Umbsrna2012 Nagelhout Pharm Test 3

Front 1

4 groups of endogenous opioid peptides?

Back 1

Enkephalins, beta-endorphin, Dynorphins, and endomorphins

Front 2

How do the pain meds work?

Back 2

agonist on the presynaptic pain neuron. By stimulating a mu receptor, the pain receptor releases endorphins, dynorphins, endomorphins, or enkephalins which bind to the presynaptic neuron and prevent release of substance P (pain transmitter).

Front 3

The three types of opiate receptors in the body?

Back 3

Mu (1 and 2 in test animals), Kappa, Delta

Front 4

Mu Effects?

Back 4

Analgesia (supraspinal, spinal), Euphoria (not sleep - do not produce anesthesia only analgesia); ventilatory depression; physical dependence; Miosis (pinpoint pupils); Constipation (marked); Bradycardia, hypothermia, urinary retention, pruritus, skeletal muscle rigidity, biliary spasm

Front 5

Mu agonists

Back 5

Endorphins, Morphine, Synthetic opioids

Front 6

Mu Antagonists

Back 6

Naloxone, Naltrexone, Nalmefene

Front 7

Kappa receptor effects

Back 7

Analgesia (supraspinal, spinal), Dysphoria (some people feel bad with narcotics), sedation, low abuse potential, miosis

Front 8

Delta Receptor effects

Back 8

Analgesia (supraspinal, spinal), depression of ventilation, physical dependence, constipation (minimal), urinary retention

Front 9

Kappa Agonists

Back 9

Dynorphins

Front 10

Delta Agonists

Back 10

Enkephalins

Front 11

Kappa Antagonists

Back 11

Naloxone, Naltrexone, Nalmafene

Front 12

Delta Antagonists

Back 12

Naloxone, Naltrexone, Nalmafene

Front 13

reversal with Naloxone works on which receptors?

Back 13

All! Mu, Kappa, Delta

Front 14

Amount of ______ is always equal to the amount of ________!

Back 14

analgesia; respiratory depression

Front 15

Classes of opioid agonists

Back 15

Phenanthrene Alkaloids
Synthetic opioids
Phenylpiperidine Derivatives
Propionilide (methadone) derivatives

Front 16

Agonists in the Phenanthrene Alkaloid class

Back 16

Naturally occurring (directly from poppy plant): Morphine, Codeine, Thebaine
Semi synthetic (start with natural product and tweak it): diacetylmorphine (heroine), hydrocodone (vicoden), hydromorphone (dilaudid), oxycodone (oxycontin), oxymorphone.

Front 17

Agonists in the Synthetic opioid class:

Back 17

Drug is completely man-made Morphinan Derivatives Levorphanol

Front 18

Agonists in the Phenylpiperidine Derivatives class

Back 18

Meperidine, Fentanyl, Sufentanil, Alfentanil, Remifentanil

Front 19

Agonists in the Propionilide class

Back 19

(methadone) derivatives

Methadone
Propoxyphene

Front 20

Demerol allergy means they can't get?

Back 20

Phenylpiperidine Derivatives:

Meperidine
Fentanyl
Sufentanil
Alfentanil
Remifentanil

Front 21

If allergic to Morphine they could get?

Back 21

Synthetic opioids: Morphinan Derivatives Levorphanol
Phenylpiperidine Derivatives: Meperidine, Fentanyl, Sufentanyl, Alfentanil, Remifentanyl
Propionilide (methadone) derivatives: Methadone, Propoxyphene

Front 22

All narcotics are metabolized by?

Back 22

The liver by cytochrome enzymes by the usual drug metabolizing routes nothing special about metab. If someone enzyme induced=metab faster (requires more opiates) if inhib=metab slower; liver disease=slower metab so needs less med than others. 3-6 hr half-life for most

Front 23

What enzyme is responsible for remifentanyl metab?

Back 23

non-esterase dependent enzymes in plasma = extremely short duration of action. Metab via ester hydrolysis = duration of action = minutes

Front 24

Demerol metab=

Back 24

gets metab to normeperidine which is an active CNS & renal toxic metab. nor=group gets knocked off. Reason use has been avoided and some hospitals took off formulary. Metab produced with several days use and can cause seizure or other CNS excitement especially with elderly or those with renal disease (b/u since not excreting via kidneys)

Front 25

which of the opioids has the shortest T1/2?

Back 25

Remifentanil = 0.17-0.33 hrs

Front 26

Acute effx of opioids

Back 26

Analgesia
Ventilatory depression
sedation
euphoria
vasodilation
bradycardia
cough suppression
miosis
nausea and vomiting
skeletal muscle rigidity
smooth muscle spasm
constipation
urinary retention
biliary spasm
pruritis, rash
antishivering (meperidine only)

Front 27

Chronic effects of opioids

Back 27

tolerance, physical dependence, constipation

Front 28

Acute effect of opioid: Analgesia:

Back 28

not anesthetics, won't put to sleep.

Front 29

Acute effect of opioid use: Ventilatory depression

Back 29

Opiates decrease sensitivity to CO2 of the respiratory center in brain. The CO2 response curve SHIFTS to the RIGHT. Higher CO2 to drive the same amount of respiratory depth and rate. Doesn't matter which narcotic if same potency. Every time you give more morphine the CO2 response curve is shifted further to the RIGHT. Opiates are respiratory depressants. The amount of respiratory depression is = to the amt of analgesia.

Front 30

Acute effect of opioid use: Sedation

Back 30

1

Front 31

Acute effect of opioid use: Euphoria

Back 31

1

Front 32

Acute effect of opioid use: Vasodilation

Back 32

1

Front 33

Acute effect of opioid use: Bradycardia

Back 33

1

Front 34

Acute effect of opioid use: Cough suppression

Back 34

1

Front 35

Acute effect of opioid use: Miosis

Back 35

1

Front 36

Acute effect of opioid use: Nausea and vomiting

Back 36

1

Front 37

Acute effect of opioid use: Skeletal muscle rigidity

Back 37

1

Front 38

Acute effect of opioid use: Smooth muscle spasm

Back 38

1

Front 39

Acute effect of opioid use: Constipation

Back 39

1

Front 40

Acute effect of opioid use: Urinary retention

Back 40

1

Front 41

Acute effect of opioid use: Biliary spasm

Back 41

1

Front 42

Acute effect of opioid use: Pruritis, rash

Back 42

1

Front 43

Acute effect of opioid use: Antishivering

Back 43

1