natgillin/translations-raw huggingface dataset:
Two of the studies involving a total of 1,353 overweight or obese patients with a BMI of 28 kg/ m2 or more and lasted from one to two years, comparing Alli given at different doses with placebo (a dummy treatment), in combination with dieting.
V dveh študijah je sodelovalo skupaj 1 353 bolnikov s prekomerno telesno maso ali debelih bolnikov, pri katerih je ITM znašal 28 kg/ m2 ali več, študiji pa sta trajali od enega do dveh let ter primerjali dajanje treh različnih odmerkov zdravila Alli s placebom (zdravilom brez zdravilne učinkovine) v kombinaciji z dieto.
Neither the patients nor the doctors knew which treatment each patient was taking until the end of the study.
Niti zdravniki niti bolniki do konca študije niso vedeli, katero zdravljenje bolnik prejema.
The third study compared Alli with placebo in 391 overweight patients with a BMI between 25 and 28 kg/ m2.
V tretji študiji so primerjali zdravilo Alli s placebom pri 391 bolnikih s čezmerno telesno maso, pri katerih je ITM znašal med 25 in 28 kg/ m2.
Alli was more effective than placebo in producing a reduction in weight in patients with a BMI of 28 kg/ m2 or more.
Zdravilo Alli je bilo bolj učinkovito kot placebo pri zmanjševanju telesne mase pri bolnikih z ITM 28 kg/ m2 ali več.
In the two studies of patients with a BMI of 28 kg/ m2 or more, patients taking Alli 60 mg had lost an average of 4.8 kg after a year, compared with 2.3 kg in those taking placebo.
Študiji bolnikov, pri katerih je ITM znašal 28 kg/ m2 ali več, sta pokazali, da so bolniki, ki so jemali zdravilo Alli, 60 mg, v povprečju izgubili približno 4, 8 kg po enem letu v primerjavi s tistimi, ki so jemali placebo in izgubili 2, 3 kg.
The study of Alli in patients with a BMI between 25 and 28 kg/ m2 failed to show a degree of weight loss that would be relevant for patients.
V študiji zdravila Alli pri bolnikih z ITM med 25 in 28 kg/ m2 ni bila dosežena stopnja zmanjšanja telesne mase, ki bi bila pomembna za bolnike.
The most common side effects with Alli (seen in more than 1 patient in 10) are oily spotting, flatus (gas) with discharge, faecal urgency (urgent need to open the bowels), fatty oily stool, oily evacuation (faeces), flatulence (gas) and soft stools.
Najpogostejši neželeni učinki zdravila Alli (opaženi pri več kot 1 bolniku od 10) so oljni madeži iz rektuma, vetrovi z uhajanjem, nujnost odvajanja, mastno ali oljnato blato, oljnato odvajanje, vetrovi in mehko blato.
For the full list of all side effects reported with Alli, see the Package Leaflet.
Za celoten seznam neželenih učinkov, o katerih so poročali pri uporabi zdravila Alli, glejte navodilo za uporabo.
Alli should not be used in people who may be hypersensitive (allergic) to orlistat or any of the other ingredients.
Zdravila Alli ne smejo uporabljati osebe, ki utegnejo biti preobčutljive za (alergične na) orlistat ali katero koli drugo sestavino zdravila.
It must not be used in people who are being treated with ciclosporin (used to prevent organ rejection in transplant patients) or with medicines used to prevent blood clots such as warfarin.
Zdravila Alli ne smejo uporabljati osebe, ki se zdravijo s ciklosporinom, (ki se uporablja proti zavrnitvi organov pri bolnikih, pri katerih je bila opravljena presaditev) ali z zdravili za preprečevanje nastanka krvnih strdkov, kot je na primer warfarin.
It must also not be used in people with a long-term malabsorption disease (where nutrients from food are not easily absorbed during digestion) or cholestasis (a liver disorder), or in women who are pregnant or breast-feeding.
Ne smejo ga uporabljati osebe z dolgotrajno malabsorpcijsko boleznijo (nezadostna absorbcija hranil iz prebavil) ali s holestazo (bolezen jeter) ter nosečnice ali ženske, ki dojijo.
The Committee for Medicinal Products for Human Use (CHMP) decided that the benefits of Alli are greater than its risks for weight loss in adults who are overweight (BMI ≥ 28 kg/ m2), taken in conjunction with a mildly hypocalorific, lower-fat diet.
Odbor za zdravila za humano uporabo (CHMP) je zaključil, da so koristi zdravila Alli pri izgubi telesne mase odraslih s čezmerno telesno maso (ITM ≥ 28 kg/ m2) ob hkratni zmerni nizkokalorični dieti z malo maščobami, večje od z njim povezanih tveganj.
The Committee recommended that Alli be given marketing authorisation.
Odbor je priporočil, da se za zdravilo Alli odobri dovoljenje za promet.
Other information about Alli:
Druge informacije o zdravilu Alli:
The European Commission granted a marketing authorisation valid throughout the EU for Orlistat GSK to Glaxo Group Limited on 23 July 2007.
Evropska komisija je dovoljenje za promet z zdravilom Alli, veljavno po vsej Evropski uniji, odobrila družbi Glaxo Group Limited dne 23. julija 2007.
This authorisation was based on the authorisation already granted in 1998 to Xenical capsules.
Odobritev je temeljila na odobritvi, ki je bila leta 1998 že dodeljena za kapsule Xenical.
The name of the medicine was changed to Alli on 12 September 2008.
Ime zdravila je bilo dne 12. septembra 2008 spremenjeno v Alli.
The full EPAR for Alli can be found here.
Celotno evropsko javno poročilo o oceni zdravila (EPAR) za zdravilo Alli je na voljo tukaj.
This summary was last updated in 04-2009.
Povzetek je bil nazadnje posodobljen 04- 2009.
EU number EU/ 1/ 07/ 401/ 007 EU/ 1/ 07/ 401/ 008 EU/ 1/ 07/ 401/ 009 EU/ 1/ 07/ 401/ 0010
Številka EU EU/ 1/ 07/ 401/ 007 EU/ 1/ 07/ 401/ 008 EU/ 1/ 07/ 401/ 009 EU/ 1/ 07/ 401/ 0010
Invented name alli alli alli alli
Zaš iteno ime alli alli alli alli
Strength 60 mg 60 mg 60 mg 60 mg
jakost 60 mg 60 mg 60 mg 60 mg
Pharmaceutical Form Capsule, hard Capsule, hard Capsule, hard Capsule, hard
farmacevtska oblika Kapsula, trda Kapsula, trda Kapsula, trda Kapsula, trda
Route of administration Oral use Oral use Oral use Oral use
pot uporabe Peroralna uporaba Peroralna uporaba Peroralna uporaba Peroralna uporaba
Packaging Bottle (HDPE) Bottle (HDPE) Bottle (HDPE) Bottle (HDPE)
ovojnina Plastenka (HDPE) Plastenka (HDPE) Plastenka (HDPE) Plastenka (HDPE)
Package size 42 60 84 90
velikost pakiranja 42 60 84 90
Each hard capsule contains 60 mg orlistat.
1 trda kapsula vsebuje 60 mg orlistata.
The capsule has a dark blue centre band, and a turquoise cap and body bearing the imprint of “ alli”.
Kapsula ima temno modro sredinsko črto, ovoj in pokrovček kapsule sta turkizne barve z napisom » alli «.
alli is indicated for weight loss in adults who are overweight (body mass index, BMI, ≥ 28 kg/ m2) and should be taken in conjunction with a mildly hypocaloric, lower-fat diet.
Zdravilo alli je indicirano za zmanjševanje telesne mase pri odraslih s čezmerno telesno maso (indeks telesne mase ITM ≥ 28 kg/ m2), ob hkratni nizkokalorični dieti z zmanjšanim vnosom maščob.
No more than three 60 mg capsules should be taken in 24 hours.
V 24- urah bolnik ne sme vzeti več kakor tri 60- mg kapsule.
While taking orlistat, the patient should be on a nutritionally balanced, mildly hypocaloric diet that contains approximately 30% of calories from fat (e. g. in a 2,000 kcal/ day diet, this equates to < 67 g of fat).
Med jemanjem orlistata naj bolnik uživa prehransko uravnoteženo, zmerno nizkokalorično dieto, ki vsebuje približno 30% kalorij iz maščob (v dieti z 2000 kcal/ dan to npr. ustreza < 67 g maščob).
alli should not be used in children and adolescents below 18 years of age due to insufficient data on safety and efficacy.
Zdravilo alli se ne sme uporabljati za zdravljenje otrok in mladostnikov, mlajših od 18 let, saj je premalo podatkov o varnosti in učinkovitosti.
There are limited data on the use of orlistat in the elderly.
2 Podatki o uporabi orlistata pri starejših so omejeni.
The effect of orlistat in individuals with hepatic and/ or renal impairment has not been studied.
Učinek orlistata pri bolnikih z okvaro v delovanju jeter ali ledvic ni bil raziskan.
2 However, as orlistat is minimally absorbed, no dosage adjustment is necessary in elderly and in individuals with hepatic and/ or renal impairment.
Ker se orlistat neznatno absorbira, pri starejših in bolnikih z okvaro v delovanju jeter ali ledvic prilagoditev odmerka ni potrebna.
• Hypersensitivity to the active substance or to any of the excipients • Concurrent treatment with ciclosporin (see section 4.5) • Chronic malabsorption syndrome • Cholestasis • Pregnancy (see section 4.6) • Breast-feeding (see section 4.6) • Concurrent treatment with warfarin or other oral anticoagulants (see sections 4.5 and 4.8)
• preobčutljivost za zdravilno učinkovino ali katerokoli pomožno snov • sočasno zdravljenje s ciklosporinom (glejte poglavje 4. 5) • kronični malabsorpcijski sindrom • holestaza • nosečnost (glejte poglavje 4. 6) • dojenje (glejte poglavje 4. 6) • sočasno jemanje z varfarinom in drugimi peroralnimi antikoagulanti (glejte poglavji 4. 5 in 4. 8)
Patients should be advised to adhere to the dietary recommendations they are given (see section 4.2).
Bolnikom je treba svetovati, da upoštevajo prejeta navodila o dieti (glejte poglavje 4. 2).
The possibility of experiencing gastrointestinal symptoms (see section 4.8) may increase when orlistat is taken with an individual meal or a diet high in fat.
Možnost pojava gastrointestinalnih simptomov (glejte poglavje 4. 8) se lahko poveča, če bolnik orlistat vzame pri enem obroku ali uživa hrano, bogato z maščobami.
For this reason, a multivitamin supplement should be taken at bedtime.
Zdravljenje z orlistatom lahko vpliva na absorpcijo liposolubilnih vitaminov (A, D, E in K) (glejte poglavje 4. 5), zato naj bolnik pred spanjem vzame multivitaminski nadomestek.
As weight loss may be accompanied by improved metabolic control in diabetes, patients who are taking a medicinal product for diabetes should consult a doctor or pharmacist before starting treatment with alli, in case it is necessary to adjust the dose of the antidiabetic medicinal product.
Ker izgubo telesne mase lahko spremlja izboljšan metabolični nadzor pri sladkorni bolezni, naj se bolniki s sladkorno boleznijo zaradi možnosti, da bo treba prilagoditi odmerek njihovih antidiabetičnih zdravil, pred začetkom zdravljenja z zdravilom alli posvetujejo z zdravnikom ali farmacevtom.
Weight loss may be accompanied by an improvement in blood pressure and cholesterol levels.
Izguba telesne mase je lahko povezana z izboljšanjem glede krvnega tlaka in nivoja holesterola.
Patients who are taking amiodarone should consult a doctor or pharmacist before starting treatment with alli (see section 4.5).
Bolniki, ki jemljejo amiodaron, naj se pred začetkom zdravljenja z zdravilom alli posvetujejo z zdravnikom ali farmacevtom (glejte poglavje 4. 5).
The use of an additional contraceptive method is recommended to prevent possible failure of oral contraception that could occur in case of severe diarrhoea (see section 4.5).
Ker je med hudo drisko peroralna kontracepcija lahko neučinkovita, je v tem primeru priporočljiva uporaba dodatne kontracepcijske metode (glejte poglavje 4. 5).
A decrease in ciclosporin plasma levels has been observed in a drug-drug interaction study and also reported in several cases, when orlistat was administered concomitantly.
Zmanjšanje plazemske koncentracije ciklosporina so opazili v interakcijski študiji zdravilo- zdravilo, o tem pa so poročali tudi, ko so bolniki sočasno jemali orlistat.
Concurrent use of alli and ciclosporin is contraindicated (see section 4.3).
Sočasna uporaba zdravila alli in ciklosporina je kontraindicirana (glejte poglavje 4. 3).
Oral anticoagulants
3 Peroralni antikoagulanti
When warfarin or other oral anticoagulants are given in combination with orlistat, international normalised ratio (INR) values could be affected (see section 4.8).
Pri sočasnem jemanju varfarina ali drugih peroralnih antikoagulantov in orlistata lahko pride do sprememb vrednosti INR (internacionalno normalizirano razmerje) (glejte poglavje 4. 8).
Concurrent use of alli and warfarin or other oral anticoagulants is contraindicated (see section 4.3).
Sočasno jemanje zdravila alli in varfarina ali drugih peroralnih antikoagulantov je kontraindicirano (glejte poglavje 4. 3).
3 The absence of an interaction between oral contraceptives and orlistat has been demonstrated in specific drug-drug interaction studies.
Odsotnost interakcije med peroralnimi kontraceptivi in orlistatom so dokazali v specifičnih interakcijskih študijah zdravilo- zdravilo.
An additional contraceptive method is recommended in case of severe diarrhoea (see section 4.4).
Dodatna kontracepcijska metoda je priporočljiva v primeru hude driske (glejte poglavje 4. 4).
However, patients should be advised to use a multivitamin supplement at bedtime to help ensure adequate vitamin intake (see section 4.4).
Vseeno je treba bolnikom svetovati, naj pred spanjem za zagotovitev ustreznega vnosa vitaminov vzamejo multivitaminski nadomestek (glejte poglavje 4. 4).
A decrease in plasma levels of amiodarone, when given as a single dose, has been observed in a limited number of healthy volunteers who received orlistat concomitantly.
Pri majhnem številu zdravih prostovoljcih, ki so sočasno z orlistatom prejeli enkraten odmerek amiodarona, so opazili zmanjšanje koncentracij amiodarona v plazmi.
Patients who are taking amiodarone should consult a doctor or pharmacist before starting treatment with alli.
Bolniki, ki jemljejo amiodaron naj se posvetujejo z zdravnikom ali farmacevtom preden pričnejo zdravljenje z zdravilom alli.
Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/ foetal development, parturition or postnatal development (see section 5.3).
Študije na živalih ne kažejo neposrednih ali posrednih škodljivih vplivov na nosečnost, razvoj zarodka/ plodu, porod ali postnatalni razvoj (glejte poglavje 5. 3).
alli is contraindicated in pregnancy (see section 4.3).
Zdravilo alli je v nosečnosti kontraindicirano.
As it is not known whether orlistat is secreted into human milk, alli is contraindicated during breast- feeding (see section 4.3).
Ker ni znano, ali orlistat pri ljudeh prehaja v mleko, je zdravilo alli med dojenjem kontraindicirano.
Orlistat has no influence on the ability to drive and use machines.
Orlistat nima vpliva na sposobnost vožnje in upravljanja s stroji.
The gastrointestinal adverse reactions identified from clinical trials with orlistat 60 mg of 18 months to 2 years duration were generally mild and transient.
Na splošno so bili blagi in prehodni.
Consumption of a diet low in fat will decrease the likelihood of experiencing adverse gastrointestinal reactions (see section 4.4).
Uživanje hrane z nizko vsebnostjo maščob zmanjša verjetnost pojava gastrointestinalnih neželenih učinkov (glejte poglavje 4. 4).
Frequencies are defined as: very common (≥ 1/ 10), common (≥ 1/ 100 to < 1/ 10), uncommon (≥ 1/ 1,000 to < 1/ 100), rare (≥ 1/ 10,000 to < 1/ 1,000) and very rare (< 1/ 10,000), not known (cannot be estimated from the available data).
Pogostnost je definirana kot: zelo pogosti (≥ 1/ 10), pogosti (≥ 1/ 100 do < 1/ 10), občasni (≥ 1/ 1. 000 do < 1/ 100), redki (≥ 1/ 10. 000 do < 1/ 1. 000), zelo redki (< 1/ 10. 000), neznana (ni možno oceniti iz razpoložljivih podatkov).
4 The frequencies of adverse reactions identified during post-marketing use of orlistat are not known as these reactions were reported voluntarily from a population of uncertain size.
Pogostnosti neželenih učinkov, ki so bile zaznane v študijah po pridobitvi dovoljenja za promet z zdravilom niso znane saj so te neželene učinke poročali prostovoljno iz populacije neznane velikosti.
Within each frequency grouping, undesirable effects are presented in order of decreasing seriousness.
Znotraj vsake skupine pogostnosti so neželeni učinki navedeni v padajočem vrstnem redu glede na resnost.
System Organ Class and Frequency Blood and the lymphatic system disorders
Organski sistem in pogostnost
Adverse Reaction/ Event
Neželeni učinek/ dogodek
Immune system disorders
Bolezni krvi in limfatičnega sistema
Decreased prothrombin and increased INR (see sections 4.3 and 4.5)
Zmanjašana vrednost protrombina in zvišana Ni znano: vrednost INR (glejte poglavji 4. 3 in 4. 5) Bolezni imunskega sistema
Hypersensitivity reactions including anaphylaxis, bronchospasm, angioedema, pruritus, rash, and urticaria
Psihiatrične motnje
Anxiety†
tesnoba †
Oily spotting Flatus with discharge Faecal urgency Fatty oily stool Oily evacuation Flatulence Soft stools
oljni madeži flatus z izcedkom nujno odvajanje blata mastno/ oljnato blato oljnat izcedek flatulenca mehko blato
Abdominal pain Faecal incontinence Liquid stools Increased defaecation
bolečina v trebuhu inkontinenca blata tekoče blato povečana pogostnost odvajanja blata
Diverticulitis Mild rectal bleeding (see section 4.4)
divertikulitis Ni znano: blaga krvavitev v predelu danke (glejte poglavje 4. 4) Bolezni jeter, žolčnika in žolčevodov
Hepatitis Cholelithiasis Increase in transaminases and in alkaline phosphatase
Hepatitis Ni znano: žolčni kamni zvišanju vrednosti transaminaz in alkalne fosfataze Bolezni kože in podkožja
Not known:
Bulozni izpuščaj Ni znano:
† It is plausible that treatment with orlistat can lead to anxiety in anticipation of or secondary to gastrointestinal adverse reactions.
5 † Verjetno je, da lahko zdravljenje z orlistatom privede do tesnobe zaradi drugačnih pričakovanj ali posledično zaradi gastrointestinalnih neželenih reakcij.
Single doses of 800 mg orlistat and multiple doses of up to 400 mg three times daily for 15 days have been studied in normal weight and obese subjects without significant clinical findings.
Enkratni odmerki orlistata 800 mg in večkratni odmerki do 400 mg 3- krat na dan 15 dni niti pri osebah z normalno telesno maso niti pri debelih bolnikih niso imeli pomembnejših kliničnih učinkov.
In addition, doses of 240 mg three times daily have been administered to obese patients for 6 months.
Dodatno so za zdravljenje debelosti bolniki 6 mesecev prejemali odmerke po 240 mg 3- krat na dan.
The majority of orlistat overdose cases received during post-marketing reported either no adverse reactions or adverse reactions that are similar to those reported with recommended doses of orlistat.
Pri večini obvestil o primerih prevelikega odmerjanja orlistata, ki so jih prejeli v času trženja zdravila, niso poročali o neželenih učinkih ali pa so bili podobni učinkom pri priporočenem odmerjanju.
5 In the event of an overdose, medical advice should be sought.
V primeru zaužitja prevelikega odmerka je treba poiskati zdravniški nasvet.
Pharmaco-therapeutic group:
Farmakoterapevtska skupina: zaviralci apetita s perifernim delovanjem, oznaka ATC:
The inactivated enzyme is thus unavailable to hydrolyse dietary fat, in the form of triglycerides, into absorbable free fatty acids and monoglycerides.
Deaktivirani encim tako zaužitih maščob v obliki trigliceridov ne more hidrolizirati v proste maščobne kisline in monogliceride, ki se lahko absorbirajo.
From clinical studies, it has been estimated that orlistat 60 mg taken three times daily blocks the absorption of approximately 25% of dietary fat.
Glede na izsledke kliničnih študij je bilo ocenjeno, da 60 mg orlistata trikrat na dan zavira absorpcijo približno 25% zaužite maščobe.
Two double-blind, randomised, placebo-controlled studies in adults with a BMI ≥ 28 kg/ m2 support the efficacy of orlistat 60 mg taken three times daily in conjunction with a hypocaloric, lower-fat diet.
Dve dvojno slepi, randomizirani, s placebom nadzorovani študiji, izvedeni pri odraslih z ITM ≥ 28 kg/ m2 podpirajo učinkovitost zdravila orlistat 60 mg v odmerku trikrat na dan v povezavi z nizkokalorično dieto.
The primary parameter, change in body weight from baseline (time of randomisation), was assessed for body weight over time (Table 1) and the percentage of subjects who lost ≥ 5% or ≥ 10% of body weight (Table 2).
Ocenjen je bil kot časovna sprememba telesne mase glede na izhodiščno vrednost (tabela 1) in kot odstotek oseb, ki so izgubile ≥ 5% ali ≥ 10% izhodiščne telesne mase (tableta 2).
Although weight loss was assessed during 12 months of treatment in both studies, most weight loss occurred within the first 6 months.
Čeprav je bila izguba telesne mase spremljana 12 mesecev jemanja v obeh študijah, pa se je večinoma telesna masa zmanjšala v prvih 6 mesecih.
Effect of 6 months treatment on body weight measured at baseline
Tabela 1: učinek 6 mesečnega zdravljenja na telesno maso glede na izhodiščno vrednost Relativna Prirejena srednja srednja
Relative
sprememba
change (kg)
sprememba
Study 1
telesne mase (v (kg) *%) * Študija 1
-1.17 -3.66
- 1, 05
-1.05 -3.59 a
- 3, 59 a
Pooled data
Orlistat 60 mg
a
- 4, 40 a a
-4.40 a
Orlistat 60 mg a
p < 0.001 versus placebo
mase (%) Placebo Orlistat 60 mg 2, 3 b
Table 2:
Študija 2
Responder analysis at 6 months
Skupni podatki
Lost ≥ 5% of baseline body weight (%) Placebo Orlistat 60 mg a
6, 5
Comparison versus placebo: a p < 0.001; b p < 0.01
Primerjava glede na placebo: a p < 0, 001; b p < 0, 01
The mean relative change in total cholesterol was -2.4% for orlistat 60 mg (baseline 5.20 mmol/ l) and +2.8% for placebo (baseline 5.26 mmol/ l).
Srednja relativna razlika skupnega holesterola je bila - 2, 4% za skupino, ki je jemala orlistat 60 mg (začetna vrednost je bila 5, 20 mmol/ l) in +2, 8% za skupino, ki je jemala placebo (začetna vrednost je bila 5, 26 mmol/ l).
The mean relative change in LDL cholesterol was -3.5% for orlistat 60 mg (baseline 3.30 mmol/ l) and +3.8% for
Srednja relativna razlika LDL holesterola je bila - 3, 5% za skupino, ki je jemala orlistat 60 (začetna vrednost je bila 3, 30 mmol/ l) in + 3, 8% za skupino, ki je jemala placebo (začetna vrednost je bila 3, 41 mmol/ l).
For waist circumference, the mean change was -4.5 cm for orlistat 60 mg (baseline 103.7 cm) and -3.6 cm for placebo (baseline 103.5 cm).
Srednja razlika obsega pasu je bila - 4, 5 cm za skupino, ki je jemala orlistat 60 mg (začetna vrednost je bila 103, 7 cm) in - 3, 6 cm za skupino, ki je jemala placebo (začetna vrednost j bila 103, 5 cm).
Plasma concentrations of intact orlistat were non-measurable (< 5 ng/ ml) 8 hours following oral administration of orlistat 360 mg.
V plazmi je bila koncentracija nespremenjenega orlistata 8 ur po peroralnem vnosu 360 mg orlistata nemerljiva (< 5 ng/ ml).
In general, at therapeutic doses, detection of intact orlistat in plasma was sporadic and concentrations were extremely low (< 10 ng/ ml or 0.02 µmol), with no evidence of accumulation, which is consistent with minimal absorption.
Do kopičenja ni prihajalo, kar je skladno z neznatno absorpcijo.
In vitro, orlistat is > 99% bound to plasma proteins (lipoproteins and albumin were the major binding proteins).
In vitro se več kot 99% orlistata veže na beljakovine v plazmi (večinoma na lipoproteine in albumin).
Based on a study in obese patients, of the minimal fraction of the dose that was absorbed systemically, two major metabolites, M1 (4-member lactone ring hydrolysed) and M3 (M1 with N-formyl leucine moiety cleaved), accounted for approximately 42% of the total plasma concentration.
Ugotovitve študije, v kateri so sodelovali bolniki s čezmerno telesno maso, so pokazale, da sta v majhnem deležu sistemsko absorbirane količine zdravila glavna dva presnovka, ki predstavljata približno 42% skupne koncentracije v plazmi, in sicer M 1 (hidrolizirani 4- členski laktonski obroč) in M 3 (M 1 s cepljenim N- formillevcinskim ostankom).
M1 and M3 have an open beta-lactone ring and extremely weak lipase inhibitory activity (1,000- and 2,500-fold less than orlistat, respectively).
M 1 in M 3 imata odprt betalaktonski obroč in zelo šibak zaviralni učinek na lipazo (1. 000 - oziroma 2. 500- krat šibkejši od orlistata).
In view of this low inhibitory activity and the low plasma levels at therapeutic doses (average of 26 ng/ ml and 108 ng/ ml, respectively), these metabolites are considered to be pharmacologically inconsequential.
Zaradi šibkega zaviralnega učinka in majhne koncentracije v plazmi po vnosu terapevtskih odmerkov (povprečno 26 ng/ ml (M 1) oziroma 108 ng/ ml (M 3)) sta oba presnovka farmakološko nepomembna.
Elimination
7 Izločanje
Approximately 97% of the administered dose was excreted in faeces and 83% of that as unchanged orlistat.
Približno 97% vnesenega odmerka se izloči z blatom, od tega 83% kot nespremenjen orlistat.