Histamine H2 receptor blockers: cov npe ntawm cov tshuaj

Qhov no pab pawg neeg yog ib tug ntawm cov kws npaj ntawm cov leading belongs rau cov kev xaiv txhais tau tias nyob rau hauv cov kev kho mob ntawm ulcerous kab mob. Tus foundations ntawm cov H2 histamine receptor blockers nyob rau hauv lub dhau los lawm ob xyoo lawm, yog suav tias yog qhov loj tshaj plaws nyob rau hauv cov tshuaj, pab kom daws tau qhov economic (pheej yig tus nqi) thiab kev teeb meem. Vim npaj H2 blockers tau ntawm txoj kev kho ntawm lub rwj mob tau zoo ho, phais tiv thaiv tau siv tsawg heev li sai tau, tus neeg mob 'lub neej zoo zoo tuaj. "Cimetidine" hu ua "kub txheej txheem" nyob rau hauv cov kev kho mob ntawm ulcers, "Ranitidine" nyob rau hauv 1998 los ua tus zus ib ntawm kev muag khoom nyob rau hauv pharmacology. Qhov loj tshaj kom zoo dua yog tsis muaj nqi, thiab yog li cov hauj lwm zoo ntawm cov tshuaj.

kev siv cov

H2 histamine receptor blockers siv rau cov kev kho mob ntawm acid txog hnyuv kab mob. tej yam mechanism - thaiv cov hlab H2 receptors (txwv tsis pub xa mus rau raws li histamine) ntawm lub pais plab mucosa hlwb. Vim li no, nws txo ntau lawm thiab tus me nyuam mus rau hauv lub lumen ntawm pais plab hydrochloric acid. Qhov no pab pawg neeg ntawm cov tshuaj muaj feem xyuam rau antisecretory anti-rwj tshuaj.

Nyob rau hauv Feem ntau, lub H2 histamine receptor blockers yog siv nyob rau hauv tus neeg mob ntawm peptic rwj kab mob ces. H2 blockers tsis tsuas txo zus tau tej cov hydrochloric acid, tab sis kuj inhibit pepsin, pais plab hnoos qeev li no tsub kom, muaj yog nce synthesis prostagladinov, nce tso pa ntawm bicarbonate. Tsav muaj nuj nqi ntawm lub plab yog normalized, pab txoj kev microcirculation.

Indications H2-blockers:

• Gastroesophageal reflux kab mob;
• mob thiab mob pancreatitis;
• dyspepsia;
• Zollinger-Ellison syndrome;
• reflux hob pa kab mob;
• mob gastritis thiab duodenitis;
• Barrett tus txoj hlab nqos mov;
• swb ulcers esophageal mucosa;
• plab lub rwj;
• thiab symptomatic rwj tshuaj;
• mob dyspepsia nrog lub hauv siab thiab epigastric mob;
• mauj mastocytosis;
• rau kev tiv thaiv ntawm kev nyuaj siab rwj;
• Mendelson lub syndrome;
• Kev tiv thaiv ntawm aspiration mob ntsws;
• los ntshav sab sauv GI.

Histamine H2 receptor blockers: kev faib tshuaj

Muaj yog ib tug faib ntawm no pab pawg neeg ntawm cov tshuaj. Lawv muab faib ua cov tsev neeg:

• Kuv tiam kev txhawj xeeb "cimetidine".
• "Ranitidine" - ib tug blocker ntawm H2 histamine receptor II tiam.
• "Famotidine" yog hais txog lub cim III.
• "Nizatidine" yog hais txog IV tiam.
• K V hais txog tiam "roxatidine".

"Cimetidine" lub kawg hydrophilic, vim rau qhov cov ib nrab-lub neej yog heev luv luv, hepatic metabolism nyob rau tib lub sij hawm muaj nuj nqis. Blocker reacted nrog cytochrome P-450 (microsomal enzyme) nrog ib tug kev hloov tus nqi ntawm hepatic xenobiotic metabolism. "Cimetidine" yog ib tug universal inhibitor ntawm lub hepatic metabolism ntawm feem ntau cov tshuaj cov. Nyob rau hauv no hais txog, nws muaj peev xwm mus nkag rau hauv ib tug pharmacokinetic sis yog li ntawd tau tsub zuj zuj thiab nce kev txaus ntshai ntawm kev phiv.

Ntawm tag nrho H2 blockers "cimetidine" zoo dua cov ntaub so ntswg allergic, uas kuj ua rau yus muaj zog phiv. Nws ntau xyoo endogenous testosterone los ntawm losis tswvyim dabtsi nrog cov peripheral receptors, yog li yuav ua tau rau kev sib deev kawg, ua rau yus mus rau ib tug txo nyob rau hauv potency, npaj impotence thiab gynecomastia. "Cimetidine" yuav ua rau mob taub hau, raws plab, myalgia thiab arthralgia, nraum, nce nyob rau hauv cov ntshav creatinine, Hematological hloov, Cns, immunosuppressive txiav txim, cardiotoxicity. H2 blocker III tiam histamine receptors - "Famotidine" - tsawg penetrates mus rau hauv cov nqaij thiab kabmob, li no zuj zus lawm tus nqi ntawm cov kev phiv. Tsis txhob ua rau kev sib deev kawg thiab npaj rau yav tom ntej tiam - "Ranitidine", "nizatidine", "roxatidine". Tag nrho cov ntawm lawv tsis nrog androgens.

Comparative yam ntxwv ntawm cov tshuaj

Ib tug piav qhia ntawm lub H2 histamine receptor blockers (tshuaj tiam ntxiv-hauv chav kawm ntawv), lub npe - "Ebrotidin" apart tseem ceeb "Ranitidine Bismuth citrate" tsis yog ib tug yooj yim sib tov, thiab ib tug complex compound. Ntawm no pib - ranitidine - txuam nrog ferric citrate vismusa.

Histamine H2 blocker tiam III "Famotidine" receptors thiab II - "Ranitidine" - muaj ib tug ntau dua selectivity tshaj lub "cimetidine". Selectivity - lub phenomenon ntawm koob tshuaj-dependent thiab txheeb ze. "Famotidine" thiab "ranitidine" yog ntau xim tshaj ib tug "Tsinitidin" nyhuv on H2 receptors. Los ntawm kev sib piv, "famotidine" haib "Ranitidine" yim lub sij hawm, "Tsinitidina" - plaub caug lub sij hawm. Lub sib txawv nyob rau hauv dag zog yuam yog txiav txim raws li ntau yam koob tshuaj ntawm cov equivalence H2-blockers uas ua rau cov hluav ntawm hydrochloric acid. Lub zog ntawm txoj kev sib khi nrog lub receptors kuj txiav txim lub caij ntawm raug. Yog hais tias cov tshuaj yog xav ua txhua yam rau lub receptor dissociates maj mam yog tshwm sim los ntawm cov nyhuv ntawm lub caij. Nyob rau basal secretion "famotidine" muaj feem xyuam rau lub feem ntau check. Kev tshawb fawb qhia tau hais tias "cimetidine" thiaj li basal secretion rau 5 teev, "Ranitidine" - 7-8 teev, 12 teev - "famotidine".

H2-blockers mus rau cov pab pawg neeg ntawm hydrophilic tshuaj. Ntawm tag nrho tiam, "cimetidine" tsawg tshaj tus hydrophilic, thaum muaj mob pesnrab lipophilic. Qhov no enables nws mus tau yooj yim mus rau lub ntau yam kabmob, tej yam nyob rau H2-receptors, uas ua rau yus muaj ntau yam tshwm sim. "Famotidine" thiab "Ranitidine" pom tau hais tias yuav heev hydrophilic, lawv tsis txeem tau cov ntaub, pre-emptive lawv feem nyob rau H2 receptors ntawm parietal hlwb.

Qhov siab tshaj plaws pes tsawg tus ntawm cov kev phiv nyob rau hauv "Cimetidine". "Famotidine" thiab "Ranitidine", vim cov kev hloov nyob rau hauv lub tshuaj qauv, tsis txhob cuam tshuam rau hepatic metabolizing enzymes thiab muab tsawg phiv.

zaj dabneeg

Lub keeb kwm ntawm no pab pawg neeg ntawm H2-blockers pib nyob rau hauv 1972. British lub tuam txhab nyob rau hauv lub laboratory nyob rau hauv cov kev taw qhia ntawm James Blake researched thiab tsim ib tug lossis loj tus naj npawb ntawm cov tebchaw uas yog structurally xws li ib tug qauv yog histamine. Thaum ib tug muaj kev ruaj ntseg kev twb kev txuas tau lawm tias, lawv twb muab cob rau cov kev soj ntsuam kev tshawb fawb. Tus thawj blocker buriamid yog tsis zoo heev. Nws qauv tau hloov lawm, nws muab metiamide. Soj ntsuam kev tshawb fawb tau qhia ntau dua miv nyuas siv zug, tab sis pom zoo toxicity, uas yog manifested nyob rau hauv daim ntawv ntawm cov granulocytopenia. Ntxiv cov kev tshawb fawb tau coj mus rau dab tsi tau qhib "Cimetidine" (I tiam yeeb siv tshuaj). Cov tshuaj tau ntse dhau raug soj ntsuam nyob rau hauv 1974 kev pom zoo nws. Ces ib yam dab tsi pib mus siv lub H2 histamine receptor blockers nyob rau hauv cov kev soj ntsuam kev xyaum, nws yog ib tug kiv puag ncig nyob rau hauv Gastroenterology. Dzheyms Blek yog rau no discovery lub Nobel nqi zog nyob rau hauv 1988.

Science tsis sawv tseem. Vim ntau yam phiv "Cimetidine" pharmacologists pib kom lub landmark nrhiav rau ntau zoo sib txuas. Yog li ntawd nws twb qhib thiab lwm yam tshiab H2 histamine receptor blockers. Tshuaj txo lub tso pa tawm, tab sis tsis muaj kev cuam tshuam nws stimulants (acetylcholine, gastrin). Sab los, "acid ricochet" oriented zaum mus nrhiav tshiab txhais tau tias los txo cov acidity.

outdated tshuaj

Muaj yog ib tug niaj hnub chav kawm ntawv ntawm cov tshuaj - proton twj tso kua mis inhibitors. Lawv yog cov superior nyob rau hauv kislotopodavleniyu, rau ib tug tsawg kawg nkaus ntawm sab los, lub sij hawm los H2 histamine receptor blockers. Yeeb siv tshuaj, cov npe ntawm uas yog saum toj no, nws yog tseem siv nyob rau hauv saib mob xyaum ntau heev vim noob caj noob ces, rau economic vim li cas (ntau zaus nws "famotidine" los yog "Ranitidine").

Antisecretory niaj hnub txhais tau tias thov kom txo tus nqi ntawm cov hydrochloric acid, yog muab faib ua ob sab kawm: tus inhibitors ntawm protonic twj tso kua mis (PPI) thiab H2 histamine receptor blockers. kawg npaj yog yus muaj los ntawm cov nyhuv ntawm tachyphylaxis thaum rov txais tos ua rau ib tug txo nyob rau hauv lub kho nyhuv. Yog tsis muaj API rau no vim tsis, yog li ntawd, nyob rau hauv sib piv rau lub H2 blockers pom zoo rau kev ntev-lub sij hawm kev kho mob.

Cov tshwm sim ntawm tachyphylaxis thaum noj H2 blockers cai txij thaum pib ntawm txoj kev kho tsis pub dhau 42 teev. Nyob rau hauv cov kev kho mob ntawm gastroduodenal rwj los ntshav yog tsis pom zoo H2 blockers, nyiam proton twj tso kua mis inhibitors.

kuj

Nyob rau hauv tej rooj plaub, histamine H2 receptor blockers (kev faib qhia saum toj no) raws li PPI tshuaj tej zaum kuj ua rau ib tug tsis kam. Nyob rau hauv kev xws cov neeg mob plab pH puag ncig xyuas yog tsis kuaj cov kev hloov nyob rau hauv intragastric acidity theem. Tej zaum kuaj mob kuj rau tej pab pawg neeg H2 blockers, 2 los yog 3 tiam los yog proton twj tso kua mis inhibitors. Thiab ua cov tshuaj nyob rau hauv xws li mob tsis ua hauj lwm, koj yuav tsum tau xaiv ib tug txawv hom ntawm cov tshuaj. Kawm tej yam H2-blockers, omeprazole thiab (IPP) qhia tau hais tias los ntawm 1 mus rau 5% ntawm cov neeg yog tsis hloov nyob rau hauv lub hnub pH-metry. Nyob rau hauv lub dynamic kev soj xyuas tus txheej txheem ntawm acid kev kho mob yog pom tias yuav tau ntau npaum tswvyim qhov twg esophageal pH xyuas xyuas thaum xub thawj, thiab ces rau lub thib tsib thiab xya hnub ntawm kev kho mob. Lub xub ntiag ntawm cov neeg mob uas ua kom tiav kuj qhia tau hais tias nyob rau hauv kev soj ntsuam xyaum, muaj yog tsis muaj yeeb tshuaj, uas yuav muaj ib tug meej efficiency.

phiv

Blockers H2 histamine receptor ua phiv uas ua zaus. Siv "Cimetidine" ua rau lawv mus 3.2% ntawm cov neeg. . "Famotidine - 1.3%," Ranitidine "- 2.7% Sab los muaj xws li:

• Kiv taub hau, mob taub hau, ntxhov siab vim, qaug zog, nkees nkees, tsis meej pem, siab, kev nyuaj siab, ntxhov siab, hallucinations, tsis taw, qhov muag plooj tsis pom kev.
• Arrhythmia xws li bradycardia, tachycardia, arrythmia, asystole.
• Zawv plab los yog cem quav, mob plab, ntuav, xeev siab.
• Mob pancreatitis.
• Npau taws me ntsis (ua npaws, ua pob liab vog, myalgia, anaphylaxis, arthralgia, erythema multiforme, angioneurotic edema).
• Cov kev hloov nyob rau hauv daim siab haumxeeb kev ntsuam xyuas, zoo los yog ces holistaticheskie kab mob siab nrog daj ntseg los yog tsis muaj nws.
• Nce creatinine.
• Kev ua txhaum ntawm cov ntshav (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, aplastic anemia thiab cerebral hypoplasia, haemolytic anemia Immune.
• Impotence.
• Gynecomastia.
• Alopecia.
• tsis libido.

Famotidine feem ntau phiv tau rau tus mob huam, feem ntau tsim raws plab, nyob rau hauv uas tsis tshua muaj mob, nyob rau hauv tsis tooj, muaj cem quav. Zawv plab tshwm sim vim hais tias ntawm antisecretory los. Vim lub fact tias tus nqi ntawm hydrochloric acid nyob rau hauv lub plab decreases, lub pH qab. Nyob rau hauv cov ntaub ntawv no, pepsinogen maj mam dhau mus ua pepsin, uas yuav pab zom proteins. Plab zom mov yog ntxhov, thiab feem ntau muaj mob raws plab.

Contraindications

Los ntawm H2 histamine receptor blockers muaj xws li ib tug xov tooj ntawm cov tshuaj, uas muaj cov nram qab contraindications:

• Teeb nyob rau hauv lub ob lub raum thiab lub siab.
• Mob npuas paug (portosystemic encephalopathy kab mob).
• Lactation.
• Npau taws me ntsis rau tej tshuaj ntawm no pab pawg neeg.
• Cev xeeb tub.
• Cov me nyuam hnub nyoog mus txog rau 14 xyoo.

Sis nrog lwm yam tshuaj

Histamine H2 receptor blockers, uas txiav txim mechanism yog tam sim no to taub muaj tej yam pharmacokinetic tshuaj cov kev sib tshuam.

Haum nyob rau hauv lub plab. Vim antisecretory nyhuv ntawm H2-blockers yuav tau xyuam rau txoj haum ntawm cov tshuaj-electrolytes, qhov muaj yog ib tug nyob tos rau lub pH, vim hais tias cov tshuaj yuav ua tau kom cov neeg kawm ntawv ntawm diffusion thiab ionization. "Cimetidine" yuav txo tau lub haum ntawm cov cuab yeej xws li "Antipyrin" "ketoconazole" "Chlorpromazine" thiab siab hlau npaj. Kom tsis txhob zoo li no malabsorption, tshuaj yuav tsum tau noj 1-2 teev ua ntej yuav siv ntawm H2 blockers.

Hepatic metabolism. H2 histamine receptor blockers (tshuaj kuv tiam tshwj xeeb tshaj yog) koom nrog cytochrome P-450, uas yog tus thawj xib fwb oxidizer siab. Lub ib nrab-lub neej yuav nce, thiab cov nyhuv tej zaum yuav manifested sprolongirovatsya overdose ntawm cov tshuaj uas yog metabolized los ntawm ntau tshaj 74%. Muaj zog tag nrho reacted nrog cytochrome P-450 nkag mus rau "Cimetidine", 10 lub sij hawm ntau tshaj qhov "Ranitidine". Sis nrog "famotidine" yog tsis tshwm sim. Vim li no, thaum uas siv cov "Ranitidine" thiab "Famotidine" tsis muaj kev ua txhaum cai tshwm sim ntawm hepatic tshuaj metabolism, los yog nws yog qhia rau ib tug me ntsis raws li. Thaum uas siv cov "Cimetidine" clearance ntawm cov tshuaj nyob rau hauv txo kwv yees li 40%, thiab yog clinically tseem ceeb.

Tus nqi ntawm hepatic ntshav txaus. Yuav txo tau hepatic ntshav txaus tshaj tawm rau 40% thaum uas siv cov ib "Cimetidine", thiab "Ranitidine" tej zaum yuav txo tau prisistemnogo siab metabolic clearance ntawm cov tshuaj. "Famotidine" nyob rau hauv cov neeg mob tsis hloov tus nqi ntawm portal ntshav txaus.

Tubular raum feem. H2-blockers eksretiruyutsya nrog active raum tubular secretion. Nyob rau hauv cov neeg mob, tau kev sis raug zoo nrog thaum uas tig mus tshuaj yog hais tias lawv ekskrektsiya nqa tawm los ntawm tib lub mechanisms. "Imetidin" thiab "Ranitidine" muaj peev xwm ntawm kev txo lub raum ekskrektsiyu rau 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" muaj tsis muaj kev hloov nyob rau hauv lub tshem tawm ntawm cov tshuaj no. Tsis tas li ntawd, nws kho koob muaj peev xwm sawv ntawm kev muab ib tug tsawg concentration nyob rau hauv ntshav, uas yuav tsis raug kev lom zem ntau lwv nrog lwm cov neeg ua hauj nyob rau hauv lub poov hlau theem ntawm secretion.

Pharmacodynamic kev sib tshuam. Sis nrog H2-blockers lwm tus antisecretory tshuaj pab pawg muaj peev xwm zuj zus lub tshuaj miv nyuas siv zug (e.g., holinoblokatorami). Thaum lawv tseem nrog cov neeg ua hauj uas ua rau Helicobacter (npaj ntawm metronidazole, Bismuth, tetracycline, clarithromycin, amoxicillin), accelerates tus zawm ntawm peptic ulcers.

Pharmacodynamic phiv sis thaum ua ke nrog tsim tshuaj, uas muaj xws li testosterone. "Cimetidine" hormone moog los ntawm losis tswvyim dabtsi nrog receptors rau ib tug 20% nyob rau hauv concentration ntshav yog nce. "Famotidine" thiab "Ranitidine" tsis muaj li ib cov nyhuv.

pauv npe

Nyob rau hauv peb lub teb chaws, sau npe thiab tso cai rau muag cov tshuaj yog H2-blockers:

"Cimetidine"

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

"Ranitidine"

Trade npe: "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 npe: "Gasterogen", "Blokatsid", "Antodin", "Kvamatel", "gastrosidin", "Letsedil", "ulfamid", "Pepsidin", "Famonit", "Famotel", "Famosan", "Famopsin" "famotidine Agos", "Famotsid", "famotidine APO", "famotidine eVKAWJ".

"Nizatidine". Trade lub npe "Aksid".

"Roxatidine". Trade lub npe "Roxane".

"Ranitidine Bismuth citrate". Trade lub npe "Pilorid".