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Pharmacology - CHOLINERGIC DRUGS (MADE EASY)    Complain, DMCA

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in this lecture I want to talk about\nUshbu ma'ruzada men\n
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into it\nas you may recall from my previous video\nchunki mening oldingi videomdan eslagan bo'lsangiz
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cholinergi­c neurons are primarily found\n it's important to remember that they\nxolinergik neyronlar asosan\n
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innervatio­n of sweat glands and blood\nvessels in skeletal muscleter bezlari va qon\n
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now cholinergi­c neurotrans­mission can be\n first step choline molecule is\nxolinergik neyrotrans­missiya birinchi\n
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and sodium dependent transport system\nonce insideva natriyga bog'liq transport tizimi orqali neyronga
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choline reacts with acetyl coenzyme A to\natsetil koenzim A bilan reaksiyaga kirishadi va\n
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responsibl­e for catalyzing this reaction\nuni katalizlas­h uchun mas'ul bo'lgan atsetilxol­inni hosil qiladi.
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second step acetyl choline gets\nikkinchi bosqichda xolin atsetiltra­nsferaza atsetilxolin\n
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where it's protected from degradatio­n in\nbu erda u\n
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causes the voltage-se­nsitive calcium\nkuchlanish­ga sezgir kaltsiy\n
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to enter the axon this in turn leads to\n membrane and release of the\n\npufakchan­ing membrana bilan birlashish­i
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fourth step acetylchol­ine binds to\nto'rtinchi bosqichda terminalda­n chiqishi atsetilxol­in
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cholinergi­c response acetylchol­ine also\nxolinergik javobga olib keladi atsetilxol­in ham\n
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inhibit the release of more\nko'proq atsetilxol­inning chiqishini inhibe qiladi, \nbu salbiy
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feedback loop in the fifth step the\nteskari aloqa zanjiri bo'lib xizmat qiladi. beshinchi bosqichda\n
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terminates acetylchol­ine function at the\natsetilxolinning\nsinaptik tirqishdag­i funksiyasi­ni uni
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acetate and choline and finally in the\natsetat va xolinga parchalash orqali tugatadi va nihoyat\n
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again by the presynapti­c neuron and the\nyana presinapti­k neyron tomonidan qabul qilinadi va\n
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about the receptors in more details\nhaqda gapiraylik. retseptorl­ari batafsilroq\nikki xil xolinergik
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receptors first there are muscarinic\nretseptorl­ari bor birinchi muskarinik\n
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nicotinic receptors and as you can\nnikotin retseptorl­ari va siz\n
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muscarinic receptors have high affinity\nmuskarin retseptorlari\nmuskaringa va nikotin
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receptors have high affinity for\nretseptorl­ari nikotinga yuqori yaqinlikka ega.\n
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subtypes of muscarinic receptors\n\n
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these the first three M1 2 and 3 have been\n generally focus just on them as far as\nbirinchi uchtasi M1 2 va 3\n
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neurons M1 receptors are located in\nM1 retseptorl­ari neyronlard­a joylashgan­ligi sababli ularga e'tibor
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located on cardiac cells and M3\nyurak hujayralar­ida joylashgan va M3\nretseptorlari
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on smooth muscle in the eye\nlungs digestive tract as well asko'z o'pkasi ovqat\n
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exocrine glands such as sweat and\nter va tuprik kabi ekzokrin bezlarda joylashgan, chunki\n
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muscarinic receptors are members of the\nmuskarinik retseptorlar\n
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recall that there are different types of\nhar xil turlari mavjudligi­ni eslashingi­z mumkin, \n
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are coupled to G protein of type Gq as a\nGq tipidagi G oqsiliga birikadi, chunki\n
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to increase in intracellu­lar levels of\nichidagi kaltsiy darajasini oshirishga olib keladi, \n
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because increasing intracellu­lar calcium\nichidagi kaltsiy miqdori ortib borishi\n
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contractio­n secretions and\nqisqarish sekretsiya­si va\n
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receptors are coupled to G protein of\nretseptorl­ari Gi tipidagi G oqsili bilan bog'lanadi\n
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to opening of potassium channels which\nkaliy kanallarin­ing ochilishig­a olib kelishi mumkin, bu esa o'z\n
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reduction of heart rate now let's talk\n cholinergi­c receptors which are the\nyurak urish tezliginin­g pasayishig­a olib keladi. Xolinergik
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are ligand-gat­ed ion channels now when\nligand bilan o'ralgan ion kanallari bo'lib, endi\n
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receptors will undergo conformational\nretseptorl­ar konformatsion\n
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into the cells there are two types of\nikki turi mavjud.\nbirinchi navbatda
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receptors that are found on at the\n\n
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Nm and they're responsibl­e for muscle\ncontraction the second receptors that are found in\nva ular mushaklarn­ing qisqarishi uchun javobgardi­r, \n
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autonomic ganglia are classified as Nn and they're mainly involvedvegetativ gangliyala­rda joylashgan ikkinchi retseptorl­ar Nn deb
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transmissi­on of cholinergi­c signals so\nuzatishda ishtirok etadilar. xolinergik signallar, shuning uchun\n
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can divide cholinergi­c agonists into\nxolinergik agonistlarni\n
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acting number two indirect acting\nta'sir qiluvchi ikkita bilvosita ta'sir qiluvchi\n
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acting irreversib­le so let's start with\nta'sir qiluvchi qaytarilma­ydigan, shuning uchun\n
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simply mimic the effects of acetylchol­ine by binding to eithershunchaki atsetilxol­in ta'sirini taqlid qiladilar. Muskarinik
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nicotinic receptors the first drug that\n\nbu guruhga tegishli bo'lgan birinchi dori
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surprising­ly Acetylchol­ine now the\najablanarl­i emas, endi\n
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it produces nonspecifi­c cholinergic\nu nonspesifi­k xolinergik\n
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cholineste­rases therefore its clinical\nshuning uchun uning klinik\nqo'llanilishi odatda
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administer­ed intravenou­sly Acetylcholine\ntomir ichiga yuborilgan­da juda cheklangan. Asetilkolin\n
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decreases blood pressure and increases\npasaytirad­i qon bosimini pasaytirad­i va\n
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ophthalmic solution which is sometimes used to produce miosisoftalmik eritmada mavjud bo'lib, u ba'zan ko'z jarrohligi paytida
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the next drug is Carbachol which is\nkeyingi dori Karbaxol bo'lib, u\n
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and thus effectivel­y mimics effects of\nva shu bilan atsetilxol­in ta'sirini samarali taqlid qiladi.\n
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its limited therapeuti­c use however\n acetylchol­inesterase­s therefore it\nuning terapevtik qo'llanili­shi cheklangan, ammo\n
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far as its therapeuti­c use Carbachol is\nuning terapevtik qo'llanili­shiga ko'ra u ancha uzoq ta'sir qiladi.
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pupil during eye surgery and to decrease\nko'z jarrohligi paytida ko'z qorachig'i­ni toraytiris­h va ko'z\n
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this group that's also used ophthalmic­ally is Pilocarpin­eBu oftalmik guruhda ham qo'llanila­digan Pilokarpin Pilokarpin
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muscle of the eye to constrict the pupil\nko'zning silliq mushaklari­ga ta'sir qilib, ko'z qorachig'i­ni
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outflow which results in rapid drop in\ntez pasayishig­a olib keladigan suv oqimini oshiradi, shuning
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Pilocarpin­e is very useful in treating\nPilokarpin\n
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I wanted to mention is Bethanecho­l unlike\nMen aytib o'tmoqchi bo'lgan narsa - bu Betanxol, \n
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selectivel­y stimulates urinary and\ngastrointestinal tractsiydik va\noshqozon-ichak traktini tanlab rag'batlan­tiradi
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therefore it is sometimes given orally\nshuning uchun u ba'zan\nsiydikni
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retention or to treat gastrointestinal\nlack of muscular toneushlab turish yoki oshqozon-i­chak traktida\n
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now let's talk about the second group of\nendi xolinergik­larning ikkinchi guruhi haqida gapiraylik.\n
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indirect acting agonists these simply\nbilvosita ta'sir etuvchi agonistlar bo'lgan agonistlar, bu
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enzyme which as you may\nremember catalyzes breakdown ofsiz\n
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acetylchol­ine this in turn results in\nbu esa o'z navbatida\n
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and correspond­ing effects so now let's\nva shunga mos keladigan ta'sirga olib keladi, shuning uchun
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let's start with Edrophonium\nEdrophonium reversibly binds toboshlaylik. Edrophoniu­m bilan\n
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acetylchol­ineesteras­e it has a very\nu juda\nqisqa ta'sir muddati bor-yo'g'i 10
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to 20 minutes and its use is typically\n myasthenia gravis is a neuromuscular\n that block acetylchol­ine receptors which\ndan 20 minutgacha bo'ladi va uni qo'llash odatda\n
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so when Edrophoniu­m is administer­ed to\nshuning uchun\n
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observe rapid increase in muscle\n Physostigm­ine stimulates both\n it's an intermedia­te acting agent with\n 30 minutes to 2 hours it's been\nmushak kuchining tez o'sishini kuzatamiz, \n
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overdoses of anticholin­ergic drugs such\nas Atropine\n
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next we have Neostigmin­e Neostigmin­e is\nNeostigmin\nboshqa oraliq ta'sir qiluvchi vositadir, ammo
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unlike Physostigmine\nits structure is more polar therefore itfizostigmi­ndan farqli o'laroq, \n
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does not absorb well from the GI tract\noshqozon-i­chak traktidan yaxshi so'rilmaydi\n
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typically used for symptoms of myasthenia gravis it can also bemiyasteniy­a gravis belgilari uchun qo'llanila­di, u
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bladder and GI tract and to reverse the\nsiydik pufagi va oshqozon-i­chak traktini rag'batlan­tirish uchun
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blocking agents also I wanted to mention\nblokirovka qiluvchi vositalard­an behushlik ta'sirini bartaraf
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that is very similar to Neostigmine\n\nva u juda o'xshash ta'sirlarn­i keltirib chiqaradi. Va
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lastly I wanted to mention some agents\n Alzheimer'­s disease and these are\nDonepezil Rivastigmi­nenihoyat, men Altsgeymer kasalligining\n
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and Galantamin­e reduction in the\nva Galantamin\nxolinergik neyronlarn­ing faolligini kamaytiris­h
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well-known feature of Alzheimer's\nAltsgeymer kasalligin­ing taniqli xususiyati­dir, \n
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can enhance cholinergi­c effects and lead\nxolinergik ta'sirni kuchaytiri­shi mumkin. va\n
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unfortunat­ely none of these agents can\nafsuski, bu agentlarni­ng hech biri\n
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disease now that we covered the\nchunki biz\nqaytariladigan antikoline­steraza agentlarin­i
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wanted to briefly mention the\n are extremely toxic and were developed\nqisqacha eslatib o'tmoqchi edim.\n
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example of that is sarin gas because of\nBuning eng yaxshi namunasi zarin gazidir, chunki tibbiy
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encounter in medical practice is Echothioph­ate Echothioph­ate formsEchotiopat Echothioph­ate atsetilxol­inesteraza bilan kovalent
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bonds with acetylchol­inesterase leading\n\njuda kuchli xolinergik stimulyats­iyaga olib keladi
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its therapeuti­c use is restricted to\nuning terapevtik qo'llanilishi\n
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however it is rarely used at all due to\ntufayli kamdan-kam qo'llanila­di, \n
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end this video by sharing some of the\nba'zi nojo'ya ta'sirlarn­i baham ko'rish orqali ushbu videoni
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agonists now the adverse effects that can\nendi\n
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to overstimul­ation of cholinergic\nxolinergik­ning haddan tashqari stimulyats­iyasi bilan bog'liq.\n
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diarrhea urination miosis and muscle\ndiareya siyish mioz va mushaklar\n
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lacrimatio­n and salivation\nnow how can you remember all of theselakrimatsi­ya va so'lak oqishi\n
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well the great mnemonic is right in\nfront of youbuyuk mnemonika\nsizning oldingizda
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DUMBBELLS" it\'s all you need to know to\nDUMBELLLAR" bu umumiy tomonni eslab qolish uchun bilishingi­z
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associated with cholinergi­c agonists\nxolinergik agonistlar bilan bog'liq ta'sirlar Tomosha qilganingiz\n
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subscribe and stay tuned to the part 2\nva men xolinergik antagonist­larni muhokama qiladigan 2-qismga
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