This set of Drug Biotechnology Multiple Choice Questions & Answers (MCQs) focuses on “Drug Addiction and Abuse – NSAIDs – 2”.
1. Which is the predominant form of cyclooxygenase enzyme?
a) COX 1
b) COX 2
c) COX 3
d) COX 4
View Answer
Explanation: The key enzyme in the cyclooxygenase pathway is the enzyme cyclooxygenase (COX). There are two forms of cyclooxygenase, COX1 (the predominant form) and COX2. NSAIDs inhibit prostaglandin and thromboxane synthesis, they are potent inhibitors of cyclooxygenase and eliminate all prostaglandins and thromboxanes in every cell they reach.
2. How does NSAIDs work?
a) Inhibit arachidonic acid
b) Inhibit Endoperoxide intermediate
c) Inhibit Prostaglandin and thromboxane synthesis
d) Inhibit cyclooxygenase
View Answer
Explanation: All NSAIDs inhibit the cyclooxygenase required for the conversion of arachidonic acid to endoperoxide intermediate (PGG2 and PGH2). NSAIDs inhibit prostaglandin and thromboxane synthesis, they are potent inhibitors of cyclooxygenase and eliminate all prostaglandins and thromboxanes in every cell they reach. The key enzyme in the cyclooxygenase pathway is the enzyme cyclooxygenase (COX). There are two forms of cyclooxygenase, COX1 (the predominant form) and COX2.
3. Which of the following has a half-life of 45 Hrs?
a) Piroxicam
b) Phenylbutazone
c) Ibuprofen
d) Indomethacin
View Answer
Explanation: Phenylbutazone a pyrazolone derivative is a powerful anti-inflammatory drug but its usefulness is limited by its toxicity chiefly short-term therapy. Piroxicam has a half-life of 45 hours and thus can be administered once a day but it can show some GI disturbance. Ibuprofen is a propionic acid derivative has the same potency as acetyl Salicylate but better tolerated (fewer side effects). Indomethacin is an indole derivative more potent than ASA but inferior at doses tolerated by rheumatoid arthritis patients, quite toxic.
4. Which of the following has the same potency as ASA and better tolerated by patients?
a) Piroxicam
b) Phenylbutazone
c) Ibuprofen
d) Indomethacin
View Answer
Explanation: Ibuprofen is a propionic acid derivative has the same potency as acetyl Salicylate but better tolerated since it has fewer side effects. Thus most of the times ibuprofen is mostly prescribed. Indomethacin is an indole derivative more potent than ASA but inferior at doses tolerated by rheumatoid arthritis patients, quite toxic.
5. Which of the following cannot be tolerated, rheumatoid arthritis patient?
a) Piroxicam
b) Phenylbutazone
c) Ibuprofen
d) Indomethacin
View Answer
Explanation: Phenylbutazone is a powerful anti-inflammatory drug. Piroxicam has a half-life of 45 hours and thus can be administered once a day. Ibuprofen is a propionic acid derivative has the same potency as acetyl Salicylate but better tolerated. Indomethacin is an indole derivative more potent than ASA but inferior at doses tolerated by rheumatoid arthritis patients, quite toxic.
6. Which of the following pyrazolone derivative’s has toxic side effects?
a) Piroxicam
b) Phenylbutazone
c) Ibuprofen
d) Indomethacin
View Answer
Explanation: Phenylbutazone a pyrazolone derivative is a powerful anti-inflammatory drug but its usefulness is limited by its toxicity chiefly short-term therapy. Piroxicam has a half-life of 45 hours and thus can be administered once a day but it can show some GI disturbance. Ibuprofen is a propionic acid derivative has the same potency as acetyl Salicylate but better tolerated (fewer side effects). Indomethacin is an indole derivative more potent than ASA but inferior at doses tolerated by rheumatoid arthritis patients it becomes toxic for these patients.
7. Which of the following is a pro-drug and related to indomethacin?
a) Piroxicam
b) Phenylbutazone
c) Sulindac
d) Indomethacin
View Answer
Explanation: Sulindac is an inactive pro-drug closely related to indomethacin. It must be metabolized by hepatic microsomal enzymes to an active form. It has a long duration of action (half-life = 8h). The adverse effects are less severe than other NSAIDs (ex. GI and renal). Indomethacin is an indole derivative more potent than ASA but inferior at doses tolerated by rheumatoid arthritis patients, quite toxic.
8. Which of the following is also known as “housekeeping enzyme”?
a) COX 1
b) COX 2
c) COX 3
d) COX 4
View Answer
Explanation: Cyclooxygenase-1 (COX-1) constitutively expressed in a wide variety of cells all over the body and thus known as “housekeeping enzyme” e.g. Gastric cytoprotection. Cyclooxygenase-2 (COX-2), inducible enzyme an immediate-early gene product in inflammatory and immune cells it is dramatically up-regulated during inflammation.
9. Which of the following responsible for inflammatory response mainly?
a) COX 1
b) COX 2
c) COX 3
d) COX 4
View Answer
Explanation: Cyclooxygenase-1 (COX-1) constitutively expressed in a wide variety of cells all over the body and thus known as “housekeeping enzyme” e.g. Gastric cytoprotection. Cyclooxygenase-2 (COX-2), inducible enzyme an immediate-early gene product in inflammatory and immune cells it is dramatically up-regulated during inflammation.
10. Why there are side effects of NSAIDs?
a) Inhibition of COX 1
b) Inhibition of COX 2
c) Inhibition of COX 3
d) Inhibition of COX 4
View Answer
Explanation: Cyclooxygenase-1 (COX-1) is expressed in a wide variety of cells all over the body and known as “housekeeping enzyme” e.g. Gastric cytoprotection. Cyclooxygenase-2 (COX-2), inducible enzyme an immediate-early gene product in inflammatory and immune cells it is dramatically up-regulated during inflammation. Adverse effects of NSAIDs are theorized to be due to inhibition of COX-1 (ex. GI complications via decreased PGE2 and potentially altered blood flow).
11. Which of the following has the least GI effect and derived from parent NSAIDs?
a) Piroxicam
b) Phenylbutazone
c) NO-NSAIDs
d) Indomethacin
View Answer
Explanation: Nitric oxide-releasing NSAIDs. It has fewer GI effects than parent NSAID from which they are derived. It has a comparable anti-inflammatory effect and superior analgesic effect. The parent NSAID is Naproxen. The possible mechanism can be that nitric oxide improves gastric blood flow.
12. How does Eicosapentaenoic acid functions to decrease the inflammation rate?
a) Decrease Prostaglandin production
b) Don’t form prostaglandin
c) Induce the formation of prostaglandins at certain times
d) The prostaglandins, thromboxane produced from EPA are less active
View Answer
Explanation: EPA is found in fish oil. It acts as a substrate for cyclooxygenases and lipoxygenases thus it competing with arachidonic acid for the enzymes. The prostaglandins, thromboxanes, and leukotrienes produced from EPA are less active than AA metabolites. These products then compete with products of AA metabolism for shared target receptors.
13. Which of the following option will correct for the marked place?
a) Urate crystal
b) Interleukin-1
c) Mononuclear phagocytes
d) Prostaglandins
View Answer
Explanation: Synoviocytes phagocytose urate crystals and then secrete inflammatory mediators. These inflammatory mediators attract and activate polymorphonuclear leukocytes and mononuclear phagocytes. Drugs active in gout inhibit crystal phagocytosis and polymorphonuclear leukocytes and macrophage release of inflammatory mediators such as prostaglandin, interleukin, and leukotriene.
14. Macrophages with a high content of EPA produce less TNF and IL-l.
a) True
b) False
View Answer
Explanation: EPA is found in fish oil. It acts as a substrate for cyclooxygenases and lipoxygenases. The prostaglandins, thromboxanes, and leukotrienes produced from EPA are less active than AA metabolites. These products then compete with products of AA metabolism for shared target receptors. Macrophages with a high content of EPA produce less TNF and IL-l. Dietary EPA supplementation can reduce tissue injury due to PGs, TXs, LTs, and cytokines.
15. Which of the following option will correct for the marked place?
a) Urate crystal
b) Polymorphonuclear leukocytes
c) Mononuclear phagocytes
d) Prostaglandins
View Answer
Explanation: Synoviocytes phagocytose urate crystals found in the bones which then secrete inflammatory mediators. These inflammatory mediators attract and activate polymorphonuclear leukocytes and mononuclear phagocytes. Drugs inhibit crystal phagocytosis and polymorphonuclear leukocytes and macrophage release of inflammatory mediators such as prostaglandin, interleukin, and leukotriene.
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