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Pain Med Board > Chapter 4. Pharmacology > Flashcards

Chapter 4. Pharmacology Flashcards

1
Q
  1. Which of the following is true regarding seizures
    as one of the multiple side effects from the use
    of opioids?
    (A) Morphine and related opioids can cause
    seizure activity when moderate doses
    are given
    (B) Seizure activity is more likely with
    meperidine, especially in the elderly
    and with renal dysfunction
    (C) Seizure activity is mediated through
    stimulation of N-methyl-D-aspartate
    (NMDA) receptors
    (D) Naloxone is very effective in treating
    seizures produced by morphine and
    related drugs including meperidine
    (E) Seizure activity is most likely related
    with the fact that opioids stimulate the
    production of γ-aminobutyric acid
    (GABA)
A
  1. (B) Extremely high doses of morphine and
    related opioids can produce seizures, presumably
    by inhibiting the release of GABA
    (at synaptic level).
    Normeperidine a metabolite of meperidine
    is prone to produce seizures and tends to
    accumulate in patients with renal dysfunction
    and in the elderly.
    Naloxone may not effectively treat seizures
    produced by meperidine.
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2
Q
  1. Which of the following is true regarding respiratory
    depression related to the use of opioids?
    (A) Opioid agonists, partial agonists, and
    agonist/antagonists produce the same
    degree of respiratory depression
    (B) Opioids produce a leftward shift of the
    CO2 response curve
    (C) Depression of respiration is produced
    by a decrease in respiratory rate, with a
    constant minute volume
    (D) Naloxone partially reverses the opioidinduced
    respiratory depression
    (E) The apneic threshold is decreased
A
  1. (E) Opioids produce a dose-dependant respiratory
    depression by acting directly on the respiratory
    centers on the brainstem. Partial agonist
    and agonist-antagonist opioids are less likely to
    cause severe respiratory depression, as are the
    selective K-agonist.
    Therapeutic doses of morphine decrease
    minute ventilation by decreasing respiratory
    rate (as oppose to tidal volume).
    Opioids depress the ventilatory response
    to carbon dioxide; the carbon dioxide–response
    curve shows a decrease slope and rightward
    shift.
    The apneic threshold is decreased and also
    the increase in ventilatory response to hypoxemia
    is blunted by opioids.
    Naloxone can effectively and fully reverse
    the respiratory depression from opioids.
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3
Q
  1. The use of which of the following opioids would
    produce the greatest incidence of delayed respiratory
    depression?
    (A) 25 μg intravenous (IV) fentanyl (bolus)
    (B) 4 mg IV morphine (bolus)
    (C) 5 μg IV sufentanil (bolus)
    (D) 8 mg epidural, preservative free
    morphine
    (E) 0.05 mg intrathecal, preservative free
    morphine
A
  1. (D) Delayed respiratory depression is likely to
    occur with larger dose of epidural opioids, particularly
    morphine which is hydrophilic and
    therefore subject to spread in the cerebrospinal
    fluid (CSF), reaching the respiratory center in
    the brainstem.
    Intrathecal doses of morphine produce only
    a uniphasic pattern of respiratory depression.
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4
Q 
144. Opioids in general reduce the sympathetic
output and produce a dose-dependant bradycardia,
EXCEPT
(A) morphine
(B) fentanyl
(C) meperidine
(D) sufentanil
(E) alfentanil
A
  1. (C) High doses of any opioid reduce sympathetic
    output allowing the parasympathetic
    output to predominate. The heart rate decreases
    by stimulation of the vagal center, especially
    with high-doses.
    Meperidine because of its similarity to
    atropine may elevate the heart rate after IV
    administration
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5
Q
  1. What is the main mechanism by which opioids
    produce analgesia?
    (A) Coupling of opioid receptors to sodium
    and potassium ion channels, therefore
    inhibiting neurotransmitter release
    (presynaptic) and inhibiting neuronal
    firing (postsynaptically)
    (B) Coupling of opioid receptor to potassium
    and calcium channels, inhibiting
    neurotransmitter release (presynaptic),
    and inhibiting neuronal firing (postsynaptically)
    (C) Coupling of opioid receptors to sodium
    and calcium channels, inhibiting
    neurotransmitter release (presynaptic),
    and inhibiting neuronal firing
    (postsynaptically)
    (D) Coupling of opioid receptors to potassium
    and calcium channels, inhibiting
    neuronal firing (presynaptically), and
    inhibiting neurotransmitter release
    (postsynaptically)
    (E) All the options are true
A
  1. (B) Opioid receptors are coupled to G proteins,
    able to affect most of the time, protein phosphorylation
    via a second messenger, thereby
    altering the conductance of potassium and calcium
    ion channels. This is believed to be the
    main mechanisms by which endogenous and
    exogenous opioids produce analgesia.
    The opening of potassium channels—the most
    well documented—will inhibit the release of neurotransmitters,
    including substance P and glutamate
    if the receptors are presynaptic. And will
    inhibit neuronal firing by hyperpolarization of the
    cell if the receptors are postsynaptic on the neurons.
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6
Q
  1. Main mechanics of spinal opioid analgesia is via
    (A) activation of presynaptic opioid receptors
    (B) activation of postsynaptic opioid
    receptors
    (C) activation of opioid receptors on the
    midbrain
    (D) activation of opioid receptors on the RVM
    (E) all of the above
A
  1. (A) The different type of opioid receptors contribute
    in different proportions to the total
    opioid receptors in the spinal cord. μ-Receptors
    constitute 70%, δ-receptors 24% and κ-receptors
    6%. The main mechanism of spinal opioid analgesia
    is through presynaptic activation of opioid
    receptors.
    Opioid receptors are synthesized in small
    diameter DRG cell bodies and transported centrally
    and peripherally. They are mainly (70%)
    located presynaptically on small diameter nociceptive
    primary afferents (C and A-δ fibers).
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7
Q 
147. Opioids act on what type of receptors targets?
(A) μ-, δ-, κ-, And ORL receptors
(B) Voltage-dependent sodium channels
(C) α2B-Adrenoreceptors
(D) NMDA receptors
(E) All of the above
A
  1. (E) Opioids produce analgesia primarily through
    interaction with μ-receptors. The activation of κ-
    and δ-receptors also causes analgesia.The ORL receptor is a member of the opioid
    receptors, although ligands do not have the same
    high affinity for this type of receptors, but effects
    of high-affinity ligands, such as antinociception,
    proprioception/hyperalgesia, allodynia and no
    effect have been reported.
    Analysis has shown that some opioid
    actions are not mediated by opioid receptors,
    morphine can inhibit voltage-dependant sodium
    (Na) current, meperidine can block voltage-
    dependant sodium (Na) channels.
    Meperidine also has agonist activity at the
    α2B-adrenoreceptor subtype.
    Methadone, meperidine, and tramadol
    inhibit serotonin and norepinephrin reuptake.
    High concentrations of opioids, including
    morphine, fentanyl, codeine, and naloxone
    directly inhibit NMDA receptor.
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8
Q 
148. Which of the following statements is true
regarding the use of oxycodone?
(A) Analgesic efficacy is not comparable
with that of morphine
(B) Typically has been used in combination
with nonopioids
(C) Not available as a long-acting
preparation
(D) Lower bioavailability than that of
morphine
(E) Consistently shows a higher induced
rate of hallucinations and itching when
compared with morphine
A
  1. (B) Oxycodone a semisynthetic derivative of
    thebaine and has analgesic efficacy comparable
    with that of morphine, with a median oxycodone
    to morphine dose ratio of 1 to 15.
    Oxycodone has been typically used in
    combination with nonopioids (acetaminophen,
    aspirin) and a long-acting preparation is available,
    which has popularized its use in cancer
    patients.
    It has a higher bioavailability than that of
    morphine (approximately 60%).
    There are not consistent observations on
    reduced rate of hallucinations and itching when
    compared with morphine.
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9
Q
  1. One important characteristic of methadone that
    has to be considered when prescribing it on an
    outpatient basis:
    (A) Usually there is a low chance for interactions
    on patients taking multiple
    medications
    (B) Withdrawal symptoms are as severe as
    with morphine
    (C) Rarely used in opioid addiction
    (D) Sedation and respiratory depression can
    outlast the analgesic action
    (E) Allows rapid titration
A
  1. (D) Methadone unlike morphine is metabolized
    through N-demethylation by the liver
    cytochrome P-450 enzyme, which activity can
    vary widely in different people.
    Methadone should be administered with
    caution in patients receiving multiple medications,
    specially antivirals and antibiotics.
    Methadone’s withdrawal symptoms tend to
    be less severe than morphine’s, this and its long
    duration of action, good oral bioavailability, and
    high potency made it the maintenance drug or
    detoxification treatment of opioid addiction.
    Methadone has biphasic elimination. Along
    β-elimination phase (ranges from 30 to 60 hours)
    producing sedation and respiratory depression
    can outlast the analgesic action which equates
    the α-elimination phase (6-8 hours).This biphasic
    pattern explains why methadone is required
    once a day for opioid maintenance therapy and
    every 4 to 8 hours for analgesia.
    Rapid titration is not possible, making this
    drug more useful for stable type of pain.
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10
Q 
150. What property of methadone makes it a good
option for opioid rotation, when tolerance
develops?
(A) Serotonin agonist
(B) α2B-Adrenoreceptor agonist
(C) μ-Agonist
(D) NMDA agonist
(E) NMDA antagonist
A
  1. (E) When tolerance to opioids, usually after
    use over long periods of time, opioid rotation,
    resting period off opioids, and addition of an
    NMDA antagonist are a number of strategies
    available.
    Opioid rotation, switching from one opioid
    to another may be helpful because of partial
    cross tolerance between opioids. Because
    methadone has NMDA receptor antagonist
    properties, makes it a good choice.
    Methadone is: μ- and δ-antagonist, NMDA
    inhibitor, inhibitor of serotonin and norepinephrine
    reuptake.
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11
Q 
151. Which one of the following is the only opioid
with prolonged activity not achieved by
controlled-released formulation?
(A) Oxycodone
(B) Fentanyl
(C) Morphine
(D) Codeine
(E) Methadone
A
  1. (E) Methadone is the only opioid with prolonged
    activity not achieved by controlledrelease
    formulation.
    Oxycodone can be formulated as controlledrelease.
    Codeine half-life is 2 to 4 hours.
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12
Q 
152. Which of the following opioids is used in the
office-based treatment of addiction?
(A) Naloxone
(B) Morphine
(C) Tramadol
(D) Buprenorphine
(E) Meperidine
A
  1. (D) Buprenorphine is a semisynthetic opioid
    with partial activity at the μ-receptor and very
    little activity at the κ- and δ-receptors.
    It has high affinity but low intrinsic activity
    at the μ-receptor and has a pharmacologic
    ceiling owing to its partial agonist activity.
    It is available in the United States to be
    used in the office-based treatment of addiction.
    It can be given for withdrawal of heroin or
    methadone, or used as a maintenance of addicts.
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13
Q 
153. Pharmacologic properties of fentanyl that make
it an ideal drug for transdermal and transmucosal
administration is
(A) high lipid solubility, high molecular
weight, and high potency
(B) low lipid solubility, high molecular
weight, and high potency
(C) low lipid solubility, low molecular
weight, and low potency
(D) high lipid solubility, low molecular
weight, and high potency
(E) high lipid solubility, low molecular
weight, and low potency
A
  1. (D) Fentanyl is a potent mu agonist, with high
    lipid solubility, low molecular weight and high
    potency, making it an ideal drug for transdermal
    and transmucosal administration.
    92% of fentanyl delivered transdermally
    reaches the circulation as unchanged fentanyl.
    Transmucosal route at the buccal and sublingual
    mucosa skips the first pass effect and
    overall bioavailability is 50%.
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14
Q
  1. Opioids can have drug interactions with
    (A) tricyclic antidepressants (TCAs)
    (B) selective serotonin reuptake inhibitor
    (SSRIs)
    (C) monoamine oxidase inhibitors (MAOIs)
    (D) metoprolol
    (E) all of the above
A
  1. (E) Opioids can have interactions with multiple
    medications, including all the medications
    mentioned above. One of the most remarkable interactions occurs if meperidine and MAOIs are combined,
    severe respiratory depression or excitation,
    arrhythmias, delusions, hyperpyrexia,
    seizures and coma can be seen
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15
Q 
155. Which of the following is a long and cumbersome
research tool for substance abuse and is
very good but not very practical in the setting
of a busy pain clinic?
(A) Screening Tool for Addiction Risk
(STAR)
(B) Severity of Opiate Dependence
Questionnaire (SODQ)
(C) Screening Instrument for Substance
Abuse Potential (SISAP)
(D) Addiction Severity Index (ASI)
(E) Prescription Drug Use Questionnaire
(PDUQ)
A
  1. (D) The Addiction Severity Index (ASI) is especially
    effective for evaluating the need for
    substance-abuse treatment. It is a 200-item,
    hour-long assessment of seven potential problem
    areas designed to be administered by a
    trained interviewer.
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16
Q
  1. An opioid specific five-question self-administered
    tool which can be completed in less than 5 minutes
    to help predict patients at high-risk for
    exhibiting aberrant opioid-related behavior is
    (A) Prescription Drug Use Questionnaire
    (PDUQ)
    (B) Opioid Risk Tool (ORT)
    (C) Screener and Opioid Assessment for
    Patients with Pain (SOAPP)
    (D) Screening Instrument for Substance
    Abuse Potential (SISAP)
    (E) Severity of Opiate Dependence
    Questionnaire (SODQ)
A
  1. (B) The Opioid Risk Tool (ORT) is a fivequestion
    self-administered assessment that can
    be completed in less than 5 minutes and used
    on a patient’s initial visit. Personal and family
    history of substance abuse; age; history of
    preadolescent sexual abuse; and the presence of
    depression, attention-deficit disorder (ADD),
    obsessive-compulsive disorder (OCD), bipolar
    disorder, and schizophrenia are assessed. The
    ORT accurately predicted which patients were
    at the highest and the lowest risk for exhibiting
    aberrant, drug-related behaviors associated
    with abuse or addiction.
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17
Q 
157. The opioid which is largely metabolized by
CYP3A4 is
(A) morphine
(B) fentanyl
(C) methadone
(D) hydromorphone
(E) oxymorphone
A
  1. (B)
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18
Q
  1. Which of the following is correct regarding
    patients who are prescribed and taking
    hydrocodone and found to have different opioid
    in their urine drug-testing results?
    (A) Norfentanyl, which is expected
    (B) Hydrocodeine, which is expected as a
    normal metabolite
    (C) Hydromorphone, which is expected as a
    normal metabolite
    (D) Hydromorphone, which is unexpected
    and patient is probably taking another
    opioid
    (E) Hydrocodeine, which is unexpected and
    patient is probably taking another
    opioid
A
  1. (C)
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19
Q
  1. An opioid-specific instrument which may be
    useful in predicting opioid misuse and is available
    as a 5-, 14-, or 24-item questionnaire as well
    as a revised version designed to be less susceptible
    to overt deception than the original version is
    (A) Prescription Drug Use Questionnaire
    (PDUQ)
    (B) Opioid Risk Tool (ORT)
    (C) Screener and Opioid Assessment for
    Patients with Pain (SOAPP)
    (D) Screening Instrument for Substance
    Abuse Potential (SISAP)
    (E) Severity of Opiate Dependence
    Questionnaire (SODQ)
A
  1. (C) Screener and Opioid Assessment for
    Patients with Pain (SOAPP) is a survey tool
    used to predict opioid abuse and is available as
    a 5-, 14-, 24-item questionnaire. Although the
    five-item questionnaire [SOAPP V LO-SF (5Q)]
    is less sensitive and specific than the longer
    version, it may suffice for use in primary care
    settings. The SOAPP-SF is scored by adding
    up the ratings of each of the five questions. The
    SQ SOAPP uses a cutoff score of 4 or above
    (of a possible 20) with a score of more than 4,
    indicating that the subject may have a potentially
    increased risk of opioid abuse.
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20
Q 
160. Aclassic example of an opioid partial agonist is
(A) naltrexone
(B) butorphanol
(C) nalbuphine
(D) buprenorphine
(E) pentazocine
A
  1. (D)
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21
Q
  1. A popular mnemonic for following relevant
    domains of outcome in pain management for
    patients on long-term opioid therapy is the socalled
    4 A’s which include all the following,
    EXCEPT
    (A) analgesia
    (B) activities of daily living
    (C) adverse events
    (D) affect
    (E) aberrant drug-taking behaviors
A
  1. (D)
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22
Q 
162. A popular pain assessment scale which is utilized
by preverbal toddler and nonverbal children
through age 7 years who may be treated
with opioids is
(A) CRIES
(B) APPT
(C) FACES
(D) FLAC C
(E) N-PASS
A
  1. (D)
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23
Q 
163. The opioid which has some component of
metabolism by CYP1A2 is
(A) morphine
(B) fentanyl
(C) methadone
(D) hydromorphone
(E) oxymorphone
A
  1. (C)
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24
Q 
164. The opioid which is a metabolite of oxycodone
via 3-0-demethylation is
(A) hydrocodone
(B) morphine
(C) codiene
(D) hydromorphone
(E) oxymorphone
A
  1. (E)
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25
Q
  1. Which of the following two opioids are inherently,
    pharmacologically, and relatively longacting?
    (A) Morphine and oxycodone
    (B) Morphine and oxymorphone
    (C) Oxycodone and fentanyl
    (D) Methadone and levorphanol
    (E) Methadone and oxymorphone
A
  1. (D)
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26
Q
  1. Oral transmucosal fentanyl citrate (OTFC) is
    applied against the buccal mucosa. The percentage
    of the total dose which is absorbed
    from the gastrointestinal (GI) tract but escapes
    hepatic and intestinal first-pass elimination is
    (A) 25%
    (B) 33%
    (C) 50%
    (D) 65%
    (E) 75%
A
  1. (A)
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27
Q 
167. OTFC is applied against the buccal mucosa.
The total apparent bioavailability is
(A) 25%
(B) 33%
(C) 50%
(D) 65%
(E) 75%
A
  1. (C)
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28
Q 
168. The fentanyl buccal tablet (FBT) utilizes an
effervescent drug delivery system and achieves
an absolute bioavailability of
(A) 25%
(B) 33%
(C) 50%
(D) 65%
(E) 75%
A
  1. (D)
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29
Q
  1. After intramuscular administration of fentanyl
    citrate, the time to onset of analgesia is roughly
    (A) 1 to 3 minutes
    (B) 7 to 15 minutes
    (C) 15 to 30 minutes
    (D) 20 to 40 minutes
    (E) 30 to 50 minutes
A
  1. (B)
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30
Q 
170. The oral bioavailability of morphine is roughly
(A) 10% to 20%
(B) 25% to 35%
(C) 35% to 45%
(D) 40% to 55%
(E) 50% to 60%
A
  1. (B)
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31
Q 
171. In humans, methadone acts as
(A) an agonist-antagonist
(B) a pure μ-agonist
(C) a μ-agonist but also with significant
actions at the δ-opioid receptor
(D) a μ-agonist but also with significant
actions at the κ-receptor
(E) a μ-, δ-, and κ-agonist
A
  1. (B)
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32
Q 
172. Atool which documents a quantitative assessment
of various opioid-adverse effects is the
(A) Pain Assessment and Documentation
Tool (PADT)
(B) Translational Analgesic Score (TAS)
(C) SAFE score
(D) Numerical Opioid Side Effect (NOSE)
(E) Severity of Opioid Dependence
Questionnaire (SODQ)
A
  1. (D)
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33
Q 
173. Which of the following is the best opioid to
administer for analgesia in a patient with
chronic kidney disease stage V?
(A) Codeine
(B) Meperidine
(C) Morphine
(D) Fentanyl
(E) Propoxyphene
A
  1. (D)
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34
Q
  1. Which of the following is the most prescribed
    opioid in the United States, which also undergoes
    O-demethylation to dihydromorphine and
    its major metabolites excreted into the urine are
    dihydrocodeine and nordihydrocodeine?
    (A) Codeine
    (B) Dihydrocodeine
    (C) Hydrocodone
    (D) Hydromorphone
    (E) Morphine
A
  1. (C)
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35
Q
  1. Which of the following is essentially responsible
    for opioid-induced respiratory depression?
    (A) μ-Receptor
    (B) δ-Receptor
    (C) κ-Receptor
    (D) σ-Receptor
    (E) ORL 1 receptor
A
  1. (A)
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36
Q
  1. Propoxyphene napsylate has a higher maximum
    daily dose than propoxyphene hydrochloride
    because
    (A) propoxyphene napsylate is less potent
    than propoxyphene hydrochloride
    (B) propoxyphene napsylate is less toxic
    than propoxyphene hydrochloride
    (C) propoxyphene napsylate is cleared
    faster than propoxyphene hydrochloride
    (D) the napsylate salt tends to be absorbed
    more slowly than the hydrochloride
    (E) the napsylate salt makes propoxyphene
    less active
A
  1. (D)
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37
Q 
177. When considering opioid rotation to methadone,
which of the following is the most appropriate
next step?
(A) Maintain the equianalgesic dose
(B) Reduce the dose by 10% to 25%
(C) Reduce the dose by 25% to 50%
(D) Reduce the dose by 50% to 75%
(E) Reduce the dose by 75% to 90%
A
  1. (E)
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38
Q 
178. When considering opioid rotation to fentanyl,
which of the following is the most appropriate
step?
(A) Maintain the equianalgesic dose
(B) Reduce the dose by 10% to 25%
(C) Reduce the dose by 25% to 50%
(D) Reduce the dose by 50% to 75%
(E) Reduce the dose by 75% to 90%
A
  1. (A)
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39
Q 
179. The equianalgesic conversion ratio of oral oxymorphone
to intravenous morphine is
(A) 1 to 1
(B) 1 to 2
(C) 1 to 3
(D) 1 to 4
(E) 1 to 5
A
  1. (A)
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40
Q
  1. By approximately what percentage is codeine
    ineffective as an analgesic in the Caucasian
    population owing to genetic polymorphisms
    in CYP2D6 (the enzyme necessary to Omethylate
    codeine to morphine)?
    (A) 2%
    (B) 5%
    (C) 10%
    (D) 25%
    (E) 33%
A
  1. (C)
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41
Q
  1. Which of the following is the correct statement
    regarding the pharmacologic properties of
    NSAIDs?
    (A) They readily cross the blood–brain
    barrier
    (B) Their chemical structure consists of aromatic
    rings connected to basic functional
    groups
    (C) They act mainly in the periphery
    (D) They have a high renal clearance
    (E) They are not metabolized by the liver
A
  1. (C) The NSAIDs are weak organic acids, consisting
    in one or two aromatic rings connected to
    an acidic functional group. They do not cross
    the blood–brain barrier, are 95% to 99% bound
    to albumin, are extensively metabolized by the
    liver and have low renal clearance (
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42
Q
  1. What are the advantages of COX-2 inhibitors
    versus NSAIDs?
    (A) Protective renal effects
    (B) Less GI side effects
    (C) Protective cardiovascular effects
    (D) Inhibits production of thromboxane A2
    (E) Increases production of lipooxygenase
A
  1. (B) Coxibs do not have any advantages in
    terms of renal effects.
    COX-2 inhibitors are associated with less
    GI toxicity than standard NSAIDs but they are
    more expensive.
    There is a possible increased risk of myocardial
    infarction (MI) and thrombotic stroke events
    associated with the continuosly long-term use of
    coxibs. Those concerns led to rofecoxib and
    valdecoxib being withdrawn from the market in
    the year 2004 and 2005, respectively.
    Regular NSAIDs inhibit the synthesis of
    TXA2 by inhibiting COX-1, which is spared
    with the use of COX-2 inhibitors.
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43
Q 
183. Which of the following best fits the pharmacologic
mechanisms of action of “traditional”
NSAIDs?
(A) Inhibition of phospholipase A2
(B) Inhibition of COX-2
(C) Inhibition of lipoxygenase
(D) Inhibition of arachidonic acid
(E) Inhibition of prostaglandin G/H
synthase enzymes
A
  1. (E) NSAIDs inhibits the prostaglandin G/H
    synthase enzymes, colloquially known as the
    COX, therefore inhibiting the synthesis of
    prostaglandin E, prostacyclin, and thromboxane.
    NSAIDs inhibit the production of not only
    COX-2 but also COX-1.
    Steroids inhibit phospholipase A2.
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44
Q
  1. The main role of prostaglandins in pain is
    (A) as important primary pain mediators
    (B) sensitization of central nociceptors
    (C) sensitization of peripheral nociceptors
    (D) facilitation of the production of pain
    mediators (ie, bradykinin, somatostatin,
    histamine)
    (E) stimulation of κ-receptors on the spinal
    cord
A
  1. (C) Prostaglandins are not important primary
    pain mediators, they do cause hyperalgesia by
    sensitizing peripheral nociceptors (to mechanical
    an chemical stimulation) to the effects of pain
    mediators, such as bradykinin, somatostatin,
    and histamine, producing hyperalgesia. They
    do so by lowering the threshold of the polymodal
    nociceptors of C fibers.
    NSAIDs act mainly in the periphery, but
    they may have a central effect. COX-2 induction
    within the spinal cord may play an important
    role in central sensitization. The acute
    antihyperalgesic action of NSAIDs has been
    shown to be mediated by the inhibition of constitutive
    spinal COX-2, which has been found
    to be upregulated in response to inflammation
    and other stressors.
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45
Q 
185. The effects of NSAIDs on the kidneys function
or renal function may include
(A) increase in renal blood flow
(B) promotion of salt and water excretion
(C) chronic interstitial nephritis
(D) increased glomerular filtration rate
(GFR)
(E) chronic papillary necrosis
A
  1. (C) In the kidney, prostaglandins help to maintain
    GFR and blood flow.
    They also contribute to the modulation of
    renin release, excretion of water, and tubular
    ion transport. In patients with normal renal
    function NSAID-induced renal dysfunction is
    extremely rare.
    Risk factors for NSAID-induced renal
    dysfunction are:
    • Prolonged and excessive NSAID use
    • Older patients
    • Chronic renal dysfunction
    • Congestive heart failure
    • Ascites
    • Hypovolemia
    • Treatment with nephrotoxic drugs (aminoglycosides
    and vancomycin)
    In these scenarios NSAIDs may decrease
    rapidly the GFR, release of renin, which can
    progress to renal failure. Sodium, water retention,
    hyperkalemia, hypertension, acute papillary
    necrosis, chronic interstitial nephritis,
    and nephrotic syndrome can also occur.
    Coxibs (COX-2 inhibitors) have similar
    renal effects and it should be closely monitored,
    as is required for conventional NSAIDs.
46
Q
  1. Platelet dysfunction secondary to the use of
    NSAIDs is a known effect, in long-term treatment
    with standard NSAIDs. What laboratory
    value is most compatible with these effects?
    (A) Prolonged prothrombin time (PT)
    (B) Prolonged partial thromboplastin time
    (PTT)
    (C) Prolonged activated clotting time (ACT)
    (D) Severely prolonged bleeding time
    (E) Below the upper limits of normal to
    mildly prolonged bleeding time
A
  1. (E) Platelets are very susceptible to COX inhibition,
    which also inhibits the endogenous procoagulant
    thromboxane. Long-term use of standard
    NSAIDs produces a consistently prolonged
    bleeding time, but the prolongation is mild and
    values tend to remain below the upper limits of
    normal.
47
Q
  1. The duration of aspirin effect is related to the
    turnover rate of COX in different target tissues,
    because aspirin
    (A) competitively inhibits the active sites of
    COX enzymes
    (B) nonirreversibly inhibits COX activity
    (C) irreversibly inhibits COX activity
    (D) noncompetitively inhibits the active
    sites of COX enzymes
    (E) acetylates COX-1
A
  1. (C) Aspirin covalently acetylates COX-1 and
    COX-2, irreversibly inhibiting COX activity. This
    makes the duration of aspirin’s effects related to
    the turnover rate of COX in different target
    tissues.
    NSAIDs competitively inhibit the active
    site of COX enzymes which relates its duration
    more directly to the time course of drug
    disposition.
48
Q
  1. The unique sensitivity of platelets to inhibition
    by low doses of aspirin (as low as 30 mg/d) is
    related to
    (A) first pass of aspirin through the liver
    (B) presystemic inhibition of platelets in the
    portal circulation
    (C) irreversible inhibition of COX
    (D) constitutively expression of COX-1 in
    platelets
    (E) good oral absorption
A
  1. (B) The unique sensitivity of platelets to inhibition
    by low doses of aspirin, as low as 30 mg/d
    is related to their presystemic inhibition in the
    portal circulation before aspirin is deacetylated
    to salicylate on first pass through the liver.
    Aspirin irreversibly inhibits COX activity,
    making the aspirin’s effect related to the
    turnover rate of COX in different target tissues.
    Enzyme turnover is most notable in platelets
    because they are anucleated with a marked limited
    capacity for protein synthesis. Therefore the
    inhibition of platelet COX-1 (COX-2 is expressed
    only in megakaryocytes) last for the lifetime of the platelet, 8 to 12 days (10 days average) after
    therapy has been stopped.
    In general NSAIDs are well absorbed orally,
    but that is not the reason for high platelet
    sensitivity to ASA.
49
Q 
189. How long before surgery NSAIDs are advised
to be stopped?
(A) 12 hours
(B) 2 to 3 days
(C) 7 days
(D) 10 days
(E) 14 days
A
  1. (B) The antiplatelet effect of NSAIDs is rapidly
    reversible, 24 hours cessation is probably sufficient,
    although 2 to 3 days cessation is advised.
    Aspirin because of its irreversible
    antiplatelet effect should be stopped 10 days
    before elective surgery.
50
Q 
190. Which of the following NSAIDs is as effective
as morphine?
(A) Ketoprofen
(B) Indomethacin
(C) Ibuprofen
(D) Ketorolac
(E) Diclofenac
A
  1. (D) Ketorolac is one of the few NSAIDs that the
    FDA approved for parenteral use. It is highly
    efficacious, with efficacy close to that of morphine
    and other opioids for simple outpatient
    procedures to major operations.
    Ketorolac’s side effects, like other NSAIDs
    include GI bleeding, other bleeding problems,
    and reversible renal dysfunction (Possibly
    related with use of high doses or failure to recognize
    its contraindications).
    Nonunion, deleterious effects in bone osteogenesis
    during bone repair are some other side
    effects, more likely to occur if ketorolac was
    administered after surgery, compared with no
    use of NSAIDs. Decreased posterior spine fusion
    rates have been demonstrated in rat models,
    with the long-term use of indomethacin, but
    even the short-term administration of NSAIDs
    may possibly significantly affect spinal fusion.
    These findings have not been confirmed in
    humans, but many surgeons prefer to avoid the
    use of NSAIDs in the postoperative period of
    bone fusion, especially in the spine. COX-2
    inhibitors can have similar effects, which is
    unlikely with short-term perioperative use in
    humans. No human studies to date document
    that coxibs have these negative effects in bone
    healing.
51
Q 
191. Rare side effect of NSAIDs is
(A) GI side effects
(B) platelet dysfunction
(C) potentially fatal hepatic necrosis
(D) renal dysfunction/failure
(E) all of the above
A
  1. (C) All are well-known and not uncommon
    side effects of NSAIDs. Borderline increases of
    one or more liver tests, may occur in up to 15%
    of patients taking NSAIDs, approximately 1%
    of patients taking NSAIDs have shown notable
    increases in alanine aminotransferase (ALT) or
    aspartate aminotransferase (AST) (X3 or more
    the upper limit of normal). These findings may
    progress, remain unchanged, or be transient
    with continuing therapy. Rare cases of severe
    hepatic reactions, including jaundice and fatal
    fulminant hepatitis, liver necrosis, and hepatic
    failure (some with fatal outcome), have been
    reported with NSAIDs.
52
Q 
192. Which of the following is (are) true regarding
oxcarbazepine?
(A) It has more adverse effects than
carbamazepine
(B) It is a sodium channel blocker
(C) Oxcarbazepine’s dose adjustment is
unnecessary for renal insufficiency
(D) Its most frequent adverse effects is
weight loss and dizziness
(E) none of the above
A
  1. (B) Oxcarbazepine [10, 11-dihydro-10-oxo-5Hdebenz
    (b, f) azepine-5-carboxanide] is an analogue
    of carbamazepine with a keto group at
    the 10 carbon position. It is roughly 50% protein
    bound in the plasma. The dose should be
    at least cut by half if the patient has significant
    renal insufficiency.
    The most frequent adverse effects experienced
    include dizziness and vertigo, weight
    gain and edema, GI symptoms, fatigue, and
    allergic-type reactions. Cross-allergy to carbamazepine
    occurs in about 25% of patients and
    may be severe.
53
Q 
193. Which of the following is a typical adverse
effect of pregabalin?
(A) Constipation
(B) Dizziness
(C) Blurred vision
(D) Dry mouth
(E) All of the above
A
  1. (E)
54
Q
  1. Which of the following is (are) false regarding
    gabapentin?
    (A) It is a first-line drug for the treatment of
    PHN and PDN (painful diabetic neuropathy)
    (B) Its dose should be reduced in renal
    insufficiency
    (C) It blocks NMDA receptors
    (D) It is thought to inhibit voltagedependent
    calcium channels
    (E) It has a chemical structure similar to
    that of GABA
A
  1. (C) A structural analogue of GABA is considered
    by many practitioners to be a first-line
    drug for treatment of PHN and PDN because
    of its tolerability and efficacy. Dose should be
    reduced in renal dysfunction. Dose increases
    are usually made every 3 to 4 days.
55
Q
  1. Which of the following is true about zonisamide?
    (A) It is a sulfonamide drug
    (B) It is a sodium channel blocker
    (C) It is 40% to 50% protein bound
    (D) It may potentially lead to renal calculi
    (E) All of the above
A
  1. (E)
56
Q
  1. Which of the following is true about antiepileptic
    drugs (AED)?
    (A) AEDs have analgesic effect in all subjects
    with neuropathic pain
    (B) If one AED is ineffective, it is not necessary
    to try another one
    (C) Newer AEDs have more side effects
    than older ones
    (D) AEDs could be combined with antidepressants
    to treat neuropathic pain
    (E) All of the above
A
  1. (D)
57
Q 
197. The antidepressant with the least anticholinergic
and least sedating effect is
(A) trazodone
(B) desipramine
(C) imipramine
(D) doxepin
(E) amitriptyline
A
  1. (B) Anticholinergic side effects are generally

very significant for TCAs.

58
Q
  1. Which of the following antidepressant agent
    selectively inhibits serotonin reuptake with
    minimal effect on norepinephrine reuptake?
    (A) Duloxetine
    (B) Protriptyline
    (C) Paroxetine
    (D) Amoxapine
    (E) Desipramine
A
  1. (C) Antidepressants which selectively inhibit
    serotonin with minimal effects on norepinephrine
    reuptake are referred to as SSRIs (eg, paroxetine).
    Protriptyline, desipramine, and amoxapine
    are secondary amine TCAs. Duloxetine inhibits
    both norepinephrine and serotonin (SNRIs).
59
Q 
199. The most common adverse effects associated
with TCA are (is)
(A) anticholinergic effects
(B) seizures
(C) arrhythmias
(D) hepatotoxicity
(E) nephrotoxicity
A
  1. (A) Side effects of antidepressants include anticholinergic
    effects, antihistaminergic effects, α1-
    aderenergic receptor bloackade, and cardiac
    effects. Individual may possess significant side
    effects in one specific area (eg, doxepin is a strong
    antihistaminergic agent). As a generalization,the most common adverse effects associated
    with TCAs are anticholinergic in nature.
60
Q 
200. The least common adverse effects associated
with TCA are (is)
(A) dry mouth
(B) seizure
(C) urinary retention
(D) blurred vision
(E) aconstipation
A
  1. (B)
61
Q 
201. Compared to TCAs, SSRIs
(A) are more effective in the treatment of
pain
(B) have more side effects
(C) have less side effects
(D) have more serious consequence of
overdosage
(E) none of the above
A
  1. (C)
62
Q 
202. Which of the following is false regarding
tramadol?
(A) It has opioid characteristics
(B) There is a dose limit of 400 mg/d
(C) It is a centrally acting analgesic
(D) No effect on norepinepherine or
serotonin
(E) Inhibits the reuptake of norepinephrine
and serotonin
A
  1. (D) Tramadol hydrochloride is a centrally
    acting analgesic which is thought to provide
    analgesia via at least two mechanisms: some
    analgesia may be derived from the relatively
    weak interaction of tramadol with the μ-opioid
    receptor. The second and major mechanism,
    which is thought to account for at least 70% of
    tramadol’ s analgesic activity, is via inhibiting
    the reuptake of norepinephrine and serotonin
63
Q 
203. The benzodiazepine which is used to treat various
neuropathic pain syndromes is
(A) diazepam
(B) midazolam
(C) clonazepam
(D) flunazepam
(E) lorazepam
A
  1. (C) Clonazepam is a benzodiazepine—which
    binds to the GABAB receptor (other benzodiazepines
    bind to the GABAA receptor) and has
    been utilized to treat various neuropathic pain
    syndrome and lower extremity muscle conditions.
64
Q
  1. Which of the following about carisoprodol is true?
    (A) Naloxone may be a useful antidote to its
    toxicity
    (B) Flumazenil may be a useful antidote to
    its toxicity
    (C) It is safe to use as a long-term treatment
    of musculoskeletal disorders
    (D) It is a GABAB receptor agonist
    (E) It has no abuse potentia
A
  1. (B) Carisoprodol may be useful for the short-term
    treatment of acute musculoskeletal disorders,
    especially in combination with acetaminophen,
    aspirin, or NSAIDs. Carisoprodol is primarily
    metabolized in the liver to several metabolites,
    including meprobamate. This metabolic conversion,
    although relatively small, has been postulated
    to be the reason that carisoprodol may have
    abuse potential. The formation of meprobamate
    from carisoprodol is by N-dealkylation via
    CYP2C19. Poor metabolizers of mephenytoin
    have a diminished ability to metabolize carisoprodol
    and therefore may be at increased risk of
    developing concentration-dependent side effects
    (eg, drowsiness, hypotension, CNS depression)
    at “usual” adult doses.
    Although the precise mechanisms of action
    of carisoprodol (as well as meprobamate) are
    uncertain, one theory is that they act as indirect
    agonists at the GABAA receptor, yielding CNS
    chloride ion channel conduction effects similar
    to benzodiazepines. Therefore, flumazenil may
    be a potentially useful antidote to carisoprodol
    toxicity.
65
Q
  1. Which of the following is true regarding
    tizanidine?
    (A) It is structurally related to clonipine
    (B) It is GABAB receptor agonist
    (C) It is GABAA receptor agonist
    (D) Its excretion occurs primarily through
    the liver
    (E) It is α2 agonist
A
  1. (E) Tizanidine is an imidazoline derivative that
    is structurally related to clonidine. Its action is
    primarily derived from agonism at the α2-
    adrenoreceptor.
    Metabolism of tizanidine occurs primarily
    in the liver through oxidative processes, and
    metabolites of the parent compound have no
    known pharmacologic activity. Excretion of
    tizanidine and its metabolites occurs primarily
    via the kidneys (53%-66%).
66
Q
  1. Which of the following is a false statement
    about ziconotide?
    (A) It is derived from conus sea snail venom
    (B) It is the synthetic form of cone snail
    peptide (conotoxin)
    (C) It is effective when given intravenously
    or orally
    (D) It is N-type calcium channel blocker
    (E) Its common side effects are dizziness,
    confusion, and headache
A
  1. (C)
67
Q
  1. Which of the following is true regarding
    capsaicin?
    (A) It is a member of the vanilloid family
    which binds to the TRPV1 receptor
    (B) It is commercially available in 0.025%
    and 0.075% concentrations
    (C) It is the active component of chili
    peppers
    (D) It depletes presynaptic substance P
    (E) All of the above
A
  1. (E)
68
Q 
208. The following are some of the side effects of
lidocaine 5% patches, EXCEPT
(A) methemoglobin
(B) edema
(C) erythema
(D) abnormal sensation
(E) exfoliation
A
  1. (A)
69
Q 
209. Calcitonin may be used as an adjuvant drug for
all the following, EXCEPT
(A) phantom limb pain
(B) sympathetically maintained pain
(C) cancer bone pain
(D) postoperative pain
(E) osteoporosis pain
A
  1. (D)
70
Q
  1. Regarding the effects produced by the different
    subtypes of opioid receptors, which of the following
    is (are) true?
    (1) κ-Receptors produce more respiratory
    depression than μ-receptors
    (2) Opioid receptors mostly affect phosphorylation
    through G protein coupling
    (3) The stimulation of μ2-receptors to produce
    analgesia without respiratory
    depression, has been supported by
    several studies
    (4) Opioid receptors act both presynaptically
    and postsynaptically
A
  1. (C) The previously proposed classification of μ-
    receptors into μ1 and μ2 subtypes, with the
    rationale that selective μ1-agonist could produce
    analgesia without the undesirable effects
    of respiratory depression has not been proven.
    Gene experiments have demonstrated that μ-
    receptors mediate all morphine activities
    including analgesia, tolerance, dependence,
    and respiratory depression.
    Opioid receptors are coupled to G proteins
    and they act mostly through phosphorylations
    via a second messenger.
    Opioids act pre- and postsynaptically.
    Presynaptically, inhibit the release of neurotransmitters
    including substance P and glutamate.
    Postsynaptically inhibit neurons by
    hyperpolarization, through the opening of
    potassium channels
71
Q
  1. The use of pure opioid agonists are preferred in
    chronic pain patients because of their
    (1) low association with addiction
    (2) superior analgesic efficacy
    (3) low potential for nausea and vomiting
    (4) easier titratable nature
A
  1. (C) When choosing between partial agonists (ie,
    buprenorphine) and mixed agonist-antagonists
    (ie, pentazocine, nalorphine) versus pure agonists,
    pure opioid agonists are preferred, especially
    in chronic pain patients, because of their
    superior efficacy and easier titratable nature
72
Q 
212. The systemic administration of opioids exerts
its analgesic effects at what level(s)?
(1) Brain cortex
(2) Brainstem and medulla
(3) Dorsal horn of the spinal cord
(4) Sensory neuron (peripheral nervous
system)
A
  1. (E) Analgesic effects of systemic administration
    of opioids result from receptor opioid
    activity at different sites, including:
  2. The sensory neuron in the peripheral nervous
    system.
  3. The dorsal horn of the spinal cord (inhibition
    of transmission of nociceptive information).
  4. The brainstem medulla (potentiates descending
    inhibitory pathways that modulate ascending
    pain signals).
  5. The cortex of the brain (decreases the perception
    and emotional response to pain).
73
Q
  1. Which of the following condition(s) increase
    the likelihood of opioid-related toxicity?
    (1) Pregnancy
    (2) Renal disease
    (3) Cardiac heart failure
    (4) Cirrhotic liver disease
A
  1. (C) The liver metabolizes opioids by dealkylation,
    glucuronidation, hydrolysis, and oxidation,
    any hepatic disease can increase the
    accumulation of toxic metabolites, that is,
    morphine-6-glucuronide, normeperidine (CNS
    toxicity), norpropoxyphene (cardiac toxicity).
    Kidneys account for 90% of opioid excretion.
    Therefore any hepatic or renal disease
    increases the likelihood of opioid-related
    toxicity.
74
Q
  1. Which of the following is (are) true concerning
    the use of epidural morphine?
    (1) A biphasic respiratory depression pattern
    can develop, with the initial phase
    within 30 minutes of the bolus dose and
    a second phase 2 to 4 hours later
    (2) Initial phase within 2 hours of the bolus
    dose and a second phase 6 to 12 hours
    later
    (3) Patients should be closely monitored for
    48 hours after the administration of
    epidural morphine
    (4) Patients should be closely monitored for
    24 hours after the administration of
    epidural morphine
A
  1. (C) The use of hydrophilic opioids like morphine
    in the epidural space produces a biphasic
    respiratory depression pattern. One portion
    of the initial bolus is absorbed systemically,
    accounting for the initial phase, which usually
    occurs within 2 hours of the bolus dose. The
    second phase occurs 6 to 12 hours later owing
    to the slow rostral spread of the remaining drug
    as it reaches the brainstem.
75
Q
  1. Opioids should be used with caution in which
    of the following scenarios?
    (1) Emphysema
    (2) Kyphoscoliosis
    (3) Chronic obstructive pulmonary disease
    (COPD)
    (4) Obstructive sleep apnea
A
  1. (E) Opioids should be used with caution in any
    situation with decrease respiratory reserve, that
    is, emphysema, obesity, scoliosis. Opioids that
    release histamine (ie, morphine) may precipitate
    bronchospasm, especially in asthma.
76
Q
  1. Indicate what part differs largely among the μ-,
    δ-, κ-, and ORL (opioid-receptor-like) receptors?
    (1) Transmembrane domains
    (2) Extracellular loops
    (3) Intracellular loops
    (4) N or C terminal tails
A
  1. (C) The opioid receptors, μ-, δ-, κ-, ORL receptors
    are highly similar, their genes have been
    cloned in many species, including humans.
    The molecular structure of these G
    protein–coupled receptors (GPCRs) comprises
    7 hydrophobic transmembrane domains interconnected
    by short loops, an intracellular
    C-terminal tail and an extracellular N-terminal
    domain.
    The transmembrane domains and intracellular
    loops have amino acid sequences that
    are 65% identical or similar, whereas the amino
    (N), carboxy (HOOC) terminal and the extracellular
    loops are very different
77
Q
  1. Opioids modify and relieve the perception of
    pain without detriment of other sensory mode
    types. While the pain is still present there is a
    dissociation of the emotional and sensory
    aspects of pain, making the patients feel more
    comfortable. Select the best reason(s) from the
    following:
    (1) Action of opioids on supraspinal structures,
    brainstem [ie, PAG (periaqueductal
    gray) the RVM (rostroventral medulla)],
    and midbrain
    (2) Action of opioids on peripheral structures
    via presynaptic receptors
    (3) Enhanced inhibitory activity on
    descending controls terminating in the
    dorsal horn of the spinal cord
    (4) Pronounced reduction in activity of OFF
    cells and decreased activity of ON cells
A
  1. (B) When noxious stimuli are produced, they
    are transmitted to higher centers through
    spinal routes arriving at the parabrachial area,
    central gray, and the amygdala. The pathways
    which project to these supraspinal sites and
    the sites themselves contribute mostly to the
    emotional aspects of pain, whereas those which
    project to the thalamus and somatosensory
    cortex produce the sensory aspects of pain.
    Opioids suppress both pathways but the
    dissociation of the emotional and sensory
    aspects of pain is most likely produced by
    brain mechanisms.
    Opioids can also prevent the supraspinal
    activation by noxious stimuli through increased
    activity in inhibitory descending controls terminating
    in the dorsal horn of the spinal cord.
    The action of opioids on peripheral structures
    does not abolish the emotional aspects of
    pain.
    There is a hypothesis describing two major
    populations of RVM output neurons, ON cells
    and OFF cells. ON cells activity coincides with
    spinal reflexes and OFF cell activity is associated
    with the suppression of those reflexes.
    Morphine produces a pronounced reduction
    in the activity of ON cells.
78
Q
  1. Opioids exert their analgesic effects through
    (1) their central action within the central
    nervous system (CNS), inhibiting directly
    the ascending transmission of painful
    stimuli from the dorsal horn at the
    spinal cord
    (2) their central action within the CNS activating
    pain control circuits descending
    from the midbrain via the RVM to the
    spinal cord dorsal horn
    (3) their peripheral actions on opioid receptors
    and the release of endogenous
    opioid-like substances
    (4) their action on the spinal cord at a
    presynaptic level only
A
  1. (A) Opioids exert their analgesic effects through
    central and peripheral mechanisms. Although it
    was believed that opioids act exclusively within
    the CNS, there are opioid receptors outside the
    CNS able to produce analgesic effects in the
    periphery. The opioid receptors are synthesized
    in the dorsal root ganglia (DRG) and transported
    toward the peripheral sensory nerve
    endings. These peripheral actions are enhanced
    under inflammatory conditions. Immune cells
    may release endogenous opioid-like substances,
    which act on opioid receptors located on the
    primary sensory neuron.
    Centrally, the opioids inhibit directly the
    ascending transmission of painful stimuli
    arising from the spinal cord (dorsal horn) and
    activate circuits that descend from the midbrain
    via the RVM to the dorsal horn.
79
Q
  1. Which of the following is (are) true regarding
    pharmacologic characteristics of opioids?
    (1) Opioids are the primary pain medication
    with ceiling effects
    (2) Opioids are the primary pain medication
    with no ceiling effects
    (3) There are sex related differences in
    opioid-mediated responsiveness
    (4) There are no sex related differences in
    opioid-mediated responsiveness
A
  1. (C) Opioids are a primary pain medication that
    has no ceiling effect , and there is no “mild”
    opioids, because they can be titrated to produce
    equianalgesic effects. Although some opioids
    have been considered “mild” because of dose-related side effects or because commercial
    preparations are combined with adjuvant
    drugs (ie, aspirin or acetaminophen) limiting its
    dosing.
    There is evidence indicating that morphine
    has greater potency but slower speed of
    onset and offset in women.
    Opioids acting in μ- and κ-receptors constrict
    the pupil by exciting the Edinger Westphal
    nucleus (parasympathetic). Long-term opioid
    use can produce tolerance to miotic effects of
    opioids.
80
Q
  1. Tramadol has some different characteristics
    when compared to some other opioids including
    (1) same side effects as morphine
    (2) risk of respiratory depression is lower at
    equianalgesic doses from that produce
    with conventional opioids
    (3) less incidence of nausea and vomiting
    (4) low abuse potential
A
  1. (C) Tramadol has a different profile from that of
    conventional opioids. It is very effective in the
    treatment of severe pain, with fewer side effects
    than morphine.
    The risk of respiratory depression is lower
    at equianalgesic doses; the risk of fatal respiratory
    depression is minimal at appropriate
    oral dosing, and limited essentially to patients
    with severe renal failure.
    Tramadol has a low abuse potential, however,
    nausea and vomiting occur at the same
    rate as with other opioids.
81
Q 
221. Morphine should be used with caution in
which situations/conditions?
(1) Short bowel syndrome
(2) Mild liver dysfunction
(3) Vomiting or severe diarrhea
(4) Renal dysfunction
A
  1. (D) Morphine is metabolized by the liver to
    morphine-6-glucuronide which is more potent
    than morphine itself and has a longer half-life,
    resulting in additional analgesia. Morphine is
    also metabolized to morphine-3-glucuronide
    which causes adverse effects and is inactive
    according to others.
    Renal dysfunction can produce accumulation
    of morphine-6-glucuronide, with subsequent
    opioid effects, including respiratory
    depression, so morphine should be used with
    care in renal dysfunction.
    Patients with liver failure can tolerate morphine
    (even in hepatic precoma), because glucuronidation
    is rarely impaired.
    Short bowel syndrome and vomiting and
    diarrhea limit the efficacy of controlled-release
    morphine, which relies in slow absorption
    from the GI tract
82
Q
  1. The transdermal fentanyl patch has differences
    versus sustained-release morphine in patients
    with cancer and chronic pain:
    (1) It can be used when the oral route can
    not be used
    (2) It is 80 times as potent as morphine
    (3) It causes less constipation than
    sustained-release morphine
    (4) Peak plasma concentration occurs in
    6 to 12 hours
A
  1. (A) Fentanyl is 80 times as potent as morphine.
    Transdermal fentanyl is extremely useful as a
    treatment in chronic pain especially in cancer
    patients. It causes less constipation than
    sustained-release morphine. Ninety-two percent
    of fentanyl delivered transdermally reaches systemic
    circulation as unchanged fentanyl.
    Peak plasma concentration after application
    is 12 to 24 hours and a residual depot
    remains in subcutaneous tissues for about
    24 hours after removal of the patch, therefore
    care needs to be taken with the use of transdermal
    system.
83
Q
  1. Which of the following is (are) correct regarding
    the use of meperidine?
    (1) The use of meperidine should be limited
    to 1 to 2 days in the management of
    acute pain
    (2) Normeperidine is a neurotoxic metabolite
    of meperidine
    (3) Meperidine should be avoided in the
    management of chronic pain
    (4) The use of meperidine is recommended
    in elderly patients
A
  1. (A) Normeperidine is a neurotoxic metabolite
    of meperidine; its accumulation is more likely
    in patients with poor renal function, especially
    in the elderly. The use of meperidine should be
    limited to 1 to 2 days for acute pain and should
    be avoided in chronic pain management.
84
Q
  1. Which of the following is (are) true regarding
    opioids distribution and biotransformation
    (metabolism)?
    (1) Fentanyl is highly protein bound
    (2) Fentanyl distributes to fat tissue and
    redistributes from there into the systemic
    circulation
    (3) Opioids are metabolized by the liver,
    CNS, kidney, lungs, and placenta
    (4) Opioid distribution is independent of
    protein binding and lipophilicity
A
  1. (A) Opioid distribution is a function of lipophilicity
    and plasma protein binding. Fentanyl is both
    lipophilic and highly protein bound. Fentanyl
    also distributes to fat tissue and redistributes
    slowly from there into the systemic circulation.
    The opioids are mainly metabolized in the
    liver and to a minor extent in CNS, kidneys,
    lung, and placenta.
85
Q
  1. What is (are) the neuroendocrine effects produced
    by opioids?
    (1) Hypogonadism
    (2) Hypothyroidism
    (3) Decreased cortisol levels
    (4) Decreased pituitary release of prolactin
A
  1. (B) Investigations have showed that endogenous
    and exogenous opioids can bind to opioid receptors
    primarily in the hypothalamus but also in the
    pituitary gland and testes, decreasing the release
    of gonadotropin-releasing hormone (GnRH),
    luteinizing hormone–follicle-stimulating hormone
    (LH–FSH), and testosterone-testicular
    interstitial fluid, respectively. Clinically this will
    manifest as hypogonadism, including: loss of
    libido, impotence, infertility (males and females),
    depression, anxiety, loss of muscle strength,
    fatigue, amenorrhea, irregular menses, galactorrhea,
    osteoporosis, and fractures.
    Opioids have also been found to decrease
    cortisol levels and cortisol responses, but they
    do not modify thyroid function.
    Opioids also have been shown to increase
    pituitary release of prolactin in preclinical studies
    and one study also documented decreased
    growth hormone (GH), without clear clinical
    significance.
86
Q 
226. Which of the following drugs may show interactions
with NSAIDs/COX-2 inhibitors?
(1) Angiotensin-converting enzyme (ACE)
inhibitors
(2) Furosemide
(3) Warfarin
(4) Lithium
A
  1. (E) NSAIDs may diminish the antihyperptensive
    effects of ACE inhibitors (ACEIs) and the natriuretic effect of furosemide and thiazides in
    some patients.
    Anticoagulant therapy with warfarin
    should be monitored, especially in the first
    few days of changing therapy, because all the
    currently available COX-2 inhibitors may
    increase serum warfarin levels.
    Lithium levels may also increase with
    celecoxib, valdecoxib, and rofecoxib.
87
Q 
227. Which of the following is (are) contraindicated
in patients allergic to sulfonamides?
(1) Rofecoxib
(2) Valdecoxib
(3) Meloxicam
(4) Celecoxib
A
  1. (C) All sulfonamides can be regarded to one of
    the two main biochemical categories, arylamines
    or nonarylamines. The sulfonamide
    allergicity is thought to be related to the formation
    of hydroxylamine a metabolite of the
    nonarylamine group. Celecoxib and valdecoxib
    belong to the former group and are contraindicated
    in patients allergic to sulfonamides.
88
Q
  1. Anti-inflammatory agent(s) which may possess
    advantages when GI side effects are a concern
    include
    (1) ibuprofen
    (2) nabumetone
    (3) diclofenac
    (4) coxibs
A
  1. (C) Nabumetone (nonacidic prodrug metabolized
    to a structural analogue of naproxen) is
    minimally toxic to the GI tract, and it is the
    choice when GI side effects are a special concern.
    Coxibs are also a good choice if there is
    any history of GI symptoms. Coxibs are associated
    with less GI toxicity than standard
    NSAIDs, since they do not inhibit the constitutive
    COX-1 and therefore the production of the
    cytoprotective PGI2 in the stomach mucosa.
89
Q
  1. Which of the following is (are) true for coxibs
    versus NSAIDs?
    (1) Coxibs are associated with less GI side
    effects
    (2) Coxibs have similar renal effects
    (3) Coxibs are not associated with platelet
    dysfunction
    (4) Coxibs are associated with increased
    incidence of nonunion and delayed
    bone healing
A
  1. (A) Coxibs show less GI side effects, and have
    similar renal effects to those of standard
    NSAIDs.
    COX-2 is not present in platetelets, and
    up-to-date under most conditions, coxibs are
    not associated with platelet dysfunction.
    There is no documentation in humans that
    the coxibs impairs bone remodeling and delay
    fracture healing.
90
Q
  1. Which of the following NSAIDs have higher
    potency (either analgesic or anti-inflammatory
    or both) compared to ASA?
    (1) Diflunisal
    (2) Indomethacin
    (3) Ketorolac
    (4) Diclofenac
A
  1. (E) The potency of NSAIDs in general is similar
    or equipotent to ASA, except for diflunisal,
    indomethacin, ketorolac, and diclofenac.
    Diflunisal is a difluorophenyl derivative
    of salicylic acid, more potent than aspirin in
    anti-inflammatory tests in animals. It is used
    primarily as analgesic in osteoarthritis and musculoskeletal
    sprains, where is 3 to 4 times more
    potent than ASA. It also produces fewer and less
    intense GI and antiplatelet effects than ASA.
    Indomethacin is 10 to 40 times more
    potent inhibitor of COX than ASA, but intolerance
    limits its dosing to short-term. It also may
    have a direct, COX-independent vasoconstrictor
    effect. Some studies have suggested the
    possibility of increased risk of MI and stroke,
    but controlled trials have not been performed.
    Ketorolac is a potent analgesic, poor antiinflammatory.
    Has been used as a short term
    alternative (less than 5 days) to opioids, for
    moderate to severe pain.
    Diclofenac is more potent than ASA; its
    potency against COX-2 is substantially greater
    than that of indomethacin, naproxen, or several
    other NSAIDs.
    Naproxen is more potent in vitro.
91
Q 
231. Scenarios in which the adjunct use of NSAIDs
can be beneficial in postoperative pain:
(1) Use of opioids
(2) No history of induced-opioid side
effects
(3) Preexisting ventilatory compromise
(4) History of GI bleeding
A
  1. (B) Amultimodal approach (the combination of
    different, appropriate pain treatments) seems to
    be the best approach in terms of synergy and
    reducing the side effects of each.
    The opioid sparing effects of NSAIDs use
    in postoperative pain, has been confirmed in
    multiple controlled trials. This can be of particular
    benefit when the opioids side effects
    are especially undesirable, including preexisting
    ventilatory compromise, strong history of
    opioid induced side effects and the very
    young
92
Q 
232. Options that can be offered to patients with
increased risk of GI toxicity:
(1) Diclofenac with enteric coat
(2) NSAIDs combined with GI prophylaxis
(3) NSAIDs combined with antacids
(4) Coxibs
A
  1. (C) Coxibs are a good choice in patients with a
    history of GI symptoms or sensitivity to NSAIDs,
    because they are associated with less GI side
    effects than standard NSAIDs. Although they
    are more expensive and they carry the concern
    of increase cardiovascular risk (increased
    thrombotic events: MI, stroke), with continuous
    and prolonged used.
    Standard NSAIDs combined with GI prophylaxis
    seems to be equally effective in terms of
    efficacy and freedom from GI toxicity. The GI
    prophylaxis can consist of: parietal cell inhibitors
    (acid inhibitors, ie, omeprazole), prostaglandin
    analogues (misoprostol), and H blockers (ie, ranitidine,
    cimetidine).
    Diclofenac is available in combination with
    misoprostol, retaining the efficacy of diclofenac
    while reducing the frequency of GI toxicity; it is
    cost effective relative to coxibs despite the cost
    of added misoprostol. Diclofenac with enteric coat does not offer a marked less GI toxicity.
93
Q 
233. Which of the following is (are) NSAID’s role in
cancer?
(1) Synergistic effect of NSAIDs and
opioids
(2) Bone and soft tissue pain relief
(3) Ability to reduce the side effects of
opioids
(4) Visceral pain relief
A
  1. (E) The combination of opioid/nonopioid (ie,
    NSAIDs) for mild to moderate cancer pain is
    synergistic and has the ability to reduce the
    side effects of each drug.
    NSAIDs in advanced cancer, are particularly
    useful for bone pain (distension of the
    periosteum by metastases, for soft tissue pain
    (distension or compression of tissues), and
    for visceral pain (irritation of the pleura or
    peritoneum).
    ASA and other salicylates are contraindicated
    in children and young adults (younger than
    20 years) with fever associated with viral illness,
    owing to the association with Reye syndrome.
    Acetaminophen: nonacidic, crosses the
    blood–brain barrier, acts mainly in the CNS,
    peripheral, and anti inflammatory effects are
    weak
94
Q
  1. Anti-inflammatory agent(s) which do not interfere
    with the cardioprotective effects of “lowdose”
    aspirin include
    (1) naproxen
    (2) ibuprofen
    (3) ketorolac
    (4) celecoxib
A
  1. (D) Unlike ibuprofen, naproxen, and ketorolac,
    celecoxib does not interfere with the inhibition
    of platelet COX-1 activity and function
    by aspirin.
95
Q
  1. Which of the following is (are) true regarding
    carbamazepine?
    (1) It blocks voltage-dependent sodium
    channels
    (2) Bicuculline antagonizes its antinociceptive
    effect
    (3) It was first used for trigeminal neuralgia
    (4) All of the above
A
  1. (E)
96
Q 
236. Pregabalin is Food and Drug Administration
(FDA) approved for
(1) diabetic neuropathy
(2) postherpetic neuralgia (PHN)
(3) fibromyalgia
(4) none of the above
A
  1. (A) The drug was approved by the European
    Union in 2004. Pregabalin received US FDA
    approval for use in treating epilepsy, diabetic
    neuropathy pain, and pain in June 2005, and
    appeared on the US market in 2005. In June
    2007 the FDA approved it as a treatment for
    fibromyalgia. It was the first drug to be
    approved for this indication and remained the
    only one, until duloxetine gained FDA approval
    for the treatment of fibromyalgia in 2008.
97
Q
  1. Which of the following is (are) true regarding
    gabapentin?
    (1) It has chemical a structure similar to
    GABA
    (2) It acts directly at GABA-binding site in
    the CNS
    (3) It inhibits voltage-dependent calcium
    channels
    (4) It is the drug of choice for fibromyalgia
A
  1. (B) GBP has a chemical structure similar to
    GABA. It seems not to act directly at the GABAbinding
    site in the CNS, however. The mechanism
    of action is still unclear. It may enhance the
    release or activity of GABA and seems to inhibit
    voltage-dependent sodium channels
98
Q
  1. Which of the following is (are) true regarding
    clonazepam?
    (1) It is a benzodiazepine
    (2) It is effective as anxiolytic and musclerelaxing
    agent
    (3) It may be useful for phantom limb pain
    (4) It has short half-life
A
  1. (A) Case report evidence suggests that clonazepam
    may have a useful effect in treatment
    of the shooting pain associated with phantom
    limb pain. Somnolence is a predominant side
    effect, and with this drug’s long half-life, daytime
    sedation may complicate use. As it
    belongs to the benzodiazepine group of drugs,
    anxiolysis and muscle relaxation may also be
    produced by its use, and this combination of
    properties may, in some patients, be useful.
99
Q
  1. Which of the following is true about
    lamotrigine?
    (1) It is an anticonvulsive agent
    (2) It is an NSAID
    (3) A rapid titration may result in skin rash
    (4) More than 300 mg/d is always needed
    for analgesia
A
  1. (B) Case report evidence suggests that lamotrigine
    may reduce the symptoms of complex
    regional pain syndrome (type 1), with the sudomotor
    changes seen in this condition being alleviated
    along with pain and allodynia. Perhaps
    the major side effect limiting rapid titration to
    a therapeutic dose is skin rash.
    Higher doses may be used, but, if no effect
    is observed at 300 mg/d, further increases are
    unlikely to produce analgesia. In view of the
    relatively long half-life of lamotrigine, oncedaily
    dosing may be appropriate.
100
Q 
240. The antidepressant(s) which is (are) tertiary
amine(s) TCA:
(1) Imipramine
(2) Nortriptyline
(3) Doxepin
(4) Desipramine
A 
240. (B) The TCAs can be divided into tertiary
amines and their demethylated secondary
amine derivatives.
Tertiary amine TCAs ("ACID T ")
Amitriptyline
Imipramine
Tripramine
Clomipramine
Doxapin
Secondary amine TCAs ("PAND")
Nortriptyline
Desipramine
Protriptyline
Amoxapine
101
Q
  1. Which of the following is true about the analgesic
    properties of TCAs?
    (1) The analgesic effects of TCA are independent
    of their effects on clinical
    depression
    (2) Onset of analgesia with TCA ranges
    from 3 to 7 days
    (3) Analgesia tends to occur at lower doses
    and plasma levels than that needed for
    antidepressant effects
    (4) TCA’s analgesic property is superior to
    that of SSRI’s
A
  1. (E)
102
Q
  1. Which of the following is (are) true about
    TCAs?
    (1) They interact significantly with the
    opioid and benzodiazepine
    (2) They do not have potential for addiction
    (3) They block calcium channels
    (4) They can cause insomnia, restlessness
    and dry mouth
A
  1. (C)
103
Q 
243. Symptoms of TCA toxicity includes which of
the following?
(1) Hyperthermia
(2) Tachycardia
(3) Seizures
(4) Hypertension
A
  1. (A)
104
Q
  1. When prescribing antidepressants for pain
    (1) explain to the patient that you are primarily
    treating the pain not depression
    (2) explain to the patient that it will not
    work immediately
    (3) explain to the patient that it may help
    sleep
    (4) none of the above
A
  1. (A)
105
Q
  1. Which of the following is (are) true regarding
    acetaminophen?
    (1) It is an aniline derivative
    (2) Induced analgesia is centrally mediated
    (3) It has peripheral mechanism of action
    (4) It is a drug of choice for relieving mild
    to moderate musculoskeletal pain
A
  1. (E)
106
Q 
246. Which of the following is (are) true regarding
acetaminophen toxicity?
(1) The liver gets the major insult
(2) The heart gets the major insult
(3) N-acetylcysteine is beneficial for
treatment
(4) Adrenergic agonists are beneficial for
treatment
A
  1. (B) The liver receives the major insult from acetaminophen
    toxicity, with the predominant lesion being acute centrilobular hepatic necrosis. It is
    suggested the use of the glutathione precursor
    of N-acetylcysteine for the treatment of acetaminophen
    intoxication in efforts to maintain
    hepatic reduced glutathione concentrations
    and adrenergic agonists may lower hepatic glutathione
    significantly.
107
Q 
247. Which of the following is (are) true about
baclofen?
(1) It is good for muscle rigidity and
spasticity
(2) It is used for neuropathic pain
(3) It is GABAB receptor agonist
(4) It is GABAA receptor agonist
A
  1. (A) Baclofen is the ρ-chlorophenyl derivative of
    GABA. Baclofen is a GABAB agonist that has
    been used for muscle spasms and spasticity, neuropathic
    pain, and so on. Baclofen may enhance
    the effectiveness of antiepileptic drugs in certain
    neuropathic pain states. Side effects include sedation,
    weakness, and confusion. Abrupt cessation
    may cause a withdrawal syndrome, such as hallucinations,
    anxiety, tachycardia, or seizures.
108
Q
  1. Which of the following is (are) true regarding
    botulinum toxin A?
    (1) The analgesic mechanism of action is
    well known
    (2) It can be administered intrathecally
    (3) Botox, Myobloc, and Dysport are available
    in the United States
    (4) Its effect lasts for about 3 to 6 months
A
  1. (D) The two clinically available botulinum toxins
    in the United States are botulinum toxin type A
    and botulinum toxin type B. A different formulation
    of botulinum toxin Ais used in Europe as
    well as a version used in China but are currently
    not available in the United States. Effects seem to
    last for roughly 3 to 6 months after injection, at
    which point a repeat injection generally reproduces
    the effect.
    Although it is generally accepted that botulinum
    toxins may lead to diminished pain in
    patients with painful muscle spasms or cervical
    dystonia by diminishing muscle tone, it
    is also felt that botulinum toxin may itself
    possess analgesic properties. The mechanism
    of botulinum toxin–induced analgesia are
    unknown.
    The most evident mechanism of botulinum
    toxin-induced analgesia is via reduction
    of muscle spasm by cholinergic chemodenervation
    at motor end plates and by inhibition of
    gamma motor endings in muscle spindles.
    Future uses of botulinum toxins for analgesia
    may lead to redesign toxins for intrathecal
    use.
109
Q
  1. Which of the following is false regarding
    cyclobezaprine?
    (1) It is structurally similar to anticonvulsive
    agents
    (2) It has cholinergic side effects
    (3) It does not require dose adjustment for
    elderly patients
    (4) It can produce sinus tachycardia
A
  1. (A) Cyclobenzaprine is structurally similar to
    TCAs and, as such, demonstrates significant
    anticholinergic side effects. It exhibits a sideeffect
    profile similar to that of the TCAs, including
    lethargy and agitation, although it usually
    does not appear to produce significant dysrhythmias
    beyond sinus tachycardia. Elderly
    patients seem to tolerate cyclobenzaprine less
    well and may develop hallucinations as well as
    significant anticholinergic side effects, such as
    sedation. The use of significant lower dosing
    schedules in elderly patients may be prudent.
110
Q 
250. Which of the following is (are) false about lidocaine
5% topical patch?
(1) Treatment for postherpetic neuralgia
(2) It may not use more than 1 patch per
day
(3) It is used 12 hours ON and 12 hours
OFF
(4) High plasma levels are normally
achieved through the skin
A
  1. (C)
111
Q
  1. Steroids produce analgesia by
    (1) anti-inflammatory effects
    (2) suppressing ectopic discharge from
    injured nerves
    (3) reducing edema
    (4) blocking sodium channels
A
  1. (A)

Pain Med Board (35 decks)

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