Anti-Inflammatories II

Question 1

Zileuton

Answer 1

LT inhibitor, blocks synthesis. treat asthma. adverse: increased liver enzymes, drug interactions. not for alcoholics

Question 2

Zafirlukast, Montelukast

Answer 2

LT inhibitor, receptor antagonist CysLT. CysLT R mediates airway inflammation, edema, constriction, thick mucus. drugs decrease chemotaxis, actions LT. treat asthma orally over weeks-months. Zafir- inhibits cytP450, may cause drug interactions

Question 3

General Steroids

Answer 3

adrenal cortex produces gluco/mineralcorticoids, adrenal androgens. glucocorticoids: protect glucose functions, promote lipolysis, vascular reactivity to vasoactive substances, suppress ACTH, TSH, GH, FSH

Question 4

General Steroid Mechanism

Answer 4

glucocorticoid R alters transcription. effects are not immediate, duration exceeds half life. immunosuppressive anti-inflammatory effects: decrease circulating inflammatory cells, neutrophil adherence, histamine release, LTC4, lymphocytes. inhibit production of arachidonic acid metabolites. prevent/reverse increased vascular permeability

Question 5

General Steroid Therapies

Answer 5

glucocorticoids admin orally/topically/parenterally/inhalation. treat rheumatic disorders, bronchial asthma, eczema, IBS, malignancies, autoimmune hepatitis

Question 6

General Steroid Adverse Effects

Answer 6

continued use- electrolyte imbalance, hypertension, hyperglycemia, CNS, Cushing’s symptoms, growth retardation, weight gain, edema, ulcers, delayed healing, thinning skin, muscle wasting. withdrawal effects- flare up of disease, acute adrenal insufficiency, anorexia, myalgia, weakness

Question 7

Etanercept

Answer 7

mimics circulating TNF R p75 with IgG1 Ab. binds TNF, interferes with it. self admin injections. adverse infections, cancer, vasculitis, liver disease

Question 8

AdalimuMAB, InflixiMAB, CertolizuMAB

Answer 8

monoclonal Ab binds TNF with high affinity, interferes with it. adverse fungal infections, TB

Question 9

Tocilizumab

Answer 9

recombinant, humanized monoclonal Ab, IL6 R antagonist. effectively treats refractory RA

Question 10

Leflunomide

Answer 10

inhibits di-hydro-orotate dehydrogenase- inhibits pyrimidine synthesis. pro-drug. decreases proliferation lymphocytes. high dose- inhibits TK+NFkB+TNFa+IL-1, down regulates cell cycle, decreases glycosylation. months to establish effect, years to eliminate. adverse liver toxicity, weight loss, early hypertension

Question 11

Hydroxychloroquine

Answer 11

decreased intracellular pH inhibits inflammatory cell function?

Question 12

Azathioprine

Answer 12

inhibits purine synthesis

Question 13

Soluble ICAM-1

Answer 13

soluble form of intercellular adhesion molecule, intercepts inflammatory cells

Question 14

Omalizumab

Answer 14

directed against IgE binding site for Fc receptor. inhibits immune response to allergens

Question 15

Glatiramer Acetate

Answer 15

stimulates myelin basic protein, competes with myelin antigens for presentation to T cells

Question 16

Cortistatin

Answer 16

endogenous cyclic neuropeptide, binds to immune cells

Question 17

Efalizumab

Answer 17

monoclonal Ab against CD11a, a leukocyte integrin. treat plaque psoriasis

Question 18

Abatacept (CTLA4Ig)

Answer 18

CD28 costimulus antagonist, blocks 2nd signal for T cell activation by binding CD80/CD86, causes anergy. treat refractory RA. inhibits progression, decreases joint inflammation/damage. adverse headache, nasopharyngitis, nausea