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Dopamine Receptor Agonists - Coggle Diagram
Dopamine Receptor Agonists
Drugs
Non-ergolines
(D2/D3 agonists)
Pramipexole
Ropinirole
Apomorphine
Rescue treatment for pts with "off" episodes (freezing)
SC injection
Piribedil
Ergot derivatives
Pergolide (D1 and D2 agonist)
Cabergoline
Bromocriptine (D2 agonist, D1 partial antagonist)
Lisuride
MOA
: Act directly at posynaptic dopamine receptors on corpus striatum cells and stimulates them. Work in the absence of dopamine.
Therapeutic uses
Adjunct to L-dopa therapy
Used initially in early Parkinson's disease
Side effects
similar to those of L-dopa
BUT
likely to cause hallucinations or sleepiness
less likely to cause involuntary movements
Ropinirole
HIgher affinity at D3
PK
: Rapidly absorbed. Oral BA ~55%. Extensively liver metabolised. <10% excreted unchanged in urine.
DD interaction
: Estrogen decreases clearance of ropinirole.
Adverse effects
CNS
: hallucinations, dizziness, somnolence, fatigue
CVS
: orthostatic hypotension, syncope
increased sweating
GI
: V/D/C, abdominal pain, dyspepsia, dry mouth, anorexia
Pramipexol
HIgher affinity at D3
PK
: Rapidly absorbed. Oral BA >90%.Extensively distributed (also in RBC) 90% excreted unchanged via kidney.
Adverse effects
CNS
: hallucinations, dizziness, somnolence, fatigue, insomnia, dyskinesia
CVS
: orthostatic hypotension, syncope
GI
: V/D/C, abdominal pain, dyspepsia, dry mouth, anorexia
Sudden onset of sleep without warning
Bromocriptine
PK
: Oral BA ~28%. Completely metabolised. Excreted via bile (for renal insuffiency).
Adverse effects
CNS
: hallucinations, dizziness, headache, insomnia
CVS
: hypotension
Addominal discomfort
Abnormal involuntary movements