Neuro Test 1: Hupka_Opiods

Front 1

What tracts/ fibers of pathways carry:

-FAST --> localized, sharp, prickling pain that is somatic and cutaneous in origin

Back 1

Aδ fibers

Neosinothalamic tract

Front 2

What tracts/ fibers of pathways carry:

SLOW – diffuse, dull, aching, burning pain, visceral and deep structure in origin

Back 2

C fibers

Paleospinothalamic tract

Front 3

Does neuropathic pain respond well to opiods?

Back 3

No..

Neropathic pain is caused by DAMAGE to neural pathways and responds poorly to opiods. Try an antidepressant!

Front 4

MOA: Opiods

Activation of ___ leads to decreased cAMP and:

-Closure of voltage-gated Ca2+ channels on PREsynaptic nerve terminals, which decreases
neurotransmitter release

-Opening of K+ channels causing
hyperpolarization (inhibition) of POSTsynaptic neurons.

**EXAM**

Back 4

Gi

**Opiod receptors are linked to G proteins**

Front 5

Morphine:

-causes direct stimulation of CTZ

are high or low doses more likely to produce emesis?

Back 5

Low doses make you puke!!

**High doses or chronic use depress vomiting center**

Front 6

Which of the following opioids is least likely to suppress cough?

-Codeine

-Morphine

-Meperidine

-Methadone

**EXAM**

Back 6

MEPERIDINE

Methadone > codeine > morphine > meperidine

**EXAM**

Front 7

Naloxone, naltrexone, and nalmefene all ANTAGONIZE opiod receptors. Which receptor sub-type do they have the greatest affinity for?

****

Back 7

μ receptor

Front 8

What receptors are blocked by naloxone? What receptor is NOT blocked?

Back 8

μ, δ, κ are all blocked by naloxone;

**N/OFQ is not**

Front 9

Name the opioid receptors

Back 9

μ
δ
κ
N/OFO

Front 10

GI side effect of opioids?

Back 10

Constipation

Front 11

MIXED AGONISTS/ANTAGONISTS:

Buprenorphine
Pentazocine
Nalbuphine
Butorphanol

These drugs are all PARTIAL AGONISTS of the μ receptor **

Which one is an ANTAGONIST of the kappa receptor?

**EXAM**

Back 11

Buprenorphine

Front 12

Morphine may cause euphoria.

What is the significance of an opioid causing euphoria?

Back 12

major contributor to abuse liability

Front 13

Morphine's Peripheral Actions:

How does morphine affect:

-GI tract

-Billiary Tract

-Urinary Tract

Back 13

-GI tract -
↑ tone, ↓ peristalsis – constipation**

-Biliary-
↑ tone of common bile duct and sphincter of Oddi to ↑ biliary
pressure causing biliary spasm

-Urinary Tract-
↑ sphincter muscle tone → ↓urinary output

Front 14

Does meperidine or morphine cause more biliary spasm? What can you use to treat biliary spasm?

Back 14

Meperidine > Morphine

Tx: nitroglycerine, atropine, naloxone

Front 15

Morphine CNS effects:

Morphine causes respiratory depression. Should you give your patient 100% O2?

Back 15

No!

Hypoxia is the only thing keeping the patient breathing (CNS)

Try naloxone to reverse morphine's effects

Front 16

Morphine Peripheral Effects:

How do most opiods affect the CV system?

**EXAM**

Back 16

Most opioids have little effect on the heart but may produce:

**DOSE-DEPENDANT BRADYCARDIA**

(↑ PNS and ↓ SNS ?)

Front 17

How can morphine, codeine, and meperidine cause:

-Itching, sweating, redness of eyes
-Bronchoconstriction

Back 17

Histamine Release!

be careful in ASTHMATICS

Front 18

Why do you want to avoid giving an opioid in someone with head trauma?

Back 18

Cerebral vasodilation --> ↑ Intracranial pressure ***

Front 19

Can morphine cross the placenta?

Who would have more CNS effects, an adult or a neonate?

*OBJ*

Back 19

Morphine crosses the placenta!!!

-Limited crossing of BBB in adults

-No fully developed BBB in neonates so increased amounts of drug can enter the CNS!

Front 20

What is the major elimination mechanism of most opioids?

**EXAM**

Back 20

**Metabolism**

Rapid glucuronide conjugation in liver and intestine

(Note: metabolites of morphine are more potent than morphine itself!)

Front 21

What is special about Codeine's metabolism and analgesic effect?

***

Back 21

Codeine is a methylated form of morphine = ORALLY ACTIVE

**must be metabolized to morphine (by CYP2D6) to be fully active**

-good for mild-moderate pain

Front 22

Morphine is good for ___ to ____ pain

Back 22

moderate to severe pain

Front 23

Which opioid is used to reduce post-surgical shivering?

**EXAM**

Back 23

Meperidine

Front 24

Patients taking opioids may experience some tolerance of some of the effects. What are the 2 effects that he pointed out that had MINIMAL to NO TOLERANCE?

**EXAM**

Back 24

miosis

constipation

(So, all patients will probably have this no matter how tolerant)

Front 25

What is the name of the morphine metabolite that is 4-6X more potent than morphine?

***

Back 25

morphine-6-glucoronide

Front 26

Bradycardia has a ___ degree of tolerance with opioid use

Back 26

Moderate degree of tolerance

Front 27

Name some contraindications to opioid use (just read)

Back 27

Bronchial asthma
Emphysema
Liver damage
Head injuries
Acute alcohol use
Previous dependence
Convulsive disorders
Abdominal pain of unknown origin

Front 28

Notes about Tolerance:

MARKED TOLERANCE occurs to the **depressant actions** of morphine

LITTLE to NO tolerance of **stimulating actions** of morphine (***miosis, constipation***)

Back 28

Front 29

This drug, in a small dose, may ENHANCE morphine's effect

Back 29

Amphetamine

Front 30

CNS depressant effects of morphine may be prolonged or exaggerated by what types of drugs?

**OBJ**

Back 30

CNS DEPRESSANTS:
-phenothiazines
-MAOI
-tricyclic antidepressants

Front 31

Indicate the primary cause of death from opioid overdose

Back 31

Respiratory Failure

Front 32

Analgesia is generally related to agonistic activity at____receptors
and to a lesser extent μ receptors

Back 32

κ receptors

Front 33

A patient you have recently given morphine presents with the following triad:

**coma, pinpoint pupils, respiratory depression**

What's going on? How do you treat it?

Back 33

Acute Overdose Symptoms!!

Tx:
-MAINTAIN RESPIRATION
-Opioid Antagonist --> IV Naloxone

Front 34

Why is methadone used for opiate-dependent individuals?

*OBJ*

Back 34

-Withdrawal Syndrome is long and relatively mild

(half-life is about 20 hrs)

Front 35

Which opioid receptor subtype causes the greatest effects of:
-analgesia
-euphoria
-miosis
-physical dependence
-respiratory depression

*OBJ*

Back 35

μ receptor

Front 36

Which opioid receptor causes dysphoria and has the least chance of causing respiratory depression?

Back 36

kappa-receptor

Front 37

Pentazocine, Morphine, Naloxone

Which is an agonist at the μ receptor?

Which is a partial agonist at the μ receptor?

Which is an antagonist at the μ receptor?

*OBJ*

Back 37

Morphine = Ag

Pentazocine = pAg

Naloxone = Ant

Front 38

naloxone vs. naltrexone

Which is administered parenterally only?

Which is orally effective?

Back 38

Parenterally only = Naloxone

Orally Effective = Naltrexone

Front 39

Should you use naloxone to stop opiate effects in a chronic user?

Back 39

No, you should avoid abrupt cessation of therapy...

Use methadone to wean pt. and prevent acute and severe withdrawal symptoms

Front 40

15. Indicate which one of the opioid analgesics is most likely to produce a serotonin syndrome if used in combination with monoamine oxidase inhibitors

serotonin syndrome (severe
restlessness, hyperpyrexia, and hypertension)

*OBJ*

Back 40

Meperidine

-meperidine blocks 5HT - NE reuptake

Front 41

17. Indicate one of the main differences between fentanyl and morphine?

**obj**

Back 41

50 -100 x more potent than morphine

Front 42

Indicate what unique pharmacokinetic aspects of remifentanil make it more useful for infusion anesthesia than the other meperidine congeners?

Back 42

-Rapidly metabolized by tissue and blood esterases giving it an extremely short half life

-Rapid onset and brief duration allows careful titration of dose
to effect (infusion anesthesia)

(continuous IV)

Front 43

Indicate the relationship between tolerance, physical dependence, and intensity of withdrawal syndrome.

Back 43

Degree of tolerance indicates the degree of PD that has developed

Greater degree of PD means higher intensity of withdrawal syndrome

Front 44

Which has a higher risk of death, opiate withdrawal or alcohol/barbituate withdrawal?

**EXAM**

Back 44

Alcohol/Barbiturate Withdrawal
(CNS depressants)

Front 45

Which is LEAST likely to cause constipation?

Codeine
Morphine
Meperidine

Back 45

Meperidine

Front 46

Which is LEAST likely to suppress cough?

Codeine
Morphine
Meperidine

Back 46

Meperidine

Front 47

What may be a side effect of meperidine metabolites?

Back 47

Metabolite= ** normeperidine **

-non-analgesic stimulant which accumulates with repeated doses and may cause seizures

- Decreased use of meperidine

Front 48

Are opioid analgesics more effective against slow or fast pain?

Back 48

Slow pain

Front 49

22. Compare the relative analgesic potency of morphine, meperidine, fentanyl

Back 49

Fentanyl >>> Morphine >> Meperidine

Front 50

23. Indicate the use of methylnaltrexone and alvimopan and the mechanism by which they work.

Back 50

**Methylnaltrexone**
reverses opioid-induced CONSTIPATION in chronic opioid users (has no analgesic effect)

**Alvimopan**
-used to treat POST-OP ILEUS after bowel resection