Medical Pharmacology Practice Questions: Chapter 33-34 Protein Tyrosine Kinase Inhibitors of EGFR: Afatinib (Gilotrif)

Nursing Cancer Chemotherapy Pharmacology Practice Questions: Chapter 33-34 Protein Tyrosine Kinase Inhibitors of EGFR: Afatinib (Gilotrif)

Afatinib (Gilotrif) drug classification:
1. Good bioavailability
2. Reversible inhibitor of EGFR (HER1) and HER2 receptor kinases.
3. Both
4. Neither
Afatinib is considered a highly selective tyrosine kinase inhibitor.
1. True
2. False
Afatinib:
1. Inhibits tyrosine kinase autophosphorylation irreversibly
2. Reduces (downregulates) ERbB signaling.
3. Both
4. Neither
Some EGFR mutations:
1. Are associated with increased receptor autophosphorylation.
2. Increased receptor autophosphorylation may cause receptor activation possibly without ligand binding.
3. Both
4. Neither
Afatinib (Gilotrif) pharmacodynamic/pharmacokinetics:
1. Elimination half-time is about a day and a half after repetitive dosing in cancer patients.
2. Reduced dosing is appropriate in patients with substantial renal disease with impairment.
3. Both
4. Neither
Afatinib:
1. Is a substrate for Pgp.
2. Coadministration of drugs which modulate Pgp can change the effective drug levels of afatinib.
3. Both
4. Neither
Afatinib pharmacokinetics/pharmacodynamics.
1. Extensive protein binding
2. Limited enzymatic metabolism.
3. Excretion mainly in feces (85%) and urine (4%), primarily as unchanged drug.
4. A & B
5. B & C
6. A & C
7. A, B & C
Principal use/uses therapeutically for Afatinib:
1. First-line treatment for metastatic non-small cell lung cancer (NSCLC) with the EGFR mutation present.
2. Appropriate for patients with nonsquamous NSCLC exhibiting progression after platinum-based chemotherapy.
3. Both
4. Neither
Most common adverse effects/effects associated with afatinib administration:
1. Diarrhea
2. Skin rash
3. Both
4. Neither
Afatinib and pregnancy:
1. "Afatinib may cause fetal harm if used during pregnancy."
2. Women with reproductive potential should use highly efficacious contraceptive measures during therapy and continue measures for at least two weeks following last afatinib dosage.
3. Both
4. Neither