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Pharm Exam 3 > week 10: CNS Drugs > Flashcards

week 10: CNS Drugs Flashcards

1
Q

What are “adaptive changes” and how does this contribute to tolerance and physical dependence?

A

Adaptive changes occur when the body physiologically adapts to adjust to the drug in the body.

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2
Q

What happens when drugs that elicit adaptive changes are abruptly discontinued?

A

When the drug is taken away abruptly, your body can go into a state of withdrawal but it’s known as abstinence syndrome due to the adaptive changes.

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3
Q

With Parkinson’s disease - what two NT do we manipulate with pharmacologic interventions?

A 
Dopamine = decreases and this decrease acts as a inhibitory factor in the disease 
ACH = increases in this disease and acts as an excitatory
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4
Q

what neurotransmitter do you want to manipulate specifically for Parkinson’s through medication usually

A

we want to increase our dopamine and to do this we use dopamine agonists

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5
Q

3 groups of dopaminergic agents in the context of PD

A
  1. Levadopa
  2. MAO B
  3. Amantadine
  4. Dopamine agonist
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6
Q

what is the MOA of levodopa

A
  • directly activates DA receptors
  • SO this is a prodrug that needs to be converted to DA in the CNS BUT in order to do this we need to avoid three things (see below)
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7
Q

What MAO B

A
  • we use this in mild to moderate cases
  • prevents dopamine breakdown → which usually MAO B breaks down
  • this is the 1st line drug because it is selective and reversible
  • Selegiline
  • Rasagline
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8
Q

what type of drug is a -giline (selegiline)

A
  • prevents dopamine breakdown → which usually MAO B breaks down
  • this is the 1st line drug because it is selective and reversible
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9
Q

what is the MOA amantadine

A

*promotes DA release and inhibits reuptake

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10
Q

what is the MOA Dopamine agonist

A

*ergot alkaloid = no selective DA receptors
*NON ergot alkaloid = SELECTIVE DA receptor
Act like dopamine
Less effective then L-Dopa BUT less risk of dyskinesia

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11
Q

what drugs are combined with levodopa

A

COMT inhibitors = carbidopa

Decarboxylase inhibitors = entacapone

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12
Q

what type of drug is carbidopa

A

COMT inhibitors

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13
Q

what type of drug is entacapone

A

Decarboxylase inhibitors

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14
Q

what else do you want to avoid with levodopa

A

Avoid high protein meals

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15
Q

why does levodopa need to be combine with other drugs in order to have an effect

A

SO this is a prodrug that needs to be converted to DA in the CNS BUT in order to do this we need to avoid three things

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16
Q

What is the difference between MAO-B & MAO-A?

A

MAO A breaks down serotonin and norepi = there is larger risk of HTN with these patients
MAO B breaks down dopamine = MORE SELECTIVE = so there is less risk of HTN when using a more selective drug

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17
Q

For cognitive impairment what drugs related to NT do we manipulate

A 
AChE = INHIBIT 
NMDA = Antagonize
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18
Q

three AChE inhibitors commonly used in Alzheimer’s Disease

A 
Donepezil = a reversible drug that is highly protein bound and CNS selective 
Galantamine = leads to reversible inhibition 
Rivastigmine = this drug is irreversible and has PNS effects
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19
Q

what class of drug is donepezil and what makes it special

A

an AChE inhibitor and is a reversible drug that is highly protein bound and CNS sensitive

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20
Q

what type of drug is galatamine

A

an ACHe inhibitor

this drug leads to reversible inhibition

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21
Q

what AChE inhibitor leads to reversible inhibition

A

Galantamine

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22
Q

what drug for alziehers leads irreversible and has PNS effects

A

Rivastigmine

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23
Q

what drug is associated with NMDA

A

Memantine

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24
Q

what AChE inhibitors is highly protein bound and CNS selective

A

Donepezil

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25
Q

Understanding the pathophysiology of MS, it makes sense that we would want to inhibit immune responses. What are the two types of drug classes used for this purpose?

A
  1. Immunosuppresants

2. Immunomodulators

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26
Q

how does a immunosuppressant work for MS

A

*inhibits DNA synthesis and repair
*decreased immune cell proliferation
Decreased myelin sheath destructions

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27
Q

how does a immunomodulator work for MS

A

*preferred choice when looking at these two options to stop the progression of the autoimmune
*can stimulate antibody production against drug itself
*special handling
Beta 1a drugs
Beta 1b drugs

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28
Q

what drug can be used for treating distressing or harmful symptoms of MS

A

Dalfampdine = will help with the gait issues

29
Q

When giving any medications that suppress immune responses, what are points of patient education?

A 
Avoid live vaccines when using 
Want to start treatment right away 
Concurrent use of immunomodulators 
High risk of infection
Can have flu like adverse effect
30
Q

what type of drug is mitoxantrone

A

used for MS

31
Q

List the three MAJOR adverse effects of mitoxantrone

A

Myelosuppression
Cardiotoxicity irreversible and leads to HF that can occur years after use
Fetal injury (even in low doses)

32
Q

what is a traditional anti seizure drug

A 
Well established 
Less well tolerated 
More cplex pK
Drug interactions due to CYP450
Less safe in pregnancy but remember some of these benefits outweigh the risks
33
Q

what is a new generation antiseiure drug

A 
Not as well established 
Well tolerated
Simpler PK
NO cyp450 interaction 
Safer in pregnacy
34
Q

what is the prototype for traditional anti seizure drugs

A

Phenytoin

35
Q

what is the MOA of Phenytoin

A
  • Selectively inhibits Na+
  • Slows recovery from inactive
  • Metabolizing enzymes in liver quickly become maxed out → narrow the dosing for this reason
36
Q

what antiseizure drug has the same MOA as phenytoin?

A

Carbamazepine

37
Q

which antiseizure drug should be avoided in pregnancy

A

Valproate

38
Q

what traditional antiseizure drug can lead to live threatening pancreatitis

A

Valproate

39
Q

what is the MOA of Valproate

A

Enhances GABA transmission and blocks Na+ like phenytoin

40
Q

what is the MOA of Ethosuximide

A

Suppression of Ca++ channel in the thalamus

Absence of seizure usage

41
Q

what are the A/E of phenytoin

A 
HIGH TOXICITY RISK
CNS sedation
Insomnia, nystamias 
Gingival hyperplasia 
Measle like rash
Necrosis with the IV
42
Q

what is Phenobarbital

A

traditional antiseizure drug

Potentiates effects of GABA used in anesthesia!!

43
Q

what is special about Phenobarbital

A

long half life
Acute intermittent porphyria
VitD metabolism

44
Q

what is the prototype of the new generation antiseizure medication

A

Oxcarbazepine

45
Q

what is Oxcarbazepine

A

Is a derivative of Carbamazepine which is a Na+ channel inactivation

46
Q

what do we want to avoid taking Oxcarbazepine with

A

Can induce CYP450
Avoid with other drugs that reduce Na+
Avoid alcohol

47
Q

what is Lamotrigine

A

new generation antiseizure medication

48
Q

what is the MOA of Lamotrigine

A

Na++ channel inactivation and Ca++ channel block

49
Q

what does Lamotrigine adversely lead to

A

Unusual AE
Hypo NA+
Hypothyroidism

50
Q

what two new generation antiseizure drugs have unknown MOA

A

Gabapentin

Levetiracetam

51
Q

what is known about pregabalin

A

Binds Ca++ and inhibits glutamate, NE, sub P
Skin rxn
Euphoria
Decreased fertility

52
Q

what new generation antiseizure medication can lead to euphoria and decreased fertility

A

Pregabalin

53
Q

what new generation antiseizure medications have minimal adverse effects

A

Gabapentin

Levetiracetam

54
Q

what drug decreases GABA reuptake in relation to new generation seizure medications

A

Tiagabine

55
Q

Topiramate

A

GABA potentiation
Na++ channel and Ca++ channel block
Metabolic acidosis
Possibly high SI

56
Q

what two drugs are used for spasticity disorders

A

Dantrolene

Baclofen

57
Q

how does dantrolene work

A
  • decreases CA++ efflux from the sarcoplasmic reticulum

* peripherally acting so reduces strength can make you weak, drowsy

58
Q

how does beclofen work

A
  • micics GABA @ hyperreactive motor neurons in spinal cord

* centrally acting

59
Q

when would you not take baclofen

A

Leads to GI issues as AE and recommended not to take if having urination isuses

60
Q

what is serotonin syndrome

A

Serotonin syndrome is when several disorders happen from CNS drugs. SS is one of them. It’s when disoders look similar but are treated inversely. It is when there is wayyy too much serotonin.

61
Q

what drug can put you at risk of serotonin syndrome

A

MAO B inhibitors can put you at risk of serotonin syndrome (this is because at high doses they aren’t selective )

62
Q

what is a controlled substance

A

a drug that has high potential for abuse

63
Q

what should you avoid when taking 1. Selegiline, a MAO-B inhibitor

A
  • SSRIs (selective serotonin reuptake inhibitors)

* tyramine containing foods

64
Q

how does Carbidopa work

A

prevents deactivation of levodopa before it gets to the CNS

65
Q

how does donepezil work

A

prevents ACh degradation in CNS

65
Q

how does donepezil work

A

prevents ACh degradation in CNS

66
Q

w does varenicline work?

A

partially agonize nicotine receptors with stronger affinity than nicotine

67
Q

when thinking about muscle spasms and treatment which may you use in order to avoid muscle weakness

A

baclofen

68
Q

for traditional antiseizure medications, why in phenytoin do you want to avoid taking drugs that are impacted. by CYP450 (indices or inhibitors)

A

because phenytoin quickly maxes out metabolizing enzymes

this means that if CYP450 being altered by another drug can cause high toxicity risk more readily

Pharm Exam 3 (5 decks)

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