qanastek/EMEA-V3 huggingface dataset:
Pelzont 1000 mg/ 20 mg modified-release tablets.
Pelzont 1, 000 mg/ 20 mg pilloli li jerħu l- mediċina b’ mod modifikat.
Each modified-release tablet contains 1000 mg of nicotinic acid and 20 mg of laropiprant.
Kull pillola li terħi l- mediċina b’ mod modifikat fiha 1, 000 mg ta ’ aċidu nikotiniku u 20 mg ta ’ laropiprant.
Excipient Each modified-release tablet contains 128.4 mg of lactose monohydrate.
Sustanza mhux attiva Kull pillola li terħi l- mediċina b’ mod modifikat fiha 128. 4 mg ta ’ lactose monohydrate.
Capsule-shaped, white to off-white tablet, with “ 552 ” debossed on one side.
Pillola bajda għal offwajt, għamla ta ’ kapsula, li għandha “ 552 ” ibbuzzat fuq naħa waħda.
Pelzont is indicated for the treatment of dyslipidaemia, particularly in patients with combined mixed dyslipidaemia (characterised by elevated levels of LDL-cholesterol and triglycerides and low HDL-cholesterol) and in patients with primary hypercholesterolaemia (heterozygous familial and non-familial).
Pelzont huwa indikat għat- trattament tad- dislipidemija, b’ mod partikolari f’ pazjenti li għandhom dislipidemija mħallta kkombinata (ikkaratterizzata minn livelli għolja ta ’ LDL- kolesterol u trigliċeridi u HDL- kolesterol baxx) u f’ pazjenti b’ iperkolesterolemija primarja (eterozigote familjali u mhux familjali).
Pelzont should be used in patients in combination with HMG-CoA reductase inhibitors (statins), when the cholesterol lowering effect of HMG-CoA reductase inhibitor monotherapy is inadequate.
Pelzont għandu jintuża fil- pazjenti flimkien ma ’ inibituri HMG- CoA reductase (statins), meta l- effett tat- tbaxxija tal- kolesterol ta ’ monoterapija b’ inibitur HMG- CoA reductase ma jkunx adegwat.
It can be used as monotherapy only in patients in whom HMG-CoA reductase inhibitors are considered inappropriate or not tolerated.
Huwa jista ’ jintuża bħala monoterapija f’ dawk il- pazjenti biss li fihom l- inibituri HMG- CoA reductase jkunu kkunsidrati bħala mhux xierqa jew mhux ittollerati.
Diet and other non-pharmacological treatments (e. g. exercise, weight reduction) should be continued during therapy with Pelzont.
Dieti u trattamenti oħra mhux farmakoloġiċi (eż. eżerċizzju, tnaqqis fil- piż) għandhom jitkomplew matul it- terapija bi Pelzont.
Posology The starting dose is one modified-release tablet (1000 mg nicotinic acid/ 20 mg laropiprant) once a day.
Pożoloġija Id- doża tal- bidu hija pillola waħda li terħi l- mediċina b’ mod modifikat (1, 000 mg aċidu nikotiniku/ 20 mg laropiprant) darba kuljum.
After four weeks, it is recommended that patients be advanced to the maintenance dose of 2000 mg/ 40 mg taken as two modified-release tablets (1000 mg/ 20 mg each) once daily.
Wara erba ’ ġimgħat, huwa rakkomandat li l- pazjenti jitmexxew għad - doża ta ’ manteniment ta ’ 2000 mg/ 40 mg meħuda bħala żewġ pilloli li jerħu l- mediċini b’ mod modifikat (1, 000 mg/ 20 mg kull waħda) darba kuljum.
Daily doses greater than 2000 mg/ 40 mg have not been studied and therefore are not recommended.
Dożi akbar minn 2000 mg/ 40 mg kuljum ma ġewx studjati u għalhekk mhumiex rakkomandati.
If Pelzont is missed for less than 7 consecutive days, patients can resume therapy at the last administered dose.
Jekk Pelzont ma jitteħidx għal inqas minn 7 ijiem konsekuttivi, il- pazjenti jistgħu jerġgħu jibdew it - terapija bl- aħħar doża mogħtija.
If Pelzont is missed for 7 or more consecutive days, therapy should be resumed at the 1000 mg/ 20 mg dose for 1 week, before advancing to the maintenance dose of 2000 mg/ 40 mg.
Jekk Pelzont ma jitteħidx għal 7 ijiem konsekuttivi jew aktar, il- bidu mill- ġdid tat- terapija għandu jsir bid- doża ta ’ 1, 000 mg/ 20 mg għal ġimgħa, qabel ma wieħed jgħaddi għad- doża ta ’ manteniment ta ’ 2000 mg/ 40 mg.
2 Those patients switching from 2000 mg or more of prolonged-release nicotinic acid can initiate Pelzont at the 2000 mg/ 40 mg dose.
Dawk il- pazjenti li jaqilbu minn 2000 mg jew aktar ta ’ aċidu nikotiniku li jerħi l- mediċina bil- mod jistgħu jibdew Pelzont bid- doża ta ’ 2000 mg/ 40 mg.
Patients switching from less than 2000 mg of prolonged-release nicotinic acid should initiate therapy at the starting dose of 1000 mg/ 20 mg and advance to the 2000 mg/ 40 mg maintenance dose after four weeks.
Il- pazjenti li jaqilbu minn anqas minn 2000 mg ta ’ aċidu nikotiniku li jerħi l- mediċina bil- mod għandhom jibdew it- terapija bid- doża tal- bidu ta ’ 1, 000 mg/ 20 mg u javvanzaw għal doża ta ’ manteniment ta ’ 2, 000 mg/ 40 mg wara erba ’ ġimgħat.
For patients switching from immediate-release nicotinic acid to Pelzont, therapy should be initiated at the 1000 mg/ 20 mg dose and advanced to the 2000 mg/ 40 mg maintenance dose after four weeks.
Fil- każ tal- pazjenti li jaqilbu minn aċidu nikotiniku ta ’ rilaxx immedjat għal Pelzont, it- terapija għandha 2 tinbeda bid- doża ta ’ 1, 000 mg/ 20 mg u tgħaddi għad- doża ta ’ manteniment ta ’ 2000 mg/ 40 mg wara erba ’ ġimgħat.
Method of administration The tablets should be taken whole, with food, in the evening or at bedtime.
Metodu ta ’ għoti Il- pilloli għandhom jittieħdu sħaħ, ma ’ l- ikel, filgħaxija jew qabel l- irqad.
To preserve the modified-release properties, the tablets must not be split, broken, crushed, or chewed before swallowing.
M’ għandekx taqsam, tkisser, tfarrak, jew tomgħod il- pillola li terħi l- mediċina b’ mod modifikat qabel ma tiblagħha.
To reduce the possibility of flushing, alcohol or hot drinks should be avoided at the time of ingestion of the medicinal product.
Biex titnaqqas il- possibilità ta ’ fawra, wieħed għandu jevita l- alkoħol jew xarbiet sħan fil- ħin li jittieħed il - prodott mediċinali.
Use in the elderly No dose adjustment is required for elderly patients.
Użu fl- anzjani M’ hemmx bżonn ta ’ aġġustament fid- doża għall- pazjenti anzjani.
Use in paediatric patients Safety and effectiveness of Pelzont in paediatric patients have not been established.
Użu f’ pazjenti pedjatriċi Is- sigurtà u l- effikaċja ta ’ Pelzont ma ġietx stabbilita f’ pazjenti pedjatriċi.
Therefore, treatment is not recommended in this age group.
Għalhekk, it- trattament mhux rakkomandat f’ dan il- grupp ta ’ età.
Use in patients with hepatic or renal insufficiency Use of Pelzont in patients with hepatic or renal insufficiency has not been studied.
Użu f’ pazjenti b’ insuffiċjenza tal- fwied jew tal- kliewi L- użu ta ’ Pelzont f’ pazjenti b’ insuffiċjenza tal- fwied jew tal- kliewi ma ġiex studjat.
Like other nicotinic acid medicinal products, Pelzont is contraindicated in patients with significant or unexplained hepatic dysfunction.
Bħal prodotti mediċinali oħra ta ’ l- aċidu nikotiniku, Pelzont huwa kontra- indikat f’ pazjenti li għandhom disfunzjoni tal- fwied sinifikanti jew mhux spjegata.
It should be used with caution in patients with renal insufficiency, because nicotinic acid and its metabolites are primarily excreted by the kidneys (see sections 4.3, 4.4 and 5.2).
Huwa għandu jintuża b’ kawtela f’ pazjenti b’ insuffiċjenza tal - kliewi, minħabba li l- aċidu nikotiniku u l- metaboliti tiegħu jitneħħew primarjament mill- kliewi (ara sezzjonijiet 4. 3, 4. 4 u 5. 2).
Concomitant therapy Acetylsalicylic acid provides no additional reduction of flushing beyond that achieved by Pelzont.
Terapija konkomitanti L- aċidu aċetilsaliċiliku ma jipprovdi l- ebda tnaqqis addizzjonali tal- fawra aktar minn dik miksuba bi Pelzont.
Therefore, treatment with acetylsalicylic acid to alleviate flushing symptoms is not necessary (see section 5.1).
Għalhekk, mhux meħtieġ trattament bl- aċidu aċetilsaliċiliku biex itaffi s- sintomi tal- fawra (ara sezzjoni 5. 1).
Because co-administration of bile acid sequestrants may reduce the bioavailability of acidic medicinal products such as nicotinic acid, it is recommended that Pelzont be administered > 1 hour before or > 4 hours after administration of a bile acid sequestrant (see section 4.5).
Minħabba li l- għoti fl- istess ħin ta ’ sekwestranti ta ’ l- aċidu biljari jista ’ jnaqqas il- bijodisponibilità ta ’ prodotti mediċinali aċidużi bħall- aċidu nikotiniku, huwa rakkomandat li Pelzont jingħata > siegħa qabel jew > 4 sigħat wara l- għoti ta ’ sekwestrant ta ’ l- aċidu biljari (ara sezzjoni 4. 5).
• Hypersensitivity to the active substances or to any of the excipients. • Significant or unexplained hepatic dysfunction. • Active peptic ulcer disease. • Arterial bleeding.
• Sensittività eċċessiva għas- sustanzi attivi jew għal xi sustanzi mhux attivi. • Disfunzjoni tal- fwied sinifikanti jew mhux spjegata. • Mard attiv ta ’ l- ulċera peptika. • Fsada arterjali.
When Pelzont is co-administered with a statin, please refer to the Summary of Product Characteristics for that particular medicinal product.
Meta Pelzont jingħata fl- istess ħin ma ’ statin, jekk jogħġbok irreferi għas- Sommarju tal- Karatteristiċi tal- Prodott ta ’ dak il- prodott mediċinali partikolari.
Hepatic effects Switching from immediate-release (crystalline) nicotinic acid to Pelzont has not been studied.
Effetti fuq il- fwied Il- qlib minn aċidu nikotiniku (kristallin) ta ’ rilaxx immedjat għal Pelzont ma ġiex studjat.
However, cases of severe hepatic toxicity, including fulminant hepatic necrosis, have occurred in
Madankollu, seħħew każijiet ta ’ tossiċità epatika severa, fosthom nekrosi epatika fulminanti, f’ pazjenti li qalbu minn aċidu nikotiniku ta ’ rilaxx immedjat għal aċidu nikotiniku li jaħdem fit- tul b’ dożi ekwivalenti.
Therefore, patients switching from immediate-release nicotinic acid to Pelzont should be initiated at the 1000 mg/ 20 mg dose.
Għalhekk, il- pazjenti li jaqilbu minn aċidu nikotiniku ta ’ rilaxx immedjat għal Pelzont għandhom jinbdew bid- doża ta ’ 1, 000 mg/ 20 mg.
Pelzont should be used with caution in patients who consume substantial quantities of alcohol and/ or have a past history of liver disease.
Pelzont għandu jintuża b’ kawtela f’ pazjenti li jikkunsmaw kwantitajiet sostanzjali ta ’ alkoħol u/ jew li għandhom storja passata ta ’ mard tal- fwied.
Like other lipid-lowering therapies, nicotinic acid medicinal products have been associated with abnormal liver function tests (see section 4.8).
Bħal terapiji oħra li jbaxxu l- lipidi, il- prodotti mediċinali ta ’ l- aċidu nikotiniku ġew assoċjati ma ’ testijiet abnormali tal- funzjoni tal- fwied (ara sezzjoni 4. 8).
Transaminase elevations were reversible upon discontinuation of therapy.
Iż- żidiet fit- transaminase kienu riversibbli malli twaqqfet it- terapija.
Liver function tests are recommended before initiation, every 6 to 12 weeks for the first year, and periodically (e. g. semi-annually) thereafter.
3 Huma rakkomandati testijiet tal- funzjoni tal- fwied qabel ma tinbeda t- terapija, kull 6 sa 12- il ġimgħa għall- ewwel sena, u perjodikament (eż. kull sitt xhur) minn hemm ’ il quddiem.
Patients who develop increased transaminase levels should be monitored until the abnormalities have resolved.
Il- pazjenti li jiżviluppaw żidiet fil- livelli ta ’ transaminase għandhom jiġu mmonitorjati sakemm l- abnormalitajiet jitilqu.
Should an increase in alanine aminotransferase (ALT) or aspartate aminotransferase (AST) of ≥ 3 X ULN persist, reduction of dose or withdrawal of Pelzont is recommended.
Jekk żieda fl- alanine aminotransferase (ALT) jew fl- aspartate aminotransferase (AST) ta ’ ≥ 3 X ULN tippersisti, huwa rakkomandat tnaqqis fid- doża jew twaqqif ta ’ Pelzont.
Effect on skeletal muscle Rare cases of rhabdomyolysis have been associated with concomitant administration of lipid-altering doses (≥ 1000 mg/ day) of nicotinic acid and HMG-CoA reductase inhibitors (statins) (see section 4.8).
Effett fuq il- muskolu skeletali Każijiet rari ta ’ rhabdomyolysis ġew assoċjati ma ’ l- għoti fl- istess ħin ta ’ dożi ta ’ aċidu nikotiniku li jibdlu l- livell tal- lipidi (≥1, 000 mg/ kuljum) u inibituri HMG- CoA reductase (statins) (ara sezzjoni 4. 8).
Physicians contemplating combined therapy with statins and Pelzont should carefully weigh the potential benefits and risks and should carefully monitor patients for any signs and symptoms of muscle pain, tenderness, or weakness, particularly during the initial months of therapy and when the dose of either medicinal product is increased.
It- tobba li jikkunsidraw terapija kkombinata bl- istatins u Pelzont għandhom iqisu bil- għaqal il - vantaġġi u r- riskji potenzjali u għandhom jimmonitorjaw sewwa l- pazjenti għal kwalunkwe sinjali u sintomi ta ’ uġigħ, sensittività, jew dgħjufija fil- muskoli, b’ mod partikolari matul l- ewwel xhur tat - terapija u meta d- doża ta ’ xi wieħed mill- prodotti mediċinali tiżdied.
Periodic serum creatine kinase (CK) should be considered in such situations, but there is no assurance that such monitoring will prevent the occurrence of severe myopathy.
F’ sitwazzjonijiet bħal dawn għandu jiġi kkunsidrat creatine kinase (CK) perjodiku fis- serum, iżda ma hemm l- ebda garanzija li tali monitoraġġ se jimpedixxi li sseħħ mijopatija severa.
Caution should be exercised in patients with pre-disposing factors for rhabdomyolysis. • Age > 70 years • Renal impairment • Uncontrolled hypothyroidism • Personal or familial history of hereditary muscular disorders • Previous history of muscular toxicity with a statin or fibrate • Alcohol abuse.
Għandha tintuża kawtela f’ pazjenti b’ fatturi ta ’ pre- dispożizzjoni għal rhabdomyolysis. • Età > 70 sena • Indeboliment tal- kliewi • Ipotirojdiżmu mhux ikkontrollat • Storja personali jew familjari ta ’ disturbi muskolari ereditarji • Storja preċedent ta ’ tossiċità muskolari bi statin jew fibrat • Abbuż mill- alkoħol.
If muscle pain, weakness or cramps occur while a patient is receiving Pelzont with a statin, their CK levels should be measured.
Jekk iseħħ uġigħ muskolari, dgħjufija jew bugħawwieġ waqt li pazjent ikun qiegħed jirċievi Pelzont bi statin, għandhom jitkejlu l- livelli CK tagħhom.
If these levels are found, in the absence of strenuous exercise, to be significantly elevated (> 5 x ULN), treatment should be stopped.
Jekk dawn il- livelli jinstabu, fin- nuqqas ta ’ eżerċizzju qawwi, li jkunu elevati ferm (> 5 x ULN), it- trattament għandu jitwaqqaf.
Renal dysfunction Because nicotinic acid and its metabolites are excreted through the kidneys, Pelzont should be used with caution in patients with renal dysfunction.
Disfunzjoni tal- fwied Minħabba li l- aċidu nikotiniku u l- metaboliti tiegħu jitneħħew mill- kliewi, Pelzont għandu jintuża b’ kawtela f’ pazjenti li jkollhom disfunzjoni tal- kliewi.
Effect on glucose Nicotinic acid medicinal products have been associated with increases of fasting blood glucose levels (see section 4.8).
Effett fuq il- glukożju Il- prodotti mediċinali ta ’ l- aċidu nikotiniku ġew assoċjati ma ’ żidiet fil- livelli ta ’ glukożju fid- demm (ara sezzjoni 4. 8)..
Diabetic or potentially diabetic patients should be observed closely.
Il- pazjenti dijabetiċi jew potenzjalment dijabetiċi għandhom jiġu osservati mill - qrib.
Adjustment of diet and/ or hypoglycaemic therapy may be necessary.
Jista ’ jkun hemm bżonn ta ’ aġġustament fid- dieta u/ jew fit- terapija ipoglikemika.
4 Acute coronary syndrome As with other nicotinic acid medicinal products, caution should be used when Pelzont is used in patients with unstable angina or in the acute phase of an MI, particularly when such patients are also receiving vasoactive medicinal products such as nitrates, calcium channel blockers, or adrenergic blocking agents.
Sindrome koronarju akut Bħal fi prodotti mediċinali ta ’ l- aċidu nikotiniku oħrajn, għandha tintuża kawtela meta Pelzont jintuża f’ pazjenti b’ anġina instabbli jew fil- fażi akuta ta ’ MI, b’ mod partikolari meta dawn il- pazjenti jkunu qegħdin jirċievu wkoll prodotti mediċinali vasoattivi bħal nitrati, imblokkaturi tal- kanali tal- kalċju, jew sustanzi ta ’ imblokk adrenerġiċi.
Haematologic effects As with other nicotinic acid medicinal products, Pelzont (2000 mg/ 40 mg) was associated with small reductions in platelet count (see section 4.8).
Effetti ematoloġiċi Bħal fi prodotti mediċinali ta ’ l- aċidu nikotiniku oħrajn, Pelzont (2000 mg/ 40 mg) ġie assoċjat ma ’ tnaqqis żgħir fl- għadd tal- plejtlits (ara sezzjoni 4. 8).
Therefore, patients undergoing surgery should be carefully evaluated.
Għalhekk, il- pazjenti sottoposti għal kirurġija għandhom jiġu evalwati b’ attenzjoni.
Effect on uric acid As with other nicotinic acid medicinal products, Pelzont (2000 mg/ 40 mg) was associated with small increases in uric acid levels (see section 4.8).
Effett fuq l- aċidu uriku Bħal fi prodotti mediċinali ta ’ l- aċidu nikotiniku oħrajn, Pelzont (2000 mg/ 40 mg) ġie assoċjat ma ’ żidiet żgħar fil- livelli ta ’ l- aċidu uriku (ara sezzjoni 4. 8).
Therefore, Pelzont should be used with caution in patients with or predisposed to gout.
Għalhekk, Pelzont għandu jintuża b’ kawtela f’ pazjenti bil- gotta jew predisposti għaliha.
Hypophosphatemia As with other nicotinic acid medicinal products, Pelzont was associated with small decreases in phosphorus levels.
4 Ipofosfatemja Bħal fi prodotti mediċinali ta ’ l- aċidu nikotiniku oħrajn, Pelzont kien assoċjat ma ’ tnaqqis żgħir fil - livelli ta ’ fosfru.
Therefore, patients with a risk for hypophosphatemia should be closely followed.
Għalhekk, il- pazjenti b’ riskju għal ipofosfatemija għandhom jiġu sorveljati mill- qrib.
Further As with other nicotinic acid medicinal products, patients with a history of jaundice, hepato-biliary disorder or peptic ulcer should be observed closely (see sections 4.2 and 4.3).
Aktar Bħal fi prodotti mediċinali ta ’ l- aċidu nikotiniku oħrajn, pazjenti bi storja ta ’ suffejra, disturbi epato - biljari jew ulċera peptika għandhom jiġu osservati mill- qrib (ara sezzjonijiet 4. 2 u 4. 3).
Excipient Pelzont contains lactose.
Sustanza mhux attiva Pelzont fih il- lattożju.
Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Pazjenti bi problemi ereditarji rari ta ’ intolleranza għall- galattożju, id- defiċjenza ta ’ Lapp lactase jew assorbiment ħażin tal- glukożju- galattożju m’ għandhomx jieħdu din il- mediċina.
Simultaneous use of alcohol or hot drinks can enhance the effects of flushing and should therefore be avoided around the time of ingestion of Pelzont.
Użu simultanju ta ’ alkoħol jew xorb sħun jista ’ jkabbar l- effetti ta ’ fawra u għalhekk dawn għandhom jiġu evitati mal- ħin ta ’ inġestjoni ta ’ Pelzont.
Nicotinic acid Effects of nicotinic acid on other medicinal products Antihypertensive therapy:
L- aċidu nikotiniku Effetti ta ’ l- aċidu nikotiniku fuq prodotti mediċinali oħra Terapija kontra l- pressjoni għolja:
Nicotinic acid may potentiate the effects of ganglionic blocking agents and vasoactive medicinal products such as nitrates, calcium channel blockers, and adrenergic receptor blocking agents, resulting in postural hypotension.
L- aċidu nikotiniku jista ’ jqawwi l- effetti ta ’ sustanzi ta ’ imblokk ganglijoniċi u prodotti mediċinali vasoattivi bħal nitrati, imblokkaturi tal- kanali tal- kalċju, u sustanzi li jimblokkaw ir- riċetturi adrenerġiċi, li jwassal għal pressjoni baxxa posturali.
HMG-CoA reductase inhibitors:
Inibituri HMG- CoA reductase:
When simvastatin is combined with nicotinic acid, a modest increase in AUC and Cmax of simvastatin acid (the active form of simvastatin) was observed, which may be devoid of clinical relevance.
Meta simvastatin jitħallat ma ’ l- aċidu nikotiniku, kienet osservata żieda modesta fl- AUC u l- Cmax ta ’ l- aċidu ta ’ simvastatin (il- forma attiva ta ’ simvastatin), li jista ’ ma jkollhiex rilevanza klinika.
The pharmacokinetic interaction of Pelzont with statins has been studied only with simvastatin (see section 4.4).
L- interazzjoni farmakokinetika ta ’ Pelzont ma ’ l- istatins ġiet studjata biss b’ simvastatin (ara sezzjoni 4. 4).
Effects of other medicinal products on nicotinic acid Bile acid sequestrants:
Effetti ta ’ prodotti mediċinali oħra fuq l- aċidu nikotiniku Sekwestranti ta ’ l- aċidu biljari:
Because co-administration of bile acid sequestrants may reduce the bioavailability of acidic medicinal products such as nicotinic acid, it is recommended that Pelzont be administered > 1 hour before or > 4 hours after administration of a bile acid sequestrant.
Minħabba li l- għoti fl- istess ħin ta ’ sekwestranti ta ’ l- aċidu biljari jista ’ jnaqqas il- bijodisponibilità ta ’ prodotti mediċinali aċidużi bħall- aċidu nikotiniku, huwa rakkomandat li Pelzont jingħata > siegħa qabel jew > 4 sigħat wara l- għoti ta ’ sekwestrant ta ’ l- aċidu biljari.
5 Supplements containing nicotinic acid:
Supplimenti li fihom l- aċidu nikotiniku:
Vitamins or other nutritional supplements containing (≥ 50 mg/ day) of nicotinic acid (or nicotinamide) have not been studied with Pelzont.
Vitamini jew supplimenti nutrizzjonali oħra li fihom (≥ 50 mg/ ġurnata) ta ’ aċidu nikotiniku (jew nicotinamide) ma ġewx studjati ma ’ Pelzont.
Physicians should consider the nicotinic acid intake from vitamins and nutritional supplements when prescribing Pelzont.
It- tobba għandhom jikkunsidraw l- ammont ta ’ aċidu nikotiniku meħud mill- vitamini u s- supplimenti nutrizzjonali meta jordnaw Pelzont.
Medicinal product / laboratory test interactions:
Interazzjonijiet tal- prodott mediċinali / testijiet tal- laboratorju:
In urine glucose tests, nicotinic acid may also give false-positive reactions with cupric sulfate solution (Benedict’ s reagent).
F’ testijiet tal- glukożju fl- awrina, l - aċidu nikotiniku jista ’ jagħti wkoll reazzjonijiet pożittivi foloz ma ’ soluzzjoni tas- sulfat kupriku (reaġent ta ’ Benedict).
Laropiprant Effects of laropiprant on other medicinal products Midazolam:
Laropiprant Effetti ta ’ laropiprant fuq prodotti mediċinali oħra Midazolam:
Multiple doses of laropiprant 40 mg did not affect the pharmacokinetics of midazolam, a sensitive CYP3A4 substrate.
Dożi multipli ta ’ laropiprant 40 mg ma affettwawx il- farmakokinetika ta ’ midazolam, substrat sensittiv ta ’ CYP3A4.
Therefore, laropiprant is not an inducer or inhibitor of CYP3A4.
Għalhekk, laropiprant mhuwiex induttur jew inibitur ta ’ CYP3A4.
However, the plasma concentration of a metabolite of midazolam, 1'-hydroxymidazolam, was increased approximately 2-fold with multiple doses of laropiprant.
Madankollu, il- konċentrazzjonijiet fil- plażma ta ’ metabolit ta ’ midazolam, 1 '- hydroxymidazolam, żdiedu b’ madwar darbtejn b’ diversi dożi ta ’ laropiprant.
Because 1'-hydroxymidazolam is an active metabolite, the sedative effect of midazolam may be increased and caution should be used when laropiprant is co-administered with midazolam.
Minħabba li 1 '- hydroxymidazolam huwa metabolit attiv, l- effett sedattiv ta ’ midazolam jista ’ jiżdied u għandha tintuża kawtela meta laropiprant jingħata fl- istess ħin ma ’ midazolam.
Other medicinal products:
Prodotti mediċinali oħra:
Co-administration of laropiprant 40 mg with midazolam increased the AUC0-∞ and Cmax of 1'-hydroxymidazolam, a midazolam metabolite, by 98% and 59%, respectively.
L- għoti fl- istess ħin ta ’ laropiprant 40 mg ma ’ midazolam żied l- AUC0- ∞ u l- Cmax ta ’ 1 '- hydroxymidazolam, metabolit ta ’ midazolam, bi 98% u 59%, rispettivament.
1'-hydroxymidazolam is metabolised predominantly by uridine diphosphate-glucuronosyltransferases (UGT) 2B4 and 2B7.
1 '- hydroxymidazolam huwa metabolizzat prinċipalment mill- uridine diphosphate - glucuronosyltransferases (UGT) 2B4 u 2B7.
Clinical and in vitro studies support the conclusion that laropiprant is a mild to moderate inhibitor of UGT2B4/ UGT2B7.
5 laropiprant huwa inibitur ħafif għal moderat ta ’ UGT2B4/ UGT2B7.
Very few medicinal products are known to be metabolised predominantly by UGT2B4 or UGT2B7.
Huma ftit ħafna l- prodotti mediċinali li huma magħrufa li jiġu metabolizzati prinċipalment minn UGT2B4 jew UGT2B7.
Caution should be used when Pelzont is co-administered with medicinal products metabolised predominantly by UGT2B4 or UGT2B7, for instance zidovudine.
Għandha tintuża attenzjoni meta Pelzont jingħata fl- istess ħin ma ’ prodotti mediċinali li jiġu metabolizzati primarjament minn UGT2B4 jew UGT2B7, per eżempju zidovudine.
In interaction studies, laropiprant did not have clinically significant effects on the pharmacokinetics of the following medicinal products: simvastatin, warfarin, oral contraceptives, rosiglitazone and digoxin.
Fi studji dwar l- effett ta ’ mediċini jew ta ’ affarijiet oħra fuq l- effett farmaċewtiku tal- prodott, laropiprant ma kellu ebda effetti kliniċi sinifikanti fuq il- farmakokinetika ta ’ dawn il- prodotti mediċinali li ġejjin: simvastatin, warfarin, kontraċettivi orali, rosiglitazone u digoxin.
Based on these data, laropiprant is not expected to cause interactions with substrates of CYP isozymes 3A4, 2C9, 2C8 and human P-glycoprotein (P-gp).
Fuq il- bażi ta ’ din l- informazzjoni, laropiprant mhux mistenni li jikkawża interazzjonijiet ma ’ substrati ta ’ l - isoenzimi CYP 3A4, 2C9, 2C8 u l- glikoproteina- P umana (P- gp).
In in vitro studies, laropiprant did not inhibit CYP1A2, CYP2B6, CYP2C19, CYP2D6, or CYP2E1-mediated reactions.
Fi studji in vitro, laropiprant ma impediex reazzjonijiet medjati minn CYP1A2, CYP2B6, CYP2C19, CYP2D6, jew CYP2E1.
In a clinical study, there was no meaningful effect of laropiprant on the inhibition of ADP-induced platelet aggregation by clopidogrel, but there was a modest increase in the inhibition of collagen-induced platelet aggregation by clopidogrel.
Fi studju kliniku, ma kien hemm ebda effett sinifikanti ta ’ laropiprant fuq l- inibizzjoni ta ’ aggregazzjoni tal- plejtlits indotti mill- ADP bi clopidogrel, iżda kien hemm żieda modesta fl - inibizzjoni ta ’ aggregazzjoni tal- plejtlits indotta mill- collagen bi clopidogrel.
The clinical significance of these observations is unknown.
L- importanza klinika ta ’ dawn l- osservazzjonijiet mhijiex magħrufa.
Acetylsalicylic acid:
Aċidu aċetilsaliċiliku:
In a clinical study, concomitant administration of laropiprant with acetylsalicylic acid did not have an effect on collagen-induced platelet aggregation or on bleeding time compared to treatment with acetylsalicylic acid alone (see section 5.1).
Fi studju kliniku, l- għoti fl- istess ħin ta ’ laropiprant ma ’ l- aċidu aċetilsaliċiliku ma kellux effett fuq l- aggregazzjoni tal- plejtlits indotta mill- collagen jew fuq il- ħin tal- fsada meta mqabbel ma ’ trattament bl- aċidu aċetilsaliċiliku biss (ara sezzjoni 5. 1).
Effects of other medicinal products on laropiprant CYP3A4 Inhibitor:
Effetti ta ’ prodotti mediċinali oħra fuq laropiprant Inibitur ta ’ CYP3A4:
Clarithromycin (a potent inhibitor of CYP3A4 and P-gp) did not have a clinically meaningful effect on the pharmacokinetics of laropiprant.
Clarithromycin (inibitur b’ saħħtu ta ’ CYP3A4 u P- gp) ma kellux effett kliniku sinifikanti fuq il- farmakokinetika ta ’ laropiprant.
Laropiprant is not a substrate of human P-gp, and therefore other inhibitors of CYP3A4 and/ or P-gp are also not expected to have a clinically meaningful impact on the pharmacokinetics of laropiprant.
Laropiprant mhux substrat tal- P- gp umana, u għalhekk inibituri oħra ta ’ CYP3A4 u/ jew P- gp ukoll mhumiex mistennija li jkollhom impatt kliniku sinifikanti fuq il- farmakokinetika ta ’ laropiprant.
6 4.6 Pregnancy and lactation
4. 6 Tqala u treddigħ
Pregnancy Pelzont There are no data from the combined use of nicotinic acid and laropiprant in pregnant women.
Tqala Pelzont M’ hemm ebda informazzjoni dwar l- użu kombinat ta ’ l- aċidu nikotiniku u laropiprant f’ nisa tqal.
The combination has not been tested in reproductive toxicity studies.
Il - kombinazzjoni ma ġietx ittestjata fi studji tat- tossiċità riproduttiva.
Therefore, Pelzont should not be used during pregnancy unless clearly necessary.
Għalhekk Pelzont m’ għandux jintuża waqt it- tqala jekk ma jkunx hemm bżonn ċar.
Nicotinic acid There are no adequate data from the use of high dose nicotinic acid in pregnant women.
Aċidu nikotiniku M’ hemm ebda dejta adegwata mill- użu ta ’ aċidu nikotiniku f’ doża għolja f’ nisa tqal.
Animal studies are insufficient with respect to reproductive toxicity (see section 5.3).
Studji fuq l - annimali mhumiex biżżejjed fir- rigward tat- tossiċità riproduttiva (ara sezzjoni 5. 3).
Laropiprant There are no data from the use of laropiprant in pregnant women.
Laropiprant M’ hemm ebda dejta mill- użu ta ’ laropiprant f’ nisa tqal.
Studies in animals have shown reproductive toxicity at high doses of laropiprant (see section 5.3).
Studji fl- annimali wrew tossiċità riproduttiva f’ dożi għoljin ta ’ laropiprant (ara sezzjoni 5. 3).
Lactation Pelzont No studies in lactating animals have been conducted with Pelzont.
Treddigħ Pelzont Ma sarux studji bi Pelzont fuq bhejjem ireddgħu.
A decision on whether to continue/ discontinue breast-feeding or to continue/ discontinue therapy should be made taking into account the benefit of breast-feeding to the child and the benefit of Pelzont to the woman.
Deċiżjoni dwar jekk jitkompliex/ jitwaqqaf it - treddigħ jew jekk titkompliex/ titwaqqaf it- terapija għandha ssir billi jiġi kkunsidrat il- benefiċċju tat - treddigħ għat- tarbija u l- benefiċċju ta ’ Pelzont għall- mara.
Nicotinic acid Nicotinic acid is excreted in human breast milk.
Aċidu nikotiniku L- aċidu nikotiniku joħroġ fil- ħalib tas- sider tal- bniedem.
Laropiprant It is unknown whether laropiprant is excreted in human breast milk.
Laropiprant Mhux magħruf jekk laropiprant joħroġx fil- ħalib tas- sider uman.
Animal studies have shown excretion of laropiprant in milk.
Studji fuq bhejjem urew il- ħruġ ta ’ laropiprant fil- ħalib.
No studies on the effects on the ability to drive and use machines have been performed.
6 Ma sarux studji dwar l- effetti fuq il- ħila biex issuq jew tħaddem magni.
However, when driving vehicles or operating machines, it should be taken into account that dizziness has been reported (see section 4.8).
Madankollu, meta wieħed isuq vetturi jew iħaddem magni, irid iżomm f’ moħħu li ġew irrappurtati każi ta ’ sturdament (ara sezzjoni 4. 8).
4.8 Undesirable effects In clinical trials, over 2500 patients received Pelzont alone or with an HMG-CoA reductase inhibitor.
Fi provi kliniċi, aktar minn 2500 pazjent irċevew Pelzont waħdu jew ma ’ inibitur HMG- CoA reductase.
Adverse reactions have usually been mild and transient.
Ir- reazzjonijiet avversi ġeneralment kienu ħfief u għaddiena.
Flushing Flushing is the most common adverse reaction of Pelzont.
Fawra Il- fawra hija l- aktar reazzjoni avversa komuni ta ’ Pelzont.
Flushing is most prominent in the head, neck, and upper torso.
Il- fawra hija prominenti l- aktar fir- ras, l - għonq u l- parti ta ’ fuq tat- torso.
In a pool of four active- or placebo-controlled clinical trials (N=2548), flushing was reported by the investigator as a possibly, probably, or definitely treatment-related adverse reaction in 12.3% of patients taking Pelzont.
Fi grupp ta ’ erba ’ provi kliniċi attivi jew ikkontrollati bil- plaċebo (N=2548), il- fawra kienet irrappurtata mill- investigatur bħala reazzjoni avversa possibbli, probabbli, jew definittivament marbuta mal- kura fi 12. 3% tal- pazjenti li ħadu Pelzont.
In these studies, the percentage of patients taking Pelzont, nicotinic acid (pooled prolonged-release formulations) or pooled placebo/ simvastatin who discontinued due to any flushing-related symptom (redness, warmth, itching and tingling) was 7.2%, 16.6%, and 0.4%, respectively.
F’ dawn l- istudji, il - perċentwali ta ’ pazjenti li kienu qegħdin jieħdu Pelzont, aċidu nikotiniku (formulazzjonijiet li jerħu l - mediċina bil- mod miġburin f’ daqqa) jew plaċebo/ simvastatin miġburin f’ daqqa li ma komplewx it - trattament minħabba xi sintomu relatat mal- fawra (fawra, sħana, ħakk u tingiż) kien ta ’ 7. 2%, 16. 6%, u 0. 4%, rispettivament.
Discontinuations due to other specific adverse reactions among patients taking Pelzont were infrequent (< 1%).
Il- każijiet ta ’ twaqqif tal- kura minħabba reazzjonijiet avversi speċifiċi oħra fost il- pazjenti li kienu qegħdin jieħdu Pelzont ma kinux frekwenti (< 1%)
7 Overall adverse reactions with Pelzont In addition to flushing, clinical adverse reactions reported by the investigators as possibly, probably, or definitely related to Pelzont in ≥ 1% of patients treated with Pelzont alone (n=947) or co-administered with statin (n=1601) and clinically meaningful adverse reactions (< 1%), for up to one year are listed below.
Reazzjonijiet avversi totali bi Pelzont Minbarra l- fawra, ir- reazzjonijiet kliniċi avversi rrappurtati mill- investigaturi bħala possibbilment, probabbilment, jew definittivament relatati ma ’ Pelzont f’ ≥1% tal- pazjenti trattati bi Pelzont waħdu (n=947) jew mogħti fl- istess ħin ma ’ statin (n=1601) u reazzjonijiet avversi li klinikament huma sinifikattivi (< 1%), sa sena huma elenkati hawn taħt.
The frequencies of adverse reactions are ranked according to the following:
Il- frekwenzi tar- reazzjonijiet avversi huma kklassifikati skond dawn li ġejjin:
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), Very rare (< 1/ 10,000).
Komuni ħafna (≥ 1/ 10), Komuni (≥ 1/ 100 sa < 1/ 10), Mhux komuni (≥ 1/ 1, 000 sa < 1/ 100), Rari (≥ 1/ 10, 000 sa < 1/ 1, 000), Rari ħafna (< 1/ 10, 000).
Adverse reaction elevations in ALT and/ or AST (consecutive, ≥ 3 X ULN), fasting glucose, uric acid (see below)
Sistema ta ’ Klassifika ta ’ l- Organi Investigazzjonijiet
elevations in CK (≥ 10 X ULN), total bilirubin, reductions in phosphorus and platelet counts (see below)
Reazzjoni avversa żidiet fl- ALT u/ jew fl- AST (konsekuttivi, ≥ 3 X ULN), glucose tas- sawm, aċidu uriku (ara taħt) żidiet fil- CK (≥ 10 X ULN), bilirubin totali, tnaqqis fil- fosfru u fl- għadd tal- plejtlits (ara taħt)
Uncommon
Frekwenza Komuni Mhux komuni
Nervous system disorders Gastrointestinal disorders Skin and subcutaneous tissue disorders
Disturbi fis- sistema nervuża Disturbi gastro- intestinali Disturbi fil- ġilda u fit- tessuti ta ’ taħt il- ġilda
dizziness, headache, paraesthesia diarrhoea, dyspepsia, nausea, vomiting erythema, pruritus, rash, urticaria
sturdament, uġigħ ta ’ ras, parasteżija dijarea, dispepsja, dardir, rimettar eritema, ħakk, raxx, urtikarja
flushing
fawra
feeling hot
sensazzjoni ta ’ sħana
Immune system disorders
Disturbi tas- sistema immunitarja
Hypersensitivity reaction (see below)
Reazzjoni ta ’ sensittività eċċessiva (ara taħt)
An apparent hypersensitivity reaction has been reported (< 1%) This is characterised by multiple symptoms that may include: angio-oedema, pruritus, erythema, paraesthesia, loss of consciousness, vomiting, urticaria, flushing, dyspnoea, nausea, incontinence of urine and stool, cold sweats, shivering, chills, increased blood pressure, lip swelling, burning sensation, drug eruption, arthralgia, leg swelling, and tachycardia.
Din hija kkaratterizzata minn bosta sintomi li jistgħu jinkludu: anġjoedema, ħakk, eritema, parasteżija, telfien mis- sensi, rimettar, urtikarja, fawra, dispneja, dardir, inkontinenza ta ’ l- awrina u l- ippurgar, għaraq kiesaħ, rogħda, kesħa, pressjoni tad- demm aktar għolja, nefħa fix- xufftejn, sensazzjoni ta ’ ħruq, eruzzjoni tal- mediċina, artralġja, nefħa fis- sieq, u takikardija.
Investigations Marked and persistent increases of serum transaminases have been reported infrequently (see section 4.4).
7 Investigazzjonijiet Żidiet ċari u persistenti tat- transaminases fis- serum ġew irrappurtati b’ mod mhux frekwenti (ara sezzjoni 4. 4).
In controlled clinical studies, the incidence of clinically important elevations in serum transaminases (ALT and/ or AST ≥ 3 X ULN, consecutive) was 1.0% for patients treated with Pelzont with or without a statin.
Fl- istudji kliniċi kkontrollati, l- inċidenza taż- żidiet kliniċi importanti fit- transaminases fis- serum (ALT u/ jew AST ≥ 3 X ULN, konsekuttivi) kienet ta ’ 1. 0% għall- pazjenti trattati bi Pelzont bi jew mingħajr statin.
These elevations were generally asymptomatic and returned to baseline after discontinuation of therapy or with continued treatment.
Dawn iż- żidiet ġeneralment kienu bla sintomi u reġgħu lura għal- linja bażi wara t- twaqqif tat- terapija jew bi trattament li ssokta.
Clinically important elevations of CK (≥ 10 X ULN) were seen in 0.3% of the patients treated with Pelzont with or without a statin (see section 4.4).
Żidiet kliniċi importanti ta ’ CK (≥ 10 X ULN) dehru f’ 0. 3% tal- pazjenti trattati bi Pelzont bi jew mingħajr statin (ara sezzjoni 4. 4).
As with other nicotinic acid medicinal products, elevations in fasting glucose (a median increase of approximately 4 mg/ dL), and uric acid (mean change from baseline of +14.7%), and reductions in platelet counts (a mean change from baseline of -14.0%) were reported in
Valuri abnormali oħra tal- laboratorju li ġew irrappurtati kienu żidiet fl- LDH, fil- glukożju waqt sawm, fl- aċidu uriku, fil- bilirubina totali, u fl- amylase, u tnaqqis fil- fosfru u fl- għadd tal- plejtlits (ara sezzjoni 4. 4).
8 controlled clinical studies with Pelzont (2000 mg/ 40 mg) (see section 4.4).
Bħal bi prodotti mediċinali oħra ta ’ l- aċidu nikotiniku, żidiet fil- glukożju tas- sawm (żieda medja ta ’ madwar 4 mg/ dL), u aċidu uriku (bidla medja mil- linja bażi ta ’ +14. 7%), u tnaqqis fl- għadd tal - plejtlits (bidla medja mil- linja bażi ta ’ - 14. 0%) ġew irrapportati fi provi kliniċi kkontrollati ma ’ Pelzont (2000 mg/ 40 mg) (ara sezzjoni 4. 4).
In diabetic patients a median increase in HbA1c of 0.2% was observed (where modification of hypoglycaemic therapy was allowed).
F’ pazjenti bid- dijabete, ġiet osservata żieda medja fil - HbA1c ta ’ 0. 2% (fejn modifika ta ’ terapija ipoglimika kienet permessa).
Nicotinic acid-related adverse reactions The following nicotinic acid-related adverse reactions have been seen in clinical trials or post-marketing experience with other nicotinic acid medicinal products at unknown frequency or in clinical trials with Pelzont (or the nicotinic acid component of Pelzont) in < 1% of the patients treated:
Reazzjonijiet avversi relatati ma ’ l- aċidu nikotiniku Ir- reazzjonijiet avversi li ġejjin relatati ma ’ l- aċidu nikotiniku dehru fi provi kliniċi jew fl- esperjenza ta ’ wara t- tqegħid fis- suq ma ’ prodotti mediċinali oħra ta ’ l- aċidu nikotiniku fi frekwenza magħrufa jew fi provi kliniċi ma ’ Pelzont (jew il- komponent ta ’ l- aċidu nikotiniku ta ’ Pelzont) < 1% tal- pazjenti ttrattati:
Atrial fibrillation and other cardiac arrhythmias, palpitations, tachycardia.
Fibrillazzjoni atrijali u arritmiji oħra tal- qalb, palpitazzjonijiet, takikardija.
Migraine, syncope.
Emigranja, sinkope.
Cystoid macular oedema, toxic amblyopia.
Edema makulari taċ- ċistojde, amblijopija tossika.
Respiratory, thoracic, and mediastinal disorders:
Disturbi respiratorji, toraċiċi u medjastinali:
Dyspnoea.
Dispneja.
Abdominal pain, mouth oedema, eructation, peptic ulcer.
Uġigħ addominali, edema fil- ħalq, tifwiq, ulċera peptika.
Acanthosis nigricans, dry skin, hyperpigmentation, macular rash, sweating (night or cold sweat), vesicular rash.
Acanthosis nigricans, ġilda xotta, pigmentazzjoni eċċessiva, raxx makulari, għaraq (bil- lejl jew kiesaħ), raxx vesikulari.
Muscular weakness, myalgia.
Dgħjufija fil- muskoli, uġigħ fil- muskoli.
Impaired glucose tolerance, gout.
Indeboliment tat- tolleranza għall- glukożju, gotta.
Rhinitis.
Rinite.
Hypotension, orthostatic hypotension.
Pressjoni baxxa, pressjoni baxxa ortostatika.
Asthaenia, chills, face oedema, generalised oedema, pain, peripheral oedema.
Astenja, kesħa, edema fil- wiċċ, edema ġeneralizzata, uġigħ, edema periferali.
Angio-oedema, type I hypersensitivity.
Anġjoedema, sensittività eċċessiva tat- tip I.
Jaundice.
Suffejra.
Anxiety, insomnia.
Ansjetà, nuqqas ta ’ rqad.
Pelzont In the event of an overdose, it is reasonable to employ the usual symptomatic and supportive measures.
Pelzont F’ każ ta ’ doża eċċessiva, huwa raġonevoli li jintużaw il- miżuri sintomatiċi u supportivi tas- soltu.
Cases of overdose have been reported; the maximum dose of Pelzont taken was 5000 mg/ 100 mg.
Ġew irrappurtati każi ta ’ doża eċċessiva; l- akbar doża ta ’ Pelzont li ttieħdet kienet 5000 mg/ 100 mg.
All patients recovered without sequelae.
Il - pazjenti kollha rkupraw mingħajr sekweli.
The most commonly reported adverse reactions from the subjects who received this higher dose were consistent with a high dose of nicotinic acid and included: flushing, headache, pruritus, nausea, dizziness, vomiting, diarrhoea, epigastric and abdominal pain/ discomfort, and back pain.
L- aktar reazzjonijiet avversi rrappurtati b’ mod komuni mill- persuni li rċevew din id- doża ogħla kienu konsistenti ma ’ doża għolja ta ’ aċidu nikotiniku u kienu jinkludu: fawra, uġigħ ta ’ ras, ħakk, dardir, sturdament, rimettar, dijarea, uġigħ/ skonfort epigastriku u addominali, u wġigħ fid- dahar.
Laboratory abnormalities included increased amylase and lipase, decreased haematocrit and occult blood in the stool.
L- abnormalitajiet tal- laboratorju kienu jinkludu żidiet fl- amylase u l - lipase, tnaqqis fl- ematokrit u demm moħbi fl- ippurgar.
Nicotinic acid For an overdose of nicotinic acid, supportive measures should be employed.
L- aċidu nikotiniku Għal doża eċċessiva ta ’ aċidu nikotiniku, għandhom jintużaw miżuri supportivi.
Laropiprant During controlled clinical trials in healthy subjects, single doses of up to 900 mg laropiprant and multiple doses up to 450 mg once daily for 10 days were generally well tolerated.
8 Laropiprant Waqt provi kliniċi kkontrollati f’ individwi b’ saħħithom, dożi singoli sa 900 mg laropiprant u dożi multipli sa 450 mg darba kuljum għal 10 ijiem ġeneralment kienu ttollerati sewwa.
There is no experience with doses of laropiprant above 900 mg in humans.
M’ hemmx esperjenza b’ dożi ’ l fuq minn 900 mg fil- bnedmin.
Prolongation of collagen-induced platelet aggregation was observed in subjects taking multiple doses of 300 mg or greater (see section 5.1).
Kienet osservata aggregazzjoni tal- plejtlits indotta mill- collagen imtawla f’ individwi li ħadu bosta dożi ta ’ 300 mg jew aktar (ara sezzjoni 5. 1).
Pharmacotherapeutic group: nicotinic acid and derivatives, ATC code:
Kategorija farmakoterapewtika: aċidu nikotiniku u derivattivi, Kodiċi ATC:
Nicotinic acid lowers the levels of low-density lipoprotein cholesterol (LDL-C), total cholesterol (TC), very low density lipoprotein cholesterol (VLDL-C), apolipoprotein B (apo B, the major LDL protein), triglycerides (TG), and lipoprotein(a) (Lp(a), a modified LDL particle) and elevates the levels of high-density lipoprotein cholesterol (HDL-C) and apolipoprotein A-I (apo A-I, the major protein component of HDL).
Pelzont fih l- aċidu nikotiniku, li f’ dożi terapewtiċi huwa sustanza li timmodifika l- lipidi, u laropiprant, antagonist selettiv b’ saħħtu tar- riċettur tal- prostaglandin D2 (PGD2) sottotip 1 (DP1). L- aċidu nikotiniku jbaxxi l- livelli tal- kolesterol ta ’ lipoproteini ta ’ densità baxxa (LDL- C), tal- kolesterol totali (TC), tal- kolesterol ta ’ lipoproteini ta ’ densità baxxa ħafna (VLDL- C), ta ’ l- apolipoproteina B (apo B, il- proteina LDL prinċipali), tat- trigliċeridi (TG), u tal- lipoproteina( a) (Lp( a), partikula LDL modifikata) u jgħolli l- livelli tal- kolesterol ta ’ lipoproteini ta ’ densità għolja (HDL- C) u ta ’ l - apolipoproteina A- I (apo A- I, il- komponent prinċipali ta ’ proteina ta ’ l- HDL).
Laropiprant suppresses PGD2 mediated flushing associated with administration of nicotinic acid.
Laropiprant irażżan il - fawra medjata minn PGD2 assoċjata ma ’ l- għoti ta ’ l- aċidu nikotiniku.
Laropiprant has no effect on lipid levels nor does it interfere with the effects of nicotinic acid on lipids.
Laropiprant m’ għandu l- ebda effett fuq il- livelli tal- lipidi u lanqas ma jinterferixxi ma ’ l- effetti ta ’ l- aċidu nikotiniku fuq il- lipidi.
Nicotinic acid Mechanism of action The mechanisms by which nicotinic acid modifies the plasma lipid profile are not fully understood.
Aċidu nikotiniku Il- mod kif jaħdem Il- mekkaniżmi li bihom l- aċidu nikotiniku jimmodifika l- profil tal- lipidi fil- plasma mhuwiex mifhum kompletament.
Nicotinic acid inhibits release of free fatty acids (FFA) from adipose tissue, which may contribute to the reduced plasma LDL-C, TC, VLDL-C, apo B, TG, and Lp(a), as well as elevated HDL-C, and apo A-I, all of which are associated with lower cardiovascular risk.
L- aċidu nikotiniku jimpedixxi r- rilaxx ta ’ aċidi grassi ħielsa (FFA – free fatty acids) mit- tessut xaħmi, li jista ’ jikkontribwixxi għat- tnaqqis fl- LDL- C, TC, VLDL- C, apo B, TG, u Lp( a) fil- plażma, kif ukoll għaż- żieda fl- HDL- C, u l- apo A- I, li kollha huma assoċjati ma ’ riskju kardjovaskulari aktar baxx.
Additional explanations that do not invoke plasma FFA reduction as the central driver of lipid profile modification include nicotinic acid-mediated inhibition of de novo lipogenesis or esterification of fatty acids into TG in the liver.
Spjegazzjonijiet oħra li ma jinvokawx it- tnaqqis tal- FFA bħala l- fattur prinċipali tal- modifika tal- profil tal- lipidi jinkludu l- inibizzjoni medjata mill- aċidu nikotiniku tal - lipoġenesi de novo u l- esterifikazzjoni ta ’ l- aċidi grassi għal TG fil- fwied.
Pharmacodynamic effects Nicotinic acid causes a relative shift in the distribution of LDL subclasses from small, dense (most atherogenic) LDL particles to larger LDL particles.
Effetti farmakodinamiċi L- aċidu nikotiniku jikkawża ċaqliq relattiv fid- distribuzzjoni tas- sottokategoriji ta ’ LDL minn partikoli żgħar u densi (l- aktar ateroġeniċi) għal partikoli LDL akbar.
Nicotinic acid also elevates the HDL2 subfraction to a greater extent than the HDL3 subfraction, thereby increasing the HDL2: HDL3 ratio, which is associated with decreased cardiovascular disease risk.
L- aċidu nikotiniku jgħolli wkoll is- sottofrazzjoni ta ’ l- HDL2 għal livell ogħla mis- sottofrazzjoni HDL3, u b’ hekk iżid il- proporzjon HDL2: HDL3, li huwa assoċjat ma ’ tnaqqis fir- riskju ta ’ mard kardjovaskulari.
HDL is hypothesised to participate in the transport of cholesterol from tissues back to the liver, to suppress vascular inflammation associated with atherosclerosis, and to have anti-oxidative and anti-thrombotic effects.
Huwa ipotizzat li l- HDL jipparteċipaw fit- trasport tal- kolesterol mit- tessuti lura lejn il- fwied, li jrażżnu l- infjammazzjoni vaskulari assoċjata ma ’ l- aterosklerosi, u li għandhom effetti anti- ossidattivi u anti- trombotiċi.
Like LDL, cholesterol-enriched triglyceride-rich lipoproteins, including VLDL, intermediate-density lipoproteins (IDL), and remnants, can also promote atherosclerosis.
Bħal- LDL, il- lipoproteini rikki fit- trigliċeridi miżjuda bil- kolesterol, fosthom il- VLDL, il- lipoproteini ta ’ densità intermedja (IDL), u l- fdalijiet jistgħu wkoll jippromwovu l- aterosklerosi.
Elevated plasma TG levels are frequently found in a triad with low HDL-C levels and small LDL particles, as well as in association with non-lipid metabolic risk factors for coronary heart disease (CHD).
Livelli għoljin ta ’ TG fil- plażma sikwit jinstabu fi trijade ma ’ livelli baxxi ta ’ HDL- C u partikoli żgħar ta ’ LDL, kif ukoll flimkien ma ’ fatturi ta ’ riskju metaboliċi mhux lipidi għal mard tal- qalb koronarju (CHD).
Treatment with nicotinic acid reduces the risk of death and cardiovascular events, and slows progression or promotes regression of atherosclerotic lesions.
It- trattament bl- aċidu nikotiniku jnaqqas ir- riskju ta ’ mewt u episodji kardjovaskulari, u jrażżan il - progressjoni jew itejjeb ir- rigressjoni tal- leżjonijiet aterosklerotiċi.
The Coronary Drug Project, a five year study completed in 1975, showed that nicotinic acid had a statistically significant benefit in decreasing nonfatal, recurrent myocardial infarctions (MI) in men 30 to 64 years old with a history of MI.
Il- Proġett tal- Mediċina Koronarja, studju ta ’ ħames snin li tlesta fl- 1975, wera li l- aċidu nikotiniku kellu benefiċċju statistikament sinifikanti fit- tnaqqis ta ’ l- infarti mijokardijaċi (MI) rikorrenti mhux fatali f’ irġiel ta ’ bejn 30 u 64 sena bi storja ta ’ MI.
Though total mortality was similar in the two groups at five years, in a fifteen-year cumulative follow-up there were 11% fewer deaths in the nicotinic acid group compared to the placebo cohort.
Għalkemm il- mortalità totali kienet simili fiż- żewġ gruppi wara ħames snin, fl- istudju kumulattiv ta ’ wara (cumulative follow- up) li dam għaddej ħmistax- il sena kien hemm 11% anqas imwiet fil- grupp ta ’ l- aċidu nikotiniku meta mqabbel mal- grupp tal- plaċebo.
10 Laropiprant Mechanism of action Nicotinic acid-induced flushing is mediated primarily by release of prostaglandin D2 (PGD2) in the skin.
9 Il- fawra indotta mill- aċidu nikotiniku hija medjata primarjament mir- rilaxx tal- prostaglandin D2 (PGD2) fil- ġilda.