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Res Quizzes > Neuropharmacology > Flashcards

Neuropharmacology Flashcards

1
Q 
Which of the following has an active metabolite?
A.	Clonazepam
B.	Carbamazepine 
C.	Phenobarbital
D.	Lorazepam
A

Carbamazepine

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2
Q 
Which of the following anti-epileptic drugs is significantly excreted unchanged in the urine?
A.	Ethosuximide
B.	Phenytoin
C.	Carbamazepine
D.	Diazepam
A

Ethosuximide

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3
Q 
A patient with hepatic failure develops several episodes of generalized seizures. Based on pharmacokinetics, which of the following would best be suited for this patient?
A.	Ethosuximide
B.	Valproic acid
C.	Topiramate 
D.	Carbamazepine
A

Topiramate

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4
Q 
Which of the following anti-epileptic drugs auto-induces its own metabolism after several weeks of use?
A.	Phenytoin
B.	Lamotrigine
C.	Topiramate
D.	Gabapentin
A

Lamotrigine

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5
Q 
Which of the following has dose dependent oral bioavailability?
A.	Lamotrigine
B.	Topiramate
C.	Ethosuximide
D.	Gabapentin
A

Gabapentin

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6
Q 
Drugs used in the treatment of Parkinsons disease are primarily mediated by which of the following dopamine receptors?
	A. D1
	B. D2
	C. D3
	D. D4
A

D2

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7
Q 
Which of the following conditions would respond to treatment with metoprolol?
	A. Physiologic tremor
	B. Essential tremor
	C. Tourettes syndrome
	D. Wilsons disease
A

Essential tremor

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8
Q 
Which of the following  is used to prevent the peripheral conversion of levodopa to dopamine increasing its bioavailability?
	A. Levodopa
	B. Carbidopa
	C. Pramipexole
	D. Bromocriptine
A

Carbidopa

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9
Q 
Which of the following drugs used for the treatment of Parkinsons disease is a selective, reversible, peripherally acting COMT inhibitor?
	A. Tolcapone
	B. Entacapone
	C. Selegiline
	D. Pramipexole
A

Entacapone

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10
Q 
Which of the following drugs used in the treatment of Parkinsons disease is a non-ergot dopamine agonist with the same efficacy as bromocriptine?
	A. Tolcapone
	B. Carbidopa
	C. Pergolide
	D. Ropirinole
A

Ropirinole

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11
Q 
Which of the following  is used to prevent the peripheral conversion of levodopa to dopamine increasing its bioavailability?
	A. Levodopa
	B. Benzserazide
	C. Pramipexole
	D. Bromocriptine
A

Benzserazide

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12
Q 
Which of the following drugs used for the treatment of Parkinsons disease is a selective, reversible, peripherally and centrally acting COMT inhibitor?
	A. Tolcapone 
	B. Entacapone
	C. Selegiline
	D. Pramipexole
A

Tolcapone

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13
Q 
Which of the following antiepileptic drugs follows zero order kinetics within its therapeutic range?
	A. Vigabatrin
	B. Lamotrigine
	C. Valproic acid
	D. Phenytoin
A

Phenytoin

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14
Q

Which of the following drugs would increase the half life of levodopa?

a. carbidopa
b. benzeraside
c. entacapone
d. all of the above

A

all of the above

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15
Q 
Which of the following anti-epileptic drug has the least protein binding?
A. Lamotrigine
B. Phenytoin
C. Topiramate
D. Gabapentin
A

Gabapentin

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16
Q 
Which of the following anti-epileptic drugs is significantly excreted unchanged in the urine?
A. Phenytoin
B. Levetiracetam
C. Lorazepam
D. Diazepam
A

Levetiracetam

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17
Q 
A patient with renal failure develops several episodes of generalized seizures. Based on pharmacokinetics, which of the following would best be suited for this patient?
A. Topiramate
B. Valproic acid
C. Phenobarbital
D. Gabapentin
A

Valproic acid

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18
Q 
In case of overdose, alkalinization of urine increases excretion of unchanged drug in which of the following antiepileptic drugs?
A.	Clonazepam
B.	Carbamazepine 
C.	Phenobarbital
D.	Lorazepam
A

Phenobarbital

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19
Q

What is the mode of action of LEVETIRACETAM?

A
  • does not share with other antiepileptic drugs any of their three main mechanisms, such as sodium channel blockade, inhibition of calcium currents, or increase in GABAergic inhibitory responses
  • can oppose the activity of negative modulators
    of GABA- and glycine-gated currents, and can partially inhibit N-type calcium currents
  • Binds to synaptic vesicle protein SV2A, which is involved in synaptic vesicle exocytosis
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20
Q

What is the mode of action of PERAMPANEL?

A

blocks the action of glutamate at AMPA receptors

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21
Q

What is the mode of action of LACOSAMIDE?

A
  • enhancing slow inactivation of voltage-gated Na channels resulting in stabilization of hyperexcitable neuronal membranes
  • Binds to collapsing response mediator protein-2 (CRMP-2), a phosphoprotein which is primarily expressed in the nervous system and is involved in neuronal differentiation and control of axonal outgrowth – suggested to mediate a putative neuroprotective effect and to prevent neurodegenerative
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22
Q

What is the mode of action of VIGABATRIN?

A
  • GABA analog
  • Binds irreversibly & covalently to GABA-transaminase causing permanent inactivation
  • Inactivation of GABA-transaminase (which is responsible for the breakdown of GABA in neurons & glia, results in an increase in brain (synaptic) GABA)
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23
Q 
Treatment of Parkinsons disease with dopaminergic agents may potentially cause hallucinations due to the effects of these drugs on which of the following pathways?
	A. Spinothalamic
	B. Mesolimbic and mesocortical
	C. Nigrostriatal
	D. Tuberohypophyseal
A

Mesolimbic and mesocortical

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24
Q 
Which of the following drugs used in the treatment of Parkinsons disease is a non-ergot dopamine agonist with the same efficacy as bromocriptine?
	A. Tolcapone
	B. Carbidopa
	C. Pergolide
	D. Pramipexole
A

Pramipexole

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25
Q

A patient with liver disease also has parkinsons disease. Which of the following dopamine agonists would probably be the safest to use?

a. pergolide
b. pramipexole
c. bromocriptine
d. ropinirole

A

Pramipexole

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26
Q

Which of the following is a COMT inhibitor, can increase and prolonged the bioavailability of exogenously administered levodopa but has been reported to cause fulminant liver failure?

a. Rasagiline
b. Selegiline
c. Entacapone
d. Tolcapone

A

Tolcapone

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27
Q

Which of the following drugs can be used for the treatment of Huntingtons disease and Tourettes syndrome?

a. Haloperidol
b. Reserpine
c. Clonidine
d. Benztropine

A

Haloperidol

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28
Q

Which of the following is an anti-viral agent that has been proven to be effective in the treatment of Parkinsons disease?

a. bromocriptine
b. pramipexole
c. pergolide
d. amantadine

A

amantadine

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29
Q

The following are advantages of dopamine agonists used for Parkinsons disease EXCEPT:

a. requires enzymatic conversion
b. no potentially toxic metabolites
c. dopamine agonists can be stored and released by degenerating neurons
d. substances with highly specific actions on receptor subtypes can be used or developed

A

requires enzymatic conversion

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30
Q

Which of the following drug used for parkinsons disease is given subcutaneously for temporary relief of off-periods of akinesia?

a. bromocriptine
b. pramipexole
c. apomorphine
d. amantadine

A

apomorphine

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31
Q

What is the mechanism of action of zonisamide?
A. enhances potassium channel opening
B. blocks GABA reuptake
C. inhibits GABA transaminase
D. blocks ligand gated calcium channels
E. blocks high frequency firing of voltage gated sodium channels

A
  • activity-dependent Na channels blocker (partial)
  • T-type Ca channels blocker
  • Inhibition of K-mediated glutamate release
  • Increase in extracellular levels of dopamine and serotonin
  • Up-regulation of excitatory amino-acid carrier-1 (EAAC-1)
  • Down-regulation of the expression of GABA transporter-1 (GAT-1)
  • low potency carbonic anhydrase inhibition
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32
Q

What is the enzyme that catalyzes the rate limiting step for the synthesis of dopamine?

A

tyrosine hydroxylase

converts tyrosine to dopamine

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33
Q

Levodopa’s absorption in the gut is greatest in the __________

A

proximal small intestine

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34
Q

Mode of action of CARBAMAZEPINE 4

A

1 Acts as a use-dependent blocker of voltage-sensitive Na-channels
2 Inhibits L-type Ca channels
3 Inhibits release of glutamate
4 moderate anticholinergic action

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35
Q

Mode of action of CLOBAZAM 3

A

just like CLONAZEPAM

  • Binds to benzodiazepine receptors at the GABA-A ligand-gated chloride channel complex
  • Enhances the inhibitory effects of GABA
  • Boosts Cl conductance through GABA-regulated channels
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36
Q

Mode of action of CLONAZEPAM 3

A

just like CLOZAPAM

  • Binds to benzodiazepine receptors at the GABAA ligand-gated chloride channel complex
  • Enhances the inhibitory effects of GABA
  • Boosts chloride conductance through GABA-regulated channels
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37
Q

Mode of action of LAMOTRIGINE 2

A
  • use-dependent blocker of v-sensitive Na channels

- Inhibits release of glutamate

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38
Q

Mode of OXCARBAZEPINE 4

A

1 use-dependent blocker of v-sensitive Na channels
2 Increases K conductance
3 Modulates high-v activated Ca channels
4 reduces glutamate release

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39
Q

Mode of PHENOBARBITAL

A

1 GABA inhibition enhancement : Enhances postsynaptic GABAA receptor-mediated Cl currents by prolonging the opening of the chloride ionophore
2 reduction of Ca-dependent action potentials

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40
Q

Mode of action of PHENYTOIN 3

A

1 use-dependent blocker of v-sensitive Na channels
2 Regulates calmodulin and second messenger systems
3 Inhibits Ca channels and Ca sequestration

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41
Q

Mode of action of PREGABALIN 1

A

1 closes N and P/Q presynaptic Ca-channels bybinding to the α2-δ subunit of v-gated Ca-channels

  • Although structurally related to GABA, it does not directly act on GABA or its receptors
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42
Q

Mode of action of VALPROATE 4

A

1 GABA: increases GABA by inhibition of GABAtransaminase, succinic semialdehyde dehydrogenase, or through an increase in glutamic acid decarboxylase
2 Na and K: Can reduce sustained repetitive high-frequency firing by blocking v-sensitive Na channels or by activating Ca-dependent K conductance
3 aspartate: Decreases brain levels of the excitatory amino acid aspartate
4 glutamate: Decreases the expression of hippocampal glutamate transporter-1

None of the identified actions are widely accepted as the predominant relevant mechanism

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43
Q

Mode of action of TOPIRAMATE (6)

A

1 GABA: Enhances GABA-mediated inhibition
2 Na: Inhibits v-dependent Na channels
3 K: Enhances K channel conduction
4 Ca: Inhibition of L-type high v-activated Ca channels
5 Glutamate: Decreases glutamate-mediated excitatory neurotransmission
6 Carbonic anhydrase: Low potency inhibition
7 Inhibits AMPA receptors

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44
Q

Anti-Epileptic Drugs that act PRIMARILY on Na Channels?

Other AEDs that may also act on Na channels?

A

Phenytoin
Carbamazepine
Oxcarbazepine
Lamotrigine

other drugs: Valproate, Zonisamide, Gabapentin, Felbamate, Topiramate

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45
Q

Anti-Epileptic Drugs that act PRIMARILY on Ca Channels?

Other AEDs that may also act on Ca channels?

A

Ethosuximide

other drugs: Phenytoin, Valproate, Phenobarbital, Lamotrigine, Carbamazepine, Oxcarbazepine, Zonisamide, Gabapentin, Felbamate, Topiramate, ?Levetiracetam

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46
Q

Anti-Epileptic Drugs that may act on K channels?

A

Oxcarbazepine

Levetiracetam

47
Q

Hepatic enzyme INDUCING AEDs

A 
Phenytoin
Phenobarbital
Carbamazepine
Oxcarbazepie
Felbamate
48
Q

Hepatic enzyme INHIBITOR AED/s

49
Q

AEDs that may cause hepatitis

A

Valproate

Lamotrigie

50
Q

AEDs that may cause APLASTIC ANEMIA

51
Q

AEDs that may cause thrombocytopenia

52
Q

AEDs that may cause agranulocytosis

A

Carbamazepine

53
Q

AEDs that may cause panceratitis

54
Q

AEDs that may cause affect insulin release and effects

A

Phenytoin

Topiramate

55
Q

AEDs that may cause GINGIVAL HYPERPLASIA

56
Q

AEDs is associated with SLE?

57
Q

AEDs associated with Dupuytren’s Contracture

A

Phenobarbital

58
Q

AEDs that may cause NEPHROLITHIASIS

A

Topiramate

Zonisamide

59
Q

AEDs that may cause HYPONATREMIA

A

Carbamazepine

Oxcarbazepine

60
Q

AEDs that may cause RASH

A

Phenytoin
Phenobarbital
Carbamazepine

61
Q

AEDs that may cause SJS

A

Carbamazepine

all other AEDs

62
Q

AEDs that may cause ALOPECIA

63
Q

AEDs that may cause HIRSUTISM

64
Q

Teratogenic AEDs

A

Valproate

Carbamazepine
Phenytoin
Phenobarbital

65
Q

AEDs that may cause PCOS

66
Q

AEDs that may cause reduced libido

A

Phenobarbital

67
Q

AEDs that may cause OSTEOPOROSIS

A

enzyme inducers
Phenytoin, Phenobarbital, Carbamazepine
Oxcarbazepie, Felbamate

68
Q

AEDs that may cause failure of OCPs

A

enzyme inducers
Phenytoin, Phenobarbital, Carbamazepine
Oxcarbazepie, Felbamate

69
Q

mTOR inhibitors

A

sirolimus - causes slight regression of bodily angiolipomas in TUBEROUS SCLEROSIS

everolimus - useful in suppressing the status epilepticus associated with TUBEROUS SCLEROSIS

rapamycin - shrink SEGAs

70
Q

Aminoglycoside effect on the nervous system

A

vestibular damage

71
Q

Furosemide effect on the nervous system

A

cochlear damage

72
Q

Nitrofurantoin, INH, Hydralazine effect on the nervous system

A

neuropathy

73
Q

Steroid conversion

A

Dexamethasone
Prednisone
Methylprednisl e

74
Q

Main complication of temezolamide

A

Thrombocytopenia

Leukopenia

75
Q

True or False: Lamotrigine is contraindicated for myoclonic jerks

A

True.
Lamotrigine is contraindicated for myoclonic jerks and syndromes with predominantly myoclonic jerks (e.g., juvenile myoclonic epilepsy, Dravet syndrome, and progressive myoclonic epilepsy)

76
Q

metabolite of clonazepam that retains some of it pharmacologic activity

A

7-aminoclonazepam

77
Q

Pharmacologically active metabolite of diazepam

A

N-desmethyldiazepam

78
Q

Pharmacologically active metabolite of carbamazepine

A

carbamazepine-10,11-epoxide

79
Q

Pharmacologically active metabolite of oxcarbazepine

A

dihydro 5H dibenzapine 5 carboxamide

80
Q

Inhibitor of de novo pathway of purine nucleotide synthesis, impairing B and T lymphocyte proliferation

A

Mycophenolate

81
Q

Genetically engineered chimeric murine-human monoclonal antibody against CD20 antigen on the surfaces of normal and malignant B cells

82
Q

Reduces expression of cytokine genes required for T cell activation and proliferation

A

Cyclosporine

83
Q

Interferes with DNA synthesis, alkylates and crosslinks DNA, interferes with cell proliferation B > T cells

A

Cyclophosphamide

84
Q

Decrease purine synthesis, interferes with DNA and RNA synthesis; also inhibits lymphocyte proliferation, interferes with antibody and cytokine production

A

Azathioprine

85
Q

maximum dose of pyridostigmine

A

600mg/day

120mg/dose with a frequency of 4 to 6x a day

86
Q

half life of pyridostigmine

duration of action?

A

T1/2 1-2hours

duration of action 6-8 hours

87
Q

SSRI with the wors profile in regard to sexual side effects

A

Sertraline

88
Q

potent SSRI without active metabolite, short half life, can cause discontinuation syndrome

A

Paroxetine

89
Q

SSRI longest half life

A

fluoxetine

90
Q

SSRI most selective for 5HT

A

citalopram

91
Q

Antipsychotics. Low potency agent, reserved for refractory schizophrenia due to risk of blood dyscrasia/ agranulocytosis potential

92
Q

Antipsychotics. More potent at 5HT2 than D2 receptor sites, but also with significant α 2 antagonism, hence improves mood and increase motor activity

A

Risperidone

93
Q

Antipsychotics. It is a 5HT and NE reuptake inhibitor, may have antidepressant effect.

A

Ziprasidone

94
Q

Antipsychotics. Similar neurochemically to clozapine but with less risk of agranulocytosis but has significant risk of weight gain, altered glucose metabolism

A

Olanzapine

95
Q

Antipsychotics. Weak D2 effect but potent α 1 and histamine blockade, with significant sedative effects

A

Quetiapine

96
Q

Antipsychotics. Partial agonist at D2 and 5 HT1A hence may increase anxiety, nausea and insomnia

A

Aripiprazole

97
Q

Bromocriptine primarily acts on which dopamine receptors

A

D2 D3 ++

D4 D5 +

98
Q

Ropinirole primarily acts on which dopamine receptors

A

D3 ++++
D2 ++
D4 +

99
Q

Pramipexole primarily acts on which dopamine receptors

A

D3 ++++
D2 ++
D4 ++

100
Q

Rotigotine primarily acts on which dopamine receptors

101
Q

Lisuride primarily acts on which dopamine receptors

A

D2 ++

D1 +

102
Q

Pergolide primarily acts on which dopamine receptors

A

D3 +++
D2 ++
D1 D5 +

103
Q

target site for the treatment of tremor-predominant PD

A

Ventral intermediate nucleus of the thalamus

104
Q

mechanism of action of Tacrine is

A

butyrylcholinesterase inhibitor

105
Q

mechanism of action of Donepezil

A

AChE inhibitor

106
Q

mechanism of action of Rivastigmine

A

AChE and butyrylcholinesterase inhibitor

107
Q

mechanism of action of Galantamine

A

AChE antagonist and allosteric nicotinic modulator

108
Q

mechanism of action of Memantine

A

noncompetitive NMDA receptor antagonist

109
Q

Cladribine

A

a purine nucleoside analogue that interferes with the behavior and proliferation of certain wbcs, particularly lymphocytes, which are involved in the pathological process of MS

110
Q

an oral medication to improve walking in patients with MS

A

Dalfampridine

111
Q

renally eliminated AEDs

A

Gabapentin
Pregabalin
Levetiracetem

112
Q

hepatic / renally eliminated AEDs

A

Topiramate
Zonisamide
Tigabine

113
Q

mode of action of Felbamate 2

A

1 Inhibits glycine-enhanced NMDA-induced intracellular calcium currents
2 Potentiates GABA responses

114
Q

mode of action of Tigabine

A

Selectively blocks reuptake of GABA by presynaptic and glial GABA transporter-1 (GAT-1

Res Quizzes (18 decks)

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