Drugs for Pain cont. Flashcards
What is the MOA for NSAIDs?
(-) COX 1 and/or COX2
Which COX is expressed in all tissues and which COX is expressed in some tissues some times?
ALL tissues = COX1
Some tissues some times = COX2
MOA for Aspirin?
IRREVERSIBLY (-) COX
What are 3 side effects of Aspirin?
- Ulcer
- Increased risk for bleeding
- Reye Syndrome
What is different about NON-Aspirin NSAIDs?
They (-) COX REVERSIBLY
– Also, have an increased risk for MI and stroke!
What do NON-Aspirin NSAIDs have an increased risk of compared to Aspirin?
Increased risk of MI and stroke
– reversibly (-) COX
NON-Aspirin NSAIDs are contraindicated in what patients?
CABG
What is the half life of Naproxen and what is good about it?
Half life = 12-17 hours
==> Best in patients that are at risk of cardiovascular complications
Which NON-Aspirin NSAID is the best choice in patients that are at risk of cardiovascular complications?
Naproxen
Which NSAID only (-) COX2?
Celecoxib
Celecoxib has LESS risk of what adverse effects seen with NSAIDs?
LESS gastric ulceration and LESS risk of bleeding
What are some adverse effects that can occur with NSAIDs that are taken during pregnancy?
Fetal oligohydramnios due to renal dysfunction
Closes ductus arteriosus early
List 4 contraindications for NSAID use
- Chronic Kidney Disease
- Gastric Ulcer
- Treatment with anticoagulants
- HTN or Heart failure
Acetaminophen does not suppress inflammation. What adverse effects can be seen with overdosage and what is the safe dose?
- Safe dose = < 3g/day
==> liver failure and death can occur with overdose
Acetaminophen is a toxic metabolite when _____ is depleted. What is the antidote?
When Glutathione is depleted
- Antidote = N-acetylcysteine
What are 2 adverse effects of Amitriptyline?
Suicidal thinking and anticholinergic effects
When may the onset of effects be seen when taking Amitriptyline?
6-8 weeks
What is an adverse effect of Duloxetine?
Suicidal thinking
Which alpha-2-delta calcium channel ligand is more sedating and has less reliable pharmacokinetics?
Gabapentin
What are the adverse effects of Gabapentin and Pregabalin?
Depression and suicide ideation
Which drug can (-) ascending pain pathways and increase descending inhibitory pain pathways?
Tramadol
MOA for Tramadol
Partial agonist at Mu opiate receptors and (-) NE/5HT reuptake
What are some (3) of the serious adverse effects of Tramadol?
Respiratory depression
Addiction/withdrawal syndrome
Interactions with drugs affecting the CYP450 enzymes
Tapentadol is a ____ mu agonist with less ______
Stronger mu agonist with less constipation
How is Ketamine given?
IV
What does Ketamine induce?
Cataleptic state with dissociation from the environment
Where does Ziconotide work?
Works at nociceptive afferent nerves of the dorsal horn
How is Ziconotide given?
Intrathecal
What is the adverse effect with Ziconotide?
Severe psych symptoms
What topical treatments (+) TRPV1 to feel like “heat”?
Capsaicin
Camphor
What topical treatment (+) TRPM8 to feel like “cold”?
Menthol
MOA for Lasmiditan?
5-HT1F Agonist
What are the effects of Lasmiditan?
Decreases stimulation of trigeminal system without causing vasoconstriction
What should you not use Dihydroergotamine with?
CYP3A4 inhibitors
What is there a risk of with Dihydroergotamine?
Vasospasm –> ischemia
