Neuro: neurodegenerative drugs

Question 1

In parkinson, as dopamine levels _______ ACH levels______

Answer 1

dopamine—-decreases

ACH—-increases

Question 2

do the parkinson drugs stop or reverse the diseaes

Answer 2

NO just help with s/s

Question 3

what is levodopa

-can it penetrate BBB

Answer 3

immediate precursor (before) of dopamine 
and is immediately converted to dopamine once it crosses the BBB

Question 4

what is carbidopa

Answer 4

dopamine decarboxylase inhibitor
–diminishes metabolism of levodopa in the periphery (reducing s/e)—-increasing the availability of levodopa to the CNS—therefore more levodopa to cross BBB and become DOPAMINE

Question 5

what happens when we add carbidopa to levodopa

Answer 5

it lowers the amount of levodopa needed by 4-5 fold!

*decreases SE too from peripherally formed dopamine

Question 6

what happens if we dont add carbidopa to levodopa?

Answer 6

the levodopa is converted to dopamine peripherally—-and less will be available to cross BBB and then the effects of the drug are diminished

Question 7

Mainstay of TX for PD???

Answer 7

L-C

*reduces severity of s/s for the first few years of tx

Question 8

Long term use of Levodopa causes?

Answer 8

“wearing off”

flucctations and diskinesias

Question 9

Peripheral SE from L-C

Answer 9

N/V
cardiac arrythmias
hypoT

Question 10

Central SE from L-C

Answer 10

visual/auditory hallucintions, dyskineseas, psych S/s

Question 11

drug-drug interactions of L-C

Answer 11

Vit B6—-pyridoxine diminishes effectiveness

Question 12

If L-C is given with _______ can cause HTN crisis

Answer 12

MAOI

Question 13

What happens if L-C given with MAOI

Answer 13

HTN CRISIS

Question 14

T1/2 of L-C

Answer 14

1-2 hours

Question 15

where is L-C absopbed

Answer 15

small intestine (if taken w/o food)

Question 16

MAO Type B

—MOA?

Answer 16

inhibits MAO type B—-enzyme that b/d dopamine

actions of levodopa are potentiated*** letting dose be reduces

Question 17

Selegiline and Rasagiline

Answer 17

MAO type B

*adjunct tx to L-C

Question 18

Catechol-O-Methyltransferease Inhibitors (COMT)
MOA–?
which of the drugs is prefered?

Answer 18

ENTACAPONE AND TOLCAPONE
MOA—enzyme COMTresp for b/d of dopamine
*entacapone prefered over Tolcapone

Question 19

Tolcapone–can cause??

Answer 19

COMT-Inhib

may cause fulminating hepatic necrosis—–need to monitor liver enzymes

Question 20

Dopamine rec agonists work where in brain

Answer 20

basal ganlia

Question 21

Which drug causes more movement disturbances and dyskineasias:
-Levodopa OR Dopamine rec agonists?

Answer 21

LEVODPA

Question 22

Bromocriptine
Pramipexole
Ropinirole

Answer 22

dopamine rec agonists

Question 23

Which receptors does Bromocriptine stimulate

Answer 23

dopamine
alpha
serotonin

Question 24

Which patients need to be cautious when using Bromocriptine

Answer 24

Hx of MI or Periph vasc disease due to incr risk of vasospasms

Question 25

what condition can administrtion of bromocriptine worsen?

Answer 25

psychiatric conditions

Question 26

Bromocriptine is a _____ derivative

Answer 26

ERGOT--fungus

Question 27

Amantadine

Answer 27

anti-viral

Question 28

MOA amantadine

Answer 28

increases presynaptic dopamine release and improves long term levodopa induces dyskineases * tolerance develops quick * few SE

Question 29

IND for amantadine

Answer 29

Early onset PD with mild s/s

Question 30

Antimuscarinics for PD MOA

Answer 30

blocks excitatory cholinergic effect

Question 31

IND for antimuscarinics in PD

Answer 31

Under 70 with TREMOR*******

Question 32

does Antimuscarinic agents improve dyskinesisas?

Answer 32

NO

Question 33

Trihexyphenidyl and Benztropine

Answer 33

Antimuscarinics for PD

Question 34

SE of Trihexyphenidyl and Benztropine

Answer 34

constipation, dry mouth, blurred vision, tachycardia urinary retention

Question 35

Contraindicatinos for Trihexyphenidyl and Benztropine

Answer 35

BPH and glaucmoma PT

Question 36

Loss of cortical neurons amyloid deposition (senile plaques) Neurofibrillary tangles--tau proteins

Answer 36

Three distinguishing features of AlzD

Question 37

Donepezil Galantamine Memantine Rivastigmine

Answer 37

Anti-AD

Question 38

1st line tx for AD

Answer 38

Acetylcholinesterase Inhibitors | ****donepezil

Question 39

MOA for Donepezil | SE

Answer 39

reversibly inhibits ACHE * **ACH levels remain high in junction * **incr in stimulation of nicotinic and muscarinic receptrs SE: -Nausea dizziness insomnia

Question 40

2nd line tx for AD | MOA of drug

Answer 40

N-methyl-d-aspartate (NMDA) Antagonist MEMANTINE MOA: blocking NMDA--decrease neuronal excitation b glutamate----helps improve cognition and funct capacty

Question 41

IND for Memantine

Answer 41

2nd line tx for AD | *used in mod-severe

Question 42

SE of memantine

Answer 42

agitation dizzines HA---CNS | dystonic rxns

Question 43

Tx for acute exacerbation of MS

Answer 43

IV corticosteroids HIGH DOSE

Question 44

TX for relapse-remitting/progressive disease of MS

Answer 44

B-interferon

Question 45

Tx for insomnia

Answer 45

Zolpidem--prefered hypnotic or Zalelon: sim to zolpidem.. but fewwer residual efects on psychomotor and cognitive funct OR Eszopiclone--good forp to six months OR Ramelteon--can be given Long term---for diff falling asleep**

Question 46

Insomina + anxiety tx

Answer 46

benzos | Flurazepam or quazepam

Question 47

ramelton or zalepon--good for what type of insomnia

Answer 47

ISSUES FALLING asleep

Question 48

are the medications used for insomnia controlled substanes?

Answer 48

yes

Question 49

DOA for phenobarb

Answer 49

long acting

Question 50

DOA for secobarbital

Answer 50

short acting 2-4hrs

Question 51

PT cannot fall asleep but can stay asleep, which barbituate to give?

Answer 51

Secobarbital

Question 52

what drugs have replaced barbituates?

Answer 52

benzos

Question 53

high doses of barbituates cause?

Answer 53

CNS depressing

Question 54

low doses of barbituates cause?

Answer 54

decr in Reticular activating system | sedation/sleep

Question 55

MOA for sedative-hypnotic drugs

Answer 55

GABA**** | regulates chlorine channel

Question 56

whhat receptor does GABA bind to

Answer 56

GABA a

Question 57

GABA effects

Answer 57

reduces generation of APs and inhibits neuronal activity

Question 58

Barbituates are used as_____ to tx___ and ____

Answer 58

sedative insomnia anxiety

Question 59

what drug is used in tx neonatal hyperbilirubinemia

Answer 59

phenobarbital

Question 60

SE of barbituates

Answer 60

sedation, nausea, ***TERATOGENI * p-450---can decr other drug levels--not good for combo use with digitalis, phenytoin * **dependency

Question 61

Barbituate OD | TX?

Answer 61

cardiac and respiratory depression**** tx with mechanical ventilaion dyalissi alkalinzation of urine with sodium bicarb

Question 62

which drug MOA * **interferes with electrolyte transport across neuroanl cell membranes * inhibit neuron activation * potentiate GABAa receptor activity * increase flow of Cl- ion---cell mem hyperpolorization

Answer 62

BARBITUATES

Question 63

anxiolytics

Answer 63

anti anxiety drugs

Question 64

Midazolam and Triazolam are ___acting

Answer 64

short

Question 65

Benzos are divinded into three groups based on

Answer 65

DOA

Question 66

``` Lorazepam temazepam oxazepam alprazolam chlordiazepoxide are all _____ acting ```

Answer 66

intermediate

Question 67

diazepam prazepam clonazepam flurazepam

Answer 67

long acting

Question 68

which benozs are used as anesthetics

Answer 68

midazolam | dizepam

Question 69

which drug prolongs effects of benzo

Answer 69

cimitidine--antihistamine

Question 70

cimitidine + benzo

Answer 70

increase DOA of benzo because it blocks enzyme inhibition