Pharm rheum review

  1. Partial agonist/antagonist at Alpha 1 and Serotonin receptors.
    Vasoconstriction. Vasoconstriction early in migraine is useful.
    Uterine contraction: used postpartum to control bleeding.
    Diagnosis of variant angina, finds reactive coronary segments.
    Ergotamine, Ergonovine
, Dihydroergotamine
  2. Ergotamine, Ergonovine
, Dihydroergotamine Toxicity
    Vasospasm can be intense and prolonged. Nausea, vomiting, diarrhea
  3. Nesiritide
    BNP analog used to improve renal sodium excretion and kidney function in severe heart failure. May cause fatal renal damage
  4. Bimatoprost
    new drug treating glaucoma that binds PGF2alpha receptor. Least toxic in this class
  5. Travoprost
    new drug that works at PGF2alpha receptors. Treats glaucoma
  6. Unoprostone
    Original PGF2alpha. Treats glaucoma
  7. Bind or block CD20, CD28 or CD80 receptors on T-Cell, B-Cell and APC Cell
    Anti RA. Rituximab, Abatacept
  8. causes vasoconstriction used to treat migraine. Can be used as anxiolytic, long onset and duration.
    5-HT1 agonist. Buspirone.
  9. blocks T and B-Cell proliferation. inhibits purine synthesis. not Azathioprine
    Mycophenolate mofetil
  10. initiates a complement reaction which stimulates phagocytosis
    Anti-Thymocyte Globulin
  11. binds IL-2 receptors on activated T-Cells.
  12. Ocular Side Effects of Latanoprost
    • Redness, Irritation, Exacerbation of herpes simplex keratitis
    • Inflammation, Change of periocular skin color, Permanently change iris color from blue to green or brown.
    • Increased length and number of lashes
  13. combined with misoprostol to induce labor.
  14. Used to treat rheumatic fever and Kawasaki dz
    Aspirin (ASA)
  15. increases hypothalamus set point – hyperthermia, fever.
  16. “Displacement reactions” –warfarin, heparin, phenytoin and sulfonylureas.
    Decreases clearance of methotrexate ~severe toxicity.
    Phenobarbital induces its metabolism.
    Antacids decrease its absorption.
    Alcohol/corticosteroids will increase its GI effects.
    ASA (aspirin)
  17. Diclofenac
    nonselective COX inhibitor. Phenylacetic acid derivative
  18. Phenylacetic acid derivative; COX-1=COX-2GI ulceration is less frequent; especially in combination with omeprazole or misoprostol. Highest incidence for renal effects (impair blood flow and glomerular filtration rate). Opthalmic preparation for postoperative opthalamic inflammation. Topical gel for solar keratoses. Rectal suppository: postoperative nausea.
  19. Nonselective COX inhibitor
    Derived from salicylic acid but not metabolized to salicylic acid or salicylate. Enterohepatic circulation, with reabsorption of its glucuronide metabolite. Cleavage of glucuronide will release the active moiety. RA treatmt. Effective for dental pain (third molar extraction).
  20. Propionic acid derivative; COX-1=COX-2. Reduction of tumor necrosis factor alpha (TNFα). Extensive hepatic metabolism but no enterohepatic circulation. Opthalmic preparation (stops intraoperative miosis). IV. Gynecologic. Rarely causes ataxia, tremor, and cogwheel rigidity (Parkinson-like effect)
  21. Phenylpropionic acid derivative; COX-1=COX-2. Closes ductus arteriosus in preterm infants. Effective in reducing fever in children > 102°. Antagonizes platelet inhibition when given concurrently with lo-dose aspirin. Holds true for most NSAIDS.
  22. Propionic acid derivative; nonselective COX inhibitor and lipoxygenase. However, not superior to any other NSAID. Probenecid elevates its levels and t1/2. Produces fluid retention.
  23. Has NSAID properties but used mainly as an analgesic. May replace morphine in certain situations of postsurgical pain. Can decrease opioid requirement. IM, IV, po, and opthalmic. Renal toxicity (limit to 7 day use).
  24. Osteoarthritis, RA, and acute painInhibits COX-2 > COX-1, thus producing less GI effects than other NSAIDs. Rash
  25. Only nonacid NSAID; converted to acetic acid, prodrugt1/2 24h; daily dosing; renal impairment doubles t ½. Less damage to GI. High doses needed; expensive. Photosensitivity
  26. Naphthylpropionic acid derivative. SR formula, oral suspension, topical, and opthalmic formulas. Rare cases of allergic pneuminitis, leukocytoclastic vasculitis, and pseudoporphyria reported. COX-1=COX-2
  27. Propionic acid derivative; very long t1/2 (60 h). Daily dosing. Lowers serum uric acid; great for GOUT.
  28. Oxicam; at high conc inhibits PMN leukocyte migration, decr O2 radical production, and inhibits lymphocyte function. Long t ½ (daily dosing)
    Very high risk of GI bleed at high dose, especially in the elderly. COX-1>COX-2
  29. Sulfoxide prodrug; enterohepatic cycling. An active sulfide metabolite is excreted in bile and reabsorbed. Prolongs duration of action. Suppresses familial intestinal polyposis- inhibits colon cancer development. Steven Johnsons Syndrome, agranulocytosis, and nephrotic syndrome. May elevate aminotransferases
  30. Have more adverse effects than NSAIDs w/o any superiority, inaddition to more GI effects. Diarrhea, Decr in hematocrit or Hb can occur w/ meclofenamic acid.
    Meclofenamic acid -for primary dysmenorrhea but therapy should not go past one week.
    Meclofenamate sodium- RA and osteoarthritis
    Fenamate-type drugs
  31. For primary dysmenorrhea but therapy should not go past 1 week. Fenamate type drugs. NSAID
    Meclofenamic acid
  32. treats RA & osteoarthritis. NSAID. Fenamate type drugs.
    Meclofenamate sodium
  33. NSAID w/ greatest toxicity
  34. NSAID w/ high GI & renal effects
  35. NSAID w/ higher liver fxn test abnormalities
    Diclofenac and sulindac
  36. Related to piroxicam in structure. Considered “preferentially” COX-2 selective rather than “highly”selective like celecoxib. Approved for osteoarthritis in the U.S.
  37. effects of cortisol deficiency
    impairs renal function (glomerular filtration), enhances vasopressin secretion, and diminishes ability to excrete water
  38. Use of corticosteroids in neoplastic dz
    Strong antiemetic
  39. corticosteroid most commonly leading to withdrawal
    dexamethasone (long acting)
  40. Lymphoma risk is incr in which RA med?
  41. hydroxychloroquine adverse effects
    ocular toxicity, GI upset, rashes. Relatively safe in pregnancy
  42. adverse effects of cyclophosphamides
    • severe bone marrow suppression, cystitis (administer fluids or Mesna).
    • Mesna- neutralizes acrolein a metabolite of cyclophosphamide --> enhance urinary excretion
    • decreasing cystitis.
  43. adverse effects of cyclosporine
    nephrotoxicity, hypertension, hyperkalemia, hepatotoxicity, hirsutism, and gingival hyperplasia
  44. Sulfasalazine MOA (anti RA)
    metabolized to sulfapyridine and 5-aminosalicylic acid which decrease IgA and IgM rheumatoid factor. Inhibits IL-1, TNF α, and NF-ĸβ which reduces radiologic disease progression
  45. Sulfasalazine adverse effects
    Nausea, vomiting, headache, rash, methemoglobinemia and hemolytic anemia, Steven-Johnson’s syndrome (rare). Decr effects of penicillin.
  46. inhibits dihydroorotate dehydrogenase, leading to a decrease in ribonucleotide synthesis and arrest at the G1 phase. “Pyrimidine
    synthesis inhibitor”. Inhibits T-cell proliferation and production of autoantibodies by B cells. Decreases TNF-α-dependent NF-ĸβ activation.
    Leflunomide MOA. Anti RA
  47. adverse effects of Leflunomide
    diarrhea, elevated liver enzymes, alopecia, weight gain, increased BP. Teragenic in pregnancy. Cholestyramine reduces drug's absorption
  48. Abatacept
    T cell modulating drug for early RA
  49. Rituximab
    B cell cytotoxic agent for early RA
  50. Infliximab Adverse Effects
    URT infections, Lupus like syndrome, Not recommended for MS pt (rare demyelination), Screen for latent TB (induces potent mac inhibition). Infusion site rxns- prevented by antihistamines and H2 blockers. Lymphoma incidence unclear (monitor)
  51. Adverse effects of Adalimumab
    Injection site rxns; rare leukopenias and vasculitits. Incidence of lymphoma not clear (but monitor). Has warning label concerning infections & TB
  52. adverse effects of Entanercept
    sepsis/infection (deadly), injection site pain, allergies, abdominal pain, screen for Tb; lymphoma unclear but monitor
  53. adverse effects of Abatacept
    increased risk of infections, rare anaphylaxis, and possible increase in lymphomas. Do not administer with anti-TNF may increase incidence of infections.
  54. adverse effects of Rituximab
    rashes (rarely anaphylactic), viral infections.
  55. Tricyclic Antidepressants (TCA): Imipramine NE, 5-HT, Amitriptyline NE, 5-HT
    Reversible block of NE and 5-HT presynaptic reuptake
  56. side effects of tricyclic antidepressants
    Sedative (drowsiness), Antimuscarinic (dry mouth), Alpha-adrenergic block (low BP)
  57. Phenelzine (irreversible) & Tranylcypromine (reversible)
    MAO-A metabolism of Norepinephrine (NE), Serotonin (5-HT) and Tyramine. MAO-A Inhibitors treat depression. Also blocks MAO-B.
  58. Selegiline & Rasagiline
    MOA-B prefers to deaminate Dopamine.MOA-B Inhibitors treat Parkinsonism
  59. Side effects of Phenelzine & Tranylcypromine
    Headache, Dry mouth (anticholinergic)
  60. side effects of Selegiline and Rasagiline
    dry mouth, dizziness
  61. Fluoxetine (Prozac), Paroxetine (Paxil), Sertraline (Zoloft), Citalopram (Celexa)
    selective serotonin reuptake inhibitors
  62. side effects of SSRI's
    Drowsiness, vivid and strange dreams, suicide ideation.
  63. 5-HT2 antagonist (also H1 and M3 antagonist)
  64. DA-2 antagonist (also H1, M3, 5-HT2, Alpha-1 block)
  65. Usefulness: Allergic rxns, Hay fever, Nightmares, Serotonin Syndrome, Carcinoid
    Side Effects: Dizziness, Drowsiness (H1), Blurred vision, Constipation, Dry mouth (M3)
  66. Usefulness: Antipsychotic (DA antagonist), Schizophrenia, Manic phase bipolar disorder, Severe N/V (anticholinergic)
    Side Effects: Constipation, sedation, dry mouth, urinary retention (anti-Ach), Hypotension (Alpha-1 antagonist), Akathisia, dystonia, tardive dyskinesia (DA antagonist)
    Chlorpromazine, Thorazine
  67. Structural pre-Prozac (fluoxetine)
    Diphenhydrinate (benedryl)
  68. Blocks T-cell proliferation. Acts downstream of IL-2 receptor. Inhibits cell cycle at the G1 to S Phase
    Toxicity: Hyperlipidemia, Anemia, Potentiates cyclosporine nephrotox.
    Sirolimus (Rapamycin)
  69. Blocks T and B Cell proliferation. Blocks purine synthesis and salvage pathways needed for replication. 6-MP
  70. Toxic for rapid growth cells, Leukopenia Thrombocytopenia, GI Ulceration, Hepatotoxicity, Risk of infection
    Reduce dose w/ allopurinol (inhibits xanthine oxidase, metabolism of 6-MP)
    Azothioprine side effects
  71. Blocks T and B Cell proliferation.Inhibits de novo purine synthesis
    Toxicity: Same as Azothioprine, minus allopurinol drug-drug interaction. No 6-MP
    Mycophenolate Mofetil
  72. GI: mucositis, stomatitis, N/V, diarrhea
    Blood: 7-10 days following dose, leukopenia and thrombocytopenia with recovery at 2 weeks. Possible pancytopenia at 2 weeks.
    Liver: Mild to mod. Hepatits
    CNS: Intrathecal admin. – seizures
    Pregnancy: Embryotoxic, teratogenic
    Renal toxicity
    Methotrexate toxicity
  73. Alkylating agent that blocks DNA replication. Toxicity: Same as Azothioprine, minus allopurinol drug-drug interaction. No 6-MP. Leukopenia, thrombocytopenia, liver toxicity, infection, ulceration
  74. Destruction of lymphocytes by complement activation and phagocytosis.
    Toxicity: Fever, Hypotension, Type III hypersensitivity reaction
    Anti-Thymocyte Globulin (ATG)
  75. Ab that Binds to IL-2 receptors on activated T-cells
    Toxicity: Potential for anaphylactoid reactions
    Daclizumab and Basiliximab
Card Set
Pharm rheum review
Pharm rheum review