Heme-onc Pharmacology Flashcards by Stephanie Joppa

Heparin toxicity

Bleeding, duh. Also, HIT.

Use protamine.

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Heparin-MOA

Cofactor for activation antithrombin. Decreases thrombin, Xa.

Monitor PTT.

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Warfarin-MOA

Interferes with gamma carboxylation of vit k dependent clotting factors II, VII, IX, X, protein C and protein S.

Extrinsic pathway. Increases PT.

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Warfarin-toxicity

Bleeding.

Teratogenic (“don’t wage WAR on the baby”)

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Thrombolytics (streptokinase, urokinase, tPA=alteplase, APSAC)

Aids conversion plasminogen to plasmin.

Plasmin cleaves thrombin and fibrin clots.

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Thrombolytics, clinical use

Early MI, early CVA

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Aspirin, MOA

Irreversibly inhibits COX.

Increases bleeding time, no effect on PT, PTT

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Aspirin, clinical use

Antipyretic, analgesic, anti inflammatory, antiplatelet

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Aspirin, toxicity

Gastric ulceration, bleeding, hyperventilation, Reye’s syndrome (kids), tinnitus

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Clopidogrel, MOA

Blocks ADP irreversibly

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Clopidogrel, clinical use

ACS, coronary stenting

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Abciximab, MOA

Binds GpIIb/IIIa on platelets, inhibiting aggregation

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Abciximab, clinical use

ACS, PTCA

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Abciximab, toxicity

Bleeding, thrombocytopenia

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Antimetabolites

Act on S phase of cell cycle

Methotrexate
5-FU
6-MP
6-TG
Cytarabine

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Methotrexate, MOA

Folic acid analog, inhibits dihydrofolate reductase.

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Methotrexate, clinical use

Cancer-leukemia, lymphomas, choriocarcinomas, sarcomas

Other-abortion, ectopic pregnancy, RA, psoriasis

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Methotrexate, toxicity

Myelosuppression-reversible with leucovorin

Fatty liver, mucositosis, teratogenic

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5-FU (fluorouracil), MOA

Pyramiding analog, inhibits thymidylate synthase

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5-FU, clinical use

Colon cancer and other solid tumors, BCC.

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5-FU, toxicity

Myelosuppression
Photosensitivity

Tx OD with thymidine

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6-mercaptopurine (MP), MOA

Purine analog, decreases de novo purine synthesis

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6-MP, clinical use

Leukemias, lymphomas

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6-MP, toxicity

Bone marrow, GI, liver.

Metabolized by Xanthine oxidase so increased toxicity if used with allopurinol.

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6-thioguanine (TG), MOA

Purine analog, decreases de novo purine synthesis

6-TG, clinical use

ALL

6-TG, toxicity

Bone marrow depression, liver. Can be given with allopurinol.

Cytarabine, MOA

Pyrimidine analog

Cytarabine, clinical use

AML, ALL, high grade NHL.

Cytarabine, toxicity

Leukopenia, thrombocytopenia, megaloblastic anemia

Dactinomycin, MOA

DNA intercalating agent

Dactinomycin, clinical use

Wilms tumor, Ewing's sarcoma, rhabdomyosarcoma. | I.e. Kids tumors

Doxorubicin, daunorubicin, MOA

Generates free radicals | Noncovalently intercalates in DNA

Doxorubicin, duanorubicin, clinical use

Hodgkins | Myelomas, a sarcomas, solid tumors (breast, ovary, lung)

Doxorubicin, daunorubicin, toxicity

Cardiotoxicity (DCM), myelosuppression, alopecia. | Dexrazoxane used to prevent cardiotoxicity

Bleomycin, MOA

Induces ROS, which cause strand breaks

Bleomycin, clinical use

Testicular cancer, Hodgkins

Bleomycin, toxicity

Pulmonary fibrosis Skin changes Minimal myelosuppression

Etoposide, MOA

Inhibits topoisomerase II

Etoposide, clinical use

Small cell of lung and prostate, testic carcinoma

Etoposide, toxicity

Myelosuppression, GI irritation, alopecia

Cyclophosphamide, MOA

Alkylation agent. Requires bioactivation by liver.

Cyclophosphamide, clinical use

NHL, breast and ovarian carcinoma. Also, immunosuppression

Cyclophosphamide, toxicity

``` Myelosuppression Hemorrhagic cystitis (partially prevented it with mesna) ```

Nitrosoureas, MOA

Alkylating agent that crosses BBB

Nitrosoureas, clinical use

Brain tumors

Nitrosoureas, toxicity

CNS toxicity (dizziness, ataxia)

Busulfan, MOA

Alkylates DNA

Busulfan, clinical use

CML. Also to ablate pt's bone marrow before transplant

Busulfan, toxicity

Pulmonary fibrosis, hyper pigmentation

Vincristine, Vinblastine, MOA

Bind to Tubulin in M phase to prevent microtubule polymerization

Vincristine, Vinblastine, clinical use

Hodgkins, Wilms tumor, choriocarcinoma, ALL

Vincristine, vinblastine, toxicity

Vincristine-neurotoxicity, paralytic ileus | Vinblastine-bone marrow suppression

Paclitaxel, taxols, MOA

Prevent mitotic spindle breakdown

Paclitaxel, taxols, clinical use

Ovarian and breast carcinomas

Paclitaxel, taxols, toxicity

Myelosuppression, hypersensitivity

Cisplatin, carboplatin, MOA

Cross link DNA

Cisplatin, carboplatin, clinical use

Testicular, bladder, ovary, lung carcinoma

Cisplatin, carboplatin, toxicity

Nephrotoxicity and acoustic nerve damage. Prevent nephrotoxicity with amifostine (free radical scavenger

Hydroxyurea, MOA

Inhibits ribonucleotide reductase thus inhibits S phase Also increases HbF

Prednisone MOA

May trigger apoptosis

Prednisone clinical use

CLL, Hodgkins, immunosuppressant in AI diseases

Prednisone toxicity

Cushing like sxs

Tamoxifen, MOA

SERM-receptor antagonist in breast, agonist in bone.

Tamoxifen toxicity

Increases risk endometrial carcinoma. Hot flashes.

Trastuzumab (herceptin), MOA

Monoclonal Ab against HER-2, a tyrosine kinase.

Trastuzumab, toxicity

Cardio toxicity

Imantinib, MOA

Bcr-abl tyrosine kinase inhibitor

Imantinib, clinical use

CML, GI stromal tumors

Imantinib, toxicity

Fluid retention

Rituximab, MOA

Monoclonal Ab against CD20, which is found on most B cell neoplasms

Rituximab, clinical use

NHL, RA

Aminocaproic acid

Reverses tPA

Protamine sulfate

Reverses heparin

Filgramstim

Granulocyte stimulating factor