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HLW
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What is a derivative of anthranilic acid, an analogue of salicyclic acid, has a slow onset of action, thus clinical efficacy requires 2-4 days?
Meclofenamic Acid
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What is a proprionic acid NSAID approved for use in humans, horses, and small animals, it is a strong inhibitor of COX, so has powerful anti-inflammatory, analgesic and antipyretic properties.
Ketoprofen
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How does ketoprofen interfere with the formation of leukotrienes?
Inhibits lipooxygenase
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What are side effects of ketoprofen (3)?
- GI upset
- CNS reactions
- Nephritis
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When is piroxicam used(3)?
- Osteoarthritis in dogs
- Transitional cell tumors in dogs (reduce size)
- Anti-inflammatory for musculoskeletal conditions
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What is an effective analgesic and antipyretic agent, but has weak anti-inflammatory activity, does not inhibit COX, but interferes with endoperoxidase intermediates formed during the arachidonic acid metabolism?
Acetaminophen
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For what animal is acetaminophen toxic?
Cats
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What are the adverse effects of acetaminophen (2)?
- Hepatotoxicity
- Methemoglobinemia
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How do you treat acetaminophen toxicity?
- Antioxidants
- Precursors of glutathione and ascorbic acid
- Cimetidine
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What are the most widely used anti-inflammatory drug, their anti-inflammatory effects are reflection of their capacity to emulate the action of endogenous corticosteroids?
Glucocorticoids
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What are the principal endogenous glucocorticoids that are produced by most mammalian species?
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Cortisol is the predominant glucocorticoid in what?
Most domestic species and man
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What animals produce mainly corticosterone?
Rodents
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Cortisol is synthesized from where?
Cholesterol in the cells of the zona fasciculata and zona reticularis of the adrenal cortex
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How is Cortisol released into the systemic circulation?
Pulsitile release and pulse amplitude varies according to a distinct ciradian pattern
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Serum glucocorticoids show what kind of change over a 24 hour period
- 3-5 fold change
- Maximal in the early morning
- Declining
- Low level early in the sleep phase
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Glucocorticoids are released in response to what, and what is it governed by?
- Physical and/or emotional trauma
- Governed by hypothalamus-pituitary-adrenocortical axis (HPAA)
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What is the first step of the HPAA and where does it go next?
Release of corticotrophin-releasing hormone from the hypothalmus which travels to the anterior pituitary
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When the CRH reaches the anterior pituitary this triggers the release of what?
Adrenocorticotrophic hormone (corticotrophin, ACTH) from the corticotrophs into systemic circulation
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What does ACTH do once it is released from the corticotrophs?
Acts on the adrenal cortex, initiating synthesis of cortisol
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The sensitivity of the hypothalamus-pituitary-adrenocortical axis is regulated by what?
Negative feedback system, through which the release of CRH and ACTH from hypothalamus and anterior pituitary gland is suppressed by glucocorticoids in circulation
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How do glucocorticoids act as transcription factors?
Induce/Repress the expression of target genes by direct interaction with specific glucocorticoid response elements in the promotor region
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Glucocorticoid increases the expression of lipocotin which can do what?
- Inhibit phospholipase A2 enzyme activity and thereby production of PGs
- Leukotrienes
- Platelet activating factor
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Another mechanism of glucocorticoid action is mediated by interaction of GRC with other transcription factors, such as nuclear factor KappaB and activating protein-1, inconsquence translocation to the nucleus is abolished, this leads to what?
Interference in the production/release of cytokines such as IL-1 and TNF
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How do glucocorticoids effect the energy metabolism (5)?
- Increases in glycogenolysis
- Lipolysis
- Gluconeogenesis
- Protein catabolism
- Reduction of peripheral use of glucose
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How do glucocorticoids effect the central nervous system (2)?
- Reduce excitation threshold
- Euphoria
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How do glucocorticoids effect the CVS (4)?
- Increase plasma volume and catecholamine tissue sensitvity
- Direct positive inotropic and chronotropic actions
- Hypertension
- Increases number and affinity of beta-adrenergic receptors on bronchial smooth muscle
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How do glucocorticoids effect the GIT (4)?
- Increase fat absorption
- Increase secretion of gastric acid, pepsin, and trypsin
- Thinning of gastric mucosa
- Decrease in Ca and iron absorption
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How do glucocorticoids effect the water and electrolyte balance (2)?
- Sodium retention
- Potassium loss
- ( => PU/PD)
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What are some immune and hematologic effects of glucocorticoids (5)?
- Reduction of lymphoid tissue
- Suppression of cell mediated immunity
- Increase erythropoiesis and platelet synthesis, lymphopenia and eosinopenia, neutrophilia
- Suppression of capillary growth
- Fibroblast proliferation
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Corticosteroids base determines what (3)?
- Anti-inflammatory Potentcy
- Na retaining potency
- Duration of action
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Endogenous glucocorticoids in the circulation are bound to ______, while exogenous glucocorticoids are bound to _______? Carrier Protein
ALB
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The ester moiety of glucocorticoids is metabolized by what?
- Hydrolysis in blood, tissues, or liver
- (Necessary to activate drug)
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Prednisone should be metabolized in the liver to the active compound _______
Prednisolone
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Cortisone should be metabolized in the liver to the active compound ________.
Hydrocortisone
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Glucocorticoids are excreted mainly in what?
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What is the most rapid route of administration of glucocorticoids?
IV
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The major problem of glucocorticoid therapy is related to the ___________ not to the __________
- Length of treatment
- Administered dose
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Replacement therapy involves the use of glucocorticoids in what amounts?
Similar to those of the naturally secreted glucocorticoids from the adrenal gland
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Physiological replacement therapy is rarely indicated in what?
Large animals
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When should the dosage of physiological replacent therapy glucocorticoids be increased?
Stress conditions
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What are examples of anti-inflammatory and anti-allergic use of glucocorticoids (3)?
- Symptomatic relief of pruritic dermatoses
- Allergic pulmonary diseases
- Allergic gastroenteritis
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Prednisone or prednisolone is most commonly used in?
Small Animals
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Dexamethasone is most commonly used in?
LA
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Unlike other immunosuppressants, glucocorticoids, do not significantly inhibit what?
Ab production by B lymphocytes
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Glucocorticoids are commonly used with NSAIDs for treating what?
- Arthritis
- Hip dysplasia
- (Chronic conditions)
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When should glucocorticoids be used (4)?
- Hypercitaminosis D
- Hypercalcemia
- Parturition induction
- Metabolic imbalances (ruminants)
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When should glucocorticoids NOT be used (6)?
- Systemic fungal infections
- Diabetes
- Viral infections
- Eye ulcers
- Pregnancy
- Wound/fracture
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What are Metabolic/endocrine side effects of glucocorticoids (6)?
- Iatrogenic cushings Dz
- Elevate insulin levels? (increase BG)
- Carbohydrate intolerance
- Reduced vitamin D
- Reduces T4/FT4
- Sex steroid levels
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What are gastrointestinal and hepatic side effects of glucocorticoids (6)?
- Polyphagia/Anorexia
- Diarrhea
- Increased gastric acid secretion
- Hepatomegaly
- Hepatopathy
- Pancreatitis
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What are musculoskeletal side effects of glucocorticoids (4)?
- Muscle atrophy
- Weakness
- Exercise intolerance
- Osteoperosis
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What are dermatologic side effects of glucocorticoids (4)?
- Calcinosis cutis
- Thin skin
- Bilateral hair loss
- Increased bruising
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What are immunologic side effects of glucocorticoids?
Exacerbation of clinical or laten infectious disease processes
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What are reproductive side effects of glucocorticoids (3)?
- High doses induce parturition during the last part of pregnancy
- Abortion
- Teratogenic effects during early pregnancy
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What are CNS side effects of glucocorticoids(4)?
- Depression
- Increased irritability
- Lethargy
- Panting
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What are renal side effects of glucocorticoids (2)?
- PU/PD
- Increased urinary Ca excretion
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What drugs can be used topical and intralesional (3)?
- Betamethasone,
- Dexamethasone
- Trimcinolone
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What drugs can be used topically of subconjunctivally to treat inflammatory conditions such as retinitis, choroiditis, optic neuritis, and orbital cellulitis (3)
- Alcoholic forms of cortisone
- Hydrocortisone
- Prednisone
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When are glucocorticoids contraindicated?
Corneal ulcers
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