CaafimaadkaDiyaarinta

GCS - in dawadan? The ficil iyo saamaynta glucocorticosteroids daroogada

Sida xaqiiqada ah aad weligaa maqlay hormoonnada steroid. Our jirka si joogto ah iyaga ka soo saartaa in ay sharciyaynta geeddi socodka nolosha. In this article, waxaan ka fiirsan doonaa glucocorticoids - hormoonnada steroid, kuwaas oo la soo saaray ee kiliyaha adrenal. Iyada oo inta badan oo naga mid ah ayaa xiiso u analogues dardaro ay - GCS. Waa maxay daawada? Waayo, taas oo ay la isticmaalay iyo nooca waxyeellada ay keeni? Aan aragno.

macluumaad guud oo ku saabsan GCS. Waa maxay daawada?

Our shaqeeyo synthesises hormoonnada steroid sida glucocorticoids. Waxaa loo soo saaray kiliyaha adrenal, iyo isticmaalka waxa inta badan la xiriira daaweynta kaafi adrenal. Maalmahan, iyadoo la isticmaalayo ma aha oo kaliya glucocorticoids dabiiciga ah, laakiin sidoo kale analogues ay isku dardaro - GCS. Waa maxay daawada? Waayo, aadanaha, analogs ula jeeddaan badan, sida ay leeyihiin on, jirka, antishock, saamayn anti-xasaasiyad jidhka anti-bararka.

Glucocorticoids u noqday isticmaalaa sida daawooyinka (gudbiyo ee maqaalka - PM) ee 40-mada ay qarnigii XX. By dhamaadka ee 30meeyada ee qarnigii labaatanaad, saynisyahano helay xeryahooda hormone steroid ee kiliyaha adrenal aadanaha, iyo in 1937 uu soo xulay deoxycorticosterone mineralocorticoid. In hore 40-mada ayaa laga dheefayo hydrokortisoni glucocorticoid iyo cortisone. saamaynta pharmacological of cortisone iyo hydrokortisoni ahaayeen si kala duwan, in la go'aansaday in ay u isticmaalaan sida daroogada. Muddo ka dib, culumadu fuliyay ay Avv.

The glucocorticoid ugu firfircoon ee u shaqeeyo aadanaha waa - cortisol (analoogga - hydrokortisoni, kuwaas oo qiimo - 100-150 rubles), oo loo arko waaweyn ah. Sidoo kale waa suurto gal ah in loo qoondeeyo firfircoon ka yar: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

Oo dhan glucocorticoids dabiiciga ah sida isticmaalka daroogada helay hydrokortisoni iyo cortisone oo kaliya. Si kastaba ha ahaatee, saamaynta dambe kooxda sababaha dhowr jeer oo ka hormone kale oo kasta, taas oo ah sababta waqtiga xaadirka ah ay isticmaalka daawada waa mid xadidan. Si aad u taariikhda, kaliya loo isticmaali hydrokortisoni glucocorticoid ama esters ay (hemisuccinate hydrokortisoni iyo copolymer hydrokortisoni).

glucocorticosteroids ku saabsan (glucocorticoids dardaro), hadda waxaan ku dhexsameeysmo jirka tiro ka mid ah wakiilada sida, dhex u fluorinated (flumethasone, triamcinolone, betamethasone, Dexamethasone, iwm) Oo aan fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

wakiilada noocan oo kale ah oo firfircoon ka badan dhigooda dabiiciga ah ay, oo waxaa looga baahan yahay si loogu daweeyo ee qaadasho yar yar.

hab ay of tallaabo of corticosteroids

tallaabo ee glucocorticoids heerka kelli si buuxda looma fahmin. Qubarada badankooda ayaa aaminsan in daawooyinkan dhaqmaan on unugyada heerka of regulation of qoraal hiddo.

Corticosteroids ula falgalaan receptors glucocorticoid intracellular joogaan in shiidaa unug kasta oo jidhka bini'aadamka. Maqnaanshaha receptors hormone (kuwaas oo ah borotiinada cytosolic) waxaa si fudud u furi. In gobolka firfircoonayn, ay qayb ka mid ah heterocomplexes, kaas oo sidoo kale ka mid ah immunophilin, borotiinada lama filaan ah kulaylka iyo sidaas yihiin.

Marka steroids gasho unugyada (iyada oo xuub), Waxay isku xidhxidhaan si receptors iyo dhaqaajiso adag "glucocorticoid + receptor", ka dib markii taas ay geleyso bu'da unugga lana macaamila gobollada DNA taasoo ku yaalaan hiddo steroid jab horumariyaha u dhiganta (waxay sidoo kale waxaa loo yaqaan glucocorticoid 'jawaabay xubno ka). Complex "+ receptor glucocorticoid" waa awoodaa inuu xeeriyo (joogsada ama, taas bedelkeeda, dhaqaajiso) geeddi-socodka of qoraal ah hiddo-gaar ah. Tani waa waxa keenaysaa in xakamaynta ama kicinta ee mRNA, iyo sidoo kale isbedel ah ee ereygu wuxuu ahaa ee falgalka kala duwan iyo borotiinada sharciyeed in ay dhexdhexaadiyaan saamaynta gacanta.

waxbarashada kala duwan ayaa muujinaya in "glucocorticoid + receptor" adag waxaa ka jawaabay arrimo qoraal kala duwan, tus, sida factor nuclear Kappa B (NF-kB), ama activator ee protein qoraal (AP-1) in nidaaminaya hiddo ku lug leh wax ka qabashada difaaca jirka, iyo caabuq (molecules Amda, hiddo-cytokine, protease iyo wixii la mid ah.).

Saamaynta ugu weyn ee GCS

saamaynta glucocorticoids on jidhka bini'aadamka tiro badan yihiin. hormoonnada waxay leeyihiin antitoxic antishock, imunnodepressivnoe, antiallergic tallaabo,, antiinflammatory iyo antiinflammatory. Bal aynu eegno dhow sida falalka corticosteroids.

  • saamaynta anti-bararka ee corticosteroids. Sababay xakamaynta dhaqdhaqaaqa ee phospholipase liberatiou A 2. Marka Iscelin of enzyme this ee jidhka bini'aadamka u dhigan (daayo) Iscelin of arachidonic acid iyo formation of qaar ka mid ah dhexdhexaadiyayaal bararka (D. sida prostaglandins, leukotrienes, iyo troboksan t.). Waxaa intaa dheer, glucocorticosteroids dhaweynta yaraynaysaa qubaan dheecaan maadoyinka, vasoconstriction (cidhiidhi), horumar of microcirculation ee barar ah.
  • saamayn Anti-xasaasiyad ah GCS. Waxay dhacdaa iyada oo sababtu tahay hoos dheecaan iyo Avv dhexdhexaadiyayaasha xasaasiyadda, yareeyo wareegaya basophils, Iscelin of sii daayo histamine ka basophils iyo unugyada waaweyn wacyi, yaraynta tirada B iyo limfosaytis T, yaraynta dareenka unugyada u dhexdhexaadiyayaal xasaasiyadda, isbedel jawaabta difaaca, iyo sidoo kale xakamaynta ee wax soo saarka antibody.
  • dhaqdhaqaaqa jirka ee GCS. Waa maxay daawada? Taas macnaheedu waa in daawada la xakameeyo immunogenez, loo xakameeyo soo saarka ee antibodies. Corticosteroids joogsada socdaalka unugyada asliga ah ee dhuuxa lafaha, joogsada waxqabadka of B iyo limfosaytis T joogsada sii daayo cytokines ka macrophages iyo leukocytes.
  • Anti-sun iyo saamaynta antishock of corticosteroids. Saamaynta hormoonnada sababa cadaadis dhiig oo sareeya ee aadanaha, iyo sidoo kale hawshooda u ah ee falgalka beerka ku lug-shiid ee xenon iyo endobiotikov.
  • dhaqdhaqaaqa Mineralocorticoid. Glucocorticosteroids leedahay awood aad ku dhex faafiyo sodium iyo biyaha ee jirka, kicin Digo ee potassium. Tani dardaro bedel aan ahayn sida ugu fiican ee hormoonnada dabiiciga ah, laakiin waa saamaynta on jidhka waxay leeyihiin.

Pharmacokinetics

Mudada uu garoomada ka mid ah steroids systemic waxa loo qaybin karaa:

  1. Glucocorticosteroids tallaabo gaaban (tus, hydrokortisoni, qiimaha oo kala duwan 100 ilaa 150 rubles).
  2. Glucocorticosteroids waqtiga celcelis ahaan tallaabo (prednisolone (feedback taas oo aan aad u wanaagsan), methylprednisolone).
  3. Glucocorticosteroids la tallaabo dheer (acetonide triamcinolone, Dexamethasone, betamethasone).

Laakiin ma aha oo kaliya mudada glucocorticosteroids laga yaabaa in lagu go'aamiyo. Qoondaynta iyaga ka mid ah ayaa sidoo kale waxaa laga yaabaa in hab maamulka:

  • afka,
  • sanka,
  • glucocorticosteroids neefsado.

kala soocidda Tani, si kastaba ha ahaatee, waxay khuseysaa oo keliya in ay glucocorticosteroids nidaamka.

Waxaa jira daawooyin qaar ka mid ah qaab cadar iyo kareemada (corticosteroids degaanka). Tusaale ahaan, "Afloderm". Reviews of daawooyinka sida ku fiican yihiin.

Bal aynu eegno noocyada corticosteroids systemic oo keliya.

Daawooyinka steroid ee afka si fiican u nuugo xiidmaha oo aan keeni karaa dhibaatooyin. Si firfircoon u xidhi borotiinka ee plasma (transcortin, albumin) ah. fiirsashada ugu badan ee corticosteroids afka in dhiig la gaaro 1.5 saacadood ka dib markii maamulka ka dib. Waxay mari biotransformation beerka, kelyaha (qayb) iyo unugyada kale by conjugation in glucuronide ama sulfate.

Qiyaastii 70% ka mid ah GCS conjugated raaca kaadida, 20% kale oo saxarada ka dib tilmaami doonaa, oo inta kalena - dareerayaasha kale ee noolaha (tus, ka dib). Qeybtii - 2 ilaa 4 saacadood.

Waxaad samayn kartaa miis yar oo la soo koobin pharmacokinetic of corticosteroids afka.

Glucocorticosteroids. Drugs (magacyada)

The bar-nolosha unugyada

Plasma bar-nolosha

hydrokortisoni

8-12 saacadood

0.5-1.5 saacadood

cortisone

8-12 saacadood

0.7-2 saacadood

Prednisolone (dib u eegista aan ahayn mid aad u wanaagsan)

18-36 saacadood

2-4 saacadood

methylprednisolone

18-36 saacadood

2-4 saacadood

fludrocortisone

18-36 saacadood

3.5 saacadood

Dexamethasone

36-54 saacadood

5 saacadood

steroids neefsado in bukaan eegida casri ah soo bandhigay acetonide triamcinolone, propionate fluticasone, furoate mometasone, budesonide iyo dipropionate beclomethasone.

beegyada uu Pharmacokinetic ayaa sidoo kale lagu soo bandhigi karaa miis:

Glucocorticosteroids. Drugs (magacyada)

The dhaqdhaqaaqa anti-bararka degaanka

mugga of qaybinta

Plasma bar-nolosha

Karti of maris iyada oo beerka

dipropionate beclomethasone

0,64 unugyada.

-

0.5 saacadood

70%

budesonide

1 unit.

4.3 l / kg

1,7-3,4 saac

90%

acetonide triamcinolone

0,27 unugyada.

1.2 l / kg

1.4-2 saacadood

80-90%

propionate fluticasone

1 unit.

3.7 l / kg

3.1 saacadood

99%

flunisolide

0.34 unugyada.

1.8 l / kg

1.6 saacadood

-

steroids sanka in daawada maanta soo bandhigay propionate fluticasone, flunisolide, acetonide triamcinolone, furoate mometasone, budesonide iyo dipropionate beclomethasone. Qaar ka mid ah iyaga ka mid ah waxaa loo yaqaan si la mid ah sida corticosteroids neefsado.

Ka dib markii codsiga ah corticosteroids sanka dose nuugo xiidmaha iyo qayb kale oo ka timaada xabka marinka hawada si toos ah dhiigga.

Glucocorticosteroids, ku xayiran jirta marinka dheef shiidka, waxaa u nuugo oo ku saabsan 1-8 boqolkiiba, iyo pass ugu horeysay iyada oo beerka biotransformed ku dhowaad gebi ahaanba si metabolites firfircoonayn.

Glucocorticosteroids oo heshay dhiiga, hydrolyze in walxaha aan firfircoonayn. Halkan waxaa miiska la koobin ay pharmacokinetic:

Glucocorticosteroids. diyaarinta

Bioavailability markii galaya dhiigga, boqolkiiba

Bioavailability marka laga mareenka caloosha iyo mindhicirka nuugo, in boqolkiiba

budesonide

34

11

dipropionate beclomethasone

44

20-25

furoate mometasone

<0.1

<1

acetonide triamcinolone

Information No

10,6-23

propionate fluticasone

0.5-2

flunisolide

40-50

21

Daroogooyinka sida "Afloderm" (feedback oo xajiya dhisayaa on shabaqa), si ay u sharxaan si gooni gooni ah macno lahayn. Mid kasta oo iyaga ka mid ah waa qayb weyn ee firfircoon, taas oo ay u badan tahay in ay mar hore ayaa la xusan. daawooyinkan - corticosteroids maxaliga ah, oo ay inta badan wakiil qaab cadar ama kareemada.

Dhig therapy glucocorticosteroid (muujinaya in loo isticmaalo)

Waayo, nooc kasta oo glucocorticosteroids tilmaamo ay si loogu isticmaalo. Sayidka, corticosteroids afka waxaa loo isticmaalaa in lagu daweeyo:

  • cudurka Crohn;
  • ulcerös kolit;
  • cudurada sanbabada interstitial;
  • ba'an syndrome neefsigu;
  • oofwareen aad u daran;
  • chronic obstructive pulmonary disease wajiga ba'an;
  • neefta bronki,
  • Graves subacute;
  • kelyaha lagu dhasho (kiiskan, qofku ma soo saari corticoids isaga iyo waxaa lagu qasbay in ay qaataan analogues ay isku dardaro);
  • kaafi adrenal ba'an.

Sidoo kale steroids loo isticmaalo daaweynta bedelka ah napochechnikovoy hoose iyo sare failure.

corticosteroids Intranasal waxaa loo isticmaalaa:

  • rhinitt idiopathic (vasomotor);
  • rhinitt non-celin xasaasiyad leh eosinophilia;
  • sanka pilipoze;
  • rhinitt xasaasiyad dilka ah (joogto ah);
  • rhinitt xasaasiyad xilliyeedka (go'aysa).

corticosteroids neefsado waxa loo isticmaalaa in lagu daaweeyo chronic obstructive pulmonary disease, neefta bronki.

sababo

Taxadarka waa in lagu daweeyo GCS ee ka mid ah xaaladaha caafimaad oo:

  • nuujinta,
  • glaucoma,
  • Qaar ka mid ah cudurada wilka, kuwaas oo ay weheliso aan caadi ahayn ee epithelium;
  • fangas ama cudurada viral isha;
  • caabuq purulent;
  • muddo tallaalka;
  • waraabowga;
  • foomka firfircoon ee qaaxada;
  • cudurka herpes,
  • caabuq fangas systemic;
  • qaar ka mid ah cudurka dhimirka oo leh calaamado wax soo saar leh,
  • degree daran of kelyaha,
  • hypertension,
  • thromboembolism;
  • boog dyspepsia ama caloosha;
  • diabetes;
  • cudurka Cushing ee.

corticosteroids sanka si adag ahaan uu in kiisaska noocaas ah:

  • sangoror soo noqnoqda ee taariikhda,
  • diathesis hemorrhagic,
  • diidmo.

Glucocorticosteroids: waxyeellooyin

Dhibaatooyinka ay keento corticosteroids loo qaybin karaa hoose iyo systemic.

waxyeelo Local

Qaybsan saamaynta corticosteroids neefsado iyo sanka.

1. waxyeello ka soo gaartey Local ka glucocorticosteroids neefsado:

  • qufacdo,
  • dysphonia;
  • candidiasis ee saabka afka iyo dalqada.

2. waxyeelo Local ah corticosteroids sanka:

  • daloolin ee septum sanka,
  • sangoror,
  • gubanaya iyo xuubka xabka qalalan oo ka mid ah sanka iyo dalqada,
  • hindhiso,
  • sanka cuncun.

waxyeelo systemic

Kala qaybiyey sidii qaybo ka mid ah jidhka, kaas oo ku shaqeeyaan.

1. Qayb ka mid ah habka dhexe ee neerfayaasha:

  • waalli;
  • niyad-jabka,
  • rayn,
  • hurdo la'aan,
  • caro.

2. Tan iyo nidaamka wadnaha iyo,

  • thromboembolism;
  • thrombosis xididka dheer,
  • cadaadiska dhiigga ee sareeya,
  • myocardiodystrophy.

3. Laga bilaabo nidaamka taranka:

  • hirsutism;
  • dib u horumarinta galmada;
  • cillad galmada;
  • caadada degganayn.

4. Laga soo bilaabo nidaamka dheefshiidka:

  • beerka dufan;
  • pankreatit;
  • dhiigbaxa mareenka caloosha iyo mindhicirka,
  • boogaha steroid ka mid ah caloosha iyo mindhicirrada.

5. Laga soo bilaabo nidaam hormoonada jidhka ah:

  • diabetes;
  • Cushing ee syndrome,
  • cayilka;
  • atrophy of kiliyaha adrenal sabab u Iscelin oo ay shaqo.

6. Laga soo bilaabo dhinaca view:

  • glaucoma,
  • dambena caadka subcapsular.

7. From nidaamka muruqyada:

  • dhumin muruqa;
  • myopathy;
  • faaqidaad koritaanka carruurta;
  • galleeyda oo laf jab avascular;
  • osteoporosis.

8. Wixii maqaarka:

  • alopecia;
  • striae;
  • khafiifiya ee maqaarka.

9. Saameynada kale ee dhinac:

  • Foomamka ba'an faafa iyo chronic ee geedi socodka bararka,
  • barar,
  • sodium iyo biyo haynta ee jirka.

tallaabooyin taxaddar

Xaaladaha qaarkood, corticosteroids waa in la isticmaalaa si taxadir leh.

Tusaale ahaan, dadka qaba cirrhosis, hypothyroidism, hypoalbuminemia, iyo bukaanada neefo ama waayeelka ah waxaa la hagaajin karaa tallaabo of corticosteroids.

In codsiga ah ee corticosteroids inta ay uurka qaado waa in ay tixgeliyaan saamaynta filayo daawaynta hooyada iyo halista uu saamayn xun ah ee daroogada ee ilmaha caloosha ku, sida corticosteroids carqaladeeyo kartaa horumarinta ee koritaanka uurjiifka iyo xataa cilladaha sida dhanxanegga dillaacii iyo wixii la mid ah.

Haddii inta lagu guda jiro isticmaalka bukaanka GCS ildaran cudurka (busbuska, jadeecada, iyo D. sidaas on.), Laga yaabaa in ay dhacaan si aad u daran.

In daaweynta bukaannada qaba corticosteroids ama cudurada bararka, shalalka (rheumatoid arthritis, cudurada mindhicirka, lupus erythematosus oo nidaamsan iyo D. sida.) Aragtida iska caabin steroid oo laga dheehan karo.

Bukaanlayda qaadato steroids afka muddo dheer, waxaa lagama maarmaan ah si teelteel ah in ay qaataan dhiig weedhu saxaarada iyo mari fibroezofagogastroduodenoskopiyu sida boog steroid inta lagu guda jiro daawaynta corticosteroids laga yaabaa in aan laguugu dhibeyn.

In 30-50% bukaannada lagu daaweeyaa corticosteroids muddo dheer, horumarinta osteoporosis. Sida caadiga ah, waxa ay saamayn ku cagta, gacanta, miskaha, feeraha, dhabarta.

Dhexgalka daroogooyinka kale

All glucocorticosteroids (soocidda aanu halkan ma laha) marka xiriir la daroogooyinka kale siin saameyn gaar ah, iyo saamaynta tani ma aha had iyo jeer fiican jidhkeenna. Halkan waxa aad u baahan tahay in aad ogaato ka hor inta codsanaya corticosteroids lala daroogooyinka kale:

  1. GCS iyo laabjeexa - glucocorticosteroids nuugista hoos.
  2. GCS iyo barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - glucocorticosteroids biotransformation beerka u korodho.
  3. GCS iyo isoniazid, erythromycin - glucocorticosteroids biotransformation beerka hoos.
  4. SCSO iyo salicylates, phenylbutazone, barbiturates, digitoxin, penicillin, chloramphenicol - reebay oo dhan daawooyinkaan waxaa la wanaajiyey.
  5. GCS iyo isoniazid - xadgudub ku ah soo gunaanadeen aadanaha.
  6. Corticosteroids iyo reserpine - ah ee gobolka niyad.
  7. GCS iyo tricyclic murugada - kordhay cadaadiska intraocular.
  8. GCS iyo agonister - talaabo daawooyinkaan waxaa sii kordhaya.
  9. Corticosteroids iyo theophylline - tallaabo anti-bararka ee glucocorticoids kordhay, horumarinta saamaynta cardiotoxic.
  10. SCSO iyo diuretics, amphotericin B, mineralocorticoid - kordhiyaa halista ah ee hypokalemia.
  11. GCS iyo si aan toos ahayn xinjirowga lidka ku ah, fibrinolytics, butadiene, ibuprofen, ethacrynic acid - la raaco waxaa laga yaabaa in ay dhibaatooyin dhiigbaxa.
  12. SCSO iyo indomethacin, salicylates - darka this keeni kartaa lesions kolit of mareenka caloosha iyo mindhicirka.
  13. Corticosteroids iyo paracetamol - sumoobo daroogada waa kordhay.
  14. Corticosteroids iyo azathioprine - kordhiyaa halista ah ee caadka, myopathy.
  15. GCS iyo mercaptopurine - isku dhafan waxay keeni kartaa in fiirsashada korodhka acid uric ee dhiigga.
  16. GCS iyo hingamin - maqalka saamaynta aan la rabin ee daroogada this (sentigiiba corneal, myopathy, dermatitis).
  17. GCS iyo methandrostenolone - xoojin waxyeello ka soo gaartey ee glucocorticoids.
  18. Corticosteroids iyo diyaarinta bir ah, androgens - kordhay Avv erythropoietin, iyo asalka this, iyo kor u erythropoiesis.
  19. GCS iyo hypoglycemic daroogada - yareynta gebi ahaanba waxtarkooda.

gunaanad

Steroids - daroogada, iyada oo aan taas daawo casri ah lagama yaabo in ay ku kici. Waxay waxaa loo isticmaalaa daaweynta ee marxaladaha aad u daran cudurka, ama si fudud si kor loogu qaado tallaabo ah ee daroogada. Si kastaba ha ahaatee, sida daawooyinka oo dhan, glucocorticosteroids waxyeelo iyo aad u leeyihiin sababo. Ha illoobin ku saabsan. Kor ayaanu ku taxnay dhammaan xaaladaha halkaas oo muhiim ma ahan in ay isticmaalaan steroids, waxaana ay sidoo kale liiska dhexgalka ee corticosteroids daawooyin kale. hab ay of tallaabo of corticosteroids iyo dhammaan dhibaatooyinka ay ayaa sidoo kale halkan ku tilmaamay si faahfaahsan. Haddaba waxaad u baahan tahay inaad ka ogaato GCS, waa in hal meel ah - this article. Si kastaba ha ahaatee, kiis kasta, ha bilaabin daawada oo kaliya ka dib markii reading macluumaadka guud oo ku saabsan GCS. daawooyinkan, dabcan, waxa laga iibsan karaa warqad dhaqtar la'aan, laakiin maxaad u baahan tahay? Ka hor inta isticmaalka daroogada kasta waa in marka hore la tashato dhakhtar takhasus u leh. Noqdaan kuwo caafimaad qaba oo aan is-Dawada!

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