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Pharm > Exam One; Therapeutic Use, MOA, AE. ; inflammatory mediators, nsaid, immunosuppressants, RA, gout > Flashcards

Exam One; Therapeutic Use, MOA, AE. ; inflammatory mediators, nsaid, immunosuppressants, RA, gout Flashcards

1
Q
  • Therapeutic use: Antipyretic, analgesic. Given in 325mg doses.
  • MOA: Inhibits COX. Peroxides inhibit function; antioxidants stimulate.
  • AE: Liver toxicity
  • Notes: Treat toxicity with N-acetylcysteine.
  • Toxicity: Liver in large doses (10g); GSH inactivates with P450
A

Acetaminophen

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2
Q

• Therapeutic Use: RA! antipyretic, Antiplatelet, analgesia, anti-inflammatory, prevents MI prophylactically.
• MOA: irreversibly Acetylates COX; salicyclate competitively inhibits. Inhibits thromboxane A2 synthesis.
o Nonimmunologic – defect in mast cell histamine storage and shunting of arachidonic acid Lipox pathways.
• AE: Everything imaginable!
• Notes: Do not give to pregnant chick in labor. Can cause a gout flare up. Large doses can stimulate glucocorticoid secretion. Epinephrine release => hyperglyemia
• Toxicity: 50-80 = respiratory alkalosis; 80-110 = metabolic acidosis; >160 = respiratory acidosis/ death.

A

Aspirin

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3
Q
  • Therapeutic Use: used in acute gouty attacks.

* MOA: an NSAID that inhibits PG synthase and urate crystal phagocytosis.

A

Indomethacin

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4
Q
  • Therapeutic Use: Hormonal agent/ Adrenocorticosteroid. part of MOPP and CVPP
  • MOA: glucocorticoid receptor; regulates transcription of specific proteins involved in the metabolism and inflammatory response.
  • AE: Cushing’s and immunosuppression
A

Prednisone

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5
Q

• MOA: binds cortisol-receptor complex and directly affects DNA to decrease cytokines, and impair macrophage, T cell and B cell function.
• AE: Affect renal secretion and need to do a withdrawal process.
o Toxicity: Cushings can develop with long term use.
• Notes: Vasoconstricts, and decreases capillary permeability.

A

Dexamethasone

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6
Q

• Therapeutic Use: Calcineurin inhibitor. Transplant rejection, autoimmune diseases (RA), ophthalmic emulsion.
• MOA:
o Cyclosporin: Binds cyclophilin C to decrease cytokine production and lower T cell response. Met by CYP3A4. Inhibits synthesis of IL-1 and IL-2.
o Tacrolimus: binds FK506 to inhibit calcineurin => lower cytokine production and T cell response. Much more potent than cyclosporine.
• AE: Serious but reversible nephrotoxicity (dose limiting), stimulates TGF-B which may lead to cancer
Notes: eryhthromycin, ketoconazole, amphotericin B, and grapefruit juice inhibit metabolism. Phenobarbital and rifampin increase clearance. Metabolized by CYP450 3A.

A

Cyclosporin A

Tacrolimus (FK506)

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7
Q

• Therapeutic Use: Antiproliferative agent. Oral, transplant rejection
• MOA: Binds FKBP-12 but doesn’t inhibit calcineurin, inhibits mTOR to inhibit T cell activation
• AE: Thromboytopenia, leucopenia, hyperlipidemia.
• Notes: No effect on cytokines.
o Rap(e) is Sirious! Unless you yell surprise.

A

Sirolimus (Rapamycin, Rapamune)

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8
Q
  • Therapeutic Use: oral and IV combine with corticosteroids to inhibit transplant rejection and RA.
  • MOA: Prodrug; inhibits purine and inosinic acid synthesis. Cytotoxic agent; anti prolif
  • AE: Bone marrow suppression, GI toxicity, mild hepatotoxicity. Carcinogenic and mutagenic.
  • Notes: Co-administeration with allopurinol may increase toxicity.
A

Azathioprine

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9
Q
  • Therapeutic Use: Oral and IV, Combine with cyclosporine (calcineurin inhibitor) and corticosteroids to prevent transplant rejection.
  • MOA: inhibits inosine monophosphate DH => lower purine synthesis and T/B lymphocytes.; anti prolif
  • AE: Diarrhea, leukopenia, cytomegalovirus.
A

Mycophenoate mofetil

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10
Q
  • Therapeutic Use: SIP-R agonist; oral; Multiple sclerosis
  • MOA: Lymphocyte homing
  • AE: lowers HR, infection, macular edema… Fetal risk
  • Notes: Additive effect w/ beta blockers to heart. Met by CYP4F2. Avoid live attenuated vaccines.
A

Fingolimod

S1P-R Agonist

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11
Q
  • Therapeutic Use: depletes T lymphocytes. Can be used with corticosteroids.
  • MOA: purified equine Ig against human thymus thymocytes.
  • AE: Hypersensitivity, Nephritis and anaphylaxis
A

Antithymocyte globulin

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12
Q
  • Therapeutic Use: acute kidney, hepatic, cardiac transplant rejection
  • MOA: binds CD3 glycoprotein on T lymphocytes (T cells cant recognize foreign Ag).
  • AE: Flu-like symptoms
A

Muromonab-CD3

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13
Q
  • Therapeutic Use: prevents renal transplant rejection.
  • MOA: Block IL-2 receptor on T lymphocytes.
  • AE:
  • Notes: Give with cyclosporine and orticosteroids.
A

Basiliximab

Daclizumab

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14
Q
  • Therapeutic Use: RA, Crohns
  • MOA: IV infused. anti-TNF-a mab (Chimeric IgG1).
  • AE: infusion reaction, Upper res and UTIs, rarely a SLE like symptom.
  • Notes: function improves with methotrexate or other DMARDs.
A

Infliximab

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15
Q
  • Therapeutic Use: RA, psoriatic arthritis, ankylosing spondylitis.
  • MOA: Given SC. contains ligand binding sequence of human TNF-a receptor fused to IgG1.
  • AE:
  • Notes: fully human IgG1 and anti-TNF –mab. Down regulates macrophage and T cell function.
A

Etanercept

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16
Q
  • Therapeutic Use: RA DMARD.
  • MOA: Inhibits AICAR and decreases PMN chemotaxis, lowers lymphocyte and macrophage function.
  • AE: Don’t use if PREGGERS. Nausea and mucosal ulcers. Must check for TB (macrophage dependent infection).
  • Notes: absorbed and hydroxylated in GI. Good for juvenile RA also. Should do a folic acid supplementation. Give with leucovorine.
A

Methotrexate

17
Q
  • Therapeutic Use: RA and juvenile chronic arthritis.
  • MOA: met by intestinal bacteria to a derivative of salicyclic acid. Decreases production of IgA and IgM
  • AE: Serious side effects.
A

Sulfasalazine

18
Q

• Therapeutic Use: Gout
• MOA: PO; competitive inhibition of xanthine oxidase. Metabolized to oxipurinol.
o Minor: depletes 5’-phosphoribosyl pyrophosphate and inhibits 5’-PRPP aminotransferase to reduce de novo purine synthesis.
• AE: Renal insufficiency hypersensitivity, GI, peripheral neuritis, necrotizing vasculitis, hepatic toxicity
• Notes: Not antagonized by salicyclates. Cyclophosphamide will increase toxicity. 1 tablet per day

A

Allopurinol

Inhibitors of Uric Acid Synthesis

19
Q
  • Therapeutic Use: Gout
  • MOA: PO; non-purine like, potent and selective inhibitor of xanthine oxidase.
  • AE:
  • Notes: Good for chronic gout or pt who cant take allopurinol. Liver metabolized and urine excreted. Use with colchicine or NSAIDs initially. No dosage adjustments required.
A

Febuxostat

Inhibitors of Uric Acid Synthesis

20
Q
  • Therapeutic Use: Uricosuric against gout.
  • MOA: PO; decrease renal active secretion of other compounds. Increase renal excretion of oxipurinol
  • AE: GI intolerance, dermatitis, nephrotic syndrome.
  • Notes: use for pt with allergic rxn to allopurinol with normal renal function. Can be given with colchicine prophylactically.
A

Probenecid

Uricosuric Agents

21
Q
  • Therapeutic Use: prophylactic, adjunct therapy to uricosurics and inhibitors of uric acid synthesis.
  • MOA: PO every 2 hours or IV. Prevents leukocyte migration and urate crystal phagocytosis. Liver deacetlyated.
  • AE:
  • Notes:
A

Colchicine

22
Q

• Therapeutic Use: use in hyperuricemia in peds cancer pt.
• MOA: IV; Catalyzes uric acid conversion to allantoin.
• AE: limited by SE; Ab production, acute renal failure, anaphylaxis, GI abnormalities.
Notes: produced by saccharomyces cerevisiae strain. Lowers urate levels better than allopurinol

A

Rasburicase

Pharm (19 decks)

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