Pharmacology: Analgesics and NSAIDs

Questions and Answers

What is the primary mechanism of action of nonsteroidal anti-inflammatory drugs (NSAIDs)?

They work by directly binding to pain receptors in the nervous system, thus reducing pain signals.

They act by inhibiting the production of prostaglandins, specifically through blocking cyclooxygenase (COX) enzymes. (correct)

They increase the production of endorphins, which naturally block pain signals.

They act as antipyretics by reducing the body's temperature set point in the hypothalamus.

Which of the following is a potential adverse effect associated with the use of NSAIDs?

Increased risk of gastrointestinal bleeding.

Suppression of the immune system.

Increased risk of allergic reactions.

All of the above. (correct)

What is the main indication for using NSAIDs?

Prevention of blood clots.

Treatment of bacterial infections.

Treatment of mild to moderate pain. (correct)

Treatment of severe pain.

Which of the following drugs is classified as a selective COX-2 inhibitor?

Celecoxib Signup and view all the answers

What is the main difference between nonselective COX inhibitors and selective COX-2 inhibitors?

Nonselective COX inhibitors block both COX-1 and COX-2 enzymes, while selective COX-2 inhibitors only block COX-2. Signup and view all the answers

Which of the following NSAIDs is also an antipyretic?

Paracetamol (Acetaminophen) Signup and view all the answers

Which of the following is a common drug interaction associated with NSAIDs?

All of the above. Signup and view all the answers

Which of the following NSAIDs is classified as a propionic acid derivative?

Ibuprofen Signup and view all the answers

What is the mechanism of action of nonselective COX inhibitors?

Inhibition of cyclooxygenase enzymes Signup and view all the answers

Which adverse effect is least commonly associated with NSAIDs?

Hepatic failure Signup and view all the answers

Which of the following is a common adverse effect associated with nonselective COX inhibitors?

Gastric mucosal damage Signup and view all the answers

What is an indication for the use of selective COX-2 inhibitors?

Treatment of inflammatory conditions Signup and view all the answers

What is a pharmacodynamic interaction of NSAIDs?

Decreased efficacy of β blockers Signup and view all the answers

Which shared toxicity may result from both nonselective COX and COX-2 inhibition?

Delay/prolongation of labour Signup and view all the answers

Which of the following is an adverse effect related to renal function for NSAID use?

Papillary necrosis Signup and view all the answers

What is NOT a potential adverse effect of NSAIDs?

Gastroparesis Signup and view all the answers

How do nonselective COX inhibitors differ from selective COX-2 inhibitors regarding antiplatelet effects?

Nonselective COX inhibitors inhibit platelet aggregation Signup and view all the answers

Which type of drug interaction occurs with sulfonylureas and NSAIDs?

Competitive inhibition Signup and view all the answers

What distinguishes the renal effect of nonselective COX inhibitors from that of selective COX-2 inhibitors?

Selective COX-2 inhibitors limit renal blood flow Signup and view all the answers

Aspirin sensitive asthma can be precipitated by which of the following?

Ibuprofen Signup and view all the answers

Which adverse effect is primarily related to gastrointestinal complications associated with NSAIDs?

Peptic ulceration Signup and view all the answers

Which of the following correctly defines a characteristic of COX-2 inhibitors?

Target primarily inflammation pathways Signup and view all the answers

Study Notes

Nonsteroidal Antiinflammatory Drugs (NSAIDs) and Antipyretic-Analgesics

Analgesics relieve pain by targeting central or peripheral pain mechanisms without significantly affecting consciousness.
They address pain symptoms without altering the underlying cause, often used alongside other treatments like antibiotics for conditions such as apical tooth abscesses.
Analgesics are categorized into two primary groups:
- Opioid (narcotic/morphine-like) analgesics
- Nonopioid (non-narcotic/antipyretic) analgesics or NSAIDs.

Classification of NSAIDs

Nonselective COX Inhibitors: Inhibit cyclooxygenase enzymes indiscriminately.
Selective COX-2 Inhibitors: Target the COX-2 enzyme specifically, aiming to reduce inflammation with fewer gastrointestinal effects.
Analgesic-antipyretics with Poor Anti-inflammatory Action: Example includes Paracetamol (Acetaminophen).

Examples of NSAIDs

Salicylates: Aspirin
Enolic Acid Derivatives:
- Nimesulide
- Diclofenac
Propionic Acid Derivatives:
- Ibuprofen
Acetic Acid Derivatives:
- Meloxicam
- Etodolac
COX-2 Inhibitors:
- Celecoxib
- Etoricoxib

Adverse Effects of NSAIDs

CNS: Headache, confusion, vertigo, seizures, and behavioral disturbances.
CVS: Increased blood pressure and risk of myocardial infarction (notably with COX-2 inhibitors).
Hepatic: Potential for raised transaminases and, in rare cases, hepatic failure.
Renal: Risks include sodium and water retention, and chronic renal failure.
Gastrointestinal: Nausea, gastric irritation, peptic ulcers, and possible bleeding.
Hematological: Includes bleeding risks, thrombocytopenia, and agranulocytosis.
Others: Asthma exacerbation, skin rashes, and angioedema.

Drug Interactions with NSAIDs

Pharmacodynamic Interactions:
- Diuretics: Decreased diuresis effect.
- β-blockers and ACE inhibitors: Reduced antihypertensive efficacy.
- Anticoagulants: Increased risk of gastrointestinal bleeding.
Pharmacokinetic Interactions:
- Interaction with drugs like phenytoin leading to competition during metabolism.

Features of COX Inhibitors

Nonselective COX Inhibitors:
- Provide analgesic, antipyretic, and anti-inflammatory effects.
- Increase the risk of gastric mucosal damage and renal issues.
Selective COX-2 Inhibitors:
- Offer analgesic and antipyretic effects with lesser gastrointestinal side effects.
- Do not inhibit platelet aggregation.

Shared Toxicities of NSAIDs

Gastric mucosal damage and increased bleeding due to inhibition of platelet function.
Renal blood flow limitations leading to fluid retention.
Potential for delaying labor and increased risk of asthma or allergic reactions in sensitive individuals.

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Description

Learn about analgesics, their mechanisms, and types, including opioid and nonopioid analgesics, as well as their uses in treating pain symptoms.