Nsaids Et Al

Front 1

COX1 vs COX2
Location

Back 1

COX 1: constitutive, blood vessels, stomach, kidney
COX 2: induced in inflammation (constitutive in Brain, Kidney, Bone)

Front 2

Thromoxanes (TXA) vs Prostaglandins (PG) vs Prostacyclins (PGI)

Back 2

TXA -> Platelet aggregation, vasoconstriction, inflammation
PG (PGE2) -> erythema, pain, vasodilate, bronchoconstrict, pyrogenic, hyperalgesia
PGI (Prostglandin I2) -> vasodilate, inhib platelet aggregation, bronchodilate

Front 3

Aspirin MOA
(Acetylsalicylic acid)

Back 3

Acetylate covalently cyclooxygenase (COX) -> irreversible inhibition
(all others reversible)
Periphery: ↓ PG -> anti-inflamm
CNS: ↓ pyrogen-induced PGs & CNS response to interleukin-1 -> reset hypothalamic set-point & vasodilation -> ↑ heat loss & sweating

Front 4

Aspirin physiological effects

Back 4

Antipyretic
Anti-inflammatory
↓ chemotaxic factors in Mф, stabilize lysozome, inhibit migration of PMN, leukocytes, & Mф -> symptomatic relief of inflammation (NOT progression of actual pathology)
Anticoagulant
Irreversible inhibition of COX -> ↓ TXA2 -> ↓ platelet aggregation -> ↑ bleeding time (lasts 8-10 days)
Effect on respiration:
Direct -> respiration center -> ↑ respiration (High doses -> ↓ respiration through medulla)
Indirect -> via CO2 -> ↑ respiration
Effect on GI:
Epigastric distress, NV, blood loss, local irritation, ↓ gastric PGs (also: ↓ mucus & bicarb secretion; ↑ acid secretion)
Uricosuric effect (↑ uric acid excretion)

Front 5

Aspirin indications

Back 5

mild/moderate pain
Fever (caution peds)
Inflammation (RA, etc)
Vascular disease (low dose)
Colon Cancer

Front 6

Aspirin metabolism

Back 6

Rapid absorb in stomach/upper small intestine
Wide distrib
Hydrolyze -> conjug (Saturates enzymes at high dose -> ZOK; T1/2 increase 2 -> 12 hrs)

Front 7

Aspirin OD treatment

Back 7

1) Emesis or lavage (w/ activated charcoal);
2) Alkalinize urine & hemodialysis (promote elim)
3) symptomatic treatment

Front 8

Salicysm symptoms

Back 8

Mild: Headache, TINNITIS, Sweating, N/V, dizzy, deaf
Severe: Coma, Metabolic acidosis

Front 9

OD Signs

Back 9

Adults: ↑ respiration -> alkalosis
Peds: Acidosis (↑ [ASA]); Hyperthermia
CNS disturb (agitation, confusion, convulsions, coma

Front 10

Aspirin uses

Back 10

1) Anti-inflamm
2) Analgesia
3) Antipyretic
4) Antiplatelet (inhibit COX -> no thromboxane in platelet; endothelial cells can recover)

Front 11

Aspirin side effects

Back 11

Epigastric distress (Nausea/vomiting); CV disorders
Coagulation disorders
Renal toxicity
Hypersensitivity
Reyes syndrome (peds)

Front 12

Reyes Syndrome

Back 12

severe hepatic injury & encephalopathy during viral infection (influenza & varicella) while taking ASA
("Rey hit in HEAD by a LIVER")

Front 13

Salsalate

Back 13

increase price, less COX inhibition

Front 14

Diflunisal

Back 14

increase price, less COX inhibition
LESS ANTIPYRETIC effects

Front 15

Indomethicin uses

Back 15

inDOmethicin (DO = Ductus Orteriosus, misspelled)

Inflamm diseases (RA, osteoarthritis, ANKYLOSING SPONDYLOSIS, acute gout)
Fever from Hodgkin's

Front 16

Endings
- sal
- ac or acin
- profen/proxen
- fenam
- oxicam

Back 16

-sal = salicylate
-ac or -acin = Acetic acid derivative
-profen/proxn = Propionic acid deriv
-fenam = Fenamate
-oxicam = Oxicam

Front 17

Indomethicin MOA

Back 17

Potent COX inhibitor
Potent anti-inflammatory

Front 18

Indomethicin Side effects

Back 18

High incidence!
"DOh! hit HEAD, so frustrated get an ULCER"
GI: peptic ulcer/bleed, anorexia, N/V/D
CNS: severe HEADACHE, vertigo, depression
Hypersensitivity rxn

Front 19

Indomethicin contraindications

Back 19

Allergy (ASA or Indomethicin)
Pregnancy
Children
Hx of ulcer
Elderly

Front 20

Ketorolac side effects

Back 20

"countdown drug" can't use >5 days -> GI irritation, bleed, ulcer, hypersensitivity rxns

Front 21

Ketorolac uses

Back 21

moderate/severe pain for SHORT TERM (alternate to opioid)
Allergic Conjunctivitis & Ocular inflamm

Front 22

Diclofenac indications

Back 22

Actinic keratosis
Acute pain from strains/sprains (transdermal patch)
Enteric-coated tablets -> delayed release
"Clof (cloth) covers skin & joints"

Front 23

Diclofenac & Misoprostol use

Back 23

pt w/ high risk of ulcer
"Miso is good for your stomach"
(aka Arthrotec)

Front 24

Sulindac use

Back 24

Prodrug: less toxic, less potent than Indomethicin
use: same as indo (Ductus arteriosus, Inflamm disease)

Front 25

Ibuprofen indications

Back 25

Mild/moderate pain
Dysmenorrhea
Fever
RA
Low incidence adverse rxn

Front 26

Naproxen indications

Back 26

Mild/moderate pain
Protein bound -> LONG HALF-LIFE

Front 27

Ketoprofen indications

Back 27

mild/moderate pain
SHORT DOA (short half-life)
"Keto countdown again"

Front 28

Mefanamic acid indications and side effects

Back 28

"Mefanamic for My Female friend during that time of the month"
(for dysmennorhea, or myalgia)
Do NOT use over 1 wk or if renal function impaired

Front 29

Meclofenamate Indications and side effects

Back 29

RA, osteoarthritis
Mild/moderate pain

Front 30

Piroxicam use
Side effects
DOA

Back 30

RA
LONG DOA
GI side effects (50 hr)

Front 31

Meloxicam MOA
Effects

Back 31

COX-2 selective
Less GI side effects
Less Platelet inhibition
Kidney toxic

Front 32

Nabumetone MOA
Effects

Back 32

(prodrug) COX-2 selective
LESS GI irritaton, bleed, ulcer
RENAL toxic

Front 33

Celecoxib indications
MOA
Effects

Back 33

Anti-inflamm.; anti-pyretic; analgesic
COX-2 selective
NO platelet inhibition
LESS GI side-effects/ulcers
(May be pro-thrombotic - ↑ CV risk: all NSAIDS & Celecoxib)

Front 34

Acetaminophen (Tylenol) indications

Back 34

Alternate to ASA: analgesia, anti-pyretic
NO ANTI-INFLAMM
Bleeding disorders, Peptic ulcer, ASA intolerance, Pediatric w/ fever & risk of Reyes

Front 35

Acetominophen (Tylenol) MOA
Side effects

Back 35

less inhibition of peripheral COX & PG (may inhib COX-3); NOT anti-inflamm
Minimal side effects (no GI or antiplatelet)
OD -> hepatotoxic (exhaust GSH)

Front 36

Acetominophen OD MOA & signs

Back 36

OD c/o exhaust all GSH supply -> toxic metabolite -> liver necrosis
Signs: Anorexia, NVD, Abdominal pain -> Jaundice & hepatic fail, coma, death

Front 37

Acetominophen OD treatment and MOA of OD treatment

Back 37

Acetylcysteine: repletes GSH (Glutathione) to bind reactive metabolite

Front 38

Acetominophen side effects
interactions
Contraindications

Back 38

Chronic ingestion -> liver damage (esp. malnourish/alcoholics)
Interact: Alcohol, barbituates, phenytoin
Contraindicate: impaired liver function & alcoholism