Unit 4- Steroid and NSAID Flashcards
Adrenal Gland Secretion
Adrenalin, corticosteroids
Pituitary Gland Secretion
Growth hormone, corticotropin (ACTH), thyrotropin (TSH), gonadotropins (LH and FSH), prolactin, vasopressin (ADH), oxytocin
Testicle Secretion
Testosterone, estrogen, progesterone
Ovary Secretion
Testosterone, estrogen, progesterone
Pancreas Secretion
Insulin, glucagon
Thyroid Secretion
Thyroxine, triiodothyronine, parathyroid
Hypothalamus Secretion
Gonadotropin releasing hormone
Steroid Hormones
Cholesterol backbone, easily crosses cell membrane; progesterone, testosterone, estrogen, cortisol
Amine Hormones
Thyroxine, catecholamines, melatonin
Peptide Hormones
Insulin, oxytocin, vasopressin, growth hormone
Endogenous Corticosteroids
Cortisol regulates metabolism and immune, Aldosterone regulates sodium and water retention
Cortisol Synthetic Analog
Hydrocortisone
Corticosteroids
Effect metabolism, electrolytes, CNS, cardiovascular, skeletal muscle, blood cells, lymphoid tissue, and immunologic system, anti inflammatory and immunosuppressive
Corticosteroid Adverse Effects
Appetite, weight gain, mood changes, muscle weakness, blurred vision, body hair growth, bruising, susceptibility to infection
Prolonged Steroid Adverse Effects
Adrenal atrophy, osteoporosis, immunosuppression, euphoria
Inflammation
Immunovascular immune response to tissue injury, eliminate injury and initiate repair, mediated by chemical mediators
Small Animal Inflammatory Diseases
IBD, gastric ulcer, septic inflammatory, skin disease, neoplasia, inflammatory joint, inflammatory oral, primary inflammatory brain disorder
Signs of Inflammation
Pain, heat, redness, swelling, loss of function
Acute Inflammation
Initial response, plasma and leukocytes mobilized to tissue
Chronic Inflammation
Prolonged, mononuclear cells at site, destruction and healing of tissue
Inflammatory Response Complex
Activation of leukocytes and release of chemical mediators, arachidonic acid metabolism, vascular permeability altered, neutrophils release free radicals, pro-inflammatory cytokines
Products of Arachidonic Acid Metabolism
Leukotrienes, thromboxanes, prostaglandins
NSAID MOA
Inhibit cyclooxygenase
COX Enzymes
Cyclooxygenase, converts prostaglandins to thromboxane A2
COX-1 Enzyme
Constitutive, has a constant level of activity, maintains gastric mucosa, vascular homeostasis, platelet aggregation, maintains blood flow, produces PGs and TXA2
COX-2 Enzyme
Inducible, expressed at sites of injury, up regulates pain receptors, mediated by inflammation, causes fever, upregulated by cancer, produces PGs, and bradykinin
COX-3 Enzyme
Regulates fever, located in the brain, discovered in dogs
5-LOX Enzyme
Produces pro-inflammatory leukotrienes
Prostaglandins
Produced in many tissues, control inflammation, blood flow, and blood clots, promote inflammation, pain, and fever
Thromboxane A2
Platelet aggregation, smooth muscle contraction, endothelial inflammatory response activation
LOX Inhibition
GI safety, greater analgesic efficacy
NSAID Functions
Analgesia, antipyresis, anti-inflammation
NSAID Uses
Osteoarthritis, rheumatoid arthritis, pancreatitis, dental pain, skin inflammation
NSAID Adverse Effects
GI complications, deteriorate osteoarthritis
Cat NSAIDs
None approved long term, Robenacoxib and Melocixam for short term, overdose leads to stomach ulcer, kidney damage, liver problem, brain damage
NSAID Pharmacokinetics
Well absorbed, bound by albumin, metabolized in liver
Coxibs
Selective COX-2 inhibitors, Deracoxib and Firocoxib
Osteoarthritis Drugs
Polysulfated glycosaminoglycan and Hyaluronate sodium
NSAIDs that poison animals
Aspirin, acetaminophen, ibuprofen, indomethacin, naproxen, cause GI ulceration, hepatic and renal toxicity
GI Mucosa COX
COX-1 produces PGE2 protecting gastric mucosa, inhibition leads to ulcer and GI bleeding
Kidney COX
COX-1 and 2 produce PGE2 and PGI2, increasing GFR and Na/H2O excretion, inhibition leads to Nz/H2O retention, hypertension, and hemodynamic acute kidney injury
Cardiovascular COX
COX-2 produces PGI2 vasodilating and inhibiting platelet aggregation, COX-1 produces TXA2 vasoconstricting and causing platelet aggregation, inhibition leads to stroke and myocardial infarction
Aspirin and COX-1
Low dose aspirin irreversibly inhibits COX-1
LOX Inhibitors
Benoxaprofen, Ketoprofen, Licofelone, and Corticosteroids, Tepoxalin approved for osteoarthritis in dogs
Selective COX-1 Inhibiting Drugs
Low dose aspirin, causes GI ulceration and bleeding
Nonselective COX Inhibiting Drugs
Naproxen, Ibuprofen, Ketoprofen, Aspirin, Flunixin meglumine, causes paradoxical hyperpyrexia
Selective COX-2 Inhibiting Drugs
Meloxicam, Etodolac, Phenylbutazone, Carprofen, Deracoxib, Firocoxib, Robenacoxib, increase blood clotting
Dual Inhibiting Drugs
Tepolaxin
Aspirin
Low dose prevents heart attack and stroke, reduces pain, fever, inflammation, and platelet aggregation
Aspirin MOA
Irreversible COX-1 inhibition, decreased PG synthesis and TXA2 expression
Aspirin Adverse Effects
GI distress, cats sensitive, pyrexia, respiratory acidosis, metabolic acidosis, dehydration, pulmonary edema, bleeding during surgery, aggravated osteoarthritis, interaction with warfarin
Aspirin Toxicity Treatment
Induce emesis, gastric lavage and charcoal, alkalinizing agent to increase urinary excretion, IV fluid therapy
Flunixin meglumine
Banamine, nonselective COX inhibitor
Flunixin MOA
Greater COX-2 inhibition in horses, greater COX-1 inhibition in dogs
Flunixin Uses
Acute, visceral, and surgical pain, alleviates colic pain, post op analgesia in horse, control pyrexia in cattle
Flunixin Adverse Effects
Myonecrosis, overdose causing ulcer, CNS depression, and anorexia in horse, renal failure and GI damage in dog
Ketoprofen
Nonselective COX inhibitor
Ketoprofen MOA
Inhibits COX-1, COX-2, and LOX
Ketoprofen Use
Acute and chronic musculoskeletal disorders in horses
Ketoprofen Adverse Effects
GI ulceration, decreased platelet aggregation
Phenylbutazone
Safety and efficacy makes it the most commonly used equine NSAID, preferential COX-2 inhibitor
Phenylbutazone Use
Osteoarthritis, lameness, rheumatism, limb pain, nonspecific inflammation
Phenylbutazone Adverse Effects
GI distress, renal papillary necrosis, death
Carprofen
Rimadyl, preferential COX-2 inhibitor
Carprofen MOA
More than 100x preference for canine COX-2
Carprofen Uses
Short and long term pain management for musculoskeletal disorders
Carprofen Adverse Effects
Lower frequency of GI ulceration, diarrhea, anorexia, vomiting, not for pregnant or lactating
Meloxicam
Metacam, preferential COX-2 inhibitor, approved in cats
Meloxicam Uses
Chronic pain and inflammation from osteoarthritis and post-operative somatic pain
Meloxicam Adverse Effects
Rare and transient, can lead to renal failure in cats, not for pregnant, lactating, or young
Etodolac
Preferntial COX-2 inhibitor
Etodolac Uses
Osteoarthritis in dogs
Etodolac Adverse Effects
Keratoconjunctivitis sicca in dogs, GI distress, CNS depression, hepatotoxicity, nephrotoxicity
Tepoxalin
Zubrin, dual inhibitor
Tepoxalin Uses
Osteoarthritis and allergy in dogs, postoperative pain control
Tepoxalin Adverse Effects
GI distress, CNS depression, hepatotoxicity, nephrotoxicity
Deracoxib
Used for osteoarthritis and post operative pain, can cause GI distress
Firocoxib
Used for osteoarthritis, higher availability in horse than dog, highly protein bound, can cause diarrhea and mouth ulceration in hose and vacuolization in brain of dogs
Dimethyl sulfoxide
Topical solvent, inhibits PG synthesis and traps free radicals, analgesic, diuretic, anticholinesterase, antibacterial and antifungal
DMSO Uses
Acute swelling from trauma, cerebral edema from spinal cord trauma, cystitis in cat, burns, skin grafts, ischemia, edema of limbs from fractures, swelling of mammary, injectiion of drugs
DMSO Adverse Effects
Transient local effects, myopia in long term use, hemolysis and hemoglobinuria from IV injection, hepatic and renal damage, CNS sedation
Polysulfated Glycosaminoglycan
Disease modifying osteoarthritis drug
PSGAG MOA
Promotes chondroprotection, increases synovial fluid, inhibits PGE2 synthesis, leukocyte migration, and interleukin levels
PSGAG Uses
Treats traumatic joint dysfunction in horse and osteoarthritis and hip dysplasia in dog
Hyaluronate Sodium
Cushions and lubricates articular soft tissue, scavenges free radicals to treat synovitis in dog and hose