GCS - ukuba eli yeza? Intshukumo kunye neziphumo neziyobisi glucocorticosteroids

Ngokuqinisekileyo ndayiva weva iihomoni steroid. umzimba wethu rhoqo uvelisa ukuba ukulawula iinkqubo ebomini. Kweli nqaku, siza kuqwalasela glucocorticoids - iihomoni steroid, leyo ziveliswa kwi uthinte adrenal. Nangona inkoliso yethu banomdla analogue zazo zokwenziwa - GCS. Yintoni liyeza? Kuba apho zisetyenziswa yaye babangela ukuba uhlobo umonakalo? Makhe sibone.

ulwazi ngokubanzi malunga GCS. Yintoni liyeza?

umzimba wethu synthesises iihomoni steroid ezifana glucocorticoids. Bona yenziweyo neuron adrenal, kwaye ukusetyenziswa kwazo kakhulu zinxulumene ekunyangeni insufficiency adrenal. Kule mihla, usebenzisa nje glucocorticoids zendalo, kodwa analogue zazo zokwenziwa - GCS. Yintoni liyeza? Kuba abantu, aba analogs kuthetha lukhulu, njengoko nayo emzimbeni anti-ukudumba, immunosuppressive, antishock, isiphumo anti-komzimba.

Glucocorticoids ezibaqhelileyo namachiza (ekubhekiselelwe kulo kwinqaku - PM) kwi-imi- 40 lwekhulu XX. Ekupheleni ye 30 zenkulungwane yamashumi amabini, izazinzulu ziye zafumanisa iikhompawundi hormone steroid kwi neuron adrenal yabantu, yaye ngowe-1937 waba ekhethiweyo deoxycorticosterone mineralocorticoid. Ekuqaleni nenani-40 zaye zathathwa glucocorticoid hydrocortisone kunye cortisone. imiphumela kwemithi yonke cortisone kunye hydrocortisone baba zahlukeneyo njalo, ukuba kwagqitywa ukusebenzisa kwabo iziyobisi. Emva kwexesha elithile, oosonzululwazi baye benza yokuqaphela zabo.

Le glucocorticoid lixakeke umzimba womuntu - cortisol (analogu - hydrocortisone, ixabiso ogama - 100-150 engange), kwaye igqalwa enkulu. Kungenzeka kwakhona ukuba isabelo esincinane esebenzayo: corticosterone, cortisone, 11-deoxycortisol,-dehydrocorticosterone 11.

Kuzo zonke glucocorticoids zendalo nokusetyenziswa kweziyobisi wafumana hydrocortisone kuphela cortisone. Nangona kunjalo, indlela oonobangela kwicala yamva rhoqo ngakumbi kunayo nayiphi na enye hormone, nto leyo esisizathu sokuba ngelo xesha lakalokunje ukusetyenziswa kwayo amayeza ulinganiselwe. Ukuza kuthi ga ngoku, esetyenziswa kuphela glucocorticoid hydrocortisone okanye esters zayo (hydrocortisone hemisuccinate kunye hydrocortisone acetate).

Ngokuphathelele glucocorticosteroids (glucocorticoids zokwenziwa), sisazithobileyo kuhlanganiswa eziliqela izinto ezinjalo, phakathi apho fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, njl) Yaye non-fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

arhente ezifana esebenzayo kunoogxa babo zendalo, kwaye kufuneka ukuba unyango ngeedosi ezincinane.

Indlela yokusebenza ye corticosteroids

Isenzo glucocorticoids kwinqanaba molekyuli akukaqondwa kakuhle. Izazinzulu zikholelwa ukuba la machiza senze kwiiseli kwinqanaba ummiselo gene tumbuluxiwa.

Corticosteroids abasebenzisana kunye receptors glucocorticoid intracellular zikhona phantse zonke iseli komzimba womntu. Xa engekho receptors traps (leyo ziiproteni cytosolic) zenziwa zingasebenzi nje. Xa urhulumente lutho, ukuba inxalenye heterocomplexes, ezibandakanya kwakhona immunophilin, iiproteni ubushushu ukothuka njalo njalo.

Xa steroids ukungena iiseli (ngokusebenzisa inwebu), bathe bandibopha ukuya receptors kunye nokusebenzisa ezintsonkothileyo "glucocorticoid + receptor", emva koko engena ngumongo iseli kwaye zisebenzisana mimandla DNA leyo ibekwe gene nomthombo Isiqwenga steroid ehambelana (nazo babiza glucocorticoid 'waphendula izinto). Complex "+ glucocorticoid receptor" uyakwazi ukulawula (kuthintelwe okanye, icala, sebenzisa) inkqubo ukhutshelo zofuzo ezithile. Le nto ikhokelela ingcinezelo okanye ukukhuthazwa mRNA, kwakunye notshintsho kuyondelelaniswe enqanda ezahlukeneyo kunye neeproteni yolawulo ukulamla neziphumo cellular.

Izifundo ezahlukeneyo zibonisa ukuba "glucocorticoid + receptor" imbaxa awasabela ngayo kunye imiba ukhutshelo ezahlukeneyo, umz, ezifana into nuclear kappa B (NF-kB), okanye isilumeki leeprothini umbhalo (AP-1) elawula izakhi inxaxheba kule omzimba, yaye ukudumba (iimolekyuli adhesion, yemfuza cytokine, protease njalo njalo.).

Iziphumo eziphambili GCS

iziphumo glucocorticoids emzimbeni womntu baninzi. Ezi hormone babe antitoxic, antishock, imunnodepressivnoe, antiallergic inyathelo, antiinflammatory kunye antiinflammatory. Makhe sihlolisise indlela izenzo corticosteroids.

• imiphumela Anti-yokukrala corticosteroids. Kwabangela ingcinezelo yomsebenzi of phospholipase A liberatiou _2. Xa inhibition yale enzyme emzimbeni yabantu zicinezelwa (release) kwi inhibition lwe CD acid kunye ukuyilwa ezinye mediators ukudumba (ezifana prostaglandins, leukotrienes, kunye troboksan t. D.). Ngaphezu koko, le glucocorticosteroids ulwamkelo kunciphisa emithanjeni fluid exudation, vasoconstriction (exineneyo), ukuphuculwa microcirculation kwi komtshiso oko.
• ukusebenza Anti-bayaliwa of GCS. Oku kwenzeka ngenxa yokuba uhle secretion kunye Yindibanisela njengabalamli nokwaliwa, ukunciphisa ajikelezayo basophils, inhibition woyekelelo histamine evela basophils kunye neeseli lwemasti ava, ukunciphisa inani B kunye lymphocyte T, ukunciphisa uvakalelo leseli ukuya njengabalamli nokwaliwa, utshintsho omzimba, kwakunye kwezithandani yemveliso omzimba.
• umsebenzi Immunosuppressive of GCS. Yintoni liyeza? Oku kuthetha ukuba amachiza anqanda immunogenez, abayithintelayo imveliso omzimba. Corticosteroids anqanda yokufuduka iiseli stem lomongo wethambo, zinqanda umsebenzi B kunye lymphocyte T zinqanda ukukhutshwa cytokines ezivela macrophage kunye leukocytes.
• Anti-ziyityhefu kwaye nefuthe antishock of corticosteroids. Isiphumo hormone ezibangelwa uxinzelelo oluphezulu lwegazi ebantwini, kwakunye ukusebenza enqanda zesibindi ababandakanyekayo ukutya of xenon kunye endobiotikov.
• umsebenzi Mineralocorticoid. Glucocorticosteroids bayakwazi ukuba ungakhawulezi sodium namanzi emzimbeni, ukuvuselela kukhuthaza potassium. Oku ababambeleyo eyenziwayo mgangathweni njengoko iihomoni zendalo, kodwa ke isiphumo emzimbeni abanazo.

Pharmacokinetics

Kuba ubude amanyathelo steroid lwenkqubo lungohlulwa lube:

1. Glucocorticosteroids amanyathelo amafutshane (umz, hydrocortisone, ixabiso apho yahluka ukusuka engange-100 ukuya-150).
2. Glucocorticosteroids nge ixesha eliqhelekileyo isenzo (prednisolone (feedback okungalungileyo kakhulu), methylprednisolone).
3. Glucocorticosteroids ngezenzo elide (triamcinolone acetonide, dexamethasone, betamethasone).

Kodwa ngexesha glucocorticosteroids inokumiselwa kuphela. Ukuhlelwa babe nako ukuba indlela wolawulo:

• ngomlomo;
• intranasal;
• glucocorticosteroids ukurhogele.

Oluhlobo, Noko ke, usebenza kuphela glucocorticosteroids kwinkqubo.

Kukho ezinye iziyobisi ngohlobo Amafutha kunye nezithambiso (corticosteroids bendawo). Umzekelo, "Afloderm". Izimvo imixube ezinjalo okulungileyo.

Makhe sijonge iintlobo corticosteroids lwenkqubo yedwa.

steroids ngomlomo baphilela ngokugqibeleleyo ethunjini ngaphandle ibangela iingxaki. Ngenkuthalo Ububophe kwiiproteni kwi plasma (transcortin, albumin). Le xi liphezulu corticosteroids yomlomo ngegazi kuso emva kweeyure 1.5 emva nolawulo. Ukuba bangenele biotransformation esibindini, zezintso (ngokomkhethe) kunye nezinye nezihlunu yi conjugation ukuba glucuronide okanye sulfate.

Malunga nama-70% of GCS conjugated kwazona kwi umchamo, omnye-20% endleni ziya kubonisa kamva, yaye abanye - kunye nezinye iincindi bemvelo (umz, kamva). Isiqingatha - ukusuka iiyure ezi-2 ukuya ku-4.

Unako ukudala itafile encinane pharmacokinetic parameters of corticosteroids ngomlomo.

Glucocorticosteroids. Iziyobisi (amagama)	Isiqingatha-ubomi kwithishyu	Plasma isiqingatha ubomi
hydrocortisone	iiyure 8-12	iiyure 0.5-1.5
cortisone	iiyure 8-12	iiyure 0.7-2
Prednisolone (review hayi elungileyo kakhulu)	iiyure 18-36	iiyure 2-4
methylprednisolone	iiyure 18-36	iiyure 2-4
fludrocortisone	iiyure 18-36	iiyure 3.5
dexamethasone	iiyure 36-54	5:00

steroids imuncwe practice clinical mihla thaca triamcinolone acetonide, fluticasone propionate, mometasone furoate, budesonide kunye beclomethasone dipropionate.

Pharmacokinetic iparameters kananjalo thaca etafileni:

Glucocorticosteroids. Iziyobisi (amagama)	Le ndawo Umsebenzi anti-ukudumba	umthamo zokusasaza	Plasma isiqingatha ubomi	Nocikizeko nokuwela esibindini
beclomethasone dipropionate	units 0,64.	-	iiyure 0.5	70%
budesonide	1 unit.	4.3 l / kg	iyure 1,7-3,4	90%
triamcinolone acetonide	units 0.27.	1.2 l / kg	iiyure 1.4-2	80-90%
fluticasone propionate	1 unit.	3.7 l / kg	iiyure 3.1	99%
flunisolide	units 0,34.	1.8 l / kg	iiyure 1.6	-

steroids ngeempumlo amayeza namhlanje thaca fluticasone propionate, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide kunye beclomethasone dipropionate. Ezinye zazo ibizwa ngendlela efanayo njengoko corticosteroids ukurhogele.

Emva kokuba isicelo le corticosteroids intranasal idosi wendele ethunjini yaye esinye isahlulo ivela isifo ngokuma ngqo kwi egazini.

Glucocorticosteroids, ivaleleke wokugaya, bathi bafakwe malunga 1-8 ekhulwini, kwaye lokuphumelela lokuqala esibindini biotransformed phantse ngokupheleleyo metabolites engasebenziyo.

Glucocorticosteroids eziye bangena igazi, hydrolyze nezinto engasebenziyo. Nantsi ke itafile pharmacokinetic iparameters zabo:

Glucocorticosteroids. amalungiselelo	Bioavailability xa ungena igazi, njengepesenti	Bioavailability xa etsalwe phecana zesisu, xa ekhulwini
budesonide	34	11
beclomethasone dipropionate	44	20-25
mometasone furoate	<0.1	<1
triamcinolone acetonide	akukho Information	10,6-23
fluticasone propionate	0.5-2
flunisolide	40-50	21

Iziyobisi ezifana "Afloderm" (feedback egcina ziyavela on kumnatha), ukuchaza ngokwahlukileyo ayenzi mqondo. Ngamnye kubo yeyona nto engundoqo esebenzayo, apho kusenokwenzeka ukuba sele ikhankanyiwe apha ngasentla. La machiza - corticosteroids zasekuhlaleni, yaye zimelwe ngokufuthi uhlobo Amafutha okanye amafutha.

Beka therapy glucocorticosteroid (ezibonisa zokusetyenziswa)

Ngohlobo ngalunye glucocorticosteroids imbonakaliso yayo ukuze zisetyenziswe. Ngenxa yoko, corticosteroids ngomlomo asetyenziselwa ukunyanga:

• isifo Crohn kaThixo;
• wenze;
• iingxaki zemiphunga Embi;
• etsolo syndrome ukukhathazeka yokuphefumla;
• inyumoniya kakhulu;
• okuqhubekayo obstructive isifo yemiphunga kwisigaba oyingozi;
• isifuba inyumoniya;
• thyroiditis subacute;
• hyperplasia azalwa adrenal (kulo mzekelo, umntu ongavelisi corticoids ngokwakhe kwaye kunyanzeleke ukuba athathe analogue zazo zokwenziwa);
• insufficiency elibukhali adrenal.

Kwakhona steroids zisetyenziswa kunyango replacement ukusilela napochechnikovoy eziziprayimari nezizisekondari.

corticosteroids Intranasal zisetyenziselwa:

• nokuthimliswa idiopathic (vasomotor);
• nokuthimliswa non-bagulayo kunye eosinophilia;
• impumlo pilipoze;
• nokuthimliswa angehli komzimba (elimandundu);
• nokuthimliswa ngamaxesha komzimba (ngakanye).

corticosteroids imuncwe zisetyenziselwa ukunyanga ezingapheliyo sisifo obstructive pulmonary, isifuba inyumoniya.

Izimo

Amanyathelo kufuneka aphathe GCS kwezi meko clinical:

• zisanyisa;
• glaucoma;
• Ezinye izigulo inwebu, ezo zidibene abanala makhwiniba le epithelium;
• amagciwane okanye izifo egazini iliso;
• isifo ubovu;
• period nokugonywa;
• negcushuwa;
• uhlobo esebenzayo sephepha;
• isifo herpes;
• izifo ezinzwaneni systemic;
• ethile isifo sengqondo iimpawu elinemveliso;
• degree kakhulu of ukusilela kwezintso;
• wegazi;
• thromboembolism;
• isilonda duodenal okanye isisu;
• diabetes;
• isifo Cushing kaThixo.

corticosteroids intranasal ngokucophelela contraindicated kwiimeko ezinjalo:

• nokopha rhoqo embalini;
• sophele diathesis;
• hypersensitivity.

Glucocorticosteroids: imiphumela emibi

engemihle corticosteroids lungohlulwa lube zasekuhlaleni zenkqubo.

ziphumo bezingalindelekanga Local

Yahlulwe imiphumela corticosteroids ukurhogele kunye intranasal.

1. iziphumo ezibi Local evela glucocorticosteroids imuncwe:

• ukukhohlela;
• dysphonia;
• candidiasis le kwisisu ngomlomo pharynx.

2. iziphumo ebezingalindelekanga weNgingqi of corticosteroids intranasal:

• perforation le zekhala ngeempumlo;
• nokopha;
• evuthayo kunye imifinya owomileyo kwiinwebu zempumlo kunye pharynx;
• uthimla;
• impumlo silume.

ziphumo bezingalindelekanga oluCwangcisiweyo

Zahlulwe amalungu omzimba, asebenza.

1. Inxalenye yenkqubo luvo:

• kwengqondo;
• ukudana;
• ibenza;
• ugwayi;
• ucaphuka.

2. Ukususela yegazi:

• thromboembolism;
• thrombosis ndlela obukhulu;
• uxinzelelo lwegazi oluphezulu;
• myocardiodystrophy.

3. Ukususela uhlelo zokuzala:

• hirsutism;
• kulibaziseke uphuhliso ngokwesondo;
• kwekhono ngokwesondo;
• Umjikelo ezingazinzanga sexesheni.

4. Ukususela ometyiso:

• okunamafutha isibindi;
• pancreatitis;
• ukopha evela iphecana zesisu;
• nezilonda steroid esiswini kunye amathumbu.

5. Ukususela inkqubo yonyango:

• diabetes;
• syndrome Cushing kaThixo;
• ukutyeba;
• yoma le neuron adrenal ngenxa inhibition umsebenzi wayo.

6. Ukususela ecaleni ngayo:

• glaucoma;
• ngomva cataract subcapsular.

7. Ukusuka kwinkqubo musculoskeletal:

• ukuchitha imisipha;
• myopathy;
• azikhuli ukukhula kwabantwana;
• necrosis kunye kwamathambo avascular;
• kwamathambo.

8 Kuba isikhumba:

• alopecia;
• striae;
• olindelwe kwesikhumba.

9. Eminye imiphumela emibi:

• etsolo iintlobo esosulelayo kunye esingapheliyo lweenkqubo arhabaxa;
• ayanda;
• sodium namanzi yokugcina emzimbeni.

amanyathelo okhuseleko

Kwezinye iimeko, corticosteroids kufuneka isetyenziswe ngobulumko.

Umzekelo, izigulane kwesibindi, hypothyroidism, hypoalbuminemia, kunye nezigulane saka okanye abakhulileyo luyaphuculwa isenzo corticosteroids.

Xa isicelo corticosteroids ngexesha lokukhulelwa kufuneka athathe ingqalelo isiphumo okulindelekileyo unyango unina kunye umngcipheko nefuthe elibi ichiza ekukhuleni kosana olungekazalwa, njengoko corticosteroids uphazamise uphuhliso ukukhula ezingekazalwa kunye iziphene ezifana inkalakahla zicandeke njalo njalo.

Ukuba ngexesha ukusebenzisa GCS isigulane ubunzima usulelo (chicken pox, yimasisi, njalo njalo. D.), Inokwenzeka nzulu kakhulu.

Xa unyango izigulane corticosteroids okanye izifo samathambo ukudumba (isifo samathambo, izifo kwesisu, systemic lupus zomzimba kunye ezifana. D.) ulubona ukumelana steroid singabonakala.

Izigulane abafumana steroid yomlomo ixesha elide, oko kuyimfuneko ngamathuba athile ukuba igazi ilindle ubugqi, badlule fibroezofagogastroduodenoskopiyu njengoko isilonda steroid ngexesha unyango kunye corticosteroids ukuze musani kuba navuso na.

Ngo malunga ne30-50% ezigulane baphathwa kunye corticosteroids ixesha elide, ukuphuhlisa kwamathambo. Ngokuqhelekileyo, oko kuchaphazela unyawo, isandla, isinqe, iimbambo, umqolo.

Intsebenziswano kunye namanye amachiza

Zonke glucocorticosteroids (Ukuhlelwa Akukhathaliseki apha) xa wadibana nezinye iziyobisi unike isiphumo ethile, yaye oku akusoloko eyakhayo umzimba wethu. Nantsi into ekufuneka uyazi phambi kokuba isicelo corticosteroids ngokubambisana namanye amachiza:

1. GCS kunye asidi - glucocorticosteroids ukufunxeka kunciphisa.
2. GCS kunye barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - glucocorticosteroids biotransformation esibindini inyuswe.
3. GCS kunye isoniazid, erythromycin - glucocorticosteroids biotransformation esibindini kunciphisa.
4. NezabaNxibelelanisi beeNdawo zokuFundela kunye salicylates, phenylbutazone, barbiturates, digitoxin, penicillin, chloramphenicol - zonke ezi iziyobisi kunyuswa emzimbeni.
5. GCS kunye isoniazid - yaphula psyche yabantu.
6. Corticosteroids kunye reserpine - ukuvela karhulumente edakumbisayo.
7. GCS kunye tricyclic lakhula - noxinzelelo intraocular.
8. GCS kunye agonists - isenzo kwala machiza liyenyuka.
9. Corticosteroids kunye theophylline - inyathelo anti-yokukrala glucocorticoids ukunyuka, ukuphuhlisa iziphumo cardiotoxic.
10. NezabaNxibelelanisi beeNdawo zokuFundela kunye womchamo, amphotericin B, mineralocorticoid - kwandisa umngcipheko hypokalemia.
11. GCS ngqo anticoagulants, fibrinolytics, butadiene, ibuprofen, ethacrynic acid - kungalandelwa kubunzima ukopha.
12. NezabaNxibelelanisi beeNdawo zokuFundela kunye indomethacin, salicylates - olu dibaniso kungabangela izibhaxu sisilonda nesiqephu zesisu.
13. Corticosteroids kunye paracetamol - ubuthi beziyobisi inyuswe.
14. Corticosteroids kunye azathioprine - kwandisa umngcipheko seengxangxasi, myopathy.
15. GCS kunye mercaptopurine - kudityaniswa kukhokelela ekwandeni yoxinaniso of uric acid egazini.
16. GCS kunye hingamin - ziyanyuswa imiphumela engamkelekanga eli chiza (Ibar kwenwebu yamehlo, myopathy, dermatitis).
17. GCS kunye methandrostenolone - abangenza imiphumela ebuhlungu glucocorticoids.
18. Corticosteroids kunye amalungiselelo nesinyithi, androgens - ukwanda Yindibanisela erythropoietin, nangalo imvelaphi, ndakumandisa erythropoiesis.
19. GCS kunye hypoglycemic neziyobisi - ukuncitshiswa phantse ngokupheleleyo ngempumelelo yabo.

isiphelo

Steroid - iziyobisi, ngaphandle apho amayeza mihla akunakwenzeka ukuba malini. Bona asetyenziswa unyango izigaba enzima kakhulu zesi sifo, okanye nje ukwandisa isenzo isiyobisi. Noko ke, njengazo zonke amayeza, glucocorticosteroids iziphumo ebezingalindelekanga kwaye Izimo kakhulu. Musa ukulibala ngayo. Ngaphezu siye zidweliswe zonke iimeko apho akukho mfuneko ukusebenzisa steroids kananjalo usinike uluhlu lwe impefumlelwano corticosteroids kunye nezinye iziyobisi. indlela yokuba isenzo corticosteroids nabo bonke yeziphumo zabo ziye ichazwe ngokwenkcukacha apha. Ngoku kufuneka ukuba uyazi GCS, kukuba endaweni enye - eli nqaku. Noko ke, xa kunjalo, musa ukuqala unyango kuphela emva kokufunda ulwazi ngokubanzi malunga GCS. La machiza, Kakade, zingathengwa ngaphandle kagqirha, kodwa kutheni kufuneka oko? Ngaphambi kokuba usebenzise naziphi na iziyobisi kuqala mabadibane yincutshe. Abe sempilweni entle kwaye hayi self-medicate!