Pharmacology of Corticosteroids
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Questions and Answers

What are the main pharmacological actions of glucocorticoids?

  • Antimicrobial and blood pressure regulation
  • Hormonal regulation and sodium balance
  • Anti-inflammatory and immunosuppressive effects (correct)
  • Pain relief and allergy suppression
  • Which drugs are classified as anti-inflammatory drugs in the context provided?

  • Antihistamines, NSAIDs, corticosteroids
  • Ciclosporin, antibiotics, NSAIDs
  • Analgesics, corticosteroids, ciclosporin
  • Corticosteroids, NSAIDs, ciclosporin (correct)
  • What is one primary mechanism by which corticosteroids exert their anti-inflammatory effects?

  • Promotion of eicosanoid synthesis
  • Inhibition of phospholipase A2 (correct)
  • Increase in leukotriene synthesis
  • Activation of arachidonic acid metabolism
  • Which hormone is primarily responsible for regulating the levels of corticosteroids?

    <p>Adrenocorticotrophic hormone (ACTH)</p> Signup and view all the answers

    What effect do mineralocorticoids primarily have on the body?

    <p>Affect sodium balance and influence blood pressure</p> Signup and view all the answers

    Which of the following is a common adverse effect associated with prolonged corticosteroid use?

    <p>Diabetes mellitus</p> Signup and view all the answers

    Which of the following is NOT an anti-inflammatory drug category mentioned?

    <p>Antiallergic drugs</p> Signup and view all the answers

    What is a therapeutic application of corticosteroids in cancer treatment?

    <p>Chemotherapy for acute leukaemia</p> Signup and view all the answers

    Which of the following eicosanoids is primarily involved in modulating inflammatory responses?

    <p>Prostaglandin E2 (PGE2)</p> Signup and view all the answers

    What is a role of ophthalmic corticosteroids?

    <p>Treating acute and chronic inflammation</p> Signup and view all the answers

    Which ophthalmic corticosteroid is typically indicated for severe inflammation?

    <p>Dexamethasone</p> Signup and view all the answers

    What factor affects the efficacy of a glucocorticoid preparation besides its strength?

    <p>The salt used in the formulation</p> Signup and view all the answers

    Which of the following statements about prednisolone acetate is true?

    <p>It penetrates the eye better when the cornea is abraded.</p> Signup and view all the answers

    In which situation is low strength prednisolone sodium phosphate preferred?

    <p>To minimize glucocorticoid side effects.</p> Signup and view all the answers

    Which combination of medications is most likely to be used for treating ocular inflammation?

    <p>Dexamethasone with antibiotics</p> Signup and view all the answers

    What condition is primarily treated with Ozurdex intravitreal implant of dexamethasone?

    <p>Macula oedema following retinal venous occlusions</p> Signup and view all the answers

    What is an acute adverse reaction associated with the short-term use of corticosteroids?

    <p>Increased intraocular pressure (IOP)</p> Signup and view all the answers

    What is the primary action of NSAIDs in the inflammatory response?

    <p>Inhibiting cyclo-oxygenase (COX)</p> Signup and view all the answers

    What is the consequence of prolonged use of ophthalmic corticosteroids?

    <p>Development of posterior sub-capsular cataract</p> Signup and view all the answers

    Which NSAID is specifically licensed for treating seasonal allergic conjunctivitis?

    <p>Diclofenac sodium</p> Signup and view all the answers

    What role do eicosanoids play in the body?

    <p>Act as mediators of the inflammatory response</p> Signup and view all the answers

    Which medication is used as an immunosuppressive for treating severe dry eye disease?

    <p>Ciclosporin</p> Signup and view all the answers

    What is the effect of vasoconstrictors in ophthalmology?

    <p>Constrict conjunctival blood vessels</p> Signup and view all the answers

    Which of the following is a mast cell stabilizer used in allergic eye disease?

    <p>Sodium cromoglicate</p> Signup and view all the answers

    What is an effect of acute allergic conjunctivitis?

    <p>Symptoms of redness and itching</p> Signup and view all the answers

    Which condition is NOT treated by ophthalmic corticosteroids?

    <p>Severe dry eye</p> Signup and view all the answers

    How long may mast cell stabilizers take to produce symptomatic relief?

    <p>7-14 days</p> Signup and view all the answers

    Which drug is an example of a topical antihistamine?

    <p>Olopatadine</p> Signup and view all the answers

    Which condition is associated with mast cell degranulation?

    <p>Vernal keratoconjunctivitis</p> Signup and view all the answers

    What is the common response of mast cells in allergic eye disease?

    <p>Release of mediators like histamine</p> Signup and view all the answers

    Signup and view all the answers

    Study Notes

    Ophthalmic Drugs 1: Anti-Inflammatory Drugs

    • Ocular Therapeutic Drugs include anti-inflammatory, anti-infective, dry eye preparations, and anti-glaucoma drugs.
    • Part 1 of the lecture covers the pharmacology, indications, and side effects of corticosteroids, non-steroidal anti-inflammatory drugs (NSAIDs), and ciclosporin.
    • Part 2 of the lecture covers anti-allergy drugs (antihistamines, mast cell stabilisers).

    Corticosteroids

    • Corticosteroids are hormones produced by the adrenal cortex.
    • These include glucocorticoids and mineralocorticoids.
    • Hormone levels are regulated by ACTH from the pituitary gland.
    • Glucocorticoids, such as cortisol, maintain blood glucose levels and promote recovery from injury.
    • Mineralocorticoids, e.g. aldosterone, affect sodium balance, causing sodium reuptake and water retention, thus influencing blood pressure.

    Corticosteroids: Actions

    • Glucocorticoids used therapeutically to treat inflammation.
    • Glucocorticoids have anti-inflammatory and immunosuppressive effects by reducing the activity of inflammatory mediators (e.g. eicosanoids, platelet-activating factor, and interleukins).
    • They also have metabolic effects on carbohydrates, proteins, and fats.
    • The steroid-receptor complex binds to glucocorticoid response elements in chromatin, affecting DNA transcription and the production of inhibitory proteins.

    Corticosteroids: Action (cont.)

    • Corticosteroids inhibit inflammation by impacting inflammatory mediators.
    • Inflammatory mediators cause effects such as swelling, redness, heat or pain; corticosteroids interfere with this process
    • This process includes chemotaxis as well as cellular migration.

    Corticosteroids: Action (cont.2)

    • Corticosteroids also inhibit eicosanoid synthesis by preventing the production of eicosanoids such as prostaglandins, thromboxane A2, prostacyclin, leukotrienes, through inhibition of cyclooxygenase and lipoxygenase.

    Corticosteroids: Therapeutic Uses (Systemic)

    • Anti-inflammatory effects (systemic or topical) for conditions such as asthma, eczema, inflammatory bowel disease, and rheumatic disease.
    • Replacement therapy for adrenal gland diseases.
    • Chemotherapy for conditions like acute leukaemia and Hodgkin lymphoma.
    • Immunosuppression, such as post-transplantation.

    Corticosteroids: Adverse Effects

    • Adverse effects are common and can be severe, dependent on dose and treatment duration.
    • Adverse effects may include impaired glucose tolerance, or diabetes mellitus, osteoporosis, Cushing's syndrome, and immune suppression.

    Ophthalmic Corticosteroids: Indications

    • Used in the treatment of acute and chronic inflammation, such as anterior uveitis and vernal conjunctivitis.
    • Used after surgery, to help reduce inflammation following procedures.
    • Intravitreal steroids are used to treat macular oedema and some cases of posterior uveitis.

    Ophthalmic Corticosteroids: Indications (cont.)

    • There's no official potency hierarchy for topical ocular glucocorticoids; efficacy depends on the salt used (prednisolone acetate is more effective than prednisolone sodium phosphate) and corneal integrity.

    Ophthalmic Corticosteroids: Indications (cont.2)

    • Prednisolone acetate and dexamethasone are used for severe inflammation, while milder forms use lower strength topical preparations like prednisolone sodium phosphate or hydrocortisone.

    • Important to minimise side effects, especially in the presence of viral infections.

    Ophthalmic Corticosteroids: Available Preparations

    • Betamethasone (Betnesol), Dexamethasone (Maxidex), Fluorometholone (FML), Loteprednol Etabonate (Lotemax), Prednisolone(Predsol, Pred Forte) etc.
    • Combination preparations with antibiotics (e.g., Betnesol N, Maxitrol, Tobradex) sometimes needed.
    • Intravitreal corticosteroids (e.g., Ozurdex) are used for macular oedema following retinal venous occlusions and non-infectious posterior uveitis.

    Ophthalmic Corticosteroids: Adverse Reactions

    • Prolonged steroid use increases risk of posterior sub-capsular cataract formation.
    • Cataracts are dose-dependent and account for approx. 4% cases, usually in patients on a high dosage over 1+ years.

    Ophthalmic Corticosteroids: Adverse Reactions (cont.)

    • Raised intraocular pressure (IOP) is a key adverse reaction to short-term use in steroid responsive individuals. This can be caused by topical, inhaled, or systematic use of steroids

    Non-steroidal Anti-inflammatory Drugs (NSAIDs)

    • Topical NSAIDs provide mild to moderate anti-inflammatory action without the side effects of corticosteroids.
    • NSAIDs prevent the formation of eicosanoids.

    Biological Actions of Eicosanoids

    • Eicosanoids are crucial mediators of the inflammatory response.
    • Key eicosanoids are prostaglandins and leukotrienes.
    • Ocular effects include vasodilation, increased IOP, miosis, and macular oedema

    Biological Actions of Eicosanoids (cont.)

    • NSAIDs primarily work by inhibiting cyclo-oxygenase (COX).

    Ophthalmic NSAIDs: Indications

    • Reduction of intra-operative and post-operative inflammation.
    • Use in some centers for post-operative pain management.
    • Reduction of pain after corneal trauma—diclofenac sodium is used in some cases.
    • Allergic conjunctivitis—diclofenac sodium and others are used in some cases.
    • Episcleritis—occasionally used, but is off-license.

    Available Topical NSAIDs

    • Diclofenac sodium (Voltarol).
    • Flurbiprofen (Ocufen).
    • Ketorolac trometamol (Acular).
    • Nepafenac (Nevanac).
    • Bromfenac (Yellox).
    • Diclofenac sodium has a licence for post-corneal trauma pain and sometimes also for seasonal allergic conjunctivitis (SAC)(See indications above)

    Ciclosporin

    • Ciclosporin inhibits cytokine release from T-lymphocytes, thus suppressing the cell-mediated immune response.
    • It is licensed for severe keratitis in dry eye disease (usually when other treatments haven't worked).
    • Licensed for severe vernal keratoconjunctivitis.

    Summary (Ophthalmic Drugs 1 Part 1)

    • In the UK, ophthalmic corticosteroids are usually reserved for managing moderate-to-severe inflammation by qualified ophthalmologists and can also be prescribed by independent optometrists.
    • Topical NSAIDs are mainly licensed to reduce post-operative inflammation; however, diclofenac is used for seasonal allergic conjunctivitis and pain.
    • Ciclosporin is an immunosuppressant, primarily used for severe cases of dry eye and vernal keratoconjunctivitis.

    The Ocular Allergic Response

    • Eyes are a common site for allergic inflammation.
    • The majority of allergic eye conditions affect the conjunctiva.
    • Mast cells play a key role in allergic responses.
    • Degranulation of mast cells releases substances like histamine.
    • Released mediators cause signs and symptoms of ocular allergy.

    Allergic Eye Diseases

    • Acute allergic conjunctivitis.
    • Seasonal/perennial allergic conjunctivitis.
    • Giant papillary conjunctivitis.
    • Atopic keratoconjunctivitis.
    • Vernal keratoconjunctivitis.

    Role of Mast Cells in Ocular Allergy

    • Mast cells are involved in processing and presenting antigens, producing IgE, and activating inflammation.
    • Mast cell degranulation occurs when inflammatory mediators are released.
    • Mast cell stabilization involves stopping degranulation, which can be done using mast cell stabilisers.

    Anti-allergy Drugs

    • Antihistamines, mast cell stabilisers, corticosteroids, NSAIDs, and vasoconstrictors are used to treat allergic eye conditions.

    Antihistamines

    • Available in topical and systemic forms (many OTC preparations).
    • Systemic antihistamines are often used for hay fever and other conditions. The common example of a topical antihistamine is cetirizine. (examples: diphenhydramine and cetirizine).
    • Topical antihistamines are a very common treatment for seasonal and perennial allergic conjunctivitis.
    • Newer antihistamines also have mast cell stabilizing properties.

    Available Anti-allergy Preparations (Topical Antihistamines)

    • Antazoline, Azelastine, Epinastine (POM), Ketotifen, and Olopatadine.

    Topical Mast Cell Stabilizers

    • Block calcium influx to mast cells, preventing degranulation, decreasing the symptoms and signs of allergic reactions.
    • Symptom relief takes 7-14 days.
    • Effective for moderate to severe allergic eye conditions.

    Available Anti-allergy Preparations(Mast Cell Stabilizers)

    • Sodium cromoglicate, Lodoxamide, and Nedocromil sodium.

    NSAIDs (for allergic conditions)

    • Diclofenac sodium (POM) is a licensed, well-tolerated NSAID for allergic eye conditions, particularly SAC, and provides symptomatic relief within 30 minutes of administration.

    Vasoconstrictors

    • Vasoconstrictors are sympathomimetic drugs, stimulating alpha adrenoceptors to cause constriction of conjunctival blood vessels. Reducing redness and inflammation.
    • Vasoconstrictors reduce conjunctival hyperemia and oedema. Examples include: Xylometazoline and Naphazoline.

    Summary (Ophthalmic Drugs 1 Part 2)

    • Several topical drugs treat allergic eye conditions, including antihistamines, mast cell stabilisers, dual-acting drugs (some over-the-counter), topical NSAIDs and vasoconstrictors.
    • Newer antihistamines also have mast cell stabilizing properties.
    • Some drugs are available over the counter.
    • Topical NSAIDs and vasoconstrictors have a limited role in treating allergic eye conditions.

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    Description

    This quiz examines the pharmacological actions of glucocorticoids and their role as anti-inflammatory agents. Participants will explore therapeutic applications in various contexts, including cancer treatment and ocular conditions. Test your knowledge on corticosteroid mechanisms and adverse effects.

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