Pharm S2B3 - Cns - Opioids

Front 1

What are the Opioids derived from?

Back 1

Opium poppy = Papaver Somniferum
-contains opiate compounds including Morphine & Codeine

Front 2

This is a tincture of opium used in the olden days, used for "nerves", cough, & diarrhea

Back 2

Laudanum

Front 3

What are the 3 different Opioid receptors?

Back 3

Mu = Morphine

Delta = Enkephalin

Kappa = Dynorphin

Front 4

What type of receptor are the Opioid receptors?
What actions do they possess?

Back 4

G-protein coupled

Close Ca++ channels on Presynaptic neurons, reducing evoked transmitter release

Open K+ channels on Postsynaptic neuron, hyperpolarizing membranes

Front 5

What actions do Mu receptors produce?

Back 5

1. Analgesic
2. Sedative
3. Euphoric effects
4. untoward side effects

Front 6

What actions do the Delta Opioid receptors possess?

Back 6

Analgesia at spinal levels

Front 7

What actions do the Kappa Opioid receptors possess?

Back 7

1. may contribute to Analgesia

2. Primarily results in Dysphoria = anxiety, depression, unease

Front 8

Although the Sigma receptor is not an Opioid receptor, what effect may Opioids have on this receptor?

Back 8

may contribute to Dysphoric effects

Front 9

Explain the ways in which Opioid drugs interact with the body's endogenous opioid peptide system to limit pain

Back 9

1. Pain-modulating descending pathways from CNS
-Periaqueductal Grey Matter (PAG)
-Rostral Ventral Medulla (RVM)

2. Pre- and Postsynaptic Spinal actions
-Inhibitory Postsynaptic Potential (IPSP)
-inhibition of neurotransmitter release

3. Opioid receptors in peripheral tissues

Front 10

What are the CNS pharmacological effects of Opioids?

Back 10

1. Analgesia = changes perception & experience of pain; does not decrease sensation
2. Euphoria/Dysphoria
3. Sedation
4. Respiratory depression
5. Cough suppression
6. Miosis (Parasympathetic)
7. Truncal Rigidity (impairs ventilation)
8. Nausea & Vomiting = Chemoreceptor Trigger Zone

Front 11

What are the Peripheral pharamacological effects of Opioids? (7)

Back 11

1. Arterial & Venous dilation
2. Constipation
3. Biliary colic (cholinergic)
4. decreased Renal blood flow = decreased renal fxn
5. decreased Uterine tone
6. Endocrine alterations
-increased ADH, Prolactin, Somatotropin release
-decreased LH release
7. Histamine release
-flushing
-sweating
-rashes & itching

Front 12

What are the clinical uses of Opioids? (5)

Back 12

1. Acute or Chronic Pain
-Analgesic
-no apparent maximal dose
-less effective for neuropathy (use adjuvant analgesics such is Imipramine or GABApentin)
2. Acute pulmonary edema or MI = decrease the sensation of crisis
3. Cough = anti-tussive
4. Diarrhea = decrease GI motility
5. Anesthesia/preoperative meds = anesthetic sparing

Front 13

What are the toxicities of Opioids? (5)

Back 13

1. Respiratory Depression = primary cause of death
2. Dysphoria
3. N/V
4. Constipation
5. Seizures = high doses - may be delta-mediated

Front 14

When dose Opioid Tolerance start?

After how long is tolerance clinically apparent?

Back 14

Starts with 1st dose

apparent in 2-3 wks

Front 15

Describe the tolerance timeline of the symptoms of opioid use

Back 15

ERA-SNCA

Front 16

What side effects are there no tolerance to with Opioid use? (3)

Back 16

1. Miosis
2. Constipation
3. Seizures

**cross tolerance occurs as well

Front 17

Describe the Abstinence Syndrome associated with Opioid Withdrawal

Back 17

1. Dysphora
2. Rhinorrhea
3. Lacrimation
4. Yawning
5. Chills
6. Vomiting
7. Diarrhea
8. Anorexia
9. Insomnia
10. Anxiety
11. Hostility

Front 18

What is compulsive drug seeking in dependent opioid individuals due to?

Back 18

due to avoiding the Withdrawal symptoms

Front 19

What are the 2 drugs used to treat ACUTE Opioid Overdose?

Back 19

1. Naloxone = IM or IV
- 1 to 2 hr duration

2. Nalmefene = IV
-Half-life = 8-10 hrs

**these can precipitate withdrawal symptoms

Front 20

What drug is used to prevent relapse in Opioid Addicts?

Back 20

Naltrexone = Oral
-Half-life = 10 hrs

Front 21

What is the relative efficacy of Opioid drugs based on?

Back 21

Analgesia

"Equianalgesic dose" = equal to 10 mg Morphine

Front 22

List the 5 High Efficacy Analgesic Opioids

What are they used for?

Back 22

1. Morphine
2. Methadone
3. Meperidine
4. Fentanyl
5. Alfentanil

Severe pain = trauma, post-surgical, MI, etc

Front 23

List the properties of Morphine

Back 23

1. High efficacy analgesic
2. Poor oral bioavailability
3. Duration is 4-5 hrs

Front 24

List the properties of Methadone

Back 24

1. High Efficacy Analgesic
2. Longer acting = ~6 hrs; plasma half-life = ~24 hrs
3. Good Oral bioavailability
4. used as maintenance in addicts

Front 25

List the properties of Meperidine

Back 25

1. High Efficacy Analgesic
2. Medium acting = 2-4 hrs
3. Antimuscuranic
4. metabolized to Normeperidine = psychoactive, seizures

Front 26

List the properties of Fentanyl

Back 26

1. High Efficacy analgesic
2. short acting = 1-1.5 hrs
3. primarily acts at MU receptors
4. poor Oral bioavailability
5. transdermal dosage forms available

Front 27

List the properties of Alfentanil (5)

Back 27

1. High efficacy analgesic
2. very short acting = 15-45 minutes
3. very potent
4. Parenteral only
5. useful for brief, painful procedures

Front 28

List the Low-Medium Efficacy Analgesics (5)

Back 28

1. Codeine
2. Hydrocodone
3. Oxycodone
4. Propoxyphene
5. Tramadol

Front 29

List the properties fo Low-Medium Efficacy Analgesics

Back 29

1. partial agonist or drugs that are not tolerated at higher doses
2. All typically administered orally
3. used for Moderate pain = broken bones, dental procedures, etc
4. often formulated with Aspirin, Acetominophen, Ibuprofen

Front 30

Low efficacy analgesic

Back 30

Codeine

Front 31

List the 2 Moderate Efficacy Analgesics

Back 31

Hydrocodone

Oxycodone

Front 32

Very low efficacy Analgesic that is only administered orally

Back 32

Propoxyphene

Front 33

Low-Medium efficacious analgesic that has Propoxyphene-like metabolites; inhibits NE & Serotonin re-uptake

Back 33

Tramadol

Front 34

What are the advantages of the Mixed Agonist-Antagonist Analgesics?

Back 34

believed to have less addictive potential & risk of respiratory depression

Front 35

Mu partial agonist

a. Buprenorphine
b. Butorphanol
c. Nalbuphine
d. Pentazocine

Back 35

Buprenorphine

Front 36

Kappa agonist, Mu partial agonist or antagonist

a. Buprenorphine
b. Butorphanol
c. Nalbuphine
d. Pentazocine

Back 36

Butorphanol & Pentazocine

Front 37

Kappa agonist, Mu antagonist

a. Buprenorphine
b. Butorphanol
c. Nalbuphine
d. Pentazocine

Back 37

Nalbuphine

Front 38

What are the Anti-diarrheal Opioids?

Back 38

Diphenoxylate

Loperamide (OTC)

**have poor permeation of the BBB

Front 39

What are the Anti-tussive Opioids? (cough suppressants)

Back 39

Codeine

Dextromethorphan (OTC)

**poor permeation of the BBB

Front 40

What is the Opioid drug of abuse?

Back 40

Heroin

Front 41

1. What opioids are only administered Parenterally? (2)

2. What opioids that are given orally avoid 1st pass metabolism? (3)

3. What opioid is given transdermally? (1)

4. What opioid is given nasally? (1)

Back 41

1. Alfentanil & Nalbuphine

2. Methadone, Levorphanol, Codeine

3. Fentanyl

4. Butorphanol

Front 42

What is the prototypical duration of action of Opioids (unless otherwise noted)?

Back 42

4 hours

Front 43

How is Morphine metabolized?

Back 43

Glucuronidated

*M-6G is more potent than Morphine

Front 44

What Opioid metabolite is psychoactive?

Back 44

Normeperidine

Front 45

What are the contraindications of Opioid usage? (5)

Back 45

1. Head injuries = Vasodilation -> increases Intracranial pressure
2. Pregnancy = fetus addiction
3. Impaired pulmonary function
4. Liver or Kidney compromised patients
5. Endocrine disorders = can result in exaggerated & prolonged effects
-Addison's disease
-Hypothyroidism

Front 46

What are the drug interaction when Pure agonists are given with Mixed Agonist-Antagonists? (2)

Back 46

1. decreased Analgesia
2. can precipitate withdrawal symptoms

Front 47

What drug interactions occur when opioids are combined with other sedative-hypnotics?

Back 47

increased Sedation & Respiratory Depression

Front 48

What drug interaction occur when Opioids are combined with Antipsychotics?

Back 48

1. Increased sedation & Respiratory depression

2. increased risk of seizures

Front 49

What drug interactions occur when Opioids are combined with MAOI's?

Back 49

1. Increased risk of Hyperpyrexic Coma (esp. Pargyline & Meperidine)

2. Hypertension