Medical Pharmacology: Cancer Chemotherapy Drugs: Anti-Metabolites Practice Questions

Cladribine, an anticancer agent classified in the "anti-metabolite" designation is an adenosine deaminase-resistant purine-analog.
1. True
2. False
Cladribine has significant and likely curative activity in which one(s) of the following:
1. Chronic lymphocytic leukemia
2. Hairy cell leukemia
3. Low-grade lymphoma
4. A & B
5. B & C
6. A & C
7. A, B & C
Activation of cladribine, a purine deoxyadenosine analogue, is dependent on deoxycytidine kinase (dCK).
1. True
2. False
The active form of cladribine (cladribine-triphosphate) :
1. Incorporation of normal dATP (deoxyadenosine triphosphate) nucleotide into DNA is inhibited
2. Cladribine triphosphate through interaction with dATP results in chain elongation termination.
3. Buildup of the triphosphate metabolite has the effects of additional DNA synthesis and repair inhibition.
4. A & B
5. A, B & C
Cladribine may also be effective in treating patients with non-Hodgkin's lymphoma.
1. True
2. False
Cladribine absorption and excretion.
1. Cladribine although reasonably well absorbed orally is usually administered by IV.
2. Cladribine is mainly subject to hepatic biotransformation and biliary excretion.
3. Cladribine does not pass the blood brain barrier and is only marginally present in the CSF.
4. All of the above
Cladribine is viewed as the drug of choice in hairy cell leukemia with about 80% of patients attaining a complete response following a single therapeutic course.
1. Through
2. False
Cladribine is considered highly toxic and attention must be paid to a variety of serious side effects including renal toxicity and pulmonary vascular damage.
1. True
2. False
A major determinant of resistance to cladribine's anticancer effect is a decrease in deoxycytidine kinase, the enzyme responsible for intracellular cladribine activation (through formation of cladribine-triphosphate)..
1. True
2. False
Although a transient myelosuppression may be observed with cladribine, myelosuppression is dose-limiting. Other toxicity/toxicities include/includes:
1. Neurotoxicity (15% of patients; the toxicity is considered mild-to-moderate)
2. Immunosuppression is associated with delayed morbidity.
3. Both
4. Neither