Opioid Analgesics Flashcards

1
Q

Opioid Agonists

A

Work and activate receptors in the brain (mu and kappa)

Tolerance: requires larger dose to get same response.
Develops: analgesia, euphoria, sedation, respiratory depression
Doesn’t develop: constipation, miosos

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2
Q

Opioid analgesics

A

Act as agonists or antagonists at opioid receptors in the brain
Used for pain; pain is treated in the brain
3 types of analgesics
3 receptors
Mu: physical dependent, low GI sexretions, euphoria, respiratory depression, pain relief
Kappa: low GI motility, sedation, pain relief
Delta

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3
Q

Opioid Agonist

Adverse Effects

A
Respiratory depression 
Intracranial pressure 
Sedation 
Euphoria 
Miosos 
Constipation 
* low cough reflex 
Orthostatic hypotension 
Urinary retention
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4
Q

Opioid Agonist

-Tolerance

A

Develop: pain relief, euphoria, sedation, respiratory depression
Doesn’t: miosos, constipation

  • cross tolerance: to other opioids, may not be complete Can be fatal.
    Reduce dose by 25-50% 30-60% to be safe.
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5
Q

Physical dependence

-all opioids

A

Concern with chronic use (more than 2 weeks)
Yawning runny nose -anorexia tremor-sneezing weakness N/V symptoms of chronic use

Gradual withdrawal over 3-7 days minimizes these reactions

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6
Q
Morphine*
Oxycodone (OxyContin) * 
Hydrocodone 
Hydromorphine
Codeine *
Meperidine 
Methadone* 
Dihydrocodeine
Opium
Nalbuphine
Tapentadol*
Levorphanol
Tramadol *
Paregoric 
*fetynyl, sufentinyl, alfentanil, remifentanil
A

Opioid receptor Agonists

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7
Q

Mixed opioid agonist-antagonists

A

Turns on some receptors and blocks others: gives good effects and minimizes others.

  • Low potential for abuse & resp depression
  • analgesic ceiling- only so much pain relief
  • can cause withdrawal response in ppl who have used opioids
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8
Q

Mixed opioid agonist antagonist

Adverse effects

A

Psychomimetic effects: hallucinations, dysphoria
Concern with chronic use
Low respiratory depression

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9
Q

Pentazocine
Butorphanol
Buprenorphine (butrans)
-suboxone

A

Mixed opioid agonist antagonists

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10
Q

Naloxone
Naltrexone
Methylnaltrexone
Alvimopan

A

Opioid receptor antagonists

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11
Q

Opioid antagonists

A

Prevents receptors from being activated/turned on
Bumps the agonist off the receptor
*prevents drug from being activate
* prevents drug from being abused; due to absorption in GI tract

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12
Q

Opioid antagonists

Use

A

1-overdose/abuse detterant
-naltrexone
-naloxone 0% bioavailablity, only works if taken orally
* snorting or injection led to 100% withdrawal (no first pass)
2-treatment of opioid constipation: restore bowel function
-methylnaltroxone
-naloxegal
* ding cross BBB Bind to receptor jn gut
3- post op Ileus
-alvimopan

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13
Q

Morphine

A
  • opioid agonist (C-2 drug)
  • high first pass metabolism:variable ab, low oral bioavailablity
  • active metabolite: M3G may cause neurotoxicity-increase renal impairment
  • old patients need low doses
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14
Q

Oxycodone (OxyContin)

A

Opioid agonist

  • resembles euphoria of heroine
  • high bioavailablity, better CNS penetration
  • “contin”: continual release
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15
Q

Hydromorphone

A

Opioid agonist

  • more potent, fewer side effects
  • active metabolite (H3G)- can contribute to neurotoxicity if renal function is impaired
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16
Q

Codeine

A

Opioid agonist
-terrible, doesn’t work
-more nausea and constipation
-* liver turns some of drug into morphine ( pro drug for morphine)
-* enzyme CYP2D6- genetically variable
Test for gene**
Activates more of the drug into morphine than a person without the enzyme

17
Q

Tapentadol & tramadol have risk of causing?

A

Serotonin syndrome

18
Q

Merperidine

A

Opioid agonist
Can Inhibit serotonin reuptake, short half life (3-4 hrs)
Toxic metabolite (tremor, rigidity, seizures, eliminated renally)
Lots of drug interactions: MAOIs: excitation, delerium, convulsions
Limited clinical role: rigors

19
Q

Fetynyl, alfentanil, sufentinyl, remifentanil

A

Opioid agonist
Rapid onset, short duration
Synthetic, highly potent opioids ( anesthesia, limited role)
-IV, IM, transdermal patch, transmucosal
-used for hospitalized patients

20
Q

Methadone

A
Opioid agonist 
Several unique actions 
-NMDA antagonist 
-**agonist at mu, kappa and delta receptor: inhibition of NE and 5-HT reuptake 
- long half life (12-190 hrs) 
-long duration with repeated dose 
- difficult to titrate
21
Q

Buprenorphine (Buprenex, butrans, subutex)

  • suboxone*
  • Buprenorphine + naloxone
  • sublingual tablet or film
A
  • mixed opioid receptor agonist/antagonist
  • special role in treating opioid dependence and managing withdrawal
  • Lower risk of resp depression, more easily obtained than methadone
22
Q

Tapentadol ( Nucynta)

Opioid agonist

A

Dual mechanism of action

  • weak mu receptor agonist
  • inhibition of NE and 5-HT reuptake
  • SS
  • AEs similiar to opioids
  • increase risk of seizure
  • may have high effects vs neuropathic pain
23
Q

Tramadol (ultram)

A

Similar but less potent opioid effects

*serotonin syndrome