Narcotic Analgesics

Question 1

What are the physiological effects of the opioids on the CNS?

Answer 1

analgesic effects:
-some sedation (not a significant CNS depressant)

• mood elevation
• nausea - direct effect on chemoreceptor trigger zone on CNS
• decreased respiration - direct effect on brain respiratory center
• decreased cough reflex
• stimulation of oculomotor n. nucleus = severe miosis aka “pin-point pupils”
• hyperthermia

Question 2

What are the physiological effects of the opioids on the GI system?

Answer 2

random GI contractions = constipation

Question 3

Name 4 additional physiological effects caused by the opioids.

Answer 3

• vasodilation = skin flushing, orthostatic hypotension
• increase cerebrospinal fluid pressure
• increase release of histamine = bronchoconstriction + itching
• ability to pass placenta

Question 4

How can opiates be classified?

Answer 4

By the receptor on which they act

Question 5

Name 3 endogenous opiate-like peptides

Answer 5

These act on specific receptors:

• enkephalins
• endorphins
• dynorphins

Question 6

What is the most significant opiate receptor subtype?

What is their effect?

Can be used to treat?

Answer 6

μ-opioid receptors (MOR)

Effects:

• euphoria
• respiration depression
• gut motility

Treat:

• pain
• cough

(pain and cough were IDed under treatment by interpretation from his notes)

Question 7

Activation of the opiate receptor results in what?

Answer 7

decrease in cAMP

Question 8

Opiates are _______, they ___________ NT release from selected neurons

Answer 8

neuromodulators, inhibit

Question 9

Describe the basis of addiction to opiates

Answer 9

cAMP is a cell signal - the cell accommodates to continual stimulation or inhibition of cAMP levels

Addiction: pleasure of addictive experience + fear of consequences of withdrawal

Question 10

Describe effects of opiate withdrawal

Answer 10

severe vasoconstriction:

• cold
• clammy
• runny nose
• piloerection = goose bumps or turkey bumps, hence, “cold turkey”

GI system effects:

• cramping
• diarrhea
• nausea

CNS effects:

• dysphoria
• restless twitching, hence, “kicking the habit”

Pupils:
mydriasis

Question 11

Tx for opiate withdrawal

Answer 11

“cold-turkey” = no tx

ultrarapid withdrawal: G.A.

Question 12

name the 3 opiate agonist types

Answer 12

1. natural analogs
2. semisynthetic analogs
3. synthetic analogs

Question 13

what are the 2 opiate natural analogs?

characteristics of each?

Answer 13

1. morphine: 1st pass effect
2. codeine:
   - partial agonist
   - low antinociceptive effects
   - not subject to 1st pass metabolism
   - greater effect on coughing (antitussive)

Question 14

what are the 3 semisynthetic opiate agonists?

characteristics of each?

Answer 14

1. heroin - 5x morphine
2. hydromorphone - 10x morphine
3. oxycodone - partial agonist is available in oral form “oxycontin”

Question 15

What are the 5 synthetic opiate analogs?

Answer 15

1. fentanyl: 80 - 100x morphine

and sufentanil / alfentanil / remifentanil (500-600x morphine)

2. meperidine: .5x morphine
3. methadone: 1x morphine
4. oxymorphone
5. levorphanol

Question 16

Name a partial opiate agonist besides codeine

Answer 16

pentazocine

Question 17

Name 3 agents that serve as opiate receptor blockers.

Answer 17

1. naloxone
2. naltrexone
3. methylnaltrexone

Question 18

name 2 agents that act both as narcotics and SSRIs

Answer 18

tramadol

tapentadol

Question 19

what are the indications for opioids?

contraindications?

Answer 19

cancer, burn, surgery, trauma, pain

contra: undiagnosed pain

head trauma - b/c of increased intracranial pressure

convulsive disorder - may increase likelihood of seizures

respiratory difficulties