Ranitidine

Identification

Summary

Ranitidine is a histamine H2 antagonist used to treat duodenal ulcers, Zollinger-Ellison syndrome, gastric ulcers, GERD, and erosive esophagitis.

Brand Names
Good Sense Acid Reducer, Wal-zan, Zantac
Generic Name
Ranitidine
DrugBank Accession Number
DB00863
Background

Ranitidine is a commonly used drug, classified as a histamine H2-receptor antagonist, and belongs to the same drug class as cimetidine and famotidine. This drug helps to prevent and treat gastric-acid associated conditions, including ulcers, because of its ability to decrease gastric acid secretion.2,11 Ranitidine is often referred to as Zantac, and is available in various forms, including tablet, injection, and effervescent tablet preparations.11,14

The prevalence of GERD is thought to be 10-20% in western countries.4 Ranitidine has proven to be an effective treatment for relieving uncomfortable symptoms of gastric acid associated conditions and is therefore widely used in GERD and other gastric-acid related conditions.5,11

Type
Small Molecule
Groups
Approved, Withdrawn
Structure
Weight
Average: 314.4
Monoisotopic: 314.141261758
Chemical Formula
C13H22N4O3S
Synonyms
  • Ranitidina
  • Ranitidine
  • Ranitidinum

Pharmacology

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) and the maintenance of gastric or duodenal ulcer healing.11,12

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Prophylaxis ofAcid aspiration syndrome•••••••••••••••••••••• ••••••
Used in combination for symptomatic treatment ofAnkylosing spondylitisRegimen in combination with: Capsicum oleoresin (DB11131), Diclofenac (DB00586)••••••••••••
Prophylaxis ofDuodenal ulcer•••••••••••••••••••••• ••••••
Treatment ofDuodenal ulcer•••••••••••••••••••••
Used in combination for symptomatic treatment ofDuodenal ulcerRegimen in combination with: Diclofenac (DB00586), Capsicum oleoresin (DB11131)••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Ranitidine decreases the secretion of gastric acid stimulated by food and drugs. It also reduces the secretion of gastric acid in hypersecretory conditions such as Zollinger-Ellison syndrome.6,11 Marked improvements in the appearance of the esophageal tissues have been observed by endoscopic imaging after ranitidine therapy.5,11

Mechanism of action

After 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 (H2) receptors, which are found on gastric parietal cells. This process leads to the inhibition of histamine binding to this receptor, causing the reduction of gastric acid secretion. The relief of gastric-acid related symptoms can occur as soon as 60 minutes after administration of a single dose, and the effects can last from 4-10 hours, providing fast and effective symptomatic relief.3,9,11

TargetActionsOrganism
AHistamine H2 receptor
antagonist
Humans
UAcetylcholinesterase
inhibitor
Humans
Absorption

Ranitidine is rapidly absorbed with peak concentrations reached within 1-3 hours after administration, and varying greatly among patients. Bioavailability is about 50%-60% due to hepatic metabolism.7,13 In a pharmacokinetic study of healthy males, the AUC 0-infinity was about 2,488.6 ng x h/mL and the median Tmax was 2.83 hours.8 Food or antacids have limited effects on absorption. One clinical study found that the administration of a potent antacid (150 mmol) in subjects in the fasted state led to decreased absorption of ranitidine.11

Volume of distribution

The volume of distribution is higher than body volume, and measures at approximately 1.4 L/kg.7,11 It concentrates in breast milk, but does not readily distribute into the cerebrospinal fluid.7

Protein binding

The plasma protein binding of ranitidine is approximately 15%.7,11

Metabolism

The major metabolite in the urine is N-oxide, which represents less than 4% of the dose. Other metabolites of ranitidine include S-oxide (1%) and desmethyl ranitidine (1%).11,13 The feces contain the remainder of the excreted ranitidine dose. Liver dysfunction has been shown to cause small, but clinically insignificant, changes in various ranitidine pharmacokinetic parameters.11

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Route of elimination

This drug is mainly excreted in the urine but also excreted in the feces.7,13 About 30% of a single oral dose has been measured in the urine as unchanged drug within 24 hours of ingestion.11

Half-life

The elimination half-life or ranitidine is about 2.5-3 hours.7,11 It may be longer after oral administration versus injection.7 The plasma half-life is longer for elderly patients population due to a decrease in renal function, and is measured at 3-4 hours.7,11

Clearance

Renal clearance is about 410 mL/min according to FDA prescribing information.11 Another resource mentions a plasma clearance of approximately 600 ml/min.7 Clearance is decreased in the elderly and those with impaired or hepatic renal function.7,11 It is recommended to decrease the dose of ranitidine by one-half in patients with renal impairment.11

Adverse Effects
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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 possible, and monitor the patient and provide supportive therapy as required.11,13

Pathways
PathwayCategory
Ranitidine Action PathwayDrug action
Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
Not Available

Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
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.
DrugInteraction
AbacavirRanitidine may decrease the excretion rate of Abacavir which could result in a higher serum level.
AbametapirThe serum concentration of Ranitidine can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Ranitidine can be increased when combined with Abatacept.
AbirateroneThe serum concentration of Ranitidine can be increased when it is combined with Abiraterone.
AcebutololThe metabolism of Acebutolol can be decreased when combined with Ranitidine.
Food Interactions
  • Take with or without food. The absorption is unaffected by food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Ranitidine bismuth citrate7AJ51I17KG128345-62-0XAUTYMZTJWXZHZ-UHFFFAOYSA-K
Ranitidine hydrochlorideBK76465IHM66357-59-3GGWBHVILAJZWKJ-UHFFFAOYSA-N
Product Images
International/Other Brands
Alquen / Gastrolav / Gastrosedol / Kuracid / Ptinolin / Raniberl / Ranicux / Ranidil / Ranidin / Ranidine / Ranidura / Ranigast / Raniplex / Ranisan / Ranitab / Ranitic / Ranitidin / Ranitin / Ranitine / Ranobel / Rantacid / Ranuber / Renatac / Sostril / Tanidina / Toriol / Ulcodin / Zandid / Zantic
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Acid ReducerTablet150 mgOralPendopharm Division Of Pharmascience IncNot applicableNot applicableCanada flag
Act RanitidineTablet150 mgOralTEVA Canada Limited2004-04-192020-08-17Canada flag
Act RanitidineTablet300 mgOralTEVA Canada Limited2004-02-192020-08-17Canada flag
Bci RanitidineTablet300 mgOralBaker Cummins IncNot applicableNot applicableCanada flag
Bci RanitidineTablet150 mgOralBaker Cummins IncNot applicableNot applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Ag-ranitidineTablet300 mgOralAngita Pharma Inc.Not applicableNot applicableCanada flag
Ag-ranitidineTablet150 mgOralAngita Pharma Inc.2019-08-142021-12-03Canada flag
Apo-ranitidineSolution75 mg / 5 mLOralApotex Corporation2006-07-14Not applicableCanada flag
Apo-ranitidine Tablet 150mgTablet150 mgOralApotex Corporation1987-12-31Not applicableCanada flag
Apo-ranitidine Tablet 300mgTablet300 mgOralApotex Corporation1987-12-31Not applicableCanada flag
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
7 Select Acid ReducerTablet, film coated150 mg/1Oral7-Eleven2014-04-222020-11-30US flag
Acid ReducerTablet75 mgOralVita Health Products Inc2006-03-312009-08-06Canada flag
Acid ReducerTablet150 mg/1OralShopko Stores Operating2013-06-052015-11-27US flag
Acid ReducerTablet, film coated75 mg/1OralRite Aid2013-06-152018-07-15US flag
Acid ReducerTablet75 mgOralVita Health Products Inc2008-01-31Not applicableCanada flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
DeramsilkRx Anodynexa PakRanitidine hydrochloride (150 mg/1) + Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1)KitOral; TopicalPatchwerx Labs2015-06-12Not applicableUS flag
DermacinRx Inflammatral PakRanitidine hydrochloride (150 mg/1) + Capsicum oleoresin (0.25 mg/1mL) + Diclofenac sodium (75 mg/1)KitOral; TopicalPureTek Corporation2015-06-122019-03-05US flag
Inflammation Reduction PackRanitidine hydrochloride (150 mg/1) + Diclofenac sodium (75 mg/1) + Lidocaine (25 mg/1g) + Prilocaine (25 mg/1g)KitOral; TopicalTmig, Inc.2015-08-18Not applicableUS flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
DeprizineRanitidine hydrochloride (4.2 g/4.2g)KitOralFusion Pharmaceuticals LLC2010-02-082014-08-01US flag
DeprizineRanitidine hydrochloride (6.4 g/6.4g)KitOralCalifornia Pharmaceuticals, Llc2016-01-012018-01-05US flag
GabitidineRanitidine hydrochloride (150 mg/1) + Choline (125 mg/1)KitOralPhysician Therapeutics Llc2011-07-07Not applicableUS flag
Ranitidine Hydrochloride Oral Suspension KitRanitidine hydrochloride (6.4 g/6.4g)KitOralCalifornia Pharmaceuticals, Llc2017-01-02Not applicableUS flag
SentradineRanitidine hydrochloride (150 mg/1) + Choline (250 mg/1)KitOralPhysician Therapeutics Llc2011-07-07Not applicableUS flag

Categories

ATC Codes
A02BA07 — Ranitidine bismuth citrateA02BA02 — Ranitidine
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
884KT10YB7
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.

US4413135
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. [Article]
  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. [Article]
  3. Pettit M: Treatment of gastroesophageal reflux disease. Pharm World Sci. 2005 Dec;27(6):432-5. doi: 10.1007/s11096-005-4798-7. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  7. Roberts CJ: Clinical pharmacokinetics of ranitidine. Clin Pharmacokinet. 1984 May-Jun;9(3):211-21. doi: 10.2165/00003088-198409030-00003. [Article]
  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. [Article]
  9. Caitlin C. Nugent; Jamie M. Terrell (2018). H2 Blockers- StatPearls. StatPearls Publishing.
  10. FDA drug approval package: Zantac [Link]
  11. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injection [Link]
  12. GlaxoSmithKline Canada Inc. Product Monograph: Zantac (ranitidine) [Link]
  13. Ranitidine product monograph [Link]
  14. Zantac injection FDA label [File]
  15. Zantac Canadian Monograph [File]
Human Metabolome Database
HMDB0259516
KEGG Drug
D00422
PubChem Compound
3001055
PubChem Substance
46505543
ChemSpider
4863
BindingDB
50103506
RxNav
9143
ChEBI
92246
ChEMBL
CHEMBL1790041
Therapeutic Targets Database
DAP000340
PharmGKB
PA451224
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Ranitidine
FDA label
Download (1.03 MB)
MSDS
Download (73.9 KB)

Clinical Trials

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Pharmacoeconomics

Manufacturers
  • Dr reddys laboratories ltd
  • Genpharm inc
  • Sandoz inc
  • Teva pharmaceuticals usa inc
  • Glaxosmithkline
  • Bedford laboratories div ben venue laboratories inc
  • Ben venue laboratories inc
  • Alpharma us pharmaceuticals division
  • Amneal pharmaceuticals
  • Apotex inc
  • Aurobindo pharma usa inc
  • Cypress pharmaceutical inc
  • Pharmaceutical assoc inc div beach products
  • Ranbaxy laboratories ltd
  • Vintage pharmaceuticals inc
  • Wockhardt ltd
  • Boehringer ingelheim pharmaceuticals inc
  • Amneal pharmaceuticals ny llc
  • Boehringer ingelheim corp
  • Contract pharmacal corp
  • Dr reddys laboratories inc
  • Glenmark generics inc usa
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan pharmaceuticals inc
  • Par pharmaceutical inc
  • L perrigo co
  • Ranbaxy pharmaceuticals inc
  • Torpharm inc
  • Watson laboratories inc
  • Wockhardt americas inc
  • Boehringer ingelheim
Packagers
  • Actavis Group
  • Advanced Pharmaceutical Services Inc.
  • Aidarex Pharmacuticals LLC
  • Amerisource Health Services Corp.
  • Amneal Pharmaceuticals
  • Apotex Inc.
  • Apotheca Inc.
  • Apothecon
  • AQ Pharmaceuticals Inc.
  • A-S Medication Solutions LLC
  • Banner Pharmacaps Inc.
  • Bedford Labs
  • Ben Venue Laboratories Inc.
  • Blenheim Pharmacal
  • Boehringer Ingelheim Ltd.
  • Bryant Ranch Prepack
  • Cardinal Health
  • Central Texas Community Health Centers
  • Chain Drug
  • Cobalt Pharmaceuticals Inc.
  • Comprehensive Consultant Services Inc.
  • Corepharma LLC
  • Coupler Enterprises Inc.
  • CVS Pharmacy
  • Dept Health Central Pharmacy
  • DHHS Program Support Center Supply Service Center
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • Doctor Reddys Laboratories Ltd.
  • DSM Corp.
  • Fusion Pharmaceuticals LLC
  • Genpharm LP
  • GlaxoSmithKline Inc.
  • Glenmark Generics Ltd.
  • Golden State Medical Supply Inc.
  • H.J. Harkins Co. Inc.
  • Heartland Repack Services LLC
  • Hospira Inc.
  • Innovative Manufacturing and Distribution Services Inc.
  • Innoviant Pharmacy Inc.
  • Ivax Pharmaceuticals
  • Kaiser Foundation Hospital
  • Keltman Pharmaceuticals Inc.
  • Lake Erie Medical and Surgical Supply
  • Liberty Pharmaceuticals
  • Major Pharmaceuticals
  • Mckesson Corp.
  • Medisca Inc.
  • Medvantx Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • Novopharm Ltd.
  • Nucare Pharmaceuticals Inc.
  • Ohm Laboratories Inc.
  • Palmetto Pharmaceuticals Inc.
  • Par Pharmaceuticals
  • Patheon Inc.
  • PCA LLC
  • PD-Rx Pharmaceuticals Inc.
  • Penn Labs
  • Perrigo Co.
  • Pharmaceutical Association
  • Pharmaceutical Packaging Center
  • Pharmedix
  • Physicians Total Care Inc.
  • Precision Dose Inc.
  • Preferred Pharmaceuticals Inc.
  • Prepackage Specialists
  • Prepak Systems Inc.
  • Prescription Dispensing Service Inc.
  • Prx Pharmaceuticals
  • Ranbaxy Laboratories
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Roxane Labs
  • Sandhills Packaging Inc.
  • Sandoz
  • Shasun Chemicals & Drugs Ltd.
  • Southwood Pharmaceuticals
  • St Mary's Medical Park Pharmacy
  • Sunmark
  • Teva Pharmaceutical Industries Ltd.
  • Torpharm Inc.
  • Tya Pharmaceuticals
  • UDL Laboratories
  • Va Cmop Dallas
  • Vangard Labs Inc.
  • Vistapharm Inc.
  • Walgreen Co.
  • Watson Pharmaceuticals
  • Wockhardt Ltd.
  • Xactdose Inc.
Dosage Forms
FormRouteStrength
TabletOral75 mg / tab
TabletOral75.0 mg / tab
TabletOral300.000 mg
SolutionIntravenous56.45 mg
TabletOral150.000 mg
InjectionIntramuscular; Intravenous50 MG/2ML
Tablet, film coatedOral400 mg
KitOral4.2 g/4.2g
KitOral6.4 g/6.4g
KitOral; Topical
Tablet, film coatedOral
Tablet, effervescentOral150 MG
Tablet, effervescentOral300 MG
TabletOral75 mg/1
Tablet, film coatedOral150.00 mg
Tablet, effervescentOral75 MG
SuspensionOral3500.000 mg
SolutionOral4.000 g
SyrupOral1.680 g
InjectionParenteral
TabletOral400 mg
SyrupOral1.500 mg
SyrupOral
Granule, for solutionOral150 MG
Syrup150 MG/10ML
TabletOral100 MG
SolutionParenteral50.000 mg
TabletOral300.00 mg
TabletOral75.000 mg
Tablet, coatedOral150 mg
Tablet, delayed releaseOral300 mg
Tablet, coatedOral334.88 mg
Tablet, coatedOral33488000 mg
SolutionIntravenous50 mg
Injection, solutionIntravenous50 MG/5ML
Tablet, coatedOral300 mg
TabletOral150 MG
TabletOral300 MG
Tablet, film coatedOral75 MG
InjectionIntramuscular; Intravenous25 mg/1mL
SolutionOral15 mg/1mL
SolutionOral15.0 mg/1mL
SolutionOral150 mg/1mL
SyrupOral15 mg/1mL
SyrupTopical15 mg/1mL
Tablet, coatedOral150 mg/1
Tablet, coatedOral75 mg/1
Tablet, film coatedOral150 mg/1
Tablet, film coatedOral300 mg/1
Tablet, film coatedOral167.4 MG
CapsuleOral150 mg/1
CapsuleOral300 mg/1
Injection
PowderNot applicable1 g/1g
SolutionOral150 mg/10mL
SolutionOral75 mg/5mL
TabletOral150 mg/1
TabletOral300 mg/1
Tablet, film coatedOral75 mg/1
InjectionIntramuscular; Intravenous25 MG/ML
Tablet, coatedOral
TabletOral
InjectionIntramuscular; Intravenous29.3 mg/ml
SyrupOral1.50 g
Tablet, coatedOral15000000 mg
TabletOral75 mg
KitOral
Solution50.000 mg
TabletOral150.00 mg
SyrupOral1.500 g
SolutionIntramuscular; Intravenous25 mg / mL
SolutionOral75 mg / 5 mL
Injection, solution
Tablet, solubleOral
InjectionIntramuscular; Intravenous
Tablet, delayed releaseOral150 mg
Granule, for solutionOral
Injection, solutionIntravenous
Syrup
SolutionIntramuscular; Intravenous25 mg/ml
SolutionIntramuscular; Intravenous
SolutionIntramuscular; Intravenous50 mg
Tablet, coatedOral167.4 mg
SolutionIntramuscular50.00 mg
InjectionParenteral50 mg
Tablet, effervescentOral
ConcentrateIntravenous
Injection, solutionIntramuscular; Intravenous50 mg/2ml
SolutionParenteral50 mg
Injection, solutionIntramuscular; Intravenous25 mg/1mL
Injection, solutionIntravenous50 mg/50mL
LiquidIntramuscular; Intravenous25 mg / mL
SolutionIntramuscular; Intravenous50 mg / 2 mL
TabletOral84 mg/1
Tablet, effervescentOral25 mg/1
Tablet, effervescentOral168 mg
Tablet, effervescentOral150 mg/1
SolutionOral15 mg / mL
Syrup150 ml
SyrupOral150 mg/10ml
TabletOral150 mg / tab
TabletOral300 mg / tab
CapsuleOral150 mg / cap
CapsuleOral300 mg / cap
TabletOral
Injection, solution25 mg/1ml
Tablet, film coatedOral150 mg
Tablet, film coatedOral300 mg
Solution25 mg/1ml
Prices
Unit descriptionCostUnit
Zantac 300 mg tablet7.96USD tablet
Ranitidine hcl powder5.2USD g
Zantac EFFERdose 25 mg Effervescent Tabs4.18USD tab
Zantac 25 efferdose tablet4.02USD tablet
Zantac 150 mg tablet3.11USD tablet
Ranitidine HCl 300 mg capsule2.85USD capsule
Ranitidine HCl 300 mg tablet2.79USD tablet
Ranitidine 300 mg tablet2.69USD tablet
Ranitidine hcl 25 mg/ml vial2.0USD ml
Zantac 25 mg/ml vial2.0USD ml
Ranitidine HCl 150 mg capsule1.58USD capsule
Zantac 25 mg/ml1.58USD ml
Ranitidine HCl 150 mg tablet1.54USD tablet
Ranitidine 150 mg tablet1.48USD tablet
Ranitidine 25 mg/ml1.26USD ml
Ranitidine HCl 15 mg/ml Syrup1.0USD ml
Ratio-Ranitidine 300 mg Tablet0.82USD tablet
Apo-Ranitidine 300 mg Tablet0.82USD tablet
Co Ranitidine 300 mg Tablet0.82USD tablet
Mylan-Ranitidine 300 mg Tablet0.82USD tablet
Nu-Ranit 300 mg Tablet0.82USD tablet
Pms-Ranitidine 300 mg Tablet0.82USD tablet
Ran-Ranitidine 300 mg Tablet0.82USD tablet
Zantac 15 mg/ml Syrup0.81USD ml
Zantac 75 tablet0.49USD tablet
Apo-Ranitidine 150 mg Tablet0.42USD tablet
Co Ranitidine 150 mg Tablet0.42USD tablet
Mylan-Ranitidine 150 mg Tablet0.42USD tablet
Nu-Ranit 150 mg Tablet0.42USD tablet
Pms-Ranitidine 150 mg Tablet0.42USD tablet
Ran-Ranitidine 150 mg Tablet0.42USD tablet
Ratio-Ranitidine 150 mg Tablet0.42USD tablet
Novo-Ranidine 300 mg Tablet0.38USD tablet
Phl-Ranitidine 300 mg Tablet0.38USD tablet
Sandoz Ranitidine 300 mg Tablet0.38USD tablet
Zantac 300 mg Tablet0.38USD tablet
Zantac 75 mg tablet0.28USD tablet
Wal-zan 75 mg tablet0.27USD tablet
Zantac 15 mg/ml Solution0.23USD ml
Ranitidine hcl 75 mg tablet0.22USD tablet
Sm acid reducer 75 mg tablet0.22USD tablet
Acid reducer 150 mg tablet0.2USD tablet
Wal-zan 75 tablet0.2USD tablet
Novo-Ranidine 150 mg Tablet0.19USD tablet
Phl-Ranitidine 150 mg Tablet0.19USD tablet
Sandoz Ranitidine 150 mg Tablet0.19USD tablet
Zantac 150 mg Tablet0.19USD tablet
CVS Pharmacy ranitidine 75 mg tablet0.15USD tablet
Apo-Ranitidine 15 mg/ml Solution0.12USD ml
Novo-Ranidine 15 mg/ml Solution0.12USD ml
Acid reducer 75 mg tablet0.11USD tablet
CVS Pharmacy acid reducer 75 mg tablet0.11USD tablet
Qc ranitidine 75 mg tablet0.07USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5098715No1992-03-242010-12-20US flag
US5102665No1992-04-072009-12-23US flag
CA1332610No1994-10-182011-10-18Canada flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)134https://www.chemicalbook.com/ChemicalProductProperty_US_CB3685534.aspx
water solubilitysoluble in waterhttps://www.chemicalbook.com/ChemicalProductProperty_US_CB3685534.aspx
logP0.2https://www.fip.org/files/fip/BPS/BCS/Monographs/Ranitidine_Hydrochloride.pdf
Caco2 permeability0.49https://www.ncbi.nlm.nih.gov/pubmed/9755906
pKa 8.2 and 2.7https://www.fip.org/files/fip/BPS/BCS/Monographs/Ranitidine_Hydrochloride.pdf
Predicted Properties
PropertyValueSource
Water Solubility0.0795 mg/mLALOGPS
logP0.79ALOGPS
logP0.99Chemaxon
logS-3.6ALOGPS
pKa (Strongest Basic)7.8Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count5Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area83.58 Å2Chemaxon
Rotatable Bond Count10Chemaxon
Refractivity94.15 m3·mol-1Chemaxon
Polarizability33.78 Å3Chemaxon
Number of Rings1Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9936
Blood Brain Barrier-0.8783
Caco-2 permeable-0.5838
P-glycoprotein substrateSubstrate0.8527
P-glycoprotein inhibitor INon-inhibitor0.8782
P-glycoprotein inhibitor IINon-inhibitor0.8893
Renal organic cation transporterNon-inhibitor0.8177
CYP450 2C9 substrateNon-substrate0.7702
CYP450 2D6 substrateSubstrate0.7414
CYP450 3A4 substrateNon-substrate0.5565
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.923
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8308
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7819
Ames testNon AMES toxic0.9132
CarcinogenicityNon-carcinogens0.8077
BiodegradationNot ready biodegradable0.9249
Rat acute toxicity2.0903 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.8628
hERG inhibition (predictor II)Non-inhibitor0.8734
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-166.67119
predicted
DeepCCS 1.0 (2019)
[M+H]+169.02922
predicted
DeepCCS 1.0 (2019)
[M+Na]+175.12248
predicted
DeepCCS 1.0 (2019)

Targets

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Details
1. Histamine H2 receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Histamine receptor activity
Specific Function
The H2 subclass of histamine receptors mediates gastric acid secretion. Also appears to regulate gastrointestinal motility and intestinal secretion. Possible role in regulating cell growth and diff...
Gene Name
HRH2
Uniprot ID
P25021
Uniprot Name
Histamine H2 receptor
Molecular Weight
40097.65 Da
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. [Article]
  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. [Article]
  3. Rubinstein R, Nissenkorn I, Cohen S: Acetylcholine mediation of the contractile response to histamine in human bladder detrusor muscle. Eur J Pharmacol. 1987 Oct 6;142(1):45-50. doi: 10.1016/0014-2999(87)90652-2. [Article]
  4. Doenicke A, Moss J, Lorenz W, Hoernecke R, Gottardis M: Are hypotension and rash after atracurium really caused by histamine release? Anesth Analg. 1994 May;78(5):967-72. doi: 10.1213/00000539-199405000-00023. [Article]
  5. Kirch W, Hutt HJ, Heidemann H, Ramsch K, Janisch HD, Ohnhaus EE: Drug interactions with nitrendipine. J Cardiovasc Pharmacol. 1984;6 Suppl 7:S982-5. [Article]
  6. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injection [Link]
Details
2. Acetylcholinesterase
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
Serine hydrolase activity
Specific Function
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name
ACHE
Uniprot ID
P22303
Uniprot Name
Acetylcholinesterase
Molecular Weight
67795.525 Da
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. [Article]
  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. [Article]
  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. [Article]
  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. [Article]
  5. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injection [Link]

Enzymes

Details
1. Cytochrome P450 3A4
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
Vitamin d3 25-hydroxylase activity
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
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
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. [Article]
  2. Ranitidine drug summary [Link]
  3. FDA Drug Development and Drug Interactions: Table of Substrates, Inhibitors and Inducers [Link]
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
Serine hydrolase activity
Specific Function
Terminates signal transduction at the neuromuscular junction by rapid hydrolysis of the acetylcholine released into the synaptic cleft. Role in neuronal apoptosis.
Gene Name
ACHE
Uniprot ID
P22303
Uniprot Name
Acetylcholinesterase
Molecular Weight
67795.525 Da
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. [Article]
  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. [Article]
  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. [Article]
  4. FDA Approved Drug Products: ZANTAC (ranitidine hydrochloride) injection [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
Data supporting this enzyme action are limited to in vitro studies.
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
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
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. [Article]
  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. [Article]
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
Steroid hydroxylase activity
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
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
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. [Article]
  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 3. [Article]
  3. Flockhart Table of Drug Interactions [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Secondary active organic cation transmembrane transporter activity
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
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
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. [Article]
  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. [Article]
Details
2. P-glycoprotein 1
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
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. [Article]
  2. Faassen F, Vogel G, Spanings H, Vromans H: Caco-2 permeability, P-glycoprotein transport ratios and brain penetration of heterocyclic drugs. Int J Pharm. 2003 Sep 16;263(1-2):113-22. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
Data for this transporter are limited to the results of an in vitro study.
General Function
Sodium-independent organic anion transmembrane transporter activity
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
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
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 16. [Article]
  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. [Article]
  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. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Quaternary ammonium group transmembrane transporter activity
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
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
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. [Article]
  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. [Article]
  3. Straight Healthcare: OCT2 [Link]

Drug created at June 13, 2005 13:24 / Updated at February 21, 2024 02:38