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

Medical Pharmacology Practice Questions: Protein Tyrosine Kinase Inhibitors of EGFR: Erlotinib (Tarceva)

Erlotinib (Tarceva) clinical use/uses:
1. Treatment of non-small cell lung cancer in certain patients.
2. Erlotinib may be used in combination with the DNA polymerase inhibitor (gemcitabine) as first-line treatment in advanced or metastatic pancreatic cancer.
3. Both
4. Neither
Erlotinib is classified as a reversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase.
1. True
2. False
The epidermal growth factor receptor (EGFR) is a tyrosine kinase.
1. True
2. False
Erlotinib (Tarceva):
1. Competitively inhibits ATP binding at the active site of EGFR.
2. Erlotinib competitively inhibits EGFR tyrosine kinase.
3. Both
4. Neither
Erlotinib pharmacodynamic/pharmacokinetics:
1. Erlotinib: about 60% absorbed following oral administration.
2. Plasma levels peak at about four hours following administration.
3. Erlotinib 1/2 for elimination is about a day and 1/2 (36 hours).
4. A & B
5. B & C
6. A & C
7. A, B, C (all choices are correct)
Primary site of erlotinib metabolism:
1. Peripheral hydrolases (plasma -esterases)
2. The liver: by means of the cytochrome P450 microsomal drug metabolizing system (primary isoforms: CYP3A4 and secondarily CYP1A2 and CYP1A1)
3. Both
4. Neither
Erlotinib in combination with gemcitabine may be used for treatment of patients with:
1. Locally advanced pancreatic cancer
2. Unresectable pancreatic cancer
3. Metastatic pancreatic cancer
4. A & B
5. B & C
6. A & C
7. A, B & C (all choices are correct)
Given the dependence of erlotinib on CYP1A1 and CYP1A2, a 25% elevation erlotinib drug dlearancein patients who are smokers may necessitate increasing drug doses.
1. True
2. False
One serious adverse reaction following erlotinib administration is severe rash (greater than 10% frequency of occurrence)
1. True
2. False
Common adverse reactions to erlotinib administration include:
1. Nail disorders
2. Diarrhea
3. Anorexia
4. Dyspnea
5. Fatigue
6. All of the above
In patients just diagnosed with non-small cell lung cancer (NSCLC), erlotinib is approved in treating those patients who have EGFR mutations only.
1. True
2. False
Rarely, erlotinib treatment may cause Stevens-Johnson syndrome/toxic epidermal necrolysis.
1. True
2. False
Example/examples of drug drug interactions involving erlotinib:
1. Erlotinib administration while the patient is also receiving proton pump inhibitors result in a reduction by about 50% in erlotinib bioavailability.
2. Patients using warfarin may exhibit reduced extrinsic coagulationduring treatment with erlotinib.
3. Both
4. Neither