N-Acetyl-L-Cysteine hmoovyog ib yam khoom organic, dawb crystalline hmoov, zoo ib yam li qej tsw, qaub saj. Nws yog hygroscopic, soluble hauv dej los yog ethanol, insoluble hauv ether thiab chloroform. Nws yog acidic nyob rau hauv aqueous tov thiab muaj thiols, uas yuav ua txhaum lub disulfide daim ntawv cog lus ( − S − S − ) ntawm mucoprotein peptide daim ntawv cog lus, kom cov mucoprotein saw ua ib tug me me molecular peptide saw thiab txo cov viscosity ntawm mucoprotein. Yog li ntawd, cov khoom no yog ib tug dissolution tshuaj rau mucophlegm, purulent hnoos qeev thiab ua pa mucus. Vim tias nws feem ntau muaj nyob rau hauv daim ntawv ntawm nac hmoov, yog li acety l cysteine feem ntau siv hauv kev tshawb nrhiav.
|
Tshuaj Formula |
C5H9NO3S |
|
Exact Mass |
163 |
|
Molecular Luj |
163 |
|
m/z |
163 (100.0%), 164 (5.4%), 165 (4.5%) |
|
Elemental Analysis |
C, 36.80; H, 5.56; N, 8.58; O, 29.41; S, 19.65 |
|
Morphological |
ua kua |
|
Xim |
soluble hauv dej |
|
Melting point |
106-108℃(lit.) |
|
Boiling point |
407.7 ± 40.0 ° C (kwv yees) |
|
Qhov ntom |
1.22 g / ml ntawm 25 ° C (lit.) |
|
Cia tej yam kev mob |
2-8 ° C |
|
kev sib hloov |
− 35.1 oC (c=2, H2O ) |
|
Acidity coefficient (pKa) |
9.52 (30 degree) |
|
Flash point |
133℃f |
|
Solubility H2O |
100 mg / mL nrog cua sov |
|
Vapor ntom ntom |
1.03 (vs huab cua) |
|
Refractive Index |
24℃(C=JPC Txoj Kev) |
Peb tuaj yeem muab tauN-Acetyl-L-Cysteine hmoov.
Lus Cim: BLOOM TECH (Txij li xyoo 2008), ACHIEVE CHEM-TECH yog lub chaw pabcuam ntawm peb.
N-Acetyl-L-Cysteine hmoov(NAC), raws li leej faj- muaj cov amino acid derivative, tau tsim los ua ib qho expectorant txij li xyoo 1960. Nws daim ntawv thov thaj chaw tau nthuav dav los ntawm kev kho kab mob ua pa mus rau kev noj zaub mov kis las, kev tiv thaiv kab mob, thiab kev zoo nkauj thiab kev tu tawv nqaij. Nws cov nqi tseem ceeb nyob hauv pawg thiol (- SH) hauv nws cov qauv molecular, uas tsis tsuas yog endows NAC nrog muaj zog antioxidant muaj peev xwm, tab sis kuj ua rau nws yog ib qho tseem ceeb precursor rau glutathione (GSH) synthesis. Hauv kev zoo nkauj thiab kev tu tawv nqaij, NAC tau dhau los ua ib qho tseem ceeb hauv kev tiv thaiv - kev laus thiab kev noj qab haus huv ntawm daim tawv nqaij los ntawm kev tshem tawm cov dawb radicals, inhibiting o, txhawb collagen synthesis, thiab tswj melanin metabolism los ntawm ntau yam. Nov yog nws cov lus piav qhia ntxaws:
Cov nyhuv antioxidant ntawm NAC yog los ntawm pawg thiol (- SH) hauv nws cov molecule, uas tuaj yeem cuam tshuam ncaj qha nrog cov pa oxygen reactive (ROS) xws li hydroxyl radicals (· OH) thiab hydrogen peroxide (H ₂ O ₂) los tsim cov thiol derivatives ruaj khov, yog li cuam tshuam cov saw ntawm cov tshuaj tiv thaiv dawb radicals. Piv txwv li, hauv vitro thwmsim, NAC tuaj yeem txo qis ROS qib ntawm keratinocytes cuam tshuam los ntawm ultraviolet (UV) hluav taws xob, tiv thaiv cov cell membrane los ntawm lipid peroxidation puas. Tsis tas li ntawd, NAC, ua tus thawj coj ntawm GSH, txhim kho kev ua haujlwm ntawm glutathione peroxidase (GPx) los ntawm kev ua kom intracellular GSH concentration, tsim kom muaj kev tiv thaiv kab mob antioxidant. Kev tshawb fawb tau pom tias kev tswj hwm qhov ncauj ntawm NAC tuaj yeem nce GSH ntawm daim tawv nqaij los ntawm 30% -50% thiab txhim kho oxidative kev nyuaj siab. Cov tawv nqaij o yog ib qho ntawm cov tseem ceeb ua rau kev laus sai.
NAC inhibits qhov kev cuam tshuam ntawm nuclear kappa B (NF - κ B) qhia txoj hauv kev, txo cov kev tso tawm ntawm pro- cov kab mob inflammatory xws li TNF - thiab IL-6, thiab alleviates qhov kev puas tsuaj ntawm daim tawv nqaij mob. Piv txwv li, hauv cov qauv pob txuv, NAC tuaj yeem txo cov qog sebaceous thiab txo cov papules inflammatory. Tsis tas li ntawd, NAC tswj hwm Th1 / Th2 tshuav nyiaj li cas, inhibits allergen induced contact dermatitis, thiab muab kev tiv thaiv rau cov leeg rhiab heev.
Lub hauv paus chiv keeb ntawm NAC: los ntawm antioxidant rau cell tiv thaiv
NAC txhawb nqa kev loj hlob ntawm keratinocytes thiab fibroblasts los ntawm kev ua kom lub zog ntxiv ntawm cov teeb liab tswj kinase (ERK) txoj hauv kev, ua kom cov tawv nqaij kho qhov teeb meem. Hauv cov qauv kev yees duab, NAC tuaj yeem ua kom tawv nqaij tuab ntawm 15% -20% thiab txo qhov tob tob. Nws cov txheej txheem suav nrog: inhibition ntawm matrix metalloproteinases (MMPs): NAC txo collagen degradation los ntawm kev txo qis ntawm MMP-1 thiab MMP-9. Txhawb nqa collagen synthesis: NAC upregulates kev qhia ntawm hom I collagen los ntawm activating TGF - / Smad txoj kev. Tiv thaiv mitochondrial muaj nuj nqi: NAC tshem tawm mitochondrial ROS, tswj ATP synthesis, thiab qeeb cellular aging.
Txo wrinkles thiab txhim kho daim tawv nqaij firmness, NAC inhibits MMP-1 kev ua si thiab txo collagen degradation. Piv txwv li, hauv vitro kev sim pom tias 10mM NAC tuaj yeem nce collagen synthesis hauv fibroblasts los ntawm 25%. NAC txhim khu kev ua haujlwm ntawm lysyl oxidase (LOX), txhawb nqa elastin fiber ntau sib txuas, thiab txhim kho daim tawv nqaij elasticity. Txoj kev tshawb fawb soj ntsuam tau pom tias tom qab 12 lub lis piam ntawm kev siv cov tshuaj nplaum txuas ntxiv uas muaj 5% NAC, qhov tob ntawm wrinkles ib ncig ntawm lub qhov muag ntawm cov neeg mob tau txo qis los ntawm 18%, thiab daim tawv nqaij firmness nce 22%. Cov tawv nqaij tsis sib xws thiab ua kom tawv nqaij dawb: NAC txo qis melanin synthesis los ntawm inhibiting tyrosinase kev ua haujlwm. Piv txwv li, hauv kev sim melanoma cell, 5mM NAC tuaj yeem txo cov ntsiab lus melanin los ntawm 30%. NAC txo cov tawv nqaij dullness los ntawm kev tshem tawm lipid peroxides.
Txoj kev tshawb fawb soj ntsuam pom tau hais tias kev siv cov ntsiab lus muaj 3% NAC rau 8 lub lis piam sib law liag ua rau cov tawv nqaij xim ci ci ntawm cov neeg mob los ntawm 15% thiab txo qhov chaw stains los ntawm 20%. Piv txwv li, hauv cov qauv atopic dermatitis, NAC tuaj yeem txo cov dej tsis zoo (TEWL) los ntawm 25%. NAC alleviates hlawv thiab stinging hnov los ntawm inhibiting TRPV1 receptor kev ua. Txoj kev tshawb fawb soj ntsuam tau pom tias kev siv cov tshuaj nplaum uas muaj 2% NAC rau plaub lub lis piam sib law liag txo qhov erythema ntawm cov leeg nqaij rhiab los ntawm 30%.
Kev phiv tshuaj
N-Acetyl-L-Cysteine hmoov(NAC), raws li thiol muaj antioxidant, yog dav siv hauv kev zoo nkauj, kev tu tawv nqaij, thiab kev tswj hwm kev noj qab haus huv vim nws cov dawb radical scavenging, glutathione synthesis txhawb, tiv thaiv - mob, thiab kev tiv thaiv ntawm tes. Txawm li cas los xij, nws cov kev cuam tshuam tsis zoo yuav tsum tau ua tiag tiag. Hauv qab no yog nws cov lus piav qhia ntxaws:
Mob plab hnyuv
thiol ({0}} SH) qauv ntawm NAC tuaj yeem ua rau lub plab zom mov ncaj qha, ua rau cov tsos mob tsis xis nyob xws li xeev siab, ntuav, mob plab, thiab raws plab. Cov tshuaj tiv thaiv no tshwj xeeb tshaj yog thaum noj NAC qhov ncauj, tshwj xeeb tshaj yog thaum pib siv theem lossis thaum noj ntau dhau. Piv txwv li, hauv kev tshawb fawb soj ntsuam ntawm cov neeg mob uas muaj tus kab mob ntsws ntev (COPD), kwv yees li 15% ntawm cov neeg mob uas tau noj 600mg / d NAC qhov ncauj qhia tias xeev siab, tab sis cov tsos mob feem ntau daws lawv tus kheej hauv 2-4 lub lis piam.
Kev faib tawm: faib cov koob tshuaj txhua hnub rau hauv 2-3 koob tshuaj kom txo tau qhov ua rau lub plab zom mov tshwm sim los ntawm kev noj ib zaug.
Noj nrog zaub mov: Noj nrog zaub mov tuaj yeem txo qhov tshwm sim ntawm plab hnyuv tsis xis nyob. Kev sim ob zaug - qhov muag tsis pom kev pom tau tias noj NAC nrog zaub mov tuaj yeem txo qhov tshwm sim ntawm xeev siab los ntawm 22% mus rau 8%.
Kev hloov koob tshuaj: Thaum pib siv cov koob tshuaj qis (xws li 300mg / d) thiab maj mam nce mus rau qhov koob tshuaj, uas yuav pab nrog kev hloov pauv hauv plab hnyuv.
Lub siab ua haujlwm tsis zoo
Txawm hais tias tsis tshua muaj, ntev -lub sij hawm los yog siv ntau dhau ntawm NAC tuaj yeem ua rau lub siab puas tsuaj, tshwm sim raws li kev nce siab transaminases (ALT, AST). Hauv kev sim tsiaj, tom qab 4 lub lis piam sib law liag ntawm kev txhaj tshuaj intraperitoneal siab - koob tshuaj NAC (500mg / kg / d) hauv cov nas, mob hepatic steatosis me me tau pom, tab sis nws zoo li qub tom qab tsis siv tshuaj.
Cov neeg muaj kev pheej hmoo suav nrog cov tib neeg uas muaj lub siab ua haujlwm tsis zoo: cov neeg mob uas muaj kab mob siab hauv qab uas siv NAC yuav tsum tau saib xyuas nruj rau daim siab ua haujlwm.
Cov neeg siv sijhawm ntev: Nws raug nquahu kom kuaj lub siab ua haujlwm ntsuas txhua 3-6 lub hlis.
kev tsis haum tshuaj
Cov tsos mob ntawm daim tawv nqaij: NAC tuaj yeem ua rau muaj kev tsis haum tshuaj xws li pob khaus, khaus, thiab urticaria, tshwj xeeb tshaj yog nyob rau hauv cov tib neeg uas muaj keeb kwm ntawm sulfur compound allergies, muaj kev pheej hmoo siab dua. Kev tshuaj xyuas rov qab tau pom tias ntawm 2300 tus neeg mob siv NAC, qhov tshwm sim ntawm kev tsis haum tshuaj yog 1.2%, nrog pob liab liab suav txog 85%. Yog tias cov tsos mob ua xua tshwm sim, NAC yuav tsum tau txiav tawm. Kev tswj qhov ncauj ntawm loratadine (10mg / d) lossis cetirizine (10mg / d) tuaj yeem txo cov tsos mob. Yog hais tias muaj qhov o ntawm lub ntsws los yog ua pa nyuaj, yuav tsum tau kho mob xwm txheej ceev.
Respiratory system teb:Muaj tsawg zaus, NAC tuaj yeem ua rau bronchospasm, tshwj xeeb tshaj yog rau cov neeg mob hawb pob uas yuav tsum tau siv ceev faj. Hauv kev sim tshuaj ntsuam xyuas randomized tsom rau cov neeg mob COPD, 0.5% ntawm cov neeg mob tau ntsib kev nyuaj siab tsis zoo tom qab nqus tau NAC cov tshuaj, tab sis cov tsos mob tau kho sai sai tom qab txiav cov tshuaj.
Neurological tsis zoo tshwm sim
Mob taub hau thiab kiv taub hau
NAC tuaj yeem ua rau mob taub hau thiab kiv taub hau los ntawm kev cuam tshuam glutamate metabolism lossis vasodilation, nrog rau qhov tshwm sim ntawm kwv yees li 3% -5%. Hauv kev sim tshuaj ntsuam xyuas cov neeg mob uas muaj obsessive-compulsive tsis meej, 6% ntawm cov neeg mob uas noj 1200mg / d NAC qhov ncauj qhia mob taub hau, tab sis tsis cuam tshuam rau kev ua raws li kev kho mob. Cov lus qhia: Tsis txhob tsav tsheb lossis siv lub tshuab ua haujlwm kom txog thaum tus neeg muaj kev cuam tshuam meej. Thaum mob taub hau tseem tsis tau nyem, nws yuav tsum tau soj ntsuam seb nws puas muaj feem cuam tshuam nrog kev sib cuam tshuam nrog lwm cov tshuaj lossis ntau npaum li cas.
Kev puas siab puas ntsws
Cov neeg laus lossis cov neeg uas muaj lub siab ua haujlwm tsis zoo yuav qee zaum muaj cov tsos mob ntawm kev puas siab puas ntsws xws li kev ntxhov siab, tsaug zog, thiab ntxhov siab thaum siv NAC. Hauv kev soj ntsuam ntawm cov neeg mob COPD cov neeg laus, qhov tshwm sim ntawm cov tsos mob puas hlwb hauv cov neeg mob hnub nyoog 80 xyoo uas siv NAC yog 2.1%, ntau dua li cov neeg mob hluas (0.5%).
Kev tswj hwm kev pheej hmoo: Cov neeg laus laus yuav tsum pib nrog koob tshuaj tsawg (300mg / d) thiab maj mam kho. Tsis tu ncua ntsuas kev txawj ntse, tshwj xeeb tshaj yog thaum ua ke nrog sedatives.
Cov tshuaj sib cuam tshuam
Anticoagulants
NAC tuaj yeem txhim kho cov teebmeem ntawm cov tshuaj tiv thaiv coagulants xws li warfarin thiab tshuaj aspirin, ua rau muaj kev pheej hmoo los ntshav. Cov txheej txheem yuav cuam tshuam nrog cov nyhuv antioxidant ntawm NAC cuam tshuam rau platelet muaj nuj nqi lossis tshuaj metabolizing enzyme kev ua haujlwm. Tswv yim: Thaum siv NAC, nws yog ib qho tsim nyog yuav tsum tau saib xyuas INR thiab kho cov koob tshuaj warfarin. Tsis txhob siv cov tshuaj uas tsis yog steroidal los tiv thaiv - cov tshuaj inflammatory xws li tshuaj aspirin ua ke.
Nitroglycerin
NAC tuaj yeem txhim kho vasodilatory nyhuv ntawm nitroglycerin, ua rau hypotension. Cov kev sim tsiaj tau pom tias kev sib xyaw ua ke ntawm NAC (200mg / kg) thiab nitroglycerin (0.1mg / kg) tuaj yeem txo qhov siab ntawm cov hlab ntsha hauv cov nas los ntawm 30%, ntau dua li cov pab pawg nitroglycerin ib leeg (15%). Lub hauv paus ntsiab lus ntawm kev kho mob: Cov neeg mob uas muaj kab mob plawv yuav tsum saib xyuas lawv cov ntshav siab thaum siv nws ua ke. Tsis txhob noj cov tshuaj NAC thiab nitroglycerin ib txhij.
Tshwj xeeb pejxeem txaus ntshai
Cov poj niam cev xeeb tub thiab lactating
Cov kev sim tsiaj tau pom tias siab - koob tshuaj NAC (Ntau dua lossis sib npaug li 1000mg / kg / d) tuaj yeem ua rau muaj kev pheej hmoo ntawm embryonic txawv txav, tab sis tib neeg cov ntaub ntawv tshawb fawb muaj tsawg. Ib txoj kev tshawb fawb ntawm 200 tus poj niam cev xeeb tub tsis pom muaj kev sib raug zoo ntawm NAC (600mg / d) thiab fetal malformations los yog yug ntxov ntxov, tab sis nws raug pom zoo kom siv nws tsuas yog thaum cov txiaj ntsig tshaj qhov txaus ntshai. NAC tuaj yeem tso rau hauv cov kua mis, tab sis qhov concentration tsawg heev (<1% maternal blood drug concentration), and there are currently no reports of adverse reactions in infants. If lactating women need to use it, it is recommended to take the medication immediately after breastfeeding to reduce infant exposure.
Cov menyuam yaus thiab cov tub ntxhais hluas
Cov ntaub ntawv kev nyab xeeb ntawm NAC hauv cov menyuam yaus feem ntau yog los ntawm kev kho mob expectorant (xws li cystic fibrosis), thiab luv luv - siv sijhawm (<4 weeks) is well tolerated. However, long-term use may affect growth and development related metabolic pathways, and the risk benefit ratio needs to be carefully evaluated. Dose adjustment: The recommended dose for children is 10-15mg/kg/d, taken in 2-3 doses to avoid exceeding the maximum adult dose (1800mg/d).
N-Acetyl-L-Cysteine (NAC) hmoov yog ntau yam thiab muaj zog ntxiv nrog ntau yam txiaj ntsig kev noj qab haus huv. Nws muaj peev xwm los txhawb cov qib glutathione, ua raws li cov tshuaj tiv thaiv kab mob ncaj qha, thiab txhawb kev tshem tawm cov tshuaj lom neeg ua rau nws muaj txiaj ntsig zoo rau kev ua pa, lub siab ua haujlwm, kev puas siab puas ntsws- nyob, thiab ntau dua. Txawm hais tias feem ntau muaj kev nyab xeeb, NAC yuav tsum tau siv nrog ceev faj, tshwj xeeb tshaj yog rau cov tib neeg uas muaj tus mob ua ntej - uas twb muaj lawm lossis cov tshuaj noj. Raws li kev tshawb fawb txuas ntxiv mus nthuav tawm cov ntawv thov tshiab thiab cov qauv tsim, NAC tau npaj los ua lub hauv paus ntawm kev noj qab haus huv thiab kev noj qab haus huv rau xyoo tom ntej. Nco ntsoov sab laj tus kws kho mob ua ntej pib NAC ntxiv kom muaj kev nyab xeeb thiab ua tau zoo.
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