Dementia medication Flashcards
hMechanism of action of donepezil
Selective reversible acetylcholinesterase inhibitor
Mechanism of action of rivastigmine
Reversible non-competitive acetylcholinesterase inhibitor (pseudo-irreversible)
Butyrylcholinesterase inhibitor
Mechanism of action of galantamine
Competitive reversible acetylcholinesterase inhibitor
Binds allosterically to the nicotinic acetylcholine receptor
Mechanism of action of memantine
Non-competitive NMDA glutamate receptor antagonist
5HT3 receptor antagonist
Half life of donepezil
70 hours
Half life of oral rivastigmine
1 hour
Half life of patch rivastigmine
3.4 hours
Half life of galantamine
7-8 hours
Half life of prolonged release galantamine
8-10 hours
Half life of memantine
60-100 hours
Acetylcholinesterase inhibitor which is available in patch form
Rivastigmine
Acetylcholinesterase inhibitor which is available in prolonged release form
Galantamine
Most common side effects of acetylcholinesterase inhibitors
Diarrhoea Nausea Anorexia Headache Dizziness
CYP enzymes involved in the metabolism of donepezil and galantamine
CYP3A4
CYP2D6
Side effects of memantine
Somnolence or agitation HTN Dizziness Dyspnoea Constipation Elevated LFTs Headache
Acetylcholinesterase inhibitor which is no longer used in the UK due to reports of fatal hepatotoxicity
Tacrine
Cholinergic side effects of acetylcholinesterases
Increased risk of GI bleeding Bradycardia Worsened COPD Urinary retention Increased seizure risk
Acetylcholinesterase inhibitor which is selective and reversible
Donepezil
Acetylcholinesterase inhibitor which is non-competitive and reversible
Rivastigmine
Acetylcholinesterase inhibitor which is competitive and reversible
Galantamine
Target for future antidementia drugs
Betasecretase enzyme
Most common side effect of acetylcholinesterase inhibitors
Nausea
Anti dementia drug which has been shown to be neuroprotective
Memantine
Type of dementia where cholinesterase inhibitors should not be used
Frontotemporal dementia
Reason to avoid cholinesterase inhibitors in frontotemporal dementia
Can worsen behavioural symptoms
Anti amyloid monoclonal antibodies which have been tested for the treatment of Alzheimer’s dementia
Solanezumab
Bapineuzumab
Antidementia medication which undergoes no hepatic conversion, and is broken down by choinesterase itself
Rivastigmine