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9 Cards in this Set

  • Front
  • Back
Mechanism of Action for Donepezil
Donepezil is a specific, noncompetitive, reversible inhibitor of acetylcholinesterase. It exhibits a relatively high degree of selectivity for neuronal AChE, only weakly inhibiting butylcholinesterase or AChE in smooth, striated, or cardiac muscle. It’s tertiary structure facilitates crossing of the BBB.
Mechanism of Action for Rivastigmine
Rivastigmine is a tertiary amine sporting a carbamoyl ester linkage that serves as a substrate for AChE. It reacts to produce an alkylcarbamoyl moiety, reversibly sequestering the enzyme in a more stable form, precluding it from hydrolyzing ACh. It also inhibits butylcholinesterase.
Mechanism of Action for Galantamine
Galantamine is a reversible inhibitor of cholinesterase activity and it also has nicotinic receptor agonist properties.
Mechanism of Action for Tacrine
Inhibits AChE by reversibly binding to the active center. It does so with a higher affinity than does edrophonium and, having primary structure rather than a quaternary one, it is more lipophilic and more readily crosses the BBB.
Mechanisms of Action for Memantine
Memantine preferentially blocks excessive activity of extrasynaptic NMDA receptors largely responsible for neuronal damage contributing to neurodegenerative diseases, such as Alzheimer’s disease.
Mechanism of Action for Levodopa
Levodopa is the immediate metabolic precursor of dopamine and is capable of crossing the BBB via L-amino acid transporter. It is given to increase dopamine levels in the brain to compensate for the loss of the dopamine-generating cells of the substantia nigra associated with Parkinson’s disease.
Mechanism of Action for Carbidopa
Carbidopa is an inhibitor of dopa decarboxylase that is incapable of crossing the BBB. When co-administered with levodopa, it inhibits the decarboxylation of levodopa in the periphery, thus facilitating levadopa’s bioavailability in the CNS.
Contraindications for Levodopa
Levodopa should not be given to patients who are psychotic or patients who have glaucoma. Levodopa + carbidopa should not be given to patients who have cardiac disease. Patients with active peptic ulcers “must be managed with care.” And levodopa is a precursor of skin melanin and thus may activate malignant melanoma. Thus history of melanoma is a relative contraindication.
Mechanism of Action for Riluzole
Presynaptically, riluzole inhibits glutamate release. Postsynaptically, riluzole blocks NMDA- and kainate-type glutamate receptors and "inhibits voltage-dependent channels." Riluzole also significantly increases glutamte uptake.