Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Blood, Lymph, Immune, Bone > Antineoplastic Agents > Flashcards

Antineoplastic Agents Flashcards

1
Q

Alkylating agents

MOA

A

Alkylating agents work by binding at the N7 position of guanine and form a crosslink in the DNA

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Alkylating agents

General Side effects

A
  1. Alkylating agents affect all cells with rapid turnover (skin, BM, GI, reproductive system)
    1. BM depression (anemia, leukopenia, thrombocytopenia, etc)
    2. alopecia
    3. ulceration of mucosal surfaces
    4. potentially carinogenic/teratogenic
    5. permanent amenorrhea
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

What drugs are in the nitrogen mustard subclass of the alkylating agents?

A

Nitrogen mustards inlude

cyclosphophamide

ifosfamide

Melphalan

Mechlorethamine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Cyclosphosphamide

does it require activation?

what is the major side effect associated with cyclosphosphamide?

A

Cyclosphosphamide is a prodrug that requires metabolic activation by hepatic P450.

The active metabolites acrolein and phosphoramide mustard cause the cytotoxic effects.

Acrolein also destroyes the urothelium and causes hemorrhagic cystitis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Cyclophosphamide

clinical use as a chemotherapy agent

A

cyclophosphamide

non-Hodgkin’s lymphoma

Burkitt’s Lymphoma

CLL

neuroblastoma

Willms tumor

rhabdomyosarcoma

Ewing Sarcoma

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

How do we prevent Hemorrhagic cystitis?

what drug causes it?

A

Cyclophosphamide’s active metabolite Acroline causes hemorrhagic cystitis.

We can prevent hemorrhagic cystitis with:

adequate hydration, mesna (N-acetylcysteine)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Ifosfamide

MOA

Side effects

Clinical indications

A

Ifosfamide is an analog of cyclophosphamide with a similar MOA and side effect profile. It must be activated by P450.

Ifosfamide can cause CNS toxicity that can result in encephalopathy. Other side effects include Hemorrhagic cystitis and nephrotoxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Ifosfamide

Clinical use

A

Ifosfamide is used for the treatment of

germ cell testicular cancer and sarcomas

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What drugs are in the Nitrosoureases sub group of Alkylating agents?

A

Nitrosoureas

  1. carmustine (BCNU)
  2. Lomustine (CCNU)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Nitrosoureas

MOA

Clinical indication

A

Carmustine and Lomustine alkylate DNA binding at the O6 position of guanine

  1. Clinical use:
    1. Brain tumors (glioblastoma multiforme)
    2. multiple myeloma, hodgkin and non-hodkin
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Nitrosoureas

Side effects

A

Side effects of carmustine and lomustine include

N/V

BM depression

Pulmonary, renal and hepatic toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Busulfan

MOA

Indications

A

Busulfan binds to the N7 of guanine.

CML (although most patients have the Philadelphia chromosome, t(9;22) which can be targeted with imatinib

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Busulfan

Side effects

A

Busulfan

N/V

BM suppression

Pulmonary fibrosis

Adenal insufficiency

Skin hyperpigmentation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Nonclassic Alkylating Agents

A

procarbazine

decarbazine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Procarbazine: Nonclassic Alkylating Agents

MOA

A

procarbazine

inhibits DNA, RNA, and protein synthesis but the mechanism is unclear

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Procarbazine

Side Effects

A

Procarbazine

CNS depression

highly carcinogenic, mutagenic, and teratogenic

Weak MAO inhibitor which can lead to a hypertensive crisis if given with other MAOi, TCA, or cheese and wine

Disulfiram-like reactions

17
Q

Platinum analogs of alkylating agents include:

A

Platinum analogs

cisplatin

carboplatin

oxaliplatin

18
Q

cisplatin

MOA

A

cisplatin

cross-links DNA at N7 of guanine

broad range of antitumor activity

19
Q

Cisplatin

Side Effects

A

Cisplatin

Neurotoxicity

Ototoxicity

Nephrotoxicity (prevent with hydration, chloride diuresis, and amifostine)

20
Q

what phase of the cell cycle do the alkylating agents target?

A

They are non-specific.

21
Q

Antimetabolites target which phase in the cell cycle?

A

S phase

22
Q

Methotrexate

MOA

A

Methotrexate competitively binds to and inhibits dihydrofolate reductase resulting in the inhibition of synthesis of tetrahydrofolate and inhibits dTMP and DNA synthesis

23
Q

Methotrexate:

Clinical Use

A
  1. Chemotherapy:
    1. Multiple cancers: ALL, lymphomas, breast, head, neck, osteosarcoma, choriocarcinoma
  2. non-chemotherapy:
    1. GVHD
    2. psoriasis
    3. RA
24
Q

Methotrexate:

Side Effects

A

Methotrexate

  1. BM depression (neutropenia and thrombocytopenia)
  2. Teratogen
  3. Alopecia, GI toxicity, dermatitis, pulmonary fibrosis
25
Q

What drug is administered along with methotrexate to “rescue normal cells from toxicity?”

A

Leucovorin

its a reduced folate but its mechanism is unclear

26
Q

What drugs are pyrimidine antagonists?

A

5-florouracil

cytarabine

gemcitabine

27
Q

5-FU

MOA

A

5-FU is inactive and requires activation to FdUMP which will inhibit thymidylate synthase

28
Q

Cytarabine

MOA

A

Cytarabine

cytidine analog and a prodrug that needs activation to Ara-CTP.

Ara-CTP competes with dCTP and inhibits DNA synthesis

S-phase specific

29
Q

Cytarabine:

Clinical Use

A

Cytarabine use is limited to

hematological malignancies

30
Q

Cytarabine

Side effects

A

Cytarabine

N/V

BM depression

cerebellar ataxia

31
Q

Gemcitabine

MOA

A

Gemcitabine

inhibits ribonucleotide reductase which decreases dNTP.

Inhibits DNA polymerase

incorporates into DNA and leads to chain termination

32
Q

What drugs are purine antagonists?

A

Purine antagonists:

6-Mercaptopurine

6-Thioguanine

Fluarabine

33
Q

6-MP and 6-TG

MOA

A

6-MP and 6-TG

require activation by HGPRT and inhibit de novo purine nucleotide synthesis

34
Q

6-MP and 6-TG

Clinical Use:

Side effects:

Drug-drug interactions

A

6-MP and 6-TG

AML and ALL (acute)

hepatotoxicity (1/3 of patients sho some cholestatic jaundice)

6-MP interacts with allopurinol or febuxostat

*6-MP is metabolized by xanthine oxidase. Allopurino and febuxostat are xanthine oxidase inhibitors so they will stop the metabolism (inactivation) of 6-MP

35
Q

Fludarabine

MOA

Clinical Use

Side Effects

A

Fludarabine incorporates into DNA and inhibits ribonucleotide reductase. It is used for treatment in Non-Hodgkin’s lymphoma and CLL.

Immunosupression

36
Q

Hydroxyurea

MOA

A

Hydroxyurea

inhibits ribonucleotide reductase resulting in a depletion of intracellular dNTPs leading to inhibition of DNA synthesis

37
Q

Hydroxyurea

Clinical Use

A

Hydroxyurea

AML, CML, melanoma

Sickle Cell disease

38
Q
A

Blood, Lymph, Immune, Bone (13 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions