Dopaminergic Drugs Flashcards
MOA: Increase DA release in nigrostriatal pathway
Indication: Parkinson’s Disease
SE: arrhythmia, nausea, anxiety, hallucinations,
dyskinesia and motor fluctuations (long term use)
L-DOPA
AADC inhibitor
Carbidopa
MOA: inhibits AADC in peripheral tissue (cannot X BBB)
Indication: concurrent rx with L-DOPA to reduce peripheral DA production
SE: augments SE of L-DOPA in CNS
Carbidopa
Ergot alkaloid with D2 agonist properties
Bromocriptine
Indications: Parkinson’s Disease
MOA in Parkinson’s: post synaptic activation in basal ganglia,
may also be neuroprotective (antioxidant, free radical scavenger, reduction of DA turnover)
therefore, best used early in disease course
SE: cardiac valvular fibrosis (long term use)
impulse control disorders (relatively rare)
Bromocriptine
Indications: Parkinson’s Disease (lower doses), Depression (higher doses)
MOA: Selective inhibition of MAO-B (can block MAO-A at high doses),
no dietary restriction at low doses.
SE: hypotension (dizziness), dry mouth, hypertensive crisis or serotonin syndrome
at higher doses,
Contraindications: concomitant use of indirect acting sympathomimetics, or
drugs that increase serotonin neurotransmission.
Selegiline
Indication: Parkinson’s Disease (more advanced)
MOA: inhibits COMT
Physiological effect: prolongs and increases effect of L-DOPA, reduces “off” time,
can reduce required L-DOPA dose
SE: dyskinesia, hallucinations, nausea, hypotension
Contraindications: liver failure (requires liver enzyme testing)
Tolcapone
MOA: D2 antagonism
Indications: acute psychosis, long-term
depot for poorly compliant schizophrenic
patients
SE: extrapyramidal motor disturbances
Haloperidol
DA reuptake inhibitors
Methylphenidate
MOA: Increased DA release in frontal cortex Indication: ADHD SE: Tachycardia Contraindication: TCA, arrhythmia, hypertension
Methylphenidate
Indication: Chemotherapy-induced-
and post-op nausea and vomiting, gastric paresis
MOA: D2 antagonist, also has 5-HT4 agonist properties
SE: akathisia, focal dystonia
Contraindications: long-term rx (3 months
can cause tardive dyskinesia)
Metaclopramide