Pharm7 Flashcards by Jordan Cartwright

Inflammation

Body’s response to injury
• Intended to be a protective mechanism to remove or neutralize the cause of the damage
Lead to repair of any damage

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What can cause Inflammation?

Trauma,
infection,
burns

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External clinical signs of inflamation

o Redness and heat =vasodilation
o Swelling and edema =increased vascular permeability- can dilute irritating chemical
o Pus =WBC’s that remove bacteria, debris, and devitalized tissue
Can be painful

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Two types produced by the adrenal gland

 Mineralocorticoids-regulate mineral levels in the body

 Glucocorticoids-exert an anti-inflammatory effect, but also have many other effects in the body

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Mineralocorticoids

regulate mineral levels in the body

Aldosterone- Sodium/ water

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Biologic effects of glucocorticoids in the body

o	Decrease inflammation
o	inhibit scar tissue formation
o	Suppress the body’s immune system
o	Affect the cellular blood count
o	Increase gastric acid secretion and decrease mucus production in GIT
o	Increase protein breakdown
o	Can induce parturition
o	Increase blood glucose levels

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Aqueous solutions of glucocorticoids

the glucocorticoid is combined with a salt and dissolved in water
can be given in large doses intravenously w/ less risk of an adverse reaction
examples: dexamethasone sodium phosphate (Azium), prednisolone sodium succinate (Solu-Delta Cortef)

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Alcohol solutions of glucocorticoids

glucocorticoid is dissolved in alcohol
the label lists the glucocorticoid as the only active ingredient
increased risk of an adverse reaction if given IV

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Suspensions of glucocorticoids

the glucocorticoid is suspended in a liquid vehicle(e.g. acetate, diacetate, pivalate, acetonide, valerate)
store at room temperature
must be shaken before use
glucocorticoid is absorbed gradually over a period of days
should never be administered IV
examples: methylprednisolone acetate (Depo-Medrol), triamcinolone acetonide (Vetalog)

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Guidelines for safe use of glucocorticoids

o Use another drug if it can accomplish the same result
o Use the smallest dose possible
o Avoid continuous use
o Be cautious when using glucocorticoids with long-lasting effect
o When discontinuing, reduce dose over a period of days
o Use may be contraindicated in some patients

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Parenteral formulations

Aqueous solutions
Alcohol solutions
Suspensions

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Dosage forms available

topical preparations,
oral and
injectable products

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Short-acting

biologic effect lasts < 12 hrs.

• hydrocortisone, cortisone- usually topically

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Intermediate-acting

effect lasts 12-36 hrs.
• prednisone, prednisolone, triamcinolone, methylprednisolone
Orally, at least once a day

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Long-acting

effect lasts more than 48 hrs.
• dexamethasone, betamethasone, flumethasone
injectable or oral

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Nonsteroidal Anti-inflammatory Drugs

(NSAIDs)
• Exert their effect by blocking enzymes in the inflammatory cascade
Interfere of arachidonic acids, and with
• Produce fewer side effects than glucocorticoids
• Highly bound to plasma proteins

Adverse effects of Nonsteroidal Anti-inflammatory Drugs include:

o GI tract- anorexia, diarrhea, melena (blood in the feces- digested), ulcer formation
 effect due to decreased protective prostaglandin production (PGE, PGI2)
o Kidney- renal tissue necrosis
 effect due to decreased protective prostaglandin production (PGE2)

Things PGI, PG12 do

o Decrease volume and acidity of gastric secretions- acid favors ulcers
o Increase NaCO3 secretion in intestinal tract- protect from ulcers
o Increase gastric and intestinal mucus production- prevent ulcers
o Increase turnover and repair of GI epithelial cells- prevent ulcers

NSAID list

o	Phenylbutazone 
o	Flunixin Meglumine 
o	Ibuprofen, Ketoprofen, Naproxen-
o	Acetylsalicylic Acid
o	Caprofen, Meloxicam, Deracoxib Etodolac, Firocoxib

Phenylbutazone

• Phenylbutazone
o Used mostly in horses
o Available in tablet, paste, and injectable forms

General characteristics of Phenylbutazone

	Inhibits cyclooxygenase
	Metabolized by the liver
	Highly protein bound
	Adverse effects include GI ulceration, renal  necrosis, retention of water and sodium, bone marrow suppression
	Cats have a very low tolerance

Flunixin Meglumine

• Flunixin Meglumine
o Mostly used in horses
o Available as an injectable, paste and granules for oral administration

General characteristics of Flunixin Meglumine

 Has potent analgesic properties
 Used to relieve severe pain in horses
 Adverse effects include GI ulceration after 3-4 days of use in dogs

Ibuprofen, Ketoprofen, Naproxen

o Commonly used in humans, ketoprofen (Ketofen) and naproxen (Equiproxen) sometimes used in animals

General characteristics of Ibuprofen, Ketoprofen, Naproxen

 All derived from propionic acid, have similar qualities  Inhibit cyclooxygenase and lipooxygenase  Adverse effects include GI ulceration after days of use in dogs

Acetylsalicylic Acid

o Commonly used human drug o Decreases platelet aggregation by decreasing thromboxane production o Metabolized in liver by binding it w/ glucuronic acid for elimination o Safer than most older NSAIDs

Carprofen (Rimadyl), Meloxicam (Metacam), Deracoxib (Deramaxx), Etodolac (Etogesic) Firocoxib (Previcox)

o Newest group of NSAID agents o Referred to as COX-2 inhibitors o Less likely to cause adverse effects than other NSAIDs  selectively inhibit production of prostaglandins associated w/ inflammation  minimal effect on GI tract and kidney o A low incidence of liver disease, renal disease, hematologic abnormalities, and serious GI disease reported

Galliprant

o Belongs to a new drug class o Blocks prostaglandin receptor associated within inflammation (EP4) ONLY Different target- alternative to COX2 Bind receptor in tissue to prevent the binding of inflammatory prostoglandics Acts like an antagonist

Acetaminophen

o (Tylenol) • Provides analgesia, fever reducer • No GI ulceration, no anti-inflammatory effect • Metabolized by liver • *Toxic metabolite produced which is bound to glutathione rendering nontoxic • Adverse effects seen w/ overdose • *Methemoglobinemia, Heinz body formation, liver tissue destruction

Chemical mediators of inflammation

Prostaglandins, thromboxanes, leuktrienes

Corticosteroids

Hormones produced by the adrenal gland | o Corticosteroid production is regulated by a feedback inhibition mechanism

Glucocorticoids

exert an anti-inflammatory effect, but also have many other effects in the body produced by adrenal gland -Cortisone, Hydrocortisone (cortisol)

The adrenal gland produces:

Cortex- hormones, androgens, mineralocorticoids | Medulla- epinephrine, norepinephrine

CRF

Corticotrophin Releasing factor | hypothalamus

Cushings Disease

too much glucocrodicoids | usually pituitary related

Iatrogenic

when we overssuppulent with glucocrodicoids, and cause cushings

PGE2

help to main normal blood flow to the kidney it is low, such as dehydration, shock - when there is decreased blood flow to the kidney –>PGE2-> dilate arteries to the kidney

Methemoglobinemia

oxidation of the iron in the hemoglobin molecule- affect oxygen carrying capacity

Phenacetin

converted into acetaminophen in the body