Module 4.4.1 (Pharmacology of Drugs for Alzheimers)

Question 1

What is alzheimers disease?

Answer 1

Alzheimer’s disease (AD) is a progressive dementia

• It results from the destruction of cholinergic and other neurons

Question 2

what are the FOUR drugs used in alzheimers disease?

Answer 2

• Donepezil
• Galantamine
• Rivastigmine
• Memantine

Question 3

What are THREE anticholinesterases used in alzheimers? What is the MOA

Answer 3

1. Donepezil
2. Galantamine
3. Rivastigmine

Mechanism of action

• ↓ Breakdown of ACh reducing the apparent deficiency of cholinergic neurotransmitter activity

Question 4

AE (CI) of Donepezil „ Galantamine „ Rivastigmine?

Answer 4

Common

• GI effects - N, V, D, anorexia, abdominal pain, dyspepsia
• Insomnia „
• Vivid dreams „
• Urinary incontinence „
• ↑ sweating „
• Rivastigmine – skin reaction to patch at application site

Infrequent

• Bradycardia „
• Heart block „
• Seizures „
• GI haemorrhage

Question 5

What are precuations and contraindications for anticholinesterases?

Answer 5

GI or uretic obstruction

Active peptic ulcer disease

Drugs with anticholinergic effects antagonize therapeutic effect

Question 6

What are some drug interactions for anticholinesterases?

Answer 6

Anticholinesterases can cause bradycardia – interact with other drugs that cause bradycardia e.g. diltiazem

Question 7

What is the MOA of memantine?

Answer 7

AD is thought to be associated with excess glutamate

• Memantine acts as a N-methyl-D-aspartate (NMDA) antagonist which may reduce glutamate-induced neuronal degradation.

Question 8

AE (CIR) of memantine?

Answer 8

Common

• Headache, insomnia, drowsiness, confusion, dizziness, agitation, hallucinations

Infrequent

• Vomiting, anxiety

Rare’

• Seizures, bradycardia, renal failure, HF

Question 9

What is a contraindication for memantine?

Answer 9

Hx of seizures