Pharm: Opioids and Analgesics Flashcards Preview

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Flashcards in Pharm: Opioids and Analgesics Deck (21):
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List the functions of the mu, delta, and kappa receptors

Mu
1. Supraspinal and spinal analgesia
2. Sedation and inhibition of respiration
3. Slow GI transit
4. Modulate hormones and NT release

Delta
1. Supraspinal and spinal analgesia
2. Modulation of hormones and NT release

Kappa
1. Supraspinal and spinal analgesia
2. Slow GI transit
3. Psychomimetic effects

1

How do the mu, delta, and kappa receptors inhibit pain?

When an agonist, like opioids, bind to these receptors, they signal a G-protein cascade that increases potassium conductance on an excitatory cell like a neuron.

This neuron is now hyperpolarized and will not fire without a large stimulus or it may not fire at all. So pain signals are not transmitted.

2

Codeine

Used for moderate pain, converted to morphine by the liver.

MOA: agonist at mu, delta, and kappa receptors

SE: addiction, sedation, depression

3

Oxycodone, Hydrocodone

Used for mild pain, more mild analogues of codeine

MOA: agonist at mu, delta, and kappa receptors

SE: addiction, sedation, depression

4

Morphine

Used for intense pain

MOA: agonist at mu, delta, and kappa receptors

SE: addiction, sedation, depression

5

Hydromorphone

Used for intense pain, more potent than morphine

MOA: agonist at mu, delta, and kappa receptors

SE: addiction, sedation, depression

6

Methadone

Used for chronic pain in cancer patients due to long half-life.

MOA: agonist at mu, delta, and kappa receptors

SE: respiratory depression (inhibits respiratory center in medulla), torsades de pointes

7

Meperidine

Used for pain management

MOA: agonist at mu, delta, and kappa receptors

SE: may cause seizures, mydriasis, poor oral bioavailability

8

Fentanyl

Used in epidurals, short acting to not harm the fetus. 100x more potent than morphine.

MOA: agonist at mu, delta, and kappa receptors

SE: sedation, addiction

9

Butorphanol

Treatment for opioid addiction, labor pain

MOA: agonist at kappa, partial agonist at mu

SE: sedation, depression

10

Buprenorphine

Used for chronic pain

MOA: agonist at mu, antagonist at kappa

SE: sedation, depression

11

Nalbuphine

Used for pre-op and post-op pain, obstetric analgesia

MOA: agonist at kappa, antagonist at mu

SE: sedation, depression

12

Naloxone

Used as an antidote for opioid intoxication

MOA: competitive antagonist at mu and kappa receptors
shorter half-life than morphine.

SE: can lead to respiratory distress due to opioid reversal

13

Naltrexone

Treatment of opioid dependence, relapse, alcohol withdrawal

MOA: competitive opioid antagonist

14

Respiratory depression is a major cause of death from opioid abuse. How do opioids cause this?

Opioid abuse leads to decreased sensitivity of chemo-sensitive neurons that sense pCO2. As CO2 levels rise in the body, the body normally compensates by increasing respiratory rate to prevent acidosis.

15

Ketamine

Treat chronic pain syndrome and post-operative pain

MOA: NMDA receptor antagonist

16

Clonidine

Treats acute and chronic pain

MOA: alpha 2 agonist

17

Gabapentin

Used as a last resort for chronic pain, and post-op pain.

MOA: GABA analog, inhibits calcium channels

SE: erratic oral bioavailability

18

Pregabalin

Treats neuropathic pain, fibromyalgia, and spinal cord injury

MOA: very potent GABA analog

19

Lamotrigine

Treats neuropathic pain, trigeminal neuralgia

MOA: sodium channel blocker

SE: skin reaction

20

Carbamazepine

Treats trigeminal neuralgia

MOA: sodium channel blocker

SE: hypotension