USMLE (Fach) / Pharmacology - Musculoskeletal, Skin, Connective Tissue (Lektion)

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  • Acetaminophen Reversibly inhibits cyclooxygenase, mostly in CNS.- inactivated peripherally Clinical use:- antipyretic- analgesic- not anti-inflammatory- used instead of aspirin to avoid Reye syndrome in children with ...
  • Aspirin NSAID that irreversibly inhibits COX-1 and COX-2 by covalent acetylation → ↓ synthesis of TXA2 and prostaglandins.COX-1 is expressed in most tissues and regulates normal cellular processes (eg, gastric ...
  • Celecoxib Reversibly and selectively inhibits COX-2, which is found in inflammatory cells and vascular endothelium and mediates inflammation and pain.- spares COX-1, which helps maintain gastric mucosa→ less ...
  • NSAIDs - Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac, meloxicam, piroxicam - Reversibly inhibit COX-1 and COX-2. Block prostaglandin synthesis Clinical use:- antipyretic- analgesic- anti-inflammatory- ...
  • Leflunomide Reversibly inhibits dihydroorotate dehydrogenase, preventing pyrimidine synthesis.- Suppresses T-cell proliferation Clinical use:- Rheumatoid arthritis- Psoriatic arthritis Adverse effects:- Diarrhea- ...
  • Bisphosphonates Alendronate, ibandronate, risedronate, zoledronate Pyrophosphate analogs. Bind hydroxyapatite in bone, inhibiting osteoclast activity.Osteoclasts that reabsorb the bone take up the bisphosphanate and ...
  • Teriparatide Recombinant PTH analog given subcutaneously daily. - ↑ osteoblastic activity when administered in pulsatile fashion. Clinical use:- Osteoporosis- Causes ↑ bone growth compared to antiresorptive ...
  • Allopurinol Chronic gout drug (preventive). Competitive inhibitor of xanthine oxidase → ↓ conversion of hypoxanthine and xanthine to urate. - Also used in lymphoma and leukemia to prevent tumor lysis-associated ...
  • Febuxostat Chronic gout drug (preventive). Inhibits xanthine oxidase.
  • Pegloticase Chronic gout drug (preventive). Recombinant uricase that catalyzes metabolism of uric acid to allantoin (a more water-soluble product).
  • Probenecid Chronic gout drug (preventive). Inhibits reabsorption of uric acid in proximal convoluted tubule (also inhibits secretion of penicillin). - Can precipitate uric acid calculi.
  • Colchicine Binds and stabilizes tubulin to inhibit microtubule polymerization, impairing neutrophil chemotaxis and degranulation. Acute and prophylactic value for gout. Adverse effects:- GI side effects- Neuromyopathic ...
  • Etanercept Fusion protein (decoy receptor for TNF-α + IgG Fc) produced by recombinant DNA. Clinical use:- Rheumatoid arthritis- Psoriasis- Ankylosing spondylitis Adverse effects: Predisposition to infection, ...
  • Infliximab, adalimumab, certolizumab, golimumab Anti-TNF-α monoclonal antibody  Clinical use:- Inflammatory bowel disease- Rheumatoid arthritis- Ankylosing spondylitis- Psoriasis Adverse effects: Predisposition to infection, including reactivation ...
  • Rasburicase - Recombinant uricase that catalyzes metabolism of uric acid to allantoin - prevention and treatment of tumor lysis syndrome
  • Cyclosporine and tacrolimus - ↓ calcineurin --> ↓ activation of T-cell transcription factors --> ↓ IL-2, IL-3, and interferon-γ Uses:- Cyclosporine is DOC for organ and tissue transplantation- Tacrolimus used alternatively ...
  • Mycophenolate - inhibitor of de novo synthesis of purines - has adjunctive immunosuppressant actions - permits dose reductions of cyclosporin to limit toxicity
  • Azathioprine - immunosuppressant converted to 6-mercaptopurine Side effects:- bone marrow suppression
  • Trastuzumab - antagonist to ERB-B2 (Her 2) Use:- breast cancer
  • Interferon-α - Hepatitis B and C - Leukemias - Melanoma
  • Interferon-β Use: Multiple sclerosis
  • Interferon-γ Chronic granulomatous disease --> ↑ TNF
  • Muromonab - suppresses T-cell proliferation Use: kidney transplant
  • Arachidonic acid pathway Leukotriens:- LTC4, LTD4, LTE4: ↑ bronchial tone- LTB4: ↑ Neutrophil chemotaxis Prostacyclin:- PGI2: ↓ platelet aggregation, ↓ vascular tone (Epoprostenol) Prosaglandins:- PGE1: ↓ vascular ...
  • Nonsteroidal anti-inflammatory drugs Ibuprofen, naproxen, indomethacin, ketorolac, diclofenac, meloxicam, piroxicam Reversibly inhibit cyclooxygenase (both COX-1 and COX-2). Block prostaglandin synthesis. Clinical use: Antipyretic, analgesic, ...
  • Calcipotriene Topical vitamin D analog Causes inhibition of keratinocyte proliferationa nd stimulation of keratinocyte differentiation. Can be used in psoriasis.
  • Retinoids Main substance: isotretinoin (Vitamin A derivative) given systemically Indication: in moderate to severe acne Mechanism of action: Retinoids normalize keratinization by inhibiting and modulating keratinocytes ...
  • Methotrexate Folic acid antagonist (antimetabolite) → purine nucleotide and thereby ↓ DNA synthesis Clinical use:- Treatment of severe psoriasis and rheumatoid arthritis- In neoplastic diseases like gestational ...
  • Hydroxychloroquine TNF & IL-1 suppressor Side effects:- Retinopathy

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