Non-Opioid Lecture part 2 Flashcards
Pharmacologic class of Aspirin?
Salicylate
- Most useful salicylate for analgesia
- Used historically to reduce fever
Chemistry of Aspirin
acetylsalicylic acid (ASA) - Acetic acid (HA) and salicylic acid (SA)
Explain the effect’s of aspirin or in other words the mechanism by which it functions
- It inhibits the synthesis of prostaglandins
- Prostaglandins are synthesized locally by inflammatory stimuli. They sensitize pain receptors (nociceptors) to substances such as bradykinin. The more synthesis, the more they sensitize and you feel pain. Therefore, reduction in prostaglandins results in reduction in pain
When is aspirin more effective? Is it more effective against throbbing pain (inflammation) or stabbing pain (direct irritation of nerve endings)?
If given BEFORE painful stimuli are experienced.
-more effective against throbbing pain
Aspirin produces peak effect on empty stomach after how long?
30 minutes
Describe the Aspirin half-life
Dose-dependent
- With a small dose, half life is 2-3 hours
- With a high dose, a half-life of 15-30 hours can be attained
Is aspirin first-order kinetics or zero-order kinetics?
Zero-order kinetics
5 main effects of aspirin
- Analgesic
- Antipyretic
- Anti-inflammatory
- Uricosuric
- Anti-platelet effect
What might be a side effect of the anti-inflammatory effect of aspirin?
Dosing used for pain control (analgesic) is not enough for anti-inflammatory effects. It is difficult to take the dosage needed for anti-inflammatory results. This could lead to GI ulceration and bleeding.
What is the danger of taking low dose aspirin and it’s effect of being uricosuric?
At low doses, there is uric acid retention. If a patient has gout and is taking probenecid to excrete the uric acid, aspirin can antagonize these effects.
Describe the mechanism to how aspirin can have an Anti-platelet effect
Aspirin inhibits cyclooxygenase which inhibits the formation of thromboxane A2
- Thromboxane A2 normally causes vasoconstriction and platelet aggregation
- By inhibiting these mechanisms, aspirin reduces risk for blood clots and stroke
What dosage is aspirin used to prevent stroke and heart attack
Low dose (81 mg)
Gastrointestinal adverse effects of aspirin occur because of 3 things
- Direct gastric irritation and inhibition of cytoprotective prostaglandins (mucus in stomach)
- Stimulation of chemoreceptor trigger zone in the CNS (nausea and vomiting)
- Exacerbates pre-existing ulcers, gastritis, hiatal hernia, reflux disease
Bleeding as an adverse effect of aspirin might have what presentation clinically?
Bleeding may be occurring in the gingiva. It may appear as gingivitis but in fact it is drug-induced bleeding. Important to ask about aspirin use.
Name the three adverse effects of aspirin
- Gastrointestinal: dyspepsia, nausea, vomiting, gastric bleeding
- Bleeding - Irreversible effects on platelets
- Reye’s syndrome - aspirin contraindicated in children/adolescents with viral infections