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Flashcards in Pharm (Comp 3) Deck (36):
1

Endogenous opioids

Examples and MOA

Endorphins, Enkephalins, Dynorphins

mu, delta, and kappa reptor agonists

2

Effects mediated by mu opioid receptor

- Analgesia
- euphoria
- physical dependence
- bradycardia
- GI transit slowing
- respiratory depression

- Modulator of hormone and NT release

3

Effects mediated by kappa opioid receptor

- spinal analgesia
- miosis
- sedation, psychomimetic effects
- diuresis
- slowed GI

4

Effects mediated by delta receptor

- Dysphoric effects
- Analgesia

- Modulator of hormone and NT release

5

Strong agonist opioids

Morphine, methadone,
heroin, meperidine, fentanyl

6

Partial/mixed opioid agonist

Pentazocine, buprenorphine

7

Weak opioid agonists

codeine, hydrocodone

8

Morphine, Hydromorphone, Oxymorphone

MOA and action/use

- Opioid receptor agonist (miu, kappa, and delta)

- Use: Alter mood/anxiolytic, sedation, depress pain reaction

9

Morphine, Hydromorphone, Oxymorphone
Toxicity

- Respiratory depression, vasodilation
- Nausea/vomiting, constipation, Biliary colic
- Itching, hypotension, bronchoconstriction (H1)
- Miosis
- Increased prolactin release, inhibition of LH release
- Tolerance, withdrawal, physical dependence, addiction
- Increases intracranial pressure

- Not in pregnancy. Meperidine preferred in labor.

10

Codeine, Hydrocodone
MOA and use

MOA: Weak opioid receptor
agonist; Metabolized to
morphine

Use: Moderate pain treatment, Anti-tussive

11

Codeine, Hydrocodone
Toxicity

- Nausea, vomiting
- drowsiness, dizziness
- constipation

- Combined with NSAIDs or acetaminophen
- Codeine --> CYP2D6 metabolism. Genetic polymorphisms may increase toxic effects.

12

Methadone
MOA and Use

- Opioid receptor agonist;
antagonism on NMDA receptor

- Use: Avoidance of
the withdrawal reaction in opioid dependence patients
- Long t1/2 allows a slow taper

13

Methadone
toxicity

Accumulates with repeated doses, which can cause respiratory depression.

14

Meperidine (Demerol)
MOA and use

Opioid receptor agonist; Antimuscarinic effects; Serotonin effects

Use: Like morphine, but less analgesia
- Good in obstetrics: less neonatal respiratory
depression. Inc contractions

15

Meperidine
Toxicity

- Normeperidine (metabolite) can induce CNS stimulation esp. renal dysfunction pts
- Serotonin syndrome with SSRIs
- Drug interactions with monamine oxidase inhibitors (MAOIs)
- Hyperrexia coma

16

Fentanyl, Alfentanil, Sufentanil, Remifentanil
MOA and Use

- Opioid receptor agonist

- 100x more potent than morphine
- IV analgesic. Used for extra-anesthetic analgesia.

17

Fentanyl, Alfentanil, Sufentanil, Remifentanil
Toxicity

Respiratory depression

*Available as transdermal (patch) and transmucosal (lozenge) formulations.*

18

Heroin/Diacetylmorphine
MOA and Use

- Opioid receptor agonist
- Semisynthetic is
metabolized to morphine for action.

- Lipid soluble and crosses blood brain barrier quickly

19

Heroin/Diacetylmorphine
Toxicity

- Super CNS action
- analgesia
- Euphoria
- dependence and addiction
- Illicit use only

20

Tramadol
MOA and Use

- Mu receptor agonist. NE and 5-HT reuptake inhibitor.

- Weak analgesic, neuropathy
Little opioid toxicities.

- High bioavailability, active metabolite.

21

Tramadol
Toxicity

- May cause hypertensive crisis with MAOI

- Often combined with acetaminophen (added liver toxicity)

22

Diphenoxylate, Loperamide
MOA

- Weak mu or kappa agonists

- Antidiarrheal

23

Diphenoxylate, Loperamide

- Diphenoxylate --> combined with atropine to reduce abuse potential

- Loperamide --> no CNS effects, does not cross BBB (Imodium, OTC use)

24

Opioid drug interactions

CNS depression with:
- ethanol
- antipsychotics
-tricyclic antidepressants
- sedative-hypnotics (eg. benzos)
- antihistamines

25

Opioid OD S&S, Treatment

- Pupillary constriction
- Comatose state
- Hypotension
- Bradycardia
- Respiratory depression

Administer naloxone and ventilation.

26

Serotonin Syndrome
- Drugs involved
- S&S
- Treatment

- SSRIs, TCAs, meperidine, dextromethorphan, St. John’s Wort, linezolid, “triptans” (2 of these combined together)

Symptoms: rigidity, hyperthermia, myclonus, delirium, hypertension, tachycardia, GI symptoms
- within 24 hrs of taking the two drugs

Treatment: Benzodiazepines, cyproheptadine, ventilation

27

Naloxone
MOA and Use

- Antagonist at all opioid receptors. IV use.

- Rapidly antagonizes all opioid effects. Precipitates withdrawal in dependent users.

28

Naloxone
Toxicity

- Fast onset and short duration of action
- Repeated administration needed until opioid is cleared from the body.

29

Naltrexone
MOA and Use

- Like Naloxone but 5x more potent; up to 72 hr duration.
- Binds all opioid receptors. Oral use.

- Maintenance therapy; May reduce alcohol cravings in alcoholics

30

Naltrexone
Toxicity

Caution in hepatic impaired pts.

31

Methylnaltrexone
MOA and Use

- μ opioid receptor antagonist

- Treats opioid-induce constipation

32

Methylnaltrexone
Toxicity

- Does not cross BBB (compound is methylated)

- Targets GI tract

33

Butorphanol, Buprenorphine, Nalbuphine, Pentazocine
MOA of each

- Butorphanol (κ agonist)

- Buprenorphine (partial μ agonist, κ antagonist). Slow dissociation from μ receptor.

- Nalbuphine and Pentazocine (κ agonist, μ antagonist)

34

Butorphanol, Buprenorphine, Nalbuphine, Pentazocine
Use

- Analgesia without euphoria, less chance for dependence.

- Buprenorphine used in some rehabilitation programs.
Slow dissociation from the mu receptor

35

Butorphanol, Buprenorphine, Nalbuphine, Pentazocine
Toxicity

- Sim to morphine
- Administering these drugs with a pure agonist (eg. morphine) can reduce efficacy of the agonist or precipitate withdrawal.

- Pentazocine can increase psychomimetic effects (kappa mediated)

36

Opioid withdrawal symptoms

- Yawning, hyperventilation
- Lacrimation, piloerection, mydriasis
- Fever, chills, hyperthermia
- muscular aches, vomiting
- anxiety and hostility