neuro drugs

Question 1

sx of PD

Answer 1

primary motor: resting tremor, rigidity, bradykinesia, gait/posture disturbances
other motor: micrographia, masked facies, dec blinking, soft voice, dysphagia, freezing
nonmotor: anosmia, sensory disturbances, mood d/o, sleep d/o, cognitive impairment, autonomic d/o (orthostasis, GI/GU/GYN disturbances)

Question 2

cause of PD

Answer 2

destruction of DA-producing cells in substantia nigra pars compacta

Question 3

levodopa

Answer 3

prodrug converted to DA by AAAD/LAAD/dopa decarboxylase

Question 4

levodopa ADR

Answer 4

arrhythmia (B-receptor activity), hypotension, vomiting, dyskinesia, on-off effects, psychosis

Question 5

levodopa drug interactions

Answer 5

B6 (increases levodopa peripheral conversion to DA)

high protein meals - dec absorption and peak plasma concentration

Question 6

carbidopa MOA and use

Answer 6

given with levodopa

inhibits peripheral AAAD to maximize levodopa reaching CNS

Question 7

tolcapone MOA

Answer 7

COMT inhibitor, preventing DA metabolism in CNS and L-dopa metabolism in periphery

Question 8

entacapone MOA

Answer 8

COMT inhibitor, preventing L-dopa metabolism in periphery

Question 9

tolcapone and entacapone ADR

Answer 9

tolcapone: hepatotoxic
entacapone: not as toxic so preferred

Question 10

selegiline and rasagiline MOA and use

Answer 10

MAO-B inhibitors (CNS)
early tx for PD or adjunct with levodopa
also used in MPTP-induced PD

Question 11

MAO-B inhibitor ADR

Answer 11

increases ADRs of L-dopa, dyskinesia, psychosis, insomnia

*no interaction with tyramine like MAO-A inhibitors

Question 12

bromocriptine and pergolide MOA, use, ADR

Answer 12

ergot alkaloid D2 agonists
use: PD, hyperprolactinemia, acromegaly
ADR: alpha-R activity causes HTN, vasoconstriction, gangrene

Question 13

pramipexole and ropinirole

Answer 13

non-ergot D2 agonists for PD

Question 14

amantadine MOA and ADR

Answer 14

causes increased DA release

ADR: livedo reticularis (small clots occlude capillaries)

Question 15

benztropine

Answer 15

muscarinic blocker to decrease tremor and rigidity in PD

ADR: atropine-like sx (dry mouth, urinary retention, constipation)

Question 16

trihexyphenidyl

Answer 16

muscarinic blocker to decrease tremor and rigidity in PD

ADR: atropine-like sx (dry mouth, urinary retention, constipation)

Question 17

diphenhydramine

Answer 17

muscarinic blocker to decrease tremor and rigidity in PD

ADR: atropine-like sx (dry mouth, urinary retention, constipation)

Question 18

drugs useful in drug-induced PD

Answer 18

MPTP-induced: selegiline, rasagiline

med-induced: benztropine, trihexyphenidyl, diphenhydramine

Question 19

cause and sx of Alzheimer’s

Answer 19

• neuronal dysfunction and loss in medial and temporal lobe, nucleus basalis of Meynert (ACh) and cortical and hippocampal cells; some effect on 5HT, glutamate, and neuropeptide
• sx: early- anterograde episodic memory loss; late- increased dependence progressing to akinetic mute state
• COD: immobility -> pneumonia, PE

Question 20

donepezil

Answer 20

non-competitive inhibition of AChE

metabolism by CYP2D6, 3A4

Question 21

rivastigmine

Answer 21

non-competitive inhibition of AChE and BuChE

metabolism by esterases (not CYP!)

Question 22

galantamine

Answer 22

competitive* inhibition of AChE

metabolism by CYP2D6, 3A4

Question 23

tacrine

Answer 23

non-competitive inhibition of AChE and BuChE

metabolism by CYP1A2

Question 24

memantine

Answer 24

adjunct or alternative tx with AChE inhibitors, decreases clinical deterioration of AD patients
non-competitive antagonist of NMDA-R

Question 25

ADRs of AChE inhibitors

Answer 25

GI distress, muscle cramping, abnormal dreams | *caution with bradycardia and syncope

Question 26

Huntington's disease

Answer 26

autosomal dominantly inherited motor incoordination and cognitive decline/personality changes early sx: fine motor incoordination, impaired rapid eye movements

Question 27

tx for HD with depression or irritability

Answer 27

fluoxetine

Question 28

tx for HD with paranoia, delusions, or psychosis

Answer 28

low dose haloperidol

Question 29

tx for HD with rigidity +/- paranoia

Answer 29

clozapine, quetiapine, carbamazepine

Question 30

tx for HD with large amplitude chorea

Answer 30

tetrabenazine (VMAT2 inhibitor) | ADR: hypotension, suicidality

Question 31

tx for HD with seizures

Answer 31

clonazepam or valproic acid

Question 32

cause and sx of ALS

Answer 32

loss of ventral horn motor neurons (LMN) and afferent cortical neurons (UMN) sx: rapidly progressive weakness, muscle atrophy, fasciculations, spasticity, dysarthria, dysphagia, respiratory compromise * spares sensory, autonomic, and oculomotor function

Question 33

riluzole MOA

Answer 33

prolongs survival of ALS by months | inhibits glutamate release, blocks NMDA and Kainate glutamate-R, and blocks v-g Na channels

Question 34

riluzole ADR

Answer 34

hepatic injury

Question 35

tx of clasped-knife spasticity in ALS

Answer 35

baclofen (GABA-B agonist), tizanidine (a2 agonist), clonazepam