Nafarelin tshuaj tsuag(Synarel) tswj gonadotropin secretion los ntawm kev ua raws li cov qauv ntawm endogenous GnRH thiab kev sib tw khi rau GnRH receptors nyob rau hauv lub caj pas anterior pituitary. Synarel qhia tau tias muaj kev sib raug zoo receptor ntau dua thiab lub sijhawm ua haujlwm ntev dua. Tsis tas li ntawd, nws cov tshuaj tsuag qhov ntswg muaj qhov zoo nrog rau kev tswj hwm yooj yim, ruaj khov bioavailability, thiab cov kab mob me me, ua rau nws siv dav hauv gynecological benign qog thiab transgender hormone kho.
Peb Cov Khoom Muag Khoom
Nafarelin COA
Kev siv hauv Uterine Fibroids
Uterine fibroids yog cov qog nqaij hlav loj tshaj plaws ntawm cov poj niam cev xeeb tub, tshwm sim los ntawm qhov txawv txav ntawm lub tsev menyuam cov leeg nqaij. Lawv cov pathogenesis zoo sib xws nrog ntev - lub sij hawm stimulation los ntawm endogenous estrogen thiab progesterone. Kev kho mob tshwm sim feem ntau suav nrog kev coj khaub ncaws txawv txav, plab plab, mob plab, thiab nce leukorrhea. Nyob rau hauv cov xwm txheej hnyav, lawv tuaj yeem ua rau muaj ntshav tsis txaus, muaj menyuam tsis taus, lossis tsis xis nyob vim yog compression ntawm cov kabmob uas nyob ib sab. Raws li GnRH agonist,nafarelin tshuaj tsuaginhibits gonadotropin secretion thiab txo cov kab mob estrogen thiab progesterone, yog li inhibiting fibroid kev loj hlob thiab alleviating cov tsos mob, ua rau nws yog ib qho tseem ceeb pharmacological kev xaiv rau uterine fibroids.
Hauv kev xyaum kho mob, nws tau qhia rau cov xwm txheej hauv qab no:
Cov neeg mob uas muaj cov tsos mob me uas tsis kam kho phais, tshwj xeeb tshaj yog cov poj niam perimenopausal. Pharmacological therapy inhibits fibroid kev loj hlob; Tom qab lub cev tsis muaj zog thiab kev poob qis hauv cov tshuaj hormones, fibroids maj mam atrophy, zam kev phais mob.
Cov neeg mob uas muaj uterine fibroids loj (5-10 cm inch) ua rau muaj kev pheej hmoo ntawm kev phais. Kev tswj xyuas ua ntej ntawm cov khoom rau 3-6 lub hlis txo cov fibroid ntim los ntawm 30% -50%, txo cov ntshav intraoperative, txo qhov kev pheej hmoo ntawm kev phais, pab tswj kev phais, thiab txo qis kev raug mob rau cov ntaub so ntswg.
Cov neeg mob uas muaj uterine fibroids nyuaj los ntawm qhov mob hnyav heev. Kev siv ua ntej txo qis kev coj khaub ncaws thiab txhim kho ntshav qab zib, tsim kom muaj lub cev zoo rau kev phais.
Cov neeg mob uas tsis kam phais los yog muaj kev phais contraindications (xws li, mob plawv, mob siab, lossis raum tsis txaus). Kev siv sijhawm ntev - tswj cov tsos mob thiab txhim kho lub neej zoo.
Cov ntaub ntawv qhov chaw: 35 Kev Noj Qab Haus Huv - Puas Yog Uterine Fibroids Kho Nrog Tshuaj? Minfukang - Leuprorelin Acetate Microspheres rau Txhaj Tshuaj.
Daim ntawv thov hauv Transgender Hormone Therapy
Transgender cov tib neeg yog cov uas lawv poj niam txiv neej tus kheej txawv ntawm lawv qhov kev sib deev thaum yug los. Ob pawg thawj yog cov poj niam hloov pauv (txiv neej yug los, poj niam txiv neej yog leej twg) thiab cov txiv neej hloov pauv (poj niam tau yug los, txiv neej poj niam txiv neej). Lub hom phiaj tseem ceeb ntawm kev hloov poj niam txiv neej txoj kev kho yog los txhawb kev txhim kho cov yam ntxwv ntawm kev sib deev theem nrab raws li tus neeg lub cev ntawm poj niam txiv neej los ntawm kev cuam tshuam hormonal exogenous, txo cov poj niam txiv neej dysphoria thiab txhim kho lub neej zoo. Raws li ib tug GnRH agonist, nws suppresses endogenous gonadotropin secretion los tsim ib tug haum endocrine ib puag ncig, pab raws li ib tug tseem ceeb adjuvant nyob rau hauv transgender hormone therapy, tshwj xeeb tshaj yog rau cov poj niam transgender.
Hauv kev hloov pauv poj niam txoj kev kho tshuaj hormones, nws feem ntau inhibits testicular androgen secretion thiab txo cov qib testosterone hauv lub cev, yog li ua rau cov txiv neej theem nrab kev sib deev yam ntxwv (xws li, Adas txiv apple, ntau lub cev plaub hau, lub suab sib sib zog nqus) thiab npaj rau kev kho estrogen tom ntej. Nce endogenous testosterone counteracts estrogen teebmeem thiab impairs txoj kev loj hlob ntawm poj niam theem nrab kev sib deev yam ntxwv. Yog li, GnRH agonist pretreatment yuav tsum tau txo qis testosterone rau cov poj niam ib txwm ua ntej pib kho tshuaj estrogen. Kev tswj hwm intranasally,nafarelin tshuaj tsuagsai suppresses pituitary LH thiab FSH secretion, ntxiv inhibiting testicular spermatogenesis thiab androgen ntau lawm.
Testosterone qib feem ntau ncav cuag lub hom phiaj hauv 2-4 lub lis piam. Kev sib xyaw tshuaj estrogen tom qab ntawd pab txhawb kev loj hlob ntawm lub mis, softening ntawm daim tawv nqaij, rog redistribution, thiab lwm yam poj niam theem nrab kev sib deev yam ntxwv, thaum alleviating poj niam txiv neej dysphoria thiab lub cev tsis xis nyob.
Kev siv hauv cov txiv neej hloov pauv yog qhov txwv, feem ntau yog rau cov neeg mob uas xav tau kev ua haujlwm ntawm zes qe menyuam thiab txo cov tshuaj estrogen. Lub hauv paus ntawm transgender txiv neej txoj kev kho cov tshuaj hormones yog androgen supplementation rau induce txiv neej theem nrab kev sib deev yam ntxwv (xws li, lub cev plaub hau loj hlob, nce nqaij loj, lub suab sib sib zog nqus). Hauv cov neeg mob uas muaj kev ua haujlwm siab ntawm zes qe menyuam thiab nce qib tshuaj estrogen, luv luv - lub sijhawm cov khoom lag luam suppresses estrogen secretion ntawm zes qe menyuam, txhim kho androgen ua tau zoo, thiab txo cov tshuaj estrogen- cuam tshuam txog kev phiv (xws li, lub mis rhiab, mob khaub thuas los ntshav).
Cov ntaub ntawv qhov chaw: Douyin Encyclopedia – Triptorelin (Drug); Xiaohe Health - Lub luag haujlwm ntawm Nafarelin yog dab tsi?
Pharmacokinetics
3.1 Absorption
Cov khoom no yog ib lub qhov ntswg formulation absorbed feem ntau los ntawm qhov ntswg mucosa. Muaj ntau cov mucosal capillaries ua rau lub cev nqus tau sai yam tsis tau ua ntej - dhau cov metabolism. Cov tshuaj tuaj yeem pom hauv plasma li ntawm 15-30 feeb ntawm kev tswj hwm, nrog rau qhov siab tshaj plaws plasma concentration ntawm 1-2 teev. Qhov ntswg patency cuam tshuam rau kev nqus tau zoo; qhov ntswg o los yog congestion yuav tsum raug cais tawm ua ntej noj.
Nws cov bioavailability yog kwv yees li 20% -40%, deb tshaj qhov kev tswj hwm qhov ncauj (tsuas yog 1% -5%), vim nws tsis txhob ua rau lub plab zom mov thiab lub siab ua ntej- dhau cov metabolism. Cov zaub mov tsis muaj qhov cuam tshuam loj rau kev nqus. Nyob rau hauv cov tshuaj kho ntau yam, ncov plasma concentration thiab cheeb tsam nyob rau hauv lub nkhaus (AUC) nce linearly nrog koob, tso cai rau tus kheej koob tshuaj titration.
Kev nqus tau sib txawv ntawm qhov ntau npaum li cas: qhov siab tshaj plaws ntawm cov ntshav plasma thiab AUC nce linearly nrog nce koob, qhia tias koob tshuaj - nyob ntawm kev nqus nyob rau hauv lub qhov rais kho. Kev noj tshuaj tuaj yeem hloov kho raws li tus kab mob hnyav rau kev kho kom zoo.
3.2 Kev faib tawm
Tom qab lub cev nqus dej, synarel yog dav faib nrog lub ntim ntawm kev faib tawm ntawm kwv yees li 20-30 L / kg. Concentrations yog siab dua nyob rau hauv cov ntaub so ntswg (pituitary caj pas, zes qe menyuam, testes) raws li nws lub hom phiaj qhov chaw, raws li zoo raws li nyob rau hauv lub siab thiab ob lub raum, txhawb metabolic thiab excretory txoj kev.
Plasma protein binding tsuas yog 20% -30%, nrog rau feem ntau cov tshuaj uas muaj nyob rau hauv daim ntawv dawb dawb, ua rau muaj kev sib cuam tshuam ntawm cov tshuaj-tshuaj yeeb thiab kev nyab xeeb siab thaum co- noj nrog cov protein ntau- khi cov tshuaj.
3.3 Metabolism
Nafarelin tshuaj tsuagFeem ntau metabolized hauv daim siab ntawm peptide daim ntawv cog lus hydrolysis los tsim cov metabolites tsis ua haujlwm. Cov kab mob plab hnyuv ua rau me me rau cov metabolism. Metabolites yog thaum kawg tawm los ntawm lub cev.
Kev tshem tawm cov ntshav plasma ib nrab- lub neej yog kwv yees li 2-4 teev, nrog rau cov metabolism sai thiab tsis tshua muaj kev pheej hmoo. Hauv cov neeg mob uas muaj lub siab tsis zoo, cov metabolism hauv qeeb qeeb thiab ib nrab - lub neej ntev, yuav tsum tau txo cov koob tshuaj thiab tshuaj xyuas tshuaj.
Unabsorbed tshuaj nkag mus rau hauv txoj hnyuv yog hydrolyzed los ntawm cov kab mob plab hnyuv mus rau hauv cov khoom tsis ua haujlwm thiab tawm hauv cov quav, nrog kev cuam tshuam tsis zoo rau tag nrho cov metabolism.
3.4 Kev tso tawm
Cov tshuaj thiab nws cov metabolites yog tawm los ntawm ob lub raum (60% -70%) thiab hnyuv (30% -40%). Hepatic metabolites thiab cov tshuaj tsis hloov pauv yog lim los ntawm glomeruli thiab tshem tawm hauv cov zis, nrog rau ib feem tawm ntawm txoj hnyuv.
Hauv lub raum tsis ua haujlwm, kev tso tawm qeeb qeeb thiab cov ntshav plasma nce ntxiv. Kev txo koob tshuaj thiab kev saib xyuas lub raum / lub siab ua haujlwm yog xav tau rau cov neeg mob uas muaj creatinine tshem tawm<30 mL/min. Hemodialysis enhances elimination, supporting dose adjustment as needed.
Nyob rau hauv cov kev kho mob, tus nqi excretion tseem nyob ruaj khov thiab koob tshuaj - ywj siab, tshem tawm cov kev pheej hmoo ntawm impaired excretion los yog tsub zuj zuj ntawm cov koob tshuaj ntau.
Cov ntaub ntawv qhov chaw: National Medical Products Administration – Pharmacokinetic Standards; Douyin Encyclopedia – Triptorelin (Drug), Finasteride (A Competitive 5 -Reductase Inhibitor).
I. Siab -Kev Ua Haujlwm Liquid Chromatography (HPLC)
HPLC yog txoj kev tshuaj ntsuam xyuas feem ntau siv rau nafarelin, tshwj xeeb tshaj yog rau kev kuaj purity formulation, aqueous drug concentration txiav txim, thiab degradation khoom tsom xam. Cov txheej txheem leverages synarel lub physicochemical zog los cais cov tshuaj los ntawm impurities thiab degradation cov khoom ntawm reversed -theem chromatography, ua raws li kev soj ntsuam kom muaj nuj nqis siv ntau yam detectors. Ib qho kev hloov pauv ib txwm - theem kem yog ua haujlwm nrog acetonitrile-dej sib tov raws li theem ntawm lub xov tooj ntawm tes, thiab kev tshawb nrhiav wavelength yog teem rau ntawm 225 nm, qhov twg synarel pom muaj zog nqus.
Cov kev tshawb fawb txhawb nqa peb lub tshuab kuaj xyuas rau synarel HPLC tsom xam: ultraviolet (UV), electrochemical (ECD), thiab fluorescence (FLD) detectors, tag nrho nrog cov lus teb zoo heev thiab cov txiaj ntsig zoo ib yam. Kev kuaj xyuas UV yog qhov yooj yim tshaj plaws rau kev tsom xam niaj hnub, nrog rau kev txwv ntawm kev kuaj pom (LOD) ntawm kwv yees li 1.5 ng. FLD muab qhov siab tshaj plaws, nrog rau LOD ntawm 0.6 ng. ECD muaj LOD ntawm kwv yees li 2.0 ng. Lub ntes tuaj yeem raug xaiv raws li kev xav tau ntawm kev txheeb xyuas. Tsis tas li ntawd, HPLC yog siv los ntsuas qhov ruaj khov ntawm synarel aqueous daws thiab saib xyuas nws cov kev degradation kinetics.
Cov ntaub ntawv qhov chaw: Taylor & Francis Online - Sib piv Electrochemical, Fluorescence, thiab Ultraviolet Detectors rau HPLC Kev Ntsuam Xyuas ntawm Decapeptide, Nafarelin; International Journal of Pharmaceutics.
II. Radioimmunoassay (RIA)
RIA feem ntau yog siv rau hauv vivo synarel concentration saib xyuas, ua kom muaj kev soj ntsuam ntau hauv cov ntshav los yog ntshav rau cov kev tshawb fawb pharmacokinetic nrog kev kuaj pom tsawg li 50 pg / mL. Txoj kev siv tshwj xeeb synarel antiserum thiab radiolabeled synarel ua tus taug qab. Raws li qhov tshwj xeeb antigen-antibody binding, free thiab bound tracers raug cais los ntsuas cov tshuaj concentration hauv cov qauv.
Cov qauv no yuav tsum tsis muaj cov qauv ua kom huv huv, yooj yim rau kev khiav lag luam, thiab xa cov neeg siab, nrog cov kab ntau ntawm 0.050-5.00 ng / mL thiab kev sib raug zoo. Antiserum qhia tsis muaj tus ntoo khaub lig-reactivity nrog endogenous GnRH, kom ntseeg tau qhov tshwj xeeb. Hauv vivo cov kev tshawb fawb paub tseeb tias muaj kev sib raug zoo ntawm RIA, HPLC, thiab HPLC- kuaj pom hluav taws xob, pab txhawb kev tshawb fawb synarel pharmacokinetic thiab toxicological.
Cov ntaub ntawv qhov chaw: Sci-Hub – Radioimmunoassay of Nafarelin ((6-(3-(2-Naphthyl)-}D-alanine))-Luteinizing Hormone-Tshem Hormone) hauv Plasma lossis Serum.
Kev tswj ntawm Hypersensitivity Reactions
Tsis tshua muaj qhov tshwm sim tsis zoo ntawm daim tawv nqaij (Stevens-Johnson syndrome, toxic epidermal necrolysis) tuaj yeem tshwm sim, tshwm sim nrog pob khaus, hlwv, mucosal erosion, kub taub hau, thiab lwm yam. Kev tswj hwm yuav tsum txiav mus tas li, thiab kev kho mob ceev pib tam sim ntawd.
Cov ntaub ntawv qhov chaw: Pfizer – SYNAREL® Warnings and Precautions.
FAQ
Dab tsi yog cov teebmeem ntawm Synarel nasal spray?
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Cov kev mob tshwm sim muaj xws lipob txuv, hloov ntawm lub mis loj, thiab kev coj khaub ncaws (lub caij nyoog) los ntshav. Hu rau koj tus kws kho mob tam sim ntawd yog tias koj muaj kev nyuaj siab, qaug dab peg, lossis teeb meem ntawm koj lub zeem muag. Synarel yog tshuaj tsuag qhov ntswg.
Koj puas tau txais koj lub sijhawm ntawm Synarel?
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Txawm li cas los xij, koj tuaj yeem cia siab tias qhov ntshav no nres ntawm nws tus kheej.Tom qab thawj ob lub hlis ntawm kev kho mob nrog SYNAREL, koj tuaj yeem cia siab tias yuav txo qis hauv kev coj khaub ncaws, thiab koj lub sijhawm yuav tsum tsis ua tag nrho.. Txawm li cas los xij, yog tias koj tsis tau noj ib lossis ntau dua ntawm SYNAREL, koj tuaj yeem ua rau qhov chaw mos los ntshav.
Cim npe nrov: Tuam Tshoj nafarelin spray manufacturers, lwm tus neeg
