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68 Cards in this Set

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Name the five classes of immunosuppressive agents
Corticosteroids, cytotoxic drugs, T-cell specific drugs, antibody therapy, cytokine/receptor antagonists
Name 5 corticosteroids
hydrocortisone, prednisone, methyl prednisolone, betamethasone, triamcinalone
Give the pathway for glucocorticoid release from the adrenal cortex.
CRF from the hypothalamus stimulate the ACTH release from the pituitary --> ACTH stimulates synthesis and secretion of glucocorticoids from the adrenal cortex.
Give the pathway for mineralocorticoid release from the adrenal cortex.
Same as glucocorticoids, but mineralocorticoids are less dependent on ACTH
What are the major products of glucocorticoids and mineralocorticoids?
glucocorticoids = cortisol… mineralocorticoids = aldosterone
What effects do low or high circulating levels of cortisol have on CRF (ACTH --> corticoids)?
Low --> stimulation of CRF release… High --> inhibition of CRF
Besides CRF, what can stimulate pituitary release of ACTH?
inflammatory cytokines, like IL-1 and TNF
given that ACTH/cortisol is at its low at midnight and at its peak at 6:00 a.m., when would you give therapeutic glucocorticoids? Why?
at 6:00 to avoid inhibition of natural production of ACTH at other times during the day
What is ACTH used for?
What are the two homeostasis effects of corticosteroids?
1. Sodium homostasis and, 2. glucose homostasis
What is the effect of aldosterone?
Na+ retention --> water retention
What is the effect of cortisol?
increased energy in the form of glucose in times of stress
What is the mechanism of cortisol?
cortisol increases liver glycogen storage, increases glucogenesis, and decreases the peripheral use of glucose..
During cortisol secretion and resulting glucogenesis and glycogen storage, what is the source of glucose?
breakdown and decreased production of muscle proteins… and loss of bone matrix
How is cortisol like aldosterone?
like aldosterone, cortisol causes Na+/water retention
Besides, glucose storage and Na+ retention properties of cortisol, what other two effects does cortisol have?
renal loss of Calcium and redistribution of body fat
Glucocorticoids effect DNA transcription as part of their mechanism, how do glucocoriticoids gain access to the DNA?
they diffuse through the membrane and bind cytoplasmic receptor to form a complex --> then complexes are transported to the nucleus --> where they are involved in gene transcription, e.g., NFkB.
What is the major therapeutic effects of glucocorticoids?
anti-inflammatory effects
What are the 4 anti-inflammatory effects of glucocorticoids?
1. decrease granulocyte and monocyte function… 2. they also decrease the numbers of monocyte, eosinophils, and lymhocytes… 3. Inhibit cytokine and growth factor synthesis, which decreases vascular permeability… 4. They also increase intracellular levels of annexins or lipocortins, which block the activation of phospholipase A2
What are the downstream effects of increasing intracelluar annexins and lipocortins?
block activation of phospholipase A2 --> block production of arachidonic acid--> block PGG, TXA2, leukotrienes --> block cellular inflammatory response, e.g., phagocytic macrophage responses --> which in turn inhibits T-cell cell medicated activation (which requires leukotrienes and antigen presentation)
What are the indications for glucocorticoids?
hypersensitivities rxns
What is the clinical use of corticosteroids with cleaved side chains?
topical (skin diseases, as well mucus membrane diseases like asthma, and rhinitis), since they will not have a systemic affect
Name the 5 corticosteroids
(HPMTB): hydrocortisone, prednisone, methylprednisolone, triamcinolone, betamethasone
Give the relative potency of the 5 synthetic corticosteroids for anti-inflammatory activity.
hydrocortisone (1)< prednisone (4) < methyl prednisolone (5) < triamcinalone (5) < betamethasone (25-40 and 10 for topical activity)
Most corticosteroids are available in topical, oral and injectable forms, what is the exception to this?
prednisone is only available in oral form
how can on manage therapeutic doses of corticosteroids without significantly depressing the hypthalmic-pituitary axis?
give every other day… and in the morning
Review the side effects of glucocorticoid therapy…
page 191 of syllabus
name 3 cytotoxic drugs used as immunomodulators
azathioprine, cyclphosphamide, methotrexate
How do cytotoxic drugs work to modulate the immunity
they block cell division, and thus have a negative inductive phase effect (they don't effect the effector phase)
which cytotoxic drug is a derivative of 6 mercaptopurine? And what is its mechanism of action?
azathioprine --> metabolized to 6-MP, which blocks purine synthesis --> its metabolites are incorportated into DNA --> inhibit DNA synthesis
What are the 5 clinical indication for azathioprine?
1. Transplant rejection… 2. Severe rheumatoid arthritis… 3. Severe SLE… 4. Wegener's granulomatosis… 5. Polyarteritis nodosa (attack of small an medium sized arteries)
T/F azothiorine blocks both B and T cell mediated immunity
What is the mechanism of action of cyclophosphamide?
cyclophosphamide is an alkylating agent related to nitrogen mustard that cross links DNA… like azathioprine, it blocks the inductive phase of immunity
T/F cyclophosphamide blocks both B and T cell immunity.
false… it's primarily B cell modulating
What is the major use of cyclophosphamide of chronic inflammatory diseases?
Wegener's granulomatosis, nephrotic syndrome, polyarteritis nodosa, and SLE
What is the major SE of cyclophosphamide?
hemorrhagic cystitis, due to urine excreted metabolites
What are the 3 mechanism of action of immunomodulator cytotoxic drug, methotrexate?
1. methotrexate inhibits DHFR and prevents DNA synthesis of rapidly dividing cells… 2. and blocks other folate dependent enzymes… 3. its anti-inflammatory effects may be due to inhibition of neutrophil chemotaxis
What are the immunomodulation clinical indications for methotrexate?
Rheumatoid arthritis, Crohn's disease
Name 2 T-cell specific drugs used in immunomodulation.
Cyclosporine and tacrolimus
What effect does cyclosporine have on T-cell activation?
it's proposed that it may decrease essential T-cell growth factors, IL-2 and gamma interferon (which activates macrophages)
Which T-cell is primarily targeted by cyclosporin?
T-helper cells and spares T-suppressor cells
What does cyclosporin bind and what is the effect of this binding?
binding of cyclosporin to cyclophilin blocks the generation of calcineurin (which is a signal for DNA synthesis) … it may also bind lymphokine regulators
What is the primary indication for cyclosporine?
prevent transplant rejection… it's also used Rx hypersensitivities, including aplastic anemia, juvinile diabetes, psoriasis, and uveitis
What is the major toxic side effect of cyclosporine?
nephrotoxicity and hypertention, and others such as hypertrichosis, encephalopathy, hepatotoxicity…
What precaution can be taken to miminize toxic effects of cyclosporine?
monitor for low serum cholesterol, which increases the risk of toxicity
Which immunosuppressive drug may reactivate EB virus, and increased one's risk of lymhoma.
What is the main clinical indications for tacrolimas?
Tacrolimas: prevent liver and kidney graft rejection… also dermatitis and other allergic conditions mediated by T-cells
What are the 2 mechanism of action of tacrolimas?
1. like cyclosporine, it decreases IL-2 and other lymphokines… however it 10-100 x more potent… 2. It also inhibits calcineurin phosphatase
What are the toxic SE of tacrolimas?
Like that of cyclosporine: nephrotoxicity and hypertention, and others such as hypertrichosis, encephalopathy, hepatotoxicity… HOWEVER, it has more neurological complications, i.e., headaches
Name 2 drugs used in human monoclonal antibody therapy
infliximab and omalizumab
What is infliximab used to treat? And what is its mechanism of action
infiximab are antibodies against TNF-∂ and used to treat Crohn's disease and Rheumatoid arthritis
What are 3 adverse side effects of infliximab use?
increased infection (e.g., TB), lymphoma and exacerbation of MS
What is the clinical indication for Omalizumab? And what is its mechanism of action?
It is a humanized monoclonal Ab IgE… used to Rx asthma
Give one example of a cytokine/receptor antagonist used to modulate the immune system.
What is etanercept's mechanism of action?
Etanercept has two binding domains, one binds to TNF with the Fc domain of human IgG and the other binds to TNF and the other binds to a phagocyte, thus both inhibiting TNF and eliminating it
Name 5 immunopotentiators
IV gammablobulin, interferons ∂, ß and gamma, Levamisole, IL-2 and BCG
What is the mechanism of action for the immunopotentiating of IV gamma globulin?
passive immunity for people that Ig of their own… painful intramuscular admin has been replaced by IVIG preparations
What are the 4 indications for IV gamma globulins?
1. Hypogammaglobulinemia… 2. Idiopathic autoimmune thrombocytopenia… 3. Prevention of infection in B cell malignancies… 4. Kawasaki's disease
what are the adverse rxns of IV gamma globulin Rx?
Anaphylatoid rxns (must be given slowly)… 2. If given to congenitally difficient IgA patients, there may be high circulating levels of anti-IgA, thus give a prep w/o IgA
What is the mechanism of action of BCG?
it was used as a vaccine for TB, , but it has been shown to stimulate macrophage and T-cell function
What is the indication for BCG use?
bladder malignancies and colon cancer
What is the mechanism of action for Levamisole? What is it used to Rx?

What is the mechanism of action of gamma interferon?
it’s a anti-helminthic drug that enhances T-cell and macrophage function…. It's used as an adjuvant to Rx colon cancer

Gamma interferon activates macrophages
What is the mechanism of action of IL-2? What is it used to Rx? What are the adverse SE?
it's a T-cell growth factor... used to Rx renal cell carcinoma…. Hypothyroidism, capillary leak syndrome --> fatal pulmonary edema
Between ∂, ß and gamm interferon, which is produced by activated T-cells and serves to activate macrophaes?
given that gamma interferon activates macrophages, in which two disease is its use indicated?
chronic granulomatous disease and visceral leishmansiasis
Which interferon is used to treat MS?
Beta interferon
Which interferon is used to Rx, hairy cell leukemia, other malignancies, Hep B and C, Kaposi's sarcoma… etc.?
alpha interferon
In determining Ab origin, what do the following represent? momab, ximab, zumab, umab
mo = mouse, xi =chimeric human, zu = humanized, umab = human (pure)