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Pharmacology > Immunosuppressant Pharmacology > Flashcards

Immunosuppressant Pharmacology Flashcards

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
Q

Cyclosporin and transplant

A

Given with glucocorticoid, used to prevent organ rejection in transplant patients. Does not suppress the bone marrow

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26
Q

Psoriasis and cyclosporin

A

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

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27
Q

Cyclosporin and RA

A

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

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28
Q

Why monitor the plasma levels of cyclosporine

A

Must be maintained to protect against organ transplant rejection

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29
Q

Why avoid grapefruit juice on cyclosporin

A

Prevents drug from being metabolized

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30
Q

Risk of lymphoma with cyclosporin

A

When combined with other immunosuppressants

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31
Q

Cyclosporin (sandimmune) side effects

A

Nephrotoxicity, hepatotoxicity, infection, hypertension, tremor, hirsutism, gynecomastia, gingival hyperplasia, hyperkalemia

32
Q

Nephrotoxicity with cyclosporin

A

Causes severe kidney damage characterized by decreased renal blood flow and decreased glomerular filtration

33
Q

Hepatotoxicity cyclosporin

A

Liver damage

Monitor AST, ALT

34
Q

Infections nd cyclosporin

A

From immune suppression

35
Q

Does cyclosporin cause bone marrow suppression

A

No however leukopenia may occur

36
Q

Cyclosporin and hyperkalemia

A

Cause retention of potassium

37
Q

Hypomagnesia and cyclosporine

A

Can lead to nephrotoxicity, resulting in mg wasting and hypomagnesemia

38
Q

Tacrolimus (prograf)

A

Immunosuppressant for organ rejection prevention and also used in atopic dermatitis

39
Q

MOA tacrolimus

A

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

40
Q

Suppression of IL2

A

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

41
Q

Why should patients on tacrolimus not drink grapefruit juice

A

Prevents metabolism and lead to toxicity

42
Q

Tacrolimus can increase a patients risk of developing ___ ___

A

Malignant lymphomas

43
Q

MOA tacrolimus

A

Inhibit calcineurin reduce IL2 so B and Cytotoxic T cells not helped

44
Q

Indications for tacrolimus

A 
Transplant rejection 
Atopic dermatitis (eczema)
45
Q

Atopic dermatitis and tacrolimus

A

Topical ointment for treating it
Works locally to suppress the release of inflammatory mediators, effectively decreasing inflammation associated with atopic dermatitis

46
Q

Tacrolimus side effects

A 
Nephrotoxicity
Neurotoxicity
Infectiondiarrhea
Nausea
Vomiting
Hypertension
Hyperkalemia
Hyperglycemia
GI distress
47
Q

Neurotoxicity seen with tacrolimus

A

Headache, tremor, insomnia

48
Q

Why tacrolimus give hyperglycemia

A

Increasedglucose levels as can interfere with insulin secretion int he body

49
Q

Methotrexate (MTX)

A

Antimetabolite and disease modifying antiheumatic drug (DMARD) that acts by inhibiting dihydrofolate reductase

50
Q

how does methotrexate work

A

Inhibit dihydrofolate reductase
Stops production of dTMP (thymidine) which is necessary for DNA , RNA and protein synthesis, thus resulting in cell death

51
Q

Side effects methotrexate

A

Myelosuppression (which can be treated with leucovorin), microcytic anemia, hepatitis, teratogen is effects and oral mucositis

52
Q

Indications for methotrexate

A

RA, cancer, medical abortion

53
Q

RA and MTX

A

Decreases severity of arthritis,

Look at CBC, AST, ALT

54
Q

Cancer MTX

A

Results incell death or rapidly dividing cancer cells. Use in leukemia’s, lymphomas, choriocarcinoma and sarcomas

55
Q

Medical abortion and methotrexate

A

Followed by vaginal misoprostol

Up to 49 days gestation

56
Q

Why is MTX+ misoprostol inferior to mifepristone+ misoprostol for medical abortion

A

The interval between treatment and complete abortion is longer
MTX is used for treatment of small, unruptured ectopic pregnancies

57
Q

MOA MTX

A

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
Q

Side effects MTX

A

Pulmonary fibrosis, myelosuppression , microcytic anemia, hepatitis, teratogenic, mucositis

59
Q

How revers myelosuppression from MTX

A

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
Q

Microcytic anemia and MTX

A

Results in functional defiency of folic acid,

61
Q

What is microcytic anemia

A

Mean corpuscular volume being greater than 100

62
Q

Azathioprine (imuran)

A

Immunosuppressant used in organ transplant and to treat autoimmune disorders

63
Q

MOA azathioprine

A

Prodrug, or precursor, to 6-mercaptopurine, which interferes with nuclei acid and DNA synthesis

64
Q

What cells are effected by azathioprine

A

proliferating cells like T and B cells leading to myelosuppression

65
Q

What metabolizes azathioprine

A

Zanthine oxidasse

66
Q

Patients taking allopurinol should reduce AZA dose. Why

A

Allopurinol inhibits xanthine oxidase

67
Q

Patients with IBD taking azathioprine also runt he risk of developing acute __-

A

Pancreatitis

68
Q

MOA azathioprine

A

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
Q

AZA->6MP

A

Via nonenzymatic nucleophilic attack by compounds found in rbc and other tissues

70
Q

What does 6MP do

A

Active form of AZA which is a thiopurine that interferes with DNA synthesis

71
Q

Indications for AZA

A

Autoimmune disorders

Kidney transplant

72
Q

What autoimmune disorders can be treated with AZa

A

SLA, croons, RA

73
Q

Side effects AZa

A

Myelosuppression
Increased toxicity with allopurinol use
Pancreatitis
Malignancy

74
Q

AZA myelosuppression

A

Severe bone marrow suppression

Can get leukopenia, thrombocytopenia, anemia’s including microcytic anemia, and/or pancytopenia may be seen in patients taking AZa

75
Q

Malignancy from AZA

A

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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