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MedChem II - stack 2

Parkinson's Disease drugs

MPTP Meperidine derivative used to produce Parkinsonism in lab animals
Benztropine mesylate (Cogentin) Trihexyphenidyl HCl (Artane) Diphenhydramine (Benadryl) Anticholinergic agents used in treatment of Parkinson's
Levodopa Dopamine precursor, converted by dopa decarboxylase in CNS
Carbidopa Frequently co-administered with Levodopa (Sinemet, Sinemet CR), inhibits peripheral dopa decarboxylase
Bromocriptine mesylate (Parlodel) Full D2, and partial D1 agonist, ergot alkaloid
Apomorphine (Apokyn) Dopaminergic agonist, may be neuroprotetive, can rapidly rescue Parkinson's patients from "frozen" state
Cabergoline (Dostinex) Long-acting dopamine receptor agonist, ergot alkaloid, high affinity for D2 receptors, used clinically to decrease elevated prolactin levels (which may lead to menstrual changes, unwanted lactation in women, impotence in men)
Pramipexole dihydrochloride (Mirapex) Dopaminergic agonist, more active at D3, versus D2 receptors, not an ergot alkaloid, may cause hallucinations
Ropinirole hydrochloride (Requip) Dopaminergic agonist, more active at D3, versus D2 receptors, not an ergot alkaloid, metabolized by CYP1A2, also used to treat restless leg syndrome
Rotigotine (Neupro) First transdermal synthetic dopaminergic agonist for Parkinsonism, more affinity for D1 receptors, but affects D2 as well
Amantadine HCl (Symmetrel) Initially used as an antiviral, increases dopamine release in the brain
Selegiline HCl (Eldepryl), also known as deprenyl Inhibits reuptake of dopamine in the CNS, selective irreversible inhibitor of MAO-B and MAO-A at higher doses, metabolites (amphetamines) may cause anxiety and insomnia
Rasagiline (Azilect) Selective irreversible MAO-B inhibitor, neuroprotective and antiapoptotic activity (may slow the rate of neuronal deterioration), no amphetamine metabolites to cause side effects
Tolcapone (Tasmar) Selective peripheral COMT inhibitor, prevents "wearing off" phenomenon of levodopa therapy, and interference of carbidopa metabolite with levodopa uptake into CNS, rarely used because it can cause serious liver disease
Entacapone (Comtan) Selective peripheral COMT inhibitor, similar to tolcapone, may be affected by drugs that interfere with biliary excretion, glucuronidation, and/or intestinal beta-glucuronidase
Created by: 100000197460889