1 Steroidal anti-inflammatory agents

Terminology

Rheumatoid arthritis (RA): Autoimune disease. dysregulation of pro-inflammatory cytokines, including TNF-α ,IL-1 → inflamation. Treatment NSAID, SAID

DMARD known: synthetic DMARDs , biological DMARDs and JAK-i

Addison's Disease:

Hypercortisolism(Cushing's disease ):

Crohn's disease:

ulcerative colitis:

Cushing's Syndrome:

glucocorticoid therapy:

Cyclooxygenases (COX):

Thromboxane (TXA2):

ALL NSAID are COX inhibitors

Hydrocortisone

Steroidal anti-inflammatory drug,Glucocorticoid receptor agonists, short acting

IND: Acute and chronic cortex adrenal insufficiency (hormonal replacement)

Prednisolone, Methylprednisolone Dexamethasone

Steroidal anti-inflammatory drug, Glucocorticoid receptor agonists, medium long acting

1 fastmembrane stabilizing effects (lysosomal, mast cell stabilization)
2. Slow, genomic effects, intracellular corticosteroid receptor activation

Anti-inflammatory, anti-edema, anti-allergic, anti-shock, immunosuppressive, antiproliferative effect

IND: Autoimmune diseases (RA), Inflammatory Bowel Disease (Crohn's disease),Transplantology, Allergy (anaphylactic shock, bronchial asthma)

Fludrocortisone

affecting the adrenal cortex, , , Long acting

SAID → Mineralocorticoid receptor agonists → water retention

Fluorinated hydrocortisone derivative, Aldosterone receptor agonist in distal renal tubules and collecting ducts DNA transcription, promotes expression of epithelial Na + channels, increases Na + reabsorption and water retention, → ↑ BP, promotes K + excretion

IND: mineralocotricoid substitution, Replacement therapy for Addison's disease

Side effect: hypertension, oedema, hypokalemia

Acetylsalicylic acid (aspirin)

NSAID, Non-selective inhibition of COX1 / COX2 (dose dependent)

1. Inhibition of COX2: Anti-inflammatory, inhibition of prostaglandin synthesis Anti-inflammatory, analgesic and antipyretic effects (medium high dose)
2. Inhibition of COX1 - irreversible ,antiplatelet effect

IND: mild/moderate acute pain

SE: gout, ulcer, bleeding, thrombosis, gastrointestinal bleeding

Contraindication: children under 12 with fever

(170x more potent on COX-1)

Diclofenac Ibuprofen

NSAID, analgesic, antipyretic, anti-inflammatory action

IND: Pain, Muscuskeletal disorders

Inhibiti: COX1/COX2, prostaglandin synthesis,

SE: prothrombotic Cardiovascular risk

Diclofenac: most anti-inflammatory

Etoricoxib

NSAID, Selective inhibition of COX2 → inhibition of prostaglandin synthesis,analgesic, antipyretic, anti-inflammatory action

IND: Musculoskeletal disorders (rheumatoid arthritis, osteoarthritis), acute pain

Interaction: increased risk of bleeding with systemic GC, anti platelets and anticoagulants; reduces the antihypertensive effect of ACE-I

SE: prothrombotic Cardiovascular risk, but at the same time less risk of bleeding

Allopurinol

xanthine oxidase inhibitor, block uric acid production

IND: Gout

Uricostatic effect

prodrug metabolized to alloxanthine →
1. Alloxanthine - irreversible xanthine oxidase inhibitor, inhibition of hypoxanthine / xanthine oxidation → blockade of uric acid synthesis
2. Inhibition of purine synthesis

Febuxostat

metabolism of uric acid, Reversible, Selective, xanthine oxidase inhibitor of non-purine origin, Uricostatic effect

IND: ➢ Chronic hyperuricemia in gout patients, Prevention of complications of chemotherapy