Opioid analgesics Flashcards Preview

Pharmacology - Test #4 > Opioid analgesics > Flashcards

Flashcards in Opioid analgesics Deck (55):
1

Difference between analgesia and anesthesia

Analgesia - Block pain transmission
Anesthesia - Block sensory neurotransmission

2

What does qd mean?

Once daily

3

What does bid mean?

Twice a day

4

What does Q12 mean?

Every 12 hours

5

What does tid mean?

three times each day

6

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

Nucleus Accumbens

7

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

amygdala

8

Name the key brain regions expressing opioid receptors

Periaqueductal Gray
Rostral ventral medulla
Dorsal Root Ganglion/Dorsal Horn

9

Opium contains two types of alkaloids, name them.

Phenanthrenes
Benzylisoquinolines

10

Phenanthrene opoids primarily show differences at

3 and 6 positions

11

Phenanthrene partial antagonism is conferred by....

bulky side groups

12

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

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.

13

Three examples of Phenanthrenes

Morphine
Hydrocodone
Buprenorphine

14

Four examples of non-Phenanthrene

Tramadol
Meperidin
Fentanyl
Methadone

15

Name a Phenanthrene antagonist

Naloxone

16

How are Phenanthrene opioids metabolized

Glucorinidation at the 3, 6 position
With morphine-6-glucoronide, the metab. is still active

17

Which organ(s) runs opioid metabolism

Metab. is largely hepatic, impaired with liver disease
Metabolites are excreted through the kidneys

18

Name the different types of Opioid receptors

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

19

Natural agonists of mu opioid receptors

Beta endorphins (endogenous morphine)

20

Why target mu opioid receptors therapeutically

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

21

Important sid effects of mu opioid drugs

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

22

Significance of the kappa opioid receptor

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

23

Name the endogenous kappa agonist

Dynorphin

24

Delta opioid receptors are being considered for treatment of...

Anxiety, Depression, OH Abuse
Ischemic Damage

25

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

They are upregulated with chronic stimulation

26

Natural ligand for delta opioid receptor?

Enkephalins (preproenkephalin)

27

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

Debate on activity, opposes classic mu effects and mediates pain

28

Describe the molecular signalling of opioids

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.

29

Presynaptic inhibition of neurotransmitter release is mediated by...

Inhibition of calcium uptake

30

Postsynaptic inhibition of pain transmission is medicated by...

hyperpolarization through GIRK channels

31

Which two opioids are typically used in surgical mu analgesia

Fentanyl
Sufentanil
Remifentanyl

32

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

Fentanyl

33

Other name for hydromorphone

Dilaudid

34

Why is morphine most common

Covered by medicare

35

Other names for hydrocodone

Lortab
Vicodin
Norco

36

Other names for oxycodone

Oxycontin, Percocet

37

Name as many clinically used opioids as you can

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

38

Other name for meperidine

Demerol

39

Other name for tramadol

Ultram

40

Negative effect of methadone

Prolonged QT

41

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

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

42

Loperamide is used for...

diarrhea

43

How do Tramadol and Tapentadol work?

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

44

Which patients is Meperidine especially dangerous in?

Patients with decreased renal function

45

Important details for Methadone

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

46

Important details on Levorphanol

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

47

Two receptors upregulated by chronic pain

AMPA, NDMA

48

Which opioids are known for NMDA action

Methadone and Levorphanol

49

Which drug is a partial mu agonist

Buprenorphine

50

Which drugs are mu antagonists

Naloxone (Narcan)
Naltrexone

51

When to use Buprenorphine

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

52

Which opioids are used for postop, epidural. Why?

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

53

Which opioids are used for pain maangement. Why?

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

54

Which opioid is used for terminal cancer pain? Why?

Morphine
Cost, History of Knowledge, No worries about dependence

55

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

Meperidine (Demerol)