Histamine H2 receptor blocker: amagama iziyobisi

Eli qela yenye phakathi amalungiselelo zoxubo ehamba phambili bobabo ukukhethwa kuthetha kwi unyango lwezifo ezilinyaziweyo. Ukufunyanwa kwe H2 histamine blocker receptor kwiminyaka engamashumi amabini edlulileyo, uthathwa inkulu amayeza, ukunceda ukusombulula kwezoqoqosho (iindleko ezifikelelekayo) kunye neengxaki zentlalo. Ngenxa amalungiselelo H2 blocker iziphumo unyango lwesifo isilonda ziye zaphucuka kakhulu, ungenelelo zotyando ziye ezisetyenziswa rhoqo kangangoko kunokwenzeka, umgangatho izigulane 'yokuphila ngcono. "Cimetidine" kuthiwa "umgangatho igolide" kwi kunyango izilonda, "Ranitidine" ngo-1998 waba yintshatsheli ukuthengiswa Pharmacology. I inzuzo enkulu kunazo zonke zamaxabiso aphantsi, yaye ukusebenza iziyobisi.

ukusetyenziswa

H2 receptor blocker histamine ezisetyenziselwa ukunyanga izifo zesisu ezinxulumene-asidi. indlela iimpembelelo - ethintela H2 receptors (ngenye kubizwa ngokuba histamine) iiseli isifo esiswini. Ngenxa yesi sizathu, kwanciphisa imveliso kunye nokunikezelwa kungena mithambo of zehydrochloric acid esiswini. Eli qela lamachiza ezinxulumene neziyobisi antisecretory anti-esiswini.

Kwiimeko ezininzi, ezi blocker H2 histamine receptor zisetyenziswa kwiimeko obubonakala sifo isilonda Peptic. H2 blocker azikho nje ekunciphiseni kwimveliso zehydrochloric acid, kodwa akuyithinteli pepsin, ngaloo ndlela yencindi esiswini kwandisa, kukho lwakukhula njini prostagladinov, ukwanda secretion of yesoda. Motor umsebenzi nesisu nganye ezinga malungu abantu, kuphucula microcirculation.

Iimpawu H2-blocker:

• isifo reflux gastroesophageal;
• ezingapheliyo kunye pancreatitis oyingozi;
• ukuqunjelwa;
• syndrome Zollinger-Ellison;
• reflux-eyabangelwa isifo yokuphefumla;
• gastritis okungapheliyo kunye duodenitis;
• emphinjeni Barret kaThixo;
• ukoyiswa izilonda isifo esophageal;
• isisu isilonda;
• neziyobisi isilonda lingaze;
• ukuqunjelwa ezingapheliyo kunye esifubeni kunye neentlungu epigastric;
• mastocytosis systemic;
• kuthintelo xi isilonda;
• syndrome mendelson kaThixo;
• Uthintelo yokulangazelela pneumonia;
• ukopha GI eliphezulu.

Histamine blocker H2 receptor: nokubekwa kwamachiza

Kukho uhlelo eli qela iziyobisi. Zahlula-hlulwe iintsapho:

• Kuba sizukulwana iinkxalabo "cimetidine".
• "Ranitidine" - a blocker of H2 histamine receptor II ngezizukulwana.
• "Famotidine" libhekisela isizukulwana III.
• "Nizatidine" libhekisela ngezizukulwana IV.
• K V ubhekisela isizukulwana "roxatidine".

"Cimetidine" komncinane esibamba, ngenxa yokuba lo isiqingatha-bomi bufutshane kakhulu, ukutya hepatic ngexesha elifanayo lebyi. Popup awasabela ngayo kunye cytochrome P-450 (microsomal enzyme) kunye nezinga utshintsho emzimbeni hepatic xenobiotic. "Cimetidine" i inhibitor yendalo nethe hepatic zamachiza ezininzi phakathi. Ngoko ke iyakwazi inxaxheba intsebenziswano pharmacokinetic ngoko nokwanda okunokwenzeka kunye yokukhulisa umngcipheko yeziphumo ebezingalindelekanga.

Phakathi zonke blocker H2 "cimetidine" ngcono izihlunu umthondo, nayo leyo ekhokelela yeziphumo ebezingalindelekanga linyukile. Asusa testosterone iqala ukuba iyabophelela kunye receptors peripheral, ngaloo ndlela ebangela kwekhono ngokwesondo, kukhokelela ekuncipheni amandla, iphuhlisa induku kunye gynecomastia. 'Cimetidine' kunokubangela yintloko, urhudo, myalgia kunye arthralgia, zezomzuzwana, ukwanda creatinine igazi, utshintsho hematological, CNS, inyathelo immunosuppressive, cardiotoxicity. H2 blocker III receptors isizukulwana histamine - "Famotidine" - singena ngaphantsi zibe ancedisana amalungu, ngokwenjenjalo nokunciphisa umthamo yeziphumo ebezingalindelekanga. Musa ukuba kwekhono ngesondo kunye amalungiselelo izizukulwana zexesha elizayo - "Ranitidine", "nizatidine", "roxatidine". bonke abasebenzisana kunye androgens.

iimpawu lokuthelekisa zamachiza

Inkcazo yezinto i blocker H2 histamine receptor (amayeza isizukulwana of extra-class), lo gama - "Ebrotidin" ngaphandle wabalaselisa "Ranitidine bismuth citrate" ayikho ngumxube elula, kunye ezimbaxa nezintsonkothileyo. Apha sekela - ranitidine - ezinxulumene vismusa ferric citrate.

Histamine H2 isizukulwana blocker III "Famotidine" receptors and II - "Ranitidine" - abe selectivity ngaphezu "cimetidine". Selectivity - le ngxaki yokusetyenziswa yedosi-oxhomekeke kunye isalamane. "Famotidine" yaye "ranitidine" uyamkhetha ngaphezu "Tsinitidin" ukusebenza H2 receptor. Xa kuthelekiswa, "famotidine" enamandla "Ranitidine" izihlandlo ezisibhozo, "Tsinitidina" - amaxesha amane. Umahluko sisebenza lilawulwa ngeedosi ezahlukeneyo ukulingana H2-blocker leyo ukuthobela kwezithandani of zehydrochloric acid. Amandla Iimbophelelo kunye receptors kwakhona limisela ixesha sesichengeni. Ukuba ichiza ubotshiwe ngamandla ukuya receptor dissociates kancinci kubangwa ifuthe ngexesha. Kwi secretion carcinomas "famotidine" ichaphazela eside kakhulu. Uphando lubonisa ukuba "cimetidine" kunciphisa secretion carcinomas ukuba iiyure ezi-5, "Ranitidine" - Iiyure 7-8, iiyure ezili-12 - "famotidine".

H2-blocker kuba iqela amachiza esibamba. Phakathi zonke izizukulwana, "cimetidine" ngaphantsi kwezinye esibamba, ngelixa obuphakathi lipophilic. Oku kwenza ukuba angene ngokulula amalungu ahlukeneyo, ifuthe H2-receptors, nto leyo ekhokelela kwiziphumo ebezingalindelekanga ezininzi. "Famotidine" yaye "Ranitidine" zithathwa esibamba kakhulu, bona musa ukungena laphu, pre-kwinjongp ifuthe lazo kwi H2 receptors iiseli Parietal.

Elona nani liphezulu yeziphumo ebezingalindelekanga kwi "Cimetidine". "Famotidine" yaye "Ranitidine", ngenxa yeenguqu kubume amachiza, musa kuchaphazela hepatic metabolizing enzyme ukunika iziphumo ebezingalindelekanga ezimbalwa.

indaba

Imbali yeli qela H2-blocker kwaqala ngo-1972. inkampani British elabhoratri phantsi kolwalathiso kaYakobi Blake uphando ukufaka inani enkulu iikhompawundi ukuba ezakheke efanayo zinemoletyhule zezi histamine. Xa iboniwe uqhagamshelwano olukhuselekileyo ukuba, ukuba anikezelwe kwizifundo zonyango. I buriamid blocker yokuqala akazange kakuhle kakhulu. isakhiwo yayo itshintshiwe, yajika metiamide. zophononongo zibonise ukusebenza ngokufanelekileyo, kodwa wabonisa zinetyhefu kakhulu, nto leyo ebonakaliswa ngokohlobo granulocytopenia. uphando kukhokelele oko kuye yavulwa "Cimetidine" (iziyobisi I sizukulwana). Eli chiza liye ngempumelelo ulingo lwezonyango evunywe ngo-1974. Ke into baqala ukusebenzisa blocker receptor H2 histamine xa kusenziwa lwezonyango, oku kuye kwaba mbuso Gastroenterology. Dzheyms Blek waba le kwafunyaniswa ibhaso yeNobel ngo-1988.

Inzululwazi ukuma ngxi. Ngenxa yeziphumo ebezingalindelekanga ezininzi "Cimetidine" pharmacologists baqalisa ukugcina uphendlo esiyimbali iikhompawundi ngempumelelo ngakumbi. Ngoko lavuleka kunye nezinye H2 histamine blocker ezintsha receptor. Iziyobisi ukunciphisa secretion, kodwa kuchaphazela mziba yayo (acetylcholine, gastrin). Iziphumo ezingalindelekanga, "ricochet acid 'ezijolise izazinzulu ukuba afune iindlela ezintsha ukunciphisa ubumuncu.

amayeza ephelelwe

Kukho udidi mihla lwamachiza - pump Proton inhibitors. Zingcono xa kislotopodavleniyu, ubuncinane ziziphumo ebezingalindelekanga, ixesha iziphumo H2 histamine receptor blocker. Iziyobisi, amagama ezidweliswe ngasentla, oko isasetyenziswa nangoku practice onyango kaninzi ngenxa yemfuza, ngenxa yezizathu zoqoqosho (it rhoqo "famotidine" okanye "Ranitidine").

Antisecretory iindlela mihla isicelo ukunciphisa ubungakanani zehydrochloric acid, yahlulwa ibe ziindidi ezibanzi ezimbini: inhibitors of kwimpompo protonic (PPI) kunye H2 blocker histamine receptor. amalungiselelo yokugqibela luphawulwa nefuthe tachyphylaxis xa yokwamkela ngokuphindaphindiweyo ebangela ukuhla isiphumo ngamayeza nokunyanga. Akukho API ukungathethi, ngoko, xa nshita blocker H2 acetyiswayo ukulungiselela unyango lwexesha elide.

Lo mkhuba tachyphylaxis xa uthatha H2 blocker baphawula ukususela ekuqaleni unyango kwisithuba seeyure 42. Xa unyango gastroduodenal isilonda ukopha akunconywa H2 blocker, ekhethwayo Proton pump inhibitors.

ukumelana

Kwezinye iimeko, blocker histamine H2 receptor (Ukuhlelwa kubonisiwe ngasentla) kwakunye namachiza PPI maxa wambi kunokubangela ukuxhathisa. Ekuqhubeni ezinjalo izigulane isisu esweni bume pH akasayi kubonakele naluphi na utshintsho kwinqanaba iasidi intragastric. Ngamanye amaxesha bekubona amatyala yokumelana naziphi blocker H2 iqela, izizukulwana-2 okanye ezi-3 okanye pump Proton inhibitors. Nokwandisa ithamo kwiimeko ezinjalo ayisebenzi, kufuneka ukhethe uhlobo olwahlukileyo iziyobisi. Ukufunda ezithile H2-blocker, omeprazole kunye (IPP) ibonisa ukuba ukususela kowoku-1 ukuya kwisi-5% of amatyala azikho utshintsho kule mihla pH-metry. In kusakhelwa olutshintshayo kwinkqubo yonyango acid kuthathwa ukuba icebo isebenzayo apho esweni pH Esophageal liphandisisiwe ekuqaleni, uze ngomhla yesihlanu nangeyesixhenxe zonyango. Ubukho kwezigulane nokumelana epheleleyo ibonisa ukuba practice lwezonyango, akukho chiza, oko kwakuza kuba ukusebenza ngokupheleleyo.

imiphumela emibi

Blocker histamine receptor iziphumo kubangela icala H2 abanezimo rhoqo. Sebenzisa 'Cimetidine "ebangela ukuba 3.2% amatyala. . "Famotidine - 1.3%," Ranitidine "- 2.7% Iziphumo ezingalindelekanga ziquka:

• Isiyezi, intloko ebuhlungu, ixhala, ukudinwa, ukozela, bedidekile, ingqondo, ukudakumba, ukuphazamiseka, ukuba nemibono, iintshukumo ihlale kuyo, ukungaboni.
• Arrhythmia kuquka bradycardia, tachycardia, arrythmia, asystole.
• Lurhudo okanye ukuqhina, iintlungu esiswini, ukugabha, isicaphucaphu.
• pancreatitis olunamandla.
• Hypersensitivity (fever, irhashalala, myalgia, anaphylaxis, arthralgia, erythema multiforme, nokudumba angioneurotic).
• Utshintsho esibindini iimvavanyo ezisebenzayo, enziwe okanye obubonakala holistaticheskie kwesibindi kunye senyongo okanye ngaphandle kwayo.
• creatinine Ukwandiswa.
• Ukutyeshelwa igazi (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, igazi aplastic kunye hypoplasia yobuchopho, igazi haemolytic Immune.
• Induku.
• Gynecomastia.
• Alopecia.
• yehle yobuntu.

Famotidine imiphumela kakhulu kwicala ithe iphecana zesisu, badla ukuphuhlisa urhudo, kwiimeko ezinqabileyo, phezu koko, kukho ukuqhina. Urhudo kwenzeka ngenxa yeziphumo antisecretory. Ngenxa yokuba imali zehydrochloric acid esiswini ehlile, ukunyuka pH. Kulo mzekelo, pepsinogen kancinci lujika lube pepsin, nto leyo inceda ndoyidiliza iiprothini. Ngenxa yesisu kuphazamisekile, yaye ngokufuthi andise urhudo.

Izimo

Ngu H2 blocker histamine receptor ziquka eziliqela iziyobisi, banayo Izimo zilandelayo:

• Yokuphazamiseka izintso wesibindi.
• Kwesibindi (isifo Encephalopathy portosystemic).
• Zisanyisa.
• Hypersensitivity ukuba nasiphi na isiyobisi kweli qela.
• Ukukhulelwa.
• Abantwana abaneminyaka ukuya kutsho kwiminyaka eli-14.

Intsebenziswano kunye namanye amachiza

Histamine H2 blocker receptor, leyo yindlela inyathelo ngoku baqonda ukuba nonxibelelwano pharmacokinetic iziyobisi ezithile.

Absorption esiswini. ukusebenza ngenxa antisecretory of H2-blocker bayakwazi ukuphembelela kukufakwa ichiza-electrolytes, apho kukho uxhomekeke kwi-pH, kuba machiza ukunciphisa iqondo kwe- kunye ionization. "Cimetidine" singanciphisa ukufunxeka izixhobo ezifana "Antipyrin" "ketoconazole" "Chlorpromazine" kunye amalungiselelo eliphezulu yentsimbi. Ukuze siphephe malabsorption ezinjalo, iziyobisi kufuneka kuthathwe kwiiyure 1-2 phambi kokuba ukusetyenziswa H2 blocker.

nethe Hepatic. H2 blocker histamine receptor (amachiza I sizukulwana ingakumbi) ukusebenzisana bayawafundisisa cytochrome P-450, nto leyo inqununu oxidizer isibindi. Kwisiqingatha ubomi iya kwandiswa, kwaye isiphumo wabonakalaliswa sprolongirovatsya libanda, beziyobisi leyo umzimba ngaphezu kwe-74%. Ngokomelela wasabela ngokuba cytochrome P-450 ongena "Cimetidine", ngaphezu amaxesha 10 ngaphezu "Ranitidine". Ukudibana ne "famotidine" nto eyenzekayo. Ngenxa yesi sizathu, xa usebenzisa i "Ranitidine" yaye "Famotidine" Akukho ukuhlukumeza yenzeka ngayo ukutya iziyobisi hepatic, okanye iboniswe kangangoko kancinane. Xa usebenzisa 'Cimetidine "kugqitywe ngayo iziyobisi ekuncipheni nama-40%, kwaye ngokwezonyango ebalulekileyo.

Izinga yokumpompoza kwegazi hepatic. Ngamana ukunciphisa hepatic ukuhamba kwegazi Velocity kwi-40% xa usebenzisa i "Cimetidine", yaye "Ranitidine" kunganciphisa kugqitywe prisistemnogo eliphezulu pathways iziyobisi. "Famotidine" kwezi meko ayitshintshi isantya sokuqukuqela kwegazi portal.

kukhuthaza Tubular sezintso. H2-blocker eksretiruyutsya kunye secretion esebenzayo sezintso tubular. Kule meko, intsebenziswano kunokwenzeka iziyobisi parallel ukuba ekskrektsiya kwenziwa iindlela efanayo. "Imetidin" yaye "Ranitidine" okwaziyo yokunciphisa ekskrektsiyu sezintso kwi-35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" akukho lutshintsho ephambili ekupheliseni kula machiza. Ngaphezu koko, umthamo wayo therapeutic iyakwazi ukunikezela xi eliphantsi kwi-plasma, singayi kakhulu ukukhuphisana namanye arhente kwi calcium of secretion.

ehlangana Pharmacodynamic. Ukudibana ne H2-blocker abanye amaqela iziyobisi antisecretory ekwaziyo yokwandisa ukusebenza enyangayo (umz, holinoblokatorami). Kunye nezenzi asebenze helicobacter (amalungiselelo metronidazole, bismuth, tetracycline, clarithromycin, amoxicillin), ibalekisa kuqhinwe izilonda Peptic.

intsebenziswano ezibi Pharmacodynamic xa zidibene iziyobisi lusekiwe, ezibandakanya testosterone. "Cimetidine" hormone wasuswa ukubopha receptors kwi-20% yoxinaniso plasma inyuswe. "Famotidine" yaye "Ranitidine" musa zibe noncedo olunjalo.

amagama trade

Kwilizwe lethu, ibhaliswe kwaye bavunyelwe ukuba athengise la machiza H2-blocker:

"Cimetidine"

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

"Ranitidine"

Amagama Trade: "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"

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

"Nizatidine". Igama Trade "Aksid".

"Roxatidine". Igama Trade "Roxane".

"Citrate bismuth Ranitidine". Igama Trade "Pilorid".