Pharmacology thiab Toxicology ntawm Carbetocin

pharmacological kev txiav txim
Carbetocin yog ib qho hluavtaws ua haujlwm ntev oxytocin 9-peptide analogue nrog agonist zog. Ib koob tshuaj txhaj tshuaj tuaj yeem siv tau tam sim ntawd tom qab phais tas nyob rau hauv epidural lossis txha nraub qaum los tiv thaiv uterine hypotension thiab postpartum hemorrhage.
Cov chaw kho mob thiab chaw muag tshuaj ntawm carbetocin zoo ib yam li cov oxytocin tshwm sim. Zoo li oxytocin, carbetocin khi rau oxytocin receptor ntawm lub tsev menyuam cov leeg nqaij, ua rau lub tsev menyuam tsis sib haum xeeb, ua rau nws qhov zaus thiab nce uterine nro raws li qhov qub contraction. Hauv cov xeev uas tsis cev xeeb tub, cov ntsiab lus ntawm oxytocin receptors nyob rau hauv lub tsev menyuam muaj tsawg heev, nce thaum cev xeeb tub thiab ncav cuag lub ncov thaum yug menyuam. Yog li, carbetocin tsis muaj txiaj ntsig rau lub tsev menyuam uas tsis xeeb tub, tab sis muaj txiaj ntsig zoo rau lub tsev menyuam hauv plab thiab lub tsev menyuam yug tshiab.
Tom qab txhaj tshuaj los yog intramuscular txhaj ntawm carbetocin, lub tsev menyuam tau cog lus sai, ncav cuag qhov pom tseeb hauv 2 feeb. Cov nyhuv nquag ntawm ib koob tshuaj txhaj tshuaj carbetocin rau ntawm lub tsev menyuam yuav kav ntev li ib teev, thiab yog li ntawd txaus los tiv thaiv kev mob ntshav qab zib tom qab yug me nyuam. Tom qab kev tswj hwm ntawm carbetocin tom qab yug me nyuam, qhov zaus thiab qhov loj ntawm kev cog lus ntev dua oxytocin.
Cov kev tshawb fawb tau pom tias thaum ib koob tshuaj ntawm 100 micrograms ntawm carbetocin tau muab tso rau hauv cov hlab ntsha tam sim ntawd tom qab kev phais mob nyob rau hauv epidural lossis txha caj qaum, carbetocin yog qhov zoo tshaj rau cov placebo hauv kev tiv thaiv uterine hypotension thiab txo qis ntshav tom qab yug menyuam.
Kev tswj hwm ntawm carbetocin nyob rau hauv thaum ntxov postpartum lub sij hawm kuj yuav txhawb uterine involution.
Toxicological Studies
Hauv txoj kev tshawb fawb txog kev mob toxicity, LD50 tau tshawb xyuas los ntawm kev txhaj tshuaj txhaj tshuaj ntawm 10 mg / kg rau nas. Sau cov kev kho mob tshwm sim ntawm tag nrho cov tsiaj ( lethargy , hunching posture , bristling , ua tsis taus pa , thiab lub cev muaj zog incoordination ). Raws li tus nqi LD50, cov koob tshuaj rau 100 grams ntawm nas yog 1000 micrograms, uas yog 10 npaug ntawm cov tshuaj siv los ntawm tib neeg.
Nees nkaum nas raug muab faib ua plaub pawg thiab muab cabetocin 1. 0 mg/kg intravenously txhua hnub. Tsis muaj kev kho mob ntsig txog kev tuag lossis kev kho mob tshwm sim tom qab 28 hnub.
Kaum rau tus poj niam hound tau muab cabetocin 1. Tom qab 28 hnub, tsis muaj kev tuag lossis cov tsos mob tshwm sim cuam tshuam nrog kev tswj hwm. Kuj tsis muaj kev hloov pauv txog kev kho mob hauv hematology, chaw kho mob biochemistry, lossis urinalysis.
Tsis muaj cov nyhuv mutagenic tau pom hauv kev sim mutagenic nrog carbetocin.
Tsis muaj kev tshawb fawb txog carcinogenic tau ua.
Vim hais tias cov tshuaj yog siv nyob rau hauv ib koob tshuaj thaum ntxov tom qab yug me nyuam, tsis muaj kev ua me nyuam thiab teratogenic thwmsim.