Neuropharmacology Flashcards
1
Q
Which of the following has an active metabolite? A. Clonazepam B. Carbamazepine C. Phenobarbital D. Lorazepam
A
Carbamazepine
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
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
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
5
Q
Which of the following has dose dependent oral bioavailability? A. Lamotrigine B. Topiramate C. Ethosuximide D. Gabapentin
A
Gabapentin
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
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
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
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
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
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
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
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
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
15
Q
Which of the following anti-epileptic drug has the least protein binding? A. Lamotrigine B. Phenytoin C. Topiramate D. Gabapentin
A
Gabapentin
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
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
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
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
20
Q
What is the mode of action of PERAMPANEL?
A
blocks the action of glutamate at AMPA receptors
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
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)
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
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
25
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
Pramipexole
26
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
Tolcapone
27
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
Haloperidol
28
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
amantadine
29
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
requires enzymatic conversion
30
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
apomorphine
31
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
- 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
32
What is the enzyme that catalyzes the rate limiting step for the synthesis of dopamine?
tyrosine hydroxylase
converts tyrosine to dopamine
33
Levodopa’s absorption in the gut is greatest in the __________
proximal small intestine
34
Mode of action of CARBAMAZEPINE 4
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
35
Mode of action of CLOBAZAM 3
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
36
Mode of action of CLONAZEPAM 3
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
37
Mode of action of LAMOTRIGINE 2
- use-dependent blocker of v-sensitive Na channels
| - Inhibits release of glutamate
38
Mode of OXCARBAZEPINE 4
1 use-dependent blocker of v-sensitive Na channels
2 Increases K conductance
3 Modulates high-v activated Ca channels
4 reduces glutamate release
39
Mode of PHENOBARBITAL
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
40
Mode of action of PHENYTOIN 3
1 use-dependent blocker of v-sensitive Na channels
2 Regulates calmodulin and second messenger systems
3 Inhibits Ca channels and Ca sequestration
41
Mode of action of PREGABALIN 1
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
42
Mode of action of VALPROATE 4
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
43
Mode of action of TOPIRAMATE (6)
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
44
Anti-Epileptic Drugs that act PRIMARILY on Na Channels?
| Other AEDs that may also act on Na channels?
Phenytoin
Carbamazepine
Oxcarbazepine
Lamotrigine
other drugs: Valproate, Zonisamide, Gabapentin, Felbamate, Topiramate
45
Anti-Epileptic Drugs that act PRIMARILY on Ca Channels?
| Other AEDs that may also act on Ca channels?
Ethosuximide
other drugs: Phenytoin, Valproate, Phenobarbital, Lamotrigine, Carbamazepine, Oxcarbazepine, Zonisamide, Gabapentin, Felbamate, Topiramate, ?Levetiracetam
46
Anti-Epileptic Drugs that may act on K channels?
Oxcarbazepine
| Levetiracetam
47
Hepatic enzyme INDUCING AEDs
```
Phenytoin
Phenobarbital
Carbamazepine
Oxcarbazepie
Felbamate
```
48
Hepatic enzyme INHIBITOR AED/s
Valproate
49
AEDs that may cause hepatitis
Valproate
| Lamotrigie
50
AEDs that may cause APLASTIC ANEMIA
Felbamate
51
AEDs that may cause thrombocytopenia
Valproate
52
AEDs that may cause agranulocytosis
Carbamazepine
53
AEDs that may cause panceratitis
Valproate
54
AEDs that may cause affect insulin release and effects
Phenytoin
| Topiramate
55
AEDs that may cause GINGIVAL HYPERPLASIA
Phenytoin
56
AEDs is associated with SLE?
Phenytoin
57
AEDs associated with Dupuytren's Contracture
Phenobarbital
58
AEDs that may cause NEPHROLITHIASIS
Topiramate
| Zonisamide
59
AEDs that may cause HYPONATREMIA
Carbamazepine
| Oxcarbazepine
60
AEDs that may cause RASH
Phenytoin
Phenobarbital
Carbamazepine
61
AEDs that may cause SJS
Carbamazepine
| all other AEDs
62
AEDs that may cause ALOPECIA
Valproate
63
AEDs that may cause HIRSUTISM
Phenytoin
64
Teratogenic AEDs
Valproate
Carbamazepine
Phenytoin
Phenobarbital
65
AEDs that may cause PCOS
Valproate
66
AEDs that may cause reduced libido
Phenobarbital
67
AEDs that may cause OSTEOPOROSIS
enzyme inducers
Phenytoin, Phenobarbital, Carbamazepine
Oxcarbazepie, Felbamate
68
AEDs that may cause failure of OCPs
enzyme inducers
Phenytoin, Phenobarbital, Carbamazepine
Oxcarbazepie, Felbamate
69
mTOR inhibitors
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
Aminoglycoside effect on the nervous system
vestibular damage
71
Furosemide effect on the nervous system
cochlear damage
72
Nitrofurantoin, INH, Hydralazine effect on the nervous system
neuropathy
73
Steroid conversion
Dexamethasone
Prednisone
Methylprednisl e
74
Main complication of temezolamide
Thrombocytopenia
| Leukopenia
75
True or False: Lamotrigine is contraindicated for myoclonic jerks
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
metabolite of clonazepam that retains some of it pharmacologic activity
7-aminoclonazepam
77
Pharmacologically active metabolite of diazepam
N-desmethyldiazepam
78
Pharmacologically active metabolite of carbamazepine
carbamazepine-10,11-epoxide
79
Pharmacologically active metabolite of oxcarbazepine
dihydro 5H dibenzapine 5 carboxamide
80
Inhibitor of de novo pathway of purine nucleotide synthesis, impairing B and T lymphocyte proliferation
Mycophenolate
81
Genetically engineered chimeric murine-human monoclonal antibody against CD20 antigen on the surfaces of normal and malignant B cells
Rituximab
82
Reduces expression of cytokine genes required for T cell activation and proliferation
Cyclosporine
83
Interferes with DNA synthesis, alkylates and crosslinks DNA, interferes with cell proliferation B > T cells
Cyclophosphamide
84
Decrease purine synthesis, interferes with DNA and RNA synthesis; also inhibits lymphocyte proliferation, interferes with antibody and cytokine production
Azathioprine
85
maximum dose of pyridostigmine
600mg/day
| 120mg/dose with a frequency of 4 to 6x a day
86
half life of pyridostigmine
| duration of action?
T1/2 1-2hours
| duration of action 6-8 hours
87
SSRI with the wors profile in regard to sexual side effects
Sertraline
88
potent SSRI without active metabolite, short half life, can cause discontinuation syndrome
Paroxetine
89
SSRI longest half life
fluoxetine
90
SSRI most selective for 5HT
citalopram
91
Antipsychotics. Low potency agent, reserved for refractory schizophrenia due to risk of blood dyscrasia/ agranulocytosis potential
Clozapine
92
Antipsychotics. More potent at 5HT2 than D2 receptor sites, but also with significant α 2 antagonism, hence improves mood and increase motor activity
Risperidone
93
Antipsychotics. It is a 5HT and NE reuptake inhibitor, may have antidepressant effect.
Ziprasidone
94
Antipsychotics. Similar neurochemically to clozapine but with less risk of agranulocytosis but has significant risk of weight gain, altered glucose metabolism
Olanzapine
95
Antipsychotics. Weak D2 effect but potent α 1 and histamine blockade, with significant sedative effects
Quetiapine
96
Antipsychotics. Partial agonist at D2 and 5 HT1A hence may increase anxiety, nausea and insomnia
Aripiprazole
97
Bromocriptine primarily acts on which dopamine receptors
D2 D3 ++
D4 D5 +
98
Ropinirole primarily acts on which dopamine receptors
D3 ++++
D2 ++
D4 +
99
Pramipexole primarily acts on which dopamine receptors
D3 ++++
D2 ++
D4 ++
100
Rotigotine primarily acts on which dopamine receptors
D1 D2 D3
101
Lisuride primarily acts on which dopamine receptors
D2 ++
| D1 +
102
Pergolide primarily acts on which dopamine receptors
D3 +++
D2 ++
D1 D5 +
103
target site for the treatment of tremor-predominant PD
Ventral intermediate nucleus of the thalamus
104
mechanism of action of Tacrine is
butyrylcholinesterase inhibitor
105
mechanism of action of Donepezil
AChE inhibitor
106
mechanism of action of Rivastigmine
AChE and butyrylcholinesterase inhibitor
107
mechanism of action of Galantamine
AChE antagonist and allosteric nicotinic modulator
108
mechanism of action of Memantine
noncompetitive NMDA receptor antagonist
109
Cladribine
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
an oral medication to improve walking in patients with MS
Dalfampridine
111
renally eliminated AEDs
Gabapentin
Pregabalin
Levetiracetem
112
hepatic / renally eliminated AEDs
Topiramate
Zonisamide
Tigabine
113
mode of action of Felbamate 2
1 Inhibits glycine-enhanced NMDA-induced intracellular calcium currents
2 Potentiates GABA responses
114
mode of action of Tigabine
Selectively blocks reuptake of GABA by presynaptic and glial GABA transporter-1 (GAT-1
