Pharmacology Winter Test 2 L3 Opioids

Front 1

What are all opioid receptors coupled to?

Back 1

Gi/o proteins

Front 2

What Do opioids do when the bind the receptors? (2 phases, both pre and post synaptic)

Back 2

1) closes voltage gated Ca2+ channels presynaptically, decreasing NT release

2) Opens post synaptic K+ channels, hyperpolarizing and inhibiting neurones

Front 3

What does activation of u (MU) receptors by opioids do?

Back 3

this produces analgesic, sedative, and euphoric effects.

as well as the side effects

Front 4

What does activation of k (Kappa) receptors by opioids do?

Back 4

this contributes to analgesia, and also dysphoria

Front 5

How do opioids act in the dorsal horn of the spine?

Back 5

these directly inhibit pain transmission in the dorsal horn.- called spinal analgesai

Front 6

how do opioid agonists affect the ascending pain pathways?

Back 6

inhibition

Front 7

How do opioid agonists affect the descending systems of pain transmission?

Back 7

these stimulate the inhibition systems

Front 8

In general how do opioids affect analgesia?

Back 8

these induce both sensory and affective (emotional) components of pain

Front 9

In general how do opioids sedation?

Back 9

these cause drowsiness, and in overdose can cause CNS depression

Front 10

In general how do opioids euphoria?

Back 10

people may experience euphoria, a decrease in anxiety or distress

Front 11

In general how do opioids cause nausea?

Back 11

this directly stimulates the CTZ in the brain causing nausea

Front 12

In general how do opioids affect cough?

Back 12

low doses suppress cough
codeine and dextromethorphan are commonly used

Front 13

In general how do opioids the respiratory system?

Back 13

there is decreased respiratory drive, which is good for pulmonary edema.

But bad for asthma/COPD as there is an overall PaCO2 increase

Front 14

In general how do opioids affect intracrainal pressure?

Back 14

these increase intracrainal pressure, as the increased PaCO2 in the blood increases vasodilation

Front 15

In general how do opioids affect the eyes?

Back 15

this causes miosis (pupil constriction)

Front 16

In general how do opioids body temp?

Back 16

lowers it

Front 17

In general how do opioids the trunk muscle tone?

Back 17

this causes truncal rigidity

Front 18

In general what do opioids to the heart?

Back 18

Bradycarida

(except for meperidine- tachycardia)

Front 19

In general how do opioids the GI system?

Back 19

constipation
decreased gastric motility
biliary colic

Front 20

In general how do opioids the GU system?

Back 20

lower urine output

Front 21

In general how do opioids affect histamine?

Back 21

these cause histamine release-
itching, usually due to injected opioids

Front 22

What are the signs of opioid overdose?

Back 22

CNS depression
depressed respiration
pin point pupils
(may be dilated near death)

Front 23

What do you do to treat opioid overdose?

Back 23

support respiration

administer naloxone (Narcan)

Front 24

What happens when opioids are given with MAO inhibitors?

Back 24

this causes a hyperpyrexic coma
should be avoided!

Front 25

What may decrease the analgesic effect of codeine derievtives?

Back 25

anything that inhibits CYP2D like SSRI's

Front 26

What is the prototype strong agonist opioid?

Back 26

Morphine (MSContin)

Front 27

What receptors does Morphine (MSContin) stimulate?

Back 27

this stimulates all opiate receptors

Front 28

What is the least effective way to dose Morphine (MSContin)?

Back 28

orally- due to high first pass metabolism

Front 29

How is Morphine (MSContin) metabolized in the body?

Back 29

this is metabolized in the liver by CYP2D6

Front 30

How long is the half life of Morphine (MSContin)?

Back 30

about 1.5-2 hours

Front 31

What is the more potent analgesic version of morphine, and how is it made?

Back 31

this is morphine 6-glucuronide
this is formed by conjugation with glucuronic acid

Front 32

How potent is hydromorphone (Dilaudid)

Back 32

this is MORE potent than morphine, and as effective

Front 33

What is hydromorphone (Dilaudid) less likely to cause than morphine?

Back 33

this is less likely to cause itching

Front 34

How long is the duration of action of Methadone (dolophine)

Back 34

this has a longer duration of action than morphine. its half life is 15-60 hours

Front 35

What is Methadone (dolophine often used to treat?

Back 35

hard to treat pain from cancer/neruopathic pain. help with withdrawal

Front 36

What is the withdrawl from Methadone (dolophine) like?

Back 36

this is milder and longer than other opioids

Front 37

What is meperidine (demerol) used for?

Back 37

this is used for very brief course in pts who are healthy, and are undergoing short painful procedures

Front 38

Why is meperidine (demerol) not used for long term use?

Back 38

this has metabolite accumulation which leads to seizures in patients with renal failure

Front 39

How does meperidine (demerol) affect the heart?

Back 39

this has antimuscarinic activity- so may cause tachycardia

Front 40

how does meperidine (demerol) affect the eyes?

Back 40

this may causes pupil dilation due to muscarinic block

Front 41

How does meperidine (demerol) affect cough?

Back 41

this does NOT suppress cough

Front 42

how does meperidine (demerol) affect the brain? What interaction does this have?**

Back 42

this blocks neuronal reuptake of serotonin

this can causes serotonin syndrome when given with SSRI's, TCA's, or MAO inhibitors

Front 43

How potent is fentanyl (sublimaze)?

Back 43

this is 100x more potent than morphine due to its high lipid solubility

Front 44

What is fentanyl used for?

Back 44

this is used for anesthesia induction and maintenance

Front 45

What metabolizes fentanyl?

Back 45

CYP3A4- so high interaction potential

Front 46

What schedule is heroin?

Back 46

schedule 1, not available in US

Front 47

What kind of drug is hydrocodone (codan)

Back 47

this is a moderate to strong opioid agonist

Front 48

How is hydrocodone (codan) metabolized?

Back 48

this undergoes complex hepatic metabolism

Front 49

What is the important metabolite produced by hydrocodone (codan)? by what enzyme?

Back 49

CYP2D6 a cytochrome P450.

this produces hydromorphone (dilaudid) which produces some of the analgesic effect

Front 50

What kinds of drug is oxycodone?

Back 50

this is a moderate to strong opioid

Front 51

What is oxycodone (oxycontin) used for?

Back 51

this is used to control moderate to severe pain

Front 52

What is Percodan?

Back 52

this is oxycodone (oxycontin) and aspirin

Front 53

What is Percoset?

Back 53

this is oxycodone (oxycontin) and acetaminophen

Front 54

What must happen in the body for oxycodone (oxycontin) to produce analgesia?

Back 54

this must be metabolized by CYP2D6

Front 55

What is Codeine used for?

Back 55

this is a moderate opioid agonist that is used as an antitussive agent

Front 56

What is Codenie metabolized into?

Back 56

this is metabolized into morphine by CYP2D6

Front 57

What does codeine do?

Back 57

this is an antitussive agent

Front 58

How is codeine metabolized?

Back 58

this is metabolized to morphine by CYP2D6

Front 59

What is Propoxyphene (Darvon)

Back 59

this is a weak analgesic

Front 60

What do high doses of Propoxyphene (Darvon) cause?

Back 60

these lead to seizures and toxic psychosis

Front 61

What is Pentazocine (Talwin)?

Back 61

this is an agonist at kappa receptors, and partial agonist at Mu receptors

Front 62

What is Pentazocine (Talwin) given for?

Back 62

this is a mixed agonist-antagonists

Front 63

What can happen when taking Pentazocine (Talwin) in opioid addicts?

Back 63

this can precipitate withdrawal symptoms

Front 64

What is Buprenorphine (Buprenex, suboxone)

Back 64

this is a mixed agonist -antagonists

Front 65

What is Buprenorphine (Buprenex, suboxone) given for?

Back 65

this is used to reduce drug craving in addicts (subutex)

Front 66

What receptors does Tramadol (Ultram) affect

Back 66

this is a weak Mu agonist

Front 67

What does Tramadol (Ultram) do?

Back 67

this inihibits reuptake of NE and 5-HT, like TCA's

Front 68

What happens with you combine Tramadol (Ultram) with antidepressants?

Back 68

this may result in seizures

Front 69

What side effect should you be aware of for Tramadol (Ultram)?

Back 69

serotonin syndrome

Front 70

What is Dextromethorphan given for?

Back 70

this is an antitussive

Front 71

What happens when combining Dextromethorphan with MAOI's

Back 71

this can cause serotonin syndrome

Front 72

What happens when ingesting pure Dextromethorphan in powdered form?

Back 72

this causes death, brain damage, seizures

Front 73

What is Naloxone (Narcan)?

Back 73

this is a pure opioid antagonist

Front 74

How long does Naloxone (Narcan) last? why is this important?

Back 74

this only lasts about 2 hours, so may requires repeated doses

Front 75

How does Naloxone (Narcan) affect addicts?

Back 75

this can precipitate withdrawal symptoms

Front 76

What is Naltrexone (ReVia)

Back 76

this is a long acting opioid antagonist

Front 77

What is Naltrexone (ReVia) used for?

Back 77

this is used to prevent recovering addicts from getting high

Front 78

What receptors does methadone block or bind?

Back 78

this blocks NMDA receptors, inhibits monoamine reuptake
strongly binds opioid receptors

Front 79

What receptors does Meperidine (demerol) bind or block?

Back 79

blocks serotonin ruptake

binds opioids

Front 80

What are the risks of long term meperidine (demerol) use?

Back 80

seizures

Front 81

What receptors does fentanyl binds?

Back 81

Opioid receptors

Front 82

What receptor does codeine bind?

Back 82

this does NOT bind MU- important because that limits the mu effects (analgesia, sedation, respiratory depression and side effects)

Front 83

What receptors does Tramadol bind or block?

Back 83

weak Mu agonist

blocks serotinin and NE reuptake