Anti-inflammatory drugs Flashcards

Question

Give an example of COX 2 preferential?

Answer 1

EP4 receptor inhibitor

Answer 2

Need to be below IC20 for COX-1 and above IC80 for COX-2 Need to look at dynamics and kinetics

Answer 3

Depedns on drug Some have free radicals scavanging activity Aspirin inhibits NFkB- transcription factor for inflammatory mediator genes--->long acting inhibition of platelet function (used to prevent thrombosis

Answer 4

Selctive for COX enzymes in the CNS- postulated different isoform Analgesic of choice in infants Toxic to cats

Answer 5

Mechanism of action: aspirin irreversibly inhibits COX 1 in platelets, preventing production of Thromboxane A2 (TXA2) (promotor platelet aggregation) Inhibits COX 1&2 in endoth cells, reducing PGI2, which inhibits platelet aggregation and promotes vasodilation Platelets lack nucleus: so cannot synthesize new COX 1 enzymes Inhibition lasts the entire life span of the platelet Endotheial cells can regenerate COX as they have a nucleus

Answer 6

Vasodilation and increase vascular permeability effects

Answer 7

Targeted vs. Broad inhibition: Its selective EP4 receptor antagonist meaning it only blocks the PGE2 EP4 receptor Traditional NSAIDs (e.g., carprofen, meloxicam, ibuprofen) inhibit COX enzymes, reducing the production of all prostanoids, including PGE₂, prostacyclin (PGI₂), and thromboxane A₂ (TXA₂). Safety profile: Grapiprant is generally safer than NSAIDs because it does not inhibit COX, sparing prostaglandins that help maintain gastrointestinal, renal, and platelet function. NSAIDs, due to their broad inhibition of prostanoids, are more likely to cause gastric ulcers, kidney damage, and bleeding risks. NSAIDs may be more effective for inflammation since they block multiple eicosanoids, reducing pain, swelling, and fever. Effectiveness for Inflammation and Pain Grapiprant is highly effective for pain relief but may be less effective for severe inflammation, as it only targets EP₄-mediated PGE₂ effects.

Answer 8

They are used to treat type I hypersensitivity reactions, such as hay fever and insect bites, but they are not very effective for canine atopy.

Answer 9

Inhibit gastric acid secretion although proton pump inhibitors are used more- H2 receptor antagonist-->inhibit its metabolism-->may become toxic To prevent motion sickness Over the counter drugs

Answer 10

Inhibit both innate and adaptive immune response Highly effective- broad range of anti inflamm actions In acute inflamm inhibition of PLA2- prevents formation of postoglandins and leukotrienes Inhibition of cytokine release: prevents induction of many processes i the acute inflammatory response including activation of leukocytes

Answer 11

Act as the break on inflammation

Answer 12

Risk of inhibiting defence mechanism- if invading pathogen Inhibit adaptive immune response to the pathogen- detrimental Suppressing inflammation as much as steroids do , prevents resolution of the initial dmg -If used short term where acute inflammation is life threatening -May need to use in chronic inflammation conditions but side effects are an issue

Answer 13

Decrease production of eicosanoids- inhibition of PLA2 and prevention of induction of COX 2 Decreased generation of cytokines secondary to inhibition of gene transcription Reduced plasma conc of complement components in plasma Decreased iNOS expression Reduced histamine releast by mast cells Increased production of anti inflammatory factors (IL10, soluble IL-1 receptor)

Answer 14

Hypertension Fluid retention Poor wound healing Hyperglycemia → steroid-induced diabetes HPA axis suppression → adrenal insufficiency on withdrawal Easy bruising

Answer 15

Conventional Immunosuppressants For Autoimmune Diseases TNF-α inhibitors – e.g. infliximab, adalimumab (RA, IBD, psoriasis) IL-6 inhibitors – e.g. tocilizumab (RA) IL-17/IL-23 inhibitors – e.g. secukinumab, ustekinumab (psoriasis, psoriatic arthritis) B-cell depleters – e.g. rituximab (RA, lupus) For Atopic/Allergic Conditions Omalizumab (anti-IgE) – asthma, chronic urticaria 🍎 3. Lifestyle & Integrative Approaches These don't replace meds, but can be powerful adjuncts. Anti-inflammatory diet (low sugar, processed foods; high omega-3s) Vitamin D optimization – often low in autoimmune patients Stress reduction – yoga, mindfulness, CBT Exercise – improves fatigue, function, mood Sleep hygiene – critical for immune regulation Gut microbiome modulation – probiotics, prebiotics, sometimes fecal transplant (esp. IBD)

Answer 16

Dose in the Morning Mimics the body’s natural cortisol peak (~6–8 AM). Minimizes suppression of ACTH production (which is highest in early morning). Take entire daily dose at once in the morning if possible. Use Alternate-Day Dosing How it works: Give the full dose every other morning (rather than daily). Why: It allows the HPA axis to recover on the “off” days. Best for: Conditions that can tolerate fluctuations in disease control (e.g. some autoimmune diseases). ⚠️ Not always possible for conditions requiring steady suppression.

Answer 17

Inflammatory Phase (Early) "M1" macrophages dominate Derived from monocytes entering damaged tissue Functions: Phagocytose dead cells, pathogens, and debris Secrete pro-inflammatory cytokines (IL-1β, TNF-α, IL-6) Activate other immune cells to fight infection 2. Proliferative Phase (Transition) Macrophages start to shift phenotype from M1 to M2 This is called macrophage polarization Triggered by cytokines like IL-4, IL-10, and signals from dying neutrophils 3. Resolution/Repair Phase (Late) "M2" macrophages dominate Functions: Secrete anti-inflammatory cytokines (IL-10, TGF-β) Promote angiogenesis (new blood vessel formation) via VEGF Recruit and activate fibroblasts → ECM production Help with tissue remodeling and scar formation