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Immunosuppressant Pharmacology Flashcards

(75 cards)

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1
Q

Prednisone (glucocorticoids)

A

Synthetic glucocorticoid medication used to treat inflammatory diseases and to prevent organ transplant rejection.

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2
Q

Side effects prednisone (glucocorticoids)

A

Osteoporosis, immunosuppression, hyperglycemia

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3
Q

Long term side effects of prednisone

A

Ocular disorders, like cataracts and glaucoma, ulcers and cushing syndrome

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4
Q

Why should patients be tapered off prednisone

A

Adrenal insuffiency can develop

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5
Q

MOA prednisone

A

It is a glucocorticoid, so it upregulated anti inflammatory proteins, decreasing immune activity (inflammation) additionally they regulate the metabolism of glucose

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6
Q

Indications for prednisone

A 
Inflammatory conditions (asthma, COPD, Rheumatic disorder, hives, allergic reactions, IBD)
Organ transplant rejection
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7
Q

Side efffects prednisone

A

Cataracts and open angle glaucoma, Cushing , ostoporosis, immunosuppression , hyperglycemia, ulcers

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8
Q

Prednisone and cataracts and open angle glaucoma

A

Increased production of free radicals along with high osmotic movement of glucose in the lens of the eye. Get eye exams every 6mo

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9
Q

Cushing and prednisone

A

Excess glucocorticoid give rapid weight gain, central obesity, moon faces, buffalo hump and abdominal striae,

Excess mineralocorticois can also lead to hyperkalemia and fluid loss

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10
Q

Prednisone and osteoporosis

A

Steroid induced
Patients should take prophylactic vitamin D
K

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11
Q

Kids on prednisone

A

Growth retardation due to inhibition of osteoblasts function and decrease GI ca absorption

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12
Q

Prednisone and immunosuppression

A

All glucocorticoids lead to immunosuppression

Infections!

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13
Q

Why not give prednisone people live vaccines

A

Immunosuppression

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14
Q

Hyperglycemia prednisone

A

Alter glucose metabolism

Glycosuria

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15
Q

Ulcer prednisone

A

Peptic ulcers, impaired ulcer healing

Don’t take if have ulcers

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16
Q

Adrenal insuffiency prednisone

A

The body decreases adrenal output of steroid hormones . So don’t abruptly stop you should taper

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17
Q

Cyclosporine (sandimmune)

A

Immunosuppressant medication used to prevent organ rejection in transplant patients as is also indicated in the treatment of psoriasis and rheumatoid arthritis.

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18
Q

MOA ciclosporin

A

Inhibits an enzyme Called calcineurin that is responsible for production of cytokines, such as il2

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19
Q

IL2 suppression

A

Decrease B cell and cytotoxic T cell production effectively suppressing the patients immune system

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20
Q

What should patients taking cyclosporin not take

A

Grapefruit juice as it prevents the drug from being metabolized and can lead to toxicity

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21
Q

When combined with other immunosuppresssants, cyclosporin can increase a patients risk of developing ___

A

Lymphomas

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22
Q

MOA cyclosporin

A

Immunosuppressant by inhibiting an enzyme called calcineurin that is responsible for production of cytokines such as IL2

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23
Q

Inhibition of calcineurin by cyclosporin

A

Suppresses IL2 which are responsible for producing B cells and cytotoxic T cells. Suppress immune system

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24
Q

Indications for cyclosporin

A

Prevent transplant rejection
Psoriasis
RA

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25
Cyclosporin and transplant
Given with glucocorticoid, used to prevent organ rejection in transplant patients. Does not suppress the bone marrow
26
Psoriasis and cyclosporin
Psoriasis causes overproduction of keratinocytes or skin cells Inflammatory T cells play a key role int he development of this disorder and are likely responsible for secreting cytokines that lead to excessive proliferation of keratinocytes. It suppresses the production of cytokines
27
Cyclosporin and RA
Immune system produces cytokines that attack synovial tissue, producing inflammation and joint destruction . Cyclosporine is used to suppress the production of cytokines thus slowing the progression of the disease
28
Why monitor the plasma levels of cyclosporine
Must be maintained to protect against organ transplant rejection
29
Why avoid grapefruit juice on cyclosporin
Prevents drug from being metabolized
30
Risk of lymphoma with cyclosporin
When combined with other immunosuppressants
31
Cyclosporin (sandimmune) side effects
Nephrotoxicity, hepatotoxicity, infection, hypertension, tremor, hirsutism, gynecomastia, gingival hyperplasia, hyperkalemia
32
Nephrotoxicity with cyclosporin
Causes severe kidney damage characterized by decreased renal blood flow and decreased glomerular filtration
33
Hepatotoxicity cyclosporin
Liver damage | Monitor AST, ALT
34
Infections nd cyclosporin
From immune suppression
35
Does cyclosporin cause bone marrow suppression
No however leukopenia may occur
36
Cyclosporin and hyperkalemia
Cause retention of potassium
37
Hypomagnesia and cyclosporine
Can lead to nephrotoxicity, resulting in mg wasting and hypomagnesemia
38
Tacrolimus (prograf)
Immunosuppressant for organ rejection prevention and also used in atopic dermatitis
39
MOA tacrolimus
Works by inhibiting an enzyme called calcineurin that is responsible for production of cytokines such as IL2
40
Suppression of IL2
Decreases B cell and cytotoxic T cell production, effectively suppressing the patients immune system
41
Why should patients on tacrolimus not drink grapefruit juice
Prevents metabolism and lead to toxicity
42
Tacrolimus can increase a patients risk of developing ___ ___
Malignant lymphomas
43
MOA tacrolimus
Inhibit calcineurin reduce IL2 so B and Cytotoxic T cells not helped
44
Indications for tacrolimus
``` Transplant rejection Atopic dermatitis (eczema) ```
45
Atopic dermatitis and tacrolimus
Topical ointment for treating it Works locally to suppress the release of inflammatory mediators, effectively decreasing inflammation associated with atopic dermatitis
46
Tacrolimus side effects
``` Nephrotoxicity Neurotoxicity Infectiondiarrhea Nausea Vomiting Hypertension Hyperkalemia Hyperglycemia GI distress ```
47
Neurotoxicity seen with tacrolimus
Headache, tremor, insomnia
48
Why tacrolimus give hyperglycemia
Increasedglucose levels as can interfere with insulin secretion int he body
49
Methotrexate (MTX)
Antimetabolite and disease modifying antiheumatic drug (DMARD) that acts by inhibiting dihydrofolate reductase
50
how does methotrexate work
Inhibit dihydrofolate reductase Stops production of dTMP (thymidine) which is necessary for DNA , RNA and protein synthesis, thus resulting in cell death
51
Side effects methotrexate
Myelosuppression (which can be treated with leucovorin), microcytic anemia, hepatitis, teratogen is effects and oral mucositis
52
Indications for methotrexate
RA, cancer, medical abortion
53
RA and MTX
Decreases severity of arthritis, | Look at CBC, AST, ALT
54
Cancer MTX
Results incell death or rapidly dividing cancer cells. Use in leukemia’s, lymphomas, choriocarcinoma and sarcomas
55
Medical abortion and methotrexate
Followed by vaginal misoprostol | Up to 49 days gestation
56
Why is MTX+ misoprostol inferior to mifepristone+ misoprostol for medical abortion
The interval between treatment and complete abortion is longer MTX is used for treatment of small, unruptured ectopic pregnancies
57
MOA MTX
Folic acid analog-prevent folic acid metabolism and thus thymidine production because it has a much higher affinity for dihydrofolate reductase than folic acid Inhibits dihydrofolate reductase-without it MTX binds competitively inhibits the biologically active form of folic acid, THF cannot be reformed
58
Side effects MTX
Pulmonary fibrosis, myelosuppression , microcytic anemia, hepatitis, teratogenic, mucositis
59
How revers myelosuppression from MTX
Leucovorin which has vitamin activity equivalent to that of folic acid but does not require dihydrofolate reductase to be converted to its biologically active form. This quickly allows thymidine levels to be restored so that DNA RNA and protein synthesis can occur
60
Microcytic anemia and MTX
Results in functional defiency of folic acid,
61
What is microcytic anemia
Mean corpuscular volume being greater than 100
62
Azathioprine (imuran)
Immunosuppressant used in organ transplant and to treat autoimmune disorders
63
MOA azathioprine
Prodrug, or precursor, to 6-mercaptopurine, which interferes with nuclei acid and DNA synthesis
64
What cells are effected by azathioprine
proliferating cells like T and B cells leading to myelosuppression
65
What metabolizes azathioprine
Zanthine oxidasse
66
Patients taking allopurinol should reduce AZA dose. Why
Allopurinol inhibits xanthine oxidase
67
Patients with IBD taking azathioprine also runt he risk of developing acute __-
Pancreatitis
68
MOA azathioprine
Antimetabolite-competes with metabolites and interfere with cell function 9cancer treat bc cells are dividing!) -makes 6-mercaptopurine (AZA quickly converted to 6MP) Inhibits synthesis of nuclei acid (inhibiting purine synthesis, structure of RNA DNA is altered)
69
AZA->6MP
Via nonenzymatic nucleophilic attack by compounds found in rbc and other tissues
70
What does 6MP do
Active form of AZA which is a thiopurine that interferes with DNA synthesis
71
Indications for AZA
Autoimmune disorders | Kidney transplant
72
What autoimmune disorders can be treated with AZa
SLA, croons, RA
73
Side effects AZa
Myelosuppression Increased toxicity with allopurinol use Pancreatitis Malignancy
74
AZA myelosuppression
Severe bone marrow suppression Can get leukopenia, thrombocytopenia, anemia’s including microcytic anemia, and/or pancytopenia may be seen in patients taking AZa
75
Malignancy from AZA
Bc it immunosuppresses can get lymphoma, particularly skin. Post transplant lymphoma and hepatosplenic T cell lymphoma (HSTCL) Inform patients of risks before take it

Pharmacology (52 decks)

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