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Pharm Exm 4 > Opioid Analgesics > Flashcards

Opioid Analgesics Flashcards

1
Q

Comorbidities for chronic pain

A
  1. Anxiety
  2. Depression
  3. Insomnia (red. immunity, inc. inflamm)
  4. Activation of Glia (astrocytes and microglia)
  5. Hyperalgesia, allodynia
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2
Q

Two types of opioid alkaloids

A

Phenanthrenes

Benzyliso-quinolines

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3
Q

Phenantherenes agents

A

Morphine (10%)

Codeine (.5%)

Thebaine (.2%)

(Also Hydrocodone, buprenorphine)

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4
Q

Benzylisoquinolines agents

A

Noscapine (6%)

Papaverine (1%)

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5
Q

Mu opioid receptor drugs - Phenanthrenes

A

Morphine

Hydrocodone

Buprenorphine (partial)

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6
Q

Mu opioid receptor drugs - Non-phenanthrenes

A

Tramadol

Meperidine

Fentanyl

Methadone

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7
Q

Morphine metabolism rxn

Enzyme?

A

Glucuronidation (3’ and 6’)

CYP-2D6

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8
Q

Effect of alcohol on morphine metabolism

A

May increase serum levels of 2D6, reducing the available time of effect.

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9
Q

Morphine excretion (where and rate?)

A

Glomerular excretion

90% excreted in 24h

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10
Q

Primary metabolite of morphine is __ conjugated

A

3’

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11
Q

Opioid receptors are ____

Three types?

A

GPCR’s

They are Gi/o coupled (inhibit cAMP)

Mu - Morphine

Kappa - Ketocyclazocine

Delta - Deferens

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12
Q

Two ‘other’ receptors (one opioid, one not)

A

Nociceptin, orphanin FQ receptor

Sigma receptor - NOT an opioid receptor

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13
Q

The types of pain for which opiates are not indicated

A

Acute, sharp pain

Neuropathic pain

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14
Q

Mu opioid AE’s

A

Respiratory depression

GI immotility

Itch

Tolerance

Urinary retention (ADH)

Nausea/Vomiting

Muscle rigidity

Miosis (PAG - Oculomotor nerve)

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15
Q

Opioid that doesnt cause Biliary SMC contraction

A

meperidine

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16
Q

Kappa natural ligand

A

Dynorphins

(preprodynorphin)

(Salvia contains an agonist. Not an alkaloid)

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17
Q

Kappa receptor function

A

Counterbalance Mu effects

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18
Q

Delta opioid natural ligand

A

Enkephalins (prepro)

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19
Q

Delta has more ___ expression

A

dynamic

(intracellular, externalized upo chronic stimuli)

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20
Q

Delta has a role in…

A

ischemia, hypoxia, stroke

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21
Q

Major Mu receptor endogenous ligand

A

Endorphins (from POMC)

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22
Q

Opioid receptor transduction hinges upon __

A

Adenylyl Cyclase inactivation

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23
Q

Two synaptic mehanisms for opioid receptors

A

Presynaptic = Inhibit Ca++ channel

Postsynaptic = Activate GIRK channel (Gby)

(Efflux of K+ = hyperpolarization)

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24
Q

What is GIRK?

A

G protein inward rectifying K+ channel

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25
Q

Covered by medicare and preferred over oxycontin

A

Morphine

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26
Q

Oxycontin plus paracetamol

A

Percocet

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27
Q

Clinically used opioid agonists

A
  1. Sufentanil
  2. Remifentanyl
  3. Fentanyl
  4. Hydromorphone
  5. Morphine
  6. Hydrocodone
  7. Oxycodone
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28
Q

Weaker clinically used opioid agonists

A

Methadone

Meperidine

Codeine

Tramadol

Loperamide

Propoxyphene (wd)

29
Q

___, ___ have SNRI properties

Use?

A

Tramadol, Tapentadol

(non-phenanthrenes)

–> management of mild non-neuropathic pain

30
Q

What are the metabolite effects of demerol that you need to watch for?

A

Active metabolite (Nor-meperidine) can accumulate, cause CNS irritability + myoclonic seizures

31
Q

Meperidine is dangerous in whom?

A

Patients with decreased renal function

(renally excreted)

32
Q

Methadone is a ____ antagonist

Half life?

A

NMDA antagonist

15-60 hrs

33
Q

This analgesic’s half life is shorter than the serum half life

A

Levorphanol

34
Q

Levorphanol is a ___ antagonist

A

NMDA

35
Q

NMDA antagonists?

Which for chronic, and which for neuropathic

A

Methadone (chronic)

Levorphanol (neuropathic)

36
Q

Buprenorphine receptor subtype activity

A

Partial mu agonist

Weak K agonist

Delta antagonist

37
Q

Buprenorphine is used for…

A

treatment for opioid withdrawal in addiction therapy

38
Q

Buprenorphine combined with …

A

naoxone (Suboxone)

39
Q

Mu antagonists

A

Naloxone (narcan)

Naltrexone (oral)

40
Q

These are used for surgery because of their fast onset and short duration

A

Fentanyl, Sufentanil, remifentanil

41
Q

These are used for post-op or epidural because of potency and longer half life than fentanyl

A

hydromorphone, morphine

42
Q

These are used for management because of oral BA

have a longer half life than fentanyl

A

Oxycodone, HC, Oxycontin

(Zohydo = extended-release HC)

43
Q

Used for terminal cancer pain because of lower cost, history of knowledge, and irrelevant risk for dependence/abuse

A

Morphine

44
Q

Used in opioid intolerance

A

Meperidine

45
Q

Issue with meperidine/demerol metabolism

A

metabolites NOT blocked by NTX

MAOi’s are contraindicated

46
Q

Shortest onset opioid

A

Fentanyl

47
Q

Opioid with longest dosing interval

A

Hydromorphone

48
Q

When dosing opoiod analgesics it is important to ______ as compared to______

A

calcuate dose compared to morphine

49
Q

Which comes first:

Somnolescence/miosis -or- Itching/urinary retention

A

Somnolescence/miosis

50
Q

Senna MOA

A

Irritates colon and causes fluid secretion and CONTRACTION

51
Q

Polythylene glycol MOA

A

Osmotic increase in GI water content

52
Q

Docusate MOA

A

softens stool and increases peristalsis

53
Q

Peripherally restructed mu antagonists

A

Methylnaltrexone (4’ amine, no BBB pass)

Alvimopan

Naloxegol

54
Q

Opioid induced itch requires ______

A

MOR1D splice variant of the mu receptor

55
Q

What is the GRPR in the MOR1D-GRPR?

What happens downstream?

A

Gastrin-Releasing Peptide Receptor

Downstream = IP3 is formed and Ca++ is released from the ER

56
Q

Symptoms with NO TOLERANCE (or limited tolerance)

A

Constipation

Itch

Miosis

57
Q

A few mechanisms for tolerance

A

Receptor adaptation

decreased receptor number

Decreased coupling to effector

58
Q

A few mechanisms for hyperalgesia

A

Altered excitability of target neurons

NMDA, Cholecystokinin, dynorphin, substance P

59
Q

Alterations in ___ and ____ receptors also contribute to pain response

A

NMDA and Substance P

60
Q

Signs of Opioid induced hyperalgesia

A

Pain not relieved by opioid

Diffuse pain

Cold pressor test (arm in ice bath–withdrawal time)

61
Q

Solution to OIH?

A

Switch opioid class - phenanthrenes vs non

(6 glucuronide metabolites of phenanthrenes act as NMDA agonists)

Methadone is NMDA antagonist

62
Q

Opioid detox - switch to ____

A

clonidine/diazepam

63
Q

Precautions taken when given to paients with these diseases

A

Respiratory compromise (CB, Asthma, Emphysema)

Seizure disorders

Hepatic disease

64
Q

DDIs for opioids

A

Depressants (EtOH, Benzo, Barbiturarates)

Antipsychotics

TCA

Antihistamines

Meperidine

65
Q

Meperidine DDI

A

MAO’s, SSRI’s

SEROTONIN SYNDROME, hyperpyrexic coma

66
Q

Tx for acute opioid toxicity

A

Resp and Cardio support

Naloxone (Narcan) … SMALL IV dose initially

67
Q

Drugs to treat opioid abuse

A

Methdone

Buprenorphine

Suboxone (bup+naloxone)

68
Q

3 approaches to long term treatment of opioid addiction

A
  1. Agonist Maintenance (Methadone Maint. Therapy)
  2. Partial Agonist Therapy (Buprenorphine)
  3. Antagonist Maintenance (Naltrexone)
69
Q

Opioids to treat Alcohol use disorders

A

Naltrexone (once per month)

Nalmefene

Pharm Exm 4 (7 decks)

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