4.1 Opioids Flashcards Preview

Pharmacology > 4.1 Opioids > Flashcards

Flashcards in 4.1 Opioids Deck (20):
1

Activation of opioid mu receptors produces which effects? (4)

1) Euphoria
2) Respiratory Depression
3) Analgesia
4) Physiological Dependence

2

Delta and Kappa opioid receptors contribute to analgesia at which level?

Spinal

3

Opioid receptors couple to which G protein?

Gi

4

What is the action of opioids on presynaptic neurons?

Close voltage gated Ca2+ channels

5

What is the action of opioids on postsynaptic neurons?

Open K+ channels

6

The analgesic effects of opioids are due to which 2 abilities?

1) Inhibit ascending pain transmission
2) Activate descending pain-inhibitory circuits

7

The descending pain-inhibitory neurons are inhibited by what?

GABA(a)

8

What categories are the Opioid Analgesics classified into? (3)

1) Pure agonists
2) Mixed agonist-antagonists
3) Antagonists

9

How do pure opioid agonist act? (2)

1) High affinity for mu receptors
2) Lower affinity for gamma and kappa receptors

10

How do Mixed agonist-antagonist opioids act?

1) Agonist and antagonist act differently on different receptors
2) Analgesic ceiling effect
3) Some drugs cause psychomimetic effects

11

What are the CNS effects of opioid use? (8)

1) Analgesia
2) Euphoria
3) Sedation and drowsiness
4) Respiratory depression
5) Cough suppression
6) Miosis
7) Truncal rigidity
8) Nausea and vomiting

12

What is pathognomonic following toxic doses of mu agonist?

Pinpoint pupils (miosis)

13

What are the peripheral effects of opioid use? (6)

1) Hypotension
2) GI tract
3) Biliary tract
4) Genitourinary tract
5) Uterus
6) Pruritis

14

Opioids are converted to what? And excreted how?

- Glucuronides
- Excretion via kidney

15

What is morphine primarily conjugated to? And the smaller portion?

- Morphine-3-glucuronide (M3G) (primary)
- Morphine-6-glucuronide (M6G) (10%)

16

Describe the metabolism of heroin

Heroin (diacetylmorphine) is hydrolyzed to monoacetylmorphine and to morphine, which is then conjugated with glucuronic acid.

17

What is the metabolite of meperidine and what does high concentrations of it cause?

- Normeperidine
- Seizures

18

Fentanyl is metabolized by which enzyme in the liver?

CYP3A4

19

Codeine, oxycodone, and hydrocodone are metabolized by what in the liver?

CYP2D6

20

What metbolites of opioids are found mainly in the urine?

Polar metabolites, including glucuronide conjugates of opioid analgesics