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tacrine

Noncovalent cholinesterase inhibitor · Cognition Enhancer (for Alzheimer's disease)

Noncovalent cholinesterase inhibitorCognition Enhancer (for Alzheimer's disease)
CDSCO approved
EXCRETION
—
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
—
not curated
Top interactionssee all 12 →
  • BupropionSevereDatabaseDDInter
  • IohexolSevereDatabaseDDInter
  • IopamidolSevereDatabaseDDInter
  • LeflunomideSevereDatabaseDDInter

Mechanism

Tacrine reversibly inhibits acetylcholinesterase (AChE) by binding with higher affinity to the active center gorge, sterically blocking acetylcholine from entering for catalysis. It has a prolonged duration of action.

Indications

alzheimer’s disease (now in disuse)

Pharmacokinetics

Bioavailability
Well absorbed after oral administration
Protein binding
Partitioning into lipid
Metabolism
Hepatic (implied by hepatotoxicity)

Side effects

Serious
  • hepatotoxicity

Drug interactions

Bupropion
Severe
Database

Drug interaction classified as: synergy

Source: DDInter

Iohexol
Severe
Database

Clinical effect not specified

Source: DDInter

Iopamidol
Severe
Database

Clinical effect not specified

Source: DDInter

Leflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

Lomitapide
Severe
Database

Clinical effect not specified

Source: DDInter

Mipomersen
Severe
Database

Clinical effect not specified

Source: DDInter

Ozanimod
Severe
Database

Clinical effect not specified

Source: DDInter

Pexidartinib
Severe
Database

Clinical effect not specified

Source: DDInter

Siponimod
Severe
Database

Clinical effect not specified

Source: DDInter

Teriflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

Tizanidine
Severe
Database

Clinical effect not specified

Source: DDInter

Tramadol
Severe
Database

Clinical effect not specified

Source: DDInter

Related guidelines

Other Noncovalent cholinesterase inhibitor drugs

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Textbook-sourced·Sources: KD Tripathi 7e, Goodman & Gilman 14e·Updated: 2026-05-10