90 Questions
Which of the following is a pharmacological action of aspirin?
Inhibition of antigen-antibody reactions
What is the mechanism of action of aspirin?
Inhibition of COX-1 and COX-2 activity
Which of the following is a shared use of NSAIDs?
Management of musculoskeletal pain
What is the effect of NSAIDs on renal function in patients with congestive heart failure?
Decrease in glomerular filtration rate
Which of the following is a shared drug interaction with NSAIDs?
Increased renal excretion of lithium
What is the effect of salicylates on body temperature?
Return to normal in the presence of salicylates
Which of the following is a pharmacokinetic property of salicylates?
Predominantly bound to plasma proteins
What is the distribution of salicylates in the body?
Wide distribution throughout body tissues
What is the effect of chronic use of high doses of NSAIDs?
Promotion of analgesic nephropathy
What is the plasma half-life of salicylate after a large dose?
15-30 hours
Which of the following is NOT a cause of inflammation?
Hypersensitivity
Which of the following is a chemical mediator of inflammation?
Platelet-activating factor (PAF)
What is the process of inflammation characterized by?
All of the above
Which of the following can cause fever?
All of the above
What triggers the initial phase of the thermoregulatory response?
Ceramide release
Which of the following is NOT a chemical mediator of inflammation?
Interferons
What are the damage- and pathogen-associated molecules recognized by cells charged with immune surveillance?
Others: endothelial intercellular adhesion molecule-1 (ICAM-1), oxygen radicals and nitric oxide
Which of the following is an immunologic mediator of inflammation?
Tumor necrosis factor (TNF)
What is the immune system's protective response to injurious stimulus called?
Inflammation
Which of the following is NOT a consequence of chronic inflammation?
Fever
Which enzyme is involved in the induction of cyclooxygenase (COX-2) during the late phase response?
COX-1
Which receptors does PGE2 act on to trigger the hypothalamus to elevate body temperature?
EP receptors on thermosensitive neurons
Which of the following is NOT a stimulus that can activate nociceptors?
Light
Which neuropeptides may be involved in the generation of pain?
Substance P and calcitonin gene-related peptide (CGRP)
Which prostaglandins reduce the threshold of stimulation of nociceptors leading to peripheral sensitization?
PGE2 and PGD2
Which tissues are commonly affected by rheumatoid arthritis (RA)?
Joints, skin, lungs, muscle, and CVS
What is the first joint tissue affected in rheumatoid arthritis?
Synovial membrane
What is the mechanism of action of non-selective NSAIDs?
Inhibit both COX-1 and COX-2
What is the shared pharmacological action of NSAIDs on the cardiovascular system?
Decreased release of vasodilator PGE2 and PGI2
What is the side effect of NSAIDs on the gastric mucosa?
Inhibition of COX-1 in gastric epithelial cells
Which of the following NSAIDs has the longest half-life?
Naproxen
Which NSAID is 20 times more potent than aspirin in inhibiting COX?
Naproxen
Which NSAID directly inhibits leukocyte function?
Indomethacin
Which NSAID causes less severe gastrointestinal effects than aspirin?
Naproxen
Which NSAID is a ketone prodrug converted to an active metabolite in the liver?
Nabumetone
Which NSAID has a preferential activity against COX-2?
Meloxicam
Which NSAID is the only FDA approved drug in the COX-2 selective inhibitors class?
Celecoxib
Which of the following is a non-selective NSAID?
Ibuprofen
What is the primary respiratory effect of salicylates in medium to large doses?
Hyperventilation
What is the compensatory response to the initial respiratory alkalosis caused by therapeutic doses of salicylates?
Increased renal excretion of bicarbonate
What is the mechanism of increased O2 consumption and CO2 production in skeletal muscle caused by salicylates?
Uncoupling of oxidative phosphorylation
What is the effect of salicylates on plasma CO2 tension (PCO2) in anti-inflammatory doses?
PCO2 decreases slightly
What is the shared side effect of non-selective NSAIDs on the gastric mucosa?
Gastric ulcers
What is the effect of salicylates on acid-base and electrolyte balance?
Increased renal excretion of bicarbonate
Which of the following is a characteristic of salicylism, a mild form of salicylate intoxication?
Hyperpyrexia
Which of the following is a consequence of salicylate-induced sweating and hyperventilation?
Dehydration
What is the reversible hepatic injury caused by large doses of salicylates called?
Hepatotoxicity
What is the effect of a single dose of aspirin on bleeding time in normal individuals?
Prolongs bleeding time for 4-7 days
What is the primary mechanism of gastric damage caused by salicylates?
Inhibition of prostaglandin synthesis
What is the effect of low doses of salicylates on urate excretion?
Decreases urate excretion
What are the neurological effects of high doses of salicylates?
Stimulation followed by depression
Which of the following is an inhibitor of Janus kinase?
Baricitinib
Which of the following is a common side effect of hydroxychloroquine?
Skin rash
Which of the following is a disease-modifying anti-rheumatic drug (DMARD) used as monotherapy or in combination with methotrexate?
Leflunomide
Which cytokines are involved in the pathogenesis of rheumatoid arthritis?
IL-1 and TNFα
Which of the following drugs can decrease signs and symptoms of rheumatoid arthritis, reduce structural damage progression, and improve physical conditions of patients?
Adalimumab
Which of the following is a common side effect associated with rheumatoid arthritis therapy?
Mucosal ulceration
Which of the following is an immunomodulatory drug that inhibits the activity of autoimmune lymphocytes?
Leflunomide
Which of the following is a shared side effect of methotrexate and leflunomide?
GI upset
Which of the following is a recombinant monoclonal antibody used to reduce signs and symptoms of moderate to severe rheumatoid arthritis?
Adalimumab
Which enzyme is inhibited by non-selective NSAIDs?
Both COX-1 and COX-2
Which type of NSAIDs is more selective in inhibiting COX-2?
COX-2 selective inhibitors
Which NSAID is commonly used as an opioid-sparing agent in certain acute trauma cases?
Ibuprofen
Which NSAID has the brand name 'Celebrex'?
Celecoxib
Which NSAID has the generic name 'Naprosyn'?
Naproxen
Which NSAID is commonly known as 'Motrin' and 'Advil'?
Ibuprofen
Which of the following is the first biotechnology-derived drug for the reduction of signs and symptoms of moderate to severe active rheumatoid arthritis in patients who have not adequately responded to one or more of the synthetic DMARDs?
Burenex®
Which of the following alkaloids is represented in the highest percentage in opium?
Morphine
Which of the following receptors do opioids mainly bind to in order to control pain and pleasurable and addictive behavior?
Mu receptors
Which of the following is the prototype receptor mu agonist?
Morphine
Which of the following is the structure of morphine that exhibits a high degree of stereoselectivity of analgesic?
Centers of chirality
Which of the following is a physiochemical property of morphine?
Amphoteric substance
Which of the following is NOT a characteristic of COX-1?
It is involved in inflammation
Which of the following is a characteristic of COX-2 selective NSAIDs?
They provide anti-inflammatory relief without compromising the gastric mucosa
What is the predominate form of acetaminophen (pKa,9.7) at physiological pH?
Ionized
What is the primary metabolite of acetaminophen in children?
O-sulfate
What is the primary mechanism of action of diclofenac?
All of the above
What is the bioavailability of diclofenac on oral administration?
50-60%
Which is the most active isomeric form of the opioid receptor?
Levorotatory enantiomorph with stereochemistry 5®, 6(S), 9)R), 13(S) and 14(R)
Which conformation is 10 times more potent than the B/C trans conformation?
B/C cis conformation
What is the pharmacophore for opioid analgesic activity?
4-phenylpiperidine structure
What is the precursor for heroin, hydromorphone, and oxymorphone?
Morphine
What is the 3,6 diacetylated form of morphine?
Heroin
What is the enzyme responsible for the O-demethylation of codeine?
Cytochrome P450 CYP2D6
Which enzyme is responsible for the metabolism of diclofenac to its major metabolite via CYP3A4?
CYP3A4
What is the major metabolite of diclofenac formed via CYP3A4?
4’-hydroxy derivative
Which enzyme is responsible for the formation of 5’-hydroxy, 3’-hydroxy, and 4’,5’-dihydroxy metabolites of diclofenac?
CYP2C9
What percentage of the dose of diclofenac is excreted as the 4’-hydroxy derivative?
20-30%
What is the preferred conformation of the N-p-chlorobenzoyl group in indomethacin?
The chlorophenyl ring is oriented away from the 2-methyl group
Which enzyme is responsible for the 5-O-demethylation of indomethacin?
CYP2C9
Study Notes
Pharmacological Actions of Aspirin and NSAIDs
- Aspirin's pharmacological action is to inhibit cyclooxygenase (COX), which leads to the inhibition of prostaglandin synthesis.
- The mechanism of action of aspirin is to irreversibly acetylate COX, thereby inhibiting its activity.
NSAIDs
- Shared use of NSAIDs: to relieve pain, reduce inflammation, and lower fever.
- Effect of NSAIDs on renal function in patients with congestive heart failure: NSAIDs can reduce renal function and exacerbate congestive heart failure.
- Shared drug interaction with NSAIDs: NSAIDs can interact with anticoagulants, increasing the risk of bleeding.
Salicylates
- Effect of salicylates on body temperature: salicylates can increase body temperature by stimulating the hypothalamus.
- Pharmacokinetic property of salicylates: salicylates have a nonlinear plasma half-life, which increases with dose.
- Distribution of salicylates in the body: salicylates are distributed widely in the body, with high concentrations in the liver, kidneys, and lungs.
Inflammation
- Process of inflammation: characterized by increased blood flow, increased permeability, and infiltration of white blood cells.
- Chemical mediators of inflammation: include histamine, bradykinin, and prostaglandins.
- Damage- and pathogen-associated molecules recognized by cells charged with immune surveillance: include PAMPs (pathogen-associated molecular patterns) and DAMPs (damage-associated molecular patterns).
Immune Response
- Immune system's protective response to injurious stimulus: characterized by inflammation, which is triggered by the activation of immune cells.
- Consequence of chronic inflammation: can lead to tissue damage and disease.
Rheumatoid Arthritis
- Tissues commonly affected by rheumatoid arthritis (RA): synovial joints, particularly the hands and feet.
- First joint tissue affected in rheumatoid arthritis: the synovial membrane.
- Mechanism of action of non-selective NSAIDs: inhibit COX-1 and COX-2, leading to the inhibition of prostaglandin synthesis.
- Shared pharmacological action of NSAIDs on the cardiovascular system: can increase blood pressure and cardiovascular risk.
Specific NSAIDs
- Aspirin: inhibits COX-1 and COX-2, with a long half-life.
- Indomethacin: has a high potency and is used to treat acute gout and rheumatoid arthritis.
- Diclofenac: has a high potency and is used to treat pain, inflammation, and fever.
- Celecoxib: is a COX-2 selective inhibitor, used to treat rheumatoid arthritis and osteoarthritis.
- Naproxen: has a long half-life and is used to treat pain, inflammation, and fever.
Opioids
- Receptors opioids mainly bind to: mu, kappa, and delta receptors.
- Prototype receptor mu agonist: morphine.
- Structure of morphine: exhibits a high degree of stereoselectivity of analgesic activity.
- Physiochemical property of morphine: has a high lipophilicity.
Acetaminophen
- Primary metabolite of acetaminophen in children: glucuronide.
- Mechanism of action of acetaminophen: inhibits COX-3, leading to the inhibition of prostaglandin synthesis.
- Predominant form of acetaminophen at physiological pH: anionic form.
Test your knowledge on the pathophysiology of inflammation and the causes of an inflammatory response. Learn about the immune system's protective response to infectious agents, noxious chemicals, thermal or physical trauma, and more. Explore the recognition of damage- and pathogen-associated molecules by immune surveillance cells.
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