Neuro: Test 2 : 14&15. Schriefer : Opiods I&ii

Front 1

what is the difference btw Nociceptive vs. Neuropathic Pain

Back 1

Nociceptive pain - caused by stimulation of nociceptive receptors and transmitted over intact neural pathways. Responds well to opioids.

Neuropathic pain – caused by damage to neural pathways. Responds poorly to opioids.

Front 2

Back 2

Front 3

what is the mechanism of action of the opiods?

Back 3

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 4

what is ziconotide

Back 4

A new analgesic, ziconotide (Prialt), blocks neuronal N-type calcium channels and mimics this effect of opioids. Approved for chronic pain. Is NOT an opioid.
May cause psychotic-like symptoms

Front 5

what kind of drug is Morphine

Back 5

Opium derivatives

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 6

what kind of drug is Codeine

Back 6

Opium derivatives

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 7

what kind of drug is Heroin

Back 7

Opium derivatives

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 8

what kind of drug is Hydromorphone / Oxymorphone

Back 8

Opium derivatives

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 9

what kind of drug is Hydrocodone

Back 9

Opium derivatives

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 10

what kind of drug is oxycodone

Back 10

Opium derivatives

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 11

what kind of drug is Pentazocine

Back 11

opiod Agonist – antagonists (partial agonists)

hits kappa receptor

Front 12

what kind of drug is Buprenorphine

Back 12

opiod Agonist – antagonists (partial agonists)

Front 13

what kind of drug is Butorphanol

Back 13

opiod Agonist – antagonists (partial agonists)

Front 14

what kind of drug is Nalbuphine

Back 14

opiod Agonist – antagonists (partial agonists)

Front 15

what kind of drug is Levorphanol

Back 15

Synthetic opioids

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 16

what kind of drug is Propoxyphene

Back 16

Synthetic opioids

Opioid receptors (mu) are linked to G proteins. Activation of Gi leads to decreased cAMP and
Closure of voltage-gated Ca2+ channels on presynaptic nerve terminals, which decreases neurotransmitter release. Transmitters affected include Ach, NE, glutamate, serotonin, and substance P.

post synaptically you have Opening of K+ channels causing hyperpolarization (inhibition) of postsynaptic neurons.

Front 17

what kind of drug is Methadone

Back 17

Synthetic opioids

Front 18

what kind of drug is Meperidine

Back 18

Synthetic opioids

Front 19

what kind of drug is Naloxone

use?

Back 19

opiod Pure antagonists

OD

Front 20

what kind of drug is Naltrexone

use?

Back 20

opiod Pure antagonists

OD

Front 21

what kind of drug is Nalmefine

use?

Back 21

opiod Pure antagonists

OD

Front 22

breakthrough pain from morphine what kind of drug do you want to use? Example?

Back 22

full agonist

a partial would initially cause some pain, so use a full agonist

Fentanyl

Front 23

what aspect of pain does morphine treat?

what does it do to niave pts not in pain

Back 23

selective on pain only

dysphoria

Front 24

what type of pt will experience vomiting on morphine

Back 24

ambulatory pts

direct stimulation of CTZ followed by depression

Front 25

overdose of morphine can lead to death, how?

Back 25

Respiratory depression: ↓ sensitivity of respiratory center to CO2 drive. ↓ both rate and depth of respiration. Overdose-death by respiratory failure.

Front 26

pinpoint pupils=

Back 26

opiods

Front 27

peripheral side effects of morphine 3

Back 27

GI tract - ↑ tone, ↓ peristalsis – constipation (need to prevent and/or treat constipation in patients taking opioids)
Biliary tract – gall bladder or bile duct spasm due to ↑ biliary pressure
Urinary tract - ↑ muscle tone → ↓ urinary output

Front 28

what is the 1st pass effect like in pts on morphine

Back 28

very high (90%) first pass effect

usually reserved for terminal ca pts

so often not given orally

Front 29

what are 2 active metabolites for morphine? effects?

Back 29

Morphine-6-glucuronide (active metabolite). Contributes significantly to analgesia when morphine given chronically by oral route

Morphine-3-glucuronide causes dysphoric side effects (ie causes the SEIZURES)

Front 30

what happens if you use opioids (morphine) during child birth?

***

Back 30

respiratory depression of the baby

crosses the bbb and placenta

Front 31

what happens if mom uses opioids throughout childbearing ?

Back 31

child will have physical dependence on the drug

***

Front 32

key to spotting opiod OD

Back 32

pinpoint pupils

Morphine
Codeine
Heroin (semi-synthetic)
Hydromorphone (Dilaudid), Oxymorphone (Opana) – semisynthetic derivatives of morphine
Hydrocodone (Vicodin), oxycodone (Percodan; Oxycontin) – semisynthetic derivatives of codeine
Meperidine (Demerol) me per’ i deen
Methadone (Dolophine) meth’ a done
Propoxyphene (Darvon) proe pox’ i feen
Levorphanol (Levo-Dromoran) lee vor’ fa nole

Front 33

tx for opiod od?

Back 33

maintain respiration and give naloxone

Front 34

major drg interaction of opiods?

what about with amphetamine

Back 34

Depressant effects may be prolonged or exaggerated by CNS depressants: phenothiazines, MAOI, tricyclic antidepressants, cimetidine

Amphetamine in small dose may enhance morphine effect

Front 35

Contraindications/cautions of morphine?

Back 35

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

most have to do with CNS depression

Front 36

codiene is similar to what? how is it different?

Back 36

morphine

relatively effective orally

note:must be metabolized to morphine (by Cyt 2D6) to be fully active – 7% of Caucasians lack this enzyme.

Front 37

Meperidine is what kind of drug? why isnt it used as often?

Back 37

Actions similar to morphine except for the following differences:
Analgesia: meperidine has a faster onset, shorter duration, and is less potent
No antitussive activity
Less constipation
Lesser degree of respiratory depression in fetus and does not inhibit uterine contraction
Less addiction liability than morphine
More effective than morphine after oral administration


*****Metabolite normeperidine is a stimulant. Normeperidine accumulates with repeated doses.-->can cause seizures!!

Front 38

what opiod do you have to worry about serotonin syndrome with?

Back 38

Meperidine

Meperidine should not be used in patients receiving MAOI – potential for serotonin syndrome (severe restlessness, fever, and hypertension). Meperidine blocks 5HT reuptake.

Front 39

this is a synthetic opiod with a short duration; 80-100 x more potent than morphine. Available in a transdermal patch (Duragesic) which provides long lasting (48-72 hrs.) pain relief. Can also be used for what?

Back 39

Fentanyl

breakthrough pain

Front 40

Loperamide is used to treat what? kind of drug?

Back 40

Opioids for Diarrhea

another: Diphenoxylate

Front 41

what type of drug is methadone? how is it different from the drug that characterizes this class? use?

Back 41

Primarily a μ agonist with actions similar to morphine except
Greater oral effectiveness

Extended duration of action in suppressing withdrawal

Slow onset. Long duration (T1/2 22 hr) may accumulate

Front 42

what is an important use of methadone?

Back 42

wean addicts off of other narcotics with oral methadone for a few weeks

Front 43

wha typ of drug is Tramadol?

Back 43

not strictly an opioid analgesic. Does produce a portion of its action by binding to μ receptors.
Also inhibits NE and 5HT reuptake

Front 44

if you are going to tx your pt for a long time w an opiod, what must you consider giving in addition?

Back 44

Laxatives

do not gain tolerance to constipation

Front 45

Butorphanol is what kind of drug? use?

Back 45

Mixed Agonist-Antagonists (Partial Agonists) opioid

quick relief from migraine pain

Front 46

moa of pentazocine?

at high doses, what effects will pentazocine produce?

Back 46

Pentazocine analgesia probably produced by an action at spinal κ receptors – adequate for moderate pain
Produces limited respiratory depression
High doses produce dysphoria and psychotomimetic effects


Mixed Agonist-Antagonists (Partial Agonists)

Front 47

CV effects of pentazocine?

besides analgesia, what can ths drug be used for?

Back 47

High doses also produce cardiovascular effects different from morphine, i.e., ↑ BP and ↑ HR
Has μ partial agonist/antagonist action. Can precipitate withdrawal in morphine/heroin dependent individuals
Tolerance develops to analgesia and behavioral effects

Mixed Agonist-Antagonists (Partial Agonists)

Front 48

Naltrexone administered? moa? use?

Back 48

monthly IM injection

pure opiod antag

prevents a person who is trying to get off the drug from having an issue if they relapse and shoot up, this will block the effecy

Front 49

person comes in and you think theyve oded on opioids, what do you give them? what if you were wrong and it wasnt opioids?

Back 49

Naloxone--opioid antag

No effect of their own. so ok

Front 50

Methylnaltrexone moa? use?

Back 50

opiod antag

Methylnaltrexone reverses opioid-induced constipation but not analgesia (doesn’t enter CNS). Used for patients receiving chronic opioids.

Front 51

Alvimopan moa? use?

Back 51

opioid antag

Alvimopan used to treat post-op ileus; given before and after bowel resection.(Stays in GI tract).

Front 52

morphine, meperidine, methadone, fentanyl patch are used for what knd of pain?

Back 52

Moderate/severe pain

Front 53

codeine, oxycodone, pentazocine alone or in combination with aspirin, ibuprofen or acetaminophen are used for what knd of pain?

Back 53

Mild/moderate

Front 54

what opiod is used to tx Acute pulmonary edema?

Back 54

morphine IV


shunts blood to periphery and reduces anxiety

Front 55

how can morphine be used in mi?

Back 55

decreas preload and afterload

Front 56

what opiod is used as an antitussive

Back 56

codiene

Front 57

remeber: codiene is a prodrug...meaning

**

Back 57

that it has to be metabolized to morphine

some ppl lack the necessary enzyme for this (CYT2D6)

Front 58

opioids used when can lead to birth defects? what kind?

Back 58

1 month prior and 3 post conception

CV effects

Front 59

What is the difference between pentazocine and naloxone?

Back 59

Pentazocine is a mixed partial opioid agonist

Naloxone is an opioid antagonist --> blocks both agonists and mixed agonists/antagonists (ie blocks pentazocine)

Front 60

Which opioid receptor is most responsible for analgesia? Dysphoria? Physical dependence? Pupillary constriction?

Back 60

Analgesia- mu
Dysphoria- kappa
Physical dependence- mu
Pupillary constriction- mu

Front 61

Opioids produce both depressant actions and stimulating actions. What is the tolerance level of these side effects?

Back 61

Marked tolerance occurs to the depressant actions of morphine (analgesia, euphoria, dysphoria, sedation, respiratory depression)

Little tolerance to the stimulating actions (miosis, constipation, convulsions, antagonist actions)