EPS)
Medicines with dopamine receptor antagonistic properties have been associated with the induction of tardive dyskinesia characterised by rhythmical involuntary movements, predominantly of the tongue and/ or face.
Zdravila z antagonističnim delovanjem na dopaminske receptorje so povezali z nastankom tardivne diskinezije, za katero so značilni nehoteni ritmični gibi, predvsem jezika in/ ali obraza.
Parkinson’ s disease and dementia with Lewy bodies
Parkinsonova bolezen in demenca z Lewyjevimi telesci
Parkinson’ s Disease may worsen with risperidone.
Pri bolnikih s Parkinsonovo boleznijo ali z demenco z Lewyjevimi telesci (DLB) je treba pri predpisovanju antipsihotikov, vključno z zdravilom RISPERDAL CONSTA, pretehtati pričakovane koristi in tveganje zdravljenja saj se Parkinsonova bolezen lahko ob jemanju risperidona poslabša.
Tissue culture studies suggest that cell growth in human breast tumours may be stimulated by prolactin.
24 Na podlagi študij tkivnih kultur sklepajo, da prolaktin lahko vzpodbuja celično rast v človeških tumorjih dojke.
Although no clear association with the administration of antipsychotics has so far been demonstrated in clinical and epidemiological studies, caution is recommended in patients with relevant medical history.
Kljub temu, da v kliničnih in epidemioloških študijah še niso dokazali jasne povezave z dajanjem antipsihotikov, je potrebna previdnost pri bolnikih z relevantno zgodovino bolezni.
RISPERDAL CONSTA should be used with caution in patients with pre- existing hyperprolactinaemia and in patients with possible prolactin-dependent tumours.
Pri bolnikih s predhodno obstoječo hiperprolaktinemijo in bolnikih z verjetnimi, od prolaktina odvisnimi tumorji je pri uporabi zdravila RISPERDAL CONSTA potrebna previdnost.
QT prolongation QT prolongation has very rarely been reported postmarketing.
Podaljšanje QT intervala je bilo zelo redko poročano v obdobju po prihodu zdravila na trg.
24 Seizures
Epileptični napadi
Priapism Priapism may occur with RISPERDAL CONSTA treatment due to its alpha-adrenergic blocking effects.
Zaradi zaviralnega delovanja zdravila RISPERDAL CONSTA na alfa receptorje se lahko pojavi priapizem.
Disruption of the body’ s ability to reduce core body temperature has been attributed to antipsychotic medicines.
Antipsihotiki lahko v telesu motijo center za sposobnost zniževanja telesne temperature.
Appropriate care is advised when prescribing RISPERDAL CONSTA to patients who will be experiencing conditions which may contribute to an elevation in core body temperature, e. g., exercising strenuously, exposure to extreme heat, receiving concomitant treatment with anticholinergic activity, or being subject to dehydration.
Kadar se zdravilo RISPERDAL CONSTA predpisuje bolnikom s stanji, ki lahko prispevajo k zvišanju telesne temperature npr. intenzivna telesna vadba, izpostavljenost močni toploti, sočasno zdravljenje z antiholinergičnimi zdravili ali dehidracija, je potrebna posebna previdnost.
Weight gain
Pridobivanje na telesni masi
Although oral risperidone has been studied, RISPERDAL CONSTA has not been studied in patients with renal or liver insufficiency.
Peroralne oblike zdravila RISPERDAL so preskušali pri bolnikih z ledvično in jetrno okvaro, zdravila RISPERDAL CONSTA pa ne.
RISPERDAL CONSTA should be administered with caution in this group of patients (see section 4.2).
Pri tej skupini bolnikov je potrebno zdravilo RISPERDAL CONSTA uporabljati previdno (glejte poglavje 4. 2).
Administration
Dajanje zdravila
This medicinal product contains less than 1 mmol sodium (23 mg) per dose, i. e., essentially ‘ sodium- free’.
To zdravilo vsebuje manj kot 1 mmol (23 mg) natrija na odmerek, kar pomeni ‘ brez natrija ’.
Interaction studies were performed with oral RISPERDAL.
25 Študije medsebojnega delovanja so se izvajale s peroralnimi oblikami zdravila RISPERDAL.
As with other antipsychotics, caution is advised when prescribing risperidone with medicinal products known to prolong the QT interval, e. g., class Ia antiarrhythmics (e. g., quinidine, dysopiramide, procainamide), class III antiarrhythmics (e. g., amiodarone, sotalol), tricyclic antidepressants (i. e., amitriptyline), tetracyclic antidepressant (i. e., maprotiline), some antihistaminics, other antipsychotics, some antimalarials (i. e., chinice and mefloquine), and with medicines causing electrolyte imbalance (hypokalaemia, hypomagnesiaemia), bradycardia, or those which inhibit the hepatic metabolism of risperidone.
Enako, kor pri ostalih antipsihotikih, je potrebna previdnost pri predpisovanju zdravil, ki podaljšujejo QT interval npr. antiaritmiki skupine Ia (kinidin, dizopiramid, prokainamid) in antiaritmiki skupine III (amiodaron, sotalol), triciklični antidepresivi (amitriptilin), tetraciklični antidepresivi (maprotilin), nekateri antihistaminiki, drugi antipsihotiki, nekatera zdravila za zdravljenje malarije (kininu sorodne učinkovine in meflokin) in zdravila, ki povzročajo motnje v ravnovesju elektrolitov (hipokaliemija, hipomagneziemija), bradikardijo ali zdravili, ki zavirajo presnovo risperidona v jetrih.
25 RISPERDAL CONSTA may antagonise the effect of levodopa and other dopamine agonists.
Zdravilo RISPERDAL CONSTA lahko zavira učinek levodope in drugih dopaminskih agonistov.
If this combination is deemed necessary, particularly in end-stage Parkinson’ s disease, the lowest effective dose of each treatment should be prescribed.
Če je ta kombinacija, posebno v končnem stadiju Parkinsonove bolezni, potrebna je treba predpisati najnižji učinkoviti odmerek vsakega zdravila.
Similar effects may be observed with e. g. rifampicin, phenytoin and phenobarbital which also induce CYP 3A4 hepatic enzyme as well as P-glycoprotein.
Podoben učinek lahko pričakujemo pri rifampicinu, fenitoinu in fenobarbitalu, ki inducirajo CYP 3A4 jetrne encime kot tudi P- glikoprotein.
When carbamazepine or other CYP 3A4 hepatic enzyme/ P-glycoprotein (P-gp) inducers are initiated or discontinued, the physician should re-evaluate the dosing of RISPERDAL CONSTA.
Preden začnemo uporabljati ali ukinemo karbamazepin ali druge induktorje jetrnih encimov CYP 3A4/ P- glikoproteina (P- gp), je treba odmerek zdravila RISPERDAL CONSTA ponovno oceniti.
Verapamil, an inhibitor of CYP 3A4 and P-gp, increases the plasma concentration of risperidone.
Verapamil, zaviralec CYP 3A4 in P- gp, zviša koncentracijo risperidona v plazmi.
Phenothiazines, tricyclic antidepressants, and some beta-blockers may increase the plasma concentrations of risperidone but not those of the active antipsychotic fraction.
Fenotiazini, triciklični antidepresivi in nekateri beta- blokatorji lahko zvišajo plazemsko koncentracijo risperidona, ne pa koncentracije aktivne antipsihotične frakcije.
See section 4.4 regarding increased mortality in elderly patients with dementia concomitantly receiving furosemide.
Glejte poglavje 4. 4, glede povečane smrtnosti pri starejših bolnikih z demenco ob sočasni uporabi furosemida in peroralnih oblik zdravila RISPERDAL.
4.6 Pregnancy and lactation
26 4. 6 Nosečnost in dojenje
Risperidone was not teratogenic in animal studies but other types of reproductive toxicity were seen (see section 5.3).
V študijah na živalih risperidon ni bil teratogen, so se pa pokazali ostali vplivi na sposobnost razmnoževanja (glejte poglavje 5. 3).
In animal studies, risperidone and 9-hydroxy-risperidone are excreted in the milk.
Raziskave na živalih so pokazale, da se risperidon in 9- hidroksi- risperidon izločata v mleko.
It has been demonstrated that risperidone and 9-hydroxy-risperidone are also excreted in human breast milk in small quantities.
Dokazano je bilo, da se risperidon in 9- hidroksi- risperidon v manjših količinah izločata tudi v materino mleko pri človeku.
There are no data available on adverse effects in breast-feeding infants.
Podatkov o neželenih učinkih pri dojenih otrocih ni na voljo.
RISPERDAL CONSTA has minor or moderate influence on the ability to drive and use machines due to potential nervous system and visual effects (see section 4.8).
Zdravilo RISPERDAL CONSTA ima blag ali zmeren vpliv na sposobnost vožnje in upravljanja s stroji zaradi možnega vpliva na živčni sistem in vid (glejte poglavje 4. 8).
Insomnia, anxiety, headache, upper respiratory tract infection, parkinsonism, depression, and akathisia.
Najpogosteje poročani neželeni učinki (pogostnost ≥1/ 10) so bili: nespečnost, tesnoba, glavobol, okužbe zgornjih dihal, parkinsonizem, depresija in akatizija.
The following are all the ADRs that were reported in clinical trials and postmarketing.
Navedene neželene učinke so poročali iz kliničnih preskušanj in post- marketinških izkušenj.
The following terms and frequencies are applied: very common (≥ 1/ 10), common (≥ 1/ 100 to < 1/ 10), uncommon (≥ 1/ 1000 to < 1/ 100), rare (≥ 1/ 10,000 to < 1/ 1,000), very rare (< 1/ 10,000), and not known (cannot be estimated from the available clinical trial data).
Uporabljajo se naslednji izrazi in pogostnosti: zelo pogosti (≥1/ 10); pogosti (≥1/ 100, < 1/ 10); občasni (≥1/ 1. 000, < 1/ 100); redki (≥1/ 10. 000, < 1/ 1. 000); zelo redki (< 1/ 10. 000), neznana (ni mogoče oceniti iz razpoložljivih podatkov).
27 Adverse Drug Reactions by System Organ Class and Frequency Category Investigations Common
27 Neželeni učinki glede na organski sistem in pogostnost Preiskave nenormalni elektrokardiogram, zvišan prolaktin v krvia, zvišana glukoza v Pogosti krvi, zvišanje jetrnih encimov, zvišana koncentracija transaminaz, zvišana gama glutamiltransferaza, povečanje telesne mase, zmanjšanje telesne mase Občasni Srčne bolezni
Electrocardiogram QT prolonged
podaljšan QT interval na elektrokardiogramu
Atrioventricular block, Tachycardia Bundle branch block, Atrial fibrillation, Bradycardia, Sinus bradycardia, Palpitations
atrioventrikularni blok, tahikardija kračni blok, atrijska fibrilacija, bradikardija, sinusna bradikardija, palpitacije
Blood and lymphatic system disorders Common Uncommon Not known
Bolezni krvi in limfatičnega sistema Pogosti Občasni Neznana Bolezni živčevja Zelo pogosti Pogosti
Parkinsonismb, Akathisiab, Headache Dizziness, Sedation, Somnolence, Tremor, Dystoniab, Tardive dyskinesia, Dyskinesiab
anemija trombocitopenija, nevtropenija agranulocitoza parkinsonizemb, akatizijab, glavobol vrtoglavica, sedacija, somnolenca, tremor, distonijab, tardivna diskinezija, diskinezijab
Convulsion, Syncope, Dizziness postural, Hypoaesthesia, Paraesthesia, Lethargy, Hypersomnia
krči, sinkopa, položajna vrtoglavica, hipoestezija, parestezije, letargija, hipersomnija
Common Not known
Pogosti Neznana
Vision blurred, Conjunctivitis Retinal artery occlusion
zamegljen vid, konjunktivitis okluzija retinalne arterije
Ear and labyrinth disorders Common Uncommon
Ušesne bolezni, vključno z motnjami labirinta Pogosti Občasni
Vertigo Ear pain
vertigo bolečine v ušesu
Respiratory, thoracic and mediastinal disorders Common Rare
Bolezni dihal, prsnega koša in mediastinalnega prostora Pogosti Redki Bolezni prebavil
Dyspnoea, Cough, Nasal congestion, Pharyngolaryngeal pain Sleep apnea syndrome
dispneja, kašelj, kongestija nosne sluznice, faringo- laringealna bolečina sindrom apneje v spanju
Vomiting, Diarrhoea, Constipation, Nausea, Abdominal pain, Dyspepsia, Toothache, Dry mouth, Stomach discomfort, Gastritis
bruhanje, driska, zaprtje, slabost, bolečine v trebuhu, dispepsija, bolečine zob, suha usta, nelagodje v želodcu, gastritis
Rare
Redki Bolezni sečil
Intestinal obstruction, Pancreatitis
intestinalna obstrukcija, pankreatitis
Renal and urinary disorders Common
Pogosti Bolezni kože in podkožja
Skin and subcutaneous tissue disorders Common Uncommon
Pogosti Občasni
Rash, Eczema Angioedema, Pruritus, Acne, Alopecia, Dry skin
izpuščaj, ekcem angioedem, srbenje, akne, alopecija, suha koža
Musculoskeletal and connective tissue disorders Common Uncommon Endocrine disorders
Bolezni mišično- skeletnega sistema in vezivnega tkiva Pogosti Občasni
Arthralgia, Back pain, Pain in extremity, Myalgia Muscular weakness, Neck pain, Buttock pain, Musculoskeletal chest pain
artralgija, bolečine v hrbtu, bolečine v okončinah, mialgija mišična šibkost, bolečine v vratu, bolečine v zadnjici, mišično- skeletne bolečine prsnega koša
Metabolism and nutrition disorders Uncommon Very rare Not known
Bolezni endokrinega sistema Redki nepravilno izločanje antidiuretskega hormona Presnovne in prehranske motnje Občasni Zelo redki Neznana
Increased appetite, Decreased appetite Diabetic ketoacidosis Water intoxication
povečan apetit, zmanjšan apetit diabetična ketoacidoza zastrupitev z vodo
Infections and infestations Very common Common
28 Infekcijske in parazitske bolezni Zelo pogosti Pogosti
Upper respiratory tract infection Pneumonia, Influenza, Lower respiratory tract infection, Bronchitis, Urinary tract infection, Ear infection, Sinusitis, Viral infection
okužbe zgornjih dihal pljučnica, gripa, okužbe spodnjih dihal, bronhitis, okužbe urinarnega trakta, ušesne okužbe, vnetje sinusov, virusne infekcije
Uncommon
Občasni Poškodbe in zastrupitve
Cystitis, Gastroenteritis, Infection, Localised infection, Subcutaneous abscess
cistitis, gastroenteritis, okužbe, lokalizirane infekcije, podkožni absces
Common Uncommon
Pogosti Občasni Žilne bolezni
Fall Procedural pain
padci procesualna bolečina
Hypertension, Hypotension Orthostatic hypotension
hipertenzija, hipotenzija ortostatska hipotenzija
General disorders and administration site conditions
Splošne težave in spremembe na mestu aplikacije Pogosti
Pyrexia, Peripheral oedema, Chest pain, Fatigue, Pain, Injection site pain, Asthenia, Influenza like illness
zvišana telesna temperatura, periferni edem, bolečine v prsih, utrujenost, bolečine, bolečine na mestu injiciranja, astenija, gripi podobna bolezen
Feeling abnormal, Chest discomfort, Induration, Injection site induration, Sluggishness, Injection site reaction
nenormalno počutje, nelagodje v prsih, brezčutnost, otrdelost na mestu injiciranja, apatija, reakcija na mestu injiciranja
Immune system disorders
Redki Bolezni imunskega sistema
Uncommon Not known
hipotermija
Hypersensitivity Anaphylactic reaction
Občasni Neznana Bolezni jeter, žolčnika in Redki
Reproductive system and breast disorders
preobčutljivost anafilaktična reakcija žolčevodov zlatenica
Common Uncommon Not known
Motnje reprodukcije in dojk Pogosti Občasni Neznana Psihiatrične motnje
Amenorrhoea, Erectile dysfunction, Galactorrhoea Sexual dysfunction, Gynaecomastia Priapism
amenoreja, erektilna disfunkcija, galaktoreja spolna disfunkcija, ginekomastija priapizem
Psychiatric disorders
Zelo pogosti Pogosti Občasni a
a
depresija, nespečnost, tesnoba agitacija, motnje spanja manija, zmanjšan libido, živčnost
Very common Common Uncommon
Hiperprolaktinemija lahko in galaktoreje. b
Depression, Insomnia, Anxiety Agitation, Sleep disorder Mania, Libido decreased, Nervousness
v nekaterih primerih vodi do ginekomastije, motnje menstruacije, amenoreje
Parkinsonism (salivary hypersecretion, musculoskeletal stiffness, parkinsonism, drooling, cogwheel rigidity, bradykinesia, hypokinesia, masked facies, muscle tightness, akinesia, nuchal rigidity, muscle rigidity, parkinsonian gait, and glabellar reflex abnormal), akathisia (akathisia, restlessness, hyperkinesia, and restless leg syndrome), tremor, dyskinesia (dyskinesia, muscle twitching, choreoathetosis, athetosis, and myoclonus), dystonia.
Lahko se pojavijo ekstrapiramidne motnje: parkinsonizem (povečano izločanje sline, muskuloskeletna togost, parkinsonizem, slinjenje, okorelost po tipu zobatega kolesa, bradikinezija, hipokinezija, obraz maske, mišična napetost, akinezija, okorel vrat, rigidnost mišic, parkinsonska drža in nenormalni glabelarni refleks), akatizija (akatizija, vznemirjenost, hiperkinezija in sindrom nemirnih nog), tremor, diskinezija (diskinezija, trzanje mišic, horeoatetoza, atetoza, in mioklonus), distonija.
Additional Adverse Drug Reactions Reported With Oral RISPERDAL but not With RISPERDAL CONSTA by System Organ Class Investigations Body temperature increased, Eosinophil count increased, White blood cell count decreased, Haemoglobin decreased, Blood creatine phosphokinase increased, Body temperature decreased Infections and Infestations Tonsillitis, Cellulitis, Otitis media, Eye infection, Acarodermatitis, Respiratory tract infection, Onychomycosis, Otitis media chronic Blood and Lymphatic Disorders Granulocytopenia
Neželeni učinki, ki so jih poročali pri uporabi zdravila RISPERDAL v peroralni obliki, ne pa pri uporabi zdravila RISPERDAL CONSTA, razvrščeni po organskih sistemih Preiskave Zvišana telesna temperatura, zvišano število eozinofilcev, znižano število belih krvničk, znižan hemoglobin, zvišana koncentracija kreatin fosfokinaze v krvi, znižana telesna temperatura
Class effects
Učinki pri celotni skupini zdravil
In the 12-week double-blind, placebo-controlled trial, 9% of patients treated with RISPERDAL CONSTA, compared with 6% of patients treated with placebo, experienced a weight gain of ≥ 7% of body weight at endpoint.
V enoletni, odprti študiji z zdravilom RISPERDAL
In the 1-year, open-label study of RISPERDAL CONSTA, changes in body weight in individual patients were generally within ±7% from baseline; 25% of patients had an increase in body weight of ≥ 7%.
30 CONSTA, so bila nihanja telesne mase ±7% od začetne vrednosti; 25% bolnikom se je telesna masa povečala za ≥ 7%.
30 Symptoms
Simptomi
In overdose, QT-prolongation and convulsions have been reported.
Pri prekomernem odmerjanju so poročali o podaljšanju QT- dobe in konvulzijah.
Therefore appropriate supportive measures should be instituted.
Za zdravilo RISPERDAL ni specifičnega antidota, zato moramo uvesti ustrezne podporne ukrepe.
Hypotension and circulatory collapse should be treated with appropriate measures such as intravenous fluids and/ or sympathomimetic agents.
Hipotenzijo in cirkulatorni kolaps moramo zdraviti s primernimi ukrepi, kot so intravenske tekočine in/ ali simpatikomimetiki.
Other antipsychotics, ATC code:
Farmakoterapevtska skupina: drugi antipsihotiki; ATC koda:
It has a high affinity for serotoninergic 5-HT2 and dopaminergic D2 receptors.
Ima visoko afiniteto za serotoninske receptorje 5- HT2 in dopaminske D2 receptorje.
Risperidone binds also to alpha1-adrenergic receptors, and, with lower affinity, to H1-histaminergic and alpha2-adrenergic receptors.
Risperidon se prav tako veže na α1 - adrenergične receptorje in z manjšo afiniteto na histaminske H1 in α 2- adrenergične receptorje.
Clinical efficacy The effectiveness of RISPERDAL CONSTA (25 mg and 50 mg) in the management of the manifestations of psychotic disorders (schizophrenia/ schizoaffective disorder) was established in one 12-week, placebo-controlled trial in adult psychotic inpatients and outpatients who met the DSM-IV criteria for schizophrenia.
Klinična učinkovitost V 12- tedenskem, s placebom kontroliranem preskušanju, v katerem so sodelovali hospitalizirani in ambulantni odrasli bolniki s simptomi psihotične motnje (shizofrenija/ shizoafektivna motnja), ki so ustrezali kriterijem DSM- IV za shizofrenijo, so dokazali učinkovitost zdravila RISPERDAL CONSTA (25 mg in 50 mg) pri obvladovanju manifestacij psihotičnih obolenj.
In a 12-week comparative trial in stable patients with schizophrenia, RISPERDAL CONSTA was shown to be as effective as the oral tablet formulation.
31 12- tedensko primerjalno preskušanje, v katerem so sodelovali stabilni bolniki s shizofrenijo, pa je pokazalo, da je zdravilo RISPERDAL CONSTA enako učinkovito kot peroralne tablete.
The long-term (50 weeks) safety and efficacy of RISPERDAL CONSTA was also evaluated in an open-label trial of stable psychotic inpatients and outpatients who met the DSM-IV criteria for schizophrenia or schizoaffective disorder.
Dolgotrajno varnost in učinkovitost (50 tednov) zdravila RISPERDAL CONSTA so ugotavljali v odprtem preskušanju, v katerem so sodelovali stabilni hospitalizirani in ambulantni bolniki s psihozo, ki so ustrezali kriterijem DSM- IV za shizofrenijo oz. shizoafektivne motnje.
Over time efficacy was maintained with RISPERDAL CONSTA (Figure 1).
Povprečje v celotnem rezultatu PANSS (Positive and negative Syndrome Scale) v času (LOCF- Last Observation Carried Forward) pri bolnikih s shizofrenijo.
31 Figure 1.
90
90 Placebo RIS 25 mg RIS 50 mg
Placebo RIS 25 mg RIS 50 mg
85 80 Mean
80
Base
vrednost
6
6 Teden
Endpt
dogodek
After a single intramuscular injection with RISPERDAL CONSTA, the release profile consists of a small initial release of risperidone (< 1% of the dose), followed by a lag time of 3 weeks.
Profil sproščanja kaže, da se po enkratnem intramuskularnem injiciranju zdravila RISPERDAL CONSTA sprva sprosti majhna količina zdravila (< 1% celotnega odmerka), nato pa sledi tritedensko obdobje, ko se zdravilo ne sprošča.
The main release of risperidone starts from Week 3 onwards, is maintained from 4 to 6 weeks, and subsides by Week 7.
Po intramuskularnem injiciranju se glavno sproščanje zdravila začne šele po treh tednih, traja 4- 6 tednov, s sedmim tednom pa upade.
Oral antipsychotic supplementation should therefore be given during the first 3 weeks of RISPERDAL CONSTA treatment (see section 4.2).
Zato morajo bolniki v prvih treh tednih zdravljenja z zdravilom RISPERDAL CONSTA sočasno jemati še dodatna peroralna antipsihotična zdravila (glejte poglavje 4. 2).
Therapeutic plasma concentrations remain until 4 to 6 weeks after the last RISPERDAL CONSTA injection.
Terapevtske koncentracije se v plazmi ohranjajo še 4- 6 tednov po zadnjem injiciranju zdravila RISPERDAL CONSTA.
After repeated intramuscular injections with 25 or 50 mg RISPERDAL CONSTA every two weeks, median trough and peak plasma concentrations of the active antipsychotic fraction fluctuated between 9.9-19.2 ng/ ml and 17.9-45.5 ng/ ml respectively.
Po večkratnih intramuskularnih injiciranjih 25 ali 50 mg zdravila RISPERDAL CONSTA vsaka dva tedna, so srednje najnižje koncentracije aktivne antipsihotične frakcije v plazmi nihale med 9, 9 in 19, 2 ng/ ml, najvišje pa med 17, 9- 45, 5 ng/ ml.
No accumulation of risperidone was observed during long term use (12 months) in patients who were injected with 25– 50 mg every two weeks.
Pri bolnikih, ki so jim dalj časa (12 mesecev) vsaka dva tedna injicirali 25– 50 mg odmerek, kopičenja risperidona niso opazili.
Distribution Risperidone is rapidly distributed.
Distribucija Risperidon se hitro porazdeli.
The volume of distribution is 1-2 l/ kg.
Volumen porazdelitve je 1- 2 l/ kg.
In plasma, risperidone is bound to albumin and alpha-1-acid glycoprotein.
V plazmi se risperidon veže na albumin in α1- kisli glikoprotein.
The plasma protein binding of risperidone is 90%; that of the active metabolite 9-hydroxy-risperidone is 77%.
Na plazemske beljakovine se veže 90% risperidona in 77% 9- hidroksi- risperidona.
Biotransformation and elimination Risperidone is metabolised by CYP 2D6 to 9-hydroxy-risperidone, which has a similar pharmacological activity as risperidone.
32 Citokrom CYP 2D6 presnovi risperidon v 9- hidroksi- risperidon, ki ima podobno farmakološko delovanje kot risperidon.
Risperidone plus 9-hydroxy-risperidone form the active antipsychotic fraction.
Risperidon skupaj z 9- hidroksi- risperidonom tvori aktivno antipsihotično frakcijo.
Extensive CYP 2D6 metabolisers convert risperidone rapidly into 9-hydroxy-risperidone, whereas poor CYP 2D6 metabolisers convert it much more slowly.
Ljudje z dobro presnovo CYP 2D6 hitro pretvorijo risperidon v 9- hidroksi- risperidon, medtem ko ga ljudje s slabo presnovo CYP 2D6 pretvorijo veliko počasneje.