GCS - o lenei vailaau? Le faatinoga ma le aafiaga o fualaau faasaina glucocorticosteroids

E moni lava ua lava e faalogo o homone steroid. e maua i latou e le aunoa o tatou tino e faatonutonu faagasologa olaga. I lenei mataupu, o le a tatou mafaufau glucocorticoids - homone steroid, ua gaosia i le cortex adrenal. Ui o le toatele oi tatou e le fiafia i latou analogues gaosi - GCS. O le a le vailaau? Lea o loo faaaogaina i latou ma le ituaiga o le faaleagaina latou faia? Sei o tatou vaai i ai.

O faamatalaga lautele e uiga i GCS. O le a le vailaau?

synthesises homone steroid tatou tino e pei o glucocorticoids. ua maua i latou e le cortex adrenal, ma o latou faaaogaina ua faapitoa e faatatau i le togafitiga o le atoatoa adrenal. I nei aso, e faaaoga e le gata glucocorticoids faalenatura, ae faapea foi o latou analogues gaosi - GCS. O le a le vailaau? Mo tagata, le uiga o nei analogs tele, e pei ona maua i luga o le tino aneti-inflammatory, immunosuppressive, antishock, aafiaga aneti-allergic.

ua avea Glucocorticoids faaaogaina o fualaau oona (o lo o faasinomia i totonu o le mataupu - PM) i le 40-tifaga o XX senituri. I le faaiuga o le 30 tausaga o le seneturi lona luasefulu, saienitisi maua tuufaatasi hormone steroid i cortex adrenal tagata, ma i le 1937 na filifilia ai o ia mineralocorticoid deoxycorticosterone. I le amataga na maua e 40-tifaga glucocorticoid hydrocortisone ma cortisone. Pharmacological aafiaga o cortisone ma hydrocortisone sa matua eseese, o le na filifili e faaaoga i latou e pei o fualaau faasaina. Ina ua mavae sina taimi, ua tauaveina e saienitisi lo latou tuufaatasia.

O le glucocorticoid sili ona toaaga i le tino o le tagata o - cortisol (analogue - hydrocortisone, o lona tau - 100-150 rubles), ma ua manatu se tele. E mafai foi ona e faasoa toaaga: corticosterone, cortisone, 11-deoxycortisol, 11-dehydrocorticosterone.

O glucocorticoids faalenatura uma e pei ona faaaogaina o fualaau oona maua na hydrocortisone ma cortisone. Ae peitai, o le aafiaga e gata itu mafuaaga soo nai lo se isi hormone, o le mafuaaga i le taimi nei ua faatapulaaina lona faaaogaina i vailaau faafomai. Ina ia aso, na faaaogaina glucocorticoid hydrocortisone po o lona esters (hydrocortisone hemisuccinate ma acetate hydrocortisone).

E tusa glucocorticosteroids (glucocorticoids gaosi), ona i ai nei tatou synthesized se numera o sea sui, i totonu o lea le fluorinated (flumethasone, triamcinolone, betamethasone, dexamethasone, ma isi) Ma e lē fluorinated (methylprednisolone, prednisolone, prednisone) glucocorticoids.

O sui toaaga lo latou counterparts faalenatura, ma o loo manaomia mo le togafitiga o inumaga laiti.

O le faiga o le gaoioiga o corticosteroids

O le gaoioiga o glucocorticoids i le tulaga molecular e le o malamalama atoatoa. Saienitisi talitonu o galue nei fualaau faasaina i le sela i le tulaga o le faatonutonuina o tusitusiga Gene.

Corticosteroids fegalegaleai ma receptors glucocorticoid intracellular oi ai i le toetoe lava sela uma o le tino o le tagata. I le toesea o receptors hormone (lea e cytosolic polotini) ua na deactivated. I le tulaga le toaaga mai, oi latou o ni vaega o le heterocomplexes, lea e aofia ai foi immunophilin, polotini ma isi mea faapena teʻi vevela.

Ina ua ati steroids le sela (e ala i le membrane), latou noatia i receptors ma le faatoaagaina mai lavelave "glucocorticoid + receptor", ina ua mavae lea e ulu atu i le feaveai vaega faaogatotonu len¯ao ma interacts i le DNA itulagi lea ua tu i le Gene tutusa steroid momoimea e faalauiloaina (latou ua valaauina foi glucocorticoid 'o le tali elemene). Faigata "+ glucocorticoid receptor" e mafai ona ia faatonutonu (taofiofia po o, itu, faatoaaga) o le faagasologa o le tusitusiga o genes patino. O le mea lenei e tau atu i le taofiofia po o le faaosofia o mRNA, faapea foi ma se suiga i le tuufaatasia o le eseese enzymes ma polotini faatonutonu e soalaupule aafiaga feaveai.

Eseese suesuega faaalia ai le lavelave "glucocorticoid + receptor" O tali i vala eseese e tusitusiga, f.t.t., e pei o kappa vala faaniukilia B (NF-KB), po o le activator o porotini tusitusiga (AP-1) e faatonutonu genes aafia i le tali sao, ma pupuga (molecules adhesion, genes cytokine, protease ma isi.).

O aafiaga autu o GCS

glucocorticoids aafiaga i le tino o le tagata e toatele. O nei homone maua antitoxic, antishock, imunnodepressivnoe, antiallergic, gaoioiga antiinflammatory ma antiinflammatory. Sei o ave a latalata vaai i le auala o le faatinoga o corticosteroids.

• aafiaga Aneti-inflammatory o corticosteroids. Mafua ai le le taofiofia o le gaoioiga o phospholipase A _2. Ina inhibition o lenei enzyme i le ua taofia tino o le tagata liberatiou (faamatuu) le inhibition o acid arachidonic ma le faatuina o nisi o puluvaga inflammatory (e pei o prostaglandins, leukotrienes, ma troboksan t. D.). Gata i lea, faaitiitia le glucocorticosteroids taliaina exudation suāvai, vasoconstriction (faaitiitia) capillaries, faaleleia o microcirculation i le Fula.
• aafiaga Aneti-allergic o GCS. E tulai mai o se taunuuga o le tuuina i lalo secretion ma le tuufaatasia o le puluvaga o allergy, faaitiitia o lo o faasalalauina basophils, inhibition o histamine faamalologa mai basophils ma pou sela sensitized, faaitiitia le aofai o B ma lymphocytes T, le faaitiitia o lagona alofa o le sela i le puluvaga o allergy, suiga puipuia tali, faapea foi ma le taofiofia o le gaosiga antibody.
• gaoioiga Immunosuppressive o GCS. O le a le vailaau? O lona uiga e faapea o le fualaau faasaina taofiofia immunogenez, taofia le tuuina atu o ni polotini e tetee. Corticosteroids taofiofia malaga o ivi sela pogai su, taofiofia le gaoioiga o B ma lymphocytes T taofiofia le faamatuu atu o cytokines mai macrophages ma leukocytes.
• Aneti-oona ma le aafiaga antishock o corticosteroids. O le aafiaga o homone e mafua mai i le toto maualuga i tagata, faapea foi ma le faatoaagaina mai o enzymes ate aafia i le metabolism o xenon ma endobiotikov.
• gaoioiga Mineralocorticoid. Glucocorticosteroids maua le tomai e retard sodium ma le vai i le tino, faaosofia le excretion o potassium. O lenei sui gaosi e le lelei e pei homone faalenatura, ae o le aafiaga i le tino latou.

Pharmacokinetics

Mo le umi o le faatinoga o steroids faiga e mafai ona vaevaeina i:

1. Glucocorticosteroids gaoioiga puupuu (f.t.t., hydrocortisone, o le tau o lea e eseese lava mai le 100 i le 150 rubles).
2. Glucocorticosteroids i se umi e tusa o le faatinoga (prednisolone (manatu faaalia lea e le lelei), methylprednisolone).
3. Glucocorticosteroids ma gaoioiga faaumiumi (triamcinolone acetonide, dexamethasone, betamethasone).

Ae e le gata mo ona mafai ona fuafuaina le umi o glucocorticosteroids. Faavasegaina o i latou e mafai foi ona avea le faiga o le pulega:

• tuufofoga;
• intranasal;
• Inhaled glucocorticosteroids.

O lenei faavasegaina, peitai, e faatatau i na o glucocorticosteroids faiga.

E i ai nisi o fualaau faasaina i le tulaga o suauu ma creams (corticosteroids lotoifale). Mo se faataitaiga, "Afloderm". Toe iloiloga o sea formulations e lelei.

Sei o tatou vaavaai i le ituaiga o na corticosteroids faiga.

mitiia atoatoa steroids Tautala i le suʻia e aunoa ma mafua ai le faafitauli. Malosi noatia e polotini i le plasma (transcortin, albumin). O le faasalaga aupito maualuga o le corticosteroids tuufofoga i le toto ua oo ina ua uma 1.5 itula talu pulega. Latou faatinoina biotransformation i le ate, fatugao (vaega) ma isi aano o le tino e conjugation e glucuronide po sulfate.

E tusa ma le 70% o conjugated GCS excreted i le miaga, o le isi 20% i le feces le a faailoa mai mulimuli ane, ma le isi vaega - ma isi vai moni (f.t.t., mulimuli ane). O le afa - mai le 2 i le 4 itula.

E mafai ona e fausia ai se tamai laulau i le faataamilosaga pharmacokinetic o corticosteroids tuufofoga.

Glucocorticosteroids. Fualaau oona (igoa)	O le afa o le olaga o le pepa solo	Plasma olaga-afa
hydrocortisone	8-12 itula	0.5-1.5 itula
cortisone	8-12 itula	0.7-2 itula
Prednisolone (iloiloga e le lelei)	18-36 itula	2-4 itula
methylprednisolone	18-36 itula	2-4 itula
fludrocortisone	18-36 itula	3.5 itula
dexamethasone	36-54 itula	5:00

Inhaled steroids i faiga togafitiga po nei tuuina triamcinolone acetonide, propionate fluticasone, mometasone furoate, budesonide ma beclomethasone dipropionate.

Pharmacokinetic tapulaa e mafai foi ona tuuina atu i se laulau:

Glucocorticosteroids. Fualaau oona (igoa)	O le gaoioiga aneti-inflammatory le lotoifale	voluma o le tufatufaina	Plasma olaga-afa	Le lelei o mau e ala i le ate
beclomethasone dipropionate	0,64 iunite.	-	0.5 itula	70%
budesonide	1 iunite.	4.3 l / kg	1,7-3,4 itula	90%
triamcinolone acetonide	0,27 iunite.	1.2 l / kg	1.4-2 itula	80-90%
propionate fluticasone	1 iunite.	3.7 l / kg	3.1 itula	99%
flunisolide	0,34 iunite.	1.8 l / kg	1.6 itula	-

Nasal steroids i vailaau tuuina atu i aso nei propionate fluticasone, flunisolide, triamcinolone acetonide, mometasone furoate, budesonide ma beclomethasone dipropionate. O nisi oi latou ua taʻua o le ala lava lea e tasi e pei corticosteroids inhaled.

Ina ua mavae le talosaga a le inumaga corticosteroids intranasal taulai atu i le suʻia ai ma se isi vaega e sau mai le mucosa ala ea tuusao i le bloodstream.

Glucocorticosteroids, maileia i le tamaitusi digestive, ua mitiia mo uiga 1-8 pasene, ma le mavae atu muamua e ala i le ate biotransformed toetoe lava atoatoa e metabolites toaaga.

Glucocorticosteroids lea ua taunuu i totonu o le toto, hydrolyze i mea toaaga. O se laulau faatasi ai ma o latou faataamilosaga pharmacokinetic:

Glucocorticosteroids. sauniuniga	Bioavailability pe a ulufale atu i le toto, o se pasene	Bioavailability pe mitiia mai le tamaitusi gastrointestinal, i pasene
budesonide	34	11
beclomethasone dipropionate	44	20-25
mometasone furoate	<0,1	<1
triamcinolone acetonide	E leai se faamatalaga	10,6-23
propionate fluticasone	0.5-2
flunisolide	40-50	21

Fualaau faasaina e pei o le "Afloderm" (manatu faaalia lea tausia popping i luga o le upega), e faamatala eseese e leai se uiga. O i latou o le elemene autu toaga, e ono ua uma ona taua i luga. O nei fualaau faasaina - corticosteroids le lotoifale, ma o loo faatusalia mai i latou le tele o taimi i le tulaga o suauu po o creams.

Tuu togafitiga glucocorticosteroid (faailoga mo le faaaogaina)

Mo ituaiga taitasi o glucocorticosteroids lona faailoga mo le faaaogaina. O lea la, o loo faaaogaina corticosteroids tuufofoga e faia:

• faamai o le Crohn;
• colitis ulcerative;
• faaletonu māmā interstitial;
• syndrome puapuaga matuitui respiratory;
• nimonia ogaoga;
• faamaʻi faalavelave chronic faaumiumi i vaega matuitui;
• sela bronchial;
• thyroiditis subacute;
• hyperplasia adrenal congenital (i le tulaga lenei, e le maua ai se tagata corticoids o ia lava ma ua faamalosia i latou e lo latou analogues gaosi);
• le atoatoa matuitui adrenal.

Foi o loo faaaogaina steroids i togafitiga le toe suia o le toilalo napochechnikovoy muamua ma lona lua.

o loo faaaogaina corticosteroids Intranasal mo:

• rhinitis idiopathic (vasomotor);
• rhinitis lē allergic ma eosinophilia;
• isu pilipoze;
• rhinitis allergic faifaipea (faatauanau);
• rhinitis allergic vaitau (o le oloia).

o loo faaaogaina corticosteroids Inhaled e taulimaina faamaʻi faaumiumi faalavelave chronic, sela bronchial.

Contraindications

e tatau ona feutagaʻi Puipuiga GCS i nei tulaga togafitiga:

• lactation;
• glaucoma;
• O nisi faamai o le cornea, o loo tuufaatasi ma le abnormalities o le epithelium;
• fungal po o faamai viral o le mata;
• siama purulent;
• vaitaimi tui;
• syphilis;
• ituaiga malosi o le fatafata vaivai;
• siama herpes;
• pipisi fungal faiga;
• nisi o maʻi o le mafaufau ma le auga fua;
• tulaga ogaoga o le toilalo Fatugao;
• toto maualuga;
• thromboembolism;
• papala duodenal po o le manava;
• maʻi suka;
• faamaʻi o Cushing.

Matua contraindicated corticosteroids intranasal i tulaga faapena:

• nosebleeds soo i le talafaasolopito;
• diathesis hemorrhagic;
• hypersensitivity.

Glucocorticosteroids: aafiaga itu

aafiaga itu o corticosteroids e mafai ona vaevaeina i le lotoifale ma faiga.

aafiaga itu i le lotoifale

Vaevaeina i le aafiaga o le corticosteroids inhaled ma intranasal.

1. aafiaga matuia i le lotoifale mai glucocorticosteroids inhaled:

• tale;
• dysphonia;
• candidiasis o le ana tuufofoga ma pharynx.

2. aafiaga itu i le lotoifale o le corticosteroids intranasal:

• perforation o le septum nasal;
• nosebleeds;
• susunuina ma membranes mucous matutu o le isu ma pharynx;
• sneezing;
• isu itchy.

aafiaga itu faiga

Vaevaeina e tusa ai ma vaega o le tino, lea e faagaoioia.

1. Vaega o le neura autu:

• psychoses;
• le atuatuvale;
• euphoria;
• moe fiti;
• irritability.

2. Talu mai le faiga cardiovascular:

• thromboembolism;
• thrombosis loloto uaua;
• toto maualuga;
• myocardiodystrophy.

3. Mai le faiga fanautama:

• hirsutism;
• faatuai atinae tau faiga aiga;
• dysfunction feusuaiga;
• taamilosaga palapala masina femoumouai.

4. Mai le faiga digestive:

• ate puta;
• pancreatitis;
• tafetotoi mai le tamaitusi gastrointestinal;
• ulcers steroid o le manava ma le loto ona.

5. Mai le faiga endocrine:

• maʻi suka;
• syndrome a Cushing;
• obesity;
• atrophy o le cortex adrenal ona inhibition o ana galuega tauave.

6. Mai le itu o manatu:

• glaucoma;
• posterior cataracts subcapsular.

7. Mai le faiga musculoskeletal:

• faamaumau maso;
• myopathy;
• stunted tuputupu ae i fanau;
• necrosis avascular ma fractures ivi;
• osteoporosis.

8. Aua le paʻu:

• alopecia;
• striae;
• thinning o le paʻu.

9. aafiaga isi itu:

• ituaiga matuitui pipisi ma faaumiumi o faiga inflammatory;
• fula;
• sodium ma le vai faatumauina i le tino.

faiga o lapataiga tau puipuiga

I nisi tulaga, e tatau ona faaaogaina corticosteroids ma le faaeteete.

Mo se faataitaiga, gasegase ma cirrhosis, hypothyroidism, hypoalbuminemia, ma gasegase matua lava po o le matutua e mafai ona faaleleia le faatinoga o corticosteroids.

I le talosaga a corticosteroids i le taimi o maitaga e tatau ona amanaia le aafiaga faamoemoeina o le togafitiga mo le tina ma le tulaga lamatia o se aafiaga le lelei o le fualaau faasaina i luga o le fetus, e pei corticosteroids e mafai ona faaleagaina ai le atinae o fetal tuputupu ae ma e oo lava i faaletonu e pei o cleft gutu ma isi.

Afai e mafatia i le taimi o le faaaogaina o le onosai GCS siama (moa pox, misela, ma isi. D.), E mafai ona tupu manatu mamafa tele.

I le togafitiga o gasegase ma corticosteroids po o faamai inflammatory autoimmune (gugu rheumatoid, faamai bowel, erythematosus lupus faiga ma le e pei o. D.) Sightings mafai ona matauina tetee steroid.

Gasegase mauaina steroids tuufofoga mo se taimi umi, e tatau i taimi e toto faataulaitu fecal ma oo fibroezofagogastroduodenoskopiyu pei papala steroid taimi o le togafitiga i le mafai ona faalavelaveina corticosteroids.

I le 30-50% o gasegase tausia ma le corticosteroids mo se taimi umi, atiina ae osteoporosis. O se tulafono, e aafia ai le vae, lima, ivinoʻo, ribs, ivitū.

Fegalegaleaiga ma isi fualaau faasaina

(E le afaina faavasegaina iinei) uma glucocorticosteroids pe a fesootai ma isi fualaau faasaina tuuina atu se aafiaga patino, ma e le lelei i taimi uma lenei aafiaga mo o tatou tino. O mea nei e tatau ona e iloa i luma o le faaaogaina o corticosteroids faatasi ma isi fualaau faasaina:

1. GCS ma antacids - glucocorticosteroids mitiia faaitiitia.
2. GCS ma barbiturates, phenytoin, hexamidine, diphenhydramine, carbamazepine, rifampicin - Ua faateleina biotransformation glucocorticosteroids i le ate.
3. GCS ma isoniazid, erythromycin - glucocorticosteroids biotransformation i le ate faaitiitia.
4. SCS ma salicylates, phenylbutazone, barbiturates, digitoxin, penisilini, chloramphenicol - o nei fualaau oona uma ua faalauteleina aveesea.
5. GCS ma isoniazid - o se solia o le psyche tagata.
6. Corticosteroids ma reserpine - o le manu mai o le tulaga le fiafia ma.
7. GCS ma tricyclic antidepressants - faateleina uunaiga intraocular.
8. GCS ma agonists - ua faateleina le faatinoga o nei fualaau faasaina.
9. Corticosteroids ma theophylline - gaoioiga aneti-inflammatory o glucocorticoids faateleina, atiina ae aafiaga cardiotoxic.
10. SCS ma diuretics, amphotericin B, mineralocorticoid - e faateleina ai le lamatia o hypokalemia.
11. GCS ma anticoagulants leai foi, fibrinolytics, butadiene, ibuprofen, acid ethacrynic - E mafai ona sosoo ai ma le faafitauli hemorrhagic.
12. SCS ma indomethacin, salicylates - lenei tuufaatasiga e mafai ona mafua manuʻa ulcerative o le tamaitusi gastrointestinal.
13. Corticosteroids ma paracetamol - Ua faateleina le toxicity o le fualaau faasaina.
14. Corticosteroids ma azathioprine - e faateleina ai le lamatia o cataracts, myopathy.
15. GCS ma mercaptopurine - tuufaatasiga e mafai ona taitai atu ai i le faateleina o faasalaga o acid uric i le toto.
16. GCS ma hingamin - faateleina aafiaga manaomia o lenei fualaau faasaina (corneal opacity, myopathy, dermatitis).
17. GCS ma methandrostenolone - faʻamau aafiaga matuia o glucocorticoids.
18. Corticosteroids ma sauniuniga uʻamea, androgens - faateleina tuufaatasia o erythropoietin, ma e faasaga i lenei soifuaga, ma faateleina erythropoiesis.
19. GCS ma fualaau faasaina hypoglycemic - faaitiitia atoatoa toetoe lava o lo latou lelei.

iʻuga

Steroids - fualaau faasaina, e aunoa ma lea e ono vailaau i ona po nei e tau. o loo faaaogaina mo le togafitia o lava laasaga matautia o le faamai, po o le na o le faaleleia ai le faatinoga o se fualaau faasaina. Ae peitai, e pei o fualaau uma, glucocorticosteroids itu aafiaga ma maua foi contraindications. Aua nei galo e uiga i ai. Luga tatou lisiina tulaga uma pe afai e le tatau ona faaaogaina steroids ma ua e tuuina mai foi se lisi o fegalegaleaiga o corticosteroids ma isi fualaau faasaina. le faiga o le gaoioiga o corticosteroids ma o latou aafiaga uma ua faamatalaina foi auiliili iinei. O lenei uma e tatau ona e iloa e uiga i GCS, o loo i se nofoaga e tasi - o lenei tusiga. Ae peitai, i so o se tulaga, aua e te amata togafitiga ina ua maea le faitauina o le faamatalaga lautele e uiga GCS. O nei fualaau faasaina, o le mea moni, e mafai ona faatau e aunoa ma se talavai, ae aisea e te manaomia ai? Ao leʻi faaaogaina vailaau oona, e tatau ona muamua feutagai a faapitoa. Ia maloloina ma lē lava medicate!