
dalphopristine

dalphopristine anedi ostrogrisin eah (virginiamycin emm, prestinamycin aiya, streptogramine eah) yokka semee-synthetic streptogramine antibiatic analog. quinupristine/dalphopristine kalayika (synersid anae vaanijya paerutoe vikrayinchabadindi) nuu 1999loe rone-poulenk roarer pharmaceuticals marketloki teesukuvacchindi. synersid (30 saatam quinupristine nundi 70 saatam dalphopristine baruvu nishpatti) nuu staphylocosi mariyu vanacomycin-nirodhaka "enterococcus facium" dwara infectionlaku chikitsa cheyadaaniki upayogistaaru.
samslaeshanha.
2-pyroline samuuhaaniki diethylaminoethythylnol jodinchadam dwara mariyu austriogrisin eah yokka sulfate yokka aakseekarana dwara, nirmanatmakamga marinta hydrophobic sammelanam erpadutundi. eee hydrophobic sammelanam uppu erpadataaniki andubaatulo unde takshana ayaneekaranam cheyagala samuuhaanni kaligi untundi.
pedda ettuna tayari.
dehydropoline ring yokka samyojita double baand meeda 2-diethylaminoethethiol yokka stereoselective maikhel-rakam jodimpunu saadhinchadam dwara dalphopristine prestinamycin aiya nundi samslaeshanha cheyabadutundi. 
. kanugonabadina modati paddhati ruthenium dioxidetho anubandhinchabadina sodiyam peeriyadetnu upayoginchi sulfur utpannaanni sulfonga neerugaa aakseekarinchadam. ayithe, 2-dasha maadhyamamlo sodiyam tungstate hydrogen peroxidenu upayoginchadam merugaina digubadini utpatti chestundi, anduvalla idhi pedda ettuna utpattiki empika chese paddhati.
quinupristine/dalphopristine yokka dalphopristine bhaagam utpatti acetone draavanaala nundi quinupristine mariyu dalphopristine yokka suddeekarana cochrystalization dwara saadhinchabadutundi.
antimicrobial activity.
okkate, dalphopristine mariyu quinupristine rendoo kooda vitro bacteriatic karyakalapalalo niraadambaramgaa untaayi. ayithe, rendu streptogramminlu kalipinappudu aneka gram-positive bacteriaku vyatiraekamgaa vitro bacteriadidal charyalo 8-16 retlu ekkuvagaa kanipistundi. 
. quinupristine/dalphopristine stephylocosy mariyu vanacomycin-resistant enterococcus facianiki vyatiraekamgaa prabhaavavantamgaa undagaa, inn vitro adhyayanalu anni jaatulu mariyu saadhaarana gram-positive bacteria jaatulaku vyatiraekamgaa bacteriadroha karyakalapalanu pradarsinchaledu.
charya yokka yantraangam.
dalphopristine mariyu quinupristine rendoo ribosome yokka 50la upabhaagamlo unna pradaesaalatoe bandhistaayi. prarambha dalphopristine binding phalitamgaa ribosome yokka conformational maarpu vastundi, idhi quinupristine dwara bindingnu penchadaaniki anumatistundi. rendu mandulanu kalisi upayoginchinappudu sthiramaina aushadha-ribosome sanklishtata erpadutundi. eee sanklishtata peptide-golusu erpadataanni nivaarinchadam dwara mariyu kottagaa erpadina peptide golusula velikiteetanu nirodhinchadam dwara protein samshlaeshanhanu nirodhistundi. chaalaa sandarbhaallo, idhi bacteria kanaala maranaaniki daariteestundi.
pratighatana yokka vidhanam.
streptogramine nirodhakata anedi enzymatic aushadha nishkriyaatmakata, efflux ledhaa sell nundi aushadham yokka kriyaaseela ravana dwara madhyavartitvam cheyabadutundi mariyu saadhaaranamgaa, ribosomal lakshya binding saitlalo conformational maarpulu. dalphopristine-nishkriyaatmaka acetyl transferes ledhaa quinupristine-nishkriyaatmaka hydroless utpatti dwara stephylococcal mariyu enterococcal jaatulalo enzymatic aushadha nishkriyaatmakata sambhavinchavachhu. kogulas-negative staphylocosi mariyu enterococcus faciumlo eee aushadham yokka efflux ledhaa kriyaaseela ravana sambhavinchavachhu. quinupristinlo matrame nirodhakathatho staphylocosylo constitutive ribosome savarana kanipinchindi.
dalphopristineku pratighatananu oke mutation point dwara ivvavacchu, quinupristine/dalphopristine aushadha nirodhakatanu andinchadaaniki dalphopristine mariyu quinupristine bhaagaalanu lakshyamgaa chesukuni bahula utparivartana paayintlu avasaramayye prayojanaanni andistundi. tulanaatmakamgaa, fraanslo sekarinchina stephylococcal isolates yokka 2-5% matrame 35 samvatsaraala viniyogamlo sambandhita streptogramine, prestinamycincu nirodhakatanu chuuputaayi.
aushadha paraspara charyalu.
dalphopristine mariyu quinupristine rendoo vistrutamgaa hepaticga metabolize cheyabadataayi, malam nundi visarjinchabadataayi mariyu cytochrome p450 (saip) 3a4 enjaim maargaaniki nirodhakam vale panicheestaayi. saip3eah4 maargam dwara jeevakriya cheyabadina mandulatho sahabaddhamaina vaadakamtho jaagratta vahinchaali. cyclosporin thoo quinupristine/dalphopristine yokka 2-5 rojula paatu upayoginchadam valla cyclosporin sthaayilu rendu retlu perugutaayani telindi.
hepatic balaheenata unna rogulalo etuvanti pratikuula prabhavalu kanipinchaledu mariyu eee roogi janabhalo quinupristine/dalphopristine motaadunu tagginchadaaniki tayaareedaaru sifaarsulu cheyaledu.
vaanijyeekarana.
dalphopristine yokka niyantrana mariyu vaanijyeekarana charitraku sambandhinchi takkuva samacharam andubaatulo unnappatikee, rone-poulencrorer pharmaceuticals tayaaru chesina synersid (quinupristine/dalphopristine), 1999loe vanacomycin nirodhaka enterococcus facium mariyu sanklishtamaina charmam mariyu charma nirmaana infectionla chikitsa kosam ive injectionga aamodinchabadindi. dalphopristine nuu vividha rasayana tayaareedaarula nundi internetlo matrame macillate uppugaa konugolu cheyavachu.

