Promethazine

Phenothiazine — DERMATOLOGICALS

Key facts

Promethazine is an ofp drug in the Phenothiazine class catalogued in DrugCentral. It was first approved by the FDA in 1951. DrugCentral lists 40 molecular targets, including HRH1, Hrh1 and CHRM4. Recorded indications include Allergic conjunctivitis, General anesthesia, Nausea and vomiting and Seasonal allergic rhinitis.

• Approval status: ofp (first approved 1951 by the FDA).
• Drug class: Phenothiazine.
• Molecular targets: HRH1, Hrh1, CHRM4 and CHRM5 (40 listed in DrugCentral).
• Indications: Allergic conjunctivitis, General anesthesia, Nausea and vomiting, Seasonal allergic rhinitis and Sedation and others.
• ATC code: D04AA10 (Antihistamines for topical use).
• Molecular formula: C17H20N2S; molecular weight 284.42 g/mol.

Indications & contraindications

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

Indications (7)

• Allergic conjunctivitis
• General anesthesia
• Nausea and vomiting
• Seasonal allergic rhinitis
• Sedation
• Urticaria
• Vasomotor rhinitis

Mechanism & targets

• Established pharmacologic class: Phenothiazine

Molecular targets (40)

Target	Gene	Action	Activity
Histamine H1 receptor	HRH1	antagonist	Ki 9.62
Histamine H1 receptor	Hrh1	unknown	Ki 9.00
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 8.97
Muscarinic acetylcholine receptor M5	CHRM5	unknown	Ki 8.48
Muscarinic acetylcholine receptor M1	CHRM1	unknown	Ki 8.48
Muscarinic acetylcholine receptor M3	CHRM3	unknown	Ki 8.38
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 8.19
Muscarinic acetylcholine receptor M2	CHRM2	unknown	Ki 7.92
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 7.68
Alpha-2B adrenergic receptor	ADRA2B	unknown	Ki 7.62
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 7.50
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 7.37
Alpha-1A adrenergic receptor	Adra1a	unknown	IC50 7.10
Cholinesterase	BCHE	unknown	Ki 7.10
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 6.92
Histamine H4 receptor	HRH4	unknown	Ki 6.82
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 6.77
D(3) dopamine receptor	DRD3	unknown	Ki 6.72
D(2) dopamine receptor	DRD2	unknown	Ki 6.61
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 6.59

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1951-03-29	FDA	—	DELCOR ASSET CORP

ATC classification

ATC code	Therapeutic hierarchy
D04AA10	DERMATOLOGICALS › ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. › ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC. › Antihistamines for topical use
R06AD02	RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Phenothiazine derivatives
R06AD52	RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Phenothiazine derivatives
V03AB05	VARIOUS › ALL OTHER THERAPEUTIC PRODUCTS › ALL OTHER THERAPEUTIC PRODUCTS › Antidotes

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
Intentional self-injury	9941.7
Intentional overdose	7765.6
Akathisia	723.0
Depressed level of consciousness	599.5
Tachycardia	534.4
Mydriasis	352.8
Somnolence	219.7
Synovitis	212.2
Hallucination	204.7
Hand deformity	202.9
Drug ineffective	194.4
Glossodynia	187.8

Chemical structure

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

• Molecular formula: C₁₇H₂₀N₂S
• Molecular weight: 284.42 g/mol
• CAS number: 60-87-7
• InChIKey: PWWVAXIEGOYWEE-UHFFFAOYSA-N
• PubChem CID: 4927

CC(CN1C2=CC=CC=C2SC2=C1C=CC=C2)N(C)C

Frequently asked questions

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

What is Promethazine used for?

DrugCentral lists the following indications for Promethazine: Allergic conjunctivitis, General anesthesia, Nausea and vomiting, Seasonal allergic rhinitis, Sedation, Urticaria and Vasomotor rhinitis.

How does Promethazine work?

Its molecular targets in DrugCentral include HRH1 (antagonist), Hrh1, CHRM4 and CHRM5.

When was Promethazine first approved?

Promethazine was first approved by the FDA in 1951.

What drug class does Promethazine belong to?

Promethazine is in the Phenothiazine class.

What is the chemical formula of Promethazine?

Promethazine has the molecular formula C17H20N2S and a molecular weight of 284.42 g/mol.

Sources

• DrugCentral drug card 2286 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200750 — compound record and bioactivity
• PubChem CID 4927 — chemical identifiers
• DrugBank DB01069 — drug record
• FDA UNII FF28EJQ494 — substance identity
• DailyMed: FDA labels for Promethazine — current prescribing information (label search)
• UniProt P35367 (HRH1) — target protein
• UniProt P08173 (CHRM4) — target protein
• UniProt P08912 (CHRM5) — target protein
• UniProt P11229 (CHRM1) — target protein
• UniProt P20309 (CHRM3) — target protein
• UniProt P28335 (HTR2C) — 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.