Narcotics

Question 1

Endogenous opioid peptides =

Answer 1

Endorphins

Question 2

Endog opioids inhibit responses to what type of stimuli? What else do they modulate?

Answer 2

Painful. Modulate GI, endocrine, and autonomic function as well as rewarding properties

Question 3

Agonists to opioid receptors act how?

Answer 3

Inhibit release of substance P and inhibit ascending transmission from dorsal horn.
Activates pain control circuits descending from midbrain

Question 4

Most prescribed opioids are selective for what opioid receptor for analgesia?

Answer 4

Mu

Question 5

Activation of opioid Mu receptor has what effects on respiration, GI tract, psychologically,

Answer 5

• Decrease resp
• Dec motility and secretion
• Activate limbic system, reward, sedative
• Stim appetite or suppress it
• Inhibit release of ACh causing gut and urinary retention
• Inhibit release of DA

Question 6

Decreased effectiveness with repeated administration. Results in less pain relief and less side effects over time

Answer 6

Tolerance

Question 7

Effects/side effects of opioids

Answer 7

Analgesia, mood alteration and reward, inhibits secretion of LH and FSH (neuroendocrine), miosis, convulsions (lowers seizure thresh), depressed respiration, antitussive, nausea/emesis, GI (terrible constipation), GU (urinary retention), skin (vasodilatation, urticaria)

Question 8

Due to their metabolism, To safely prescribe opiates in the usual doses it’s important that a patient has normal functioning of which two organs?

Answer 8

Kidneys and liver

Question 9

Active metabolite with higher potency of morphine

Answer 9

M-6-glucuronide

Question 10

Low receptor affinity, analgesia via conversion to morphine in a small amount

Answer 10

Codeine

Question 11

Codeine conversion effected by what enzyme?

Answer 11

CYP2D6

Question 12

Synthetic codeine analog, weak Mu agonist, with methylated metabolite more potent analgesic. Less effective for severe pain and less constipating

Answer 12

Tramadol

Question 13

Part of tramadol’s analgesia results from inhibition of uptake of what two nt’s?

Answer 13

NE and Seratonin

Question 14

Fentanyl is how potent? How long of a half-life?

Answer 14

Very potent, very long half-life

Question 15

Without much subQ tissue to absorb and release it, patients who are very thin might not have pain relief from transdermal patches of what drug?

Answer 15

Fentanyl

Question 16

Iatrogenic OD’s occur most commonly with what two opioids?

Answer 16

Fentanyl and methadone - don’t adjust dose any more frequently than 7 days

Question 17

Cheaper tx for chronic pain and for heroine abusers

Answer 17

Methadone

Question 18

Potent oral analgesic assoc’d with widespread abuse and overdose

Answer 18

Oxycodone (percocet = acetaminophen w/ oxy)

Question 19

Meperidine (demerol) no longer recommended due to what?

Answer 19

Toxic metabolite which accum’s the longer you’re on it, interacts with other drugs, causes seizures

Question 20

Congeners of meperidine (imodium and lomotil; loperamide and diphenoxylate respectively) are very effective in treating what?

Answer 20

Diarrhea

Question 21

Useful in tx of opioid toxicity

Answer 21

Naloxone (note: dose only lasts 15 minutes)

Question 22

What type of release opioids are used for breakthrough dosing?

Answer 22

Immediate-release, NOT extended-release opioids

Question 23

What dose is used for breakthrough dosing?

Answer 23

5-15% of 24h dose given every hour prn

Question 24

How are opioids cleared?

Answer 24

Conjugation in liver, excretion by kidney

Question 25

If someone is dehydrated, in renal failure, or severe hepatic failure, what do you do to the dosing interval and size? If they're anuric or oliguric, what do you do to routine dosing?

Answer 25

Decrease the interval (make less frequent) or decrease the dose. Stop routine dosing and use ONLY as needed

Question 26

Is mixed agonist-antagonist recommended? Why?

Answer 26

No - analgesic ceiling effect

Question 27

What factors characterize addiction?

Answer 27

``` Psychological dependence Compulsive use Loss of control over drugs Loss of interest in pleasurable activities Continued use of drugs in spite of harm ```

Question 28

2 proposed mechanisms for tolerance?

Answer 28

Phosphorylation and internalization of receptors

Question 29

Agitation, abd pain, diarrhea, N/V, yawning, piloerection signal what is happening

Answer 29

Withdrawal

Question 30

A process of neuroadaptation that can be accompanied by withdrawal symptoms upon abrupt stoppage of opioids that is NOT considered addiction

Answer 30

Physical dependence

Question 31

What are we adjusting for when we start switch a new drug and give at only a percentage of the equianalgesic dose?

Answer 31

Incomplete cross-tolerance

Question 32

Common opioid adverse effects

Answer 32

Constipation, dry mouth, n/v, sedation, sweats

Question 33

Uncommon opioid adverse effects

Answer 33

bad dreams/hallucinations, dysphoria/delirium, myoclonus/seizures, pruritus/urticaria, resp depression, urinary retention

Question 34

In constipation, what agents are actually avoided and what are used?

Answer 34

Don't use bulk forming agents like metamucil for risk of bowel obstruction. Use stimulant laxative (ex: Senna) with or wihtout a stool softener (docusate sodium). START when you start the opioid

Question 35

Mechanism of action of opioids is via...

Answer 35

GPCopioidRs

Question 36

Tolerance occurs with all side effects except...

Answer 36

Constipation