GCS - cewa wannan magani? A mataki da effects da kwayoyi glucocorticosteroids

Lalle ne ku taba ji na steroid ji ba gani. Jikin mu kullum samar da su don tsara rayuwa tafiyar matakai. A cikin wannan labarin, za mu duba glucocorticoids - steroid hormones, wanda aka samar a cikin adrenal bawo. Duk da yake mafi yawan mu kasance sha'awar su roba analogues - GCS. Mene ne magani? Domin wanda suke amfani da abin da irin lalacewar da suka sa? Bari mu gani.

Janar bayani game da GCS. Mene ne magani?

Our kwayoyin synthesises steroid hormones kamar glucocorticoids. Suna samar da adrenal bawo, kuma su yi amfani da yafi alaka da magani daga adrenal insufficiency. A zamanin yau, ta amfani ba kawai na halitta glucocorticoids, amma kuma su roba analogues - GCS. Mene ne magani? Domin Adam, wadannan analogs nufi mai yawa, kamar yadda da a jiki anti-mai kumburi, immunosuppressive, antishock, anti-rashin lafiyan sakamako.

Glucocorticoids sun zama amfani da kwayoyi (ake magana a kai a cikin labarin - PM) a cikin 40-ies na XX karni. By karshen 30s na karni na ashirin, masana kimiyya sun samu steroid hormone mahadi a mutum adrenal bawo, da kuma a 1937 ya aka zaba mineralocorticoid deoxycorticosterone. A farkon 40-ies aka samu glucocorticoid hydrocortisone da cortisone. Pharmacological effects na cortisone da hydrocortisone kasance haka bambancin, cewa an yanke shawarar yin amfani da su a matsayin kwayoyi. Bayan wani lokaci, masana kimiyya sun za'ayi su kira.

A mafi yawan aiki glucocorticoid a cikin mutum kwayoyin ne - cortisol (analogue - hydrocortisone, wanda farashin - 100-150 rubles), kuma shi ne dauke da manyan. Shi ne kuma zai yiwu ware kasa aiki: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

Daga cikin dukkan halitta glucocorticoids matsayin miyagun ƙwayoyi amfani samu kawai hydrocortisone da cortisone. Duk da haka, da karshen haddasawa illa akai akai fiye da wani hormone, wanda shi ne dalilin da ya sa a yanzu da amfani a magani yana da iyaka. Don kwanan wata, kawai amfani glucocorticoid hydrocortisone ko ta esters (hydrocortisone hemisuccinate da hydrocortisone acetate).

Game da glucocorticosteroids (roba glucocorticoids), da sannu za mu hada a yawan irin jamiái, daga cikinsu da fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, da dai sauransu) Kuma ba fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

Irin wannan jamiái aiki fiye da su halitta takwarorinsu, kuma ana buƙatar domin lura da karami allurai.

Ginshikai na mataki na corticosteroids

A mataki na glucocorticoids a matakin kwayoyin da aka ba cikakken gane. Masana kimiyya yi imani da cewa wadannan kwayoyi aiki a kan Kwayoyin a matakin tsari na gene kwafi.

Corticosteroids hulɗa tare da kwayuka glucocorticoid rabe ne ba a kusan kowace cell na jikin mutum. A cikin rashi na hormone rabe (wanda suke cytosolic sunadaran) suna kawai deactivated. A m jihar, su wani bangare ne na heterocomplexes, da suka hada da ma immunophilin, zafi tura sunadarai da sauransu.

Lokacin da steroids shiga cikin sel (ta hanyar da membrane), an ɗaure su rabe da kuma kunna hadaddun "glucocorticoid + tsoka mai amsa sigina", bayan da ta shiga cikin cell tsakiya da kuma interacts tare da DNA yankuna da ake located a cikin kiran kasuwa gutsure steroid m gene (su ma kira glucocorticoid 'ya ce abubuwa). Complex "+ glucocorticoid tsoka mai amsa sigina" shi ne iya gwada (hana ko, conversely, kunna) da aiwatar da kwafi na wasu kwayoyin halittu. Wannan shi ne abin da take kaiwa zuwa danniya ko ruri daga mRNA, kazalika da canji a cikin kira na daban-daban enzymes da tsaiko sunadaran cewa lũra salula effects.

Daban-daban nazarin ya nuna cewa hadaddun "glucocorticoid + tsoka mai amsa sigina" An mayar da martani tare da daban-daban kwafi dalilai, msl, kamar nukiliya factor kappa B (NF-KB), ko activator na kwafi gina jiki (AP-1) cewa tsara kwayoyin halittu da hannu a cikin rigakafi martani, da kuma kumburi (mannewa kwayoyin, cytokine kwayoyin halitta, protease da sauransu.).

Babban sakamakon GCS

glucocorticoids effects a kan jikin mutum suna da yawa. Wadannan hormones da antitoxic, antishock, imunnodepressivnoe, antiallergic, antiinflammatory da antiinflammatory mataki. Bari mu dauki wani kusa look at yadda da ayyuka na corticosteroids.

• Anti-mai kumburi effects na corticosteroids. Sa da danniya na aiki na phospholipase A _2. Lokacin da hanawa da wannan enzyme a jikin mutum da aka suppressed liberatiou (saki) da hanawa na arachidonic acid da kuma samuwar wasu kumburi shiga tsakani (kamar prostaglandins, leukotrienes, kuma troboksan t. D.). Bugu da ƙari, cikin liyafar glucocorticosteroids rage m exudation, vasoconstriction (takaita) capillaries, kyautata na microcirculation a cikin kumburi.
• Anti-rashin lafiyan sakamako na GCS. Yana auku a sakamakon rage mugunya, kuma kira na shiga tsakani na alerji, rage zagawa da basophils, hanawa na histamine saki daga basophils da mast Kwayoyin sensitized, rage yawan B da kuma T lymphocytes, Munã rage ji na ƙwarai daga Kwayoyin ga shiga tsakani da na alerji, na rigakafi da martani canje-canje, kazalika da danniya da antibody samar.
• Immunosuppressive aiki na GCS. Mene ne magani? Wannan yana nufin cewa kwayoyi hana immunogenez, kashe samar da antibodies. Corticosteroids hana hijirarsa na bargo kara Kwayoyin, hana na ayyuka na B da kuma T lymphocytes hana a saki cytokines daga macrophages da leukocytes.
• Anti-mai guba da kuma antishock sakamako na corticosteroids. A sakamakon hormones lalacewa ta hanyar hawan jini a cikin mutane, kazalika da kunnawa da hanta enzymes da hannu a cikin metabolism na xenon da endobiotikov.
• Mineralocorticoid aiki. Glucocorticosteroids suna da ikon retard sodium da kuma ruwa a jiki, ta da tukar tumbi da potassium. Wannan roba musanya ba kamar yadda mai kyau a matsayin halitta ji ba gani, amma shi ne sakamako a kan jikin suke da shi.

Pharmacokinetics

Domin lokacin kiranka na mataki na tsari steroids za a iya raba:

1. Glucocorticosteroids short mataki (msl, hydrocortisone, farashin wanda dabam daga 100 zuwa 150 rubles).
2. Glucocorticosteroids da wani talakawan duration na mataki (prednisolone (feedback wanda ba kyau sosai), methylprednisolone).
3. Glucocorticosteroids tare da shafe tsawon mataki (triamcinolone acetonide, dexamethasone, betamethasone).

Amma ba kawai domin lokacin kiranka na glucocorticosteroids iya ƙaddara. Nau'in su iya zama da yanayin da gwamnati:

• baka.
• intranasal.
• Inhaled glucocorticosteroids.

Wannan rarrabuwa, duk da haka, shafi kawai ga tsarin glucocorticosteroids.

Akwai wasu kwayoyi a cikin nau'i na man shafawa da kuma creams (gida corticosteroids). Alal misali, "Afloderm". Sharhi kan irin formulations ne mai kyau.

Bari mu dubi iri na tsari corticosteroids kadai.

Na baka steroids daidai tunawa a cikin hanji ba tare da haddasa matsaloli. Rayayye kisa to sunadarai a cikin jini (transcortin, albumin). Matsakaicin taro na baka corticosteroids a cikin jini da aka kai bayan 1.5 sa'o'i bayan gwamnati. Sun sha biotransformation a cikin hanta, koda (partially) da kuma sauran tsokoki da Tasrifu zuwa glucuronide ko sulfate.

Aƙalla kashi 70% na conjugated GCS excreted a cikin fitsari, wani 20% a cikin tumbi zai nuna daga baya, da kuma sauran - tare da wasu nazarin halittu ruwaye (msl, daga baya). A rabin - daga 2 zuwa 4 hours.

Za ka iya ƙirƙirar wani kananan tebur da pharmacokinetic sigogi na baka corticosteroids.

Glucocorticosteroids. Kwayoyi (sunayen)	A rabin-rai na nama	Jini rabin-rai
hydrocortisone	8-12 hours	0.5-1.5 sa'o'i
cortisone	8-12 hours	0.7-2 hours
Prednisolone (reviews ba sosai da kyau)	18-36 hours	2-4 hours
methylprednisolone	18-36 hours	2-4 hours
fludrocortisone	18-36 hours	3.5 hours
dexamethasone	36-54 hours	5:00

Inhaled steroids a zamani na asibiti yi gabatar triamcinolone acetonide, fluticasone propionate, mometasone furoate, budesonide da beclomethasone dipropionate.

Pharmacokinetic sigogi kuma za a iya gabatar a cikin wani tebur:

Glucocorticosteroids. Kwayoyi (sunayen)	A gida anti-kumburi aiki	juz'i na rarraba	Jini rabin-rai	Yadda ya dace da nassi ta hanyar hanta
beclomethasone dipropionate	0,64 raka'a.	-	0.5 hours	70%
budesonide	1 naúrar.	4.3 l / kg	1,7-3,4 hour	90%
triamcinolone acetonide	0,27 raka'a.	1.2 l / kg	1.4-2 hours	80-90%
fluticasone propionate	1 naúrar.	3.7 l / kg	3.1 hours	99%
flunisolide	0,34 raka'a.	1.8 l / kg	1.6 hours	-

Hanci steroids a magani yau gabatar fluticasone propionate, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide da beclomethasone dipropionate. Wasu daga cikin su suna kira wannan hanya kamar yadda inhaled corticosteroids.

Bayan aikace-aikace na da kashi intranasal corticosteroids tunawa a cikin hanji da kuma wani sashi zo daga airway mucosa kai tsaye zuwa cikin jini.

Glucocorticosteroids, makale a cikin narkewa kamar fili, suna tunawa for game 1-8 kashi, da farko izinin tafiya a cikin hanta biotransformed kusan gaba daya zuwa m metabolites.

Glucocorticosteroids wanda sun samu cikin jini, hydrolyze to m abubuwa. A nan ne mai cin abinci tare da su pharmacokinetic sigogi:

Glucocorticosteroids. shirye-shirye	Bioavailability lokacin shigar da jini, a matsayin mai yawan	Bioavailability lokacin tunawa daga cikin gastrointestinal fili, a cikin kashi
budesonide	34	11
beclomethasone dipropionate	44	20-25
mometasone furoate	<0.1	<1
triamcinolone acetonide	babu Information	10,6-23
fluticasone propionate	0.5-2
flunisolide	40-50	21

Kwayoyi kamar "Afloderm" (feedback da rike popping up a kan net), to bayyana dabam ya sa hankalta. Kowane daga cikinsu shi ne babban aiki sashi, wanda shi ne wata ila don sun riga sun ambata a sama. Wadannan kwayoyi - gida corticosteroids, kuma suna wakilci mafi sau da yawa a cikin nau'i na man shafawa, ko creams.

Sanya glucocorticosteroid far (alamomi don amfani)

Domin kowane irin glucocorticosteroids anta don amfani. Saboda haka, baka corticosteroids suna amfani da su bi:

• Crohn ta cuta.
• ulcerative colitis.
• interstitial huhu cuta.
• m na numfashi wuya ciwo.
• mai tsanani da ciwon huhu.
• kullum obstructive na huhu cuta a cikin m lokaci.
• Bronchial fuka.
• subacute thyroiditis.
• nakasar adrenal hyperplasia (a wannan yanayin, mutum ba ya nuna corticoids kansa kuma aka tilasta ya dauki su roba analogues).
• m adrenal insufficiency.

Har ila yau, ana amfani da steroids a maye far na firamare da kuma sakandare napochechnikovoy gazawar.

Intranasal corticosteroids ana amfani da:

• idiopathic rhinitis (vasomotor).
• ba rashin lafiyan rhinitis da eosinophilia.
• pilipoze hanci.
• perennial rashin lafiyan rhinitis (m).
• yanayi rashin lafiyan rhinitis (intermittent).

Inhaled corticosteroids suna amfani da su bi kullum obstructive na huhu cuta, Bronchial asma.

contraindications

Kariya kamata mu bi GCS a wadannan asibiti yanayi:

• lactation.
• glaucoma.
• Wasu cututtuka na cornea, wanda ake hada da munanan na epithelium.
• fungal ko kwayar cututtuka na ido.
• surkin jini kamuwa da cuta.
• alurar riga kafi lokaci.
• syphilis.
• aiki nau'i na da tarin fuka.
• herpes kamuwa da cuta.
• tsari fungal cututtuka.
• wasu shafi tunanin mutum da rashin lafiya tare da m cututtuka.
• m mataki na koda gazawar.
• hauhawar jini.
• thromboembolism.
• duodenal miki ko ciki.
• ciwon sukari.
• Cushing ta cutar.

Tsananin contraindicated intranasal corticosteroids a irin haka:

• m nosebleeds a tarihi.
• hemorrhagic diathesis.
• hypersensitivity.

Glucocorticosteroids: illa

Side effects na corticosteroids za a iya raba gida da kuma tsari.

Local illa

Kasu kashi sakamakon inhaled da intranasal corticosteroids.

1. Local illa daga inhaled glucocorticosteroids:

• tari.
• dysphonia.
• candidiasis da na baka rami da kuma pharynx.

2. Local gefen sakamakon intranasal corticosteroids:

• perforation na hanci septum.
• nosebleeds.
• kona da bushe mucous membranes na hanci da kuma pharynx.
• sneezing.
• itchy hanci.

Tsari illa

Raba bisa ga sassa na jiki, wanda aiki.

1. Part na tsakiya m tsarin:

• psychoses.
• ciki;
• asar, sai murna.
• rashin barci.
• irritability.

2. Tun da zuciya da jijiyoyin jini tsarin:

• thromboembolism.
• zurfin jannayẽnsa thrombosis.
• hawan jini.
• myocardiodystrophy.

3. Daga cikin haihuwa tsarin:

• hirsutism.
• jinkirta jima'i ci gaba;
• jima'i tabarbarewa.
• m hailar sake zagayowar.

4. Daga cikin narkewa kamar tsarin:

• m hanta.
• pancreatitis.
• zub da jini daga gastrointestinal fili.
• steroid ulcers na ciki da kuma hanjinsu.

5. Daga cikin tsarin endocrine:

• ciwon sukari.
• Cushing ta ciwo.
• kiba.
• atrophy na adrenal bawo saboda hanawa na ta aikin.

6. Daga gefe na view:

• glaucoma.
• na baya subcapsular cataracts.

7. Daga cikin musculoskeletal tsarin:

• tsoka, halakarwa.
• myopathy.
• tsumburai girma a cikin yara;
• avascular necrosis da kashi samu karaya.
• osteoporosis.

8. Don fata:

• alopecia.
• striae.
• thinning na fata.

9. Sauran gefen effects:

• m dauke da kwayar cutar da kullum siffofin kumburi tafiyar matakai.
• ƙaruwa.
• sodium da kuma ruwa riƙewa a cikin jiki.

rigakafi

A wasu lokuta, corticosteroids ya kamata a yi amfani da hankali.

Alal misali, marasa lafiya da cirrhosis, hypothyroidism, hypoalbuminemia, da kuma na tsufa marasa lafiya ko tsofaffi za a iya inganta mataki na corticosteroids.

A cikin aikace-aikace na corticosteroids a lokacin daukar ciki ya kamata ya yi la'akari da da ana tsammanin sakamakon da jiyya ga uwar da hadarin wani mummunan sakamako daga cikin miyagun ƙwayoyi a kan tayin, kamar yadda corticosteroids iya rushe ci gaban fetal girma da kuma ko da lahani kamar kogon palate da sauransu.

Idan a lokacin da yin amfani da GCS haƙuri shan wahala kamuwa da cuta (kaza pox, kyanda da da sauransu. D.), Yana iya faruwa da gaske.

A lura da marasa lafiya da corticosteroids ko autoimmune kumburi cututtuka (rheumatoid amosanin gabbai, hanji cututtuka, na tsari lupus erythematosus da kuma kama. D.) Sightings steroid juriya za a iya lura.

Marasa lafiya samun baka steroids na dogon lokaci, shi wajibi ne lokaci-lokaci don daukar fecal occult jini da kuma wuce fibroezofagogastroduodenoskopiyu kamar yadda steroid miki a lokacin jiyya da corticosteroids iya ba za a gaji da damuwa.

A 30-50% da marasa lafiya bi da tare da corticosteroids na dogon lokaci, ci gaba osteoporosis. Kamar yadda mai mulkin, shi rinjayar da kafa, hannu, kafafuwa, hakarkarinsa, kashin baya.

Hulda da sauran kwayoyi

All glucocorticosteroids (rarrabuwa ba kome a nan) a lokacin da a lambar sadarwa tare da sauran kwayoyi ba wani sakamako, kuma wannan sakamako ne ba ko da yaushe tabbatacce ga jikin mu. Ga abin da kuke bukatar sani kafin da ake ji corticosteroids a tare da sauran kwayoyi:

1. GCS da antacids - glucocorticosteroids sha rage-rage.
2. GCS da barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - glucocorticosteroids biotransformation a cikin hanta da aka ƙara.
3. GCS da isoniazid, erythromycin - glucocorticosteroids biotransformation a cikin hanta rage-rage.
4. SCS da salicylates, phenylbutazone, barbiturates, digitoxin, penicillin, chloramphenicol - duk wadannan kwayoyi an inganta kawar.
5. GCS da isoniazid - wani take hakkin dan Adam psyche.
6. Corticosteroids da reserpine - fitowan depressive jihar.
7. GCS da tricyclic antidepressants - ƙara intraocular matsa lamba.
8. GCS da agonists - mataki na wadannan kwayoyi na karuwa ne.
9. Corticosteroids da theophylline - anti-mai kumburi mataki na glucocorticoids ƙaruwa, ci gaba cardiotoxic effects.
10. SCS da diuretics, amphotericin B, mineralocorticoid - na kara hadarin hypokalemia.
11. GCS da kuma kai tsaye ba anticoagulants, fibrinolytics, butadiene, ibuprofen, ethacrynic acid - iya bi ta hemorrhagic rikitarwa.
12. SCS da indomethacin, salicylates - wannan hade zai iya sa ulcerative raunuka na gastrointestinal fili.
13. Corticosteroids da paracetamol - da yawan guba daga cikin miyagun ƙwayoyi ne ta ƙara.
14. Corticosteroids da azathioprine - na kara hadarin cataracts, myopathy.
15. GCS da mercaptopurine - hade iya kai wa ga ta ƙara maida hankali uric acid a cikin jini.
16. GCS da hingamin - Littafi maras so sakamakon wannan magani (corneal shirin hana haske, myopathy, dermatitis).
17. GCS da methandrostenolone - fadada illa na glucocorticoids.
18. Corticosteroids, da baƙin ƙarfe shirye-shirye, androgens - ƙara kira na erythropoietin, kuma da wannan bango, kuma Ya ƙãra erythropoiesis.
19. GCS da hypoglycemic kwayoyi - kusan cikakkiyar akan rage su tasiri.

ƙarshe

Steroids - kwayoyi, tare da abin da zamani magani ne mai wuya ga kudin. Suna amfani domin lura da sosai tsanani, saukarwa da cutar, ko kuma kawai don bunkasa mataki na mai magani. Duk da haka, kamar yadda da dukan magunguna, glucocorticosteroids illa kuma da contraindications ma. Kada ka manta game da shi. Sama da muka lissafa duk lokuta inda ba lallai ba ne su yi amfani da steroids kuma sun ma bayar da jerin da hulda da corticosteroids tare da wasu kwayoyi. ginshikai na mataki na corticosteroids da kuma duk abin da suka effects sun kuma an aka bayyana a cikin daki-daki, a nan. Yanzu duk kana bukatar ka sani game da GCS, an a wuri guda - wannan labarin. Duk da haka, a cikin wani hali, kada a fara jiyya kawai bayan karanta janar bayani game da GCS. Wadannan kwayoyi, ba shakka, za a iya saya ba tare da takardar sayen magani, amma me ya sa ba ka bukatar shi? Kafin yin amfani da wani kwayoyi kamata farko tuntubar wani gwani. Zama lafiya da kuma ba kai-medicate!