DRUGS USED FOR PARKINSONISM/DRUGS OF ABUSE Flashcards
(31 cards)
inhibits peripheral metabolism via dopa
decarboxylase
CARBIDOPA
What drugs are dopamine agonists that are ergot alkaloids (4)
Bromocriptine, Pergolide, Cabergoline, Piribedil
MOA of Bromocriptine, Pergolide, Cabergoline, Piribedil?
Partial agonist at dopamine D2 receptors in brain,
D2 agonism leads to inhibition of prolactin release
Piribedil also has alpha 2 antagonistic action. Additional use for???
intermittent claudication.
Non ergot dopamine agonists drugs (3)
Pramipexole, Ropinirole, Rotigotine
MOA of PRAMIPEXOLE and ROPIRINOLE?
Partial agonist at dopamine D2 (pramipexole) &
D3 receptors (ropinirole) in brain
MNEMONICS:
D2 = pramipexole
Imagine twins (2 babies) being carried in a pram by their mom Pam
Also remember that P comes before R and 2 comes before 3 (P =
pramipexole = D2; R = ropinirole = D3)
SE of Pramipexole, Ropinirole,
ICD or impulse control disorder: compulsive
gambling, hypersexuality, overeating
MOA of APOMORPHINE
Agonist at dopamine D2 receptors.
Antagonist at 5-HT and alpha adrenoceptors.
Rescue treatment for off-periods of Parkinson’s
disease (temporary relief), Alcoholism, Opiate addiction,
Erectile dysfunction, Alzheimer’s disease
APOMORPHINE
SE of APOMORPHINE
- QT prolongation
- Severely emetogenic
Treatment of Nausea caused by apomorphine?
TRIMETHOBENZAMIDE! Do not use Ondansetron
MAO- B inhibitors used for parkinsonism?
Selegiline, Rasagiline, Safinamide
SE of MAO-B Inhibitors?
Serotonin syndrome
COMT inhibitors used in Parkinsonism?
Tolcapone, Entacapone
SE of ENTACAPONE, TOLCAPONE?
- Orange urine
- Hepatotoxicity (Tolcapone)
- SEs Related to increased levels of L-DOPA
TOLCAPONE, ENTACAPONE MOA?
Block L-dopa metabolism by inhibiting catechol-Omethyltransferase
in periphery (both) and CNS
(tolcapone only)
MNEMONICS:
TWOlcapone – tolcapone inhibits both central and peripheral COMT
while entacapone only inhibits centrally
MOA: Amantadine?
Alter dopamine release in striatum, has anticholinergic
properties, blocks NMDA and glutamate receptors
SE of Amantadine?
Livedo reticularis
What drugs causes Livedo Reticularis?
A man reads FHM and GQ!
Amantadine Gemcitabine
Hydroxyurea Quinidine
Minocycline
Anticholinergic drugs used in parkinsonism?
Benztropine, Biperiden, Trihexyphenidyl, Procyclidine
MOA of anticholinergic drugs used in parkinsonism?
Block muscarinic receptors = dec. excitation in
cholinergic neurons in striatum
neurodegenerative disease caused by
degeneration of dopaminergic neurons in the substantia nigra
Paralysis Agitans aka Parkinsons Dse
Classic triad (4) of Parkinsons?
PARKINSON DISEASE: It’s a TRAP! Tremor, Rigidity, Akinesia, Postural
Instability!
Treatment Strategies for Parkinson’s Disease?
Restore dopaminergic activity in the basal ganglia via:
▪ (1) dopamine precursors (increase level of levodopa)
▪ (2) dopamine agonists
▪ (3) drugs that inhibit its metabolism