Parkinson's Flashcards
What are the approaches to treating Parkinson’s
- Increase endogenous dopamine
- Decrease cholinergic activity
- Activate dopamine receptors with synthetic dopamine agonists
- Block adenosine A2A receptor activity
How do you increase endogenous dopamine?
- Use of L-dopa
- Inhibit metabolism of dopa decarboxylase
- Inhibit metabolism by COMT
- Inhibit central/peripheral metabolism by MAO-B
- Increase dopamine release and inhibits reuptake
Drugs that inhbit COMT
- Entacapone
- Tolcapone
- Opicapone
Drugs that inhbit MAOB
- Rasagiline
- Selegiline
- Safinamide
What PK drugs that induce endogenous dopamine can also be used as monotherapy?
MAOB inhibitors
Which PK drug can produce methamphetamines if a toxicology report is done?
Selegiline
What PK drug increases dopamine release and inhibits it reuptake?
Amantadine
Dosing for Rasagiline as adjunctive and as monotherapy
Adjunctive: 0.5 mg
Monotherapy: 1 mg
What should you be cautious with in Safanimide therapy?
Hepatic impairment (Child Pugh Class C)
Abrupt discontinuation - withdrawal emergent NMS-like syndrome
What is the effect of Amantadine?
It reduces rigidity, tremor, bradykinesia and L-Dopa induced dyskinesia
What should you monitor with Amantadine dosing?
Renal elimination; adjust dose with renal impairment
What’s a transient adverse effect of Amantadine
Livedo reticularis; mottling of the skin
What is a side effect of selegiline?
It can cause insomnia and jitteriness
What PK drug is potentially disease modifying?
Rasagiline
What is the PKPD and dosing strategy surrounding Opicapone?
With a mod fat/calorie meal, its Cmax, AUC and Tmax decrease
It is also to be dosed at bedtime at least 1 hour before and 1 hour after eating
What PK drug is available in combo with Carbidopa/Levodopa?
Entacapone (200 mg)
STALEVO
True or False. Carbidopa can be used a monotherapy to help treat Parkinson’s
False. Never you give it alone
True or False. COMT inhibitors can be used as monotherapy to help treat Parkinson”s
False. No effect in absence of L-Dopa