Pharmacology: NSAIDs and COX Inhibitors Quiz

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Questions and Answers

What is the primary mechanism of action for COX-2 inhibitors?

  • Inhibiting the COX-1 enzyme
  • Blocking the COX-2 enzyme, thus reducing pain and inflammation (correct)
  • Increasing stomach acid secretion
  • Stimulating prostaglandin synthesis

Which of the following is a common adverse effect associated with aspirin use?

  • Hypoglycemia and pancytopenia
  • Hepatotoxicity and hepatic failure
  • Agranulocytosis and aplastic anemia
  • Gastric upset and gastrointestinal bleeding (correct)

Which of the following NSAIDs is described as having powerful anti-inflammatory effects but weak analgesic and antipyretic activities?

  • Phenylbutazone (correct)
  • Indomethacin
  • Ibuprofen
  • Mefenamic acid

Which enzyme is responsible for the gastrointestinal side effects associated with traditional NSAIDs?

<p>Cyclooxygenase-1 (COX-1) (C)</p> Signup and view all the answers

What is the primary mechanism through which most NSAIDs exert their anti-inflammatory and analgesic effects?

<p>Inhibition of prostaglandin biosynthesis (C)</p> Signup and view all the answers

A patient is experiencing an adverse reaction, exhibiting jaundice and skin eruptions, which drug is most suspect?

<p>Acetaminophen (B)</p> Signup and view all the answers

What is the key difference in the action between traditional NSAIDs and COX-2 inhibitors?

<p>Traditional NSAIDs block both COX-1 and COX-2, while COX-2 inhibitors primarily target COX-2. (C)</p> Signup and view all the answers

A patient experiences pain following a surgical procedure, which has lasted for 2 months. How would this type of pain be classified?

<p>Acute pain (B)</p> Signup and view all the answers

Which of the following is NOT a characteristic of non-narcotic analgesics?

<p>Potential for physical dependency (C)</p> Signup and view all the answers

Which of the following best describes autacoids?

<p>Locally acting hormone-like substances produced by various tissues (C)</p> Signup and view all the answers

Which of the following NSAIDs is frequently used to treat acute gout and acute rheumatoid arthritis when other agents have failed?

<p>Phenylbutazone (A)</p> Signup and view all the answers

What effect does aspirin have on platelet aggregation?

<p>It inhibits platelet aggregation (C)</p> Signup and view all the answers

What are prostaglandins derived from?

<p>20-carbon fatty acid (B)</p> Signup and view all the answers

Which enzyme is responsible for the synthesis of prostaglandins from arachidonic acid?

<p>Cyclooxygenase (COX) (B)</p> Signup and view all the answers

Which drug is considered an analgesic and antipyretic, but does not possess anti-inflammatory properties?

<p>Acetaminophen (C)</p> Signup and view all the answers

Which of the following is a common clinical use for Aspirin?

<p>To treat inflammation associated with joint pain (D)</p> Signup and view all the answers

Which of the following best describes the primary function of COX-I?

<p>Continuous synthesis of prostaglandins contributing to normal homeostasis. (B)</p> Signup and view all the answers

What is a primary function of autacoids?

<p>To modulate local circulation and influence inflammation (B)</p> Signup and view all the answers

Which of the following is NOT listed as an adverse effect of ibuprofen?

<p>Ulceration (A)</p> Signup and view all the answers

What effect does aspirin have on the time it takes for blood to clot?

<p>It prolongs the time it takes for blood to clot (C)</p> Signup and view all the answers

Which role is specific to thromboxane A2 (TXA2)?

<p>Platelet aggregation (D)</p> Signup and view all the answers

Which medication is associated with the adverse effects of agranulocytosis and aplastic anemia?

<p>Phenylbutazone (A)</p> Signup and view all the answers

How do autacoid antagonists work?

<p>By inhibiting the synthesis of certain autacoids or interfering with their receptor interactions. (B)</p> Signup and view all the answers

Which of the following is NOT a condition where chronic pain is commonly observed?

<p>Post-surgical recovery (B)</p> Signup and view all the answers

What is the primary mechanism of action of leukotriene antagonists?

<p>Competitive inhibition of leukotrienes at their receptor sites or inhibition of lipoxygenase. (C)</p> Signup and view all the answers

A patient who is allergic to aspirin and has a history of bleeding disorders is seeking an analgesic and antipyretic medication. Which of these drugs is most suitable?

<p>Acetaminophen (C)</p> Signup and view all the answers

Which of the following is an example of a COX-2 Inhibitor?

<p>Celecoxib (C)</p> Signup and view all the answers

Besides its analgesic and antipyretic effects, what is another notable property of aspirin?

<p>It has an anticoagulant and antiplatelet effect (B)</p> Signup and view all the answers

Which of the following is a major physiological function of leukotrienes?

<p>Bronchoconstriction (B)</p> Signup and view all the answers

Which of these symptoms is caused by histamine's direct action on the vascular system?

<p>Localized redness due to arteriole dilation (B)</p> Signup and view all the answers

What is the physiological origin of histamine?

<p>Dietary histidine (A)</p> Signup and view all the answers

Which of the following is most closely associated with the release of histamine?

<p>Inflammation and allergic reactions or hypersensitivity reactions (D)</p> Signup and view all the answers

Which of the following is NOT a primary effect of H1 receptor activation?

<p>Regulation of gastric acid secretion (A)</p> Signup and view all the answers

Antihistamines primarily work by:

<p>Blocking histamine from binding to receptor sites (A)</p> Signup and view all the answers

Which of these is NOT a common use for antihistamines?

<p>Treatment of bacterial infections (B)</p> Signup and view all the answers

Which characteristic is most indicative of first-generation antihistamines?

<p>Sedating (A)</p> Signup and view all the answers

Which of the following is a second generation antihistamine?

<p>Loratadine (B)</p> Signup and view all the answers

Which of the following is a common side effect associated with antihistamine use?

<p>Drowsiness (C)</p> Signup and view all the answers

What is the primary function theorized for the third histamine receptor?

<p>Autoreceptor function (B)</p> Signup and view all the answers

Which of these is NOT an effect of H1 receptor activation?

<p>Reduction in itching (A)</p> Signup and view all the answers

Which of the following is NOT a common side effect associated with first-generation antihistamines?

<p>Increased appetite (C)</p> Signup and view all the answers

What is the primary mechanism of action for H2-receptor antagonists?

<p>Inhibition of gastric acid secretion (C)</p> Signup and view all the answers

A patient experiences confusion while taking a medication; which of the following medications is most likely responsible?

<p>Cimetidine (B)</p> Signup and view all the answers

Which of the following best describes the difference in drug interactions between ranitidine and cimetidine?

<p>Ranitidine has fewer interactions with other drugs than cimetidine. (D)</p> Signup and view all the answers

What adverse effect is specifically associated with antihistamines, but not with H2-receptor antagonists based on the given text?

<p>Hypotension (B)</p> Signup and view all the answers

Flashcards

Inflammation

A natural response to tissue injury, usually caused by physical trauma, chemicals, or microbes.

NSAIDs (Nonsteroidal Anti-inflammatory Drugs)

A group of medications that reduce pain and inflammation by decreasing prostaglandin synthesis.

Pain

An unpleasant experience associated with actual or potential tissue damage.

Acute Pain

Pain lasting less than 3-6 months, varying in intensity.

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Chronic Pain

Pain lasting more than 6 months, ranging from mild to severe.

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Nonnarcotic analgesic

A medication that relieves pain without causing physical dependency, unlike narcotic analgesics.

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Aspirin (Acetylsalicylic Acid)

A well-known nonnarcotic analgesic with antipyretic, anti-inflammatory, and analgesic properties.

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Aspirin's effect on bleeding

Aspirin's ability to prolong bleeding time by inhibiting platelet aggregation.

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What is Aspirin?

Aspirin is a commonly used medication with analgesic, antipyretic, and anti-inflammatory properties. It reduces pain, fever, and inflammation. It is also used to prevent heart attacks and strokes in some individuals.

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What is Indomethacin?

Indomethacin is a nonsteroidal anti-inflammatory drug (NSAID) with potent anti-inflammatory, analgesic, and antipyretic effects. It is used to treat various inflammatory conditions like rheumatoid arthritis, osteoarthritis, and acute gout.

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What is Mefenamic Acid?

Mefenamic acid is an NSAID with analgesic, antipyretic, and anti-inflammatory properties. It is used for pain relief, including menstrual cramps, and can be helpful for musculoskeletal injuries.

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What is Phenylbutazone?

Phenylbutazone is a potent NSAID with a strong anti-inflammatory effect. It is used primarily for short-term treatment of acute gout and rheumatoid arthritis when other NSAIDs fail.

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What is Diclofenac?

Diclofenac is an NSAID with anti-inflammatory, analgesic, and antipyretic properties, often used to treat musculoskeletal pain and stiffness, including ankylosing spondylitis.

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What is Ibuprofen?

Ibuprofen is an NSAID with analgesic and anti-inflammatory properties, particularly strong for pain relief. It is used for arthritis, pain, and fever.

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What is Acetaminophen (Paracetamol)?

Acetaminophen (Paracetamol) is an analgesic and antipyretic drug, effective for pain and fever relief. It lacks significant anti-inflammatory properties. It is often preferred for those allergic to aspirin and who have bleeding disorders.

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What are NSAIDs?

NSAIDS (Nonsteroidal Anti-Inflammatory Drugs) are a group of medications used to reduce pain, fever, and inflammation. They work by inhibiting the production of prostaglandins, which are involved in these processes.

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COX-2 inhibitor

A type of nonsteroidal anti-inflammatory drug (NSAID) that specifically inhibits the COX-2 enzyme, responsible for pain and inflammation, while minimizing the inhibition of COX-1, which protects the stomach lining.

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Prostaglandins

Naturally-occurring fatty acids that regulate various bodily functions, including inflammation, blood clotting, and stomach acid production.

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Cyclooxygenase (COX)

The enzyme responsible for producing prostaglandins, which play a role in inflammation and pain.

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COX-1

One of the two forms of the COX enzyme, primarily involved in protecting the stomach lining and regulating blood clotting.

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COX-2

One of the two forms of the COX enzyme, primarily involved in triggering pain and inflammation.

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Autacoids

A class of compounds that act as local hormones or messengers, playing crucial roles in regulating inflammation, blood pressure, and other bodily processes.

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Autacoid antagonists

Substances that block the effects of autacoids by either inhibiting their production or interfering with their interaction with receptors.

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Prostanoic acid

A 20-carbon fatty acid containing a 5-carbon ring, serving as the precursor for various prostaglandins.

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What are prostaglandins?

Prostaglandins are a group of lipids that act as signaling molecules in the body. They are synthesized from arachidonic acid by the enzyme cyclooxygenase (COX).

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What is the role of COX-1?

COX-1 is constitutively expressed, meaning it's always present in the body and involved in daily production of prostaglandins. These contribute to normal homeostasis, like protecting the stomach lining.

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What is the role of COX-2?

COX-2 is induced by inflammation or injury. It produces prostaglandins that contribute to the inflammatory response.

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What is Thromboxane A2 (TXA2) and its role?

Thromboxane A2 (TXA2) is a type of prostaglandin responsible for causing blood platelets to clump together, which can help with blood clotting.

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What are leukotrienes and how are they produced?

Leukotrienes are another group of lipids made from fatty acids that have different roles than prostaglandins. They are produced by the enzyme lipoxygenase.

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What are Leukotriene antagonists?

Leukotriene antagonists are medications that block the action of leukotrienes. They either inhibit the enzyme that makes leukotrienes or block their receptors.

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What is Histamine?

Histamine is a chemical messenger that triggers various responses in the body, including allergic and inflammatory reactions. It's released in times of injury or during allergic reactions.

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What are Histamine antagonists?

Histamine antagonists are medications that block the effects of histamine by binding to its receptors. This action can help treat various symptoms caused by histamine, such as itching, swelling, or redness.

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Antihistamines

A group of medications that block the effects of histamine, a chemical released by the body in response to allergens.

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Sedating Antihistamines

A type of antihistamine that causes drowsiness and sedation, often used for sleep.

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Non-Sedating Antihistamines

A type of antihistamine that causes less drowsiness and fewer side effects.

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H2-receptor Antagonists

Medications that block histamine receptors in the stomach, reducing acid production.

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Cimetidine

A type of H2-receptor antagonist used to treat ulcers and heartburn.

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What are the roles of H1 and H2 histamine receptors?

Histamine receptors are responsible for initiating various bodily reactions. H1 receptors primarily affect areas like smooth muscles in the bronchi and intestines, blood vessels, and even contribute to itching sensations. H2 receptors play a crucial role in the regulation of gastric acid secretion.

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What are antihistamines and how do they work?

Antihistamines are medications used to counteract the effects of histamine on various organs and structures. They work by blocking histamine from binding to its receptors. This prevents histamine from causing its typical effects like inflammation, itching, and stomach acid secretion.

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Describe first-generation antihistamines.

First-generation antihistamines often have a sedative effect and are typically short-acting. They include drugs like chlorpheniramine, diphenhydramine, and promethazine.

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What are second-generation antihistamines?

Second-generation antihistamines are known for their longer duration of action and are generally non-sedating. They include drugs like loratadine, cetirizine, and fexofenadine.

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What are common side effects of antihistamines?

Common side effects of antihistamines include drowsiness, hallucinations, and sedation. These effects are more prevalent with first-generation antihistamines.

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What are some uses of antihistamines?

Antihistamines are widely used to manage various allergic conditions, including seasonal and perennial allergies, allergic rhinitis, allergic conjunctivitis, mild angioneurotic edema and urticaria, and allergic reactions to drugs, blood, or plasma. They can also be used to alleviate coughs related to colds or allergies, as adjunctive therapy in anaphylactic shock, and for other purposes like treating motion sickness or providing sedation.

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How are antihistamines categorized?

Antihistamines are categorized based on their generation and have varying characteristics like duration of action and sedative effects.

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How do antihistamines help manage allergies?

Antihistamines can effectively reduce the symptoms of seasonal and perennial allergies. They work by blocking histamine, a chemical released by the body during allergic reactions, from binding to its receptors.

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Study Notes

Non-Narcotic Analgesics, Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

  • Inflammation is a protective response to tissue injury (physical trauma, noxious chemicals, or microbes).
  • NSAIDs differ in mechanism from anti-inflammatory steroids or narcotic analgesics.
  • Most NSAIDs work by inhibiting prostaglandin biosynthesis.

Pain Definitions

  • Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage.
  • Acute pain lasts less than 3-6 months, ranging from mild to severe. Causes include postoperative, procedural, and traumatic pain.
  • Chronic pain lasts longer than 6 months, ranging from mild to severe. Associated conditions include cancer, AIDS, multiple sclerosis, sickle cell disease, and end-stage organ failure.

Anti-Inflammatory Drugs

  • Common NSAIDs include aspirin, diflunisal, diclofenac, etodolac, fenamates, fenoprofen, flurbiprofen, ibuprofen, indomethacin, ketoprofen, methylsalicylate, nabumetone, naproxen, oxaprazin, phenylbutazone, piroxicam, sulindac, and tolmetin.
  • COX-2 inhibitors include celecoxib.
  • Non-narcotic analgesics include acetaminophen and phenacetin.

Drugs for Arthritis, Gout, and COX-2 Inhibitors

  • Drugs for arthritis include chloroquine, gold salts, methotrexate, and D-penicillamine.
  • Drugs for gout include allopurinol, colchicine, probenecid, and sulfinpyrazone.

Prostaglandins

  • Prostaglandins are 20-carbon fatty acids with a 5-carbon ring, derived from arachidonic acid.
  • They are synthesized by cyclooxygenase (COX) enzymes, with COX-1 contributing to normal homeostasis, and COX-2 being involved primarily in inflammation and injury.
  • COX-2 inhibitors selectively inhibit the synthesis of prostaglandins associated with inflammation.

Leukotrienes

  • Leukotrienes are 20-carbon fatty acid derivatives formed by lipoxygenase.
  • They play a role in bronchoconstriction, mucus secretion, lymphocyte proliferation and differentiation, and heart negative inotropy.
  • Leukotriene antagonists, like zileuton, zafirlukast, and montelukast, are used in asthma treatment to reduce bronchospasm stemming from leukotriene-mediated responses.

Histamine and Antagonists

  • Histamine is a biogenic amine derived from histidine, which mediates various cellular responses (allergic and inflammatory).
  • Histamine acts on H1 and H2 receptors, affecting blood vessels, smooth muscle activity (bronchial and intestinal), capillary permeability, and pruritus.
  • H2 receptors are primarily related to gastric acid secretion.
  • Antihistamines block histamine receptor sites, decreasing allergic responses and inflammatory reactions.

H1 Antagonists

  • These drugs block the histamine effects on bronchial and intestinal smooth muscle, small blood vessels and sensory impulses for itching.

H2 Antagonists

  • H2-receptor antagonists inhibit gastric acid secretion in the body.
  • Drugs like cimetidine, ranitidine, and famotidine commonly fall into this category.

Antihistamine Uses, including Adverse Effects

  • Antihistamines are used to treat allergic symptoms, allergic reactions, coughs, anaphylactic shock, and parkinsonism.
  • Adverse effects can include drowsiness, hallucinations, sedation, and anticholinergic effects (dry mouth, throat, and nose).

Other Information

  • Aspirin is an antipyretic and anti-inflammatory analgesic, affecting platelet aggregation (clotting) time and risk of myocardial infarction, transient ischemic attacks, and strokes (primarily in men).
  • Indomethacin is a potent anti-inflammatory, antipyretic, and analgesic used in rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, and acute gout.
  • Mefenamic acid is an anti-inflammatory, analgesic, and antipyretic used in rheumatoid arthritis, soft tissue injury, and dysmenorrhea.
  • Phenylbutazone has a strong anti-inflammatory effect but a weak analgesic effect. It's for acute gout and rheumatoid arthritis.
  • Diclofenac is a potent anti-inflammatory, analgesic, and antipyretic used for ankylosing spondylitis and musculoskeletal injuries.
  • Ibuprofen is an anti-inflammatory analgesic more potent than aspirin and acetaminophen. It's used to treat arthritis and osteoarthritis.
  • Acetaminophen/Paracetamol is an analgesic and antipyretic drug with no anti-inflammatory activity. It's considered safer than aspirin for those with aspirin allergies. Adverse reactions include skin reactions and liver damage, especially with high doses.
  • COX-2 inhibitors (celecoxib, refecoxib) have anti-inflammatory and analgesic effects equal to other NSAIDs but with less gastric side effects.
  • Autacoids are hormone-like substances from diffuse tissues (e.g., prostaglandins, histamine, serotonin, angiotensins, kinins).

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