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56 Cards in this Set

  • Front
  • Back
Define Nociceptive pain
Stim. of peripheral nerve
Are All of the following are considered nociceptive pain?

Cold, Burn, Alc. on wound
Herptetic neuralgia, Phantom limb pain
Cold, burn, alc. on wound are nociceptive pain
MOA of Opioids?
G-protein coupled receptors in CNS and spinal cord regions involved in modulation of pain

Close voltage-gated Ca2+ channels on presynaptic nerve terminals --> reducing transmitter release

Hyperpolarize = inhibit post-synaptic neurons by opening K+ channels
What receptors do opiods have actions at?
Mu, Kappa and delta

They can be agonists at one and antagonists at another
What are the actions of the mu receptor acted on by opiods?
Supraspinal and spinal analgesia, inhibition of respiration, slowed GI transit, modulation of hormone and NT release, euphoria
What are the actions of the delta receptor acted on my opioids?
suprespinal and spinal analgesia, modulation of hormone and NT release
What are the actions of the kappa receptor acted on by opioids?
Supraspinal and spinal analgesia, psychomotor effects, slowed GI transit, dysphoria
T/F: If you give exogenous Opioids, you can spur release of endogenous opioids
TRUE
What are the sites of opioid action in the ascending pathway?
Periphery, Dorsal Horn, ventral caudal thalamus
What is the role of the descending pathway in opioid drugs?
Lesser understood - thought to inhibit pain transmission neurons
What are the sites of opioid action in the descending pathway?
Periaquaductal gray
Rostral ventral medulla
Dorsal Horn
Frequent repeated doses of a drug produce a gradual loss of effectiveness. What does this describe?
Tolerance
When a drug is stopped or antagonist administered and the pt. experiences withdrawal syndrome, what does this define?
Dependence

(The Symptoms themselves are the withdrawal)
What are the possible hypotheses for tolerance?
cAMP upregulation
NMDA
Receptor recycling
Receptor uncoupling


Note - persistent administration of opioids increases the sensation of pain
A pt comes in after stopping an opioid, describing the sensation of euphoria and analgesia, mental clouding b/c they can't do their taxes, sedation, respiratory depression, Anti-diuresis, N, V, and cough suppression. What level of Tolerance does this describe?
HIGH
A pt stops their opioid med and you note bradycardia on PE. What level of tolerance are they experiencing?
Modertate
What are the symptoms of LOW tolerance?
Miosis, Constipation, Convulsions
T/F: Opioids are well absorbed through most routes, but undergo significant first pass effect
TRUE - Subcu, IM, Oral

Codeine + Ocycodone do NOT undergo significant first pass effects
do Opioids localize rapidly or slowly to highly perfused tissue sites?
Rapidly to places like brain, kidney, lung, liver, spleen

= what makes them fun to abuse
Whats the main reservoir of opioids?
Skeletal muscle
A pt is elderly an thus their metabolism has slowed substantially. After giving them codeine, would you expect to see more codeine or morphine in their system?
Codeine

Codeine --> Morphine via CYP2D6

Slow metabolizers can't covert it fast, thus we'll see build up of Codeine

Note: Oxycodone and Hydrocodone are also metabolized by CYP2D6
What are the CNS affects of Opioids?
Euphoria, Dysphoria, Sedation, Respiratory Depression, Cough suppression, miosis, truncal rigidity, N, V, Temp (u agonists = hyperthermia, kappa agonist = hypothermia)
What are the effects of opioids on CV?
MOST cause bradycardia,

Meperidine causes Tachycardia
What do opioids do to GI tract, Biliary tract, and Renal system?
GI = constipation b/c they dec. motility
Biliary = contract biliary sm. m = biliary colic, Inc. amylase and lipase
Renal = depressed due to dec. renal plasma flow
A Preggo Pt on an opioid wants to know what SE's she can exect in terms of her uterus. (and neuroendocrine, pruritis, immune system). what do you tell her?
Uterus = prolong labor
Neuroendocrine = stimulate release of ADH, prolactin, somatropin, inhibit LH
Pruritis = flushing and warming of skin
Immune function = inhibit or augments it
What do we need to monitor in a pt who has been on opioids for a long time?
Their immune function
What are the clinical uses of opioids?
Analgesia, Acute pulm edema, cough, D, Shiverring
A pt suffers from the shivers every time he sees a cup of sugar. What do you give him to tx?
Meperidine = anti-shiver via alpha-2 receptor subtype
Pt going in for Sx gets opioids for what reason?
Pre-Sx = sedative, analgesic
During -Sx = they can minimize CV depression
What are the Strong Agonist Opioid agents to know?
Morphine, Hydromorphone, Heroin, Methadone, Meperidine, Fentanyl
What are the Mild-moderate opioid agents to know?
Codeine, Hydrocodone, oxycodone, diphenoxylate, Loperamide, Buprenorphine, Naloxone, Naltrexone, Tramadol, Dextromethrophan
How do all the opioids we learned about work?
Agonists of the Mu receptor
What is methadone used for?
Heroine addicts = suppresses opioid withdrawal symptoms, analgesia

Tolerance and physical dependence develop slowly and withdrawal symptoms are more mild, but more prolonged than morphine
Whats one of the major side effects of Methadone?
Prolonged QT = why its black boxed
Whats the primary use of codeine?
Antitussive (anti-cough), pain relief
Between Fentanyl and Meperidine, which one is more widely used?
Fentanyl

(DON'T USE meperidine with tachycardia b/c it can cause QT prolongation)
T/F: Hydrocodone and Oxycodone are less efficacious than morphine
TRUE
How do we get a fatal overdose of Hydrocodone or oxycodone?
Drugs that have been modified to release all of the drug at once --> fatal
What are Loperamide and Diphenoxylate used for?
Diarrhea
What do we combine Loperamide and Diphenoxylate with to reduce abuse?
Atropine
What receptor do Naloxone and Naltrexone work through?
Mu
T/F: Naloxone and Naltrexone have little action in the absence of agonist
TRUE
T/F: in the presence of agonist for ex. morphine, the opioids effects are reversed in 3 minutes with Naloxone and Naltrexone
TRUE

= normalizes repiration, level of consciousness, pupils, bowel activity, awareness of pain
Whats one of the main problems associated with administering Naloxone?
Within 3 minutes, you can see withdrawal symptoms
A pt comes in having overdosed on opioids, and is now in a coma. What do you use to tx?
Naloxone
Why does Buprenorphine have a long DOA?
Slow dissociation from the receptor
T/F: Buprenorphine is as effective as Methadaone for tx of opioid dependence
TRUE
What is Tramadol used for? SE's?
Use = Pain

SE = Lowers seizure threshold, serotonin uptake syndrome
Dextromethorphan use?
Anti-tussive
What do the withdrawal symptoms from opioids depend on?
Strength of opioid
When does tolerance from an opioid begin?
After the first dose

Minimize tolerance by giving smaller doses with longer intervals between dosing
T/F: Physical dependence develops as tolerance develops
TRUE
What are the withdrawal symptoms seen with opioids?
Rhinorrhea, lacrimation, yawning, chill, goosebumps, hyperventilation, hyperthermia, mydriasis, muscular aches, V/D, Anxiety, hostility

# and severity depend on degree of dependence
T/F: The longer the half life of the drug, the longer time it takes to reach withdrawal symptoms
TRUE
How do we prevent dependence on opioids?
Establish therapeutic goal before starting therapy, once effective dose is established, limit dose to this level, Look at other options, Evaluate frequently
In what pt. populations should we need to watch use of opioids?
Preggos, impaired hepatic function, endocrine disease, head injuries, impaired pulmonary function