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24 Cards in this Set
- Front
- Back
Selegiline (type, mech, SE)
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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. |
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Rasagiline (type, mech, SE)
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Type - MAO-B inhibitor.
Mech - Irreversible inhibitor. SE - Similar to Selegiline but no amphetamine metabolites. Can trigger serotonin syndrome. Metabolized by p450 |
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Entacapone (type, mech, SE)
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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. |
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Tolcapone (type, mech, SE)
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Type - COMT inhibitor.
Mech - Peripheral and central COMT inhibitor. More potent than entacapone. SE - Alters liver function, increased DA stim, prolonged dyskinesia, psychiatric syndromes. |
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Pramipexole (type, mech, SE)
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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" |
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Ropinirole (type, mech, SE)
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Type - Dopamine agonist
Mech - D3>D2. Also approved for restless leg syndrome. SE - Dyskinesia, side effects similar to L-dopa, p450 |
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Trihexyphenidyl (type, mech, SE)
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Type - Centrally acting antimuscarinic.
Mech - Centrally acting muscarinic antagonist. Better at treating tremor than bradykinesia SE - standard anti muscarinic side effects |
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Benztropine (type, mech, SE)
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type - centrally acting antimuscarinic, dopamine ruptake inhibitor
Mech - Muscarinic antagonist. Also blocks dopamine reuptake. SE - standard anti muscarinic SEs as well as sedation. |
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Orphenadrine (type, mech, SE)
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type - Centrally acting antihistamine
mech - antihistamine, antimuscarinic via NMDA antagonist. Most effective on tremor. SE - anti muscarinic and sedative, Inhibits CYP2B6 and 2D6 |
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Amantadine (type, mech, SE)
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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 |
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What toxins can lead to the onset of parkinsons disease
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-carbon monoxide
-manganese -phenothiazines and other antipsychotics |
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4 major dopaminergic pathways in the brain
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1) mesocortical pathway
2) mesolimbic pathway 3) nigrostriatal pathway 4) tuberinfundibular pathway |
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2 methods of Levodopa metabolism
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1) Decarboxylation by L-aromatic amino acid decarboxylase
2) O-methylation by COMT |
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Absorbtion of Levodopa
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Largely decarboxylated in GI tract but in presence of decarboxylase inhibitor, amount in plasma is similar to IV
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Where are the highest accumulations of L-Dopa in brain located
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Hypothalmus (Nori) and striatum (DA)
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How does D1 receptor work in response to dopamine and what are the D1 receptors
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D1 and D5
^cAMP ^PIP2 hydrolysis calcium mobalization PKC activation |
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How do D2 receptors work in response to dopamine and what are the D2 receptors
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D2, D3, D4
Decrease cAMP Increase K+ current Decrease voltage gated Ca current |
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What are some drug incompatibilities/interactions with L-dopa
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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 |
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What side effects of L-dopa can and cannot be tolerated.
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Nausea vomiting hypotension can be tolerated
Dyskinesia and psychiatric problems cannot |
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Carbidopa
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peripheral decarboxylase inhibitor. Coadministered with L-dopa to reduce amount of L-dopa that needs to be given.
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When are anticholinergics counterindicated
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Patients with:
-prostatic hyperplasia -obstructive gi disease -narrow angle glaucoma -Use with other anticholinergics |
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What type of neurons degenerate in huntingtons disease
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GABAergic neurons in the striatum
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Tetrabenazine (type, mech, SE)
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For huntingtons, depletes monoamines by blocking vesicular uptake
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Treatment for tourettes
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Dopamine antagonists - haloperidol, primozide.
Tricyclic antidepressants and A2 agonists like clonidine are also used. |