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Pharm III Unit II > 5 DMARDs > Flashcards

5 DMARDs Flashcards

1
Q

What are the goals of therapy for chronic inflammatory diseases?

A 
Relief of pain
Reduction of inflammation
Protection of articulate structures
Maintenance of function
Control of systemic involvement
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2
Q

What are the different drug classes that can be used for the treatment of chronic inflammatory disease?

A

NSAIDs (cox-inhibitors)

Disease Modifying Anti-Rheumatic Drugs (DMARDs)
• Not analgesic and take time to work
• Various MOAs

Cortical steroids
• Inhibit AA release
•Inhibit immune response

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3
Q

How do Gold Salts work?

A

SUPPRESS CELLULAR IMMUNITY

  • Inhibition of phagocytosis
  • Uncouple oxidative phosphorylation and inhibit cellular respiration
  • Stabilize lysosomal membranes and inhibit actions of lysosomal enzymes
  • React with proteins (sulfhydryl groups)
  • Inhibit proteolytic enzymes of leukocytes
  • Prevent prostaglandin synthesis
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4
Q

Toxic effects of gold salts

A

BONE MARROW DAMAGE

Dermatitis

ENTEROCOLITIS

Jaundice

Peripheral neuropathy

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5
Q

Chelating drug that is effective in both rheumatoid arthritis and Wilson’s disease

A

Penicillamine

Exact mechanism unknown but somewhat resembles gold compounds and may be as effective as gold

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6
Q

What toxicities are possible with penicillamine

A

Pruritis, rash, alteration in taste

Thrombocytopenia, leukopenia, agranulocytosis, aplastic anemia

Proteinuria, hypoalbuminemia, Nephrotic Syndrome

Lupus-like disease, pemphigus, Goodpasture’s syndrom, myasthenia gravis, polymyositis, stenosis alveolitis

Patients over 65 have higher risks

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7
Q

Hydroxychloroquine (Plaquenil) possesses _______, ________, and _______ properties

A

Antihistaminic

Anticholinesterase

Antiprotease

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8
Q

MOA for hydroxychloroquine (Plaquenil)

A

Inhibits prostaglandin synthesis, biosynthesis of mucopolysaccharide, and responses to chemotactic stimuli and phagocytosis

Stabilizes lysosomes

Reacts with nucleic acids and tissue proteins

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9
Q

Hydroxychloroquine (Plaquenil) toxicities

A

Pruritis

Hemolysis (G6PD deficient)****

Ototoxicity

Retinopathy

Peripheral neuropathy

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10
Q

Prodrug that was originally used to treat inflammatory bowel disease but now used to RA

A

Sulfasalazine (Azulfidine)

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11
Q

How does sulfasalazine compare to gold salts and penicillamine?

A

Equi-effective with injectable gold compounds and is better tolerated

As effective as penicillamine and less toxic

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12
Q

Toxicities of sulfasalazine

A

GI disturbances, rash

Hepatitis and blood dyscrasias are rare

Monitor for hepatitis and marrow suppression is recommended for 2-3 weeks during first three months of treatment and less frequently thereafter

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13
Q

Chimeric IgG1k monoclonal antibody targeted against tumor necrosis factor alpha (TNFa)

A

Infliximab (Remicade)

Model agent of the class

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14
Q

What is the target of Infliximab (Remicade)

A

Chimeric IgG1k monoclonal antibody targeted against tumor necrosis factor alpha (TNFa)

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15
Q

Infliximab is composed of …

A

Human constant and murine variable regions (it’s chimeric)

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16
Q

How is Infliximab (Remicade) used?

A

Approved for Crohn’s disease and rheumatoid arthritis

Combined with methotrexate

Administered intravenously

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17
Q

Adverse reactions to infliximab (Remicade)

A

HA and infusion reactions

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18
Q

Contraindications for Infliximab (Remicade)

A

Pregnancy
Breast feeding
Children
Infections

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19
Q

Recombinant human IgG1 monoclonal antibody specific for tumor necrosis factor alpha (TNFa)

A

Adalimumab (Humira)

Has human-derived heavy and light chain variable regions and human IgG1:k constant regions (100% human peptide)

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20
Q

MOA for Adalimumab (Humira)

A

Recombinant human IgG1 monoclonal antibody specific for tumor necrosis factor alpha (TNFa)

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21
Q

Why does Adalimumab (Humira) not have hypersensitivity reactions like other DMARDs?

A

It’s not chimeric - it’s composed of 100% human peptide sequences)

22
Q

Which drug is formally FDA approved for monotherapy in the treatment of RA?

A

Adalimumab (Humira)

23
Q

How is Adalimumab (Humira) administered?

A

SQ, half-life about 8-10 days

24
Q

Most common adverse events reported by patients taking Adalimumab (Humira)

A 
Rash
Flu-like sx
Fatigue
HA
Pruritis
N/V

NO hypersensitivity reactions

25
Q

Humanized antibody that is a potent neutralizer of TNFa

A

Certrolizumab pergola (Cimiza)

26
Q

Human-derived monoclonal antibody with human-derived variable and constant regions TNFa

A

Golimumab

27
Q

Dimeric fusion protein produced by recombinant DNA technology and consisting of the extracellular ligand-binding portion of the human 75 kilo dalton (p75) tumor necrosis factor receptor

A

Etanercept (Enbrel)

28
Q

MOA for Etanercept (Enbrel)

A

Inhibits tumor necrosis factor by blocking its receptor

29
Q

Adverse effects of Etanercept (Enbrel)

A

Injection site reaction
Infections
Increased incidence of antibody formation

30
Q

Contraindications for Etanercept (Enbrel)

A 
Bone marrow suppression
Breast-feeding
Children
DM
Infection
Sepsis
Vaccination 
Varicella
31
Q

Chimeric murine/human monoclonal antibody that binds specifically to CD20, a B-lymphocyte differentiation antigen on pre-B and mature B-lymphocytes

A

Rituximab (Rituxan)

32
Q

MOA for Rituximab (Rituxan)

A

Chimeric murine/human monoclonal antibody that binds specifically to CD20, a B-lymphocyte differentiation antigen on pre-B and mature B-lymphocytes

33
Q

Where is the target of Rituximab (CD20) found?

A

Expressed on >90% of B-cell non-Hodgkin’s lymphoma but not on hematopoietic stem cells, pro-B cells, normal plasma cells, or other normal tissues

34
Q

How is Rituximab used?

A

For the treatment of relapsed or refractory B-cell NHL and is being studied in other B-cell malignancies, including chronic lymphocytic leukemia

35
Q

Fully human recombinant fusion protein categorized as a costimulatory or second-signal blocker of T cell activation

A

Abatacept (Orencia)

Competes with CD28 (on T cell) for CD80 and CD86 binding —> disturbs a key mechanisms of inflammation and progressive joint destruction in RA

36
Q

Inhibitor of dihydroorotate dehydrogenase (DHODH), an enzyme located in cell mitochondria that catalyze a key step in de novo pyramiding synthesis

A

Leflunomide (Arava)

37
Q

Secondary MOA for Leflunomide (Arava)

A

Inhibition of cytokines and growth factor receptor associated tyrosine kinase activity

Inhibits the induction of COX-2

38
Q

Contraindications for Leflunomide (Arava)

A

Pregnancy
Breast feeding
Hepatic failure
Renal failure

39
Q

Prodrug that inhibits lymphocyte purine synthesis by reversible and noncompetitively inhibiting the enzyme in Osi energy monophosphate dehydrogenase (IMPDH)

A

Mycophenolate mofetil (Cellcept)

40
Q

MOA for Mycophenolate mofetil (Cellcept)

A

Prodrug that inhibits lymphocyte purine synthesis by reversible and noncompetitively inhibiting the enzyme in Osi energy monophosphate dehydrogenase (IMPDH)

41
Q

What are the two Interleukin receptor antagonists we discussed?

A

Anakinra (Kineret)

Tocilizumab (Actemra)

42
Q

Recombinant, non-glycosylated form of the human interleukin-1 receptor antagonist (IL-1Ra)

A

Anakinra (Kineret)

43
Q

How is Anakinra (Kineret) used?

A

RA patients experienced improvements of swollen and painful joints within 4-13 weeks

44
Q

Contraindications for Anakinra (Kineret)

A

Breast feeding
Children
Hypersensitivity reactions
Renal disease

45
Q

Humanized interleukin-6 (IL-6) receptor-inhibiting monoclonal antibody

A

Tocilizumab (Actemra)

Competes with IL-6 for binding

46
Q

What drug is used to treat adults with moderate-severe RA who have an inadequate response or are intolerant to methotrexate?

A

Tofacitinib (Xeljanz) - a Janus kinase (JAKs) inhibitor

47
Q

MOA for Tofacitinib (Xeljanz)

A

Primarily inhibits JAK1 and JAK3 and to a lesser extent JAK2

48
Q

What is the major drawback of Tofacitinib (Xeljanz)?

A

Serious infections and malignancies may be precipitated by tofacitinib

49
Q

Oral Janus kinase (JAK) inhibitor with a greater affinity for JAK1 and JAK2 relative to JAK3

A

Baricitinib (Olumiant)

50
Q

Indications for Baricitinib (Olumiant)

A

Treatment of adult patients with moderate-severe active RA

May be used as a monotherapy or in combo with methotrexate or other non-biologic DMARDs

51
Q

What are the boxed warnings for Baricitinib (Olumiant)?

A

Risk for serious infections, malignancy, and thrombosis

Pharm III Unit II (8 decks)

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