GCS - kuti mankhwalawa? Kanthu ndi zotsatira za mankhwala glucocorticosteroids

Ndithudi inu munayamba mwamvapo za mahomoni steroid. Thupi lathu nthawi zonse umabala iwo zonse zamoyo. M'nkhani ino tikambirana glucocorticoids - steroid mahomoni omwe amatuluka mu kotekisi adrenal. Ngakhale ambiri a ife chidwi analogues awo kupanga - GCS. mankhwala ndi chiyani? Umene ntchito ndi wotani kuwononga iwo chifukwa? Tiyeni tiwone.

General zokhudza GCS. mankhwala ndi chiyani?

chamoyo wathu synthesises mahomoni steroid monga glucocorticoids. Iwo amatuluka ndi kotekisi adrenal, ndi ntchito yawo makamaka zokhudzana ndi mankhwala a insufficiency adrenal. Masiku ano, ntchito osati glucocorticoids zachilengedwe, komanso analogues awo kupanga - GCS. mankhwala ndi chiyani? Kwa anthu, analogs izi zikutanthauza kwambiri, monga pa thupi odana ndi yotupa, immunosuppressive, antishock, odana ndi matupi awo sagwirizana kwenikweni.

Glucocorticoids akhala ntchito ngati mankhwala (anatchula m'nkhani - PM) mu 40 ntchentche wa XX atumwi. Pofika kumapeto kwa 30s zaka mazana makumi awiri, asayansi apeza mankhwala steroid timadzi mwa anthu adrenal kotekisi, ndipo mu 1937 anasankhidwa mineralocorticoid deoxycorticosterone. Kumayambiriro 40 ntchentche anali linachokera glucocorticoid hydrocortisone ndi cortisone. Zotsatira pharmacological wa cortisone ndi hydrocortisone anali osiyanasiyana, kuti anaganiza kuwagwiritsa ntchito mankhwala osokoneza bongo. Patapita nthawi, asayansi ikuchitika kaphatikizidwe awo.

The glucocorticoid achangu mu thupi la munthu ndi - tochepa (analogue - hydrocortisone, amene mtengo - 100-150 rubles), ndipo amaona yaikulu. N'zothekanso kuonetsetsa layamba: corticosterone, cortisone, 11 deoxycortisol, 11 dehydrocorticosterone.

Wa glucocorticoids zonse zachilengedwe monga kugwiritsa ntchito mankhwala imapezeka hydrocortisone ndi cortisone. Komabe, yotsirizira zotsatira zimayambitsa mbali kambirimbiri kuposa timadzi ina, nchifukwa chake pa nthawi ino ntchito mankhwala yochepa. Pakali pano, ankangomva glucocorticoid hydrocortisone kapena esters ake (hydrocortisone hemisuccinate ndi hydrocortisone nthochi).

Ponena glucocorticosteroids (kupanga glucocorticoids), panopa ife apanga angapo wothandizila amenewa, Pakati pa fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, etc.) Ndipo sanali fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

wothandizila amenewa yogwira kuposa anzawo zachilengedwe, ndiponso zifunika zochizira Mlingo wocheperako.

Limagwirira cha zochita za corticosteroids

Zimene glucocorticoids pa mlingo maselo si bwino. Asayansi amakhulupirira kuti mankhwala zinthu pa maselo pa mlingo wa lamulo la galamafoniyo mbewu.

Corticosteroids kucheza ndi okhudza maselo ambiri glucocorticoid zolandilira alipo pafupifupi yonse yochepetsetsa ya thupi. Popeza zolandilira timadzi (amene ali cytosolic mapuloteni) Kungoti deactivated. M'chigawo wofooka, iwo ali mbali ya heterocomplexes, amene akuphatikizapo komanso immunophilin, mapuloteni kutentha mantha ndi zina zotero.

Pamene mankhwala kudutsa maselo (kudzera Kakhungu ndi), amanga kwa maselo ndi yambitsa zovuta "glucocorticoid + cholandilira", kenako akulowa selo phata ndi interacts ndi zigawo DNA zomwe zili jini kulimbikitsa mpukutu steroid lolingana (iwo akutchedwanso glucocorticoid 'anayankha zinthu). Ovuta "+ glucocorticoid cholandilira" amatha zonse (ziletsa kapena, Tikawonetsetsa yambitsa) ndondomeko galamafoniyo imene imachititsa ena. Izi zimathandiza yimitsira kapena kukondoweza kwa mRNA, komanso kusintha kaphatikizidwe wa michere zosiyanasiyana ndi mapuloteni zolimbana kuti ayimire zotsatira ma.

maphunziro osiyanasiyana amasonyeza kuti zovuta "glucocorticoid + cholandilira" interacts ndi zinthu zosiyana galamafoniyo, mwachitsanzo, monga nyukiliya chinthu kappa B (NF-KB) ndi activator mapuloteni galamafoniyo (AP-1) kuti zonse majini nawo poyankha cha m'thupi ndipo kutupa (guluu wolimba mamolekyulu, majini cytokine, protease ndi zina zotero.).

Zotsatira waukulu GCS

Zotsatira glucocorticoids pa thupi ndi ambiri. mahomoni awa ali antitoxic, antishock, imunnodepressivnoe, antiallergic, antiinflammatory ndi antiinflammatory kanthu. Tiyeni tione mmene zochita za corticosteroids.

• Anti-yotupa zotsatira za corticosteroids. Anapangitsa yimitsira za ntchito ya phospholipase A liberatiou _2. Pamene chopinga wa puloteni imeneyi mu thupi la munthu kuletsedwa (kumasulidwa) ndi chopinga asidi arachidonic ndi mapangidwe ena owayimira yotupa (monga prostaglandins, leukotrienes, ndi troboksan T. D.). Komanso, phwando glucocorticosteroids kumachepetsa madzimadzi exudation, vasoconstriction (kuchepetsa) capillaries, kusintha kwa microcirculation mu kutukusira kwa.
• Anti-matupi awo sagwirizana zotsatira za GCS. Kumachitika chifukwa cha kutsitsa katulutsidwe ndi kaphatikizidwe amkhalapakati a ziwengo, kuchepetsa kufalitsidwa basophils, chopinga wa histamine kumasulidwa ku basophils ndi maselo mlongoti kupatsa, kuchepetsa chiwerengero cha B ndipo T lymphocytes, kuchepetsa tilinazo maselo kwa amkhalapakati a ziwengo, chitetezo ayankhe kusintha, komanso yimitsira kupanga oteteza.
• Immunosuppressive ntchito GCS. mankhwala ndi chiyani? Izi zikutanthauza kuti mankhwala ziletsa immunogenez, kuletsa kupanga chitetezo. Corticosteroids ziletsa kusamuka maselo tsinde mafupa, ziletsa ntchito B ndipo T lymphocytes ziletsa amasulidwe cytokines ku macrophages ndi leukocytes.
• Anti-poizoni ndi antishock zotsatira za corticosteroids. Zotsatira za mahomoni chifukwa cha kuthamanga magazi anthu, komanso kutsegula kwa michere chiwindi nawo kagayidwe wa xenon ndi endobiotikov.
• Mineralocorticoid ntchito. Glucocorticosteroids angathe achigonjetse soda ndi madzi m'thupi, Zimachititsa excretion wa potaziyamu. Izi mmalo kupanga si abwino monga mahomoni achilengedwe, koma ndi mphamvu pa thupi ali.

Pharmacokinetics

Pakuti nthawi ya zochita za mankhwala zokhudza zonse angathe kugawidwa:

1. Glucocorticosteroids lalifupi kanthu (mwachitsanzo, hydrocortisone, mtengo umene umasiyana rubles 100 150).
2. Glucocorticosteroids ndi nthawi avareji kanthu (prednisolone (maganizo omwe si zabwino kwambiri), methylprednisolone).
3. Glucocorticosteroids ndi kanthu yaitali (triamcinolone acetonide, dexamethasone, betamethasone).

Koma osati pa nthawi yonse ya glucocorticosteroids akhoza zotsimikizika. Gulu la iwo angakhalenso akafuna makonzedwe:

• m'kamwa;
• intranasal;
• Mpweya glucocorticosteroids.

Gawo Komabe, amangonena za dongosolo glucocorticosteroids.

Pali mankhwala ena mu mawonekedwe a mafuta ndi creams (corticosteroids wamba). Mwachitsanzo, "Afloderm". Reviews a formulations amenewa ndi abwino.

Tiyeni tione mitundu ya corticosteroids zokhudza zonse yekha.

mankhwala Oral mwangwiro odzipereka mu intestine popanda kuchititsa mavuto. Mwakhama kumumanga kwa mapuloteni mu madzi ndi (transcortin, albumin). Ndende pazipita corticosteroids m'kamwa mwa magazi kukufika pambuyo maola 1.5 pambuyo utsogoleli. Akukumana biotransformation mu chiwindi, impso (pang'ono) ndipo zimakhala ena mwa conjugation kuti glucuronide kapena sulphate.

Pafupifupi 70% ya GCS conjugated excreted mu mkodzo, wina 20% mu ndowe adzasonyeza kenako, ndi zina - ndi madzi ena kwachilengedwenso (mwachitsanzo, zitatha). The theka - kuchokera maola 2 kapena 4.

Mukhoza jambulani tebulo kakang'ono ndi magawo pharmacokinetic wa corticosteroids m'kamwa.

Glucocorticosteroids. Mankhwala (maina)	Hafu ya moyo minofu	Madzi a m'magazi theka moyo
hydrocortisone	maola 8-12	maola 0.5-1.5
cortisone	maola 8-12	maola 0.7-2
Prednisolone (ndemanga si zabwino kwambiri)	maola 18-36	maola 2-4
methylprednisolone	maola 18-36	maola 2-4
fludrocortisone	maola 18-36	maola 3.5
dexamethasone	maola 36-54	5:00

Mpweya mankhwala kuchita ano matenda anapereka triamcinolone acetonide, fluticasone propionate, mometasone furoate, budesonide ndi beclomethasone dipropionate.

magawo Pharmacokinetic angathe kuwonetsa tebulo:

Glucocorticosteroids. Mankhwala (maina)	M'deralo odana ndi yotupa ntchito	buku la yogawa	Madzi a m'magazi theka moyo	Dzuwa la kudutsa chiwindi
beclomethasone dipropionate	0,64 mayunitsi.	-	maola 0.5	70%
budesonide	1 unit.	4.3 L / kg	ola 1,7-3,4	90%
triamcinolone acetonide	0,27 mayunitsi.	1.2 L / kg	maola 1.4-2	80-90%
fluticasone propionate	1 unit.	3,7 L / kg	maola 3.1	99%
flunisolide	0,34 mayunitsi.	1.8 L / kg	maola 1.6	-

mankhwala m'mphuno mankhwala lero anapereka fluticasone propionate, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide ndi beclomethasone dipropionate. Ena mwa iwo akutchedwa monga momwe corticosteroids Mpweya.

Pambuyo ntchito mlingo intranasal corticosteroids odzipereka mu intestine ndi gawo lina amachokera airway mucosa mwachindunji mu m'magazi.

Glucocorticosteroids, kukanirira mu kapepala kakuti m'mimba, ali odzipereka kwa 1-8 peresenti, ndi chiphaso choyamba kudzera chiwindi biotransformed pafupifupi kwathunthu metabolites kulalikira.

Glucocorticosteroids amene analowa magazi, hydrolyze kuti zinthu kulalikira. Apa ndi tebulo ndi magawo awo pharmacokinetic:

Glucocorticosteroids. kukonzekera	Bioavailability pamene adalowa magazi, monga kuchuluka ndi	Bioavailability pamene odzipereka kwa mundawo m'mimba, mu peresenti
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

Mankhwala monga "Afloderm" (maganizo amene amasunga zayamba mmwamba pa ukondewo), pofotokoza payokha amapanga sazindikira. Aliyense wa iwo ndi waukulu yogwira pophika, zomwe zikuoneka kuti kale tatchulazi. Izi mankhwala - corticosteroids m'derali ndipo iwo amakhala nthawi zambiri mu mawonekedwe a mafuta kapena creams.

Ikani mankhwala glucocorticosteroid (zikuonetsa ntchito)

Pakuti mtundu uliwonse wa glucocorticosteroids zizindikiro zake ntchito. Choncho, corticosteroids m'kamwa ntchito pofuna kuchiza:

• matenda amene amatupitsa;
• anam'peza matenda a m'matumbo;
• interstitial m'mapapo matenda;
• pachimake kupuma mavuto syndrome;
• aakulu chibayo;
• aakulu obstructive m'mapapo mwanga matenda mu gawo pachimake;
• bronchial mphumu;
• subacute thyroiditis;
• kobadwa nako adrenal hyperplasia (mu nkhani iyi, munthu sangabereke corticoids yekha ndi amakakamizidwa kutenga analogues awo kupanga);
• pachimake adrenal insufficiency.

Komanso mankhwala ntchito m'malo mankhwala a pulayimale ndi sekondale napochechnikovoy kulephera.

corticosteroids Intranasal ntchito:

• idiopathic rhinitis (vasomotor);
• si matupi awo sagwirizana rhinitis ndi eosinophilia;
• pilipoze mphuno;
• osatha matupi awo sagwirizana rhinitis (kulimbikira);
• nyengo matupi awo sagwirizana rhinitis (likukulira).

corticosteroids Mpweya ntchito pofuna kuchiza aakulu obstructive m'mapapo mwanga matenda, bronchial mphumu.

contraindications

CHENJEZO kuchitira GCS zinthu izi matenda:

• mkaka wa m'mawere;
• khungu;
• Matenda a diso, amene amaphatikizidwa ndi kuvutika kwa epithelium ya;
• mafangasi kapena matenda tizilombo diso;
• purulent matenda;
• nthawi katemera;
• chindoko;
• yogwira mawonekedwe a chifuwa chachikulu;
• nsungu matenda;
• zokhudza zonse mafangasi matenda;
• ena matenda okhudza ubongo ndi zizindikiro zipatso;
• digiri aakulu kulephera aimpso;
• oopsa;
• thromboembolism;
• mmatumbo chilonda kapena m'mimba;
• shuga;
• matenda Cushing a.

Mosamalitsa contraindicated intranasal corticosteroids mu Zikatero:

• nosebleeds pafupipafupi m'mbiri;
• hemorrhagic diathesis;
• hypersensitivity.

Glucocorticosteroids: mavuto

Zotsatira zake zoyipa za corticosteroids akhoza kugawidwa mu m'deralo ndi zokhudza zonse.

Zotsatira zoyipazi Local

Ogaŵikana zotsatira za corticosteroids Mpweya ndi intranasal.

1. Local mavuto kwa glucocorticosteroids Mpweya:

• kutsokomola;
• dysphonia;
• candidiasis wa M'mimbamo m'kamwa, pharynx.

2. zotsatira Local mbali ya corticosteroids intranasal:

• perforation wa m'mphuno septum;
• nosebleeds;
• moto ndi youma nembanemba mucous ya mphuno ndi pharynx;
• sneezing;
• kuyabwa mphuno.

zotsatira zokhudza zonse mbali

Anagawa monga ziwalo za thupi, amene ntchito.

1. Gawo wa chapakati mantha dongosolo:

• psychoses;
• maganizo;
• euphoria;
• tulo;
• irritability.

2. Popeza dongosolo mtima:

• thromboembolism;
• kwambiri mtsempha thrombosis;
• kuthamanga magazi;
• myocardiodystrophy.

3. ziwalo zoberekera:

• hirsutism;
• anachedwa chitukuko cha kugonana;
• kukanika kugonana;
• wosakhazikika kusamba mkombero.

4. dongosolo m'mimba:

• mafuta m'chiwindi;
• kapamba;
• magazi kwa mundawo m'mimba;
• zilonda steroid kwa m'mimba ndipo matumbo.

5. dongosolo endocrine:

• shuga;
• syndrome Cushing ndi;
• kunenepa;
• manja a kotekisi adrenal chifukwa chopinga wa ntchito yake.

6. Kuchokera mbali ya view:

• khungu;
• zapambuyo ng'ala subcapsular.

7. dongosolo minofu ndi mafupa:

• minofu zingatiwonongere;
• myopathy;
• kungokhala pamodzimodzi kukula ana;
• avascular necrosis ndi fupa fractures;
• kufooka kwa mafupa.

8. khungu:

• alopecia;
• striae;
• kupatulira wa khungu.

9. Other mavuto:

• pachimake opatsirana ndi aakulu mitundu ya njira yotupa;
• kutupa;
• soda ndi madzi posungira mu thupi.

kusamala

Nthawi zina, corticosteroids ayenera kugwiritsidwa ntchito mosamala.

Mwachitsanzo, odwala matenda enaake, hypothyroidism, hypoalbuminemia, ndi odwala senile kapena achikulire patsogolo ntchito ya corticosteroids.

Mu ntchito corticosteroids pa mimba ayenera kuganizira zotsatira sikhala wa mankhwala mayi ndi chiopsezo cha zoyipa za mankhwala pa mwana wosabadwayo, monga corticosteroids angasokoneze chitukuko cha kukula yoopsa ngakhalenso kupunduka monga vuto ndi zina zotero.

Ngati pa ntchito GCS mtima amadwala matenda (nthomba, chikuku, ndi zina zotero. D.), Ndi kumachitika kwambiri kwambiri.

Mankhwalawa odwala corticosteroids kapena autoimmune matenda yotupa (nyamakazi, matenda matumbo, zokhudza zonse lupus erythematosus ndi zina zotero. D.) Zipangizo steroid kukana zingaoneke.

Odwala kulandira mankhwala m'kamwa kwa nthawi yaitali, m'pofunika nthawi kutenga fecal zamatsenga magazi ndi pochitika fibroezofagogastroduodenoskopiyu monga steroid chilonda pa mankhwala ndi corticosteroids mwina kusokonezedwa.

Mu 30-50% odwala mankhwala corticosteroids kwa nthawi yaitali, kukhala kufooka kwa mafupa. Monga ulamuliro, sukhala phazi, dzanja, mafupa a chiuno, nthiti, msana.

Mogwirizana ndi mankhwala ena

glucocorticosteroids onse (gulu zilibe kanthu pano) pamene anakumana ndi mankhwala ena kupereka zotsatira zina, ndi mawu amenewa si nthawi zonse zabwino kwa thupi lathu. Apa pali chimene muyenera kudziwa patsogolo ntchito corticosteroids molumikizana ndi mankhwala ena:

1. GCS ndi Mankhwalawa ayenera kumwedwa - glucocorticosteroids mayamwidwe amachepetsa.
2. GCS ndi barbiturates, phenytoin, hexamidine, ndi diphenhydramine, carbamazepine, rifampicin - glucocorticosteroids biotransformation mu chiwindi ndi kuchuluka.
3. GCS ndi isoniazid, mankhwalawa - glucocorticosteroids biotransformation mu chiwindi amachepetsa.
4. SCS ndi salicylates, phenylbutazone, barbiturates, digitoxin Penicillin, chloramphenicol - onse mankhwala kumatheka kuwonongedwa.
5. GCS ndi isoniazid wa - kuphwanya psyche anthu.
6. Corticosteroids ndi reserpine - zikamera wa boma maganizo.
7. GCS ndi tricyclic antidepressants - kuthamanga intraocular.
8. GCS ndi agonists - kanthu mankhwala zikuchulukirachulukira.
9. Corticosteroids ndi theophylline - odana ndi yotupa kanthu za glucocorticoids ukuwonjezeka, kukhala zotsatira cardiotoxic.
10. SCS ndi okodzetsa, amphotericin B, mineralocorticoid - kumaonjezera ngozi ya hypokalemia.
11. GCS ndi mosadziwika anticoagulants, fibrinolytics, butadiene, ibuprofen, asidi ethacrynic - ingathe kuchitidwa ndi mavuto hemorrhagic.
12. SCS ndi indomethacin, salicylates - kuphatikiza zingachititse zotupa anam'peza pa mundawo m'mimba.
13. Corticosteroids ndi paracetamol - ndi kawopsedwe wa mankhwala ndi kuchuluka.
14. Corticosteroids ndi azathioprine - kumaonjezera ngozi ya ng'ala, myopathy.
15. GCS ndi mercaptopurine - kuphatikiza akhoza patsogolo ndende asidi uric m'magazi.
16. GCS ndi hingamin - nakweza zotsatira zapathengo za mankhwala (corneal Kuwonekera, myopathy, dermatitis).
17. GCS ndi methandrostenolone - azimveka mavuto glucocorticoids.
18. Corticosteroids ndi kukonzekera chitsulo, androgens - kuchuluka kaphatikizidwe wa erythropoietin, ndi maziko awa, ndipo inachuluka erythropoiesis.
19. GCS ndi hypoglycemic mankhwala - pafupifupi kuchepetsa mogwira awo.

Pomaliza

Mankhwala - mankhwala, amene popanda mankhwala amakono n'zokayikitsa ndalama. Iwo amagwiritsa ntchito mankhwala a magawo kwambiri za matenda, kapena kungoti kuti kumapangitsanso kanthu za mankhwala a. Komabe, monga mankhwala, glucocorticosteroids mavuto onse mbali ndi kukhala contraindications kwambiri. Musaiwale za izo. Tanena kutchulidwa milandu onse kumene si koyenera kugwiritsira ntchito mankhwala ndipo nawonso anapereka mndandanda wa ntchito mogwirizana kwa corticosteroids ndi mankhwala ena. limagwirira cha zochita za corticosteroids ndipo onse obwera awo akhala anafotokoza apa. Tsopano muyenera kudziwa za GCS, ali mu malo amodzi - nkhaniyi. Komabe, mu Mulimonsemo, musayambe mankhwala pokhapokha kuwerenga zambiri za GCS. Mankhwalawa, ndithudi, zikhoza kugulidwa popanda dongosolo, koma n'chifukwa chiyani muyenera izo? Musanagwiritse ntchito mankhwala aliyense kaye katswiri. Kukhala wathanzi ndi musalankhule medicate!