PD Medications
Types
- DA precursors
- DA receptor agonists
- Anticholinergics
- MAO-B inhibitors
- COMT inhibitors
- Adenosine antagonists
- Amantadine
- Pimavanserin
- AChE inhibitors & NMDA antagonists
DA precursor
Levodopa
+benserazide, +carbidopa, +carbidopa/entacapone
- B/L: no in USA
- Sinemet IR
> avoid near protein meals
> start 1/2 tab TID for 1wk, and inc to 1 tb TID until next appointment
> iron can dec C/L intake
> if needs to inc C/L therapy, there are 2 ways: frequency vs dosing
- Rytary & Crexont
> pts feel that takes time to kick in effect
- Rytary color related to strength
- Conversion from IR C/L to Rytary ER
- Crexont color related to strength
- Conversion from IR C/L to Crexont ER
> 1st calculate total IR C/L in a day; later categorize according to most frequent IR C/L dose
- Dhivy
> scored into 4 parts; Sinemet is only 2 parts
> allows precise titration especially for sensitive patients
Rescues
- unpredictable OFF periods
Levodopa inhaled (Inbrija)
Levodopa Cyclops
Apomorphine
Apokyn Pen and Kynmobi Film
- Apokyn start 0.1 mL; max 0.6 mL per dose; min q2h; total 20 mg/d
Pumps:
PEG/J infusion: LECIGON; Duodopa
IV: DiZ-101
SC: Foslevodopa; ND 0612; DiZ-102
LECIGON (Crono)
C/L + entacapone 1:4:4 ratio
- carbidopa 5 mg + levodopa 20 mg + entacapone 20 mg per ml
- AM + continuous
AM dose = AM LD dose x 0.8/ 20
Continuous dose = ([TLD (except AM) x 0.8]/20)/(number of hr patient is typically awake [eg, 16 hr])
*Oral to intestinal dose conversion is 80% 2/2 higher bioavailability
Duopa (CADD Legacy 1400)
C/L intestinal gel pump
- carbidopa 4.63 + levodopa 20 mg/mL
- AM + continuous
AM dose = AM LD dose x 0.8/ 20
Continuous dose = ([TLD (except AM) x 0.8]/20)/(number of hr patient is typically awake [eg, 16 hr])
Vyalev (Produodopa)
foscarbidopa/foslevodopa
- (120mg/2,400mg)/10mL single-dose vial
- Hourly base continuous infusion rate (mL/hr) = ([TLD x 1.3] / 240) / (number of hr patient is typically awake [eg, 16 hr])
- Maximum recommended daily dose: 3,525 mg foslevodopa (equivalent to ~2,500 mg levodopa)
- optional loading dose: First morning dose of oral immediate release levodopa x 1.3 and divide by 240
- extra dose: If ≥2 extra doses are used during 24-hour/day treatment period, consider revising base continuous infusion rate; options 0.1 mL = ~17 mg levodopa; 0.15 mL = ~25.5 levodopa; 0.2 mL = ~34 levodopa; 0.25 mL = ~42.5 levodopa; 0.3 mL = ~51 levodopa
DA receptor agonists
Ergo: bromocriptine, cabergoline
Non-ergo: Pramipexole, ropinirole, rotigotine
Anticholinergic
- Trihexyphenidyl and benztropine
> reserved for bad PD, only tremor, in young individuals, before DBS procedure
MAO-B inhibitors
- can be monotherapy (except safinamide), usually takes 1 wk for effects (red C/L), theoretical neuroprotection
- drug interaction: avoid SSRIs, TCAs, and meperidine
- choose selegiline, if fatigue, due to stimulant effects
COMT inhibitors
- adjunctive to C/L- days for effect, except opicapone
Entacapone + C/L (Stalevo)
- name based on levodopa dose: Stalevo 50 means 50 mg of LVD, Stalevo 100 means 100 mg of LVD
Adenosine antagonist
Istradefylline (Nourianz)
> adjunctive to C/L
> selective adenosine A2A receptor antagonist
> use when unable to prescribe MAO-B & COMT inhibitors
Amantadine
- choose Gocovri, if side effects or cannot take BID Symmetrel
Pimavanserin (Nuplazid)
- hallucinations & delusions associated with PDP
Switching from off-label antipsychotics to pimavanserin
AChE Inhibitors & NMDA antagonists
- preferential for rivastigmine due to PDD
- if fatigue, memantine, although there is no statistical benefit
- Exelon patch locations