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Pharm I: Exam 2 > OPIATES > Flashcards

Flashcards in OPIATES Deck (44):
1

What is the biological response to stimulation of Mu (µ) receptors?

  • Respiratory depression
  • Physical depression
  • Tolerance
  • Constipation
  • Euphoria
  • Miosis (primary analgesia response)

2

What is the biological response to stimulation of Kappa receptor? 

  • Spinal cord analgesia and sedation without respiratory depression
  • Miosis

3

What is the biological response to stimulation of Sigma receptor?

  • Vasomotor stimulation 
  • Psychotomimetic effects
  • Miosis
  • Binds non-opioid agents

4

What is the biological response to stimulation of Delta receptors?

  • Enkephalins more selective with Delta receptors in periphery 

5

What opioids are the Pure/Strong Agonists? (5) How do they function?

Bind to Mu receptors (analgesia without "ceiling effect")

  • Phenanthrenes
    • Morphine
    • Hydromorphone
  • Phenylheptlamines
    • Methadone
  • Phenylpiperidines
    • Meperidine
    • Fentanyl (most widely used)

6

How does Morphine function?

  • Inhibits pain reflexes (via inhibition of neurotransmitter release)
  • Inhibit pain transmission
  • Modulates pain in spinal cord

7

What are the receptor binding affinities of Morphine?

  • Mu: Highest
  • Kappa: Varies
  • Delta: Varies
  • Sigma: Lowest

8

What are the ACTIONS of Morphine? (10)

  • Analgesia (INC pain threshold, alter brain's perception of pain)
  • Euphoria (contentment, well-being)
  • Respiratory
  • DEC cough reflex (antitussive effects via non-analgesic receptors)
  • Miosis (Mu and Kappa; little tolerance observed in addicts)
  • Emesis (stimulation of chemoreceptor trigger zone)
  • GI
  • CV
  • Histamine release (Hives, sweating, vasodilation, bronchoconstriction)
  • Hormonal actions

9

What are Respiratory-related ACTIONS of Morphine

  • Respiratory Depression
    • DEC CO2 sensitivity at respiratory center neurons

 

10

What are GI-related ACTIONS of Morphine

  • Relieves diarrhea
  • Causes constipation via DEC GI motility, and INC GI tone and anal sphincter

11

What are CV-related ACTIONS of Morphine

  • HIGH DOSE: Bradycardia and/or HPOTN
  • INC CSF
    • Morphine contraindicated w/ Severe brain injury

12

What are HORMONAL ACTIONS of Morphine

  • Inhibits release of GRH and CRH
  • DEC [LH], [FSH],[ACTH], [ß-endorphin]
  • DEC testosterone and cortisol levels
  • INC PRL, GH release (via dopaminergic inhibition)
  • INC ADH (leads to fluid retention)

13

What are the therapeutic uses for Morphine?

  • Analgesia
  • Diarrhea (RARE)
  • Cough (RARE)

14

What are ADRs for Morphine?

  • Respiratory and circulatory depression
  • Constipation
  • Sedation
  • Dizziness
  • HPOTN
  • N/V
  • Sweating
  • Euphoria
  • Dysphoria
  • Dry mouth (Xerostomia)
  • Syncope
  • Urinary retention

(Patients w/ renal failure more prone to ADR)

15

What precautions should be considered before administering Morphine? (pre-existing conditions)

  • Head injuries (INC ICP)
  • Acute asthmatic attack
  • COPD
  • BPH/urethral stricture
  • Elderly/neonates
  • Compromised BP

16

What are drug interactions with Morphine(CC)

  • Co-current use of CNS depressants (e.g. EtOH, Antipsychotic, BZDP)
  • Cimetidine: INC serum concentrations

17

What is being monitored with Morphine?

  • Pain control
  • Signs of respiratory/CV depression

18

How does Meperidine function? 

Antimuscarinic activity (Binds to kappa receptor)

19

What are therapeutic uses for Meperidine?

  • Post-surgical (spinal analgesia)

20

What are ADRs of Meperidine?

  • Seizures
    • LARGE DOSE
    • Renal Failure
    • HX seizures
    • Long-term use (cancer patients)
    • Drug interactions 

21

What are the contraindications for Meperidine?

  • TX MAOI within past 14-21 days
  • Patients with CHRONIC PAIN

22

What are the precautions for Meperidine?

  • Elderly
  • HX 
    • Renal failure
    • Hepatic failure

23

What are drug interactions with Meperidine? (MC BP)

  • MAOI (BP changes, excitatory, rigidity)
  • Chlorpromazine
  • Barbituates
  • Phenytoin (DEC concentration, INC normeperidine)

24

What should be monitored for with Meperidine?

  • S/Sx jerking or twitching (may indicate normeperidine accumulation)
  • Pain score evaluation

25

How does Methadone function?

Binds to Mu receptor for analgesia effect (substituted for morphine and heroin in controlled withdrawal – LONG half-life)

26

What are ADRs of Methadone?

  • HIGH-RISK toxicity (long half-life)
  • Withdrawal symptoms

27

What are drug interactions of Methadone(I I)

  • Inducers: DEC levels and effects
  • Inhibitors: INC levels and effects

28

What should be monitored for with Methadone?

  • Signs of Withdrawal:
    • Lacrimation
    • Rhinorrhea
    • Diaphoresis
    • Yawning
    • Restlessness
    • Insomnia
    • Dilated Pupils
    • Respriatory Depression

29

How does Fentanyl compare to Morphine?

MORE POTENT than morphine

30

What are therapeutic uses for Fentanyl

  • Acute/postoperative pain
  • Anesthesia (combination w/ Doperidol) 

31

What are ADRs of Fentanyl?

  • NO histamine release (possibly preferred when CV stability is not an issue)

32

What are drug interactions with Fentanyl(CII)

  • CNS depressants
  • Inducers (DEC effects)
  • Inhibitors (INC effects)

33

What are contraindications for Fentanyl

  • Patch for acute/postoperative pain
  • ABUSE
  • LACK OF TITRATION
  • VARIABLE ABSORPTION

34

What opioids are considered mild/moderate agonists? (5)

  • Phenanthrenes
    • Codeine
    • Oxycodone 
    • Hydrocodone
  • Phenylpiperidine
    • ​​Diphenoxylate
    • Loperamide

35

What are indications are considered for codeine, oxycodone, hydrocodone?

  • LESS efficacious than morphine
  • TX w/ ASA, APAP

36

What are therapeutic uses for diphenoxylate?

  • Management of diarrhea (Combo with atropine)

(Limited abuse potential)

37

What are therapeutic uses for Loperamide?

  • Management of diarrhea

(Limited abuse potential)

38

What opioids are considered partial agonist/antagonists? (4)

  • Phenanthrenes
    • Nalbuphine
    • Buprenorphine
  • Morphinans
    • Butorphanol
  • Benzomorphans
    • Pentazocine

39

How does Buprenorphine function?

  • Partial Mu agonist
  • Analgesia

40

How does Buprenorphine compare to Morphine?

  • 20X MORE POTENT than Morphine
  • Similiar ADRs, but may antagonize respiratory depression caused by Morphine
  • Long-acting (effects slower developing)

41

How does Butorphanol compare to Nalbuphine/Buprenorphine?

  • Equivalent analgesic effect
  • More sedative (kappa receptor agonist)

42

How does Pentazocine function?

  • Mild Mu and Kappa agonist 
  • Originally developed for analgesic effect with minimal abuse potential

43

What medication considered opioid antagonists? (NAME NN)

  • Naloxone (short-acting, precipitates withdrawal in 30 secs, duration 60-100 min)
  • Naltrexone (long-acting, up to 48 hours)

44

How does Tramadol function?

  • weak Mu agonist
  • Inhibit NE/serotonin reuptake in CNS