Opioid Analgesics 2 Flashcards Preview

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Flashcards in Opioid Analgesics 2 Deck (36)
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1

What opioid receptor will give you spinal analgesia, miosis (pinpoint pupils) and sedation?

Kappa

2

What opioid receptors give you analgesia, emotion and seizures?

Delta

3

What opioid receptors give you dyphoria, hallucinations, nightmares, anxiety?

Sigma 

4

What opioid receptor gives you just analgesia?

Epsilon

5

The strength of attachment of an opioid drug to its binding site is proportional to what?

It's potency

The stronger the affinity - the higher the potency

6

Opioids act by?

  • Presynaptic inhibition of production of neurotransmitters C-fiber endings
  • Postsynaptic suppression of evoked activity in nociceptive path or remove the remaining parts of the regulation of inhibition of nociceptive impulses
  • Increased transmission of the descending inhibition of spinal nociceptive conduction

7

What do opioids cause (3 things)?

  1. Hyperpolarization of nerve cells
  2. Inhibition of nerve firing
  3. Presynaptic inhibition of transmitter release

8

What are the examples of opioids?

  • Endogenous opioid peptides
  • Opium alkaloids (poppy plants - morphine and codeine)
  • Semi-synthetic opioids 
  • Fully synthetic opioids 

9

What's a pure agonist, and what is the prime example of a pure agonist?

Complete receptor activation - mu and kappa activated

Unlimited analgesia - MORPHINE

10

What's a major problem with opioids?

Tolerance - the potency of the drug declines so that progessively higher concentrations are required to produce the same degree of analgesia - 

11

What are the characteristics of a partial agonist and give an example?

Example: buprenorphine (Buprenex)

Parital mu activation, good analgesia but limited effect

12

If one become tolerant to one opioid what is a possibility with other opioids?

They can become cross-tolerant to other opioids

13

What is an example of agonist/antagonist?

Example: pentazocine (Talwin) 

  • Mu - anatagonist
  • Kappa - agonist (sedative prior to sugery, supplement to surgical anesthesia)

14

What is an example of a pure antagonist, and what are the characteristics?

Example: naloxone (Narcan)

No analgesia

15

What is used for an antidote of overdosed opioids?

naloxone (Narcan) 

Pure antagonist - used for complete or partial reversal of opioid depression

16

Where are opioids absorbed?

Most are well-absorbed orally

Lungs, nasal and oral mucosa, and intact skin all good places as well

17

What's the distribution of opioids?

First pass effect reduces bioavailability, can pass to fetus

18

***What are the desired clinical effects of opioid drugs?

  • Potent analgesia
  • Sedation and euphoria
  • Cough suppression
  • GI effects
    • increase smooth muscle tone
    • decrease propulsion and motility
    • used for treatment of diarrhea

19

What's the number one compliant of people who take opiates?

Constipation

20

All opiates have the same adverse reactions, what are the?

  • Physical addiction
  • Respiratory depression
  • Nausea and vomiting
  • Constipation
  • Miosis (pinpoint pupils)
  • Urinary retention
  • CNS effects - stimulatory effects, anxious
  • Cardiovascular - bradycardia (depressent)
  • Biliary tract constriction 
  • Histamine release - itching and urticaria

21

Why don't we use opioids in pregnancy?

Prolongs labor, depresses fetal respiration if given near term, infants born addicted

22

The severity of the side effects of opiates are proportional to its _________?

Efficacy

23

What are signs of opioid overdose?

  • Respiratory depression
  • Pinpoint pupils
  • Coma

Treat with anatagonist - naloxone

24

What are signs of opioid withdrawal?

  • Yawning, lacrimatoin, perspiration, piloerection, irritability, tachycardia, tremors, etc

25

What are most of the hypersensitivity reactions to opioids?

Most are dermatologic - skin rashes, urticaria

If true allergy - avoid

26

What are the clinical indications for opioids?

  • In dentistry:
    • Analgesia, sedation
  • In medicine:
    • Analgesia, sedation, cough suppression, diarrhea

27

How do you obtain opium?

Dried juice obtained from unripe seed capsules of poppy plant (25% of dried juice consists of the alkaloids: morphine, codeine, papaverine)

28

What are the drugs used in dentistry that are derivatives from opium alkaloids?

Morphine, Codeine

29

What is Heroin?

Synthesized morphine product (diacetyl morphine)

30

What are the pure agonists?

  • oxycodone (Percodan, Percocet)
  • hydrocodone (Vicodin, Lorcet)
  • codeine
  • dihydrocodeine (Synalgos D-C)
  • propoxyphene (Darvon) 
  • meperidine (Demerol)
  • fentanyl