Kamano lipakeng tsa sebopeho sa lik'hemik'hale le pharmacodynamics

Mochine oa ts'ebetso oa GCS o amahanngoa le bokhoni ba bona ba ho sebelisana le li-receptor tse ling ho cytoplasm ea sele: steroid - receptor tata e kenella ka har'a sele ea sele, e tlama ho DNA, e amang phetisetso ea liphatsa tsa lefutso tse ngata, e lebisang phetohong ea motsoako oa liprotheine, li-enzymes, acid acid. GCS e ama mefuta eohle ea metabolism, e na le anti-inflammatory, anti-allergic, anti-shock le immunosuppression.

Mochine oa phello e khahlanong le ho ruruha ea corticosteroids ke ho hatella methati eohle ea ho ruruha. Ka ho tsitsisa li-membrane tsa sebopeho sa cellular le subcellular, incl. lysis, lithibela-mafu tse thibelang ho ruruha tsa cellidal li thibela ho lokolloa ha li-enzyme tsa protheine ho tsoa seleng, li thibela ho thehoa ha li-radicals tsa oksijene tsa mahala le lipid peroxides kahara litho. Boemong ba ho ruruha, li-corticosteroids li qobella likepe tse nyane le ho fokotsa ts'ebetso ea hyaluronidase, ka tsela eo e thibela sethala sa ho ruruha, thibela ho hokahana ha li-neutrophils le monocytes ho vasotine endothelium, ho fokotsa ho kenella ha tsona liseleng, le ho fokotsa mosebetsi oa macrophages le fiberroblasts.

Ts'ebetsong ea matla a khahlanong le ts'oaetso, karolo ea bohlokoa e bapaloa ke bokhoni ba GCS ba ho thibela ho kopanngoa le ho lokolloa ha babuelli ba tšoaetso (PG, histamine, serotonin, bradykinin, jj.). Ba susumetsa motsoako oa lipocortin, inhibitors ea phospholipase A2 biosynthesis, mme ba fokotsa sebopeho sa COX-2 molemong oa ts'oaetso. Sena se lebisa tokollong e lekanyelitsoeng ea arachidonic acid e tsoang phospholipids ea membrane ea lisele le ho fokotseha ha sebopeho sa metabolites ea eona (PG, leukotrienes le elemente activation factor).

GCS e ka thibela karolo ea kholo, hobane ba fokotsa ho kenella ha monocytes ka har'a lithane tse omisitsoeng, ho thibela ho nka karolo ha bona mohatong ona oa ho ruruha, ho thibela ho hlophisoa ha li-mucopolysaccharides, liprotheine le ho thibela ts'ebetso ea li-lymphopoiesis. Ka ho ruruha ha lefu la tšoaetso ea corticosteroids, ho fanoa ka boteng ba phello ea immunosuppressive, ho bohlokoa ho kopanya le kalafo ea antimicrobial.

Tšusumetso ea immunosuppression ea corticosteroids e bakiloe ke ho fokotseha hoa palo le ts'ebetso ea T-lymphocyte e potolohang maling, ho fokotseha ha tlhahiso ea li-immunoglobulin le tšusumetso ea lisele tsa T-assist ho B-lymphocyte, ho fokotseha ha dikahare tse tlatselletsang maling, ho thehoa ha li-immune system tse thata le ho kenella ha lintho tse ngata tse potang. .

Tšusumetso ea khale ea corticosteroids e bakoa ke ho fokotseha ha palo ea li-basophil tse potolohang, tlolo ea ts'ebelisano ea li-receptor tsa Fc tse holim 'a lisele tsa methapo e nang le sebaka sa Fc sa IgE le karolo ea C3 e tlatselletsang, e thibelang lets'oa ho kena seleng mme e tsamaisana le ho fokotseha ha tokollo ea histamine, heparin, le seroton. le babuelli ba bang ba mofuta oa hang-hang 'me ba thibela phello ea bona liseleng tsa moferefere.

Phello ea bohanyetsi e bakoa ke ho nka karolo ha GCS taolong ea molumo oa methapo, khahlano le semelo sa bona, kutloelo ea methapo ea mali ho li-catecholamines e eketseha, e lebisang keketseho ea khatello ea mali, liphetoho tsa metabolism ea metsi, sodium le metsi li bolokiloe, palo ea plasma e eketseha le hypovolemia e fokotseha.

Ho mamella le litlamorao

Sehlopha sena sa lithethefatsi hangata se baka litlamorao: ho hatelloa ke ho sebetsa hoa 'mele, ho mpefatsa ha mafu a tšoaetsanoang a mafu a tšoaetsanoang le mafu a ka mpeng ho ka etsahala. Ka tšebeliso ea nako e telele, keketseho ea khatello ea mali, nts'etsopele ea lefu la tsoekere la steroid, edema, bofokoli ba mesifa, myocardial dystrophy, syndrome ea Itsenko-Cushing, adrenal atrophy e ka etsahala.

Ka linako tse ling ha u sebelisa lithethefatsi, ho na le ho ba le khatello ea maikutlo, ho hloka boroko, khatello e eketsehileng ea kelello, psychosis. Ka tšebeliso ea nako e telele ea li-corticosteroids, synthesis ea masapo le calcium-phosphorus metabolism e kanna ea senyeha, eo qetellong e lebisang ho osteoporosis le ho phatloha habonolo.

Contraindication

• Hypersensitivity.
• Tšoaetso e matla.
• Maloetse a fungal le fungal.
• Lefuba le matla.
• AIDS
• Ulceric ulcer, ho tsoa mali.
• Mefuta e matla ea khatello ea mali.
• Itsenko-Cushing's syndrome.
• Jade
• Syphilis
• Lefu la tsoekere.
• Osteoporosis
• Boimana
• Ho anyesa.
• Psychoses e hlobaetsang.
• Bana ba banyenyane.

• Manonyeletso a tšoaetsanoang (a baktheria, a vaerase, a fungal) a letlalo le li-membrane tsa mucous.
• Tumelo ea letlalo.
• Tlokotsi ea botsepehi ba letlalo le li-membrane tsa mucous.
• Bana ba banyenyane.

Tšebelisano

GCS e ntlafatsa phello ea bronchodilating ea β-adrenostimulants le theophylline, e fokotsa phello ea hypoglycemic ea li-insulin le li-antidiabetesic tsa molomo, ketso ea anticoagulant ea coumarins (anticoagulants e sa tobang).

Diphenin, ephedrine, phenobarbital, rifampicin le lithethefatsi tse ling tse khothalletsang ho kenngoa ha li-enzymes tsa sebete sa microsomal li khutsufatsa T1 / 2 GCS. Hormone e holang le li-antacid li fokotsa ho monya li-corticosteroids. Ha e kopantsoe le pelo glycosides le diuretics, kotsi ea arrhythmias le hypokalemia ea eketseha, ha e kopantsoe le li-NSAIDs, menyetla ea tšenyo ea mpeng le monyetla oa ho tsoa mali ka mpeng.

Mochine oa ts'ebetso le litlamorao tse ka sehloohong tsa pharmacodynamic

Li-glucocorticoids li kenella kahare ho li-membrane tsa sele ka har'a cytoplasm ebe li tlama ho li-receptor tse khethehileng tsa glucocorticoid. Ho rarahaneng ho hlahisitsoeng ho kenella ka hare ho nucleus mme ho thusa ho theha i-RNA, e lebisang tlholehong ea liprotheine tse ngata tsa taolo. Lintho tse 'maloa tse sebetsang ka bioloji (catecholamines, babuelli ba methapo) ba khona ho kenya tšebetsong likarolo tsa glucocorticoid-receptor, ka ho etsa joalo ba fokotsa ts'ebetso ea li-glucocorticoids. Litlamorao tse kholo tsa glucocorticoids ke tse latelang.

• Tšusumetso ea sesole sa 'mele.

- Phello e khahlanong le ho ruruha (haholo-holo ka mefuta ea ho kulisa le ea ho itšireletsa mafung) ka lebaka la tšenyo e sa lekanyetsoang ea PG, RT le cytokines, ho fokotseha ha maikutlo a capillary, ho fokotseha ha chemotaxis ea lisele tsa immunocompetent le thibelo ea ts'ebetso ea fibroblast.

- Khatello ea ho se sebetse hantle ha cellular, karabelo ea autoimmune nakong ea phetiso ea litho, mosebetsi o fokotsehileng oa T-lymphocyte, macrophages, eosinophils.

• Kameho ho metabolism ea-electrolyte.

- Ho fokotseha ha 'mele oa sodium le metsi ion (ho eketsa botjha ka hare ho distal renal tubules), ho felisoa ka mafolofolo ha ion ea potasiamo (ho lithethefatsi tse nang le ts'ebetso ea mineralocorticoid), ho eketsa boima ba' mele.

- Phokotseho ea ho kenngoa ha li-ion tsa calcium ka lijo, ho fokotseha ha litaba tsa tsona liseleng tsa masapo (osteoporosis), le keketseho ea tlhahiso ea moroto.

• Tšusumetso lits'ebetsong tsa metabolic.

- Bakeng sa metabolism ea lipid - ho aroloa hape ha lithane tsa adipose (ho eketsoa hoa mafura sefahlehong, molaleng, senyepa sa mahetla, mpa), hypercholesterolemia.

- Bakeng sa metabolism ea carbohydrate - ho hlohlona ha tsoekere maling, ho fokotseha ha tumello ea membrane ea lisele bakeng sa tsoekere (nts'etsopele ea lefu la tsoekere la steroid e ka etsahala).

- Bakeng sa metabolism ea protheine - ho hlohlelletsa ha anabolism ka har'a sebete le ts'ebetso ea catabolic liseleng tse ling, ho fokotseha ha litaba tsa li-globulin ka plasma ea mali.

• Kameho ho CVS - khatello e matla ea mali (phallo ea methapo ea mali (steroid hypertension) ka lebaka la ho bolokoa ha mokelikeli 'meleng, keketseho ea letsoalo le methapo ea methapo ea kutlo lipelong le methapong ea mali, le keketseho ea khatello ea khatello ea angiotensin II.

• Kameho ho sistimi ea hypothalamus-pituitary-adrenal gland - inhibition ka lebaka la mochine o mobe oa ho araba.

• Tšusumetso maling - lymphocytopenia, monocytopenia le eosinopenia, ka nako e ts'oanang li-glucocorticoids li hlohlelletsa ho eketseha ha lisele tse khubelu tsa mali, li eketsa palo e felletseng ea li-neutrophils le liplatelete (liphetoho tsa sebopeho sa methapo ea mali li hlaha nakong ea lihora tse 6-12 kamora ho tsamaisoa le ho tsoela pele ka tšebeliso e telele ea meriana ena bakeng sa libeke tse 'maloa).

Li-glucocorticoids bakeng sa ts'ebeliso ea methapo ha li qhibilihe hantle ka metsing, li na le mafura le tse ling tse lokolohileng. Li potoloha maling li le maemong a mangata a liprotheine (a sa sebetseng). Mefuta e sa ts'oaneng ea li-glucocorticoids ke li-esters tsa metsi a qhibilihang ka letsoai kapa letsoai (litlama, hemisuccinates, phosphates), e lebisang ho qaleheng ha ts'ebetso kapele. Litlamorao tsa ho emisoa ha li-glucocorticoids tse nyane butle-butle li tsoela pele butle, empa li ka nka likhoeli tse 0.5-1, li sebelisetsoa liente tsa intraarticular.

Li-glucocorticoids bakeng sa tsamaiso ea molomo li ananeloa hantle ho tsoa ho tšilo ea lijo, C_tlhokomeliso maling, e hlokomeloa ka mor'a lihora tse 0.5-1,5. Lijo li liehisa ho kenngoa, empa ha li ame ho hlaka hoa lithethefatsi (tab. 27-15).

TLHOKOMELISO EA Glucocorticoids KA MOTSE OA HO SEBETSA

1. Glucocorticoids bakeng sa tšebeliso ea lihlooho:

A) bakeng sa ts'ebeliso letlalong (ka mokhoa oa setlolo, tranelate, emulsion, phofo):

- fluocinolone acetonide (sinaflan, flucinar)

- flumethasone pivalate (lindinden)

- betamethasone (celestoderm B, celeston)

B) ho kenya leihlo le / kapa tsebe, ka tsela ea setlolo sa mahlo:

- betamethasone n (betamethasone dipropionate, jj) B) bakeng sa ts'ebeliso ea inhalation:

- beclomethasone (beclometh, becotide)

- fluticasone propionate (flixotide)

D) bakeng sa tsamaiso ea methapo ea kutlo:

D) bakeng sa kenyelletso liseleng tsa periarticular:

Litlamorao tsa Metabolic

Li-Glucocorticoids li na le matla a khahlanong le khatello ea maikutlo, a anti-shock. Boemo ba bona ba mali bo nyoloha haholo ka khatello ea maikutlo, likotsi, ho felloa ke mali le maemo a makatsang. Keketseho ea boemo ba bona tlasa maemo ana ke o mong oa mekhoa ea ho ikamahanya le 'mele khatello ea maikutlo, tahlehelo ea mali, ntoa khahlanong le ho thothomela le litlamorao tsa khatello ea maikutlo. Glucocorticoids e eketsa khatello ea mali ea systemic, e eketsa methapo ea kutlo ea methapo le methapo ea methapo ho catecholamines, hape e thibela desensitization ea li-receptors ho catecholamine maemong a tsona a phahameng. Ntle le moo, glucocorticoids e boetse e hlohlelletsa erythropoiesis marong, e leng se etsang hore phallo ea mali e eketsehe ka potlako.

Kameho ho metabolism edit |