Week 4 - Neuro Drugs

Question 1

nimodipine

Answer 1

Ca++ channel blocker, CNS, dilates small vessels preserving cerebral perfusion

Question 2

tissue plasminogen activator (TPA) - alteplase - activase

Answer 2

Tx for ischemic or embolism strokes, contraindicated in hemorrhagic strokes, dissolves blood clots, given within 3-4.5 hours of stroke onset, thrombolytic

Question 3

tissue plasminogen activator mechanism

Answer 3

IV, made with recombinant DNA technology, restores patency of thrombosed vessels, binds to fibrin in clot and causes plasminogen to turn into plasmin which causes fibrinolysis

Question 4

tissue plasminogen contraindications

Answer 4

intracranial or subarachnoid hemorrhage, high BP (>185/110), rapidly resolving, MI/stroke/head injury in last 3 months, surgery in past 2 weeks, active bleeding, acute trauma (fracture), anticoagulation therapy, GI bleed (look for occult blood)

Question 5

aspirin

Answer 5

antiplatelet, 24-48 hrs after ischemic or transient ischemic stroke, 24 hrs after thrombolysis, prevents stroke recurrence

Question 6

clopidogrel

Answer 6

antiplatelet, for pts allergic to aspirin

Question 7

antihypertensive drugs and stroke

Answer 7

high BP with stroke often, antihypertensive Tx if BP >220/120, risk - lowering BP will decrease cerebral perfusion

Question 8

mechanism of ganiciclovir

Answer 8

prodrug phosphorylated by viral thymidine kinase, inhibits viral DNA synthesis, competitive DNA poly binding and chain termination, not effective against latent virus, tx for CMV

Question 9

mechanism of acyclovir

Answer 9

prodrug phosphorylated by viral thymidine kinase, inhibits viral DNA synthesis, competitive DNA poly binding and chain termination, not effective against latent virus, tx for HSV1 and HSV2

Question 10

mechanism of trifluridine

Answer 10

progrud that must be phosphorylated by host kinases (higher toxicity), inhibits viral DNA synthesis, competitively binds DNA pol and chain termination, topical tx for HSV keratoconjunctivitis

Question 11

mechanism of penicillin

Answer 11

cell wall inhibitor, binds penicillin binding proteins, can cause seizures at high levels by blocking binding of inhibitory GABA to receptors

Question 12

mechanism of albendazole

Answer 12

microtubule inhibitor, tx for taenia solium (neurocysticerosis) - good for roundworms and tapeworms

Question 13

mechanism of sulfadiazine + pyrimethamine

Answer 13

folate synthesis inhibitor, tx for toxoplasmosis

Question 14

tx huntington depression

Answer 14

common, SSRIs / tricyclics, counseling

Question 15

tx huntington psychosis / agitation

Answer 15

atypical antipsychotics, quetiapine (does not worsen motor), risperidone / haloperidol / olanzapine (may help chorea too)

Question 16

tx huntington cognitive decline

Answer 16

none, compensatory strategies, social supports, OT for independence, assistance with driving, finances, personal care

Question 17

non-pharm tx huntington chorea

Answer 17

non-pharm - may not be bothersome / reduce stress / reduce anxiety / reduce depression / calm environment / adaptive equipment

Question 18

tetrabenazine

Answer 18

tx huntington chorea, monoamine-depleting agent - inhibits presynaptic dopamine release and blocks CNS dopamine receptors, reduces mild chorea, may worsen suicidal thoughts/depression/cognitive/psychiatric, if not tolerated can give amantadine which is an NMDA receptor antagonist

Question 19

neuroleptics

Answer 19

tx huntington chorea, block post-synaptic dopamine receptors, treats both psychiatric and motor

Question 20

atypical antipsychotics

Answer 20

tx for mild to moderate huntington chorea, olanzapine, risperidone, clozapine, aripirazole, quetiapine

Question 21

typical antipsychotics

Answer 21

tx moderate to severe huntington chorea, haloperidol, fluphenazine

Question 22

deep brain stimulation

Answer 22

tx for severe chorea, worsens bradykinesia

Question 23

huntington investigational tx

Answer 23

memantine - slow cognitive effects, creatine/HUFA/minocycline - slow apoptosis

Question 24

haloperidol

Answer 24

typical anti-psychotic, dopamine DA2 receptor antagonist, causes parkinsonism motor effect

Question 25

clozapine

Answer 25

atypical anti-psychotic, dopamine DA2 receptor antagonist with faster off-rate, 5TH serotonin receptor antagonist, increases NMDA receptor activity

Question 26

monoamine oxidase (MAO) inhibitor

Answer 26

anti-depressant, monoamine oxidase degrades norepinephrine and serotonin, blocking MOA increases NE and 5HT at synapse

Question 27

tricyclics (imipramine)

Answer 27

anti-depressant, decreases norepinephrine and serotonin reuptake, increasing NE and 5HT at synapse

Question 28

specific serotonin reuptake inhibitors (SSRI)

Answer 28

anti-depressant, decrease serotonin reuptake, increasing 5HT at synapse

Question 29

anti-depressants

Answer 29

long latency for effective tx (weeks/months), possibly due to neural plasticity and time needed to change gene expression

Question 30

deep brain stimulation

Answer 30

anti-depressant, used in pts who do not respond to drugs, stimulate the nucleus accumbens

Question 31

carbidopa / levodopa (sinernet - 1:10 or 1:4)

Answer 31

empiric tx for parkinson

Question 32

carbidopa

Answer 32

prevents peripheral metabolism of levodopa, means more gets into CNS, tx for parkinson, increased to prevent nausea / vomiting side effect of excess peripheral dopamine

Question 33

levodopa

Answer 33

naturally metabolized to dopamine, tx for parkinson, side effect induced dyskinesia, decreases akinesia, rigidity, tremor - if pt responds to drug then confirms parkinson

Question 34

ropinirole

Answer 34

additional tx for parkinson, D2 / D3 dopamine receptor agonist in putamen, given for increased cogwheel rigidity without spasticity, side effect sleep attacks and edema, high dopamine levels can cause psychosis (hallucinations)

Question 35

pallidotomy

Answer 35

removed globus pallidus internus on one side, done to reduce tremor, rigidity, akinesia in late parkinson, removes GPi over inhibition of thamalus

Question 36

adverse effects of levodopa tx for parkinson

Answer 36

orthostatic hypotension, nausea / vomiting due to stimulation at chemoreceptor trigger zone, involuntary dyskinesia, psychosis (high dopamine in limbic system) - all due to high levels of dopamine in CNS

Question 37

drug interaction with levodopa

Answer 37

pyridoxine (vit B6), coenzyme to peripheral l-aromatic amino acid decarboxylase enzyme that metabolizes levodopa to dopamine - caution multivitamins

Question 38

carbodopa

Answer 38

inhibits l-aromatic amino acid decarboxylase, prevents peripheral metabolism of levodopa - more gets into CNS

Question 39

trihexyphenidyl (artane)

Answer 39

alternative tx for parkinson, CNS muscarinic receptor antagonist, anticholinergic

Question 40

amanradine (symmetrel)

Answer 40

antiviral, parkinson tx, NMDA receptor antagonist, used with levodopa

Question 41

COMT inhibitors (stalevo)

Answer 41

tx parkinson, decreases L-DOPA metabolism, given with l-dopa/carbodopa

Question 42

pramipexole (mirapex)

Answer 42

tx parkinson, partial receptor of D2 dopamine receptor

Question 43

selegiline (eldepryl)

Answer 43

tx parkinson, inhibits monamine oxidase that breaks down dopamine, allows for lower levodopa dosage

Question 44

levodopa

Answer 44

amino acid that can cross BBB, dopamine can not cross BBB, 95% is metabolized in gut need large doses to reach brain, must give with carbodopa enzyme inhibitor

Question 45

chlorpromazine

Answer 45

dopamine antagonist, will worsen Parkinson

Question 46

bromocriptine

Answer 46

dopamine agonist that inhibits prolactin release, can treat amenorrhea with galactorrhea caused by pituitary tumor