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Phar 752
Exam #4, 10 December 2002
Page 1
Name (Last , First)
Student ID #
This test consists of 50 questions worth a total of 100 points. There are a total of 14
pages. Check that your test is complete. Record your answers for questions on a
scantron sheet and turn in BOTH this printed exam and the scantron.
An anxiety disorder that is characterized by excessive anxiety and worry
most of the time is classified as: (2 pts)
Generalized anxiety disorder
Agoraphobia
Panic disorder
Obsessive-compulsive disorder (OCD)
Post-traumatic stress disorder
The amygdala is a central component of an interconnected network of brain
structures which is involved in the experience and expression of emotion.
The name of this network is: (2 pts)
A. The ascending arousal system
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The limbic system
C. The thalamocortical system
D. The serotonergic system
E. The corticotropin system
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Phar 752
Exam #4 , 10 December 2002
Page 2
Name (Last, First)
Student ID #
Refer to Figure 1 to answer this question. Choose the correct match: (2 pts)
1 = antidepressant
It 2 = antidepressant
C. 3 = bus pirone
D. 1 = benzodiazepine
E. 2 = benzodiazepine
Figure 1
High
Time (weeks)
Low
-C
Choose the statement that best describes buspirone: (2 pts)
A. It is a good antidepressant
B. It is effective in treating panic disorder
It is effective in treating generalized anxiety disorder
D. It makes anxiety worse in the short term
E. It causes dependence
Which statement best describes the sedative mechanism of action of
dexmedetomidine? (2 pts)
A. Inhibition of the histamnergic component of the ascending arousal system.
Inhibition of the noradrenergic component of the ascending arousal system.
C. Inhibition of the GABAergic component of the ascending arousal system.
D. Inhibition of the cholinergic component of the ascending arousal system.
B. Inhibition of the serotonergic component of the ascending arousal system.
Phar 752
Exam #4, 10 December 2002
Page 4
Name (Last , First)
Student il #
'
cr
G4(:", €). Drug A has anxiolytic , memory impairment (amnesic) and hypnotic (sleep- inducing) effects , while Drug B has an Which one of the following is most likely? (2 pts) A. Drug A is a parial agonist at the benzodiazepine receptor, while Drug B is a full agonist at the benzodiazepine receptor. B. Drug A is a full agonist at the benzodiazepine receptor , while Drug B is an antagonist at the benzodiazepine receptor. C. Drug A is a full agonist at the benzodiazepine receptor , while Drug B is an inverse agonist at the benzodiazepine receptor. D. Drug A is an antagonist at the benzodiazepine receptor , while Drug B is a parial agonist at the benzodiazepine receptor. Drug A is a full agonist at the benzodiazepine receptor , while Drug B is a parial agonist at the benzodiazepine receptor. 11. Choose the correct statement about the etiology of epilepsy (2 pts) A. Always caused by an infection. B. Always caused by a brain tumor. C. Never caused by head trauma. D. Cause always unknown. Q Cause often unknown. ir12. Choose the correct statement about the treatment of epilepsy (2 pts) .. Epilepsy can be cured with available drugs. -I Epilepsy can sometimes be cured with neurosurgery. (Q Epilepsy can always be controlled with available drugs. .. If left untreated , epilepsy usually goes away spontaneously. Epilepsy can be cured with a brain transplant. 13. A seizure caused by abnormal neuronal activity confined to a local area of the brain and resulting in impairment or loss of consciousness would most likely be classified as: (2 pts) A. A typical generalized absence seizure. ## (! A complex parial seizure. C. A simple parial seizure. D. An atypical generalized absence seizure. E. A generalized tonic-clonic seizure. Phar 752 Exam # , 10 December 2002 Page 5 Name (Last, First) Student ID # What is the mechanism of action of ethosuximide? (2 pts) A: Blocks voltage-dependent Na+ channels. B. Increases GABA release in the synapse. C. Increases the activity of GABA receptors. (Q Blocks T - type Ca 2+ channels. Blocks L-type Ca 2+ channels. Which mechanism of drug action is likely to be the most effective for suppressing tonic-clonic seizures with least possible effect on normal brain function? (2 pts) A. Block of voltage-dependent Na+ channels that is independent of action potential frequency. B. Block of voltage-dependent Na + channels that increases with action potential frequency. C. Block of T -type Ca 2+ channels that is independent of action potential frequency. Block of T -type Ca 2+ channels that increases with action potential frequency. ,. Block of GABA receptor cr channels that increases with action potential frequency. 16. Choose the correct statement: (2 pts) A. Parial seizures are always preceded by an increase in interictal activity. B. Parial seizures are always preceded by a decrease in interictal activity. Parial seizures are sometimes preceded by an increase in interictal activity. D. Parial seizures are never preceded by an increase in interictal activity. E. Parial seizures are never preceded by a decrease in interictal activity. 17. J: Which one of these drugs inhibits GABA aminotransferase? (2 pts) A. Phenytoin B. carbamazepine C. clonazepam (a benzodiazepine) Valproate E. Ethosuximide Phar 752 Exam # , 10 December 2002 Page 7 Name (Last, First) Student ID # t22. Radioactive deoxyglucose can be injected into the bloodstream and used to produce an image of glucose metabolism in the li ving brain. This method imaging is known as: (2 pts) A. Positron Emission Tomography (PET) (! Magnetic Resonance Imaging (MRI) 23. Which of the following is considered an excitatory amino acid neurotransmitter: (2 pts) ## A. GABA ( Glutamate C. Tryptophan D. Dopamine E. Tyrosine 24. Which of the following receptors belongs in the family of ligand- gated ion channels: (2 pts) A. DI ## Dopamne receptor .. GABA receptor y 5- receptor D. mu type opioid receptor em None of the above 25. Which of the following brain regions is primarly responsible for maintaining posture, a sense of balance and coordinating movement: (2 pts) A. Hippocampus B. Cerebral cortex C. Limbic system D. Locus Ceruleus Cerebellum 26. Catecholamne-containing neurons have a distinct appearance characterized by the presence of: (2 pts) A. Proopiomelanocortin B. nodes of Ranvier C. Vesicles ## Varcosities ## E. GABA transamnase Phar 752 Exam #4, 10 December 2002 Page 8 27. Name (Last , First) Student ID # Parkinson s Disease is characterized by a loss of dopaminergic projection neurons arsing (cell bodies are located) in which brain region: (2 pts) A. Ventral Tegmental Area B. Nucleus Accumbens Substantia Nigra D. Arcuate nucleus E. Nucleus Basilis -8B. 29. Ingestion of shellish contamnated with domoic acid has resulted in severe memory deficit in humans. A likely explanation for this is that domoic acid is: (2 pts) A glutamate receptor agonist A glutamate receptor antagonist A glycine receptor antagonist A GABA receptor agonist A GABA receptor antagonist The action of serotonin (5-HT) at neuronal synapses is termnated by: ( pts) Tiyptophan hydroxylase Monoamne oxidase Reuptake via the plasma membrane serotonin transporter A. I only B. il only e. I and II only ( II and III only , II and III 30. D. - Activation of which of the following ligand- gated ion channels results in hyperpolarzation of the postsynaptic neuron: (2 pts) NMA-type glutamate receptor Strychnine-sensitive glycine receptor GABA receptor A. I only B. III only e. I and II only (I II and III only E. I, II and III Phar 752 Exam # , 10 December 2002 Page 10 34. Name (Last , First) Student ID # What metabolite, which also has antianxiety action on its own , is shared by diazepam, chlordiazepoxide, and clorazepate? (2 pts) A. ' Temoxepam Oxazepam e. Demoxepam D. Alprazolam ' N-desmethylchlordiazepoxide Which of the following anxiolytics can be directly glucuronidated eliminating the need for metabolism involving cytochrome P 450 and preventing the buildup of active metabolites? (2 pts) A. A and D CI A and E e. Band C D. D and E E. B andE 35. 36. 37. Quazepam Diazepam Flurazepam clonazepam Lorazepam The following structure represents a prodrug of the benzodiazepines. What metabolic steps are necessary to provide the active ## drg? ( pts) Decarboxylation and 3- hydroxylation demethylation and decarboxylation Ester hydrolysis and decarboxylation Deesterification and N- demethylation Ester hydrolysis and N- demethylation \ \ H3q -C-o-fV "' C b- - Azole class benzodiazepines have reduced half- lives compared to many classical benzodiazepines because they are efficiently hydroxylated and then glucuronidated. What are the two most common sites of hydroxylation in the azole class of benzodiazepines? (2 pts) (C - N ### --N Phar 752 Exam # , 10 December 2002 Page 11 38. 39. Name (Last , First) Student ID # The toxicity associated with one of the anti epileptic drugs has been proposed to be due to a minor compound that arises from multiple metabolic steps. Which AED is metabolized to this potentially toxic aldehyde derivative which can alkylate proteins? (2 pts) carbamazepine Vi gab atrin Felbamate Topiramate Ethosuximide Which antiepileptic agent is a prodrug that is activated by phosphatase metabolism? (2 pts) Trimethadione. ## (J Fosphenytoin. ## "J Lamotrigine. Oxcarbazepine ## -E Primidone 40. Which of the following is consistent with the known structure-activity relationships of barbiturates used as sedatives? (2 pts) ,k' For sedative action , 5 disubstituion is necessary. Thiobarbiturates have increased solubility and decreases duration of action relatively to traditional barbiturates, but provide quicker onset. The pKa s of the barbiturates are all between 4. , which allows the anionic form to predominate in vivo for maximal interaction with the GABA receptor. Branching at the C5 chain or unsaturation in the chain increases activity, decreases duration , and decreases toxicity. The potency increases as the total number of carbons attached at C5 increases up to a total of 7 -9 carbons, then tails off. 41. Of the following antiepileptic drugs , which one is not known to induce or inhibit metabolic enzymes? (2 pts) "k Phenobarbital. Levetiracetam. Valproate Carbamazepine Phenytoin Phar 752 Exam #4, 10 December 2002 Page 13 Name (Last, First) Student ID # 45. What type of metabolic conversion is involved in the formation of the active metabolite of oxcarbazepine? (2 pts) '" Epoxidation of a double bond Reduction of a ketone to an alcohol Hydroxylation Ester hydrolysis Dealkylation Valproic acid acts as an AED by a varety of mechanisms and therefore is useful to treat several types of seizures , but its use is limited by drg interactions and toxicity. As with some of the other AEDs , metabolism is implicated in the toxicity of valproate. Which statement regarding valproate metabolism is accurate? (2 pts) A. The carboxylate of valproate is reduced to an aldehyde which can alkyl ate proteins, leading to liver toxicity. B. Valproate is oxidized to a 4- pentenoic acid metabolite that is believed to contribute to toxicity. e. Valproate is epoxidized to a toxic intermediate. D. Hydroxylation of the sidechain of valproate produces a toxic metabolite. E. O-Dealkylation of valproate releases a toxic aldehyde intermediate. 47. Which statement most accurately reflects the action of primidone as an antiepileptic drug? (2 pts) A. Primidone is a prodrg which is converted to phenobarbital , which has antiepileptic action. B. Primidone is mildly effective as an AED , but its only active metabolite phenobarbital contributes the bulk of activity. e. Primidone is an effective AED which has no active metabolites. (Q Primidone and its two active metabolites , phenobarbital and . phenylethylmalonamde, all contribute to anti seizure action. E. Primidone is a unique prodrug ester of valproic acid and lorazepam which releases the two active AEDs upon ester hydrolysis. Phar 752 Exam #4, 10 December 2002 Page 14 Name (Last , First) Student ID # 48. Which AED was designed as a more lipophilic derivative of nipecotic acid , a known inhibitor of GABA reuptake? (2 pts) A. Topiramate B. Zonisamide. C. Vigabatrin. C Tiagabine. E. Gabapentin. 49. Based on the structure-activity relationships of the classical antiepileptic drgs which of the following structures represents a drug that is effective against absence seizures? (2 pts) CH );o CH2 C A CH2 C A 50. An inducer of UDP-glucuronsyltransferase wil significantly decrease the half-life of which AED? (2 pts) A. Phenobarbital (g Lamotrigine e. Zonisamde D. Vigabatrin E. Phenytoin
