CNS 1 - Sedatives. Hypnotics. Alcohols. AEDs. Anti-parkinsonism Flashcards
(171 cards)
0
Q
Which drug prolongs the duration of chloride channel opening of GABA A?
A
Barbiturates
1
Q
Which drug increases GABA effect by increasing the freq of opening GABA A?
A
Benzodiazepines
2
Q
This classification of drug has a calming effect but NO effect on motor or mental functions?
A
Sedatives
3
Q
This drug classification has more pronounced depression than sedation.
A
Hypnotics
4
Q
What do you call the principle involve in depression induced by hypnotics?
A
Graded dose dependent depression
5
Q
True or false. BDZ causes withdrawal symptoms?
A
True
6
Q
Is it safe to use BDZ for anxipus, pregnant patients?
A
No. It crosses placental barrier and BBB.
7
Q
This drug induces sedation but has no ANS, analgesia and antipsychotic property?
A
BDZ
8
Q
Ability to cross the BBB depends on?
A
Lipophilicity
9
Q
This drug’s MOA is terminated via redistribution to fat.
A
BDZ
10
Q
True or false. BDZ doesnt produce active metabolites?
A
False
11
Q
Among the metabolites produced, which is/are rapidly conjugated?
A
Triazolam. Alprazolam
12
Q
What cyrochrome p450 affects your BDZ biotransformation?
A
CYP3A4
13
Q
Give BDZs that are rapidly slowly absorbed.
A
S-LOT
14
Q
Give BDZ drug/s that despite having an active metabolite are rapidly conjugated.
A
Alprazolam. Triazolam
15
Q
Name BDZs that has active metabolites.
A
FATCMD
16
Q
True or false. Midazolam is preferred over chlordiazepoxide for the elderly.
A
True. Short acting. Less accumulation
17
Q
What is the problem with giving short acting BDZs?
A
Rebound effects and withdrawal s/sx
18
Q
What type of BDZs are preferred for those tapering off? Name some.
A
Long acting. FQ CDC
Flurazepam Quezepam Chlordia Dia Clora
19
Q
BDZs that have intermediate duration of effect?
A
LiTE
Lorazepam
Temzepam
Estazolam
20
Q
Do long acting BDZs have withdrawal s/sx? If yes, when?
A
Delayed 1-2wks
21
Q
Give the unwanted side effects of BDZs
A
HaTID
Hang over effects
Tolerance
Increase sensitivity
Dependence /Depression (CP)
22
Q
Give the desired effects of BDZs.
A
SHAMA
Sedation Hypnosia Anesthesia Muscle relaxant Anticonvulsant
23
Q
In cases of acute overdosage of BDZs what be given?
A
Flumazenil. BDZ ANTAGONIST
24
True or false. BDZs has a high risk o drug interaction.
False
25
BDZs have low therapeutic index. True or false.
False
26
What BDZ can be given for PANIC ATTACKS?
Alprazolam. Short acting
27
What anxiolytic can be given for epilepsy?
Clonazepam. Long acting.
28
For delirium tremens?
Lorazepam
29
For active seizure?
Diazepam
30
Anxiolytics given for alcohol withdrawal.
Cloazepate.
Chlordiazepoxide.
Diazapam.
Oxazepam.
31
What BDZ can be used as an anesthetic?
Midazolam
32
For sleep disorders?
Flurazepam. Temazepam. Triazolam. Quezepam
33
Unwanted effects of Flumazenil.
Cardiac arrythmias.
| Seizure
34
True or false. BDZs have fast elimination rates.
False. Slow, preferred due to longer CNS effects
35
Why is flumazenil a good bdz antagonist?
Short half life. Rapid hepatic clearance. Rapid onset of action
36
This BDZ SUBTYPE, has the greatest risk for tolerance but has the lowest risk for withdrawal.
Zaleplon.
37
How many weeks does it take for zaleplon to have tolerance? How about Eszopiclone? And Zolpidem?
5 weeks. 6months. High doses.
38
Among BDZ subtype, which has rebound insomnia?
Zolpidem. Zaleplon.
39
Do all BDZ subtype has rebound insomnia? If no, which one doesn't have?
Eszopiclone
40
BDZ ST that can be used to induce sleep.
Zaleplon.
41
Which can be used to maintain sleep? What type and name of drug?
Eszopiclone. BDZ subtype
42
Decreases REM and latency of sleep but has a longer duration of axn.
Zolpidem
43
Between BDZ and its ST which has a longer duration of action.
BDZ
44
This anxiolytic drug affects ALL GABA A receptors.
BDZ
45
This affects GABA A alpha 1.
Zolpidem. Zaleplon.
46
This affects GABA A alpha 1 and 3
Eszopiclone
47
This drug affects GABA A by increasing the duration of the opening of the chloride channel.
Barbiturates
48
Barbiturate with half life of 4-5 days.
Phenobarbital. Luminal
49
Short acting barbiturate.
Seconal. Secobarbital
50
Half life of 18h, barbiturate
Secobarbital
51
Pentobarbital.
Intermediate acting barbiturate. 48h. 3 days
52
Nembutal
Intermediate acting
53
Thiopental
Ultra short barbiturate
54
Barbiturate used in anesthesia induction
Thiopental
55
Used for febrile seizure
Phenobarbital
56
What makes thiopental ultra short acting?
Very lipid soluble
57
Barbiturates cause full surgical anesthesia
True
58
All barbiturates has SLOW hepatic metab EXCEPT?
Thiopental. Rapidly acting and metabolized
59
Which barbiturate remains unchanged in urine?
Phenobarbital
60
Do barbiturates cause CP depression in oral doses?
No, only IV.
61
Phenobarbital causes enzyme induction in short term use
False, long term use.
62
What are the contraindications in giving barbiturates. May choose more than 1.
```
A. Pregnant
B. Acute porphyria
C. Renal impairment
D. Liver impairment
E. Bronchial asthma
F. Hypertensive
```
All of the above
63
What mechanism terminates action of barbiturates, especially Thiopental.
Redistribution.
64
Redistribution leads to what effect?
A. Prolongation of effect
B. Termination of effect
B. Termination
65
Flumazenil and TCAs causes what when combined.
Seizure. Cardiac arryhmias
66
What classification does buspirone falls?
Non benzodiazepine
67
This drug is desired because of the absence of withdrawal rxn despite abrupt discontinuation.
Buspirone
68
Buspirone has rebound insomnia like zaleplon.
False.
69
Buspirone has the following properties.
Anticonvulsant
Hypnotic
Muscle relaxant
False. It only relieves anxiety.
70
Used in generalized anxiety.
Buspirone
71
Buspirone is used in panic attacks. True or false.
False. Alprazolam is for panic attacks
72
Rifampin is an inducer or inhibitor.
Inducer.
73
Give inhibitors of CYP3A4.
KEto. NeGra.
Ketoconazole
Erythromycin
Nefazedone
Grapefruit juice
74
Buspirone has an affinity for what receptor?
Dopamine 2
75
Also known as an 5HT partial agonist
Non BDZ - Buspirone
76
What 2 drug induces sleep by decreasing sleep latency?
Ramelteon.
| Zaleplon
77
What is the difference between zaleplon and ramelteon?
Zaleplon activates GABA A alpha 1 receptor. Ramelteon activates MT 1 and 2 agonist.
78
Main enzyme for ramelteon metabolism
CYP1A2
79
Ramelteon undergoes extensive first pass metabolism which has shorter half life than parent drug. Trie or false.
False. Longer half life than parent drug
80
What sedatives undergoes extensive hepatic metabolism?
Ramelteon and Buspirone
81
What differentiates your buspirone and ramelteon on abuse possibility?
Buspirone - MINIMAL
| Ramelteon - ZERO
82
This drug causes hyperprolactinemia.
Ramelteon
83
Its ok to take ramelteon to patients with HPN and diabetes.
No worsens conditions.
84
It is best to take melatonin agonist with fatty meals to fasten absorption.
False. Decreases absorption
85
Inhibitors of CYP1A2 increases ramelteon in plasma.
True. Ciprofloxacin. Tacrine. Fluvoxamine. Zileuton.
86
What antihistamine generation causes sedation?
1st
87
What is the expected result when a patient is given with Doxylamine?
Sedation
88
What drug can be used to alleviate physiologic component of anxiety?
Beta blokers
89
This can be given for performance anxiety.
Beta blockers
90
Antidepressant that has NO anti cholinergic effect.
Mirtazapine. Tetracyclics
91
This causes orthostasis and dizziness. Used as an antidepressant.
Trazodone
92
Main drug classification for anxiety.
BDZ
93
For alcohol withdrawal.
CODaC
Clorazepate
Oxazepam
Diazepam
Chlordiazepoxide
94
Among all sedative hypnotics which causes the highest tolerance? The lowest?
Barbiturates. Non-BDZ
95
Among all sed-hyp which has no withdrawal sx.
5HT-1 partial agonist
96
With continuous use of BDZ, eventually it changes hepatic drug metabolizing enzyme. True or false.
False
97
Among BDZ what can be used for situational sleep disorder?
Triazolam
98
Alcohol peak blood concentration
30mins
99
Concentration of alcohol rises quickly in what body part?
Brain
100
Which gender are more at risk for heart and liver damage in alcohol consumption?
Female
101
Most of the alcohol taken are metabolized and excreted as urine. True or false.
False. 90% liver. 10% lungs and urine
102
Which enzyme acts on Ethanol? Inhibits what enzyme?
Fomepizole. Alcohol dehydrogenase
103
Disulfiram inhibits what enzyme? And what product? Producing what product?
Aldehyde dehydrogenase.
Acetate
Acetaldehyde
104
What is the effect of having an increase muscle built?
More area for alcohol to deposit. Decreased blood conc
105
Give some disulfiram rxns.
Facial flushing.
Nausea and vomiting
Dizziness
Headache
106
What causes disulfiram rxn?
Accumulation of acetaldehyde
107
What other drugs causes disulfiram like rxns
Metronidazole
OHA
Cephalosporins
108
Alcohol has high caloric value resulting to body weight increase. True or false.
False. It doesnt necessarily result on increased body weight
109
Alcohol activates what CYP. Give the effect.
CYP2E1. Transforms acetaminophen to chemicals that causes liver damage
110
What endorphin blocker can be given to decrease alcohol craving?
Opiod antagonist. Naltrexone
111
DOC for alcohol withdrawal.
Naltrexone
112
Given to prevent seizure during alcohol withdrawal.
Topiramate
113
This drug is given to decrease emesis in AW and craving too
Ondansetron
114
Acamprosate MOA
NMDA receptor blocker
| GABA A agonist
115
DOC for acute methanol and ethylene glycol intox.
Fomepizole
116
Has high affinity to alcohol dehydrogenase more than methanol
Ethanol
117
Competitively inhibits oxidation of methanol
Ethanol
118
Stages of ethylene glycol oxidation.
EDARO
```
Excitation
Depression
Acidosis (metabolic)
Renal insufficiency
Oxalate accumulate
```
119
This must be watched out for in times of methanol poisoning.
Visual disturb.
Coma.
Resistant acidosis
120
What electrolytes are involve in EPSP and IPSPs?
EPSP - Na and Ca influx
| IPSP - Cl influx and K efflux
121
Gold standard for diagnosing seizure
EEG
122
Anti seizure drugs are poorly absorbed. True or false
False
123
This drug increases the available levodopa peripherally.
Carbidopa
124
Inhibits dopa decarboxylase
Carbidopa
125
Gold standard for parkinsons
Levodopa
126
Inhibits COMT
Entacapone
127
Usually given in young patients with PD
Dopamine agonist
128
This ergot dopamine receptor acts on D2.
Bromocriptine. Yow, Bro dalawa tayo
129
PD drug that has low fluctuation response
Dopamine agonist
130
Sinemet is safe to those with glaucoma.
False. Ulcer. Psychosis. Melanoma
131
Modulates GAD TRANSPORT
Valproate
132
Modulates GAD
Gabapentin
133
Doc for absence seizure
Ethosuximide
134
Among AEDs which doesnt have CNS depression
Ethosuximide
135
Irreversibly inhits GABA transaminase
Vigabatrin
136
Inhibits GABA re uptake
Tiagabine
137
Acts on potassium channels that may cause toxicity. AED
Valproate
138
What can be a sub for ethosuximide
Valproate
139
True or false. AEDs acting on Na channels can affect both high firing and physilogic firing.
False
140
This AED acts mainly on Na and T type Ca.
Zonisamide
141
AEDs acting on Na channels
Carbamazepine. Phenytoin
142
Associates with rash. AED
Lamotrigine
143
This AED causes both renal stones and cognitive impairment.
Zonisamide
144
Causes gingival hyperplasia and hirsutism
Phenytoin
145
AED that causes neural tube defect and as a treatment for mania and trig neuralgia
Carbamazepine
146
Causes ataxia and blurred vision. AED
Carbamazepine
BAN-Car Mania
147
Cytochrome responsible for AED metab
CYP3A4. 2C19. 2C9
148
Give the inducers of AED
FOXT from 3A pupunta sa CPPP
149
Inhibitors of AED
FOX TV kasi 19 y/o na aya
150
AED with aplastic anemia
Felbamate
151
What 2 AED causes renal stones
Topimarate
| Zonisamide
152
What AED Causea cogntive slowing
TiTo ZoX
153
Peripheral COMT
Entacapone
154
What PD drug causes hepatotoxicity
Talcapone
155
This drug imitates dopamine
Dopamine agonist
156
Which ergot derivative is more potent?
Bromocroptine
157
What dopamine agonist causes valvular problems
Pergolide
158
This non ergot derivative has neuroprotective propery
Pramipexole
159
Rotigotine is a skin patch dopamine agonist
True
160
Apomorphine is given IM to rescue tx induced dyskinesia
False. SQ
161
This MOA acts on dopamine only
Moa B
162
Moa causes what syndrome when coombined with meperidine an TCA
Serotonin sydrome
163
This is the more potent MOA B
Rasagiline
164
This antagonizes adenosine receptors that are believes to inhibit d2
Amantidine
165
Used for excessive sleepiness
Modafinil
166
Among all PD which cannot be used alone
COMT
167
Common ADR for COMT
Orange colored urine
168
Livedo reticularis and peripheral edema are common in Amantidine
True
169
Doc for febrile seizure
Phenobarbital
170
Do migraine, neuropathic pain and dystonia
Gabapentin
