Opiate Analgesics

Front 1

What is analgesia?

Back 1

Relief of pain without loss of consciousness

Front 2

Where do opiates come from?

Back 2

They are alkaloids from opium poppy seeds.

Examples include morphine, codeine

Front 3

What are Opioids?

Back 3

Natural and semisynthetic opiates and synthetic drugs with similar actions.

Front 4

How do opioid receptors work? What areas of the body do they work in? (2)

Back 4

Interact with specific protein receptors in the CNS and GI tract. Depending on where they act in the brain, they can mediate various effects.

Front 5

Receptor families are classified as...(4)

Back 5

1. Mu
2. Kappa
3. Delta
4. Sigma

Front 6

What do opiod receptors do in the...
1. Brainstem?
2. Medial thalamus?
3. Spinal cord?
4. Hypothalamus
5. Limbic system

Back 6

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

Front 7

What are endogenous opiates?

What are they otherwise known as?

Describe their structure and duration.

Back 7

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.

Front 8

What is an example of an endogenous opiate?

Back 8

Runner's high - after pain, exhaustion you feel a good, feel a release or a high.

Front 9

What are strong opioid analgesics used for? Strong agonists?

Where do they act and on what receptors?

Back 9

Used to treat severe pain.
Act on mu and kappa receptors in the CNS

Front 10

What are some examples of strong agonists of opioid analgesics?

Back 10

MMDD: Morphine, methadone, demerol and duragesic.

Hint 10

MMDD

Front 11

What is the gold standard for pain?

Back 11

Morphine

Front 12

Describe Demerol.

Back 12

-Synthetic agent
-Can cause weird reactions such as dysmorphia, but is still used

Front 13

How is the drug Duragesic administered? Describe it's duration.

Back 13

Can be injected or delivered via a patch (3 day duration)

Short duration

Front 14

1. When are moderate opioid agonists used?
2. What receptors do they act on?
3. How are they used?

Back 14

-Used to treat pain of moderate intensity
-Act on mu and kappa receptors
-Used in combo w/ Acetaminophen or Aspirin

Front 15

Name four examples of moderate opioid agonists.

Back 15

1. Codeine
2. Hydrocodone
3. Oxycodone
4. Propoxphene

Hint 15

CHOP

Front 16

Rank the following in order of most potent to least potent. Hydrocodone, Codeine, Oxycodone

Back 16

Oxycodone>Hydrocodone>Codeine

Front 17

What is Codeine and what is is used in combo with?

Back 17

Tylenol #3 is a combo w/ Acetaminophen

Front 18

What is an example of hydrocodone? What is it used in combo w/?

Back 18

Vicodan w/ Acetaminophen

Front 19

What can oxycodone be used in combo with?

Back 19

Acetaminopeh AND aspirin

Front 20

What is the most potent oral pain medication?

Back 20

Oxycodone

Front 21

How do mixed agonists-antagonists work?

Why are they beneficial?

Back 21

Stimulate one opioid receptor (kappa) and block another (mu) simultaneously.

They produce adequate analgesia with less risk of tolerance and dependence.

Front 22

What are some examples of Mixed Agonists-Antagonists? (3)

Back 22

Talwin (abused by junkies), Nubain, Stadol (addicting, nasal inhalant)

Hint 22

TNS

Front 23

How do Antagonists opioids work?

When are they primarily used?

Tolerance?

Back 23

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.

Front 24

What are some examples of antagonists?

Back 24

Narcan and Trexan

Front 25

How do opioid ANTAGONISTS work?

Back 25

Effects produced by opioid analgesics are due to their interaction with Mu and Kappa receptors.

Front 26

What are Mu receptors responsible for?

Back 26

Analgesia at the supraspinal level, euphoria, respiratory depression and physical dependence.

Front 27

What are Kappa recpetors responsible for?

Back 27

Analgesia at the spinal level, miosis and sedation.

Front 28

What are sigma receptors responsible for?

Back 28

Dysphoria, hallucinations, paranoia and cardiac stimulant actions.

Front 29

Drugs that act on mu-receptors have high abuse potential. Why?

Back 29

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.

Front 30

What effect does morphine have on the CNS system? (4)

Dose?

Back 30

-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.

Front 31

What effect does morphine have on the respiratory system? (1)

Back 31

Changes the sensitivity of the repiratory center to blood levels of CO2.

Front 32

Effect of Morphine on cough? (1)

Back 32

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.

Front 33

What are some GI effects of morphine? (2)

Back 33

-Decrease motility which leads to constipation
-Increase tone of sphincter of Oddi (bile duct) and anus.

Front 34

Other uses of Morphine? (2)

Back 34

1. Release of histamine from mast cells, causes itching
2. Prolongation of labor

Front 35

What are the SE of using Morphine? (6)

Back 35

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

Front 36

What are the therapeutic uses of morphine? (3)

Back 36

1. Analgesia
2. Treatment of diarrhea
3. Relief of cough, as long as it's not over done

Front 37

What is the prototype moderate opioid agonists used?

Back 37

Codeine

Front 38

1. How is codeine administered?
2. SE?
3. Uses?
4. Combinations?

Back 38

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

Front 39

What is the prototype for Mixed agonists-antagonists?

Back 39

Talwin

Front 40

1. How is Talwin administered?
2. SE?
3. Uses?

Back 40

1. Orally or parenterally
2. Anxiety, Hallucinations, dependence and abuse. May precipitate w/drawal in addicted patients.
3. Relieve moderate pain

Front 41

What is the prototype for ANTAGONISTS?

Back 41

Narcan

Front 42

1. How does Narcan work?
2. Uses?
3. Tolerance?
4. Administered?

Back 42

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

Front 43

Implications for PT related to SE?

Back 43

-Respiratory depression, dizziness, sedation and how that can impact physical performance/endurance of patients undergoing rehab

Front 44

PT implications in regard to tolerance?

Back 44

-Tolerance to drugs and physical dependence/psychological may affect performance

Front 45

PT implications in regard to timing with opiate analgesics?

Back 45

May need to adjust PT session to match maximum pain relief (medication peak) unless the SE are a concern at that time.