Neuro: Opioids

Front 1

T/F: Opioids are better at suppressing sharp discrete pain (neospinothalamic pathway) than dull pain(paleospinothalamic pathway).

Back 1

F. Opioids are better at treating dull pain.

Front 2

Which opioid receptor is involved in supraspinal analgesia?

Back 2

mu receptor. Inhibits pain transmission and the affective response to pain.

Front 3

What type of derivatives do you get when substitute -OCH3 group at position 3 on the 5-ring structure of opioids?

Back 3

codeine derivatives: treat moderate pain.

Front 4

What type of derivatives do you get when substitute position 6 on the 5-ring structure of opioids?

Back 4

morphine: better absorption orally.

Front 5

What type of derivatives do you get when substitute allyl group at position 17 on the 5-ring structure of opioids?

Back 5

pure opioid antagonist

Front 6

If you substitute a allyl group at position 17 of hydromorphone, what do you get?

Back 6

naloxone: a pure antagonist.

Front 7

What are the effects of morphine on CNS? (10)

Back 7

1. analgesia
2. drowsiness and mental clouding
3. euphoria and dysphoria
4. miosis
5. reduced respiration
6. nausea, vomiting
7. cadiovascular system
8. constipation
9. sphinctor of oddi constriction
10. urinary retention

Front 8

How does morphine cause drowsiness and mental clouding?

Back 8

It supresses NE firing.

Front 9

How does morphine cause euphoria?

Back 9

disinhibition of reward system

Front 10

If a patient comes in with pinpoint pupil even under dim light, what would you suspect? And what might this person die of?

Back 10

morphine overdose
respiratory failure

Front 11

How does morphine cause reduced respiration?

Back 11

decreased sensitization to CO2. CO2 is the primary drive to respiration.

It also depresses respiratory center in medulla: depression of cough reflex, therapeutic at lower doses.

Front 12

Why should patients lie down when giving first couple doses of morphine? (hint: This is also the reason why ambulatory patients are more likely to vomit)

Back 12

Morphine stimulate vestibular system additive to chemoreceptor trigger zone (medulla) which transmits impulses to vomit center.

Front 13

After a few doses of morphine, it actually inhibits vomiting. Why?

Back 13

Morphine penetrates to the brainstem and suppresses the vomit center.

Front 14

What are some cardiovascular effects of morphine?

Back 14

1. suppression of baroreceptor reflex
2. release histamine which cause vascular smooth muscle relaxation and bronchoconstriction.
3. suppresses adrenergic tone and reduces reflex vasoconstriction caused by postural changes.
4. cerebral vessel dilation due to increase in CO2, and lead to increased intracranial pressure.

Front 15

Why do some people scratch after taking morphine?

Back 15

Morphine causes release of histamine.

Front 16

How does morphine raise intracranial pressure?

Back 16

Decreased respiration causes build up of CO2 which leads to cerebral artery dilation, thus increases intracranial pressure.

Front 17

What is the double negative effect of morphine on digestive system?

Back 17

1. increase tone in longitudinal and sphicter muscle: constipation.
2. reduced peristalsis: constipation.

Front 18

What is the main problem of using morphine on cancer patients?

Back 18

constipation

Front 19

Why do you need an extremely high dose morphine to treat patients with biliary colic?
What could be used instead?

Back 19

Morphine constrict sphintor of oddi, increases pressure in the bile tree.

Demerol(meperidine) could be used instead.

Front 20

How does morphine cause urinary retention?

Back 20

Morphine inhibits detrusor muscle and increases sphinctor tone.

Front 21

Name some synthetic opioids. (7)

Back 21

1. Morphine
2. Meperidine(Demerol)
3. Methadone
4. Codiene
5. Fentanyl
6. Tremadol
7. Oxymorphone

Front 22

What are the advantage and downside of Meperidine(demerol)?

Back 22

Advantage: less biliray spasm, useful in treating biliary colic.

Downside:
1. widely abused because of its short duration.
2. metabolite highly reactive with MAO inhibitors.
3. anticholinergic: cardiovascular dysfunction, effects on serotonine systems.

Front 23

Diphenoxylate is a derivative of ____. What are its uses?

Back 23

meperidine
Diphenoxylate is useful in treating diarrhea, but it is not well absorbed in the gut.

Front 24

Loperamide is a derivative of ____. What are its uses?

Back 24

meperidine
Loperamide can be used for diarrhea, and has low abuse potential because it does not cross BBB. It increases anal sphinctor tone.

Front 25

Name two derivatives of meperidine that treat diarrhea.

Back 25

Diphenoxylate
Loperamide

Front 26

What are some advantages of methadone?

Back 26

1. longer duration: increased protein binding in the plasma.
2. better oral absorbance

Front 27

What is methadone useful in?

Back 27

1. analgesia
2. heroin abuse

Front 28

Which is a congener of methadone that is not widely used because of its toxicity and less activity?

Back 28

Propoxyphene

Front 29

What is an opioid that is useful in treating cough, mild pain, and diarrhea?

Back 29

codeine

Front 30

Which drug blocks the effect of codeine?

Back 30

Prozac: inhibit P450 that converts codiene to morphine.

Front 31

Which opioid is useful for neuroleptic anesthesia?

Back 31

Fentanyl in combination with butyrophenone: 80 times more potent than morphine, short acting.

Front 32

Fentanyl patches are used for ____.

Back 32

severe chronic pain, produce less constipation.

Front 33

Name one opioid that can be helpdul in cancer patients.

Back 33

Fentanyl patches
Alvimopam

Both produce less constipation

Front 34

Which opioid is a good choice for treat children with pain and anxiety?

Back 34

Fentanyl lozenges.

Front 35

Which opioid has similar action as antidepressants duloxetine and vanlefaxine?

Back 35

tramadol: weak mu agonist, blocks reuptake of serotonine and NE.

Front 36

What is a common opioid used for treating severe pain in outpatient setting?

Back 36

Hydrocodone in combination with NSAIDS.

Front 37

What is the sustained release form of oxymorphone?

Back 37

oxycontin

Front 38

What are the 2 types of partial agonists?

Back 38

1. Partial mu agonist
2. mixed mu antagonist and kappa agonist

Front 39

Low dose partial mu agonist ____ (will/will not) substitute for morphine where as high dose will ____.

Back 39

Low dose partial mu agonist will substitute for morphine where as high dose will precipitate withdrawl.

Because high dose will compete with morphine for receptors.

Front 40

What is the name of the one partial mu agonist?

Back 40

Buprenorphine: respiratory depression ceiling.

- highly lipophilic
- treatment for opioid dependence.

Front 41

What are the three pure mu antagonist?

Back 41

1. Naloxone: short acting
2. Naltrexone: long acting
3. Nalmefene: intermediate duration

All three can precipitate withdrawal in the opioid dependent patients.

Front 42

In patients with morphine dependence, mixed agonist-antagonist will____.

Back 42

only precipitate withdrawal

Front 43

Rank the following in decreasing mu agonist effect:
pentazocine
buphrenorphine
nalbuphine

Back 43

buphrenorphine > pentazocine > nalbuphine

Front 44

What are the ingredients in T's and Blues (heroin addicts)? How to solve this problem?

Back 44

Pentazocine and Tripelenamine (antihistamine)

Add naloxone with pentazocine: when inject with tripelenamine will make addicts sick. In normal use, naloxone will degrade very fast without any effects.

Front 45

Name the 4 mixed agonist-antagonists.

Back 45

1. pentazocin
2. nalbuphine
3. butorphanol

Front 46

Whicn agonist-antagonist has most profound respiratory ceiling effect?

Back 46

nalbuphine: due to kappa effect.

Front 47

Which drug has pure kappa effect?

Back 47

butorphanol

Front 48

How is opioid best administered?

Back 48

Intramuscularly.

Front 49

Why does IV opioids require great care in administering?

Back 49

Potential severe respiratory depression and gut spasm.

Front 50

Which is more lipid soluble, heroin or morphine?

Back 50

heroin

Front 51

What is the one class of drug that require glucuronide conjugation for its active function?

Back 51

opioids.

subsequent glucuronide conjugation at 3 position will make the molecule more polar and facilitate excretion.

Front 52

T/F: Tolerance is most noted for the depressant activities of opioids, and less so for the stimulant effects.

Back 52

T.

Front 53

What is the withdrawal syndrome? How is it different from the drug's therapeutic effect?

Back 53

The withdrawal syndrome develops when drug is removed after the drug has become required for the tissue's homeostasis.

The symptoms are opposite to the actual therapeutic effects. Ex. opioids: nausea, vomit, diarrhea, yawning, leg twitching, cramps, sweating, chills, goose flesh (rebound hyper-excitability due to NE over-reactivity).

Front 54

Which type of people will show miosis, constipation, along with less euphoria, less respiratory depression?

Back 54

People who are tolerant and dependent upon opioids.

Front 55

T/F: There is cross tolerance among drugs within the same class as well as drugs of different classes.

Back 55

F. Cross reaction only with drugs within the same class.

Front 56

What is the classical triad of opioid overdose symptoms?

Back 56

respiratory depression
coma
pinpoint pupils

Front 57

How do you treat opioid overdose?

Back 57

1. ventilation of airway
2. slow administration of opioid antagonist naloxone.

Front 58

If an unexperienced ER doctor gave a large dose of naloxone to treat an opioid overdosed patient, what will happen and how do you reverse effect?

Back 58

Patient will experience dangerous withdrawal.

Clonidine (alpha 2 antagonist) can be used to reduce NE-related effects. (giving more opioids will not help)

Front 59

What is a good dosage of opioid to give to a patient with acute pain before making a diagnosis?

Back 59

1/2 of the standard dosage because you don't want to mask the symptoms that will help you making the diagnosis.

Front 60

Why is the under-treatment of severe pain a significant problem?

Back 60

Because only 2/3 of the patients respond well to the standard dose. So for those who is still complaining of pain under standard dosage, you need to ramp up the dosage.

Front 61

What is the benefit of patient-controlled analgesia? and what is one caution needs to be addressed?

Back 61

1. when patient feels in control, less total amount of opioids is actually administered.

2. Need to keep other people(family members) away from the control.

Front 62

Where is patient-controlled analgesia used?

Back 62

Used for post operation pain, sickle cell crisis, and cancer.

Front 63

T/F: Control of pain is better and with lower dose when scheduled to prevent the re-occurrence of pain rather than repeatedly suppressing it after it returns.

Back 63

T.

Front 64

How are opioids helpful in cardiac emergencies such as acute ventricular failure?

Back 64

It decreases O2 consumption and lower cardiac work load.

Front 65

Name a sigma receptor stimulator that helps in treating cough.

What is the most commonly used opioid for cough?

Back 65

Dextromethorphan: does not work in kids.

Most often used: codeine.

Front 66

What are the reasons that care should be taken to treat patients with cranial injuries using opioids? (2)

Back 66

1. opioids increases intracranial pressure.

2. opioids produce CNS and respiratory depression which will mask clinical symptoms.

Front 67

What type of opioids can be used to treat patients with asthma attacks or chronic compromised respiratory reserve?

Back 67

kappa agonist: less respiratory effects.

Front 68

What are some drug-drug interactions with opioids? (5)

Back 68

1. MAO inhibitors: potentiates opioid effects. Avoid Merperidine and its congeners.
2. NSAIDS/ASA: good pain control with lower doses.
3. tricyclic antidepressants(gabapentine, pheytoin, carbamazepine, clonazepine) and phenothiazines.
4. sympathomimetics: ex. cocaine, or amphetamine enhance euphoria.
5. depressants: alcohol.