Cimetidine

Histamine-2 Receptor Antagonist — ALIMENTARY TRACT AND METABOLISM

Key facts

Cimetidine is an ofp drug in the Histamine-2 Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1977. Its mechanism of action is classified as Histamine H2 Receptor Antagonists. DrugCentral lists 6 molecular targets, including HRH2, HRH2 and SLC47A1. Recorded indications include Duodenal ulcer disease, Gastric ulcer, Gastroesophageal reflux disease and Heartburn.

• Approval status: ofp (first approved 1977 by the FDA).
• Drug class: Histamine-2 Receptor Antagonist.
• Mechanism of action: Histamine H2 Receptor Antagonists.
• Molecular targets: HRH2, HRH2, SLC47A1 and Hrh2 (6 listed in DrugCentral).
• Indications: Duodenal ulcer disease, Gastric ulcer, Gastroesophageal reflux disease, Heartburn and Indigestion and others.
• ATC code: A02BA01 (H2-receptor antagonists).
• Molecular formula: C10H16N6S; molecular weight 252.34 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (11)

• Duodenal ulcer disease
• Gastric ulcer
• Gastroesophageal reflux disease
• Heartburn
• Indigestion
• Maintenance of Healing Duodenal Ulcer
• Multiple endocrine adenomas
• Systemic mast cell disease
• Upper gastrointestinal hemorrhage
• Upper GI Bleed Prevention
• Zollinger-Ellison syndrome

Off-label uses (4)

• NSAID-Induced Gastric Ulcer
• Pancreatic insufficiency
• Prevention of Stress Ulcer
• Urticaria

Contraindications (3)

• Disease of liver
• Impaired renal function disorder
• Malignant tumor of stomach

Mechanism & targets

• Mechanism of action (MoA): Histamine H2 Receptor Antagonists
• Established pharmacologic class: Histamine-2 Receptor Antagonist

Molecular targets (6)

Target	Gene	Action	Activity
Histamine H2 receptor	HRH2	unknown	Kd 6.58
Histamine H2 receptor	HRH2	antagonist	Kd 6.14
Multidrug and toxin extrusion protein 1	SLC47A1	unknown	IC50 5.92
Histamine H2 receptor	Hrh2	antagonist	Ki 5.90
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 5.16
Multidrug and toxin extrusion protein 2	SLC47A2	inhibitor	Ki 5.10

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1977-08-16	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
A02BA01	ALIMENTARY TRACT AND METABOLISM › DRUGS FOR ACID RELATED DISORDERS › DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) › H2-receptor antagonists
A02BA51	ALIMENTARY TRACT AND METABOLISM › DRUGS FOR ACID RELATED DISORDERS › DRUGS FOR PEPTIC ULCER AND GASTRO-OESOPHAGEAL REFLUX DISEASE (GORD) › H2-receptor antagonists

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Chronic kidney disease	402.7
Body tinea	187.7
Urine abnormality	170.7
Inhibitory drug interaction	154.3
Infection susceptibility increased	150.3
Poor quality sleep	135.1
Urine leukocyte esterase positive	130.0
Lymphocyte count decreased	129.0
Glucose tolerance impaired	115.4
Bone density decreased	97.0
Culture urine positive	91.8
Impaired work ability	87.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Cimetidine is on its molecule page.

• Molecular formula: C₁₀H₁₆N₆S
• Molecular weight: 252.34 g/mol
• CAS number: 51481-61-9
• InChIKey: AQIXAKUUQRKLND-UHFFFAOYSA-N
• PubChem CID: 2756

CNC(NCCSCC1=C(C)NC=N1)=NC#N

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Cimetidine used for?

DrugCentral lists the following indications for Cimetidine: Duodenal ulcer disease, Gastric ulcer, Gastroesophageal reflux disease, Heartburn, Indigestion, Maintenance of Healing Duodenal Ulcer, Multiple endocrine adenomas and Systemic mast cell disease and others.

How does Cimetidine work?

Cimetidine is classified as Histamine H2 Receptor Antagonists; its molecular targets in DrugCentral include HRH2, HRH2 (antagonist), SLC47A1 and Hrh2 (antagonist).

When was Cimetidine first approved?

Cimetidine was first approved by the FDA in 1977.

What drug class does Cimetidine belong to?

Cimetidine is in the Histamine-2 Receptor Antagonist class.

What is the chemical formula of Cimetidine?

Cimetidine has the molecular formula C10H16N6S and a molecular weight of 252.34 g/mol.

Sources

• DrugCentral drug card 645 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201051 — compound record and bioactivity
• PubChem CID 2756 — chemical identifiers
• DrugBank DB00501 — drug record
• FDA UNII 80061L1WGD — substance identity
• DailyMed: FDA labels for Cimetidine — current prescribing information (label search)
• UniProt P25021 (HRH2) — target protein
• UniProt Q96FL8 (SLC47A1) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt Q86VL8 (SLC47A2) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.