Antineoplastic therapy - Alkylating agents 19-32

Question 1

Name the nitrosureas

Answer 1

Carmustine
Lomustine
Streptozocin

Question 2

How is Carmustine administered?

Answer 2

IV, also transdermal wafer in brain after brain tumor removal

Question 3

How is Lomustine administered?

Answer 3

Oral

Question 4

How is Carmustine activated?

Answer 4

Non-enzymatically

Question 5

How is Lomustine activated?

Answer 5

Non-enzymatically

Question 6

How does Carmustine work?

Answer 6

Alkylates DNA and carbamoylate proteins

Question 7

How does Lomustine work?

Answer 7

Alkylates DNA and carbamoylate proteins

Question 8

What is Carmustine used for?

Answer 8

Brain tumors, melanoma, non-Hodgkin’s lymphoma

Question 9

What is Lomustine used for?

Answer 9

Brain tumors, melanoma, non-Hodgkin’s lymphoma

Question 10

Toxicity associated with Carmustine?

Answer 10

Nausea, vomiting, fibrosis, myelosuppression, RENAL TOXICITY, secondary leukemia

Question 11

Toxicity associated with Lomustine?

Answer 11

Nausea, vomiting, fibrosis, myelosuppression, RENAL TOXICITY, secondary leukemia

Question 12

How is Dacarbazine activated?

Answer 12

P-450 system to Diazomethne, a cytotoxic agent

Question 13

How is Procarbazine activated?

Answer 13

P-450 system to Diazomethne, a cytotoxic agent

Procarbazine also has several active metabolites including H2O2 and formaldehyde

Question 14

Which drug has active metabolites H2O2 and formaldehyde?

Answer 14

Procarbazine

Question 15

What is Dacarbazine used for?

Answer 15

Hodgkin’s disease, malignant melanoma

ABVD regimen

Question 16

What is Procarbazine used for?

Answer 16

Hodgkin’s disease, malignant melanoma

MOPP regimen

Question 17

Toxicities associated with Dacarbazine

Answer 17

Severe N/V
Myelosuppression
Alopecia
Flu-like syndrome
Renal/hepatotoxicity

Question 18

Toxicities associated with Procarbazine?

Answer 18

Myelosuppression
Alopecia
Flu-like syndrome
CNS depression
Renal/hepato toxicity
Leukogenic
Immunosuppressant
Infertility

Question 19

How is Temozolamide administered?

Answer 19

IV, oral

Question 20

What drug is the DOC for malignant gliomas and astrocytoma together with radiation?

Answer 20

Temozolamide

TEAMzolamide - TEAM UP with radiation for malignant gliomas and astrocytoma

Question 21

What is the MOA of temozolamide?

Answer 21

Similar to dacarbazine - prodrug to MTIC which is a cytotoxic agent

Question 22

How is Altretamine administered?

Answer 22

Oral

Question 23

How is Altrematine activated?

Answer 23

Activated to alkylating agent

Question 24

What is Altrematine used for?

Answer 24

It is 2nd line for ovarian cancer

Question 25

Toxicities of Altrematine?

Answer 25

Myelosuppression Nausea/vomiting Neurotoxicity - ataxia, depression, confusion, hallucinations

Question 26

How is Thiotepa activated?

Answer 26

Converted to TEPA | Multiple metabolites, many of which are active

Question 27

How does Thiotepa work?

Answer 27

Cross links DNA

Question 28

What is Thiotepa used for?

Answer 28

Bladder, breast, Hodgkin's, ablation of bone marrow

Question 29

Toxicity of Thiotepa?

Answer 29

Allopecia, hematological, immunological, coma, seizures

Question 30

How is Busulfan administered?

Answer 30

Oral

Question 31

How does Busulfan work?

Answer 31

Alkyl sulfonate acts like mustards

Question 32

What is Busulfan used for?

Answer 32

Chronic myelogenous leukemia (CML) | Used with cyclophosphamide to ablate marrow before transplant

Question 33

Toxicities associated with Busulfan?

Answer 33

Diarrhea, mild nausea, vomiting, myelosuppression, pulmonary fibrosis, secondary malignancies, infertility, teratogenic, HIGH DOSE SEIZURES must use antiepileptics, can cause busulfan lung which is fatal after 3 years

Question 34

Which drug must be taken with epileptics if given in high doses?

Answer 34

Busulfan

Question 35

How is Cisplatin activated?

Answer 35

Water activated

Question 36

How does Cisplatin work?

Answer 36

Doesn't formally alkylate DNA | Cross-link 7-nitrogen on guanine or adenine within same strand, blocks reading by enzymes

Question 37

What is Cisplatin used for?

Answer 37

Bladder, cervical, ovarian, testicular, melanoma, esophageal, head and neck, non-small cell lung tumors, colorectal cancer

Question 38

Which drug reacts with sulfhydryl groups?

Answer 38

Cisplatin