Cyclizine

RESPIRATORY SYSTEM

Key facts

Cyclizine is an ofm drug catalogued in DrugCentral. DrugCentral lists 16 molecular targets, including HRH1, HTR2A and CHRM4. Recorded indications include Allergic conjunctivitis, Allergic rhinitis, Common cold and Cough.

• Approval status: ofm.
• Molecular targets: HRH1, HTR2A, CHRM4 and CHRM3 (16 listed in DrugCentral).
• Indications: Allergic conjunctivitis, Allergic rhinitis, Common cold, Cough and Motion sickness and others.
• ATC code: R06AE03 (Piperazine derivatives).
• Molecular formula: C18H22N2; molecular weight 266.39 g/mol.

Indications & contraindications

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

Indications (10)

• Allergic conjunctivitis
• Allergic rhinitis
• Common cold
• Cough
• Motion sickness
• Nasal congestion
• Nasal discharge
• Seasonal allergic rhinitis
• Sneezing
• Vasomotor rhinitis

Contraindications (55)

• Acidosis
• Acute abdominal pain
• Acute exacerbation of asthma
• Acute hepatitis
• Acute pancreatitis
• Adrenal cortical hypofunction
• Angle-closure glaucoma
• Arterial thrombosis
• Arteriosclerotic vascular disease
• Atrophoderma
• Benign intracranial hypertension
• Benign prostatic hyperplasia
• Bladder outflow obstruction
• Bradycardia
• Central nervous system depression
• Chronic disease of respiratory system
• Chronic heart failure
• Chronic idiopathic constipation
• Conduction disorder of the heart
• Coronary arteriosclerosis
• Decreased respiratory function
• Dependent drug abuse
• Diabetes mellitus
• Disease of liver
• Disorder of coronary artery
• Disorder of gallbladder
• Drug AND/OR toxin-induced diarrhea
• Dysfunction of sphincter of Oddi
• Epilepsy
• Hypertensive disorder
• + 25 more

Mechanism & targets

Molecular targets (16)

Target	Gene	Action	Activity
Histamine H1 receptor	HRH1	antagonist	Ki 8.35
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 7.19
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 6.92
Muscarinic acetylcholine receptor M3	CHRM3	unknown	Ki 6.80
Muscarinic acetylcholine receptor M1	CHRM1	unknown	Ki 6.79
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 6.62
Muscarinic acetylcholine receptor M2	CHRM2	unknown	Ki 6.38
Muscarinic acetylcholine receptor M5	CHRM5	unknown	Ki 6.34
5-hydroxytryptamine receptor 2C	HTR2C	unknown	Ki 6.27
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 6.24
Alpha-1D adrenergic receptor	ADRA1D	unknown	Ki 6.22
Sodium-dependent dopamine transporter	SLC6A3	unknown	Ki 6.22
D(3) dopamine receptor	DRD3	unknown	Ki 5.99
Alpha-1B adrenergic receptor	Adra1b	unknown	Ki 5.86
Cytochrome P450 2D6	CYP2D6	unknown	IC50 5.21
Amine oxidase [flavin-containing] B	MAOB	unknown	—

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
—	FDA	—	GLAXOSMITHKLINE

ATC classification

ATC code	Therapeutic hierarchy
R06AE03	RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Piperazine derivatives
R06AE53	RESPIRATORY SYSTEM › ANTIHISTAMINES FOR SYSTEMIC USE › ANTIHISTAMINES FOR SYSTEMIC USE › Piperazine derivatives

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
Neutropenic sepsis	334.9
Vomiting	216.5
Desmoplastic small round cell tumour	194.5
Mucosal inflammation	163.0
Skin candida	134.9
Diarrhoea	125.1
Pituitary tumour benign	114.7
Constipation	105.2
Neuropathy peripheral	96.9
Ejection fraction decreased	92.2
Foetal exposure during pregnancy	87.8
Febrile neutropenia	85.9

Chemical structure

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

• Molecular formula: C₁₈H₂₂N₂
• Molecular weight: 266.39 g/mol
• CAS number: 82-92-8
• InChIKey: UVKZSORBKUEBAZ-UHFFFAOYSA-N
• PubChem CID: 6726

CN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=CC=C1

Frequently asked questions

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

What is Cyclizine used for?

DrugCentral lists the following indications for Cyclizine: Allergic conjunctivitis, Allergic rhinitis, Common cold, Cough, Motion sickness, Nasal congestion, Nasal discharge and Seasonal allergic rhinitis and others.

How does Cyclizine work?

Its molecular targets in DrugCentral include HRH1 (antagonist), HTR2A, CHRM4 and CHRM3.

What is the chemical formula of Cyclizine?

Cyclizine has the molecular formula C18H22N2 and a molecular weight of 266.39 g/mol.

Sources

• DrugCentral drug card 749 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200497 — compound record and bioactivity
• PubChem CID 6726 — chemical identifiers
• DrugBank DB01176 — drug record
• FDA UNII QRW9FCR9P2 — substance identity
• DailyMed: FDA labels for Cyclizine — current prescribing information (label search)
• UniProt P35367 (HRH1) — target protein
• UniProt P28223 (HTR2A) — target protein
• UniProt P08173 (CHRM4) — target protein
• UniProt P20309 (CHRM3) — target protein
• UniProt P11229 (CHRM1) — target protein
• UniProt P41595 (HTR2B) — 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.