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Derm Pharm 2020 > 3 - Mycophenolate Mofetil > Flashcards

3 - Mycophenolate Mofetil Flashcards

1
Q

MMF is a prodrug

A

True

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2
Q

The active antimetabolite of MMF is mycophenolic acid

A

True

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3
Q

Mycophenolic acid has antibacterial properties

A

True

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4
Q

Mycophenolic acid has antiviral properties

A

True

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5
Q

Mycophenolic acid has antifungal properties

A

True

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6
Q

Mycophenolic acid has antitumour properties

A

True

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7
Q

Mycophenolic acid has immunosuppressive properties

A

True

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8
Q

MMF has greater bioavailability and tolerability than Mycophenolic acid

A

True

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9
Q

MMF is an ester of mycophenolic acid

A

True

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10
Q

MMF is converted to mycophenolic acid by esterases in the plasma, liver and kidney

A

True

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11
Q

Mycophenolic acid is inactivated in the liver via glucuronidation

A

True

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12
Q

Mycophenolic acid is inactivated in the liver

A

True

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13
Q

Glucuronidation of mycophenolic acid in the liver yields the inactive compound mycophenolic acid glucuronide

A

True

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14
Q

Mycophenolic acid glucuronide (inactive metabolite of mycophenolic acid) is secreted into bile and recycled to the liver via enterohepatic recirculation

A

True

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15
Q

The enterohepatic recirculation of mycophenolic acid glucuronide is vital for maintaining mycophenolic acid serum levels

A

True

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16
Q

Mycophenolic acid glucuronide (inactive metabolite) is converted back to mycophenolic acid by beta-glucuronidase

A

True

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17
Q

The high levels of beta-glucuronidase (to convert mycophenolic acid glucuronide to mycophenolic acid) found in the epidermis accounts for the efficacy of MMF

A

True

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18
Q

The high levels of beta-glucuronidase (to convert mycophenolic acid glucuronide to mycophenolic acid) found in the GI tract accounts for the most common adverse effects of MMF

A

True

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19
Q

The first peak of MMF plasma levels occurs in the first hour

A

True

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20
Q

A second MMF plasma level peak occurs after 6-12 hours due to enterohepatic recirculation of mycophenolic acid glucuronide

A

True

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21
Q

Over 90% of the administered MMF dosage is excreted in urine as mycophenolic acid glucuronide (inactive metabolite)

A

True

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22
Q

Dose reduction of MMF is not necessary in renal impairment

A

True (renal impairment does not have a significant impact on mycophenolic acid)

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23
Q

MMF and mycophenolic acid is bound to serum albumin

A

True

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24
Q

A decrease in MMF dosing may be necessary in situations which alter albumin levels

A

True (altered albumin levels may occur in liver or renal disease or concomitant use of medications that compete for albumin binding sites)

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25
Q

Exposure to increased amounts of unbound mycophenolic acid (active metabolite/drug) may be a predictor of infections

A

True

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26
Q

Exposure to increased amounts of unbound mycophenolic acid (active metabolite/drug) may be a predictor of haematologic toxicity

A

True

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27
Q

Mycophenolic acid inhibits inosine monophosphate dehydrogenase in the de novo purine synthesis pathway

A

True (just like MTX - an antimetabolite)

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28
Q

By inhibiting inosine monophosphate dehydrogenase in the purine synthesis pathway, mycophenolic acid deprives T and B lymphocytes of purine metabolites necessary for growth and replication (hence causes selective immunosuppression)

A

True

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29
Q

The immunosuppressive effects of MMF are related to the effects of purine biosynthesis affecting lymphocytes

A

True

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30
Q

By selectively inhibiting the de novo purine synthesis pathway within activated lymphocytes, MMF targets the lymphocytes most responsible for disease whilst having a minimal effect on other organs and cell types

31
Q

MMF also reduces the recruitment of inflammatory cells

32
Q

MMF is used off label for dermatologic diseases

A

True (as a steroid-sparing agent and for severe refractory disease that has failed other treatment regimens)

33
Q

MMF is comparable to other immunosuppressants as a corticosteroid-sparing agent in treatment of Pemphigus

34
Q

MMF is not first line treatment in psoriasis

35
Q

Azathioprine is associated with a significantly higher rate of elevated LFTs as compared to MMF in the treatment of bullous pemphigoid

36
Q

MMF shows promise in the treatment of the associated interstitial lung disease in dermatomyositis

37
Q

MMF is efficacious in the treatment of interstitial lung disease associated with diffuse systemic sclerosis, although efficacy is less convincing for cutaneous disease

38
Q

Peptic ulcer disease is a relative contraindication of MMF

39
Q

Cholestyramine (interferes with enterohepatic recirculation) is relatively contraindicated with MMF

40
Q

Concomitant administration of Azathioprine with MMF increases risk of bone marrow suppression

41
Q

The risk of MMF in causing lymphoproliferative disorders and NMSCs is unclear

42
Q

The risk of malignancy associated with MMF (lymphoproliferative disorders and NMSCs) likely relates to the effects of cumulative immunosuppression from multiple drugs rather than an MMF specific effect

43
Q

GI symptoms are most common with MMF

44
Q

GI symptoms associated with MMF are dose related

45
Q

Adverse GI effects associated with MMF improve over time

46
Q

Administration of MMF with food and BD or TDS dosing improves GI tolerability

47
Q

MMF is not hepatotoxic although elevated transaminases have been reported

A

True (the significance of the elevated transaminases is unclear)

48
Q

MMF can cause elevated transaminases

A

True (though significance is unclear)

49
Q

MMF is less hepatotoxic than Azathioprine

50
Q

MMF does not cause nephrotoxicity

51
Q

Haematologic toxicity associated with MMF is dose-dependant

52
Q

The haematologic toxicity associated with MMF is rapidly reversible with cessation of therapy

53
Q

Risk of Infections with MMF are more common in transplant patients used as anti-rejection treatment

54
Q

Progressive multifocal leukoencephalopathy was associated in patients on MMF with transplanted organs and long-standing SLE on concomitant immunosuppression

55
Q

The role of MMF to the development of progressive multifocal leukoencephalopathy is unclear

A

True (occurred in transplant patients and SLE patients already at increased risk for this condition)

56
Q

Fetal malformations are associated with MMF (teratogenic)

57
Q

Antacids and PPIs reduce serum levels of mycophenolic acid

A

True (MMF requires gastric acidity for conversion to the active metabolite mycophenolic acid)

58
Q

Oral iron supplementation does not affect serum MMF levels

A

True (although it is advisable to give MMF 1 hour before iron containing products)

59
Q

Salicylic acid competes with mycophenolic acid for albumin binding sites and can increase the free active fraction of mycophenolic acid

60
Q

Phenytoin competes with mycophenolic acid for albumin binding sites and can increase the free active fraction of mycophenolic acid and vice versa increase free phenytoin levels

61
Q

Xanthine bronchodilators (theophylline) compete with mycophenolic acid for albumin binding sites and can increase the free active fraction of mycophenolic acid and vice versa increase free levels of theophylline

62
Q

Antivirals (acyclovir, ganciclovir, valganciclovir) inhibit renal tubular secretion of mycophenolic acid and thus increase the serum levels of mycophenolic acid

A

True (caution with co-administration especially in renal impairment)

63
Q

There is a potential risk of neutropenia with both valacyclovir and MMF

64
Q

There is a risk of decreased serum levels of levonorgestrel (progestin component of OCP) with Co-administration with MMF

65
Q

Co-administration of MMF does not affect the serum levels of desogestrel, gestodene and ethinyl oestradiol

A

True (in contrast to levonorgestrel, levels of these do not appear to be affected by MMF although caution is still advised)

66
Q

Live vaccines are contraindicated in patients on MMF

A

True (risk of reduced immunologic response or increased risk of disseminated viral infection)

67
Q

MMF may increase levels of Cyclosporine

68
Q

Antibacterials may reduce serum levels of mycophenolic acid because of reduced enterohepatic recirculation

A

True (multiple classes including metronidazole, cephalosporins, aminoglycosides, macrolides, etc)

69
Q

Bile acid sequestrants I.e. Cholestyramine reduces the enterohepatic recirculation of mycophenolic acid glucuronide (hence reduce serum levels of mycophenolic acid)

70
Q

Probenecid competes with mycophenolic acid for renal tubular secretion and thus increase the serum levels of mycophenolic acid

71
Q

Concomitant use of MMF and narcotics may increase risk of seizures

72
Q

MMF has been linked to rising Hep C viral titres and Hep C induced acute hepatitis

A

True (although MMF is safe to use in patients infected with Hep B and C)

73
Q

MMF has been associated with reactivation of latent TB

74
Q

MMF may cause genitourinary symptoms I.e. Urgency, frequency, dysuria

Derm Pharm 2020 (47 decks)

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