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Index
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PHARMACOLOGY 1
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Drugs Neurodegenerative CHAPTER 8
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Level 2
level: Level 2
Questions and Answers List
level questions: Level 2
Question
Answer
Metabolic PRECURSOR of DOPAMINE RESTORES DOPAMINERGIC NEUROTRANSMISSION in the neostriatum ENHANCES SYNTHESIS of DOPAMINE in the surviving neurons of the substantia nigra Relief provided is only SYMPTOMATIC Its effect can be enhanced by coadministering: CARBIDOPA Short Half life (1-2 HOURS)
Levodopa
Dopamine Decarboxylase Inhibitor Does not cross blood brain barrier COADMINISTERED with LEVODOPA to enhance its effects Increases BIOAVAILABILITY of levodopa Lowers the dose of levodopa to 4 to 5 fold
Carbidopa
Increases breakdown of Levodopa and diminishes its effectiveness
Vitamin B6 (PYRIDOXINE)
Also called as DEPRENYL Selectively inhibits MONOAMINE OXIDASE (MAO) TYPE B which metabolizes Dopamine. Administered with LEVODOPA INCREASES DOPAMINE levels in the BRAIN LITTLE POTENTIAL to cause HYPERTENSIVE CRISES High Dose: causes SEVERE HYPERTENSION Metabolized to Methamphetamine and Amphetamine
Selegiline
IRREVERSIBLE and Selective Inhibitor of brain MAO TYPE B 5x MORE POTENT that Selegiline Not metabolized to amphetamine-like substance
Rasagiline
CATHECHOL-O-METHYLTRANSFERASE (COMT) INHIBITORS (Selectively and Irreversibly) DECREASES plasma concentrations of 3-O-METHYLDOPA INCREASES uptake of LEVODOPA REDUCES the symptoms of "WEARING OFF" phenomena in Levodopa-Carbidopa Adverse Effects: Same with Levodopa
1 Entacapone - (Safer) 2 Tolcapone - (Longer duration of action) - (but causes HEPATIC NECROSIS)