DMARDs study guide answers- Khan

Properties of DMARDs

• effect on disease progression?

• effect on immune response?

• Toxic?

• Diversity?

Properties of DMARDs

• effect on disease progression?

• effect on immune response?

• Toxic?

• Diversity?

• impede disease progression

• decrease immune response

• high incidence of toxicity

• very diverse class of meds

MOA of MTX

• inhibits folate synthesis

  • specifically inhibits dihydrofolate reductase= decreased folate

Boxed warning of MTX

• GI: mucositis, stomatitis

• Hepatotoxicity

• Myelosuppression

• Teratogenic

Why folate supplementation with MTX?

Reduces hematological and liver toxicity

Where is sulfasalazine activated?

colon

Chloroquine ADRs

• RETINOPATHY

• skin discoloration

Active moiety of Sulfasalazine

5-ASA (5-amino salicylic acid)

Contraindications of Sulfasalazine

sulfa and salicylate allergy

MOA of leflunomide

action is due to an active metabolite (teriflunomide)

• active metabolite formed in the liver and plasma

• inhibits dihydrorotate dehydrogenase (DHODH)

• basically we inhibiting pyrimidine synthesis

KNOW THE NAME OF THE ENZYME

Boxed warnings of leflunomide

• elevated liver enzymes

• must rule out pregnancy

Contraindications of leflunomide

• PREGNANCY

Leflunomide drug elimination methods

• activated charcoal

• chloestyramine

Boxed warnings for TNF Blockers

Increased risk of:

• serious infections

• TB

• Lymphoma (cancer)

Boxed Warning for Tocilizumab (actemra)

SERIOUS INFECTIONS

Boxed Warning for Anakinra (kineret)

• serious infections

• malignancies

Rituximab MOA

Humanized mab binds to CD20 antigen on surface of B-lympocytes

RItuximab Boxed warnings

• infusion-associated symptom complex with the first infusion

• progressive multifocal encephalopathy

• serious skin reactions

• HBV activation

TNF Blocker individual properties (ex: what type of antibody)

• Golimumab

• Recombinant human anti-TNF monoclonal antibody

TNF Blocker individual properties (ex: what type of antibody/protein )

• Infliximab

• Chimeric Antibody (25% mouse, 75% human)

TNF Blocker individual properties (ex: what type of antibody/protein )

• Adalimumab

• Recombinant human anti-TNF monoclonal antibody

TNF Blocker individual properties (ex: what type of antibody/protein)

• Etanercept

• Recombinant Fusion Protein

TNF Blocker individual properties (ex: what type of antibody)

• Certolizumab Pegol

• PEG attached to antibody

Name the prodrugs in treating RA

• leflunomide

• Sulfasalazine

Compare the MOA of tocilizumab versus ankinra

• tocilizumab- humanized Ab against IL-6 receptors

• anakinra- IL-1 receptor antagonist, protein not Ab

TNF blocker but not antibody

• Etanercept