Histamine H2 receptor blockers: mabitso a lithethefatsi

Sehlopha sena ke e 'ngoe har'a litokisetso meriana ea itlhommeng pele ka ke ea tlhopho bolela ka ho phekola mafu a ulcerous. Ho sibolloa ha H2 histamine receptor blockers ka lilemo tse mashome a mabeli tse fetileng, ho nkoa ka kholo ka ho fetisisa ka moriana, ho thusa ho rarolla mathata a moruo le (ka theko e tlaase theko) le mathata a sechaba. Ka lebaka la litokisetso H2 blockers liphello tsa phekolo ea lefu seso ba ntlafalitse haholo, tsereletsi ho buoa 'nile ha sebelisoa ka tlase hangata kamoo ho ka khonehang, boleng bakuli ba bophelo ba ntlafala. "Cimetidine" bitsoang "khauta tekanyetso" ea ho phekola sa liso tsa ka maleng, "Ranitidine" ka 1998 ea e-ba 'mampoli oa thekiso ka pharmacology. Ka ba molemo ho kholo ka ho fetisisa e theko e tlase, 'me kahoo ho atleha ea lithethefatsi.

tshebediso ya

H2 histamine receptor blockers sebediswa bakeng sa kalafo ya mafu acid e amanang gastrointestinal. sephetho mochine - thibela H2 receptors (ho seng joalo e bitsoa histamine) ya lisele tse gastric mucosa. Ka lebaka lena, ho fokotswa tlhahiso le pelehi ka lumen ea acid e hydrochloric gastric. Sehlopha sena sa ho sebelisa lithethefatsi amanang le lithethefatsi antisecretory-ba khahlanong le seso.

Maemong a mangata, ho H2 histamine receptor blockers sebelisoa maemong a sa peptic liponahatso lefu seso. H2 blockers ha feela fokotsa tlhahiso ea asiti hydrochloric, empa hape thibela metsoako pepsin, mucus gastric ka tsela eo eketsa, ho na le e eketseha tswakana prostagladinov, e ile ea eketseha secretion ea bicarbonate. Motor mosebetsi wa mala ke boetse maemong, ntlafatsa microcirculation.

Ho bonahala H2-blockers:

• gastroesophageal reflux lefu;
• foleng le a hlobaetsang le pancreatitis;
• dyspepsia;
• Zollinger-Ellison lefu;
• reflux-hlohlelletsoa lefu matšoafo;
• foleng gastritis le duodenitis;
• metso Barrett ya;
• hlōloa liso esophageal mucosa;
• mala seso;
• le seso lithethefatsi bontshang matshwao;
• foleng dyspepsia ka sefubeng le bohloko epigastric;
• systemic mastocytosis;
• bakeng sa thibelo ea ho imeloa kelellong seso;
• lefu Mendelson ya;
• Thibelo ea serame sa matšoafo aspiration;
• tsoa mali ka holimo GI.

Histamine H2 receptor blockers: tlhophiso ea lithethefatsi

Ho na le ke tlhophiso ea sehlopha sena sa lithethefatsi. Di arotsoe ka malapa a:

• Etsoe ke dingongoreho moloko "cimetidine".
• "Ranitidine" - e blocker tsa H2 histamine receptor II o mong.
• "Famotidine" le bolela moloko o III.
• "Nizatidine" e bolela IV o mong.
• K V e bua moloko "roxatidine".

"Cimetidine" e monyenyane hydrophilic, ka lebaka la ena halofo bophelo bo bokhutšoanyane haholo, e amanang le sebete metabolism ka nako e tšoanang e nang le morero. Blocker a ileng a itšoara ka cytochrome P-450 (microsomal potlakisang tsebetso ea lik'hemik'hale) le sekgahla sa ho fetoha ha e amanang le sebete xenobiotic metabolism. "Cimetidine" ke sesitisa bokahohleng ea metabolism e amanang le sebete ea lithethefatsi ho fetisisa har'a. Tabeng ena, ho ke ke khona ho kena sebelisana le pharmacokinetic Ka hona khoneha bokella le likotsi tse eketsehileng tsa litla-morao.

Har'a H2 blockers tsohle "cimetidine" molemo dinama tse nyenyane tse ho kenella ka hare, e leng se boetseng isang litla eketsehileng lehlakoreng. O nka sebaka e se nang sesosa testosterone tloha tlamang le receptors le pheriferale, kahoo a etsa hore ho se sebetse ho kopanela liphate, etsa hore fokotseha ka ho potency, develops ho hloka matla le gynecomastia. "Cimetidine" ho ka etsa hore hlooho, letšollo, myalgia le arthralgia, e fetang, keketseho ea creatinine mali, liphetoho hematological, CNS, immunosuppressive bohato, cardiotoxicity. H2 blocker III isa molokong o mong histamine receptors - "Famotidine" - tlase phunyelletsa ka lisele tse le ho makala, ka tsela eo fokotseha le palo ya litla-morao. U se ke ua etsa hore ho se sebetse ho kopanela liphate le ka litokisetso tsa meloko e tlang - "Ranitidine", "nizatidine", "roxatidine". Kaofela ha bona ba u se ke ua kopana le androgens.

Bapisang litšobotsi tsa lithethefatsi

Tlhaloso ea blockers H2 histamine receptor (meriana moloko oa eketsehileng-sehlopha sa), lebitso - "Ebrotidin" ntle totobatsa "Ranitidine bismuth citrate" hase motsoako e bonolo, 'me e le motsoako e rarahaneng. Mona theha - ranitidine - amanang le ferric citrate vismusa.

Histamine H2 blocker isa molokong o mong III "Famotidine" receptors le II - "Ranitidine" - ba le selectivity a maholo ho feta "cimetidine". Selectivity - lipono tse makatsang tsa lethal dose-itšetlehileng ka eona le e lekanyelitsoeng. "Famotidine" le "ranitidine" khetha ho feta "Tsinitidin" phello H2 receptors. Ha ho bapisoa, "famotidine" matla "Ranitidine" ka makhetlo a robeli, "Tsinitidina" - mashome a mane linako tse ling. Ho se tšoane ha a qobelle ba ikemiselitse ho latela tekanyetso tse sa tšoaneng tsa ditekani H2-blockers eo sebetsa ka hatelloang ea acid e hydrochloric. Matla a ka tiisa litlamo le receptors e boetse e etsang qeto ea hore ka nako ea ho pepesehela. Ha ea lithethefatsi e ka matla tlameha ho receptor le dissociates butle ho bakoa ke phello ea nako e. Ka basal secretion "famotidine" ama tsoarellang ho fetisisa. Liphuputso li bontša hore "cimetidine" fokotsa basal secretion bakeng sa lihora tse 5, "Ranitidine" - lihora tse 7-8, 12 lihora tse - "famotidine".

H2-blockers ho matleng a sehlopha sa lithethefatsi hydrophilic. Har'a meloko eohle, "cimetidine" ka tlaase ho e hydrophilic a mang, ha a ntse a ka tekano lipophilic. Sena se nolofalletsa ho habonolo phunyeletse makala a sa tšoaneng, ho ama ba H2-receptors, leng isang litla ngata lehlakoreng. "Famotidine" le "Ranitidine" li nka hore ke haholo hydrophilic, ha ba phunyeletse ka lesela, pele ho emptive tshusumetso bona ka H2 receptors ea lisele parietal.

The lebetsoeng le nomoro ea litla-morao ka "Cimetidine". "Famotidine" le "Ranitidine", ka lebaka la ho liphetoho ka sebopeho lik'hemik'hale, u se ke ua ama ea e amanang le sebete metabolizing enzyme le fa litla mmalwa lehlakoreng.

pale

Histori ea sehlopha sena sa H2-blockers qala ka 1972. khampani British ka laboratoring tlas'a tataiso ea James Blake batlisisitsoeng le tsa maiketsetso nomoro ea tonanahali ea metsoako tse structurally tšoanang le molek'hule e ke histamine. Hang ka mabapi se sireletsehileng di khetholloa, ba ne ba isoe ho lithuto tsa tleleniki. Pele blocker buriamid e ne e se e atlehang haholo. sebopeho lona fetotsoe, e ile metiamide. lithuto tsa Clinical li bontšitse bohlokwa ba tsamaiso e khōloanyane, empa o ile a bontša toxicity boholo, boo e bontšoa ka mokgwa wa granulocytopenia. lipatlisiso tse eketsehileng e ile ea etsa hore seo e se o ile a bula "Cimetidine" (Ke molokong o mong ka lithethefatsi). Lithethefatsi e ka katleho fetile liteko tse matla tsa tleleniki ka 1974 amohelehang eona. Ebe ntho e 'ngoe o ile a qala ho sebelisa H2 histamine receptor blockers ikatisetsa litleleniki tsa, e ne e le phetoho e khōlō gastroenterology. Dzheyms Blek ne ho sibolloa ena Khau ea Nobel ka 1988.

Saense ha e ema. Ka lebaka la litla multiple lehlakoreng "Cimetidine" pharmacologists o ile a qala ho boloka batla ikhethang bakeng sa metsoako e atlehang haholoanyane. Kahoo, ho ile ha buloa 'me tse ling tse ncha H2 histamine receptor blockers. Lithethefatsi fokotsa secretion, empa ha e ame tse susumetsang tsa lona (acetylcholine, gastrin). Le litla-morao, "acid e ricochet" sekametseng bo-rasaense ba ho batla ho bolela le lecha ho fokotsa acidity.

moriana siiloe ke nako

Ho na le ke sehlopha sa kajeno ea lithethefatsi - inhibitors proton e pompo. Ba le phahametse ka kislotopodavleniyu, bakeng sa bonyane ba litla-morao, 'me lekhetlong litla H2 histamine receptor blockers. Lithethefatsi, mabitso a ba tse thathamisitsoeng ka holimo, ho e ntse e sebediswang ikwetlisetse tlelenike hangata ka lebaka la ho liphatsa tsa lefutso, ka mabaka a moruo (hangata e "famotidine" kapa "Ranitidine").

Antisecretory ho bolela mehleng ea kajeno ba sebelisa ho fokotsa palo ea acid e hydrochloric, ba arotsoe ka lihlopha tse peli tse sephara: ho inhibitors ea pompo protonic (PPI) le H2 histamine receptor blockers. litokisetso ho qetela a tšoauoa ka phello ea tachyphylaxis ha phetoa baeti ba fihlelang ho baka ho fokotseha ha phello phekolo. Ha ho na API lebaka la ho haelloa hona, ka lebaka leo, ho fapana ho blockers H2 ba kgothaletswa bakeng sa phekolo ea nako e telele.

Lipono tse makatsang tsa tachyphylaxis ha nka H2 blockers hlokomela ho tloha qalong ea phekolo ka hare ho lihora tse 42. Ka ho phekola gastroduodenal mali seso e sa kgothaletswa H2 blockers, itlhopheang proton e pompa inhibitors.

hanyetsa

Maemong a mang, histamine H2 receptor blockers (tlhophiso ea bontša ka holimo) hammoho le PPI lithethefatsi ka linako tse ling etsa hore ho hanyetsa. Ka khanna joalo bakuli ba mala ph tikoloho ya go baya leitlho e sa lemoha liphetoho leha e le efe intragastric acidity boemong ba. Ka linako tse ling lemoha maemo a ho ho hanyetsa sehlopha leha e le efe H2 blockers, litloho-2 kapa 3 kapa inhibitors proton e pompo. Le ho eketseha lethal dose ea maemong a joalo ha se sebetse, o lokela ho khetha mokgwa o fapaneng wa lithethefatsi. Ho ithuta tse itseng H2-blockers, omeprazole le (IPP) e bontša hore ho tloha ho 1 ho fihlela ho 5% ea linyeoe le tse sa liphetoho ka letsatsi ph-metry. Ka hlokomela matla ya tshebetso ya ho kalafo asiti e nkoa e le e sekemeng sebetsang hantle ka ho fetisisa moo Esophageal ph boalosi e fuputswa qalong, 'me joale ka letsatsi la bohlano le la bosupa ea phekolo. Ho ba teng ha bakuli ba hanyetsa ka ho feletseng ho bontša hore ho ka go ikatisetsa litleleniki tsa, ha ho na ea lithethefatsi, e neng e tla ba le bokgoni feletseng.

litla-morao

Blockers H2 histamine receptor litla sesosa lehlakoreng le fapaneng maqhubu. Sebelisa "Cimetidine" etsa hore ba 3.2% ea linyeoe. . "Famotidine - 1.3%," Ranitidine "- 2,7% Side litla kenyeletsa:

• Ho tsekela, ho tšoaroa ke hlooho, ho tšoenyeha, mokhathala, ho otsela, ferekane, kelello, ho tepella maikutlo, pherekano, lipono, mekhatlo involuntary, thothofatsang Pono.
• Arrhythmia ho akarelletsa bradycardia, tachycardia, arrythmia, asystole.
• Letšollo kapa pipitlelano, bohloko mpeng, ho hlatsa, ho nyekoa ke pelo.
• Hlobaetsang pancreatitis.
• Hypersensitivity (feberu, lekhopho, myalgia, anaphylaxis, arthralgia, etymology multiforme, angioneurotic edema).
• Liphetoho ka sebete liteko tshebetso, mokgwa oo kopantsweng kapa liponahatso holistaticheskie lefu la sebete le nyooko kapa ka ntle ho eona.
• Eketseha creatinine.
• Ho tlola mali (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, aplastic khaello ea mali le hypoplasia bokong, haemolytic khaello ea mali 'mele.
• Ho hloka matla.
• Gynecomastia.
• Alopecia.
• fokotseha libido.

Famotidine litla-morao ho fetisisa e ka pampitšana ea gastrointestinal, ba atisa ho ba le letšollo, maemong a sa tloaelehang, ho fapana le hoo, ho na le pipitlelano. Letšollo le hlaha ka lebaka la litla antisecretory. Ka lebaka la 'nete ea hore palo ea acid e hydrochloric ka mpeng ea decreases, ho ph eketseha. Tabeng ena, pepsinogen butle fetoha pepsin, e thusang heletsa liprotheine. Tshilo ya dijo e tšoenngoa, 'me hangata develops letšollo.

Contraindications

Ke H2 histamine receptor blockers kenyeletsa 'maloa a lithethefatsi, e leng na le contraindications ho latelang:

• Meferefere ka liphio le sebete.
• Ho thatafala ha sebete (portosystemic magazine lefu).
• Diabolololo.
• Hypersensitivity ho lithethefatsi leha e le life tsa sehlopha sena.
• Ho ima.
• Bana ba lilemo li ho fihlela ho lilemo tse 14.

Sebelisana le lithethefatsi tse ling

Histamine H2 receptor blockers, eo bohato mochine e hona joale utloisisoa hore na itseng ditshebeditsano pharmacokinetic lithethefatsi.

Absorption ka mpeng. Ka lebaka antisecretory phello ea H2-blockers khona ho susumetsa absorption ea lithethefatsi electrolyte, moo ho na le ke ho itšetleha ka ph, hobane lithethefatsi ka fokotsa tekanyo ea ho diffusion le ionization. "Cimetidine" ka fokotsa absorption ea lisebelisoa tse kang "Antipyrin" "ketoconazole" "Chlorpromazine" le litokisetso phahameng tšepe. Ho qoba malabsorption joalo, lithethefatsi lokela ho ho nkoa ka lihora tse 1-2 pele ho tšebeliso ea H2 blockers.

E amanang le sebete metabolism. H2 histamine receptor blockers (lithethefatsi ke isa molokong o mong ka ho khetheha) mafolofolo kopana le cytochrome P-450, e leng mosuoe-hlooho oxidizer sebete. The halofo bophelo tla eketseha, 'me phello e ka' na ho bonahala sprolongirovatsya overdose ea lithethefatsi e metabolized ke ho feta 74%. Matla le ho feta tsohle a ileng a itšoara ka cytochrome P-450 kena "Cimetidine", ka makhetlo a 10 ho feta "Ranitidine". Sebelisana le "famotidine" e sa etsahala. Ka lebaka lena, ha ba sebelisa "Ranitidine" le "Famotidine" ha ho na tlōlo le hlaha ea metabolism e amanang le sebete lithethefatsi, kapa e bontša ka tekanyo e nyenyane. Ha u sebelisa "Cimetidine" rengwa ea lithethefatsi ka fokotswa ka bang 40%, 'me ke ea bongaka bohlokoa.

Tekanyo ea phallo e amanang le sebete mali. E ka fokotsa e amanang le sebete phallo ea mali lebelo ho 40% ha sebelisa "Cimetidine", le "Ranitidine" a ka fokotsa prisistemnogo phahameng metaboliki rengwa lithethefatsi. "Famotidine" maemong ana ha fetola lebelo la phallo-portal ea mali.

Tubular renal excretion. H2-blockers eksretiruyutsya le a sebetsang a renal secretion tubular. Maemong ana, sebelisana khoneha le lithethefatsi e tšoanang ha ba ekskrektsiya etsoang ke mekgwa e tšoanang. "Imetidin" le "Ranitidine" ea nang le bokhoni ba ho fokotsa ekskrektsiyu renal ho 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" ha e na ho fetoha ha ho felisoa ha lithethefatsi tsena li ka. Ho feta moo, lethal dose lona phekolo e nang le bokhoni ba ho fana ka ea mahloriso tlaase ka lero la mali, eo bo ke ke ba haholo-holo ka ho phehisana le mahlahana a mang a maemo le k'halsiamo ea secretion.

Pharmacodynamic ditshebeditsano. Sebelisana le H2-blockers bang lihlopha antisecretory lithethefatsi khonang ho eketsa phekolo bohlokwa ba tsamaiso (mohlala, holinoblokatorami). Hammoho le mahlahana a hore ho sebetsa ka helicobacter (litokisetso tsa metronidazole, bismuth, tetracycline, clarithromycin, amoxicillin), eketsa rag tsa liso peptic.

Pharmacodynamic bohloko sebelisana ha ho kopantswe le lithethefatsi e thehilweng, e leng kenyeletsa testosterone. "Cimetidine" hormona mahae tloha tlamang le receptors ka 20% ea mahloriso ka lero la mali e ile ea eketseha. "Famotidine" le "Ranitidine" u se ke ua ba le le phello e joalo.

mabitso a kgwebo ya

Naheng ea heso, ngolisitsoeng le lumelloa ho rekisa lithethefatsi tsena li ka ke H2-blockers:

"Cimetidine"

mabitso Trade: "Altramet", "Belomet", "Apo-cimetidine", "Yenametidin", "Gistodil", "New tsimetin", "Neytronorm", "Tagamet", "Simesan", "Primamet", "Tsemidin" "Ulkometin", "Ulkuzal", "Tsimet", "Tsimegeksal", "Tsigamet", "cimetidine-Rivofarm", "cimetidine Lannaher".

"Ranitidine"

Trade mabitso: "Atsilok", "Ranitidine Vramed", "Atsideks", "Asitek", "Gistak" "Vero ranitidine," "Zoran", "Zantin", "Ranitidine Sedico," "Zantac", "Ranigast" "Raniberl 150", "Ranitidine", "Ranison" "Ranisan", "Ranitidine Akos", "Ranitidine BMS", "Ranitin" "Rantak" "Renks" "Rantag" "Yazitin" "Ulran "" Ulkodin ".

"Famotidine"

mabitso Trade: "Gasterogen", "Blokatsid", "Antodin", "Kvamatel", "gastrosidin", "Letsedil", "ulfamid", "Pepsidin", "Famonit", "Famotel", "Famosan", "Famopsin" "famotidine Agos", "Famotsid", "famotidine Apo", "famotidine Acre".

"Nizatidine". Trade lebitso "Aksid".

"Roxatidine". Trade lebitso "Roxane".

"Ranitidine bismuth citrate". Trade lebitso "Pilorid".