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
  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: Adult
    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 orally twice daily
    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: 400-800 mg orally twice daily
    3. Famotidine (Pepcid)
      1. Oral dosing: 20 to 40 mg orally twice daily
    4. Nizatidine (Axid)
      1. Oral dosing: 150 mg orally twice daily
  3. Preparations: Children
    1. Ranitidine (Zantac) 15 mg/ml oral syrup
      1. Age <16 years old
        1. Dose: 5-10 mg/kg/day (max 300 mg) divided every 12 hours
      2. Adult dosing for over age 16 years old
        1. Dose: 150 mg twice daily
    2. Cimetidine (Tagamet) 300 mg/ml oral solution
      1. Newborns
        1. Dose: 5-10 mg/kg/day divided every 8-12 hours
      2. Infants
        1. Dose: 10-20 mg/kg/day divided every 6-12 hours
      3. Children <12 years old
        1. Dose: 20-40 mg/kg/day divided every 6 hours
      4. Adult dosing for over age 12 years old
        1. Dose: 800 mg orally twice daily
    3. Famotidine (Pepcid) 40 mg/5ml oral suspension
      1. Age 0-3 months
        1. Dose: 0.5 mg/kg/day orally daily
      2. Age 3 months to 16 years old
        1. Dose: 0.5 mg/kg orally twice daily
    4. Nizatidine (Axid) 15 mg/ml
      1. Age 6 months to 11 years old
        1. Dose: 5-10 mg/kg/day divided every 12 hours
      2. Adult dosing over age 12 years old
        1. Dose: 150 mg orally twice daily
    5. References
      1. Baird (2015) Am Fam Physician 92(8): 705-14 [PubMed]
  4. Precautions: Impaired Renal Function
    1. Creatinine Clearance <30 ml/min
      1. Give Cimetidine at half dose
    2. Creatinine Clearance <50 ml/min
      1. Give all H2 Blockers (except Cimetidine) at half dose
  5. 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 [PubMed]
  6. Disadvantages
    1. Even generic costs still approch Proton Pump Inhibitors
      1. (2003) Red Book, Medical Economics Data, Montvale, NJ
  7. Adverse Effects
    1. Cimetidine has more Drug Interactions and side effects
    2. Confusion
      1. Avoid H2 Blockers in cognitive Impairment (Dementia, Delirium)
  8. References
    1. (2012) Presc Lett, 19(7): 38
Medication Costs
Ranitidine (on 6/18/2017 at Walmart.com)
Ranitidine 150mg #60 tablets for $4.00 $0.07 each
Ranitidine 150mg #180 tablets for $10.00 $0.06 each
Ranitidine 300mg #30 tablets for $4.00 $0.13 each
Ranitidine 300mg #90 tablets for $10.00 $0.11 each
Famotidine (on 6/18/2017 at Walmart.com)
Famotidine 20mg #60 tablets for $4.00 $0.07 each
Famotidine 20mg #180 tablets for $10.00 $0.06 each
ranitidine (on 5/17/2017 at Medicaid.Gov Pharmacy Drug pricing)
RANITIDINE 15 MG/ML SYRUP Generic $0.02 per ml
RANITIDINE 150 MG CAPSULE Generic $0.63 each
RANITIDINE 150 MG TABLET Generic $0.06 each
RANITIDINE 300 MG CAPSULE Generic $1.26 each
RANITIDINE 300 MG TABLET Generic $0.12 each
RANITIDINE 75 MG TABLET Generic OTC $0.07 each
zantac (on 1/1/2017 at Medicaid.Gov Pharmacy Drug pricing)
ZANTAC 150 MG TABLET Generic $0.06 each
ZANTAC 300 MG TABLET Generic $0.12 each
ZANTAC 75 MG TABLET Generic OTC $0.07 each
cimetidine (on 5/17/2017 at Medicaid.Gov Pharmacy Drug pricing)
CIMETIDINE 200 MG TABLET Generic $0.32 each
CIMETIDINE 300 MG TABLET Generic $0.32 each
CIMETIDINE 300 MG/5 ML SOLN Generic $0.06 per ml
CIMETIDINE 400 MG TABLET Generic $0.53 each
CIMETIDINE 800 MG TABLET Generic $1.09 each
nizatidine (on 5/17/2017 at Medicaid.Gov Pharmacy Drug pricing)
NIZATIDINE 15 MG/ML SOLUTION Generic $0.53 per ml
NIZATIDINE 150 MG CAPSULE Generic $0.22 each
NIZATIDINE 300 MG CAPSULE Generic $0.63 each
famotidine (on 5/17/2017 at Medicaid.Gov Pharmacy Drug pricing)
FAMOTIDINE 10 MG TABLET Generic OTC $0.11 each
FAMOTIDINE 20 MG TABLET Generic $0.04 each
FAMOTIDINE 40 MG TABLET Generic $0.08 each
FAMOTIDINE 40 MG/5 ML SUSP Generic $0.81 per ml
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.

Cimetidine (C0008783)

Definition (NCI_NCI-GLOSS) 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 GASTRIN output.
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 (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 Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002927
SnomedCT 373541007, 83532008
LNC LP16078-5, MTHU004923
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, Cimetidine [Chemical/Ingredient], Guanidine, N''-Cyano-N-Methyl-N'-(2-(((5-Methyl-1H-Imidazol-4-yl)Methyl)Thio)Ethyl)-, Cimetidine (product), Cimetidine (substance)
Swedish Cimetidin
Czech cimetidin
Finnish Simetidiini
Russian TSIMETIDIN, ЦИМЕТИДИН
Japanese シメチジン
Croatian CIMETIDIN
Polish Cymetydyna
Norwegian Cimetidin
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 Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D015738
SnomedCT 387211002, 39128000
LNC LP14346-8, MTHU011541
English Famotidine, Propanimidamide, 3-(((2-((aminoiminomethyl)amino)-4-thiazolyl)methyl)thio)-N-(aminosulfonyl)-, famotidine (medication), histamine-2 receptor antagonists famotidine, 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
Norwegian Famotidin
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)


Ranitidine (C0034665)

Definition (CHV) a kind of antiacid drug
Definition (CHV) a kind of antiacid drug
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.
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.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D011899
SnomedCT 372755005, 48174005
LNC LP17253-3, MTHU005040
English Ranitidin, Ranitidine, N (2-(((5-((Dimethylamino)methyl)-2-furanyl)methyl)thio)ethyl)-N'-methyl-2-nitro-1,1-ethenediamine, 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, Ranitidine (product), Ranitidine (substance)
Swedish Ranitidin
Czech ranitidin
Finnish Ranitidiini
Russian RANITIDIN, РАНИТИДИН
Japanese ラニチジン
Croatian RANITIDIN
Polish Ranitydyna
Norwegian Ranitidin
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)


Nizatidine (C0085154)

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.
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.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D016567
SnomedCT 108664005, 386887009
LNC LP19170-7, MTHU007483
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
Norwegian Nizatidin
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)


Tagamet (C0592157)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D002927
English tagamet, Tagamet
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 Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D011899
English zantac, zantac [brand name], Zantac
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Pepcid (C0678119)

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


Axid (C0678129)

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


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