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Exam 1 PHCL 3100
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32
Pharmacology
Undergraduate 3
02/17/2013

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Cards

Term
Name all potential AD drugs
Definition
Aspirin, naproxen, lovastatin, antihypertensives, doneprezil, rivastigmine, memantine, and caffeine
Term
Name all potential Parkinson's Disease drugs
Definition
Levadopa + carbidopa=Sinemet, entacapone, benzatropine, bromcriptine, amantadine, selegiline, apomorphine
Term
Name the old drug used for PD that is now used for treating motion sickness
Definition
Scopolamine
Term
Name the 2 key physical signs of AD
Definition
Amyloid plaques, fibrillary tangles
Term
Anti-degeneration drugs for AD
Definition
NSAIDS (naproxen and aspirin), statins (e.g. lovastatin), antihypertensives,
Term
Naproxen, Aspirin
Definition
2-years NSAID tx taken long before reduced later AD risk by 55%
Term
Lovastatin
Definition
May reduce AD risk by reducing hypercholesterolemia
Term
Antihypertensive Drugs
Definition
High bp in middle age correlates with increased AD incidence later
Term
Which neurotransmitters would you choose to enhance attention, memory and/or alertness?
Definition
Glutamate, and Acetylcholine
Term
Reversible Cholinesterase Inhibitors for minor enhancement of neurotransmission and cognition in AD
Definition
Donepezil, Rivastigmine
Term
Donepezil
Definition
CNS selective
Acetyl-cholinesterase inhibitor
cholinergic side effects
NO direct hepatotoxicity
Hepatotoxic interactions (drug of choice for AD patients who are NOT on multi-drug regimens)
Term
Rivastigmine
Definition
-ALSO CNS acetyl-cholinesterase inhibitor
-short half-life, but more sustained action than Donepezil
-also cholinergic side effects
-also no direct hepatotoxicity
-NO HEPATOTOXIC drug interactions
DRUG OF CHOICE FOR PTS on multi-drug regimens
Term
Reversible NDMAr antagonists for AD patients
Definition
Memantine
Term
Memantine
Definition
-reversible NMDAr antagonist
-moderate affinity for the NMDA glutamate receptor allows it to be knocked off by big pulses of glutamate during learning
-therefore, it blocks low-level chronic glutamate toxicity but still allows learning
-Additive benefit (longer delay of cognitive decline) when used with reversible cholinesterase inhibitors
Term
Potential AD drugs
Definition
Caffeine (Brain adenosine-sleep receptor blocker, cAMP and Ca2+ enhancing stimulant)----may delay onset of AD with longterm use...Possibly an AD vaccine
Term
Sx of PD
Definition
Bradykinesia, tremor, rigidity/akinesia
Term
Causes of PD
Definition
Rarely genetic, may be triggered by antipsychotics, toxins like MPTP, CO, CN; encephalitis; Concussions (repetitive)
Term
Neurological Basis of PD
Definition
Loss of DA Input on D2 Receptors. Also when ACh is released form the Caudate onto D2 receptors, it inhibits movement
Term
L-Dopa+carbidopa=Sinemet
Definition
Levodopa is a precursor to DA but only 5% gets into blood-brain barrier to be converted into DA. Resulting metabolite causes nausea and vomiting. Peripheral DA and NE toxicity!
NEED Carbidopa which inhibits peripheral decarboxylation of L-Dopa to DA, allowing more L-Dopa to get into brain.
Term
DA Replacement Therapy
Definition
Sinemet, Entacapone
Term
Entacapone
Definition
Peripheral COMT inhibitor, blocks synthesis of inactive L-Dopa metabolite that competes with L-Dopa at blood-brain barrier. Decreases L-Dopa elimination and increases half-life and bioavailability. EXTENDS SINEMET DURATION OF ACTION AND DECREASES ITS "ON/OFF" AND "WEARING OFF" EFFECTS.
Term
Levodopa/Sinemet
Definition
Bradykinesia/akinesia reduced
-tremor reduced less consistently
-Life expectancy increased but no cure!
-BENEFIT PER DOSE SHORTENS AS DISEASE PROGRESSES: MOTOR FLUCTUATIONS
Term
Side effects of Levodopa or Sinemet
Definition
-Orthostatic hypotension, nausea/vomiting
-Dyskinesia, psychiatric effects (including psychosis)
Term
Anticholinergics
Definition
First PD Drug was Scopolamine
-Anticholinergics used in early stage PD
-Tremor often responds better than L-Dopa
-ACh stimulates motion suppression, so anti-cholinergics enhance motion
E.G. Benzatropine
Term
Side effects of Anticholinergics
Definition
Low therapeutic index, SLUD
IN ELDERLY: SLUD, Sedation, delerium, tachycardia
Term
Side effects of Anticholinergics
Definition
Low therapeutic index, SLUD
IN ELDERLY: SLUD, Sedation, delerium, tachycardia
Term
Side effects of Anticholinergics
Definition
Low therapeutic index, SLUD
IN ELDERLY: SLUD, Sedation, delerium, tachycardia
Term
DA Receptor Agonists
Definition
None of these are effective as L-Dopa
-use as monotherapy for early stage PD
-Use as adjunct therapy for late stage PD
-mimics DA, BUT LONGER HALF-LIFE THAN L-Dopa, and more prolonged action on DA receptors
-SIDE EFFECTS: Can cause dyskinesias and hallucinations
Term
Bromocriptine
Definition
D2 Receptor agonist
-monotherapy early PD, adjunct therapy late PD
-can treat PD-associated hyperprolactinemia (DA needs to act on D2 receptors in pituitary to block prolaction secretion)
-SIDE EFFECT: fibrosis, as well as dyskinesis and hallucinations typical of DA or other DA receptor agonists
Term
Amantidine
Definition
-antiviral drug (PD therapeutic effect first noted on elderly flu pts)
-Enhances DA release from SNc;
Blocks GLU(GLU & ACh may have similar roles in caudate)
-Early PD monotherapy, late PD adjunct therapy
Term
Selegiline
Definition
Inhibits metabolism of DA to DOPAC via MAO-B inhibition; USE: DA-like effects; Early PD monotherapy, later adjunct therapy
ONLY Mild benefit; expensive!
SIDE EFFECT: Interacts with tricyclic and SSRI antidepressants--> serotonin syndrome (inc BP)
Term
Apomorphine
Definition
"Off" State Emergency Rescue Drug
-Powerful D1/D2 agonist.
-Rescues PD pts rapidly from an "off" (immobile) state
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