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Cology 2 Exam 4 > Antineoplastic therapy - Alkylating agents 19-32 > Flashcards

Antineoplastic therapy - Alkylating agents 19-32 Flashcards

1
Q

Name the nitrosureas

A

Carmustine
Lomustine
Streptozocin

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2
Q

How is Carmustine administered?

A

IV, also transdermal wafer in brain after brain tumor removal

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3
Q

How is Lomustine administered?

A

Oral

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4
Q

How is Carmustine activated?

A

Non-enzymatically

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5
Q

How is Lomustine activated?

A

Non-enzymatically

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6
Q

How does Carmustine work?

A

Alkylates DNA and carbamoylate proteins

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7
Q

How does Lomustine work?

A

Alkylates DNA and carbamoylate proteins

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8
Q

What is Carmustine used for?

A

Brain tumors, melanoma, non-Hodgkin’s lymphoma

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9
Q

What is Lomustine used for?

A

Brain tumors, melanoma, non-Hodgkin’s lymphoma

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10
Q

Toxicity associated with Carmustine?

A

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

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11
Q

Toxicity associated with Lomustine?

A

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

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12
Q

How is Dacarbazine activated?

A

P-450 system to Diazomethne, a cytotoxic agent

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13
Q

How is Procarbazine activated?

A

P-450 system to Diazomethne, a cytotoxic agent

Procarbazine also has several active metabolites including H2O2 and formaldehyde

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14
Q

Which drug has active metabolites H2O2 and formaldehyde?

A

Procarbazine

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15
Q

What is Dacarbazine used for?

A

Hodgkin’s disease, malignant melanoma

ABVD regimen

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16
Q

What is Procarbazine used for?

A

Hodgkin’s disease, malignant melanoma

MOPP regimen

17
Q

Toxicities associated with Dacarbazine

A 
Severe N/V
Myelosuppression
Alopecia
Flu-like syndrome
Renal/hepatotoxicity
18
Q

Toxicities associated with Procarbazine?

A 
Myelosuppression
Alopecia
Flu-like syndrome
CNS depression
Renal/hepato toxicity
Leukogenic
Immunosuppressant
Infertility
19
Q

How is Temozolamide administered?

A

IV, oral

20
Q

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

A

Temozolamide

TEAMzolamide - TEAM UP with radiation for malignant gliomas and astrocytoma

21
Q

What is the MOA of temozolamide?

A

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

22
Q

How is Altretamine administered?

A

Oral

23
Q

How is Altrematine activated?

A

Activated to alkylating agent

24
Q

What is Altrematine used for?

A

It is 2nd line for ovarian cancer

25
Q

Toxicities of Altrematine?

A

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

26
Q

How is Thiotepa activated?

A

Converted to TEPA

Multiple metabolites, many of which are active

27
Q

How does Thiotepa work?

A

Cross links DNA

28
Q

What is Thiotepa used for?

A

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

29
Q

Toxicity of Thiotepa?

A

Allopecia, hematological, immunological, coma, seizures

30
Q

How is Busulfan administered?

A

Oral

31
Q

How does Busulfan work?

A

Alkyl sulfonate acts like mustards

32
Q

What is Busulfan used for?

A

Chronic myelogenous leukemia (CML)

Used with cyclophosphamide to ablate marrow before transplant

33
Q

Toxicities associated with Busulfan?

A

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

34
Q

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

A

Busulfan

35
Q

How is Cisplatin activated?

A

Water activated

36
Q

How does Cisplatin work?

A

Doesn’t formally alkylate DNA

Cross-link 7-nitrogen on guanine or adenine within same strand, blocks reading by enzymes

37
Q

What is Cisplatin used for?

A

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

38
Q

Which drug reacts with sulfhydryl groups?

A

Cisplatin

Cology 2 Exam 4 (16 decks)

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