Histamine H2 yokwamukela blocker: amagama izidakamizwa

Leli qembu elilodwa phakathi amalungiselelo zemithi ekuholeni kungokwalabo Ukukhetha kusho ekwelapheni izifo ulcerous. Ukutholakala kwe-H2 histamine yokwamukela blocker kule minyaka engamashumi amabili, kubhekwa kwekulu imithi, ukusiza ukuxazulula kwezomnotho (engambi eqolo) nezinkinga zenhlalo. Ngenxa amalungiselelo H2 blocker imiphumela yokwelapha yesifo isilonda iye yathuthuka kakhulu, ukungenelela kuhlinzwa ziye zasetshenziswa kancane njalo ngangokunokwenzeka, izinga yeziguli zokuphila ngcono. "Cimetidine" esibizwa ngokuthi i "izinga legolide" e ekwelapheni izilonda, "Ranitidine" ngo-1998 baba iqhawe ukuthengiswa kwemithi. Inzuzo enkulu eziphansi, futhi ngaleyo ndlela ukusebenza izidakamizwa.

ukusetshenziswa

H2 histamine yokwamukela blocker esetshenziselwa ukwelapha izifo ezihlobene acid-emathunjini. umthelela indlela - ekuvimbeni H2 receptor (ngenye ukubizwa ngokuthi histamine) we esiswini mucosa amaseli. Ngenxa yalesi sizathu, kwanciphisela ukukhiqizwa futhi ukulethwa ku mafutha anciphisa isikhala esingaphakathi we esiswini hydrochloric acid. Leli qembu kwezidakamizwa kuhlobene izidakamizwa antisecretory anti-isilonda.

Ezimweni eziningi, le blocker H2 histamine yokwamukela asetshenziswa amacala peptic isifo isilonda ukubonakaliswa. H2 blocker kungukuthi kuphela ukwehlisa ukukhiqizwa hydrochloric acid, kodwa futhi zivimbele pepsin, ngaleyo ndlela isikhwehlela esiswini kwandisa, kukhulile zamagama prostagladinov, kukhuphuke uketshezi of Bicarbonate. Motor umsebenzi esiswini sibuyela kwesejwayelekile, kuthuthukisa microcirculation.

Izinkomba H2-blocker:

• gastroesophageal isifo Reflux;
• chronic pancreatitis acute;
• dyspepsia;
• Zollinger-Ellison syndrome;
• Reflux olubangelwa nezifo zokuphefumula;
• kolwelwesi chronic duodenitis;
• emphinjeni Barrett sika;
• ukunqotshwa izilonda mucosa ngomphimbo;
• isisu isilonda;
• futhi lingaze izidakamizwa isilonda;
• dyspepsia ezingamahlalakhona esifubeni ubuhlungu epigastric;
• mastocytosis letindzala;
• nokuvimbela ukucindezeleka isilonda;
• Mendelson Syndrome;
• Ukuvimbela nenshisekelo i-pneumonia,
• ukopha GI engenhla.

Histamine H2 yokwamukela blocker: ngezigaba izidakamizwa

Kukhona Ukwahlukaniswa leli qembu izidakamizwa. Basuke ihlukaniswe imindeni:

• Ngoba mina isizukulwane ukukhathazeka "cimetidine".
• "Ranitidine" - okuvimba of H2 histamine yokwamukela II isizukulwane.
• "Famotidine" libhekisela isizukulwane III.
• "Nizatidine" libhekisela IV isizukulwane.
• K V libhekisela isizukulwane "roxatidine".

"Cimetidine 'nomncane kunabo hydrophilic, ngenxa yalokhu isigamu-ukuphila kufushane kakhulu, umzimba hepatic ngesikhathi esifanayo okunenjongo. Blocker wasithukuthelela cytochrome P-450 (microsomal enzyme) nge ushintsho ngesilinganiso hepatic umzimba xenobiotic. "Cimetidine" kuyinto inhibitor jikelele umzimba hepatic izidakamizwa kakhulu phakathi. Kule ndaba, ikwazi ukungena nokuxhumana pharmacokinetic Ngakho kungenzeka abekwe okwandisa ingozi nemiphumela engathandeki yalawo maphilisi.

Phakathi kwabo bonke labo blocker H2 "cimetidine" izicubu Ukungena kangcono, nakho kuholela nemiphumela engemihle. Asusa testosterone endogenous kusukela ephonsa la mangqamuzana neuropathy, senze nezinkinga zobulili, kuholela ukwehla potency, eba namandla futhi gynecomastia. "Cimetidine" kungabangela ubuhlungu bekhanda, uhudo, myalgia futhi arthralgia, lezivakashi, ukwanda egazini creatinine, izinguquko hematological, CNS, isenzo immunosuppressive, cardiotoxicity. H2 blocker III isizukulwane histamine receptor - "Famotidine" - Bufinyelela kancane ku izicubu kanye izitho, kanjalo nokunciphisa inani amathuba okuba nemiphumela engemihle. Musa abangele nenkinga ocansini futhi unamasu izizukulwane ezizayo - "Ranitidine", "nizatidine", "roxatidine". Bonke musa uxhumana androgens.

izici ngokuqhathanisa izidakamizwa

Incazelo blocker H2 histamine yokwamukela (imithi isizukulwane extra-ekilasini), igama - "Ebrotidin" ngaphandle egqanyisiwe "Ranitidine bismuth citrate" akuyona inhlanganisela elula, futhi ekhuthaza eziyinkimbinkimbi. Lapha basekela - ranitidine - elihlobene ne ferric vismusa citrate.

Histamine H2 blocker isizukulwane III "Famotidine" receptor futhi II - "Ranitidine" - abe selectivity njengengcebo enkulu kunemicebo "cimetidine". Selectivity - lo mkhuba umthamo ancike isihlobo. "Famotidine" futhi "ranitidine" ekhetha ngaphezu "Tsinitidin" nomthelela H2 receptor. Ngokuqhathanisa, "famotidine" enamandla "Ranitidine" izikhathi eziyisishiyagalombili, "Tsinitidina" - izikhathi ezingamashumi amane. Umehluko sisebenza zinqunywa ngokwentando ngemithamo ezihlukahlukene kwefrakshini H2-blocker okuyinto isinyathelo nokucindezela hydrochloric acid. Amandla eboshwe kanye receptor futhi inquma ubude ukuchayeka. Uma izidakamizwa kakhulu nakanjani yokwamukela dissociates kancane kubangelwa umphumela isikhathi. On the basal uketshezi "famotidine" kuthinta isikhathi eside kunazo zonke. Ucwaningo lubonisa ukuthi "cimetidine" kunciphisa uketshezi basal phezu amahora 5, "Ranitidine" - amahora 7-8, amahora angu-12 - "famotidine".

H2-blocker uphakathi kwabantu abangenalo leli izidakamizwa hydrophilic. Phakathi zonke izizukulwane, "cimetidine" esingaphansi nezinye hydrophilic, kuyilapho ngokulinganisela lipophilic. Lokhu kwenza ukuba kalula zingene izitho ezihlukahlukene, umthelela H2-receptor, okuholela eminingi engemihle. "Famotidine" futhi "Ranitidine" abhekwa hydrophilic kakhulu, abazi zingene Indwangu, pre-emptive umthelela H2 receptor ka parietal amaseli.

Inombolo enkulu yemiphumela emibi e "Cimetidine". "Famotidine" futhi "Ranitidine", ngenxa yezinguquko isakhiwo zamakhemikhali, musa kuthinte hepatic metabolizing enzyme ukunikeza ayinayo imiphumela eminingi engemihle.

indaba

Umlando waleli qembu H2-blocker waqala ngo-1972. senkampani endaweni yokucwaninga ngaphansi kokuqondisa James Blake kucwaningwe kwemiqondo lenqwaba compounds ukuthi kukhona ikhipha efana molecule kukhona histamine. Kanye ukuxhumana okuphephile sezihlonziwe, zazinikezwa ukuba izifundo zokwelapha. Eyokuqala blocker buriamid kwakungelona ngempumelelo kakhulu. isakhiwo sayo kushintshiwe, sasiwumsebenzi metiamide. izifundo zokwelapha baye babonisa ngempumelelo enkulu, kodwa wabonisa ubuthi esikhulu, okungekho kubonakala ngesimo granulocytopenia. ukucwaninga okwengeziwe kwaletha siphi uvulekele "Cimetidine" (mina isizukulwane izidakamizwa). Umuthi isidlulile ngempumelelo zokwelapha e 1974 sivunyiwe ke. Khona-ke into waqala ukusebenzisa H2 histamine yokwamukela blocker ku practice emitholampilo, kwaba revolution Gastroenterology. Dzheyms Blek Lesi ukutholakala uMklomelo KaNobel ngo-1988.

Isayensi akemi namanje. Ngenxa amaningi side effects "Cimetidine" pharmacologists waqala ukugcina search mlando compounds ephumelela kakhudlwana. Ngakho-ke, lapho kwavulwa namanye amasha H2 histamine yokwamukela blocker. Izidakamizwa ukunciphisa uketshezi, kodwa akuphazamisi izinto ezisigcina yayo (acetylcholine, gastrin). Imiphumela engemihle, "Ricochet acid" ngamakhasimende ososayensi ukucinga izindlela ezintsha ukuze unciphise asidi.

imithi ephelelwe yisikhathi

Kukhona isigaba yesimanje izidakamizwa - proton futha inhibitor. Ziyakwazi baphakame kislotopodavleniyu, iminyaka engengaphansi side effects, isikhathi imiphumela H2 histamine yokwamukela blocker. Izidakamizwa, amagama abalwe ngenhla, isasetshenziswa umkhuba emtholampilo ngempela ngokuvamile ngenxa yezakhi zofuzo, ngenxa yezizathu zezomnotho (kaningi ke "famotidine" noma "Ranitidine").

izindlela Antisecretory yesimanje isetshenziswa inciphise hydrochloric acid, zihlukaniswe ngezigaba ezimbili ezibanzi: i-inhibitor of futha protonic (PPI) kanye H2 histamine yokwamukela blocker. amalungiselelo zokugcina zinezikhathi umphumela tachyphylaxis lapho reception okuphindaphindiwe kubangela kuncipha nomphumela oqabulayo. Akukho-API lokhu kuntuleka, ngakho-ke, ngokungafani kuya blocker H2 anconywe yokwelapha eside.

Lo mkhuba tachyphylaxis uma nithatha H2 blocker waphawula kusukela ekuqaleni ukwelashwa kungakapheli amahora 42. Ekwelapheni gastroduodenal isilonda ukopha is hhayi Kunconywa H2 blocker, i-proton encomekayo futha inhibitor.

ukumelana

Kwezinye izimo, histamine H2 yokwamukela blocker (ngezigaba kuboniswe ngenhla) kanye PPI izidakamizwa ngezinye izikhathi kubangele ukumelana. Ekuqhubeni ezinjalo iziguli esiswini pH imvelo lokuqapha ayitholiwe noma yiziphi izinguquko ku intragastric asidi ezingeni. Ngezinye izikhathi Kutholwe amacala ukumelana kunoma yiliphi iqembu H2 blocker, izizukulwane 2 noma ezingu-3 noma i-proton futha inhibitor. Futhi okwandisa umthamo ezimweni ezinjalo akusebenzi, udinga ukukhetha uhlobo oluhlukile izidakamizwa. Ukutadisha ezithile H2-blocker, omeprazole futhi (IPP) ebonisa ukuthi kusukela ku-1 kuya ku-5% amacala akuzona izinguquko nsuku zonke pH-metry. Ngo okwashiwo othakazelisayo inqubo yokwelapha acid ubhekwa isikimu kahle kunazo zonke lapho ngomphimbo zokuqapha pH amaphoyisa ayaphenya ngalolo daba ekuqaleni, bese kakhulu ngosuku lwesihlanu neyesikhombisa yokwelashwa. Ukuba khona iziguli ukumelana ephelele bubonisa ukuthi umkhuba emtholampilo, akukho izidakamizwa, okuyinto wayeyoba kahle ngokuphelele.

side effects

Blocker H2 histamine yokwamukela imbangela imiphumela emibi imvamisa obuhlukahlukene. Sebenzisa "Cimetidine" okubangela ukuba 3.2% of amacala. . "Famotidine - 1.3%," Ranitidine "- 2.7% Imiphumela engemihle zihlanganisa:

• Isiyezi, ubuhlungu bekhanda, ukukhathazeka, ukukhathala, ukozela, udidekile ingqondo, ukucindezeleka, ukuyaluza, ukuhhema, ukunyakaza okungalindelekile, angaboni kahle.
• Arrhythmia kuhlanganise bradycardia, tachycardia, arrythmia, asystole.
• Isifo sohudo noma ukuqunjelwa, ubuhlungu besisu, ukuhlanza okungapheli, isicanucanu.
• pancreatitis olunamandla.
• Hypersensitivity (imfiva, ukuqubuka, myalgia, anaphylaxis, arthralgia, erythema multiforme, edema angioneurotic).
• Izinguquko Ezenzeka isibindi ukuhlolwa kokusebenza, ezihlangene noma ukubonakaliswa holistaticheskie ukusha kwesibindi kohlobo ne-jaundice noma ngaphandle kwalo.
• creatinine Eliphakeme.
• Ukuphulwa igazi (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, anaemia aplastic futhi hypoplasia palsy, anaemia haemolytic Immune.
• Ubuthakathaka.
• Gynecomastia.
• Alopecia.
• kwehle libido.

Famotidine imiphumela emibi kakhulu uye ku pheshana emathunjini, ngokuvamile ukuthuthukisa uhudo, ezimweni ezingajwayelekile, kunalokho, kukhona ukuqunjelwa. Uhudo kwenzeka ngenxa imiphumela antisecretory. Ngenxa yokuthi inani hydrochloric acid esiswini incipha, ukwanda pH. Kulokhu, pepsinogen kancane liphenduka pepsin, esiza sokudiliza amaprotheni. Ukugaya kuyaphazamiseka, futhi ngokuvamile eba nesifo sohudo.

Izimo

Ngu H2 histamine yokwamukela blocker zibandakanya inombolo kwezidakamizwa, okuyinto unayo Izimo ezilandelayo:

• Yokuphazamiseka nezinso isibindi.
• Isifo sokusha (portosystemic encephalopathy isifo).
• Lactation.
• Hypersensitivity kunoma izidakamizwa yaleli qembu.
• Ukukhulelwa.
• Izingane ezineminyaka engu-kuze iminyaka 14.

Ukuxhumana nezinye izidakamizwa

Histamine H2 yokwamukela blocker, okuyinto isenzo indlela manje waqonda ukuba ekuhlanganyeleni okuthize pharmacokinetic izidakamizwa.

Absorption esiswini. umphumela Ngenxa antisecretory of H2-blocker bayakwazi ukuthonya ukumuncwa zomuthi-electrolyte, lapho kukhona ukuncika pH, ngoba izidakamizwa kungehlisa degree of okusheshayo futhi ionization. "Cimetidine" kunganciphisa ukumuncwa amathuluzi ezifana "Antipyrin" "ketoconazole" "Chlorpromazine" futhi okusezingeni eliphezulu yensimbi amalungiselelo. Ukuze ugweme malabsorption ezinjalo, izidakamizwa kumele kuthathwe 1-2 amahora ngaphambi ukusetshenziswa H2 blocker.

umzimba Hepatic. H2 histamine yokwamukela blocker (izidakamizwa mina isizukulwane ikakhulukazi) ngenkuthalo uxhumana cytochrome P-450, okuyinto uthishanhloko oxidizer isibindi. Ingxenye-ukuphila izokwenyuka, futhi umphumela ungase kubonakaliswe sprolongirovatsya ukweqisa izidakamizwa zomuthi okuyinto akheka ngaphezu kuka-74%. Stronger zonke wasithukuthelela cytochrome P-450 ingena "Cimetidine", izikhathi 10 ngaphezulu kakhulu 'Ranitidine ". Ukuxoxa "famotidine" ayenzeki. Ngenxa yalesi sizathu, uma usebenzisa "Ranitidine" futhi "Famotidine" kungekho ukuphulwa kwenzeka ka hepatic izidakamizwa umzimba, noma-ke uboniswa ngezinga kancane. Uma usebenzisa "Cimetidine" imvume izidakamizwa e encishisiwe cishe 40%, kanti isifo abalulekile.

Izinga hepatic ukugeleza kwegazi. Kwangathi wehlise hepatic ukugeleza kwegazi Isivinini 40% uma usebenzisa "Cimetidine", kanye "Ranitidine" kungehlisa izinga prisistemnogo okusezingeni eliphezulu imvume umzimba izidakamizwa. "Famotidine" kulezi zimo ayishintshi ngesilinganiso portal ukugeleza kwegazi.

Tubular excretion kwezinso. H2-blocker eksretiruyutsya esisebenzayo kwezinso uketshezi ijabulise. Kulezi zimo, ukuxhumana kungenzeka nge izidakamizwa parallel uma ekskrektsiya owenziwa izindlela ezifanayo. "Imetidin" futhi "Ranitidine" uyakwazi ukunciphisa ekskrektsiyu kwezinso kuya 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" ayinalo izinguquko ekuqedweni le mithi. Ngaphezu kwalokho, umthamo zayo zokwelapha uyakwazi ukuhlinzeka lokuhlushwa ongaphakeme e-plasma, okuyinto ngeke kakhulu ukuncintisana namanye amanxusa ku izinga le-calcium of uketshezi.

ekusebenzisaneni Pharmacodynamic. Ukuxoxa H2-blocker abanye izidakamizwa antisecretory amaqembu uyakwazi okwandisa kusebenta zokwelapha (isib holinoblokatorami). Inhlanganisela nge ejenti ukuthi isinyathelo helicobacter (unamasu metronidazole, bismuth tetracycline, clarithromycin, amoxicillin), ngesivinini kokuqina izilonda peptic.

Pharmacodynamic nokuxhumana enqabayo lapho kuhlangene izidakamizwa esungulwe, okuyinto zihlanganisa testosterone. "Cimetidine" i-hormone dengwane ephonsa receptor phezu 20% lokuhlushwa plasma luyanda. "Famotidine" futhi "Ranitidine" Awunayo mphumela.

amagama akho okuhweba

Ezweni lethu, ebhalisiwe bavunyelwe nokudayisa lezi mithi H2-blocker:

"Cimetidine"

amagama Trade: "Altramet", "Belomet", "Apo-cimetidine", "Yenametidin", "Gistodil", "tsimetin okusha", "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".

"Ranitidine bismuth citrate". igama Trade "Pilorid".