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PHARMA 2.0 > CNS 1 - Sedatives. Hypnotics. Alcohols. AEDs. Anti-parkinsonism > Flashcards

CNS 1 - Sedatives. Hypnotics. Alcohols. AEDs. Anti-parkinsonism Flashcards

0
Q

Which drug prolongs the duration of chloride channel opening of GABA A?

A

Barbiturates

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1
Q

Which drug increases GABA effect by increasing the freq of opening GABA A?

A

Benzodiazepines

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2
Q

This classification of drug has a calming effect but NO effect on motor or mental functions?

A

Sedatives

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3
Q

This drug classification has more pronounced depression than sedation.

A

Hypnotics

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4
Q

What do you call the principle involve in depression induced by hypnotics?

A

Graded dose dependent depression

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5
Q

True or false. BDZ causes withdrawal symptoms?

A

True

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6
Q

Is it safe to use BDZ for anxipus, pregnant patients?

A

No. It crosses placental barrier and BBB.

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7
Q

This drug induces sedation but has no ANS, analgesia and antipsychotic property?

A

BDZ

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8
Q

Ability to cross the BBB depends on?

A

Lipophilicity

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9
Q

This drug’s MOA is terminated via redistribution to fat.

A

BDZ

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10
Q

True or false. BDZ doesnt produce active metabolites?

A

False

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11
Q

Among the metabolites produced, which is/are rapidly conjugated?

A

Triazolam. Alprazolam

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12
Q

What cyrochrome p450 affects your BDZ biotransformation?

A

CYP3A4

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13
Q

Give BDZs that are rapidly slowly absorbed.

A

S-LOT

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14
Q

Give BDZ drug/s that despite having an active metabolite are rapidly conjugated.

A

Alprazolam. Triazolam

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15
Q

Name BDZs that has active metabolites.

A

FATCMD

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16
Q

True or false. Midazolam is preferred over chlordiazepoxide for the elderly.

A

True. Short acting. Less accumulation

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17
Q

What is the problem with giving short acting BDZs?

A

Rebound effects and withdrawal s/sx

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18
Q

What type of BDZs are preferred for those tapering off? Name some.

A

Long acting. FQ CDC

Flurazepam
Quezepam
Chlordia
Dia
Clora
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19
Q

BDZs that have intermediate duration of effect?

A

LiTE

Lorazepam
Temzepam
Estazolam

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20
Q

Do long acting BDZs have withdrawal s/sx? If yes, when?

A

Delayed 1-2wks

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21
Q

Give the unwanted side effects of BDZs

A

HaTID

Hang over effects
Tolerance
Increase sensitivity
Dependence /Depression (CP)

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22
Q

Give the desired effects of BDZs.

A

SHAMA

Sedation
Hypnosia
Anesthesia
Muscle relaxant
Anticonvulsant
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23
Q

In cases of acute overdosage of BDZs what be given?

A

Flumazenil. BDZ ANTAGONIST

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24
Q

True or false. BDZs has a high risk o drug interaction.

A

False

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25
Q

BDZs have low therapeutic index. True or false.

A

False

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26
Q

What BDZ can be given for PANIC ATTACKS?

A

Alprazolam. Short acting

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27
Q

What anxiolytic can be given for epilepsy?

A

Clonazepam. Long acting.

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28
Q

For delirium tremens?

A

Lorazepam

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29
Q

For active seizure?

A

Diazepam

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30
Q

Anxiolytics given for alcohol withdrawal.

A

Cloazepate.
Chlordiazepoxide.
Diazapam.
Oxazepam.

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31
Q

What BDZ can be used as an anesthetic?

A

Midazolam

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32
Q

For sleep disorders?

A

Flurazepam. Temazepam. Triazolam. Quezepam

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33
Q

Unwanted effects of Flumazenil.

A

Cardiac arrythmias.

Seizure

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34
Q

True or false. BDZs have fast elimination rates.

A

False. Slow, preferred due to longer CNS effects

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35
Q

Why is flumazenil a good bdz antagonist?

A

Short half life. Rapid hepatic clearance. Rapid onset of action

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36
Q

This BDZ SUBTYPE, has the greatest risk for tolerance but has the lowest risk for withdrawal.

A

Zaleplon.

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37
Q

How many weeks does it take for zaleplon to have tolerance? How about Eszopiclone? And Zolpidem?

A

5 weeks. 6months. High doses.

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38
Q

Among BDZ subtype, which has rebound insomnia?

A

Zolpidem. Zaleplon.

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39
Q

Do all BDZ subtype has rebound insomnia? If no, which one doesn’t have?

A

Eszopiclone

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40
Q

BDZ ST that can be used to induce sleep.

A

Zaleplon.

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41
Q

Which can be used to maintain sleep? What type and name of drug?

A

Eszopiclone. BDZ subtype

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42
Q

Decreases REM and latency of sleep but has a longer duration of axn.

A

Zolpidem

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43
Q

Between BDZ and its ST which has a longer duration of action.

A

BDZ

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44
Q

This anxiolytic drug affects ALL GABA A receptors.

A

BDZ

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45
Q

This affects GABA A alpha 1.

A

Zolpidem. Zaleplon.

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46
Q

This affects GABA A alpha 1 and 3

A

Eszopiclone

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47
Q

This drug affects GABA A by increasing the duration of the opening of the chloride channel.

A

Barbiturates

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48
Q

Barbiturate with half life of 4-5 days.

A

Phenobarbital. Luminal

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49
Q

Short acting barbiturate.

A

Seconal. Secobarbital

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50
Q

Half life of 18h, barbiturate

A

Secobarbital

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51
Q

Pentobarbital.

A

Intermediate acting barbiturate. 48h. 3 days

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52
Q

Nembutal

A

Intermediate acting

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53
Q

Thiopental

A

Ultra short barbiturate

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54
Q

Barbiturate used in anesthesia induction

A

Thiopental

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55
Q

Used for febrile seizure

A

Phenobarbital

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56
Q

What makes thiopental ultra short acting?

A

Very lipid soluble

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57
Q

Barbiturates cause full surgical anesthesia

A

True

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58
Q

All barbiturates has SLOW hepatic metab EXCEPT?

A

Thiopental. Rapidly acting and metabolized

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59
Q

Which barbiturate remains unchanged in urine?

A

Phenobarbital

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60
Q

Do barbiturates cause CP depression in oral doses?

A

No, only IV.

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61
Q

Phenobarbital causes enzyme induction in short term use

A

False, long term use.

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62
Q

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
A

All of the above

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63
Q

What mechanism terminates action of barbiturates, especially Thiopental.

A

Redistribution.

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64
Q

Redistribution leads to what effect?

A. Prolongation of effect
B. Termination of effect

A

B. Termination

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65
Q

Flumazenil and TCAs causes what when combined.

A

Seizure. Cardiac arryhmias

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66
Q

What classification does buspirone falls?

A

Non benzodiazepine

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67
Q

This drug is desired because of the absence of withdrawal rxn despite abrupt discontinuation.

A

Buspirone

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68
Q

Buspirone has rebound insomnia like zaleplon.

A

False.

69
Q

Buspirone has the following properties.

Anticonvulsant
Hypnotic
Muscle relaxant

A

False. It only relieves anxiety.

70
Q

Used in generalized anxiety.

A

Buspirone

71
Q

Buspirone is used in panic attacks. True or false.

A

False. Alprazolam is for panic attacks

72
Q

Rifampin is an inducer or inhibitor.

A

Inducer.

73
Q

Give inhibitors of CYP3A4.

A

KEto. NeGra.

Ketoconazole
Erythromycin
Nefazedone
Grapefruit juice

74
Q

Buspirone has an affinity for what receptor?

A

Dopamine 2

75
Q

Also known as an 5HT partial agonist

A

Non BDZ - Buspirone

76
Q

What 2 drug induces sleep by decreasing sleep latency?

A

Ramelteon.

Zaleplon

77
Q

What is the difference between zaleplon and ramelteon?

A

Zaleplon activates GABA A alpha 1 receptor. Ramelteon activates MT 1 and 2 agonist.

78
Q

Main enzyme for ramelteon metabolism

A

CYP1A2

79
Q

Ramelteon undergoes extensive first pass metabolism which has shorter half life than parent drug. Trie or false.

A

False. Longer half life than parent drug

80
Q

What sedatives undergoes extensive hepatic metabolism?

A

Ramelteon and Buspirone

81
Q

What differentiates your buspirone and ramelteon on abuse possibility?

A

Buspirone - MINIMAL

Ramelteon - ZERO

82
Q

This drug causes hyperprolactinemia.

A

Ramelteon

83
Q

Its ok to take ramelteon to patients with HPN and diabetes.

A

No worsens conditions.

84
Q

It is best to take melatonin agonist with fatty meals to fasten absorption.

A

False. Decreases absorption

85
Q

Inhibitors of CYP1A2 increases ramelteon in plasma.

A

True. Ciprofloxacin. Tacrine. Fluvoxamine. Zileuton.

86
Q

What antihistamine generation causes sedation?

A

1st

87
Q

What is the expected result when a patient is given with Doxylamine?

A

Sedation

88
Q

What drug can be used to alleviate physiologic component of anxiety?

A

Beta blokers

89
Q

This can be given for performance anxiety.

A

Beta blockers

90
Q

Antidepressant that has NO anti cholinergic effect.

A

Mirtazapine. Tetracyclics

91
Q

This causes orthostasis and dizziness. Used as an antidepressant.

A

Trazodone

92
Q

Main drug classification for anxiety.

A

BDZ

93
Q

For alcohol withdrawal.

A

CODaC

Clorazepate
Oxazepam
Diazepam
Chlordiazepoxide

94
Q

Among all sedative hypnotics which causes the highest tolerance? The lowest?

A

Barbiturates. Non-BDZ

95
Q

Among all sed-hyp which has no withdrawal sx.

A

5HT-1 partial agonist

96
Q

With continuous use of BDZ, eventually it changes hepatic drug metabolizing enzyme. True or false.

A

False

97
Q

Among BDZ what can be used for situational sleep disorder?

A

Triazolam

98
Q

Alcohol peak blood concentration

A

30mins

99
Q

Concentration of alcohol rises quickly in what body part?

A

Brain

100
Q

Which gender are more at risk for heart and liver damage in alcohol consumption?

A

Female

101
Q

Most of the alcohol taken are metabolized and excreted as urine. True or false.

A

False. 90% liver. 10% lungs and urine

102
Q

Which enzyme acts on Ethanol? Inhibits what enzyme?

A

Fomepizole. Alcohol dehydrogenase

103
Q

Disulfiram inhibits what enzyme? And what product? Producing what product?

A

Aldehyde dehydrogenase.
Acetate
Acetaldehyde

104
Q

What is the effect of having an increase muscle built?

A

More area for alcohol to deposit. Decreased blood conc

105
Q

Give some disulfiram rxns.

A

Facial flushing.
Nausea and vomiting
Dizziness
Headache

106
Q

What causes disulfiram rxn?

A

Accumulation of acetaldehyde

107
Q

What other drugs causes disulfiram like rxns

A

Metronidazole
OHA
Cephalosporins

108
Q

Alcohol has high caloric value resulting to body weight increase. True or false.

A

False. It doesnt necessarily result on increased body weight

109
Q

Alcohol activates what CYP. Give the effect.

A

CYP2E1. Transforms acetaminophen to chemicals that causes liver damage

110
Q

What endorphin blocker can be given to decrease alcohol craving?

A

Opiod antagonist. Naltrexone

111
Q

DOC for alcohol withdrawal.

A

Naltrexone

112
Q

Given to prevent seizure during alcohol withdrawal.

A

Topiramate

113
Q

This drug is given to decrease emesis in AW and craving too

A

Ondansetron

114
Q

Acamprosate MOA

A

NMDA receptor blocker

GABA A agonist

115
Q

DOC for acute methanol and ethylene glycol intox.

A

Fomepizole

116
Q

Has high affinity to alcohol dehydrogenase more than methanol

A

Ethanol

117
Q

Competitively inhibits oxidation of methanol

A

Ethanol

118
Q

Stages of ethylene glycol oxidation.

A

EDARO

Excitation
Depression 
Acidosis (metabolic)
Renal insufficiency 
Oxalate accumulate
119
Q

This must be watched out for in times of methanol poisoning.

A

Visual disturb.
Coma.
Resistant acidosis

120
Q

What electrolytes are involve in EPSP and IPSPs?

A

EPSP - Na and Ca influx

IPSP - Cl influx and K efflux

121
Q

Gold standard for diagnosing seizure

A

EEG

122
Q

Anti seizure drugs are poorly absorbed. True or false

A

False

123
Q

This drug increases the available levodopa peripherally.

A

Carbidopa

124
Q

Inhibits dopa decarboxylase

A

Carbidopa

125
Q

Gold standard for parkinsons

A

Levodopa

126
Q

Inhibits COMT

A

Entacapone

127
Q

Usually given in young patients with PD

A

Dopamine agonist

128
Q

This ergot dopamine receptor acts on D2.

A

Bromocriptine. Yow, Bro dalawa tayo

129
Q

PD drug that has low fluctuation response

A

Dopamine agonist

130
Q

Sinemet is safe to those with glaucoma.

A

False. Ulcer. Psychosis. Melanoma

131
Q

Modulates GAD TRANSPORT

A

Valproate

132
Q

Modulates GAD

A

Gabapentin

133
Q

Doc for absence seizure

A

Ethosuximide

134
Q

Among AEDs which doesnt have CNS depression

A

Ethosuximide

135
Q

Irreversibly inhits GABA transaminase

A

Vigabatrin

136
Q

Inhibits GABA re uptake

A

Tiagabine

137
Q

Acts on potassium channels that may cause toxicity. AED

A

Valproate

138
Q

What can be a sub for ethosuximide

A

Valproate

139
Q

True or false. AEDs acting on Na channels can affect both high firing and physilogic firing.

A

False

140
Q

This AED acts mainly on Na and T type Ca.

A

Zonisamide

141
Q

AEDs acting on Na channels

A

Carbamazepine. Phenytoin

142
Q

Associates with rash. AED

A

Lamotrigine

143
Q

This AED causes both renal stones and cognitive impairment.

A

Zonisamide

144
Q

Causes gingival hyperplasia and hirsutism

A

Phenytoin

145
Q

AED that causes neural tube defect and as a treatment for mania and trig neuralgia

A

Carbamazepine

146
Q

Causes ataxia and blurred vision. AED

A

Carbamazepine

BAN-Car Mania

147
Q

Cytochrome responsible for AED metab

A

CYP3A4. 2C19. 2C9

148
Q

Give the inducers of AED

A

FOXT from 3A pupunta sa CPPP

149
Q

Inhibitors of AED

A

FOX TV kasi 19 y/o na aya

150
Q

AED with aplastic anemia

A

Felbamate

151
Q

What 2 AED causes renal stones

A

Topimarate

Zonisamide

152
Q

What AED Causea cogntive slowing

A

TiTo ZoX

153
Q

Peripheral COMT

A

Entacapone

154
Q

What PD drug causes hepatotoxicity

A

Talcapone

155
Q

This drug imitates dopamine

A

Dopamine agonist

156
Q

Which ergot derivative is more potent?

A

Bromocroptine

157
Q

What dopamine agonist causes valvular problems

A

Pergolide

158
Q

This non ergot derivative has neuroprotective propery

A

Pramipexole

159
Q

Rotigotine is a skin patch dopamine agonist

A

True

160
Q

Apomorphine is given IM to rescue tx induced dyskinesia

A

False. SQ

161
Q

This MOA acts on dopamine only

A

Moa B

162
Q

Moa causes what syndrome when coombined with meperidine an TCA

A

Serotonin sydrome

163
Q

This is the more potent MOA B

A

Rasagiline

164
Q

This antagonizes adenosine receptors that are believes to inhibit d2

A

Amantidine

165
Q

Used for excessive sleepiness

A

Modafinil

166
Q

Among all PD which cannot be used alone

A

COMT

167
Q

Common ADR for COMT

A

Orange colored urine

168
Q

Livedo reticularis and peripheral edema are common in Amantidine

A

True

169
Q

Doc for febrile seizure

A

Phenobarbital

170
Q

Do migraine, neuropathic pain and dystonia

A

Gabapentin

PHARMA 2.0 (3 decks)

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