Anti-inflammatories and Corticosteroids Flashcards

1
Q

Prostaglandins are produced in almost all tissues and act _____

A

locally
(they don’t circulate in the blood)

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2
Q

Function of Prostaglandins

A
  • Modulate pain, inflammation, and fever
  • Control physiologic functions such as acid secretion and mucus production in the GI tract, uterine contractions, and renal blood flow
  • Released in allergic and inflammatory processes and direct inflammatory response
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3
Q

_____ is the primary precursor of prostaglandins
and is a component of the phospholipids of cell membranes

A

Arachidonic acid

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4
Q

Free arachidonic acid is released from _____

A

tissue phospholipids by phospholipase A2

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5
Q

Prostaglandins are synthesized from
arachidonic acid via the _____

A

cyclooxygenase pathway

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6
Q

COX enzymes functions

A

COX-1: Responsible for the physiologic production of prostanoids; “housekeeping functions, regulates normal cellular processes
COX-2: Causes elevated production of prostanoids that occur during chronic inflammation and cancer, Expressed in tissue such as brain, kidney, and bone

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7
Q

T/F COX-1 and COX-2 have differences
in binding site shape which allow
for selective inhibitors

A

T

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8
Q

NSAIDs (Nonsteroidal Anti-inflammatory Drugs) MOA

A

● Inhibit the synthesis of prostaglandins
● Primarily inhibit the cyclooxygenase enzymes that catalyze the first step in prostanoid biosynthesis

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9
Q

Aspirin is a _____ NSAID

A

Non-Selective NSAID

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10
Q

NSAID analgesic effects:

A

○ PGE2 sensitizes nerve endings so NSAIDs decrease PGE2 synthesis, which decreases pain sensation
○ Inhibiting COX-2 which is released during inflammation and injury and is thought to cause the analgesic effect

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11
Q

NSAIDs lower body temp by impeding ____
synthesis; essentially resetting the thermostat
towards normal

A

PGE2

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12
Q

Non-Selective NSAIDs

A

● Aspirin (ASA)
● Ibuprofen (Ibu, Motrin, Advil)
● Naproxen (Aleve)
● Diclofenac (Voltaren)
● Ketoprofen (Orudis)
● Piroxicam (Feldene)
● Meloxicam (Mobic)
● Indomethacin (Indocin)
● Ketorolac (Toradol)

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13
Q

NSAIDS most important effects

A

Anti-inflammatory
Analgesic
Antipyretic

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14
Q

Contraindications for NSAIDS

A

● NSAID induced asthma orurticaria
● Aspirin triad
● 3rd Trimester of Pregnancy
● CABG surgery periop use
● Hypersensitivity to NSAIDs

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15
Q

Additional contraindication for Indomethacin (NSAID)

A

Neonatal: renal impairment, active bleeding, necrotizing enterocolitis, congenital heart
disease

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16
Q

Additional contraindication for Ketorolac (NSAIDS)

A

Pre-op major surgery, CABG periop pain, labor
and delivery, coagulation disorders

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17
Q

NSAIDS BBWs:

A
  • increase risk of serious and potentially fatal GI adverse events such as bleeding, ulcers, and stomach or intestine perforation
  • increase risk of serious and potentially fatal
    cardiovascular thrombotic events, including MI and stroke; contraindicated for CABG perioperative pain
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18
Q

____ is an NSAID with indications for more moderate to severe pain

A

Ketoralac

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19
Q

NSAIDs Side Effects (Common)

A

● Stomach upset
● Dyspepsia
● N/V
● HA
● Dizziness
● Anemia
● Peripheral edema
● Hemorrhage
● Urinary retention
● Cough
● Diarrhea

20
Q

NSAIDs Adverse Reactions (Major):

A

● GI bleeding
● GI ulcers
● Hemorrhage
● Prolonged bleeding time
● HTN
● MI
● Anaphylaxis
● Nephrotoxicity
● Hepatotoxicity
● Stevens-Johnson syndrome
● Toxic Epidermal Necrolysis

21
Q

Avoid NSAIDs in pts with ____

A

asthma

22
Q

Why we should Avoid NSAIDs in the 3rd trimester of pregnancy

A

○ Can cause premature closing of ductus arteriosus
○ Acetaminophen is preferred during pregnancy

23
Q

NSAIDs prevent the synthesis of ___ and ___, which
maintain renal blood flow especially in marginally functioning kidneys

A

PGE2 and PGE1

24
Q

T/F Aspirin Only exhibits anti-inflammatory properties at high doses

A

T

25
Q

Aspirin is An _____ inhibitor of cyclooxygenase activity

A

irreversible

26
Q

Indications for Aspirin

A

● Fever
● Reduce risk of CV events → MIs, TIAs, CVAs
● Mild pain

27
Q

Contraindications for Aspirin

A

● Avoid in pts <20 yrs old with
viral infections → Reye
syndrome
● Pts with gout
● Pts taking probenecid
● Aspirin Triad (asthma, nasal
polyps, aspirin sensitivity)
● GI bleeds/Active PUD
● G6PD Deficiency
● Uncontrolled HTN
● Coagulation disorders

28
Q

Side Effects (Common) for Aspirin:

A

● GI pain
● Ulcers
● GI bleeding
● N/V
● Dizziness
● Rash
● Tinnitus

29
Q

Adverse Reactions (Major) in Aspirin:

A

● Hemorrhage
● Reye Syndrome
● Nephrotoxicity
● Anaphylaxis
● Bronchospasm
● Renal failure
● GI perf/ulcer

30
Q

Selective NSAIDS

A

Celecoxib (Celebrex): Selective to COX-2 inhibitors

31
Q

Celecoxib MOA

A

MOA: selective for inhibition of COX-2 rather than COX-1
Intended to preserve gastric cytoprotective effects that are
mediated by COX-1 while maximizing the anti-inflammatory
effects mediated by COX-2

32
Q

Indications for use of Celecoxib

A

● Approved for the treatment of RA and OA
● Acute mild to moderate pain

33
Q

Contraindications of Celecoxib

A

● Use caution in pts with sulfonamides allergy or who have
had anaphylaxis reactions to aspirin or other NSAIDs
● Avoid in pts with severe hepatic or renal disease

34
Q

Side effects of Celecoxib

A

HA, dyspepsia, diarrhea, and abdominal pain

35
Q

Corticosteroid Secretion

A
  1. Stress → CRH (corticotropin-releasing hormone) releases from the hypothalamus
  2. ACTH (adrenocorticotropic
    hormone) releases from the anterior pituitary
  3. Cortisol releases from the adrenal cortex which inhibits feedback
36
Q

Glucocorticoid Properties

A

Anti-inflammatory
Immunosuppressive
Increase resistance to stress

37
Q

Glucocorticoid Properties

A
  • Promote normal intermediary metabolism
  • Alter blood cell levels
38
Q

______ → acts on distal tubules and collecting ducts,
causes reabsorption of sodium, bicarbonate, and water. Also
decreases reabsorption of potassium which, with H+, is lost in
urine

A

Aldosterone

39
Q

Glucocorticoids MOA

A

● Largely unknown
● Influence the inflammatory response by stabilizing mast cell
and basophil membranes, resulting in decreased histamine
release

40
Q

Short Acting Glucocorticoids

A

● Hydrocortisone (Cortef)
● Cortisone (Cortone)

41
Q

Intermediate Acting Glucocorticoids

A

● Prednisone (Sterapred)
● Prednisolone (Orapred)
● Methylprednisolone (Medrol)
● Triamcinolone (Kenalog)

42
Q

Long Acting Glucocorticoids

A

● Betamethasone (Diprolene)
● Dexamethasone (Decadron) - first line treatment for croup

43
Q

Mineralocorticoids

A

Fludrocortisone (Florinef)

44
Q

Glucocorticoids Indications

A

● Inflammatory conditions: RA, skin issues, asthma maintenance control, asthma exacerbations, active inflammatory bowel disease
● Allergies: allergic rhinitis, drug allergic reactions
● Acceleration of lung maturation
● Diagnosis of Cushing syndrome
● Replacement therapy for adrenocortical insufficiency

45
Q

Glucocorticoids side effects

A

● Increased appetite
● Weight gain
● Emotional disturbances
(There is more but these are most common Lauren said)

46
Q

Major Reactions (Major) of Glucocorticoids:

A

● Adrenal insufficiency
● Anaphylaxis
● Cushing syndrome
● DM
● Seizures
● GI perf
● Hypokalemic alkalosis

47
Q

Follow up/Monitoring of Glucocorticoids:

A

● Caution in pregnancy
○ Prednisone- preferred, minimizes effects on the fetus
● Caution with abrupt discontinuation of medication
○ May cause adrenal suppression
○ Suggest tapering