Histamine H2 tsoka mai amsa sigina blockers: sunayen da kwayoyi

Wannan rukuni ne guda daga cikin Pharmaceutical shirye-shirye na jagorancin nasa ne da selection yana nufin a lura da ulcerous cututtuka. A samu na H2 histamine tsoka mai amsa sigina blockers a cikin shekaru biyu da suka gabata, an dauki mafi girma a magani, taimaka a warware tattalin arziki (araha kudin) da kuma matsalolin zamantakewa. Saboda shirye-shirye H2 blockers sakamakon far na miki cutar sun inganta muhimmanci, m shisshigi an yi amfani da kasa akai-akai kamar yadda zai yiwu, marasa lafiya 'ingancin rayuwa inganta. "Cimetidine" da ake kira "zinariya misali" da magani daga ulcers, "Ranitidine" a 1998 ya zama zakara na tallace-tallace a pharmacology. Babbar amfani ne low cost, kuma ta haka ne tasiri na kwayoyi.

da yin amfani da

H2 histamine tsoka mai amsa sigina blockers amfani domin lura da acid da alaka gastrointestinal cututtuka. da tasiri inji - tarewa H2 rabe (in ba haka ba gaba ka koma ga histamine) na ciki mucosa Kwayoyin. Domin wannan dalili, shi rage samar da ceto a cikin lumen na ciki hydrochloric acid. Wannan kungiyar da kwayoyi alaka antisecretory anti-miki kwayoyi.

A mafi yawan lokuta, da H2 histamine tsoka mai amsa sigina blockers ake amfani da su a lokuta da peptic miki cutar manifestations. H2 blockers ba kawai rage samar da hydrochloric acid, amma kuma hana pepsin, ciki gamsai haka qara, a can ne ta ƙara kira prostagladinov, ta ƙara mugunya bicarbonate. Motor aiki na ciki ne bisa al'ada, da inganta microcirculation.

Alamomi H2-blockers:

• gastroesophageal reflux cuta.
• kullum da kuma m pancreatitis.
• dyspepsia.
• Zollinger-Ellison ciwo.
• reflux-jawo numfashi cuta.
• kullum gastritis da kuma duodenitis.
• Barrett ta esophagus.
• kashi ulcers esophageal mucosa.
• ciki miki.
• kuma symptomatic miki kwayoyi.
• kullum dyspepsia tare da kirji da epigastric zafi.
• tsari mastocytosis.
• don rigakafin danniya miki.
• Mendelson ta ciwo.
• Rigakafin tsammãni ciwon huhu.
• zub da jini babba GI.

Histamine H2 tsoka mai amsa sigina blockers: rarrabuwa da kwayoyi

Akwai rarrabuwa na wannan kungiyar da kwayoyi. Sun kasu kashi iyalan:

• Domin na ƙarni damuwa "cimetidine".
• "Ranitidine" - a shafi na H2 histamine tsoka mai amsa sigina II tsara.
• "Famotidine" yana nufin tsara III.
• "Nizatidine" yana nufin IV tsara.
• K V tana nufin tsara "roxatidine".

"Cimetidine" da kalla hydrophilic, saboda wannan rabin rayuwa ne sosai takaice, hanta metabolism a lokaci guda m. A shafi mayar da martani tare da cytochrome P-450 (microsomal enzyme) tare da wani canji kudi na hanta xenobiotic metabolism. "Cimetidine" ne a duniya hanawa na hanta metabolism na mafi kwayoyi tsakanin. A wannan batun, shi ne iya shiga wani pharmacokinetic hulda haka zai yiwu jari da kuma ya karu kasada na illa.

Daga cikin dukan H2 blockers "cimetidine" mafi tsoka shigar azzakari cikin farji, wanda kuma take kaiwa zuwa ƙãra illa. Ya maye gurbin na ciki testosterone daga dauri da na gefe rabe, haka haddasa jima'i tabarbarewa, take kaiwa zuwa wani karu a iko, tasowa rashin ƙarfi, kuma gynecomastia. "Cimetidine" zai iya sa ciwon kai, gudawa, myalgia da arthralgia, mai shudewa, karuwa a jini creatinine, hematological canje-canje, CNS, immunosuppressive mataki, cardiotoxicity. H2 shafi III tsara histamine rabe - "Famotidine" - kasa da ke shiga cikin kyallen takarda da kuma gabobin, game da shi ragewa adadin illa. Kada sa jima'i tabarbarewa da kuma shirye-shirye na gaba - "Ranitidine", "nizatidine", "roxatidine". Dukan su ba hulɗa tare da androgens.

Comparative halaye na kwayoyi

A bayanin da H2 histamine tsoka mai amsa sigina blockers (magunguna ƙarni na karin-aji), da sunan - "Ebrotidin" baya alama "Ranitidine bismuth citrate" ba sauki cakuda, da kuma wani hadadden fili. Ga kafa - ranitidine - dangantawa da ferric citrate vismusa.

Histamine H2 shafi tsara III "Famotidine" rabe da kuma II - "Ranitidine" - da mafi selectivity fiye da "cimetidine". Selectivity - sabon abu na kashi-dogara da zumunta. "Famotidine" da "ranitidine" shi ne mafi zabe fiye da wani "Tsinitidin" sakamako a kan H2 rabe. By kwatanta, "famotidine" m "Ranitidine" sau takwas, "Tsinitidina" - arba'in sau. Bambance-bambance a karfi suna m bisa ga m allurai na daidaitawa H2-blockers wanda aiki a kan danniya na hydrochloric acid. A ƙarfi daga cikin shaidu da rabe kuma kayyade tsawon lokaci na daukan hotuna. Idan da miyagun ƙwayoyi ne karfi da daure su cikin tsoka mai amsa sigina dissociates sannu a hankali ne ya sa ta sakamako na tsawon lokaci. A muhimmi mugunya "famotidine" rinjayar da mafi m. Nazarin ya nuna cewa "cimetidine" rage muhimmi mugunya kan 5 hours, "Ranitidine" - 7-8 hours, 12 hours - "famotidine".

H2-blockers kasance a cikin rukuni na hydrophilic kwayoyi. Daga cikin dukan zamanai, "cimetidine" kasa fiye da sauran hydrophilic, yayin da moderately lipophilic. Wannan damar da shi zuwa ga sauƙi shiga cikin daban-daban gabobin, da tasiri a kan H2-rabe, wadda take kaiwa zuwa dama illa. "Famotidine" da "Ranitidine" an dauke su sosai hydrophilic, ba su shiga cikin masana'anta, pre-emptive da tasiri a kan H2 rabe na parietal Kwayoyin.

Matsakaicin yawan illa a "Cimetidine". "Famotidine" da "Ranitidine", saboda canje-canje a cikin sinadaran tsarin, ba zai shafi hanta metabolizing enzymes kuma ba m illa.

labarin

A tarihin wannan kungiyar na H2-blockers fara a shekara ta 1972. Birtaniya kamfanin a cikin dakin gwaje-gwaje karkashin shugabanci na James Blake gudanar da bincike da kuma hada wata babbar lamba na mahadi da cewa suna da fasali kama wani kwayoyin ne histamine. Da zarar da haɗi da aka gano, an mika wa asibiti karatu. A farko a shafi buriamid ya ba sosai tasiri. Da tsarin da aka canza, ya juya metiamide. Clinical karatu sun nuna mafi inganci, amma ya nuna babban yawan guba, wanda aka bayyana a cikin nau'i na granulocytopenia. Bugu da ari bincike ya kai ga abin da aka bude "Cimetidine" (I tsara kwayoyi). A miyagun ƙwayoyi ya samu nasarar wuce gwajinsu a 1974 amince da shi. Sa'an nan wani abu ya fara amfani da H2 histamine tsoka mai amsa sigina blockers a asibiti yi, shi ne juyin juya hali a gastroenterology. Dzheyms Blek ya ga wannan samu Nobel Prize a 1988.

Kimiyya ba tsaya har yanzu. Saboda mahara illa "Cimetidine" pharmacologists fara ci gaba da alama search for more tasiri mahadi. Sabõda haka, shi da aka bude da sauran sabon H2 histamine tsoka mai amsa sigina blockers. Kwayoyi rage mugunya, amma ba ya shafar ta stimulants (acetylcholine, gastrin). Side effects, "acid ricochet" daidaitacce masana kimiyya don bincika sabuwar wajen rage acidity.

m magani

Akwai wani zamani aji na kwayoyi - proton famfo hanawa. Su ne m, a kislotopodavleniyu, don m gefen effects, lokaci effects H2 histamine tsoka mai amsa sigina blockers. Kwayoyi, sunayen da aka jera a sama, shi ne har yanzu amfani da na asibiti yi quite sau da yawa saboda halittar jini, domin dalilan tattalin arziki (mafi sau da yawa shi "famotidine" ko "Ranitidine").

Antisecretory zamani wajen amfani da su rage adadin hydrochloric acid, an raba su kashi biyu azuzuwan: da hanawa na protonic famfo (PPI) da kuma H2 histamine tsoka mai amsa sigina blockers. karshe shirye-shirye ne halin da sakamakon tachyphylaxis lokacin da maimaita liyafar sa a rage a cikin warkewa sakamako. Babu API domin wannan rashin, sabili da haka, a bambanci ga H2 blockers suna shawarar ga dogon lokacin da far.

The sabon abu na tachyphylaxis lokacin shan H2 blockers lura tun farkon far cikin 42 hours. A lura da gastroduodenal miki zub da jini ba da shawarar H2 blockers, fi so proton famfo hanawa.

juriya

A wasu lokuta, histamine H2 tsoka mai amsa sigina blockers (rarrabuwa nuna a bisa), kazalika da PPI kwayoyi wani lokacin sa mai juriya. A gudanar da irin wannan marasa lafiya ciki PH yanayi monitoring ba a gano wani canje-canje a intragastric acidity matakin. Wani lokaci gano lokuta da juriya da duk wani rukunin H2 blockers, 2 ko 3 da al'ummomi ko proton famfo hanawa. Da kuma kara da kashi a irin haka ba ya aiki, kana bukatar ka zabi wani daban-daban irin miyagun ƙwayoyi. Karatu wasu H2-blockers, omeprazole kuma (IPP) ya nuna cewa daga 1 zuwa 5% daga cikin lokuta ba canje-canje a cikin kullum PH-metry. A tsauri kallo na aiwatar da acid magani aka dauke su mafi m makirci inda Esophageal PH monitoring aka bincika a farko, sa'an nan a karo na biyar da kuma rana ta bakwai da magani. A gaban marasa lafiya da cikakken juriya nuna cewa a asibiti yi, babu wani magani, wadda zai yi wani cikakken dace.

illa

Blockers H2 histamine tsoka mai amsa sigina hanyar illa tare da sãɓãwar launukansa mita. Yi amfani da "Cimetidine" haddasa su zuwa 3.2% na lokuta. . "Famotidine - 1.3%," Ranitidine "- 2.7% Side effects sun hada da:

• Juwa ko jiri, ciwon kai, tashin hankali, gajiya, drowsiness, rikita, hankali, ciki, agitation, hallucinations, involuntary ƙungiyoyi, Heart hangen nesa.
• Arrhythmia ciki har da bradycardia, tachycardia, arrythmia, asystole.
• Zawo ko maƙarƙashiya, ciki zafi, amai, tashin zuciya.
• M pancreatitis.
• Hypersensitivity (zazzabi, rash, myalgia, anaphylaxis, arthralgia, erythema multiforme, angioneurotic edema).
• Canje-canje a cikin hanta aikin gwaje-gwaje, blended ko bayyananen holistaticheskie hepatitis da jaundice ko ba tare da shi.
• Karuwan creatinine.
• Take hakki na jini (leukopenia, pancytopenia, granulocytopenia, agranulocytosis, thrombocytopenia, aplastic anemia da cerebral hypoplasia, haemolytic anemia rigakafi.
• Rashin ƙarfi.
• Gynecomastia.
• Alopecia.
• rage libido.

Famotidine mafi illa ya kan gastrointestinal fili, sau da yawa inganta zawo, a rare lokuta, a maimakon haka, akwai maƙarƙashiya. Zawo ya auku saboda antisecretory effects. Saboda gaskiya cewa adadin hydrochloric acid a cikin ciki rage-rage, PH ƙaruwa. A wannan yanayin, pepsinogen sannu a hankali ya jũya a cikin pepsin, wanda taimaka karya saukar da sunadarai. Narkewa an gaji da damuwa, kuma sau da yawa tasowa zawo.

contraindications

By H2 histamine tsoka mai amsa sigina blockers hada da wani yawan kwayoyi, wanda da wadannan contraindications:

• Disturbances a cikin kodan da kuma hanta.
• Cirrhosis (portosystemic encephalopathy cuta).
• Lactation.
• Hypersensitivity zuwa wani magani na wannan kungiya.
• Pregnancy.
• Yara shekaru har zuwa shekaru 14.

Hulda da sauran kwayoyi

Histamine H2 tsoka mai amsa sigina blockers, wanda mataki inji yanzu gane su da wasu pharmacokinetic miyagun ƙwayoyi interactions.

Absorption a ciki. Saboda antisecretory sakamako na H2-blockers iya shafar sha na da miyagun ƙwayoyi-Wutan, inda a can ne a dogara a kan PH, saboda kwayoyi na iya rage mataki na yadawa da kuma ionization. "Cimetidine" na iya rage sha na kayan aikin kamar "Antipyrin" "ketoconazole" "Chlorpromazine" da kuma babban baƙin ƙarfe shirye-shirye. Don kauce wa irin wannan malabsorption, kwayoyi dole ne a dauki 1-2 hours kafin amfani da H2 blockers.

Hanta metabolism. H2 histamine tsoka mai amsa sigina blockers (kwayoyi na zamani musamman) rayayye hulɗa tare da cytochrome P-450, wanda shi ne babba oxidizer hanta. A rabin-rai za a ƙara, da kuma sakamako iya bayyana sprolongirovatsya yawan abin sama da miyagun ƙwayoyi da aka metabolized ta fiye da 74%. Karfi duk ya mayar da martani tare da cytochrome P-450 ya shiga "Cimetidine", sau 10 fiye da da "Ranitidine". Hulda da "famotidine" ba faruwa. Saboda wannan dalili, lokacin amfani da "Ranitidine" da "Famotidine" ba take hakkin ya auku na hanta miyagun ƙwayoyi metabolism, ko shi da aka nuna wa wani kadan har. Lokacin amfani "Cimetidine" yarda da kwayoyi a rage kusan 40%, kuma shi ne asibiti muhimmanci.

A kudi na hanta jini ya kwarara. Zai iya rage hanta jini ya kwarara gudu zuwa 40% lokacin amfani da "Cimetidine", da kuma "Ranitidine" zai iya rage prisistemnogo high na rayuwa yarda da kwayoyi. "Famotidine" a cikin wadannan lokuta ba ya canza kudi na portal jini ya kwarara.

Tubular koda tukar tumbi. H2-blockers eksretiruyutsya tare da aiki na koda tubular mugunya. A irin haka ne, zai yiwu hulda da layi daya kwayoyi idan sun ekskrektsiya za'ayi da wannan sunadaran. "Imetidin" da "Ranitidine" iya rage koda ekskrektsiyu zuwa 35% procainamide, quinidine, atsetilnovokainamida. "Famotidine" yana da wani canje-canje a kawar da wadannan kwayoyi. Bugu da ƙari kuma, da warkewa kashi ne iya samar da wani low maida hankali a jini, wanda ba za a fi mayar da gasa da sauran jamiái a cikin alli matakan mugunya.

Pharmacodynamic interactions. Hulda da H2-blockers wasu antisecretory kwayoyi kungiyoyin iya kara warkewa inganci (msl, holinoblokatorami). Hade da jamiái da cewa aiki a kan helicobacter (shirye-shirye na metronidazole, bismuth, tetracycline, clarithromycin, amoxicillin), accelerates da tightening na peptic ulcers.

Pharmacodynamic m hulda a lokacin da a hade tare da kafa kwayoyi, wanda sun hada da testosterone. "Cimetidine" hormone gudun hijira daga dauri da rabe a kan wani 20% maida hankali a jini ne ta ƙara. "Famotidine" da "Ranitidine" ba su da irin wannan sakamako.

cinikayya sunayen

A kasar mu, rajista da kuma yarda ka sayar da wadannan kwayoyi ne H2-blockers:

"Cimetidine"

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

"Ranitidine"

Ciniki sunayen: "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"

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

"Nizatidine". Ciniki sunan "Aksid".

"Roxatidine". Ciniki sunan "Roxane".

"Ranitidine bismuth citrate". Ciniki sunan "Pilorid".