Raws li tus neeg sawv cev zoo tshaj plaws peptide cov tswv cuab ntawm gonadotropin - tso cov tshuaj hormone (GnRH) agonist tsev neeg, qhov kev ua haujlwm ntawmtriptorelin acetate 3.75 mgnyob rau hauv vivo tsis yog ib qho inhibitory nyhuv, tab sis nthuav tawm ib qho tshwj xeeb peb -theem evolution txheej txheem nrog meej lub cev ntu, uas kuj yog lub ntsiab lus tseem ceeb ntawm nws cov tshuaj pharmacological. Tshwj xeeb, tom qab cov tshuaj nkag mus rau hauv lub cev, nws luv luv activates pituitary GnRH receptor raws li ib tug agonist nyob rau hauv thawj theem, ua rau ib tug ncua sij hawm tso tawm ncov ntawm gonadotropins (feem ntau luteinizing hormone LH thiab follicle stimulating hormone FSH), uas yog hu ua flare up effect; Raws li kev siv tshuaj txuas ntxiv mus, cov hlwb pituitary yuav hloov kho lub sijhawm ntev - ua kom GnRH receptors, maj mam nkag mus rau lub xeev ntawm pituitary desensitization.
Khoom Description
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Triptorelin AcetateCOA
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| Certificate of Analysis | ||
| Compound npe | Triptorelin Acetate | |
| Qib | Pharmaceutical qib | |
| CAS Nr. | 140194-24-7 | |
| Ntau | 38g | |
| Ntim txheem | PE hnab + Al foil hnab | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
| Ntau No. | 202601090068 | |
| MFG | Peb 9, 2026 | |
| EXP | Peb 8, 2029 | |
| Qauv |
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| Yam khoom | Enterprise txheem | Kev txheeb xyuas qhov tshwm sim |
| Qhov tshwm sim | Dawb los yog yuav luag dawb hmoov | Ua raws |
| Cov ntsiab lus dej | Tsawg dua lossis sib npaug li 5.0% | 0.54% |
| Poob rau ziab | Tsawg dua lossis sib npaug li 1.0% | 0.42% |
| Hnyav Hlau | Pb Tsawg dua lossis sib npaug li 0.5ppm | N.D. |
| Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Hg Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Cd Tsawg dua lossis sib npaug li 0.5ppm | N.D. | |
| Purity (HPLC) | Ntau dua lossis sib npaug li 99.0% | 99.98% |
| Ib leeg impurity | <0.8% | 0.52% |
| Tag nrho microbial suav | Tsawg dua lossis sib npaug li 750cfu / g | 95 |
| E. Coli | Tsawg dua lossis sib npaug li 2MPN / g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (los ntawm GC) | Tsawg dua lossis sib npaug li 5000ppm | 500ppm ua |
| Cia |
Khaws rau hauv qhov chaw kaw, tsaus, thiab qhuav hauv qab -20 degree |
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| Tshuaj Formula | C64H82N18O13 |
| Exact Mass | 1310.63 |
| Molecular Luj | 1311.47 |
| m/z | 1310.63 (100.0%), 1311.63 (69.2%), 1312.64 (23.6%), 1311.63 (6.6%), 1313.64 (4.5%), 1312.63 (4.3%), 1312.64 (2.7%), 1313.64 (1.8%), 1313.63 (1.6%) |
| Elemental Analysis | C, 58.61; H, 6.30; N, 19.22; O, 15.86 |
Qhov kawg tshwm sim ntawm pituitary desensitization yog qhov tseem ceeb inhibition ntawm gonadotropin secretion, uas ua rau txo qis hauv testosterone (txiv neej) lossis estrogen (poj niam) qib hauv lub cev, thaum kawg ncav cuag castration lossis postmenopausal theem. Qhov kev ua tiav ntawm cov saw hlau no tsis yog ib qho kev cais peb theem, tab sis kev sib cuam tshuam thiab kev loj hlob ntawm cov organic tag nrho, uas ua ke ua lub hauv paus tseem ceeb ntawm kev siv tshuaj kho mob thiab nws cov txheej txheem tseem ceeb ntawm kev ua haujlwm rau kev kho mob ntsig txog kab mob. Hauv kab lus hauv qab no, peb yuav muab cov yam ntxwv ntawm cov molecules, cov hlwb, thiab tag nrho lub cev los ua cov ncauj lus kom ntxaws ntxaws thiab kev soj ntsuam ntawm peb qhov tseem ceeb pharmacological txuas.
Thawj ntu ntu stimulation ntawm gonadotropin tso tawm (flare up effect)
Thawj cov nyhuv ntawmtriptorelin acetate 3.75 mgtsis yog qhov ncaj qha inhibition, tab sis theej ua kom cov pituitary GnRH receptors ua tus agonist, ua rau lub sijhawm luv luv hauv gonadotropins, lub npe hu ua cov nyhuv flare. Raws li ib qho hluavtaws GnRH analogue, nws 6th D-tryptophan hloov L-glycine ntawm natural GnRH. Qhov kev hloov kho cov qauv no tsis yog tsuas yog ua kom nws txoj kev sib raug zoo nrog cov receptor, ua rau nws cov affinity 50-100 npaug ntawm natural GnRH, tab sis kuj endows nws muaj zog enzymatic tsis kam, ncua ib nrab-lub neej los ntawm feeb mus rau cov sij hawm ntawm cov tshuaj hormones ntuj, muab lub hauv paus ruaj khov rau kev ua haujlwm txuas ntxiv mus; Tsis zoo li cov kev cai pulsatile ntawm tej yam ntuj tso GnRH, nws lov lub physiological atherosclerosis nyob rau hauv ib tug tsis pulsatile sustained binding hom, ua rau receptor overactivation thiab qhib lub hauv paus molecular ntawm flare up effect.Los ntawm qhov kev xav ntawm cov tshuaj hormone tso tawm kinetics, lub ncov ntshav concentration ntawm cov tshuaj tuaj yeem ncav cuag li 40 feeb tom qab txhaj tshuaj subcutaneous.
Hauv 24-72 teev tom ntej no, qib ntawm luteinizing hormone (LH) tuaj yeem nce mus rau 5-8 npaug ntawm tus nqi hauv paus, thiab follicle stimulating hormone (FSH) kuj yuav nce synchronously tab sis tsawg dua, xav txog qib ntawm cov tshuaj hormones poj niam txiv neej. Txiv neej Testosterone tuaj yeem nce luv luv los ntawm 50-100%, thiab poj niam cov tshuaj estrogen tseem yuav qhia txog qhov sib xws. Cov nyhuv no feem ntau kav ntev li 1-2 lub lis piam ua ntej nkag mus rau lub sijhawm poob sai, ua tiav qhov kev hloov pauv mus rau kev hloov pauv. Ntawm qib cellular signaling mechanism, cov tshuaj no activates Gq/11 protein ua ke receptors, pib txoj kev phospholipase C, txhawb kev tso tawm ntawm intracellular calcium khw muag khoom, thiab ua rau lub exocytosis ntawm gonadotropin cia granules, ua tiav sai tso LH thiab FSH.
Nyob rau tib lub sijhawm, nws luv luv upregulates transcription ntawm cov noob caj noob ces gonadotropin, ntxiv txhim kho cov tshuaj hormone synthesis thiab txhim kho cov txheej txheem ntawm kev ua kom muaj zog ntawm cov qib cellular. Txawm hais tias qhov kev hloov pauv no ua rau lub hauv paus rau cov teebmeem tshuaj tom ntej, kuj tseem muaj qee qhov kev pheej hmoo ntawm kev kho mob. Hauv kev kho mob qog noj ntshav prostate, nce qib testosterone ib ntus tuaj yeem ua rau mob pob txha lossis mob urinary ob leeg. Yog li ntawd, nws yuav tsum tau ceeb toom rau qhov kev pheej hmoo no thiab muab cov tshuaj tiv thaiv androgen rau kev tiv thaiv; Cov poj niam cov neeg mob yuav hnov mob luv luv los yog cov tsos mob hnyav dua thaum lub sijhawm no. Hauv kev kho mob, cov neeg mob yuav tsum tau ceeb toom ua ntej thiab saib xyuas kom muaj kev nyab xeeb ntawm cov tshuaj.
Cov ntaub ntawv Source:
Kev Hloov Kho ntawm Triptorelin: Tam sim no xav txog Androgen Deprivation Therapy rau Prostate Cancer. PIB: 27375389
Cov teebmeem ntawm kev kho lub sijhawm ntev - nrog GnRH agonists ntawm pituitary muaj nuj nqi rov qab. Fertil Steril, 2017
Pituitary desensitization thiab txo qis hauv LH thiab FSH tom qab noj tshuaj tas mus li
Thaum cov tshuaj tsis tu ncua nyob rau ntawm cov tshuaj kho mob, qhov ntev - lub sij hawm ua kom GnRH receptors los ntawm pituitary hlwb raug hloov pauv, hu ua desensitization, uas thaum kawg ua rau muaj kev cuam tshuam tseem ceeb ntawm gonadotropin secretion thiab dhau los ua qhov txuas txuas mus rau cov tshuaj siv los kho cov teebmeem. Nyob rau theem receptor, GnRH receptors uas txuas ntxiv mus los ntawm cov tshuaj tau hloov pauv hloov pauv, ua rau receptor internalization thiab lysosomal degradation, ua rau 70-80% txo qis hauv receptor density ntawm lub xovtooj ntawm tes. Tib lub sijhawm, receptor mRNA qhia yog downregulated, thiab cov synthesis ntawm lub xeev receptors degradation; Qhov tseem ceeb tshaj, G protein ua ke txoj kev taw qhia txoj hauv kev tsis muaj kev sib txuas, thiab txawm tias cov receptor thiab ligand tseem tuaj yeem khi.
Nws tsis tuaj yeem ua tau zoo hloov cov teeb liab, thaiv cov teeb liab kis ntawm gonadotropin secretion ntawm qib receptor.Cov kev hloov pauv ntawm qib receptor ntxiv ua rau kev hloov kho ntawm pituitary cell muaj nuj nqi, thiab gonadotropin hlwb nkag mus rau "lub sij hawm refractory", nrog rau kev txo qis hauv kev teb rau cov stimuli tom ntej. Cov txheej txheem sib txuas ntawm cov tshuaj hormone synthesis thiab secretion raug cuam tshuam, ua rau txo qis hauv LH thiab FSH tso tawm qib qis dua 10-20% ntawm cov hauv paus. Nyob rau tib lub sijhawm, MAPK phosphatase induction nce, inhibiting teeb liab cascade amplification, tsim ib lub xeev inhibitory ruaj khov, ua kom ruaj khov hauv cov qib gonadotropin.Los ntawm qhov kev xav ntawm kev sib raug zoo ntawm lub sij hawm, cov txheej txheem desensitization feem ntau pib nyob rau lub lim tiam thib ob ntawm cov tshuaj.Thiab qhov txo qis hauv LH / FSH nyob rau hauv 10 hnub ntawm cov tshuaj.
Lub xeev inhibitory ruaj khov tuaj yeem ua tiav nyob ib ncig ntawm 4 lub lis piam ntawm cov tshuaj, thaum lub sijhawm LH theem feem ntau poob mus rau qhov tsis paub meej.Muaj qhov sib txawv ntawm lub sijhawm ntawm desensitization ntawm ntau hom tshuaj. Kev ua yeeb yam ntev ntev (xws li 3.75mg microspheres) tuaj yeem tuav lub xeev desensitization ruaj khov mus txog 30 hnub, thaum daim ntawv 22.5mg ntau npaum li cas tuaj yeem nyob ntev li 6 lub hlis, ua tau raws li qhov xav tau ntawm kev kho mob sib txawv. Tsis tas li ntawd, cov nyhuv inhibitory txuas ntxiv tseem yuav ua rau cov kev tawm tswv yim tsis zoo ntawm cov hypothalamic pituitary gonadal axis, ua rau "tshuaj-induced hypogonadotropin xeev". Nyob rau tib lub sijhawm, qhov rhiab heev ntawm lub caj pas pituitary rau kev tawm tswv yim inhibition ntawm kev sib deev cov tshuaj hormones yog txo, ntxiv consolidating inhibitory nyhuv ntawm gonadotropins thiab muab guarantees rau tom qab sib sib zog nqus poob ntawm cov tshuaj hormones.
Cov ntaub ntawv Source:
Gonadotropin{0}} tso cov tshuaj hormones (GnRH) agonists. Hnub tim, 2023
Pituitary thiab extrapituitary ua ntawm gonadotrophin- tso cov tshuaj hormones thiab nws cov analogues. Hum Reprod, 1999
Gonadotrophin- tso cov tshuaj hormones thiab GnRH agonists: cov txheej txheem ntawm kev ua. Pub Med, 2003
Peb -phase pharmacological teebmeem ntawmtriptorelin acetate 3.75 mgtsis yog cov theem sib cais, tab sis ua tiav cov tshuaj siv tshuaj uas muaj kev sib raug zoo, kev vam meej, thiab kev sib cuam tshuam. Hom kev ua tshwj xeeb no tau dhau los ua nws qhov tseem ceeb hauv kev kho mob kom zoo dua piv rau lwm hom tshuaj hormone tswj cov tshuaj, ua kom pom nws tus nqi tshwj xeeb hauv kev kho cov kab mob hormonal.
Ntawm lawv, qhov tshwm sim tshwm sim, raws li qhov pib hloov pauv ntawm tag nrho cov txheej txheem tshuaj, txawm hais tias tsuas yog tshwm sim raws li lub ncov luv luv ntawm gonadotropin tso tawm, qhia meej txog nws cov khoom tseem ceeb raws li GnRH agonist - nws tsis ncaj qha cuam tshuam cov teebmeem inhibitory, tab sis tswj los ntawm txoj hauv kev ntawm activating receptors ua ntej thiab tom qab ntawd inducing subseque. Cov txheej txheem stimulation thawj zaug no tsis yog tsuas yog ib qho kev qhia ntawm kev pib ua yeeb tshuaj, tab sis kuj nteg lub hauv paus ntawm lub cev tsim nyog rau pituitary desensitization tom ntej.Yog tsis muaj cov nyhuv excitatory luv luv, cov txheej txheem desensitization tom ntej tsis tuaj yeem pib ua haujlwm zoo. Pituitary desensitization, raws li qhov tseem ceeb nruab nrab ntawm kev sib txuas ntawm thawj zaug stimulation thiab cov nyhuv kho zaum kawg.
Ua lub luag haujlwm tseem ceeb hauv kev ua kom muaj kev hloov pauv hloov pauv hauv cov hlwb pituitary los ntawm kev siv tshuaj tas mus li, suav nrog kev tshem tawm cov receptor, teeb liab txoj hauv kev uncoupling, thiab lwm yam, yog li thaiv tag nrho cov kev tso tawm tsis zoo ntawm gonadotropins. Kev ruaj ntseg thiab kev pheej hmoo ntawm kev tswj hwm hauv qhov txuas no ncaj qha txiav txim siab tag nrho cov txiaj ntsig kho mob ntawm cov tshuaj thiab yog lub hauv paus ntawm kev ua tiav cov hom phiaj kho mob. Kev txo qis ntawm cov tshuaj hormones poj niam txiv neej mus rau castration (txiv neej) lossis postmenopausal (poj niam) qib yog qhov kawg kawg ntawm tag nrho cov tshuaj siv tshuaj thiab qhov ncaj qha ntawm cov txiaj ntsig kho mob. Los ntawm kev tswj hwm qib ntawm cov tshuaj hormones poj niam txiv neej hauv lub cev ntawm qib qis pathological, nws tuaj yeem cuam tshuam txoj kev loj hlob thiab kev loj hlob ntawm cov kab mob hormonal dependent, txo cov kab mob -cov tsos mob, thiab muab kev txhawb zog pharmacological rau kev kho mob ntawm cov kab mob hormonal dependent.
Cov ntaub ntawv
Triptorelin Acetate Microspheres rau Prostate Cancer: Pharmacokinetics thiab Efficacy. Clin Pharmacokinet, 2016
Cov kws tshaj lij pom zoo ntawm daim ntawv thov kev kho mob ntawm GnRH-a hauv obstetrics thiab gynecology Suav Journal of Obstetrics thiab Gynecology, 2018
Agonist-induced internalization thiab downregulation ntawm gonadotropin- tso cov tshuaj hormones. Am J Physiol Cell Physiol, 2009
Triptorelin piv rau Leuprolide: Kev Tshawb Fawb Sib Piv hauv Prostate Cancer. Urology, 2015
FAQ
- Kev siv triptorelin acetate 3.75 mg yog dab tsi?
Triptorelin txhaj tshuaj yog siv los kho qee yam mob qog noj ntshav prostate. Nws kuj yog siv los kho lub hauv paus precocious puberty (CPP; ib qho mob ua rau cov menyuam yaus nkag mus rau kev laus dhau los sai, ua rau muaj kev loj hlob sai dua li cov pob txha zoo li qub thiab kev loj hlob ntawm kev sib deev).
- Triptorelin acetate txhaj tshuaj 3.75 mg siv rau hauv IVF yog dab tsi?
Decapeptyl (triptorelin) yog gonadotropin - tso cov tshuaj hormone (GnRH) agonist analogue tshuaj. Nws yog siv rau hauv kev pabcuam kev yug me nyuam los tswj kev ua haujlwm ntawm zes qe menyuam hauv vitro fertilization (IVF) cycles.
Cim npe nrov: Tuam Tshoj triptorelin acetate 3.75 mg manufacturers, lwm tus neeg
