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24 Cards in this Set

  • Front
  • Back
Selegiline (type, mech, SE)
Type - MAO-B Inhibitor
Mech - Selective, irreversible inhibitor. Works in CNS Inhibits oxidation of MPTP. May be neuroprotective against radicals.
SE - Nausea, insomnia, hallucinations, Amphetamine metabolites.
Rasagiline (type, mech, SE)
Type - MAO-B inhibitor.
Mech - Irreversible inhibitor.
SE - Similar to Selegiline but no amphetamine metabolites. Can trigger serotonin syndrome. Metabolized by p450
Entacapone (type, mech, SE)
Type - COMT inhibitor
Mech - Inhibits COMT in periphery (No BBB). Used as an add on with L-dopa.
SE - Alters liver function, increased DA stim, prolonged dyskinesia, psychiatric syndromes.
Tolcapone (type, mech, SE)
Type - COMT inhibitor.
Mech - Peripheral and central COMT inhibitor. More potent than entacapone.
SE - Alters liver function, increased DA stim, prolonged dyskinesia, psychiatric syndromes.
Pramipexole (type, mech, SE)
Type - Dopamine agonist
Mech - D3 selective. Acts on presynaptic autoreceptors. Used off label for cluster headaches, restless leg syndrome, and bipolar depression.
SE - Dyskinesia, dizziness, psychiatric probs, sudden onset of sleep, and "Las Vegas Pill"
Ropinirole (type, mech, SE)
Type - Dopamine agonist
Mech - D3>D2. Also approved for restless leg syndrome.
SE - Dyskinesia, side effects similar to L-dopa, p450
Trihexyphenidyl (type, mech, SE)
Type - Centrally acting antimuscarinic.
Mech - Centrally acting muscarinic antagonist. Better at treating tremor than bradykinesia
SE - standard anti muscarinic side effects
Benztropine (type, mech, SE)
type - centrally acting antimuscarinic, dopamine ruptake inhibitor
Mech - Muscarinic antagonist. Also blocks dopamine reuptake.
SE - standard anti muscarinic SEs as well as sedation.
Orphenadrine (type, mech, SE)
type - Centrally acting antihistamine
mech - antihistamine, antimuscarinic via NMDA antagonist. Most effective on tremor.
SE - anti muscarinic and sedative, Inhibits CYP2B6 and 2D6
Amantadine (type, mech, SE)
Type - Antiviral, enhances DA neurotransmission and is a mild antimuscarniic.
Mech - enhances DA release and inhibits NMDA recpetor mediated Ach release.
SE - Less effective than levodopa, decline in efficacy in months
What toxins can lead to the onset of parkinsons disease
-carbon monoxide
-manganese
-phenothiazines and other antipsychotics
4 major dopaminergic pathways in the brain
1) mesocortical pathway
2) mesolimbic pathway
3) nigrostriatal pathway
4) tuberinfundibular pathway
2 methods of Levodopa metabolism
1) Decarboxylation by L-aromatic amino acid decarboxylase
2) O-methylation by COMT
Absorbtion of Levodopa
Largely decarboxylated in GI tract but in presence of decarboxylase inhibitor, amount in plasma is similar to IV
Where are the highest accumulations of L-Dopa in brain located
Hypothalmus (Nori) and striatum (DA)
How does D1 receptor work in response to dopamine and what are the D1 receptors
D1 and D5
^cAMP
^PIP2 hydrolysis
calcium mobalization
PKC activation
How do D2 receptors work in response to dopamine and what are the D2 receptors
D2, D3, D4
Decrease cAMP
Increase K+ current
Decrease voltage gated Ca current
What are some drug incompatibilities/interactions with L-dopa
Pyridoxine - P- amino acid decarboxylase is a pyridpxine dependent enzyme. It will reduce amount of l-dopa getting to the brain
Reserpine - repletes central dopamine
Phenothiazines - Block dopamine receptors
What side effects of L-dopa can and cannot be tolerated.
Nausea vomiting hypotension can be tolerated
Dyskinesia and psychiatric problems cannot
Carbidopa
peripheral decarboxylase inhibitor. Coadministered with L-dopa to reduce amount of L-dopa that needs to be given.
When are anticholinergics counterindicated
Patients with:
-prostatic hyperplasia
-obstructive gi disease
-narrow angle glaucoma
-Use with other anticholinergics
What type of neurons degenerate in huntingtons disease
GABAergic neurons in the striatum
Tetrabenazine (type, mech, SE)
For huntingtons, depletes monoamines by blocking vesicular uptake
Treatment for tourettes
Dopamine antagonists - haloperidol, primozide.
Tricyclic antidepressants and A2 agonists like clonidine are also used.