Analgesics Flashcards
T/F: Omega 6 fatty acids are pro-inflammatory.
True. Omega 6 FA are pro-inflammatory vs. Omega 3 FA which are anti-inflammatory
T/F: Lipocortin is an enzyme in the inflammatory pathway.
False. Lipocortin is not an ENZYME. It is a protein that inhibits phospholipaseA2 in the inflammatory pathway.
What are the five cardinal signs of inflammation?
Heat, redness, swelling, pain and loss of function
T/F: Tissue repair is part of the inflammatory pathway.
False. Tissue repair is post-inflammatory process.
What are the products of the three inflammatory pathways.
Leukotrienes,prostaglandins and thromboxane a2, and platelet activating factor (PAF)
T/F: COX2 is an inducible enzyme.
True. Injury or inflammation will cause COX-2 production.
Allodynia (decreased pain tolerance) can result from what?
Allodynia can result when prostaglandins (PGE2, PGF2a), leukotrienes, and Substance P sensitize pain fibers
T/F: Bradykinin, norepinephrine, and histamine stimulate pain fibers.
True.
Bradykinin, norepinephrine, and histamine STIMULATE pain fibers
What is Nociception?
Transmission of pain.
T/F: Endorphins (natural opioids) are Induced by Tricyclic Antidepressants (TCADs).
True.
Endorphins are induced/elevated by Tricyclic Antidepressants (TCADs). This is why TCADs can also be used for pain.
*Endorphins are also elevated in crushing’s syndrome.
What is the mode of action for Acetaminophen/Tylenol®/paracetamol?
Acetaminophen acts by CENTRALLY inhibiting COX–> reduces (pain & fever).
*metabolism is through the liver.
T/F: ASA is GI irritant whereas acetaminophen is not.
True.
What is the standard dose of ASA/Aspirin?
325mg
T/F: Oral NSAIDs are metabolized in the kidneys.
True
What are the adverse reactions of ASA (non-topical)?
Headache
Nausea
Abdominal cramps, bleeding, ulceration
Hemorrhagic diathesis: bleeding time doubles
Tinnitus -> Hearing loss
Nephrotoxicity+
Respiratory alkalosis -> metabolic acidosis#
Acute poisoning by respiratory depression
Non-immune, low dose hypersensitivity*
What is Reye’s syndrome?
Adverse reaction in children taking ASA to reduce fever in viral infections (eg. chicken pox or influenza)
GI disturbances
Liver degeneration
Encephalopathy
- upto 35% mortality!
What are the NSAIDs’ contraindications?
Active peptic ulcer Chronic GIT inflammation Bleeding disorders Heavy alcohol use NSAID/ASA induced asthma Known hypersensitivity Chronic hepatic or renal disease, diabetes Hypertension or congestive heart failure Pregnancy: especially 3rd trimester Corneal denervation, dry eye
What is the most prescribed NSAID topical drug?
Acular LS (generic: Ketorolac)
T/F: Ilevro qd is a pro-drug NSAID topical that is hydrolyzed to Amfenac in anterior chamber.
True.
What are the adverse reactions of NSAIDs topicals?
Burning, stinging
Corneal toxicity, melting =O (OMG!)
Vitreous detachment
Delayed wound healing
Prolonged bleeding time
Elevated IOP:
-Noted risk w/ diclofenac & nevanac
-Risk in combining topical NSAIDs w/ PG analoguesWhat are the main differences between NSAIDs and Narcotics?
Narcotics: Have no ceiling effect Cause miosis Are addictive Are not available in topicals Are for severe acute pain Have no anti-inflammatory, anti-platelet, or anti-pyretic effects.
NSAIDs (the exact opposite): are used for mild-modern pain.
T/F: Hydrocodone (Vicodin®) is a schedule II drug.
True.
Schedule II: High Abuse, some medical use, high risk of dependency
What are the adverse reactions of opioids?
Nausea and vomiting (stimulation of chemoreceptor trigger zone and delayed gastric emptying
Miosis (excitation of Edinger-Westphal nucleus)
Flushing & itching (histamine release)
Sedation
Constipation
Cough suppression
Respiratory depression (2)
Dependence
About how many days after a patient stops taking Aspirin would you see then having normal blood clotting again?
About 7-10 days when new platelets are born and start making COX1. (since ASA irreversibly inhibits COX1 for the life time of platelets, pt will not have normal clotting until new platelets are born.
T/F: At the dose levels of 325mg-650mg Aspirin is anti-inflammatory.
True.
** also at this dose the t1/2 (half life) of Aspirin is about 10hrs
T/F: Acetaminophen is GI irritant.
False.
What is the pregnancy rating for Aspirin?
D
**Vs. pregnancy rating of B for Acetaminophen
What is the mode of action of Aspirin/ASA?
Irreversible inhibition of Cox1.
*acts predominately peripheral.
Respiratory alkalosis which leads to metabolic acidosis is one of the adverse side effects of Aspirin. What is the mechanism that leads to this?
Salicylate uncouples oxidative phosphorylation such that oxygen consumption is elevated, resulting in elevated CO2 generation–> leads to respiratory alkalosis.
Why should aspirin and salicylates including Pepto Bismol
not be used in children under the age of 15?
Because of the possibility of getting Ray’s syndrome (if they have viral infections).
T/F: Llevro is inactive until it reaches the Anterior chamber.
True.
Llevor is a pro-drug. so it is not active until it reaches the anterior chamber where it is metabolized to Amfenac
Which two topical NSAIDs are noted for risk of elevating IOP?
Diclofenac & Nevanac
What do natural and semi-synthetic opioids have in common?
They both have phenanthrene backbone.
T/F: Morphine, codedine, hydrocodone and meperidine all cause release of histamine which lead to itching and flushing.
True.
T/F: Heroin is a semi-synthetic opioid roughly 4X as potent as morphine.
True.
