Exam I: Non-Narc Analgesics Flashcards
Product “labeling” and package inserts for drugs are strictly regulated by what organization?
FDA
Any change in labelling post NDA must be approved by the FDA
“Package inserts” for drugs is intended for interpretation for patient, healthcare professionals or both?
Healthcare professionals
FDA’s intent with the design of the current revision of the Package Insert is to improve patient ____ and _____?
Improve patient safety and efficacy
This section of a package insert will tell you information on PK and PD.
Clinical pharmacology
This section of a package insert describes controlled clinical trials that were submitted to the FDA (Phase I – III trials).
Clinical studies
“Off label” uses are in the package insert of a drug.
True/False
False
FDA approved indications only (no off label indications)
There are counseling tips in a package insert of a drug.
True/False
True
Can scripts be legally written for an “off label” use of a drug?
Yes, this is legal.
Can drug manufacturers promote off label uses of a drug? (Before 2015 court ruling)
Manufacturers are strictly prohibited (by the FDA) from any overt or covert promotion of products for off-label uses.
Did the 2015 court ruling that now allows drug manufacturers to promote off label uses of a drug have a big impact in the pharmaceutical industry?
No, there is still a process to get these off label uses on package inserts.
FDA still needs to approve all indications
Prazosin (Minipress) is an antihypertensive medication that has an “off label” use to treat what?
Nightmares related to PTSD
This source provides a compilation of package inserts for major brand name products.
Physicians’ Desk Reference, now called Prescribers Digital Reference (“The PDR”)
Name 4 facts of the PDR.
- Does not include generic products
- Updated yearly
- Organized by a drug company (room for some bias)
- Well indexed with picture of dosage forms
This source is available as a book and online. Organizes drug by therapeutic class. Mentions off label uses and costs.
Drug Facts and Comparisons
This source is published by the ASHP. Evaluates how good a drug is. Less detail than Drug Facts and Comparisons.
American Hospital Formulary Service (AHFS) Drug Information
Prevalence of Americans suffering from pain is around?
more than 100 million Americans
Somatic vs Visceral pain?
Somatic pain (Localized) – can be related to trauma, dental pain etc.
Visceral pain (Deeper): harder to localize, can be related to cancer, kidney stones etc.
Examples of neuropathic pain. Does it respond well to NSAIDs.
Does not respond well to NSAIDs
ex. Diabetic neuropathy
Post-herpetic neuralgia (happens after viral infection, most common complication of shingles)
What is psychosomatic pain? Does it respond well to NSAIDs?
Does not respond well to NSAIDs
Under stress, more susceptible to pain. Pain usually unexplainable.
What is nociceptive pain? Does it respond well to NSAIDs?
Responds well to Non-Narc analgesics in general
Pain that signals tissue damage. Involved with stimulation of sensory nerves. Can be sharp, throbbing, burning.
Most widely used and sold over the counter analgesic class?
NSAIDs
What are Salicylates? Name one of the salicylates (Hint: available OTC)
Precursors to the NSAIDs, in the 19th century this was an herbal drug (willow bark) that was found to have analgesic properties
Aspirin (Acetylsalicylic Acid, ASA) is an NSAID precursor
What drug class are “FENAC” drugs in?
NSAIDs
Pharmacologic Classification of NSAIDs.
Cyclo-oxygenase = COX inhibitor
Inhibition of COX enzymes and the related inhibition of Prostaglandin synthesis.
This is associated with inflammation and pain synthesis.
Are NSAIDs or steroids more potent anti-inflammatory drugs?
Steroids are more potent
Therapeutic Classification of NSAIDs.
Analgesic - relieve pain
Antipyretic - Fever reducing
Anti-inflammatory
How does aspirin affect platelet function?
A single dose of Aspirin irreversibly inhibits platelet function for the 8 to 10 day life of the platelet.
Two common side effects of aspirin.
GI bleeding and Tinnitus (ringing in the ears)
Why is aspirin not recommended for children?
Reye’s Syndrome (ASA-specific)
A rare life-threatening condition in children, especially if aspirin is administered subsequent to a viral infection.
Results in liver failure, cerebral edema, encephalitis.
DDI for NSAIDs (including aspirin)
NSAIDs [including aspirin] increase the INR in patients on warfarin, and increase the risk of bleeding.
Yosprala® is an aspirin-omeprazole combo. What benefit does it have?
Used to protect against the GI effects of aspirin.
Durlaza® vs OTC aspirin?
Aspirin 81 mg enteric - BID = 162 mg/day
Durlaza® 24-hour ER - 162.5 mg - Patients only have to take one day instead of two 81 mg aspirin
How are non-selective COX inhibitors different from other NSAIDs? These NSAIDs end in what suffices?
Inhibit both COX 1 and 2 enzymes
- PROFEN
- FENAC
Name 3 non-selective COX NSAIDs that do not end in -PROFEN or -FENAC.
- Aspirin
- Naproxen
- Indomethacin
Naproxen advantages over Ibuprofen.
Longer duration of action than ibuprofen.
Twice a day is adequate enough for pain.
Lowest risk of cardiovascular side effects. Typically used for inflammation of the joints (i.e. arthritis)
How are partially selective COX inhibitors different from other NSAIDs? Name two drugs in this group.
More selective than non-selective NSAIDs.
Less selective than COXIBs
Less likely to inhibit platelet aggregation or to cause GI bleeding
- Etodolac
- Meloxicam
ADRs of NSAIDs
- Coagulation Disorders - increased risk of bleeding
- Pregnancy - increased risk of miscarriage. Should be discontinued (6 - 8 weeks prior to delivery)
- Reye’s Syndrome in children
- Skin reactions (ie. Stevens-Johnson Syndrome, Toxic Epidermal Necrolysis)
Excedrin Migraine® is a combo of what three drugs?
Aspirin + Acetaminophen + Caffeine
How does caffeine help with migraines and headaches?
Blood vessels widen during headaches
Caffeine constricts blood vessels
Also helps if headache is caused by caffeine withdrawal
Pharmacological classification of COXIBs.
Most selective NSAID
Only inhibits COX 2 enzymes
Functional differences of COX-1 and COX-2
COX-1 : protects the mucosal lining of the stomach by increasing the protective mucous
COX-2 : produces inflammation and pain
How COXIBs differ from other NSAIDs?
- Most selective
- Most protective to patients at higher risk for GI effects.
- No significant cardiovascular side effects.
- Does not have much of an antipyretic effect (does not reduce fever) ***
Chemical class of COXIBs with NSAIDs. (structure name)
Diaryl-substituted pyrazoles
Contraindications for Celecoxib.
Patients who have had open heart surgery.
Limit use for patients at risk for stroke or heart attack.
Indications for COXIBs.
Osteoarthritis and Rheumatoid Arthritis
Primary Dysmenorrhea
Familial Adenomatous Polyposis – (FAP)
Acetaminophen is the analgesic, antipyretic of choice for what 4 patient groups?
- 12 years old and younger (No possibility of Reye’s)
- Pregnant women in third trimester
- Patients at serious GI toxicity risk
- Patients taking warfarin or some other anticoagulant drug
Acetaminophen vs NSAIDs (5)
- Less effective analgesic
- No cardioprotective effects like aspirin
- Does not increase risk of stroke or heart attack
- No GI toxicity
- Does not have anti-inflammatory effects
Acetaminophen toxicity?
Hepatic (liver) toxicity that are dose related
