Oxybutynin

Cholinergic Muscarinic Antagonist — GENITO URINARY SYSTEM AND SEX HORMONES

Key facts

Oxybutynin is an ofp drug in the Cholinergic Muscarinic Antagonist class catalogued in DrugCentral. It was first approved by the FDA in 1975. Its mechanism of action is classified as Cholinergic Muscarinic Antagonists. DrugCentral lists 15 molecular targets, including CHRM3, Chrm3 and CHRM1. Recorded indications include Bladder muscle dysfunction - overactive, Hyperhidrosis of palms, Increased Urinary Frequency and Neurogenic bladder.

• Approval status: ofp (first approved 1975 by the FDA).
• Drug class: Cholinergic Muscarinic Antagonist.
• Mechanism of action: Cholinergic Muscarinic Antagonists.
• Molecular targets: CHRM3, Chrm3, CHRM1 and CHRM4 (15 listed in DrugCentral).
• Indications: Bladder muscle dysfunction - overactive, Hyperhidrosis of palms, Increased Urinary Frequency, Neurogenic bladder and Urge incontinence of urine and others.
• ATC code: G04BD04 (Drugs for urinary frequency and incontinence).
• Molecular formula: C22H31NO3; molecular weight 357.49 g/mol.

Indications & contraindications

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

Indications (6)

• Bladder muscle dysfunction - overactive
• Hyperhidrosis of palms
• Increased Urinary Frequency
• Neurogenic bladder
• Urge incontinence of urine
• Urgent desire to urinate

Contraindications (24)

• Angle-closure glaucoma
• Atony of colon
• Benign prostatic hyperplasia
• Bladder outflow obstruction
• Chronic heart failure
• Conduction disorder of the heart
• Disease of liver
• Disorder of coronary artery
• Drowsy
• Gastric retention
• Gastroesophageal reflux disease
• Gastrointestinal hypomotility
• Gastrointestinal obstruction
• Hiatal hernia
• Hypertensive disorder
• Hyperthyroidism
• Kidney disease
• Myasthenia gravis
• Paralytic ileus
• Retention of urine
• Severe chronic ulcerative colitis
• Sinus tachycardia
• Toxic megacolon
• Ulcerative colitis

Mechanism & targets

• Mechanism of action (MoA): Cholinergic Muscarinic Antagonists
• Established pharmacologic class: Cholinergic Muscarinic Antagonist

Molecular targets (15)

Target	Gene	Action	Activity
Muscarinic acetylcholine receptor M3	CHRM3	antagonist	Ki 9.11
Muscarinic acetylcholine receptor M3	Chrm3	unknown	Ki 9.02
Muscarinic acetylcholine receptor M1	CHRM1	antagonist	Ki 9.00
Muscarinic acetylcholine receptor M4	CHRM4	unknown	Ki 8.44
Muscarinic acetylcholine receptor M1	Chrm1	unknown	Ki 8.23
Muscarinic acetylcholine receptor M2	Chrm2	unknown	Ki 8.16
Muscarinic acetylcholine receptor M2	CHRM2	antagonist	Ki 8.09
Sigma non-opioid intracellular receptor 1	SIGMAR1	unknown	Ki 7.99
Muscarinic acetylcholine receptor M5	CHRM5	unknown	Ki 7.85
Sodium-dependent dopamine transporter	SLC6A3	unknown	Ki 7.17
D(3) dopamine receptor	DRD3	unknown	Ki 6.84
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 6.30
Cytochrome P450 2C19	CYP2C19	unknown	IC50 6.22
Membrane-associated progesterone receptor component 1	Pgrmc1	unknown	Ki 6.09
Sodium-dependent noradrenaline transporter	SLC6A2	unknown	Ki 5.59

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2023-03-27	PMDA	—	Hisamitsu Pharmaceutical Co., Inc.
1975-07-16	FDA	—	—

ATC classification

ATC code	Therapeutic hierarchy
G04BD04	GENITO URINARY SYSTEM AND SEX HORMONES › UROLOGICALS › UROLOGICALS › Drugs for urinary frequency and incontinence

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
Urinary tract infection	535.1
Fall	383.1
Multiple sclerosis relapse	373.2
Anticholinergic syndrome	276.7
Vaginal flatulence	233.7
Female genital tract fistula	215.4
Multiple sclerosis	208.4
Proctitis	201.4
Radiculopathy	198.1
Vaginal discharge	195.2
Urinary incontinence	171.9
Systemic lupus erythematosus	171.5

Chemical structure

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

• Molecular formula: C₂₂H₃₁NO₃
• Molecular weight: 357.49 g/mol
• CAS number: 5633-20-5
• InChIKey: XIQVNETUBQGFHX-UHFFFAOYSA-N
• PubChem CID: 4634

CCN(CC)CC#CCOC(=O)C(O)(C1CCCCC1)C1=CC=CC=C1

Frequently asked questions

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

What is Oxybutynin used for?

DrugCentral lists the following indications for Oxybutynin: Bladder muscle dysfunction - overactive, Hyperhidrosis of palms, Increased Urinary Frequency, Neurogenic bladder, Urge incontinence of urine and Urgent desire to urinate.

How does Oxybutynin work?

Oxybutynin is classified as Cholinergic Muscarinic Antagonists; its molecular targets in DrugCentral include CHRM3 (antagonist), Chrm3, CHRM1 (antagonist) and CHRM4.

When was Oxybutynin first approved?

Oxybutynin was first approved by the FDA in 1975.

What drug class does Oxybutynin belong to?

Oxybutynin is in the Cholinergic Muscarinic Antagonist class.

What is the chemical formula of Oxybutynin?

Oxybutynin has the molecular formula C22H31NO3 and a molecular weight of 357.49 g/mol.

Sources

• DrugCentral drug card 2028 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1133 — compound record and bioactivity
• PubChem CID 4634 — chemical identifiers
• DrugBank DB01062 — drug record
• FDA UNII K9P6MC7092 — substance identity
• DailyMed: FDA labels for Oxybutynin — current prescribing information (label search)
• UniProt P20309 (CHRM3) — target protein
• UniProt P11229 (CHRM1) — target protein
• UniProt P08173 (CHRM4) — target protein
• UniProt P08172 (CHRM2) — target protein
• UniProt Q99720 (SIGMAR1) — target protein
• UniProt P08912 (CHRM5) — 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.