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PPP-3 > Other immunosuppressive drugs > Flashcards

Other immunosuppressive drugs Flashcards

1
Q

PK with cyclosporine

A
  • Variable F
  • CYP and PGP substrate
  • Eliminated via bile
  • Factors that affect PK: time-post transplant, high fat meals, bile production, liver disease, gastroparesis, diarrhea, age, other meds, SNPs
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2
Q

More specific side effects of cyclosporine

A

Neurologic (seizures, headache, tremor), GI, hyperglycemia, liver toxicity but rare, hypomagnesemia, hyperkalemia, HTN
–> most common AE is nephrotoxicity and depends on concentration of cyclosporine

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3
Q

T/F: Cyclosporine interacts w statins

A

True and is OATP mediated because cyclosporine is an OAT substrate (tacrolimus is not)

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4
Q

T/F: You should take sirolimus 2 hours after cyclosporine

A

False, it should be at least 4 hours after d/t CYPs

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5
Q

How to monitor cyclosporine

A

Target trough or peak and therapeutic range should be 100-350 ng/ml
Note: drug monitoring is important since it has a narrow therapeutic range and has multiple toxicities

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6
Q

T/F: Tacrolimus is the most widely used immunosuppressant

A

True

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7
Q

Tacrolimus PK

A
  • Even more variable F
  • CYP and PGP substrate
  • Same AEs and interactions seen with cyclosporine
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8
Q

CYP3A5 polymorphisms affecting tacrolimus concentrations and dosing

A
  1. Extensive metabolizer has 2 functional alleles & cause lower concentrations of drug (increase dose)
  2. Intermediate metabolizer has 1 functional allele & cause lower concentrations of drug (increase dose)
  3. Poor metabolizer has 3 non-functional alleles and does not need a dose change
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9
Q

How to monitor tacrolimus

A
  • Trough or peak concentrations and therapeutic levels are 5-20 ng/ml
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10
Q

Sirolimus & everolimus MOA

A

Inhibits mTOR1 which is responsible in regulating cell growth and proliferation

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11
Q

Sirolimus PK

A
  • CYP3A4 and PGP substrate
  • Highly variable
  • Really long t 1/2
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12
Q

What are side effects of sirolimus?

A
  1. Delayed wound healing, mouth ulcers, thrombocytopenia, leukopenia, dyslipidemia, proteinuria
  2. Dose adjustments- within 5-7 days of last dose
  3. Drug interactions- cyclosporine
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13
Q

Everolimus PK

A
  1. CYP3A4 and PGP substrate
  2. Shorter half life
    Note- cyclosporine inhibits everolimus metabolism
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14
Q

What are side effects of everolimus?

A

Delayed wound healing, leukopenia, hyperlipidemia, proteinuria (no ulcers or thrombocytopenia)

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15
Q

Azathioprine MOA

A

Inhibits de novo purine synthesis and incorporates into DNA –> inhibits T and B cell proliferation

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16
Q

How does TPMT effect azathioprine dosing?

A
  1. Low or deficient= consider alt dosing or extreme dose reduction
  2. Intermediate TPMT= start at 30-70% target dose
17
Q

What are side effects of azathioprine?

A

Bone marrow suppression, myopathy, alopecia, pancreatitis, hepatitis
Note: monitor WBC, Hgb, Hct, Plt

18
Q

Mycophenolate MOA

A

Inhibits de novo guanosine synthesis by inhibiting inosine monophosphate dehydrogenase (IMPDH)
Note: specific to lymphocytes

19
Q

Mycophenolate indication

A

Maintenance therapy only after organ transplant

20
Q

Mycophenolate adverse effects + interactions

A

AE: GI (dose limiting), neutropenia, anemia
Drug interactions are antacids and cholestyramine
Note- enteric coated has decreased GI side effects

21
Q

Corticosteroids indication

A

Maintenance or treatment of rejection and are considered broad spectrum

22
Q

What two drugs block IL-2

A

Daclizumab and basiliximab

23
Q

What are specific indications for belatacept (inhibits T cell activation)?

A

Approved for prevention of acute kidney transplant rejection and used in EBV+ patients but has increased risk of PTLD

24
Q

Antithymocyte globulin (polyclonal antibody)

A

MOA: depletes circulating T cells within 24 hours
Indication: induction or treatment of rejection
AEs: cytokine release syndrome, bone marrow suppression, increased risk of CMV and cancers

25
Q

Bortezomib

A

MOA: proteasome inhibitor that targets plasma cells and decreases production of donor specific antibodies
Indication: treats antibody-mediated rejection post organ transplant

26
Q

Eculizumab

A

MOA: anti-C5 mAB and inhibits complement activation
Indication: treats antibody-mediated rejection post organ transplant

27
Q

T/F: antibody mediated rejection is easy to treat

A

False, it is hard to treat because no definitive tx and we need better drugs

PPP-3 (21 decks)

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