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

Drug Action in the CNS - Craviso Flashcards

1
Q

Tight junctions in the BBB exist between (astrocytes/endothelial cells)

A

endothelial cells

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2
Q

What types of things pass through channels in the BBB?

A

small ions and water

Na, K and Cl

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3
Q

What things travel via membrane transport (aka passive diffusion) through the BBB?

A
  1. Small lipophilic molecules (O2 and CO2)
  2. Anesthetics, barbiturates
  3. ethanol
  4. nicotine
  5. caffeine
    (all the things that make you feel good)
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4
Q

What things travel via carrier mediated transport (aka solute carriers) through the BBB?

A

Metabolism products

  1. energy transport systems
    a. (Glucosde via. GLUT-1)
    b. monocarboxylates, lactate, pyruvate (MCT1)
    c. creatine (CrT)
  2. amino acid transport systems
    a. large neutral amino acids (LAT1)
  3. organic cation/anion transporters, aka nucleosides
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5
Q

What things travel via receptor mediated transport through the BBB?

A 
HORMONES HAVE RECEPTORS
insulin
transferrin
leptin
IgG
TNFa
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6
Q

what things travel via adsorption-mediated transcytosis sytems?

A

histone and albumin

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7
Q

What things are ACTIVELY EFFLUXED from the brain via the BBB?

A

P-glycoprotein
BRCP
MRP 1,2,4,5

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8
Q

What is the role of P-glycoprotein? (P-gp)

A

membrane transporter that modulates drug distribution

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9
Q

What types of cells express high levels of Pgp?

A

capillary endothelial cells of the BBB

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10
Q

Which drugs are substrates for Pgp?

A 
chemo agents (vinca alkaloids, doxorubicin), abx like rifampin
anti-epileptics
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11
Q

How does high levels of Pgp expression effect drug transmission to the brain?

A

low levels of drug in the brain

it is a hypothesis for refractory epilepsy and multidrug resistance in general

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12
Q

membrane transport of drugs via passive diffusion relies on (blank) solubility

A

lipid solubility

the greater the lipid solubility, the faster the penetration

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13
Q

Which two compounds have higher than expected concentration in the brain for their lipid solubility?

A

glucose

L-DOPA

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14
Q

Which two compounds have lower than expected concentration in the brain for their lipid solubility?

A

phenobarbitol and phenytoin

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15
Q

What are the areas of the brain where the bbb is more permeable?

A 
P-CAMP
AREA POSTREMA
Median eminence
Pituitary gland
Pineal gland
Choroid plexus capillaries
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16
Q

T/F: viral and fungal infections can increase bbb permeability

A

false; viral and bacterial

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17
Q

What is the best route of drug admin for global delivery?

A

vascular route

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18
Q

T/F: each neuron has it s own capillary

A

true

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19
Q

Drugs that influence behavior and improve the functional status of patients with neurological or psychiatric diseases act by (blanking or blanking) neural excitability, usually by targeting specific transmitter systems.

A

enhancing or blunting

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20
Q

drugs that effect synthesis, storage, release, reuptake and/or degradation of neurotransmitters; agonist or antagonist activity at nerve terminal autoreceptors
are (pre/post) synaptic modifiers

A

presynaptic

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21
Q

drugs that are receptor agonist, antagonist or modulatory activity; degradation of neurotransmitters are (pre/post) synaptic modulators

A

post-synaptic

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22
Q

T/F: drugs may have direct effects on voltage gated ion channels

A

true

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23
Q

T/F: drugs may have non-specific effects on membranes overall

A

true

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24
Q

what is the chemoreceptor trigger zone for vomiting?

A

area postrema

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25
What four chemicals does the area postrema sense that induces vomiting?
5-HT3 D2 M1 NK1
26
can antiemetic drugs be used for post operative and radiation induced emesis?
yes
27
How do 5-HT3 receptor antagonsists work?
serotonin reeptors are Na channels, peripherally block intestinal vagal afferents
28
What are the common 5-HT3 receptor antagonist
``` ZOFRAN KYTRIL Anzemet Lotronex Aloxi ```
29
What is the only NK1 receptor antagonist
Emend, can give oral or IV
30
Do corticosteroids act directly on neurotransmitters?
nope
31
Which corticosteroids are used to treat nausea?
dexamethasone | methylprednisone
32
Substituted benzamides are what class of antagonists?
d2 receptor
33
what effect to D2 receptor antagonists have on GI motility?
increase GI motility
34
T/F: d2 receptor antagonists may be used alone in anti emetic therapy
true
35
What drug class do you use to treat unproductive N/V?
``` D2 receptors antagonists (phenothiazines) Phenergan Compazine H1 antagonists Doxylamine ```
36
What are the common d2 receptor antagonists?
Reglan (oral, IV, IM) | Tigan
37
What are the side effects of D2 receptor antagonists (think of what they act on!
restlessness, fatigue, headache, insomnia, confusion, dystonias and tardive dyskinesia (
38
when are oral cannabinoids approved for use?
when the pt. doesn't respond to other drugs
39
oral cannabinoids can be used in conjunction with other drugs for (blank) emesis
refractory
40
What are the common cannabinoid drugs?
marinol | cesamet
41
What are the side effects of cannabinoids?
euphoria, dysphoria, hallucinations; abuse potential
42
T/F: smoking marijuana can decrease emesis
true
43
What is the MOA of H1 receptor antagonists?
blocks mAChR
44
What is a delayed release drug used in the N/V in pregnancy?
doxylamine
45
what are the SE of the H1 antagonists?
sedation and anti-muscarinic effects
46
What class of drugs should you use for motion sickness?
short term immediate relief H1 receptor antagoinists Dramamine (oral IV) Antivert for vertigo long term control: mACh antagonists Scopolamine--skin patch placed behind the ear
47
What are the three strategies in antiseizure therapy?
1. Enhance GABAergic neurotransmission 2. Attenuate glutaminergic neurotransmission 3. Modify ion conductance through channels
48
What are the four methods of enhancing GABAergic transmission?
1. enhance synth 2. block degradation 3. block reuptake 4. enhance post-synaptic GABAa receptor activity
49
Tiagabine has a (pos/neg) effect on GABA transporter activity
negative
50
Vigabatrin has a (pos/neg) effect on GABA-T enzyme
negative
51
Benzos and phenobarbitol have a (pos/neg) effect on GABA-a receptors
positive
52
T/F: Vigabatrin works on presynaptic cells and glial cells
true
53
Do benzos and phenobarbitol work on pre or post synaptic cells?
post
54
Modification of GABA transporters happens on which two cells?
presynaptic and glial cells
55
how does inhibition of voltage gated Na channels work in antiseizure therapy?
blockage prevents depol which prevents vesicular release of glutamate
56
Gabapentin and Pregabaline block the A2d subunit of the L-type (Na/Ca) channel
Ca
57
Levetircetam blocks what step in glutaminergic transmission?
SV2A enzyme storing glutamate in the vesicles
58
Felbamate blocks the (NMDA/AMPA) receptor on the post synaptic neuron
NMDA
59
Topiramate blocks the (NMDA/AMPA) receptor on the post synaptic neuron
AMPA/kainate
60
phenytoin and carbamazepine block type 1 voltage gated Na channels on the (pre/post) synaptic neuron
presynaptic
61
lamotrigine blocks type (1/2) voltage gated Na channels on the pre synaptic neuron
type 2
62
retigabine blocks all (Na/K) channels on the presynaptic neuron
K chanels
63
Ethosuximide and valproate block the type 2 Na channels on the (pre/post) synaptic neurone
post
64
Alzheimers is caused by a loss of ACh neurons in what two areas of the brain?
pyramidal neurons of the hippocampus and cholinergic neurons of the basal forebrain
65
Donepezil is used to treat alzheimer's by increasing ACh levels via....
reversible AChase inhibitor
66
Memantine is a low affinity open channel blocker of (AMPA/kainate) receptors that selectively inhibits the pathological activation of the receptor in Alzheimer's
ampa
67
Parkinson's is caused by a loss of dopaminergic neurons in what area of the brain?
substania nigra
68
parkinson's leads to a shortage of D neurons in the (intra/extra)pyramidal circuit
extrapyramidal
69
What is the main MOA of parkinson's Tx?
increase Dopaminergic neruons via L-DOPA and DM agonists
70
huntington's is due to a mutation in what protein?
htt
71
Chorea is characteristic of (HD/PD)
PD
72
chorea is caused by an imbalance in dopamine signaling as well as what other transmitter?
gaba
73
Tetrabenazine is used to treat HD by depleting dopamine via selectively and reversibly inhibiting which enzyme?
VMAT2
74
T/F: D2 receptor antagonists control movement as well as psychosis associated with HD
true
75
ALS is caused by a degeneration of which three nerve tracts?
1. spinal 2. bulbar 3. cortical ^^motor neurons
76
Muscle weakness, muscle atrophy, fasciculations,spasticity, dysarthria, dysphagia and respiratory compromise are characteristic of which degenerative dz?
ALS
77
Treatment of ALS involves inhibiting (glutamate/glycine) release
glutamate
78
Tx of ALS involves of (NMDA/kainate/both) type glutamate receptors
true
79
T/F: Tx of ALS involves blocking VGCCs
false; voltage gated Na channels
80
Riluzole is a drug used to treat ALS by blocking voltage gated (blank) channels
Na
81
Baclofen is a drug used to treat spasticitiy in ALS by targeting the GABA-(a/b) receptor
B
82
Tizanindine is an (a1/a2)-adrenergic receptor agonist used in ALS treatment
a2
83
What are the two ways that toelrance to CNS drugs is developed?
pharmocokinetic aka altered metabolism physiologic aka long term alterations
84
Describe the physiologic changes that result in CNS drug tolerance?
up or down regulation of receptors | changes at other synapses for other neurotransmitters
85
T/F: tolerance to one drug will produce tolerance to other drugs within the same class
true aka cross tolerance
86
drug use pimarily to receive rewarding effects is what type of SUD?
psychologic
87
drug use primarily to avoid withdrawal symptoms is what type of SUD?
physiologic
88
What is cross-dependence?
drugs within the same class support individuals physically dependent on other drugs in the same class; useful during detox
89
drugs of high abuse are schedule what?
shedule 1
90
what are the prescribing restrictions on sched. 2 drugs?
no telephone Rx, no refills
91
What are the restrtictions on sched. 3 drugs?
Rx must be rewritten after six months or five refills
92
What are the restrictions on sched. 4 drugs?
must be rewritten after six months or five refills, but diff. penalties for illegal possession
93
T/F: sched. 5 drugs are available OTC
true
94
T/F: schedule 1 drugs can be used for medical treatment
yes, only GHB for narcolepsy and marijuana in some states
95
ACE inhibitors can show what types of psychiatric symptoms?
mania, anxiety, hallucinations, depression, psychosis
96
Acetazolamides can show what types of psychiatric symptoms?
depression, delirium, confusion, stupor (elderly are very prone)
97
Clarithromycin can show what types of psychiatric symptoms?
mania
98
Digoxin can show what types of psychiatric symptoms?
delirium, depression, psychosis, visual hallucinations (elderly at high risk)
99
Mefloquine can show what types of psychiatric symptoms?
vivid dreams or nightmares
100
metronidazole can show what types of psychiatric symptoms?
depression, agitation, confusion
101
What are the non-CNS drugs that can show what types of psychiatric symptoms?
``` ACE inhibitor Acetazolamide Clarithromycin Digoxin Mefloquine Metronidazole ```
102
drugs with high lipophilicity will cross the bbb and store in what tissues?
fat
103
drugs with a high degree of plasma protein binding have what factor that must be considered?
other drugs that displace its binding will result in more side effects and higher serum concentration
104
what is the depot effect?
drugs that store in fat can be released over time after the actual administration of the drug has stopped
105
What are considerations specific to the liver that you should take into account when writing an rx?
Status of liver function Individual variations in rate of metabolism Saturation kinetics Conversion to an inactive versus an active metabolite Inhibition by other drugs Induction of metabolism by itself or another drug
106
What are specific concerns when prescribing drugs for the elderly?
``` CONCERNS: Diminished hepatic and renal function Paradoxical reactions Polypharmacy Greater susceptibility to side effects (some may be life-threatening) ```

Block 8 Week 1 Colt (10 decks)

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