General
Preferred name
RANITIDINE
Synonyms
HSDB 3925 ()
Ranitidin ()
AH19065 ()
RANITIDINE HYDROCHLORIDE ()
RANITIDINE BISMUTH CITRATE ()
Tritec ()
NSC-757851 ()
Zantac ()
Gavilast-P ()
Zantac 150 ()
AH 19065 ()
Gavilast ()
Rantec ()
Zantac 75 Relief ()
Ranitil ()
Ranitic ()
Zaedoc 300 ()
Raciran 300 ()
Ranzac ()
Raniplex ()
Zantac 75 Dissolve ()
Zantac 25 ()
Zantac 75 Relief Dissolve ()
Histac ()
Vivatak ()
Raciran 150 ()
Ranicalm ()
Zantac 300 ()
Ranitidine hcl ()
Zantac 75 ()
Zaedoc 150 ()
AH-19065 ()
Taladine ()
Azantac ()
Dumoran ()
Ranitidine Bismutrex ()
GR-122311X ()
Pylorid ()
GR 122311X ()
P&D ID
PD071722
CAS
66357-35-5
Tags
drug
biased GPCR ligand
available
Approved by
FDA
First approval
1983
1996
1977
Drug Status
approved
withdrawn
Max Phase
Phase 4
Drug indication
Antagonist (to histamine-H2 receptors)
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
HALF-LIFE
2.5-3 hours [FDA label]. The plasma half-life is longer for elderly patients population due to a decrease in renal function, and is measured at 3-4 hours [FDA label].
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 [A176852], [FDA label]. Marked improvements in the appearance of the esophageal tissues have been observed by endoscopic imaging after ranitidine therapy [A176849]. ; ; ;
MOA
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, leading to 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 [A176774, T533].
ROE
This drug is mainly excreted in the urine. About 30% of a single oral dose has been measured in the urine as unchanged drug within 24 hours of ingestion [FDA label].
INDICATION
This drug is used alone or with concomitant antacids for the following conditions [FDA label]:; ; **Duodenal ulcer**; ; Treatment of active duodenal ulcer (short-term), maintenance therapy of duodenal ulcers after healing (reduced dose); ; **Pathological hypersecretion of gastric acid**; ; Zollinger-Ellison syndrome, systemic mastocytosis, and other conditions causing gastric acid hypersecretion; ; **Gastric ulcer**; ; Short term treatment of active gastric ulcer (benign), maintenance of healing after gastric acid ulcer therapy (reduced dose); ; **Other conditions**: ; ; Treatment of GERD symptoms (symptoms usually improve within 24 hours), treatment of erosive esophagitis (endoscopically diagnosed) and maintenance of healing [FDA label]; ; ; ; ; ; ; ; ; ; ; ;
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%). 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 [FDA label].
ABSORPTION
Ranitidine is 50% absorbed after an oral tablet and both the syrup and effervescent tablet formulations are found to be bioequivalent to the tablet form. After an intravenous (IV) injection, average peak levels of 440 to 545 ng/mL are attained about 2-3 hours after a single 150 mg dose. 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 showed decreased absorption of ranitidine [FDA label].
TOXICITY
**LD50**; ; 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 [F4253].; ; **Overdosage**; ; There has been limited experience with overdosage. Reported acute ingestions of up to 18 grams orally have been associated with temporary adverse effects that are similar to the normal adverse effects of this drug (see adverse effects section). Gait abnormalities and hypotension have also been observed. When overdose is suspected, attempt to remove unabsorbed ranitidine from the gastrointestinal tract, monitor the patient and provide supportive therapy as needed [FDA label].; ; **Pregnancy** ; ; Ranitidine is a pregnancy category B drug, meaning that animal studies have not shown harm caused by the drug to the fetus. Studies have been completed in rats and rabbits at doses reaching 160 times the human dose and have demonstrated that ranitidine does not exert effects on fertility or fetal growth. No sufficient and well-controlled studies in pregnant women have been performed. Because animal reproduction studies are not always reflective of human response, this drug should be used during pregnancy only if clearly required [FDA label].; ; **Nursing Mothers**; ; Ranitidine has been detected in human breastmilk. Use caution ranitidine is given to a nursing mother [FDA label].
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
12
BiasDB
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMatrix
EU-OPENSCREEN Bioactive Compound Library
Ki Database
LSP-MoA library (Laboratory of Systems Pharmacology)
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
46
Molecular Weight
314.14
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
10
Ring Count
1
Aromatic Ring Count
1
cLogP
1.46
TPSA
83.58
Fraction CSP3
0.54
Chiral centers
0.0
Largest ring
5.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Immunology/Inflammation
Neuroscience
Target
H2 receptor
MOA
Histamine Receptor antagonist
Source data
