Module 3 Analgesics and Drug Abuse Flashcards
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)
Acetaminophen (Tylenol) = APAP
Acetyl-para-aminophenol
NOT NSAID - Not inflammation
derived form coal tar and is part of the class of drugs known as “aniline analgesics”
most commonly used drugs for the safe and effective treatment of pain and fever. widely used OTC drugs
acetaminophen + opioid
Vicodin; Lortab; Tylenol 3 and Tylenol 4
does not cause GI irritation
good choice for pt who experience upset stomach when taking NSAIDS
Narcotic and non-Narcotic combinations - OTC
Aspirin and antacid combinations
- Alka-seltzer tablets
- Buffered aspirin
aspirin and APAP
*Excedrin (acetaminophen, aspirin and caffeine)
Narcotic and non-Narcotic combinations - Rx
- Percodan
- Vicodin
- Lortab
- Percocet
- Vicoprofen
aspirin combined w/ an opioid
* Percodan (oxycodon + aspirin) - Sch II
acetaminophen combined w/ an opiod
- Vicodin and Lortab (acetaminophen + hydrocodone) - Sch II
- Percocet (acetaminophen + oxycodone) Sch II
a traditional NSAIDS and an opioid narcotic
* Vicoprofen (hydrocodone + ibuprofen) - Sch II
Acetaminophen Overdose
Accidental overdose of Tylenol occurs more frequency than ever due to the wide use of that drug in many OTC products.
It causes liver damage and is one of the most frequent causes of liver failure requiring liver transplantation in the U.S.
Ergotamine
Other category of Analgesics
*** used to treat Migraine headaches
derived from a fungus that sometimes contaminates rye and other grains.
Causes vasoconstriction by stimulating serotonin receptors as well as norephinephrine and dopamine receptors.
serotonin receptor agonist “-triptan” drugs
considered “miracle” drugs for migraine sufferers because of their ability to stop a migraine headache at its earliest signs.
serotonin
5-hydroxytriptamine or 5-HT
involved with aggression, anxiety, appetite, memory, mood, nausea, and sleep
Imitrex (sumatriptan)
was the first triptan to be approved, and its initial release only provided a self-injectable form of the epiPen
Cluster headaches
another type of vascular headache syndrome that affects men more often than women.
Shingles
Caused by Herpes Zoster Virus (HZV)
is in the same family as the Herpes Simplex viruses (HSV)
Is a painful skin eruption cases by the same virus that causes chicken pox in childhood. it can lead to a “post herpetic neuralgia” - an incapacitation nerve pain syndrome.
Pregabalin (Lyrica)
Anticonvulsants - treating fibromyalgia and earned 3.1 billion for Pfizer in 2010
Also use to treat migraine headach
prednisone
is the corticosteroids sometimes, steroids are injected around the base of the spine to relieve low back pain (epidural steroid injections)
Lidocaine (Lidoderm patch)
creams or gels containing topical analgesics
rubbed into the tender area
Capsaicin
a naturally occurring substance found in chili peppers
used in sports creams and topical drugs for arthritis, treat muscle and joint pain.
The ideal analgesic drug would
- provide maximum pain relief
- produce no side effects
- cause no dependence or addiction
Acetaminophen has two distint therapeutic effects
- analgesic - relieve pain?
- Antipyretic - reduce fever
does not have the anti-inflammatory properties that aspirin has. cannot be used to treat inflammation
does not have the anticoagulant effect that aspirin has, so it cannot be used to prevent a heart attack or stroke.
The risk of NSAIDs use
bleeding from a peptic ulcer
Ketorolac (Toradol)
is a potent NSAID often given IM to send pt home after surgery
also widely used in professional athletics.
Drugs have been used to treat Migraine headaches
- Ergotamine - a pwoerful vasoconstrictor
- Beta blockers and CCB (verapamil)
- SSRI antidepressants (Prozac (fluoxetine) and duloxetine (Cymbalta)
- A few anti-seizure and anti-psychotic drugs - Pregabalin (lyrica)
Vascular Headaches (migraine headache)
the group of medications are the serotoni (5-HT1B rc agonist) Triptan drugs
Imitrix (sumatriptan) was the first drug act as agonists or antagonists at various serotonin rc.
amitriptyline (Elavil)
Tricyclic antidepressants TCA, often help nerve Paine better than opioids - treat Shingles
RSD
Reflex sympathetic dystrophy or complex regional pain syndrome.
ex. bumping your hand on a door…pain on the hand
Ketamine
mu and Kappa rc Agonist
the stronger pain reliever
Ultram (tramadol)
mu and Kappa rc Agonist
alternative to strong opioids which very mild opioid effect
