NSAID's and Acetaminophen (Exam 3; Dr. Gupta)
Place the following NSAIDs in order from most potent to least: (Group together the drugs with similar level of potency) -Aspirin -Ibuprofen -Indomethacin -Ketoprofen -Ketorolac -Naproxen -Celecoxib
1) Ketorolac (100 level of potency) 2) Indomethacin (40 level of potency) 3) Ketoprofen and Celecoxib (20 level of potency) 4) Ibuprofen and Naproxen (4 level of potency) 5) Aspirin (1 level of potency)
Which of the following drugs most commonly interact with NSAIDs? (select all that apply) A) ACE Inhibitors B) Corticosteroids C) Warfarin D) Methotrexate E) Suflonylurea F) Hypoglycemic agents
A) ACE Inhibitors B) Corticosteroids C) Warfarin D) Methotrexate E) Suflonylurea F) Hypoglycemic agents
Which of the following ↓ effectiveness, ↑risk of bradycardia and syncope in elderly, hypertensive, diabetes, and heart patients when taken with NSAIDs? A) ACE inhibitors B) Corticosteroids C) Warfarin D) Warfarin, Methotrexate, Sulfonylureas, Hypoglycemic agents
A) ACE inhibitors
Which of the following is TRUE regarding pain therapy in the elderly? (select all that apply) A) Acetaminophen is a good option B) Use NSAIDs for the shortest period of time (lowest dose with mucosal protective agents) C) H. pylori infection increases risk of GI complications D) NSAIDs are not recommended in heart failure patients E) NSAIDs can be used in Heart Failure patients if they are used with gastro-protective therapy
A) Acetaminophen is a good option B) Use NSAIDs for the shortest period of time (lowest dose with mucosal protective agents) C) H. pylori infection increases risk of GI complications D) NSAIDs are not recommended in heart failure patients E) NSAIDs can be used in Heart Failure patients if they are used with gastro-protective therapy
What are the major properties of NSAID use? (Select all that apply) A) Analgesic (Pain) B) Antipyretic (Fever) C) Anti-inflammatory D) Uricosuric effects
A) Analgesic (Pain) B) Antipyretic (Fever) C) Anti-inflammatory D) Uricosuric effects
Which of the following are common symptoms of GI effects associated with NSAIDs? (select all that apply) A) Anorexia B) Nausea C) Dyspepsia D) Abdominal pain E) Diarrhea
A) Anorexia B) Nausea C) Dyspepsia D) Abdominal pain E) Diarrhea
Diclofenac, Etodolac, Indomethacin, Sulindac, Bromfenac are all examples of: A) Aryl and heteroaryl acetic acids B) Aryl and heteroaryl propionic acids
A) Aryl and heteroaryl acetic acids
Which of the following NSAIDs inhibits platelet aggregation and is used to prevent and treat arterial thromboembolic disorders? A) Aspirin B) Indomethacin C) Naproxen D) Ibuprofen
A) Aspirin
Which of the following drugs has shown a 50% reduction in the risk of colon cancer? A) Aspirin B) Indomethacin C) Naproxen D) Ibuprofen
A) Aspirin
Which of the following should not be used in children with febrile viral illness due to Reye's syndrome? A) Aspirin B) Acetaminophen C) NSAIDs
A) Aspirin
Which of the following NSAIDs can be used to treat dysmenorrhea? (select all that apply) A) Aspirin B) Ibuprofen C) Naproxen D) Celebrex E) Ketoprofen F) Meloxicam
A) Aspirin B) Ibuprofen C) Naproxen D) Celebrex E) Ketoprofen
Aspirin at low dose is more selective for: A) COX-1 B) COX-2
A) COX-1
NSAIDs cause gastric damage (ulceration) by inhibiting prostaglandins synthesis by blocking ____ enzyme in the GI A) COX-1 B) COX-2
A) COX-1
____ is primarily inhibited in the kidneys by NSAIDs resulting in adverse effects A) COX-1 B) COX-2
A) COX-1
Which of the following are true regarding counseling points for NSAIDs? (select all that apply) A) Can cause ulcers and bleeding in GI tract B) Must be taken with food C) Can be taken with or without food D) Can increase chance of heart attack E) Can increase blood pressure
A) Can cause ulcers and bleeding in GI tract B) Must be taken with food D) Can increase chance of heart attack E) Can increase blood pressure
Which of the following are true about osteoarthritis? (select all that apply) A) Caused by damage of joint cartilage which in turn causes wear and tear of the joints B) Joint bone rub against one another resulting in a very severe pain C) Starts by affecting a single joint and the damage may spread to other joints D) Resulting inflammation of the joints causing lots of pain and affecting joint motion
A) Caused by damage of joint cartilage which in turn causes wear and tear of the joints B) Joint bone rub against one another resulting in a very severe pain C) Starts by affecting a single joint and the damage may spread to other joints
Blood pressure, renal, and renovascular complications occur more commonly with: A) Celecoxib B) Traditional NSAIDs
A) Celecoxib
Which of the following NSAID is truly selective for COX-2? A) Celecoxib B) Etodolac C) Meloxicam
A) Celecoxib
Which of the following is a synthetic PGE2? A) Dinoprostone B) Misoprostol
A) Dinoprostone
Which of the following are toxicities that are involved with Salicylates? (select all that apply) A) GI ulceration and hemorrhage B) Nephrotoxicity C) Hepatic injury (long-term use) D) Hyper-activity E) Reye's syndrome
A) GI ulceration and hemorrhage B) Nephrotoxicity C) Hepatic injury (long-term use) D) Hyper-activity E) Reye's syndrome
What of the following are the SAFE pathways to metabolize acetaminophen? (select all that apply) A) Glucuronidation B) Sulfonation C) GSH conjugation D) SH-Hepatic Proteins
A) Glucuronidation B) Sulfonation C) GSH conjugation
Aryl and heteroaryl propionic acids (-pro) include? (select all that apply) A) Ibuprofen B) Ketoprofen C) Fenoprofen D) Flurbiprofen E) Naproxen F) Oxaprozin
A) Ibuprofen B) Ketoprofen C) Fenoprofen D) Flurbiprofen E) Naproxen F) Oxaprozin
Diclofenac and Misoprostol combination is most useful in: A) In elderly B) In pregnant patient to prolong labor C) To terminate intrauterine pregnancy D) Cervical ripening
A) In elderly
Which of the following are true regarding NSAIDs and their effects on kidneys? (select all that apply) A) Increase water and sodium retention B) Oppose effects of diuretics and anti-hypertensives C) Exacerbate problems and hypertensive complications D) Worsen congestive heart failure E) Chronis uses of high doses of NSAIDs may cause analgesic nephropathy (slowly progressive renal failure)
A) Increase water and sodium retention B) Oppose effects of diuretics and anti-hypertensives C) Exacerbate problems and hypertensive complications D) Worsen congestive heart failure E) Chronis uses of high doses of NSAIDs may cause analgesic nephropathy (slowly progressive renal failure)
TXA₂ is produced by activated platelets via COX-1 enzyme. This results in detrimental effects to the heart due to: (select all that apply) A) Increased platelet aggregation B) Vasoconstriction C) Vasodilation D) Decreased platelet aggregation
A) Increased platelet aggregation B) Vasoconstriction
What is the significance of the methyl substitutions in -profens? (select all that apply) A) Increases anti-inflammatory activity B) Decreases anti-inflammatory activity C) Increases Hepatotoxicity D) Decreases Hepatotoxicity
A) Increases anti-inflammatory activity D) Decreases Hepatotoxicity
Which of the following are true about Indomethacin? (select all that apply) A) Indole derivative B) Largely more potent than aspirin, Ibuprofen, Naproxen C) Not as widely used D) Associated with significant GI and CNS side effects such as headache, vertigo, dizziness, psychiatric disorders
A) Indole derivative B) Largely more potent than aspirin, Ibuprofen, Naproxen D) Associated with significant GI and CNS side effects such as headache, vertigo, dizziness, psychiatric disorders
Which of the following NSAIDs can be used to treat PDA in neonates? (select all that apply) A) Indomethacin injection B) Ibuprofen injection C) Naproxen injection D) Aspirin injection E) Celecoxib injection
A) Indomethacin injection B) Ibuprofen injection
Which of the following are therapeutic uses of NSAIDs? (select all that apply) A) Inflammation (swelling, pain, fever) B) Rheumatoid arthritis, osteoarthritis, gout C) Dysmenorrhea D) Prophylaxis of MI/Stroke (Aspirin) E) Alzheimer's F) Prophylaxis of colon cancer
A) Inflammation (swelling, pain, fever) B) Rheumatoid arthritis, osteoarthritis, gout C) Dysmenorrhea D) Prophylaxis of MI/Stroke (Aspirin) E) Alzheimer's F) Prophylaxis of colon cancer
Which of the following is TRUE regarding sulindac? (select all that apply) A) It has an indene ring (less toxic) B) It has anti-inflammatory activity with reduced CNS & GI effects C) It is less water soluble D) It contains -SOCH₃ group which can cause hypersensitivity (SJS)
A) It has an indene ring (less toxic) B) It has anti-inflammatory activity with reduced CNS & GI effects C) It is less water soluble D) It contains -SOCH₃ group which can cause hypersensitivity (SJS)
Which of the following is TRUE regarding the ceiling effect? (select all that apply) A) Its a dose beyond which there is NO additional therapeutic effect B) Analgesic doses of NSAIDs are small & have a ceiling C) Anti-inflammatory doses of NSAIDs are higher and have NO ceiling D) Inflammation does not equal pain
A) Its a dose beyond which there is NO additional therapeutic effect B) Analgesic doses of NSAIDs are small & have a ceiling C) Anti-inflammatory doses of NSAIDs are higher and have NO ceiling D) Inflammation does not equal pain
Which of the following is TRUE regarding nabumetone? (select all that apply) A) Its a prodrug (non-acidic NSAID) B) Its a ketone derivative having naphthalene nucleus (photosensitive) C) It does NOT have -COOH thus does not cause direct damage to GI D) ↓ GI ulcerations E) It shows some COX-2 selectivity F) It has a long-half life
A) Its a prodrug (non-acidic NSAID) B) Its a ketone derivative having naphthalene nucleus (photosensitive) C) It does NOT have -COOH thus does not cause direct damage to GI D) ↓ GI ulcerations E) It shows some COX-2 selectivity F) It has a long-half life
Salicylates can be used for: (select all that apply) A) Mild-to-moderate pain B) Moderate-to-severe pain C) Headache D) Myalgia E) Arthralgia
A) Mild-to-moderate pain C) Headache D) Myalgia E) Arthralgia
Which of the following is NOT a desired pathway with acetaminophen? A) NAPQI conjugating with liver proteins B) Sulfate conjugation in children C) N-acetylcysteine forming non-toxic water soluble conjugates D) N-acetylcysteine promoting GSH synthesis to decrease acetaminophen toxicity
A) NAPQI conjugating with liver proteins
What is the non-acidic prodrug producing acetic acid derivative? A) Nabumetone B) Diclofenac C) Sulindac D) Indomethacin E) Bromfenac
A) Nabumetone
Which of the following is 10 times more potent than aspirin? A) Naproxen B) Celecoxib C) Ketorolac D) Aspirin E) Nabumetone
A) Naproxen
Which of the following types of pain are targeted by NSAIDs? (select all that apply) A) Nociceptive pain B) Inflammatory pain C) Neuropathic pain D) Functional pain
A) Nociceptive pain B) Inflammatory pain
Aspirin is absorbed in relative acidic conditions (stomach). Agents that increase gastric pH (ex: antacids) decrease? A) RATE of absorption B) EXTENT of absorption
A) RATE of absorption
Which isomer of ibuprofen and naproxen is more potent? A) S-isomer B) R-isomer
A) S-isomer
Acetaminophen can be toxic due to: (select all that apply) A) Saturation of normal metabolism (Toxic dose; Repeated supra-therapeutic concentration) B) Alcoholism C) Induction of CYPs D) GSH depletion (alcohol, malnutrition, fasting) E) Drug interactions
A) Saturation of normal metabolism (Toxic dose; Repeated supra-therapeutic concentration) B) Alcoholism C) Induction of CYPs D) GSH depletion (alcohol, malnutrition, fasting) E) Drug interactions
Which of the following is/are TRUE about prostaglandins? (select all that apply) A) Short half-lives B) Produced locally at the site of inflammation C) Basic in nature D) All prostaglandins can induce inflammation E) All derived from arachidonic acid
A) Short half-lives B) Produced locally at the site of inflammation E) All derived from arachidonic acid
Which of the following are common side effects of NSAIDs? (select all that apply) A) Stomach upset/Ulcers/Bleeding B) Kidney damage C) Liver damage D) Ringing in the ears
A) Stomach upset/Ulcers/Bleeding B) Kidney damage C) Liver damage D) Ringing in the ears
Which of the following are true about the uses of Misoprostol? (select all that apply) A) Termination of intrauterine pregnancy B) Off label use for early pregnancy loss, incomplete abortion treatment and labor induction C) Prevention of NSAID-induced gastric ulcers
A) Termination of intrauterine pregnancy B) Off label use for early pregnancy loss, incomplete abortion treatment and labor induction C) Prevention of NSAID-induced gastric ulcers
Which of the following are advantages of prostaglandins (PGE₂ & PGI₂)? (select all that apply) A) They are gastroprotective B) They enhance mucosal blood flow C) They confer physical protection by forming mucosal gel D) They inhibit gastric acid secretion E) They promote NaHCO₃ production
A) They are gastroprotective B) They enhance mucosal blood flow C) They confer physical protection by forming mucosal gel D) They inhibit gastric acid secretion E) They promote NaHCO₃ production
Which of the following is the preferred treatment in childhood fever? A) Aspirin B) Acetaminophen C) NSAIDs
B) Acetaminophen
Which of the following 2 drugs can be regarded as analgesic/anti-pyretic and NOT anti-inflammatory? A) Ibuprofen B) Acetaminophen C) Diflunisal D) Salicylamide
B) Acetaminophen D) Salicylamide
Increased expression of ____ is seen in some cancer cells. Angiogenesis essential to tumor growth requires this A) COX-1 B) COX-2
B) COX-2
Meloxicam, Etodolac, Nabumetone are considered as relatively selective for _____ A) COX-1 B) COX-2
B) COX-2
Which of the following is a COX-2 selective inhibitor? A) Naproxen B) Celecoxib C) Ketorolac D) Aspirin E) Nabumetone
B) Celecoxib
Which of the following are true about rheumatoid arthritis? (select all that apply) A) Caused by damage of joint cartilage which in turn causes wear and tear of the joints B) Chronic disease results of body immune cells attacking body's cell C) Resulting in inflammation of the joints causing lots of pain and affecting joint motion D) Can start by affecting several joints at a go
B) Chronic disease results of body immune cells attacking body's cell C) Resulting in inflammation of the joints causing lots of pain and affecting joint motion D) Can start by affecting several joints at a go
Which of the following ↑frequency and severity of GI ulceration with NSAIDs? A) ACE inhibitors B) Corticosteroids C) Warfarin D) Warfarin, Methotrexate, Sulfonylureas, Hypoglycemic agents
B) Corticosteroids
All NSAIDs relieve fever by inhibiting PG synthesis in the ______, but are not capable of reducing body temperature below normal (hypothermia) A) Pituitary Gland B) Hypothalamus C) Frontal Lobe D) Parietal Lobe
B) Hypothalamus
Which of the following is a synthetic PGE1? A) Dinoprostone B) Misoprostol
B) Misoprostol
The patency of the ductus arteriosus is maintained by: A) PGI2 B) PGE2 C) PGF2a D) PGF2B
B) PGE2
Which of the following prostaglandins are responsible for the effects seen in dysmenorrhea (↑contraction of uterus, ↑cramping & ↑pain)? (Select all that apply) A) PGI2 B) PGE2 C) PGF2a D) PGF2B
B) PGE2 C) PGF2a
Which of the following prostaglandins contribute to an increase in uterine contractions during pregnancy? (select all that apply) A) PGI2 B) PGE2 C) PGF2a D) PGF2B
B) PGE2 C) PGF2a
All of the following can be regarded as endogenous pathways related with acetaminophen EXCEPT: A) Glucuronidation B) Sulfate Conjugation C) N-acetylcysteine conjugation D) GSH conjugation E) Conjugation with hepatic protein
C) N-acetylcysteine conjugation
This agent is effective in reducing fever, alleviating pain, and reducing inflammation in children? A) Aspirin B) Acetaminophen C) NSAIDs
C) NSAIDs
Which of the following prostaglandins raises the temperature set point which then is lowered by NSAIDs? A) PGI2 B) PGH2 C) PGE2 D) PGF2
C) PGE2
Which of the following Salicylates has analgetic/antipyretic effects ONLY (no inflammatory activity)? A) Sodium Salicylate B) Aspirin C) Salicylamide D) Diflunisal
C) Salicylamide
PGI₂ is produced by endothelial cells via COX-1 & COX-2 enzyme. This results in protective effects to the heart due to: (select all that apply) A) Increased platelet aggregation B) Vasoconstriction C) Vasodilation D) Decreased platelet aggregation
C) Vasodilation D) Decreased platelet aggregation
Which of the following ↑plasma level, ↑risk of bleeding when taken with NSAIDs (concurrent use should be avoided)? A) ACE inhibitors B) Corticosteroids C) Warfarin D) Warfarin, Methotrexate, Sulfonylureas, Hypoglycemic agents
C) Warfarin
Which of the following are FALSE about the Sulfonamide group in Celecoxib? A) Required for activity B) Decreases gastric and renal side effects (COX-2 selectivity) C) Increase in allergy side effects D) Decrease in allergy side effects E) Causes Cardiovascular risks
D) Decrease in allergy side effects
Which of the following Salicylates has a long half-life? A) Sodium Salicylate B) Aspirin C) Salicylamide D) Diflunisal
D) Diflunisal
Which of the following anti-depressant drugs that is useful for chronic pain in osteoarthritis? A) Fluoxetine B) Venlafaxine C) Escitalopram D) Duloxetine
D) Duloxetine
Which of the following pathways is considered to be a toxic metabolic pathway of acetaminophen? A) Glucuronidation B) Sulfonation C) GSH conjugation D) SH-Hepatic Proteins
D) SH-Hepatic Proteins
Which of the following agents may be displaced from their protein binding sites leading to ↑ toxicity when taken with NSAIDs? A) ACE inhibitors B) Corticosteroids C) Warfarin D) Warfarin, Methotrexate, Sulfonylureas, Hypoglycemic agents
D) Warfarin, Methotrexate, Sulfonylureas, Hypoglycemic agents
Which of the following is available as an ophthalmic solution used for the treatment of postoperative inflammation and reduction of ocular pain in patients who have undergone cataract surgery? A) Nabumetone B) Diclofenac C) Sulindac D) Indomethacin E) Bromfenac
E) Bromfenac
____ is a toxic byproduct that is produced during the metabolism of acetaminophen
NAPQI
T/F: Acetaminophen (Tylenol) is the only anti-pyretic analgesic in the market
True
T/F: Acetaminophen has almost NO anti-inflammatory activity and has no gastric or platelet side effects like NSAIDs
True
T/F: Aspirin could displace other drugs highly bound to plasma (anticoagulants)
True
T/F: COX-1 is the main isoform in platelets
True
T/F: Celecoxib alters the vascular homeostasis by removing the cardioprotective effects of PGI2 leaving the atherogenic properties of TXA2 intact. This increases the risk of myocardial infarction, heart attack, stroke, and thrombosis
True
T/F: Celecoxib is the only drug available that is considered for be truly selective COX-2 inhibitor
True
T/F: Diflunisal has analgesic & anti-inflammatory effects and is more potent than aspirin. It has no auditory side effects and has less intense GI effects
True
T/F: Dinoprostone can cause uterine contractions
True
T/F: Excessive levels of PGs/hormones causes mensural cramps
True
T/F: Gastric damage can occur with oral, parenteral, and transdermal administration of NSAIDs
True
T/F: Gastritis and peptic ulceration with bleeding are adverse effects of NSAIDs
True
T/F: Ibuprofen and Naproxen are available in liquid suspensions
True
T/F: Ibuprofen can be useful in relieving some symptoms associated with osteo- as well as rheumatoid arthritis
True
T/F: Irreversible binding of glutathione to NAPQI (metabolite of acetaminophen) forms a highly water soluble conjugate that can be easily eliminated by kidneys
True
T/F: Long term use of NSAIDs can lead to analgesic nephropathy
True
T/F: Low dose aspirin selectively inhibits (reduces) the synthesis of TXA2. It irreversibly inhibits COX-1 that catalyzes an early step in TXA2 synthesis
True
T/F: N-acetylcysteine (Mucomyst) is the antidote for acetaminophen overdose. Activated charcoal can be used but it removes drug from the stomach NOT the blood & is only useful in binding drug that has not yet been digested
True
T/F: NSAIDs can prolong labor by inhibiting PGs. However, use in late pregnancy may increase risk of postpartum hemorrhage
True
T/F: NSAIDs target the enzyme COX responsible for conversion of arachidonic acid to prostaglandin which results into inflammation
True
T/F: NSAIDs target the enzyme COX responsible for the conversion of arachidonic acid to prostaglandin (resulting in inflammation). All NSAIDs inhibit COX (cyclooxygenase).
True
T/F: Nabumetone contains a naphthalene nucleus which can cause photosensitivity
True
T/F: Nabumetone is metabolized via liver enzymes to acetic acid derivative (active drug)
True
T/F: Naphthalene nucleus in naproxen can cause photosensitivity
True
T/F: Oxicams such as Prioxicam and Meloxicam are enolic acid class of NSAIDs. They contain alkene and alcohol groups
True
T/F: Prostaglandins is derived from arachidonic acid and is a precursor for many other prostaglandins
True
T/F: Prostaglandins reduce the threshold to stimulation of pain receptors by peripheral and central sensitization of nociceptors
True
T/F: Salicylism is generally observed at 6-10g per dose of aspirin. It is manifested by vomiting, sweating, tinnitus, dizziness, hallucinations, convulsions
True
T/F: Selective COX-2 inhibitors may eliminate (reduce) side effects such as gastric and renal effects associated with non-selective NSAIDs because of COX-1 inhibition
True
T/F: The hypothalamus regulates temperature set point and maintains body temperature
True
T/F: Use of NSAIDs can result in loss of cardio protection due to inhibition of COX enzymes resulting in reduced production of PGI2
True
T/F: Use of NSAIDs during early pregnancy increases the risk of miscarriage
True
