Module 3 Analgesics and Drug Abuse Flashcards
(49 cards)
Name the two major categories of analgesics
- Centrally acting Opioid Narcotics
- Peripherally acting Non-opioid analgesics
- Other (misc)
Analgesic
used to denote a medication that gives pain relief without resulting in loss of consciousness.
Analgesia and sedation
Difference effects
Conscious and sedation
not much of a difference
Opiate
opiates are the naturally occurring mu receptor agonists derived from opium. opium, morphine codeine
Opioid
natural or synthetic, are mu receptor agonists.
Narcotic definition
pertaining to or producing narcosis “sleep” , “benumbing”, “deadening”
Any of the prohibited (schedule I - 5) controlled substance
ex. LSD, cocaine, heroin, methamphetamine
defined by the Controlled Substance Act 1973 (CSA)
what are the 3 opiates mu receptor agonist?
Natural sources
Opium
Morphine
codeine
what are the 3 synthetic sources Opioids? mu rc agonist
demerol, Vicodin and Lortab
Meperidine (demerol - first synthesized opiod)
hydrocodone (in Vicodin and Lortab)
NSAIDS
NON-steroidal anti-inflammatory drugs - aspirin-like drugs
the first NSAID discovered was aspirin
Aspirin (acetylsalicylic acid)
1899 - derived from the bark of the willow tree
first NSAID discovered
Traditional NSAIDS - available OTC
Ibuprofen (Motrin, Advil)
Naproxen (Aleve)
Eicosanoids
a group of locally -acting hormones
All NSAIDs work
by blocking a group of locally-acting hormones called “eicosanoids”
speificallally, NSAIDS block those eicosanoids that are prostaglandins (PG) and thromboxanes
all aspirin-like drugs
were classified as “nonsteroid inhibitors” (non-steroidal antiinflammatory inhibitors, or NSAIDS)
AA Cascade
Arachidonic acid
all eicosanoids are formed in a series of metabolic reactions called AA cascade.
they help control many normal body processes as well as contributing to pain, inflammation, fever and muscle cramps.
two pathways in AA cascade
- COX (cyclooxygenase) leads to the production of eicosanoids called thromboxanes and prostaglandins
- Lipoxygenase oxidation leads to the production of eicosanoids called leukotrienes
COX and lipoxygenase are
enzyme
Drug properties of NSAIDS
- Analgesia - through inhibition of prostaglandins
- Anti-inflammation - also through inhibitions of PGs
- Antipyresis (reduce fever) - acting on the hypothalamus
- Anticoagulation - with exception of COX-2 inhibitors, all NSAIDS inhibit platelet aggregation (keep them from stiicking together)
Aspirin - Salicylates - adverse effects
Reye’s syndrome (an immune disease)
a disorder of the liver and the brain, that occurs at a higher rate in children under 19 while taking “salicylates” during certain viral infections (colds, flu and chicken pox)
Aspirin - Salicylates - side effects
- these drugs can cause peptic ulcer disease PUD and GI bleeding.
- in high doses salicylates can cause a ringing of the ears
they are acids and because they inhibit “protective prostaglandins”
The four therapeutic effects of aspirin:
- Analgesia - through inhibition of prostaglandins
*Anti-inflammation - also through inhibitions of PGs
*Antipyretic (reduce fever) - acting on the hypothalamus
except platelet - Anticoagulant - Aspirin prolongs the clotting time of the blood by inhibiting thromboxane
Two forms of the cyclooxygenase enzyme
COX 1 - Found throughout the body and performs many “housekeeping” functions
COX 2 - found to be active only in states of inflammation
Name 3 COX2 NSAIDs
they are not “anti coagulation”
- Vioxx (rofecoxib
- Bextra (valdecoxib)
these two drugs off the market due to higher rates of coronary artery disease and stroke - Celebrex (celecoxib) - is the only one left (Rx only)
