MSK Exam 4 (Jin)

What are the 3 gold compound DMARDs?

- Aurothioglucose

- Auranofin

- Gold sodium thiomalate

MOA of gold compounds

Inhibit lysosomal enzymes (hydrolase) blocking the inflammatory response

Which gold compound should not be used in juvenile patients?

Auranofin

What gold compounds are given through IM injection?

- Gold sodium thiomalate

- Aurothioglucose

What gold compound is orally active?

Auranofin

What is this compound?

Aurothioglucose

What is this compound?

Auranofin

What is this compound?

Gold sodium thiomalate

ADEs of gold compounds

- Dermatitis

- Mouth lesions

- Pulmonary disorders

- Nephritis

- Hematologic disorders

DDI of gold compounds?

- Concurrent administration of drugs that produce blood dyscrasia (antimalarial and immunosuppressive drugs?

What is this compound?

Chloroquine

What is this compound?

Hydroxy Chloroquine

When would you expect to see benefit from the antimalarial agents for RA?

1-2 months

Severe ADE of Chloroquine?

Retinal damage (phytotoxicity)

- loss of visual acuity

- DC prompt when signs first appear

What are the antimalarials used for RA treatment?

- Chloroquine

- Hydroxy chloroquine

T/F Hydroxychloroquine is less toxic and more effective than chloroquine?

False

- it is less toxic and less effective

Immunosuppressant drugs are indicated in RA for patients who...?

- Severe active disease who have not responded to full dose NSAID and at least one DMARD and corticosteroid

What are the immunosuppressants used in RA treatment?

- Leflunomide

- Sulfasalazine

- Azathioprine

- Methotrexate

- Cyclophosphamide

What is this compound?

Leflunomide

What is this compound?

Sulfasalazine

What is this compound?

Azathioprine

MOA of Leflunomide?

- pyrimidine synthesis inhibitor

- anti-inflammatory and immunosuppressive

- pro-drug

- active metabolite: teriflunomide

- teratogenic

Active metabolite of Leflunomide?

Teriflunomide

Explain Azathioprine

- Purine analog

- Antimetabolite

- Teratogenic

Explain Sulfasalazine

- Broken down by intestinal bacteria into sulfapyridine and 5 amino salicylic acid

Explain Cyclophosphamide

- Cytotoxic agent used for refractory RA or life threatening RA

- Teratogenic

Explain Methotrexate

- Antifolate drug

- Severe active RA in adults who have had insufficient response to first line therapy

What is this compound?

Cyclophosphamide

What is this compound?

Methotrexate

- Etanercept

- Infliximab

- Adalimumab (Humira)

- Rituximab

Are examples of what type of RA drug?

- TNF a blockers

What is the best selling drug ever?

- Humira (adalimumab)

- Anakinra

- Tocilizumab

Are examples of what type of RA drug?

IL receptor antagonists

Gout is characterized by the elevated levels of _____ _____ in the plasma and urine?

Uric acid

Uric acid is formed by the oxidation of ___1___ by the enzyme __2____ ______

1. Xanthine

2. Xanthine oxidase

What is the primary treatment for acute gout?

- Colchicine

Explain Colchicine

- Natural product

- Does not alter serum levels

- Slows the inflammation process initiated by the deposition of urate crystal

What is this compound?

Colchicine

What is this compound?

Probenecid

What is this compound?

Sulfinpyrazone

What drugs increase uric acid secretion?

- Probenecid

- Sulfinpyrazone

Explain Probenecid

- Promote excretion of uric acid by inhibiting urate anion exchange transporter by decreasing the reabsorption of uric acid

- Does not help with acute attack

- Antagonized by salicylates

Explain Sulfinpyrazone

- Increases uric acid secretion

- Antagonized by salicylates

- Similar to probenecid

What gout medications decrease uric acid formation?

- Allopurinol

- Febuxostat

Explain Allopurinol

- Drug of choice for chronic gouty arthritis

- Can't terminate acute attack once it has begun

- Inhibitor of xanthine oxidase

- Salicylates do not interfere with its action

Explain Febuxostat

- 1st nonprime selective xanthine oxidase inhibitor

What is this compound?

Allopurinol

What is this compound?

Febuxostat

What gout drug enhance degradation of uric acid?

Pegloticase

Explain Pegloticase

- Enhances uric acid degradation by converting it into a more excretable metabolite

- Tetrameric protein biologics