Anti-Neoplastic Agents Flashcards

1
Q

MECHLORETHAMINE

A

Alkylating Agent

No longer used

PROPERTIES:
*VESICANT (blistering)
*BIFUNCTIONAL

Side Effects: Nausea vomiting, etc.

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2
Q

CYCLOPHOSPHAMIDE (CYTOXAN®)

A

Alkylating Agent

Activated in the Liver by P450.

Hemhorrhagic Cytitis (urinary bladder inflammation)

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3
Q

IFOSFAMIDE

A

Alkylating Agent, like Cyclophosphamide

*LESS MYELOSUPPRESSIVE

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4
Q

NITROSOUREA ALKYLATING AGENTS

A

Lipid soluble! Can be used in brain, etc.

CCNU would be an example of an abreviation. NU = Nitrosourea.

Lomustine and Carmustine are examples

Mechanisms of Action

  • ALKYLATES DNA: CROSS LINKS
  • Might be effective in CARBAMOYLATES PROTEIN (ADDS UREA MOIETY)

Side Effects: CNS

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5
Q

Platinums

A

CISPLATIN

OXALIPLATIN

Uses:

TESTICULAR

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6
Q

CISPLATIN

A

Nephrotoxicity

Severe Nausea

Ototoxic

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7
Q

OXALIPLATIN

A

LESS RESISTANCE

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8
Q

MITOMYCIN

A

TEMPORARY BENEFICIAL EFFECTS (not curative agent)

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9
Q

Anti-Metabolites

A
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10
Q

Methotrexate

A
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11
Q

6-Mercaptopurine

A

Pro-Drug

Picks up a Ribose and a Phosphate

Interferes with RNA and DNA.

TOXICITIES:
***HEMATOLOGICAL

***THERAPEUTIC PLACE:
ANTI – LEUKEMIC CHEMOTHERAPY

GOUT:

Allopurinol very similar to Hypoxanthine. Lots of purines are kicked out due to neoplasm death.
6-MP is metabolized via Xanthine oxidase. So, it becomes toxic. So, allopurinol needs to be given in a lower dose, or you will have toxicity issues.

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12
Q

6-Thioguanine

A

Uses:

ADULT ACUTE LEUKEMIA

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13
Q

5-FLUOROURACIL

A

Pro-drug

Pyrimadine antagonist

THYMIDYLATE SYNTHASE INHIBITED BY 5-FdUMP

Thymine less death. If you don’t have Thymine, you don’t have DNA.

Interferes with dUMP

TOXICITIES:***HEMATOLOGICAL

THERAPEUTIC PLACE: SOLID TUMORS ]:

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14
Q

CYTOSINE ARABINOSIDE
[CYTARABINE]

A

Pro-drug

Pyrimidine analog

Inactive unless gets all the phosphates (3) and the Ribose

**AFFECTS RNA / DNA METABOLISM

TOXICITIES:***HEMATOLOGICAL

THERAPEUTIC PLACE: - NOT for SOLID TUMORS!
- ACUTE GRANULOCYTIC / ACUTE MYELOID LEUKEMIAS)

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15
Q

Methotrexate

A

Anti-Metabolite (Anti-Folic Acid)

Inhibits Folate Reductase:

Methotrexate stops FH2 to FH4.
Carbon transfer from Methylene to FH4 and then transfers to dUMP to make TMP. That pathway is stopped also.

effectively stops the one carbon transfer necessary to make Thimadine.

Needs to pick up Glutamate to be active, so tumor has more of the enzyme adding glutamate. So, its more functional in Tumor cells.

Toxicity:

*MYELOSUPPRESSION (LEUKOPENIA, THROMBOCYTOPENIA) (LIFE – THREATENING INFECTION)
*GI ULCERS (STOMATITIS)

* NEPHROTOXICITY

Antidote: CITROVORUM FACTOR (LEUCOVORIN ) - Can give patient a lethal dose, and then an antedote.

  • What it is: N5 - FORMYL THF, FOLINIC ACID

Uses:

CHORIOCARCINOMA
ACUTE LYMPHOCYTIC LEUKEMIA

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16
Q

PEMETREXED

A

Same as methotrexate, just a derivative

Mech of action:

**DIHYDROFOLATE REDUCTASE
****THYMIDYLATE SYNTHETASE

17
Q

VINCRISTINE AND VINBLASTINE

(VINCA ALKALOIDS)

A

Interfere with Mitosis. Block assembly of Tubulin dimer.

TOXICITIES:
VINBLASTINE : BONE MARROW DEPRESSION
VINCRISTINE : NEUROLOGICAL (PERIPHERAL )

VINCRISTINE – INDUCE REMISSION IN ACUTE LEUKEMIA, PED. SOLID TUMORS

VINBLASTIN: HODGKIN’S DISEASE

18
Q

EPI PODO PHYLLO TOXINS

A

AFFECT TOPOISOMERASE II (__REGULATE WINDING OF DNA)

  • ETOPOSIDE – BREAST CANCER, KAPOSI’S SARCOMA, TESTICULAR TUMORS
  • TENIPOSIDE – ALL CHILDREN

Tox:

*MYELOSUPPRESSIVE

*NAUSEA

19
Q

CAMPTOTHECINS

A

TOPO 1

20
Q

TAXOL

A

Taxols never allow disassembly, mitosis messed up.

THERAPEUTIC USE:

OVARIAN, BREAST, LUNG CANCERS

TOXICITIES:
*MYELOSUPPRESSION (NEUTROPENIA)
***PERIPHERAL NEUROPATHIES

21
Q

ANTHRACYCLINES

A

DAUNORUBICIN: R = - CO – CH3

DOXORUBICIN: R = – CO - CH2OH - Breast Cancer,** ****TESTICULAR

MECHANISMS OF ACTION:
A) **INTERCALATE WITH DNA (gets inbetween)
B) **INHIBIT (INTERFERES) TOPOISOMERASE II
D) *FORM FREE RADICALS - REACTIVE

Cumulative

TOXICITIES:
***BONE MARROW DEPRESSION
***CARDIAC TOXICITY (FREE RADICALS)

“RADIATION RECALL REACTION”:

22
Q

ACTINOMYCIN D

A

Pediatric

Intercalating

23
Q

BLEOMYCIN

A

BINDS TO DNA
***FORMS FREE RADICALS

USES:
**TESTICULAR TUMORS

TOXICITIES:
***PULMONARY FIBROSIS (ELDERLY PATIENTS)

24
Q

Targeted Therapy

A

NIB - Tyrosine Kinase Inhibitor

IMUS - mTOR

IMAB – MONOCLONAL ANTIBODY AGAINST EGFR

TOXITICITES:
*PALMAR / PLANTAR SYNDROME
*RASH

*USE: RENAL CELL CARCINOMA

Extend life expectancy.

25
Q

TORISEL® (TEMSIROLIMUS)

A

ANGIOGENESIS INHIBITOR

TOXICITES – SERIOUS:

26
Q

PREDNISONE

A

Hormone Treatment

Inhibits RNA and Protein Synthesis

27
Q

LEUPROLIDE

A

Pharm: Castration

***ESTROGEN / TESTOSTERONE PRODUCTION DECREASES

USE: PROSTATIC CARCINOMA / BREAST CANCER
TOXICITIES:
HOT FLASHES
SOME CARDIAC EFFECTS

28
Q

TAMOXIFEN

A

BINDS TO ESTROGEN RECEPTORS

*** Increases RISK OF ENDOMETRIAL CANCER

29
Q

*HERCEPTIN® (TRASTUZUMAB)

A

MONOCLONAL ANTIBODY

30
Q

******** SECONDARY ******** MALIGNANCIES DUE TO CANCER TREATMENT

A

***ACUTE MYELOGENOUS LEUKEMIA (AML)