pab pawg no yog cov kev npaj tshuaj kho mob ua ntej, koom nrog txoj kev xaiv hauv kev kho mob peptic ulcers. Qhov kev tshawb pom ntawm H2 histamine receptor blockers nyob rau ob lub xyoo dhau los yog suav tias yog qhov loj tshaj plaws hauv cov tshuaj, pab daws kev lag luam (tus nqi pheej yig) thiab teeb meem hauv zej zog. Ua tsaug rau H2-blockers, cov txiaj ntsig ntawm kev kho mob peptic ulcers tau zoo tuaj, kev phais mob tau siv tsawg li ntau tau, thiab kev ua neej zoo ntawm cov neeg mob tau txhim kho. "Cimetidine" tau raug hu ua "tus qauv kub" hauv kev kho mob ntawm qhov txhab, "Ranitidine" hauv xyoo 1998 tau los ua tus tuav ntaub ntawv muag khoom hauv chaw muag tshuaj. Qhov loj ntxiv yog tus nqi qis thiab tib lub sijhawm ua haujlwm ntawm cov tshuaj.
Siv
H2 histamine receptor blockers yog siv los kho cov kab mob acid-dependent ntawm txoj hnyuv. Cov txheej txheem ntawm kev txiav txim yog qhov thaiv ntawm H2 receptors (lwm yam lawvhu ua histamine) hlwb ntawm lub plab mucosa. Vim li no, kev tsim khoom thiab nkag mus rau hauv lumen ntawm lub plab ntawm hydrochloric acid yog txo. Cov tshuaj no belongs rau cov tshuaj antisecretory antiulcer.
Feem ntau, H2 histamine receptor blockers yog siv rau qhov tshwm sim ntawm peptic ulcer. H2 blockers tsis tsuas yog txo qis kev tsim cov hydrochloric acid, tab sis kuj inhibit pepsin, thaum lub plab hnyuv nce, cov synthesis ntawm prostaglandins nce ntawm no, thiab tso tawm ntawm bicarbonates nce. Lub cev muaj zog ntawm lub plab yog normalized, microcirculation txhim kho.
Indications rau H2 blockers:
- Ygastroesophageal reflux;
- mob ntev thiab mob pancreatitis;
- dyspepsia;
- YZollinger-Ellison syndrome;
- kab mob ua pa reflux;
- mob plab thiab duodenitis;
- Barrett's esophagus;
- qhov txhab ntawm cov roj ntawm cov esophageal mucosa;
- plab plab;
- mob plab tshuaj thiab cov tsos mob;
- mob dyspepsia nrog retrosternal thiab epigastric mob;
- Ysystemic mastocytosis;
- rau kev tiv thaiv kev ntxhov siab;
- Mendelssohn's syndrome;
- tiv thaiv kab mob aspiration pneumonia;
- ntshav siab ntawm GI sab sauv.
H2 histamine receptor blockers: faib cov tshuaj
Muaj kev faib tawm ntawm pawg tshuaj no. Lawv muab faib los ntawm tiam:
- Rau kuv tiamhais txog Cimetidine.
- "Ranitidine" yog ib qho blocker ntawm H2 histamine receptors ntawm tiam II.
- Famotidine belongs rau tiam III.
- Nizatidin belongs rau tiam IV.
- Roxatidin belongs rau V tiam.
"Cimetidine" yog qhov tsawg tshaj plaws hydrophilic, vim qhov no, ib nrab-lub neej luv luv, thaum lub siab metabolism tseem ceeb. Cov blocker cuam tshuam nrog cytochromes P-450 (ib qho microsomal enzyme), thaum tus nqi ntawm cov metabolism hauv hepatic ntawm xenobiotic hloov. "Cimetidine" yog universal inhibitor ntawm hepatic metabolism ntawm feem ntau cov tshuaj. Hauv qhov no, nws muaj peev xwm nkag mus rau hauv cov tshuaj pharmacokinetic, yog li ntawd, kev sib sau ua ke thiab muaj kev pheej hmoo ntau ntxiv ntawm cov kev mob tshwm sim tuaj yeem ua tau.
Ntawm txhua H2 blockers, "Cimetidine" nkag mus rau cov ntaub so ntswg zoo dua, uas tseem ua rau muaj kev phiv ntau ntxiv. Nws displaces endogenous testosterone los ntawm nws kev twb kev txuas nrog peripheral receptors, yog li ua rau kev sib deev tsis ua hauj lwm, ua rau ib tug txo nyob rau hauv potency, tsim impotence thiab gynecomastia. "Cimetidine" tuaj yeem ua rau mob taub hau, raws plab, ntuav myalgia thiab arthralgia, nce ntshav creatinine, hematological hloov pauv, CNS qhov txhab, cov teebmeem tiv thaiv kab mob, cov teebmeem cardiotoxic. Blocker H2 histamine receptors III tiam - "Famotidine" - tsawg nkag mus rau hauv cov ntaub so ntswg thiab kabmob, yog li txo cov kev mob tshwm sim. Tsis ua rau kev sib deev tsis zooKev npaj ntawm cov tiam tom ntej - "Ranitidine", "Nizatidin", "Roxatidin". Tag nrho cov ntawm lawv tsis cuam tshuam nrog androgens.
Cov yam ntxwv sib piv ntawm cov tshuaj
Muaj cov lus piav qhia ntawm H2 histamine receptor blockers (kev npaj ntawm lub cim ntxiv), lub npe yog "Ebrotidine", "Ranitidine bismuth citrate" yog singled tawm, qhov no tsis yog ib qho yooj yim sib tov, tab sis ib tug complex compound.. Ntawm no lub hauv paus - ranitidine - khi rau trivalent bismus citrate.
Blocker H2 histamine receptors III tiam "Famotidine" thiab II - "Ranitidine" - muaj kev xaiv ntau dua li "Cimetidine". Selectivity yog ib koob tshuaj-dependant thiab txheeb ze tshwm sim. "Famotidine" thiab "Ranitidine" xaiv ntau dua "Cinitidine", cuam tshuam rau H2 receptors. Rau kev sib piv: "Famotidine" yog yim lub sij hawm ntau zog tshaj "Ranitidine", "Cinitidine" yog plaub caug npaug zog dua. Qhov sib txawv ntawm potency yog txiav txim los ntawm koob tshuaj sib npaug cov ntaub ntawv ntawm txawv H2 blockers uas cuam tshuam rau hydrochloric acid suppression. Lub zog ntawm kev sib txuas nrog receptors kuj txiav txim siab lub sijhawm ntawm kev raug. Yog hais tias cov tshuaj muaj zog khi rau lub receptor, dissociates maj mam, lub sij hawm ntawm cov nyhuv yog txiav txim. Nyob rau basal secretion "Famotidine" cuam tshuam qhov ntev tshaj plaws. Cov kev tshawb fawb qhia tias "Cimetidine" muab qhov txo qis hauv basal secretion rau 5 teev, "Ranitidine" - 7-8 teev, 12 teev - "Famotidine".
H2-blockers yog cov pab pawg ntawm cov tshuaj hydrophilic. Ntawm txhua tiam neeg, Cimetidine tsis tshua muaj dej ntau dua li lwm tus, thaum muaj lipophilic tsawg. Qhov no ua rau nws muaj peev xwm nkag mus rau hauv ntau yam kabmob, cuam tshuam rau H2 receptors, uas ua rau muaj ntau yam kev phiv. "Famotidine" thiab "Ranitidine" yog suav tias yog hydrophilic heev, lawv nkag mus rau hauv cov ntaub so ntswg tsis zoo, lawv cov txiaj ntsig tseem ceeb ntawm H2 receptors ntawm parietal hlwb.
Tus lej siab tshaj ntawm cov kev mob tshwm sim hauv "Cimetidine". "Famotidine" thiab "Ranitidine", vim muaj kev hloov pauv hauv cov qauv tshuaj, tsis cuam tshuam rau metabolizing daim siab enzymes thiab muab cov kev mob tshwm sim tsawg dua.
History
Keeb kwm ntawm pawg H2-blockers no tau pib xyoo 1972. Ib lub tuam txhab Askiv hauv chav kuaj hauv qab kev coj noj coj ua ntawm James Black tau tshawb xyuas thiab tsim cov khoom sib txuas ntau uas zoo sib xws hauv cov qauv rau cov tshuaj histamine molecule. Thaum pom cov tshuaj tiv thaiv kev nyab xeeb, lawv raug xa mus rau kev sim tshuaj. Thawj thawj buriamid blocker tsis zoo tag nrho. Nws cov qauv tau hloov pauv, methiamide tig tawm. Cov kev tshawb fawb soj ntsuam tau pom tias muaj txiaj ntsig zoo dua, tab sis muaj kev lom ntau dua tau tshwm sim nws tus kheej, uas tshwm sim nws tus kheej hauv daim ntawv ntawm granulocytopenia. Cov hauj lwm ntxiv tau coj mus rau qhov kev tshawb pom ntawm "Cimetidine" (Kuv tiam ntawm cov tshuaj). Cov tshuaj tau dhau qhov kev sim ua tiav, xyoo 1974 tau pom zoo. Ces lawv los uasiv histamine H2 receptor blockers nyob rau hauv kev kho mob xyaum, nws yog ib tug kiv puag ncig nyob rau hauv gastroenterology. James Black tau txais Nobel nqi zog xyoo 1988 rau qhov kev tshawb pom no.
Kev tshawb fawb tsis nyob twj ywm. Vim muaj ntau yam kev mob tshwm sim ntawm Cimetidine, cov kws kho mob tau pib tsom mus nrhiav cov tshuaj zoo dua. Yog li lwm yam tshiab H2 blockers ntawm histamine receptors tau tshawb pom. Cov tshuaj txo qis qis, tab sis tsis cuam tshuam rau nws cov stimulants (acetylcholine, gastrin). Cov kev mob tshwm sim, "acid rebound" cov kws tshawb fawb los tshawb nrhiav tshiab txhais tau tias txo acidity.
Cov tshuaj tsis siv tshuaj
Muaj ntau cov tshuaj niaj hnub no hu ua proton twj tso kua mis inhibitors. Lawv yog cov zoo tshaj nyob rau hauv cov kua qaub, nyob rau hauv qhov tsawg kawg nkaus ntawm kev phiv, nyob rau hauv lub sij hawm ntawm raug rau histamine H2 receptor blockers. Cov tshuaj uas nws cov npe teev saum toj no tseem siv tau ntau zaus hauv kev kho mob vim yog caj ces, rau kev lag luam (feem ntau nws yog "Famotidine" lossis "Ranitidine").
Cov tshuaj tiv thaiv niaj hnub siv los txo cov tshuaj hydrochloric acid tau muab faib ua ob pawg loj: proton twj tso kua mis inhibitors (PPIs), nrog rau H2 histamine receptor blockers. Cov tshuaj tom kawg yog tus cwj pwm los ntawm cov txiaj ntsig ntawm tachyphylaxis, thaum rov ua haujlwm ua rau txo qis hauv kev kho mob. PPIs tsis muaj qhov tsis zoo no, yog li lawv raug pom zoo rau kev kho mob ntev, tsis zoo li H2 blockers.
Qhov tshwm sim ntawm kev txhim kho ntawm tachyphylaxis thaum noj H2-blockers tau pom txij thaum pib kho hauv 42 teev. Nyob rau hauv kev kho mob ntawm gastroduodenal ulcer los ntshav, nws tsis pom zoo kom siv H2-blockers, nyiam yog muab rau proton twj tso kua mis inhibitors.
Txhob Cia Siab
Histamine H2 receptor blockers (qhia tawm saum toj no) thiab PPIs qee zaum ua rau muaj kev tawm tsam hauv qee kis. Thaum saib xyuas pH ntawm lub plab ib puag ncig hauv cov neeg mob zoo li no, tsis muaj kev hloov pauv hauv qib ntawm intragastric acidity raug kuaj pom. Qee zaum cov xwm txheej ntawm kev tiv thaiv rau ib pawg ntawm H2 blockers ntawm 2nd lossis 3rd tiam los yog kuaj pom proton twj tso kua mis inhibitors. Ntxiv mus, nce koob tshuaj nyob rau hauv xws li mob tsis muab ib tug tshwm sim, nws yog tsim nyog los xaiv ib tug txawv hom tshuaj. Kev tshawb fawb ntawm qee qhov H2-blockers, nrog rau omeprazole (PPI) qhia tau hais tias los ntawm 1 txog 5% ntawm cov neeg mob tsis muaj kev hloov pauv hauv pH-metry txhua hnub. Nrog rau kev saib xyuas zoo ntawm cov txheej txheem ntawm kev kho cov kua qaub dependence, feem ntau rational tswvyim yog xam, qhov twg txhua hnub pH-metry yog kawm nyob rau hauv thawj, thiab ces nyob rau hauv lub thib tsib thiab xya hnub ntawm kev kho mob. Lub xub ntiag ntawm cov neeg mob uas muaj kev tiv thaiv tiav qhia tau hais tias hauv kev kho mob tsis muaj tshuaj uas yuav muaj txiaj ntsig zoo.
Side effects
H2 histamine receptor blockers ua rau muaj kev phiv nrog ntau zaus. Kev siv "Cimetidine" ua rau lawv nyob rau hauv 3, 2% ntawm cov neeg mob. Famotidine - 1.3%,"Ranitidine" - 2.7%. Cov kev mob tshwm sim muaj xws li:
- kiv taub hau, mob taub hau, ntxhov siab vim, qaug zog, tsaug zog, tsis meej pem, kev nyuaj siab, ntxhov siab, hnov lus, tsis xav txav, pom kev cuam tshuam.
- Arrhythmia, suav nrog bradycardia, tachycardia, extrasystole, asystole.
- Zoo los yog cem quav, mob plab, ntuav, xeev siab.
- Tus mob pancreatitis.
- Hypersensitivity (ua npaws, tawm pob, myalgia, anaphylactic shock, arthralgia, erythema multiforme, angioedema).
- Kev hloov pauv hauv daim siab ua haujlwm, sib xyaw lossis holistic kab mob siab nrog lossis tsis muaj jaundice.
- siab creatinine.
- Cov kab mob hematopoietic (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, aplastic anemia thiab cerebral hypoplasia, hemolytic immune anemia.
- Impotence.
- Gynecomastia.
- Alopecia.
- Txuag libido.
Famotidine muaj feem cuam tshuam rau hauv plab hnyuv, nrog raws plab feem ntau tshwm sim, tsis tshua muaj, ntawm qhov tsis sib xws, cem quav tshwm sim. Mob plab tshwm sim vim muaj cov nyhuv antisecretory. Vim qhov tseeb tias cov tshuaj hydrochloric acid nyob rau hauv lub plab txo qis, pH qib nce. Hauv qhov no, pepsinogen maj mam hloov mus rau pepsin, uas pab zom cov protein. Kev zom zaub mov tsis zoo, thiab feem ntau raws plab tshwm sim.
YContraindications
To H2 blockershistamine receptors suav nrog ntau cov tshuaj uas muaj cov hauv qab no contraindications rau kev siv:
- Kev cuam tshuam hauv lub raum thiab lub siab.
- Cirrhosis ntawm daim siab (keeb kwm ntawm portosystemic encephalopathy).
- Lactation.
- Hypersensitivity rau ib yam tshuaj nyob rau hauv pawg no.
- Kev cev xeeb tub.
- Cov menyuam yaus hnub nyoog qis dua 14.
Sib tham nrog lwm yam cuab yeej
H2 blockers ntawm histamine receptors, lub tswv yim ntawm kev ua ntawm uas tam sim no nkag siab, muaj qee yam tshuaj pharmacokinetic kev sib cuam tshuam.
Absorption hauv plab. Vim yog cov teebmeem antisecretory ntawm H2 blockers, lawv muaj peev xwm cuam tshuam rau kev nqus ntawm cov tshuaj electrolyte qhov twg muaj kev vam khom ntawm pH, vim tias qib ntawm diffusion thiab ionization yuav txo qis hauv cov tshuaj. "Cimetidine" tuaj yeem txo qhov nqus ntawm cov tshuaj xws li "Antipyrin", "Ketoconazole", "Aminazin" thiab ntau yam kev npaj hlau. Txhawm rau zam qhov tsis zoo li no, cov tshuaj yuav tsum tau noj 1-2 teev ua ntej siv H2 blockers.
Hepatic metabolism. Blockers ntawm H2 histamine receptors (kev npaj ntawm thawj tiam tshwj xeeb) nquag cuam tshuam nrog cytochrome P-450, uas yog lub ntsiab oxidizer ntawm lub siab. Nyob rau tib lub sij hawm, ib nrab-lub neej nce, cov nyhuv yuav ntev thiab ib tug overdose ntawm cov tshuaj, uas yog metabolized los ntawm ntau tshaj 74%, tej zaum yuav tshwm sim. Cimetidine ua rau muaj zog tshaj plaws nrog cytochrome P-450, 10 npaug ntau dua Ranitidine. Kev sib cuam tshuam nrog "Famotidine" tsis tshwm sim kiag li. Vim li no, thaum siv Ranitidine thiab Famotidine, tsis muaj kev ua txhaum ntawm lub siab metabolism ntawm cov tshuaj, los yog nws manifests nws tus kheej mus rau ib tug me me npaum li cas. Thaum siv Cimetidine, kev tshem tawm cov tshuaj txo qis li ntawm 40%, thiab qhov no yog qhov tseem ceeb hauv kev kho mob.
Hepatic blood flow rate. Nws tuaj yeem txo qis cov ntshav siab txog li 40% thaum siv Cimetidine, nrog rau Ranitidine, tuaj yeem txo cov metabolism hauv cov tshuaj tua kab mob siab. "Famotidine" nyob rau hauv cov ntaub ntawv no tsis hloov tus nqi ntawm portal ntshav txaus.
Tubular excretion ntawm ob lub raum. H2-blockers raug tso tawm nrog kev tso tawm ntawm cov tubules ntawm lub raum. Hauv cov xwm txheej no, kev sib cuam tshuam nrog cov tshuaj sib xyaw ua ke tuaj yeem ua tau yog tias lawv raug tshem tawm los ntawm tib lub tshuab. "Imetidine" thiab "Ranitidine" tuaj yeem txo lub raum tso tawm mus rau 35% ntawm novocainamide, quinidine, acetylnovocainamide. "Famotidine" tsis cuam tshuam rau kev tso tawm ntawm cov tshuaj no. Tsis tas li ntawd, nws cov tshuaj kho mob muaj peev xwm muab cov ntshav plasma qis uas yuav tsis sib tw nrog lwm tus neeg ua haujlwm ntawm calcium secretion.
Kev sib cuam tshuam ntawm tshuaj. Kev sib cuam tshuam ntawm H2-blockers nrog pab pawg ntawm lwm cov tshuaj antisecretory tuaj yeem nce ntxivKev kho mob zoo (piv txwv li, nrog anticholinergics). Kev sib xyaw nrog cov tshuaj uas ua rau Helicobacter (cov tshuaj ntawm metronidazole, bismuth, tetracycline, clarithromycin, amoxicillin) ua kom nrawm nrawm ntawm cov kab mob peptic.
Pharmacodynamic tsis zoo cuam tshuam tau raug tsim los thaum ua ke nrog cov tshuaj uas muaj testosterone. "Cimetidine" cov tshuaj hormones hloov chaw los ntawm nws txoj kev sib txuas nrog cov receptors los ntawm 20%, thaum lub concentration ntawm cov ntshav plasma nce. Famotidine thiab Ranitidine tsis muaj txiaj ntsig zoo li no.
npe lag luam
Cov tshuaj hauv qab no ntawm H2-blockers tau sau npe thiab tso cai muag hauv peb lub tebchaws:
"Cimetidine"
Lub npe lag luam: Altramet, Belomet, Apo-cimetidine, Yenametidine, Histodil, Novo-cimetine, Neutronorm, Tagamet, Simesan, Primamet ", "Cemidin", "Ulcometin", "Ulkuzal", "Cymet", " Cimehexal", "Cygamet", "Cimetidin-Rivopharm", "Cimetidin Lannacher".
"Ranitidine"
Lub npe lag luam: "Acilok", "Ranitidine Vramed", "Acidex", "Asitek", "Histak", "Vero-ranitidine", "Zoran", "Zantin", "Ranitidine Sediko", "Zantak ", "Ranigast", "Raniberl 150", "Ranitidine", "Ranison",Ranisan, Ranitidin Akos, Ranitidin BMS, Ranitin, Rantak, Renks, Rantag, Yazitin, Ulran, Ulkodin.
"Famotidine"
", "Famopsin", "Famotidine Akos", "Famocide", "Famotidine Apo", "Famotidine Akri".
"Nizatidin". Lub npe lag luam "Axid"
"Roxatidine". Lub npe lag luam "Roxan".
"Ranitidine bismuth citrate". Lub npe lag luam "Pylorid"
