Levodopa is immediate precursor to dopamine and is able to cross the BBB
anorexia, nausea, vomiting, tachycardia, ventricular extrasystoles, hypotension, discoloration of saliva and urine, visual/auditory hallucinations, dyskinesias, depression, psychosis, anxiety
contraindicated in closed angle glaucoma, hypersensitivity, concomitant MAOI use, caution in hx of melanoma
Dopamine precursor clinical info
Interactions with MAOI (hypertensive crisis), Antipsychotic drugs (can block dopamine receptors, clozapine better), vitamin B6 (increase peripheral break down, but not an issue if using combo form)
Absorption is affected by drugs that delay or promote gastric emptying
Most clinically effective therapy for PD symptoms, effective for all 3 cardinal symptoms (resting tremor, bradykinesia, rigidity)
Catechol-o-methyltransferase: Entacapone
inhibit conversion of levodopa to 3-O-methyldopa in periphery and CNS, allowing for higher concentration
Can be initial therapy or adjunct with levodopa, selegiline has higher incidence of HTN and is metabolized by amphetamine so can lead to insomnia, Rasagiline 5x as potent
Theorized to slow disease progression caused by reduced oxidative stress
Antiviral: Amantadine
An antiviral that increases release of dopamine, blocks cholinergic receptors, inhibits NMDA type of glutamate receptors
Can be initial monotherapy for mild-moderate disease or adjunct w/ levodopa in advances disease, may improve rigidity and bradykinesia, and may be useful to tx dyskinesias associated with long term dopaminergic treatment
fewer long term motor complications but less effective, may need to decrease levodopa if taking together, does NOT cause fibrosis or peripheral vasospasm as seen with ergot derivative
Rotigotin is transdermal patch to tx early PD, admin once daily
Initial or adjunct w/ levodopa, longer duration of action than levodopa (good for pts w/ fluctuations in response to levodopa treatment)
Cholinergic receptor antagonists: Benztropine
compete with acetylcholine at muscarinic receptors in the CNS