Brainscape's Knowledge GenomeTM

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


See full index

Clinical PK > Immunosuppresants > Flashcards

Immunosuppresants Flashcards

1
Q

What are the 4 immunosuppressant drugs?

A

Cyclosporine microemulsion (CSA)
Tacrolimus (TAC)
Sirolimus (SRL)
Everolimus (EVR)

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

What is the brand name of CSA?

A

Neoral

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

What is the brand name of TAC?

A

Prograf, Envarsus XR, Astagraf XL

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

What is the brand name of SRL?

A

Rapamune

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

What is the brand name of EVR?

A

Zostress

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

What is the indication for the immunosuppressant drugs?

A

Prevention of allograft rejection

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

What is the conversion ratio from PO to IV for CSA?

A

3:1 conversion ratio PO:IV

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

What CSA medication is the original formulation, has poor absorption and has a variable PK in patients?

A

Oral Sandimmune

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

What CSA medication is a microemulsion, has improved absorption and less variability in PK for patients

A

Oral Neoral

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

What CSA medication is considered therapeutically interchangeable with Oral Neoral?

A

Gengraf (generic CSA formulation)

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

What is the bioavailability (F) in Neoral?

A

F = 5 to 70%

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

What is the volume of distribution (Vd) in Neoral?

A

Vd = 3 to 7 L/kg

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

What does Neoral bind to in the blood affecting Vd? By how much percent?

A

Erythrocytes; 70%

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

What does Neoral bind to in plasma affecting Vd?

A

Lipoproteins

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

What is Neoral metabolized by?

A

Hepatic and intestinal CYP3A4

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

What is Neoral transported by after being metabolized?

A

P-gp

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

Can variations of intestinal P-gp and CYP3A4 affect F for CSA?

A

YES

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

How is Neoral eliminated?

A

Eliminated by kidneys

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

What is the t 1/2 of Neoral?

A

12 to 16 hours

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

What are two strategies to monitor CSA?

A
  1. Pre-dose trough whole blood concentration (C0)

2. Single point sampling 2 hours after drug administration (C2)

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

Which strategy to monitor CSA is thought to be a bit less inaccurate?

A

C2

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

Roughly what is the initial dose of CSA?

A

4 mg/kg PO q12h

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

CSA should be titrated based off what?

A

Steady-state trough (C0) blood levels

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

For the first 6 months of post-transplant of a liver or kidney organ, what should the therapeutic C0 level be for CSA?

A

200-250 ng/mL

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

For the first 6 months of post-transplant of a heart or lung organ, what should the therapeutic C0 level be for CSA?

A

250-300 ng/mL

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

In the first month of post-transplant, how many times a week should the trough (C0) levels be monitored for CSA?

A

3 times a week

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

In the next two months from the first month of post-transplant, how many times a week should the C0 levels be monitored for CSA?

A

2 times a week

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

In the next 3 months from the three months of post-transplant, how many times a week should the C0 levels be monitored for CSA?

A

once a week

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

How many times should the C0 levels be monitored when a patient has passed 6 months from their post-transplant or had any dose changes to CSA?

A

Once a month

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

To achieve therapeutic C0 levels in CSA, how should doses be adjusted?

A

25 to 50 mg PO q12h

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

What is the conversion ratio from PO to IV for TAC?

A

5:1 conversion ratio from PO:IV

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

What is the name of the TAC medication that has poor absorption and highly variable PK?

A

Prograf

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

What is the name of the TAC medication that is an extended release tablet?

A

Envarsus XR

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

What is the name of the TAC medication that is an extended release capsule?

A

Astagraf XL

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

What is the F for Prograf?

A

F = 5 to 67%; mean 27%

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

What is the F for Envarsus XR?

A

F = about 50% higher than Prograf

37
Q

(T/F) - Astagraf is better taken with food and in the morning hours for better bioavailability

A

FALSE - it’s better taken in the morning hours and with an EMPTY stomach

38
Q

What is the Vd of Prograf, Envarsus XR, and Astagraf XL?

A

Vd = 5 to 6 L/kg

39
Q

What do the 3 TAC drugs bind to in blood? What’s the percentage?

A

Erythrocytes by 70 to 80%

40
Q

What do the 3 TAC drugs bind to in plasma? What’s the percentage?

A

Albumin and alpha-1 acid glycoprotein by 88%

41
Q

How are the 3 TAC drugs metabolized?

A

Hepatic and intestinal CYP3A4

42
Q

How are the 3 TAC drugs transported after being metabolized?

A

By the P-gp

43
Q

(T/F) - Variations in the P-gp and CYP3A4 can affect the bioavailability in the 3 TAC drugs

A

TRUE

44
Q

How is Prograf eliminated and what is the half life mean?

A

Minimal renal elimination; t 1/2 = 12 hours

45
Q

How is Envarsus XR eliminated and what is the half life?

A

Minimal renal elimination; t 1/2 = 31 +/- 8 hours

46
Q

How is the Astagraf XL eliminated and what is the half life?

A

Minimal renal elimination; t 1/2 = 38 +/- 3 hours

47
Q

What are two strategies for TAC monitoring?

A
  1. High correlation between trough (C0), Cmax, and AUC 0-4

2. Pre-dose trough whole blood concentration (C0) is the standard care

48
Q

What is the initial dosing for Prograf?

A

0.05 mg/kg PO q12h

49
Q

What is the conversion dose of Prograf to Envarsus XR?

A

80% of Prograf taken QD

50
Q

What is the conversion dose of Prograf to Astagraf XL?

A

Same as Prograf taken QD

51
Q

What is the target therapeutic C0 level of TAC?

A

5 to 15 ng/mL

52
Q

The target therapeutic C0 level of TAC in a liver or kidney transplant is what? For how long should it be that range?

A

8 to 10 ng/mL for 6 months

53
Q

The target therapeutic C0 level of TAC in a heart or lung transplant is what? For how long should it be that range?

A

10 to 15 ng/mL for 6 months

54
Q

How should C0 levels be monitored for Prograf during the 6 months?

A

First month: 2/3 x weekly
Second and third month: 2 x weekly
Fourth, fifth, and sixth month: once a week

55
Q

(T/F) - After the 6 months from post-transplant or any dose adjustments to Prograf, C0 levels should be monitored once every two weeks

A

FALSE - once a month

56
Q

How should C0 levels be monitored for Envarsus XR and Astagraf XL after post-transplant?

A

Three months: once a week

Monthly after first three months

57
Q

How is the dose of Prograf adjusted to reach therapeutic levels?

A

0.5 to 2 mg PO q12h

58
Q

Is SRL available intravenously?

A

NO

59
Q

What is the SRL brand name that has poor absorption, highly variable PK, and also known as rapamycin?

A

Rapamune

60
Q

CSA has been administered in a patient and Rapamune has been assigned to that patient. When do you administer Rapamune? Why?

A

4 hours after CSA due to an interaction

61
Q

What is the F of Rapamune?

A

F = 15% (poorly absorbed)

62
Q

What is the Vd of Rapamune?

A

Vd = 4 to 20 L/kg ( ~12 L/kg)

63
Q

What is Rapamune highly bound to in the blood? By how much percent?

A

Erythrocytes; 95%

64
Q

What is Rapamune highly bound to in the plasma? By how much percent?

A

Lipoproteins; 40%

65
Q

What is Rapamune metabolized by and how is it transported?

A

CYP3A4 and transported by P-gp

66
Q

How is Rapamune eliminated? & what is the half-life?

A

Minimal renal elimination; t 1/2 = 57 to 63 hours

67
Q

Can Rapamune be given as a LD, MD or both?

A

BOTH

68
Q

What are two strategies for SRL monitoring?

A
  1. High correlation between C0 and AUC

2. Whole blood trough C0 monitoring is standard of care

69
Q

What is the dose for SRL in a low-moderate immunological risk (kidney or liver transplant)?

A

2 mg QD

70
Q

What is the dose for SRL in a high immunological risk (heart or lung transplant)?

A

5 mg QD

71
Q

What is the therapeutic C0 levels for SRL?

A

5 to 15 ng/mL

72
Q

How would you monitor the C0 levels for SRL?

A

First month: once a week

Next 3 months or any dose adjustments: monthly

73
Q

How is the SRL dose adjusted?

A

0.5 to 1 mg/day

74
Q

What EVR brand drug has variable oral bioavailability and interindividual PK variability?

A

Zostress

75
Q

(T/F) - EVR tablets and dispersible tablets are interchangeable

A

TRUE

76
Q

What is the EVR brand name that is ONLY indicated for subependymal giant cell astrocytoma (SGCA)

A

Afinitor Disperz

77
Q

What is the F of EVR?

A

F = 30% (reduces w/ meals)

78
Q

What is the Vd of EVR?

A

Vd = 2 to 5 L/kg

79
Q

What is EVR bounded to in plasma? What is the percentage?

A

Protein - 70%

80
Q

How is EVR metabolized?

A

CYP3A4 and P-gp

81
Q

How is EVR eliminated?

A

Feces (80%) and minimal renal excretion (5%)

82
Q

What is the half-life of EVR?

A

T 1/2 = 30 hours

83
Q

What are 2 strategies for EVR monitoring?

A
  1. High correlation between trough (C0), Cmax, and AUC 0-4

2. Predose trough whole blood concentration (C0) is the standard care

84
Q

What is the dose of EVR for liver transplant?

A

1 mg BID

85
Q

What is the dose of EVR for renal transplant?

A

0.7 mg BID

86
Q

What is the therapeutic trough level range for EVR?

A

3 to 8 ng/mL

87
Q

How are trough levels monitored for EVR?

A

One month: 1-2 x week

After one month: clinically as indicated

88
Q

How are EVR doses adjusted to reach therapeutic trough levels?

A

0.25 to 0.5 mg PO q12h

Clinical PK (11 decks)

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