Phenacetin rau Antipyretic thiab Analgesic Cas: 62-44-2

Nws yog dab tsi: Tshuaj lom neeg tus kheej thiab keeb kwm

Synthesized nyob rau hauv 1878 los ntawm German Chemist Hermann Hinsberg, phenacetin tshwm sim los ntawm kev txiav txim siab los hloov cov tshuaj tuataus los ntawm metaus - Nqa cov kev tsis sib haum xeeb). Phenacetin tus qauv tshwj xeeb muaj acetamide pab pawg sib txuas nrog ib para {{}} Ethiety (C1013No2). Qhov kev hloov kho me me no zoo li me me - hloov acetanilide hydrogen nrog ib pawg ethoxy (-oc2h5) - muaj pov thawj pivotal. Nws tseem txo qhov mob methemoglobin - sib haum muaj peev xwm thaum khaws cov teebmeem analgesic thiab antipyretic. Qhia tau Clapic hauv 1887, nws tau nrawm nrawm vim nws txoj kev ua tau zoo thiab pom kev nyab xeeb piv rau predipyrine thiab acetanilide nws tus kheej.

Phenacetin muaj ob peb cov yam ntxwv tseem ceeb uas tau txhawb nws txoj kev saws me nyuam kom thoob plaws xya caum xyoo:

● Ua tau zoo Dual kev txiav txim:Nws ua npaws (antipyretic) thiab unceviat me rau mob hnyav (mob taub hau, thiab tsis xis nyob nrog mob khaub thuas thiab mob khaub thuas.

Cov kev ua kom muaj txiaj ntsig solubility thiab nqus:Tsis zoo li cov tshuaj aspirin, uas tuaj yeem ua rau lub plab, phenacetin yog dej ntws - insoluble tab sis yooj yim nqus ntawm lub plab zom mov. Qhov no ua rau tus smoother pib ua rau ntau tus neeg siv.

● Nco ntsoov paub txoj moo zoo:Thaum pib, nws muaj kev nyab xeeb dua li acetanilide hais txog cov mob cyanosis thiab muaj tsawg dua cov tshuaj aspirin. Qhov "maj mam" kev lees paub yog qhov tseem ceeb heev rau ntau dua- {2} {2} Serker Kev Txais.

● Synergistic muaj peev xwm:Phenacetin tsis tshua siv ib leeg. Nws lub hwj chim tiag nteg nyob rau hauv kev sib xyaw ua ke, feem ntau muaj npe nrov nrog aspirin thiab caffeine (ntsiav tshuaj), thiab tom qab nrog codeine. Cov kev sib xyaw ua ke no tau siv Synergistic cuam tshuam: cov tshuaj aspirin muab cov tshuaj tiv thaiv nruab nrab, thiab codeine ntxiv opioid {{}} theem mob nyem nyem. Cov synergy ua APC cov qauv kws tshwj xeeb nrov.

Eng Central mechanism tivthaiv:Thaum sib qhia tawm peripheral cyclooxygarase (COx) inpirition nrog cov tshuaj aspirin (tab sis tsis muaj peev xwm tsawg dua), cov ntaub ntawv pov thawj pom zoo phenacetin li cassabnrallynyob rau hauv lub hlwb thiab tus txha caj qaum. Nws cov metabolite nquag, Paracetamol (acetaminophen), yog paub rau central cox-2 thiab mariant "carbor, thiab kev tawm tsam ntawm kev nqis los ntawm txoj kev. Phenacetin nws tus kheej yuav pab ncaj qha rau qhov kev ua haujlwm hauv nruab nrab ua ntej metabolism.

Los ntawm 1890s los ntawm xyoo 1950, phenacetin yog ib qho kev kho mob ubiquitous)

● Ua mob ua poj niam ua npau taws (antipyresis):Kev kho mob tseem ceeb rau kev fevers txuam nrog kev kis tus mob xws li khaub thuas thiab mob khaub thuas.

Tshuaj xyuas qhov mob (Analesia):Dav siv rau mob taub hau (suav nrog migraines), mob hniav, coj khaub ncaws coj khaub ncaws (DysmenorrSea), neuralgias, thiab rheumatic qhov mob.

● "Muaj kev nyab xeeb" OTC xwm txheej:Nws thawj qhov kev nyab xeeb profile coj mus rau cov ntaub ntawv muaj kev tiv thaiv, ua nws tsev neeg staple.

● Kev sib xyaw kev kho cov tho kev siv hluav taws xob:Nws lub luag haujlwm hauv ApC zoo heev hauv APC thiab APC + codeine sib xyaw ua ke ua ntej rau kev ua ke rau kev sib xyaw ua ke. Qhov pom tau tau txais txiaj ntsig tau txhim kho kev ua tau zoo nrog cov tshuaj uas muaj peev xwm txo cov tshuaj thiab kev tsim kom muaj kev tsim nyognyob rau hauv lub sij hawm luv luv.

● Mechanism ntawm kev nqis tes ua:

○ Attipyricity:Feem ntau cov nyiaj txiag los ntawm inhibiting prostaglandin synthesis hauv hypothalamus (lub hlwb lub hlwb thermoregulatory Center) ntawm COX Enzyme inhibition. Qhov no txwv tsis pub nce ntawm lub cev "ntsuas cua sov" teeb tsa tshwm sim los ntawm pyrogens.

○ Ntsuas:Ib lub me ntsis sib xws:

Periperal:Kev inhibition dag ntawm cox enzymes ntawm lub xaib ntawm kev raug mob, txo prostaglandin - Kev mob mob kom zoo nkauj.

    ◇Central:Lub hom phiaj xwm txheej. Phenacetin thiab nws cov metabolites (tshwj xeeb tshaj yog paracetamol) Inhibit Cox, tshwj xeeb yog ISOForms hauv lub hlwb (COX-2, muaj peev xwm txo cov prostaglandin synthesis koom nrog kev ua mob. Lawv kuj ua kom cov neeg inusities txoj hauv kev cuam tshuam nrog Serotonin (5-ht), Dampening mob teeb liab kev kis mob hauv tus txha caj qaum.

● Muab tshuaj (keeb kwm):Raug ib tus neeg laus cov neeg laus koob nrov nrov los ntawm300 mg rau 600 mgCov. Cov koob tshuaj txhua hnub tuaj yeem ncav cuag1.5 grams rau 3 grams, feem ntau muab faib ua 3-4 txheej txheem. Qhov tseeb, kev sib xyaw ua ke (zoo li APC ntsiav tshuaj uas muaj 150-250mg cov tshuaj tsw qab, 200-250mg feffirin, 200-250mg cov paffeine) tau nquag coj ntau zaus, ua rau muaj kev sib tw muaj ntau yam.

● Metabolism thiab "kev voj voog":Phenacetin undergoes ntau ua ntej -}} dhau metabolism hauv daim siab. Tus thawj txoj hauv kev koom nrog:

○ Deethylation:(Txoj kev loj) cov ntaub ntawv covua zogmetaboliteParacetamol (acetaminophen)Cov. Qhov no yog lub luag haujlwm rau ib feem tseem ceeb ntawm lub hauv paus analgesic thiab antipyretic teebmeem.

Ydroxylation:Ntawvtsawgmetabolites, suav nrog 2-hydroxyphenetidine thiab 3-hydroxyphenetidine.

○ Deacetylation:Cov ntawv p - phenetidine, uas yog ntxiv oxidized.

Tanda lub tswvyim:Tsis zoo li txhais tau txog kev ua haujlwm zoo li Anabolic Steroids, phenacetin's "yog hais txog nws cov kev sib tw metabolic. Ib feem loj cycles los ntawm paracetamol, uas yog tom qab ntawd txuas ntxiv conjugated (glucuronidated lossis sulfated) rau kev nyab xeeb tawm. Txawm li cas los xij, ib feem tseem ceeb yuav siv lwm txoj kev metabolic paths ua rau muaj tshuaj lom neeg lom neeg.

Ib nrab - lub neej:Phenacetin nws tus kheej muaj qhov tsis tshua muaj ntshav ib nrab ib nrab - lub neej, kwv yees ntawmKwv yees li 45 feeb txog 1.5 teevhauv tib neeg. Qhov kev ploj ntais nrawm los ntawm kev ncig ua si tau txais nrawm hepatic cov metabolism. Txawm li cas los xij, ib nrab - lub neej ntawm nwsua zogmetabolite, paracetamol, ntev dua (ib ncig1.5 txog 3 teev). Thuam, ib nrab - lub neej ntawm nwsNephrotoxic thiab Carcinogenic Metabolitestau tsawg txhais tab sis lawv txoj kev ris nra hnyav, tshwj xeeb tshaj yog nrog ntev ntev {{}} dose nkag, muaj pov thawj kev tsis zoo.

Phenacetin's Golden era xaus li ntev {}} {} Txoj kev pheej hmoo yog qhia txog kev pheej hmoo mus rau kev lom zem,

Analgesic Analgesic Nephopaty (Phenacetin Magritis): This was the defining toxicity. Chronic abuse (often >1Kg Cumulers Tshuaj Ntau Xyoo) ua rau lub raum tsis txaus ntseeg tus cwj pwm los ntawm:

○ Paposis:Kev tuag ntawm cov lus qhia ntawm lub raum papillae, tseem ceeb rau zis.

Parentititial:O thiab scarring ntawm lub raum cov ntaub ntawm lub tubules.

○ Me nyuam:Ntaus nqi rau ntau yam:

◇ Qhov tseeb ncaj qha ntawm phenacetin thiab nws cov metabolites thiab nws cov metabolites (p}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}} ecines papillary vasculature.

Accument Cov metab nrho cov metabolites hauv lub raum me me vim yog cov tshuaj tiv thaiv kab mob.

◇ oxidative kev nyuaj siab thiab lipid peroxidation nyob rau hauv lub raum.

◇ ischemia (txo cov ntshav txaus) rau papillae.

Elegences:Kev vam meej rau lub raum tsis ua hauj lwm, kub siab, mob txeeb chaw, thiab muaj kev pheej hmoo ntawm cov kabmob Urothelial.

●hthemoglobinemia thiab hemolytic anemia:Thaum tsis tshua muaj pa ntau dua nrog acetanilide, kev ua phem rau kev tsis muaj pa medomogogy (G6yPing Dehydrogenase (G6PD) tsis muaj peev xwm. Cov qia no los ntawm oxidative metabolites zoo li hydroxylamines thiab Nitroses derivatives ua mob hemoglobin thiab ntshav liab mis.

● Carcinogenicity:Kev Kawm Txog Kev Kawm Epidemiological, tshwj xeeb yog los ntawm cov cheeb tsam nrog siab phenacetin kev tsim txom (piv txwv li, Australia, qhia txog qhov kev pheej hmoo siabUrothelial Carcinomas(Cov qog nqaij hlav ntawm lub plab zom mov, tso zis, thiab zais zis). Qhov no tau txuas ncaj qha rau cov Nepropathy thiab tus mob mob tso zis rau cov phenacetin amine metabolens, uas yog paub Carcinogens muaj peev xwm ua rau DNA kev puas tsuaj.

Lwm yam tshuaj lom:Cov tawv nqaij tiv thaiv (pob pob, cov tshuaj sib xyaw ua pa), muaj kev cuam tshuam nrog cov tshuaj ntxiv rau kev txhawj xeeb.

Anwhothming cov pov thawj ntawm kev loj hlob loj thiab carcinogenicity coj mus rau lub ntiaj teb kev cai teb:

Ua lag luam rho tawm:Pib thaum xyoo 1960 thiab ua kom nrawm nroos txog xyoo 1970 thiab 1980s, phenacetin tau muab rho tawm hauv ntau lub tebchaws (piv txwv li, UK 1980, Australia, ntau lub tebchaws European). Tam sim no tau txwv lossis txwv tsis pub siv thoob ntiaj teb.

● Cov Paracetamol:Ironically, phenacetin txoj kev poob siab cem txoj hauj lwm ntawm nws cov metabolite loj,Paracetamol (acetaminophen)Cov. Paracetamol khaws cia lub hauv paus analgesic thiab antipyretic tau txais kev pheej hmoo ntawm nepapotoxicity thiab carapeTicTicity ntawm kho cov tshuaj ( Paracetamol tau los ua cov xwm txheej tsis yog- opioid analgesic, hloov phenacetin hauv OTC thiab cov tshuaj sib txuas.

● ● Kev qhia qib siab:

Staaib cov toxicity yog qhov tseem ceeb:Phenacetin underscores uas cov tshuaj muaj kev nyab xeeb rau luv-}}}- kev noj haus. Nws yuam ib lub paradigm hloov mus rau nruj ntev -} kev ntsuas kev nyab xeeb.

○ Metabolites Math:Cov tshuaj lom tsis yog los ntawm niam txiv yeeb tshuaj, tab sis los ntawm nws cov metabolites. Nkag siab metabolic pathways yog qhov tseem ceeb rau kev ntsuas kev nyab xeeb.

○ Cov kev pheej hmoo ua ke:Thaum sib xyaw ua ke muab cov txiaj ntsig, lawv tuaj yeem npog npog cov koob tshuaj ntawm ib leeg ntawm tus kheej thiab ua haujlwm lom zem rau kev nyiam. Phenacetin cov koob tshuaj ntau hauv cov kev sib txuas ua ke tau yog qhov tseem ceeb hauv cov neeg mob Mepropathy raug mob.

○ Post - Kev Ua Lag Luam Kev Lag Luam yog qhov tseem ceeb:Ntau cov tshuaj lom neeg tsuas yog tawm tom qab siv tau ntawm kev siv thoob plaws, ua rau muaj kev tsim nyog ntawm kev siv lub tshuab pharics.

○ Qhov kev pheej hmoo ntawm Otc tsim txom:Kev siv tau yooj yim rau kev siv tshuaj muaj zog tuaj yeem ua rau muaj kev mob siab rau mob siab thiab vam khom, tshwj xeeb yog thaum kho mob ntev.

Kev Lag Luam Npe	Clomiphene, Clomifene, Clomid
Cas	62-44-2
Tus hniav loj	179.216
Mf	C10H13no2
Kev coj dawb huv	Saum toj no 98%
Kev tsim nyog	Dawb crystalline hmoov

 

 

Kev xav tau, thov hu rau peb

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Phenacetin tsis yog ib hom tshuaj xwb; Nws yog qhov tshwm sim uas ua kom pom kev kho analgesic rau ntau tiam neeg. Nws cov kev ua kom muaj zog thiab ua kom muaj txiaj ntsig, tshwj xeeb hauv kev sib txuas ua ke, muab txoj nyem ncaj rau ntau lab. Txawm li cas los xij, nws txoj kev khi lus yog irrevocably khi rau tus neeg soj xyuas phem ntawm analgesic nephropathy thiab urothialial cancer ua rau muaj kev raug tsim txom. Nws zaj dab neeg yog ib zaj dab neeg muaj zog, ceev faj txog cov kev siv tshuaj yeeb, cov xwm txheej tsis txaus ntseeg, thiab qhov tseem ceeb rau kev saib xyuas kev nyab xeeb ntev. Thaum hloov los ntawm kev nyab xeeb paracetamol, phenacetin tseem ceeb toom keeb kwm ntawm tus kheej yog tsis tau muaj kev nyab xeeb heev ntawm cov tshuaj muaj kev vam meej. Nws nce thiab caij nplooj ntoos hlav tseem hloov chaw muag khoom, kev lom zem, thiab kev cai siv yeeb tshuaj.

Cim npe nrov: Phenacetin rau Antipyrict thiab Analgesic Cas: 62-44-2, Suav Teb Ua Haujlwm Antipyretic thiab Analgesic Cas: 62-44-2 Cov Chaw Tsim Tshuaj, Chaw Tsim Tshuaj, Hoobkas