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MS 2 - Unit 3 > Pharmacology - Narcotics > Flashcards

Pharmacology - Narcotics Flashcards

1
Q

What are the three types of endogenous opioids?

A

enkephalins, endorphins, and dynorphins

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2
Q

What accounts for “Stress analgesia” (e.g. in war etc.)

A

β-endorphin and ACTH share common precursor and are co-released with stress - result is release of cortisol + endogenous opioids

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3
Q

3 common functions of endogenous and exogenous opiods:

A

inhibition of pain perception,

modification of
gastrointestinal/autonomic function

reward properties

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4
Q

Name and function of 4th endogenous opioid discovered in 1995

A

nociceptin/orphanin FQ

drug reward and reinforcement, feeding, learning and memory

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5
Q

4 types of opioid receptors and corresponding chromosomes

A

MOR - mu opioid receptor, chromosome 6)
DOR - delta opioid receptor, chromosome 1)
KOR - kappa opioid receptor, chromosome 8)
NOR - N/OFQ opioid receptor, chromosome 20).

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6
Q

Common features of opioid receptors

A

All are G protein-coupled receptors, with extracellular,
transmembrane, and intracellular domains.

Classes have homology in the receptor types

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7
Q

How are opioid receptors activated?

A

Ligands are recognized on the extracellular domain; G proteins bind to the
cytoplasmic aspect of the receptor, and activate/bind GTP

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8
Q

Signaling pathway initiated by ligand binding to opioid GCPRs

A
  • Adenylyl cyclase activity is inhibited
  • Voltage-gated Ca2+ channels on the cell membrane close
  • K+ current is stimulated through several channels
  • PKC and PLCβ are activated
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9
Q

How do mu opioid receptors influence neuronal excitability?

A

via “disinhibition” of presynaptic release of GABA

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10
Q

What does activation of opioid receptors do?

A

agonists inhibit release of substance P and
ascending transmission of pain from dorsal horn neurons by activating pain
control circuits descending from the midbrain

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11
Q

T/F exogenous opioids are alkyloids where as endogenous opioids are peptides

A

true

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12
Q

binding site of peptides

A

extracellular loops in combination

with the core

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13
Q

What accounts for different effects and side effects as well as metabolism of different ligands?

A

small chemical modifications of the

ligands result in changes in signal transduction sequences

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14
Q

T/F tollerance toward and opioid over time results in decreased side effects

A

True

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15
Q

tollerance is associated with:

A

decreased effectiveness, and decreased side effects,

with repeated administration

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16
Q

Molecular basis for tolerance involves:

A

phosphorylation or receptor internalization

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17
Q

Side effects of opioids

A 
Analgesia
Mood alteration; stimulation of reward centers
Miosis
Convulsions
Decreased respiration
Cough suppression (antitussive)
Nausea and emesis
Constipation
Urinary retention
dermal vasodilatation and urticaria (hives)
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18
Q

What causes opioid induced uticaria (itching/hives)

A

Opioids stimulate mast cell degranulation and release of histamine

can be managed with an antihistamine (non sedating are preferred to avoid synergy with analgesic e.g. loratadine, fexofenadine)

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19
Q

What causes nausea and emesis

A

Direct stimulation of the
medullary trigger zone for emesis

Delayed gastric emptying

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20
Q

T/F cough suppressant activity is unrelated to respiratory depression

A

True - may be mediated

through receptors unrelated to GPCRs

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21
Q

Mechanism for opioid induced decrease in respiration

A

direct stimulation

of brainstem respiratory centers

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22
Q

T/F Opioids lower seizure threshold

A

true

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23
Q

What causes opioid induced miosis? What receptor is involved?

A

direct stimulation of oculomotor complex to effect papillary constricution (mimicking parasympathetic response)

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24
Q

Mechanism for mood alteration/reward

A

opioids directly stimulate the dopamine pathway in the ventral striatum (VTA)
– stimulates limbic functions (e.g. motivation and affection)

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25
Q

T/F opioid induced miosis and constipation lessen with tolerance

A

False

26
Q

T/F oral, sublingual, transmucosal, rectal absorption of opioids undergo significant first pass metabolism

A

True

27
Q

T/F opioid absorption is slow

A

False - rapid!

28
Q

Steps of opioid metabolism:

A

Occurs in liver - glucuronidation is primary metabolic
pathway

Opioids and their metabolites are then excreted by the kidney

29
Q

Factors that require dose adjustment to prevent overdose:

A

cirrhosis,
chronic or acute renal
insufficiency,
dehydration

30
Q

Who should NOT have regular opioid dosing but can be treated on PRN basis?

A

oliguric or anuric patients

31
Q

Peak serum concentration times based on administration method (IV, subQ, intramuscular, oral)

A

5-10 minutes I.V.
30 minutes subQ or intramuscular administration,
one hour for oral

32
Q

What is “bolus effect”? When does it occur?

A

swings in plasma concentration, with sedation
occurring as a result of high blood levels and breakthrough pain when the serum
levels are at trough

most commonly with intravenous or intramuscular
administration

33
Q

Pain medications for mild pain vs moderate pain vs severe pain (3 step-laddar from WHO) :

A 
Step 1: mild
ASA (aspirin) 
Acetaminophen
NSAIDs
\+/- adjuvants
Step 2: moderate
A/Codeine
A/Hydrocodone
A/Oxycodone
A/Dihydrocodeine
Tramadol
\+/- adjuvants.
Step 3: severe
Morphine
Hydromorphone
Methadone
Levorphenol
Fentanyl
Oxycodone
\+/-adjuvants
34
Q

T/F acceptable adjuvants to narcotics include acetaminophen, NSAIDS, tricyclics, anticonvulsants

A

True

35
Q

benefit of adjuvants

A

“spare” use of

higher dose opioids

36
Q

T/F morphine-6-glucuronide (M-6) is an active metabolite while morphine-3-glucuronide (M-3) is inactive

A

True

37
Q

T/F codiene itself is largely inactive but undergoes demethylation to active morphine

A

true

38
Q

T/F only 10% of the ingested dose of codeine is demethylated

to morphine

A

True

39
Q

Conversion of codeine to morphine is dependent on

A

the CYP2D6 pathway

40
Q

T/F 10% of Caucasions are unable to convert codeine to morphine and have nausea and vomiting instead of analgesia

A

true

41
Q

T/F antitussive effect of codiene involves

non-opioid receptors that bind codeine itself

A

true

42
Q

synthetic codeine analog, and a weak mu
agonist, which has a demethylated metabolite that is a more potent analgesic

developed to be less addictive but still has adictive potential

less constipating than morphine

effective for moderate pain

A

Tramadol

43
Q

highly lipid soluble, strong opioid used intravenously and in a
transdermal patch.

A

Fentanyl

44
Q

T/F suspected MOA of tramadol is inhibition of

norepinephrine and serotonin uptake

A

True

45
Q

extended duration of action with 90%

bound to plasma proteins. accumulates in tissues - used as maintenance treatment for heroine addiction

A

Methadone

46
Q

Doing changes of methadone and fentanyl patches should be restricted to

A

1/week because of long half life

47
Q

opioid no longer in use due to toxic metabolite that causes mental status changes and seizures

A

Meperidine

metabolite normeperidine

48
Q

2 most common opioid antagonists

A

Naloxone

Naltrexone

49
Q

approved for use in the treatment of alcoholism

A

Naltrexone

50
Q

useful in the treatment of acute opioid toxicity. Can only

be administered parenterally (IM, SQ, IV), and has a short half life

A

Naloxone

51
Q

MDD of acetaminophen

A

3000 mg in 24 hours

52
Q

Withdrawal symptoms brought about by abrupt discontinuation of opioids in tollerant patients

ideal dose reduction paradigm?

A 
yawning,
sweating, 
piloerection, 
vomiting, 
pain
shit-squirts 
muscle spasms

reduced by half every 2 to 3 days

53
Q

T/F With
parenteral dosing half life is shorter and doses must be given
MORE frequently and can result in bolus effect

solution is continuous IV/intrathecal infusion

A

true

54
Q

Dosing paradigms for immediate vs extended release opioids vs transdermal fentanyl patches

A

immediate release preparations is every 4 hours

extended release preparations is every 8-24 hours,
usually every 12 hours

every 72 hours

55
Q

T/F Oral breakthrough
prescriptions should always be immediate release preparation,
actual dose is calculated as 10% of the total 24 hour dose

A

True

56
Q

What is Equianalgesic dosing?

A

dose equivalent when switching from one opioid to another

oral doses are
usually two or three times higher than parenteral doses (e.g. I.V. /I.M) because of first pass metabolism

57
Q

T/F cross tolerance to another opioid is usually incomplete so dosing is adjusted downward by 25-50% of the calculated equianalgesic
dose.

A

true

58
Q

T/F True opioid allergies are rare - history of urticaria alone probably side effect, not an allergy, but urticaria and bronchospasm might be

A

true

59
Q

T/F overdoses have quadupled in past 12 years

A

true

60
Q

What is I-STOP? What has it resulted in?

A

NYS Prescription Monitoring Program - Starting in 2015 prescribers must check a state
database before writing prescriptions for opioids + pharmacies file data for prescriptions to central database

less opioid prescribing

MS 2 - Unit 3 (45 decks)

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