natgillin/translations-raw huggingface dataset:
Reducing the dose of levodopa (see 4.2) may often mitigate these adverse reactions.
Zmanjšanje odmerka levodope (glejte 4. 2) lahko velikokrat ublaži neželene učinke.
In clinical trials, diarrhoea developed in 16% and 18% of patients receiving Tasmar 100 mg tid and 200 mg tid respectively, compared to 8% of patients receiving placebo.
Diareja: v kliničnih preskušanjih se je diareja pojavila pri 16% bolnikov, ki so prejemali 100 mg trikrat na dan, in pri 18%, ki so prejemali 200 mg trikrat na dan, v primerjavi z 8% bolnikov, ki so prejemali placebo.
Diarrhoea led to withdrawal of 5% and 6% of patients receiving Tasmar 100 mg tid and 200 mg tid respectively, compared to 1% of patients receiving placebo.
Diareja je bila vzrok ukinitvi zdravila Tasmar pri 5% bolnikov, ki so jemali zdravilo Tasmar 100 mg trikrat na dan, in 6% bolnikov z odmerjanjem 200 mg trikrat na dan v primerjavi z 1% bolnikov, ki so prejemali placebo.
Due to the interaction between high dose benserazide and tolcapone (resulting in increased levels of benserazide), the prescriber should, until more experience has been gained, be observant of dose-related adverse events (see 4.5).
Interakcija z benserazidom: zaradi medsebojnega delovanja med velikimi odmerki benserazida in tolkapona (ki se kažejo v povišanih vrednostih benserazida), mora biti predpisovalec, preden dobi več izkušenj, pozoren na od odmerka odvisne neželene učinke (glejte 4. 5).
Tasmar should not be given in conjunction with non-selective monoamine oxidase (MAO) inhibitors (e. g. phenelzine and tranylcypromine).
Zaviralci MAO- A: zdravilo Tasmar ne smemo jemati skupaj z neselektivnimi zaviralci monoaminooksidaze (MAO), npr. fenelzinom ali tranilciprominom.
The combination of MAO-A and MAO-B inhibitors is equivalent to non-selective MAO-inhibition, therefore they should not both be given concomitantly with Tasmar and levodopa preparations (see also 4.5).
Kombinacije zaviralcev MAO- A in MAO- B se skupaj z zdravilom Tasmar in pripravki levodope ne sme jemati, saj je kombinacija enakovredna neselektivnemu zaviranju MAO (glejte tudi 4. 5).
Selective MAO-B inhibitors should not be used at higher than recommended doses (e. g. selegiline 10 mg/ day) when co- administered with Tasmar.
Selektivnih zaviralcev MAO- B se ne sme uporabljati v odmerkih, večjih od priporočenih (npr. selegilin 10 mg/ dan), kadar se jemljejo skupaj z zdravilom Tasmar.
Since clinical information is limited regarding the combination of warfarin and tolcapone, coagulation parameters should be monitored when these drugs are co-administered.
Varfarin: klinične informacije o kombinaciji varfarina in tolkapona so omejene, zato je treba ob sočasnem dajanju teh dveh zdravil spremljati koagulacijske parametre.
Each tablet contains 7.5 mg lactose; this quantity is probably not sufficient to induce symptoms of lactose intolerance.
Intoleranca za laktozo: vsaka tableta vsebuje 7, 5 mg laktoze, ta količina pa verjetno ni zadostna, da bi sprožila simptome laktozne intolerance.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose- galactose malabsorption should not take this medicine.
Bolniki z redko dedno obliko galaktozne intolerance, pomanjkanjem Lapp laktaze ali malabsorpcijo glukoze- galaktoze, tega zdravila ne smejo jemati.
Patients with severe renal impairment (creatinine clearance < 30 ml/ min) should be treated with caution.
Posebne skupine bolnikov: bolnike s hudo ledvično okvaro (očistek kreatinina < 30 ml/ min) je treba zdraviti s previdnostjo.
No information on the tolerability of tolcapone in these populations is available (see 5.2).
Ni podatkov o prenašanju tolkapona pri teh skupinah bolnikov (glejte 5. 2).
Patients who have experienced somnolence and/ or an episode of sudden sleep onset must refrain from driving or operating machines.
Bolniki, ki so občutili zaspanost in/ ali doživeli obdobje nenadnega uspavanja morajo opustiti vožnjo ali upravljanje s stroji.
Furthermore a reduction of levodopa dosage or termination of therapy may be considered.
Nadalje je potrebno razmisliti o zmanjšanju odmerka levodope ali prekinitvi zdravljenja.
Although tolcapone is highly protein bound, in vitro studies have shown that tolcapone did not displace warfarin, tolbutamide, digitoxin and phenytoin from their binding sites at therapeutic concentrations.
Vezava na proteine: čeprav se tolkapon v veliki meri veže na proteine, so in vitro študije pokazale, da pri terapevtskih koncentracijah ne spodriva varfarina, tolbutamida, digitoksina in fenitoina iz njihovih vezalnih mest.
5 Catechols and other drugs metabolised by catechol-O-methyltransferase (COMT):
5 Kateholi in druga zdravila, ki se presnavljajo s katehol- O- metiltransferazo (COMT): tolkapon lahko vpliva na farmakokinetiko učinkovin, ki se presnavljajo s COMT.
Tolcapone may influence the pharmacokinetics of drugs metabolised by COMT.
Na farmakokinetiko COMT substrata karbidope učinkov niso opazili.
The plasma concentrations of benserazide observed after co-administration of tolcapone and benserazide-25 mg/ levodopa were still within the range of values observed with levodopa/ benserazide alone.
Plazemske koncentracije benserazida so bile po sočasnem dajanju tolkapona in 25 mg benserazida z levodopo še vedno v mejah vrednosti, opaženih po samostojnem dajanju kombinacije levodopa/ benserazid.
On the other hand, after co-administration of tolcapone and benserazide-50 mg/ levodopa the benserazide plasma concentrations could be increased above the levels usually observed with levodopa/ benserazide alone.
Po drugi strani pa lahko po sočasnem dajanju tolkapona in 50 mg benserazida z levodopo plazemske koncentracije benserazida narastejo prek običajnih ravni, opaženih po dajanju kombinacije levodopa/ benserazid.
The effect of tolcapone on the pharmacokinetics of other drugs metabolised by COMT such as α -methyldopa, dobutamine, apomorphine, adrenaline and isoprenaline have not been evaluated.
Učinek tolkapona na farmakokinetiko drugih zdravil, ki se presnavljajo s COMT, kot je α- metildopa, dobutamid, apomorfin, adrenalin in izoprenalin, ni bil ocenjen.
The prescriber should be observant of adverse effects caused by putative increased plasma levels of these drugs when combined with Tasmar.
Predpisovalec mora biti pozoren na neželene učinke, povzročene z domnevno zvišanimi plazemskimi ravnimi teh učinkovin, kadar se kombinirajo z zdravilom Tasmar.
Due to its affinity for cytochrome CYP2C9 in vitro, tolcapone may interfere with drugs whose clearance is dependent on this metabolic pathway, such as tolbutamide and warfarin.
Učinek tolkapona na presnavljanje drugih zdravil: zaradi in vitro afinitete tolkapona za citokrom CYP2C9, lahko med tolkaponom in zdravili, katerih očistek je odvisen od te presnovne poti, kot sta tolbutamid in varfarin, pride do medsebojnega delovanja.
Tolcapone did not change the pharmacokinetics of desipramine, even though both drugs share glucuronidation as their main metabolic pathway.
Tolkapon ni spremenil farmakokinetike dezipramina, čeprav se obe zdravili presnavljata z glukuronidacijo kot glavno presnovno potjo.
Since tolcapone interferes with the metabolism of catecholamines, interactions with other drugs affecting catecholamine levels are theoretically possible.
Zdravila, ki povišajo kateholamine: ker tolkapon vpliva na presnovo kateholaminov, so interakcije z ostalimi zdravili, ki vplivajo na kateholamine, teoretično možne.
Tolcapone did not influence the effect of ephedrine, an indirect sympathomimetic, on hemodynamic parameters or plasma catecholamine levels, either at rest or during exercise.
Tolkapon ni vplival na učinek efedrina, indirektnega simpatomimetika, na hemodinamske parametre ali ravni kateholaminov v plazmi tako med počitkom kot aktivnostjo.
Since tolcapone did not alter the tolerability of ephedrine, these drugs can be co-administered.
Ker tolkapon ni spremenil prenašanja efedrina, se lahko ti dve zdravili dajeta skupaj.
When Tasmar was given together with levodopa/ carbidopa and desipramine, there was no significant change in blood pressure, pulse rate and plasma concentrations of desipramine.
Ko so zdravilo Tasmar dajali skupaj z levodopo/ karbidopo in dezipraminom, ni bilo pomembnih sprememb v krvnem tlaku, srčni frekvenci in plazemskih koncentracijah dezipramina.
Overall, the frequency of adverse events increased slightly.
Skupno se je pogostnost neželenih učinkov rahlo povečala.
These adverse events were predictable based on the known adverse reactions to each of the three drugs individually.
Te neželene učinke je bilo mogoče napovedati na osnovi znanih neželenih reakcij vsakega od treh zdravil posamezno.
Therefore, caution should be exercised when potent noradrenaline uptake inhibitors such as desipramine, maprotiline, or venlafaxine are administered to Parkinson’ s disease patients being treated with Tasmar and levodopa preparations.
Kadar močne zaviralce ponovnega privzema noradrenalina, kot so dezipramin, maprotilin ali venlafaksin, dajemo bolnikom s Parkinsonovo boleznijo, zdravljenim z zdravilom Tasmar in pripravki levodope, je potrebna previdnost.
In clinical trials, patients receiving Tasmar/ levodopa preparations reported a similar adverse event profile independent of whether or not they were also concomitantly administered selegiline (a MAO-B inhibitor).
V kliničnih preskušanjih so bolniki, ki so prejemali zdravilo Tasmar in pripravke z levodopo, poročali o podobnem profilu neželenih učinkov neodvisno od tega, ali so sočasno jemali selegilin (zaviralec MAO- B).
In rats and rabbits, embryo-foetal toxicity was observed after tolcapone administration (see 5.3).
Nosečnost: toksični vpliv na zarodek ali plod je bil opažen po dajanju tolkapona pri podganah in zajcih (glejte 5. 3).
There are no adequate data from the use of tolcapone in pregnant women.
Ni primernih podatkov o uporabi tolkapona pri nosečnicah.
Therefore, Tasmar should be used during pregnancy only if the potential benefit justifies the potential risk to the foetus.
Zdravilo Tasmar naj se zato v nosečnosti uporablja le, če pričakovana korist upravičuje možno tveganje za plod.
The safety of tolcapone in infants is unknown; therefore, women should not breast-feed during treatment with Tasmar.
Dojenje: tolkapon se je v študijah na živalih izločal v materino mleko.
6 4.7 Effects on ability to drive and use machines
6 Varnost tolkapona za dojenčke ni znana; zato naj ženske med zdravljenjem z zdravilom Tasmar ne dojijo.
No studies on the effects of Tasmar on the ability to drive and use machines have been performed.
4. 7 Vpliv na sposobnost vožnje in upravljanja s stroji
There is no evidence from clinical studies that Tasmar adversely influences a patient’ s ability to drive and use machines.
Iz kliničnih študij ni dokazov, da bi zdravilo Tasmar negativno vplivalo na bolnikovo sposobnost vožnje in upravljanja s stroji.
However patients should be advised that their ability to drive and operate machines may be compromised due to their Parkinson’ s disease symptoms.
Vseeno je treba bolnikom pojasniti, da je lahko njihova sposobnost vožnje in upravljanja s stroji zaradi simptomov Parkinsonove bolezni zmanjšana.
Patients being treated with Levodopa and presenting with somnolence and/ or sudden sleep episodes must be informed to refrain from driving or engaging in activities where impaired alertness may put themselves or others at risk of serious injury or death (e. g. operating machines) until such recurrent episodes and somnolence have resolved (see also Section 4.4)
Bolnike, ki se zdravijo z levodopo in so občutili zaspanost in/ ali doživeli obdobja nenadnega uspavanja moramo obvestiti, da opustijo vožnjo ali vključevanje v dejavnosti, kjer bi zaradi zmanjšane pozornosti sebe ali druge izpostavili tveganju za resne poškodbe ali smrt (npr. upravljanje strojev), dokler taka ponavljajoča se obdobja in zaspanost ne minejo (glejte tudi poglavje 4. 4).
The most commonly observed adverse events associated with the use of Tasmar, occurring more frequently than in placebo-treated patients are listed in the table below.
Najpogosteje opaženi neželeni učinki, povezani z uporabo zdravila Tasmar, ki so se pojavili pogosteje kot pri s placebom zdravljenih bolnikih, so našteti v spodnji preglednici.
However, Tasmar, as a COMT inhibitor, is known to increase the bioavailability of the co-adminstered levodopa.
Zdravilo Tasmar, kot COMT zaviralec, zviša biološko uporabnost sočasno dajane levodope.
The only adverse event commonly leading to discontinuation of Tasmar in clinical trials was diarrhoea (see 4.4).
Edini neželeni učinek, ki je pogosto vodil k prekinitvi jemanja zdravila Tasmar v kliničnih preskušanjih, je bila diareja (glejte 4. 4).
Increases to more than three times the upper limit of normal (ULN) in alanine aminotransferase (ALT) occurred in 1% of patients receiving Tasmar 100 mg three times daily, and 3% of patients at 200 mg three times daily.
Povišanje alanin- aminotransferaze (ALT) do več kot trikratne zgornje referenčne vrednosti, se je pojavilo pri 1% bolnikov, ki so prejemali zdravilo Tasmar 100 mg trikrat na dan in pri 3% bolnikov, ki so prejemali zdravilo Tasmar 200 mg trikrat na dan.
Increases were approximately two times more likely in females.
Povišanja so bila dvakrat verjetnejša pri ženskah.
The increases usually appeared within 6 to 12 weeks of starting treatment, and were not associated with any clinical signs or symptoms.
Navadno so se pojavila med 6 in 12 tednom zdravljenja, in niso bila povezana z nobenimi kliničnimi znaki ali simptomi.
Rare cases of severe hepatocellular injury resulting in death have been reported during marketed use (see 4.4).
Redki primeri hude hepatocelularne poškodbe s smrtnim izidom so bili opisani v času trženja zdravila (glejte 4. 4).
Isolated cases of patients with symptoms suggestive of Neuroleptic Malignant Syndrome Symptom Complex (see 4.4) have been reported following reduction or discontinuation of Tasmar and following introduction of Tasmar when this was accompanied by a significant reduction in other concomitant dopaminergic medications.
Opisani so bili posamezni primeri bolnikov s simptomi, ki so nakazovali na maligni nevroleptični sindrom z vrsto simptomov (glejte 4. 4), nastalimi po zmanjšanju odmerka ali prekinitvi zdravila Tasmar, in po uvedbi zdravila Tasmar, kadar so obenem bolniku precej zmanjšali odmerke ostalih sočasno prejetih dopaminergikov.
In addition, rhabdomyolysis, secondary to NMS or severe dyskinesia, has been observed.
Poleg tega je bila opažena rabdomioliza, pridružena NMS ali hudi diskineziji.
Tolcapone and its metabolites are yellow and can cause a harmless intensification in the colour of the patient’ s urine.
Razbarvanje urina: tolkapon in njegovi presnovki so rumeni in lahko povzročijo neškodljivo ojačitev barve bolnikovega urina.
Experience with Tasmar obtained in parallel placebo-controlled randomised studies in patients with Parkinson’ s disease is shown in the following table, which lists adverse reactions with a potential relationship to Tasmar.
Izkušnje z zdravilom Tasmar, dobljene v vzporednih, s placebom kontroliranih študijah pri bolnikih s Parkinsonovo boleznijo, so prikazane v naslednji preglednici, ki navaja neželene reakcije z možno povezavo z zdravilom Tasmar.
Summary of potentially Tasmar-related adverse reactions, with crude incidence rates for the phase III placebo-controlled studies:
Povzetek neželenih reakcij, potencialno povezanih z zdravilom Tasmar, z grobimi deleži pojavnosti za fazo III s placebom kontroliranih študij:
Incidence*
Pogostnost *
Tolcapone N=296 (%)
Tolkapon N=296 (%)
Tolcapone N=298 (%)
Tolkapon N=298 (%)
Gastrointestinal disorders Very common Nausea Anorexia Diarrhoea Common Vomiting Constipation Xerostomia
Bolezni prebavil
17.8 12.8 7.7 3.7 5.0 2.3
Zelo pogosto
30.4 18.9 15.5 8.4 6.4 4.7
Slabost Anoreksija Driska
34.9 22.8 18.1 9.7 8.4 6.4
17, 8 12, 8 7, 7
Abdominal pain 2.7 Dyspepsia 1.7
30, 4 18, 9 15, 5
4.7 4.1
34, 9 22, 8 18, 1
5.7 3.0
Pogosto
General disorders and administration site conditions
Bruhanje Zaprtje Kserostomija Bolečine v trebuhu
Common
8, 4 6, 4 4, 7 4, 7
Chest pain 1.3
9, 7 8, 4 6, 4 5, 7
3.4
Dispepsija
1.0
1, 7
Common
4, 1
7.4
3, 0
Nervous system disorders Very common Dyskinesia Dystonia Headache Dizziness Common Hypokinesia Psychiatric disorders Very common Sleep disorder Excessive dreaming
Splošne težave in spremembe na mestu aplikacije
19.8 17.1 7.4 9.7 0.7 18.1 17.1
1, 0
41.9 18.6 9.8 13.2 0.7 23.6 21.3
Infekcijske in parazitske bolezni
51.3 22.1 11.4 6.4 2.7 24.8 16.4
Infekcije zgornjih dihal
Somnolence Confusion Hallucination Renal and urinary Common Urine disorders discoloration
Diskinezija Distonija Glavobol Omotica
13.4 8.7 5.4 0.7
19, 8 17, 1 7, 4 9, 7
17.9 10.5 8.4 2.4
41, 9 18, 6 9, 8 13, 2
14.4 10.4 10.4 7.4
51, 3 22, 1 11, 4 6, 4
Respiratory, thoracic and Common Influenza mediastinal disorders
Hipokinezija
1.7
0, 7
3.0
0, 7
4.0
2, 7
Skin and subcutaneous Common Sweating tissue disorders increased
Spalne motnje Prekomerne sanje Somnolenca Zmedenost Halucinacija
2.3
23, 6 21, 3 17, 9 10, 5 8, 4
4.4
24, 8 16, 4 14, 4 10, 4 10, 4
7.4
7, 4 4, 0
Vascular disorders Very common Orthostatic complaints
Povečano potenje 2, 3 Ortostatične 13, 8 motnje
13.8
4, 4 16, 6
16.6
7, 4 16, 8
16.8
Pogosto
Common Syncope
Sinkopa
* Very common (> 1/ 10); common (> 1/ 100< 1/10), uncommon (> 1/1,000 < 1/ 100); rare (1/10,000 < 1/ 1,000); very rare (< 1/10,000)
* 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)
The peak plasma concentrations of tolcapone at this dose were on average 30 µg/ ml (compared to 3 and 6 µg/ ml with 100 mg tid and 200 mg tid of tolcapone respectively).
Najvišje plazemske koncentracije tolkapona pri tem odmerku so bile v povprečju 30 µg/ ml (v primerjavi s 3 µg/ ml pri 100 mg odmerku trikrat na dan in 6 µg/ ml pri 200 mg tolkapona trikrat na dan).
Hospitalisation is advised.
8 Ukrepi pri prevelikem odmerjanju: priporoča se hospitalizacija.
Based on the physicochemical properties of the compound, hemodialysis is unlikely to be of benefit.
Glede na fizikalno- kemijske lastnosti učinkovine hemodializa verjetno ne bo koristila.
Tolcapone is an orally active, selective and reversible catechol-O-methyltransferase (COMT) inhibitor.
Tolkapon je peroralno aktivni, selektivni in reverzibilni zaviralec katehol- O- metiltransferaze (COMT).
Administered concomitantly with levodopa and an aromatic amino acid decarboxylase inhibitor (AADC-I), it leads to more stable plasma levels of levodopa by reducing metabolism of levodopa to 3-methoxy-4-hydroxy-L-phenylalanine (3-OMD).
Če je dan sočasno z levodopo in zaviralcem aromatske aminokislinske dekarboksilaze (AADC- I), omogoča bolj stabilne plazemske vrednosti levodope z zmanjšanjem presnove levodope v 3- metoksi - 4- hidroksil- L- fenilalanin (3- OMD).
High levels of plasma 3-OMD have been associated with poor response to levodopa in Parkinson’ s disease patients.
Visoke vrednosti plazemskega 3- OMD povezujejo s slabim odzivom na levodopo pri bolnikih s Parkinsonovo boleznijo.
Tolcapone markedly reduces the formation of 3-OMD.
Tolkapon občutno zmanjša nastajanje 3- OMD.
Pharmaco-therapeutic group:
Farmakoterapevtska skupina: antiparkinsoniki.
Anti-Parkinson drug, ATC code:
Oznaka ATC:
Clinical pharmacology
Klinična farmakologija
With 200 mg tolcapone, maximum inhibition of erythrocyte COMT activity is, on average, greater than 80%.
Z 200 mg tolkapona je maksimalno zaviranje eritrocitne COMT aktivnosti v povprečju večje od 80%.
During dosing with Tasmar 200 mg three times daily, erythrocyte COMT inhibition at trough is 30% to 45%, with no development of tolerance.
Med odmerjanjem zdravila Tasmar 200 mg trikrat na dan je zaviranje eritrocitne COMT tik pred naslednjim odmerkom 30% do 45% brez razvoja tolerance.
However, a study in Parkinson’ s patients confirmed that after treatment discontinuation there was no significant change in levodopa pharmacokinetics or in patient response to levodopa compared to pretreatment levels.
Toda študija pri Parkinsonovih bolnikih je potrdila, da v primerjavi z vrednostmi pred zdravljenjem, po prekinitvi zdravljenja ni bilo pomembnih sprememb v farmakokinetiki levodope ali v odzivu bolnika na levodopo.
This is due to a decrease in clearance in L-dopa resulting in a prolongation of the terminal elimination half-life (t1/ 2) of levodopa.
To je zaradi zmanjšanja očistka L- dope, ki se kaže v podaljšanju končne eliminacijske razpolovne dobe (t1/ 2) levodope.
Plasma levels of 3- OMD were markedly and dose-dependently decreased by tolcapone when given with levodopa/ AADC-I (aromatic amino acid decarboxylase - inhibitor) (benserazide or carbidopa).
Tolkapon je znatno in od odmerka odvisno znižal plazemske vrednosti 3 - OMD, kadar se je dajal skupaj z levodopo/ AADC- I (zaviralcem aromatske aminokislinske dekarboksilaze) (benserazidom ali karbidopo).
Tolcapone’ s effect on levodopa pharmacokinetics is similar with all pharmaceutical formulations of levodopa/ benserazide and levodopa/ carbidopa; it is independent of levodopa dose, levodopa/ AADC-I (benserazide or carbidopa) ratio and the use of sustained-release formulations.
Neodvisen je od odmerka levodope, razmerja levodopa/ AADC- I (benserazid ali karbidopa) in uporabe pripravkov s podaljšanim sproščanjem.
Double blind placebo controlled clinical studies have shown a significant reduction of approximately 20% to 30% in OFF time and a similar increase in ON time, accompanied by reduced severity of symptoms in fluctuating patients receiving Tasmar.
Dvojno slepe s placebom kontrolirane klinične študije so pokazale pomembno zmanjšanje prekinitvenega (OFF time) obdobja za približno 20 do 30% in podobno povečanje vključitvenega (ON time) obdobja, skupaj z zmanjšano resnostjo simptomov bolnikov s fluktuacijami, ki prejemajo zdravilo Tasmar.
Investigator’ s global assessments of efficacy also showed significant improvement.
Preiskovalčevo celostno vrednotenje učinkovitosti je prav tako pokazalo pomembno izboljšanje.
A double-blind trial compared Tasmar with entacapone in Parkinson's disease patients who had at least three hours of OFF time per day while receiving optimised levodopa therapy.
Dvojno slepo preskušanje je primerjalo zdravilo Tasmar z entakaponom pri bolnikih s Parkinsonovo boleznijo, ki so imeli najmanj triurno prekinitveno (OFF time) obdobje na dan, medtem ko so prejemali optimizirano terapijo z levodopo.
The primary outcome was the proportion of patients with a 1 or more hour increase in ON time (see Table 1).
Primarni izid je bilo razmerje bolnikov z eno - ali večurnim povečanjema vključitvenega (ON time) obdobja (glejte preglednico 1).
9 Tab.
9 Preglednica 1.
1 Primary and Secondary Outcome of double-blind Trial Primary Outcome
Primarni in sekundarni izidi dvojno slepega preskušanja Primarni izidi
Entacapone N=75
entakapon tolkapon n = 75 n = 75
p value
p - vrednost
Number (proportion) with ≥ 1 hour ON time response Secondary Outcome
število (delež) odgovorov z ≥ enournim vključitvenim (ON time) obdobjem Sekundarni izidi
NA
ni na voljo
In the therapeutic range, tolcapone pharmacokinetics are linear and independent of levodopa/ AADC-I (benserazide or carbidopa) coadministration.
V terapevtskih odmerkih je farmakokinetika tolkapona linearna in neodvisna od sočasnega dajanja levodope/ AADC- I (benserazida ali karbidope).
Tolcapone is rapidly absorbed with a tmax of approximately 2 hours.
Absorpcija: tolkapon se hitro absorbira s tmax približno 2 uri.
The absolute bioavailability of an oral administration is around 65%.
Absolutna biološka uporabnost po peroralnem dajanju je okoli 65 -%.
At these doses, Cmax is approximately 3 and 6 µg/ ml, respectively.
Pri teh odmerkih je Cmax približno 3 (pri 100 mg) in 6 µg (pri 200 mg).
Food delays and decreases the absorption of tolcapone, but the relative bioavailability of a dose of tolcapone taken with a meal is still 80% to 90%.
Hrana upočasni in zmanjša absorpcijo tolkapona, relativna biološka uporabnost odmerka tolkapona, če ga jemljemo s hrano, pa je še vedno 80 - do 90 -%.
The volume of distribution (Vss) of tolcapone is small (9 l).
Porazdelitev: volumen porazdelitve (Vss) tolkapona je majhen (9 l).