Medical Pharmacology Practice Questions: Chapters 33-34 Retinoids

Retinoids are classified as this type of anticancer agent.
1. DNA polymerase inhibitor
2. Promoter of cellular differentiation
3. Alkylating agent
4. Topoisomerase inhibitor
Agent/agents classified as differentiation promoting drug(s):
1. All-trans retinoic acid (ATRA, tretinoin)
2. Arsenic trioxide (ATO)
3. Both
4. Neither
Differentiating agents in cancer chemotherapy are designed to overcome the blockade of further differentiation associated with malignant cells.
1. True
2. False
All-trans retinoic acid (ATRA, tretinoin) and arsenic trioxide (ATO) are able to restore differentiation in a particular leukemia due to a genetic translocation resulting in a fusion protein that blocks differentiation.
1. True
2. False
All-trans retinoic acid (ATRA, tretinoin) and arsenic trioxide (ATO) are useful in treating this cancer
1. Chronic myelogenous leukemia (CML)
2. Acute promyelocytic leukemia
3. Both
4. Either
The principal mechanism of action of all-trans retinoic acid (Tretinoin) with respect to its anticancer property is:
1. Accelerating DNA repair
2. Increasing sensitivity to traditional alkylating anticancer drugs
3. Binding to RARA-PML fusion protein, thus activating transcription.
4. None of the above
All-trans retinoic acid (ATRA, tretinoin) pharmacodynamic/pharmacokinetic properties include/includes:
1. Primary site of metabolism: liver (80%)
2. Administration of ATRA (tretinoin) coadministered with drugs that induce higher levels of CYP3A4 may lead to ATRA resistance.
3. Both
4. Neither
Inhibitors of cytochrome P450 microsomal metabolizing enzymes e.g. antifungal imidazoles, may prevent ATRA (tretinoin) degradation which may cause:
1. Hypercalcemia
2. Kidney failure
3. Both
4. Neither
Concerning pharmacological action/actions of ATRA (tretinoin):
1. As a single agent this drug reverses acute promyelocytic leukemia (apo) associated hemorrhagic diathesis.
2. ATRA (tretinoin) in combination with an anthracycline drug may induce remission with an 80% or better likelihood of long-term survival, free of relapse.
3. Both
4. Neither
If clinically used as a single agent remission inducer (particularly in patients with >5000 leukemic cells per mm3, ATRA (tretinoin) increases in cytokine and neutrophils of leukemic origin may occur. This response can cause notable morbidity in about 20% of patients.
1. True
2. Falls
Arsenic trioxide (ATO) is a particularly effective treatment in patients with relapsed APL; the response rate in this population may be >85%.
1. True
2. False