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Heme/Onc > Pharmacology > Flashcards

Pharmacology Flashcards

1
Q

HIV Entry Inhibitors

A

Enfuvertide

Maraviroc

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2
Q

Maraviroc

A

Blocks CCR5; viral resistance with mutations in gp120
Metabolized via CYP3A4
Rash, infections, hepatotoxicity, MI, allergic reaction

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3
Q

Enfuvertide

A

Blocks gp41 fusion - prevents fusion of HIV

Mimics HR2, binds to HR1

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4
Q

NRTIs

A

Nucleoside Reverse Transcriptase Inhibitors
- Cause chain termination
- Resemble & compete with nucleotides
Accumulates in ALL cells but affinity for HIV RT is more than that for cell DNA pool

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5
Q

Adverse effects of NRTIs

A

High affinity for mitochondrial DNA polymerase

  • Bone marrow suppression
  • Hepatomegaly with steatosis
  • Optic neuritis, peripheral neuropathy
  • Pancreatitis
  • Lactic acidosis
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6
Q

NRTIs

A 
Zidovudine
Lamivudine
Abacavir
Tenofovir
Emtricitabine
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7
Q

Zidovudine

A

aka AZT - first antiretroviral made available

- Nucleoside analog with altered sugar moiety

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8
Q

Lamivudine

A

Less toxicity than Zidovudine

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9
Q

Abacavir

A

Contraindicated in HLA-B*5701 due to hypersensitivity reaction

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10
Q

Tenofovir

A

Lactic acidosis, hepatotoxicity

Only actual nucleotide

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11
Q

Emtricitabine

A

used in polytherapy

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12
Q

NNRTIs

A

Nevirapine
Delaviridine, Efavirenz
Directly inhibit viral RT pool, do not need enzymatic activation, does not affect host DNA polymerase
Resistance common

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13
Q

Adverse effects of NNRTIs

A

Rash
Psychiatric (depression, suicidal thoughts)
Insomnia

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14
Q

Integrase inhibitors

A

Raltegravir (-tegravir)

Inhibits integration of HIV cDNA into host DNA

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15
Q

Adverse effects of Integrase inhibitors

A

Insomnia, flu-like

Suicidal risks, renal failure, rhabdomyolysis

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16
Q

Protease inhibitors

A

Darunavir, Ritonavir, Saquinavir
Atazanavir, Fosamprenavir, Indinavir, Lopinavir
Bind to protease active site, prevent viral polyprotein cleavage

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17
Q

Adverse effects of Protease Inhibitors

A

Nausea/vomiting, loss of appetite, diarrhea, extremity numbness
Liver problems, pancreatitis, allergic reactions, arrhythmias
Also - Hyperlipidemia, insulin resistance, lipodystrophy

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18
Q

Ritonavir

A

Protease inhibitor - inhibits CYP3A4

Used to enhance other PIs (lower doses(

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19
Q

Cobicistat

A

Not a PI, used to lower dose of other antiretrovirals

Used with Elvitegravir (Integrase inhibitor)

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20
Q

HIV Regimen

A

Polytherapy, individualized to combat drug resistance

2 NRTIs with 1 PI (w/ Ritonavir)

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21
Q

Innate immunity

A 
1st defense against Pathogens
Physical barriers (skin)
Biochemical (component, lysozyme, interferons)
Cellular components (neutrophils, macrophages, NK T-cells)
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22
Q

Hypersensitivity Type I

A

Immediate, IgE mediated
Cells degranulate, release of histamine, leukotrienes
Eosinophils
Can cause anaphylaxis

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23
Q

Hypersensitivity Type II

A

Formation of antibody-antigen complexes between foreign antigen and IgM or IgG
Ex: Blood transfusion reaction, can be drug-induced (Penicillin)

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24
Q

Hypersensitivity Type III

A

Antigen/Antibody complexes deposit on basement membrane in tissue and vessels
Activation of complement to produce components with anaphylatoxic and chemotactic activity
Rash and arthritis
3-4 days after exposure to antigen

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25
Q

Hypersensitivity Type IV

A

Delayed Hypersensitivity
Cell-mediated, antigen-specific TH1 cells
Induces local inflammatory response
Influx of antigen-nonspecific inflammatory cells, macrophages
Poison Ivy, PPD

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26
Q

X-linked Agammaglobulinemia

A

Failure of immature B-lymphocytes to mature into antibody-producing plasma cells due to defect in Bruton’s Tyrosine Kinase
Susceptibility to recurrent bacterial infectinos

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27
Q

DiGeorge’s Syndrome

A

Deletion of 22q11, failure of 3rd and 4th pharyngeal arches to develop
Failure of thymus to develop, Diminished T-cell responses
Increased susceptibility to Viruses and Fungi

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28
Q

SCID

A

Defect in ADA enzyme leads to accumulation of toxic-deoxy ATP in cells
Leads to death of T and B lymphocytes
Treat with purified enzyme (pegademase) and transfer of ADA-gene modified lymphocytes

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29
Q

What is the effect of HIV/AIDS on T Cells

A

Depletes CD4 helper cells, imbalance of TH1/TH2

Increased TH2 leads to hypergammaglobulinemia, loss of cytotoxic lymphocyte activity and delayed hypersensitivity

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30
Q

Glucocorticoids

A

First hormonal agents with lymphocytic properties
Decrease size and lymphoid content of lymph node and spleen
Modify cellular function - no direct cytotoxicity; toxic to some T-Cells

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31
Q

Function of glucocorticoids

A

Diminish function of primary antibody; modulate allergic reactions

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32
Q

Clinical use of glucocorticoids

A

Used for treatment of asthma or premedication for blood products or chemotherapy

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33
Q

Cyclosporine

A

Calcineurin inhibitor
Forms complex with cyclophilin which inhibits cytoplasmic phsphatase calcineurin
Metabolized by P450

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34
Q

Use of calcineurin inhibitors

A

Organ transplantation
Treat graft vs. host disease after hematopoietic stem cell transplantation
Some autoimmune disorders

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35
Q

Calcineurin

A

Required for activation of T-cell-specific transcription factor NF-AT - involved in synthesis of ILs by activated T cells

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36
Q

Toxicities of Calcineurin inhibitors (i.e. Cyclosporine)

A

Nephrotoxicity, hypertension, hyperglycemia, liver dysfunction, hyperkalemia, altered mental status, seizures, hirsutism

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37
Q

Tacrolimus

A

Calcineurin Inhibitor FK506
Binds to immunophilin FK-binding protein
10-100x more potent in inhibiting immune response than cyclosporine
Metabolized by P450

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38
Q

How is dosage of tacrolimus determined?

A

Trough blood level at steady state

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39
Q

Toxicities of Tacrolimus

A

Nephrotoxicity, neurotoxicity, hyperglycemia, hypertension, hyperkalemia, GI complains

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40
Q

Proliferation Signal Inhibitors

A

Sirolimus (rapamycin), Everolimus
Bind to Immunophilin FK506 binding protein 12
Forms active complex that blocks mTOR
Given PO

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41
Q

mTOR

A

Molecular target of Rapamycin

Component of complex intracellular pathway involved in cell growth, proliferation, angiogenesis, and metabolism

42
Q

Mechanism of Proliferation Signal Inhibitors (PSIs)

A

Blocking mTOR can lead to inhibition of IL-driven T-cell proliferation
Also inhibition of B-cell proliferation and Ig production

43
Q

PSI toxicities

A

P450 metabolism - significant drug interactions

Myelosuppression, hepatotoxicity, diarrhea, hypertriglyceridemia, pneumonitis, and HA

44
Q

Mycophenolate Mofetil

A

aka MMF
Inhibits T and B-lymphocyte responses by inhibiting de novo synthesis of purines
Not metabolized by P450 but interactions still occur

45
Q

Thalidomide

A

Sedative drug - severe teratogenic effects
Immunomodulatory agent, inhibits angiogenesis
Anti-inflammatory

46
Q

Mechanism of Thalidomide

A

Inhibits TNF-alpha, reduces phagocytosis by neutrophils
Increases production of IL-10
Enhances cell-mediated immunity via interactions with T cells, alters adhesion molecule expression

47
Q

Indications for Thalidomide

A

Used for treatment of multiple myeloma and leprosy

48
Q

Adverse effects of Thalidomide

A

Teratogenicity, peripheral neuropathy, constipation, rash, fatigue, hypothyroidism, increased DVT

49
Q

Lenalidomide

A

Novel immunomodulatory agent
More potent, less toxic than thalidomide
Used for myelodysplastic syndrome and relapsed and refractory myeloma

50
Q

Azathioprine

A

Prodrug of mercaptopurine, functions as anti-metabolite

Xanthine oxidase splits mercaptopurine to 6-thiouric acid prior to excretion - drug interaction with allopurinol

51
Q

Use of Azathioprine

A

Maintain renal allografts

Other solid organ transplants

52
Q

Toxicities of Azathioprine

A

Bone marrow suppression
Skin rash
Fever, nausea, vomiting, diarrhea, hepatotoxicity

53
Q

Leflunomide

A

Prodrug of inhibitor of pyrimidine synthesis, given PO
Long half-life
Only for RA
Increase in liver enzymes, renal impairment, teratogenicity

54
Q

Hydroxychloroquine

A

Antimalarial agent - suppresses intracellular antigen processing and loading onto MHC II molecules
Increases pH of lyosomal and endosomal compartments
Decreases T cell activation

55
Q

Indications for Hydroxychloroquine

A

RA

SLE

56
Q

Antilymphocyte and antithymocyte antibodies

A

Used for suppressing T cells
Used in solid organ and stem cell transplants
Can cause lymphoma in renal transplant patients

57
Q

Immune Globulin Intravenous (IVIG)

A

Pool of different antibodies have normalizing effects upon patient’s immune response
Used for autoimmune disordersm Ig deficiencies, HIV, bone marrow transplants

58
Q

Classes of Monocloncal antibodies used in treatment of cancer

A

Unconjugated

Immunoconjugates conjugated to toxin (immunotoxin), chemotherapy agent, radioactive particle

59
Q

-omab

A

Murine (mouse) monoclonal antibody

60
Q

-umab

A

Human monoclonal antibody

61
Q

-ximab

A

Chimeric monoclonal antibody

62
Q

-zumab

A

Humanized monoclonal antibody

63
Q

Alemtuzumab

A

Recombinant humanized monoclonal antibody against CD52 - induces cell lysis and death of B, T, NK lymphocytes and macrophages
Used for Relapsed/Refractory B-cell CLL

64
Q

Toxicity of Alemtuzumab

A

Severe infusion reactions (anaphylaxis)
Hematologic toxicity
Opportunistic infections (black box warning) - premedicate with diphenhydramine and acetaminophen

65
Q

Bevacizumab

A

Recombinant humanized MAb against circulating VEGF

Used for colorectal cancer, NSCLC, breast cancer

66
Q

Toxicities of Bevacizumab

A

Hypertension, infusion related syndromes, proteinuria, thrombotic events, black box warning for GI perforation
DO NOT USE WITHIN 28 days of major surgery

67
Q

Cetuximab

A

Recombinant chimeric MAb that binds to extracellular domain of EGFR on both normal and tumor cells
Inhibits cell growth, induces apoptosis
Colorectal cancer, head and neck cancer

68
Q

Toxicity of Cetuximab

A 
Infusion related syndromes
Development of acne-like rash
Constitutional symptoms (asthenia, fatigue)
GI complaints
Abdominal pain
Hypomagnesemia
69
Q

Retuximab

A

Chimeric MAb against CD20 on normal and malignant B cells

First-line therapy for CD20 positive B-cell NHL, relapsed or refractory CD20 positive B-cell NHL

70
Q

Toxicity of Retuximab

A

Tumor lysis syndrome, opportunistic infections
Cough, dyspnea, rhinitis or sinusitis
Infusion reactions and other severe reactions (within 30-120 mins of starting infusion)

71
Q

Treatment of severe reactions to Retuximab

A

Cessation or slowing of infusion and symptomatic treatment

Infusion-related syndromes decrease with subsequent infusions

72
Q

Trastuzumab

A

Humanized MAb binds to HER-2, inhibits cell-cycle progression by decreasing cells entering S-phase
Drug interactions with anthracyclines and taxanes
Used for breast cancer

73
Q

Trastuzumab toxicity

A

Cardiomyopathy, infusion-related reactions, hypersensitivity reactions, N/V, diarrhea, myelosuppression

74
Q

Treatment of vasculitis

A

Steroids
Cyclophosphamide
Azathioprine
Plasma exchange

75
Q

Treatment of Goodpasture’s Disease

A

Prednisolone
Cyclophosphamide
Plasma Exchange

76
Q

Treatment of SLE

A

Steroids (Prednisolone tablets, methylprednisone IV)
Cyclophosphamide
Azathioprine

77
Q

Treatment of Sjogren’s Syndrome

A

Hydroxychloroquine

78
Q

Treatment of Dermatomyositis

A 
Prednisone
Methotrexate
Azathioprine
Mycophenolate
Hydroxychloroquine
Chloroquine
79
Q

Treatment of Psoriasis

A

Betamythasone, 0.05% cream

Cyclosporine

80
Q

Four most common cancers

A

Prostate
Breast
Lung - most common cause of cancer-related deaths in US
Colorectal

81
Q

Steps of Carcinogenesis

A

Initiation
Promotion
Conversion/Transformation
Progression

82
Q

Tissue types from which tumors may arise

A

Epithelial tissue
Connective Tissue
Lymphoid Tissue
Nerve Tissue

83
Q

Adjuvant therapy

A

The use of systemic agents to eradicate micrometastatic disease following localized modalities such as surgery or radiation or both

84
Q

Neoadjuvant therapy

A

Drug therapy given preoperatively - make other treatment modalities more effective by reducing tumor burden and destroying micrometastases

85
Q

Lab values required prior to administration of Chemo

A

WBC > or = 3,000
ANC > or = 1,500
Platelet count > or = 100,000
Renal and Hepatic function

86
Q

Cure

A

Implies that the patient is entirely free of disease and has the same life expectancy of a cancer-free individual

87
Q

Complete response

A

Means complete disappearance of all cancer without evidence of new disease for at least 1 month after treatment

88
Q

Partial response

A

Defined as 30% or greater decrease in tumor size or other objective disease markers and no evidence of any new disease for at least 1 month

89
Q

Stable disease

A

Tumor neither grows nor shrinks

90
Q

Progressive disease

A

20% increase in tumor size or development of any new lesions while receiving treatment

91
Q

Cell-cycle Specific Anti-Neoplastic Agents

A 
Antimetabolites
Taxanes
Vinca alkaloids
Epipodophyllotoxins
Antitumor antibiotics
92
Q

Cell-cycle Non-specific Anti-Neoplastic Agents

A 
Alkylating agents
Anthracyclines
Platinum analogs
Camptothecins
Antitumor antibiotics
93
Q

Antimetabolites/Antifolates

A

Folate vitamins essential cofactors in DNA synthesis

Dihydrofolate reductase inhibited by methotrexate and other antifolates

94
Q

Methotrexate

A

Anti-folate, transported intracellularly by active transport system like physiologic folates

95
Q

Methotrexate toxicity

A

Myelosuppression, mucositis, diarrhea

Leucovorin used as rescue agent

96
Q

Pemetrexed

A

Multitargeted antifolate that inhibits pathways in thymidine and purine synthesis
Decreased risk of development of drug resistance

97
Q

Indications for Pemetrexed

A

NSCLC, being studied in breast cancer

98
Q

Toxicity of Pemetrexed

A

Myelosuppression, Nausea/Vomiting, mucositis, diarrhea, constipation

99
Q

Fluorouracil (5-FU)

A

Prodrug - must be metabolized to nucleotide form

Lecovorin enhances cytotoxicity

100
Q

Toxicity of Fluorouracil

A

Myelosuppression, Diarrhea, mucositis, hand-foot syndrome ( painful tingling, erythema, rash, dryness, desquamation of hands and feet)

Heme/Onc (2 decks)

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