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56 Cards in this Set

  • Front
  • Back
Is pain subjective or objective?
subjective - whatever the patient says it is
NSAIDs categorized by
structure
Acetylsalicylic acid
-class
NSAID
Indomethacin
-class
NSAID
Meloxicam
-class
NSAID
Ibuprofen
-class
NSAID
Naproxen
-class
NSAID
Ketorolac
-class
NSAID
Which drug is the prototype NSAID?
Aspirin
NSAID MOA
Blocks synthesis of prostaglandins by irreversibly binding to COX I and/or COX II enzymes
Adverse effects of NSAIDs
GI distress
Prolonged bleeding
Tenitis
Which NSAID is better tolerated than Aspirin and Ibuprofen?
Meloxicam (Mobic)
In an ideal world, NSAIDs would:
Block only COX II, which catalyzes teh type of prostaglandin r/t pain
HOWEVER, blocking only COX II may be associated with MI risk.
What is the problem with NSAIDs binding to COX I?
COX I catalyzes the production of TXA2 and protective prostaglandins in the stomach. Hence the GI irritation.
If there is a question pertaining to triglycerides:
The answer is probably Indomethacin (Indocin)
One alternative use for Indomethacin:
Closes the ductus arteriosis in babies (whose should have already closed) through its vasodilating effects (counterintuitive)
Binding to COX II prevents the production of ____, where binding to COX I prevents the production of ___
Inflammatory prostaglandins associated with hyperalgesia

Protective prostaglandins
Celecobix (Celebrex)

-MOA
-Problem with drug
The one cyclooxygenase II (COX II) inhibitor known to be safe

New, so no generic = expensive
New, so limited testing = less safe
The "other" antiinflammatory
-Name
-Trade
-MOA
Acetaminophen (Tylenol)

Inhibits prostaglandin synthesis in the central nervous system.
Why is Tylenol dangerous when taken with alcoholic beverage?
Alcohol can cause CYP enzymes to convert tylenol to a toxic metabolite
Is acetominophen an NSAID?
NO
From which plant is opoid drugs derived?
Poppies
Sedative and opoid effects
What percent of acetominophen excreted unchanged?
What percent converted to non-toxic metabolite?
2%

94%
Three types of opoid receptors
Mu

Delta

Kappa
Adverse effects of opioids
Respiratory depression
Constipation
Altered mental status
Where are opiate receptors located?
In dorsal horn of gray matter
1. soma of interneurons
2. axon terminal of afferant neurons (from periphery)
How do opiates affect the receptors on the afferent neurons?
Bind to receptor to inhibit the axon from releasing more neurotransmitter. The neuron then cannot complete the message of pain to CNS.
Where are mu receptors located and how do opiates act at these sites?
Found on the soma of secondary neurons. Opiates bind to the mu receptors and cause an efflux of K+ from the cell -- causing hyperpolarization. The cell then cannot transmit pain stimulus to brain.
Pharmacokinetics of morphine:
One of the metabolites is also active in the CNS.
Renal excretion
Morphine
-Class
Opiate (Morphine)
Codeine
-Class
-Also
Opiate (Morphine drug)

Also antitussive
Hydromorphone
-Class
Opiate (Morphine drug)
Hydrocodone with acetaminophen
-Class
Opiate (Morphine drug)
Oxycodone
-Class
Opiate (Morphine drug)
How do opiates act on the receptors on afferent neuron axon terminals?
Binds and causes decreased Ca++ influx into cell and decreases neurotransmitter released onto interneurons.
How is codeine related to morphine?
Structurally similar, some of codeine is converted to morphine by CYP enzymes.
However, most pain relieved by parent compound.
Hydromorphone (Dilaudid)

-Compared to morphine
-Metabolites
Actually more potent than morphine when given orally.

No active metabolites.
Where does oxycodone fall on the rank of potency and abuse potential?
Oxycodone has less potency and abuse potential than morphine, but more than codeine.
Which form of oxycodone is especially likely to be abused?
Sustained release patch.
Meperidine

-Class
-Trade
Opiate (Meperidine drug)

Demerol
Fentanyl

-Class
-Trade
Opiate (Meperidine drug)

Duragesic
Two patient rights to keep in mind while giving meperidine
-Right route (There are many many routes for this drug)

-Right dose (The doses vary greatly between routes)
In what ways are Meperidine and Morphine similar?
Similar in the amount of respiratory depression and sedation.
Why is meperidine ideal for OB use?
Because has much less respiratory depression on infants.
Which patients will not receive meperidine and why?
Renal patients and patients with chronic pain - because toxic metabolites can accumulate.
Why is codeine not always effective?
Because some people have variations in CYP 450 enzymes that alter the drug in ineffective ways.
Two noted routes of administration for fentanyl:
Buccal (lozenge)

Transdermal
Methadone

Class
Trade
Opiate (Methadone drug)

Dolophine
Propoxyphene

Class
MOA
Opiate (Methadone-like drug)

Darvon
What are methadone-like drugs used for?
They are a long acting PO drug used to wean people off of opiates.
Tramadol

Class
Trade
Trade w/ acetaminophen
MOA
Opiates (other)

Ultram
Ultracet

Binds to mu receptors and inhibits reuptake of NE and 5HT.
Lidocaine

Class
Trade
MOA
Topical analgesic

Lidoderm

Stabilizes neuronal membranes; inhibits ion fluxes required for conduction of pain impulse.
Nalbuphine

Class
Trade
MOA
Opioid agonist/antagonist mix

Nubain

Stimulates kappa, blocks mu; less respiratory depression and potential for abuse but CANNOT be reverse with antagonist.
Butorphanol

Class
Trade
MOA
Opioid agonist/antagonist mix

Stadol

Stimulates kappa; blocks mu. Causes more sedation; less potential for abuse.
Naloxone

Class
Trade
Opiate antagonist

Narcan
Narcan MOA
Antagonizes opiate receptors to treat opiate OD.