Drugs Flashcards
Tacrine
Cholinesterase Inhibitor
Used for AD
Not used much because of side effects
Donepezil
Cholinesterase inhibitor
Used for AD
Rivastigmine
Cholinesterase inhibitor
Used for AD
Glantamine
Cholinesterase Inhibitor
Used for AD
Cholinesterase inhibitors for AD
Side Effects
GI
Mucle Cramping
Abnormal Dreams
Memantine
NMDA channel blocker
Used to slow AD
Side Effects: headache and dizziness
L-DOPA
Restores DA in basal ganglia
Mech: uses AA transporter to enter brain
Decarbozylated to DA in DA cells (L-AAAD)
L-DOPA kinetics
2% get in brain (metabolized by peripheral L-AAAD or COMT
Short half-life (1-3 hrs
Absorption dependent on GI content
Carbidopa
inhibitor of peripheral L-AAAD
Increases CNS concentration of L-DOPA
Entacapone
COMT inhibitor
L-DOPA Use
Very effective for PD against all symptoms
benifits outlast half-life
best results for first few years, so not used until symptoms are present
L-DOPA Side Effects
Dyskinesia
Dementia, Confusino (treat with antipsychotic [clozapine]
GI
CV (postural hypotension, arrhythmias, HTN
L-DOPA interactions
Pyridoxine
MAO inhibitors
Halothane
Antipsychotics that are DA antagonist
L-DOPA contraindication
Glaucoma
psychosis
Cardiac disease that ivolves arrhytmias
Malignant melanoma
DA receptor agonist
Miic DA without need for intact nerve teminals
Mech: Agonsit of DA receptors in striatum
Advantages: No enzymatic conversion
selectivity for receptor subtypes
longer half life
less DA dependent oxidative stress
Pramipexol
D2 agonist
most commonly used currently for PD
Ropinerole
D2 agonist
most commonly used currently for PD
Apomorphine
High D4 affinity, moderate affinity for D2, D3, and D5
subq injections for immediate thrapy of an off episode
Pramipexol/Ropinerole Kinectics
can be titrated to therapeutic doses over a week or less
DA agonists Side effects
nausea
fatique
sudden attacks of daytime sleep
CNS toxicity (confusion [dont use in elderly pts], dyskinesia)
Apomorphine can cause increased QT prolongation and injection site RXNs
Selegiline/Rasagiline
MAO-B inhibitors
prolong the action of DA amd may reduce oxidative stress on neurons
Mech- selective, irreersible inhibiton of MAO-B
Seleginlin/Rasaglinie Use
Prescribed as soon as the diesae is diagnosed
used together with L-DOPA in advanced diseases
anti depreseant
modest effects on progression
Sele/Rasa Side Effects
Well tolerated in early disease
late- worsens side effects of L-DOPA
metabolized to amphetamines (nxiety and insomina)
Sele/Rasa interactions
when given with meperidine, tricyclic antidepressants and SSRI causes serotionin syndrome