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NSAIDs Flashcards

1
Q

What are eicosanoids?

A

Eicosanoids are potent and bioactive lipid signals that are generated from the essential Polyunsaturated Fatty Acid (PUFA) arachidonic acid. Every cell in your body can generate these lipid signals.

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2
Q

NSAIDs - Mechanism of Action

A
  • inhibit cyclooxygenase (synthesis PGs & TXA)
  • two cyclooxygenase enzymes (COX-1, COX-2)
    - COX-1 and COX-2 selectivity of NSAIDS
  • free radial scavengers (e.g. salicylate anti- oxidant), indirect effect inhibition of general eicosanoid formation
  • Aspirin covalent modification of enzyme
    – irreversible inhibition
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3
Q

steroids inhibit…

A

phospholipases

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4
Q

cox1 and cox2 inhibitors, aspirin, indomethacin inhibit

A

cyclooxygenase

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5
Q

prostacylin PGI2 causes

A

vasodilation, inhibits platelet aggregation

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6
Q

thromboxane A2, TXA2 causes

A

vasoconstriction, promotes platelet aggregation

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7
Q

Leukotriene causes

A

vasoconstriction, bronchospasm increased permeability

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8
Q

Lipoxin causes

A

vasodilation, inhibit neutrophil chemotaxis, stimulate monocyte adhesion

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9
Q

PGE causes

A

vasodilation, potentiate edema

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10
Q

NSAID general actions

A

anti-inflammatory, analgesic, antipyretic, platelet function
-analgesic: PG related, direct action on nerves pain amplification dorsal horn, inflammatory pain, analgesia superior to opioids for inflammation associated pain

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11
Q

cox1 vs cox2 structures

A

-both have different sized substrate channels
-cox2 has solvent accessible pocket which led to design of cox2 selective inhibitors

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12
Q

Common Systemic OTC NSAID drugs

A

aspirin, ibuprofen, naproxen
-tylenol not NSAID but analgesic, its MOA is not inhibition of cox and has no anti-inflammatory actions

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13
Q

NSAID Ophthalmic Use and drugs

A

initial use maintain pupil dilation post surgery
-flubiprofen: inoperative miosis, OL- postop inflammation, uveitis
-Ketorolac: pain, allergies, inflammation post-op OL: cystoid macular edema
-Suprofen (1%): intraoperative miosis OL: contact lens GPS
-Diclofenac (0.1%): intraoperative miosis, inflammation post-op, pain; OL: allergies
Nepafenac (0.1%): post-op pain & inflammation
Bromfenac (0.09%): post-op pain & inflammation

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14
Q

Applications of Ophthalmic Formulations

A
  • prevent intraoperative miosis (often coadministered with mydriatic)
    * effect small when used alone
    * effect slightly greater in light irides
  • prevent/treat cystoid macular edema
  • control post-operative inflammation &/or pain
  • prevent breakdown & re-establishing BAB (some equi-effective to corticosteroids)
  • allergies, ocular itching (seasonal, GPC)

Systemic NSAID’s
* adjunct to ophthalmic therapy
* more generalized effect (no benefit to ocular pain)

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15
Q

NSAIDs - Side Effects of Ophthalmic NSAIDs

A
  • rebound inflammation not seen
  • transient ocular irritation (stinging, burning, conjunctival hyperemia)
    * 15%, diclofenac to 40%, ketorolac
  • delayed wound healing, corneal melts (diclofenac, ketorolac, bromfenac, flurbiprofen?)
  • allergies
  • soft contact lens, ocular irritation (diclofenac, ketorolac)
  • Dry Eye complaints (12%)
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16
Q

NSAID Precaution & Drug Interactions

A
  • product-dependent (ophthalmic vs. systemic)
  • soft contact lenses (irritation/preservative issues)
  • older eyes + intraocular surgery
  • children?
  • pregnant women?
  • drug interactions (endogenous role of PG? cAMP?)
    * brimonidine, carbachol & NSAIDs (?)
    * PG analogs & NSAIDs (?)
17
Q

Additional Actions & Effects

A
  • aspirin irreversibly inhibits COX activity
    * low dose analgesic & “blood thinning”, reduced risk stroke & heart disease
    * high dose (12-20 tablets/per day) anti-inflammatory
    * reduced cancer risk (colon, prostate)
  • acetaminophen not anti-inflammatory
    * good antipyretic/analgesic activity
  • diflusinal no antipyretic activity (salicylate derivative)
  • diclofenac & indomethacin high potency anti-inflammatory drugs, not well tolerated
  • COX-2 inhibitors (celecoxib & meloxicam) more selectively anti-inflammatory? (no direct platelet effect-but COX-2 is constitutively expressed in the healthykidney, heart and some blood vessels)
  • interdrug variability in duration of action (hrs to weeks)
18
Q

Systemic Uses

A

symptomatic &/or anti-inflammatory
* analgesia (headache, dental, dysmenorrhea)
* fever
* corns, muscle sprains etc (topical salicylates)
* auto-immune diseases (e.g. rheumatoid arthritis)
* gout
* post surgery (pain control+)
* prophylaxis for colon cancer (aspirin, rofecoxib-vioxx)
* Cardiovascular uses (aspirin)

  • most administered orally
    (exceptions: topically for eyes & skin; intramuscular injections)
19
Q

OTC Drug Selection for Acute Conditions

A

short term analgesia
* acetaminophen
* ibuprofen/naproxen
* aspirin

Fever
* acetaminophen
* aspirin (low potency, blood brain barrier)
* Ibuprofen/naproxen

inflammatory pain and inflammation (cold, sprains, flu, etc)
* aspirin
* ibuprofen/naproxen

external applications (corns, muscle sprains etc)
* aspirin/salicylates (oil of wintergreen)
* salicylate – Acne cream/facial washes

20
Q

NSAIDs & Chronic Pain/Inflammation

A

chronic pain/inflammation/arthritis
* high dose aspirin
* naproxen
* piroxicam
* diflunisal
* celecoxib! [rofecoxib-Vioxx removed due to CV risk]
* meloxicam

special application of aspirin
* colon cancer (prophylaxis)
* cardioprotection, stroke

role for COX-II inhibitors?
* rheumatoid arthritis (platelet sparing, limit GI irritation)
* cancer [unacceptable CV risk]
* expensive and no better than aspirin for cancer prophylaxis

21
Q

NSAIDs Side-Effects & Drug Interactions

A
  • Side effects (virtually all cells have COX enzymes, fetal development)
    * problem of high doses, chronic use &/or potent drugs
    * numerous for most
    * reduced with selectivity? (COX-2 vs. 1- & 2- inhibitors)
    * even acetaminophen rel. dangerous (alcohol-hepatitis)
  • Drug interactions (PG regulate renal function)
    * problematic for most (clearance issues)
22
Q

Systemic SEs of Aspirin

A
  • GI distress/bleeding
  • prolongation of bleeding
  • hypersensitivity
  • Reye’s syndrome
  • indoleacetic acids generally high intolerance
  • less GI effects with proprionic acid derivatives
    & COX-2 selective inhibitors compared to aspirin
  • CNS effects
  • toxic doses (salicylism) can be deadly
23
Q

Salicylate toxicity symptom

A

tinnitus- ringing in the ears is first sign of poisoning

24
Q

Acetaminophen/Paracetamol Side Effects

A
  • acetaminophen hepatotoxicity
  • acetaminophen extremely toxic to cats and lethal to snakes
  • Post Hoc analysis of concluded that use of acetaminophen in the first years of life is associated with risk of severe asthma symptoms, rhinoconjunctivitis and eczema.
25
Q

NSAID Ocular Side-Effects

A
  • corneal erosion
  • corneal deposits
  • keratitis
  • corneal ulceration
  • retinal hemorrhage
  • epithelial breakdown

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