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Pharm 2 Final - NSAIDS/Tylenol
NSAIDS/Tylenol
97
Health Care
Graduate
05/01/2009

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Cards

Term
60-81 mg of ASA will irreversibly inhibit _____________ production in PLTs and will inhibit their aggregation.
Definition
thromboxane
Term
Why should you D/C salicylates one week prior to surgery?
Definition
because they prolong BT
Term
Mild salicylate toxicity is called:
Definition
salicylism
Term
salicylism sxs include:
Definition

N/V

HA

mental confusion

tinnitis

dizziness

Term
Severe salicylate toxicity sxs include:
Definition

those of salicylism plus

restlessness, delirium, hallucinations,

convulsions, coma,

resp. & metabolic acidosis

and death from resp. failure

Term
How do you treat severe salicylate toxicity?
Definition

dialysis and

frequent correction of acid-base & electrolyte imbalance

 

Na Bicarbonate

Term
Acetaminophen uses:
Definition

mild analgesic

antipyretic

minimal anti-inflammatory effect

Term
How is acetaminophen metabolized?
Definition

1. by several pathways in the liver, excreted renally

 

2. a small portion is converted into a hepatotoxic metabolite by CYP 450

Term
How long does it take for acetaminophen toxicity to occur?
Definition
24 hours
Term
Ingestion of __________ mg of tylenol is enough to cause life-threatening hepatotoxicity?
Definition
6.5-9.5
Term
What can you use to treat tylenol toxicity?
Definition

Acetylcysteine

 

(it conjugates the intermediate compound and makes it harmless)

Term
What do you use to treat inflammatory arthritidies?
Definition

NSAIDs

corticosteroids

DMARDs

Term
which drugs are best to use during acute phase inflammation?
Definition
NSAIDs
Term
which drugs are best to use during chronic phase inflammation?
Definition

corticosteroids

DMARDs

Term
Which cyclooxygenase enzyme is widespread with relatively constant levels in various tissues?
Definition
COX-1
Term
Which cyclooxgenase enzyme is called the "housekeeping enzyme" and is produced in response to pro-inflammatory substances?
Definition
COX-2
Term
Which cytokines are the most important in terms of their roles in the inflammatory process?
Definition

TNF-alpha

IL-1

Term
What different properties do NSAIDs have?
Definition

analgesic

antipyretic

anti-inflammatory

Term
NSAIDs inhibit _____________, the enzymes in the synthesis of _______________ from arachidonic acid and other fatty acids. (MOA)
Definition

cyclooxygenase

 

prostagladins

Term
NSAIDS, at low doses, are indicated for:
Definition

mild to moderate pain

counteracting fever

Term
NSAIDs, at high doses, are indicated for:
Definition
treating inflammatory responses assc. with arthritic conditions
Term
What are some of the AEs associated with NSAID use?
Definition

GI toxicity

renal impairment, fluid retention

hypersensitivity reactions

inhibition of uterine contrations

premature closure of the ductus arteriosus

Term
Which drug is used to treat patent ductus arteriosus?
Definition
Indomethacin
Term
What are some of the AEs of NSAIDs that are not associated with COX inhibition?
Definition
hepatic, dermatologic and CNS effects
Term
NSAIDs may increase ___________ levels by inhibiting its excretion.
Definition
Lithium
Term
ASA competes with what drug for protein binding sites?
Definition
Warfarin
Term
Which drugs, when combined with NSAIDs, enhance the chance of peptic ulceration?
Definition
corticosteroids
Term
NSAIDs decrease the ___________ of methotrexate.
Definition
Clearance
Term
Which patients should use NSAIDs with caution?
Definition

those with renal impairment,

HF, HTN, edema, or

hypersensitivity reactions to any other NSAIDs

Term
Aspirin, Salsalate and Diflunisal are what type of NSAID?
Definition
salicylates
Term
Which salicylate has an active metabolite and what it is?
Definition
ASA, its salicylic acid
Term
Which salicylates irreversibly inhibit cyclooxygenase and which reversibly inhibit it?
Definition

ASA - irreversibly

 

Diflunisal and Salsalate - reversibly

Term
What does ASA prevent?
Definition
the sensitization of pain receptors to both mechanical and chemical stimuli
Term
How is the antipyretic effect of salicylates achieved?
Definition
by block PG synthesis at the thermoregulatory centers in the hypothalamus
Term
Which salicylate is used as an antipyretic?
Definition
ASA
Term
It takes about ______ times the analgesic dose of aspirin to provide an anti-inflammatory effect.
Definition
6
Term
Why should you not give a child aspirin if you think they may have a viral infection?
Definition

bc they may get Reye's syndrome

 

(a fatal, fulminating hepatitis with cerebral edema)

Term
How do salicylates effect respiration?
Definition

1. at therapeutic doses: increases respiration

 

2. at higher doses: may cause hyperventilation and resp. alkalosis

 

3. at toxic doses: central resp. paralysis and resp. acidosis

Term
What is the HL of salicylates?
Definition

at low, analgesic doses: 4-6 hrs

 

at high, anti-inflammatory doses: 15-30 hrs

Term
Why is ASA not very popular?
Definition
bc of its assc with peptic ulcers
Term
How much occult blood can you lose in one day taking normal doses of aspirin?
Definition
3-8 ml
Term
How do salicylates effect the GI system?
Definition

They increase gastric acid secretion by inhibiting PGI2 and they decrease mucus secretion by inhibiting PGE-2 and PGF-2

 

this can cause peptic ulceration, occult blood loss and rarely hemorrhage

Term
What is the dosage range of ASA used to prevent PLT aggregation?
Definition
60-81 mg
Term
What salicylate SEs are associated with their effect on the kidneys?
Definition

edema (from Na and water retention)

 

hyperkalemia

Term
Which NSAID cannot cause interstitial nephritis?
Definition
ASA
Term
Salicylic acid is used to treat:
Definition
corns, warts and calluses
Term
Methyl salicylate is used topically as...
Definition
a counterirritant in liniments
Term
How are salicylates absorbed?
Definition

1. Through intact skin

2. Though the stomach and small intestine (PO)

3. rectally (slow and unreliable)

Term
To whom might you give salicylate suppositories?
Definition
children with vomiting
Term
what salicylate does not cross the BBB or placenta?
Definition
Diflunisal
Term
What percentage of people taking salicylates will have a hypersensitivity reaction?
Definition
15%
Term
How is aspirin eliminated when taken at low doses?
Definition
renally by first order kinetics
Term
How is aspirin eliminated when taken at high, anti-inflammatory doses?
Definition
hepatic metabolite pathways are saturates and zero order kinetics occur
Term
What are the symptoms of salicylate hypersensitivity?
Definition

urticaria

bronchoconstriction

angioneurotic edema

Term
What are the 5 different groups of NSAIDs?
Definition

1. salicylates

2. proprionic acids

3. acetic acid derivatives

4. alkones

5. oxicams

Term
What are the AEs of salicylates?
Definition

- gastric distress, N/V

- microscopic GI bleeding

- prolonged BT

- resp. distress at high doses

- hyperthermia at toxic doses

- hypersensitivity

- Reye's Syndrome

Term
Ibuprofen and Naproxen are in what group of NSAIDs?
Definition
proprionic acid derivatives
Term
What is the max dose for proprionic acid derivatives?
Definition
they are all different
Term
What different properties do proprionic acid derivatives have?
Definition

analgesic

antipyretic

anti-inflammatory

 

anti-PLT, although they are not prescribed for this action

Term
What are the most common SEs of proprionic acid derivatives?
Definition

N, heartburn,

epigastric pain,

rash, dizziness

Term
What percentage of patients on Naproxen experience GI toxicity?
Definition
20%
Term
Fenoprofen (a proprionic acid derivative) is used exclusively as an:
Definition
anti-inflammatory agent
Term
What is Ketoprofen (a proprionic acid derivative) indicated for?
Definition

RA, OA

mild to moderate pain

dysmenorrhea

Term
Ketoprofen is more _________ than other proprionic acid derivatives.
Definition
renotoxic
Term
Why is it good practice to not leave a patient on a proprionic acid derivative for long periods of time?
Definition
bc of their GI effects
Term
Oxaproxin (a proprionic acid derivative) is approved for:
Definition
OA and RA
Term
How often must one take Oxaproxin?
Definition
once a day bc it has a long DOA
Term
Which Acetic Acid Derivative accumulates in the joints?
Definition
Diclofenac
Term
Which drugs are Acetic Acid Derivatives?
Definition

Indomethacin

Ketoralac

Etodolac

Sulindac

Diclofenac

Tometin

Term
All Acetic Acid Derivatives are good _____________ but are not used as _____________.
Definition

pain relievers

 

antipyretics

Term
What are the indications for Indomethacin?
Definition

RA, OA

Acute gouty arthritis

ankylosing spondylitis

closure of a patent ductus arteriosus

Term
Indomethacin is not recommended as...
Definition
a simple analgesic or antipyretic bc of its potential for toxicity
Term
Indomethacin produces more ____ and ____ effects than most other NSAIDs.
Definition
CNS and GI
Term
What percentage of Indomethacin users get a severe frontal HA?
Definition
25-50%
Term
What are the SEs of Indomethacin?
Definition

Severe HA                         

Vertigo, confusion and psych disturbances

GI problems

Major hematologic problems

Ocular problems

Hepatitis, pancreatitis

hypersensitivity reaction

Term
Which Acetic Acid Derivative is administered as a prodrug?
Definition
Sulindac
Term
What is Sulindac used to treat?
Definition

OA, RA

Gout

Ankylosing Spondylitis

Term
Which Acetic Acid Derivative is ONLY used as an analgesic?
Definition
Ketoralac (Toradol)
Term
Ketoralac is used to for:
Definition
moderate to severe, acute pain management
Term
How long should someone take Ketoralac?
Definition
no more than 5 days
Term
what are ketoralac's contraindications?
Definition

ASA allergy

PUD, GI bleed or perforation

renal or hepatic disease

labor and delivery

any bleeding tendency

nursing moms

Term
Which drug is an Alkone NSAID?
Definition
Nabumetone
Term
Nabumetone is used for ______________ only.
Definition
arthritic conditions
Term
Which drugs are Oxicam NSAIDs?
Definition

Piroxicam

Meloxicam

Term
What is Meloxicam's biggest use?
Definition
OA
Term
Which NSAID is the most selective for COX-2?
Definition
Meloxicam
Term
The frequency of GI SEs is less with ___________ than with other NSAIDs.
Definition
Meloxicam
Term
Piroxicam has a long _______ and used to treat ____________.
Definition

DOA

 

arthritic conditions

Term
What are your first and second choices for COX-2 inhibition?
Definition

1. Celecoxib (celebrex)

2. Meloxicam

Term
COX-2 selective inhibitors are associated with an increased incidence of ___________ as compared to NSAIDs.
Definition
severe adverse effects (including CV)
Term
Max adult dose of tylenol
Definition
4 grams/day
Term
Tylenol is not very helpful in treating what kind of arthritidies?
Definition
inflammatory
Term
TNF alpha and IL-1 contribute to __________ seen in chronic inflammation arthritis
Definition
tissue damage
Term
_______________ and ___________ are targets of antiiflammatory drug therapy
Definition

TNF alpha

 

IL-1

Term
what drug is the only COX-2 inhibitor still on the market?
Definition
Celecoxib - celebrex
Term
All NSAIDs should be taken with ______
Definition
food
Term
which drugs prompted the use of child-safe caps?
Definition
ASA and Iron
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