H2 olemba mabuku a histamine receptors: mayina a mankhwala

gulu Ichi ndi chimodzi mwa kukonzekera mankhwala a utsogoleri ndi wa kusankha akutanthauza zochizira matenda ulcerous. Kupezeka kwa H2 histamine cholandilira blockers pa zaka ziwiri zapitazi, imatengedwa waukulu mankhwala, kuthandiza kuthetsa chuma (angakwanitse mtengo) ndi mavuto. Chifukwa kukonzekera H2 blockers zotsatira za mankhwala a matenda chilonda akweza kwambiri, zikunena opaleshoni akhala akugwiritsidwa ntchito kamodzikamodzi ngati n'kotheka, khalidwe odwala a moyo bwino. "Cimetidine" chinatchedwa "golide muyezo" mu zilonda zam'mimba, "Ranitidine" mu 1998 anakhala ngwazi ya malonda mu mankhwala. Akhudza ndi mtengo wotsika, motero mphamvu ya mankhwala.

ntchito

H2 histamine cholandilira blockers ntchito zochizira matenda asidi zokhudzana m'mimba. Impact limagwirira - kutsekereza H2 maselo (mwinamwake amatchedwa histamine) ya maselo chapamimba mucosa. Pachifukwa ichi, yafupika kupanga ndi yobereka mu lumen wa acid amathiridwa muzituluka. Gulu la mankhwala zokhudza mankhwala antisecretory odana ndi chilonda.

Nthawi zambiri, H2 histamine cholandilira blockers ntchito milandu zilonda mawonetseredwe matenda chilonda. H2 blockers osati kuchepetsa kupanga acid amathiridwa, komanso ziletsa pepsin, ntchofu chapamimba Choncho kumawonjezera, pali chinawonjezeka kaphatikizidwe prostagladinov, kuchuluka katulutsidwe wa bicarbonate. Njinga ntchito ya m'mimba ndi dekhetsa, bwino microcirculation.

Zikuonetsa H2-blockers:

• gastroesophageal Reflux matenda;
• aakulu ndi pachimake kapamba;
• dyspepsia;
• Zollinger-Ellison syndrome;
• Reflux chovutika matenda kupuma;
• aakulu gastritis ndi duodenitis;
• kum'mero Barrett ndi;
• kugonjetsedwa zilonda esophageal mucosa;
• mmimba chilonda;
• ndi chilonda mankhwala symptomatic;
• aakulu dyspepsia ndi chifuwa ndi ululu epigastric;
• zokhudza zonse mastocytosis;
• chifukwa kupewa maganizo chilonda;
• syndrome Mendelson ndi;
• Kupewa chibayo chiyembekezo;
• magazi chapamwamba GI.

Histamine H2 cholandilira blockers: gulu la mankhwala

Pali gulu la gulu la mankhwala. Iwo agawidwa mu mabanja:

• Pakuti ine nkhawa m'badwo "cimetidine".
• "Ranitidine" - ndi blocker wa H2 histamine cholandilira II m'badwo.
• "Famotidine" amatanthauza m'badwo III.
• "Nizatidine" amatanthauza IV m'badwo.
• K V amatanthauza m'badwo "roxatidine".

"Cimetidine" wamng'ono hydrophilic, chifukwa ichi theka moyo ndi waufupi kwambiri, kwa chiwindi kagayidwe nthawi yomweyo waphindu. Blocker anachitira ndi cytochrome P-450 (microsomal enzyme) ndi mlingo kusintha kwa chiwindi xenobiotic kagayidwe. "Cimetidine" ndi woletsa chilengedwe kagayidwe kwa chiwindi mankhwala ambiri mwa. Pa nkhani imeneyi, ndi adakhoza kulowa mogwirizana ndi pharmacokinetic Choncho nkotheka kudzikundikira ndi mavuto ochuluka mavuto.

Pakati H2 blockers onse "cimetidine" bwino minofu malowedwe, amenenso zimabweretsa zotsatira kuchuluka mbali. N'kubweretsa amkati testosterone kwa kumanga ndi maselo a zotumphukira, motero kuchititsa kukanika kugonana, kumabweretsa kuchepa mu potency, akufotokozera mpheto ndi gynecomastia. "Cimetidine" zingachititse mutu, m'mimba, myalgia ndi arthralgia, chosakhalitsa, kuwonjezeka creatinine magazi, kusintha hematological, CNS, immunosuppressive kanthu, cardiotoxicity. H2 blocker III m'badwo histamine zolandilira - "Famotidine" - zochepa Chifalikira ku zimakhala ndi ziwalo, potero kucheperachepera kuchuluka kwa mavuto. Kodi si chifukwa kukanika kugonana ndi kukonzekera za mibadwo ya m'tsogolo - "Ranitidine", "nizatidine", "roxatidine". Onse a iwo kucheza ndi androgens.

Poyerekeza makhalidwe a mankhwala

Kumasulira kwa blockers H2 histamine cholandilira (mankhwala m'badwo wa owonjezera kalasi), dzina - "Ebrotidin" popanda anatsindika "Ranitidine bismuth citrate" si osakaniza osavuta, ndi pawiri zovuta. Apa kuyikapo - ranitidine - kugwirizana ndi ferric citrate vismusa.

Histamine H2 blocker m'badwo III "Famotidine" zolandilira ndi II - "Ranitidine" - ndi selectivity choposa "cimetidine". Selectivity - chodabwitsa cha mlingo amadalira ndi wachibale. "Famotidine" ndi "ranitidine" kusankha kuposa "Tsinitidin" zimakhudzanso H2 zolandilira. Yerekezani, "famotidine" wamphamvu "Ranitidine" nthawi zisanu ndi zitatu, "Tsinitidina" - makumi nthawi. Kusiyana mu mphamvu atsimikiziridwa malinga Mlingo osiyanasiyana pazikhala kufanana H2-blockers zomwe kanthu pa yimitsira asidi hydrochloric. Mphamvu ya kumangidwa ndi maselo komanso ndiyo nthawi kukhudzana. Ngati mankhwala kwambiri womangika kwa lilime la dissociates pang'onopang'ono chifukwa cha zotsatira za nthawi ya. Pa woyambira katulutsidwe "famotidine" amakhudza cholimba kwambiri. Kafukufuku amasonyeza kuti "cimetidine" kumachepetsa woyambira katulutsidwe kwa maola 5, "Ranitidine" - 7-8 maola, 12 maola - "famotidine".

H2-blockers a gulu la mankhwala hydrophilic. Mwa mibadwo yonse, "cimetidine" zosakwana hydrophilic ena, pamene amtengo lipophilic. Zimenezi zimathandiza kuti mosavuta mkatikati ziwalo zosiyanasiyana, mmene pa H2-zolandilira, imbaenda zotsatira ambiri mbali. "Famotidine" ndi "Ranitidine" amaonedwa kukhala kwambiri hydrophilic, iwo mkatikati nsalu, chisanadze emptive zimakhudza awo pa H2 maselo maselo parietal.

The pazipita angapo mavuto mu "cimetidine". "Famotidine" ndi "Ranitidine", chifukwa kusintha kapangidwe mankhwala, musati bwanji kwa chiwindi metabolizing michere ndi kupereka zotsatira ochepa mbali.

nkhani

Mbiri ya gulu la H2-blockers inayamba mu 1972. kampani British mu zasayansi motsogoleredwa ndi James Blake anafufuza apanga nambala yaikulu mankhwala amene amapanga ofanana molekyulu ali histamine. Kamodzi kugwirizana otetezeka akhala amadziŵika, iwo anaperekedwa m'manja mwa maphunziro matenda. Woyamba blocker buriamid sanali kwambiri. akuphatikizapo lasinthidwa, kunapezeka metiamide. maphunziro chipatala asonyeza efficacy wamkulu, koma anasonyeza kawopsedwe lalikulu limene akuwonetseredwa mu mawonekedwe a granulocytopenia. mudziwe zambiri zachititsa kuti zimene chatsegulidwa "cimetidine" (I m'badwo mankhwala). Mankhwala ali bwinobwino zapita mayesero matenda mu 1974 anavomereza izo. Ndiye chinachake anayamba ntchito H2 histamine cholandilira blockers kuchita matenda, zinali kusintha gastroenterology. Dzheyms Blek anali kwa kupezeka kwa Nobel Prize m'chaka cha 1988.

Science alibe kuima. Chifukwa zotsatira angapo mbali "cimetidine" pharmacologists nayamba kulisunga kusaka chosaiwalika cha mankhwala aluso. Choncho linatsegulidwa ndipo ena atsopano H2 histamine cholandilira blockers. Mankhwala kuchepetsa katulutsidwe, koma sikumangotikhudza ogalamutsa ake (acetylcholine, gastrin). Zotsatira zoyipa za mankhwalawa, "asidi ricochet" zochokera asayansi kufunafuna njira zatsopano kuchepetsa acidity.

mankhwala chakale

Pali kalasi ya makono ya mankhwala - zoletsa purotoni mpope. Iwo ali opambana mu kislotopodavleniyu, osachepera mavuto, nthawi zotsatira H2 histamine cholandilira blockers. Mankhwala, maina a amene tatchula, izo akadali ntchito mchitidwe matenda nthawi zambiri chifukwa chibadwa zifukwa zachuma (nthawi zambiri "famotidine" kapena "Ranitidine").

Antisecretory njira zamakono ntchito kuchepetsa asidi hydrochloric, anawagawa m'magulu awiri yotakata: ndi zoletsa ya mpope protonic (PPI) ndi H2 histamine cholandilira blockers. Kukonzekera otsiriza yodziwika ndi zotsatira za tachyphylaxis pamene mobwerezabwereza phwando amachititsa kuchepetsa zotsatira achire. Palibe API posowa Chotero, motsutsana ndi blockers H2 ali akulimbikitsidwa mankhwala yaitali.

Chodabwitsa tachyphylaxis pamene mukumwa H2 blockers anati kuyambira chiyambi cha mankhwala pasanathe maola 42. Mankhwalawa gastroduodenal magazi chilonda ali osavomerezeka H2 blockers, yochezera purotoni mpope zoletsa.

kukaniza

Nthawi zina, histamine H2 cholandilira blockers (gulu tanena) komanso PPI mankhwala amayambitsa ndi kukana. Kuchititsa ngati odwala m'mimba pH malo polojekiti si wapezeka kusintha kulikonse mu intragastric acidity mlingo. Nthawi zina wapezeka milandu kukana kwa gulu lililonse H2 blockers, mibadwo 2 kapena 3 kapena zoletsa purotoni mpope. Ndipo akawawonjezere mlingo mu Zikatero sachiza, inu muyenera kusankha mtundu wina wa mankhwala. Kuphunzira ena H2-blockers, omeprazole ndi (IPP) chimasonyeza kuti kuyambira 1 mpaka 5% milandu si kusintha mu tsiku pH-metry. Mu kuonerera zazikulu za ndondomeko ya mankhwala asidi imatengedwa kuti chiwembu kothandiza kwambiri komwe Esophageal pH polojekiti ndi ankafufuza poyamba, ndiyeno pa tsiku lachisanu ndi chiwiri la mankhwala. Kupezeka kwa odwala ndi kukana kwathunthu limasonyeza kuti mchitidwe matenda, palibe mankhwala, amene adzakhala ndi dzuwa mtheradi.

zotsatira zoyipazi

Blockers H2 histamine cholandilira zotsatira chifukwa mbali yosiyana pafupipafupi. Gwiritsani ntchito "cimetidine" kuwachititsa 3.2% ya milandu. . "Famotidine - 1.3%," Ranitidine "- 2,7% Zotsatira zoyipa monga:

• Chizungulire, kupweteka mutu, nkhawa, kutopa, kugona, osokonezeka, maganizo maganizo, mukubwadamuka, kuyerekezera zinthu m'maganizo, kayendedwe musanaganizire, amaona masomphenya.
• Arrhythmia kuphatikizapo bradycardia, tachycardia, arrythmia, asystole.
• Kutsekula m'mimba kapena kudzimbidwa, kupweteka m'mimba, kusanza.
• Pachimake kapamba.
• Hypersensitivity (malungo, zotupa myalgia, anaphylaxis, arthralgia, erythema multiforme, angioneurotic edema).
• Kusintha chiwindi mayesero zinchito, ziziwayendera kapena mawonetseredwe holistaticheskie chiwindi ndi matenda a chikasu ndiyo kapena popanda izo.
• Kuchuluka creatinine.
• Kupondelezedwa kwa magazi (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, aplastic magazi m'thupi ndi hypoplasia oziziritsa, haemolytic magazi m'thupi.
• Kusabala.
• Gynecomastia.
• Alopecia.
• utachepa libido.

Famotidine mavuto ambiri ali pa mundawo m'mimba, nthawi zambiri kutsekula m'mimba, mu nthawi zina, m'malo mwake, pali kudzimbidwa. M'mimba kumachitika chifukwa cha zotsatira antisecretory. Chifukwa chakuti chiwerengero cha acid amathiridwa mmimba amachepetsa, pH ukuwonjezeka. Pankhaniyi, pepsinogen pang'onopang'ono inasanduka pepsin, amene amathandiza kuphwanya mapuloteni. Chimbudzi akawinduka, ndipo nthawi zambiri akufotokozera m'mimba.

contraindications

Ndi H2 histamine cholandilira blockers monga nambala ya mankhwala, amene ali ndi contraindications zotsatirazi:

• Chisokonezo mu impso ndi chiwindi.
• Matenda enaake (portosystemic encephalopathy matenda).
• Mkaka wa m'mawere.
• Hypersensitivity kuti mankhwala aliyense wa gulu lino.
• Mimba.
• Ana a zaka mpaka zaka 14.

Mogwirizana ndi mankhwala ena

Histamine H2 cholandilira blockers, amene kanthu limagwirira tsopano anazindikira kuti ena ankachita pharmacokinetic mankhwala.

Mayamwidwe mmimba. Chifukwa antisecretory zotsatira za H2-blockers amatha kulimbikitsa mayamwidwe wa mankhwala electrolytes, pamene pali kudalira pH, chifukwa mankhwala akhoza kuchepa mlingo wa mayamwidwe ndi ionization. "Cimetidine" akhoza kuchepetsa mayamwidwe zipangizo monga "Antipyrin" "ketoconazole" "Chlorpromazine" ndi kukonzekera mkulu chitsulo. Kupewa malabsorption amenewa, mankhwala ayenera kumwedwa maola 1-2 pamaso ntchito ya H2 blockers.

Kwa chiwindi kagayidwe. H2 histamine cholandilira blockers (mankhwala Ine m'badwo makamaka) mwachangu kucheza ndi cytochrome P-450, amene ali wamkulu oxidizer chiwindi. Hafu ya moyo udzakhala wautali ndi mmene uoneke sprolongirovatsya ambiri osokoneza wa mankhwala amene zimapukusidwa ndi oposa 74%. Wamphamvu zonse anachitira ndi cytochrome P-450 akulowa "cimetidine", nthawi 10 kuposa "Ranitidine". Mogwirizana ndi "famotidine" sizikuchitika. Pachifukwa ichi, pamene ntchito "Ranitidine" ndi "Famotidine" palibe kuphwanya kumachitika a kagayidwe kwa chiwindi mankhwala, kapena imasonyezedwa Pamlingo pang'ono. Pamene ntchito "cimetidine" chilolezo cha mankhwala yafupika pafupifupi 40%, ndipo ndi kukomoka kwambiri.

Mlingo wa otaya kwa chiwindi magazi. Mwina kuchepa kwa chiwindi magazi mathamangidwe 40% pamene ntchito "cimetidine", ndi "Ranitidine" mwina ndichepe prisistemnogo mkulu kagayidwe kachakudya chilolezo cha mankhwala. "Famotidine" mu milandu sasintha mlingo wa otaya zipata magazi.

Tubular aimpso excretion. H2-blockers eksretiruyutsya ndi yogwira aimpso katulutsidwe tubular. Mu milandu, mogwirizana n'zotheka ndi mankhwala yomweyi ngati ekskrektsiya ikuchitika ndi njira zofanana. "Imetidin" ndi "Ranitidine" angathe kuchepetsa ekskrektsiyu aimpso kuti 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" alibe kusintha kuwonongedwa kwa mankhwala. Komanso, mlingo wake achire angathe kupereka ndende otsika mu plasma, amene sati kwakukulukulu kupikisana ndi wothandizila ena zimatiyika kashiamu wa katulutsidwe.

Pharmacodynamic ankachita. Mogwirizana ndi H2-blockers ena magulu antisecretory mankhwala angathe kuwonjezera achire efficacy (mwachitsanzo, holinoblokatorami). Mothandizana ndi nthumwi kuti kuchita helicobacter (kukonzekera za mankhwalawa bismuth, tetracycline, clarithromycin, amoxicillin), Iyamba Kuthamanga kumangika zilonda zilonda.

Pharmacodynamic chowawa zimachitika pamene pamodzi ndi mankhwala anakhazikitsa, monga testosterone. "Cimetidine" timadzi anathaŵa kumanga ndi maselo pa 20% ndende mu madzi ndi kuchuluka. "Famotidine" ndi "Ranitidine" alibe chotsatira.

maina malonda

Mu dziko lathu, mayina n'kulola kugulitsa mankhwala awa ali H2-blockers:

"Cimetidine"

maina 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 maina: "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"

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

"Nizatidine". Trade dzina "Aksid".

"Roxatidine". Trade dzina "Roxane".

"Ranitidine bismuth citrate". Trade dzina "Pilorid".