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45 Cards in this Set

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What is analgesia?
Relief of pain without loss of consciousness
Where do opiates come from?
They are alkaloids from opium poppy seeds.

Examples include morphine, codeine
What are Opioids?
Natural and semisynthetic opiates and synthetic drugs with similar actions.
How do opioid receptors work? What areas of the body do they work in? (2)
Interact with specific protein receptors in the CNS and GI tract. Depending on where they act in the brain, they can mediate various effects.
Receptor families are classified as...(4)
1. Mu
2. Kappa
3. Delta
4. Sigma
What do opiod receptors do in the...
1. Brainstem?
2. Medial thalamus?
3. Spinal cord?
4. Hypothalamus
5. Limbic system
1. Mediate control of respiration, BP, cough, pupillary diameter, nausea, vomiting, and stomach secretions. (All CN functions)
2. Mediate deep pain
3. Mediate spinal analgesia
4. Mediate neuroendocrine secretions
5. Influence emotional behavior, which can present with SE
What are endogenous opiates?

What are they otherwise known as?

Describe their structure and duration.
Opiate-like substances released by the body to control pain under specific conditions.

Otherwise known as endorphins and enkephalins.

Peptides with very short duration of action.
What is an example of an endogenous opiate?
Runner's high - after pain, exhaustion you feel a good, feel a release or a high.
What are strong opioid analgesics used for? Strong agonists?

Where do they act and on what receptors?
Used to treat severe pain.
Act on mu and kappa receptors in the CNS
What are some examples of strong agonists of opioid analgesics?
MMDD: Morphine, methadone, demerol and duragesic.
What is the gold standard for pain?
Describe Demerol.
-Synthetic agent
-Can cause weird reactions such as dysmorphia, but is still used
How is the drug Duragesic administered? Describe it's duration.
Can be injected or delivered via a patch (3 day duration)

Short duration
1. When are moderate opioid agonists used?
2. What receptors do they act on?
3. How are they used?
-Used to treat pain of moderate intensity
-Act on mu and kappa receptors
-Used in combo w/ Acetaminophen or Aspirin
Name four examples of moderate opioid agonists.
1. Codeine
2. Hydrocodone
3. Oxycodone
4. Propoxphene
Rank the following in order of most potent to least potent. Hydrocodone, Codeine, Oxycodone
What is Codeine and what is is used in combo with?
Tylenol #3 is a combo w/ Acetaminophen
What is an example of hydrocodone? What is it used in combo w/?
Vicodan w/ Acetaminophen
What can oxycodone be used in combo with?
Acetaminopeh AND aspirin
What is the most potent oral pain medication?
How do mixed agonists-antagonists work?

Why are they beneficial?
Stimulate one opioid receptor (kappa) and block another (mu) simultaneously.

They produce adequate analgesia with less risk of tolerance and dependence.
What are some examples of Mixed Agonists-Antagonists? (3)
Talwin (abused by junkies), Nubain, Stadol (addicting, nasal inhalant)
How do Antagonists opioids work?

When are they primarily used?

Block ALL opioid receptors, no selectivity.

In the treatment of opioid overdose or to rapidly reverse the effects of opiates when pain control is no longer needed and the patient remain sedated/incapacitated.

i.e. outpatient surgery, diagnostic tests

There is no tolerance to these drugs. Can use them again and again without developing a tolerance to them.
What are some examples of antagonists?
Narcan and Trexan
How do opioid ANTAGONISTS work?
Effects produced by opioid analgesics are due to their interaction with Mu and Kappa receptors.
What are Mu receptors responsible for?
Analgesia at the supraspinal level, euphoria, respiratory depression and physical dependence.
What are Kappa recpetors responsible for?
Analgesia at the spinal level, miosis and sedation.
What are sigma receptors responsible for?
Dysphoria, hallucinations, paranoia and cardiac stimulant actions.
Drugs that act on mu-receptors have high abuse potential. Why?
Cause euphoria. The psychological addiction to opiates is far more challenging to over come than the physical addiction. May require months of counseling after the short (72 hours) physical withdrawal phase.
What effect does morphine have on the CNS system? (4)

-Change pain perception and patient reaction to pain
-Increases tolerance for pain
-Causes Euphoria
-Stimulates chemoreceptor trigger zone leading to nausea and vomiting.

It's a dose-related analgesic.
What effect does morphine have on the respiratory system? (1)
Changes the sensitivity of the repiratory center to blood levels of CO2.
Effect of Morphine on cough? (1)
Depression of cough reflex and make for an excellent antitussive treatment. It's a good way to check to see how deep someone is under.
What are some GI effects of morphine? (2)
-Decrease motility which leads to constipation
-Increase tone of sphincter of Oddi (bile duct) and anus.
Other uses of Morphine? (2)
1. Release of histamine from mast cells, causes itching
2. Prolongation of labor
What are the SE of using Morphine? (6)
1. Respiratory depression
2. Tolerance. Have to progressively increase dose to illicit same response.
3. Physical dependence, esp w/ people who have an addicting personality
4. Nausea and vomiting
5. Constipation, don't use with HR pts. Usually opiate are given with anti-constipation.
6. Urinary retention
What are the therapeutic uses of morphine? (3)
1. Analgesia
2. Treatment of diarrhea
3. Relief of cough, as long as it's not over done
What is the prototype moderate opioid agonists used?
1. How is codeine administered?
2. SE?
3. Uses?
4. Combinations?
1. Orally
2. Less SE than morphine
3. Useful and commonly used as a cough suppressant. Short term use.
4. Combined w/ Acetaminophen for synergy
What is the prototype for Mixed agonists-antagonists?
1. How is Talwin administered?
2. SE?
3. Uses?
1. Orally or parenterally
2. Anxiety, Hallucinations, dependence and abuse. May precipitate w/drawal in addicted patients.
3. Relieve moderate pain
What is the prototype for ANTAGONISTS?
1. How does Narcan work?
2. Uses?
3. Tolerance?
4. Administered?
1. Blocks opioid receptors to precipitate a w/drawal syndrome in opioid addicted patients.
2. Reverse the sedative, respiratory depressant and adverse CV effects of opioids. Get opioid addicted patients in w/drawal or treatment of overdose.
3. There is no tolerance to its anatagonistic actions
4. Parenterally/injection ONLY. Not administered orally, life-saving antidote
Implications for PT related to SE?
-Respiratory depression, dizziness, sedation and how that can impact physical performance/endurance of patients undergoing rehab
PT implications in regard to tolerance?
-Tolerance to drugs and physical dependence/psychological may affect performance
PT implications in regard to timing with opiate analgesics?
May need to adjust PT session to match maximum pain relief (medication peak) unless the SE are a concern at that time.