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4q Pharm Test2 > Immunosupressive Drugs > Flashcards

Immunosupressive Drugs Flashcards

1
Q

Uses of immunosuppressive drugs (4)

A
  1. prevent rejection following organ transplant: life long treatment
  2. tx acute rejection episodes: short term treatment
  3. tx various autoimmune d/os: long-term tx
  4. tx allergies & asthma
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2
Q

Corticosteroids (prednisone) affect immune system : short term? long term? how?

A

SHORT TERM: ANTI-INFLAMMATORY effects occur rapidly (hours-days)
IMMUNOSPRESSIVE effects take time (SEVERAL WEEKS) to develop

affect most aspects of immune response

  • DEPRESS MACROPHAGE FXN
  • MODIFY fxn of T HELPER cells by inhibiting expression of genes for IL-1, IL-2, IL-6, interferon alpha and TNF-alpha
  • INHIBIT RESPONSE of cytotoxic T cells & NKI cells to IL2 & other cytokines
  • INHIBIT T CELL PROLIFERATION
  • frequently used short term (2-3 mos) POST-TRANSPLANT to decrease likelihood of rejection
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3
Q

Corticosteroid uses (3)

A
  • w/other immunosuprressives in transplant pts to prevent rejection
  • minimize allergic response to antilymphocytic globulin or monoclonal antibodies
  • AUTOIMMUNE DZs
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4
Q

Corticosteroids (SEs w/chronic use)

A
  • HYPERGLYCEMIA -OSTEOPOROSIS
  • suppression of HPA axis
  • truncal obesity, moon face, buffalo hump, salt retention
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5
Q

T cell suppressants: name the 3 approved drugs

and what do they do

A

Cyclosporine (Sandimmune)
Tacrolimus (FK506; Prograf)
Sirolimus (Rapamune)

selectively inhibit fxn of T-lymphocytes
precent cell-mediated immunological rxns, such as rejection

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6
Q

Cyclosporine (Sandimmune; Neoral)

A
  • inhibits T-cell activation w/out causing bone marrow suppression
  • binds to cyclophilin, inhibiting fxn of CALCINEURIN, needed for ACTIVATION of T-cells
  • used to prevent rejection in organ transplant pts
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7
Q

Cyclosporine: drug interactions, therapeutic range

A

drug intrxns are COMMON
1. pentobarbital, PHENYTOIN & RIFAMPIN induce CYP3A4 & DECREASE CNCTRN (PR decreases cyclosporine concentration)

  1. ERYTHROMYCIN, KETOCONAZOLE, GRAPEFRUIT JUICE & VERAPAMIL inhibit CYP3A4 & INCREASE CNCNTRTN (K-Veg increases cyclosporine concentration)

therapeutic range: NARROW
-monitor blood levels [rejection if dose too low, toxicity if dose to high]

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8
Q

Cyclosporine uses (4)

A
  1. prevent rejection in organ transplant patients (heart, kidney, liver, lung)
  2. may be combined w/other immunosuppressive drugs
  3. BONE MARROW transplants
  4. tx of various AUTOIMMUNE d/os (psoriasis, DM type 2, RA, IBD, severe asthma, etc)
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9
Q

Cyclosporine toxicity

A

potentially serious
GINGIVAL HYPERPLASIA,

HTN (in 30% of renal, almost all hrt transplant pts)

RENAL TOXICITY (very common, maintain fluid intake

HYPERGLYCEMIA

hirsuitism, hyperlipidemia, gallstomes
D, N/C, anorexia, abdominal pain

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10
Q

Tacrolimus; FK506 (Prograf): how does it work (2)

A

T cell suppressor

  • INHIBITS FXN OF CALCINEURIN through binding FK506
  • INHIBITS T-Cell activation & decreases IL-2 & IL-4
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11
Q

Tacrolimus; FK506 (Prograf): indications, administration, therapeutic range, spec instructions?

A

used more commonly than cyclosporine; (U) better tolerated

  • DOC to PREVENT REJECTION
  • “RESCUE” DURING A REJECTION EPISODE
  • uses same as cyclosporine

IV, oral, topical for atopic dermatitis

narrow therapeutic range
FOOD DECREASES ABSORPTION BY >80%; BEST TAKEN ON AN EMPTY STOMACH

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12
Q

Tacrolimus; FK506 (Prograf): side effects

A

nephrotoxicity & HTN are dose limiting SEs, kidney fxn & BP are monitored frequently

HYPERGLYCEMIA is common, may require use of insulin

increase in OPPORTUNISTIC INFECTIONS & NEOPLASMA, ESP SKIN CA

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13
Q

Tacrolimus; FK506 drug intrxns

A

-metabolized by CYP3A4 (like cyclosporine)
NO GRAPEFRUIT JUICE WHEN TAKIN TACROLIMUS
narrow therapeutic range, BLOOD LEVELS MONITORED REGULARLY
-nephrotoxicity additive if given w/cyclosporine

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14
Q

Pimecrolimus (Elidel): use, administration, side effects, mechanism

A

CREAM used TOPICALLY for TX of ATOPIC DERMATITIS

  • less likely to cause skin atrophy than corticosteroid creams
  • burning & SKIN IRRITATION may occur initially
  • mechanisms of action is similar to Tacrolimus
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15
Q

Sirolimus (Rapamune): what does it do, administration, absorption, metabolism, positive effects, negative effects

A

BLOCKS RESPONSE OF T-CELLS to IL2, inhibits B cell proliferation

  • reduces rejection after kidney & heart transplants
  • long-lasting effect
  • NO renal damage (so starting to replace cyclosporine & tacrolimus)

oral absorption reduced significantly by food; metabolized by CYP3A4

may cause anemia, leucopenia, impair wound healing, increase cholesterol & TRIGLYCERIDES

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16
Q

Mycophenolate Mofetil (CellCept); Mycophenolate (Myfortic)

what does it do?

how is it administered? absorbed? excreted?

A

decrease proliferation
-inhibit inosine monophosphate dehydrogenase, needed for DE NOVO purine synthesis in T & B lymphocytes (specific for these cells, others don’t use this pathway

SELECTICLEY SUPPRESSES LYMPHOCYTE PROLIFERATION & ANTIBODY FORMATION by B cells

  • inhibits recruitment of leukocytes to inflammatory sites
  • given orally, rapidly absorbed, 90% excreted in urine
17
Q

Mycophenolate Mofetil (CellCept); Mycophenolate (Myfortic): uses, side effects

A

Uses: combined w/cyclosporine or tacrolimus & glucocorticoids TO PREVENT REJECTION
-used in rejection episodes refractory to other drugs, or where other drugs aren’t tolerated

SEs:
GI most common: N/V, diarrhea, abdominal pain, constipation, dyspepsia, anorexia
-increased incidence of INFECTIONS & sepsis
-SKIN RASH; leucopenia possible

18
Q

Azathioprine (Imuran): how does this think work

A

converted in vivo to 6-mercaptupurine, which inhibits de novo purine synthesis->blocks gene translation, inhibits cell proliferation, lymphocyte fxn, delayed hypersensitivity rxn & cellular cytotoxicity after transplant

19
Q

Azathioprine (Imuran): Uses, SEs, interactions

A

adjunct to PREVENT REJECTION in organ transplant pts
tx of SEVER REHEUMATOID ARTHRITIS

SE: BONE MARROW SUPPRESSION: (C) leukopenia, thrombocytopenia, anemia
-increased risk of INFECTIONS, esp herpes
-N/V/D/pancreatitis/alopecia
-skin rashes, drug fever, (P) hepatotoxicity
FETAL TOXICITY: don’t use in pregao

AZATHIOPRINE IS METABOLIZED BY XANTHINE OXIDASE, in pts tx w/allopurinol (Xylorpim, the does of azathioprine must be reduces significantly)

20
Q

Cyclophasphamide (Cytoxan): effects

A

direct effect on T and B lymphocytes, esp those that have undergone antigenic differentiation & division

CAN INHIBIT ESTABLISHED IMMUNE RESPONSE

21
Q

Cyclophasphamide (Cytoxan): uses, side effects

A

ORGAN TRANSPLANT RESCUE & BONE MARROW transplants

tx of severe MS, RA, lupus

ANTINEOPLASTIC

SEs: HEMORRHAGIVE CYSTITIS: prevent w/hydration & MESNA
n/v
BONE MARROW SUPPRESSION
aspermia after 3-6 mos therapy, ovulation impairment, infertility
BLADDER fibrosis & carcinoma
alopecia

22
Q

Methotrexate (Folex): mech of action, uses, SEs

A

inhibits DIHYDROFOLATE REDUCTASE: disrupts folate-dependent steps in purine synthesis, well absorbed orally, excreted by kidneys

uses: IMMUNOSUPPRESSION in organ transplant recipients
psoriasis
RHEUMATOID ARTHRITIS

SEs: BONE MARROW SUPPRESSION, alopecia, hepatotoxicity, FETAL DEATH-DO NOT USE IN PREGNANCY

23
Q

Thalidomide (Thalomid)

A

SUPPRESSES TNF-alpha
USED FOR PRECENTION OF GRAFT-VS HOST

USES:
HIV-related wasting syndrome decrease ulcers
causes weight gain

SEs: PREGNANCY CATEGORY X-TERATOGENIC, drowsiness, dizziness, HA, neutropenia in up to 20% of HIV pts, constipation & peripheral neuropathy

24
Q

Name 3 category X drugs (not all from immunosuppression lecture)

A

Thalidomide
Ribavirin
Efavirenz

25
Q

Muromonab CD3, OKT3 (Orthoclone): activity, use, toxicity

A

mouse monoclonal ANTIBODY TO THE T3 (CD3) site on T-lymphocytes

blocks activity of cytotoxic T-cells & prevents generation of new cytotoxic T cells, rarely

rarely used for acute transplant rejection b/c of toxicities:
CYTOKINE RELEASE SYNDROME (flu-like response, shock) occurs w/first dose, starts within 30 mins & may last hours, prevent by pretx with corticosteroids
-FEVER, CHILLS, NAUSEA COMMON
-chest pain & dyspnea, rarely sever pulmonary edema which has been fatal

26
Q

Daclizumab (Zenepax); Basiliximab (Simulect)

what are they?

what do they do?

what are they used for?

SEs?

drug intrxns?

A

HUMANIZED monoclonal antibodies that bind to & block IL-2 receptor on surface of activated T-lymphocytes

REDUCES REJECTION AFTER RENAL TRANSPLANT

FEW SEs or drug intrxns b/c produced by recombinant DNA technology

DOESN”T cause cytokine release syndromes, but may rarely cause anaphylaxis

LONG HALF-LIFE, effects persist for 4-6 weeks after two infusions

no drug interactions

27
Q

Interleukin-2, Aldesleukin (Proleukin): what does this do, uses (2)

A
  • stimulates production & activity of T CELLS
  • increase # of B CELLS
  • stimulates MACROPHAGES
  • induces INTERFERON GAMMA production

uses: METASTATIC RENAL CELL CARCINOMA (5-10% effectiveness)
malignant melanoma

28
Q

Interleukin-2,Aldesleukin (Proleukin): toxicity

A

must be administered in a hospital setting; SEVERE HYPOTENSION & reduced organ perfusion
-PULMONARY congestion, dyspnea, loss of plasma proteins & fluid into extracellular space
-HEMATOLOGIC: anemia & thrombocytopenia
-FEVER< CHILLS< PAIN, nausea, vomiting, diarrhea
renal: oliguria, BUN elevation, serum creatinine elevation
CNS: mental status changes, irritability, confusion, depression
-increased risk of infections

29
Q

Oprelvekin, rh-IL-11 (Neumega)

A

recombinant version of human INTERLEUKIN-11

administered subcutaneously to PREVENT SEVERE CHEMOTHERAPY-INDUCED THROMBOCYTOPENIA

FLUID RETENTION, peripheral edema; moderate decreases in hemoglobin may occur

30
Q

Granulocyte Colony-Stimulating Factor; Filgrastim (Neupogen):

what is it

what is it used for

administration

side effects

A

human recombinant G-CSF (filgrastim)

use: tx severe NEUTROPENIA after autologous hematopoetic stem cell transplant

NEUTROPENIA DUE TO CANCER CHEMOTHERAPY OR INTERFERON THERAPY

REVERSE NEUTROPENIA CAUSED BY ZIDOVUDINE in AIDS pts

admin: SUBCUTANOUS (PEGylated to provide slow-release depot) or slow IV infusion

SE:moderate BONE PAIN, local skin rxns at injection site

31
Q

Epoetin alfa (Epogen; Procrti), Darbopoetin alfa (Aranesp):

what is it

uses

SEs

A
  • recombinant human erythropoietin
  • acts on EPO receptors on red cell progenitors to stimulate erythroid proliferation

USES:
1. anemia due to chemo (a/w interferon of CA chemo)
-(U) used when hemoglobin <10mg/dL
2. EPO deficiency in pts w/chronic kidney disease
Darbopoetin has longer duration of action

SEs: HTN, increased risk of blood clots
hemoglobin should be kept below 12 to decrease SEs

32
Q

Interferons

A

cytokines produced by leukocytes & T cells; ANTIVIRAL & antiproliferation effects
-produced in rspnse to VIRAL & OTHER STIMULI
-interferons INDUCE ANTIVIRAL PROTEINS that protect from viral infection, by inhibiting virus-directed translation & transcription
-increase expression of class I MHC on infected cells
3 major families: alpha, beta, gamma

(U) administered subcutaneously

33
Q

Interferon alpha-2b (Intron-A; PEG-INtron)

A

-used for tx of chorionic VIRAL HEPATITIS B & C (for 6 months to 1 yr)
~80% effective in HBV
~50-60% effective against HCV combined w/oral ribavirin
-approved for use in hairy cell leukemia, Kaposi’s sarcoma, codylomata acuminate (injected into wart)
-long-term release polyethylene glycol prep, is taken once per week (PEG-Intron)

34
Q

Interferon beta-1b (Betaseron)

A

suppresses class II MHC presentation & decreases antigen presentation in the nervous system

  • decreases frequency of exacerbations of relapsing-remitting MULTIPLE SCLEROSIS
  • INTERFERON BETA-1a also approved for tx MS

4q Pharm Test2 (7 decks)

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