
lercanidipine

lercanidipine (vyaapaaranaamam sanidip, mattullavaykkoppam) oru antihypertensive (rakthasammardham kuraykkunnathu) marunnaan. ithu kaalsyam chaanal blockerukalude dihydropyridine vibhaagathil pedunnu, ithu rakthakkuzhalukal vishramikkukayum thurakkukayum cheiyunnathu rakthathe sareerathinu chuttum kooduthal swathanthramaayi sanjarikkaan anuvadikkunnu. ithu rakthasammardham kuraykkukayum hridayathe kooduthal kaaryakshamamaayi pravartthikkaan anuvadikkukayum cheiyunnu.
pazhaya dihydropyridinukale apekshichu eee marunnu valare pathukkeyaanu pravartthikkunnathu. ithinu prathikoola phalangal kuravaayirikkaam, pakshe mayakkumarunnu edapedalukalkku thaarathamyena uyarnna saadhyathayund.
1984ll pettant nediya ithu 1997ll vaidyashaasthraparamaaya upayogathinu amgeekarikkappettu.
medical upayogangal.
avashya rakthaathimardhathinte (uyarnna rakthasammardham) chikilsaykkaayi lercanidipine upayogikkunnu.
vrukka prasnangalulla hypertensive rogikale chikilsikkunnathil lercanidipine oru nalla ejantaanennu thonnunnu.
ethirvashangal.
mattu dihydropyridinukaleppo, asthiramaaya aanjina pectories, aniyanthrithamaaya hridayasthambhanam, myocardial infarction kazhinju taamasiyaathe, idathu ventricular puranthallal thadassamulla rogikalil lercanidipine virudhamaayi kaanapedunnu. garbhaavasthayilum garbhinikalaayirikkaavunna sthreekalilum ithu virudhamaanu, kaaranam garbhasthashishuvinte surakshayekkurichulla daattayum athupole thanne karal, vrukkasambandhamaaya gurutharamaaya vaikalyamulla rogikalilum illa.
karal ensaimaaya saip3eiii4-nte sakthamaaya inhibittarukalumaayo immunosaprasant marunnaaya siklosporin-maayo marunnu samyojippikkaruth.
prathikoola phalangal.
lercanidipine pothuve nannayi sahikkappedunnu; eee marunnu upayogichu chikilsikkunna oru sathamaanathiladhikam rogikalil orotta prathikoola phalavum nireekshikkappettilla. thalavedana, thalakarakkam, tachycardia (hridayamidippu), hridayamidippu, flush, edema enniva ulppedunna eee classile mattu marunnukalkk samanamaaya paarshwafalangalaanu saadhaarana paarshwafalangal. 10, 000 peril oraalil thaazhe rogikalil hypersensitivity prathikaranangal sambhavikkunnu.
nephedipine polulla aadya thalamura dihydropyridinukalumaayi thaarathamyappeduthumbol lercanidipin keezhil eedemakal valare kuravaanu. mattu paarshwafalangalkku, daatta anishchithathvathilaanu lercanidipine aadya thalamura marunnukalumayi thaarathamyam cheytha oru padanatthil thalavedanayudeyum flushinteyum aavruthiyilum vyathyasamonnum kandethiyilla, ennaal amlodipin, phelodipin allengil nitrendipine (kuranjathu randaam thalamura) ennivayil ninnu lercanidipine (kuranjathu randaam thalamura) lake maarunnath mattoru padanatthil paarshwafalangal ganyamaayi kurachu.
amithamaya alavil.
saadhaarana chikitsa dosinte 80 madangu vare amithamaayi kazhikkunnathayi vivarichittundu. prathekshikkunna lakshanangalil kadinamaaya hypotension (thaazhnna rakthasammardham), reflex tachycardia enniva ulppedunnu. hridayathinte autrioventricular nodil kaalsyam chaanalukal thadassappedunnathu moolavum brady cardia (mandagathiyilulla hridayamidippu) sambhavikkam. rakthasammardhavum hridayathinte pravartthanavum nireekshikkukayallathe chikilsayilla. rakthathile plasma proteinukalumaayum koshangalude lipid membranukalumaayum bandhappettirikkunnathil lercanidipininte bhooribhaagavum phalapradamallaathathaanu.
ashayavinimayam.
karal ensime saip3eiii4 eee padaarthatthe upapachayam cheiyunnu. oru padanatthil, sakthamaaya saip3eiii4 inhibittar kettokanasol lercanidipininte paramavadhi raktha plasma saandrata ettu gadakavum vakrathinu keezhilulla pradesham 15 gadakavum vardhippichu. mattoru padanatthil, ore samayam nalkumbol siklosporin lercanidipine plasmayude alavu moonnirattiyaakki. eee ensaiminte mattu inhibittarukalaaya itraconasol, erythromycin, grapefruit jyoos ennivayum plasmayude saandrata vardhippikkumennum angane antihypertensive prabhavam vardhippikkumennum prathekshikkunnu. neremarichu, carbamasepine, refampicin, sent johns vortt thudangiya saip3eiii4 inductorukal orupakshe plasmayude alavum lercanidipininte falapraptiyum kuraykkunnu. thaarathamyappeduthumbol, saip3eiii4 madhyastha edapedalukalkulla saadhyatha amlodipinu kuravaanu.
lercanidipine siklosporin, degoxin ennivayude plasmayude alavu vardhippikkunnu.
farmacology.
pravartthana samvidaanam.
mattu dihydropyridine klaas kaalsyam chaanal blokkarukaleppole, lercanidipine rakthakkuzhalukalude minusamarnna peshi koshangalile ell-type kaalsyam chaanalukale thadayukayum avaye vishramikkukayum angane rakthasammardham kuraykkukayum cheiyunnu. noonn-dihydropyridine kaalsyam chaanal blockermaraya verapamil, dilttiyasem ennivayil ninnu vyathyasthamayi, ithu autrioventricular nodile kaalsyam chaanalukalil ganyamaayi pravarthikkunnilla, athinaal saadhaarana chikitsa dosukalil hridayamidippu kuraykkunnilla.
pharmacokinetics.
lercanidipine pathukke ennaal kudalile poornnamaayum agiranam cheyyappedunnu. vipulamaaya phastt paas prabhavam kaaranam ithinu motham 10 sathamaanam jaiva labhyathayund, allengil kozhupulla bhakshanathinu sesham kazhichaal 40 sathamaanam vare. rakthathile ettavum uyarnna plasmayude alavu 1.5 muthal 3 manikkoorin sesham athunnu. eee padaartham tissukalilekku vegathil vitharanam cheyyukayum lipid membranukalumaayi bandhippikkukayum avide athu oru dippo roopappedukayum cheiyunnu. rakthachamkramana bhinnasankhya eathaandu poornnamaayum (> 98 sathamaanam) plasma proteinukalumaayi bandhappettirikkunnu.
ithu karalil poornnamaayum metabolise cheyyappedunnu, pradhaanamaayum saip 3 eiii 4 vazhi. elemination ardhaayuss 8 muthal 10 manikkoor vareyaanu, marunnu shekharikkunnilla. dippo prabhavam kaaranam, antihypertensive pravartthanam kuranjathu 24 manikorengilum neendunilkkum. 50 sathamaanavum moothrathiloode puranthallappedunnu.
rasathanthram.
alpam manja niratthilulla kristalin podiyaaya hydrochloridinte roopathilaanu lercanidipine upayogikkunnathu, ithu kristtal roopathil i allengil kristtal roopathil urukunnu. ithu chlorophomilum methanol eluppathil layikkunnu, pakshe praayogikamaayi vellathil layikkunnilla. eee uyarnna lipophilisity (pazhaya dihydropyridinukalumaayi thaarathamyappeduthumbol) manahpoorvvam ullathaanu, kaaranam ithu padaartham lipid membranukalumaayi bandhippikkukayum deerghakaala pravartthanam anuvadikkukayum cheiyunnu.
lercanidipine thanmaathraykk oru asamamaya kaarban aattamund. s"-enantiomer "r"-enantiomarinekkaal kooduthal phalapradamaanenkilum, vipananam cheytha formulationukalil randinteyum 1:1 misritham adangiyirikkunnu (i.iii., racemate).
shareerathile draavakangalil kandethal.
liqvid chromatography-maas spectrometry reethikaliloode lercanidipininte raktha plasmayude saandrata kandethanakum.

