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Clinical Neuro
Opiods
86
Biology
Graduate
01/17/2008

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Cards

Term
what are the 3 types of opiod receptor
Definition
Mu, kappa and delta
Term
Name the endogenous opiods
Definition

Enkelphalin

Dynorphin

Beta-Endorphin

Term
Where is Enkephalin distributed
Definition
Brain, spinal cord, adrenal medulla and GI
Term
Which receptors does Enkephalin bind too?
Definition
Binds to delta and mu
Term
Which receptors does Dynorphin bind to
Definition
kappa
Term
What's the distribution of Dynorphin
Definition
Brain and Spinal cord
Term
Where would you find beta endorphin
Definition
Cell bodies in the intermediate lob of the pituitary and the hypothalamus
Term
Beta-endorphin is released due to _____? Which receptors does it bind to
Definition

Stress

Mu and delta

Term
Name the factors regulated by MU
Definition

Analgesia

Sedation

Miosis

Euphoria

Constipation

Respiratory distress

Nausea/vomiting

Pruritius

Term
Kappa regulates what?
Definition

Sedation

Miosis

Analgesia

diuresis

dysphoria

psychotomimetic effect

Term
delta receptors regulate what?
Definition

Analgesia

Emotion

Reward

Seizures

Term
Opiods as a analgesic act on 3 locations, what are they
Definition

Central or supraspinal

Spinal

Peripheral

Term
When an opiod acts as an analgesic on the supraspinal, what does it activate?
Definition
Activation of descending pain inhibitory pathways
Term
What's the mechanism of action of an opiod on the spinal cord
Definition
Inhibits the Dorsal horn pain transmission neurons
Term
Where are the opiod receptors located in the periphery
Definition
A & C fibers
Term
What's the effect of opiods on respiration
Definition
Depresses respiration
Term
How do opiods decrease respiration
Definition

Decrease the response of the brainstem respiratory centers to carbon dioxide tension

Decrease pontine and medullary centers that regulate respiratory frequenceReduce TV and respiratory rate

Term
How do opiods suppress cough
Definition
Depresses the cough reflex in the brainstem
Term
How do opiods cause nausea and vomiting
Definition
Stimluate chemo receptor zones in the medulla
Term
Miosis due to opiods occurs because
Definition
Pupillary constriction due to central effect on CN III
Term
What is opiods effect on the GI tract
Definition
Constipation
Term
How do opiods cause constipatoin
Definition

increase smooth muscle tone

decrease propulsive motility

decrease gastric acid, pancreatic, biliary and intestinal secretion

Term
What is pruitis? do opiods cause this?
Definition
pruitis is caused by opiods and it is flushing and warming of the skin also sweating and itching
Term
What are opiod effects on the CVS
Definition

Histamine release leads to peripheral vasodilation

Orthostatic hypotension

Cerebral vasodilation secondary to respiratory depression

Term
What are signs of acute opiod toxicity
Definition

1. stupor, miosis and depressed respiration

2. Coma follows and BP falls

3. Puppillary dilation, shock and death

Term
Morphine acts primarly on what receptor?
Definition
Mu
Term
How is morphine metabolized
Definition
glucuronidation in the liver
Term
What is the active form of morphine
Definition
Morphine-6-glucurionide
Term
How is morphine eliminated
Definition
the conjugated form is eliminated by the kidney
Term
what are the side effects of morphine
Definition

1. nausea & vomiting

2. Sedation/dizziness, mental clouding

3. Flush of the face and neck

4. Pruritis

5. Postural hypotension

Term
How would you treat the mental status change from morphine
Definition
Haloperidol
Term
What are the contraindiction for morphine
Definition

1. Compromised respiratory function

2. Kidney disease

3. Liver disease

4. Head trauma

Term
At what dose is codeine used as a antitussive?
Definition
15-20 mg
Term
what are the adverse effects of codeine
Definition

1. Low incidence of nausea, dizziness, sedation & constipation

Term
Codeine has a ___ dependence
Definition
Low
Term
what would you use codeine for?
Definition

1. Oral analgesic & antitussive

2. Mild and moderate pain

Term
Heroin is more ____ soluble than morphine and is metabolized to ______
Definition

lipid

morphine

Term
What is heroin used for?
Definition

1. cough

2. Mild to moderate pain

Term
Oxycodone is equipotent to
Definition
Morphine
Term
Oxycodone is used for
Definition
Moderate to severe pain
Term
Dihydrocodeine is used for
Definition
Mild to moderate pain
Term
Dihydrocodeine is formualted w/
Definition
aspirin or acetaminophen
Term
Hydromorphone has a high ______ liability
Definition
abuse
Term
Hydromorphine is more ______ than morphine
Definition
potent
Term
When should you give hydromorphine to a patient
Definition
For severe pain
Term
The metabolite form of Meperidine produces
Definition
CNS excitation that leads to tremors and convulsion
Term
What's the MOA of merperidine
Definition
Mu receptor agaonist and some anti-muscarinic properties
Term
Merperidine is used for
Definition
Moderate to severe pain
Term
What advantages does methadone have over morphine
Definition
Equipotent w/ greater oral availability
Term
Methadone acts on what receptors
Definition
It's a Mu agonist and a NMDA antagonist
Term
What do you use to treat heroin dependency
Definition
Methadone
Term
Methadone is used for
Definition

Moderate to severe pain

Treament of heroin dependency

Term
Is propoxyphene a CNS stimulant?
Definition
No, it's metabolite is
Term
Propoxyphene is used for
Definition
Mild pain
Term
When would you use Fentanyl, Sufenanyl and Alfentanil
Definition

Supplement during GA

Provides CV stability during surgery

Good for short procedures

Term

____ is 100x more potent than morphine

_____ is 10x more potent than fentanyl

Definition

Fentanyl

Sufentanyl

Term
What is the definition of a Mixed Opiod receptor
Definition
Possess both opiod receptor agonist and antagonist
Term
What advantages do mixed opioids have
Definition

Less respiratory depression

Lower abuse potential

Term
Name the mixed opiods
Definition

1. Pentazocine

2. Butorphanol

3. Buprenorphine

4. Nalbuphine

Term
Which receptors do Pentazocine bind to
Definition

1. Kappa agonist

2. Weak mu antagonist

Term
Pentazocine is metabolized by
Definition
glucurnidation
Term
Pentazocine can have what effect in an opioid dependent person
Definition
Can percipitate in abstience syndrome
Term
What advantage does Pentazocine have over morphine
Definition
Can not antagonized morphine induced respiratory depression
Term
What are the adverse effects of Pentazocine
Definition
1. conspitation, dizziness
2. Psychotomimetic effefcts
3. Increase HR and BP
Term
Butorphanol is a agonist at which receptor. How about a weak agonist
Definition
Kappa agonist and a weak mu agonist
Term
Butorphanol is used when?
Definition
Moderate to severe pain
Migraines
Term
What is the adverse effect of Butorphanol
Definition
Dysphoria due to kappa agonist
Term
What kind of agonist is Buprenorphine
Definition
Mu receptor agonist
Term
Buprenorphine can prevent _____ w/draw
Definition
opioid
Term
When do you use buprenorphine
Definition
Moderate to severe pain
Treatment of heroin dependence
Term
Nalbuphine is an agonist which receptors and an antagonist at
Definition
Kappa receptor agonist
Mu receptor antagoinst
Term
Can Nalbuphine precepitiate withdraw in opiod dependent person
Definition
Yes
Term
What are the adverse effects of Nalbuphine
Definition
Sedation, seating and headace
dysphoria at high doses
Term
What's the MOA of Tramadol
Definition
weak mu agonist
Inhibits uptake of NE and 5-HT
Term
when would you use Tramadol. What are it's adverse effect
Definition
Moderate pain
Nausea, constipation
Term
Diphenoxylate and Loperamide are used for
Definition
Anti-diarrhea
Term
Opioid receptor antagonist have a high affinity for which receptor?
Definition
Mu followed by kappa and delta
Term
would you give Naloxone orally?
Definition
No, it's ineffective
Term
You use Naloxone for
Definition
Acute opiod toxicity
Term
Naltrexone has a _____ duration of action
Definition
long
Term
Naltrexone is used as an adjunct for
Definition
treatment of Heroin and alcoholism
Term
What adverse reactions do opiods have? Why don't you want to give opiods when they're taking these drugs
Definition
Antipsychotics, tricyclic antidepressants and sedative-hypnotics
Can lead to greater respiratory depression and orthostatic hypotension
Term
Do you want to give opiods to a person on a local anesthetic?
Definition
No, supra-additive toxicity can happen
Term
If you give _____ and MAO I, it can result in severe reactions that include excitation, ridigity, HTN and death
Definition
Meperidien
Term
Do you want to use opioids in labor?
Definition
No, it can cross the placental barrier and cause neonatal opioid depression
Term
Would you use morphine in Acute pulmonary edema? Why?
Definition
Yes, it's effective in relieving the dyspnea from pulmonary edema associated w/ LV failure
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