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Questions and Answers
Which of the following is a pharmacological action of aspirin?
Which of the following is a pharmacological action of aspirin?
- Increased reabsorption of chloride
- Inhibition of PG-induced secretion of renin
- Promotion of hyperkalemia
- Inhibition of antigen-antibody reactions (correct)
What is the mechanism of action of aspirin?
What is the mechanism of action of aspirin?
- Stabilization of capillary permeability
- Formation of 15-epi-lipoxins
- Inhibition of COX-1 and COX-2 activity (correct)
- Acetylation of COX-2 leading to anti-inflammatory actions
Which of the following is a shared use of NSAIDs?
Which of the following is a shared use of NSAIDs?
- Induction of labor
- Prevention of postpartum hemorrhage
- Management of musculoskeletal pain (correct)
- Treatment of hypertension
What is the effect of NSAIDs on renal function in patients with congestive heart failure?
What is the effect of NSAIDs on renal function in patients with congestive heart failure?
Which of the following is a shared drug interaction with NSAIDs?
Which of the following is a shared drug interaction with NSAIDs?
What is the effect of salicylates on body temperature?
What is the effect of salicylates on body temperature?
Which of the following is a pharmacokinetic property of salicylates?
Which of the following is a pharmacokinetic property of salicylates?
What is the distribution of salicylates in the body?
What is the distribution of salicylates in the body?
What is the effect of chronic use of high doses of NSAIDs?
What is the effect of chronic use of high doses of NSAIDs?
What is the plasma half-life of salicylate after a large dose?
What is the plasma half-life of salicylate after a large dose?
Which of the following is NOT a cause of inflammation?
Which of the following is NOT a cause of inflammation?
Which of the following is a chemical mediator of inflammation?
Which of the following is a chemical mediator of inflammation?
What is the process of inflammation characterized by?
What is the process of inflammation characterized by?
Which of the following can cause fever?
Which of the following can cause fever?
What triggers the initial phase of the thermoregulatory response?
What triggers the initial phase of the thermoregulatory response?
Which of the following is NOT a chemical mediator of inflammation?
Which of the following is NOT a chemical mediator of inflammation?
What are the damage- and pathogen-associated molecules recognized by cells charged with immune surveillance?
What are the damage- and pathogen-associated molecules recognized by cells charged with immune surveillance?
Which of the following is an immunologic mediator of inflammation?
Which of the following is an immunologic mediator of inflammation?
What is the immune system's protective response to injurious stimulus called?
What is the immune system's protective response to injurious stimulus called?
Which of the following is NOT a consequence of chronic inflammation?
Which of the following is NOT a consequence of chronic inflammation?
Which enzyme is involved in the induction of cyclooxygenase (COX-2) during the late phase response?
Which enzyme is involved in the induction of cyclooxygenase (COX-2) during the late phase response?
Which receptors does PGE2 act on to trigger the hypothalamus to elevate body temperature?
Which receptors does PGE2 act on to trigger the hypothalamus to elevate body temperature?
Which of the following is NOT a stimulus that can activate nociceptors?
Which of the following is NOT a stimulus that can activate nociceptors?
Which neuropeptides may be involved in the generation of pain?
Which neuropeptides may be involved in the generation of pain?
Which prostaglandins reduce the threshold of stimulation of nociceptors leading to peripheral sensitization?
Which prostaglandins reduce the threshold of stimulation of nociceptors leading to peripheral sensitization?
Which tissues are commonly affected by rheumatoid arthritis (RA)?
Which tissues are commonly affected by rheumatoid arthritis (RA)?
What is the first joint tissue affected in rheumatoid arthritis?
What is the first joint tissue affected in rheumatoid arthritis?
What is the mechanism of action of non-selective NSAIDs?
What is the mechanism of action of non-selective NSAIDs?
What is the shared pharmacological action of NSAIDs on the cardiovascular system?
What is the shared pharmacological action of NSAIDs on the cardiovascular system?
What is the side effect of NSAIDs on the gastric mucosa?
What is the side effect of NSAIDs on the gastric mucosa?
Which of the following NSAIDs has the longest half-life?
Which of the following NSAIDs has the longest half-life?
Which NSAID is 20 times more potent than aspirin in inhibiting COX?
Which NSAID is 20 times more potent than aspirin in inhibiting COX?
Which NSAID directly inhibits leukocyte function?
Which NSAID directly inhibits leukocyte function?
Which NSAID causes less severe gastrointestinal effects than aspirin?
Which NSAID causes less severe gastrointestinal effects than aspirin?
Which NSAID is a ketone prodrug converted to an active metabolite in the liver?
Which NSAID is a ketone prodrug converted to an active metabolite in the liver?
Which NSAID has a preferential activity against COX-2?
Which NSAID has a preferential activity against COX-2?
Which NSAID is the only FDA approved drug in the COX-2 selective inhibitors class?
Which NSAID is the only FDA approved drug in the COX-2 selective inhibitors class?
Which of the following is a non-selective NSAID?
Which of the following is a non-selective NSAID?
What is the primary respiratory effect of salicylates in medium to large doses?
What is the primary respiratory effect of salicylates in medium to large doses?
What is the compensatory response to the initial respiratory alkalosis caused by therapeutic doses of salicylates?
What is the compensatory response to the initial respiratory alkalosis caused by therapeutic doses of salicylates?
What is the mechanism of increased O2 consumption and CO2 production in skeletal muscle caused by salicylates?
What is the mechanism of increased O2 consumption and CO2 production in skeletal muscle caused by salicylates?
What is the effect of salicylates on plasma CO2 tension (PCO2) in anti-inflammatory doses?
What is the effect of salicylates on plasma CO2 tension (PCO2) in anti-inflammatory doses?
What is the shared side effect of non-selective NSAIDs on the gastric mucosa?
What is the shared side effect of non-selective NSAIDs on the gastric mucosa?
What is the effect of salicylates on acid-base and electrolyte balance?
What is the effect of salicylates on acid-base and electrolyte balance?
Which of the following is a characteristic of salicylism, a mild form of salicylate intoxication?
Which of the following is a characteristic of salicylism, a mild form of salicylate intoxication?
Which of the following is a consequence of salicylate-induced sweating and hyperventilation?
Which of the following is a consequence of salicylate-induced sweating and hyperventilation?
What is the reversible hepatic injury caused by large doses of salicylates called?
What is the reversible hepatic injury caused by large doses of salicylates called?
What is the effect of a single dose of aspirin on bleeding time in normal individuals?
What is the effect of a single dose of aspirin on bleeding time in normal individuals?
What is the primary mechanism of gastric damage caused by salicylates?
What is the primary mechanism of gastric damage caused by salicylates?
What is the effect of low doses of salicylates on urate excretion?
What is the effect of low doses of salicylates on urate excretion?
What are the neurological effects of high doses of salicylates?
What are the neurological effects of high doses of salicylates?
Which of the following is an inhibitor of Janus kinase?
Which of the following is an inhibitor of Janus kinase?
Which of the following is a common side effect of hydroxychloroquine?
Which of the following is a common side effect of hydroxychloroquine?
Which of the following is a disease-modifying anti-rheumatic drug (DMARD) used as monotherapy or in combination with methotrexate?
Which of the following is a disease-modifying anti-rheumatic drug (DMARD) used as monotherapy or in combination with methotrexate?
Which cytokines are involved in the pathogenesis of rheumatoid arthritis?
Which cytokines are involved in the pathogenesis of rheumatoid arthritis?
Which of the following drugs can decrease signs and symptoms of rheumatoid arthritis, reduce structural damage progression, and improve physical conditions of patients?
Which of the following drugs can decrease signs and symptoms of rheumatoid arthritis, reduce structural damage progression, and improve physical conditions of patients?
Which of the following is a common side effect associated with rheumatoid arthritis therapy?
Which of the following is a common side effect associated with rheumatoid arthritis therapy?
Which of the following is an immunomodulatory drug that inhibits the activity of autoimmune lymphocytes?
Which of the following is an immunomodulatory drug that inhibits the activity of autoimmune lymphocytes?
Which of the following is a shared side effect of methotrexate and leflunomide?
Which of the following is a shared side effect of methotrexate and leflunomide?
Which of the following is a recombinant monoclonal antibody used to reduce signs and symptoms of moderate to severe rheumatoid arthritis?
Which of the following is a recombinant monoclonal antibody used to reduce signs and symptoms of moderate to severe rheumatoid arthritis?
Which enzyme is inhibited by non-selective NSAIDs?
Which enzyme is inhibited by non-selective NSAIDs?
Which type of NSAIDs is more selective in inhibiting COX-2?
Which type of NSAIDs is more selective in inhibiting COX-2?
Which NSAID is commonly used as an opioid-sparing agent in certain acute trauma cases?
Which NSAID is commonly used as an opioid-sparing agent in certain acute trauma cases?
Which NSAID has the brand name 'Celebrex'?
Which NSAID has the brand name 'Celebrex'?
Which NSAID has the generic name 'Naprosyn'?
Which NSAID has the generic name 'Naprosyn'?
Which NSAID is commonly known as 'Motrin' and 'Advil'?
Which NSAID is commonly known as 'Motrin' and 'Advil'?
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?
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?
Which of the following alkaloids is represented in the highest percentage in opium?
Which of the following alkaloids is represented in the highest percentage in opium?
Which of the following receptors do opioids mainly bind to in order to control pain and pleasurable and addictive behavior?
Which of the following receptors do opioids mainly bind to in order to control pain and pleasurable and addictive behavior?
Which of the following is the prototype receptor mu agonist?
Which of the following is the prototype receptor mu agonist?
Which of the following is the structure of morphine that exhibits a high degree of stereoselectivity of analgesic?
Which of the following is the structure of morphine that exhibits a high degree of stereoselectivity of analgesic?
Which of the following is a physiochemical property of morphine?
Which of the following is a physiochemical property of morphine?
Which of the following is NOT a characteristic of COX-1?
Which of the following is NOT a characteristic of COX-1?
Which of the following is a characteristic of COX-2 selective NSAIDs?
Which of the following is a characteristic of COX-2 selective NSAIDs?
What is the predominate form of acetaminophen (pKa,9.7) at physiological pH?
What is the predominate form of acetaminophen (pKa,9.7) at physiological pH?
What is the primary metabolite of acetaminophen in children?
What is the primary metabolite of acetaminophen in children?
What is the primary mechanism of action of diclofenac?
What is the primary mechanism of action of diclofenac?
What is the bioavailability of diclofenac on oral administration?
What is the bioavailability of diclofenac on oral administration?
Which is the most active isomeric form of the opioid receptor?
Which is the most active isomeric form of the opioid receptor?
Which conformation is 10 times more potent than the B/C trans conformation?
Which conformation is 10 times more potent than the B/C trans conformation?
What is the pharmacophore for opioid analgesic activity?
What is the pharmacophore for opioid analgesic activity?
What is the precursor for heroin, hydromorphone, and oxymorphone?
What is the precursor for heroin, hydromorphone, and oxymorphone?
What is the 3,6 diacetylated form of morphine?
What is the 3,6 diacetylated form of morphine?
What is the enzyme responsible for the O-demethylation of codeine?
What is the enzyme responsible for the O-demethylation of codeine?
Which enzyme is responsible for the metabolism of diclofenac to its major metabolite via CYP3A4?
Which enzyme is responsible for the metabolism of diclofenac to its major metabolite via CYP3A4?
What is the major metabolite of diclofenac formed via CYP3A4?
What is the major metabolite of diclofenac formed via CYP3A4?
Which enzyme is responsible for the formation of 5’-hydroxy, 3’-hydroxy, and 4’,5’-dihydroxy metabolites of diclofenac?
Which enzyme is responsible for the formation of 5’-hydroxy, 3’-hydroxy, and 4’,5’-dihydroxy metabolites of diclofenac?
What percentage of the dose of diclofenac is excreted as the 4’-hydroxy derivative?
What percentage of the dose of diclofenac is excreted as the 4’-hydroxy derivative?
What is the preferred conformation of the N-p-chlorobenzoyl group in indomethacin?
What is the preferred conformation of the N-p-chlorobenzoyl group in indomethacin?
Which enzyme is responsible for the 5-O-demethylation of indomethacin?
Which enzyme is responsible for the 5-O-demethylation of indomethacin?
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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.
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