Histamine H2 ihe nnabata blockers: aha ọgwụ

Otu a bụ otu n'ime ọgwụ preparations nke na-eduga na-eweta nhọrọ pụtara na ọgwụgwọ nke ulcerous ọrịa. The chọpụtara nke H2 histamine ihe nnabata blockers na abụọ gara aga ọtụtụ afọ, a na-ewere ndị kasị ibu na nkà mmụta ọgwụ, na-enyere dozie aku (ezi uche price) na-elekọta mmadụ nsogbu. N'ihi preparations H2 blockers pụta ọgwụ nke ọnyá afọ ọrịa nwere mma budata, ịwa ahụ adọ e ji obere ugboro ugboro dị ka omume, ọrịa àgwà nke ndụ ka mma. "Cimetidine" na-akpọ "gold ọkọlọtọ" na ọgwụgwọ nke ọnyá, "Ranitidine" na 1998 ghọrọ dike nke ahịa na pharmacology. Nnukwu uru bụ ala na-eri, ma si otú irè nke ọgwụ ọjọọ.

na ojiji nke

H2 histamine ihe nnabata blockers eji maka ọgwụgwọ nke acid-metụtara eriri afọ ọrịa. mmetụta usoro - igbochi H2 anabata (ma kwuru na dị ka histamine) nke gastric mucosa mkpụrụ ndụ. N'ihi nke a, ọ belata mmepụta na nnyefe n'ime lumen nke gastric hydrochloric acid. Otu a ọgwụ ọjọọ eme ihe metụtara antisecretory mgbochi ọnyá afọ ọgwụ ọjọọ.

N'ọnọdụ ka ukwuu, nke H2 histamine ihe nnabata blockers na-eji ikpe nke peptic ọnyá afọ ọrịa n'obiọma. H2 blockers na-abụghị nanị belata mmepụta nke hydrochloric acid, ma inhibit pepsin, gastric imi otú enwekwu, e nwere mụbara njikọ prostagladinov, mụbara secretion nke bicarbonate. Motor ọrụ nke afo bụ normalized, mma microcirculation.

Egosi H2-blockers:

• gastroesophageal reflux ọrịa;
• -adịghị ala ala na nnukwu pancreatitis;
• dyspepsia;
• Zollinger-Ellison syndrome;
• reflux na-akpata akụkụ okuku ume na ọrịa;
• adịghị ala ala mgbu na duodenitis;
• Barrett si na nkọlọ;
• imeri Ọnya esophageal mucosa;
• afo ọnyá afọ;
• na symptomatic ọnyá afọ ọgwụ ọjọọ;
• adịghị ala ala dyspepsia na obi na epigastric mgbu;
• systemic mastocytosis;
• maka mgbochi nke nrụgide ọnyá afọ;
• Mendelson si syndrome;
• Prevention of ọchịchọ oyi baa;
• agba ọbara elu gị.

Histamine H2 ihe nnabata blockers: nhazi ọkwa ọgwụ

E nwere a nhazi ọkwa nke a ìgwè nke ọgwụ ọjọọ. Ha na-ekewa ezinụlọ:

• N'ihi na m na ọgbọ nchegbu "cimetidine".
• "Ranitidine" - a blocker nke H2 histamine ihe nnabata II emana.
• "Famotidine" na-ezo aka ọgbọ III.
• "Nizatidine" na-ezo aka IV emana.
• K V ezo ọgbọ "roxatidine".

"Cimetidine" ọ dịghị ihe ọzọ hydrophilic, n'ihi na a ọkara ndụ dị nnọọ mkpụmkpụ, hepatic metabolism n'otu oge bara uru. Blocker meghachi omume na cytochrome P-450 (microsomal enzyme) na a mgbanwe ọnụego hepatic xenobiotic metabolism. "Cimetidine" bụ a eluigwe na ala inhibitor nke hepatic metabolism nke ọtụtụ ọgwụ ọjọọ n'etiti. Na nke a, ọ bụ ike banye a pharmacokinetic mmekọrịta ya mere o kwere omume ìgwè na ụba ize ndụ nke mmetụta.

N'etiti ihe niile H2 blockers "cimetidine" mma anụ ahụ penetration, nke nwekwara na-eduga ná ụba mmetụta. Ọ na-anọchi endogenous testosterone si nkịtị na elu-anabata, si otú eme mmekọahụ dysfunction, na-eduga ná a ọnụ ke potency, amalite adịghị na gynecomastia. "Cimetidine" nwere ike ime ka isi ọwụwa, afọ ọsịsa, myalgia na arthralgia, na-akwụsị akwụsị, na-abawanye na ọbara creatinine, hematological mgbanwe, CNS, immunosuppressive edinam, cardiotoxicity. H2 blocker III ọgbọ histamine anabata - "Famotidine" - obere penetrates n'ime anụ ahụ na akụkụ, si otú usen ego nke mmetụta. Ghara ime ka mmekọahụ dysfunction na preparations nke ọgbọ - "Ranitidine", "nizatidine", "roxatidine". All n'ime ha adịghị emekọ androgens.

Comparative e ji mara ọgwụ

A nkọwa nke H2 histamine ihe nnabata blockers (ọgwụ ọgbọ nke mmezi-klas), aha - "Ebrotidin" iche pụta ìhè "Ranitidine bismuth citrate" abụghị a dị mfe ngwakọta, na a mgbagwoju compound. Ebe a idabere - ranitidine - jikọtara ferric citrate vismusa.

Histamine H2 blocker ọgbọ III "Famotidine" anabata na II - "Ranitidine" - nwere a ukwuu selectivity karịa "cimetidine". Selectivity - onu nke dose-dabere na ikwu. "Famotidine" na "ranitidine" bụ nhọrọ karị karịa a "Tsinitidin" mmetụta na H2 anabata. Site tụnyere, "famotidine" dị ike "Ranitidine" ugboro asatọ, "Tsinitidina" - iri anọ ugboro. The iche iche na ike na-ekpebisi ike dị iche iche doses nke narị afọ ise tupu H2-blockers nke-eme ihe na suppression nke hydrochloric acid. The ike nke nkekọ na-anabata na-ekpebi oge nke ikpughe. Ọ bụrụ na ọgwụ a na-ike-agbụ na ihe nnabata dissociates nwayọọ nwayọọ na-kpatara mmetụta nke oge. Na basal secretion "famotidine" na-emetụta ndị kasị inogide. Studies na-egosi na "cimetidine" ebelata basal secretion maka 5 awa, "Ranitidine" - 7-8 awa, 12 awa - "famotidine".

H2-blockers nwe ìgwè hydrophilic ọgwụ ọjọọ. N'etiti ihe niile ọgbọ, "cimetidine" erughị ọzọ hydrophilic, mgbe moderately lipophilic. Nke a na-enyere ya mfe banye n'ime ihe dị iche iche akụkụ, mmetụta na H2-anabata, nke na-eduga ọtụtụ mmetụta. "Famotidine" na "Ranitidine" na-ahụta ka ukwuu hydrophilic, ha adịghị banye n'ime ákwà, tupu emptive ha mmetụta na H2 anabata nke parietal mkpụrụ ndụ.

Karịa ọnụ ọgụgụ nke mmetụta na "Cimetidine". "Famotidine" na "Ranitidine", n'ihi mgbanwe ndị na-chemical Ọdịdị, adịghị emetụta hepatic n'ịgbari enzymes na-enye ole na ole mmetụta.

akụkọ

The akụkọ ihe mere eme nke a ìgwè nke H2-blockers malitere na 1972. British ụlọ ọrụ na laabu n'okpuru nduzi nke James Blake nnyocha ma synthesized a nnukwu ọnụ ọgụgụ nke ogige ndị structurally yiri a molekul bụ histamine. Ozugbo a ala njikọ e kwuru, ha na-enyefe na-adakarị ọmụmụ. The mbụ blocker buriamid bụ nnọọ irè. Ya Ọdịdị a gbanwee, ọ tụgharịa metiamide. Clinical ọmụmụ gosiri ukwuu nrụpụta, ma gosiri oké toxicity, nke na-egosipụta na ụdị granulocytopenia. Ọzọkwa nnyocha emewo ka ihe e meghere "Cimetidine" (I ọgbọ ọgwụ ọjọọ). The ọgwụ ọma gafere adakarị ọnwụnwa ke 1974 mma ya. Mgbe ihe malitere iji H2 histamine ihe nnabata blockers na-adakarị omume, ọ bụ a mgbanwe ke Gastroenterology. Dzheyms Blek bụ n'ihi na nke a chọpụtara na Nobel Nrite na 1988.

Science adịghị guzo. N'ihi multiple mmetụta "Cimetidine" pharmacologists malitere na-ịrịba ama search maka irè karị ogige. N'ihi ya, e meghere na ndị ọzọ ọhụrụ H2 histamine ihe nnabata blockers. Drugs belata secretion, ma adịghị emetụta ya stimulants (acetylcholine, gastrin). Mmetụta, "acid ricochet" gbakwasara ọkà mmụta sayensị ịchọ ọhụrụ iji belata acidity.

bụzi ihe mgbe ochie na nkà mmụta ọgwụ

E nwere oge a na klas nke ọgwụ ọjọọ - proton mgbapụta inhibitors. Ha na-elu na kislotopodavleniyu, maka a kacha nta nke mmetụta, oge mmetụta H2 histamine ihe nnabata blockers. Drugs, aha nke na-depụtara n'elu, ọ ka na-eji na-adakarị omume ezi mgbe ruru ka mkpụrụ ndụ ihe nketa, n'ihi na akụ na ụba (ọzọ mgbe ọ "na-famotidine" ma ọ bụ "Ranitidine").

Antisecretory oge a etinyere ibelata ego nke hydrochloric acid, na-kewara abụọ sara mbara klas: na inhibitors nke protonic mgbapụta (mba) na H2 histamine ihe nnabata blockers. ikpeazụ preparations na-ji mmetụta nke tachyphylaxis mgbe ugboro ugboro n'ikuku na-akpata a gụnyere ya ná ọgwụgwọ mmetụta. E nweghị API a enweghị, ya mere, dị iche na H2 blockers na-atụ aro n'ihi na ogologo oge ọgwụ.

Onu nke tachyphylaxis mgbe ewere H2 blockers hụrụ kemgbe mmalite nke ọgwụ n'ime 42 awa. Na ọgwụgwọ nke gastroduodenal ọnyá ọbara ọgbụgba adịghị atụ aro H2 blockers, họọrọ proton mgbapụta inhibitors.

eguzogide

Mgbe ụfọdụ, histamine H2 ihe nnabata blockers (nhazi ọkwa gosiri n'elu) nakwa dị ka mba ọgwụ ọjọọ mgbe ụfọdụ ime ka a na-eguzogide. Na-eduzi ndị dị otú ahụ ọrịa afo onye Onyenwe anyị + na gburugburu ebe obibi nlekota oru na-adịghị ahụrụ ọ bụla mgbanwe na intragastric acidity larịị. Mgbe ụfọdụ, ahụrụ ikpe nke iguzogide ìgwè ọ bụla H2 blockers, 2 ma ọ bụ 3 ọgbọ ma ọ proton mgbapụta inhibitors. Na-amụba dose dị otú ahụ ikpe-adịghị arụ ọrụ, mkpa ka ị họrọ a dị iche iche ụdị ọgwụ. Ịmụ ihe ụfọdụ H2-blockers, omeprazole na (IPP) na-egosi na site 1 5% nke ikpe na-adịghị mgbanwe kwa onye Onyenwe anyị +-metry. Na ike chọpụtara nke usoro nke acid ọgwụgwọ a na-atụle ga-kasị oru oma atụmatụ ebe Esophageal onye Onyenwe anyị + nlekota na-nyochaworo na mbụ, na mgbe ahụ na ise na asaa, ụbọchị nke ọgwụgwọ. Ọnụnọ nke ọrịa na-ezu na-eguzogide na-egosi na na-adakarị omume, ọ dịghị ọgwụ, nke ga-enwe ihe zuru arụmọrụ.

mmetụta

Blockers H2 histamine ihe nnabata-eme ka mmetụta na mgbanwe ugboro. Jiri "Cimetidine"-eme ka ha 3.2% nke ikpe. . "Famotidine - 1.3%," Ranitidine "- 2,7% Mmetụta na-agụnye:

• Dizziness, isi ọwụwa, nchegbu, ike ọgwụgwụ, iro ụra, mgbagwoju anya, uche, ịda mbà n'obi, n'ahụhụ, ịmụ anya arọ nrọ, na ịsụ mmegharị, bịara ikiri ọhụụ.
• Arrhythmia tinyere bradycardia, tachycardia, arrythmia, asystole.
• Afọ ọsịsa ma ọ bụ afọ ntachi, abdominal mgbu, vomiting, ọgbụgbọ.
• Nnukwu pancreatitis.
• Hypersensitivity (fever, ọkụ ọkụ, myalgia, anaphylaxis, arthralgia, erythema multiforme, angioneurotic edema).
• Mgbanwe imeju ọtọ ule, blended ma ọ bụ ngosipụta holistaticheskie ịba ọcha n'anya na jaundice ma ọ bụ na-enweghị ya.
• Mụbara creatinine.
• Imebi ọbara (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, aplastic anaemia na ọrịa ụbụrụ hypoplasia, haemolytic anaemia Dịghịzi.
• Enweghi ike.
• Gynecomastia.
• Alopecia.
• ebelata libido.

Famotidine kasị mmetụta nke na eriri afọ tract, mgbe mgbe, ịzụlite afọ ọsịsa, na obere okwu, na Kama nke ahụ, e nwere afọ ntachi. Afọ ọsịsa emee n'ihi antisecretory mmetụta. N'ihi na eziokwu na ego nke hydrochloric acid ke afo mbelata, onye Onyenwe anyị + na-abawanye. Na nke a, pepsinogen nwayọọ nwayọọ amama n'ime pepsin, nke na-enyere gbarie na-edozi. Mgbaze kpaghasịrị, mgbe amalite afọ ọsịsa.

contraindications

Site H2 histamine ihe nnabata blockers agụnye ọtụtụ ọgwụ ọjọọ eme ihe, nke nwere ndị na-esonụ contraindications:

• Na-enwe nsogbu akụrụ na imeju.
• Imeju (portosystemic encephalopathy ọrịa).
• Lactation.
• Hypersensitivity ọ bụla ọgwụ nke otu a.
• Pregnancy.
• Children noo ruo afọ 14.

Mmekọrịta ndị ọzọ ọgwụ ọjọọ eme ihe

Histamine H2 ihe nnabata blockers, nke edinam usoro a na ugbu a ghọtara na ụfọdụ pharmacokinetic ọgwụ interactions.

Absorption ke afo. N'ihi antisecretory mmetụta nke H2-blockers na-enwe ike na-emetụta ndị absorption nke ọgwụ-electrolytes, ebe a na nduzi na onye Onyenwe anyị +, n'ihi na ọgwụ ọjọọ nwere ike ibelata ogo mgbasa na ionization. "Cimetidine" nwere ike belata absorption ngwaọrụ ndị dị otú ahụ dị ka "Antipyrin" "ketoconazole" "Chlorpromazine" na elu na ígwè preparations. Iji zere ndị dị otú ahụ malabsorption, ọgwụ ọjọọ ga-a 1-2 awa tupu ojiji nke H2 blockers.

Hepatic metabolism. H2 histamine ihe nnabata blockers (ọgwụ ọjọọ m ọgbọ karịsịa) ifịk ifịk emekọ cytochrome P-450, nke bụ isi ihe na oxidizer imeju. The ọkara ndụ ga-amụba, na mmetụta nwere ike gosipụtara sprolongirovatsya ovadozu nke ọgwụ nke na-metabolized site karịa 74%. Ike niile meghachi omume na cytochrome P-450 abatakwa "Cimetidine", 10 ugboro karịa "Ranitidine". Mmekọrịta "famotidine" na-adịghị eme. N'ihi nke a, mgbe na-eji "Ranitidine" na "Famotidine" ọ dịghị mebiri emee nke hepatic ọgwụ metabolism, ma ọ bụ na ọ na-egosi na a nta ruo n'ókè. Mgbe na-eji "Cimetidine" nwechapụ nke ọgwụ ọjọọ na-ebelata ihe dị 40%, na bụ clinically ịrịba.

Ọnụego hepatic ọbara. Nwere ike ibelata hepatic ọbara ike ọsọ 40% mgbe eji a "Cimetidine", na "Ranitidine" nwere ike ibelata prisistemnogo elu metabolic nwechapụ nke ọgwụ ọjọọ. "Famotidine" na okwu ikpe ndị a adịghị agbanwe ọnụego portal ọbara.

Tubular gbasara akụrụ excretion. H2-blockers eksretiruyutsya na-arụsi ọrụ ike gbasara akụrụ tubular secretion. Na ndị a, o kwere omume na mmekọrịta na yiri ọgwụ ọjọọ ma ọ bụrụ na ha ekskrektsiya rụrụ site n'otu usoro. "Imetidin" na "Ranitidine" ike nke na mbenata gbasara akụrụ ekskrektsiyu 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" enweghị mgbanwe mkpochapu ndị a ọgwụ ọjọọ. Ọzọkwa, ya ọgwụgwọ dose bụ ike nke na-enye a ala ịta na plasma, nke na-agaghị n'ụzọ mpi ndị ọzọ mmadụ na calcium etoju nke secretion.

Pharmacodynamic interactions. Mmekọrịta H2-blockers ọzọ antisecretory ọgwụ ọjọọ dị iche iche ike nke na-amụba ọgwụgwọ nrụpụta (e.g., holinoblokatorami). Nchikota na mmadụ na-eme ihe na helicobacter (preparations nke metronidazole, bismuth, tetracycline, clarithromycin, amoxicillin), accelerates tightening nke peptic ọnyá afọ.

Pharmacodynamic oghom mmekọrịta mgbe jikọtara na guzosie ike ọgwụ ọjọọ eme ihe, nke na-agụnye testosterone. "Cimetidine" hormone obibi site nkịtị na-anabata a 20% ịta na plasma na-ụba. "Famotidine" na "Ranitidine" enweghị mmetụta dị otú ahụ.

ahia aha

Na mba anyị, aha na-ekwe na-ere ọgwụ a na-H2-blockers:

"Cimetidine"

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

"Ranitidine"

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

"Nizatidine". Trade aha "Aksid".

"Roxatidine". Trade aha "Roxane".

"Ranitidine bismuth citrate". Trade aha "Pilorid".