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Pharm Test 3 > Opiod Agonists And Antagonists > Flashcards

Opiod Agonists And Antagonists Flashcards

0
Q

3 classes of opioid drugs

A

Full agonists

Partial agonists

Antagonists

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1
Q

Opioid analgesics

A

Control moderate to severe pain -can produce dependence

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2
Q

Full agonists

A

Codeine, hydrocodone, fentanyl, Lopermide, Methadone, Morphine, Oxycodone

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3
Q

Partial agonists

A

Buprenorphine, Pentazocine, Tramadol

Agonists when given alone
Antagonists when on board with full agonists
Most are kappa receptor agonists and Mu receptor antagonists

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4
Q

Antagonist

A

Naloxone

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5
Q

Antitussive agent

A

Dextromethorphan

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6
Q

Types of opiate receptors

A

Mu- morphine-like actions,Euphoria,Respiratory depression,Physical dependence,GI Actions
All full agonists act here
Kappa- Pentazocine like actions, miosis, sedation, dysphoria, hallucinations
Delta - Enkephalins like receptors, dependence, euphoria,analgesia

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7
Q

Endogenous opioid peptide families

A

Enkephalins
Short, opiate receptor agonists, short lived
Dynorophins
Longer, opiate receptor agonists, longer lived
Endorphins
Opiate receptor agonists, longest acting endogenous peptide

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8
Q

Prototype and standard for opioid drugs

A

Morphine

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9
Q

Metabolism of morphine

A

Conjugation w/glucaronic acid in the liver
Most metabolizes are inactive
Tolerance develops

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10
Q

Actions of morphine

A 
Analgesia
     Block pain transmission
     Most effective against continuous dull pain
     Raises the pain threshold
     Anti-anxiety effect
Respiratory depression (primary cause of overdose death)
Nausea and vomiting
GI effects -constipation 
     Little to no tolerance develops 
Drowsiness and sedation 
Miosis
Euphoria and tranquility 
Pruritis 
Orthostatic HTN
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11
Q

Morphine analgesia

A 
Symptomatic relief of pain
Moderate to severe
Used primarily against acute pain
Sickle cell crisis pain
Dyspnea in end stage lung cancer
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12
Q

Morphine side effects

A 
Dependence
Increased pressure in biliary and urinary tracts 
Allergic rxns
Neonates and elderly much more sensitive
Dysphoria and excitement
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13
Q

Morphine contraindications

A

Those with decreased respiratory reserve
Head injuries- May obscure important signs
Pregnancy

Don’t combine with any CNS depressant

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14
Q

Codeine

A

More reliable when given orally than morphine
Metabolized by CYP2D6 into morphine
Used to treat mild to moderate pain
Cough suppressant
More constipation
Less potential for abuse and addiction than morphine

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15
Q

Methadone

A

Same effects as morphine
Pharmacokinetics different
Metabolized by CYP3A4 and excreted slowly
Longer lasting than morphine if used chronically
Can have serious cardiovascular effects (prolonged QT interval)

Used for tx of drug dependence

16
Q

Fentanyl

A

Extremely potent opioid agonists
Primarily used as anesthetic medsd
Treating chronic and breakthrough pain

Analgesia - short onset time, shorter duration of action
Less effect on cardiovascular system
More likely to produce muscle rigidity of chest and ab muscles

17
Q

Hydrocodone (Vicodin)

A

Most commonly prescribed drug 2002-2012

Metabolized by conjugation

18
Q

Oxycodone

A

More potent than codeine
Effective orally
Abuse of timed release formulations is major problem

19
Q

Loperamide (Imodium)

A

Potent anti-diarrheal drug

Action limited to GI tract bc it crosses mucosal membranes poorly

20
Q

Dextromethorphan

A

Cough suppressant

No analgesia

21
Q

Pentazocine

A

Synthetic opioid generally similar to morphine
Kappa agonist, Mu antagonist

Analgesia
Dysphoria ( in high doses, why it’s not generally used for severe pain)
Increase BP and HR
Will precipitate withdrawal in opioid defendant ppl due to antagonist action ( not morphine withdrawal)

22
Q

Buprenorphine

A

Agonist at Mu, kappa antagonist (opposite)
Analgesia in moderate to severe pain
Tx for opioid dependence

23
Q

Tramadol

A

Very weak partial agonist opioid
Weak Mu partial agonist
Also inhibits NE and 5HT transport

Can produce dependence
Seizures and serotonin syndrome seen

24
Q

Naloxone

A

Opioid antagonist
Used to counteract the effects of opioids
Must be given continuously, not effective orally

25
Q

Diagnosis of opioid overdose

A

Respiratory depression
Miosis
Coma

Pharm Test 3 (8 decks)

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