Chapter 13 - Antiinflammatories Flashcards
Inflammation
Protective mechanism that is designed to remove or neutralize the underlying cause of injury (physical, chemical, or biologic)
What are the 5 cardinal signs of inflammation?
1) Redness 2) Heat 3) Swelling/Edema 4) Pain 5) Loss of function
The two larger groups of antiinflammatory drugs used to reduce pain and discomfort
Steroidal antiinflammatory drugs and NSAIDs
Nociceptor
Pain receptor
Transduction
Conversion of physical change into a pain nerve signal
Pain pathway
Painful stimulus at nociceptor -> transduction -> transmission of pain along sensory nerves to the spinal cord -> modification and modulation of pain as it ascends spinal cord -> perception of pain signals the brain
Arachidonic Acid Cascade/Pathway
One of the principal mechanisms by which inflammatory mediators are generalized
What does the arachidonic acid cascade create?
Eicosanois -> enzymatically generates prostaglandins, leukotrienes and other inflammatory mediators
When trauma occurs to cell membranes what enzyme is activated?
Phospholipase
Phospholipase converts phospholipid molecules (that make up the cellular membrane) into what?
Arachidonic acid
What 2 enzymes may then act on Arachidonic acid?
Cyclooxygenase enzymes (COX) or Lipoxygenase enzymes
What do COX enzymes produce when they act on arachidonic acid?
Protaglandins and thromboxanes
What do Lipoxygenase enzymes produce when they act on arachidonic acid?
Leukotrienes
How do corticosteroids (specifically glucocorticoids) reduce inflammation?
By blocking the action of Phospholipase in the early portion of the pathway and reducing production of most of the inflammatory mediators (also blocks COX)
How do NSAIDs reduce inflammation?
NSAIDs inhibit COX (and to varying degrees) lipoxygenase - decreasing production of prostaglandins, leukotrienes and thromboxane) reducing inflammatory mediators, therefore decreasing the inflammatory effect of other inflammatory mediators (histamine, kinins, substance p and superoxide radicals)
Mineralcorticoids
Affect the minerals in the body (Na, K and other lytes) involved with water and electrolyte balance but have little to no antiinflammatory effect
Aldosterone
Mineralcorticoid hormone
What is aldosterones primary effect and use?
Increase the sodium retained in the body - Hypoadrenocorticism (Addisons)
What is Desoxycorticosterone Pivalate?
Percoten-V - mineralcorticoid, mimics effects of aldosterone and used to treat animals with addisons disease
Where are glucocorticoid receptors found in the body?
Found on ALL cells in the body, but Liver is primary systemic target for many glucocorticoid effects
What are the two natural glucocorticoids and what produces them?
1) Cortisol 2) Cortisone - Adrenal gland
How long do short-acting glucocorticoids exert their biologic activity on the body?
less than 12 hours (Hydrocortisone/cortisone)
How long do intermediate-acting glucocorticoids exert their biologic activity on the body?
12 to 36 hours (prednisone/prednisolone/methylprednisolone/Triamcinolone)
How long do long-acting glucocorticoids exert their biologic activity on the body?
48 hours or longer (Dexamethasone/Betamethasone/Flumethasone and Idoflupredone)
“Low” doses of glucocorticoids used to achieve normal physiology (addisons) are referred to as ____ doses.
Physiologic
“Medium” doses of glucocorticoids Supraphysiologc doses are referred to as ____ doses.
Antiinflammatory
“High” doses of glucocorticoids are referred to as ____ doses.
Immunosuppressive
