Chlorphenamine

Histamine-1 Receptor Antagonist — RESPIRATORY SYSTEM

Key facts

Chlorphenamine is an ofp drug in the Histamine-1 Receptor Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1950. Its mechanism of action is classified as Histamine H1 Receptor Antagonists. DrugCentral lists 15 molecular targets, including Hrh1, HRH1 and HRH1. Recorded indications include Allergic conjunctivitis, Allergic rhinitis, Common cold and Dermatographic urticaria.

• Approval status: ofp (first approved 1950 by the FDA).
• Drug class: Histamine-1 Receptor Antagonist.
• Mechanism of action: Histamine H1 Receptor Antagonists.
• Molecular targets: Hrh1, HRH1, HRH1 and SLC6A4 (15 listed in DrugCentral).
• Indications: Allergic conjunctivitis, Allergic rhinitis, Common cold, Dermatographic urticaria and Influenza-like symptoms and others.
• ATC code: R06AB04 (Substituted alkylamines).
• Molecular formula: C16H19ClN2; molecular weight 274.80 g/mol.

Indications & contraindications

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

Indications (12)

• Allergic conjunctivitis
• Allergic rhinitis
• Common cold
• Dermatographic urticaria
• Influenza-like symptoms
• Itching of skin
• Nasal congestion
• Nasal discharge
• Seasonal allergic rhinitis
• Sneezing
• Urticaria
• Vasomotor rhinitis

Contraindications (88)

• Achalasia of esophagus
• Acidosis
• Acute abdominal pain
• Acute erosive gastritis
• Acute exacerbation of asthma
• Acute hepatitis
• Acute nephropathy
• Acute pancreatitis
• Acute Thromboembolic Stroke
• Acute tuberculosis
• Agoraphobia
• Alcohol intoxication
• Alcohol withdrawal delirium
• Alcoholism
• Anemia
• Anemia due to enzyme deficiency
• Angle-closure glaucoma
• Arterial thrombosis
• Arteriosclerotic vascular disease
• Asthenia
• Atony of colon
• Autonomic dysreflexia
• Benign intracranial hypertension
• Benign prostatic hyperplasia
• Bladder outflow obstruction
• Bleeding
• Blood coagulation disorder
• Body fluid retention
• Bradycardia
• Brain damage
• + 58 more

Mechanism & targets

• Mechanism of action (MoA): Histamine H1 Receptor Antagonists
• Established pharmacologic class: Histamine-1 Receptor Antagonist

Molecular targets (15)

Target	Gene	Action	Activity
Histamine H1 receptor	Hrh1	unknown	Ki 8.70
Histamine H1 receptor	HRH1	antagonist	Ki 8.15
Histamine H1 receptor	HRH1	unknown	IC50 8.06
Sodium-dependent serotonin transporter	SLC6A4	unknown	Kd 7.82
Histamine H4 receptor	HRH4	unknown	Ki 6.67
Sodium-dependent dopamine transporter	SLC6A3	unknown	Kd 5.97
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 5.96
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Kd 5.84
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 5.17
Sodium channel alpha subunits; brain (Types I, II, III)	SCN1A|SCN2A|SCN3A	unknown	IC50 5.00
Cytochrome P450 2D6	CYP2D6	unknown	Ki 4.97
MBT domain-containing protein 1	MBTD1	unknown	IC50 4.47
Lethal(3)malignant brain tumor-like protein 1	L3MBTL1	unknown	IC50 4.39
Lethal(3)malignant brain tumor-like protein 3	L3MBTL3	unknown	IC50 4.38
Chloroquine resistance transporter	CRT	unknown	IC50 4.27

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1950-08-15	FDA	—	BAYER HEALTHCARE LLC

ATC classification

ATC code	Therapeutic hierarchy
R06AB04	RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Substituted alkylamines
R06AB54	RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Substituted alkylamines

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
Drug ineffective	354.8
Contraindicated product administered	180.9
Treatment failure	164.8
Chest discomfort	157.1
Dyspnoea	155.3
Cough	127.4
Drug intolerance	126.8
Neuropathy peripheral	126.0
Flushing	122.8
Delusion of grandeur	121.5
Pemphigus	115.5
Synovitis	111.6

Chemical structure

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

• Molecular formula: C₁₆H₁₉ClN₂
• Molecular weight: 274.80 g/mol
• CAS number: —
• InChIKey: SOYKEARSMXGVTM-UHFFFAOYSA-N
• PubChem CID: 2725

CN(C)CCC(C1=CC=C(Cl)C=C1)C1=CC=CC=N1

Frequently asked questions

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

What is Chlorphenamine used for?

DrugCentral lists the following indications for Chlorphenamine: Allergic conjunctivitis, Allergic rhinitis, Common cold, Dermatographic urticaria, Influenza-like symptoms, Itching of skin, Nasal congestion and Nasal discharge and others.

How does Chlorphenamine work?

Chlorphenamine is classified as Histamine H1 Receptor Antagonists; its molecular targets in DrugCentral include Hrh1, HRH1 (antagonist), HRH1 and SLC6A4.

When was Chlorphenamine first approved?

Chlorphenamine was first approved by the FDA in 1950.

What drug class does Chlorphenamine belong to?

Chlorphenamine is in the Histamine-1 Receptor Antagonist class.

What is the chemical formula of Chlorphenamine?

Chlorphenamine has the molecular formula C16H19ClN2 and a molecular weight of 274.80 g/mol.

Sources

• DrugCentral drug card 616 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201659 — compound record and bioactivity
• PubChem CID 2725 — chemical identifiers
• DrugBank DB01114 — drug record
• FDA UNII 3U6IO1965U — substance identity
• DailyMed: FDA labels for Chlorphenamine — current prescribing information (label search)
• UniProt P35367 (HRH1) — target protein
• UniProt P31645 (SLC6A4) — target protein
• UniProt Q9H3N8 (HRH4) — target protein
• UniProt Q01959 (SLC6A3) — target protein
• UniProt Q12809 (KCNH2) — target protein
• UniProt P23975 (SLC6A2) — 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.