Pharmacology

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S_Test
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106186
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Pharmacology
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2011-10-12 13:49:20
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Pharmacology Exam II
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  1. Eicosanoids
    Subatances produced by the tissues that produce the signs of inflammation and start the healing process.
  2. Dosage Form
    • -Tablets
    • -Solutions
    • -Capsules
    • -Liniment
    • -Caplets
    • -Creams
    • -Etc.
  3. Dosage
    • The amount any patient should be given over time
    • ex. 5ml/kg, PO, b.i.d.
  4. Analgesics
    Drugs that reduce the perception of pain without significant loss of other sensations.
  5. Dose
    • The amount of a drug administered at one time.
    • ex. 2 tablets, 1.5 mls, 2 Tbl
  6. Arachidonic Acid Pathway
    • The domino effect caused when tissue is traumatized.
    • Trauma occurs
    • The Phospholipids of the cell membrane are converted into Arachidonic Acid by the enzyme Phospholipase.
    • AA is then acted on by either cyclooxygenase (COX) to make prostaglandins and thromboxanes (which are eicosanoids), or lipoxygenase (LOX) to make leukotrienes.
  7. Corticosteroids
    • Thchnically adrenocorticosteroids
    • Produced by cortex of the Adrenal gland
    • mineralocorticoids and glucocorticoids
    • Inhibits Phospholipase/stabilizes phospholipid membranes
  8. Addison's Dz
    • Hypoadrenocorticism
    • Low functioning adrenal gland cortex which leads to Hyperkalemia (too much K in blood stream) and hyponatremia (too little Na in blood stream) due to lack of aldosterone production.
    • Tx w/ mineralocorticoids.
  9. Glucocorticoid production
    • Hypothalamus releases corticotropin releasing factor (CRF)
    • Anterior pituitary gland releases adrenocorticotropic hormone (ACTH)
    • Adrenal glands release glucocorticoids
    • Glucocorticoids block Phospholipase, stabilize Phospholipid membranes, and block COX
  10. Hydrocortisone
    • A glucocorticoid a.k.a. cortisol
    • Provides needed systemic effect on body
    • Provides negative feedback to Hypothalamus and anterior pituitary gland
  11. Cortisone
    • A glucocorticoid
    • Provides needed systemic effect on body
    • Provides negative feedback to Hypothalamus and anterior pituitary gland
  12. Exogenous glucocorticoids
    • Administered drugs used to reduce inflammation and have the same negative-feedback effect on the hypothalamus and pituitary gland as endogenous cortisol
    • The negative feedback to the pituitary gland can result in side effects.
    • Ex. prednisone, prednisolone, methylprednisolone
  13. Short-acting glucocorticoid
    • Exerts an antiinflammitory effect for less than 12 hrs.
    • ex. Hydrocortisone common in topical
  14. Intermediate-acting glucocordicoids
    • exert their boilogic activity for 12-36 hrs.
    • Includes the "preds" (prednisone, prednisolone, methylprednisolone, and isoflupredone) and triamcinolone.
  15. Signs of inflammation
    • Redness
    • Heat
    • Edema
    • Pain
    • Loss of function
  16. Arachidonic Acid Cascade
  17. Inflammation
    • Increases blood flow to injured area
    • Increases Leukocyte migration
    • Increases phagocytosis activity
    • acute vs. cronic
  18. 2 classes of antiinflammitories
    • steroidal (corticosteroids)
    • nonsteroidal (NSAIDs)
  19. NSAIDs
    • Block COX (Cyclooxygenase) and (LOX) Lipooxygenase
    • reducing production of Prostaglandins, thromboxane, and leukotrienes
  20. Corticosteroids and NSAIDs also decrease production of several other compounds...
    • Histamine
    • Kinins
    • Substance P
    • Superoxide Radicals
  21. Mineralocorticoids
    • Affect minerals in the body (Na, K, & other electrolytes)
    • Involved in water and electrolyte balance in body
    • little-no antiinflammitory effect
    • Aldosterone - promotes Na reabsorption (K excretion)
  22. Glucocorticoids
    • Antiinflammitory effect-inhibits Phospholipsae (COX)
    • Decreasing production of Prostaglandins, and leukotrienes involved w/ inflammation
    • Inhibit production of mediators involved in toxic & immune-mediated cellular damage (preventing allergic reactions)
    • Reduce production of cell factors that cause increased vascular permiability of capillaries (reduce swelling)
    • Increases blood-glucose level (enhanses deposition of glycogen in liver)
    • On negitive feedback loop w/ Hypothalamus and Pituitary gland (CRF & ACTH)
  23. Steroids Ex.
    • Prednisone
    • Dexamethesone
  24. NSAIDs Ex.
    • Aspirin
    • Rimadyl
    • Deramaxx
    • Metacam
  25. Cortisone
    must be converted by the liver to hydrocortisone
  26. Prednisone
    Must be converted by the liver to prednisolone
  27. Long-acting glucocorticoids
    • Exert activity for more than 48 hrs.
    • dexamethasone
    • betamethasone
    • flumethasone
  28. Aqueos solution glucocorticoids
    • Made water soluable by combining with salt
    • Can be given in Lg doses IV w/ less risk of adverse reactions than alcohol solutions or suspensions.
  29. Alcohol solution glucocorticoids
    Don't need salt to dissolve
  30. Suspension glucocorticoids
    • Opaque
    • Need resuspension (ex shaking) before use
    • Terms: acetate, diacetate, pivalate, acetonide, valerate
    • Longer release (Lg crystals- dissolve)
    • SQ
    • must be stored in temp. range
  31. Negative effects of glucocorticoids
    • Delays healing of wounds
    • Greater opportunity for infection
    • Muscle wasting/atrophy, thin skin, alopecia, osteoporosis, pot belly from weakening of abd. muscles due to catabolism
    • Can induce abortion/parturition
    • Hyperglycemia threat to diabetics
    • Possibility of developing Cushings or Addisons
    • Alters hemogram-stress leukogram
  32. Glucocorticoid uses
    • Non-infectious inflammation
    • Allergies, allergic reactions
    • Pruritis
    • Immune-mediated disease
    • Anaphylactic shock
    • Adrenal insufficiency (Addison’s)
    • Spinal cord trauma
    • Neoplasia
    • AFTER diagnosis is made!!
  33. Glucocorticoid routs
    • PO
    • IV (SLOW)
    • IM
    • Topical
    • Intra-articular
    • Intralesional
    • Subconjunctival
  34. Glucocorticoid Contradictions
    • Undiagnosed conditions
    • Fungal infections
    • Modified live virus vaccine
    • Cornial ulcer
    • Pregnant animals
    • Horses-laminitis!
    • Immature animal
    • Liver Dz
  35. Glucocorticoid effected leukogram
    • Cause WBCs to move into tissues (Ex lungs, spleen) and out of systemic circulation
    • Lower Lymphocytes, Monocytes, and Eosinophils. (-penia)
    • Higher Neutrophils (neutrophilia) and platelets
    • Like a stress leukogram
  36. catabolism
    • Breakdown of proteins for amino acids for gluconeogenisis
    • Over time can cause muscle wasting, thinning of skin, alopecia, & decreased bone density.
    • "Pot belly"
  37. Corneal Ulcer
    Contradiction for use of glucocorticoids which may deepen the ulcer and slow its healing.
  38. Opthalmic corticosteroids - horses
    normal fungus fought off by the cell-mediated immunity may cause infection with steroids and a scratch.
  39. diabetes mellitus + glucocorticoids
    may require an increase in insulin dose if given for an extended period
  40. Hyperadrenocorticism or Cushing's
    • Overuse of exogenous glucocorticoids (iatrogenic) or overproduction by the body.
    • Alopetia
    • Thin skin
    • Muscle atrophy
    • Pot belly
    • Polyuria
    • Polydipsia
    • polyphagia
  41. Hypoadrenocorticism or Addison's
    • Can be caused by stopping steroid use "cold turkey" production of CRF and ACTH will resume but the adrenal gland is unable to respond
    • Weakness
    • Lethargy
    • Vomiting
    • Diarrhea
    • Death in severe cases
  42. Steroid potency low to high
    • Cortisone
    • Hydrocortisone
    • Prednisone
    • Methylprednisolone
    • Dexamethasone
    • Betamethasone
  43. methylprednisolone sodium succinate
    SoluMedrol ®
  44. Rules of thumb for glucocorticoids
    • Use NSAIDs instead if avalible without contradictions
    • Avoid continuous use (adrenal atrophy)
    • Use intermediate acting for systemic administration
    • Aim for smallest effective dose then reduce (alternate day)
    • When used over extended period reduce gradually
  45. Hydrophilic glucocorticoids
    • Very soluble
    • Ok admin. IV
    • released for only mins. after injection
    • Succinate
    • Phosphate
    • May be given in Lg doses (shock, trauma)
    • Ex.SoluMedrol ® (methylprednisolone sodium succinate
  46. Moderately soluble glucocorticoids
    • released days - weeks after
    • Lg crystals Suspended in liquid (SHAKE)
    • Do NOT give IV!!
    • Acetate
    • Pivalate
    • Ex. DepoMedrol® (methylprednisolone acetate)
  47. Poorly Soluble glucocorticoids
    • Lipophilic
    • Released for weeks
    • Acetonide
    • Topical preps
    • Ex. Vetalog® (triamcinolone acetonide)
  48. NSAIDs vs steroids
    • block further down AA pathway, less effective
    • Many same steroidal effects w/ less adverse effects
    • not good for severe bone or intense pain
    • Do NOT use NSAIDs & CCS together!!
  49. COX 1
    • Exists in stomach, Kidney, and other organs
    • Produces prostiglandins for physiological regulation
    • In stomach promotes protective mucus layer, good blood flow, decrease acidity
    • In kidney counteracts vasoconstriction
  50. COX 2
    Enzyme, produces prosteglandins associated w/ signs of inflammation
  51. NSAID side effects
    • Diarrhea
    • Anorexia
    • Lethargy
    • Melina
    • GI Ulcers
    • Hepatotoxic
    • Increased bleeding tendency
    • Affects renal prostiglandins: lower blood flow, low GFR, papillary necrosis (lack of O2
    • Never w/ dehydrated or hypotensive shock!!
    • Caution in geriatrics
  52. All NSAIDs are...
    • Anti-inflammitory
    • Antipyretics (fever reducer)
    • Analgesics
  53. Some NSAIDs
    • Aspirin
    • Phenylbutazone
    • Flunixin meglimine
    • Carprofen
    • Meloxicam
    • Etodolac
    • Deracoxib
    • Tepaxolin
  54. Aspirin
    • Salicylic Acid
    • Nonselective NSAID
    • Terminate use 1 wk prior to Sx
    • Cats extremely sensitive
    • Uses: arthritis, lower PLT aggrigation, decrease thromboembolism in HW Tx, decrease thrombi in cats w/ hypertrophic cardiomyopothy
    • SE: Vom.,gastric bleeding, increased clotting time
  55. Phenylbutazone
    • Bute
    • Common use w/ horses
    • Lots of interactions
    • IV and PO
    • Highly protein bound
    • Uses: osteoarthritis, colic, lameness, mild-mod pain
    • SE: GI bleeding, GI upset, GI ulcers, renal necrosis, bone marrow supression (rare)
    • Tissue necrosis if injected perivascular!!!!!
  56. Flunixin meglumine
    • Banamine®
    • Horses & calves
    • more potent than Bute good analgesic
    • Anti-endotoxic effect
    • IV, IM, PO
    • Uses: Colic, shock, corneal ulcers, keratitis, uvelitis
    • SE: GI upset, neprotoxicity
  57. Carprofen
    • Rimadyl®
    • Selective
    • Less ulcerogenic potential
    • Analgesia in Sx
    • Dogs & cats
    • Injectable & PO
    • SID or BID
    • Uses: DJD (degenerative joint Dz), post op pain
    • SE: GI ulcers, bleeding
  58. Etodolac
    • EtoGesic®
    • nonselective
    • dogs
    • Uses: osteoarthritis
    • SE: anorexia, V/D, lethargy, liver, DRY EYE!!
  59. Meloxicam
    • Metacam®
    • Selective
    • Dogs
    • Oral suspension SID
    • SE: V/D
  60. Deracoxib
    • Deramaxx®
    • Selective
    • Dogs
    • Uses: post-op pain & oseoarthritis
    • SID chewable tab
  61. Ketoprofen
    • Ketofen®
    • COX & LOX inhibition
    • Dogs, horses, & cats
    • Uses: pain w/ musculoskelital dz, post-op pain
    • SE: GI bleeding, GI ulcers, renal dysfunction, generalized bleeding
    • Naproxen, Aleve, Orudis KT Very toxic in dogs!!!
  62. Tepoxalin
    • Zubrin®
    • COX & LOX inhibition
    • Uses: osteoarthritis in dogs
    • Rapidly dissolving tablet SID PO
  63. Firocoxib
    • Previcox®
    • Selective
    • Used for osteoarthritis in dogs
  64. Hyaluronic acid
    • Legend®, and others
    • component of sinovial fluid, acts as lubricant
    • Dogs & horses
    • IV, intra-articular, IM in dogs
  65. Polysulfated glycoaminoglycans/ PSGAGS
    • Adequan®
    • Chondroprotective, anti-inflammitory
    • Used for arthritis in horses (IA &IM) and dogs (IM)
  66. DIMETHYLSULFOXIDE (DMSO)
    • Clear liquid solvent
    • Scavenges free radicals
    • Used as carried to deliver drugs through skin
    • Approved use:Topically to decrease swelling in horses & dogs
    • SE: garlic taste, skin irritation, teratogenic
    • WEAR GLOVES!!!
  67. Cosequin® (glucosamine, chondroitin sulfate, manganese sulfate)
    • Neutroceutical
    • Precursor of cartilage matrix
    • Repairs damaged cartilage
  68. Acetaminophen
    • Tylenol TM
    • Not NSAID
    • Antipyretic, analgesic, not anti-inflammitory
    • No GI upset, ulcers, or PLT clumping
    • Not metabolized well in cats 500mg = death
  69. Prosteglandin E
    • Increases gut mucous layer
    • Decreases HCL production
    • Increases gut motility
    • improves blood flow to gut
    • Parasympathetic
  70. Oxyntic (parietal) cells have receptors and are stimulated to produce HCl by:
    • Histamine
    • Gastrin
    • Acetylcholine
  71. Histamine is released by:
    • Mast cells and Basophils in inflammitory response
    • Mast cell toumors (Boxers)
  72. Emetics
    • Induce Vomiting
    • To reduce absorption of ingested toxin
    • Must be relyable and work quickly
  73. Vomiting reflex stimulated by:
    • Direct stimulation of EC (emetic center)
    • Vagus Nerve
    • Chemoreceptor Triggor Zone (CRTZ)
    • Inner ear nerves
    • Higher brain centers
  74. Neuron receptors for emisis
    • Seratonin Rc.
    • Alpha Rc.
    • Block these to control emisis
    • Cats especially sensitive to the stimulation of these
  75. CRTZ stimulant side effects
    Toxins associated in renal failure

    Excessive ketones in diabetes mellitus

    Bacterial or metabolic toxins
  76. Dopaminergic antagonists or antidopaminergic
    drugs
    • Decreases vomiting
    • Have little effect on cats
    • Work well on dogs, have many D2 receptors in CRTZ
  77. Xylazine
    • Powerful emetic on cats (Alpha2 agonist)
    • Sedative, anesthetic
  78. Do not induce vomiting if animal is...
    • comatose
    • debilitated
    • extremely depressed
    • unconscious
    • lacking gag reflex
    • chicken bones
    • gasoline
  79. Centraly acting emitics (nervous system)
    • apomorphine (dogs, conjunctival sac)
    • xylazine (cats a2 receptors, can be reversed)
  80. Locally acting emetics (stomach)
    • Giver PO 1 dose, do not repeat
    • Syrup of Ipecac - Do NOT use!!
    • Hydrogen peroxide - not always relyable
    • Warm concentrated salt water, Na toxisity
    • Solution of powdered mustard and water ?
  81. Antiemetics
    • Prevent or decrease vomiting
    • Should only be used when vomiting is no longer beneficial
    • May mask clinical signs, keep bod substance in GI longer
  82. Chlorpromazine (Compazine, DarbazineTM)
    • Phenothiazine Tranquilizer
    • Used for motion sickness
    • acute gastroenteritis
  83. TYPES OF ANTIEMETICS
    • Phenothiazine
    • Tranquilizers
    • Procainamide
    • Derivative (metoclopramide)
    • Cisapride
    • Antihistamines
    • Anticholinergics
    • Maropitant
  84. Phenothiazine Tranquilizers should not be used in
    Dehydrated or sesure prone pt.
  85. METOCLOPRAMIDE (REGLANTM)
    • Blocks dopamine and Seratonin Rc
    • Increase stomach motility
    • Don’t use with atropine or narcotic analgesics (negate)
    • Cats & horses can become frenzied
    • prokinetic
  86. CISAPRIDE (PROPULSIDTM)
    • $$$
    • does not cross BBB
    • For use in gastric stasis vomiting, prokinetic agent
    • Dogs w/ megaesophogus
    • Cats w/ megacolon
  87. Antihistamines
    • Motion sickness, middle ear infection
    • Dogs: BenadrylTM (diphenhydramine) DramamineTM (dimenhydrinate)
    • First generation H1 antagonists
  88. Anticholinergic drugs a.k.a. Parasympatholytic
    • Blocks parasympathetic NS
    • Do not completely block emisis
    • may increase emisis w/ decreased gastric motility or gastric atoney
    • Not usualy for antiemetic unless IBD
  89. CereniaTM
    • Substance P induces vomiting via NK1 receptors in the G.I. tract and brain
    • NK1 Rc antagonist
    • injectable and tablet
  90. Narcotic Antidiarrheals
    • diphenoxylate (Lomotil®),
    • paregoric (tincture of opium)
    • loperamide (Imodium and Imodium A-D OTC)
    • Sevear dry mouth if abused
    • C-V or C-III
    • increased intracranial pressure w/ head trauma
    • analgesic makes dz motering hard
    • “Morphine mania” in cats
    • prolonged contact time with mucosa and pathogenic bacteria
  91. Antidiarrheal Anticholonergic/ Parasympatholytic drugs
    • Decrease effect of Ach neurotransmitter on GI tract
    • Used as antispasmodics, decrease spastic colonic contractions
    • Not as effective against small bowel dz
  92. Antidiarrheals that block hypersecretion
    • Block liquid contact with mucosa
    • Bismuth subsalicylate (Pepto-BismolTM and Kaopectate TM)
    • Flunixin meglumine (BanamineTM) for horses & cattle
    • Sulfasalizine (Asulfidine)
  93. lipid soluble vitamins
    • A
    • D
    • E
    • K
  94. Non-systemic antacids
    • May cause electrolyte imbalance w/ prolonged use
    • Ca, Mg, Al
    • Gastric acid rebound syndrom
    • Constipation
    • Diarrhea
  95. Systemic antacids
    • decrease production of stomach acid
    • Cimetidine (Tagamet®)
    • ranitidine (Zantac®)
    • famotidine (Pepcid®)
    • Alternate w/ cardiac & other drugs
  96. Omeprazole (Prilosec)
    • binds to luminal surface of parietal cells and inhibits the
    • hydrogen pump that transports hydrogen ions into stomach lumen
  97. Sucralfate (Carafate)
    • Needs ulcer to bind with
    • "gastric band-aid"
    • needs acidic environment
    • Stimulates PGE production
  98. Misoprostol (Cytotec)
    • $$$ the good stuff
    • Use for Dx ulcer
    • Wear gloves if pregnant
  99. Ruminatorics
    • Increases Parasympathetic NS
    • Increases motility
  100. Neostigmine (Stiglyn®)
    • combines with acetylcholineseterase
    • prevents breakdown of acetylcholine
    • Do not use with GI obstruction, asthma, bradycardia or with organophosphates or any other drug that increases parasympathetic tone

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