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VET - Pharm > Lec7 > Flashcards

Lec7 Flashcards

1
Q

What is inflammation?

A

a natural response of living tissue to injury and infection to initiate the healing process; Is the protective response elicited by injury or destruction of tissues

May be caused by chemical, physical or biologic agents

Serves to destroy, dilute, and sequester both the injurious agent and the injured tissue

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2
Q

What are the characteristics of Inflammation?

A

Pain – due to tissue swelling and release of prostaglandins

Heat – due to increased blood accumulation

Redness – due to blood accumulation

Swelling – increased capillary permeability allows plasma to leak into the interstitial tissue at the injury site

Loss of Function or Decreased Range of Motion – pain and fluid accumulation

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3
Q

What is the Inflammatory Pathway

A

Tissue trauma –> Phospholipase release –> break down to Arachidonic Acid –> enzyme reactions (Cyclogenase, Lipoxygenase) –> Cylogenase rxns: Prostaglandins and Thromboxanes, Lipoxygenase rxns: Leukotrienes

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4
Q

How does Cyclogenase act in inflammation?

A

–> Prostaglandins (inflammation mediator/vasodilation) and Throboxanes (platelet aggregation/ smooth muscle constriction)

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5
Q

How does Lipoxygenase act in inflammation?

A

–> Leukotrienes (induce inflammation / increased vascular permeablilty, WBC migration)

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6
Q

How does histamine participate in inflammation

A
  • Released by mast cells when mast cell membranes come in contact with extracellular fluid involved with tissue trauma
  • Dilation of Capillaries (Increases blood vessel permeability/Decreases blood pressure )
  • Contraction of Smooth Muscle (Bronchial/Increased Gastric Contraction/Increased Heart Rate)
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7
Q

Corticosteroids

A
  • produced by the adrenal gland
  • Can usually be recognized by the ending “sone”
  • Two Groups of Corticosteroids Produced by the Adrenal Cortex
  • Affect glucose metabolism
  • Generally cause an increase in blood glucose levels
  • Raise concentration of liver glycogen
  • Affect carbohydrate, protein, and fat metabolism
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8
Q

What are the different Corticosteroids based on the duration of action?

A

Short Acting (Less than or Equal to 12 Hour Duration)
- Hydrocortisone (Usually Topical)
- Cortisone (Converted by the Liver into Active Hydrocortisone)
Intermediate Acting (12 – 36 Hour Duration)
- prednisone (Converted in the Liver into Prednisolone)
- prednisolone – Tablets, Injection, Opthalmic Ointment
- triamincinolone (Vetalog®) - Tablet, Topical, Suspension for Inj.
- methylprednisolone (Medrol®) - Tablets
- isoflupredone (Predef 2X®)
Long Acting (48 Hour or Longer)
- dexamethasone (Azium®) - Tablets, Injection, Opthalmic Suspension
- betamethasone (Betasone®) - Injection, Topical
- flumethasone (Synalar®) - Topical Cream and Solution
- mometosone (Mometomax®) - Topical

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9
Q

How are the Corticosteroid preparations made?

A

Usually a Steroid Combined with a Salt to Make It More Soluble in Water
- Aqueous Solutions

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10
Q

What are the advantages of Corticosteroid preparations?

A

Can Be Given in Large Doses IV

Relatively Rapid Onset Because of Route

Especially Important in Shock,

IHA/ITP and Severe Allergic Reactions

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11
Q

Indications of Corticosteroids

A

Reduce Inflammation

Reduce Pain

“Feel Good” Drugs

Relive Pruritis (Itching)

Reduce Scarring by Delaying Healing

Reduce Tissue Damage

Treats Shock

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12
Q

Contraindications / Side Effects of Corticosteroids

A

Stimulate Breakdown of Glucose Stores Causing Hyperglycemia

Inhibit Fibrocartilage Growth

Decrease Immune Response by Inhibiting Lymphocytes

Also Neutrophils and Macrophages

Catabolic Effects – Break Down Protein

Weakened Musculature

Thinning of Skin

Hair Loss

Decreased Bone Density

“Iatrogenic” Cushing’s Disease

Induced Abortions

Polyuria/Poldipsia/Polyphagia

Decrease or Inhibit the Release of Stomach Protective Prostaglandins

May Result in Stomach Ulcers due to Increase in Gastric Acid Volume and Decrease in Gastric Acid pH

Elevated Liver Enzymes

Steroids Should Be Discontinued Slowly When Used Long Term

Quick Withdrawal = Negative Feedback on Hypothalmus = Addisonian Crisis

Leads to Imbalance of Electrolytes

Increased Potassium / Decreased Sodium

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13
Q

What precautions should be taken for the safe use of steroids

A

Use of Nonsteroidal Antiinflammatory Medications whenever possible

Use of Herbal and Nutraceutical Therapies

Omega 3 Fatty Acids

Smallest Dose Possible That Provides Clinical Response

Apply Locally Whenever Possible

Maintains Normal Adrenal Cortex Function

Still Maintains a High Local Level of Corticosteroid

Avoid Continuous Use Due to Negative Feedback and Adrenal Atrophy

Iatrogenic Cushing’s Disease

Caution With Pregnant Animals

Will Terminate Late-Stage Pregnancy

Remember Steroids DO NOT Cure Any Specific Disease!!

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14
Q

What are NSAIDs

A

Nonsteroidal Anti-Inflammatory Drugs

Decrease Inflammation Without the Use of Steroids

Work By Inhibiting Two Forms of Cyclogenase

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15
Q

List the differences between Cyclogenase-1 and Cyclogenase-2

A

Cyclogenase-1

Commonly Called COX-1

More Involved With the Stomach Hence GI Effects

Gastric Ulceration and Bleeding

Cyclogenase-2

Commonly Called COX-2

More Involved in Inflammation

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16
Q

What are the adverse effects associated with NSAIDs?

A

Some Species Are More Tolerant Than Others (Horses > Dogs > Cats /Also Individual Variation Between Patients)

Highly Bound to Albumin in the Blood Stream

Low Albumin May Increase Circulating NSAID’s

Liver Disease

Young or Old Animals

Supposedly Fewer Side Effects Than Glucocorticoids

Main Adverse Effect is GI Distress

Vomiting/Diarrhea

Gastric Ulcers and Bleeding Due to Inhibition of Prostaglandins

Increase in Gastric Acid Volume

Decrease in Gastric Acid pH

Increase Pepsin

Decrease Gastric and Enteric Mucus Production

Hepatotoxic

Bone Marrow Suppression

Reduced Platelet Aggregation Causing Decreased Clotting Ability

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17
Q

What are the need to know NAIDS?

A

Phenylbutazone, Aspirin, etodolac, flunixin meglumine, meclofenamic, Propionic Acid Derivatives, carprofen

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18
Q

phenylbutazone

A

(Butazolidin® = “Bute”)
- Pyrazolone derivative
- Commonly Used in Horses
- Pain Associated With Musculoskeletal System
- Mild to Moderate Analgesic, Antipyretic, and Anti-Inflammatory
- Metabolized by Liver to Form Oxyphenbutazone
- Highly Protein Bound
- Careful Giving to Animals With Low Albumin
- Adverse effects include GI ulcers in horses if used in high doses, and renal papillary necrosis if dehydrated or pre-existing renal compromise
- Well tolerated in dogs, less data available for cats
- Not used in humans due to bone marrow suppression
- Paste, Tablet, Powder, Bolus for Oral use, Topical Gel, IV injectable, Tissue necrosis if injected S.C. or I.M.

19
Q

Aspirin

A

(Acetylsalicylic Acid)
- The Oldest Anti-inflammatory Agent
- Family of salicylate including bismuth subsalicylate (Pepto Bismol®)
- Inhibits the Cyclogenase Inflammatory Pathway Resulting in Decreased Prostaglandin Formation and Decreased Platelet Function
- Useful in Decreasing Platelet Aggregation by Blocking Thromboxane
- An Adjunct to Postadulticide Treatment of Heartworm Parasites (Reduces Platelet Clumping Associated With Narrowed Pulmonary Arteries)
- Heart Wall Disease (Anywhere There is Blood Turbulence)
- Blood Clots – Cats With Saddle Thrombus Disease
- Caution: Cats can’t Metabolize Aspirin as Rapidly as Dogs (Half Life in Dog = 8 Hours /Half Life in Cat = 30 Hours )

20
Q

etodolac

A

(Etogesic®)
- Indol Acetic Acid Derivative
- Anti-inflammatory and Analgesic for Osteoarthritis in Dogs
- Oral Preparation with Once Daily Dosing
- Side Effects: Vomiting, Diarrhea and Lethargy
- Is believed to be More Selective Inhibitor of COX-2
- Inhibits the Prostaglandins for Inflammation without affecting COX-1 (Therefore More Protective Effects of Prostaglandins for Stomach and Kidney)

21
Q

flunixin meglumine

A

(Banamine®)
- A Potent Inhibitor of Cyclogenase
- Potent Analgesic (onset in 15 minutes), Antipyretic, and Anti-Inflammatory
- Mainly Used for Musculoskeletal and Colic Pain (No. 1 Use in Horse for Colic)
- Also used for Shock, Intervertebral Disc Disease, and Pain Secondary to Surgery
- Blocks the Effects of Endotoxins (parvovirus)
- Labeled for Horses and Cattle (Used Off-label in Dogs and Other Species With Extreme Caution / Typically Only for Single Dose /Common to Have GI Side Effects)
- Although still labeled for both IV and IM injection, most equine clinicians avoid IM use due to risk of Clostridial infection
- Injectable solution is being used orally, but is off- label use

22
Q

meclofenamic acid

A

(Arquel®)
- Representative Drug of the Fenamate Group
- Cyclogenase Inhibitor
- Primarily an Analgesic and Anti-Inflammatory in Horses for joint pain and osteoarthritis (Accumulates in the Joint Fluid After Oral Administration)
- Comes in Granule Form that is Mixed in the Feed

23
Q

Propionic Acid Derivatives

A

The “fen” Group of NSAID’s
ibuprofen, ketoprofen, carprofen,naproxen
- Block Both Cyclogenase and Lipogenase
- Mainly used as analgesics
- Some are antipyretic and anti-inflammatory
- Adverse effects include nephrotoxicity and hepatotoxicity

24
Q

carprofen

A

(Rimadyl®)
- Commonly used for osteoarthritis pain, musculoskeletal pain and acute pain related to surgery or trauma in dogs (Believed to target COX-2, so less inhibition of prostaglandins associated with GI protection and renal blood flow)
- Liver toxicities have been documented, especially in Labrador Retrievers (Blood work to assess liver enzymes should be done 7-14 days after initiating therapy and periodically thereafter (every six months) )
- Injectable and tablets
- Approved for BID or SID dosing

25
Q

NSAIDs “Coxib Class”

A
  • COX-2 Inhibitors Newer category of NSAIDs developed to be more specific in their inhibition of COX-2, without interfering with the protective COX-1
  • Members include deracoxib (Deramaxx®), firocoxib (Previcox®, Equioxx®), and meloxicam (Metacam®), robenacoxib (Onsior®)
  • Uses in veterinary medicine mainly for control of inflammation and postoperative pain
26
Q

deracoxib

A

(Deramaxx®)
- Member of the COXIB class
- Used to decrease pain, inflammation, and fever
- Also indicated for osteoarthritis and control of postoperative pain associated with orthopedic surgery in dogs
- Available as chewable tablets that should be given after eating to increase bioavailability
- Adverse effects include v/d, anorexia, and elevated kidney and liver values
- Should perform bloodwork prior to initiating therapy

27
Q

firocoxib

A

(Previcox®, Equioxx®)
- Member of the COXIB class with the same indications for use in dogs as deracoxib
- Chewable tablets can be administered with or without food
- Formulated as an oral paste for horses to be given once daily for osteoarthritis (maximum 14 day regimen)
- Used in cats as single dose for fever reduction

28
Q

meloxicam

A

(Metacam®)
- Member of the oxicam class of COX-2 inhibitors
- Has anti-inflammatory, analgesic and antipyretic effects (Also inhibits leukocyte infiltration into the inflamed area)
- Used in dogs for alleviation of pain and inflammation due to acute/chronic musculoskeletal disorders and postoperative pain (Available as an oral suspension that is best applied to food)
- Used in cats as a one-time SQ injection for control of postoperative pain and inflammation
- Should not be used in animals with liver, cardiac, kidney or GI problems, or pregnant/lactating animals
- Adverse effects include v/d, anorexia, and lethargy
- Used in horses for pain/inflammation associated with surgery
- Used in pigs for mastitis/metritis

29
Q

robenacoxib

A

(Onsior®)
- Potent and selective COX-2 inhibitor
- Used for pain/inflammation of osteoarthritis in dogs and postoperative pain/inflammation in CATS
- Used orally or SQ injectable for three days in cats and long term for osteoarthritis in dogs (not approved for dogs in USA)
- Adverse side effects include v/d, GI ulcers, anorexia, behavior changes in cats (depression/restlessness)

30
Q

How do dual pathway NSAIDs work?

A

block both COX and LOX in the inflammatory pathway

31
Q

What is LOX inhibition?

A

LOX inhibition leads to decreased synthesis of inflammatory leuokotrienes along with inhibition of prostaglandins

32
Q

Diclofenac sodium

A

(Surpass®)
- is a non-specific COX-1 and 2 and has some LOX inhibition
- Available as a topical cream approved for use in horses to reduces pain and inflammation
- Local control of joint pain when applied topically to the hock, knee, fetlock and pastern joints
- Can be used for up to 10 days with minimal side effects
- Rubber gloves should be worn during application due to human absorption

33
Q

Superoxide Radical Deactivation

A
  • Superoxide radicals are produced by inflammation
  • Destroy tissue cells / Degrade hyaluronic acid (Main component of joint fluid, Is responsible for joint fluid viscosity/lubrication)
  • Agents in this group convert superoxide radicals into oxygen and water, thereby reducing cellular damage
  • Also called “free radical scavengers”
  • Includes dimethyl sulfoxide (DMSO, Domoso®) and orgotein (superoxide dismutase, Palosein®)
34
Q

dimethyl sulfoxide

A

(DMSO, Domoso®)
- Known for its ability to penetrate skin and is used off label frequently as a carrier of other medications
(Labeled for reduction of swelling via topical application for things such as lick granulomas and constricted ear canals / Used IV for treatment of various inflammatory conditions including CNS swelling )
- Available as a gel and solution
- WEAR GLOVES when applying topically as it will absorb readily into human skin
- Leaves a garlic smell/aftertaste
- Teratogenic in some species
- May cause skin irritation/burning of treated area

35
Q

orgotein

A

(superoxide dismutase, Palosein®)
- Similar in action to DMSO
- Used IM and Intra-Articularly in horses for joint disease (SQ in Dogs)
- Prevents destruction of hyaluronic acid /Prevents or reduces joint damage

36
Q

Glycosaminoglycans

A
  • Glycoproteins (proteoglycans) form part of the extra-cellular matrix of connective tissue such as cartilage
  • Proteoglycans resemble polysaccharides
  • Includes hyaluronic acid, glucosamine, chondroitin, and polysulfated glycosaminoglycans (PSGAGs)
37
Q

Essential Fatty Acids

A
  • Omega 3 and Omega 6 unsaturated fats
  • Increase cell membrane stability and have antioxidant activity
  • Found in fish and linseed oils
  • Good for skin, hair coat, joint and heart health
38
Q

Glucosamine and Chondroitin Sulfate

A
  • Considered Nutraceuticals
  • Play a role in the maintenance of cartilage structure and function
  • Help stimulate cartilage cell growth
  • Helps maintain cartilage strength and resilience
  • Helpful in the control of inflammation and pain associated with Osteoarthritis /Degenerative Joint Disease (DJD)
  • Many products and combinations available in tablet, capsule and food supplement forms
39
Q

hyaluronic acid supplement

A
  • hyaluronate sodium (Legend®, Hyalovet®)
  • Normally a part of joint fluid
  • Administered intra-articularly in horses to help cushion degenerating joints (Relieves joint pain and improves mobility)
  • Can also be administered IV in horses
  • Oral supplements available for small animals
40
Q

Polysulfated glycosaminoglycans

A

(PSGAGs)
- Appear in a drug called Adequan® that is a semisynthetic mix of glycosaminoglycans from bovine cartilage
- Can be given intra-articularly or IM in horses and dogs
- Similar to natural mucopolysaccharides found in cartilaginous tissues
- Inhibits proteolytic enzymes which degrade proteoglycans
- Promotes production of joint fluid from the synovial membrane and has some anti-inflammatory action

41
Q

methyl sulfonyl methane

A

“MSM”
- Dietary supplement form of sulfur that supports healthy connectibve tissue like tendons, ligaments, and muscles
- Adjunct therapy for arthritis seem in many combination products

42
Q

acetaminophen

A

(Tylenol®)
- Non-narcotic analgesic (NOT an NSAID)
- Limited antipyretic and anti-inflammatory effects
- Rarely used in veterinary medicine
- Conjugated with glucuronic acid in liver metabolism (Contraindicated in cats at any dosage / Toxic metabolites build up and cause the conversion of hemoglobin to methemoglobin)
- Can cause liver and kidney dysfunction in any animal
- Warn clients that it is toxic to animals!

43
Q

Antihistamines

A
  • Drugs that counteract the effect of Histamine
  • Histamine causes bronchoconstriction and inflammatory changes when released from mast cells
  • Antihistamines or H1 blockers compete with histamine for receptor sites, preventing histamine response (act as competitive antagonists)
  • Do not have an effect after histamine attaches to its receptor site
  • Does NOT prevent histamine release like steroids do
  • The three most commonly used in veterinary medicine are diphenhydramine (Benadryl®), chlorpheniramine (Chlortrimeton®), and hydroxyzine (Atarax®)
  • Have been shown to decrease steroid dose by as much as 50% when used in combination
  • Adverse effects include drowsiness, dry mucous membranes, decreased GI secretions, and CNS stimulation in high doses
44
Q

What are the two types of histamine receptors?

A

H1 - Constrict extravascular smooth muscles when stimulated, H1 blockers are used to treat pruritis, laminitis (large animals), motion sickness, anaphylactic shock and some respiratory conditions

H2 - Increase Gastric Secretions

VET - Pharm (17 decks)

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