Rivastigmine

Cholinesterase Inhibitor — NERVOUS SYSTEM

Key facts

Rivastigmine is an ofp drug in the Cholinesterase Inhibitor class catalogued in DrugCentral. It was first approved by the EMA in 1998. Its mechanism of action is classified as Cholinesterase Inhibitors. DrugCentral lists 14 molecular targets, including BCHE, ACHE and BCHE. Recorded indications include Alzheimer's disease and Dementia associated with Parkinson's Disease.

• Approval status: ofp (first approved 1998 by the EMA).
• Drug class: Cholinesterase Inhibitor.
• Mechanism of action: Cholinesterase Inhibitors.
• Molecular targets: BCHE, ACHE, BCHE and Bche (14 listed in DrugCentral).
• Indications: Alzheimer's disease and Dementia associated with Parkinson's Disease.
• ATC code: N06DA03 (Anticholinesterases).
• Molecular formula: C14H22N2O2; molecular weight 250.34 g/mol.

Indications & contraindications

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

Indications (2)

• Alzheimer's disease
• Dementia associated with Parkinson's Disease

Off-label uses (2)

• Diffuse Lewy body disease
• Moderate to Severe Alzheimer's Type Dementia

Contraindications (17)

• Anorexia nervosa
• Asthma
• Atrioventricular block
• Chronic obstructive lung disease
• Conduction disorder of the heart
• Diarrhea
• Extrapyramidal disease
• Gastrointestinal hemorrhage
• Gastrointestinal ulcer
• Nausea
• Neuromuscular block, function
• Parkinsonism
• Seizure disorder
• Sick sinus syndrome
• Urinary tract obstruction
• Vomiting
• Weight loss

Mechanism & targets

• Mechanism of action (MoA): Cholinesterase Inhibitors
• Established pharmacologic class: Cholinesterase Inhibitor

Molecular targets (14)

Target	Gene	Action	Activity
Cholinesterase	BCHE	inhibitor	IC50 7.52
Acetylcholinesterase	ACHE	inhibitor	IC50 7.43
Butyrylcholinesterase	BCHE	unknown	IC50 6.80
Butyrylcholinesterase; Protein Bche	Bche	unknown	IC50 6.46
Acetylcholinesterase	ACHE	unknown	IC50 6.21
Cholinesterase	BCHE	unknown	IC50 6.08
Acetylcholinesterase	Ache	unknown	IC50 5.95
Cholinesterase	Bche	unknown	IC50 5.80
Acetylcholinesterase	Ache	unknown	IC50 5.74
Acetylcholinesterase	ache	unknown	IC50 5.38
Cholinesterase	BCHE	unknown	IC50 5.20
MAP/microtubule affinity-regulating kinase 4	MARK4	unknown	IC50 5.17
Acetylcholine receptor subunit epsilon	Chrne	unknown	IC50 5.05
Fatty-acid amide hydrolase 1	FAAH	unknown	IC50 4.85

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2000-04-21	FDA	—	NOVARTIS
1998-05-12	EMA	—	—

ATC classification

ATC code	Therapeutic hierarchy
N06DA03	NERVOUS SYSTEM › PSYCHOANALEPTICS › ANTI-DEMENTIA DRUGS › Anticholinesterases

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
Hallucination	1108.7
Product adhesion issue	869.1
Fall	722.3
Dementia	657.2
Application site erythema	654.8
On and off phenomenon	615.4
Aggression	543.5
Confusional state	490.0
Agitation	483.6
Death	473.9
Application site pruritus	464.6
Freezing phenomenon	441.6

Chemical structure

• Molecular formula: C₁₄H₂₂N₂O₂
• Molecular weight: 250.34 g/mol
• CAS number: 123441-03-2
• InChIKey: XSVMFMHYUFZWBK-NSHDSACASA-N
• PubChem CID: 77991

CCN(C)C(=O)OC1=CC=CC(=C1)[C@H](C)N(C)C

Frequently asked questions

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

What is Rivastigmine used for?

DrugCentral lists the following indications for Rivastigmine: Alzheimer's disease and Dementia associated with Parkinson's Disease.

How does Rivastigmine work?

Rivastigmine is classified as Cholinesterase Inhibitors; its molecular targets in DrugCentral include BCHE (inhibitor), ACHE (inhibitor), BCHE and Bche.

When was Rivastigmine first approved?

Rivastigmine was first approved by the EMA in 1998.

What drug class does Rivastigmine belong to?

Rivastigmine is in the Cholinesterase Inhibitor class.

What is the chemical formula of Rivastigmine?

Rivastigmine has the molecular formula C14H22N2O2 and a molecular weight of 250.34 g/mol.

Sources

• DrugCentral drug card 2392 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1201092 — compound record and bioactivity
• PubChem CID 77991 — chemical identifiers
• DrugBank DB00989 — drug record
• FDA UNII PKI06M3IW0 — substance identity
• DailyMed: FDA labels for Rivastigmine — current prescribing information (label search)
• UniProt P06276 (BCHE) — target protein
• UniProt P22303 (ACHE) — target protein
• UniProt Q96L34 (MARK4) — target protein
• UniProt O00519 (FAAH) — 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.