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PP personal > Anti - cancer drugs 1.1 > Flashcards

Anti - cancer drugs 1.1 Flashcards

1
Q

MOA of alkylating agents

A

Transfer alkyl group to DNA in the N-7 position of guanine during cell division (prevents normal function)

Leads to:
DNA strand breakage
crosslinking of the two strands

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2
Q

Active form of Cyclophosphomide

A

Phosphoramide mustard

activated by p450 enzymes

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3
Q

uses of Cyclophoshomide (3)

A

Non-Hodgkin’s lymphoma
breast/ovarian cancer
neuroblastoma

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4
Q

ADR of Cyclophosphamide (5)

A

hemorrhagic cystitis (metabolite - acrolein)
SIADH
Bladder cancer
pulmonary toxicity
Vesicle formation (accidental leaking out of vessels)

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5
Q

Symptoms of hemorrhagic cystitis (3)

A

Suprapubic pain
Hematuria
Cyctoscopic findings

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6
Q

Treatment/prevention of drug induced hemorrhagic cystitis

MOA

A

MESNA ( sodium 2-mercaptoethane sulfonate)(+hydration)

MOA: binds to acrolein and inactivates it

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7
Q

MOR of alkylating agents (3)

A

Increased DNA repair
Decreased drug permeability
Production of “trapping” agents (thiols)

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8
Q

Platinum analogs (3)

A

Cisplatin
Carboplatin (less renal tox. but more BM depression)
Oxaliplatin (peripheral neuropathy)

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9
Q

Aklylating agent commonly used in testicular carcinoma

A

Cisplatin

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10
Q

Uses of cisplatin (3)

A

Testicular carcinoma
Lung/ovary/bladder cancer
MARROW SPARING

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11
Q

ADR of cisplatin (4)

A

Nephrotoxicity
Ototoxicity (acoustic nerve damage)
Peripheral neuritis
Severe nausea and vomiting (highly emetic)

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12
Q

MOA of procarbazine (2)

A

Alkylates DNA

Forms hydrogen peroxide –> generates free radicals –> DNA damage

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13
Q

Uses of procarbazine (1)

A

Hodgkins lymphoma

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14
Q

ADR of procarbazine (2)

A 
Disulfiram like rxns (after alcohol intake)
- Flushing, throbbing headache, nausea, vomiting, sweating, hypotension and confusion
Secondary cancers (acute leukemia) - after years
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15
Q

List Nitrosureas (4)

A 
"Te(a)m ZoLo Car must cross the brain"
Temozolomide
Streptrozotocin
Lomustine
Carmustine
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16
Q

Uses of nitrosureas

A

Meningioma
Glioblastoma
Medulloblastoma
Metastatic tumor

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17
Q

Nitrosurea used to treat insulinoma

A

Streptozotocin

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18
Q

List purine antagonists (2)

A

6-mercaptopurine (6-MP)

6-thioguanine (6-TG)

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19
Q

List pyrimidine antagonists (3)

A

Methotrexate (MTX)
5‐fluorouracil (5-FU)
Cytarabine (ara-C)

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20
Q

MOA of Methotrexate

A

Folic acid analog; binds to dihydrofolate reductase (active catalytic site) w/ high affinity –> impairs formation of DNA RNA and key cellular proteins

Cell cycle specific during S phase

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21
Q

Uses of methotrexate (4)

A

Choriocarcinoma (malignant mole) –usually curative
Anti-neoplastic (Eg. ALL, NHL)
Rheumatoid arthritis
Psoriasis

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22
Q

ADR of methotrexate (4)

A

Bone marrow suppression (BMS)
Mucositis
Folic acid deficiency
Renal toxicity: crystallization of metabolite of MTX

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23
Q

What reduces toxic effects of MTX on normal cells?

A

folinic acid (leucovorin, 5-formyltetrahydrofolate)

Rescue from the L

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24
Q

MOR for methotrexate (4)

A

Decreased drug transport
Decreased polyglutamate formation
Altered DHFR
Increased levels of DHFR

25
Q

MOA of 5-fluorouracil

A
  1. 5-FU –> 5-FdUMP; 5-FdUMP competes w/ dUMP for thymidylate synthase = thymidineless death (cells)
  2. 5-FdUTP incorporates into DNA = block DNA synthesis
  3. 5-FUTP incorporates into RNA = mess w/ mRNA translation
26
Q

MOR of 5-fluorouracil

A

Decreased activation of 5-FU, decreased thymidylate synthase activity

27
Q

Uses of 5-fluorouracil

A

Carcinomas of:
breast
GI tract
hepatoma

Not underlined: ovary, cervix, urinary bladder, prostate, pancreas, and oropharyngeal ca., colon cancer

28
Q

ADR of 5-fluorouracil

A

Hand and foot syndrome
neurologic deficits
bone marrow depression

Not bold: Nausea, mucositis, diarrhea, hyperpigmentation, Alopecia

29
Q

Antidote for 5-fluorouracil overdose

A

Uridine triacetate (Vistogard®)

30
Q

MOA of cytarabine

A

Eventually converted to ara-CTP (active form)
Inhibits DNA polymerase
Incorporates into DNA and RNA, causing termination
Most specific for s phase of all anti metabolites

31
Q

Uses of cytarabine

A

Hematologic malignancy (AML, non-hodgkin’s lymphoma)

32
Q

ADR of cytarabine

A

High doses cause neurotoxicity (cerebellar dysfunction and peripheral neuritis)
Hand-foot syndrome

Not bold: BM depression
corneal toxicity, keratoconjuctivitis

33
Q

MOR of 6-Mercaptopurine & Thioguanine

A

cancer cells having decreased activity of HGPRT

Cancer cells also increased alkaline phosphatase that inactivates toxic nucleotides

34
Q

MOA of 6-Mercaptopurine & Thioguanine

A

Both are activated by HGPRT to toxic nucleotides (TIMP)
6-MP inhibits conversion of IMP to adenylic acid (AMP) and guanine
6-TG inhibits guanine synthesis from IMP

35
Q

MOA of Hydroxyurea

A

inhibiting ribonucleotide diphosphate reductase; decreases production of deoxyribonucleotide

36
Q

Uses of Hydroxyurea

A

Polycythemia vera and thrombocytosis
Sickle cell disease (increase fetal Hg)*
Second line treatment for psoriasis
CML*

37
Q

ADR of hydroxyurea

A

BM depression

38
Q

List Vinca alkaloids (3)

A

Vinblastine*
vincristine*
Vinorelbine

39
Q

MOA vinca alkaloids

A

drugs block the formation of mitotic spindle by preventing the assembly of tubulin dimers into microtubules

Act primarily on the M phase of cancer cell cycle

40
Q

MOR of vinca alkaloids

A

Increased efflux of drugs from tumor cells (P-glycoprotein)

41
Q

Uses of vinblastine

ADR of vinblastine

A

Uses: (ABVD)
Hodgkin’s disease Lymphomas
Carcinoma of Breast
Testicular tumors

ADR: Bone marrow suppression***
anorexia
nausea, vomiting &Diarrhea
Alopecia

BLASTS marrow

42
Q

Uses of vincristine

ADR of vincristine

A 
Uses: (MOPP) (oncovin)
Childhood leukemias*
Childhood-Wilm’s tumor*
Neuroblastoma
Hodgkin’s disease

ADR:
Peripheral neuritis with
Paresthesia, Muscle weakness
SIADH

Marrow SPARING

43
Q

List Taxanes (2)

A

Paclitaxel

Docetaxel

44
Q

MOA of Taxanes

A

interfere with mitotic spindle

Prevent microtubule dis-assembly into tubulin monomers

45
Q

ADR of Taxanes

A

Neutropenia
Peripheral neuropathy
Hypersensitivity reactions (corticosteroids & H1 blockers)

46
Q

List Podophyllotoxins

List Camptothecins

A

Podophyllotoxins: Etoposide, Teniposide

Camptothecins: Topotecan, Irinotecan

47
Q

MOA of Etoposide, Teniposide

Uses of Etoposide, Teniposide

A

MOA: Inhibiting topoisomerase II
Most active in late S and early G2 phase

Uses: combination Rx in small cell carcinoma of lung, prostate and testicular carcinomas

48
Q

MOA of Topotecan, Irinotecan

Uses of Topotecan, Irinotecan

A

MOA: inhibiting topoisomerase-I

Uses: Second line Rx for ovarian ca. and small cell ca. of lung

49
Q

List anthracyclines (3)

A

Doxorubicin (Adriamycin)*
Daunorubicin*
Mitoxantrone

50
Q

MOA of Doxorubicin & Daunorubicin

A

block RNA and DNA synthesis and cause strand scission by:
Intercalating between base pairs
Inhibiting topoisomerase II
Generating free radicals
Altering cellular membrane fluidity and iron transport

CCNS drugs

51
Q

Uses of Doxorubicin & Daunorubicin

A

ABVD regimen in Hodgkin’s lymphoma, NHL

52
Q

ADR of anthracyclines

Antidote?

A

Cardiac toxicity (due to generation of free radicals)

  • Acute: arrhythmias, ECG changes, pericarditis, myocarditis
  • Chronic: Dilated cardiomyopathy, heart failure

Radiation recall rxn
BM depression
Total alopecia

Antidote: dexrazoxane

53
Q

MOA of Bleomycin

A

binds to DNA –> single and double strand breaks following free radical formation and inhibition of DNA synthesis

DNA fragmentation via oxidation of a DNA-bleomycin-Fe(II) complex –> chromosomal aberrations

CCS drug –> accumulation of dividing cells in G2

54
Q

Uses of Bleomycin

A

ABVD regimen for Hodgkin’s

Intracavitary therapy in ovarian and breast cancers (Sclerosing agent)

55
Q

ADR of Bleomycin

A

Pulmonary fibrosis

56
Q

MOA of dactinomycin

Uses of dactinomycin

A

MOA: Intercalation between G-C pair of DNA

Uses: choriocarcinoma (malignant mole) if no response to MTX

57
Q

Uses of asparaginase

ADR of asparaginase

A

Use: childhood acute lymphoblasticleukemia (ALL)

ADR: Hypersensitivity reactions (can be severe)
Pancreatitis***

Clue for pancreatitis: elevated S.amylase/ S. lipase levels

58
Q

Treatment regimens for Hodgkin Lymphoma

List ABVD
List MOPP

A 
ABVD: 
Adriamycin (doxorubicin)
Bleomycin
Vinblastine
Dacarbazine
MOPP:
Mechlorethamine
Vincristine (oncovin)
Procarbazine
Prednisone
59
Q

Treatment regimens for Non‐Hodgkin Lymphoma
CHOP, RCHOP, CVP

List all drugs used in these combinations

A 
Rituximab
Cyclophosphamide
Hydroxydaunorubicin (doxorubicin)
Oncovin (vincristine)
Prednisone

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