Gastroenterology Book

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H2 Receptor Antagonist

Aka: H2 Receptor Antagonist, H2 Antagonist, H2 Blocker, Ranitidine, Zantac, Cimetidine, Tagamet, Nizatidine, Axid, Famotidine, Pepcid
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  1. Mechanism
    1. Inhibits histamine action at parietal cell H2 receptor
    2. Decreases basal and food stimulated acid secretion
    3. Inhibits 50-80% of daily gastric acid secretion
  2. Preparations
    1. Ranitidine (Zantac)
      1. Bolus IV Dosing: 50 mg IV q6-8h
      2. Continuous IV Dosing: 6.25 mg/h IV
      3. Oral Dosing: 150 mg PO bid
    2. Cimetidine (Tagamet)
      1. Bolus parenteral dosing: 300 mg IV or IM q6h
      2. Continuous IV Dosing: 37.5 mg/h IV
      3. Oral Dosing: 400 mg PO bid
    3. Famotidine (Pepcid)
      1. Oral dosing: 20 to 40 mg PO bid
    4. Nizatidine (Axid)
      1. Oral dosing: 150 mg PO bid
  3. Efficacy
    1. Similar efficacy among all 4 agents
    2. H2 Blockers are not as effective in Tobacco abuse
      1. Carafate and Prilosec preferred in this population
    3. Symptomatic relief of GERD in weeks in 70% of cases
      1. Devault (1999) Am J Gastroenterol 94:1434-42
  4. Disadvantages
    1. Even generic costs still approch Proton Pump Inhibitors
      1. (2003) Red Book, Medical Economics Data, Montvale, NJ
  5. Adverse Effects
    1. Cimetidine has more drug interactions and side effects
Medication Costs
RANITIDINE (on 2/10/2012 at Target.com)
RANITIDINE 150 MG Tablet #30 for $4.00 ($0.13/unit)
RANITIDINE 300 MG Tablet #30 for $4.00 ($0.13/unit)
CIMETIDINE (on 2/10/2012 at Target.com)
CIMETIDINE 800 MG* Tablet #30 for $4.00 ($0.13/unit)
FAMOTIDINE (on 2/10/2012 at Target.com)
FAMOTIDINE 20 MG Tablet #30 for $4.00 ($0.13/unit)
Ranitidine HCl (on 2/9/2012 at DrugStore.com)
Ranitidine HCl 15mg/ml Syrup #30 for $29.99 ($1.00/unit)
Ranitidine HCl 300mg Capsules #30 for $30.99 ($1.03/unit)
Ranitidine HCl 150mg Capsules #60 for $50.99 ($0.85/unit)
Ranitidine HCl 150mg Tablets #90 for $17.99 ($0.20/unit)
Ranitidine HCl 300mg Tablets #30 for $15.99 ($0.53/unit)
Ranitidine 75 (on 2/9/2012 at DrugStore.com)
Ranitidine 75 30 75mg Tablets Box #1 for $13.99 ($13.99/unit)
Zantac (on 2/9/2012 at DrugStore.com)
Zantac 150mg Tablets #60 for $259.00 ($4.32/unit)
Zantac 15mg/ml Syrup #300 for $224.99 ($0.75/unit)
Zantac 300mg Tablets #30 for $240.99 ($8.03/unit)
Zantac EFFERdose (on 2/9/2012 at DrugStore.com)
Zantac EFFERdose 25mg Effervescent Tabs #60 for $241.00 ($4.02/unit)
Cimetidine (on 2/9/2012 at DrugStore.com)
Cimetidine 300mg Tablets #100 for $16.66 ($0.17/unit)
Cimetidine 400mg Tablets #90 for $31.99 ($0.36/unit)
Cimetidine 200mg Tablets #30 for $18.99 ($0.63/unit)
Cimetidine HCl (on 2/9/2012 at DrugStore.com)
Cimetidine HCl 300mg/5ml Solution #237 for $35.99 ($0.15/unit)
Tagamet (on 2/9/2012 at DrugStore.com)
Tagamet 300mg Tablets #60 for $81.99 ($1.37/unit)
Nizatidine (on 2/9/2012 at DrugStore.com)
Nizatidine 300mg Capsules #30 for $54.00 ($1.80/unit)
Nizatidine 150mg Capsules #60 for $51.98 ($0.87/unit)
Nizatidine 15mg/ml Solution #473 for $272.00 ($0.58/unit)
Zymaxid (on 2/9/2012 at DrugStore.com)
Zymaxid 0.5% Solution 2.5ml Bottle #1 for $96.89 ($96.89/unit)
Maxidex (on 2/9/2012 at DrugStore.com)
Maxidex 0.1% Suspension 5ml Bottle #1 for $61.36 ($61.36/unit)
Axid (on 2/9/2012 at DrugStore.com)
Axid 15mg/ml Solution #480 for $409.84 ($0.85/unit)
Axid 150mg Capsules #60 for $172.98 ($2.88/unit)
Axid 300mg Capsules #30 for $169.98 ($5.67/unit)
Famotidine (on 2/9/2012 at DrugStore.com)
Famotidine 20mg Tablets #30 for $19.99 ($0.67/unit)
Famotidine 40mg Tablets #90 for $18.98 ($0.21/unit)
Famotidine 40mg/5ml Suspension 50ml Bottle #1 for $155.98 ($155.98/unit)
Pepcid (on 2/9/2012 at DrugStore.com)
Pepcid 30 20mg Tablets Bottle #1 for $71.99 ($71.99/unit)
Pepcid 30 40mg Tablets Bottle #1 for $125.99 ($125.99/unit)
Pepcid 40mg/5ml Suspension 50ml Bottle #1 for $175.99 ($175.99/unit)
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Tagamet (C0592157)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D002927
English tagamet, Tagamet
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Nizatidine (C0085154)

Definition (MSH) A histamine H2 receptor antagonist with low toxicity that inhibits gastric acid secretion. The drug is used for the treatment of duodenal ulcers.
Definition (NCI) A competitive and reversible histamine H2-receptor antagonist with antacid activity. Nizatidine inhibits the histamine H2-receptors located on the basolateral membrane of the gastric parietal cell, thereby reducing basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to stimuli.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D016567
SnomedCT 108664005, 386887009
English Nizatidine, N-(2-(((2-((Dimethylamino)methyl)-4-thiazolyl)methyl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine, 1,1-Ethenediamine, N-(2-(((2-((dimethylamino)methyl)-4-thiazolyl)methyl)thio)ethyl)-N'-methyl-2-nitro-, nizatidine, nizatidine (medication), histamine-2 receptor antagonists nizatidine, NIZATIDINE, Nizatidine [Chemical/Ingredient], Nizatidine (product), Nizatidine (substance)
Swedish Nizatidin
Czech nizatidin
Finnish Nitsatidiini
Russian NIZATIDIN, НИЗАТИДИН
Japanese ニザチジン
Polish Nizatydyna
Spanish nizatidina (producto), nizatidina (sustancia), nizatidina, Nizatidina
French Nizatidine
German Nizatidin
Italian Nizatidina
Portuguese Nizatidina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Axid (C0678129)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D016567
English axid, Axid
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Cimetidine (C0008783)

Definition (CSP) histamine congener; competitively inhibits histamine binding to H2 receptors, inhibits gastric acid secretion, pepsin, and gastrin output, and blocks the activity of cytochrome P-450.
Definition (NCI) A drug usually used to treat stomach ulcers and heartburn. It is also commonly used in a regimen to prevent allergic reactions.
Definition (NCI) A histamine H(2)-receptor antagonist. Enhancing anti-tumor cell-mediated responses, cimetidine blocks histamine's ability to stimulate suppressor T lymphocyte activity and to inhibit natural killer (NK) cell activity and interleukin-2 production. Cimetidine also may inhibit tumor growth by suppressing histamine's growth-factor activity and blocking histamine-induced stimulation of vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor. (NCI04)
Definition (MSH) A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRINS output. It also blocks the activity of CYTOCHROME P-450 which might explain proposals for use in NEOADJUVANT THERAPY.
Definition (PDQ) A histamine H(2)-receptor antagonist. Enhancing anti-tumor cell-mediated responses, cimetidine blocks histamine's ability to stimulate suppressor T lymphocyte activity and to inhibit natural killer (NK) cell activity and interleukin-2 production. Cimetidine also may inhibit tumor growth by suppressing histamine's growth-factor activity and blocking histamine-induced stimulation of vascular endothelial growth factor (VEGF), a pro-angiogenic growth factor. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39185&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=39185&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C374" NCI Thesaurus)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D002927
SnomedCT 373541007, 83532008
English Cimetidine, N-Cyano-N'-methyl-N''-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)ethyl)guanidine, cimetidine, Guanidine, N-cyano-N'-methyl-N''-(2-(((5-methyl-1H-imidazol-4-yl)methyl)thio)ethyl)-, N-Cyano-N'-methyl-N''-[2-[[(5-methyl-1H-imidazol-4-yl)methyl]thio]ethyl]guanidine, histamine-2 receptor antagonists cimetidine, cimetidine (medication), CIMETIDINE, Guanidine, N''-Cyano-N-Methyl-N'-(2-(((5-Methyl-1h-Imidazol-4-Yl)Methyl)Thio)Ethyl)-, Cimetidine [Chemical/Ingredient], Cimetidine (product), Cimetidine (substance)
Swedish Cimetidin
Czech cimetidin
Finnish Simetidiini
Russian TSIMETIDIN, ЦИМЕТИДИН
Japanese シメチジン
Croatian CIMETIDIN
Polish Cymetydyna
Spanish cimetidina (producto), cimetidina (sustancia), cimetidina, Cimetidina
French Cimétidine
German Cimetidin
Italian Cimetidina
Portuguese Cimetidina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Famotidine (C0015620)

Definition (NCI) A propanimidamide and histamine H2-receptor antagonist with antacid activity. As a competitive inhibitor of histamine H2-receptors located on the basolateral membrane of the parietal cell, famotidine reduces basal and nocturnal gastric acid secretion, resulting in a reduction in gastric volume, acidity, and amount of gastric acid released in response to various stimuli.
Definition (MSH) A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D015738
SnomedCT 387211002, 39128000
English Famotidine, Propanimidamide, 3-(((2-((aminoiminomethyl)amino)-4-thiazolyl)methyl)thio)-N-(aminosulfonyl)-, famotidine, famotidine (medication), histamine-2 receptor antagonists famotidine, FAMOTIDINE, Famotidine [Chemical/Ingredient], Famotidine (product), Famotidine (substance)
Swedish Famotidin
Czech famotidin
Finnish Famotidiini
Russian FAMOTIDIN, ФАМОТИДИН
Japanese ファモチジン
Croatian FAMOTIDIN
Polish Famotydyna
Spanish famotidina (producto), famotidina (sustancia), famotidina, Famotidina
French Famotidine
German Famotidin
Italian Famotidina
Portuguese Famotidina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Pepcid (C0678119)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D015738
English pepcid, Pepcid
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Zantac (C0592278)

Definition (CHV) brand name of an heartburn medication
Definition (CHV) brand name of an heartburn medication
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D011899
English zantac, zantac [brand name], Zantac
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Ranitidine (C0034665)

Definition (CHV) a kind of antiacid drug
Definition (CHV) a kind of antiacid drug
Definition (MSH) A non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.
Definition (CSP) N-2-(5-dimethylamino)methyl-2- furanylmethyl thioethyl-N'-methyl-2-nitro-1,1 -ethenediamine; cimetidine analog; H2 histamine receptor antagonist used to treat gastric ulcers.
Definition (NCI) A member of the class of histamine H2-receptor antagonists with antacid activity. Ranitidine is a competitive and reversible inhibitor of the action of histamine, released by enterochromaffin-like (ECL) cells, at the histamine H2-receptors on parietal cells in the stomach, thereby inhibiting the normal and meal-stimulated secretion of stomach acid. In addition, other substances that promote acid secretion have a reduced effect on parietal cells when the H2 receptors are blocked.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D011899
SnomedCT 372755005, 48174005
English Ranitidin, Ranitidine, N (2-(((5-((Dimethylamino)methyl)-2-furanyl)methyl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine, ranitidine, 1,1-Ethenediamine, N-(2-(((5-((dimethylamino)methyl)-2-furanyl)methyl)thio)ethyl)-N'-methyl-2-nitro-, N-[2-[[[5-[(Dimethylamino)methyl]-2-furanyl]methyl]thio]ethyl]-N'-methyl-2-nitro-1,1-ethenediamine, ranitidine (medication), histamine-2 receptor antagonists ranitidine, RANITIDINE, Ranitidine [Chemical/Ingredient], ranitidin, Ranitidine (product), Ranitidine (substance)
Swedish Ranitidin
Czech ranitidin
Finnish Ranitidiini
Russian RANITIDIN, РАНИТИДИН
Japanese ラニチジン
Croatian RANITIDIN
Polish Ranitydyna
Spanish ranitidina (producto), ranitidina (sustancia), ranitidina, Ranitidina
French Ranitidine
German Ranitidin
Italian Ranitidina
Portuguese Ranitidina
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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