Analgesics Flashcards
What is the strongest OTC analgesic?
Naproxen (Aleve),
1380mg equivalent dose of naproxen=10mg of morphine
What are the maximum dosing for ibuprofen and naproxen?
1200mg/day of ibuprofen
440mg/day of naproxen
Is there a difference between frequently taking smaller doses vs. Infrequently taking larger doses?
It doesn’t matter as long as the patient is not using more than the legal requirements
What is the difference between opioid and non-opioid analgesics
Increases in morphine dose always results in greater pain relief. Increases in pain relief for non-opioid analgesics like ibuprofen and acetaminophen eventually plateau
Can ibuprofen have anti-inflammatory relief within legal OTC dosing?
No, anti-inflammatory effect only begins past the max OTC dose. An MD can prescribe higher doses of analgesics that can actually reduce inflammation
What is the most convenient OTC analgesic?
Naproxen (Aleve)
Are Advil liquid gels more effective compared to tablets?
They are no more effective, decrease in absorption time is irrelvant.
Tablets are cheaper, and make more sense
What are some side effects associated with ibuprofen?
Hives, facial swelling, asthma (these can occur independently),
Stomach bleeding is always mentioned as a severe, but rare side effect
Does acetaminophen have a better side effect profile at OTC levels?
Not really, especially at OTC doses
At Rx doses, acetaminophen has fewer GI side effects
Are nausea eipigastric pain, and heart burn following analgesic use associated with the development of gastric ulcers?
No, they do not directly cause GI bleeds.
For patients that were on 2x daily dose, only 1-2% of patients developed GI bleeds
Is hepatotoxicity a side effect of Tylenol (acetaminophen)?
Hepatotoxicity is not a side effect, it is a sign of overdose
How can some of the GI side effects of Tylenol (acetaminophen) can be attenuated?
Taking pill with food will help reduce GI irritation, but it will delay and reduce some of the analgesic effects
What are the attitudes of pharmacists with balancing risks and benefits of drug therapy?
Pharmacists are risk-averse, and they will try to minimize side effects even if riskier options to resolve conditions exist
If we want to be risk-averse and not recommend drugs, we need to give patients alternatives
What is the #1 reason for liver transplants?
Acetaminophen related hepatotoxicity
16,000 deaths in the USA in 2014
Is acetaminophen overdosing worse compared to ibuprofen overdosing?
Ibuprofen is a lot more safer, acetaminophen toxicity can cause severe liver issues
Do people who experience chronic pain also suffer from insomnia?
Yes, 60-80% of pain patients have trouble sleeping
Why is pain worse at night?
Natural cortisol(endogenous anti-inflammatory) levels decrease at night resulting in less natural pain relief
People also remain still for the entire night, and this could cause joints to stiffen up
What is the most common type of pain treated with OTC analgesics?
Muscle/Back/Joint pain accounts for 42%
Headaches/Migraine accounts for 24%
Cold/Flu accounts for 11%
Other pain accounts for 23%
How many people experience severe pain?
11% of people have severe pain, and out of these people 12% have untreated cases
What is the advice from MDs regarding analgesics?
MDs want us to use less analgesics and focus more on treating the condition directly instead
What are the two common types of non-trauma head related pains?
Headaches and Migraines
Are Tylenol arthritis the best product for arthritis?
Studies show acetaminophen is just as good as placebo.
Be less likely to recommend chronic use of acetaminophen
What is the average age of arthritis diagnosis?
50 years, but symptoms start to develop at 47.5 years
What is the drug of choice for dysmenorrhea (painful periods)?
NSAIDs
Do current acetaminophen and ibuprofen combination products make sense?
No, doses for ibuprofen and acetaminophen are simply too low in Advil Plus (acet+ibu)
People simply take the two products separately and use max dose for both
What is the benefit of acetaminophen+caffeine combo products?
They show significantly improved efficacy in the treatment of patients with tension type headaches or migraines
What are medication overuse headaches?
Headaches can become more common following frequent use of analgesics. It is kind of like rebound congestion in topical decongestants
What analgesic combination is prone to cause medication overuse headaches?
OTC analgesics that combine caffeine, aspirin, and acetaminophen are common culprits
What is the max therapeutic duration for a caffeine-containing headache agent?
9 days/month according to the slides, but JT recommends 15 days/month
What is the Codeine-2D6 issue?
Codeine is a prodrug for morphine, but the enzyme that converts codeine into morphine has variable efficiency.
This means that some individuals rapidly break down codeine into morphine (toxicity), while others break down codeine too slowly (subtherapeutic)
Do modern guidelines reccomend codiene as an analgesic?
No. Due to the Codiene-2D6 issue, they no longer reccomend the drug
What OTC analgesics pose the greatest concern for overdoses?
Acetaminophen and ASA
Should children be checked out after they consume large amounts of OTC analgesics?
Yes, people should take the child alongside the bottles the child consumed to a poison control/MD
What dose of acetaminophen can cause hepatoxicity in adults?
7.5-10 grams within 8 hours (24 regular pills or 15 extra strength pill)
What dose of acetaminophen can cause hepatotoxcity in kids?
150-200 mg/kg
What is a cause of accidental acetaminophen poisoning?
Taking acetaminophen via different products (happens unintentionally)
If someone takes more than the daily max dose of acetaminophen (4g), are they in big trouble?
No, but we shouldn’t exceed the max dose
Are ibuprofen overdoses more severe compared to acetaminophen?
No, but we still need patients to head over to the ER and get checked out
Is ibuprofen completely safe in patients on warfarin?
No, ibuprofen competitively binds to plasma proteins. This results in a higher amount of free warfarin in the blood.
Does acetaminophen interact with warfarin?
Yes, but the mechanism is unknown.
Acetaminophen doses of more than 2.5g can increase bleeding
Do NSAIDs like ibuprofen interact with DOACs
Yes, these patients have a higher risk of bleeding while on NSAIDs and DOACs
Can young children develop asthma due to acetaminophen use in pregancy?
Possible, acetaminophen reduces natural levels of glutathione (eliminates free radical), effectively increasing oxidative stress
Can young children develop ADHD due to acetaminophen use in pregnancy?
Possible, acetaminophen during pregancy has been associated with neurodevelopmental and behavioral disorders
What is the relationship between NSAIDs and asthma?
Some forms of asthma are aspirin-sensitive. In these patients, NSAIDs like ibuprofen can trigger symptoms of asthma or allergies
When does aspirin-sensitive asthma develop?
The sensitivity developes in adulthood, typicaly in people between 20-50 years old
How common are aspirin allergies?
1-2% in general population
10-30% in people who already have allergic rhinitis, asthma, or urticaria
This reaction is due to COX-1 blockade
What is the cross-sensitivity of aspirin allergies between other NSAIDs?
It is high (98-100%)
If you are allergic to aspirin, you are allergic to lots of other NSAIDs too
Can people who have non-aspirin-sensitive asthma use NSAIDs?
Yes
What are the risks of telling asthma patients who are unaware of their aspirin-sensitive status to not use NSAIDs?
This advice negatively impacts asthmatics who are not aspirin-sensitive because they are unable to use the drugs that would otherwise work perfectly fine
What are the benefits and risks associated with aspirin 81mg?
Benefit: Prevents heart attacks by reducing the adhesion of platelets (reduce clotting)
Risk: Increased risk for GI bleeds
What is the consequence of taking another NSAID alongside aspirin for cardio-protection?
Other NSAIDs like ibuprofen can bind to the COX-1 receptor on platelets and prevent aspirin from binding and conferring its cardio-protective effects
What can be done to limit interactions between NSAIDs for pain and aspirin for anti-platelet activity?
Take single doses of NSAID drug 2 hours after aspirin, or 8 hours before taking aspirin.
This is hard to schedule over a long period of time and its often unsuccessful
Can higher doses of aspirin give patients pain management and cardio-protection?
Technically yes, at 325mg BID, but this dose is so high that it poses great concern for GI bleeds
Do topical NSAIDs interact with oral aspirin?
No, diclofenac (NSAID drug) is commonly prepared as a topical ointment and it does not interact with oral aspirin
How does the FDA rank the safety of drugs used in pregnancy?
New scale from 2015
Drugs in Category A are very benign and pose no harm to the fetus, but there are very few drugs in this class
Category B, C, and D are all more riskier drugs in pregnancy
Category X includes drugs that are known teratogens (ex. isotretinoin)
What is the safety of acetaminophen in pregnancy?
It is a Category B drug, but we should still consider its potential effect on the onset of ADHD and asthma
What is the safety of ibuprofen in pregnancy?
NSAIDs inhibit prostaglandins, a chemical that is responsible for maintaining heart structures in fetal hearts (PDA).
If this structure is not present due to NSAID inhibition, this structure collapses and blood gets into lung capillaries while in-utero, causing lung damage.
Category C below 30 weeks
Category D above 30 weeks
What fetal safety category is Naproxen a part of?
Category D, poses serious harm to fetus
If taken in the 1st trimester, Naproxen can cause a spontaneous abortion
What are some of the relevant functions of COX-1 enzymes?
Helps protect GI from bleeds
Negative impact on CV
What are some of the relevant functions of COX-2 enzymes?
Causes inflammation (healing process)
Positive CV impact
What is the effect of NSAIDs on the COX enzymes?
Ibuprofen and naproxen are non-selective COX inhibitors.
They effectively eliminate all of the functions of both COX enzymes
Are GI bleeds at OTC dosing for NSAIDs very common?
No, they are rare
Heartburn and dyspepsia on the other hand are alot more common
Is ASA safer for GI bleeds or cardiovascular system compared naproxen?
ASA is safer for GI compared to Naproxen
Is Naproxen safer for GI bleeds or cardiovascular system compared to ASA?
Naproxen is safer for the cardiovascular system compared to ASA
What drugs do NSAIDs interact with?
Anticoagulants (GI risk)
BP medications (bleeding risk)
SSRIs (GI risk)
ASA 81mg (GI risk)
Alcohol (GI risk)
Other drugs that negatively affect the GI tract (ex. oral steroids)
What is the interaction between alcohol and acetaminophen?
Acute alcohol consumption actually helps protect against hepatotoxicity by competing with the conversion of acetaminophen into toxic metabolites.
Chronic alcohol consumption on the other hand can increase risk for hepatoxicity. Chronic alcoholics have more P450 enzymes breaking down acetaminophen into toxic metabolites vs. other non-toxic metabolites
What are some things pharmacists have to worry about NSAID use in the elderly?
They have decreased clearance
More drug interactions
More conditions
More bleeding risk
More cardioovascular risk
What are the benefits and risks of NSAID use in sports?
A lot of atheletes will take NSAIDs to help deal with pain and fatigue, but NSAIDs can have bad effects as the athlete becomes dehydrated
