alkylating agents

Question 1

what are the alkylating agents?

Answer 1

cylcophosphamide

mechlorethamine

melphalan

chlorambucil

nitrosureas (azithrocin, carbamucin)

aziridines: thiotepa
alkysulfontate: busulfan

Question 2

non-classical alkylating agents (3)

Answer 2

procarbazine

decarbazine

bendamustine

Question 3

platinum-analog alkylating agents

Answer 3

1. cisplatin
2. carboplatin
3. oxaliplatin

Question 4

antimetabolites: antifolates

Answer 4

methotrexate

Question 5

CTCL

Answer 5

mechlorethamine

Question 6

multiple myeloma

Answer 6

melphalan with dexamethasone

Question 7

CLL

Answer 7

chronic lymphoblastic leukemia: chlorambucil

Question 8

generates botH alkylating and carbamylating moieties

Answer 8

nitrosureas

Question 9

malignant gliomas

Answer 9

carbamustine

Question 10

high affinity for islets of langerhas

Answer 10

streptozocin

Question 11

causes diabetes in exp animals

Answer 11

strepazocin, a nitrosurea

Question 12

human pancreatic islet cell carcinoma

Answer 12

streptozocin

Question 13

carcinoid tumors

Answer 13

streptozocin

Question 14

hepatic CYPs rapidly convert X drug into a desulfurated primary metabolite TEPA

Answer 14

thiotepa. alog with TEPA, binds to DNA to form DNA cross links

Question 15

used for high dose chemo regimens in transplants for hematological malignances

Answer 15

thiotepa

Question 16

AE: pulmonary fibrosis, hepatic VOD at high doses. What is the most common AE at a standard dose?

Answer 16

myelosuppression: busulfan
note: VOD “veno-occlusive disease”

Question 17

non-enzyme inducing benzos recommended with this drug

Answer 17

busulfans

Question 18

anti convulsants given with these drugs to reduce CNS toxicities, except which?

Answer 18

phenytoin- induce GSTs that metabolize the busulfan faster

Question 19

chronic myeloid leukemia

Answer 19

busulfans

Question 20

exact mechanism unknown but prolongs interphase of the cell cycle. how is this drug activated?

Answer 20

CYP activated to highly reactive alkylating agent: procarbazine

Question 21

increases expression of MGMT, accelerating catabolism of drug and therefore resistance

Answer 21

procarbazine

Question 22

concomittant CNS suppressants should be avoided in pts receiving this drug

Answer 22

procarbazine .

Question 23

used in MOPP regimen fir Hodgkin lymphoma

Answer 23

Procarbazine

Question 24

part of the PVC regimen for treating hodgkin lymphoma

Answer 24

procarbazine, along with vincristine and lomustine

Question 25

prodrug--\> monomethyl triazeno metabolite MTIC. how does resistance begin in this drug?

Answer 25

Docarbazine: resistance develops due to removale of methyl groups by MGMT

Question 26

primarily indicated against hodgkin lymphoma but also mildly effective against malignant melanoma and adult sarcomas

Answer 26

docarbazine

Question 27

inhibits mitotic checkpoints and induces mitotic catastrophe. what is the other aspect of the MOA and its AEs?

Answer 27

benamustine: forms cross links with DNA resulting in single and double stranded DNA breaks myelosuppreesion, rapidly reversible mucositis