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Pharmacy Drugs > 430 Immunosuppressive Agents > Flashcards

430 Immunosuppressive Agents Flashcards

1
Q

Rh(D) antibodies (RhoGAM)

A

Administered to the Rh negative mother within 72 hours after birth (neutralize the Rh positive antigens at birth)

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2
Q

Cyclosporine MOA

A

Enters T cell, binds to cyclophilin receptor creating a cyclophilin-cyclosporine complex
Inhibits calcineurin
Inhibits synthesis and secretion of IL-2
Inhibits expression of IL-2 receptors

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3
Q

Cyclosporine ADME (bioavailability, peak, half-life, metabolism, excretion)

A 
Bioavailability 20-50% 
Peak < 3-4hrs 
Half-life 6hrs
Metabolized by liver 
Excreted in bile
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4
Q

Cyclosporine DDI

A

Induce cyt P450–accelerate clearance

Inhibit cyt P450–reduce clearance

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5
Q

Cyclosporine toxicity

A

renal and nephrotoxicity

HTN, neurological, elevated hepatic transaminase, hirsutism and gingival hyperplasia

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6
Q

Cyclosporine indications

A

tissue transplantation
GVHD
Autoimmune diseases

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7
Q

Tacrolimus MOA

A

Enters T cell, binds to immunophilin FKBP, creating a Tacrolimus-immunophilin complex
Inhibits calcineurin
Inhibits IL-2 synthesis and secretion
Inhibits expression of IL-2 receptor

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8
Q

Tacrolimus ADME (bioavailability, peak, metabolism, half-life, excretion)

A 
Bioavailability 25% 
Peak 1-4 hrs 
Metabolized in liver 
Half-life 10hrs 
Excreted in urine
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9
Q

Tacrolimus side effects

A

HA, tremors, insomnia, nausea, GI discomfort, lymphoproliferative disorders

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10
Q

Tacrolimus indications

A

Tissue transplantation

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11
Q

Rapamycin MOA

A

Enter T cell and bind to immunophilin, creating rapamycin-immunophilin complex
Inhibits mTOR (which inhibits IL-2 signaling)
Inhibits cyclin E (which inhibits cell cycle from G1 to S phase)
-blocks T cell proliferation
-apoptosis

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12
Q

Rapamyin ADME (metabolism)

A

Metabolized in liver

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13
Q

Rapamycin DDI

A

Induce cyt P450–accelerate clearance

Inhibit cyt P450–reduce clearance

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14
Q

Rapamycin side effects

A

impaired wound healing (b/c of apoptosis), allergic reaction, increase risk of infection

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15
Q

Rapamycin Indications

A

Prevention of tissue rejection
Cancer
Good in combination with cyclosporine

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16
Q

Everolimus MOA

A

Enter T cell and bind to immunophilin, creating everolimus-immunophilin complex
Inhibits mTOR (which inhibits IL-2 signaling)
Inhibits cyclin E (which inhibits cell cycle from G1 to S phase)
-blocks T cell proliferation
-apoptosis

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17
Q

Everolimus indications

A

Prevention of graft rejection
Cardiac allograft vasculopathy
Post-transplant lymphoproliferative disorders

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18
Q

Fingolimod MOA

A

Binds to G-protein linked S1P1 receptor present of lymphocytes and thymocytes
Internalization of the receptor (unable to egress from lymphoid organs)

Second MOA—causes lymphocytes to move from circulation into secondary lymphoid tissues (decrease peripheral blood lymphocyte count)

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19
Q

Fingolimod indications

A 
Multiple sclerosis (delay progression) 
Potential for heart failure and arrhythmia
20
Q

Fingolimod side effects

A

Fatal infection
Bradycardia
Hemorrhage

21
Q

Belatacept MOA

A

Fused Fc of IgG1 with EXTRA cellular domain of CTLA-4 (CD152) binds to CD80/86 to decrease activation of helper T cells

22
Q

Belatacept indications

A

Prophylaxis for rejection of kidney transplant

ONLY given to Epstein-Barr seropositive patients

23
Q

Belatacept side effects

A

Increase risk of post-transplant lymphoproliferative disorder (PTLD)
Increase risk of infection
Development of malignancies

24
Q

Abatacept MOA

A

Differs from Belatacept by TWO amino acids

Fused Fc of IgG1 to CTLA-1 (CD152) binds to CD80/86 and decreases T cell activation

25
Q

Abatacept Indications

A

Treat RA in those who don’t respond to other treatments (delays progression of structural damage)

NOT used in combination with Kineret and TNFalpha drugs

26
Q

Abatacept side effects

A

Flu-like symptoms: fatigue, sore throat, drug cough, trouble breathing, wheezing, fever, chills, night sweats

27
Q

Adrenocortical steroids MOA

A

Inhibit T cell proliferation
Inhibit expression of encoding cytokines (IL-2, IL-1, IL-6, IFNalpha, TNFalpha)
Anti-adhesion effects

28
Q

Adrenocortical steroids Indications

A

Preventing transplant rejection
Autoimmune disorders
Minimize allergic reactions with monoclonal antibodies

LARGE doses—reversal of acute graft rejection
LOW doses—prevent GVHD

29
Q

Cytotoxic drugs MOA

A

Kill both B and T cells

Prevent the expansion of both B and T cells

30
Q

Azathioprine (cytotoxic drug) indications

A

Prevent transplant rejection (combination with other immunosuppressive agents or prednisone)
Reserved for patients not responding to other therapies

31
Q

Azathioprine (cytotoxic agent) side effects

A 
Leukopenia 
Thrombocytopenia 
GI toxicity 
Hepatotoxicity 
Carcinogenicity
32
Q

Mycophenolate Mofetil MOA

A

Selective for B and T lymphocytes because of its reliance on the de novo pathway (NOT salvage pathway)
Suppresses lymphocyte proliferation and antibody formation by B cells
Inhibit recruitment of leukocyte glycoproteins to inflammatory sites

33
Q

Mycophenolate Mofetil ADME (bioavailability, metabolism, elimination)

A

Bioavailability 94%
Metabolized by glycuronyl transferase to active metabolite
Eliminated in urine

34
Q

Mycophenolate Mofetil DDI

A

Antacids containing Mg and Al leads to decreased absorption

35
Q

Mycophenolate Mofetil Indications

A

After renal, heart, liver transplantation

Combination with cyclosporine and corticosteroids

36
Q

Cyclophosphamide MOA

A

Alkylates DNA in proliferating cells (B and T cells)

37
Q

Cyclophosphamide indications

A

Large doses: immunosuppressive agent in bone marrow transplants
Small doses: treat variety of autoimmune disorders

38
Q

Methotrexate indications

A

treatment of RA

39
Q

Methotrexate side effects

A

Chronic use of low dose can produce liver toxicity

40
Q

Muromonoab-CD3 (OKT3) MOA

A

Polyclonal antibody directed against T cells and specific for 20,000-dalton glycoprotein in CD3 complex
Antibody itself is directed against polypeptide present in CD3 complex

41
Q

Muromonoab-CD3 (OKT3) indications

A

Adjuvant for acute rejection in allograft (no prevention of rejection except in bone marrow transplantation to prevent GVHD)

42
Q

Muromonoab-CD3 (OKT3) side effects

A

Flu-like symptoms (chills, fever)
Dyspnea, chest pain, wheezing, GI effects
Pulmonary edema (fatal)
Reversible CNS syndrome

43
Q

Methoxsalen indications

A

ONLY used for treatment of T cell lymphoma resistant to standard therapy

44
Q

Methoxsalen MOA

A

2 hours after patient is given methoxsalen blood is removed and exposed to ultraviolet light—radiated cells are returned to patient and process repeated again in 24hrs
Methoxsalen intercalates into DNA and modifies DNA structure inhibiting T cell function (killing T cells and stop immune reaction)

45
Q

Immunostimulants (boost immune response)

A

BCG (vaccine for TB, protects against leprosy)
Levamisole
Isoprinosine
Cytokines (IFN alpha, IL-2)

Pharmacy Drugs (37 decks)

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