Opioid analgesics

Question 1

Difference between analgesia and anesthesia

Answer 1

Analgesia - Block pain transmission

Anesthesia - Block sensory neurotransmission

Question 2

What does qd mean?

Answer 2

Once daily

Question 3

What does bid mean?

Answer 3

Twice a day

Question 4

What does Q12 mean?

Answer 4

Every 12 hours

Question 5

What does tid mean?

Answer 5

three times each day

Question 6

The _____ in the brain assigns aversive or pleasurable qualities to pain

Answer 6

Nucleus Accumbens

Question 7

The ____ in the brain is involved in fear/pain expectation

Answer 7

amygdala

Question 8

Name the key brain regions expressing opioid receptors

Answer 8

Periaqueductal Gray
Rostral ventral medulla
Dorsal Root Ganglion/Dorsal Horn

Question 9

Opium contains two types of alkaloids, name them.

Answer 9

Phenanthrenes

Benzylisoquinolines

Question 10

Phenanthrene opoids primarily show differences at

Answer 10

3 and 6 positions

Question 11

Phenanthrene partial antagonism is conferred by….

Answer 11

bulky side groups

Question 12

Significance of knowing which drugs are Phenanthrene and which are non-Phenanthrene?

Answer 12

Some patients respond better to one type than the other, so in patients struggling with pain or side effects of one, the other may help a lot.

Question 13

Three examples of Phenanthrenes

Answer 13

Morphine
Hydrocodone
Buprenorphine

Question 14

Four examples of non-Phenanthrene

Answer 14

Tramadol
Meperidin
Fentanyl
Methadone

Question 15

Name a Phenanthrene antagonist

Answer 15

Naloxone

Question 16

How are Phenanthrene opioids metabolized

Answer 16

Glucorinidation at the 3, 6 position

With morphine-6-glucoronide, the metab. is still active

Question 17

Which organ(s) runs opioid metabolism

Answer 17

Metab. is largely hepatic, impaired with liver disease

Metabolites are excreted through the kidneys

Question 18

Name the different types of Opioid receptors

Answer 18

G Protein Coupled (Family A/Gio coupled)
Mu
Kappa
Delta
Nociceptin, orphanin FQ receptor

Question 19

Natural agonists of mu opioid receptors

Answer 19

Beta endorphins (endogenous morphine)

Question 20

Why target mu opioid receptors therapeutically

Answer 20

Analgesia (NOT for sharp localized, neuropathic pain)
Sedation
Antitussive (suppresses the cough reflex)

Question 21

Important sid effects of mu opioid drugs

Answer 21

Resp. Depression
Constipation, Pruritis
Tolerance/Dependence
Urinary Retention
Nausea/Vom
Muscle Rigidity
Miosis

Question 22

Significance of the kappa opioid receptor

Answer 22

Involved in negative feedback loop, inhibiting the release of dopamine. The first dopamine causes dynorphin transcription. Its release activated presynaptic kappa receptors on dopaminergic terminals, inhibiting further release

Question 23

Name the endogenous kappa agonist

Answer 23

Dynorphin

Question 24

Delta opioid receptors are being considered for treatment of…

Answer 24

Anxiety, Depression, OH Abuse

Ischemic Damage

Question 25

Why are delta opioid so interesting in the context of chronic pain?

Answer 25

They are upregulated with chronic stimulation

Question 26

Natural ligand for delta opioid receptor?

Answer 26

Enkephalins (preproenkephalin)

Question 27

Why do we care about the orphanin opoid receptor like subtype 1

Answer 27

Debate on activity, opposes classic mu effects and mediates pain

Question 28

Describe the molecular signalling of opioids

Answer 28

opioid binds to GPCR. They're all Gi/o coupled, which causes them to inhibit ACyc, and thus decrease cAMP. They also turn on GIRK, causing hyperpolarization and inhibiting NT release.

Question 29

Presynaptic inhibition of neurotransmitter release is mediated by...

Answer 29

Inhibition of calcium uptake

Question 30

Postsynaptic inhibition of pain transmission is medicated by...

Answer 30

hyperpolarization through GIRK channels

Question 31

Which two opioids are typically used in surgical mu analgesia

Answer 31

Fentanyl Sufentanil Remifentanyl

Question 32

Which opioid can be used via IV, Patch, or Lollipop

Answer 32

Fentanyl

Question 33

Other name for hydromorphone

Answer 33

Dilaudid

Question 34

Why is morphine most common

Answer 34

Covered by medicare

Question 35

Other names for hydrocodone

Answer 35

Lortab Vicodin Norco

Question 36

Other names for oxycodone

Answer 36

Oxycontin, Percocet

Question 37

Name as many clinically used opioids as you can

Answer 37

``` Sufentanil, Remifentanyl, Fentanyl Morphine, Hydromorphone Codeine, Hydrocodone, Oxycodone Meperidine, Methadone Tramadol, Loperamide, Propoxyphene ```

Question 38

Other name for meperidine

Answer 38

Demerol

Question 39

Other name for tramadol

Answer 39

Ultram

Question 40

Negative effect of methadone

Answer 40

Prolonged QT

Question 41

Meperidine is used to treat... | Problems with meperidine?

Answer 41

``` Rigors Its metabolite (normeperidine) is neurotoxic (tremors, twitches, seizures) ```

Question 42

Loperamide is used for...

Answer 42

diarrhea

Question 43

How do Tramadol and Tapentadol work?

Answer 43

Mild opioid analgesic SNRI properties Help with management of mild neuroathic pain

Question 44

Which patients is Meperidine especially dangerous in?

Answer 44

Patients with decreased renal function

Question 45

Important details for Methadone

Answer 45

Primarily used for opioid dependence It has a long duration of action/half life (15-60 hrs) NMDA antagonist to help Chronic pain treatment

Question 46

Important details on Levorphanol

Answer 46

Long half life (16 hr) | NMDA antagonist for neuropathic pain

Question 47

Two receptors upregulated by chronic pain

Answer 47

AMPA, NDMA

Question 48

Which opioids are known for NMDA action

Answer 48

Methadone and Levorphanol

Question 49

Which drug is a partial mu agonist

Answer 49

Buprenorphine

Question 50

Which drugs are mu antagonists

Answer 50

Naloxone (Narcan) | Naltrexone

Question 51

When to use Buprenorphine

Answer 51

Used to treat opioid withdrawl in addiction therapy | Combined with naloxone for maintenence therapy

Question 52

Which opioids are used for postop, epidural. Why?

Answer 52

Hydromorphone, Morphine | 4-5X the half life of fentanyl

Question 53

Which opioids are used for pain maangement. Why?

Answer 53

Oxycodone, Hydrocodone, Oxycontin, Zohydro | Oral bioavailability, longer halflife

Question 54

Which opioid is used for terminal cancer pain? Why?

Answer 54

Morphine | Cost, History of Knowledge, No worries about dependence

Question 55

Which opioid is used for patients with a history of trouble tolerating opioids?

Answer 55

Meperidine (Demerol)