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Heme-onc drugs > Biweekly 2 > Flashcards

Biweekly 2 Flashcards

1
Q

Bevacizumab

A

VEGF inhibitor
Anti-angiogenesis
MOA: IgG that binds against VEGF
Side Effects: Hypertension, impaired wound healing, bowel perforation, proteinuria, pulmonary hemorrhage, CHF, deep venous and arterial thrombosis, pulmonary embolism, other thrombo-embolic events, reversible posterior leukoencephalopathy syndrome (RLS) .

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2
Q

Bleomycin

A

Antibiotic
Natural Product
MOA: Mixture of fungal glycopeptides. Strandcision. It binds to DNA and binds to iron atom, and oxidizes it, and these nip up DNA.
Inhibits S/G2 phase of cell cycle.
Side Effects: Main one is pulmonary, there is dose dependent toxicity and idiosyncratic.

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3
Q

Carboplatin

A

Alkylating Agent
Platinum Coordination
MOA: Gets hydroxylated to get activated, and they are alkylating, and they cause kinks, breaks, etc in DNA
Side Effects: Less nephrotoxicity, N/V, neuropathy than cisplatin. More myelosupression than cisplatin.

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4
Q

Carmustine

A

Alkylating Agent
Nitrosurea
It is hydrophobic and is injected with alcohol, resulting in burning at site of injection.
SIDE EFFECT: There is myelosupression on days 21-28
Administer every 6-8 weeks
Available in wafers for direct brain implantation

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5
Q

Cetuximab

A

EGFR inhibitor
Monoclonal Antibody
MOA: IgG against extracellular domain of EGFR
Side Effects: Severe anaphylaxis, skin rash, acne, folliculitis, diarrhea, abdominal pain, lung inflammation, hypomagnesemia.

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6
Q

Cisplatin

A

Alkylating Agent
Platinum Coordination
ERCC1 increase leads to cisplatin resistance in lung cancer
MOA: Gets hydroxylated to get activated, and they are alkylating, and they cause kinks, breaks, etc in DNA
Side Effects: More nephrotoxicity, N/V, neuropathy than carboplatin. Less myelosupression than carboplatin.

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7
Q

Cyclophosphamide

A

Alkylating Agent( microsomal P450 activates it)
Nitrogen Mustard
Acrolein, a byproduct, can cause severe hemorrhagic cystitis. MESNA is used as a cryoprotectant
Toxicity: Bone marrow supression days 8-14, cystitis, cardiac toxicity(high doses), immunosupression

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8
Q

Cytarabine (AraC)

A

Antimetabolite
Pyrimidine Antagonist
MOA: Mimic of cytosine. Inhibits at S phase of Cell cycle.
Side effects: Myelosupression, fevers, arthralgias, irreversible cerebellar toxicity, and ocular toxicity

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9
Q

Docetaxel

A

Microtubule inhibitor
Antimitotic Agent
MOA: Stabilizes microtubules, leading to apoptosis( same as paclitaxel). Can be used in cancers resisitant to paclitaxel. Inhibits at M phase of Cell cycle
Side Effects: hypersensitivity, myelosupression, edema)

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10
Q

Doxorubicin

A

Anthracycline
Antibiotic
MOA: Intercalating agent between DNA base pairs and results in free oxygen radicals.
Side Effects: Cardiotoxic( maximal lifetime dose of 550mg/m2), as well as the other normal myelosupressive, N/v etc.

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11
Q

Erlotinib

A 
EGFR inhibitor
Targeted Molecule
T790M mutation in EGFR leads to increase resistance to erlotinib
MOA: Tyrosine kinase inhibitor
Side Effects: Acneiform Rash
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12
Q

Fludarabine

A

Antimetabolite
Purine Antagonist
MOA: Inhibits at S Phase of Cell cycle

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13
Q

5-Fluorouracil

A

Antimetabolite
Pyrimidine Antagonist
Used in combination with leucovorin to increase its activity
MOA: Inhibits both DNA and RNA synthesis. It inhibits thymidylate synthase, and the leucovorin stabilizes the enzyme so it has a greater effect, but also a greater toxicity.
Inhibits at S phase of Cell Cycle
Side Effects: Mucositis, myelosupression, hand-foot syndrome

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14
Q

Imatinib

A

TKI
Targeted Molecule
GLEEVAC USED FOR CML
MOA: Inhibits BCR-ABL tyrosine kinase by binding to ATPase site and inhibiting ATP cleavage and transphosphorylation

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15
Q

Irinotecan

A

Topoisomerase I Inhibitor
Natural Product
MOA: Topoisomerase I inhibitor. Inhibits at S Phase of cell cycle
Side effects: Myelosupression, transaminitis, fever, and the big one is diarrhea; acute and delayed.

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16
Q

Methotrexate

A

Antimetabolite
Folic Acid Antagonist
DHFR increase leads to methotrexate resistance
MOA: Inhibits DHFR, leading to an inability to synthesize DNA. Inhibits at S phase of Cell Cycle
High Dose Methotrexase requires leucovorin rescue
Side Effects: Myelosupression, N/V, mucositis, hepatotoxicity, neurotoxicity, nephrotoxicity.

17
Q

Paclitaxel

A

Microtubule Inhibitor
Semi-natural Product( dissolved in Cremaphor AL, which can lead to anaphylaxis)
MOA: Stabilize microtubules in cell so that the cells cannot dissemble and divide, and they undergo apoptosis. Inhibits at M phse of cell cycle
Side Effects: Hypersensitivity, cardiotoxic, myelosupressive, N/V, alopecia.

18
Q

Rituximab

A

Immunological Agent
Monoclonal Antibody
MOA: IgG against CD20 on B cells
Side Effects:
Cytokine-release syndrome/tumor lysis syndrome
Prolonged and severe lymphopenia, immunosuppression, opportunistic infections, reactivation of viral hepatitis.
Severe mucocutaneous reactions (Rituxan®)
Pancytopenia/bone marrow failure (CAMPATH®)

19
Q

Thalidomide

A

Antiangiogenic Agent
Small Molecule
Side Effects: teratogenic, neurotoxic

20
Q

Trastuzumab

A

Immunological Agent
Monoclonal Antibody
MOA: IgG that targets HER-2/neu, a member of the EGFR family
Side Effects: Congestive heart failure (CHF)/dysfunction, diarrhea

21
Q

Vinblastine

A

Microtubule Inhibitor
Natural Product
MOA: Probably similar to vincristine, mitotic spindle poison, leading to fragmentation of microtubules. Inhibits M phase of cell cycle.

22
Q

Vincristine

A

Microtubule Inhibitor
Natural Product
MOA: Mitotic Spindle Poison, leading to fragmentation of microtubules.
Inhibits M phase of cell cycle
Side Effect: Neuropathy, including constipation

23
Q

mechlorethamine

A

Alkylating Agent

Nitrogen Mustard

24
Q

Leucovorin

A

Used for methotrexate rescue therapy and in combination with 5-FU for modulation

25
Q

Alkylating agents MOA

A

Inactive until metabolized by the P450 system, leads to cross linking of DNA and eventually apoptosis of cell

Heme-onc drugs (1 decks)

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