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Opiates Handout
Test Two - Opiate Notes
213
Nursing
Graduate
10/14/2013

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Term
Pain Definitions (Three).
Definition
It is what the patient says it is.
Term
Hyperalgesia.
Definition
Decreased pain threshold.
Term
Windup Phenomenon.
Definition
Synaptic potentials increase with amplitude with each repeated stimulus. Pain gets greater with each stimulus causing the pain.
Term
What is a nociceptor?
Definition
Pain receptor.
Term
Allodynia.
Definition
Pain evoked by a non-noxious stimulus. A stimulus that normally does not cause pain.
Term
What is preemptive analgesia?
Definition
Analgesic given prior to stimulus.
Term
Define Acute Pain (4 things).
Definition
Rapid, defined onset with limited duration.
Term
What are the two types of acute pain?
Definition
monophasic - one time cause, surgery.
Term
Define Chronic pain.
Definition
Delayed, poorly defined onset.
Term
What is associated with chronic pain?
Definition
Depression .
Term
What may be associated with chronic pain?
Definition
Allodynia and hyperagesia may be associated.
Term
Skeletal muscle spasm.
Definition
Pain caused by muscle spasm stimulating pain receptors.
Term
What is fast pain?
Definition
Short, well localized. Matched to type of stimulus.
Term
What is slow pain?
Definition
Throbbing, burning, or aching pain.
Term
Characteristics of temperature sensation?
Definition
Follows same path as slow pain.
Term
What are the two types of visceral pain?
Definition
Visceral and Somatic.
Term
Define Visceral Pain.
Definition
Assoicated with cramping pain caused by ischemia caused by stretching, distension, and spasm.
Term
What kinds of organs is cramping pain specific to?
Definition
Visceral pain to the hollow organs such as bowel, bladder, gastric, and uterine.
Term
What kind of organs is a sharp pain specific to?
Definition
Visceral pain to the solid organs such as liver.
Term
Define somatic pain.
Definition
A sharp stabbing pain, well localized.
Term
Describe Neuropathic Pain.
Definition
Peripheral or central stimulation.
Term
Perception of pain is a subjective experience. What three areas that compose this subjective perception?
Definition
Sensory - Intensity, location and duration.
Term
What influences pain response?
Definition
Genetics.
Term
What kind of activity is provoked by pain in the anatomic nervous system?
Definition
Efferent activity. Motor response to avoid or correct painful stimuli.
Term
Spontaneous firing can occur from the reusult of?
Definition
Nerve injury.
Term
Describe complex regional pain syndrom. (long)
Definition
First described in civil war "causalgia".
Term
What does the increased sympathetic response in complex regional pain syndrome eventually lead to?
Definition
Changes at all neuraxial levels leading to sensitization of pain pathways maintaining chronic neuropathy.
Term
What is the primary receptor that is activated in the sensitization of the dorsal horn? What drug has the potential to be a antagonist to this?
Definition
N-methyl-D-Asparate (NMDA).
Term
What does the pathophysiology of pain involve? (four things)
Definition
Transduction.
Term
Define Transduction.
Definition
Noxious stimuli translated into electrical activity.
Term
Describe transduction as it relates to nociceptor activation.
Definition
Injury stimulates Protaglandin, serotonin, and bradykinins to activate pain fibers.
Term
During transduction what do the peripheral neurons release?
Definition
Substance P and other mediators.
Term
Describe nociceptors in terms of their nerve endings.
Definition
Nociceptors have open affernet nerve endings of myelinated A-delta and C-delta fibers.
Term
What are the two types of A-delta neruons?
Definition
Mechanosensitive and Mechanothermal.
Term
What kind of stimuli are polynodal C sensitive to?
Definition
Heat, mechanical and chemical stimuli.
Term
What can stimulate polynodal C type nociceptors?
Definition
Acetylcholine, bradykinin, histamine, prostaglandins, and K+.
Term
Do pain receptors adapt?
Definition
No, they act as a protective mechanism that allows for constant awareness of injury.
Term
Describe Transmission (periphery to spinal cord).
Definition
Impulse travels via axons of the primary afferent neurons to the dorsal horn of the spinal cord.
Term
What are the tracts called that the dorsal horn projects to the brain?
Definition
Ascending Tracts
Term
How are pain signals transmitted to the thalmus?
Definition
Via the spinothalmic tract (ascending trat).
Term
What transmits pain informaion to reticular formation, mesencephalon, and hypothalamus?
Definition
spinoreticular, spinomesenecephalic, and spinohypothalamic tracts.
Term
How do opioids block the flow of information?
Definition
Opioids can inhibit sensations at the dorsal horn and can bind to sites in the brain to activate descending pathways to further inhibit.
Term
What drug mimics GABA to inhibit nociceptive transmission?
Definition
Baclofen.
Term
Where do the afferent A-Delta fibers enter and terminate in the spinal cord?
Definition
Enter - dorsal nerve roots.
Term
After termination in 1 and 5 in the dorsal horn, what do the fibers of afferent A-Delta do?
Definition
Excite second order neurons of the spinothalamic tract then give rise to long fibers which cross to the opposite side of the spinal cord and up to the brain via the neospinalthalmic pathway.
Term
Describe A Delta Fibers
Definition
Fast transmission fiber.
Term
Glutamate from A Delta fibers binds to what?
Definition
AMPA receptors postsynaptically.
Term
Describe A Beta Fibers.
Definition
Large, heavily myelinated.
Term
What kind of fibers are present for slow transmission?
Definition
Type C.
Term
Describe the path of Type C Afferent fibers.
Definition
Enter via dorsal nerve.
Term
Describe Type C Fibers.
Definition
Unmyelinated, slow.
Term
How do pain impulses travel in the brain?
Definition
Thalamus to somatosensory area of cortex.
Term
Where do afferent C fibers end?
Definition
The RAS area.
Term
Describe how pain is modulated.
Definition
Spinal interneurons release inhibitory amino acids (GABA) and neuropeptides (endogenous opioids) that bind to afferent primary and dorsal horn neurons and inhibit pain.
Term
Describe the Gate Control Theory.
Definition
Dorsal horn functions as a gate.
Term
What do the spinothalmic and the medullary fibers release to inhibit pain responses?
Definition
GABA.
Term
What effect do MAO and Tricyclics have on pain inhibition.
Definition
Block the reuptake of norepi and cause an increase in concentration leading to inhibited pain responses. Ie, ANS compensation.
Term
Where does clonidine have its greatest effect?
Definition
Clonidine works best supraspinal.
Term
What kind of agonist is Clonidine?
Definition
Conidine is Alpha 2 agonist.
Term
When are analgesia properties seen?
Definition
Analgesic properties seen after one dose. Useful in augementing morphine or local blocks.
Term
WHat are the side effects of clonidine?
Definition
Sedation (alpha 2 agonist).
Term
How does Ketamine effect the NMDA receptor?
Definition
Ketamine is an antagonist at NMDA receptor sites. NDMA is an excitatory neuro transmitter for pain.
Term
What receptors does Klonidine function at other than NMDA?
Definition
Ketamine functions at opiate and muscarinic receptors.
Term
Describe effect that ketamine has on patient?
Definition
Higher BP, Higher HR.
Term
General Description of an NSAID.
Definition
Decrease pain receptor actiavtion from prostaglandin.
Term
Describe COX-1.
Definition
Good kind.
Term
Describe COX-2.
Definition
Mainly found in inflamatory cells.
Term
What NSAID is the safest for renal impairment?
Definition
Aspirin.
Term
What are the limits for both children and adult for acetaminophen?
Definition
Adults: 4 Grams.
Term
Acetaminophen IV for analgesia DOA and onset?
Definition
Onset: < 10 min
Term
Acetaminophen IV for Antipyretic DOA and onset?
Definition
Onset: < 30 min.
Term
IV Acetaminophen.
Definition
Given: 15 min.
Term
How fast is IV infusion given?
Definition
Concentration: 100ml amp, 10mg/ml.
Term
What are the effects of using a non-selective NSAID?
Definition
Renal impairment, blocks prostaglandin in stomach, and platelet inhibition.
Term
What are the concerns related to toradol?
Definition
GI bleeding > than aspirin.
Term
What may be a relative contraindication to a patient getting toradol?
Definition
Asthma
Term
What is the max dose of toradol for an adult.
Definition
120mg over 24 hours.
Term
WHat are the potential side effects of NSAIDS?
Definition
Bleeding.
Term
What kind of receptor is an opiate receptor?
Definition
G-protein.
Term
Activation of the opiate receptor causes the inhibition of
Definition
Adenylyl Cyclase, which in turn causes a decrease in CAMP.
Term
Where are opiate receptors located?
Definition
Brain and spinal cord.
Term
How is classification opioid receptors accomplished?
Definition
Classified by receptor affinity for opioid peptides.
Term
Activation of a Mu1 receptor causes?
Definition
Bradycardia.
Term
Activation of a Mu2 receptor causes?
Definition
Spinal analgesia.
Term
What kind of agonist are highly specific to Mu receptors?
Definition
Opioid Receptors.
Term
Spinal anesthesia is mediated by primarily what receptor?
Definition
Mu-2
Term
Supraspinal anesthesia is mediated by what receptors?
Definition
Mu-2
Term
What receptors cause respiratory depression?
Definition
All except Mu-1.
Term
What receptors causes dependence?
Definition
Delta and Mu-2.
Term
Supraspinal analgesia is primarily mediated by what receptor?
Definition
Mu-1.
Term
What receptor causes Euphoria?
Definition
Mu-1.
Term
What receptor causes dysphoria?
Definition
Kappa.
Term
What receptor is most important for peripheral pain?
Definition
Delta.
Term
What receptors cause sedation?
Definition
Mu-1, Mu-2, and Kappa.
Term
What does the term neuraxial analgesia refer to? What is it based on?
Definition
Epidural and suarachoid opiates. Based on opioid receptors in the spinal cord.
Term
What results in systemic absorption in regards to spinal anesthesia.
Definition
Venous Plexus.
Term
What complication can be caused by cephalad migration of a drug interacting with the trigeminal nucleus?
Definition
Herpes Simplex.
Term
What accounts for differences in synthetic opioids?
Definition
Receptor affinity, potency, duration.
Term
Is there a ceiling affect with opioids?
Definition
No ceiling affect with opioids.
Term
Is there a celing affect with NSAIDS?
Definition
Yes, there is a ceiling affect with NSAIDs.
Term
Where do synthetic opioids act?
Definition
At the opiate receptor pre and post and at primary afferent neurons.
Term
What are the CNS effects of morphine like drugs?
Definition
decreased stress respons to surgical stimulation, decreased MAC of volatile agents, analgesia, euphoria (in presence of pain), dysphoria (when not in pain), sedation, respiratory depression.
Term
What are the GI effects of morphine like drugs?
Definition
Biliary tract-spasm of sphincter of Odi, pancreatic ducts (reversible by:
Term
What are the Gu effects of morphine like drugs?
Definition
Urinary retention, urgency, difficulty voiding (increase tone of ureter.
Term
What are the cutaneous effects of morphine like drugs?
Definition
Vessel dilation, localized histamine release (rarely IgE mediated), pruitis, erythema.
Term
Dose Analgesia
Definition
25 to 100mg.
Term
Onset.
Definition
1 min.
Term
Peak.
Definition
5 to 20 min.
Term
Duration.
Definition
2 to 4 hours.
Term
Elemination 1/2 Time.
Definition
3 to 5 hours.
Term
Metabolized via.
Definition
Liver.
Term
Strength.
Definition
1/10 potency of morphine.
Term
What is the active metabolite in Meperidine? What is it responsible for?
Definition
Normeperidine. It is responsible for CNS effects ie. Seizures.
Term
When is Meperidine contraindicated?
Definition
If patient taking MAO inhibitors.
Term
What receptors does Meperidine work at?
Definition
Mu and Kappa opiate receptors.
Term
What are two common side effects of Meperidine?
Definition
Hyperpyrexia and Dysphoria.
Term
What is the typical use for meperidine?
Definition
Postop shivers.
Term
What is the max dose for 24 hours? What is the max length of time meperidine should be use for?
Definition
Should not exceed 600mg in 24 hours. Should not be used greater than 48 hours.
Term
Dose (Induction)
Definition
1 milligrams/kg (said to induce surgical anesthesia).
Term
Dose Analgesia
Definition
2 to 15 milligrams titratd to effect 1-2 milligrams doses.
Term
Onset.
Definition
1 to 5 minutes. IM More towards 5min.
Term
Peak.
Definition
5 to 20 minutes IV 30-60min IM.
Term
Duration.
Definition
2 to 7 hours.
Term
Elemination 1/2 Time.
Definition
1.7 to 3.3 hours.
Term
Metabolized via.
Definition
Conjungation in liver.
Term
Excreted.
Definition
Mainly kidney. 7 to 10% billiary.
Term
How does the CSF effect differ from the effect of drug in plasma?
Definition
CSF peak take lags behind plasma, but last longer than plasma
Term
What are active metabolites of morphine
Definition
Morphine 3 etheral sulfate, morephine 3 glucoronide, morephine 6 glucuronide.
Term
What is metabolized to morphine as well as other metabolites
Definition
Codeine
Term
Why does PO morphine not work well?
Definition
90% first pass effect.
Term
What does morphine cause the release of that causes it to not be a good choice for an asmatic
Definition
Histamine.
Term
Fenatnyl Concentration
Definition
50mcg/ml. (epidural 5mcg/ml.
Term
Dose (Induction)
Definition
5 to 40mcg/kg.
Term
Dose Analgesia
Definition
0.7 to 2mcg/kg.
Term
Sole Anesthetic TIVA
Definition
50 to 150mcg/kg.
Term
PCA.
Definition
15 to 100mcg/hr.
Term
Epidural.
Definition
25 to 60mcg/hr.
Term
Onset.
Definition
30 seconds.
Term
Peak.
Definition
5 to 15 minutes.
Term
Duration.
Definition
30 to 60 minutes.
Term
Volume of Dist.
Definition
4L/kg.
Term
Protein Bound
Definition
84%
Term
Elemination 1/2 Time.
Definition
219 minutes.
Term
Metabolized via.
Definition
Liver: N-demethylation to norfentanyl.
Term
Excreted.
Definition
Kidney. Present in urine for 72 hours.
Term
What are you synthetic opiates (phenylpiperidines)?
Definition
Meperidein, Fentaynyl, Sufentanil, Alfentanil, Remifentanil.
Term
How much stronger is Fentanyl than morphine
Definition
100x stronger.
Term
How does duration of action and elmination time differ from morphine?
Definition
Morphine has a longer duration of action, but fentanyl takes longer to elminate due to a greater lipid solubility.
Term
How does onset differ between fentanyl and morphine?
Definition
Morphine has a slower onset 1-5min, Fentanyl 30 seconds. Due to greater greater lipid solubility allowing for rapid passage through blood brain barrier.
Term
First pass pulmonary effect?
Definition
Yes, significant
Term
How does fentanyl effect cardiac tissue?
Definition
Minimal effect on cardiac output, minimal cardiac depression, but may cause bradycardia due to carotid sinus reflex.
Term
If Fentanyl is given at a high rate of speed, what can it cause?
Definition
Rigid Chest.
Term
How does fentanyl cause an increase in ICP?
Definition
Due to an increase in CO2 due to respiratory depression.
Term
Sufentanil Concentration.
Definition
50mcg/ml.
Term
Dose (Induction).
Definition
2 to 10mcg/kg.
Term
Dose Analgesia.
Definition
0.6 to 4mcg/kg.
Term
Sole Anesthetic TIVA.
Definition
10 to 30mcg/kg.
Term
Onset.
Definition
1 to 3 min.
Term
Peak.
Definition
3 to 5 min.
Term
Duration.
Definition
20 to 45 min.
Term
Volume of Dist.
Definition
2.48 (smaller than fent).
Term
Protein Bound
Definition
92% (larger than fent).
Term
Elemination 1/2 Time.
Definition
149 min.
Term
Metabolized via.
Definition
Liver CP450.
Term
Excreted.
Definition
Urine and feces.
Term
Strength.
Definition
10x Stronger than Fentanyl.
Term
Lipid solubility?
Definition
High.
Term
How does the elmination half life and context sensitive half time differ from fentanyl?
Definition
Elimination half life and contect sensitive half life of sufentanil is shorter due to a higher protein binding and smaller volume of distribution.
Term
How does respiratory depression differ from fentanyl.
Definition
Sufentanil has a greater respiratory depression.
Term
Note:
Definition
Bradycardia dose dependent, increased ICP only with increased CO2
Term
Duration:
Definition
10-15 min. 1/3 that of fentanyl.
Term
Onset:
Definition
1 minute. 5x faster than fentanyl.
Term
Metabolized:
Definition
Liver (variable).
Term
Volume of Distribution.
Definition
Low volume of distribution.
Term
Solubility.
Definition
low solubility.
Term
Protein Bound.
Definition
high protein binding.
Term
Remifentanyl Concentration.
Definition
Abailable 3, 5, and 10mg powder for recontitution.
Term
Dose Analgesia.
Definition
0.5 to 1mcg/kg. over 30 seconds.
Term
Dose Infusion.
Definition
.05 to 2mcg/kg.
Term
Onset.
Definition
Less than 1 min. (ultra short acting).
Term
Peak.
Definition
1 min.
Term
Duration.
Definition
5 to 10 min.
Term
Context sensitive half time.
Definition
5 min.
Term
Volume of Dist.
Definition
small.
Term
Protein Bound
Definition
70% protein bound.
Term
Elemination 1/2 Time.
Definition
1 to 20 minutes
Term
Metabolized via.
Definition
Ester hydrolysis to inactive metabolite.
Term
Excreted.
Definition
Kidney.
Term
Strength.
Definition
15-20x stronger than alfentanyl or 2x as potent as fentanyl.
Term
Why is remifentanil not recommended as a sole agent?
Definition
Due chest rigidity and uncertain loss of conciousness. Should be supplemented with N2O, forane, or propofol.
Term
What might you want to give with remifentanyl? How do you want to infuse?
Definition
Infuse slow and give a non depolarizing muscle relaxant for chest rigidity
Term
What differs in chemical make up of remifentanil compared to fentanyl? What does this allow for?
Definition
Remifentanyl has a ester linkage. This allows for ultrashort duration and with no cumulative effects. Rapid on and rapid off.
Term
Why is remifentanil cleared so quickly? What is its clearance rate compared to fentanyl?
Definition
Ester Hydrolysis by plasma/tissue esterase causes fast clearance. Remifentanil clears 8 times faster than fentanyl.
Term
How are renal and hepatic functions effected with remifentanyl?
Definition
No effect.
Term
Notes:
Definition
Post op anesthesia.
Term
Dose.
Definition
0.2 to 0.6mg q2-q3 hours.
Term
Protein Binding.
Definition
Low.
Term
Metabolism.
Definition
Liver.
Term
Excretion.
Definition
Kidney.
Term
Concentration.
Definition
0.4mg/ml amp. Draw up with 3cc NS for a .1mg per ml concentration
Term
Dose.
Definition
0.05 to .1 mg increments to effect.
Term
Onset.
Definition
1 to 2 min.
Term
Duration.
Definition
30 to 45 min.
Term
Elemination 1/2 Time.
Definition
60 to 90 min.
Term
Metabolism.
Definition
Liver, undergoes first pass effect 1/5 oral potency.
Term
What kind of antagonist is it? What sites does it affect?
Definition
Pure opiod agonist at mu, delta, and kappa sites.
Term
What are the side effects of Naloxone?
Definition
Potential reversal of hypotension. Nausea and vomiting related to rapid infusion.
Term
What should be watched for after giving?
Definition
Renarcotization.
Term
How should Naloxone be given?
Definition
Slowly in 0.5 to .1mg increments. Repeat 2 to 3 min.
Term
Naltrexone
Definition
PO. 24 hour duration.
Term
Dose
Definition
0.5 to .1mg IV
Term
Half Time.
Definition
10 hours.
Term
How is drug compared to Narcan?
Definition
Equal potency. Longer duration due to slow metabolism by the liver.
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