H2 histamine Kanotokonya blockers: mazita zvinodhaka

Boka iri nderimwe pakati mishonga kugadzirirwa kutungamirira ndowenyika Kusarudzwa zvinoreva pakurapa ulcerous zvirwere. Yawanikwa H2 histamine Kanotokonya blockers mumakore maviri adarika, runoonekwa makurusa mukurapa, kubatsira kugadzirisa zvemari (inokwanisika mutengo) uye zvinetso zvenzanga. Nokuda kugadzirira H2 blockers migumisiro yokurapa kuti urikanwi chirwere kwakavandudza zvinokosha, kuvhiya kupindira zvave zvishoma kazhinji sezvinobvira, unhu varwere 'upenyu akavandudzika. "Cimetidine" anonzi "yemandorokwati" pakurapa maronda, "Ranitidine" muna 1998 akava mudziviriri rokutengesa mu pharmacology. The guru anobatsirwei yakaderera cost, uye saka kubudirira zvinodhaka.

kushandiswa

H2 histamine Kanotokonya blockers akashandiswa pakurapa gastrointestinal zvirwere asidhi-ukama. matambudziko mashandiro - ichivharira H2 receptors (zvimwe vachinzi histamine) ari gastric mucosa masero. Nokuda kwechikonzero ichi, hazvina akaderedza kugadzirwa uye hurukuro kupinda lumen pamusoro gastric hydrochloric acid. boka iri zvinodhaka chokuita antisecretory Anti-urikanwi zvinodhaka.

Kazhinji, kuti H2 histamine Kanotokonya blockers zvinoshandiswa vanenge peptic urikanwi chirwere kuratidzwa. H2 blockers vasiri chete kuderedza kugadzirwa hydrochloric acid, asi tunodzivisa pepsin, saka gastric madzihwa kunowedzera, pane rwuchiwanzwa kwetunhu prostagladinov, vakawedzera secretion kuti bicarbonate. Motor basa mudumbu iri normalized, kunonatsiridza microcirculation.

Zvairatidza H2-blockers:

• gastroesophageal reflux chirwere;
• Pfungwa nomuviri zvemwana asati chisingaperi uye rikwanise;
• dyspepsia;
• Zollinger-Ellison urwere;
• reflux Kutemeswa kufema chirwere;
• chisingaperi gastritis uye duodenitis;
• Barrett kuti yegurokuro;
• kukundwa nemaronda esophageal mucosa,
• nomudumbu. urikanwi;
• uye symptomatic urikanwi zvinodhaka;
• chisingaperi dyspepsia ne chipfuva uye epigastric kurwadziwa;
• systemic mastocytosis;
• nokuti kudzivirirwa kunetseka urikanwi;
• Mendelson kuti urwere;
• Kudzivirira chido nemabayo;
• ropa repamusoro GI.

Histamine H2 Kanotokonya blockers: kupatsanura zvinodhaka

Pane kupatsanura boka iri zvinodhaka. Vari rakakamurwa mhuri:

• Nokuti ini chizvarwa zvaimunetsa "cimetidine".
• "Ranitidine" - mumwe blocker pamusoro H2 histamine Kanotokonya II chizvarwa.
• "Famotidine" rinoreva rudzi III.
• "Nizatidine" rinoreva IV chizvarwa.
• K V rinoreva chizvarwa "roxatidine".

"Cimetidine" muduku hydrophilic, nokuda ichi hafu-upenyu hupfupi chaizvo, hepatic muviri panguva iyoyo zvinovaka. Blocker vakaita pamwe cytochrome P-450 (microsomal enzayemu) pamwe neshanduko yevanhu hepatic xenobiotic muviri. "Cimetidine" ndiyo zvakasikwa inhibitor pamusoro hepatic muviri mishonga kupfuura pakati. Panyaya iyi, zviri kukwanisa kupinda pharmacokinetic kusakarongeka saka zvinoita kuwanda uye vakawedzera ngozi nemishonga.

Pakati zvose H2 blockers "cimetidine" nani zvinyama kupinda, izvo inoenda vawedzere marwadzo. Iye unotsiva endogenous testosterone kubva tichisunga pamwe peripheral receptors, nokudaro vachikonzera pabonde dysfunction, kunoita kuti vasanyanye potency, anovandudza kusabetsera uye gynecomastia. "Cimetidine" anogona kukonzera nomusoro, manyoka, myalgia uye arthralgia, zvinopfuura, kuwedzera creatinine ropa, hematological kuchinja, CNS, immunosuppressive chiito, cardiotoxicity. H2 blocker III rudzi histamine receptors - "Famotidine" - shoma Chinopinda kupinda nyama uye nhengo, nokudaro kudzikira uwandu nemishonga. Regai kukonzera zvepabonde dysfunction uye kugadzirirwa zvizvarwa - "Ranitidine", "nizatidine", "roxatidine". Vose regai kushamwaridzana androgens.

Okufananidza zvechadenga zvinodhaka

A rondedzero H2 histamine Kanotokonya blockers (mishonga chizvarwa mamwe-kirasi), zita - "Ebrotidin" voga pachena "Ranitidine bismuth citrate" hakusi nyore musanganiswa, uye kunzwisisa akakura. Pano vanovakira - ranitidine - chokuita ferric citrate vismusa.

Histamine H2 blocker chizvarwa III "Famotidine" receptors uye II - "Ranitidine" - vane selectivity kupfuura "cimetidine". Selectivity - the Chiitiko kuti dose-nemataundi uye hama. "Famotidine" uye "ranitidine" zvakawanda zvokusarudza kupfuura "Tsinitidin" kukanganisa H2-Kanotokonya. Kuenzanisa, "famotidine" simba "Ranitidine" kasere "Tsinitidina" - nguva makumi mana. The kusiyana simba takatsunga maererano mishonga yakasiyana-siyana pamusoro yokuenzana H2-blockers izvo kuita kudzvinyirira pakati hydrochloric acid. Simba zvisungo pamwe receptors uyewo kunotema ya chokupfeka. Kana mushonga wacho zvakasimba vakasungwa Kanotokonya dissociates zvishoma nezvishoma anokonzerwa nokuitika nguva. On the basal secretion "famotidine" kunokanganisa zvikuru yakasimba. Ongororo dzinoratidza kuti "cimetidine" kunoderedza basal secretion kwemaawa 5, "Ranitidine" - maawa 7-8, maawa 12 - "famotidine".

H2-blockers ndezvaJehovha boka hydrophilic zvinodhaka. Pakati kumarudzi, "cimetidine" shoma kupfuura mamwe hydrophilic, apo mwero lipophilic. Izvi zvinoita kuti zvinopfuura siyana zvomukati, zvakamubaya pamusoro H2-receptors, iyo inotungamira vazhinji nemishonga nyore. "Famotidine" uye "Ranitidine" vanoonekwa kuti zvikuru hydrophilic, havasi zvinopfuura rejira, pre-emptive kukanganisa kwavo pamusoro H2 receptors ose parietal masero.

The kunonyanyisa Kuwanda nemishonga mu "Cimetidine". "Famotidine" uye "Ranitidine" nokuda nokuchinja makemikari mamiriro, regai kukanganisa hepatic metabolizing makemikari uye kupa zvishoma nemishonga.

nyaya

Nhoroondo boka iri H2-blockers zvakatanga muna 1972. boka British murabhoritari vachitungamirirwa James Blake akaongorora uye synthesized akawandisa yeimwe vari zvayakaita yakafanana morekuru zviri histamine. Kamwe yakachengeteka kwokubatana vaizivikanwa, vakanga mumaoko yokuora zveBhaibheri. Yokutanga blocker buriamid haana chaizvo. nechivako Its rakachinjwa, ndokudzokera metiamide. Ongororo Clinical dzakaratidza zvikuru efficacy, asi akaratidza toxicity guru, iro kunoratidzwa muchimiro granulocytopenia. Kumwe kutsvakurudza chakaita kuti chii wakashamira "Cimetidine" (Ini chizvarwa zvinodhaka). The mushonga yakabudirira vakapfuura miedzo zvekuchipatara muna 1974 vanotenderwa izvozvo. Zvadaro chimwe chinhu vakatanga kushandisa H2 histamine Kanotokonya blockers mu kurapwa tsika zvakanga yechimurenga gastroenterology. Dzheyms Blek waiva kuwanikwa Nobel Prize muna 1988.

Science haadi mira. Nokuda vakawanda nemishonga "Cimetidine" pharmacologists akatanga kuchengeta muganhu kutsvaka hubudirire yeimwe. Saka yakavhurwa uye dzimwe itsva H2 histamine Kanotokonya blockers. Drugs kuderedza secretion, asi asingaiti kukanganisa muviri wayo (acetylcholine, gastrin). Nemishonga, "iine acid ricochet" nezvatinovavarira masayendisiti kutsvaga nzira itsva kuti kuderedza acidity.

chikare mushonga

Pane boka ano zvinodhaka - hwepurotoni pombi FIs. Ndivo vachipfuma kislotopodavleniyu, nokuti zvishoma parutivi kwemigumisiro, nguva migumisiro H2 histamine Kanotokonya blockers. Zvinodhaka, mazita ayo pamusoro apa, zviri zvichiri kushandiswa mune kurapwa tsika kazhinji nokuda genetics, nezvikonzero zvoupfumi (kakawanda nayo "famotidine" kana "Ranitidine").

Modern antisecretory yomuchipatara inoshandiswa kuderedza uwandu hydrochloric acid, vari huviri paupamhi makirasi: ari FIs ose protonic Pombi (PPI) uye H2 histamine Kanotokonya blockers. gadziriro okupedzisira vanoonekwa ne mugumisiro tachyphylaxis kana akadzokorora kugamuchirwa kunokonzera zvinoderedza iri mishonga chaizvoizvo. Hapana API iyi kushaiwa, saka, mukusiyana kuti H2 blockers vari pachii kurapa-refu.

Chiitiko pamusoro tachyphylaxis kana kutora H2 blockers vakachengeta kubva pakutanga yokurapa mumaawa. 42 In pakurapa gastroduodenal urikanwi ropa haisi varumbidzwa H2 blockers, nzvimbo hwepurotoni pombi FIs.

musimbwa

Mune zvimwe zviitiko, histamine H2 Kanotokonya blockers (kupatsanura apa) uyewo PPI zvinodhaka dzimwe nguva kuti kurwisa. In kuitisa dzakadaro varwere dumbu ph ezvinhu zvichiongororwa haina kuona chero kuchinja intragastric acidity pamwero. Dzimwe nguva padzakacherechedza zviitiko kurwisa chero boka H2 blockers, 2, kana 3 zvizvarwa kana hwepurotoni pombi FIs. Uye kuwedzera dose Muzviitiko zvakadaro zvikasashanda, unofanira kusarudza yakasiyana mhando zvinodhaka. Kudzidza mamwe H2-blocker uye omeprazole (IPP) chinoratidza kuti kubvira 1 kusvika 5% dzokushungurudzwa havasi kuchinja chamazuva ph-metry. Mune simba Kuongorora nedanho iine acid kurapwa ichaongororwa kuti zvikuru vakarongeka zano apo Esophageal ph zvichiongororwa iri kuongororwa pakutanga, uye zvino nezuva rechishanu uye rechinomwe zuva kurapwa. Kuvapo varwere kurwisa kwakakwana kunoratidza kuti muna kurapwa tsika, hapana mushonga, izvo kuti Mhedziso kunyatsoshanda.

nemishonga

Blockers H2 histamine Kanotokonya chikonzero nemishonga pamwe siyana maitikiro. Shandisa "Cimetidine" zvichiita kuti 3.2% nyaya. . "Famotidine - 1.3%," Ranitidine "- 2.7% Side Marwadzo dzinosanganisira:

• Dzungu, kutemwa nomusoro, kuzvidya mwoyo, kurukutika, hope, kuvhiringidzika, pfungwa, mwoyo, kushungurudzika, aone zvinhu zvisipo, involuntary kufamba, madzerere.
• Arrhythmia kusanganisira bradycardia, tachycardia, arrythmia, asystole.
• Manyoka kana kupatira, abdominal marwadzo, kurutsa, kuda kurutsa.
• Chenjera pfungwa nomuviri zvemwana asati.
• Hypersensitivity (fivha, mapundu, myalgia, anaphylaxis, arthralgia, erythema multiforme, angioneurotic edema).
• Aichinja chiropa dzichipfekeka miedzo, sezvaiita kana anokuzviratidza holistaticheskie chiropa pamwe jaundice kana pasina izvozvo.
• Inosimudzira creatinine.
• Kutyorwa ropa (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, aplastic kupererwa neropa uye chepfungwa hypoplasia, haemolytic kupererwa neropa Immune.
• Kusabetsera.
• Gynecomastia.
• Alopecia.
• ungaderedza libido.

Famotidine kupfuura marwadzo anenge ari nemudumbu, kazhinji kuva manyoka, muna zvisingawanzoitiki nguva nekusiyana, pane kupatira. Manyoka kunoitika pamusana antisecretory migumisiro. Nokuti kuti huwandu hydrochloric asidhi mudumbu zvinoderedza, kuti ph inowedzerawo. Saka pepsinogen zvishoma nezvishoma ichichinja pepsin, iyo inobatsira kukamurwa mapurotini. Kugaya akashatirwa, uye kazhinji anovandudza manyoka.

Contraindications

By H2 histamine Kanotokonya blockers zvinosanganisira zvinoverengeka zvinodhaka, vane zvinotevera contraindications:

• Kuvhiringidzika itsvo uye chiropa.
• Cirrhosis (portosystemic encephalopathy chirwere).
• Lactation.
• Hypersensitivity chero mushonga yeboka iri.
• Pregnancy.
• Vana vane makore kusvika makore 14.

Kudyidzana nevamwe zvinodhaka

Histamine H2 Kanotokonya blockers, iyo chiito mashandiro yava kunzwisisa kuti zvimwe pharmacokinetic zvinodhaka mukukurukurirana.

Absorção de Água mudumbu. Nokuda antisecretory mugumisiro H2-blockers vanokwanisa kupesvedzera Absorção de Água zvinodhaka-electrolytes, apo pane kuvimba pamusoro ph, nekuti zvinodhaka anogona kuchiderera mwero diffusion uye ionization. "Cimetidine" anogona kuderedza Absorção de Água kuti munowanika "Antipyrin" "ketoconazole" "Chlorpromazine" uye gadziriro dzakakwirira simbi. Kuti tidzivise malabsorption kwakadaro, zvinodhaka anofanira kutorwa maawa 1-2 pamberi kushandiswa H2 blockers.

Hepatic muviri. H2 histamine Kanotokonya blockers (zvinodhaka I chizvarwa kunyanya) vanoshingaira kushamwaridzana cytochrome P-450, inova huru oxidizer chiropa. The hafu-upenyu achawedzerwa nokuitika hwuratidzwe sprolongirovatsya ovhadhozi zvinodhaka iyo rinoita zvinopfuura 74%. Akasimba vose vakaita pamwe cytochrome P-450 anopinda "Cimetidine", 10 nguva kupfuura "Ranitidine". Kudyidzana ne "famotidine" haasi kuitika. Nokuda kwechikonzero ichi, apo uchishandisa "Ranitidine" uye "Famotidine" hapana kukanganisa kunoitika pakati hepatic zvinodhaka muviri, kana zviri kuratidzwa zvishoma pamwero. Kana kushandisa "Cimetidine" Clearance zvinodhaka akaderedzwa vangasvika 40%, uye akaora chinokosha.

Mwero ropa riyerere hepatic. Anogona kuderera hepatic ropa riyerere velocity kusvika 40% kana kushandisa "Cimetidine", uye "Ranitidine" anogona kuderera prisistemnogo yakakwirira metabolic Clearance zvinodhaka. "Famotidine" muzviitiko izvi haachinji mwero ropa riyerere portal.

Tubular renal excretion. H2-blockers eksretiruyutsya nokuva renal tubular secretion. Muzviitiko izvi, zvinobvira kusakarongeka pamwe inofambirana zvinodhaka kana ivo ekskrektsiya kuitwa chete zvigadziriswe. 'Imetidin "uye" Ranitidine "anokwanisa kuderedza renal ekskrektsiyu kusvika 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" asina kuchinja kuchaitwa zvinodhaka izvi. Uyezve, ayo kuchirapa dose anokwanisa kupa munhu pasi wevasungwa munguva plasma, chisingazozikamwi zvikuru kukwikwidzana nevamwe vamiririri iri karusiyamu kwevari secretion.

Pharmacodynamic mukukurukurirana. Kudyidzana pamwe H2-blockers vamwe antisecretory zvinodhaka mapoka anokwanisa kuwedzera kuchirapa efficacy (semuenzaniso, holinoblokatorami). Pamwe nevasori kuti ashandise helicobacter (kugadzirirwa metronidazole, bismuth, tetracycline, clarithromycin, amoxicillin), Inowedzera kuti tightening pamusoro peptic maronda.

Pharmacodynamic rwakashata kusakarongeka kana pamwe yakasimbiswa zvinodhaka, izvo zvinosanganisira testosterone. 'Cimetidine "kemikari Kubviswa kusunga pamwe receptors on 20% wevasungwa munguva yeplasma inowedzerwa. "Famotidine" uye "Ranitidine" haana zvakadaro zvakaitika.

tengeserana mazita

In nyika yedu, vakanyorwa uye akabvumira kuti kutengesa zvinodhaka ava H2-blockers:

'Cimetidine "

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

"Ranitidine"

Trade mazita: "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"

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

"Nizatidine". Trade zita "Aksid".

"Roxatidine". Trade zita "Roxane".

"Ranitidine bismuth citrate". Trade zita "Pilorid".