Immunopharmacology TUCOM

30 terms by mquacine

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Prednisone

Corticosteroid
Immunosuppressant
Short-duration
MOA: converted in-vivo to prednisolone
DMARD Tox

Dexamethasone

Corticosteroid
Immunosuppressant
Long-action
MOA: DMARD
Tox: DMARD

DMARD MOA

inhibits transcription of inflammatory mediators
Increase some anti-inflammatory regulator genes
Decrease production of cytokines
Reduced expression of adhesion molecules =decreased leukocyte adhesion

Cytokines Effected by DMARDS

IL-2
TNF-a
GM-CSF
IL-3
IL-4
IL-5
CXCL8

DMARD Toxcities

Osteoporosis
Neuropsychiatric
Cushingoid appearance
impaired glucose metab
cataract glaucoma
Skin thinning
cardiovascular

DMARD clinical Uses

prevention of acute allograft rejection
Treatment of all inflammatory conditions
Short-term anti-inflammatory

NSAIDS MOA

reduce inflammation
target non-specifc inflammtory cells
overlapping therapuetic goals
Not-immunosuppressive
inhibits PG synthesis
inhibits COX1/COX2 activity
no effect on T/B cells

NSAIDS clinical Uses

Inflammatory conditions
Not for transplantation

NSAID Drugs

Aspirin
Ibuprophen
Naproxene
Celecoxib

Azthioprine

Purine Antagonist
MOA: pro-drug 6-mercaptopurine
Clinical Uses: Tx of Rheumatoid Arthritis Anti-inflammatory, graft rejection
Adverse Effects: Myelosuppression, Dose dependent, Neutropenia, thrombocytopenia
Contra-Indication: current infection
pancreatitis

Cyclophosphamide

DNA-Alkylating Agent
Clinical Uses: prevention/reversal and reversal of graft rejection
Treatment of auto-immune disease
SLE
Myasthenia Gravis

Chlorambucil

DNA-Alkylating Agent
Clinical Uses: prevention/reversal and reversal of graft rejection
Treatment of auto-immune disease
SLE
Myasthenia Gravis

Mycophenolate Mofetil

MOA: MMF converted in-vivo to mycophenolic acid
Inhibits T/B cell proliferation
Prevents DNA synthesis by inhibiting IMP-DH prevents guanosine nucleotide production
Clinical Uses: Prevention of GVHD
graft rejection
Lupus nephritis
Toxcities: Diarrhea, vomitting, nausea, meylosupression
Contraindication: Hepatic Insufficiency

Methotrexate

Cytotoxic Drug
MOA: Folic acid antagoinst
Clinical Uses: Rheumatoid arthritis Gold standard drug

Cyclosporin

Calcineurin Inhibitor
MOA: prevents IL2/IL-2 receptor production
Clinical Uses: prevetion of graft rejection, not reverse graft rejection
Tox: Reversible B-lympoproliferatie disorders, Nephrotoxic

Tacrolimus

Calcineurin Inhibitor
MOA: binds FK protein inhibits IL-2 Secretion and other cytokines
Clinical Use: Prevention/Rejection of organ transplantation
Toxcities: Nephrotoxic, Diabetes, peripheral neuropathy

Calcineurin Inhibitors MOA

prevent Ca2+ binding to calcineurin
black signal transduction pathway
Prevents IL-2 produciton
Prevents T-cell proliferation
B cell phagocyte function spared

Sirolimus

mTOR inhibitor
MOA: Inhibits T-cell proliferation
binds FKBP-12 and inhibits mTOR pathway
Blocks IL-2 signalling
Clinical Uses: prevention of renal transplant rejection
Adverse Effects: Nephrotoxicity, Hypercholestrolemia, Hyper triglyceridemia, mylosuppression

Etanercept

Soluable ligand/Receptor drugs
MOA: TNF receptor Fc fusion protein, Binds soluable TNF, Blocks TNF
Clinical Uses: Used for Rheumatoid Arthritis, Crohn's Disease, Ulcerative Colitis, Psoriasis

Abatacept

Soluable Ligand/Receptor Drugs
MOA: Soluable CTLA4-Ig, competitive inhibitor of CD28
prevents co-stimulatory CD80/86
Prevents T-cell activation and cytokine release
Clinical Uses: Treatment of Rheumatoid Arthritis

Ankinra

IL-1 cytokine antagonist
Soluable Ligand Receptor Drugs
MOA: sIL1 receptor antagonist
Clinical Uses: RA

Gemtuzumab

Leukemia/lymphoma therapy
MOA: anti CD33 w/calicheamicin. Binds CD33+ cells Drug is internalized binds to DNA resulting in DNA double stranded breaks and cell death

Denileukin

Leukemia/lymphoma therapy
Conjugate
MOA: IL2+Diptheria toxin fusion protein. Binds to IL2r+ cells
Toxins prevent protein synthesis and cell death
Clinical Uses: cutaneous T-cell Lymphoma

Rituximab

Leukemia/lymphoma Therapy
MOA: CD20 binding, Blocks Ca2+ channel on B-cell
Clinical Uses: CLL, B-cell lymphoma

Trastuzumab

Cancer Treatment
MOA: HER2/neu, Growth Factor receptor
Clical Uses: Breast Cancer

Daclizumab

Immunosuppresant for Organ Transplantation
MOA: IL2r, CD25
Clinical Uses: Allograft rejection
GVHD

Infliximab

TNF antagonist
Immunosuppresant
MOA: TNF targeting
Clinical Uses: Crohns disease, RA, Ulcerative Colitis,

Natalizumab

Lymphocyte Trafficking Inhibitors
MOA:alpha-4 integrin blocks vascular adhesion molecuels prevents T lymphocyte entry into brain or gut
Clinical Uses: Relapsing MS, Crohns Disease
Adverse Effects: Risk ofr multi focal leukoencephalopathy

Fingolimod

Lymphocyte Trafficking Inhibitors
MOA: Prodrug, Phosphorylated by sphingosine kinase
Blocks lymphocyte from exiting lymph nodes causes lymphopenia
Targets CD4>CD8>b-cells
Clinical Uses: Relapsing MS, Taken Orally
Adverse Effect: Bradycardia, Opportunistic infections

Omalizumab

Immunosupressant
MOA: IgE antagonist
Clinical Uses: Asthma

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