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Block 8 Week 1 > Craviso: Drug Action in the CNS > Flashcards

Craviso: Drug Action in the CNS Flashcards

1
Q

Belongs to a family of membrane transporters that modulate drug distribution; capillary endothelial cells of the BBB have high levels compared to other tissues

A

P-glycoprotein

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2
Q

What does transport of drugs through membranes by passive diffusion depend on?

A

the lipid solubility of the drug

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3
Q

The greater the lipid solubility, the (blank) a drug enters the CNS

A

faster

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4
Q

What are two drugs that have a high lipid solubility, but do not get across the BBB efficiently?

A

phenobarbital

phenytoin

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5
Q

What are two drugs that have a low lipid solubility, but diffuse across the BBB more readily?

A

glucose

L-DOPA

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6
Q

List some regions where the BBB is more permeable

A 
area postrema*
median eminence
pituitary gland
pineal gland
choroid plexus capillaries
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7
Q

These can cause an increase in BBB permeability

A

bacterial and viral infections

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8
Q

What is the most promising method for global drug delivery?

A

vascular route

**each neuron has its own capillary for O2 supply, for the supply of other nutrients, and for removing metabolic waste

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9
Q

How do drugs that influence behavior and improve the functional status of patients w neurological/psych diseases act?

A

by enhancing or blunting neural excitability, usually by targeting specific transmitter systems

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10
Q

What are some ways that drugs affect the neurons pre-synaptically?

A

synthesis
storage
release
reuptake/degradation of neurotransmitters

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11
Q

What are some ways that drugs affect neurons post-synaptically?

A

receptor agonists, antagonists

degradation of neurotransmitters

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12
Q

What is the main goal of antiemetic therapy?

A

block neurotransmission at the chemoreceptor trigger zone, at afferent inputs to the emetic center and in the emetic center

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13
Q

3 receptors in the chemoreceptor trigger zone?

A

5HT3
D2
M1
NK1

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14
Q

Antiemetic drug; 5HT3 receptor antagonist; also acts peripherally to block intestinal vagal afferents

A

ondansetron (Zofran)

granisetron (Kytril)

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15
Q

Antiemetic drug; NK1 receptor antagonist

A

aprepitant (Emend)

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16
Q

5HT3 receptors are (blank) channels

A

Na+

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17
Q

Corticosteroid used with antiemetic drugs

A

dexamethasone

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18
Q

D2 receptor antagonist; may also act peripherally to enhance GI motility; alone or in combo for treating CTI nausea and vomiting; also used for treating unproductive nausea and vomiting

A

Metoclopramide (Reglan)

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19
Q

Side effects of Metoclopramide?

A

dystonias

tardive dyskinesia

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20
Q

Oral cannabinoid; thought to act in higher cortical centers; approved for use in patients not responding to other antiemetic agents; can be used for breakthrough or refractory emesis

A

Dronabinol (Marinol)

**synthetic form of THC

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21
Q

What is smoking marijuana used for medically? Side effects?

A

pain, inflammation, spasticity;

euphoria, dysphoria, hallucinations, abuse potential

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22
Q

There are two antiemetic drugs used to control non-productive nausea and vomiting. What are they?

A

Promethazine - D2 receptor antagonist
Doxylamine - H1 receptor antagonist

**both also block mACh receptors

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23
Q

Two H1 receptor antagonists that provide short-term, immediate relief for motion sickness

A

Dimenhydrinate (Dramamine)

Meclizine (Antivert)

24
Q

A muscarinic receptor antagonist that is used for long-term, sustained control of motion sickness; skin patch placed behind the ear that produces less side effects than via the oral route

A

Scopolamine

25
Q

What are four strategies for antiseizure therapy?

A
  1. enhance synthesis of GABA
  2. block degradation of GABA
  3. block reuptake of GABA
  4. enhance postsynaptic GABA-A receptor activity
26
Q

So, one way to prevent seizures is to upregulate GABA activity. What is one other neurotransmitter that you could alter?

A

glutamine (downregulate it)

27
Q

Besides GABA and glutamine, what is another way you could decrease seizures?

A

block ion conductance through channels (block Ca++ and Na+ influx, or K+ efflux)

28
Q

Loss of basal forebrain cholinergic neurons that cause a striking deficiency in ACh

A

Alzheimer’s disease

29
Q

How to treat Alzheimer’s?

A

increasing ACh levels using reversible cholinesterase inhibitors

30
Q

List 3 medications for Alzheimer’s and how they work

A

Donepezil (Aricept) and Ravistigmine (Excelon) - reversible cholinesterase inhibitors;

Memantine - low affinity open channel blocker of NMDA receptors (inhibits the pathological activation of the receptor)

31
Q

Progressive loss of dopaminergic neurons in substantia nigra leading to shortage of dopamine in extrapyramidal movement circuit

A

Parkinson’s disease

32
Q

Primary treatment for Parkinson’s disease

A

increase dopamine levels (L-DOPA)

33
Q

Why do we treat Parkinson’s disease with L-DOPA instead of dopamine?

A

dopamine doesn’t cross the BBB

34
Q

Characterized by chorea – irregular, unpredictable involuntary muscle jerks at different parts of the body that impair voluntary activity that is the result of a loss of neurons from structures of the basal ganglia, imbalances both in GABA functions (diminished) and dopamine functions (enhanced)

A

Huntington’s disease

35
Q

How to treat Huntington’s disease?

A

Tetrabenazine - a selective and reversible centrally-acting dopamine depleting drug

D2 receptor antagonists to control abnormal movements and relieve the psychosis that accompanies the disease

36
Q

a selective and reversible centrally-acting dopamine depleting drug (inhibits VMAT2)

A

tetrabenazine

**inhibits the transporter that takes dopamine into vesicles for storage and release

37
Q

Degeneration of spinal, bulbar and cortical motor neurons that leads to muscle weakness, muscle atrophy and fasciculations, spasticity, dysarthria, dysphagia and respiratory compromise

A

Amyotrophic lateral sclerosis

38
Q

How to treat ALS?

A

Riluzole - involves glutamate release, blocks NMDA and kainate glutamate receptors to inhibit voltage-dependent Na+ channels

39
Q

Two drugs used to treat spasticity?

A

Baclofen - a GABA-B receptor agonist

Tizanidine - an alpha-2 adrenergic receptor agonist

40
Q

A GABA-B receptor agonist

A

Baclofen

41
Q

An alpha 2 adrenergic receptor agonist

A

Tizandine

42
Q

reduced drug effect with repeated use and higher doses required to produce the same effect

A

tolerance

43
Q

What are two ways to get drug tolerance?

A

pharmacokinetic - altered metabolism

physiologic - long-term alterations (at site where drug acts or at other synpases for other neurotransmitters)

44
Q

tolerance to a drug in one class

e.g., sedative-hypnotics) will lead to tolerance to others in the same class (sedative-hypnotics

A

cross-tolerance

45
Q

repeated, compulsive use of a drug that deviates from the social norms of a given culture; disregard of harmful interpersonal or social consequences e.g., ethanol, opiate analgesics, cocaine and other recreational drugs

A

dependence

46
Q

drugs within a pharmacological class (e.g., opiate analgesics) support individuals physically dependent on other drugs in the same class - useful property for “detox”

A

cross-dependence

47
Q

(All non-research use illegal under federal law) – highest abuse potential

A

Schedule I

48
Q

(No telephone prescriptions, no refills)

A

Schedule II

49
Q

(Prescription must be rewritten after 6 months or five refills)

A

Schedule III

50
Q

(Prescription must be rewritten after 6 months or five refills; differs from Schedule III in penalties for illegal possession)

A

Schedule IV

51
Q

(As any other non opioid prescription drug may also be dispensed without prescription unless additional state regulations apply)

A

Schedule V

52
Q

Which schedule of drugs do these fall under?

Stimulants
Depressants
Hallucinogens
Narcotics
Marijuana
A

Schedule I

53
Q

Which schedule of drugs do these fall under?

Opioids
Cocaine, Amphetamine, Amphetamine Complex, etc

A

Schedule II

54
Q

3 important considerations when prescribing CNS drugs?

A

lipophilicity - drug can accumulate in fatty tissue
high degree of plasma protein binding
metabolism via the liver

55
Q

Concerns when prescribing CNS drugs for the elderly?

A

diminished hepatic/liver function
paradoxical reactions
polypharmacy
greater susceptibility to side effects

56
Q

What are some specificity considerations to keep in mind when thinking about CNS drugs?

A

some CNS drugs don’t have an established mechanism;
classified according to primary mechanism of action but can have a similar therapeutic effect via another mechanism;
classified according to therapeutic use, but can have a variety of uses

Block 8 Week 1 (12 decks)

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