Pharmacology Chapter 16 Flashcards

Aspirin (Ecotrin)

• Classification: Salicylate
• Mechanism of Action: Inhibits synthesis of prostaglandins, blocking inflammation and pain transmission centrally and peripherally.
• Pharmacokinetics: Administered orally (PO) or rectally (PR).
• Indications:
  • Alleviates mild to moderate pain (analgesic) and fever (antipyretic).
  • Inhibits platelet aggregation to prevent blood clots; beneficial in cardiac diseases.
  • Low doses manage ischemic strokes, transient ischemic attacks, angina, and acute myocardial infarction (MI).
• Contraindications:
  • Allergies to salicylates or NSAIDs.
  • Conditions like bleeding abnormalities and renal impairment.
  • In children/teenagers with viral infections, it risks Reye syndrome.
  • Should be avoided during pregnancy and lactation.
• Adverse Effects:
  • Gastrointestinal discomfort, potential ulcers and bleeding.
  • Acute toxicity symptoms: tachypnea, confusion, seizures, and cardiovascular collapse.
  • Chronic use can lead to salicylism causing dizziness and tinnitus.
• Interactions: Increased risk of bleeding when combined with other blood-thinning medications.

NSAIDs (Non-Steroidal Anti-Inflammatory Drugs)

• Mechanism of Action: Block COX-1 and COX-2 enzymes, reducing prostaglandin formation in the central and peripheral nervous systems.

Selective NSAIDs

• Block only COX-2, minimizing gastric and renal side effects, while still addressing pain and inflammation.

Non-Selective NSAIDs

• Inhibit both COX enzymes, resulting in anti-inflammatory and analgesic effects; also possess anti-platelet properties.

• Pharmacokinetics: Administered orally (PO) or intravenously (IV).

• Contraindications:

  • Allergies to NSAIDs or salicylates, and avoid specific NSAIDs like celecoxib in sulfonamide allergies.
  • Contraindicated in heart failure, hypertension, and peptic ulcers.
  • Use with caution in individuals with renal or hepatic dysfunction, and avoid in children under six months.

• Adverse Effects:

  • Gastrointestinal issues such as nausea and GI bleeding; should be taken with food.
  • Risk of hypertension and kidney dysfunction.
  • Asthma patients may experience bronchoconstriction.
  • Black box warnings for increased cardiovascular and gastrointestinal risks; not recommended after coronary bypass surgery.

• Interactions: Increased bleeding risk when combined with other medications and underlying kidney dysfunction.

Prototypes of NSAIDs

• Ibuprofen (Advil) - non-selective, propionic acid derivative with analgesic, anti-inflammatory, and antipyretic properties.
• Celecoxib (Celebrex) - selective NSAID with similar therapeutic benefits but potentially fewer gastrointestinal side effects.

Non-NSAIDs

• Key Prototypes:
  • Acetaminophen (Tylenol)
  • Ofirmev (IV)
• Classification: Non-NSAIDs.