Pharmacology Notes

Basic Immune System Components

• T cells: Kill infected cells or activate other immune cells.
• B cells: Produce antibodies.
• Macrophages: Can either invoke

Prototype Immunosuppressant Drugs

• Cyclosporin
• Tacrolimus
  • Can be given PO or IV.
  • Oral preparation: immediate release or extended release.

Nursing Care Considerations for Immunosuppressants

• Monitor drug levels to ensure they are within the therapeutic range.
• Emphasize the importance of adherence to the medication regimen.
  • Missing doses increases the risk of organ rejection.
  • Consistent medication levels are needed to suppress the immune system and prevent rejection.
• Instruct patients to report any signs of infection, such as fever.
  • Important because immunosuppressants can mask typical infection symptoms.
• Advise patients to avoid live vaccines.
  • Live vaccines can cause infection in immunocompromised individuals.
• Regular laboratory monitoring:
  • Kidney function.
  • Liver function.
  • Drug levels (if applicable).

Anti-Inflammatory Drugs: General Information

• Reduce inflammation

Anti-Inflammatory Drugs: GI Effects

• Gastric distress, heartburn, nausea, bleeding.
• Can be reduced by taking medication with food or a full glass of water.
• Aspirin:
  • Intermittent use: small risk of bleeding.
  • Daily use: cumulative blood loss can cause anemia.
  • Caution with other anticoagulants (warfarin, Coumadin).
    • Increased risk of bleeding and ulcerations.
  • Alcohol: Increases the risk of gastric bleeding.

Aspirin Precautions

• Avoid in children due to the risk of Reye's syndrome.
  • Reye's syndrome: Encephalopathy and fatty liver degeneration.
• Caution with other anticoagulants: increased bleeding risk.

Ibuprofen

• Antiplatelet effect: increases bleeding risk.
• Use for dysmenorrhea (painful menstruation).
  • Works by inhibiting COX enzymes.
• Drug interactions:
  • Can decrease the impact

Acetaminophen (Tylenol)

• Primary uses: analgesic and antipyretic.
• Not effective as an anti-inflammatory or anti-rheumatic.
• No risk of Reye's syndrome.
• Risk of hepatic failure, coma, and death with long-term high-dose use.
• Treatment:
  • Signs and symptoms of liver damage.

Pediatric Considerations for OTC Analgesics

• Aspirin is contraindicated in children due to the risk of Reye's syndrome.
• Ibuprofen and acetaminophen are available in children's formulations.

Immunosuppression: Adverse Effects

• Increased risk of infection.
• Thinning of the skin.
• Decreased bone density.
• Impaired growth in children.
• Suppression of the HPA axis.

Glucocorticoids

• Effective for relieving a gouty attack.
  • Start with NSAIDs; if ineffective, use glucocorticoids.
• Cushing's syndrome:
  • Prolonged exposure to high levels of cortisol.
  • Can be caused by prolonged steroid use (iatrogenic Cushing's).
  • Typical symptoms.
• Injury to rapidly dividing cells.
• Suppression of bone marrow function: decreases in all types of blood cells.
  • Caution in patients with hematologic disorders.

Colchicine

• PGP (P-glycoprotein) transporter protein can reduce serum drug levels, leading to an increase in colchicine.
• CYP3A4 inhibitors (ketoconazole, clarithromycin, HIV protease inhibitors) increase colchicine levels.

Uric Acid Lowering Agents for Gout

• Inhibit uric acid formation.
• Increase uric acid excretion (probenecid and proglutase).

Methotrexate

• Gold standard for rheumatoid arthritis (RA) treatment.
• Prevents long-term disability in RA patients.
• Folate antagonist: necessary for DNA synthesis and cellular replication.
• Mechanism of action in RA is not fully understood.
  • Appears to be from immunosuppression secondary to reducing B and T lymphocyte activity.
• Screen for infectious profiles (HIV, hepatitis B, hepatitis C) before starting treatment.
• Monitoring during treatment: CBC.
• Prevents joint destruction and can stop or partially reverse joint disruptions in RA patients.
• Also used for psoriasis, cancer chemotherapy.