IPS2: Pharmacology - Part 6.3.3 - Drugs for Rheumatologic Disorder - DMARDs, Glucocorticoids

DMARDS except:

a. Disease-modifying Antirheumatic Drugs

b. Slow-acting Antirheumatic Drugs

c.Chemically diverse agents

d. Do not just take away the pain, they can instead alter or even reverse disease progression

e. Full effects: 6-12 months

f. None

f. None

DMARDs can be

a. Nonbiologic or the small molecule drugs

b. Biologic or the large molecule drugs

c. Both

d. None

c. Both

Recombinant DMARDs.

a. Nonbiologic

b. Biologic

c. Both

d. None

b. Biologic

Nonbiologic DMARDs except:

a. Methotrexate

b. Antimalarials

c. Gold Compounds

d. Sulfasazaline

e. Leflunomide

f. None

f. None

Nonbiologic DMARD:

1st line DMARD

a. Methotrexate

b. Antimalarials

c. Gold Compounds

d. Sulfasazaline

e. Leflunomide

a. Methotrexate

True about Methotrexate except:

a. Inhibition of AICAR transformylase = ↑ AMP = ↑ release of Adenosine

b. Inhibition of Thymidylate synthetase = ↑ AMP = ↑ release of Adenosine

c. ↑ release of Adenosine: Inhibition of Inflammation

d. Only low dose must be administered.

e. Higher doses induce anti-cancer effect and hepatotoxic

f. None

f. None

Nonbiologic DMARD:

2nd line DMARDs.

a. Methotrexate

b. Antimalarials

c. Gold Compounds

d. Sulfasazaline

e. Leflunomide

b. Antimalarials

MOA of antimalarials such as Hydroxychloroquine & Chloroquine.

a. Inhibit T-lymphocytes responses to mitogens

b. Inhibit movement of inflammatory cells (Chemotaxis)

c. Inhibit DNA & RNA synthesis

d. a and b

e. b and c

f. All

f. All

Toxic effect/s of antimalarials.

a. Optic neuritis

b. Cinchonism

c. Both

d. None

c. Both

Nonbiologic DMARD:

No longer recommended due to significant toxicities as well as questionable efficacy.

a. Methotrexate

b. Antimalarials

c. Gold Compounds

d. Sulfasazaline

e. Leflunomide

c. Gold Compounds

Gold Compounds.

a. Aurothiomalate

b. Aurothioglucose

c. Auranofin

d. a and b

e. b and c

f. All

f. All

Parenteral Gold Compounds.

a. Aurothiomalate

b. Aurothioglucose

c. Auranofin

d. a and b

e. b and c

f. All

d. a and b

Oral Gold Compounds.

a. Aurothiomalate

b. Aurothioglucose

c. Auranofin

d. a and b

e. b and c

f. All

c. Auranofin

Gold compounds toxicity

a. Nephrotic syndrome

b. Hypersensitivity

c. Both

d. None

Metabolite/s of Sulfasazaline.

a. Sulfapyridine

b. 5-aminosalicylate

c. Both

d. None

c. Both

Metabolite of Sulfasazaline postulated to be active as a DMARD.

a. Sulfapyridine

b. 5-aminosalicylate

c. Both

d. None

a. Sulfapyridine

Also known as mesalamine which is applicable to patients with inflammatory bowel disease.

a. Sulfapyridine

b. 5-aminosalicylate

c. Both

d. None

b. 5-aminosalicylate

Toxicities of sulfasalazine.

a. Nausea & Vomiting

b. Skin rashes and discoloration

c. Hemolytic anemia

d. a and b

e. a and c

f. All

f. All

Nonbiologic DMARD:

Prodrug metabolized to A77-1726.

a. Methotrexate

b. Antimalarials

c. Gold Compounds

d. Sulfasazaline

e. Leflunomide

e. Leflunomide

Nonbiologic DMARD:

Inhibits dihydroorotate dehydrogenase inhibiting ribonucleotide synthesis resulting to arrest of cell cycle.

a. Methotrexate

b. Antimalarials

c. Gold Compounds

d. Sulfasazaline

e. Leflunomide

e. Leflunomide

Biologic DMARD

a. Large molecule drugs

b. Recombinant DNA technology

c. Both

d. None

c. Both

Biologic DMARDS except:

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

f. None

f. None

Biologic DMARDS:

T-cell modulating biologic; Inhibits activation of T-cells

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

a. Abatacept

Biologic DMARDS:

Used as monotherapy or in combination with methotrexate in patient with rheumatoid arthritis.

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

a. Abatacept

Biologic DMARDS:

1) B-cell depleting agent; targets CD20 B-lymphocytes = reduced inflammation

2) Combined with Methotrexate

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

b. Rituximab

Biologic DMARDS:

Inhibits IL-6-mediated signalling.

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

c. Tocilizumab

Biologic DMARDS:

Used for moderate or severe rheumatoid arthritis (RA).

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

c. Tocilizumab

Biologic DMARDS:

1) IL-1 Neutralizing Agent

2) Recommended for RA, but less effective compared to other biologics

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

d. Anakinra

Route of Anakinra

a. SC

b. ID

c. IV

d. IM

a. SC

Adverse effects of anakinra.

a. Severe infection

b. Irritation at the site of injection

c. Both

d. None

c. Both

TNF-alpha Blockers except:

a. Infliximab

b. Certolizumab

c. Adalimumab

d. Golimumab

e. Etanercept

f. None

f. None

Biologic DMARDS:

1) Inhibit 5-TNF-alpha → Inhibit inflammation → Inhibits symptoms associated with different rheumatologic diseases like RA

2) Adverse effect is severe infection

a. Abatacept

b. Rituximab

c. Tocilizumab

d. Anakinra

e. TNF-alpha Blockers

e. TNF-alpha Blockers

Glucocorticoids can be used for.

a. Respiratory disease

b. Rheumatologic disease

c. Endocrine disorder

d. a and b

e. b and c

f. All

f. All

Glucocorticoids.

a. Administered PO (Systemic)

b. Administered IV (Systemic)

c. Administered Intrasynovial (Local)

d. a and b

e. b and c

f. All

f. All

Used in management of Rheumatoid Arthritis and Systemic Lupus Erythematosus

a. Glucocorticoids administered PO (Systemic)

b. Glucocorticoids administered IV (Systemic)

c. Glucocorticoids administered Intrasynovial (Local)

d. a and b

e. b and c

f. All

d. a and b

Particular for patients who have Life-threatening SLE.

a. Pulse therapy of Methylprednisolone (500mg IV for 5 days) - Intermittently

b. Pulse therapy of Methylprednisolone (1000mg IV for 3 days) - Intermittently

c. Pulse therapy of Methylprednisolone (300mg IV for 3 days) - Intermittently

d. Pulse therapy of Methylprednisolone (1000mg IV for 10 days) - Intermittently

b. Pulse therapy of Methylprednisolone (1000mg IV for 3 days)

Glucocorticoids.

Used in management of osteoarthritis (OA) that is unrelieved with 1 st line agents like NSAIDs or analgesics.

a. Glucocorticoids administered PO (Systemic)

b. Glucocorticoids administered IV (Systemic)

c. Glucocorticoids administered Intrasynovial (Local)

d. a and b

e. b and c

f. All

c. Glucocorticoids administered Intrasynovial (Local)

Given every 4-6 months only, to prevent joint destruction.

a. Glucocorticoids administered PO (Systemic)

b. Glucocorticoids administered IV (Systemic)

c. Glucocorticoids administered Intrasynovial (Local)

d. a and b

e. b and c

f. All

c. Glucocorticoids administered Intrasynovial (Local)