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Anti - cancer drugs 1.1 Flashcards

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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)

Study These Flashcards
A

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

25
MOA of 5-fluorouracil
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
MOR of 5-fluorouracil
Decreased activation of 5-FU, decreased thymidylate synthase activity
27
Uses of 5-fluorouracil
Carcinomas of: breast GI tract hepatoma Not underlined: ovary, cervix, urinary bladder, prostate, pancreas, and oropharyngeal ca., colon cancer
28
ADR of 5-fluorouracil
Hand and foot syndrome neurologic deficits bone marrow depression Not bold: Nausea, mucositis, diarrhea, hyperpigmentation, Alopecia
29
Antidote for 5-fluorouracil overdose
Uridine triacetate (Vistogard®)
30
MOA of cytarabine
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
Uses of cytarabine
Hematologic malignancy (AML, non-hodgkin’s lymphoma)
32
ADR of cytarabine
High doses cause neurotoxicity (cerebellar dysfunction and peripheral neuritis) Hand-foot syndrome Not bold: BM depression corneal toxicity, keratoconjuctivitis
33
MOR of 6-Mercaptopurine & Thioguanine
cancer cells having decreased activity of HGPRT | Cancer cells also increased alkaline phosphatase that inactivates toxic nucleotides
34
MOA of 6-Mercaptopurine & Thioguanine
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
MOA of Hydroxyurea
inhibiting ribonucleotide diphosphate reductase; decreases production of deoxyribonucleotide
36
Uses of Hydroxyurea
Polycythemia vera and thrombocytosis Sickle cell disease (increase fetal Hg)* Second line treatment for psoriasis CML*
37
ADR of hydroxyurea
BM depression
38
List Vinca alkaloids (3)
Vinblastine* vincristine* Vinorelbine
39
MOA vinca alkaloids
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
MOR of vinca alkaloids
Increased efflux of drugs from tumor cells (P-glycoprotein)
41
Uses of vinblastine ADR of vinblastine
Uses: (ABVD) Hodgkin’s disease Lymphomas Carcinoma of Breast Testicular tumors ADR: Bone marrow suppression*** anorexia nausea, vomiting &Diarrhea Alopecia BLASTS marrow
42
Uses of vincristine ADR of vincristine
``` Uses: (MOPP) (oncovin) Childhood leukemias* Childhood-Wilm’s tumor* Neuroblastoma Hodgkin’s disease ``` ADR: Peripheral neuritis with Paresthesia, Muscle weakness SIADH Marrow SPARING
43
List Taxanes (2)
Paclitaxel | Docetaxel
44
MOA of Taxanes
interfere with mitotic spindle | Prevent microtubule dis-assembly into tubulin monomers
45
ADR of Taxanes
Neutropenia Peripheral neuropathy Hypersensitivity reactions (corticosteroids & H1 blockers)
46
List Podophyllotoxins List Camptothecins
Podophyllotoxins: Etoposide, Teniposide Camptothecins: Topotecan, Irinotecan
47
MOA of Etoposide, Teniposide Uses of Etoposide, Teniposide
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
MOA of Topotecan, Irinotecan Uses of Topotecan, Irinotecan
MOA: inhibiting topoisomerase-I Uses: Second line Rx for ovarian ca. and small cell ca. of lung
49
List anthracyclines (3)
Doxorubicin (Adriamycin)* Daunorubicin* Mitoxantrone
50
MOA of Doxorubicin & Daunorubicin
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
Uses of Doxorubicin & Daunorubicin
ABVD regimen in Hodgkin’s lymphoma, NHL
52
ADR of anthracyclines Antidote?
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
MOA of Bleomycin
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
Uses of Bleomycin
ABVD regimen for Hodgkin’s | Intracavitary therapy in ovarian and breast cancers (Sclerosing agent)
55
ADR of Bleomycin
Pulmonary fibrosis
56
MOA of dactinomycin Uses of dactinomycin
MOA: Intercalation between G-C pair of DNA Uses: choriocarcinoma (malignant mole) if no response to MTX
57
Uses of asparaginase ADR of asparaginase
Use: childhood acute lymphoblasticleukemia (ALL) ADR: Hypersensitivity reactions (can be severe) Pancreatitis*** Clue for pancreatitis: elevated S.amylase/ S. lipase levels
58
Treatment regimens for Hodgkin Lymphoma List ABVD List MOPP
``` ABVD: Adriamycin (doxorubicin) Bleomycin Vinblastine Dacarbazine ``` ``` MOPP: Mechlorethamine Vincristine (oncovin) Procarbazine Prednisone ```
59
Treatment regimens for Non‐Hodgkin Lymphoma CHOP, RCHOP, CVP List all drugs used in these combinations
``` Rituximab Cyclophosphamide Hydroxydaunorubicin (doxorubicin) Oncovin (vincristine) Prednisone ```

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