Analogues ntawm penicillin tau qhib lub sijhawm tshiab rau cov kws kho mob hauv kev kho cov kab mob sib kis. Lawv tiv taus ntau dua rau cov kab mob enzymes thiab qhov hnyav ntawm lub plab, thiab muaj kev phiv tsawg dua.
About penicillins
Penicillins yog cov tshuaj tua kab mob qub tshaj plaws. Lawv muaj ntau hom, tab sis qee qhov ntawm lawv tau poob lawv qhov cuam tshuam vim kev tiv thaiv. Cov kab mob muaj peev xwm hloov tau thiab ua rau qhov tsis hnov tsw ntawm cov tshuaj no. Qhov no yuam cov kws tshawb fawb los tsim cov pwm tshiab, analogues ntawm penicillin, nrog cov khoom tshiab.
Penicillins muaj toxicity tsawg rau lub cev, siv dav dav thiab qhia tau zoo ntawm cov kab mob bactericidal, tab sis kev tsis haum rau lawv muaj ntau dua li cov kws kho mob xav tau. Qhov no yog vim cov organic xwm ntawm cov tshuaj tua kab mob. Lwm qhov tsis zoo kuj tuaj yeem raug ntaus nqi los ntawm qhov nyuaj ntawm kev sib txuas nrog lwm cov tshuaj, tshwj xeeb tshaj yog cov zoo sib xws hauv chav kawm.
History
Thawj qhov hais txog penicillins hauv cov ntaub ntawv tau tshwm sim hauv xyoo 1963, hauvib phau ntawv hais txog Indian tshuaj txiv neej. Lawv siv cov tshuaj sib xyaw ua ke ntawm fungi rau kev kho mob. Thawj zaug hauv ntiaj teb kev pom kev, Alexander Fleming tau tswj kom tau lawv, tab sis qhov no tsis tshwm sim lub hom phiaj, tab sis los ntawm kev sib tsoo, zoo li txhua qhov kev tshawb pom zoo.
Ua ntej Tsov Rog Ntiaj Teb Zaum Ob, cov kws kho mob hauv tebchaws Askiv tau ua haujlwm txog qhov teeb meem ntawm kev tsim cov tshuaj hauv cov ntim uas xav tau. Tib qhov teeb meem tau daws nyob rau hauv parallel hauv Tebchaws Meskas. Txij thaum ntawd los, penicillin tau dhau los ua cov tshuaj siv ntau tshaj plaws. Tab sis dhau sij hawm, lwm pab pawg ntawm cov tshuaj tua kab mob raug cais thiab ua ke, uas maj mam hloov nws ntawm lub podium. Tsis tas li ntawd, cov tshuaj tiv thaiv tau pib tsim cov kab mob, ua rau nws nyuaj rau kev kho mob hnyav.
Lub hauv paus ntsiab lus ntawm kev siv tshuaj tua kab mob
Cov phab ntsa ntawm cov kab mob muaj cov tshuaj hu ua peptidoglycan. Cov tshuaj tua kab mob penicillin cuam tshuam rau kev sib txuas ntawm cov protein no los ntawm inhibiting tsim cov enzymes tsim nyog. Cov kab mob tuag vim tsis muaj peev xwm rov ua dua tshiab ntawm phab ntsa ntawm tes.
Txawm li cas los xij, qee cov kab mob tau kawm los tiv thaiv kev ua phem phem li no. Lawv tsim beta-lactamases, uas rhuav tshem cov enzymes uas cuam tshuam rau peptidoglycans. Txhawm rau tiv thaiv qhov teeb meem no, cov kws tshawb fawb yuav tsum tsim cov tshuaj tua kab mob penicillin uas tuaj yeem rhuav tshem beta-lactamase ib yam nkaus.
Kev phom sij rau tib neeg
Thaum pib ntawm lub sijhawm tshuaj tua kab mob, cov kws tshawb fawb tau xav txog tias lawv yuav ua li cas rau tib neeg lub cev, vim tias yuav luag tag nrhocov metrics nyob yog tsim los ntawm cov proteins. Tab sis tom qab muaj cov kev tshawb fawb txaus, peb pom tias tsis muaj peptidoglycan hauv peb lub cev, uas txhais tau hais tias cov tshuaj tsis tuaj yeem ua rau muaj kev phom sij loj.
Action spectrum
Xyaum txhua yam ntawm penicillins cuam tshuam rau cov kab mob gram-zoo ntawm cov genus staphylococcus, streptococcus, corynebacterium diphtheria thiab cov kab mob plague. Tsis tas li ntawd, lawv cov spectrum ntawm kev ua muaj xws li tag nrho cov kab mob gram-negative microorganisms, gonococci thiab meningococci, anaerobic bacilli thiab txawm ib co fungi (piv txwv li, actinomycetes).
Cov kws tshawb fawb tab tom tsim ntau thiab ntau hom tshuaj penicillins, sim tiv thaiv cov kab mob kom tsis txhob siv rau lawv cov kab mob bactericidal, tab sis cov tshuaj pab pawg no tsis tsim nyog rau kev kho cov kab mob nosocomial lawm. Ib qho ntawm cov khoom tsis zoo ntawm hom tshuaj tua kab mob no yog dysbacteriosis, txij li tib neeg txoj hnyuv raug colonized los ntawm cov kab mob uas nkag siab rau cov teebmeem ntawm penicillin. Qhov no tsim nyog nco ntsoov thaum noj tshuaj.
hom hom (kev faib tawm)
Cov kws tshawb fawb niaj hnub no qhia txog kev faib cov tshuaj penicillins ua plaub pawg:
- Ntuj, uas yog synthesized los ntawm nceb. Cov no suav nrog benzylpenicillins thiab phenoxymethylpenicillin. Cov tshuaj no muaj qhov nqaim ntawm qhov ua haujlwm, feem ntau tawm tsam cov kab mob gram-tsis zoo.
- Semi-synthetic tshuaj tiv thaiv penicillinase. Lawv yog siv los kho ntau yam kab mob. Cov neeg sawv cev: methicillin, oxacillin, nafcillin.
-
YCarboxypenicillins (carbpenicillin).
-
Pab pawg ntawm cov tshuaj dav dav:
- ureidopenicillins;-amidopenicillins.
Biosynthetic Forms
Piv txwv li, nws tsim nyog muab qee yam tshuaj uas muaj ntau tshaj plaws nyob rau lub sijhawm uas sib haum rau pab pawg no. Tej zaum qhov nto moo tshaj plaws ntawm pennicillins tuaj yeem suav hais tias yog "Bicillin-3" thiab "Bicillin-5". Lawv tau pioneer ib pab pawg ntawm cov tshuaj tua kab mob ntuj thiab yog cov flagships nyob rau hauv lawv cov qeb kom txog rau thaum ntau cov ntaub ntawv ntawm cov tshuaj tua kab mob tuaj nrog.
- "Extencillin". Cov lus qhia rau kev siv hais tias nws yog tshuaj tua kab mob beta-lactam ntev. Cov lus qhia rau nws siv yog exacerbations ntawm rheumatic kab mob thiab kab mob tshwm sim los ntawm treponema (syphilis, yaws thiab pinta). Muaj nyob rau hauv hmoov. "Extencillin" cov lus qhia rau kev siv tsis pom zoo kom ua ke nrog cov tshuaj uas tsis yog-steroidal anti-inflammatory (NVPS), vim muaj kev sib tw sib tw. Qhov no yuav cuam tshuam rau kev ua tau zoo ntawm kev kho mob.
- "Penicillin-V" belongs rau pawg phenoxymethylpenicillins. Nws yog siv los kho cov kab mob sib kis ntawm cov kab mob ENT, daim tawv nqaij thiab cov mucous membranes, gonorrhea, syphilis, tetanus. Nws yog siv los ua kev tiv thaiv kev tiv thaiv tom qab kev phais, txhawm rau tiv thaiv kev mob rheumatism, chorea, kab mob endocarditis.
- Tshuaj tua kab mob "Ospen" yog ib qho piv txwv ntawmyav dhau los tshuaj. Nws tuaj nyob rau hauv daim ntawv ntawm cov ntsiav tshuaj los yog granules. Nws tsis pom zoo kom ua ke nrog NVPS thiab cov tshuaj tiv thaiv qhov ncauj. Feem ntau siv rau kev kho mob thaum yau.
Semi-synthetic forms
pawg tshuaj no suav nrog tshuaj kho cov tshuaj tua kab mob uas tau los ntawm pwm.
- Thawj ntawm daim ntawv teev npe no yog "Amoxicillin". Cov lus qhia rau kev siv (nqi - txog ib puas rubles) qhia tau hais tias cov tshuaj muaj ib tug dav spectrum ntawm kev txiav txim thiab yog siv rau cov kab mob ntawm yuav luag txhua lub zos. Nws qhov zoo dua yog tias nws ruaj khov nyob rau hauv ib puag ncig acidic ntawm lub plab, thiab tom qab nqus tau, cov concentration hauv cov ntshav siab dua li lwm cov neeg sawv cev ntawm pab pawg no. Tab sis tsis txhob muab "Amoxicillin". Cov lus qhia rau kev siv (tus nqi yuav txawv nyob rau hauv ntau cheeb tsam) ceeb toom tias cov tshuaj yuav tsum tsis txhob muab rau cov neeg mob uas muaj mononucleosis, ua xua thiab cov poj niam cev xeeb tub. Kev siv mus ntev tsis tuaj yeem ua tau vim muaj qhov cuam tshuam loj heev.
- Oxacillin sodium ntsev yog tshuaj thaum cov kab mob tsim penicillinase. Cov tshuaj yog acid-resistant, nws tuaj yeem noj hauv qhov ncauj, nws zoo absorbed hauv cov hnyuv. Nws yog tawm sai sai los ntawm ob lub raum, yog li nws yog ib qho tsim nyog yuav tsum ua kom lub siab xav tau nyob rau hauv cov ntshav. Qhov tsuas yog contraindication yog kev tsis haum tshuaj. Muaj nyob rau hauv cov ntsiav tshuaj lossis hauv vials ua kua rau txhaj tshuaj.
- Tus neeg sawv cev kawg ntawm cov tshuaj tua kab mob ib nrab yog ampicillin trihydrate. Cov lus qhia rau kev siv (cov ntsiav tshuaj) qhiatias nws muaj kev ua haujlwm dav dav, cuam tshuam rau cov kab mob Gram-negative thiab Gram-positive. Nws tau txais txiaj ntsig zoo los ntawm cov neeg mob, tab sis yuav tsum ceev faj rau cov neeg uas noj cov tshuaj tiv thaiv coagulants (piv txwv li, cov neeg muaj kab mob ntawm cov hlab plawv), vim tias cov tshuaj muaj zog rau lawv qhov kev ua.
Solvent
Penicillins muag hauv khw muag tshuaj ua hmoov rau txhaj. Yog li ntawd, rau intravenously los yog intramuscular tswj, lawv yuav tsum tau yaj nyob rau hauv ib tug kua. Hauv tsev, koj tuaj yeem siv cov dej distilled rau kev txhaj tshuaj, isotonic sodium chloride tov los yog tov ntawm ob feem pua novocaine. Nws yuav tsum nco ntsoov tias cov kuab tshuaj yuav tsum tsis txhob sov heev.
Indications, contraindications thiab phiv
Cov lus qhia rau kev kho tshuaj tua kab mob yog kuaj pom: lobar thiab focal pneumonia, pleural empyema, sepsis thiab septicemia, septic endocarditis, meningitis, osteomyelitis. Cov kab mob tonsillitis, diphtheria, scarlet fever, anthrax, gonorrhea, syphilis, purulent daim tawv nqaij kab mob poob rau hauv lub teb ntawm kev ua.
Muaj ob peb contraindications rau kev kho mob nrog penicillin pawg. Ua ntej, lub xub ntiag ntawm hypersensitivity rau cov tshuaj thiab nws derivatives. Qhov thib ob, tsim kev kuaj mob vwm, uas ua rau nws tsis tuaj yeem txhaj tshuaj rau hauv cov leeg txha caj qaum. Raws li kev xeeb tub thiab lactation, nyob rau hauv cov ntaub ntawv no, cov txiaj ntsig kev cia siab yuav tsum muaj ntau tshaj qhov kev pheej hmoo, vim hais tias placental barrier yog permeable rau penicillins. Thaum noj tshuajtus me nyuam yuav tsum tau hloov mus rau lwm txoj kev pub mis ib ntus, vim tias cov tshuaj nkag mus rau hauv cov mis nyuj.
Cov kev mob tshwm sim tuaj yeem tshwm sim ntawm ntau qib ib zaug.
Los ntawm ib sab ntawm lub hauv nruab nrab lub paj hlwb, xeev siab, ntuav, excitability, meningism, convulsions thiab txawm coma yog ua tau. Kev tsis haum tshuaj yog tshwm sim nyob rau hauv daim ntawv ntawm daim tawv nqaij ua pob liab vog, kub taub hau, mob pob qij txha thiab o. Cov neeg mob anaphylactic poob siab thiab tuag tau raug tshaj tawm. Vim muaj cov kab mob bactericidal, candidiasis ntawm qhov chaw mos thiab qhov ncauj kab noj hniav tuaj yeem ua tau, nrog rau dysbacteriosis.
Txoj kev siv
Nrog ceev faj, yuav tsum tau muab tshuaj rau cov neeg mob uas muaj lub siab tsis zoo thiab lub raum ua haujlwm, nrog lub plawv tsis ua haujlwm. Nws yuav tsum tsis txhob raug pom zoo siv rau cov neeg uas muaj kev tsis haum tshuaj, nrog rau cov neeg uas muaj qhov tsis haum rau cephalosporins.
Yog tias tsib hnub tom qab pib kho, tsis muaj kev hloov pauv ntawm tus neeg mob tus mob, ces nws yuav tsum tau siv cov tshuaj penicillin analogs lossis hloov cov tshuaj tua kab mob. Ib txhij nrog kev teem sijhawm, piv txwv li, cov tshuaj "Bicillin-3", yuav tsum tau saib xyuas kom tsis txhob muaj cov kab mob fungal superinfection. Rau qhov no, cov tshuaj tiv thaiv kab mob tau sau tseg.
Nws yuav tsum tau piav qhia meej rau tus neeg mob tias kev cuam tshuam ntawm cov tshuaj tsis muaj laj thawj zoo ua rau cov kab mob tsis zoo. Thiab kom kov yeej nws, koj yuav xav tau cov tshuaj muaj zog uas ua rau muaj kev phiv loj heev.
Analogues ntawm penicillin tau dhau los ua qhov tseem ceeb hauv cov tshuaj niaj hnub no. Txawm hais tias qhov no yog thawj pab pawg tshuaj tua kab mob, nws tseem muaj feem cuam tshuam rau kev kho mob meningitis, gonorrhea thiab syphilis, muaj qhov dav txaus spectrum ntawm kev txiav txim thiab mob me me uas yuav tsum tau muab rau cov menyuam yaus. Tau kawg, zoo li txhua yam tshuaj, penicillins muaj contraindications thiab phiv, tab sis lawv muaj ntau tshaj li offset los ntawm kev siv.
