Blockers receptor histamine H2: magacyada daawooyinka

Koox Tani waa mid ka mid ah diyaarinta dawooyinka ee hogaaminaya iska leh doorashada ka dhigan tahay in daawaynta cudurada mid qoon leh. helay oo ka mid ah blockers receptor histamine H2 in labadii sano ee lasoo dhaafay, waxaa loo arkaa ugu weyn ee daawada, caawiyo si ay u xalliyaan (kharashka la awoodi karo) dhaqaalaha iyo dhibaatooyinka bulshada. Sababo la xiriira diyaarinta H2 blockers natiijooyinka daaweynta cudurka boog ayaa si weyn u soo hagaagtay, qalliin ayaa loo isticmaalaa si aan joogto ahayn ee suurtogalka ah, oo tayo leh bukaanka nolosha hagaagtay. "Cimetidine" loo yaqaan "Heerka dahab ah" in daaweyn jiray boogaha, "ranitidine" sanadkii 1998 noqday horyaalka ee iibka ee dawooyinkooda. Faa'iidada ugu weyn waa qiime jaban, oo sidaas waxtarka daawooyinkaan.

isticmaalka

blockers receptor histamine H2 loo isticmaalaa daawaynta cudurada caloosha acid-xiriira. saameynta hab ay - xanibeen receptors H2 (haddii kale loo yaqaan histamine) oo ka mid ah unugyada xabka gastric. Sababtan awgeed, waxaa hoos u-soo-saarka iyo gaarsiinta galay Lumen ee gastric Aashito. Kooxdaan daroogada la xiriira daawooyinka anti-boog antisecretory.

Xaaladaha intooda badan, ugu blockers receptor histamine H2 waxaa loo isticmaalaa in kiisaska ee daliilka cudurka boog ulcer. blockers H2 waxa kaliya ee aan loo yareeyo wax soo saarka ee Aashito, laakiin sidoo kale la xakameeyo pepsin, xab gastric sidaas kordhiyaa, waxaa kor u kacay prostagladinov Avv, kor u dheecaan ah ee bicarbonate. function Motor ee caloosha waa caadi, hagaajinaysaa microcirculation.

Tilmaamayaasha H2-blockers:

• cudurka reflux gastroesophageal;
• chronic iyo pankreatit ba'an;
• dyspepsia;
• Zollinger-Ellison syndrome,
• reflux-laaluusheen cudurka neefsashada;
• gastritis chronic iyo duodenitis;
• hunguriga Barrett ayaa;
• guuldaradii boogaha xabka esophageal;
• caloosha boog;
• iyo daawooyinka boog astaamaha;
• dyspepsia chronic la xabadka iyo xanuun gaastari;
• mastocytosis systemic;
• Waayo, ka hortagga boog stress,
• Mendelson ee syndrome,
• Ka hortagga pneumonia rajo gelin darteed,
• dhiig GI sare.

Histamine blockers receptor H2: dirka daroogada

Waxaa jira kala soocidda ka mid ah kooxdan oo ah daroogada. Waxay kala qaybsan yihiin qoysaska:

• Waayo, anigu waxaan walaac qarnigan "cimetidine".
• "Ranitidine" - xanibaha ah H2 receptor histamine II qarnigan.
• "Famotidine" waxa loola jeedaa jiilka III.
• "Nizatidine" waxa loola jeedaa jiilka IV.
• K V loola jeedaa jiilka "roxatidine".

"Cimetidine" ugu yaraan hydrophilic, ay sabab u tahay taas bar-nolosha waa mid aad u gaaban, shiid, cagaarshowga waqti isku mid macno leh. Blocker jawaabay cytochrome P-450 (enzyme microsomal) heerka isbedelka shiid xenobiotic cagaarshowga ah. "Cimetidine" waa inhibitor a universal-shiid ah, cagaarshowga daroogada ugu dhex. Marka tan la eego, waa inay galaan dhexgalka a pharmacokinetic sidaas daraaddeed raasamaal iyo khataraha macquulka ah kordhay waxyeellooyinka awoodaan.

Ka mid ah oo dhan blockers H2 "cimetidine" lays unug fiican, kaas oo sidoo kale keenaysaa in waxyeelo kordhay. Waxa uu bedelayaa testosterone qoomiyadda ka qabanaya la receptors durugsan, sidaas keenaya cillad galmada, waxay keenaysaa in hoos u dhac in awoodba, uu yeesho awood darro iyo gynecomastia. "Cimetidine" keeni kartaa madax xanuun, shuban, myalgia iyo arthralgia, transient, korodhsan kariyaatiniin dhiig, isbedel hematological, habdhiska, ficil jirka, cardiotoxicity. H2 xanibaha III receptors jiilka histamine - "Famotidine" - irbadu yar galay unugyada iyo xubnaha, oon hoos u xaddiga waxyeellooyin. Ha keeni cillad galmada iyo diyaarinta jiilalka mustaqbalka - "ranitidine", "nizatidine", "roxatidine". Dhammaan wax ma la macaamilaan androgens.

sifooyinka barbardhiga ee daroogada

Sharaxaad ka mid ah blockers receptor histamine H2 (daawo jiilka of class dheeri ah), magaca - "Ebrotidin" gooni iftiimiyay "ranitidine bismuth sitraydh" ma aha isku dar ah oo fudud, iyo xarunta adag. Halkan saleeyaan - ranitidine - xidhiidha vismusa sitraydh ferric.

H2 histamine jiilka xanibaha III receptors "Famotidine" iyo II - "ranitidine" - leeyihiin selectivity ka weyn ee "cimetidine". Selectivity - arrin ku dose-tiirsane ah oo qaraabo. "Famotidine" iyo "ranitidine" waa ka xushay badan "Tsinitidin" saameyn on receptors H2. By la barbardhigo, "famotidine" awood badan "ranitidine" sideed jeer, "Tsinitidina" - afartan jeer. The kala duwan ee ciidamada ayaa lagu go'aamiyey sida ay qaadasho kala duwan oo ka mid ah isu-H2-blockers oo dhaqmaan on xakamaynta Aashito. xoogga bonds la receptors ayaa sidoo kale go'aaminaya mudada soo-gaadhista. Haddii daroogada si adag xidhxidhan receptor ka fogeeyay si tartiib ah waxaa keena saamaynta mudada. On dheecaan "famotidine" ee asalka saameeyaa ugu raagaya. Cilmigu wuxuu caddeeyay in "cimetidine" yaraynaysaa dheecaan asalka ka badan 5 saacadood, "ranitidine" - 7-8 saacadood, 12 saacadood - "famotidine".

H2-blockers ka tirsan tahay koox ee daroogada hydrophilic. Ka mid ah iyo qarniyada oo dhan, "cimetidine" ka yar kale hydrophilic ah, halka dhexdhexaad lipophilic. Tani waxay awood u si fudud geli xubnaha kala duwan, saamaynta ay ku H2-receptors, taas oo horseedaysa in ay waxyeelo badan. "Famotidine" iyo "ranitidine" waxaa loo arkaa in ay heer sare hydrophilic, iyagu ma ay gelin dhar, pre-rebshedaha ay saameynta ku receptors H2 unugyada parietal.

Tirada ugu badan ee waxyeelo ee "cimetidine". "Famotidine" iyo "ranitidine", ay sabab u tahay isbeddel ah ee qaab-dhismeedka kiimikada, ma saamayn cagaarshowga ee metabolizing falgalka iyo siin waxyeelo yar.

story

Taariikhda kooxdan oo ah H2-blockers bilaabay 1972. Shirkadda British shaybaarka hoos jihada ee James Blake cilmi-baaris oo ku dhexsameeysmo jirka tiro badan oo xeryahooda in qaab ahaan la mid yihiin Britain waa histamine. Marka la xidhiidha ammaan ah oo la aqoonsaday, ay ku wareejiyeen waxbarashada clinical. The buriamid xanibaha marka hore ma ahaa mid aad u wax ku ool ah. Its qaab-dhismeedka ayaa la bedelay, waxay u leexatay metiamide. waxbarashada Clinical ay muujiyeen awood ka weyn, laakiin tusay sumoobo weyn, kaas oo lagu muujiyey qaab granulocytopenia. cilmi baaris dheeraad ah ayaa keentay in "cimetidine" (daroogada aan jiilka) waxa la furay. daroogada ayaa si guul leh u maray tijaabo ee 1974 waxaa la ogolaaday. Markaas wax bilaabay in ay isticmaalaan blockers receptor histamine H2 in bukaan eegida, waxa uu ahaa kacaan in gastroenterology. Dzheyms Blek ahaa daahfurka this Nobel Prize ee 1988.

Science ma weli taagan. Maaddaama ay waxyeelo badan pharmacologists "cimetidine" waxay bilaabeen inay sii search for durkin xeryahooda wax ku ool ah. Sidaas awgeed waxa la furay iyo blockers kale oo cusub histamine H2 receptor. Daawooyinka loo yareeyo dheecaan ka, laakiin wax saameyn ah kuma kiciya ay (acetylcholine, gastrin). Dhibaatooyinka ay keento, "ricochet acid" u janjeedha saynisyahano in la raadiyo hab cusub si loo yareeyo ashitada.

daawo dhacsan

Waxaa jira fasalka casriga ah ee daroogada - inhibitors bamka proton. Waxay yihiin ka xoogbadan, ee kislotopodavleniyu, ugu yaraan waxyeelo, waqti saamaynta H2 blockers receptor histamine. Daroogooyinka, magacyada kuwaas oo kor ku xusan, waxaa weli loo isticmaalaa in bukaan eegida arrin inta badan ay sabab u tahay genetics, sababo dhaqaale (more inta badan waxa "famotidine" ama "ranitidine").

hab casri ah Antisecretory codsatay in la yareeyo xaddiga Aashito, qaybsan yihiin laba fasal oo ballaadhan, oo inhibitors ee bamka protonic (PPI) iyo H2 blockers receptor histamine. diyaarinta la soo dhaafay waxaa lagu gartaa saamaynta tachyphylaxis markii dhaweynta soo noqnoqda sababa hoos u dhac ku saamaynta ku daweynta. Ma jiro API for la'aanta this, sidaas darteed, in la barbardhigo blockers H2 waxaa lagu talinayaa in therapy muddo dheer.

Arrin ku tachyphylaxis marka la qaadanayo blockers H2 arkay tan iyo bilowgii therapy 42 saacadood gudahood. In daaweynta dhiig boog gastroduodenal laguma talinayo blockers H2, proton doorbidayso inhibitors bamka.

caabin

Xaaladaha qaarkood, blockers receptor H2 histamine (soocidda kor ku xusan) iyo sidoo kale daawooyinka PPI mararka qaarkood keeni iska caabin ah. In loo qabanayo sida bukaan socodka caloosha deegaanka pH aan ogaado wixii isbeddel ah ee heerka ashitada intragastric. Mararka qaarkood la ogaado xaaladood oo iska caabin ah si ay wax blockers H2 group, 2 ama 3 ka ab ama inhibitors bamka proton. Iyo kordhinta qiyaasta in kiisaska noocaas ah uma shaqeeyo, waxaad u baahan tahay si ay u doortaan nooca kala duwan ee daroogada. Waxbarasho gaar ah H2-blockers, omeprazole iyo (Individual Program Plan) ayaa muujinaysa, in laga bilaabo 1 ilaa 5% ee kiisaska aan ahayn isbeddel ah ee maalin walba pH-metry. In daawashada firfircoon ka ahaa nidaamka daaweynta acid waxaa loo arkaa inay qorshaha ugu hufan halkaas oo la socodka pH Esophageal waxaa baaritaan marka hore, ka dibna maalintii shanaad iyo bisha toddobaad oo daaweyn ah. Joogitaanka bukaanka qaba dhamaystiran iska caabin ah waxay muujinaysaa in in bukaan eegida, waxaa jira ma jirto daroogo, taas oo yeelan doonta tayada shaqo wayn.

waxyeellooyin

Blockers receptor histamine saamaynta sababta kooxda H2 leh inta jeer ee kala duwan. Isticmaal "cimetidine" iyaga keenaya in 3.2% ka mid ah xaaladaha. . "Famotidine - 1.3%," ranitidine "- 2.7% Dhibaatooyinka ay keento waxaa ka mid ah:

• Dawakh, madax xanuun, walaaca, daal, hurdo, wareersan, maanka, murugada, kacsanaan, dhalanteed, dhaqdhaqaaq aan ikhtiyaarka lahayn, aragga indhaha oo isku darsamay.
• Arrhythmia oo ay ku jiraan bradycardia, tachycardia, arrythmia, asystole.
• Shuban ama calool, calool xanuun, matag, yalaalugo.
• pankreatit Ba'an.
• Diidmo (qandho, finan, myalgia, anaphylaxis, arthralgia, multiforme erythema, barar angioneurotic).
• Isbeddelka ku dhaca beerka baaritaano functional, milmay ama daliilka holistaticheskie hepatitis la joonis ama waxa aan.
• kariyaatiniin kordhay.
• Xadgudubyada dhiigga (leukopenia, pancytopenia, granulocytopenia, Agranulocytosis, Torombositobiiniya, anemia aplastic iyo hypoplasia cerebral, anemia haemolytic Immune.
• Hamo.
• Gynecomastia.
• Alopecia.
• hoos libido.

Famotidine saamaynta ugu ayaa on mareenka caloosha iyo mindhicirka, inta badan waxay yeeshaan shuban, marmar dhif ah, on lid ku ah, waxaa jira caloosha oo. Shuban dhacdaa sababtoo ah saamaynta antisecretory. Sababo la xaqiiqada ah in xaddiga Aashito caloosha ka hoos, pH uu kordho. Xaaladdan oo kale, si tartiib ah pepsinogen beddelin pepsin, taas oo ka caawisaa dumin brotiin. Dheefshiidka loo jeediyo, oo inta badan uu yeesho shuban.

sababo

By H2 blockers receptor histamine ka mid ah tiro ka mid ah daroogada, kuwaas oo ah sababo soo socda:

• Rabshadaha ee kelyaha iyo beerka.
• Cirrhosis (cudur encephalopathy portosystemic).
• Nuujinta.
• Diidmo in daroogada mid ka mid ah kooxdan.
• Uurka.
• Carruurta da'doodu tahay ilaa 14 sano.

Dhexgalka daroogooyinka kale

blockers receptor histamine H2, taas oo hab ficil waxaa haatan la fahamsan yahay inay leeyihiin isdhexgalka daroogada pharmacokinetic qaarkood.

Nuugista ee caloosha. saamayn Sababo antisecretory of H2-blockers waxay awoodaan in ay saameyn ku nuugo oo ka mid ah daroogada-electrolytes, halkaas oo ay jiraan tiirsanaanta a on pH ah, maxaa yeelay, daroogada yareyn kartaa heerka uu sida- iyo ionization. "Cimetidine" yarayn kartaa nuugo qalabka sida "Antipyrin" "ketokonazol" "chlorpromazine" iyo diyaarinta sare bir ah. Si looga fogaado nuugeynin sida, daroogada waa in la qaataa 1-2 saacadood ka hor isticmaalka blockers H2.

Dheef-cagaarshowga. blockers receptor histamine H2 (daroogada aan jiilka gaar ahaan) si firfircoon ula falgalaan P-450 cytochrome, taas oo ah beerka oxidizer maamulaha. The bar-nolosha la kordhin doonaa, iyo saamaynta ay ka muuqato badinta sprolongirovatsya ee daroogada taas oo metabolized in ka badan 74%. Xoog oo dhan ka jawaabay cytochrome P-450 galo "cimetidine", 10 jeer in ka sii badan "ranitidine". Dhexgalka "famotidine" aan dhacaya. Sababtan awgeed, marka la isticmaalayo "ranitidine" iyo "Famotidine" xadgudub ma dhacdaa shiid daroogada, cagaarshowga, ama waxa ay muujineysaa in yar ilaa xad ah. Marka la isticmaalayo "cimetidine" oggalaansho daroogada ee hoos ku dhowaad 40%, iyo waa Caafimaad ahaan la taaban karo.

Heerka socodka dhiigga cagaarshowga. hoos u dhici doono xawaaraha socodka dhiigga cagaarshowga in 40% marka la isticmaalayo a "cimetidine", iyo "ranitidine" hoos u dhici doono ansixin dheefshiidka prisistemnogo sare ee daroogada. "Famotidine" in kiisaskan aysan waxba ka beddelin heerka of socodka dhiigga portal.

Digo kelyaha embriyaha. eksretiruyutsya H2-blockers leh dheecaan embriyaha kelyaha firfircoon. Xaaladahan, dhexgalka suurto gal daawooyin isku midka ah haddii ay ekskrektsiya fuliyay by habab isku mid ah. "Imetidin" iyo "ranitidine" awood yaraynta ekskrektsiyu ah kelyaha in ay 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" ma laha isbedel ku tirtiridda daawooyinkan. Intaas waxaa sii dheer, ay dose-daweynta waa karti u leh uruuray hooseeyo ee plasma, taas oo aan la inta badan la tartami doona wakiilada kale ee heerarka calcium of dheecaan ah.

isdhexgalka Pharmacodynamic. Dhexgalka H2-blockers dadka kale kooxaha daroogada antisecretory awood sii kordhaysa oggolyahay ku-daweynta (tus, holinoblokatorami). Isku dhafan oo wakiilada in dhaqmaan on Helicobacter (diyaarinta of metronidazole, bismuth, tetracycline, clarithromycin, amoxycillin), dedejisaa giijisan ee boogaha ulcer.

dhexgalka kasin Pharmacodynamic markii daawooyinka la aasaasay, taas oo ka mid ah testosterone marka la isku daro. "Cimetidine" hormone barakacay ka qabanaya la receptors on fiirsashada 20% ah ee plasma waxaa kor u kacay. "Famotidine" iyo "ranitidine" ma saamayn caynkaas ah.

magacyada ganacsiga

In dalka, ka diiwaan gashan oo loo ogol yahay inuu iska iibiyo daawooyinka kuwanu waa H2-blockers:

"Cimetidine"

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

"Ranitidine"

magacyada Ganacsiga: "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"

magacyada Ganacsiga: "Gasterogen", "Blokatsid", "Antodin", "Kvamatel", "gastrosidin", "Letsedil", "ulfamid", "Pepsidin", "Famonit", "Famotel", "Famosan", "Famopsin" "famotidine Agos", "Famotsid", "famotidine NUSOJ", "Weyniga famotidine".

"Nizatidine". Magaca ganacsiga "Aksid".

"Roxatidine". Magaca ganacsiga "Roxane".

"Sitraydh bismuth ranitidine". Magaca ganacsiga "Pilorid".