Ngaba i-buprenorphine ikamva lonyango lwangaphantsi?
Ubunzima bomntu, ubunzima be-opioid kunye nobuhlungu obungapheliyo buchasene ngqo. Nangona i-CDC ibonisa ukuba "ubungqina bonyango lwe-opioid lwangexesha elide ngaphandle kokunyamezeleka okungapheliyo ngaphandle kokunyamekela kokuphela komsebenzi kuhlala kungaphelelanga, kungabikho ubungqina obunelungelo lokufumana iingenelo zexesha elide ngokubhekiselele kwonyango lwama-opioid," inyaniso ihlala i-opioids ukungenelela kwinqununu ekwenzeni unyango olungapheliyo.
Nangona ababoneleli bokunakekelwa ngokusisiseko banokwenza i-opioids yeentlungu ezingapheliyo, abanqwenela ukwenza njalo ngenxa yokwesaba ukugqithisa isigulane okanye ukuxhomekeka. Uninzi lwamagqirha enyango oluphambili lufumana ithemba lokunika izigulane ii-opioids ixesha elide kakhulu elixinezelekileyo kwaye ngokukhawuleza zibhekise ezi gulane kwiingcali zentlungu.
Nangona ukungafuni ukunyanga, ubuhlungu obungapheliyo buya rhoqo. Ngo-2010, iipesenti ezingama-31 zamaMerika zafumana ubuhlungu obungapheliyo, obuchazwa njengentlungu ehlala ngaphezu kweenyanga ezintathu ukuya ezintandathu. Ngenxa yokuba uninzi lwabantu abaneentlungu ezingapheliyo zifumaneka kumaziko oonyango olusisiseko, kuya kuba yintlupheko xa sineendlela ezikhuselekileyo kunye nesebenzayo kwii-opioids-ezinye iyeza eziya kuthi zizigulane zizivelele. Iyeza elibizwa ngokuba yi-buprenorphine ngolunye usuku luza kuncedisa eli bhili-mali.
Yintoni iBuprenorphine?
I-Buprenorphine ingowesigaba sezilwanyana ezibizwa ngokuba yi-opioid ekhethekileyo-i-agonist-antagonists.
Ukongezelela kwesinye isiyobisi esibandakanya i-buprenorphine kunye ne-naloxone (i-Suboxone), i-buprenorphine isetyenziselwa ukwelashwa kwe-opioid ukunyathela ukuxhomekeka kwe-opioid (kuxhomekeke kwi-heroin okanye kwiidakamizwa zonyango). La machiza asebenza ngokuthintela iimpawu zokuxotha xa umntu oxhomekeke kwi-opioids eyeka ukuthatha i-opioids.
I-Buprenorphine iyisiphumo se-opioid semisynthetic ye-opium alkaloid thebaine, efumaneka kwi-opium poppy ( uPapaver somniferum ). Ngokuqinisekileyo kuthatha amashumi eminyaka ukuba abaphandi baqulunqe izidakamizwa, kwaye kwakukho iinzame ezininzi ezahlulekayo ngaphambi kokuba inkampani yeNgesi yenze imveliso ngo-1966. Ngowe-1978, ukuqulunqwa kwe-buprenorphine kwangeniswa ngokulandelelana, kulandelwa yelwimi elincinci (lisetyenziswe phantsi kolwimi) iteration ngowe-1982. Ngowe-1985, i-buprenorphine yaziswa e-United States njenge-opioid analgesic.
Ingaba isebenza kanjani
I-Buprenorphine ineendlela ezichanekileyo zesenzo ezenza kube lula ukuba kusebenze ukuxhomekeka kwe-opioid kodwa mhlawumbi ubuhlungu obungapheliyo, kwakhona.
Okokuqala, i-buprenorphine inomlinganiselo ophezulu wokubophelela kwi-μ-opioid receptor, ejongene nokukhululeka kwentlungu. Ngaphezu koko, i-buprenorphine inezinga elincinci lokuhlukana ukusuka kwi-μ-opioid receptor, oku kuthetha ukuba ihlala iqhotyoshelwe ixesha elide kumlamkeli, kwaye iyenze igalelo elide.
Okwesibini, nangona i-buprenorphine ithanda i-μ-opioid receptor ngokukodwa, isebenza nje ngokuba yi-μ-opioid receptor agonist, oku kuthetha ukuba ngelixa i-buprenorphine ikhusela i-opioid, i-action yayo ayinamandla ngaphezu kwe-opioids.
Okwesithathu, i-buprenorphine yinto epheleleyo ye-opioid receptor antagonist.
Ukuqaliswa kweziphumo ze-κ-opioid receptor kwimiphumo ye-opioids. Ngamanye amazwi, i-buprenorphine ayiyi kuyenza "phezulu."
Lawulo
Njengoko kushiwo ngaphambili, i-naloxone idla ngokudibanisa ne-buprenorphine ngendlela ye-Suboxone. I-Naloxone i-short-acting actor, opioid receptor antagonist. Xa zidibaniswe kumanqanaba aphantsi kunye ne-buprenorphine, i-naloxone inokumelana nemiphumo eyingozi ye-opioid-kuquka ukucindezeleka okuphefumulayo, ukudibanisa, kunye ne-hypotension-ngaphandle kokunciphisa i-analgesia, okanye ukukhululeka kwentlungu. Ukongezelela, ukongezwa kwe-naloxone kwi-buprenorphine kusebenza njengonqanda ukusetyenziswa kakubi kweziyobisi.
Ngokutsho kweNIH:
I-Buprenorphine iza njengepilisi yecala. Ukuhlanganiswa kwe-buprenorphine kunye ne-naloxone kuza njengephilisi yecala (Zubsolv) kunye nefilimu engaphantsi (i-Suboxone) ukuthatha phantsi kweelwimi kunye ne-buccal [cheek] ifilimu (i-Bunavail) ukuyifaka phakathi kwegum kunye nehlathi.
I-Buprenorphine iphinda ifike kwi-patch transdermal, i-formulation intravenous, kwaye, ngoku kutshanje, i-spray spray. NgoDisemba 2017, kwaziswa ukuba i-FDA ihlaziya ukuhlalutya ngokutsha kwenkcazo epheleleyo yokunyanga iintlungu.
Imiphumela
Nangona kungabi nengozi njenge-opioids, zombini i-buprenorphine kunye ne-Suboxone ingaba nemiphumo emibi echaphazelekayo kuquka oku kulandelayo:
- Umqolo obuhlungu
- Umbono ongezantsi
- Ukutyunjwa
- Unzima ngokulala
- Umlomo onzima
- Intloko
- Intlungu yesisu
- Intlungu
Iziphumo ezibi kakhulu, ezifana nobunzima bokuphefumula okanye ukuvuvukala komlomo okanye ulwimi, zifuna unyango olusondeleyo. Kubaluleke kakhulu, ukuxuba i-buprenorphine kunye nezinye iziyobisi ezinjenge-benzodiazepines zingabhubhisa.
Buprenorphine for Pain Pain
Kuhlalutyo oluchanekileyo olushicilelwe ngoDisemba 2017, i-Aiyer kunye nabalobi babambisene bahlola ukuphumelela kwe-buprenorphine ekulawuleni ubuhlungu obungapheliyo. Abaphandi bahlalutya iilingo ezingama-25 ezilawulwa ngandlela-thile ezibandakanya amaqhinga amahlanu e-buprenorphine:
- Buprenorphine engabonakaliyo
- Buprenorphine
- I-buprenorphine / i-naloxone (i-Suboxone)
- Buccal buprenorphine
- Uhlobo lwe-transpermal buprenorphine
Ngokubanzi, abaphandi bafumene ukuba uphando lwe-14 kwe-25 lucebise ukuba i-buprenorphine nayiphi na indlela yokuqulunqa yayiphumelele unyango lweentlungu ezingapheliyo. Ngokukodwa, izifundo ezili-10 kwezi-15 zabonisa ukuba i-transdermal buprenorphine iyasebenza, kwaye izifundo ezimbini zintathu zibonise ukuba i-buccal buprenorphine iyasebenza. Kuphela kwezifundo ezintandathu kuphela kuboniswe ukuba i-buprenorphine okanye i-intravenous buprenorphine yayisebenzisekile unyango lweentlungu ezingapheliyo. Kubaluleke kakhulu, akukho miphumo embi kakhulu echazwe kuyo nayiphi na yezifundo, ezibonisa ukuba i-buprenorphine iphephile.
Ngo-2014, abaCote kunye nababhali-mbhalisi bashicilele ukuhlaziywa okucwangcisiweyo ekuhloliseni ukuphumelela kwe-buprenorphine engaphantsi kwonyango lwentlungu engapheliyo. Nangona uninzi lwazo zihlolisise zihlolisise kwaye zincinci, abaphandi bafumene ukuba i-buprenorphine yesigxina yayiphumelele ekuphatheni ubuhlungu obungapheliyo. Kuyabonakala ukuba, abalobi be-Cote kunye nababambisene nabo bahlanganisa uluhlu olulandelayo lwezibonelelo ezinokwenzeka ze-buprenorphine:
- Ukwenyuka okwenziweyo kwintlungu e-neuropathic ngenxa yeprofayili yayo ekhethekileyo.
- Ukunciphisa ukusetyenziswa kwabalupheleyo kunye nokukhubazeka kwemithwaba ngenxa yempembelelo encinci kwi-half-life and metabolites.
- Ukunciphisa ubuncinane be-immunosuppression xa kuthelekiswa ne-morphine kunye ne-fentanyl ngokusekelwe kubungqina obuncinci obuvela kumsebenzi wesikhokelo kunye nekliniki.
- Isiphumo sokufakwa kwesicindezelo sokuphefumula xa sisetyenziswe ngaphandle kwezinye iimbandezelo zesistim se-nervous, mhlawumbi ngenxa yokuba umsebenzi wangaphakathi wokuvelisa i-analgesia ingaba ngaphantsi kweyokuphefumula okuphefumulayo.
- Impembelelo encinci kwi-hypogonadism, njengoko kuboniswe kwipilisi yesondlo.
- Ukuphuhliswa okuphantsi kokunyamezela, mhlawumbi ngokusebenzisa ukuphikisana kwama-kappa okanye i-opioid-receptor-like (ORL-1) i-agonism.
- Impembelelo ye-antihyperalgesic, mhlawumbi ngenxa yokuchasana kwe-kappa okanye i-ORL-1 agonism.
- Impembelelo yokuxhatshazwa kwezigulane ezingaphenduliyo unyango oluqhelekileyo.
Okuthakazelisayo, ixhomekeke ukuba ngenxa yeendawo zayo ezibophayo, i-buprenorphine inokukwazi ukunceda abantu abafumana i-hyperalgesia-eyabangela i-opioid.
Kwinqaku ebizwa ngokuthi "Uhlolo olubanzi lwe-hyperalgesia," u-Lee kunye nabalobi be-co-o-hyperlageia abanjelwe i-opioid njengale ilandelayo:
I-hyperalgesia (i-OIH) eyenziwa ngama-opioid ichazwa njenge-state of nociceptive sensitization ebangelwa ukugqithiselwa kwi-opioids. Le meko ibonakaliswa yimpendulo eyimpendulo apho isigulane esifumana i-opioids kunyango lwentlungu ingaba yinkxalabo ethile kwizinto ezithile ezibuhlungu. Uhlobo lweentlungu ezinokuthi lunokufana nolunokuba lubuhlungu okanye luyahlukahluka kwiintlungu zangaphambili. I-OIH ibonakala iyinto ecacileyo, ecacileyo kunye neyophawu elingazichaza ukulahlekelwa kwe-opioid ngempumelelo kwezinye izigulane.
Ingqalelo, intlungu ye-nociceptive yintlungu ebuhlungu ebangelwa umonakalo kwinxalenye yomzimba. Kucatshulwa ukuba i-buprenorphine inempahla ye-antinociceptive.
Kwinqaku le-2014 elipapashwe kwi- Anesthesiology , uKhen kunye nababhali-mbhali babhale oku kulandelayo:
I-Buprenorphine iboniswe ukuba iguqule i-hyperalgesia eyenziwe ngama-opioid ngokusebenzisa 'u-antinociception' owenziwe yi-buprenorphine. Ngaphezu koko, i-buprenorphine yintlanzi ye-κ-receptor kwaye inokukhuphisana nempembelelo yedynorphin, i-κ-receptor agonist. Ngenxa yokuba umgogodla we-spinal dynorph ukwandiswa emva kokubonakala kwe-opioid kwaye unomdla kwi-OIH, le mpu melelo ye-buprenorphine kwisayithi yokubopha i-κ-receptor inganciphisa umphumo we-spinal dynorphin obangela ukuhla kwe-OIH.
Ukuchaza iBuprenorphine
Kwinqanaba elilinganiselwe, eUnited States, buprenorphine sele isetyenziselwa ukunyanga intlungu. I-Suboxone inqunyulwe ngaphandle-ilebula yokunyangwa kwentlungu engapheliyo. Ukongezelela, i-pdermal buprenorphine ipatch iyatholakala ekwenzeni unyango olungapheliyo eMelika.
Nangona kunjalo, akukho mbono malunga nokusebenza kwe-buprenorphine kule njongo. Okwangoku, izifundo ezimbalwa ezihlola umphumo we-buprenorphine kwiintlungu ezingapheliyo zihluke kakhulu kwiindlela zabo, kwaye kunzima kakhulu ukuthelekisa omnye nomnye.
Ngaphambi kokuba umrhumo we-buprenorphine unyango lweengxaki ezingapheliyo ziba ngumkhwa wesiseko, imicimbi eyahlukeneyo iya kufuneka ixazululwe. Ngokomzekelo, izifundo zangoku zisebenzisa iintlobo ezahlukeneyo zezilingo xa zivavanya ukusebenza ngendlela enjalo ngokunika uhlalutyo olungavumelaniyo. Izikali zokulinganisa ubuhlungu kwizifundo zokuhlola i-buprenorphine ziza kufuneka zilungiswe. Ukongezelela, izicwangciso zolawulo kunye nendlela yokulawula kuya kufuneka ukuba ihlolwe ngeentetho ezahlukeneyo zentlungu engapheliyo.
Ukuba umyalelo we-buprenorphine wokuba ubuhlungu obungapheliyo buye waba ngubuchule-obusekelwe, oogqirha bokunakekelwa ngokusisiseko babeya kubongwa ngokukodwa kulo mkhuba. Ngo-2000, uMthetho weMithi yoLwaphulo lweMilutha yase-United States wenziwe ngokomthetho kumagqirha okunyamekela okuphambili ukubonelela ngonyango lwama-opioid endaweni yokusebenzisa iShedyuli III, IV, kunye neV. Ngo-2002, i-FDA yamkela unyango lwegulane nge-buprenorphine, ibonakalisa njengesilwanyana seShedyuli III.
Yonke into yokuba ugqirha oyintloko oyinyango kufuneka ayenze ukuze akwazi ukunyusa i-buprenorphine kwisilungiselelo sesigulane esingaphandle, ukugqiba iiyure ezisibhozo zoqeqesho. Nangona kunjalo, bambalwa abanikezeli-nkonzo bonyango abaye bafanelekela ukunyusa i-buprenorphine.
Nangona uninzi lwamagqirha enyango oluphambili luya kukhwaza ngesicetyhulwa, akuyi kuba yinto enkulu yokwelula ukuba ucinge ukuba oogqirha bokunakekelwa ngonyango ngelinye ilanga bangayichukumisa intlungu engapheliyo kwisilungiselelo sesipilisi usebenzisa i-buprenorphine. Ukongezelela kumagqirha okunakekelwa kweprayimari anokukwazi ukunyusa i-buprenorphine, i-CDC inakho izikhokelo kwindawo yokulungiselela unyango olusisigxina ukuphatha intlungu engapheliyo kunye ne-opioids.
Okubaluleke kakhulu, izikhokelo zeCDC zincoma ukuba oogqirha bokunakekelwa kwinqununu bamisela i-opioids yeentlungu ezingapheliyo kuphela xa unyango olungenalo opioid alunelwanga, kwaye lunikwe i-opioids kwisala ephantsi kakhulu. Kulo mongo, i-buprenorphine ingaqwalaselwa ngokuthe ngenye indlela i-opioid enye.
> Imithombo:
> Ayer R, et al. Ukunyangwa kobuhlungu obungapheliyo kunye ne-Buprenorphine eyahlukeneyo: UkuHlola okuHlolo kweeNkcazo zeZliniki. Anesthesia & Analgesia. 2017. [epub phambi kokuprinta]
> Chen KY, Chen L, Mao J. Buprenorphine-Naloxone Therapy kwi-Pain Management. Anesthesiology. 2014; 120 (5): 1262-74.
> I-Cote J, i-Montgomery L. I-Buprenorphine yesiNgesi njenge-Analgesic kwi-Pain Pain: I-Review Review. Uphulo lweMpilo. 2014; 15: 1171-1178.
> Dowell D, Haegerich TM, iChou R. I-CDC Isikhokelo sokuLawulwa kwama-Opioids for Pain Pain - United States, 2016. MMWR. 2016; 65 (1): 1-49.
> Lee M, et al. Ukuhlaziywa okupheleleyo kwe-Opioid-Induced Hyperalgesia. Ugqirha wezinhlungu. 2011; 14 (2): 145-61.