SCS - ke eng meriana? Liphello le liphello tsa glucocorticosteroid litokisetso

Ka sebele u kile ua utloa ka li-hormone tsa steroid. 'Mele oa rona o tsoelapele ho o tsoela pele ho laola mekhoa ea bophelo. Sehloohong sena re tla tšohla li-hormone tsa glucocorticoids, tse etsoang ka adrenal cortex. Le hoja boholo ba rona re thahasella lipapiso tsa bona tse entsoeng ka mahlahahlaha - GCS. Hona ke eng meriana? Li sebelisetsoa eng le li kotsi life tseo li li etsang? A re boneng.

Boitsebiso bo tloaelehileng ka GCS. Hona ke eng meriana?

'Mele oa rona o etsa li-hormone tse joalo tsa steroid joaloka glucocorticoids. Li hlahisoa ke adrenal cortex, 'me tšebeliso ea tsona e amana haholo le phekolo ea ho se sebetse ha adrenal. Mehleng ena, ha ho sebelisoe feela glucocorticoids ea tlhaho, empa le lipapiso tsa bona tsa tlhaho - GCS. Hona ke eng meriana? Bakeng sa moloko oa batho, litšoantšo tsena li na le lintho tse ngata tseo li lokelang ho li etsa, kaha li na le li-anti-inflammatory, immunosuppressive, anti-shock, anti-allergenic 'meleng.

Li-glucocorticoids li ile tsa qala ho sebelisoa e le meriana (ka ho eketsehileng sehloohong-lithethefatsi) lilemong tsa bo-40 tsa lekholo la bo20 la lilemo. Qetellong ea lilemong tsa bo-30 tsa lekholo la bo20 la lilemo, bo-rasaense ba ile ba sibolla metsoako ea hormone ea steroid ka adrenal cortex ea motho, 'me e se e le 1937 mineralocorticoid deoxycorticosterone e ne e arohane. Mathoasong a 40-ies, glucocorticoids hydrocortisone le cortisone le tsona li ne li hlophisitsoe. Liphello tsa khase ea cortisone le hydrocortisone li ne li fapane hoo ho ileng ha etsoa qeto ea ho li sebelisa e le lithethefatsi. Ka mor'a nakoana, bo-rasaense ba ile ba etsa hore ba qale.

Glucocorticoid e sebetsang ka ho fetisisa meleng oa motho ke cortisol (analog - hydrocortisone, theko ea eona ke 100-150 ruble), e nkoa e le eona e ka sehloohong. Hape hoa khoneha ho bona hore ha ho na letho le sebetsang: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

Har'a tsohle tsa tlhaho tsa glucocorticoids, hydrocortisone feela le cortisone e ne e sebelisoa e le lithethefatsi. Leha ho le joalo, e qetella e baka litla-morao hangata ho feta leha e le efe e 'ngoe ea hormone, ka lebaka la hona joale tšebeliso ea eona meriana e lekanyelitsoe. Ho fihlela joale, glucocorticoids e sebelisa hydrocortisone feela kapa esters (hydrocortisone hemisuccinate le hydrocortisone acetate).

Ha e le li-glucocorticosteroids (synthetic glucocorticoids), li-agent tse ngata li entsoe, ho akarelletsa le fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, joalo-joalo) le e seng fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

Chelete e joalo e sebetsa ho feta basebetsi ba bona ba tlhaho, mme litekanyetso tse nyane li hlokahalang bakeng sa phekolo.

Mokhoa oa ketso ea GCS

Phello ea glucocorticosteroids lebaleng la limolek'hule ha e e-s'o hlakisoe ho fihlela qetellong. Bo-rasaense ba lumela hore lithethefatsi tsena li etsa lisele ho lisele tse boemong ba molao oa phetolo ea liphatsa tsa lefutso.

Glucocorticosteroids e kopana le li-receptor tsa glucocorticoid intracellular, tse teng hoo e batlang e le sele e 'ngoe le e' ngoe 'meleng oa motho. Ha ho se na hormone ena, li-receptors (ke liprotheine tsa cytosolic) li se li sa sebetse. Lefatšeng le sa sebetseng, ke karolo ea li-heterocomplex, tse kenyeletsang immunophilin, li-protein tse chesang mocheso, joalo-joalo.

Ha li-glucocorticosteroids li kenella ka seleng (ka hara membrane), li tlama li-receiptor 'me li nolofatse mokokotlo oa glucocorticoid + receptor, ka mor'a moo e kena ka hare ho nucleus ea seleng ebe e sebelisana le DNA tsa marang-rang tse teng karolong e khothalletsang liphatsa tsa lefutso tsa steroid (li boetse li bitsoa glucocorticoid -e leng likarolo tse nyatsang). E rarahaneng "glucocorticoid + receptor" e khona ho laola (thibela kapa, ka lehlakoreng le leng, e sebelise) mokhoa oa ho ngoloa ha liphatsa tsa lefutso. Sena ke sona se lebisang ho fokotsa kapa ho tsosolosa mRNA e thehoang, hammoho le phetoho ea li-enzyme tse fapaneng tsa taolo le liprotheine tse kopanelang liphello tsa lisele tsa cellular.

Liphuputso tse fapa-fapaneng li bontša hore mochine oa glucocorticoid + receptor o kopana le lintlha tse fapaneng tsa ho ngolisa, ka mohlala, tse kang nuclear nyutlelie ea Kappa B (NF-kB) kapa protheine ea phetoho ea activator (AP-1), e laolang liphatsa tsa lefutso tse kenang likarolong tsa 'mele oa ho itšireletsa mafung le Ho ruruha (limolek'hule tsa ho khomarela, liphatsa tsa lefutso tsa cytokine, proteinase, joalo-joalo).

Liphetho tse kholo tsa GCS

Liphello tsa glucocorticosteroids 'meleng oa motho li ngata. Li-hormone tsena li na le li-antitoxic, li-anti-shock, tse se nang tšusumetso ea maikutlo, li khahlanong le khatello ea mali, liketsong tse nyatsang le tse khahlanong le ho ruruha. A re ke re hlahlobisise kamoo GCS e sebetsang kateng.

• Phoso e khahlanong le ho ruruha ha GCS. Ka lebaka la ho felisoa ha mosebetsi oa phospholipase A _2. Ka thibelo ea enzyme ena 'meleng oa motho, ho felisoa ha ho lokolloa ha arachidonic acid le ho thibela ho thehoa ha basebelisi ba itseng ba ho ruruha (joalo ka prostaglandins, leukotrienes, troboxane, joalo-joalo). Ho feta moo, ho kenngoa ha glucocorticosteroids ho lebisa ho fokotseha ha metsi a feteletseng, vasoconstriction (ho fokotseha) ha li-Capillaries, ntlafatso ea microcirculation ho tsepamisa maikutlo ho hoholo.
• Antiallergic phello ea GCS. E hlaha ka lebaka la theola secretion le tswakana tsa mediators tsa allergy, fokotsa e potoloha basophils, thibelo ea histamine lokolloa basophils le lisele tse palo sensitized, fokotsa palo ea B le T lymphocytes, fokotsa nahanela ea lisele ho mediators tsa allergy, boitshireletso ba mmele ka karabelo liphetoho, hammoho le hatelloang ea tlhahiso antibody.
• Ketsahalo ea immunosuppressive ea SCS. Hona ke eng meriana? Sena se bolela hore lithethefatsi li thibela immunogenesis, ho thibela tlhahiso ea li-antibodies. Li-glucocorticosteroids li thibela ho falla ha lisele tsa masapo a masapo, li thibela mosebetsi oa B-le T-lymphocyte, ho thibela ho lokolloa ha li-cytokines ho tloha macrophages le leukocyte.
• Antitoxic le khahlanong le ts'ebetso ea liphello tsa SCS. Phello ena ea li-hormone e bakoa ke ho eketsa khatello ea mali ho batho, hammoho le ho ts'oaetso ha li-enzyme tsa sebete, tse kenyeletsang metabolism ea xeno-endobiotics.
• Ketsahalo ea Mineralocorticoid. Li-glucocorticosteroids li na le bokhoni ba ho thibela sodium le metsi 'meleng oa motho, ho etsa hore ho be le potlako ea potasiamo. Lintho tsena tse entsoeng ke li-hormone tsa tlhaho ha lia tšoane le li-hormone tsa tlhaho, empa li ntse li na le phello e joalo 'meleng.

Pharmacokinetics

Nakong ea khato, systemic glucocorticosteroids e ka aroloa ka:

1. Glucocorticosteroids e nang le ketso e khutšoanyane (mohlala, hydrocortisone, theko ea eona e fapaneng le li-ruble tse 100 ho isa ho tse 150).
2. Glucocorticosteroids e nang le nako e tloaelehileng ea khato (prednisolone (litlhaloso tsa eona tse seng ntle haholo), methylprednisolone).
3. Glucocorticosteroids e nang le khato e telele (triamcinolone acetonide, dexamethasone, betamethasone).

Empa ha se feela nako ea ketso e ka khethollang glucocorticosteroids. Ts'ebetso ea bona e ka boela ea ba ho latela mokhoa oa tsamaiso:

• Lipuo;
• Intranasal;
• Inhaled glucocorticosteroids.

Leha ho le joalo, sehlopha sena se sebetsa feela ho systemic glucocorticosteroids.

Hape ho na le litokisetso tse itseng ka mafura le litlolo (li-SCS). Ka mohlala, "Afloderm". Tlhahlobo ka lithethefatsi tse joalo li ntle.

A re shebeng mefuta ea mefuta ea GCS e arohaneng.

Mantsoe a molomo oa glucocorticosteroids a kenngoa ka mokhoa o phethahetseng ka pampiri ea lijo empa a sa bake mathata. Kopanya ka matla liprotheine ka lero la mali (transcortin, albumin). Matšoao a mangata a molomo oa glucocorticosteroids maling a fihlella ka mor'a lihora tse 1,5 kamora 'muso. Ba e-na le li-biotransformation sebeteng, liphio (karoloana) le litsong tse ling ka ho kopanya li-sulfate kapa glucuronide.

Hoo e ka bang karolo ea 70% ea GCS e kopanetsoeng e ntšitsoe ka metsing, e leng karolo e 20 lekholong e tla ntšoa hamorao ka li-feces, le tse setseng - tse ling tse nang le li-biological (mohlala, ka mor'a moo). Half-life e tsoa lihora tse 2 ho isa ho tse 4.

Hoa khoneha ho bokella tafoleng e nyenyane le mekhahlelo ea pharmacokinetic ea GCS ea molomo.

Glucocorticosteroids. Litokisetso (mabitso)	Half-life of tissue	Bophelo ba halofo ea mali ea mali
Hydrocortisone	Lihora tse 8-12	Lihora tse 0,5-1,5
Cortisone	Lihora tse 8-12	Lihora tse 0,7-2
Prednisolone (litlhaloso ha li hantle hantle)	Lihora tse 18-36	Lihora tse 2-4
Methylprednisolone	Lihora tse 18-36	Lihora tse 2-4
Fludrocortisone	Lihora tse 18-36	Lihora tse 3,5
Dexamethasone	Lihora tse 36-54	Lihora tse 5

Inhaled glucocorticosteroids metseng ea meriana ea hona joale e emeloa ke triamcinolone acetonide, fluticasone propionate, mometasone furoate, budesonide le beclomethasone dipropionate.

Methati ea bona ea pharmacokinetic e ka boela ea emeloa ka mokhoa oa tafole:

Glucocorticosteroids. Litokisetso (mabitso)	Mosebetsi o khahlanong le ho ruruha	Moqolo oa ho aba	Bophelo ba halofo ea mali ea mali	Tsela e nepahetseng ea ho feta sebeteng
Beclomethasone dipropionate	Diyuniti tse 0,64.	-	0.5 hora	70%
Budesonide	Sehlopha se le seng	4,3 l / kg	1.7-3.4 lihora	90%
Triamcinolone acetonide	Diyuniti tse 0,27.	1.2 l / kg	Lihora tse 3-4-2	80-90%
Fluticasone propionate	Sehlopha se le seng	3.7 l / kg	3.1 lihora tse	99%
Flunisolide	0.34 diyuniti.	1.8 l / kg	Lihora tse 1.6	-

Li-intranasal glucocorticosteroids ea meriana ea kajeno e emeloa ke fluticasone propionate, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide le beclomethasone dipropionate. Tse ling tsa tsona li bitsoa ho tšoana le ho hasoa ha glucocorticosteroids.

Ka mor'a hore u sebelise GCS ea intranasal, karolo e itseng ea tekanyo e kenngoa ka maleng, 'me karolo ea eona e tsoa ka lehare la pampiri ea phefumoloho ka ho toba maling.

Li-glucocorticosteroids, tse kenngoeng ka pampiri ea lijo, li kenngoa ka karolo ea 1-8 lekholong, 'me ha li qala ho feta sebeteng, li batla li fetohile ka ho feletseng ho metabolite e sa sebetseng.

Li-glucocorticosteroids tse kenang maling li haelloa ke hydrolyzed e le lintho tse sa sebetseng. Tafole ena e na le mekhahlelo ea bona ea pharmacokinetic:

Glucocorticosteroids. Litokisetso	Ho ba motlakase ha o kenella mali, ka karolo ea lekholo	Ho fokotsa likokoana-hloko ha u kenngoa ho pampiri ea mathe, ka liphesente
Budesonide	34	11th
Beclomethasone dipropionate	44	20-25
Mometasone furoate	<0.1	<1
Triamcinolone acetonide	Ha ho tlhahisoleseding	10.6-23
Fluticasone propionate	0.5-2
Flunisolide	40-50	21

Lithethefatsi tse kang "Afloderm" (litlhaloso mabapi le hore na li ntse li hlahella hokae ka letlooa), ha ho na ntlha ea ho hlalosa ka ho khetholla. Nthong e 'ngoe le e' ngoe ho tsona ho na le ntho e sebetsang e matla, e leng, mohlomong e seng e boletsoe ka holimo. Lithethefatsi tsena ke li-glucocorticosteroids tsa moo, 'me li atisa ho hlahisoa ka mokhoa oa mafura kapa litlolo.

Sebaka sa GCS sa phekolo (litlhahiso tsa tšebeliso)

Bakeng sa mofuta o mong le o mong oa glucocorticosteroids, lipontšo tsa ho sebelisoa. Kahoo, molomo oa glucocorticosteroids o sebelisoa ho tšoara:

• Lefu la Crohn;
• Nonspecific ulcerative colitis;
• Matšoafo a matšoafo;
• Phekolo e bohloko ea matšoafo;
• Pneumonia e matla;
• Boloetse bo sa foleng ba ho thibela lefu la mokoallo boemong ba ho fokotsa matla;
• Phoso ea bronchial;
• Subacute thyroiditis;
• Ho se sebetse ha pelo ea adrenal cortex (tabeng ena motho ha a hlahise corticoids ka boeena 'me o qobelloa ho nka lipapiso tsa bona tsa maiketsetso);
• Ho se fumanehe hantle ha adrenal.

Hape, li-glucocorticosteroids li sebelisetsoa phekolo ea phetolo ea phetoho e ka sehloohong le ea bobeli ea likhahla.

Li-grancocorticosteroids tsa intranasal li sebelisetsoa:

• Idiopathic rhinitis (sepakapaka);
• E seng ea phekolo ea mali e nang le li-eosinophilia;
• Filipi ea nko;
• Selemo se seng le se seng sa allergenic rhinitis (e tsitsitseng);
• Nako ea ho hlasela ha rhinitis (lipakeng).

Inhaled glucocorticosteroids e sebelisoa ho phekola lefu le sa foleng la pulmonary, lefu la bronchial asthma.

Litlhōlisano

Mehato lokela ho tšoara GCS ka maemo ana litleleniki tsa:

• diabolololo;
• glaucoma;
• Ba bang ba mafu a ea cornea, e leng ba ho kopantswe le sa tloaelehang la epithelium ea;
• fungal kapa mafu a bongata ba kokwanahloko ea leihlo;
• purulent tshwaetso;
• nako ente;
• mokaola;
• a sebetsang a foromo ke lefuba;
• herpes tshwaetso;
• systemic fungal mafu a tsoaetsanang;
• ba bang ba lefu la kelello le matšoao a behang;
• lengolo la e mpe ea ho hloleha renal;
• kgatelelo ya madi;
• thromboembolism;
• duodenal seso kapa mpeng;
• lefu la tsoekere;
• lefu Cushing e.

Tieo contraindicated intranasal corticosteroids maemong a joalo:

• mokola khafetsa histori;
• hemorrhagic diathesis;
• hypersensitivity.

Glucocorticosteroids: litla-morao

litla-morao tsa corticosteroids ka aroloa moo le systemic.

litla-morao Local

Arotsoe ka liphello tsa corticosteroids hema le intranasal.

1. Local litla bohloko ho tswa glucocorticosteroids hema:

• khohlela;
• dysphonia;
• candidiasis ea cavity molomo le pharynx.

2. litla Local mahlakoreng corticosteroids intranasal:

• perforation tsa nasal septum;
• mokola;
• tukang le omileng lera la mucous ea nko le pharynx;
• e thimola;
• itchy nko.

litla systemic lehlakoreng

Aroloa ho latela likarolo tse ling tsa 'mele, eo sebetsa.

1. Karolo ea tsamaiso ea methapo e bohareng:

• psychoses;
• ho tepella maikutlong;
• nyakallo;
• lefu la ho hlobaela;
• teneha.

2. Ho tloha tsamaiso ea pelo le methapo:

• thromboembolism;
• tebileng mothapo thrombosis;
• phahameng khatello ea mali;
• myocardiodystrophy.

3. Ho tloha tsamaiso ea ho hlahisa bana:

• hirsutism;
• lieha ntshetsopele ya bokgoni ba ho kopanela liphate;
• ho se sebetse thobalano;
• tsitsang matsatsing potoloho.

4. From tsamaiso tshilong ya dijo:

• tse mafura sebete;
• pancreatitis;
• tsoa mali ho tswa ho pampitšana gastrointestinal;
• liso tsa ka maleng steroid ea mala le mala.

5. Ho tloha ka tsamaiso ea endocrine:

• lefu la tsoekere;
• lefu Cushing ya;
• botenya;
• felloa ke matla ea cortex adrenal ka lebaka la ho thibelo ea mosebetsi oa eona.

6. From lehlakoreng la pono:

• glaucoma;
• kamorao lera subcapsular.

7. Ho tloha ka tsamaiso ea musculoskeletal:

• mesifa senyehang;
• myopathy;
• tswela pele ka botlalo kgolo ya ka bana;
• avascular necrosis le masapo fractures;
• osteoporosis.

8. Ka letlalo:

• alopecia;
• striae;
• thinning ea letlalo.

9. Other litla-morao:

• a hlobaetsang a tšoaetsanoang le sa foleng mefuta e meng ea dithulaganyo hlabang;
• ho ruruha;
• sodium le metsi tshegetsa le go tlotla ka 'mele.

mehato precautionary

Maemong a mang, corticosteroids lokela ho sebelisoa ka hloko.

Mohlala, bakuli ba ho thatafala ha sebete, hypothyroidism, hypoalbuminemia, 'me bakuli ba senile kapa batho ba hōlileng ka ho ntlafatsoa bohato ba corticosteroids.

Ha a sebelisa corticosteroids nakong ea bokhachane lokela ho nahana ka phello ho lebelletsoe tsa kalafo bakeng sa 'mè oa le menyetla ea ho ba le phello e mpe ea lithethefatsi ka lesea, joalokaha corticosteroids ka senya tsoelo-pele ea kgolo ya fetal le esita le likoli tse kang mahalapa lefarung joalo joalo.

Haeba nakong tshebediso ya GCS mamello le bothata ba tshwaetso (khoho pox, maselese, 'me joalo-joalo. D.), E ka' na etsahala ka ho teba haholo.

Ka ho phekola bakuli ba corticosteroids kapa autoimmune mafu a hlabang (ramatiki, mafu a mantle a, systemic lupus erythematosus le tse ling. D.) Sightings steroid ho hanyetsa ka ho ketekoa.

Bakuli ba fumana steroid molomo bakeng sa nako e telele, ho hlokahala nako le nako ho nka fecal boloi mali le feta fibroezofagogastroduodenoskopiyu ka steroid seso nakong kalafo le corticosteroids ka 'na ha ba tšoenyehe.

Ka 30-50% ea bakuli tšoaroa ka corticosteroids bakeng sa nako e telele, ho ntshetsa pele osteoporosis. E le busa, e ama maoto, letsoho, noka, likhopo, lesapo la mokokotlo.

Sebelisana le lithethefatsi tse ling

glucocorticosteroids tsohle (tlhophiso ha ho tsotellehe mona) ha a kopana le lithethefatsi tse ling tse fa le phello e itseng, 'me e le hantle sena ha se kamehla positive, bakeng sa' mele ea rōna. Mona 's seo u se lokela ho tseba pele ho sebelisa corticosteroids ka kopanelo le lithethefatsi tse ling:

1. GCS le antacids - glucocorticosteroids absorption decreases.
2. GCS le barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - glucocorticosteroids biotransformation ka sebete e ile ea eketseha.
3. GCS le isoniazid, erythromycin - glucocorticosteroids biotransformation ka sebete decreases.
4. SCS le salicylates, phenylbutazone, barbiturates, digitoxin, penicillin, chloramphenicol - kaofela ha lithethefatsi tsena li ka e ntlafatsoa felisoa.
5. GCS le isoniazid - ho tlōla le e tlameletswe dikelellong tsa batho.
6. Corticosteroids le reserpine - ho hlaha ha boemo tepelletsang.
7. GCS le tricyclic antidepressants - eketseha khatello ea intraocular.
8. GCS le agonists - ketso ya lithethefatsi tsena li ka e ntse e eketseha.
9. Corticosteroids le theophylline --ba khahlanong le a hlabang bohato ba glucocorticoids eketseha, hlahisa liphello cardiotoxic.
10. SCS le diuretics, amphotericin B, mineralocorticoid - ho eketsa kotsi ea hypokalemia.
11. GCS le sa tobang anticoagulants, fibrinolytics, butadiene, ibuprofen, acid e ethacrynic - ka lateloa ke mathata hemorrhagic.
12. SCS le indomethacin, salicylates - motswako ena ho ka etsa hore diso ulcerative pampitšaneng ena gastrointestinal.
13. Corticosteroids le paracetamol - the toxicity ea lithethefatsi e eketseha.
14. Corticosteroids le azathioprine - ho eketsa kotsi ea lera, myopathy.
15. GCS le mercaptopurine - motswako ka lebisa ho eketseha mahloriso ea acid e uric maling.
16. GCS le hingamin - Amplified litla sa batleheng ya lithethefatsi ena (corneal opacity, myopathy, dermatitis).
17. GCS le methandrostenolone - amplify litla bohloko tsa glucocorticoids.
18. Corticosteroids le litokisetso tšepe, androgens - eketseha tswakana ea erythropoietin, le khahlanong le semelo sa ena, 'me e ile ea eketseha erythropoiesis.
19. GCS le hypoglycemic lithethefatsi - hoo e ka bang ka ho feletseng phokotso ea katleho ea bona.

bofello

Steroid - lithethefatsi, ntle le e leng moriana morao-rao ke a hlola a chelete. Di sebediswa bakeng sa kalafo ya mekhahlelo e matla haholo ea lefu lena le, kapa e le feela ho ntlafatsa ketso ya lithethefatsi ka. Leha ho le joalo, joalokaha eka ke ka meriana, glucocorticosteroids liphello tsohle lehlakoreng le na le contraindications haholo. Se ke la lebala ka eona. Ka holimo re ho tse thathamisitsoeng ka maemong 'ohle moo ho ke ke ha hlokahala hore ho sebelisa steroid' me ba boetse a fana ka lethathamo la sebelisana tsa corticosteroids le lithethefatsi tse ling. ea mochine oa ketso ea corticosteroids 'me kaofela ha litla bona le tsona li hlalosa ka ho qaqileng mona. Joale sohle seo u lokelang ho se tseba mabapi le GCS, e sebakeng se seng ka - sehlooho sena. Leha ho le joalo, haeba leha e le efe, u se ke ua qala kalafo feela ka mor'a ho bala boitsebiso bo akaretsang mabapi GCS. lithethefatsi tsena li ka, ka ho hlakileng, ka rekoa ntle lengolo la ngaka, empa ke hobane'ng ha u hloka? Pele ho sebelisa lithethefatsi leha e le ofe pele sheba 'setsebi. Phela hantle 'me a sa ho intša medicate!