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Wolff Pharmacology Review > Transplant Drugs & HIV Antiretrovirals > Flashcards

Transplant Drugs & HIV Antiretrovirals Flashcards

1
Q

organ rejection that happens within days due to reactivation of sensitized T cells

A

accelerated

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2
Q

refers to organ rejection that develops over days to weeks in association with primary activation of T cells in response to antigens expressed on the surface of allograft cells and/or on antigen presenting cells that have phagocytosed allograft cell proteins

A

acute

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3
Q

can cause a prolonged and potentially life-threatening asystole in a transplanted (=denervated) heart

A

adenosine

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4
Q

blocking this is a reason to take drugs such a s prednisone, cyclosporine and mycophenolate

A

allograft rejection

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5
Q

xanthine oxidase inhibitor used to prevent gouty arthritis and uric acid nephropathy in patients predisposed to hyperuricemia or having it due to excess cell turnover from cancer +/- chemotherapy; its use mandates a reduction in azathioprine dosage

A

allopurinol

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6
Q

developed in horses or rabbits, administered to selectively inactivate/destroy T cells as part of transplant induction therapy or when they are causing acute rejection of a transplanted organ despite other immunosuppressive therapy

A

antithymocyte globulin

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7
Q

anti-proliferative agent that helped make allogeneic transplantation possible, it is somehow more effective at blocking de novo purine synthesis and DNA replication than direct administration of its active metabolite, 6-mercaptopurine

A

azathioprine

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8
Q

mouse monoclonal antibody against human IL-2 receptor that can be used to inhibit T cell activation/proliferation as part of transplant induction therapy, tolerability was improved by creating a chimera in which the antibody contains a human constant region

A

basiliximab

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9
Q

proliferate and differentiate into antibody-producing plasma cells when fragments of a molecule that was captured by the surface expression of their unique antibody and then inserted into MHC class II antigens on their surface is recognized as foreign by a helper T cell

A

B cells

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10
Q

major adverse effect of most anti-proliferative drugs, increases susceptibility of transplant recipient to infection and bleeding

A

bone marrow suppression

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11
Q

most effective immunosuppressive drugs in routine use

A

calcineurin inhibitors

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12
Q

T cell population that surveys MHC class II molecules for unrecognized peptide fragments derived from phagocytosis, and, upon recognizing a foreign molecule, activates macrophages, stimulates production of antibodies, etc.

A

CD4

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13
Q

T cell population that surveys cell protein synthesis by examining fragments of those proteins inserted into the MHC class 1 proteins on their cell surface, and destroys those cells that are recognized as synthesizing foreign proteins

A

CD8

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14
Q

refers to organ rejection occurring over months to years for which there is ~no effective therapy, characterized by interstitial fibrosis, thickened vascular walls, etc.

A

chronic

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15
Q

pharmacological dosages of exogenous glucocorticoids can also cause this

A

Cushing Syndrome

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16
Q

first drug discovered that caused immunosuppression without bone marrow suppression, its binding to cyclophilin blocks calcineurin-mediated dephosphorylation of NFAT

A

cyclosporine

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17
Q

refers to the unpleasant consequences (e.g., fever, chills, dyspnea, nausea, possibility of anaphylactoid shock) associated with the administration of an antibody generated in a different species; can be especially bad during initial administration but then decreases over time, in part because of concurrent administration of glucocorticoids

A

cytokine release syndrome

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18
Q

risk of developing this is significant following renal transplantation, especially when immunosuppressive drugs are added to glucocorticoids

A

diabetes

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19
Q

a sirolimus-like drug but with a shorter half-life (~30 hrs vs 62 hrs), means steady-state levels can be achieved faster and also that drug will disappear faster if discontinued due to adverse effects

A

everolimus

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20
Q

pharmacological doses blunt acute organ rejection in part by suppressing NFkappaB driven gene expression in cells triggered by the recognition of a foreign antigen

A

glucocorticoids

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21
Q

its de novo synthesis is blocked by mycophenolate; stops proliferation of lymphocytes since they cannot use purine salvage pathways like other cells

A

guanine

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22
Q

potential cosmetic challenge with cyclosporine that is not a problem with tacrolimus

A

hirsutism

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23
Q

organ rejection that occurs within minutes due to preformed antibodies and complement activation

A

hyperacute

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24
Q

side effect of therapy with cyclosporine and sirolimus but not tacrolimus

A

hypercholesterolemia

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25
Q

consequence of the renal afferent arteriolar constriction caused by cyclosporine and tacrolimus in solid organ transplant recipients

A

hypertension

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26
Q

proinflammatory signaling molecule released by antigen-presenting cells that facilitates activation of lymphocytes

A

IL-1

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27
Q

molecule released by activated T cells that binds to receptors on their surface to promote the characteristic T cell response (= growth, proliferation and differentiation of effector T cells)

A

IL-2

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28
Q

the first and still by far most transplanted organ

A

kidney

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29
Q

organ in addition to liver for which sirolimus is contraindicated as anti-rejection therapy after transplantation

A

lung

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30
Q

accumulation of lymph in unusual space (e.g., retroperitoneal cavity after renal transplant), risk is increased by sirolimus

A

lymphocele

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31
Q

cell population unable to use guanine salvage pathways, therefore must synthesize new guanine during proliferation (= reason for cell-selectivity of mycophenolate)

A

lymphocytes

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32
Q

approved for use only when there is a glucocorticoid-resistant flare-up in the acute rejection of a transplanted organ

A

muromonab CD3

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33
Q

non-competitive reversible inhibitor of inosine monophosphate dehydrogenase used for its antiproliferative effects in lymphocytes (they need this enzyme to synthesize guanosine nucleotides)

A

mycophenolate

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34
Q

dose-limiting for both cyclosporine and tacrolimus, especially cyclosporine

A

nephrotoxicity

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35
Q

its migration into the lymphocyte nucleus after its dephosphorylation by calcineurin is crucial for the generation of gene products such as IL-2 that are characteristic of T cell activation

A

NFAT

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36
Q

among the cells that contributes to acute allograft rejection, for example, via antibody-dependent cell-mediated cytotoxicity

A

NK cells

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37
Q

widely known name for muromonab-CD3 (“nab” rather than “mab” is correct spelling), the original and still-used mouse monoclonal antibody against human CD3 (= T cell receptor) that causes its rapid internalization and thereby prevents T cell activation

A

OKT3

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38
Q

example of a drug that causes sequestration of circulating lymphocytes and also decreases their number via apoptosis

A

prednisone

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39
Q

wise to take extra measures to prevent this if taking anti-proliferative agents

A

pregnancy

40
Q

reason, for example, for administering basiliximab or rATG immediately before kidney transplantation and for a few days after, during what is referred to as “transplant induction therapy”

A

prophylaxis

41
Q

does not occur when nifedipine or hydralazine are administered to a heart transplant recipient

A

reflex tachycardia

42
Q

attempts to minimize this are the reason that sirolimus is added to lowered doses of cyclosporine or tacrolimus

A

renal damage

43
Q

binds to FKB12, but inhibits protein kinase mTOR, which in lymphocytes is an important downstream signaling component of IL-2 receptor-stimulated proliferation and differentiation

A

sirolimus

44
Q

aka FK-506, binds to the immunophilin FKB12 to inhibit calcineurin phosphatase activity; exerts beneficial effects in organ transplantation similar to those caused by cyclosporine

A

tacrolimus

45
Q

effect observed with sirolimus, means that foreign antigens present during its use are not rejected immediately when/if sirolimus is discontinued

A

tolerizing

46
Q

encompasses the dream of transplanting pig organs into humans

A

xenotransplantation

47
Q

the only NRTI that is a guanosine analog, relatively safe in most but can cause a unique and potentially fatal hypersensitivity syndrome in those with the HLA-B*5701 locus

A

abacavir

48
Q

symptoms of this appear when HIV RNA copy numbers are high in plasma and CD4+ lymphocyte numbers are low

A

AIDS

49
Q

government run website that provides latest consensus guidelines for treatment of HIV in the US

A

aidsinfo

50
Q

when boosted, a first-choice protease inhibitor for treatment-na‹ve HIV patients due to its long half-life and reduced side effects, but can cause unconjugated hyperbilirubinemia not associated with hepatitis

A

atazanavir

51
Q

carries by far the greatest risk of transmitting HIV, but now a negligible cause for HIV transmission in the US (risk ~ 1:1.4 million)

A

blood transfusion

52
Q

having this fall to <350 cells/mm3 currently has an AI level of support for initiation of antiretroviral therapy

A

CD4 count

53
Q

common side effect of efavirenz, but typically subsides and rarely leads to discontinuation of the drug

A

CNS toxicity

54
Q

emergence of this tropism in HIV renders it resistant to maraviroc

A

CXCR4

55
Q

cytochrome P450 isozyme that is inhibited, induced, etc., by a wide range of drugs including several antiretroviral drugs, which leads to potentially troublesome drug interactions

A

CYP3A4

56
Q

when boosted, a first-choice protease inhibitor for treatment-na‹ve HIV patients due to its long half-life and reduced side effects, but can cause sulfa drug hypersensitivity reactions

A

darunavir

57
Q

prodrug formulation of tenofovir, a phosphorylated adenosine analog, to overcome its otherwise poor bioavailability

A

disoproxil

58
Q

HIV integrase strand inhibitor with ~ 14 hr half-life (i.e., suitable for once per day dosing)

A

dolutegravir

59
Q

the current NNRTI of choice for treatment-na‹ve HIV patients, in part because it is co-formulated with tenofovir and emtricitabine for convenient once/day dosing; teratogen

A

efavirenz

60
Q

HIV integrase strand inhibitor with suitable for once per day dosing due to prolongation of half-life with cobicistat

A

elvitegravir

61
Q

cytidine analog, one of the least toxic anti-retroviral drugs and an NRTI of first choice for HIV treatment-na‹ve patients due to its long half-life and co-formulation with tenofovir +/- efavirenz

A

emtricitabine

62
Q

a 36 aa peptide that inhibits formation of a 6-helix bundle critical for HIV fusion with the host cell membrane, drug is a last resort since expensive and must be administered subQ 2X/day

A

enfuvirtide

63
Q

HIV gene that encodes for gp120 and gp41

A

env

64
Q

NNRTI approved for use in treatment-experienced people infected with HIV since it still works after HIV mutations that cause resistance to some other NNRTI

A

etravirine

65
Q

HIV gene that contains the nucleocapsid core and matrix proteins

A

gag

66
Q

also sensitive to some HIV drugs such as tenofovir disoproxil fumarate and emtricitabine; discontinuation of these drugs can cause a disease flare-up

A

HBV

67
Q

cells infected with HIV typically only have one copy of this, unlike the virion which characteristically possess two copies of its precursor

A

HIV DNA

68
Q

early protease inhibitor requiring 3X/day dosing, now perhaps more noteworthy for its ability to cause crystaluria

A

indinavir

69
Q

enzyme responsible for insertion of retroviral DNA into the human genome, and an excellent drug target since mammalian genomes lack enzymes with this capability

A

integrase

70
Q

risk of acquiring HIV infection during this is fortunately much lower than during childbirth or blood transfusion

A

intercourse

71
Q

earlier cytidine-like NRTI, interesting in that HIV can develop resistance to it relatively quickly but doing so increases reverse transcriptase fidelity, slows replication, and thereby helps to increase the long-term effectiveness of zidovudine

A

lamivudine

72
Q

~irreversible disfiguring re-distribution of body fat associated with HIV and its treatment

A

lipodystrophy

73
Q

HIV protease inhibitor only available as a boosted combination, inhibits both HIV-1 and HIV-2, and often works after failure of another PI-containing regimen

A

lopinavir

74
Q

will block HIV entry if an expensive test with a long turnaround time shows that the virion requires the CCR5 co-receptor

A

maraviroc

75
Q

blockade of DNA polymerase here is thought to be responsible for some of the adverse effects associated with some NRTI

A

mitochondria

76
Q

typically 4-5 are required for HIV to develop resistance to protease inhibitors, reason resistance is slow to develop and seldom a cause for treatment failure

A

mutations

77
Q

among the toxicities associated with some NRTI that is thought to be due to inhibition of DNA polymerase gamma

A

myopathy

78
Q

ending of generic drug name that identifies the drug as an HIV protease inhibitor

A

navir

79
Q

an NNRTI, early studies with it demonstrated the importance of combination therapy in treating HIV after the virusin ~1/3 of patients developed resistance to it after a single monotherapy exposure

A

nevirapine

80
Q

class of drugs that selectively inhibits only HIV-1 reverse transcriptase; binds to a distant hydrophobic pocket in a manner that causes a conformational change and noncompetitively inhibits enzymatic activity

A

NNRTI

81
Q

a two-drug combination from this antiretroviral drug therapy class with zidovudine as its prototype provides the backbone for current HIV treatment strategies

A

NRTI

82
Q

aka MDR1, a transporter that interacts with many drugs and site at which competition can influence the drug toxicities

A

p-glycoprotein

83
Q

required of NRTI for them to be active

A

phosphorylation

84
Q

HIV gene that contains reverse transcriptase, protease, integrase, etc.

A

pol

85
Q

the combination of tenofovir disoproxil fumarate and emtricitabine is this for treatment-naive HIV patients due to its safety and efficacy, and also due to the convenience of a once/day co-formulation +/- efavirenz

A

preferred NRTI backbone

86
Q

should be given anti-retroviral therapy as soon as possible, irrespective of viral load or CD4 count, but efavirenz should not be used during the first trimester

A

pregnant woman

87
Q

HIV enzyme that cleaves at the N-terminal side of Pro residues in the long polypeptides (e.g., gag, pol) packaged into newly budded virions to release the enzymes and cell components required for their metamorphosis into a mature virus capable of causing infection

A

protease

88
Q

first generation integrase inhibitor, seems likely to be displaced from preferred therapy list by new drugs elvitegravir and dolutegravir since their longer half-lives permit once daily dosing

A

raltegravir

89
Q

reason to avoid some antiretroviral drugs such as indinavir and enofovir and/or decrease the dosages/use with caution

A

renal insufficiency

90
Q

weaker HIV protease inhibitor discovered to be a potent inhibitor of CYP3A4, reason it is now routinely used to “boost” other protease inhibitors

A

ritonavir

91
Q

first HIV protease inhibitor, its short half-life caused a troublesome pill burden and it is among the agents well-known for promoting irreversible lipodystrophy with long-term use

A

saquinavir

92
Q

among early thymidine NRTI, notable for causing many of the toxicities associated with the drug class including CNS toxicity, fat wasting, and the ability to cause lactic acidosis and hepatic steatosis

A

stavudine

93
Q

portion of generic drug name indicating that the drug is an HIV integrase inhibitor

A

tegravir

94
Q

adenosine analog that is the only NRTI nucleotide (i.e., has a phosphate already attached, so only needs 2 more to be active), an NNRTI of choice due to its relative safety, long half-life and co-formulation in once/day pills

A

tenofovir

95
Q

NRTI do this during reverse transcriptase mediated synthesis of proviral DNA

A

terminate elongation

96
Q

reason for a thorough evaluation of patient history and contemplation of new strategy rather than adding a single new drug to an HIV treatment regimen or stopping treatment altogether

A

treatment failure

97
Q

thymidine analog and the first anti-retroviral drug discovered, this NRTI is still in widespread use in resource-poor settings due to its well-known tolerability, toxicity and efficacy profiles

A

zidovudine

Wolff Pharmacology Review (12 decks)

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