Salicylates (NSAIDs) Flashcards
What 2 plants are salicylates?
- Willow bark (oral)
- Oil of wintergreen
Salicylates are hydrolyzed into? What is the significance of that metabolite?
Salicylic acid - responsible for therapeutic and toxic effects
At what blood level of salicyclic acid does the person NEED to go for hemodialysis?
> 80mg/dL
At what blood level of salicylic acid does toxicity begin?
40mg/dL
What are the 3 most important things that are happening in the body during early salicylate toxicity?
- Respiratory alkalosis - breathing a lot = CO2 being expelled
- Metabolic acidosis
- Normo-hyperglycemia in the periphery only
What are the 3 most important things that are happening in the body during late salicylate toxicity?
- Respiratory acidosis
- Metabolic acidosis
- Normo-hypoglycemia
Antidote for salicylate toxicity? Yes or no?
No
What is the managment strategy for salicylate toxicity? (2)
- ABCs/symptomatic & supportive care
- Pay special attention to hydration, oxygenation, electrolytes and blood glucose
Therapeutic levels of salicylate concentrations are? (range)
5-25 mg/dL
Low serum pH (acidic serum) favors salicylate entering CSF and tissues. Why?
As blood pH falls, there is an increased proportion of non-ionized salucylate (lipid soluble) (weak acid) that more readily distributes into the CSF and other tissues. Therefore, blood pH must be considered in conjunction with the salicylate concentration
Salicylate concentration should be measured every _ hours until: (3)
2
- Clinical improvement AND
- Low serum salicylate conc
- Normal to high serum pH
What is the most important piece of supportive care for salicylate toxicity management?
Alkalinization
- Salicylate = weak acid, so increasing pH (basic) ionizes the salicylate, causing it to be renally excreted (and prevent tubular reabsorption back into blood). Also decreases CNS toxicity
Name the full COX-1 and 2 inhibitor NSAIDs (9)
1. Aspirin
2. Piroxicam
3. Sulindac
4. Ibuprofen
5. Ketorolac
6. Diclofenac
7. Naproxen
8. Ketoprofen
9. Indomethacin
Name the preferential COX-2 and partial COX-1 inhibitor NSAIDs (5)
- Etodolac
- Meloxicam
- Nimesulide
- Nabumetone
- Tolmetin
Name the primary COX-2 inhibitors with little action at COX-1
1. Celecoxib
- Actually, just know they all end in -coxib
Name the weak COX-1 and COX-2 inhibitor NSAIDs
- 5-ASA
- Paracetamol
- Dilfunisal
- Sulfasalazine
What is the name of the NSAID that is no longer used in humans, but still used in horses?
Phenylbutazone
Earlier toxicity with salicylates presents with:
A. Metabolic alkalosis and respiratory acidosis
B. Respiratory acidosis and metabolic acidosis
C. Respiratory alkalosis and metabolic acidosis
D. Metabolic alkalosis and respiratory alkalosis
C
Prostaglandin inhibition from NSAID poisoning leads to:
A. GIT hyperperfusion and hypermotility
B. CNS depression leading to coma
C. Seizures
D. Vasoconstriction and renal hypoperfusion
A
Which symptom is an early indication of salicylate poisoning?
A. Tinnitus
B. Cardiac arrhythmia
C. Seizures
D. Diarrhea
A
The ______________ of salicylate to salicylic acid is easily saturable, which is the main cause of toxicity.
A. Conjugation
B. Hydrolysis
C. CYP Phase II metabolism
D. Oxidation
B
Salicylate-induced hypoglycemia and cerebral edema directly contribute to:
A. Mental status changes
B. Metabolic acidosis
C. Cardiac abnormalities
D. Rhabdomyolysis
A
Blood pH should be monitored until what change occurs in the serum?
A. Serum pH increases
B. Serum salicylate levels are increasing
C. Stomach pH decreases
D. Seizures occur
A
Which liquid drink is recommended for children suffering from NSAID toxicity?
A. Milk
B. Orange juice
C. Large volume of water
D. None of the above
A
What is considered a life-threatening dose of ibuprofen?
A. >400 mg/kg
B. >200 mg/kg
C. >50 mg/kg
D. >100 mg/kg
A
Which of the following groups of NSAIDs are the most toxic?
A. Mefenamic and phenylbutazone
B. Ketoprofen and naproxen
C. Celecoxib and ibuprofen
D. Pyrazolones and oxicams
A
Which prostaglandin is responsible for pain and fever:
A. PGE4
B. PGE2
C. PGI2
D. TXA2
B
Celecoxib and Rofecoxib are primarily:
A. Cox-1 inhibitors
B. Cox -2 inhibitors
C. Bothe Cox-1 and Cox-2 inhibitors
D. Do not inhibit Cox-1 or Cox-2
B