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Pharmacology - Test #4 > Opioid analgesics > Flashcards

Opioid analgesics Flashcards

1
Q

Difference between analgesia and anesthesia

A

Analgesia - Block pain transmission

Anesthesia - Block sensory neurotransmission

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2
Q

What does qd mean?

A

Once daily

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3
Q

What does bid mean?

A

Twice a day

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4
Q

What does Q12 mean?

A

Every 12 hours

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5
Q

What does tid mean?

A

three times each day

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6
Q

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

A

Nucleus Accumbens

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7
Q

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

A

amygdala

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8
Q

Name the key brain regions expressing opioid receptors

A

Periaqueductal Gray
Rostral ventral medulla
Dorsal Root Ganglion/Dorsal Horn

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9
Q

Opium contains two types of alkaloids, name them.

A

Phenanthrenes

Benzylisoquinolines

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10
Q

Phenanthrene opoids primarily show differences at

A

3 and 6 positions

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11
Q

Phenanthrene partial antagonism is conferred by….

A

bulky side groups

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12
Q

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

A

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.

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13
Q

Three examples of Phenanthrenes

A

Morphine
Hydrocodone
Buprenorphine

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14
Q

Four examples of non-Phenanthrene

A

Tramadol
Meperidin
Fentanyl
Methadone

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15
Q

Name a Phenanthrene antagonist

A

Naloxone

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16
Q

How are Phenanthrene opioids metabolized

A

Glucorinidation at the 3, 6 position

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

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17
Q

Which organ(s) runs opioid metabolism

A

Metab. is largely hepatic, impaired with liver disease

Metabolites are excreted through the kidneys

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18
Q

Name the different types of Opioid receptors

A 
G Protein Coupled (Family A/Gio coupled)
Mu
Kappa
Delta
Nociceptin, orphanin FQ receptor
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19
Q

Natural agonists of mu opioid receptors

A

Beta endorphins (endogenous morphine)

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20
Q

Why target mu opioid receptors therapeutically

A

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

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21
Q

Important sid effects of mu opioid drugs

A 
Resp. Depression
Constipation, Pruritis
Tolerance/Dependence
Urinary Retention
Nausea/Vom
Muscle Rigidity
Miosis
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22
Q

Significance of the kappa opioid receptor

A

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

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23
Q

Name the endogenous kappa agonist

A

Dynorphin

24
Q

Delta opioid receptors are being considered for treatment of…

A

Anxiety, Depression, OH Abuse

Ischemic Damage

25
Q

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

A

They are upregulated with chronic stimulation

26
Q

Natural ligand for delta opioid receptor?

A

Enkephalins (preproenkephalin)

27
Q

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

A

Debate on activity, opposes classic mu effects and mediates pain

28
Q

Describe the molecular signalling of opioids

A

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
Q

Presynaptic inhibition of neurotransmitter release is mediated by…

A

Inhibition of calcium uptake

30
Q

Postsynaptic inhibition of pain transmission is medicated by…

A

hyperpolarization through GIRK channels

31
Q

Which two opioids are typically used in surgical mu analgesia

A

Fentanyl
Sufentanil
Remifentanyl

32
Q

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

A

Fentanyl

33
Q

Other name for hydromorphone

A

Dilaudid

34
Q

Why is morphine most common

A

Covered by medicare

35
Q

Other names for hydrocodone

A

Lortab
Vicodin
Norco

36
Q

Other names for oxycodone

A

Oxycontin, Percocet

37
Q

Name as many clinically used opioids as you can

A 
Sufentanil, Remifentanyl, Fentanyl
Morphine, Hydromorphone
Codeine, Hydrocodone, Oxycodone
Meperidine, Methadone
Tramadol, Loperamide, Propoxyphene
38
Q

Other name for meperidine

A

Demerol

39
Q

Other name for tramadol

A

Ultram

40
Q

Negative effect of methadone

A

Prolonged QT

41
Q

Meperidine is used to treat…

Problems with meperidine?

A 
Rigors
Its metabolite (normeperidine) is neurotoxic (tremors, twitches, seizures)
42
Q

Loperamide is used for…

A

diarrhea

43
Q

How do Tramadol and Tapentadol work?

A

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

44
Q

Which patients is Meperidine especially dangerous in?

A

Patients with decreased renal function

45
Q

Important details for Methadone

A

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
Q

Important details on Levorphanol

A

Long half life (16 hr)

NMDA antagonist for neuropathic pain

47
Q

Two receptors upregulated by chronic pain

A

AMPA, NDMA

48
Q

Which opioids are known for NMDA action

A

Methadone and Levorphanol

49
Q

Which drug is a partial mu agonist

A

Buprenorphine

50
Q

Which drugs are mu antagonists

A

Naloxone (Narcan)

Naltrexone

51
Q

When to use Buprenorphine

A

Used to treat opioid withdrawl in addiction therapy

Combined with naloxone for maintenence therapy

52
Q

Which opioids are used for postop, epidural. Why?

A

Hydromorphone, Morphine

4-5X the half life of fentanyl

53
Q

Which opioids are used for pain maangement. Why?

A

Oxycodone, Hydrocodone, Oxycontin, Zohydro

Oral bioavailability, longer halflife

54
Q

Which opioid is used for terminal cancer pain? Why?

A

Morphine

Cost, History of Knowledge, No worries about dependence

55
Q

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

A

Meperidine (Demerol)

Pharmacology - Test #4 (9 decks)

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