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Oncology > Pharm > Flashcards

Pharm Flashcards

1
Q

Heparin MOA

A

Activates antithrombin, which decreases action of IIa (thrombin) and factor Xa
LMWH acts predonminantly on factor Xa
Fondaparinux acts only on factor Xa
Acts in blood

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2
Q

Which anticoagulant does not cross the placenta?

A

Heparin

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3
Q

Which are the direct thrombin inhibitiors?

A

Bivalirudin
Argatroban
Dabigatran

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4
Q

Warfarin MOA

A

Interferes with gamma-carboxylation of vitamin-K dependent clotting facotrs II, VII, IX, and X, and protein C and S
Affects on extrinsic pathway (increases PT)
Acts @ liver

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5
Q

Which are the direct factor Xa inhibitors?

A

Apixaban

Rivoroxaban

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6
Q

How do thrombolytics work?

A

Directly or indirectly aid conversion of plasminogen to plasmin, which cleaves thrombin and fibrin clots
Increases PT
Increases PTT
No change in platelet count

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7
Q

Which are the ADP receptor inhibitors?

A

clopidogrel
prasugrel
ticagrelor (reversible)
ticlopidine

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8
Q

How do ADP receptor inhibitors work?

A

Inhibit platelet aggregation by irreversibly blocking ADP (P2Y12) receptor
Prevent expression of glycoproteins IIb/IIIa on platelet surface

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9
Q

Which are the glycoprotein IIb/IIIa inhibitors?

A

Abciximab - made from monoclonal antibody Fab fragments
Eptifibatide
Tirofiban
(prevent platelet agg)

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10
Q

Azathioprine MOA and use

A

Purine (thiol) analog
Leads to decreased purine synthesis
Metabolized into 6-MP
Used to prevent organ rejection, RA, IBD, SLE

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11
Q

With which medications should azathioprine NOT be used?

A

Azathioprine and 6-MP are metabolized by xanthine oxidase; therefore, both have increased toxicity when used with allopurinol or febuxostat

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12
Q

Cladribine MOA, use, and adverse effects

A

Purine analog with multiple mechs (inhibition of DNA polymerase, DNA strand breaks)
Used in hair cell leukemia
SEs: myelosuppression, nephrotoxicity, neurotoxicity

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13
Q

Cytarabine MOA, use, and adverse effects

A

Pyrimidine analog that results in DNA chain termination. At higher doses, also inhibits DNA pol
Used for leukemias and lymphomas
SEs: myelosuppression with megaloblastic anemia (“CYTarabine with panCYTopenia”)

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14
Q

5FU MOA, use, and adverse effects

A

Pyrimidine analog bioactivated to 5-FdUMP, which complexes with thymidylate synthase and folic acid
Complex inhibits thymidylate synthase, leading to decreased dTMP and decreased DNA synthesis
Used in colon cancer, pancreatic cancer, actinic keratosis, basal cell carcinoma
SEs: myelosuppression, palmar-plantar erythrodysesthesia (hand-foot syndrome)

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15
Q

Methotrexate MOA, use, and adverse effects

A

Folic acid analog that competitively inhibits dihydrofolate reductase, leading to decreased dTMP and decreased DNA synthesis
Used in lymphomas, leukemias, choriocarcinoma, sarcomas. Non-neoplastic: can also be used in ectopic pregnancy, medical abortion (with misoprostol), RA, PsC, IBD, vasculitis
SEs: myelosuppression, hepatotoxicity, mucositis, pulmonary fibrosis, folate deficiency, rare nephrotoxicity

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16
Q

Bleomycin MOA, use, and adverse effects

A

Antitumor antibiotic
Induces free radical formation, leading to breaks in DNA strands
Used in testicular cancer and Hodgkin’s lymphoma
SEs: Pulmonary fibrosis, skin hyperpigmentation

17
Q

Dactinomycin MOA, use, and adverse effects

A

Antitumor antibiotic
Intercalates into DNA, preventing RNA synthesis
Used in Wilms tumor, Ewing sarcoma, rhabdomyosarcoma; also used for childhood tumors
SEs: myelosuppresion

18
Q

Doxorubicin MOA, use, and adverse effects

A

Antitumor antibiotic
Generates free radicals. Intercalates DNA leading to breaks in DNA and decreased replication. Interferes with topoisomerase II enzyme
Used in solid tumors, leukemias, lymphomas
SEs: cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia
Dexrazoxane can be used to prevent cardiotoxicyt

19
Q

Busulfan MOA, use, and adverse effects

A

Alkylating agent
Cross-links DNA
Used to ablate patient’s bone marrow before bone marrow transplantation
SEs: severe myelosuppression (in almost all cases), pulmonary fibrosis, hyperpigmentation

20
Q

Cyclophosphamide and/or ifosfamide MOA, use, and adverse effects

A

Alkylating agent
Cross-link DNA at guanine
Requires bioactivation by liver
Used in solid tumors, leukemia, lymphomas
SEs: myelosuppression, SIADH, hemorrhagic cystitis
- NOTE: hem cystitis is prevented with mesna and/or adequate hydration

21
Q

Nitrosoureas MOA, use, and adverse effects

A

Alkylating agent
Requires bioactivation. Cross blood-brain barrier. Cross-links DNA.
Used for brain tumors (including GBM)
SEs: CNS toxicity (convulsions, dizziness, ataxia)

22
Q

Procarbazine MOA, use, and adverse effects

A

Alkylating agent
Cell cycle phase: nonspecific alkylating agent (mech not yet defined)
Used for Hodgkin lymphoma, brain tumors
SEs: bone marrow suppression, pulmonary toxicity, leukemia

23
Q

Taxanes (aka paclitaxel) MOA, use, and adverse effects

A

Microtubule inhibitor
Hyperstabilizes polymerized microtubules in M phase so that mitotic spindle cannot break down (anaphase cannot occur)
Used for ovarian and breast carcinomas
SEs: myelosuppression, neuropathy, hypersensitivity

24
Q

Vincristine, vinblastine MOA, use, and adverse effects

A

Microtubule inhibitor
Vinca alkaloids that bind beta-tubulin and inhibit its polymerization into microtubules leading to prevention of mitotic spindle formation (M-phase arrest)
Used for solid tumors, leukemias, Hodgkin’s (vinblastine) and Non-Hodgkin’s (vincristine) lymphomas
SEs: Vincristine: neurotoxicity (areflexia, peripheral neuritis), constipation (including paralytic ileus)
Vinblastine: bone marrow suppression - “blasts the bone marrow”

25
Q

Cisplatin MOA, use, and adverse effects

A

Cross-links DNA
Used in testicular, bladder, ovary, and lung carcinomas
SEs: nephrotoxicity, peripheral neuropathy, ototoxicity
Prevent nephrotoxicity with amifostine (free radical scavenger) and chloride (saline) diuresis

26
Q

Etoposide/tenoposide MOA, use, and adverse effects

A

Inhibits topoisomerase II leading to increased DNA degradation
Used in solid tumors (particularly testicular and small cell lung cancer), leukemias, lymphomas
SEs: myelosuppression, alopecia

27
Q

Irinotecan/topotecan MOA, use, and adverse effects

A

Inhibit topoisomerase I and prevent DNA unwinding and replication
Used in colon cancer (irinotecan); ovarian and small cell lung cancers (topotecan)
SEs: severe myelosuppression, diarrhea

28
Q

Hydroxyurea MOA, use, and adverse effects

A

Inhibits ribonucleotide reductase leading to decreased DNA synthesis (S-phase specific)
Used in myeloproliferative disorders (eg CML, polycythemia vera), sickle cell (increases HbF)
SEs: severe myelosuppression

29
Q

Bevacizumab MOA, use, and adverse effects

A

Monoclonal antibody against VEGF. Inhibits angiogenesis (“BeVacizumab inhibits Blood Vessel formation”)
Used in solid tumors (colorectal cancer, renal cell carcinoma), wet age-related macular degeneration
SEs: hemorrhage, blood clots, impaired wound healing

30
Q

Erlotinib MOA, use, and adverse effects

A

EGFR tyrosine kinase inhibitor
Used in non-small cell lung carcinoma
SEs: rash

31
Q

Cetuximab MOA, use, and adverse effects

A

Monoclonal antibody against EGFR
Used in Stage IV colorectal cancer (wild-type KRAS), head and neck cancer
SEs: rash, elevated LFTs, diarrhea

32
Q

Imatinib MOA, use, and adverse effects

A

Tyrosine kinase inhibitor of BCR-ABL (Philadelphia chromosome fusion gene in CML) and c-kit (common in GI stromal tumors)
Used in CML, GI stromal tumors (GIST)
SEs: fluid retention

33
Q

Rituximab MOA, use, and adverse effects

A

Monoclonal antibody against CD20 (found on most B-cell neoplasms)
Used in Non-Hodgkin’s lymphoma, CLL, ITP, RA
Increases risk of progressive multifocal leukoencephalopathy

34
Q

Bortezomib/carfilzomib MOA, use, and adverse effects

A

Proteasome inhibitors, induce arrest at G2-M phase and apoptosis
Used in multiple myeloma, mantle cell lymphoma
SEs: peripheral neuropathy, herpes zoster reativation

35
Q

Tamoxifen/raloxifene MOA, use, and adverse effects

A

Selective estrogen receptor modulators (SERMs) - receptor antagonists in breast and agonists in bone. Block the binding of estrogen to ER+ cells
Used in breast cancer treatment and prevention. Raloxifene also useful to prevent osteoporosis.
SEs: tamoxifen: partial agonist in endometrium, which increases the risk of endometrial cancer; “hot flashes”
raloxifene: no increase in endometrial carcinoma, because it is an estrogen receptor antagonist in endometrial tissue
Both increase risk of thromboembolic events (DVT/PE)

36
Q

Trastuzumab (herceptin) MOA, use, and adverse effects

A

Monoclonal antibody against HER-2 (c-erbB2), a tyrosine kinase receptor. Helps kill cancer cells that overexpress HER-2 through inhibition of HER-2 initiated cellular signaling and antibody-dependent cytotoxicity
Used in HER-2+ breast cancer and gastric cancer
SEs: cardiotoxicity (“heartceptin” damages the heart)

37
Q

Rasburicase MOA, use, and adverse effects

A

Recombinant uricase that catalyzes metabolist of uric acid to allantoin
Used in prevention and treatment of tumor lysis syndrome

38
Q

Vemurafenib MOA, use, and adverse effects

A

Small molecule inhibitor of BRAF+ oncogene in melanoma

VEmuRAF-enib is for V600E-mutated BRAF inhibition

Oncology (3 decks)

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