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Pharm II
NSAIDs
43
Pharmacology
Professional
03/26/2014

Additional Pharmacology Flashcards

 


 

Cards

Term
Clinical Obj of Pain Mgmt
Definition
Minimize debilitating pathologic pain while maintaining the protective aspects associated with physiologic pain
-preemptive analgesia
-balanced analgesia
-dose to effect case by case
Term
Importance of Pain Assessment
Definition
-Can be difficult to assess
-recognize behavior associated with pain
-chronic pain is more difficult to recognize
-anticipate levels of pain associated with surgical procedures, illness, or injuries
-physiologic parameters are NOT good indicators
Term
Inflammatory pain
Definition
-Vasodilation of local blood vessels
-Increased perm of capillaries
-granulocytes and monocyte migration
-swelling of the tissue
*Release of inflammatory mediators*
-activation of macrophages
Term
Good COX, Bad COX
Definition
-Not all Cox-2 is inducible
-Cox-1 derived PG's might mediate pain, inflammation and fever
-Cox-2 also involved in gene expression, neoplasia, bone modeling
-Some Cox-2 selective only effective at doses high enough to also inhibit Cox-1
-Cox-2 are generally safer in the GI tract
Term
PK of NSAID's
Definition
-well absorbed orally (some exceptions)
-lipophilic and low Vd
-Very high plasma protein binding
-mostly elim by liver
-extensive enterohepatic recycling in some cases
Term
Drugs Interxns with NSAID's
Definition
-Furosemide (synergistic incerase of kidney tox)
-ACE inhibitors (suppress vasodilation effects, increased renal tox)
-Fluoroquinolones (may decrease seizure threshold)
-Aminoglycosides (NSAID's may increase their renal toxicity effects)
-Antacids (interfere with absorption)
Term
Adverse effects of NSAID's
Definition
-mediated by inhibition of protective PG's
-Cats may be more sensitive to toxicity due to the lack of glucoronidation pathway
-enterohepatic circulation in dogs
Term
GI tox
Definition
-most common dose-limiting factor
-avoid concurrent use with glucocorticoids
-GI adaptation
-prevent toxicity when used long term by giving GI protectants (sucralfate) and synthetic PG's
Term
Renal Tox
Definition
-decrease renal blood flow
-decrease glomerular filtration
-major concern in:
-periop period
-hypotensive, hypovolemic situations
-CKD
-CHF
Term
Hematological and Liver Tox
Definition
-NSAID's can cause idiosyncratic hepatotox in dogs (related to individual's sensitivity to drug)
-Avoid with bleeding disorders
-avoid during sx where hemorrhage may be a problem
Term
Question:
Which of the following is the most common concern with chronic NSAID use?
Definition
development of GI ulcers
Term
Question:
How can you best prevent the development of the occurrence of GI ulcers?
Definition
Titrate dose to a minimum
Term
General Principles of NSAID use
Definition
-Monitor: renal, liver, and coag status
-Cytoprotective measures
-Apply preemptively
-Avoid high doses
Term
Aspirin
Definition
-Preferential COX-1 inhibitor
-oral only
-Metabolized by LIVER (accumulates in cats due to glucuronide conjugation)
-Metabolites excreted by kidneys (tubular absorption depends on pH)
Term
Aspirin Uses
Definition
-analgesic, anti-inflammatory, antiplatelet
-Antiplatelet effect good with HW and feline thromboembolism
Term
Aspirin Adverse Effects
Definition
-GI irritation
-Decrease clotting (stop 1 week prior to sx)
-Cartilage damage in arthritic dogs?
Term
Question:
Which of the following is true about aspirin?
Definition
It can be used as a blood thinner
Term
Phenylbutazone
Definition
-IV and oral
-Cox-1 inhibitor
-good absorption and wide dist
-nonlinear PK (@ high doses or chronic use, the metabolism becomes saturated and the drug can accumulate)
-Therapeutic efficacy for 24 hrs
Term
Phenylbutazone Uses
Definition
-Large and food animals

Cattle: prolonged 1/2 life; used for arthritis and mild laminitis; PROHIBITED IN DAIRY COWS

Horses:
-cheap and effective
-chronic therapy --> decrease dose and increase interval
Term
Phenylbutazone Adverse Effects
Definition
-GI are most important in herbivore
-Renal (chronic use)
-blood dyscriasis in dogs
Term
Question:
Which of the following can be expected with long term use of Bute in horses?
Definition
Drug elim decreases after awhile and dose needs to be decreased
Term
Flunixin Meglumine (Banamine)
Definition
-very potent COX inhibitor (mostly COX-1)
-oral and injectable
-fast absorption with 80-90% bioavailability
-wide dist
- 1/2 life varies by species
Term
Flunixin Meglumine Uses
Definition
Horses:
-colic, colitis, endotoxic shock, resp and ocular dz, laminitis
-low dose so as to not mask colic signs

Cattle:
-acute coliform mastitis with endotoxic shock, resp dz, septicemia, pain

Dogs:
-musculoskeletal disorders, endotoxic shock, sx
-tx beyond 3 days is toxic
Term
Flunixin Meglumine Adverse Effects
Definition
-similiar to Bute (GI, renal, dyscriasis)
-IM injections are irritant (clostridial myositis in horses)
Term
Ketoprofen
(anafen)
Definition
-Inhibits more COX-1 than COX-2
-used in dogs, cats, horses (post-op and chronic use--> not to be used pre-op due to bleeding)
-effects like 12-24 hrs
-one of the safest orally in SA (esp cats)
-less toxic than Banamine in horses

-Cattle: tx of E. coli endotoxic induced mastitis
Term
Question:
Which of the following NSAID's is more appropriate in the tx of acute mastitis in dairy cattle?
Definition
Flunixin and Ketoprofen

CANT USE BUTE- PROHIBITED
Term
Carprofen (Rimadyl)
Definition
-Chronic and perioperative pain tx in dogs
-greater effect on COX-2
-safe in cats after single dosing
-Min antithromboxane activity
-Idiosyncratic liver tox in dogs is possible
Term
Piroxicam (Feldene)
Definition
-Cox-1 inhibition
-very long 1/2 life in dogs (40hrs)
-infreq dosing
-enterohepatic recycling
Term
Piroxicam Uses
Definition
Dogs:
-tx of inflammation associated with TCC, cystitis, urethritis
-antitumor activity in TCC (acts as immunomodulator)
Term
Piroxicam Adverse effects
Definition
-GI tox
Term
Meloxicam (Metacam)
Definition
-COX-2 inhibition
-oral syrup and injectable form
-osteoarthritis, post-sx
-safer than piroxicam
Term
Etodolac (Etogesic)
Definition
-COX-2
-chronic arthritis in dogs
-well absorbed orally
Term
Deracoxib (Deramaxx)
Definition
-COX-2 inhibition
-chronic tx of pain and inflammation
-good oral absorption
-drugs excreted with bile and feces
-nonliner elimination
-safe
Term
Firocoxib (previcox)
Definition
Cox-2 inhibition
-large volume of dist.
-chronic tx of pain and inflammation
-Drug excreted with bile and feces
Term
Robenacoxib (onsior)
Definition
Dogs:
-tx of pain and inflammation assoc with chronic osteoarthritis
-no time limit for tx

Cats:
-tx of acute pain and inflammation assoc with musculo-skeletal disorders
-tx up to 6 days
Term
Tepoxalin (Zubrin)
Definition
-COX/LOX
-osteoarthritis in dogs
Term
Naproxen (Aleve)
Ibuprofen (Advil)
Definition
-very potent OTC drugs
-COX-1
-considerable tox in dogs and cats
-enteroheptaic recycling
Term
Acetominaphen (Tylenol)
Definition
-acts only on centrally prod COX
-TOXIC IN CATS due to lack of glucoronidation enzymes
-safer in dogs
Term
Question:
Which of the following NSAID's is contraindicated in dogs?
Definition
Naproxen
Term
Question:
Based only on its MOA, which of the following drugs is less likely to impact the GI with long-term usein dogs?
Definition
Etodolac (Etogesic)
Term
Question:
Which of the following NSAID's exhibits a low 24% plasma protein binding?
Definition
None of them
Term
Question:
Which of the following is FDA approved for use in cats?
Definition
Robenacoxib (onsior)
Term
Which of the following can be expected with long term use of acetaminophen in cats?
Definition
The need to buy another cat (ha, he made a funny =p )
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