Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Immunology Drugs > HIV Drugs > Flashcards

HIV Drugs Flashcards

1
Q

What are the different types of HIV?

A

HIV 1 and HIV 2

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What is the difference of HIV 1 & HIV 2?

A

HIV 1 is world wide
HIV 2 is endemic in West Africa

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

HIV mutation?

A

HIV mutates rapidly

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What is the probability of HIV developing resistance dependent upon?

A

The probability of developing resistance is directly related to total viral load

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

What kind of responses does Anti-Retroviral Therapy cause?

A

Immunologic response
Virologic response

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

What does ART do to plasma levels of HIV?

A

Decreases HIV plasma levels to undetectable levels.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

What are the advantages of ART/HAART?

A

Delay or reverse loss of immune function,
Decrease certain complications,
Preserve health,
Prolong life,
Decrease transmission

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

What are the disadvantages of ART/HAART?

A

It is expensive
Risk of longterm side effects
Serious drug interactions
Life-long medication

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

What happens if there is discontinuation of the HIV medication?

A

Rebound in HIV replication

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

What are the goals of treatment?

A

Reduce HIV-associated morbidity
Prolong duration and quality of life
Preserve immunologic function
Suppress plasma HIV viral load
Prevent transmission

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What are the classifications of HIV drugs?

A

NRTIs
NNRTIs
PIs
INSTI
CCR5 antagonist
Fusion Inhibitors
Attachment Inhibitors
Post-attachment inhibitors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What is the first line of treatment for HIV?

A

NRTIs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

What are NRTIs?

A

Nucleoside reverse transcriptase inhibitors;
Chemical relatives of naturally occurring nucleosides or nucleotides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

What is the MOA of NRTIs?

A

Suppress RT-mediated viral DNA synthesis
Suppress mitochondrial DNA polymerization

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

What are the adverse effects of NRTIs?

A

Peripheral neuropathies
Pancreatitis
Lipoatrphy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

In order for NRTIs to be effective, what must happen to them first?

A

They must undergo intracellular conversion to their active forms

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

What are examples of NRTIs

A

Zidovudine
Abacavir
Lamivudine
Tenofovir

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

What is Zidovudine?

A

Analog of thymidine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

What is the function of Zidovudine when combined with other antiretroviral drugs?

A

Decrease viral load,
Increase CD4 T-cell count
Delay onset
Reduce symptom severity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

What is the MOA of Zidovudine?

A

Premature strand termination
Competes with natural nucleoside triphosphates for binding to the active site of reverse transcriptase
Competitive inhibition of enzyme

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

What are the therapeutic uses of Zidovudine?

A

HIV 1
Drug of choice for preventing mother to infant transmission during labor and delivery

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

What are the PK of Zidovudine?

A

Always combined with other antiretroviral drugs
Penetrates CNS better than most other antiretroviral drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

What are the adverse effects of Zidovudine?

A

Severe anemia
Neutropenia
Lactic acidosis with hepatic steatosis
GI disturbances
CNS reactions
Myopathy

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

What are the drug interactions of Zidovudine?

A

Drugs that are myelosuppressive, nephrotoxic or directly toxic increase the risk of hematologic toxicity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

What is the antiviral that should NOT be taken with Zidovudine?

A

Ganciclovir

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

What is Abacavir?

A

An analogue of guanosine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

What is the MOA of Abacavir?

A

Premature termination and direct inhibition of RT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

What are the therapeutic effects of Abacavir?

A

HIV 1 infections only

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

What are the adverse effects of Abacavir?

A

Hypersensitivity reactions in patients

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
30
Q

What kind of patients should not be given Abacavir?

A

Sensitized patients
Can check through the genetic test (HLA-B*5701)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
31
Q

What is Lamivudine?

A

Analogue of cytidine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
32
Q

What are the therapeutic uses of Lamivudine?

A

HIV 1
Hepatitis B virus

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
33
Q

What are the PK of Lamivudine?

A

Oral
High bioavailability
Food reduces rate of absorption
Eliminated in the urine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
34
Q

What are the adverse effects of Lamivudine?

A

Best tolerated
Minimal side effects
Insomnia
Headaches
Small risk of fatal lactic acidosis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
35
Q

What is Tenofovir?

A

Analogue of adenine
Nucleotide reverse transcriptase inhibitor

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
36
Q

What is the MOA of Tenofovir?

A

Inhibits viral DNA synthesis
Competes with natural substrate to reverse transcriptase
Causes premature termination

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
37
Q

What are the therapeutic uses of Tenofovir?

A

HIV 1
HBV infection

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
38
Q

What is the difference between NRTIs and NNRTIs?

A

NRTIs inhibit synthesis of HIV DNA
NNRTIs directly inhibit reverse transcriptase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
39
Q

Are NNRTIs in their active or inactive form?

A

Active form when administered

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
40
Q

What are the main examples of NNRTIs?

A

Efavirenz
Rilpivirine
Nevirapine
Delavirdine
Etravirine
Doravirine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
41
Q

Which is the preferred NNRTI for HIV treatment?

A

Efavirenz

42
Q

What is the MOA of Efavirenz?

A

Binds directly to the centre of reverse transcriptase (RT) and inhibits it

43
Q

What are the therapeutic uses of Efavirenz?

A

HIV 1 infection

44
Q

What other drugs is Efavrenz used in combination with?

A

Zidovudine & Lamivudine

45
Q

What are the PK of Efavirenz?

A

Orally taken on an empty stomach
Crosses BBB
Metabolised by CYP450
Excreted in urine and feaces
Long half-life (40 to 55 hours)

46
Q

What are the adverse effects of Efavirenz?

A

CNS symptoms
Rash
Teratogenicity
Liver damage

47
Q

What are the drug interactions of Efavirenz?

A

Ccompetes with other drugs for CYP450
Can accelerate its own metabolism and that of protease inhibitors
Decreases hormonal contraceptives
St. John worts can reduce levels of Efavirenz

48
Q

Which drug combination with Efavirenz can increase levels of both drugs and cause toxicity?

A

Ritonavir

49
Q

What are PIs given with to reduce viral load to undetectable levels?

A

NRTIs

50
Q

What are some general side effects of PIs?

A

Fat redistribution
Hyperglycemia/diabetes
Reduced bone mineral density
Bleeding in hemophiliacs
Elevation of triglycerides and transaminases

51
Q

The combination of which drugs can cause rhabdomyolysis?

A

PIs with simvastatin or lovastatin

52
Q

What are the general PK of PIs?

A

Metabolised by CYP450
Induce certain CYP450 isozymes and inhibit other
Resistance to one PI may mean resistance to others

53
Q

What pharmacokinetic boosters are PI administered with?

A

Ritonavir or Cobicistat

54
Q

What are the examples of PIs?

A

Lopinovar/Ritonavir
Indinavir
Atazanavir
Darunavir

55
Q

What name are Lopinovar and Ritonavir given under?

A

Kaletra

56
Q

What are the therapeutic uses of Kaletra?

A

HIV in adults & children older than 6 months old

57
Q

How is Lopinavir metabolised?

A

CYP450; CYP3A4

58
Q

What does Ritonavir inhibit?

A

CYP3A4

59
Q

Which levels does Kaletra increase?

A

Lopinovar

60
Q

What is the MOA of Kaletra?

A

Block protease
HIV remains immature and non-infectious

61
Q

What are the PK of Lopinavir/ Kaletra?

A

Orally taken
Absorption is higher with food
99% bound to blood plasma
Metabolised by CYP3A4
Excreted in urine & feces

62
Q

What are the adverse effects of Kaletra?

A

GI disturbances
Cardiac effects; QT & PR prolongation
Toxicity in newborns

63
Q

What are the drug interactions of Kaletra?

A

Inhibit and induce CYP450
Disulfiram or Meronidazole

64
Q

What is the therapeutic use of Indinavir?

A

HIV 1

65
Q

What is Indinavir usually combined with?

A

2 NRTIs

66
Q

What is the major adverse effect of Indinavir?

A

Nephrolithiasis

67
Q

What reduces the availability of Atazanavir?

A

Agents that reduce acidity

68
Q

Adverse effect of Atazanavir?

A

Nephrolithiasis

69
Q

What is Darunavir?

A

2nd generation PI

70
Q

What is the therapeutic use of Darunavir?

A

HIV strains that are resistant to other PIs

71
Q

What is Darunavir usually given with?

A

Ritonavir
Cobicistat

72
Q

What are the adverse effects of Darunavir?

A

It has a sulphonamide group; careful with patients with sulfonamide allergy

Signs of glucose dysregulation are NOT reported

73
Q

What are examples of integrase strand transfer inhibitors?

A

Raltegravir
Dolutegravir

74
Q

What is the MOA of Raltegravir?

A

Prevents insertion of HIV DNA –> stops HIV replication

75
Q

What is the therapeutic use of Raltegravir?

A

HIV 1

76
Q

What is Raltegravir given with?

A

Tenofovir + Emtricitabine OR Lamivudine

77
Q

What are the PK of Raltegravir?

A

Orally taken
Metabolised by UGT

78
Q

What are the adverse effects of Raltegravir?

A

Insomnia and headaches
Severe hypersensitivity (RARE)

79
Q

What are the drug interactions of Raltegravir?

A

Inhibitors of UGT can increase its levels
Inducers of UGT lower its levels
Antacids and polyvalent cations reduce bioavailability

80
Q

What is the first line integrase inhibitor

A

Dolutegarvir

81
Q

What are examples of HIV Fusion Inhibitors?

A

Enfuvirtide

82
Q

What is the MOA of Enfuvirtide?

A

Binds to GP41 and prevents fusion

83
Q

What is the PK of Enfuvirtide?

A

SQ

84
Q

What is the therapeutic use of Enfuvirtide?

A

HIV1 that is resistant to other ART agents

85
Q

What are the adverse effects of Enfuvirtide?

A

Injection site reactions
Pneumonia
Hypersensitivity reactions

86
Q

What is an example of CCR5 antagonist?

A

Maraviroc

87
Q

What are the uses of Maraviroc?

A

Indicated for combined use with other ART for patients > 16 years of age

88
Q

What are the PK of Maraviroc?

A

Half-life of 14 to 18 hours
Metabolised by CYP3A4

89
Q

What are the adverse effects of Maraviroc?

A

Cough
Dizziness
Rash
Fever
URTI
LIVER INJURY !!
Cardiovascular events (rare)

90
Q

What are the drug interactions of Maraviroc?

A

Increased by CYP3A4 inhibitors
Decreased by CYP3A4 inducers

91
Q

What is an example of Capsid Inhibitor?

A

Ienacapavir

92
Q

What is the MOA of Ienacapavir?

A

Prevents functional disassembly of the capsid in infected cells
Inhibits viral nuclear import
Inhibits assembly

93
Q

What are the PK of Ienacapavir?

A

SQ or tablet

94
Q

What are the therapeutic uses of Ieancapavir?

A

HIV 1 with multidrug resistance

95
Q

What are the side effects of Ienacapavir?

A

Nausea
Hyperglycemia

96
Q

What is an example of Attachment Inhibitors?

A

Fostemsavir

97
Q

What is the MOA of Fostemsavir?

A

Binds to GP120 protein on the outer surface of HIV
Prevents HIV from entering CD4 cells

98
Q

What is an example of POST-attachment inhibitors?

A

Ibalizumab

99
Q

What is Ibalizumab?

A

Monoclonal antibody that binds to domain 2 of CD4 immune cells

100
Q

What is the MOA of Ibalizumab?

A

Promotes steric hindrance and prevents conformational changes that allow for HIV 1 viral entry

101
Q

What are the approved regimens?

A

2 NRTIs + One protease inhibitor + Ritonavir/Cobicistat

2 NRTIs + NNRTI

2 NRTIs + Integrase inhibitor

Immunology Drugs (7 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions