Anti-Neoplastic Drugs

Front 1

Methotrexate

Back 1

Folic Acid Analogue

Mechanism:

*S-phase of cell cycle
*Inhibits Purine and Thymidylate synthesis (uracil and cytosine are normal)
*Inhibits Dihydrofolate reductase

Adverse Reaction:

*hepatotoxicity *Teratogenesis *miscarriage *neurotoxicity

Front 2

6-Mercaptopurine

Back 2

Purine Analogue

Mechanism:

*S-phase of cell cycle
*Inhibits Purine Synthesis
*Inhibits Inosine monophosphate dehydrogenase (IMPDH) prevents IMP conversion to AMP and GMP

Adverse Reaction:

*Pancreatitis *liver toxicity *bone marrow suppression

Front 3

6-thioguanine

Back 3

Purine Analogue

Mechanism:

*S-phase of cell cycle
*Inhibits Purine Synthesis
*Inhibits Inosine monophosphate dehydrogenase (IMPDH) prevents IMP conversion to AMP and GMP
*Inhibits DNA replication

Adverse Reaction:

*Pancreatitis *liver toxicity *bone marrow suppression

Front 4

5-fluoroacil

Back 4

Pyrimidine Analogue

Mechanism:

*S-phase of cell cycle
*Inhibits Pyrimidine synthesis.
*Inhibits Thymidylate synthase

Adverse Reaction:

*leucopenia *thrombocytopenia *agranulocytosis *coronary vasospasm

Front 5

Hydroxyurea

Back 5

Purine and Pyrimidine Synthesis Inhibitor

Mechanism:

*S-phase of cell cycle
*Inhibits purine and pyrimidine synthesis
*Inhibits ribonucleuotide reductase --> cannot convert nucleuotides to deoxynucleotides

Adverse Reaction:

*Leukemia

Front 6

Vinblastine

Back 6

Microtubule polymerization inhibitors

Mechanism:

*M-phase of cell cycle
*Inhibit microtubule polymerization --> cannot synthesize DNA and RNA

Adverse Reaction:

*myelosuppression *peripheral neuropathy *ototoxicity *seizures *SIADH

Front 7

Vincristine

Back 7

Microtubule polymerization inhibitors

Mechanism:

*M-phase of cell cycle
*Inhibit microtubule polymerization --> cannot synthesize DNA and RNA

Adverse Reaction:

*myelosuppression *peripheral neuropathy *ototoxicity *seizures *SIADH

Front 8

Paclitaxel

Back 8

Microtubule de-polymerization inhibitor

Mechanism:

*M-phase of cell cycle
*Inhibit microtubule de-polymerization by binding to B-tubulin

Adverse Reaction:

*more hypersensitivity than docetaxel *anaphylaxis

Front 9

Docetaxel

Back 9

Microtubule de-polymerization inhibitor

Mechanism:

*M-phase of cell cycle
*Inhibit microtubule de-polymerization by binding to B-tubulin

Adverse Reaction:

*More neutropenia than paclitaxel

Front 10

Mechlorethamine (mustargen)

Back 10

DNA interactive agents/alkylating agents - Nitrogen Mustards

Mechanism:

*Non-cell cycle specific
*Covalently binds and crosslinks DNA via alkylation of guanine

Adverse Reaction:

*Acute myelogenous leukemia.

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Cyclophosphamide

Back 11

DNA interactive agents/alkylating agents - Nitrogen Mustards

Mechanism:

*Non-cell cycle specific
*Activated by CyP450
*covalently binds and cross links DNA via alkylation of guanine

Adverse Reaction:

*Hemorrhagic cystitis *cardiotoxicity

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Melphalan

Back 12

DNA interactive agents/alkylating agents - Nitrogen Mustards

Mechanism:

*Non-cell cycle specific
*Covalently binds and crosslinks DNA via alkylation of guanine

Adverse Reaction:

*Acute myelogenous leukemia

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Carmustine

Back 13

Nitrosoureas

Mechanism:

*non-cell cycle specific
*Crosses Blood brain barrier
*Covalently binds and crosslinks DNA via alkylation of guanine

Adverse Reaction:

*pulmonary fibrosis *renal failure

Front 14

Cisplatin

Back 14

Platinum Coordinator

Mechanism:

*non-cell cycle specific
*Covalently binds and crosslinks DNA via alkylation of guanine
*requires hydration (prevents renal toxicity)


Adverse Reaction:

*nephrotoxicity, neurotoxicity, ototoxicity

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Carboplatin

Back 15

Platinum Coordinator

Mechanism:

*non-cell cycle specific
*Covalently binds and crosslinks DNA via alkylation of guanine
*does not require hydration

Adverse Reaction:

*neurotoxicity

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Bleomycin

Back 16

Bleomycins

Mechanism:

*oxidative damage to deoxyribose of thymidylate and other nucleotides --> breaks in DNA

Adverse Reaction:

*Pulmonary fibrosis

Front 17

Busulfan

Back 17

Bleomycins

Mechanism:

*covalently binds and crosslinks DNA via alkylation of guanine
*metabolized after alkylation

Adverse Reaction:

*pulmonary fibrosis *reproductive toxicity *teratogenesis

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Mitomycin

Back 18

Bleomycins

Mechanism:

*covalently binds and crosslinks DNA via alkylation of adenine and guanine --> single and double strand DNA breaks *chromosome breaks

Adverse Reaction:

*stomatitis *fever *dermatitis

Front 19

Irinotecan

Back 19

Topoisomerase Interactant

Mechanism:

*binds and stabilizes topoisomerase 1 cleavable complex --> accumulation of DNA single-strand breaks

Adverse Reaction:

*severe diarrhea *thromboembolism

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Doxorubicin

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Anthracyclins – antibiotic chemotherapeutic agents

Mechanism:

*Blocks transcription of DNA polymerase and RNA polymerase

Adverse Reaction:

*cardiotoxicity

Front 21

Tamoxifen

Back 21

Estrogen receptor modulator

Mechanism:

*Inhibits estrogen binding to estrogen receptors in some tissues (breast) *estrogen agonist effects in other tissues (cardiac)

Adverse Reaction:

*endometrial cancer *thromboembolism *hot flushes

Front 22

Goserelin Acetate

Back 22

Anti-androgen

Mechanism:

*Gonadotropin Releaseing Hormone Analog --> transient ↑ of FSH and LH --> followed by ↓ in FSH and LH

Adverse Reaction:

*pain at injection site *gynecomastica *impotence

Front 23

Imatinib Mesylate (Gleevec)

Back 23

Anti-androgen

Mechanism:

*inhibits tyrosine kinase of Platelet derived growth factor receptor (PDGFR) *inhibits ABL kinase (BCR-ABL fusion protein of t(9;22)

Adverse Reaction:

*idiopathic hypereosinophilic syndrome

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Thalidomide

Back 24

Miscellaneous

Mechanism:

*inhibits angiogenesis by inhibiting formation of new blood vessels from existing vasculature.

Adverse Reaction:

*teratogenesis