Ch 15 1 Pharm

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jld15
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303866
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Ch 15 1 Pharm
Updated:
2015-06-09 17:04:21
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15 Pharm
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Ch 15 1 Pharm
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  1. NSAIDs extra
    • Can be used as anti-cancer drug but since most cells have prostaglandins side effects
    • Higher the dose higher the side effect
  2. Nonsteroidal Anti-Inflammatory Drug Objectives
    • Decrease inflammation
    • Relieve mild-to-moderate pain (Analgesia)
    • Decrease elevated body temperature (Antipresis)
    • Decrease blood clotting (Anticoagulation)
  3. Why is Acetaminophen is not considered an NSAID
    Bc not anti inflammatory or anticoagulant
  4. Prostaglandins
    • Lipid-like compound that exhibits a wide range of physiologic activities
    • Every cell except RBC’s produce prostaglandins
    • --- so NSAID’s can affect most organs and tissues
    • Pro inflammatory: trauma or change increases synthesis
  5. Thromboxane
    • Derived from same precursor as prostaglandin; COX enzyme
    • cause clot fomation
  6. Leukotrienes
    • Mediate airway inflammation conditions (asthma, allergic reaction)
    • Pro inflammatory
  7. Eicosanoids
    Prostaglandins, thromboxanes, and leukotrienes
  8. Excessive Prostaglandin Synthesis Repercussions
    • Local Inflammation
    • ----PGE2 mediate local erythema and edema
    • --------Increasing blood flow
    • --------Increasing capillary permeability
    • --------Increase permeability of histamine and bradykinin
    • ----LTB4: leukotrienes
    • --------Increase vascular permeability
    • Pain
    • ----Increase sensitivity of pain receptors
    • Fever
    • ----Pyrogenic: help produce elevated body temp during fever
    • ----Promote fever by stimulating vagal afferent neurons
    • Dysmenorrhea
    • Thrombus formation (clot formation)
    • ----TXA2: cause platelet aggregation
    • Others:
    • ----Hypertension
    • ----Neoplasms (colon cancer)
    • ----Respiratory dysfunction (asthma)
    • ----Neurologic disorders (MS)
    • ----Allergic encephalomyelitis
    • ----Affect disorders
    • ----Endocrine dysfunction (Bartter syndrome, DM)
  9. Mechanism of Action: NSAID’s
    • Potent inhibitor of cyclooxygenase (COX enzyme)
    • ----Blocks production of prostaglandins and thromboxanes
    • COX-1 and COX-2 enzymes
  10. COX-1
    needed for normal cellular activity and prostaglandin synthesis to help maintain function of organ
  11. COX-2
    • produced from injured cells
    • That’s why we have cox-2 inhibitors
  12. Aspirin
    • Acetylsalicylic acid
    • Best representative of an NSAID
    • Inhibits prostaglandin synthesis
  13. Aspirin uses
    • Pain and inflammation
    • ----Headache
    • ----Toothache
    • ----Diffuse muscle aches
    • ----Cramps with dysmenorrhea
    • ----Pain following surgery
    • ----Decrease need for opioids
    • Fever
    • ----Contradicted in children
    • Vascular disorders
    • ----Inhibits platelet clotting through inhibition of thromboxane biosynthesis
    • --------Preventing MI, stroke
    • Prevention of cancer
    • ----Inhibit prostaglandins that promote tumor growth
  14. Aspirin Adverse effects
    • GI problems
    • ----hemorrhage and ulceration
    • --------Due to loss of protective prostaglandins in mucosal lining
    • Hepatotoxicity (high doses)
    • Acute renal failure (ARF)
    • Overdose
    • Reye syndrome
    • May delay healing
    • ----Inhibition of prostaglandins retards bone healing and formation of new bone
    • ----Inhibit synthesis and transport of CT components such as proteoglycans

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