NSAIDS + Opioids Flashcards

1
Q

A 55-year-old woman is having a colonoscopy. Aside from other medications for sedation, it is likely she will receive which of the following analgesics?

A
Methadone

B
Meperidine

C
Buprenorphine

D
Fentanyl

E
Pentazocine

A

D
Fentanyl

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2
Q

A 42-year-old man with chronic pain is brought to the emergency room because of over-sedation and respiratory depression while using fentanyl patches. He is given intravenous naloxone. He is not given oral naloxone because naloxone

A
is not absorbed from the GI tract.

B
undergoes first-pass metabolism in the liver.

C
is metabolized to an inactive metabolite in the GI lining.

D
is excreted unchanged in the urine.

E
is destroyed by stomach acid.

A

B
undergoes first-pass metabolism in the liver.

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3
Q

48-year-old man is being treated with a long-acting opiate for pain associated with terminal cancer. He is also prescribed a transmucosal fentanyl formulation (lollipop) for “breakthrough” pain. The transmucosal formulation is an effective analgesic because it

A
avoids first pass metabolism of fentanyl.

B
avoids nausea and vomiting that is associated with the systemic use of fentanyl.

C
delivers fentanyl directly to opiate receptors in the mouth.

D
avoids constipation.

E
avoids respiratory depression.

A

A
avoids first pass metabolism of fentanyl.

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4
Q

A 50-year-old woman with back pain is administered an opiate agonist. After 2 weeks of therapy, she notices that she needs to increase the dose to get the same analgesic effect. She is experiencing

A
physical dependence.

B
addiction.

C
tolerance.

D
withdrawal.

E
drug-seeking behavior.

A

C
tolerance.

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5
Q

A 43-year-old man with postsurgical pain is placed on an intravenous patient-controlled analgesia pump with morphine as the analgesic. This form of analgesic administration is preferred to oral administration because morphine

A
is not absorbed orally.

B
administered orally is rapidly eliminated in the urine.

C
administered orally does not penetrate the brain.

D
administered orally causes more severe constipation.

E
administered parenterally bypasses first-pass metabolism.

A

E
administered parenterally bypasses first-pass metabolism.

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6
Q

The morphine metabolite that may be responsible for most of morphine’s analgesic activity is

A
desmethylmorphine.

B
morphine-6-glucuronide.

C
morphine sulfate.

D
N-acetylmorphine.

E
hydroxymorphine.

A

B
morphine-6-glucuronide.

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7
Q

A 20-year-old man is given codeine to relieve the pain of a sprained ankle. After two days the man returns to his doctor saying that the codeine is not effective. A likely cause is due to

A
poor absorption.

B
rapid urinary excretion.

C
poor metabolism.

D
high protein binding.

E
poor brain penetration.

A

C
poor metabolism.

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8
Q

A 53-year-old man is requesting meperidine for his chronic back pain. His physician is reluctant to use meperidine for the treatment of chronic pain because of

A
metabolite toxicity.

B
poor oral absorption.

C
increased addiction potential.

D
patient noncompliance.

E
likelihood that meperidine will be diverted for sale on the street.

A

A
metabolite toxicity.

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9
Q

A 32-year-old woman has been taking an oxycodone-acetaminophen product for chronic arthritic pain. On a follow-up appointment her serum aminotransferases are elevated and she is slightly jaundiced. She admits to increasing the dose of the oxycodone combination product over the past several weeks. The most likely cause of her liver injury is

A
oxycodone.

B
hepatitis A.

C
hepatitis C.

D
arthritis.

E
acetaminophen.

A

E
acetaminophen.

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10
Q

Which NSAID has the least anti-inflammatory efficacy?

A
Aspirin

B
Acetaminophen

C
Ibuprofen

D
Naproxen

E
Celecoxib

A

B
Acetaminophen

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11
Q

Which NSAID permanently inactivates TxA2 synthesis by platelets?

A
Aspirin

B
Acetaminophen

C
Ibuprofen

D
Naproxen

E
Celecoxib

A

A
Aspirin

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12
Q

What is the primary mechanism of action of allopurinol in treating gout?

A
It is an analgesic agent.

B
It is an anti-inflammatory agent.

C
It blocks inflammatory responses to urate crystals.

D
It inhibits urate formation.

E
It augments urate excretion.

A

D
It inhibits urate formation

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13
Q

The cardiovascular risk associated with celecoxib results from

A
inhibition of prostaglandin production in the gastric epithelium.

B
inhibition of platelet thromboxane production.

C
effects on myocardial ion channels.

D
inhibition of prostaglandin in the kidney.

E
enhanced prostacyclin production by vascular endothelium.

A

D
inhibition of prostaglandin in the kidney

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14
Q

Diclofenac has a t1/2 in plasma of 1 to 2 hours, yet its therapeutic effects in treating rheumatoid arthritis last for much longer. This prolongation of therapeutic effect is due to

A
irreversible inhibition of COX-1 and COX-2.

B
its relative selectivity for COX-2.

C
its accumulation in synovial fluid.

D
the formation of a long-lived active metabolite.

E
CNS effects unrelated to inhibition of prostaglandin synthesis.

A

C
its accumulation in synovial fluid.

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15
Q

Most clinically used opioid analgesics are selective for
which type of opioid receptor?
(A) kappa (κ)
(B) alpha (α)
(C) beta (β)
(D) mu (μ)
(E) delta (δ)

A

(D) mu (μ)

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16
Q
  1. Codeine has a greater oral bioavailability compared
    with morphine because of which reason?
    (A) codeine undergoes less first-pass metabolism
    (B) morphine is conjugated more quickly
    (C) morphine directly passes into systemic circulation
    (D) codeine is available only in liquid formulation
    (E) codeine is metabolized more by hepatic enzymes
A

(A) codeine undergoes less first-pass metabolism

17
Q

Which of the following statements best explains the
observation that morphine is more likely to cause
nausea and vomiting in ambulatory patients?
(A) morphine inhibits chemoreceptor trigger zone
neurons
(B) morphine sensitizes medulla cough center neurons
(C) opioids cause sedation, which makes walking more
difficult
(D) patients on opioids eat more
(E) opioids increase vestibular sensitivity

A

(E) opioids increase vestibular sensitivity

18
Q

Which of the following opioids is so lipophilic that it
is marketed in a skin patch used to treat chronic pain?
(A) morphine
(B) naltrexone
(C) scopolamine
(D) methadone
(E) fentanyl

A

(E) fentanyl

19
Q

In a case of an opioid overdose, naloxone can be given
in repeated doses because of which property of
naloxone?
(A) may have a shorter half-life than the opioid agonist
(B) is effective only at high cumulative doses
(C) is needed to stimulate the respiratory center
(D) is safe only in extremely small doses
(E) is only a partial opioid agonist

A

(A) may have a shorter half-life than the opioid agonist

20
Q

Aspirin is often used in low doses to prevent platelet
aggregation by inhibiting the synthesis of which
substance?
(A) leukotriene
(B) prostacyclin (PGI2)
(C) thromboxane A2
(D) arachidonic acid
(E) phospholipase A

A

(C) thromboxane A2

21
Q

Acetaminophen is a potent analgesic and antipyretic
NSAID but differs from other agents in that it has no
antiinflammatory action. Which of the following
reasons explains this unique aspect of acetaminophen?
(A) the distribution of acetaminophen does not reach peripheral sites of inflammation
(B) acetaminophen is not an inhibitor of the COX enzyme
(C) antiinflammatory doses of acetaminophen are too high and toxic
(D) it is selective for a newly discovered isozyme of COX
(E) acetaminophen undergoes significant first-pass metabolism

A

(D) it is selective for a newly discovered isozyme of COX

22
Q

Which of the following agents augments the physiologic concentration of IL-1Ra proteins in the treatment of RA?
(A) adalimumab
(B) leflunomide
(C) etanercept
(D) infliximab
(E) anakinra

A

(E) anakinra

23
Q

With respect to antigout therapy, inhibition of tubulin polymerization into microtubules is important given the role of which process in which aspect of the disease?
(A) leukotriene synthesis
(B) uric acid production
(C) kidney reabsorption of uric acid
(D) leukocyte migration
(E) plasma binding of uric acid

A

(D) leukocyte migration

24
Q

A 45-year-old obese man with a history of alcohol abuse and hypertension develops joint swelling and pain. His urate excretion rate is 950 mg/day. Which of the following agents is the best treatment for his condition?
(A) probenecid
(B) allopurinol
(C) piroxicam
(D) lesinurad
(E) colchicine

A

(B) allopurinol

25
Q

Selective Cyclooxygenase 2 Inhibitors

A

Celecoxib (Celebrex)

26
Q

Disease Modifiying Anti-Rheumatic Drugs (DMARDS)
Auranofin (Ridaura)
Aurothioglucose (Solganal)
Gold Sodium Thiomalate (Aurolate)
Other Disease Modifying Anti-Rheumatic Drugs
Etanercept (Enbrel)
Hydroxychloroquine (Plaquenil)
Leflunomide (Arava)
Methotrexate (Rheumatrex)
Penicillamine (Cuprimine)
Sulfasalazine (Azulfidine)

A
  • Auranofin (Ridaura)
  • Aurothioglucose (Solganal)
  • Gold Sodium Thiomalate (Aurolate)
26
Q

Disease Modifiying Anti-Rheumatic Drugs (DMARDS)

A
  • Auranofin (Ridaura)
  • Aurothioglucose (Solganal)
  • Gold Sodium Thiomalate (Aurolate)
27
Q

Drugs for Gout: Prevention

A
  • Allopurinol (Zyloprim)
  • Febuxostat (Uloric)
  • Pegloticase (Krystexxa)
  • Rasburicase (Elitek)
  • Lesinurad (Zurampic)
28
Q

Drugs for Gout: Acute Attacks

A
  • Colchicine (Colcrys)
  • Indomethacin (Indocin)
  • Prednisone (Deltasone)
29
Q

NSAIDS (MOA)

A
  • Inhibition of Cyclooxygenase (COX) an enzyme that catalyzes the first step in the synthesis of prostaglandins from arachidonic acid and other precursor fatty acids
  • COX is a microsomal enzyme existing as a dimer linked to form a functional unit in the lumen and membrane of the endoplasmic reticulum
  • NSAIDS decrease COX activity by competitive inhibition
  • Net effect is a decrease in the production of prostaglandins and other autocoids
30
Q

Cox-1

A
  • Helps in synthesis of PG that have cytoprotective effect on the GI tract
  • Catalyzes formation of thromboxane A2 in platelets leading to hemostasis
  • Participates in renal homeostasis
31
Q

Cox-2

A

Inducible enzyme upregulated in inflammatory processes by cytokines and endotoxins and tumor promoters
Participates in renal homeostasis
Celecoxib (Celebrex)
Produce less GI bleeding and ulcers than nonselective agents

32
Q

COX 3

A

Acetaminophen inhibits COX 3 potently and has little anti-inflammatory action

33
Q

Aspirin (Toxic Effects)

A
  • 3-6 grams: Anti-inflammatory Effects, Tinnitus
  • 6-10grams: Hyperventilation and Respiratory Alkalosis
  • 10-20grams: Fever, Dehydration, Metabolic Acidosis
  • 20-30grams: Shock, Coma, Respiratory and Renal Failure, Death