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CNS Pharmocology

CNS Pharmocology UCLA

What physiologic effects of free radical molecules may result in damage or cell death? peroxidation of lipids (p. 953) oxidative damage to DNA (p. 956) oxidation of LDL cholesterol (p. 956) - forms atherosclerotic plaque blood vessel injury (p. 198)
Name three drugs or vitamins that may reduce damage produced by free radicals. Vitamin C Vitamin E Selegiline Gingko Biloba
Describe the possible sites of drug action on neurotransmission. Modulate neurotransmitter release Modulate neurotransmitter clearance from the synaptic cleft Modulate effects of the neurotransmitter at the post-synaptic receptor
Name two neurochemical strategies for drug therapy in Parkinson’s disease. Increase DA activity Decrease Ach activity
Which class of drug may be most useful in mild or early PD? MAO-B inhibitors
MAO-B Inhibitors selegiline and rasagiline
anticholinergic drugs trihexyphenidyl bentztropine biperiden diphenhydramine
Dopamine agonists ergot derivatives: bromocriptine, pergolide non-ergot derivatives: pramipesole, ropinirole, apomorphine
bromocriptine, pergolide ergot derivatives, DA agonist for PD
pramipesole, ropinirole, apomorphine Non-ergot derivatives, DA agonist for PD
carbidopa and entacapone used together as a Levodopa (l-dopa) to decrease metabolism
Name another clinical use for the antimuscarinics trihexyphenidyl and benztropine reduce tremor and possibly rigidity in PD
trihexyphenidyl and benztropine antimuscarinic for PD
Describe the mechanism of action for levodopa and carbidopa. inhibits decarboxylation of levodopa in the intestine & peripheral tissues, thereby making more levodopa available to the CNS cannot pass BBB, therefore, does not prevent the conversion of levodopa to dopamine by decarboxylases in the brain
L-dopa ups DA enters brain via active transport system once in brain, drug undergoes uptake into the few dopaminergic nerve terminals that remain in the striatum then l-dopa converts to dopamine
Describe early and late adverse effects of levodopa. Early:N/V, postural hypotension Late: Dyskinesias in 1st yr. Loss of effectiveness, dysrhthmias, psychosis
What are some strategies for dealing with loss of effectiveness in L-Dopa problems after 3-5 years of therapy? ncrease total dosing or dose frequency Use sustained release formulations supplement with other PD medications Take a drug holiday
Created by: UCLAnurse