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Culture Documents
DB00863
DB00863
DB00863
Indication
This drug is used alone or with concomitant antacids for the following conditions: short-term
treatment of active duodenal ulcer, treating gastric acid hypersecretion due to Zollinger-Ellison
syndrome, systemic mastocytosis, and other conditions that may pathologically raise gastric acid
levels. It also used in the short term treatment of active benign gastric ulcers and maintenance
therapy of gastric ulcers at a reduced dose. In addition to the above, ranitidine can be used for
the treatment of GERD symptoms, treatment of erosive esophagitis (endoscopically diagnosed)
11,12
and the maintenance of gastric or duodenal ulcer healing.
Duodenal Ulce
Erosive Esophagiti
Gastric Ulce
Gastric hypersecretio
Healin
Heartbur
Osteoarthritis (OA
Rheumatoid Arthriti
Stress Ulcer
Zollinger-Ellison Syndrom
Pharmacodynamics
Ranitidine decreases the secretion of gastric acid stimulated by food and drugs. It also reduces
6,11
the secretion of gastric acid in hypersecretory conditions such as Zollinger-Ellison syndrome.
Marked improvements in the appearance of the esophageal tissues have been observed by
5,11
endoscopic imaging a er ranitidine therapy.
Mechanism of action
A er a meal, the hormone gastrin, produced by cells in the lining of the stomach, stimulates the
release of histamine, which then binds to histamine H2 receptors, leading to the secretion of
gastric acid. Ranitidine reduces the secretion of gastric acid by reversible binding to histamine
Adverse Effects
Toxicity
Oral doses of 1,000 mg/kg in mice and rats were not found to be lethal. Intravenous LD50 values
in mice and rats were 77 and 83 mg/kg, respectively.12
Overdose information
There has been limited experience with ranitidine overdose. Reported acute ingestions of up to 18
grams orally were followed by temporary adverse effects similar to the normal adverse effects of
this drug, including tachycardia, bradycardia, dizziness, diarrhea, nausea, and vomiting, among
other effects.12 Gait abnormalities and hypotension have also been observed. When an overdose
with ranitidine is suspected, remove unabsorbed ranitidine from the gastrointestinal tract if
11,13
possible, and monitor the patient and provide supportive therapy as required.
Affected organisms
Pathways
Drug action
Pharmacogenomic Effects/ADRs
Not Available
INTERACTIONS
Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are
experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not
necessarily mean no interactions exist.
APPROVED
VET APPROVED
NUTRACEUTICAL
ILLICIT
WITHDRAWN
INVESTIGATIONAL
EXPERIMENTAL
ALL DRUGS
DRUG INTERACTION
Ag-ranitidine Tablet Oral Angita Pharma Inc. Not applicable Not applicable
Apo-ranitidine Tablet 150mg Tablet Oral Apotex Corporation 1987-12-31 Not applicable
Apo-ranitidine Tablet 300mg Tablet Oral Apotex Corporation 1987-12-31 Not applicable
Good Sense Acid Reducer Tablet 75 mg/1 Oral bryant ranch prepack 2009-05-21 Not applicable
Unapproved/Other Products
MARKETING MARKETING
NAME INGREDIENTS DOSAGE ROUTE LABELLER START END
Over the Counter Products
MARKETING MARKETING
NAME DOSAGE STRENGTH ROUTE LABELLER START END
7 Select Acid Tablet, film 150 mg/1 Oral 7-Eleven 2014-04-22 2020-11-30
Reducer coated
Acid Reducer Tablet, film 75 mg/1 Oral Nucare Pharmaceuticals,inc. 2018-10-01 Not
coated applicable
Acid Reducer Tablet, film 75 mg/1 Oral Winco Foods 2012-08-02 Not
coated applicable
Acid Reducer Tablet, film 75 mg/1 Oral Good Sense 2013-10-11 Not
coated applicable
Acid Reducer Tablet 75.0 mg Oral Stanley Pharmaceuticals, A Division Of Vita Health 2000-03-27 2004-07-26
Products Inc.
Acid Reducer Tablet 150 mg/1 Oral Shopko Stores Operating 2013-06-05 2015-11-27
Acid Reducer Tablet, film 75 mg/1 Oral Ohm Laboratories Inc. 2012-07-10 2019-09-11
coated
Acid Reducer Tablet, film 75 mg/1 Oral Preferred Plus (Kinray) 2014-01-27 Not
coated applicable
Mixture Products
MARKETING MARKETING
NAME INGREDIENTS DOSAGE ROUTE LABELLER START END
DeramsilkRx Ranitidine hydrochloride (150 mg/1) + Capsicum oleoresin (0.25 mg/1mL) Kit Oral; Patchwerx 2015-06-12 Not
Anodynexa Pak + Diclofenac sodium (75 mg/1) Topical Labs applicable
08 01
DermacinRx Ranitidine hydrochloride (150 mg/1) + Capsicum oleoresin (0.25 mg/1mL) Kit Oral; PureTek 2015-06-12 2019-03-05
Inflammatral Pak + Diclofenac sodium (75 mg/1) Topical Corporation
Inflammation Ranitidine hydrochloride (150 mg/1) + Diclofenac sodium (75 mg/1) + Kit Oral; Tmig, Inc. 2015-08-18 Not
Reduction Pack Lidocaine (25 mg/1g) + Prilocaine (25 mg/1g) Topical applicable
Histamine H2 Antagonist
OAT1/SLC22A6 inhibitor
OAT1/SLC22A6 Substrate
OAT3/SLC22A8 Substrate
OCT1 inhibitor
OCT1 substrate
OCT2 Inhibitor
OCT2 Substrate
P-glycoprotein inhibitor
P-glycoprotein substrate
Classification
Not classified
CHEMICAL IDENTIFIERS
UNII
884KT10YB
CAS number
66357-35-5
InChI Key
VMXUWOKSQNHOCA-UHFFFAOYSA-N
InChI
InChI=1S/C13H22N4O3S/c1-14-13(9-17(18)19)15-6-7-21-10-12-5-4-11(20-12)8-16(2)3/h4-5,9,14-15H,6-8,10H2,1-3H3
IUPAC Name
[1-({2-[({5-[(
dimethylamino)methyl]furan-2-yl}methyl)sulfanyl]ethyl}amino)-2-nitroethenyl](methyl)amine
SMILES
CNC(NCCSCC1=CC=C(CN(C)C)O1)=C[N+]([O-])=O
REFERENCES
Synthesis Reference
John W. Clitherow, "Intermediates in the preparation of ranitidine." U.S. Patent US4413135, issued
November, 1981.
US441313
General References
1. Mauran A, Goze T, Abadie D, Bondon-Guitton E, Chevrel P, Schmitt L, Montastruc JL, Montastruc F: Mania associated with ranitidine: a
case report and review of literature. Fundam Clin Pharmacol. 2016 Aug;30(4):294-6. doi: 10.1111/fcp.12201. Epub 2016 May 5.
PubMed:2708338 ]
2. Grant SM, Langtry HD, Brogden RN: Ranitidine. An updated review of its pharmacodynamic and pharmacokinetic properties and
therapeutic use in peptic ulcer disease and other allied diseases. Drugs. 1989 Jun;37(6):801-70. doi: 10.2165/00003495-198937060-00003.
PubMed:266793 ]
3. Pettit M: Treatment of gastroesophageal reflux disease. Pharm World Sci. 2005 Dec;27(6):432-5. doi: 10.1007/s11096-005-4798-7.
PubMed:1634194 ]
4. Badillo R, Francis D: Diagnosis and treatment of gastroesophageal reflux disease. World J Gastrointest Pharmacol Ther. 2014 Aug
6;5(3):105-12. doi: 10.4292/wjgpt.v5.i3.105. [PubMed:2513303
]
5. Sontag S, Robinson M, McCallum RW, Barwick KW, Nardi R: Ranitidine therapy for gastroesophageal reflux disease. Results of a large
double-blind trial. Arch Intern Med. 1987 Aug;147(8):1485-91.PubMed:330767
[ ]
6. Vezzadini P, Bonora G, Tomassetti P, Pazzaglia M, Labo G: Medical treatment of Zollinger-Ellison syndrome with ranitidine. Int J Tissue
React. 1983;5(4):339-43.
PubMed:632333
[ ]
7. Roberts CJ: Clinical pharmacokinetics of ranitidine. Clin Pharmacokinet. 1984 May-Jun;9(3):211-21. doi: 10.2165/00003088-198409030-00003.
PubMed:632958 ]
8. Gschwend MH, Guserle R, Erenmemisoglu A, Martin W, Tamur U, Kanzik I, Hincal AA: Pharmacokinetics and bioequivalence study of
ranitidine film tablets in healthy male subjects. Arzneimittelforschung. 2007;57(6):315-9. doi: 10.1055/s-0031-1296625.
PubMed:1768807][
9. Caitlin C. Nugent; Jamie M. Terrell (2018). H2 Blockers- StatPearls. StatPearls Publishing.
10. FDA drug approval package: Zantac Lin ][
11. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injectionLin ] [
12. GlaxoSmithKline Canada Inc. Product Monograph: Zantac (ranitidine)Lin ] [
13. Ranitidine product monograph Lin []
14. Zantac injection FDA label Fil[ ]
15. Zantac Canadian Monograph Fil ][
External Links
HMDB000193
KEGG Drug
D0042
PubChem Compound
300105
PubChem Substance
4650554
ChemSpider
486
BindingDB
5010350
RxNav
914
ChEBI
9224
ChEMBL
CHEMBL179004
DAP00034
PharmGKB
PA45122
Guide to Pharmacology
RxList
Drugs.com
Wikipedia
Ranitidin
Water Solubility
0.0795 mg/mL
ALOGPS
logP
0.79
ALOGPS
logP
0.99
ChemAxon
logS
-3.6
ALOGPS
7.8
ChemAxon
Physiological Charge
ChemAxon
ChemAxon
ChemAxon
83.58 Å2
ChemAxon
10
ChemAxon
Refractivity
94.15 m3·mol-1
ChemAxon
Polarizability
33.78 Å3
ChemAxon
Number of Rings
ChemAxon
Bioavailability
ChemAxon
Rule of Five
Yes
ChemAxon
Ghose Filter
Histamine H2 receptor
Molecular Weight
40097.65Da
References
1. Pattichis K, Louca LL: Histamine, histamine H2-receptor antagonists, gastric acid secretion and ulcers: an overview. Drug
Metabol Drug Interact. 1995;12(1):1-36.PubMed:755499
[ ]
2. Grant SM, Langtry HD, Brogden RN: Ranitidine. An updated review of its pharmacodynamic and pharmacokinetic properties
and therapeutic use in peptic ulcer disease and other allied diseases. Drugs. 1989 Jun;37(6):801-70. doi: 10.2165/00003495-
198937060-00003. PubMed:266793
[ ]
3. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injectionLin ] [
2. Acetylcholinesteras
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
The FDA label indicates that ranitidine is not an anticholinergic agent, likely because its weak anticholinergic effects
observed in studies do not result in clinical effects.
General Function
Specific Function
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the
synaptic cle . Role in neuronal apoptosis.
Gene Name
ACHE
Uniprot ID
P2230
Uniprot Name
Acetylcholinesterase
Molecular Weight
67795.525Da
References
1. Petroianu GA, Arafat K, Schmitt A, Hasan MY: Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in
vitro effect of ranitidine. J Appl Toxicol. 2005 Jan-Feb;25(1):60-7. doi: 10.1002/jat.1036. [
PubMed:1566902 ]
2. Kounenis G, Koutsoviti-Papadopoulou M, Elezoglou V: The inhibition of acetylcholinesterase by ranitidine: a study on the guinea
pig ileum. J Pharmacobiodyn. 1986 Nov;9(11):941-5. PubMed:355988
[ ]
3. Aono M, Moriga M, Mizuta K, Narusawa H: Cholinergic effects of histamine-H2 receptor antagonists partly through inhibition of
acetylcholinesterase. Gastroenterol Jpn. 1986 Jun;21(3):213-9. doi: 10.1007/bf02774563.
PubMed:287409
[ ]
4. Laine-Cessac P, Turcant A, Premel-Cabic A, Boyer J, Allain P: Inhibition of cholinesterases by histamine 2 receptor antagonist
drugs. Res Commun Chem Pathol Pharmacol. 1993 Feb;79(2):185-93.
PubMed:809573
[ ]
Lin ] [
5. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injection
ENZYMES
1. Cytochrome P450 1A
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate Inhibitor
Curator comments
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or
flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an
NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P0517
Uniprot Name
Molecular Weight
58293.76Da
References
1. Martinez C, Albet C, Agundez JA, Herrero E, Carrillo JA, Marquez M, Benitez J, Ortiz JA: Comparative in vitro and in vivo
inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2-receptor antagonists. Clin Pharmacol Ther. 1999
PubMed:1022377
Apr;65(4):369-76. doi: 10.1016/S0009-9236(99)70129-3. [ ]
2. Zhou Q, Yan XF, Zhang ZM, Pan WS, Zeng S: Rational prescription of drugs within similar therapeutic or structural class for
gastrointestinal disease treatment: drug metabolism and its related interactions. World J Gastroenterol. 2007 Nov
14;13(42):5618-28.[PubMed:1794893]
2. Cytochrome P450 2D
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Data regarding this enzyme action are limited to in vitro studies and show weak inhibition,
General Function
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the
metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P1063
Uniprot Name
Molecular Weight
55768.94Da
References
1. Martinez C, Albet C, Agundez JA, Herrero E, Carrillo JA, Marquez M, Benitez J, Ortiz JA: Comparative in vitro and in vivo
inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2-receptor antagonists. Clin Pharmacol Ther. 1999
Apr;65(4):369-76. doi: 10.1016/S0009-9236(99)70129-3.
PubMed:1022377
[ ]
2. Sideras K, Ingle JN, Ames MM, Loprinzi CL, Mrazek DP, Black JL, Weinshilboum RM, Hawse JR, Spelsberg TC, Goetz MP:
Coprescription of tamoxifen and medications that inhibit CYP2D6. J Clin Oncol. 2010 Jun 1;28(16):2768-76. doi:
10.1200/JCO.2009.23.8931. Epub 2010 May[PubMed:2043962
3. ]
3. Flockhart Table of Drug InteractionsLin
[ ]
3. Cytochrome P450 3A
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Data limited to one in vitro study, with results showing weak inhibition and likely to have little clinical significance.
General Function
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an
NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P0868
Uniprot Name
Molecular Weight
57342.67Da
References
1. Martinez C, Albet C, Agundez JA, Herrero E, Carrillo JA, Marquez M, Benitez J, Ortiz JA: Comparative in vitro and in vivo
inhibition of cytochrome P450 CYP1A2, CYP2D6, and CYP3A by H2-receptor antagonists. Clin Pharmacol Ther. 1999
PubMed:1022377
Apr;65(4):369-76. doi: 10.1016/S0009-9236(99)70129-3. [ ]
2. Ranitidine drug summaryLin[ ]
Lin ] [
3. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers
4. Acetylcholinesteras
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Though ranitidine has been found to weakly inhibit acetylcholinesterase, the FDA label mentions that it is not an
anticholinergic agent.
General Function
Specific Function
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the
synaptic cle . Role in neuronal apoptosis.
Gene Name
ACHE
Uniprot ID
P2230
Uniprot Name
Acetylcholinesterase
Acetylcholinesterase
Molecular Weight
67795.525Da
References
1. Petroianu GA, Arafat K, Schmitt A, Hasan MY: Weak inhibitors protect cholinesterases from strong inhibitors (paraoxon): in
vitro effect of ranitidine. J Appl Toxicol. 2005 Jan-Feb;25(1):60-7. doi: 10.1002/jat.1036.
PubMed:1566902
[ ]
2. Laine-Cessac P, Turcant A, Premel-Cabic A, Boyer J, Allain P: Inhibition of cholinesterases by histamine 2 receptor antagonist
drugs. Res Commun Chem Pathol Pharmacol. 1993 Feb;79(2):185-93. [
PubMed:809573 ]
3. Aono M, Moriga M, Mizuta K, Narusawa H: Cholinergic effects of histamine-H2 receptor antagonists partly through inhibition of
acetylcholinesterase. Gastroenterol Jpn. 1986 Jun;21(3):213-9. doi: 10.1007/bf02774563. [
PubMed:287409 ]
4. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injection Lin []
TRANSPORTERS
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate Inhibitor
General Function
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model
compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O1524
Uniprot Name
Molecular Weight
61153.345Da
References
1. Meyer MJ, Seitz T, Brockmoller J, Tzvetkov MV: Effects of genetic polymorphisms on the OCT1 and OCT2-mediated uptake of
ranitidine. PLoS One. 2017 Dec 13;12(12):e0189521. doi: 10.1371/journal.pone.0189521. eCollection 2017. [
PubMed:2923675 ]
2. Han TK, Everett RS, Proctor WR, Ng CM, Costales CL, Brouwer KL, Thakker DR: Organic cation transporter 1 (OCT1/mOct1) is
localized in the apical membrane of Caco-2 cell monolayers and enterocytes. Mol Pharmacol. 2013 Aug;84(2):182-9. doi:
10.1124/mol.112.084517. Epub 2013 May [16.PubMed:2368063]
2. P-glycoprotein
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate Inhibitor
General Function
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P0818
Uniprot Name
Molecular Weight
141477.255Da
References
1. Lentz KA, Polli JW, Wring SA, Humphreys JE, Polli JE: Influence of passive permeability on apparent P-glycoprotein kinetics.
Pharm Res. 2000 Dec;17(12):1456-60. PubMed:1130395
[ ]
2. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of
PubMed:1295418
heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [ ]
3. Collett A, Higgs NB, Sims E, Rowland M, Warhurst G: Modulation of the permeability of H2 receptor antagonists cimetidine and
ranitidine by P-glycoprotein in rat intestine and the human colonic cell line Caco-2. J Pharmacol Exp Ther. 1999 Jan;288(1):171-
8. [PubMed:986276]
4. Dou L, Mai Y, Madla CM, Orlu M, Basit AW: P-glycoprotein expression in the gastrointestinal tract of male and female rats is
influenced differently by food. Eur J Pharm Sci. 2018 Oct 15;123:569-575. doi: 10.1016/j.ejps.2018.08.014. Epub 2018 Aug 15.
PubMed:3011885]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Actions
Substrate
Curator comments
Data for this transporter are limited to the results of an in vitro study.
General Function
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the
brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC
Uniprot Name
Molecular Weight
59855.585Da
References
1. Tahara H, Kusuhara H, Chida M, Fuse E, Sugiyama Y: Is the monkey an appropriate animal model to examine drug-drug
interactions involving renal clearance? Effect of probenecid on the renal elimination of H2 receptor antagonists. J Pharmacol
Exp Ther. 2006 Mar;316(3):1187-94. Epub 2005 Nov PubMed:1629187
16. [ ]
2. Torres AM: Renal elimination of organic anions in cholestasis. World J Gastroenterol. 2008 Nov 21;14(43):6616-21. doi:
10.3748/wjg.14.6616.[PubMed:1903496 ]
3. Kusuhara H, Sugiyama Y: Active efflux across the blood-brain barrier: role of the solute carrier family. NeuroRx. 2005 Jan;2(1):73-
85. doi: 10.1602/neurorx.2.1.73.
[PubMed:1571705 ]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine,
noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O1524
O15244
Uniprot Name
Molecular Weight
62579.99Da
References
1. Meyer MJ, Seitz T, Brockmoller J, Tzvetkov MV: Effects of genetic polymorphisms on the OCT1 and OCT2-mediated uptake of
ranitidine. PLoS One. 2017 Dec 13;12(12):e0189521. doi: 10.1371/journal.pone.0189521. eCollectionPubMed:2923675
2017. [ ]
2. Nies AT, Schwab M: Organic cation transporter pharmacogenomics and drug-drug interaction. Expert Rev Clin Pharmacol. 2010
Nov;3(6):707-11. doi: 10.1586/ecp.10.60. [
PubMed:2211177 ]
3. Straight Healthcare: OCT2 Lin
[ ]
Drug created on June 13, 2005 07:24 / Updated on January 16, 2021 12:52
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