``` N/V Hepatotoxic Pancreatitis Myelosupression (bac & viral) Malignancy ```

Transplant Drugs Flashcards by Kaylyn Freeman

What are the 3 drugs of triple maintenance therapy? (name drug type not specifics)

Anti-metabolite.
Calcineurin Inhibitor
Prednisone

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what is the main anti-metabolite drug used w/ triple therapy?

mycophenolate

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what is the main calcineurin Inhibitor drug used w/ triple therapy?

tacrolimus

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Is Azathioprine a prodrug?

yes

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what does azathioprine get converted into?

6 MP

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MOA of azathioprine

decrease B and T lymphocytes, decrease IG synthesis, decrease IL-2 secretion

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what happens if you have a generic alteration of TPMT?

you can’t degrade 6MP causing increased immunosuppression (pt would need lower aza dose)

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what often blocks XO in the azathioprine/6MP pathway?

gout medications, causing increased concentration of 6MP and increased immunosupression

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what allele for azathioprine requires dose reduction?

heterozygous for non-functional allele

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what allele type can you not give azathioprine?

homozygous for non-functional allele

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what drugs should be avoided w/ azathioprine use?

ACEI
allopurinol/febuxostat
Aminosalicylates

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what happens if you give ACEI + Azathioprine?

anemia

severe leukopenia

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what happens if you give Allopurional/febuxo + azathiroprine?

inhibition of XO leads to increase myelosuppression risk

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what happens if you give aminosalicylates + azathioprine?

inhibition of TPMT leads to increase myelosuppression risk

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ADR of azathioprine?

N/V
Hepatotoxic
Pancreatitis
Myelosupression (bac &amp; viral)
Malignancy

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what cancer are azathioprine pts @ risk for?

Skin SCC

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what pts have increase risk of malignant dz?

renal transplant pts

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Mechanism of Mycophenolate

decrease B & T cell proliferation

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indications of Mycophenolate use

transplants
auto-immune dz pts
GVHD

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what can decrease absorption of mycophenolate?

Fe
antacids
cholestyramine

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if you decrease the absorption of mycophenolate what happens?

increased risk of REJECTION

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ADR of mycophenolate

N/V/D/abd cramp
myelosuppression
miscarriage & birth defects

Cyclosporine MOA

decrease production/release of IL-1 and inhibits IL-2 induced activation of resting T lymphocytes

indications for cyclosporine

transplant
auto-immune dz: RA, psoriasis, IBD
ophthalmic emulsion

what ophthalmic condition does cyclosporine tx?

keratoconjunctivitis sicca-associated ocular inflammation (aka helps increase tear production)

drug interactions of cyclosporine?

*nephrotox with other nephrotoxic drugs (gentamicin) | pGp & 3A4 substrate (also inhibits 3A4)

ADR of cyclosporine?

``` nephrotoxic--AKI (most significant ADR) HTN neurotoxic PTDM Increase lipids & uric acid myelosuppression gingival` hyperplasia hirsutism N/V/D ```

Tacrolimus stands for what?

tsukuba macrolide immunosupressant

MOA of tacrolimus

binds to immunophillin to modulate T cells

indications of tacrolimus PO

transplant | ulcerative colitis

indications of tacrolimus topical

mod/severe atopic dermatitis

drugs interactions of tacrolimus?

*nephrotox with other nephrotoxic drugs (gentamicin) | pGp & 3A4 substrate (also inhibits 3A4)

ADR of tacrolimus

similar to cyclosporine

what ADR occurs more with tacrolimus vs cyclosporine?

PTDM

what ADR occurs less with tacrolimus vs cyclosprine?

every other ADR is less w/ tacrolimus

what is prednisone converted to?

predisolone

drug interactions of prednisone?

antagonistes anti DM meds

ADRS of acute use of prednisone

insomnia nervousness increase appetite hyperglycemia

ADRs of chronic use of prednisone

``` hirsutism cataract fat redistribution* fluid retention osteoporosis/AVN* poor would healing HPA-axis suppression/growth impression* myopathy *= M/C ADR ```

what type of myopathy do pts taking prednisone get?

proxmial muscle weakness w/o myalgis or tenderness

what part of the body gets weakness 1st?

how severe is the muscle weakness associated with prednisone?

affects ADLs

what dose makes the myopathy of prednisone uncommon?

<10mg/d

what dose makes myopathies of prednisone v' common?

>40mg-60mg/d for more than 1 month

what kind of a drug is sirolimus/rapamycin?

MTOR inhibitor

MOA of sirolimus/rapamycin

inhibit MTOR to then suppress cytokine driven T cell proliferation

what can siroliumus replace in triple therapy?

anti-metabolite or calcineurin inhibitor

main thing to monitor w/ sirolimus/rapamycin

drug interactions of sirolimus/rapamycin

Cyp3A4 substrate and pgp

ADR of sirolimus/rapamycin

``` HA tremor HTN edema PTDM renal dysfunction ```

MOA of belatacept

T cell costimulation blocker | inhibits production of cytokines

use of belatacept

renal transplant in pts who are EBV serotype +

ADR of belatacept

``` leukopenia anemia N/V/D increase malignancy risk PT lymphoproliferative disorder (PTLD) ```