Histamine H2 receptor blockers: ingoa o taero

Tenei rōpū Ko tetahi i roto i te mau faaineineraa ho'oraa o te arata'iraa no ki te tikanga te kōwhiringa i roto i te maimoatanga o mate whai puku. Ko te kitea o te blockers receptor H2 histamine i roto i te tekau tau e rua kua pahure, whakaaro te te nui rawa i roto i te rongoa, te āwhina ki te whakaoti i te ōhanga (utu utu) me ngā raruraru pāpori. Nā ki teuteu H2 blockers hua o therapy o mate whewhe kua pai ake tino, kua wawaotanga hāparapara kua whakamahia iti pinepine rite taea, pai ake te kounga o te ora tūroro '. "Cimetidine" ka karanga te "paerewa koura" i roto i te maimoatanga o tuwhenua, "Ranitidine" i roto i 1998 ka te toa o hoko i roto i te Pūtaiao. Ko te painga nui he utu iti, a ko te kupu i te whai huatanga o te raau taero.

te whakamahi o

H2 blockers receptor histamine whakamahia mo te maimoatanga o pā-waikawa mate gastrointestinal. te huarahi pānga - ārai H2 receptors (te kore tuku ki rite histamine) o te pūtau mucosa pekitīlia. Hoki tenei take, heke reira production me tuku ki te lumen o te waikawa pūmāota pekitīlia. Tenei rōpū o taero e pā ana ki antisecretory taero anti-whewhe.

I roto i te nuinga o te wā, kei te whakamahia te blockers H2 histamine receptor i roto i te wā o mau faaiteraa mate whewhe keté. e kore e H2 blockers whakaiti anake te hanga o te waikawa pūmāota, engari tautāwhi i hoki pepsin, hūpē pekitīlia faarahi kupu, i reira te nui haere prostagladinov kōtuitanga, nui haere secretion o warorua. he tonu o Motor mahi o te puku, whakapiki i microcirculation.

Tuhinga H2-blockers:

• mate Reflux gastroesophageal;
• mau tonu, me te pancreatitis whakapeka;
• dyspepsia;
• Zollinger-Ellison syndrome;
• Reflux-piri mate romahā;
• gastritis ma'i me duodenitis;
• pū kai o Barrett;
• hinga tuwhenua mucosa esophageal;
• puku whewhe;
• me taero whewhe symptomatic;
• dyspepsia ma'i ki pouaka me te mamae epigastric;
• mastocytosis pūnahanaha;
• mo te ārai o te ahotea whewhe;
• syndrome o Mendelson;
• Prevention o wawata kakā;
• toto GI runga.

Histamine blockers H2 receptor: whakarōpū o taero

He he he whakarōpū o tenei rōpū o taero. E wehea ratou ki te mau utuafare:

• Hoki ahau whakatupuranga āwangawanga "cimetidine".
• "Ranitidine" - he pūārai o H2 histamine receptor II whakatupuranga.
• "Famotidine" e pā ana ki te whakatupuranga III.
• "Nizatidine" e pā ana ki te IV whakatupuranga.
• K V pā whakatupuranga "roxatidine".

"Cimetidine" te iti rawa hydrophilic, e tika ana ki tenei hawhe-ora he poto rawa, ka pākia ate i te wa ano e whai hua ana. ähua Kaipuru ki cytochrome P-450 (microsomal paru) ki te auau huringa o te pākia e xenobiotic ate. "Cimetidine" Ko te inhibitor ao o te pākia e ate o te nuinga o raau taero i roto i. I roto i tenei whakaaro, he mea e taea ki te tomo ki te pāhekoheko pharmacokinetic reira whakaeminga taea, me te nui haere tūponotanga o ngā pānga taha.

I roto i blockers H2 katoa "cimetidine" pai kătahi kikokiko, e arata'i hoki ki ngā pānga taha nui haere. whakakapi ia testosterone endogenous i here ki te mau farii ohipa piringa, ko te kupu meinga pōrearea fakasekisualé, arata'i ki te hekenga i roto i mananga, whakawhanake paruparu me te gynecomastia. "Cimetidine" Ka taea e meinga pāhoahoa, korere, myalgia me arthralgia, rangitahi, hua i roto i te toto creatinine, huringa hematological, CNS, mahi immunosuppressive, cardiotoxicity. H2 pūārai III receptors whakatupuranga histamine - "Famotidine" - iti te ô i ki te kopa me okana, reira whakaiti i te nui o ngā pānga taha. Kaua e meinga pōrearea fakasekisualé me taka o whakatupuranga heke mai - "Ranitidine", "nizatidine", "roxatidine". Katoa o ratou kore e taunekeneke ki androgens.

āhuatanga whakatairite o taero

He whakaahuatanga o te blockers H2 histamine receptor (rongoa whakatupuranga o anō-piha), te ingoa - "Ebrotidin" motu miramira "Ranitidine bismuth citrate" Ko e kore te ranunga ohie, me te pūhui matatini. Here fakatu'unga - ranitidine - e pā ana ki vismusa citrate ferric.

Histamine H2 pūārai whakatupuranga III "Famotidine" receptors me II - "Ranitidine" - E te selectivity nui atu te "cimetidine". Selectivity - te āhuatanga o te horopeta-ti'aturi, me te whanaunga. "Famotidine" me "ranitidine" ko atu whiriwhiri atu i te "Tsinitidin" pānga i runga i receptors H2. Na roto i te whakarite, "famotidine" kaha "Ranitidine" waru nga wa, "Tsinitidina" - e wha tekau nga wa. kua oti te whakarite nga rerekētanga i roto i te mana rite ki ngā pota o te ōritenga H2-blockers e mahi i runga i te pehanga o te waikawa pūmāota. whakatau hoki i te kaha o nga here ki nga receptors te roanga o te rongo. Ki te te kaha herea te tarukino ki te receptor dissociates āta meinga e te pānga o te roanga. I runga i te basal secretion "famotidine" pānga te roa tino. whakaatu Studies e "cimetidine" whakaiti secretion basal mō te 5 haora, "Ranitidine" - 7-8 haora, 12 haora - "famotidine".

no H2-blockers ki te rōpū o te raau taero hydrophilic. I roto i nga whakatupuranga katoa, "cimetidine" iti iho i te tahi atu hydrophilic, i tika lipophilic. āhei ana tēnei ki reira tomo ngāwari te ngā whekau, te pānga i runga i te H2-receptors, e arata'i ki maha ngā pānga taha. "Famotidine" me "Ranitidine" e whakaaro ki te kia tino hydrophilic, e kore ratou e ô i te papanga, i mua-kāwanatanga ratou pānga i runga i nga receptors H2 o ngā pūtau kōpako.

Ko te tau mōrahi o ngā pānga taha i roto i "Cimetidine". "Famotidine" me "Ranitidine", e tika ana ki ngā rerekētanga i roto i te hanganga matū, e kore e pā te ate metabolizing whākōkī, me te hoatu iti pānga taha.

kōrero

tīmata te hītori o tenei rōpū o H2-blockers i roto i 1972. kamupene Ingarangi i roto i te taiwhanga i raro i te aronga o Hemi Blake rangahautia ka synthesized he maha nui o pūhui e e te hanganga rite ki te rāpoi ngota he histamine. Kia Kua tāutuhia te hononga haumaru, i tukua e ratou i runga i ki rangahau haumanu. kihai i tino whai hua te buriamid pūārai tuatahi. Kua puta ke, kua tona hanganga, tahuri reira metiamide. Kua whakaaturia ngā Haumanu miramira nui, engari whakakitea te tāoke nui, whakakitea nei i roto i te puka o te granulocytopenia. Kua arahina rangahau atu ki i te mea kua whakatuwheratia "Cimetidine" (ahau whakatupuranga taero). Te raau Kua pai te haere tamataraa haumanu i roto i 1974 whakaaetia reira. Na ka anga te tahi mea ki te whakamahi i te blockers receptor H2 histamine i mahi haumanu, ko te reira i te revolution i roto i gastroenterology. ko Dzheyms Blek mo tenei kitea te Nobel i 1988.

e kore e Pūtaiao tu tonu. Nā ki ngā pānga taha maha timata "Cimetidine" pharmacologists ki te pupuri i te rapu te rohe mō pūhui whai hua atu. Na ka whakatuwheratia reira me ētahi atu blockers receptor H2 histamine hou. Drugs whakaiti te secretion, engari e kore e pā ona stimulants (acetylcholine, gastrin). ngā pānga taha, "ricochet waikawa" hāngai pūtaiao ki te rapu mō tikanga hou ki te whakaiti i te kawatanga.

rongoā tawhito

He he he piha hou o taero - inhibitors iraoho papu. He pai i roto i te kislotopodavleniyu ratou, mo te iti o ngā pānga taha, wā pānga H2 blockers histamine receptor. Drugs, nga ingoa o nei e whakarārangitia i runga ake, kua whakamahia te reira tonu i roto i te mahi haumanu rawa maha e tika ana ki te iranga, hoki take ōhanga (atu pinepine te reira "famotidine" ranei "Ranitidine").

tikanga hou Antisecretory tono ki te whakaiti i te nui o te waikawa pūmāota, kua wehea ki ngā akomanga whānui e rua: te inhibitors o papu protonic (ppi) me H2 blockers histamine receptor. Kei te āhuatanga e te pānga o tachyphylaxis ina ai fariiraa faahiti te whakaiti i roto i te pānga haumanu taka whakamutunga. Kahore he kahore API mo tenei kore, na reira, i roto i te rerekē ki te blockers H2 e tūtohutia hoki therapy wā roa-.

Ko te āhuatanga o tachyphylaxis ka tango H2 blockers kitea mai te timatanga o te therapy i roto i 42 haora. I roto i te maimoatanga o te toto whewhe gastroduodenal kore te H2 blockers, iraoho pai inhibitors papu tūtohutia.

ātete

I roto i ētahi wā, blockers histamine H2 receptor (whakarōpū tohua i runga ake) me te ppi taero meinga ētahi wā he ātete. I roto i te whakahaere i taua tūroro puku aroturuki taiao pH kore e kitea tetahi huringa i roto i te taumata kawatanga intragastric. I te tahi taime kitea take o ātete ki tetahi blockers rōpū H2, 2 ranei 3 whakatupuranga inhibitors iraoho papu ranei. A, te whakanui ake i te horopeta i roto i ngā take pērā kore e mahi, e hiahia ana koe ki te whiriwhiri i te momo rerekē o te tarukino. Te tai'oraa i etahi H2-blockers, omeprazole me (IPP) whakaatu e i te 1 ki te 5% o te take e kore e huringa i roto i te rā pH-metry. I roto i te kitea hihiri o te tukanga o te maimoatanga waikawa whakaaro te ki hei te kaupapa tino pai te wahi uiui, aroturuki pH Esophageal te i te tuatahi, a ka i te rima, me te whitu o maimoatanga te ra. Ko te aroaro o tūroro ki te ātete tino tohu e i roto i te mahi haumanu, i reira he kahore tarukino, e pai ai he pai tūturu.

pānga taha

Blockers H2 histamine receptor pānga taha take ki rerekē auau. Whakamahia "Cimetidine" meinga ratou ki 3.2% o te wā. . "Famotidine - 1.3%," Ranitidine "- 2.7% pānga taha ngā:

• Whanoke, pāhoahoa, manukanuka, rohirohi, te momoe, raruraru, hinengaro, korekore, rōpū,, moemoea, nekehanga tumu, kite te peroo.
• Arrhythmia tae atu bradycardia, tachycardia, arrythmia, asystole.
• Korere kōroke ranei, mamae puku, ruaki, whakapairuaki.
• pancreatitis whakapeka.
• Hypersensitivity (kirika, hikaka, myalgia, anaphylaxis, arthralgia, erythema multiforme, edema angioneurotic).
• Huringa i roto i te ate whakamātautau mahi, huri, faaiteraa ranei holistaticheskie kakā ki jaundice ranei kahore reira.
• creatinine nui ake.
• Maumaui o toto (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, anemia aplastic me hypoplasia kaka, anemia haemolytic Immune.
• Paruparu.
• Gynecomastia.
• Alopecia.
• heke libido.

Famotidine pānga tino taha kua runga i te wahi gastrointestinal, maha whakawhanake korere, i roto i ngā take onge, i runga i te anga ke, i reira he kōroke. puta korere no o ngā pānga antisecretory. Nā ki te meka e te nui o te waikawa pūmāota i roto i te kopu heke, te piki pH. I roto i tenei take, āta tahuri pepsinogen ki pepsin, e tauturu wahia iho pūmua. Kei te ohorere nakunaku, a maha whakawhanake korere.

contraindications

E H2 blockers histamine receptor ngā he maha o taero, e whai i nga contraindications e whai ake nei:

• Raruraru i roto i nga whatukuhu, me te ate.
• Cirrhosis (mate encephalopathy portosystemic).
• Hohipera.
• Hypersensitivity ki tetahi tarukino o tenei rōpū.
• Hapūtanga.
• pakeke tamariki ake ki te 14 tau.

Ngā pāhekoheko ki ētahi atu taero

blockers receptor Histamine H2, e matau nei mahi tikanga inaianei ki te whai i etahi taunekeneke pharmacokinetic tarukino.

Absorption i roto i te kopu. Nā pānga antisecretory o H2-blockers e taea ki te whakaawe i te absorption o te raau taero-electrolytes, te wahi i reira he he fakafalala i runga i te pH, no te mea taero e taea whakaiti i te tohu o te tūringiringi me ionization. "Cimetidine" taea te whakaiti i te absorption o taputapu pērā i "Antipyrin" "ketoconazole" "Chlorpromazine" me taka rino tiketike. Hei karo taua malabsorption, me raau taero e tangohia 1-2 haora i mua i te whakamahi o blockers H2.

pākia ate. H2 blockers histamine receptor (taero ahau whakatupuranga rawa) kaha taunekeneke ki cytochrome P-450, i te mea te ate oxidizer tino. Ka nui haere te hawhe-te ora, a ka kia whakakitea ai te pānga sprolongirovatsya tuwhena rawa o te raau taero metabolized nei e neke atu i te 74%. Kaha ähua katoa ki cytochrome P-450 tomo "Cimetidine", 10 nga wa neke atu i te "Ranitidine". e kore te Ngā pāhekoheko ki "famotidine" tupu. Hoki tenei take, ka whakamahi i te "Ranitidine" me "Famotidine" kahore ofatiraa puta o ka pākia tarukino ate, ranei kei te whakaaturia i te reira ki te whānuitanga iti. A, no te whakamahi i "Cimetidine" whakawātea o raau taero i roto i iti 40%, me he hauora nui.

Ko te auau o te rere toto ate. Kia whakaiti ate tere rere toto ki 40% i te whakamahi i te "Cimetidine", me "Ranitidine" kia whakaiti whakawātea pūkoro prisistemnogo nui o taero. "Famotidine" i roto i enei take e kore e huri i te auau o te rere toto tomokanga.

Tubular excretion tākihi. eksretiruyutsya H2-blockers ki hohe secretion tubular tākihi. I roto i enei take, pāhekoheko taea ki taero whakarara ki te ekskrektsiya kawea ratou i te taha o te taua tikanga. "Imetidin" me "Ranitidine" ahei o te whakaiti i te ekskrektsiyu tākihi ki te 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" e kore huringa i roto i te whakakorenga o aua taero. I tua atu, he ahei o te whakarato i te kukū iti i roto i te wē, e kore nei e te nuinga whakataetae ki ētahi atu māngai i roto i nga taumata konupūmā o secretion tona whängainga whakaora.

taunekeneke Pharmacodynamic. Ngā pāhekoheko ki H2-blockers ētahi atu rōpū taero antisecretory ahei o te whakanui ake i te miramira haumanu (hei tauira, holinoblokatorami). I ngā ki āpiha e mahi i runga i helicobacter (taka o metronidazole, bismuth, tetracycline, clarithromycin, amoxicillin), whakatere te tightening o keha keté.

taunekeneke kino Pharmacodynamic ka ngā ki pumau taero, e ngā testosterone. nui haere "Cimetidine" taiaki ngā i here ki receptors i runga i te 20% kukū i roto i te wē te. "Famotidine" me "Ranitidine" e kore e whai i te pānga taua.

ingoa hokohoko

I roto i to tatou whenua, rēhitatia me whakaaetia ki te hoko i enei taero e H2-blockers:

"Cimetidine"

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

"Ranitidine"

ingoa 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"

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

"Nizatidine". ingoa Trade "Aksid".

"Roxatidine". ingoa Trade "Roxane".

"Citrate bismuth Ranitidine". ingoa Trade "Pilorid".