GCS - kuti mushonga uyu? The chiito uye Migumisiro zvinodhaka glucocorticosteroids

Zvirokwazvo iwe waita akambonzwa steroid mahormone. muviri wedu nguva dzose pave navo waidzora pezvakaitwa upenyu. Munyaya ino, tichakurukura glucocorticoids - steroid mahormone, izvo anogadzirwa adrenal cortex. Apo vazhinji vedu tiri kufarira kwavo chakaita zvokugadzirwa analogues - GCS. Chii mushonga? Nokuti izvo zvavari kushandiswa uye rudzii kukuvara vanovakonzera? Ngationei.

General ruzivo pamusoro GCS. Chii mushonga?

muviri wedu synthesises steroid mahormone zvakadai glucocorticoids. Vari neve adrenal cortex, uye kushandiswa kwawo dzinowanzotsigi- chokuita mishonga adrenal insufficiency. Mazuvano, achishandisa kwete zvoga glucocorticoids, asiwo chakaita zvokugadzirwa analogues dzavo - GCS. Chii mushonga? Nokuti vanhu, analogs izvi zvinoreva zvakawanda, sezvo tine pamusoro muviri Anti-anogumbura, immunosuppressive, antishock, Anti-sema mugumisiro.

Glucocorticoids vajaira sezvo zvinodhaka (anotaurwa munyaya - PM) muna 40-ies pamusoro XX remakore. By pakuguma 30s remakore rechimakumi maviri, masayendisiti akawana steroid kemikari yeimwe nevanhu adrenal cortex, uye muna 1937 akasarudzwa mineralocorticoid deoxycorticosterone. Mukutanga 40-ies vakanga mumichero glucocorticoid hydrocortisone uye cortisone. Pharmacological migumisiro cortisone uye hydrocortisone vakanga siyana, kuti kwakasarudzwa kuzvishandisa sezvo zvinodhaka. Kwapera nguva, masayendisiti vakaita kwetunhu yavo.

Zvikuru kushingaira glucocorticoid ari munhu muviri ndiwo - cortisol (analogue - hydrocortisone, ane mutengo - 100-150 rubles), uye sechinhu chikuru. Zvinogonekawo kuti govera sekwaserera: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

Zvose zvakasikwa glucocorticoids zvinodhaka akawana chete hydrocortisone uye cortisone. Zvisinei, yokupedzisira zvinokonzera nemishonga kakawanda kupfuura chero rimwe kemikari, ndokusaka panguva ino kushandiswa kwayo mukurapa ishoma. To musi, chete akashandisa glucocorticoid hydrocortisone kana esters ayo (hydrocortisone hemisuccinate uye hydrocortisone acetate).

Achitaura glucocorticosteroids (chakaita zvokugadzirwa glucocorticoids), parizvino isu synthesized inoverengeka vamiririri zvakadaro, ramakagadzwa fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, etc.) Uye non-fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

nevasori kwakadaro achishingaira kupfuura zvavo dzinongoitika dzomuzana, uye zvinodiwa kuti mishonga mishonga zviduku.

The mashandiro chiito pamusoro corticosteroids

Zvakaitwa glucocorticoids panguva samolecular pamwero haisi aizvinzwisisa. Masayendisiti anodavira kuti zvinodhaka izvi kuita masero pachiyero mutemo Gene transcription.

Corticosteroids anosangana intracellular glucocorticoid receptors varipo anenge muchitokisi dzose dzemuviri. Pasina kemikari receptors (izvo cytosolic mapuroteni) vari nyore deactivated. Munguva akaneta mamiriro, ndivo chikamu heterocomplexes, izvo zvinosanganisira uyewo immunophilin, kupisa kuvhunduka mapuroteni nezvakadaro.

Apo steroids zvinopfuura masero (kuburikidza Kamudzira), vanosunga kune receptors uye Activate kunzwisisa "glucocorticoid + Kanotokonya", pashure pacho anopinda muchitokisi musimboti uye interacts pamwe DNA kunzvimbo idzo dziri muna nditsigire chinyorwa steroid runoenzanirana Gene (vari anonziwo glucocorticoid 'akapindura zvinhu). Complex "+ glucocorticoid Kanotokonya" anogona waidzora (tunodzivisa kana, Ukuwo, Activate) chirongwa transcription vamwe majini. Izvi ndizvo zvinotungamirira kudzvinyirira kana kweiyi mRNA, uyewo kuchinja mune kwetunhu makemikari siyana uye pamutemo mapuroteni kuti svitsanisa cellular migumisiro.

zvidzidzo Various anoratidza kuti kunzwisisa "glucocorticoid + Kanotokonya" interacts nedzimwe transcription zvinhu, somuenzaniso, akadai renyukireya chinhu kappa B (NF-kB) uye activator mapuroteni transcription (AP-1) kuti waidzora majini muzvirongwa masoja norudaviro uye kuzvimba (adhesion mamorekuru, cytokine majini, runovharidzira mamwe uye zvichingodaro.).

The chikuru Migumisiro GCS

glucocorticoids migumisiro iri muviri womunhu vakawanda. mahormone ava antitoxic, antishock, imunnodepressivnoe, antiallergic, antiinflammatory uye antiinflammatory chiito. Ngatitorei vanyatsoona kuti zviito corticosteroids.

• Anti-anogumbura anokonzerwa corticosteroids. Akakonzera kudzvinyirira webasa phospholipase A _2. Kana chinovhiringidza kuti enzayemu iri muviri womunhu woutsinye liberatiou (kusunungurwa) ari chinovhiringidza pakati arachidonic asidhi uye paumbwe dzimwe anogumbura nevamiririri (zvakadai prostaglandins, leukotrienes, uye troboksan t. D.). Uyezve, mabiko glucocorticosteroids kunoderedza Urume exudation, vasoconstriction (aienda) capillaries, kuvandudzika kuti microcirculation napakatsva.
• Anti-sema mugumisiro GCS. It kunoitika pamusana richikwidibira secretion uye kwetunhu nevamiririri venyika chisimbwa, kuderedza achiparadzira basophils, chinovhiringidza kuti histamine yokusunungurwa kubva basophils uye rechikepe masero sensitized, kuderedza B uye T lymphocytes, kuderedza aikanganiswa masero kuti nevamiririri venyika chisimbwa, masoja mhinduro kuchinja, uyewo kudzvinyirira kuti antibody kugadzirwa.
• Immunosuppressive basa GCS. Chii mushonga? Izvi zvinoreva kuti mishonga tunodzivisa immunogenez, vamise kugadzirwa antibodies. Corticosteroids tunodzivisa yokutama mwongo hunde masero, tunodzivisa basa B uye T lymphocytes tunodzivisa kusunungurwa cytokines kubva macrophages uye leukocytes.
• Anti-chepfu uye antishock mugumisiro corticosteroids. Maratidzirwo mahormone kukonzerwa cheBP muvanhu, uyewo activation kuti chiropa makemikari munyaya muviri kuti xenon uye endobiotikov.
• Mineralocorticoid basa. Glucocorticosteroids anokwanisa kutadzisa yavaibvisa uye mvura mumuviri, tunhu excretion kuti potassium. Izvi Sevamiririri chakaita zvokugadzirwa havasi tangofanana dzinongoitika mahormone, asi sei muviri zvavanazvo.

Pharmacokinetics

Nokuti ya zviito systemic steroids unogona kukamurwa:

1. Glucocorticosteroids pfupi chiito (semuenzaniso, hydrocortisone, mitengo yakanga zvichisiyana 100 kusvika 150 rubles).
2. Glucocorticosteroids neavhareji nguva chiito (prednisolone (inofambiswa zvisina kunaka kwazvo), methylprednisolone).
3. Glucocorticosteroids pamwe kwenguva refu chiito (triamcinolone acetonide, dexamethasone, betamethasone).

Asi kwete chete kwenguva ya glucocorticosteroids anogona tsunga. Kupatsanura vavo kuva chimiro chourongwa:

• zvokuudzwa;
• intranasal;
• Inhaled glucocorticosteroids.

Zvisinei, kupatsanura ichi, rinongoshandisirwa hurongwa glucocorticosteroids.

Pane zvimwe zvinodhaka ari muchimiro kwamafuta uye mumakenduru (local corticosteroids). Somuenzaniso, "Afloderm". Reviews pamusoro Formulations akadaro akanaka.

Ngatitarisei mhando systemic corticosteroids oga.

Oral steroids zvakakwana kunakidzwa ura pasina kukonzera zvinetso. Nokushingaira kusungira kuti mapuroteni ari plasma (transcortin, sealbumin). The kunonyanyisa wevasungwa nomumukanwa corticosteroids muropa zvasvika pashure maawa 1.5 pashure kutarisira. Ivo vanosangana biotransformation ari chiropa, itsvo (zvishomanana) uye dzimwe nzvimbo dzomuviri kubudikidza conjugation kuti glucuronide kana sulfate.

Inenge 70% kubva conjugated GCS yabudiswa muna weti, mumwe 20% muna mutsvina yadzo vachava anoratidza gare gare, uye vakasara - dzimwe utachiona zvinwiwa (semuenzaniso, gare gare). The hafu - kubva 2 kusvika 4 maawa.

Unogona kuumba diki tafura pamwe pharmacokinetic parameters nomumukanwa corticosteroids.

Glucocorticosteroids. Zvinodhaka (mazita)	The hafu-upenyu tishu	Plasma hafu-upenyu
hydrocortisone	maawa 8-12	maawa 0.5-1.5
cortisone	maawa 8-12	maawa 0.7-2
Prednisolone (Wongororo hazvisi zvakanaka chaizvo)	maawa 18-36	maawa 2-4
methylprednisolone	maawa 18-36	maawa 2-4
fludrocortisone	maawa 18-36	maawa 3.5
dexamethasone	maawa 36-54	5:00

Inhaled steroids vemazuva kunotoda tsika akapa triamcinolone acetonide, fluticasone propionate, mometasone furoate, budesonide uye beclomethasone dipropionate.

Pharmacokinetic parameters kunogonawo anounzwa mune tafura:

Glucocorticosteroids. Zvinodhaka (mazita)	The omunharaunda Anti-anogumbura basa	Vhoriyamu kuparadzirwa	Plasma hafu-upenyu	Kunyatsoshanda ndima kubudikidza chiropa
beclomethasone dipropionate	0,64 dzakabatana.	-	maawa 0.5	70%
budesonide	1 chikwata.	4.3 l / makirogiramu	1,7-3,4 awa	90%
triamcinolone acetonide	0.27 dzakabatana.	1.2 l / makirogiramu	maawa 1.4-2	80-90%
fluticasone propionate	1 chikwata.	3.7 l / makirogiramu	maawa 3.1	99%
flunisolide	0.34 dzakabatana.	1.8 l / makirogiramu	maawa 1.6	-

Nasal steroids mukurapa nhasi akapa fluticasone propionate, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide uye beclomethasone dipropionate. Vamwe vavo vanonzi zvakafanana sezvo inhaled corticosteroids.

Pashure pokushandisa dose intranasal corticosteroids kunakidzwa ura uye mumwe mugove rinobva yemweya mucosa zvakananga kupinda muropa.

Glucocorticosteroids, parumananzombe zvomudumbu turakiti, vari zvakawanda nokuti inenge 1-8 muzana, uye wokutanga Pfuurai chiropa biotransformed zvinenge zvakakwana kuti vakaneta metabolites.

Glucocorticosteroids izvo vakapinda ropa, hydrolyze kune vakaneta zvinhu. Heino imwe tafura yavo pharmacokinetic parameters:

Glucocorticosteroids. gadziriro	Bioavailability kana vachipinda ropa, sezvo chikamu	Bioavailability kana wefodya kubva nemudumbu, mu muzana
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

Zvinodhaka akadai "Afloderm" (inofambiswa izvo zvinoramba popping ari mambure), kurondedzera aparadzane haatombotauri musoro. Mumwe nomumwe wavo ari mukuru vanoshingaira chirungiso, izvo kazhinji kare ataurwa pamusoro. zvinodhaka izvi - omunzvimbo corticosteroids, uye vari kumiririrwa kazhinji muchimiro kwamafuta kana mumakenduru.

Isa glucocorticosteroid kurapa (zvairatidza kuti kushandiswa)

Nokuti mumwe mhando glucocorticosteroids zvairatidza ayo kushandiswa. Saka, nemumuromo corticosteroids inoshandiswa kurapa:

• Crohn nehosha;
• maronda colitis;
• interstitial bapu zvirwere;
• chenjera kufema nenhamo chirwere;
• zvakakomba nemabayo;
• chisingaperi obstructive pulmonary zvirwere rikwanise chokutambudzika;
• Árbol asima;
• subacute thyroiditis;
• vachiberekwa adrenal hyperplasia isiri yekenza (iyi, munhu haaiti corticoids pachake uye anomanikidzwa kutora chakaita zvokugadzirwa analogues dzavo);
• chenjera adrenal insufficiency.

Uyewo steroids zvinoshandiswa yokutsiva kurapa pamusoro nesekondari napochechnikovoy kukundikana.

Intranasal corticosteroids inoshandiswa:

• idiopathic rhinitis (vasomotor);
• non-sema rhinitis pamwe eosinophilia;
• pilipoze mhino;
• perennial sema rhinitis (asingakurumidzi);
• pamwaka sema rhinitis (inoratidza).

Inhaled corticosteroids anoshandiswa kurapa chirwere obstructive pulmonary chirwere, Árbol asima.

Contraindications

Zvokungwarira vanofanira kubata GCS mu kurapwa ezvinhu aya:

• lactation;
• yemaziso;
• Zvimwe zvirwere cornea, ayo zvikabatanidzwa abnormalities of epithelium;
• fungal kana nemavhairasi nezvirwere ziso;
• purulent chirwere;
• kubaya kumwedzi;
• njovhera;
• vanoshingaira chimiro tibhii;
• herpes chirwere;
• systemic fungal noutachiona;
• vamwe pfungwa kurwara ne zvibereko zviratidzo;
• zvakakomba mwero renal kukundikana;
• neBP;
• thromboembolism;
• duodenal urikanwi kana dumbu;
• chirwere cheshuga;
• chirwere Cushing vake.

Kunyatsoteerera contraindicated intranasal corticosteroids Muzviitiko zvakadaro:

• kakawanda nosebleeds munhoroondo;
• Hemorrhagic diathesis;
• hypersensitivity.

Glucocorticosteroids: nemishonga

Side Migumisiro corticosteroids zvinogona rakakamurwa omunharaunda uye systemic.

Local nemishonga

Akakamurwa migumisiro inhaled uye intranasal corticosteroids.

1. Local nemigumisiro kubva inhaled glucocorticosteroids:

• kukosora;
• dysphonia;
• candidiasis of nomumukanwa mhango uye pharynx.

2. Local divi Migumisiro intranasal corticosteroids:

• perforation of nasal septum;
• nosebleeds;
• unopfuta uye chakaoma mucous membranes mhino uye pharynx;
• sneezing;
• itchy mhino.

Systemic nemishonga

Yakakamurwa maererano nhengo dzomuviri, iyo ishande.

1. Chikamu musimboti tsinga:

• psychoses;
• kuora mwoyo;
• euphoria;
• kushaya hope;
• kugumbuka.

2. Sezvo kumwoyo:

• thromboembolism;
• yakadzika tsinga thrombosis;
• cheBP;
• myocardiodystrophy.

3. Kubva dzokubereka nadzo:

• hirsutism;
• kunonoka kurara budiriro;
• pabonde dysfunction;
• kusagadzikana kumwedzi.

4. Kubva zvomudumbu hurongwa:

• nuna chiropa;
• pfungwa nomuviri zvemwana asati;
• ropa kubva nemudumbu;
• steroid nemaronda mudumbu uye ura.

5. Kubva kwemakemikari anobudiswa hurongwa:

• chirwere cheshuga;
• Cushing kuti urwere;
• kufutisa;
• atrophy of adrenal cortex nokuda chinovhiringidza vayo basa.

6. Kubva kurutivi maonero:

• yemaziso;
• posterior subcapsular tsanga.

7. Kubvira zvetsandanyama nemapfupa hurongwa:

• tsandanyama kuparadza;
• myopathy;
• kukakanganiswa kukura mune vana;
• avascular necrosis uye mapfupa mitswe;
• osteoporosis.

8. Nokuti ganda:

• alopecia;
• striae;
• rive dete ganda.

9. Other nemishonga:

• chenjera chirwere uye chisingaperi siyana anogumbura pezvakaitwa;
• bundu;
• yavaibvisa uye mvura chengetedzo mumuviri.

matanho okudzivirira

Mune zvimwe zviitiko, corticosteroids anofanira kushandiswa nokungwaririra.

Somuenzaniso, varwere cirrhosis, hypothyroidism, hypoalbuminemia, uye varwere penga nokuda kokuchembera kana vakura huchawedzerwa kuitwa corticosteroids.

In kushanda corticosteroids panguva yepamuviri vanofanira kufunga kuti zvinotarisirwa mugumisiro marapirwo kuti amai uye mukana inokanganisa zvinodhaka riri mudumbu, sezvo corticosteroids anogona kuvhiringidza kukura fetus kukura uye kunyange kuremara zvakadai mumukaha mukanwa uye zvichingodaro.

Kana panguva kushandisa GCS murwere anotambura chirwere (huku pox, gwirikwiti, uye zvichingodaro. D.), Zvimwe kuitika zvikuru.

Mukurapa varwere corticosteroids kana autoimmune anogumbura zvirwere (dzinonzi rheumatoid arthritis, zvirwere bowel, chinonzi systemic lupus erythematosus uye zvakafanana. D.) Sightings steroid nemishonga inogona kuchengetwa.

Varwere kugamuchira zvokuudzwa steroids kwenguva refu, zvakakodzera nenguva kutora fecal zvemashiripiti ropa uye zvakaitika fibroezofagogastroduodenoskopiyu sezvo steroid urikanwi panguva kurapwa pamwe corticosteroids arege kuvhiringidzwa.

Muna 30-50% wevarwere kubatwa corticosteroids kwenguva refu, kutanga osteoporosis. Kazhinji, zvinokanganisawo rutsoka, ruoko, chiuno, mbabvu, nomuzongoza.

Kudyidzana nevamwe zvinodhaka

glucocorticosteroids All (kupatsanura hazvina basa pano) apo uchikurukura nevamwe zvinodhaka kupa mumwe mugumisiro, uye izvi hazvisi zvakanaka kuti muviri yedu nguva dzose. Hezvi zvaunofanira kuziva vasati kushandisa corticosteroids pachiimbwa zvimwe zvinodhaka:

1. GCS uye antacids - glucocorticosteroids Absorção de Água kunoderedza.
2. GCS uye barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - glucocorticosteroids biotransformation ari chiropa inowedzerwa.
3. GCS uye isoniazid, erythromycin - glucocorticosteroids biotransformation ari chiropa kunoderedza.
4. VVZR uye salicylates, phenylbutazone, barbiturates, digitoxin, kuti penicillin, chloramphenicol - zvose zvinodhaka izvi kunosimudzirwa kubviswa.
5. GCS uye isoniazid - kutyora dzevanhu psyche.
6. Corticosteroids uye reserpine - the kwaita mwoyo mamiriro.
7. GCS uye tricyclic antidepressants - kwakawedzera intraocular kumanikidzwa.
8. GCS uye agonists - kuitwa mishonga iyi iri kuramba ichiwedzera.
9. Corticosteroids uye theophylline - Anti-anogumbura kuitwa glucocorticoids kunowedzera, kutanga cardiotoxic migumisiro.
10. VVZR uye diuretics, amphotericin B, mineralocorticoid - kunowedzera mukana hypokalemia.
11. GCS uye zvisina kunanga anticoagulants, fibrinolytics, butadiene, ibuprofen, ethacrynic asidhi - zvingateverwa nezvikuru Hemorrhagic matambudziko.
12. VVZR uye indomethacin, salicylates - mubatanidzwa uyu anogona kukonzera maronda maronda ari nemudumbu.
13. Corticosteroids uye paracetamol - the toxicity zvinodhaka inowedzerwa.
14. Corticosteroids uye azathioprine - kunowedzera mikana tsanga, myopathy.
15. GCS uye mercaptopurine - mubatanidzwa kungaita kuti vawedzere Kuwanda uric asidhi muropa.
16. GCS uye hingamin - yakakura pasingadiwi kunoita zvinodhaka ichi (corneal opacity, myopathy, dermatitis).
17. GCS uye methandrostenolone - kuatsanangura nemigumisiro ine glucocorticoids.
18. Corticosteroids uye gadziriro simbi, androgens - zvakawedzera kwetunhu erythropoietin, uye pamusoro ichi necheseri, uye kwakawedzera erythropoiesis.
19. GCS uye hypoglycemic zvinodhaka - kutopedza rutapudzo kubudirira kwavo.

mhedziso

Steroids - zvinodhaka, pasina iro mushonga ano angangotadza marii. Ivo inoshandiswa pakurapa kwazvo nzendo chirwere, kana kungoti yokuwedzera zvinoitwa zvinodhaka. Zvisinei, sezvo vose mishonga, glucocorticosteroids nemishonga uye contraindications zvakare. Usakanganwa nezvazvo. Above isu zvawanyora ose zviitiko apo hazvina zvakakodzera kushandisa steroids uye akapawo mazita nesungano pakati corticosteroids nevamwe zvinodhaka. kuti mashandiro chiito pamusoro corticosteroids uye zvose zvavo migumisiro yave anorondedzerwa zvizere pano. Zvino imi mose kuziva pamusoro GCS, iri panzvimbo imwe - nyaya ino. Zvisinei, chero zvazvingava, musatanga kurapwa chete pashure pokuverenga Vhuṱanzi pamusoro GCS. zvinodhaka izvi, Chokwadi, zvinogona kutengwa pasina mushonga, asi nei munoda here? Usati kushandisa chero zvinodhaka vanofanira kutanga kubvunza nyanzvi. Utano kwete kuzvidzora medicate!