GCS - i keia laau lapaau? I ka hana a me ka 'ole o ka ai' glucocorticosteroids

Heʻoiaʻiʻo au i lohe ai hoi no steroid hormones. Mākou kino mau produces ia e hooponopono i ola keʻano o ka hanaʻana. Ma keia 'atikala, mākou e noonoo glucocorticoids - steroid hormones, a i hua mai i loko o ka adrenal cortex. I ka hapanui o mākou e hoihoi i loko o kā lākou kemikala analogues - GCS. He aha ka lapaau? No ka a ka mea i hoʻohana a me ke ano o ka poho ka mea, i? E ka ike.

General 'ike e pili ana i GCS. He aha ka lapaau?

Mākou meaola synthesises steroid hormones e like me glucocorticoids. Ka mea, i hua mai ma ka adrenal cortex, a me kā lākou hoʻohana uaʻano nui e pili ana i ka iapaau ana o adrenal insufficiency. Kēia manawa, hoʻohana 'ole wale maoli glucocorticoids, akā, i ko lakou kemikala analogues - GCS. He aha ka lapaau? No ka manaʻo kanaka, kēia mau analogs ana paha o ka puu, me i ma luna o ke kino Anati-hoʻoʻino, immunosuppressive, antishock, Anati-allergic hopena.

ua lilo Glucocorticoids hoʻohana like ai '(haawiia i loko o ka' atikala - PM) ma ka 40-ies o XX kenekulia. Ma ka pau ana o ka 30s o ka iwakalua kenekulia,ʻepekema i loaʻa steroid hōmona i huiʻia i loko o kanaka adrenal cortex, a ma ka 1937 wae aku la oia i mineralocorticoid deoxycorticosterone. I ke kakahiaka nui 40-ies i loko glucocorticoid hydrocortisone a me ka cortisone. Pharmacological 'ole o ka cortisone a me ka hydrocortisone ua ai like, i ka mea i manao e hana ia e like me ka ai'. Ma hope o kekahi manawa, ua lawe mai ka noiʻi lākou hoʻololi kemikala.

Ka K'lauea glucocorticoid i loko o ke kanaka meaola mea - cortisol (mea like - hydrocortisone, kona kumukuai - 100-150 rubles), a me ka mea, ua manaoia he kumu nui. Ua mea i hiki ke kālā līkaia emiʻeleu: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

No a pau na glucocorticoids maoli e like me ka lāʻau i loaʻa wale hydrocortisone a me cortisone. Naʻe, i ka hope kumuʻaoʻao 'ole oi pinepine ma mua o kekahi' ē hōmona, i mea ke kumu ma ka keia manawa kona hoʻohana ma ka lapaau mea i kaupalena '. I ka lā, wale hoʻohana glucocorticoid hydrocortisone a me kona nā mea kemika (hydrocortisone hemisuccinate a me ka hydrocortisone'ākeka).

E pili ana i glucocorticosteroids (kemikala glucocorticoids), lawe hou mākou synthesized i ka helu ana o na konohiki, i waena a me ka fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, etc.) A 'ole-fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

Na konohiki hana ma mua o kā lākou maoli counterparts, a ua koi no ka iapaau ana o ka uuku nā māhele.

Keʻano papa hana o ka hana ana o corticosteroids

uaʻAʻole maopopo maopopo i ka hana ana o glucocorticoids ma ka hakakino kiʻekiʻe. ʻepekema, i mau ai 'hana ma luna keena ma ka pae o ka rula o ka'ōewe EKOLU.

Corticosteroids pāʻani aku me ka intracellular glucocorticoid receptors a pau loa imua i kaʻaneʻane na halepaahao o ke kanaka kino. I ka wa e kaawale aku o ka hōmona receptors (a mea cytosolic nā polokina) e wale deactivated. Ma ka AEeOEXAaI moku'āina, ka mea, i kekahi o na heterocomplexes, i loaʻa i immunophilin, wela hawewe nā polokina, a pela aku.

steroid i komo iloko o na keena (ma kaʻili lahilahi) wā, e nakinaki i ka receptors, a haʻalele luna ' "glucocorticoid + mea loaʻa", ma hope i ka mea komo i ka halepaahao nucleus a me ka hana me ka DNA wahi a i aia i loko o ka ka mea hoʻopaipai apana nahaha steroid like'ōewe (ka mea, i kekahi kapa glucocorticoid 'wahi a hehee wale). Complex "+ glucocorticoid mea loaʻa" mea hiki ke hooponopono i (inhibit paha, conversely, haʻalele) i ke kaʻina hana o ka Ekolu a o kekahi mau nā'ōewe. Kēia ka mea hiki aku ai i ka suppression paha stimulation o mRNA, e like me ka loli i loko o ka hoʻololi kemikala o nā nā'ūhū a me hoʻokonukonu nā polokina e mediate ke kelepona hele 'ole.

Ke Kula Kaiapuni 'haʻawina hōʻike i ka luna' "glucocorticoid + mea loaʻa" E hoʻolauna me kekahi EKOLU kumumea, no kekahi laʻana, e like me nukelea ololi kappa B (NF-kB) a me ka activator kumuʻiʻo EKOLU (AP-1) e hooponopono i na nā'ōewe komo i loko o ka'ōnaehana paleʻea pane a aat (mea pīlali nā lātoma, cytokine nā'ōewe, protease, a no laila, ma luna o.).

Ke kumu 'ole o GCS

glucocorticoids 'ole ma ke kanaka kino, he lehulehu. Mau hormones i antitoxic, antishock, imunnodepressivnoe, antiallergic, antiinflammatory a me ka antiinflammatory hana. E ka lawe i ka pilina nana i ana i ka hana o corticosteroids.

• Anati-hoʻoʻino hopena o corticosteroids. Kena ae la i ka suppression o ka ha awina o phospholipase A _2. A inhibition o keia'ūhū i loko o ke kanaka kino ua uhi pū liberatiou (hoʻokuʻu) ka inhibition o arachidonicʻakika a me ke kahua o kekahi hoʻoʻino uao (e like me prostaglandins, leukotrienes, a me ka troboksan na. D.). A, ke hiki aku glucocorticosteroids ho'ēmi i kā loli exudation, vasoconstriction (hou) capillaries, hana o microcirculation i loko o ka li nui.
• Anati-allergic hopena o GCS. Ua lŘlŘ like me ka hopena o hakumakuma secretion a me ka hoʻololi kemikala o uao o ka allergy, ho'ēmi i hoʻolahaʻia basophils, inhibition o histamine kala mai basophils a me kia keena sensitized, hoemi i ka helu ana o B a me T lymphocytes, hoemi pā lonoaʻili o aeee i na uao o ka allergy,'ōnaehana paleʻea muli o loli, e like me suppression o ka lāʻau lapaʻau kino? Iecaianoaaiiuo.
• Immunosuppressive haʻawina o GCS. He aha ka lapaau? Kēia 'o ia hoʻi i ka ai' inhibit immunogenez, uhi ka? Iecaianoaaiiie o nā mea'aʻaʻa. Corticosteroids inhibit Polenekia o ka iwi ka lolo kumu keena, inhibit i ka ha awina o B a me T lymphocytes inhibit i ke kala o cytokines mai macrophages a me leukocytes.
• Anati-ʻawahia a me ka antishock kanawai o corticosteroids. Ke kanawai o hormones, kena ae la ia e kiʻekiʻe ke koko, i loko o kānaka, e like me ka ho'ā hope o ke akepaʻa nā'ūhū komo i loko o ka pūnao o xenon a me ka endobiotikov.
• Mineralocorticoid ha awina. Glucocorticosteroids i ka hiki e retard paʻakai a me ka wai i loko o ke kino, hoʻoulu i ka excretion o potasiuma. Kēia kemikala ae pani ai iʻaʻole like ka maikai me maoli hormones, akā, ka mea, o ke kanawai ma ka kino ka mea, i.

Pharmacokinetics

No ka mea lōʻihi like 'ole o ka hana o ka systemic steroid i hiki ke maheleia i:

1. Glucocorticosteroids pōkole hana (e laʻa me, hydrocortisone, ke kumukuai o ka i loli aʻe mai ka 100 a hiki i 150 rubles).
2. Glucocorticosteroids me ka awelika lōʻihi like 'ole o ka hana (prednisolone (manaʻo i mea ole loa maikaʻi), methylprednisolone).
3. Glucocorticosteroids me ka hooloihi ae i hana (triamcinolone acetonide, dexamethasone, betamethasone).

Akā,ʻaʻole wale no e e hooponoponoia ia mea, i ka lōʻihi like 'ole o ka glucocorticosteroids. Mea Maluna o ia i kekahi e kaʻano o ka hooponopono:

• ku una ha;
• intranasal;
• Ana glucocorticosteroids.

Kēia Mea Maluna, nae, pili wale i ka'ōnaehana glucocorticosteroids.

Aia nō kekahi ai 'i loko o ka palapala o ka mea poni, a holika (kūloko corticosteroids). No ka laʻana, "Afloderm". Reviews o ia mau mea haʻilula keimikala i maikai.

E ka nana aku i ke ano o ka systemic corticosteroids wale.

Ke Ku una Ha steroid i kēlā wahi aku me ke kemu i loko o ka naʻau liʻiliʻi me ka hoʻomakaʻu pilikia. 'Imi nakinaki i nā polokina i loko o ka wai koko (transcortin, albumin). ʻO kā mākou lehulehu o ku una ha corticosteroids i loko o ke koko ua hiki aku ma hope o 1.5 hola ma hope hooponopono. Ka mea, undergo biotransformation ma ke akepaʻa, hakuʻala (hapa 'ia) a me ka' ē aʻe nā'aʻaʻa ma conjugation e glucuronide paha sulufahate.

Kahi o 70% o ka conjugated GCS excreted i loko o ka mimi, kekahi 20% i loko o nā feces, e hōʻike hope, a me ke koena - me nā liluwelo fluids (e laʻa me, hope). Ka hapalua - mai ka 2 a hiki i 4 hola.

Oe ke hana i kekahi mea uuku papaaina me ka pharmacokinetic kiko'î o ku una ha corticosteroids.

Glucocorticosteroids. Ai '(inoa)	Ka hapa-ola o ka'aʻaʻa	Wai koko hapa-ola
hydrocortisone	8-12 hola	0.5-1.5 hola
cortisone	8-12 hola	0.7-2 hola
Prednisolone (hōʻike manaʻo nō,ʻaʻole loa maikaʻi)	18-36 hola	2-4 hola
methylprednisolone	18-36 hola	2-4 hola
fludrocortisone	18-36 hola	3.5 hola
dexamethasone	36-54 hola	5:00

Ana steroid i loko o ke kālā no lapaʻau me ka hana pono imua o triamcinolone acetonide, fluticasone propionate, mometasone furoate, budesonide a me ka beclomethasone dipropionate.

Pharmacokinetic kiko'î hoi hiki ke hooku iho la ia ia ma ka papaʻaina.

Glucocorticosteroids. Ai '(inoa)	Ke kūloko Anati-hoʻoʻino ha awina	ka leo o ka haawi aku	Wai koko hapa-ola	Ka hoʻokōʻana o ka hooholo ma ke ake
beclomethasone dipropionate	0,64 huahelu.	-	0.5 hola	70%
budesonide	1 pa alima.	4,3 L / kg	1,7-3,4 hola	90%
triamcinolone acetonide	0,27 huahelu.	1,2 L / kg	1.4-2 hola	80-90%
fluticasone propionate	1 pa alima.	3,7 L / kg	3.1 hola	99%
flunisolide	0,34 huahelu.	1.8 L / kg	1,6 hola	-

Nasal steroid i ka lapaau i keia la imua o fluticasone propionate, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide a me ka beclomethasone dipropionate. Kekahi o lakou, ua kapaia ka mea e like me ana corticosteroids.

Ma hope o ke noi ana o ka mahele lāʻau intranasal corticosteroids ke kemu i loko o ka naʻau liʻiliʻi, a kekahi hapa mai, mai ka airway mucosa 'ana i loko o ke koko.

Glucocorticosteroids, trapped ma ka digestive'āpana, i hoʻokemuʻia no kahi o 1-8 pakeneka, a me ka mea mua, e hele ia ma ke akepaʻa biotransformed kokoke loa i ka AEeOEXAaI metabolites.

Glucocorticosteroids a i loaa i loko o ke koko, hydrolyze i AEeOEXAaI waiwai. Eia ka ka papaʻaina a me kā lākou pharmacokinetic kiko'î:

Glucocorticosteroids. hoomakaukau	Bioavailability komo ka wā i ke koko, e like me ka pakeneka	Bioavailability ka wā o ke kemu, mai ka gastrointestinal'āpana, ma ka pakeneka
budesonide	34	11
beclomethasone dipropionate	44	20-25
mometasone furoate	<0,1	<1
triamcinolone acetonide	No Information	10,6-23
fluticasone propionate	0.5-2
flunisolide	40-50	21

Ai 'e like me "Afloderm" (manaʻo i mālama i popping mai ma luna o ka upena), e hōʻike kaawale i ole ano. Kēlā me kēia no ia mea i ka papa kuhikuhiEʻeleu 'Oponopono, a mea paha i ka ua mua, ua kau aʻela ma luna. Mau ai '- i nā corticosteroids, a me ka mea, i na poe loa pinepine i loko o ka palapala o ka mea poni a me holika.

E kau glucocorticosteroid Inc (nāʻikepili no ka hoʻohana)

No kēlā me kēiaʻano o ka glucocorticosteroids kona nāʻikepili no ka hoʻohana. Pela, ua hoʻohana 'ku una corticosteroids e hana:

• Crohn ka maʻi;
• ulcerative colitis;
• interstitial akemāmā kāna hana;
• huʻi naehana pilikia maʻi pale;
• loa pneumonia;
• maʻi obstructive pulmonary maʻi i loko o huʻi pae;
• bronchial asthma;
• subacute thyroiditis;
• congenital adrenal hyperplasia (i loko o keia hihia, he kanaka, aole ia e paka corticoids ia ia iho, a ua kiola, e lawe i ko lakou kemikala analogues);
• huʻi adrenal insufficiency.

No hoi i hoʻohana steroid ma hope Inc o iniiaiie a me ka haumāna napochechnikovoy ole.

Intranasal corticosteroids mea hoʻohana no:

• idiopathic rhinitis (vasomotor);
• ole-allergic rhinitis me ka eosinophilia;
• pilipoze ihu;
• perennial allergic rhinitis (koʻikoʻi);
• naciiiuo allergic rhinitis (intermittent).

Ana corticosteroids e hoʻohana i ka hana maʻi obstructive pulmonary maʻi, bronchial asthma.

Contraindications

Kaiapuni e hana GCS i loko o kēia mau wahi, i hiki lapaʻau:

• lactation;
• glaucoma;
• Kekahi mau maʻi o ka cornea, a i hui ai me abnormalities o ka epithelium;
• fungal a mea hoʻomaʻi maʻi o ka maka;
• purulent maʻiʻaʻai;
• vaccination au;
• syphilis;
• ʻeleu ke ano o ka tuberculosis;
• herpes maʻiʻaʻai;
• systemic fungal nā mea palahēhē;
• kekahi noʻonoʻo maʻi me ka hoʻomāhuahua ai symptoms;
• loa degere o kaʻaʻa puʻuwai ole;
• hypertension;
• thromboembolism;
• duodenal ulcer paha'ōpū;
• mimikō;
• Cushing ka maʻi.

Pololei contraindicated intranasal corticosteroids i loko o ia hihia.

• pinepine nosebleeds ma ka mōʻaukala;
• hemorrhagic diathesis;
• hypersensitivity.

Glucocorticosteroids:ʻaoʻao loa

ʻaoʻao 'ole o nā corticosteroids hiki ke maheleia i kūloko a me ka systemic.

Localʻaoʻao waiwai

Maheleia i loko o ka hopena o ka ana a me ka intranasal corticosteroids.

1. Local adverse 'ole mai ana glucocorticosteroids:

• cough;
• dysphonia;
• candidiasis o ku una ha i ka lua a me ka pharynx.

2. Localʻaoʻao hopena o intranasal corticosteroids:

• perforation o ka nasal septum;
• nosebleeds;
• ke ahi a me ka maloo mucous membranes o ka ihu a me ka pharynx;
• kiheʻana;
• itchy ihu.

Systemicʻaoʻao waiwai

I puunaue e like me ka māhele o ka kino, i hana.

1. Part o ka Central ko mākou hopohopo'ōnaehana:

• psychoses;
• kaumaha;
• euphoria;
• Kanikani'āʻula;
• irritability.

2. No ka mea'ōnaehana mānowai koko'ōnaehana:

• thromboembolism;
• hohonu aa koko thrombosis;
• kiʻekiʻe ke koko;
• myocardiodystrophy.

3. Mai ka reproductive'ōnaehana:

• hirsutism;
• hoolohi moe ulu ana;
• moe dysfunction;
• lolelua ka menstrual pōʻaiapuni.

4. Mai ka digestive'ōnaehana:

• momoma ake;
• pancreatitis;
• kahe ana ke koko mai ka gastrointestinal'āpana;
• steroid ulcers o ka'ōpū a me ka naʻau liʻiliʻi.

5. Mai ka endocrine'ōnaehana:

• mimikō;
• Cushing ka maʻi pale;
• obesity;
• atrophy o ka adrenal cortex ma muli o ka inhibition o kona kuleana pili i.

6. Mai kaʻaoʻao o Hawaii:

• glaucoma;
• posterior subcapsular cataracts.

7. Mai ka musculoskeletal'ōnaehana:

• Muscle i hoomaunauna aku ai;
• myopathy;
• stunted ka ulu ana i loko o na keiki;
• avascular necrosis a me ka iwi fractures;
• osteoporosis.

8. No ka meaʻili.

• alopecia;
• striae;
• thinning o ka ili.

9. Otherʻaoʻao ole:

• huʻi infectious a me ka maʻi ano o ka hoʻoʻino keʻano o ka hanaʻana;
• haanou ana;
• paʻakai a me ka wai ka mālama i loko o ke kino.

precautionary ana

Ma kekahi mau hihia, e ke hoʻohana corticosteroids me ka mālama nui.

No ka laʻana, nā mea maʻi me ka cirrhosis, hypothyroidism, hypoalbuminemia, a me nā mea maʻi senile ole kūpuna i hiki ke hoʻokāʻoi hana o corticosteroids.

Ma ka noi o corticosteroids i hāpai keiki e lawe i ka mooolelo o ka kakali ana i kanawai o ka lapaau no ka makuwahine, a me ka pilikia o ka hopena maikaʻi kanawai o ka lāʻau ma luna o ka fetus, like corticosteroids hiki loko o ka ulu ana o fetal ulu, a e like mā e like me mauae kīleo , a no laila, ma luna o.

Inā i hoʻohana o GCS hoomanawanui poino maʻiʻaʻai (moa pox,ʻo Waimānalo, a no laila, ma luna o. D.), Ua kānāwai loa seriously.

Ma ka iapaau ana o nā mea maʻi me ka corticosteroids a autoimmune hoʻoʻino mai (rheumatoid arthritis, na naau oʻu maʻi, systemic lupus erythematosus a me ka e like. D.) Sightings steroid ia'ku hiki ke malama.

E hoomanawanui i ka loaa una steroid no ka lōʻihi manawa, ia mea e pono ai kekahi manawa e lawe fecal occult koko, a hele aku fibroezofagogastroduodenoskopiyu like steroid ulcer i lapaʻau me corticosteroids hiki ole ke nee.

I 30-50% o nā mea maʻi ia me corticosteroids no ka lōʻihi manawa, hoʻomōhala osteoporosis. E like me ka rula, ka mea e loli ai ka wawae, ka lima, pelvis, o kona iwiʻaoʻao, spine.

AaOIeIOUIeXAOAaIN me nā ai '

All glucocorticosteroids (Mea Maluna 'aʻole i mea' aneʻi) ia ma ka hui 'ana me nā ai' e haawi aku i ka kekahi kanawai, a me keia keia mea,ʻaʻole mau maikaʻi no mākou kino. Eia mea e pono ai, e ike mua ana corticosteroids ma ka huipūʻana me nā ai ':

1. GCS a antacids - glucocorticosteroids omo emi.
2. GCS a me barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - glucocorticosteroids biotransformation ma ke akepaʻa ua mahuahua.
3. GCS a me isoniazid, erythromycin - glucocorticosteroids biotransformation ma ke akepaʻa emi.
4. SCS a me salicylates, phenylbutazone, barbiturates, digitoxin, penicillin, chloramphenicol - a pau o kēia mau ai 'ua hoʻokāʻoi hoʻopau.
5. GCS a isoniazid - he 'aʻe' ana o ke kanaka psyche.
6. Corticosteroids a me reserpine - ka muli o depressive moku'āina.
7. GCS a tricyclic antidepressants - māhuahua intraocular puʻe.
8. GCS a me agonists - i ka hana o kēia mau ai 'no ka hana.
9. Corticosteroids a theophylline - Anati-hoʻoʻino hana o glucocorticoids, piʻi pū, hoʻomōhala cardiotoxic 'ole.
10. SCS a me diuretics, amphotericin B, mineralocorticoid - maoli i ka pilikia o ka hypokalemia.
11. GCS a me kaʻauhau'ēʻaʻe anticoagulants, fibrinolytics, butadiene, ibuprofen, ethacrynicʻakika - i e hahai ma hemorrhagic complications.
12. SCS a me indomethacin, salicylates - keia hui pu ana, hiki i ulcerative lesions o ka gastrointestinal'āpana.
13. Corticosteroids a me paracetamol - ka kaʻawahia o ka lāʻau ua mahuahua.
14. Corticosteroids a azathioprine - maoli i ka pilikia o cataracts, myopathy.
15. GCS a mercaptopurine - hui pu ana, ke alakai i māhuahua lehulehu o uricʻakika i loko o ke koko.
16. GCS a hingamin - listen hua'ōlelo i makemake 'ole o kēia k (corneal opacity, myopathy, dermatitis).
17. GCS a methandrostenolone - listen adverse hopena o glucocorticoids.
18. Corticosteroids a me ka hao hoomakaukau, androgens - māhuahua hoʻololi kemikala o erythropoietin, a kū'ē i kēia kāʻei kua, a mahuahua erythropoiesis.
19. GCS a hypoglycemic ai '- kokoke e piha ka ho'ēmiʻana o ko lākou laulā.

ka hopena

Steroid - ai ', me ka i laekahi lapaau mea olelo lealea, e loaʻa. Ka mea, i hoʻohana 'ia no ka iapaau ana o ka loa hanahana loa kuʻina o ka maʻi, ai wale no ka hōʻoi' i ka hana o ka lāʻau. Eia naʻe, e like me nā mea a pau lapaʻauʻia, glucocorticosteroidsʻaoʻao 'ole, a i contraindications pū. Mai hoʻopoina no ia. Ma luna o mākou i helu 'ia ma nā mea a pau nā hihia i kahi ia mea,ʻaʻole e pono e hoʻohana steroid i, a ua hoomakaukau no hoi i ka papa inoa o ka AaOIeIOUIeXAOAaIN o corticosteroids me'ē aʻe ai'. i keʻano papa hana o ka hana ana o corticosteroids a me nā mea a pau o ko lākou mau waiwai i oleloia ua hiki aku no hoi ma ka au mamuliʻaneʻi. Ano a pau e pono ai, e ike no GCS, ua ma kekahi wahi - keia 'atikala. Eia naʻe, ma kekahi hihia, mai hoʻomaka lapaau e heluhelu ana i ka mau 'ike e pili ana i GCS wale nō ma hope. Mau ai ', o ka papa, hiki ke kuai me ke kuhikuhi, akā, no ke aha la oe e pono ia? Ma mua o ka hoʻohana 'ana i kekahi ai' e mua nīnau i ka hoʻomalu. E ola a me ka ole ka hoʻoponopono-lapaʻau!