GCS - e tenei rongoā? Ko te mahi me te pānga o taero glucocorticosteroids

He pono ake kua rongo koutou o hormones pūtaiaki. To tatou tinana hua tonu ratou ki te whakahaere i ngā tukanga ora. I roto i tenei tuhinga, ka whakaaro matou glucocorticoids - hormones pūtaiaki, e kua whakaputaina i roto i te uho adrenal. Ahakoa he te nuinga o tatou hiahia i roto i o ratou analogues waihanga - GCS. He aha te mea rongoā? Hoki e whakamahia ratou me te aha te huru o te kino meinga ratou? Kia kite a.

mōhiohio General e pā ana ki GCS. He aha te mea rongoā?

To tatou rauropi synthesises hormones pūtaiaki pērā i glucocorticoids. E whakaputaina ratou i te uho adrenal, a kei te nuinga e pā ana ratou whakamahi ki te maimoatanga o te iti hoki adrenal. I tčnei wā, te whakamahi i kore anake glucocorticoids tūturu, engari ano hoki ratou analogues waihanga - GCS. He aha te mea rongoā? Hoki te tangata, te tikanga o enei analogs he rota, rite i runga i te tinana anti-inflammatory, immunosuppressive, antishock, pānga anti-mate pāwera.

Kua riro Glucocorticoids whakamahia rite taero (e whakahuatia ki roto i te tuhinga - PM) i roto i te 40-doma o XX rautau. Na roto i te mutunga o nga 30raa o te rau tau rua tekau, kua kitea kaipūtaiao pūhui taiki pūtaiaki i roto i te uho adrenal tangata, a i roto i te tau 1937 i tīpakohia e ia deoxycorticosterone mineralocorticoid. I roto i te wawe 40-doma i ahu mai glucocorticoid hydrocortisone me cortisone. i pera kanorau pānga pharmacological o cortisone, me te hydrocortisone, e i whakaritea e te reira ki te whakamahi ia ratou kia rite ki taero. I muri i te tahi mau wa, kua kawea kaiputaiao i to ratou kōtuitanga.

Ko te glucocorticoid tino kaha i roto i te rauropi tangata ko - cortisol (orotahi - hydrocortisone, tona utu - 100-150 moni), a kua whakaaro reira he nui. Ko reira taea hoki ki te tohatoha iti kaha: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

O nga glucocorticoids taiao katoa rite whakamahi tarukino kitea hydrocortisone me cortisone anake. Heoi, i te pānga taha take whakamutunga atu pinepine atu i tetahi atu taiki, i te mea he aha i te wa nei tona whakamahi i roto i te rongoā he iti. Ki te rā, whakamahia anake glucocorticoid hydrocortisone ona hākawa (hydrocortisone hemisuccinate me hydrocortisone tāpia) ranei.

E pā ana glucocorticosteroids (glucocorticoids waihanga), lolotonga synthesized matou he maha o taua āpiha, i roto i nei te fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, etc) ka kore-fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

Taua āpiha kaha atu i to ratou ritenga māori, me e hiahiatia ana mo te maimoatanga o pota iti.

Ko te tikanga o te mahi o corticosteroids

e kore e matau tino te mahi o glucocorticoids i te taumata rāpoi. whakapono Scientists e ngāue enei taero i runga i ngā pūtau i te taumata o te ture o te tuhi ira.

Corticosteroids taunekeneke ki he hakari i roto i tata pūtau katoa o te tinana tangata receptors glucocorticoid intracellular. I roto i te ngaro o receptors taiaki (e he pūmua cytosolic) e taupāhohea noa. I roto i te āhua paruparu, he wahi o nga heterocomplexes, e ngā ano immunophilin, pūmua ru wera, me te pera atu ratou.

A, no te tomo steroids te pūtau (i roto i te membrane), herea ratou ki receptors me whakahohe matatini "glucocorticoid + receptor", i muri nei tomo te reira i te karihi pūtau me te taunekeneke ki te rohe DNA e kei roto i te ira kaiwhakatairanga kongakonga pūtaiaki hāngai (e huaina ana hoki e ratou glucocorticoid 'ka mea huānga). taea ki te whakahaere i (te tautāwhi ranei, hei kōrero, whakahohe) te tukanga o te te tuhi o etahi ira Complex "+ receptor glucocorticoid" ko. Ko tenei te mea arata'i ki pehanga whakaongaonga o mRNA ranei, me te he huringa i roto i te kōtuitui o ngā whākōkī me pūmua whakaritenga e takawaenga pānga pūtau.

whakaatu Various rangahau e tali te matatini "glucocorticoid + receptor" te ki ngā āhuatanga tuhi, hei tauira, pērā i take karihi Kappa B (NF-kB), ranei te activator o patohanga pūmua (AP-1) e whakahaere ira whai wāhi i roto i te whakautu ārai, me mumura (rāpoi adhesion, ira cytokine, protease me pera i runga i.).

Ko te pānga matua o GCS

He maha ngā pānga glucocorticoids i runga i te tinana tangata. Ēnei hormones i antitoxic, antishock, imunnodepressivnoe, antiallergic, mahi antiinflammatory me antiinflammatory. Kia tango o te titiro i te āhua o te mahi o corticosteroids.

• pānga Anti-inflammatory o corticosteroids. Meinga te pehanga o te mahi o te phospholipase te liberatiou _2. A, no te tāmia inhibition o tenei whākōkī i roto i te tinana tangata te (tuku) te inhibition o te waikawa arachidonic me te hanganga o te tahi mau kaitakawaenga inflammatory (pērā i prostaglandins, leukotrienes, me troboksan t. D.). Ano, te glucocorticosteroids fariiraa whakaiti inu exudation, vasoconstriction (whāiti) tōiti, whakapai ake o microcirculation i te mumura.
• pānga Anti-mate pāwera o GCS. puta te reira i rite ki te hua o te tukupu secretion me kōtuitui o kaiwhakaako o mate pāwera, whakaiti komuhumuhu basophils, inhibition o tuku histamine i basophils me ngā pūtau rewa sensitized, whakaiti i te maha o te B, me te lymphocytes T, te whakaiti te tūtohutanga o ngā pūtau ki nga kaiwhakaako o te mate pāwera, huringa whakautu ārai, me te pehanga o te antibody production.
• mahi Immunosuppressive o GCS. He aha te mea rongoā? Tenei te tikanga e te raau taero tautāwhi i immunogenez, pehi te hanga o paturopi. Corticosteroids tautāwhi i hekenga o wheua wheua pūtau kakau, tautāwhi i te mahi o te B, me te T lymphocytes tautāwhi i te tuku o cytokines i macrophages me leukocytes.
• Anti-paitini, me te pānga antishock o corticosteroids. Ko te pānga o hormones meinga e te pēhanga toto tiketike i roto i te tangata, kia rite ki te pai kia rite ki te faaitoitoraa o whākōkī ate whai wāhi i roto i te pākia o hautūāpōkere me endobiotikov.
• mahi Mineralocorticoid. Glucocorticosteroids i te kaha ki te faataere konutai me te wai i roto i te tinana, whakaongaonga te excretion o pāhare pāporo. e kore e rite pai rite hormones tūturu tenei whakakapi waihanga, engari ko te reira i te pānga i runga i te tinana i ratou.

Pharmacokinetics

Hoki te roanga o te mahi o steroids pūnahanaha taea te wehea ki:

1. Glucocorticosteroids mahi poto (hei tauira, hydrocortisone, te utu o e rerekē i 100 ki te 150 moni).
2. Glucocorticosteroids ki te roanga toharite o te mahi (prednisolone (urupare e kore he tino pai i), methylprednisolone).
3. Glucocorticosteroids ki te mahi auroa (triamcinolone acetonide, dexamethasone, betamethasone).

Ko e kore anake hoki e takoto ai te roanga o glucocorticosteroids. kia hoki kia Whakarōpū o ratou te aratau o whakahaere:

• waha;
• intranasal;
• glucocorticosteroids hau.

Tenei whakarōpūtanga, Heoi, pā anake ki glucocorticosteroids pūnaha.

He te tahi mau raau taero i roto i te puka o hinu me aihikirīmi (corticosteroids rohe). Hei tauira, "Afloderm". He pai Reviews o taua formulations.

Kia titiro a i ngā momo o corticosteroids pūnahanaha anake.

steroids Oral tino whenumi i roto i te whēkau, kahore ai raruraru. Tino herea ki pūmua i roto i te wē (transcortin, albumin). tae te kukū mōrahi o corticosteroids waha i roto i te toto e i muri i 1.5 haora i muri i whakahaere. mamae ratou biotransformation i te ate, tākihi (wāhanga) me ētahi atu te kopa i conjugation ki glucuronide pūkawa ranei.

Tata 70% o te GCS conjugated excreted i te mimi, tetahi 20% i roto i te feces ka tohu i muri, me te toenga - ki ētahi atu fluids koiora (hei tauira, i muri mai). Ko te hawhe - i te 2 ki te 4 haora.

Ka taea e koe te hanga i tētahi ripanga iti ki te tawhā pharmacokinetic o corticosteroids-waha.

Glucocorticosteroids. Drugs (ingoa)	Ko te hawhe-ora o te kikokiko	Wē hawhe-ora
hydrocortisone	8-12 haora	0.5-1.5 haora
cortisone	8-12 haora	0.7-2 haora
Prednisolone (kore e tino pai arotake)	18-36 haora	2-4 haora
methylprednisolone	18-36 haora	2-4 haora
fludrocortisone	18-36 haora	3.5 haora
dexamethasone	36-54 haora	5:00

steroids hau i roto i te mahi haumanu hou aroaro triamcinolone acetonide, fluticasone propionate, mometasone furoate, budesonide me beclomethasone dipropionate.

taea hoki te aroaro tawhā Pharmacokinetic i roto i te ripanga:

Glucocorticosteroids. Drugs (ingoa)	Ko te mahi anti-inflammatory rohe	rōrahi o te tohatoha	Wē hawhe-ora	Te kaha o te irava i roto i te ate
dipropionate beclomethasone	0,64 wae.	-	0.5 haora	70%
budesonide	1 kōwae.	4.3 l / kg	1,7-3,4 haora	90%
acetonide triamcinolone	0.27 wae.	1.2 l / kg	1.4-2 haora	80-90%
propionate fluticasone	1 kōwae.	3.7 l / kg	3.1 haora	99%
flunisolide	0.34 wae.	1.8 l / kg	1.6 haora	-

steroids nasal i roto i te rongoā aroaro i tenei ra fluticasone propionate, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide me beclomethasone dipropionate. E huaina etahi o ratou i te ara ano rite corticosteroids hau.

I muri i tono o nga corticosteroids intranasal horopeta whenumi i roto i te whēkau, me tetahi atu wahi mai i te mucosa airway tika ki te bloodstream.

Glucocorticosteroids, mau i roto i te wahi kūnatu, e riro hoki e pā ana ki 1-8 ōrau, me te haere tuatahi i roto i te ate biotransformed tata rawa ki metabolites tautauā.

Glucocorticosteroids e kua eke ki te toto, hydrolyze ki matū tautauā. Tenei ko te tepu ki o ratou tawhā pharmacokinetic:

Glucocorticosteroids. mau faaineineraa	Bioavailability ka tomo i te toto, ka rite ki te ōrau	Bioavailability ka whenumi i te wahi gastrointestinal, i roto i te ōrau
budesonide	34	11
dipropionate beclomethasone	44	20-25
furoate mometasone	<0.1	<1
acetonide triamcinolone	Kāore he Mōhiohio	10,6-23
propionate fluticasone	0.5-2
flunisolide	40-50	21

Drugs pērā i "Afloderm" (urupare e pupuri ana tarapeke ki runga i runga i te kupenga), ki te tuhituhi i wehe hanga kahore tikanga. Ia o ratou ko te whakauru matua kaha, i te mea pea ki te kua kua oti whakahuatia i runga ake. Enei taero - corticosteroids rohe, a kua māngai ratou tino maha i roto i te puka o hinu aihikirīmi ranei.

A tuu i therapy glucocorticosteroid (tohu mō te whakamahi)

Hoki ia momo o glucocorticosteroids ona tohu mō te whakamahi. Ko te kupu, Kei te whakamahia corticosteroids waha ki te hamani:

• mate o Crohn;
• colitis ulcerative;
• disorders pūkahukahu interstitial;
• whakapeka syndrome romahā te pouri;
• kakā nui;
• ma'i mate pūkahukahu taunutia i roto i te wāhanga whakapeka;
• huangō arahau;
• thyroiditis subacute;
• congenital hyperplasia adrenal (i roto i tenei take, he tangata e kore e hua i corticoids ia me te takoha ki te tango i to ratou analogues waihanga);
• whakapeka iti hoki adrenal.

Hoki e whakamahia steroids i roto i te whakakapinga therapy o te kore napochechnikovoy tuatahi, me te tuarua.

E whakamahia corticosteroids Intranasal hoki:

• Rhinitis idiopathic (vasomotor);
• Rhinitis kore-mate pāwera ki eosinophilia;
• pilipoze ihu;
• te koiora Rhinitis pāwera (tamau);
• Rhinitis pāwera kaupeka (taratahi).

E whakamahia corticosteroids inhaled ki te hamani ma'i mate pūkahukahu taunutia, huangō arahau.

contraindications

kia hamani Whakatūpatotanga GCS i roto i teie mau huru haumanu:

• hohipera;
• papahewa;
• Ētahi mate o te taupoki io, e kua ngā ki abnormalities o te epithelium;
• fungal ranei mate viral o te kanohi;
• purulent mate;
• wā werohanga;
• pakewakewa;
• puka kaha o te mate kohi;
• herpes mate;
• mate fungal pūnaha;
• etahi mate hinengaro ki ngā tohu hua;
• tohu nui o te mate täkihi;
• takawhita;
• thromboembolism;
• whewhe duodenal puku ranei;
• mate huka;
• mate o Cushing.

corticosteroids intranasal tino contraindicated i roto i ngā take pēnei i:

• nosebleeds auau i roto i te hītori;
• hemorrhagic diathesis;
• hypersensitivity.

Glucocorticosteroids: pānga taha

Ka taea te wehea pānga te taha o corticosteroids ki rohe, me te nahanaha.

pānga taha Local

Wehea ki te pānga o hau me intranasal corticosteroids.

1. paanga kino Local i glucocorticosteroids hau:

• mare;
• dysphonia;
• candidiasis o te kōhao-waha, me te pharynx.

2. pānga taha Local o corticosteroids intranasal:

• perforation o te pakitara wehewehe nasal;
• nosebleeds;
• tahu a maroke kiriuhi mucous o te ihu, me te pharynx;
• tihe;
• ihu oranga.

pānga taha pūnahanaha

Wehea rite ki nga wahi o te tinana, e mahi.

1. wāhanga o te pūnaha io pokapū:

• psychoses;
• korekore;
• euphoria;
• ohoroa;
• kārangirangi.

2. Mai te pūnaha Cardiovascular:

• thromboembolism;
• Thrombosis rua hohonu;
• pēhanga toto tiketike;
• myocardiodystrophy.

3. Mai i te pūnaha whakaputa uri:

• hirsutism;
• roa te whanaketanga fakasekisualé;
• pōrearea fakasekisualé;
• iu huringa paheketanga.

4. Mai i te pūnaha kūnatu:

• fatty ate;
• pancreatitis;
• toto i te wahi gastrointestinal;
• tuwhenua pūtaiaki o te puku, me te paru.

5. Mai i te pūnaha endocrine:

• mate huka;
• syndrome o Cushing;
• mōmona;
• atrophy o te uho adrenal tika ki inhibition o tona mahi.

6. Mai te taha o te tirohanga:

• papahewa;
• posterior awhiowhio wai subcapsular.

7. Mai i te pūnaha musculoskeletal:

• uaua pahua;
• myopathy;
• akaaka tupu i roto i te tamariki;
• necrosis me wheua piere avascular;
• osteoporosis.

8. hoki te kiri:

• alopecia;
• striae;
• thinning o te kiri.

9. Ētahi atu ngā pānga taha:

• whakapeka puka hopuhopu, me te ma'i o ngā tukanga inflammatory;
• huamo;
• konutai me te wai te pupuri i roto i te tinana.

mehua whakatūpato

I roto i ētahi wā, kia whakamahia corticosteroids ki te tūpato.

Hei tauira, e taea te whakarei tūroro ki cirrhosis, hypothyroidism, hypoalbuminemia, me tūroro taipāpā ranei ruhiruhia mahi o corticosteroids.

tango i roto i te tono o corticosteroids i roto i hapūtanga kia ki pūkete te pānga e tūmanakohia o te maimoatanga mo te whaea, me te mōrea o te pānga kino o te tarukino i runga i te kukune, rite taea corticosteroids whakapōrearea i te whanaketanga o te tupu fetal me ara hē pērā i ngao ngatata , me te pera i runga i.

Ki te i roto i te whakamahi o GCS manawanui mamae mate (koroputa, karawaka, a na i runga i. D.), kia puta te reira rawa tino.

I roto i te maimoatanga o te tūroro ki corticosteroids autoimmune mate inflammatory (kaikōiwi, whēkau mate, erythematosus lupus pūnahanaha me te rite. D.) ranei kitenga taea te kite ātete pūtaiaki.

Tūroro te fariiraa i steroids-waha mo te wa roa, he mea e tika ana ia wā ki te tango i fecal toto wananga, me te haere fibroezofagogastroduodenoskopiyu rite whewhe pūtaiaki i roto i te maimoatanga ki kore ai e ohorere corticosteroids.

I roto i te 30-50% o tūroro peratia ki corticosteroids mo te wa roa, te whakawhanake osteoporosis. Ka rite ki te tikanga, pānga reira te waewae, ringa, papatoiake, rara, tuaiwi.

Ngā pāhekoheko ki ētahi atu taero

glucocorticosteroids katoa (e kore e whakarōpū mea faufaa konei) ka i roto i te whakapā ki ētahi atu taero hoatu he tetahi pānga, a kahore he tonu pai hoki to tatou tinana tenei pānga. Tenei te mea e hiahia ana koe ki te mohio i mua i te tono corticosteroids roto i te taha ki te tahi atu raau taero:

1. heke glucocorticosteroids absorption - GCS me patu waikawa.
2. GCS me barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - nui haere glucocorticosteroids biotransformation i roto i te ate te.
3. GCS me isoniazid, erythromycin - glucocorticosteroids biotransformation i roto i te ate heke.
4. SCS me salicylates, phenylbutazone, barbiturates, digitoxin, rongoā paturopi, chloramphenicol - whakakorenga whakarei te katoa o enei raau taero.
5. GCS me isoniazid - he takahi o te konä tangata.
6. Corticosteroids me reserpine - te putanga o te kāwanatanga fakalotofo'í.
7. GCS me tricyclic pōuritanga - nui haere pēhanga intraocular.
8. GCS me agonists - Kei te piki haere te mahi o enei taero.
9. Corticosteroids me theophylline - mahi anti-inflammatory o piki glucocorticoids, whakawhanake pānga cardiotoxic.
10. SCS me Diuretics, amphotericin B, mineralocorticoid - faarahi te mōrea o te hypokalemia.
11. kia aru e fifi hemorrhagic - GCS me autaki anticoagulants, fibrinolytics, butadiene, ibuprofen, waikawa ethacrynic.
12. SCS me indomethacin, salicylates - tenei huinga e taea meinga pāpaka ulcerative o te wahi gastrointestinal.
13. Corticosteroids me paracetamol - nui haere te tāoke o te tarukino te.
14. Corticosteroids me azathioprine - faarahi te mōrea o awhiowhio wai, myopathy.
15. GCS me mercaptopurine - huinga e taea arahi ki nui haere kukū o mua i roto i te toto.
16. GCS me hingamin - roa'tu, pānga e hiahiatia o tenei tarukino (Āheiō Corneal, myopathy, dermatitis).
17. GCS me methandrostenolone - faananea paanga kino o glucocorticoids.
18. Corticosteroids me taka rino, androgens - nui haere te kōtuitanga o erythropoietin, a ki tenei whakamārama, ka nui haere erythropoiesis.
19. GCS me hypoglycemic taero - tata oti whakaiti o ratou tōtika.

mutunga

Steroids - raau taero, kahore nei he pea ki te utu rongoā hou. E whakamahia ratou mo te maimoatanga o ngā wāhanga tino nui o te mate, ranei noa ki te whakarei ake i te mahi o te tarukino. Heoi, ka rite ki ki rongoā katoa, glucocorticosteroids pānga taha, me te whai rawa contraindications. Kaua e wareware e pā ana ki reira. Runga ake kua whakarārangitia matou nga take katoa te wahi e kore te mea e tika ana ki te whakamahi i steroids me kua ngā ano he rārangi o te pāhekoheko o corticosteroids ki ētahi atu taero. te huarahi o te mahi o corticosteroids me katoa o ratou pānga kua hoki kua whakaahuatia i roto i te taipitopito konei. Na katoa e hiahia ana koe ki te mohio e pā ana ki GCS, kei roto i te wahi kotahi - i tenei tuhinga. Heoi, i roto i tetahi take, e kore e tīmata maimoatanga i muri anake pānui i te mōhiohio whānui e pā ana ki GCS. Enei taero, o te akoranga, e taea te hokona kahore te whakahaunga, engari he aha e hiahia ana koe i te reira? I mua te whakamahi i tetahi taero kia tuatahi kōrero i te tohunga. Kia hauora, me te kore whaiaro medicate-!